Page last updated: 2024-12-05

efavirenz

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Description

Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in combination with other antiretroviral medications to treat HIV infection. It was first synthesized in the early 1990s by researchers at DuPont Pharmaceuticals. Efavirenz works by blocking the activity of reverse transcriptase, an enzyme that HIV uses to convert its genetic material into DNA. This prevents the virus from replicating and spreading. Efavirenz is a highly potent anti-HIV drug, but it can cause side effects such as dizziness, drowsiness, and nightmares. However, its ability to penetrate the central nervous system has led to its study for potential use in treating other neurological conditions such as Alzheimer's disease and Parkinson's disease. Its effectiveness in treating HIV infection and its potential applications in other neurological disorders make it a significant research target.'

efavirenz: HIV-1 reverse transcriptase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID64139
CHEMBL ID223228
CHEBI ID119486
SCHEMBL ID37762
MeSH IDM0258297
PubMed CID3203
CHEMBL ID59507
SCHEMBL ID464769
MeSH IDM0258297

Synonyms (202)

Synonym
BIDD:GT0383
bdbm2483
(4s)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1h-3,1-benzoxazin-2-one
sustiva
HMS3393J08
viraday
CHEMBL223228
efavirenz teva
efavirenzum
(-)-efavirenz
met-stromal cell-derived factor-1.beta. (human) & efavirenz
met-sdf-1.beta. & efavirenz
l-743726
stocrin
(-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2h-3,1-benzoxazin-2-one
MLS001424087
C08088
154598-52-4
efavirenz
sustiva (tm)
dmp-266
nsc742403
eravirenz
l-743,726
efv ,
strocin (tm)
(4s)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1h-3,1-benzoxazin-2-one
2h-3,1-benzoxazin-2-one, 6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-, (4s)-
MLS000759465
smr000466351
1IKW
(s)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-benzo[d][1,3]oxazin-2-one
(s)-6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-(s)-6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2h-3,1-benzoxazin-2-one4-(trifluoromethyl)-2h-3,1-benzoxazin-2-one
DB00625
6-chloro-4-(2-cyclopropyl-1-ethynyl)-4-trifluoromethyl-(4s)-1,4-dihydro-2h-benzo[d][1,3]oxazin-2-one
1IKV
sustiva (tn)
D00896
efavirenz (jan/usp/inn)
dmp 266
(4s)-6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2h-3,1-benzoxazin-2-one
l 743726
hsdb 7163
(s)-6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2h-3,1-benzoxazin-2-one
(s)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2h-3,1-benzoxazin-2-one
HMS2051J08
HMS2090N16
CHEBI:119486 ,
(4s)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2h-3,1-benzoxazin-2-one
2h-3, 6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-, (4s)-
nsc-742403
A809555
(4s)-6-chloranyl-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1h-3,1-benzoxazin-2-one
dtxsid9046029 ,
dtxcid7026029
tox21_111582
cas-154598-52-4
BCP9000636
S4685
CCG-101011
(s)-efavirenz
je6h2o27p8 ,
nsc 742403
efavirenz [usp:inn:ban]
efavirenz, (s)
unii-je6h2o27p8
(4s)-6-chloro-4-(2-cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2h-3,1-benzoxazin-2-one
BCPP000245
AB21723
efavirenz [mi]
efavirenz [usp-rs]
efavirenz [orange book]
efavirenz [jan]
efavirenz [who-ip]
efavirenz [vandf]
telura component efavirenz
efavirenz [who-dd]
efavirenz [ema epar]
efavirenz [mart.]
efavirenz [hsdb]
efavirenz [inn]
efavirenz [usan]
efavirenzum [who-ip latin]
efavirenz [usp monograph]
atripla component efavirenz
efavirenz component of atripla
AKOS015894951
DL-535
HY-10572
AB00639956-06
efv & plga
efavirenz & plga
NC00261
SCHEMBL37762
NCGC00159337-04
tox21_111582_1
AB00639956-08
(s)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2h-3,1-benzoxazin-2-one
(s)-6-chloro-4-(cyclopropyl-ethynyl)-1,4-dihydro-4-(trifluoromethyl)-2h-3,1-benzoxazine-2-one
(s)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2h-3,1-ben zoxazin-2-one
efavirenz & interleukin 28a
efv & interleukin 29
efavirenz & ifnl1
efv & ifnl1
efavirenz & interferon lambda-1
efv & ifnl3
efv & interleukin 28a
efavirenz & il-28a
efv & il-29
efv & il-28a
efavirenz & interferon lambda-3
efavirenz & il-28b
efv & interferon lambda-3
efv & ifnl2
efavirenz & ifnl2
efv & interferon lambda-2
efavirenz & interleukin 29
efv & interleukin 28b
efv & interferon lambda-1
efavirenz & interferon lambda-2
efavirenz & interleukin 28b
efavirenz & ifnl3
efavirenz & il-29
efv & il-28b
(s)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2h-benzo[d][1,3]oxazin-2-one
AC-25006
E0997
J-520431
sr-01000759360
SR-01000759360-4
SR-01000759360-5
KS-5380
efavirenz, united states pharmacopeia (usp) reference standard
efavirenz, >=98% (hplc)
(s)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1h-benzo[d][1,3]oxazin-2(4h)-one
HMS3713M14
NCGC00271713-05
dmp-266; efavirenz
Q422645
F17329
Z2177953192
BCP27719
AMY229
NCGC00159337-12
NCGC00271713-08
(rac)-efavirenz
(rac)-dmp 266; (rac)-efv; (rac)-l-743726
dmp266
gtpl11287
efavirenz 100 microg/ml in acetonitrile
EN300-219935
BC164402
efavirenz- bio-x
l-741211
NCGC00159337-02
NCGC00159337-03
l 741211
2h-3,1-benzoxazin-2-one, 6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-
6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2h-3,1-benzoxazin-2-one
smr000718784
MLS001304019
154635-17-3
177530-93-7
FT-0667824
6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1h-3,1-benzoxazin-2-one
CHEMBL59507
BBL010771
6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2h-3,1-benzoxazin-2-one
STK582240
HMS2231D09
AKOS005506207
racemic-efavirenz
6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2h-3,1-benzoxazin-3-one
rac-efavirenz
l741211
6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1h-benzo[d][1,3]oxazin-2(4h)-one
FT-0625647
NCGC00159337-06
2h-3,1-benzoxazin-2-one, 6-chloro-4-(2-cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-, (4s)-
HMS3373J19
AB00876268-06
(+/-) 6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2h-3,1-benzoxazin-2-one
(+) 6-chloro-4-cyclopropylethynyl-4-trifluoromethyl- 1,4-dihydro-2h-3,1-benzoxazin-2-one
(+) 6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2h-3,1-benzoxazin-2-one
(+/-)6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2h-3,1-benzoxazin-2-one
SCHEMBL464769
MLS006011825
tox21 111582
mfcd05662344
6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-4h-3,1-benzoxazin-2-ol
STL454184
efavirenz racemic; ((+/-)-6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2h-3,1-benzoxazin-2-one)
efavirenz racemic
6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2h-benzo[d][1,3]oxazin-2-one
VS-02672
6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1h-3,1-benzoxazin-2-one
6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2h-3,1-benzoxazin-2-one
DTXSID00861416
(+/-)-efavirenz
efavirenz racemic (20mg)
(s)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1h-3,1-benzoxazin-2-one
SY009682

Research Excerpts

Toxicity

DPQ was highly efficacious and safe for the treatment of malaria in HIV-infected patients concurrently taking efavirenz- or nevirapine-based ART. Both low-dose efvirenz and integrase strand transfer inhibitors tended to be protective of discontinuations due to adverse events.

ExcerptReferenceRelevance
"Eight patients who were infected with human immunodeficiency virus, and who had each sustained an adverse drug reaction while following a regimen including nevirapine, were switched to a regimen including efavirenz."( The tolerability of efavirenz after nevirapine-related adverse events.
Barry, M; Clarke, S; Harrington, P; Mulcahy, F, 2000
)
0.31
"The rate of adverse events was examined in 250 subjects enrolled in the expanded access program in a single institution located in Madrid, Spain."( [Toxicity associated to efavirenz in HIV-infected persons enrolled in an expanded access program].
Barreiro, P; Dona, C; González-Lahoz, J; Jiménez-Náchera, I; Soriano, V, 2000
)
0.31
"The rate of adverse events grade moderate-to-severe in patients receiving EFV is relatively low (13."( [Toxicity associated to efavirenz in HIV-infected persons enrolled in an expanded access program].
Barreiro, P; Dona, C; González-Lahoz, J; Jiménez-Náchera, I; Soriano, V, 2000
)
0.31
" Similar serious psychiatric adverse effects have been associated with this agent."( Central nervous system adverse effects with efavirenz: case report and review.
Puzantian, T, 2002
)
0.31
"To evaluate the incidence and severity of adverse events (AEs) and treatment interruption (TI) with efavirenz in a population with a high rate of intravenous drug use (IVDU)."( Safety and tolerance of efavirenz in different antiretroviral regimens: results from a national multicenter prospective study in 1,033 HIV-infected patients.
Pérez-Molina, JA,
)
0.13
" Most patients experienced at least one drug-related adverse event that was not considered treatment-limiting by the investigator."( Efficacy and safety of a quadruple combination Combivir + abacavir + efavirenz regimen in antiretroviral treatment-naive HIV-1-infected adults: La Francilienne.
Chemlal, K; de Truchis, P; Devidas, A; Force, G; Mamet, JP; Mechali, D; Praindhui, D; Pulik, M; Rouveix, E; Welker, Y, 2002
)
0.31
"Safety and efficacy results from this study demonstrated that the quadruple regimen Combivir/abacavir/efavirenz is generally safe and displays potent and durable antiretroviral activity in antiretroviral treatment-naive HIV-1-infected patients, offering a promising therapeutic option in a PI-sparing strategy."( Efficacy and safety of a quadruple combination Combivir + abacavir + efavirenz regimen in antiretroviral treatment-naive HIV-1-infected adults: La Francilienne.
Chemlal, K; de Truchis, P; Devidas, A; Force, G; Mamet, JP; Mechali, D; Praindhui, D; Pulik, M; Rouveix, E; Welker, Y, 2002
)
0.31
"Simplification is safe and effective, but it should be offered to patients with shorter treatment duration, and in good clinical and immunovirological conditions."( Simplification of protease inhibitor-containing regimens with efavirenz, nevirapine or abacavir: safety and efficacy outcomes.
Adorni, F; Bini, T; Bongiovanni, M; Capetti, A; Castelnuovo, B; Chiesa, E; Cicconi, P; d'Arminio Monforte, A; Faggion, I; Melzi, S; Mussini, C; Rizzardini, G; Rusconi, S; Sollima, S; Tordato, F, 2003
)
0.32
" Severe adverse events due to HAART have been already reported for post exposure prophylaxis in HIV infected patients."( [Acute liver toxicity of antiretroviral therapy (HAART) after liver transplantation in a patient with HIV-HCV coinfection and associated hepatocarcinoma (HCC)].
Antonini, M; Boschetto, A; D'Offizzi, G; Del Nonno, F; Ettorre, GM; Lonardo, MT; Maritti, M; Moricca, P; Narciso, P; Palmieri, GP; Perracchio, L; Santoro, E; Vennarecci, G; Visco, G,
)
0.13
" Assessment consisted of CD4+ cell count, plasma HIV-1 RNA load, and adverse effects of study medications."( Nevirapine plus efavirenz plus didanosine: a simple, safe, and effective once-daily regimen for patients with HIV infection.
Carroll, H; Conlon, V; Green, A; Green, DC; Green, R; Jefferson, R; Jordan, WC; Tolbert, L; Yemofio, F, 2003
)
0.32
" Although data from observational studies and follow-up of children enrolled in clinical trials have not shown uninfected, zidovudine-exposed children to be at increased risk of adverse events including cancer in the short- to medium-term, the possibility that they may be at risk of cancer at older ages cannot be excluded."( Antenatal and neonatal antiretroviral therapy in HIV-infected women and their infants: a review of safety issues.
Newell, ML; Thorne, C,
)
0.13
" Adverse events were consistent with prior data for each of the separate agents."( Pharmacokinetics and safety of GW433908 and ritonavir, with and without efavirenz, in healthy volunteers.
Ballow, C; Hendrix, CW; Lou, Y; Piliero, PJ; Preston, SL; Stein, DS; Wire, MB, 2004
)
0.32
" Patients in both groups tolerated the therapy well; the adverse effects profile was comparable except that group A patients had a higher incidence of hepatitis than group B patients (13."( Safety and antiretroviral effectiveness of concomitant use of rifampicin and efavirenz for antiretroviral-naive patients in India who are coinfected with tuberculosis and HIV-1.
Patel, A; Patel, B; Patel, J; Patel, K; Rani, S; Shah, N, 2004
)
0.32
" Severe adverse reactions included rash (two), toxic hepatitis (six), Immune Reconstitution Syndrome (seven), and four deaths."( Efficacy and safety of Efavirenz in HIV patients on Rifampin for tuberculosis.
Alves, CR; Badaro, R; Brites, C; Netto, EM; Oliveira, AS; Pedral-Sampaio, DB, 2004
)
0.32
" The incidence of rash in the NVP group was significantly higher in female patients with higher CD4 cell counts, while adverse events in the EFV group were not associated with CD4 cell count."( The effect of baseline CD4 cell count and HIV-1 viral load on the efficacy and safety of nevirapine or efavirenz-based first-line HAART.
Andrews, S; Grinsztejn, B; Lange, JM; Lazanas, MK; Montaner, J; van Leth, F; Wilkins, E, 2005
)
0.33
" These data have now provided a clear and clinically relevant understanding of the individual profiles of drugs within the nucleoside analogue reverse transcriptase inhibitor , HIV protease inhibitor and non-nucleoside analogue reverse transcriptase inhibitor drug classes, and have provided a rational basis for assessing and monitoring these adverse effects in clinical practice."( Adverse effects of antiretroviral therapy for HIV infection: a review of selected topics.
Mallal, S; Nolan, D; Reiss, P, 2005
)
0.33
"The relationships between adverse events (AEs) and plasma concentrations of nevirapine (NVP) and efavirenz (EFV) were investigated as part of the large, international, randomized 2NN study."( Are adverse events of nevirapine and efavirenz related to plasma concentrations?
Baraldi, E; Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, JM; MacGregor, TR; Montella, F; Robinson, PA; Russell, DB; Thompson, MA; Uip, DE; van Leth, F, 2005
)
0.33
" We aimed to determine whether monitoring the plasma concentration of efavirenz could predict neuropsychiatric adverse events associated with long-term therapy with efavirenz."( Prediction of neuropsychiatric adverse events associated with long-term efavirenz therapy, using plasma drug level monitoring.
Antón, R; Borrás, J; Gutiérrez, F; Martín-Hidalgo, A; Masiá, M; Navarro, A; Padilla, S, 2005
)
0.33
"8%) of the patients experienced CNS-related adverse effects, ranging from insomnia and abnormal dreams to depression with suicidal ideation."( Prediction of neuropsychiatric adverse events associated with long-term efavirenz therapy, using plasma drug level monitoring.
Antón, R; Borrás, J; Gutiérrez, F; Martín-Hidalgo, A; Masiá, M; Navarro, A; Padilla, S, 2005
)
0.33
" Patients achieving higher plasma levels are at increased risk of experiencing neuropsychiatric adverse events."( Prediction of neuropsychiatric adverse events associated with long-term efavirenz therapy, using plasma drug level monitoring.
Antón, R; Borrás, J; Gutiérrez, F; Martín-Hidalgo, A; Masiá, M; Navarro, A; Padilla, S, 2005
)
0.33
" This is a retrospective analysis of virologic efficacy and changes in adverse neuropsychiatric effects and serum lipid levels after this switch."( Switch from efavirenz to nevirapine associated with resolution of efavirenz-related neuropsychiatric adverse events and improvement in lipid profiles.
Curtin, JM; Ward, DJ, 2006
)
0.33
" Both regimens were reasonably well tolerated, although more gastrointestinal adverse events were reported with saquinavir-SGC/ritonavir."( Efficacy, safety and pharmacokinetics of once-daily saquinavir soft-gelatin capsule/ritonavir in antiretroviral-naive, HIV-infected patients.
Burnside, AF; Jayaweera, DT; Montaner, JS; Saag, MS; Schutz, M; Schwartz, R; Walmsley, S, 2006
)
0.33
" Gastrointestinal adverse effects were commonly associated with treatment failure in the saquinavir-SGC/ritonavir arm of the study."( Efficacy, safety and pharmacokinetics of once-daily saquinavir soft-gelatin capsule/ritonavir in antiretroviral-naive, HIV-infected patients.
Burnside, AF; Jayaweera, DT; Montaner, JS; Saag, MS; Schutz, M; Schwartz, R; Walmsley, S, 2006
)
0.33
" All available safety data (including data beyond 48 weeks) were used in all analyses, which included calculation of treatment emergent laboratory values, adverse events (AEs), serious AEs, fatalities, drug discontinuations and any summaries by study week of safety data."( Long-term safety and tolerability of the lamivudine/abacavir combination as components of highly active antiretroviral therapy.
Brothers, CH; Castillo, SA; Hernandez, JE, 2006
)
0.33
"This analysis indicates that the combination of lamivudine/abacavir is generally safe for the majority of patients when used as part of combination therapy."( Long-term safety and tolerability of the lamivudine/abacavir combination as components of highly active antiretroviral therapy.
Brothers, CH; Castillo, SA; Hernandez, JE, 2006
)
0.33
"Liver toxicity is one of the most relevant adverse effects of antiretroviral therapy."( Liver toxicity induced by non-nucleoside reverse transcriptase inhibitors.
Mira, JA; Pineda, JA; Rivero, A, 2007
)
0.34
" Study medication administration was stopped for 14 children, mostly because of nonadherence (4 cases) or virologic rebound (5 cases) and because of adverse events (unrelated death and grade 2 liver toxicity) in 2 cases."( Once-daily highly active antiretroviral therapy for HIV-infected children: safety and efficacy of an efavirenz-containing regimen.
Bekker, V; Jurriaans, S; Kuijpers, TW; Lange, JM; Pajkrt, D; Scherpbier, HJ, 2007
)
0.34
" No patient discontinued due to renal adverse events."( The safety and efficacy of tenofovir DF in combination with lamivudine and efavirenz through 6 years in antiretroviral-naïve HIV-1-infected patients.
Cassetti, I; Cheng, AK; Enejosa, J; Etzel, A; Madruga, JV; Suleiman, JM; Zhong, L,
)
0.13
" TDF treatment was not associated with renal adverse events or limb fat loss in antiretroviral-naïve patients."( The safety and efficacy of tenofovir DF in combination with lamivudine and efavirenz through 6 years in antiretroviral-naïve HIV-1-infected patients.
Cassetti, I; Cheng, AK; Enejosa, J; Etzel, A; Madruga, JV; Suleiman, JM; Zhong, L,
)
0.13
" Two subjects with rashes during the first 2 weeks of therapy were the only adverse events leading to study-drug discontinuation."( Long-term safety and efficacy of a once-daily regimen of emtricitabine, didanosine, and efavirenz in HIV-infected, therapy-naive children and adolescents: Pediatric AIDS Clinical Trials Group Protocol P1021.
Abrams, E; Blum, MR; Britto, P; Chittick, GE; Cunningham, C; Dickover, R; Draper, L; Flynn, P; Hu, C; Hughes, M; Kraimer, J; McKinney, RE; Ortiz, AA; Rathore, M; Reynolds, L; Rodman, J; Scites, M; Serchuck, LK; Smith, ME; Spector, S; Tran, P; Weinberg, A; Yogev, R, 2007
)
0.34
"A once-daily regimen of emtricitabine, didanosine, and efavirenz proved to be safe and tolerable and demonstrated good immunologic and virologic efficacy in this 2-year study."( Long-term safety and efficacy of a once-daily regimen of emtricitabine, didanosine, and efavirenz in HIV-infected, therapy-naive children and adolescents: Pediatric AIDS Clinical Trials Group Protocol P1021.
Abrams, E; Blum, MR; Britto, P; Chittick, GE; Cunningham, C; Dickover, R; Draper, L; Flynn, P; Hu, C; Hughes, M; Kraimer, J; McKinney, RE; Ortiz, AA; Rathore, M; Reynolds, L; Rodman, J; Scites, M; Serchuck, LK; Smith, ME; Spector, S; Tran, P; Weinberg, A; Yogev, R, 2007
)
0.34
" Adverse CNS effects were observed in 19 patients soon after therapy onset."( No observable correlation between central nervous system side effects and EFV plasma concentrations in Japanese HIV type 1-infected patients treated with EFV containing HAART.
Hamaguchi, M; Hirano, A; Ibe, S; Kaneda, T; Kudaka, Y; Mamiya, N; Okumura, N; Suzuki, T; Takahashi, M, 2007
)
0.34
"Simplification to a once-daily regimen containing TDF, 3TC, and EFV is virologically and immunologically effective, well-tolerated, and safe with benefits in the lipid profile in the majority of patients."( Effectiveness and safety of simplification therapy with once-daily tenofovir, lamivudine, and efavirenz in HIV-1-infected patients with undetectable plasma viral load on HAART.
Aguirrebengoa, K; Alvarez, ML; Arazo, P; Arrizabalaga, J; Chocarro, A; Echevarría, S; Fariñas, MC; Ferrer, P; García-Palomo, D; Iribarren, JA; Labarga, P; Letona, S; Muñoz-Sánchez, MJ; Oteo, JA; Peralta, G; Pinilla, J; Uriz, J,
)
0.13
" Overall, 29 adverse events were recorded in 23 patients, the majority associated with neuropsychiatric symptoms of EFV."( Efficacy and safety of a once daily regimen with efavirenz, lamivudine, and didanosine, with and without food, as initial therapy for HIV Infection: the ELADI study.
Asensi, V; Barreiro, P; de Mendoza, C; Estrada, V; González-Lahoz, J; Jiménez-Nacher, I; Palacios, R; Rivas, P; Rodríguez-Novoa, S; Sánchez-Conde, M; Santos, J; Sanz, J; Sola, J; Soriano, V, 2007
)
0.34
" All papers, abstracts, or presentations, regardless of study design, that made reference to the response of patients who were switched from one NNRTI to another as a result of an adverse drug reaction were included."( Is it safe to switch between efavirenz and nevirapine in the event of toxicity?
Maartens, G; Mehta, U, 2007
)
0.34
"HIV-infected women on selected ARV regimens or no ARV were administered DMPA 150 mg intramuscularly and evaluated for 12 weeks for adverse events, changes in CD4+ count and HIV RNA levels, and ovulation."( Safety and tolerability of depot medroxyprogesterone acetate among HIV-infected women on antiretroviral therapy: ACTG A5093.
Clax, PA; Cohn, SE; Hitti, J; Lertora, JJ; Muderspach, L; Park, JG; Stek, A; Watts, DH; Yu, S, 2008
)
0.35
" Nine Grade 3 or 4 adverse events occurred in seven subjects; none were judged related to DMPA."( Safety and tolerability of depot medroxyprogesterone acetate among HIV-infected women on antiretroviral therapy: ACTG A5093.
Clax, PA; Cohn, SE; Hitti, J; Lertora, JJ; Muderspach, L; Park, JG; Stek, A; Watts, DH; Yu, S, 2008
)
0.35
"The aim of this study was to measure the cumulative incidence of adverse events (AEs) related to nevirapine in patients switched from efavirenz to immediate full-dose nevirapine (FDN)."( Efavirenz replacement by immediate full-dose nevirapine is safe in HIV-1-infected patients in Cambodia.
Chhneang, V; Fernandez, M; Laureillard, D; Moeung, S; Ngeth, C; Piketty, C; Prak, N; Quillet, C; Riel, V; Song, S, 2008
)
0.35
" These effects were seen without any documented adverse drug reactions or changes in viral and immunologic control."( Safety and efficacy of simvastatin for the treatment of dyslipidemia in human immunodeficiency virus-infected patients receiving efavirenz-based highly active antiretroviral therapy.
Bain, AM; Bedimo, R; Busti, AJ; Eaton, SA; Nguyen, ST; Payne, KD; Rahman, AP, 2008
)
0.35
" Although mild neuropsychiatric symptoms are a well-known adverse effect of this medication, to our knowledge, this is the first report of status epilepticus with routine efavirenz dosing."( Status epilepticus resulting from severe efavirenz toxicity in an HIV-infected patient.
Kwara, A; Nijhawan, AE; Venna, N; Zachary, KC, 2008
)
0.35
"Mood disorders and other neuropsychiatric disorders are common adverse events limiting tolerability of alpha-interferon (IFN) therapy for hepatitis C virus (HCV)."( Effect of treatment with efavirenz on neuropsychiatric adverse events of interferon in HIV/HCV-coinfected patients.
Casado, JL; Corral, I; Dronda, F; Hernández, B; Moreno, A; Moreno, S; Pérez-Elías, MJ; Quereda, C; Rodríguez-Sagrado, MA, 2008
)
0.35
" Adverse events and concomitant medications were systematically recorded once monthly."( Effect of treatment with efavirenz on neuropsychiatric adverse events of interferon in HIV/HCV-coinfected patients.
Casado, JL; Corral, I; Dronda, F; Hernández, B; Moreno, A; Moreno, S; Pérez-Elías, MJ; Quereda, C; Rodríguez-Sagrado, MA, 2008
)
0.35
"Neuropsychiatric adverse events are common in HIV/HCV patients receiving IFN, usually mild or moderate."( Effect of treatment with efavirenz on neuropsychiatric adverse events of interferon in HIV/HCV-coinfected patients.
Casado, JL; Corral, I; Dronda, F; Hernández, B; Moreno, A; Moreno, S; Pérez-Elías, MJ; Quereda, C; Rodríguez-Sagrado, MA, 2008
)
0.35
" Although frequency of severe renal toxicity was higher than has been reported in the literature, it was safe in patients with no comorbid renal conditions."( Effectiveness and safety of generic fixed-dose combination of tenofovir/emtricitabine/efavirenz in HIV-1-infected patients in Western India.
Bele, V; Dravid, A; Gupte, N; Joshi, K; Pujari, S, 2008
)
0.35
" The patient showed prompt and stable suppression of cryptococcosis and plasma viremia of HIV at long-term follow-up (66 wk), with no significant adverse events."( Long-term efficacy and safety of TDM-assisted combination of voriconazole plus efavirenz in an AIDS patient with cryptococcosis and liver cirrhosis.
Carbonara, S; Ciracì, E; Cusato, M; Heichen, M; Monno, L; Regazzi, M; Stano, F; Villani, P, 2009
)
0.35
"More than 50% of patients who start efavirenz treatment develop limiting neuropsychiatric adverse events (NPAEs)."( Stepped-dose versus full-dose efavirenz for HIV infection and neuropsychiatric adverse events: a randomized trial.
Gutiérrez-Valencia, A; López-Cortés, LF; Lozano, F; Palacios, R; Rivero, A; Ruiz-Valderas, R; Terrón, A; Viciana, P, 2009
)
0.35
" Significantly fewer drug-related clinical adverse events occurred in patients on raltegravir (n=124 [44."( Safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: a multicentre, double-blind randomised controlled trial.
Barnard, RJ; Berger, DS; DeJesus, E; DiNubile, MJ; Lazzarin, A; Leavitt, R; Lennox, JL; Madruga, JV; Miller, MD; Nguyen, BY; Pollard, RB; Rodgers, AJ; Sklar, P; Williams-Diaz, A; Xu, X; Zhao, J, 2009
)
0.35
"In AIDS Clinical Trials Group A5095, 9% of participants who experienced an adverse event related to efavirenz substituted nevirapine."( Substitution of nevirapine because of efavirenz toxicity in AIDS clinical trials group A5095.
Gulick, RM; Kmack, A; Krambrink, A; Kuritzkes, DR; Ribaudo, HJ; Schouten, JT; Shikuma, C; Webb, N, 2010
)
0.36
" The adverse event rate was similar between arms (except drug hypersensitivity, reported more in the abacavir/lamivudine arm)."( Randomized comparison of renal effects, efficacy, and safety with once-daily abacavir/lamivudine versus tenofovir/emtricitabine, administered with efavirenz, in antiretroviral-naive, HIV-1-infected adults: 48-week results from the ASSERT study.
Branco, T; Cavassini, M; Domingo, P; Fisher, M; Givens, N; Khuong-Josses, MA; Lim, ML; Moyle, GJ; Norden, AG; Pearce, HC; Podzamczer, D; Post, FA; Rieger, A; Stellbrink, HJ; Vavro, C, 2010
)
0.36
"People with HIV infection have several risk factors for developing neuropsychiatric adverse events: preexisting conditions, HIV disease stage, and antiretroviral treatment."( Analysis of neuropsychiatric adverse events during clinical trials of efavirenz in antiretroviral-naive patients: a systematic review.
Balkin, A; Gazzard, B; Hill, A,
)
0.13
" Maraviroc recipients had greater CD4 increases (+ 212 vs + 171 cells/mm(3)) and fewer adverse event discontinuations (6."( Efficacy and safety of maraviroc versus efavirenz, both with zidovudine/lamivudine: 96-week results from the MERIT study.
Burnside, R; Craig, C; Di Perri, G; Frank, I; Goodrich, J; Heera, J; Mayer, H; McCracken, J; Pontani, D; Saag, M; Sierra-Madero, J; Wood, R,
)
0.13
" Multivariate analyses were performed to compare, between the ddI and ZDV groups, the proportion of patients with a viral load <500 copies/ml during follow-up; the increase in the CD4 cell count; survival; treatment changes and severe adverse events."( Long-term effectiveness and safety of didanosine combined with lamivudine and efavirenz or nevirapine in antiretroviral-naive patients: a 9-year cohort study in Senegal.
Delaporte, E; Diouf, A; Etard, JF; Girard, PM; Landman, R; Laurent, C; Molinari, N; Ndoye, I; Ngom Guèye, NF; Sow, PS; Tchatchueng Mbougua, JB, 2011
)
0.37
" Safety and tolerability were assessed throughout the study by continuous collection of adverse events (AEs), including adverse drug reactions, illnesses with onset during the study, exacerbation of previous illnesses, and clinically significant changes in physical examination findings."( Safety and tolerability of lersivirine, a nonnucleoside reverse transcriptase inhibitor, during a 28-day, randomized, placebo-controlled, Phase I clinical study in healthy male volunteers.
Choo, H; Davis, J; Goodrich, J; Hackman, F; Langdon, G; Lewis, D; Ndongo, MN; Tawadrous, M, 2010
)
0.36
"A randomized, double-blind trial in patients with viral suppression but ongoing CNS adverse events after more than 12 weeks EFV."( A phase IV, double-blind, multicentre, randomized, placebo-controlled, pilot study to assess the feasibility of switching individuals receiving efavirenz with continuing central nervous system adverse events to etravirine.
Fisher, M; Garvey, L; Hadley, W; Higgs, C; Mandalia, S; Nelson, M; Nicola, M; Perry, N; Waters, L; Winston, A, 2011
)
0.37
" Baseline CNS adverse events were similar."( A phase IV, double-blind, multicentre, randomized, placebo-controlled, pilot study to assess the feasibility of switching individuals receiving efavirenz with continuing central nervous system adverse events to etravirine.
Fisher, M; Garvey, L; Hadley, W; Higgs, C; Mandalia, S; Nelson, M; Nicola, M; Perry, N; Waters, L; Winston, A, 2011
)
0.37
"Switching EFV to ETR led to a significant reduction in overall G2-4 CNS adverse events, including insomnia, abnormal dreams and nervousness as individual adverse event."( A phase IV, double-blind, multicentre, randomized, placebo-controlled, pilot study to assess the feasibility of switching individuals receiving efavirenz with continuing central nervous system adverse events to etravirine.
Fisher, M; Garvey, L; Hadley, W; Higgs, C; Mandalia, S; Nelson, M; Nicola, M; Perry, N; Waters, L; Winston, A, 2011
)
0.37
"Although efavirenz is a universally recommended treatment for naive HIV-infected individuals, neuropsychiatric adverse events are common."( A comparison of neuropsychiatric adverse events during 12 weeks of treatment with etravirine and efavirenz in a treatment-naive, HIV-1-infected population.
Banhegyi, D; Gazzard, B; Hill, A; Marks, S; Nelson, M; Podzamczer, D; Stark, T; Stellbrink, HJ; van Delft, Y; Vingerhoets, J, 2011
)
0.37
" The primary end point was the percentage of patients with grade 1-4 drug-related treatment-emergent neuropsychiatric adverse events up to week 12."( A comparison of neuropsychiatric adverse events during 12 weeks of treatment with etravirine and efavirenz in a treatment-naive, HIV-1-infected population.
Banhegyi, D; Gazzard, B; Hill, A; Marks, S; Nelson, M; Podzamczer, D; Stark, T; Stellbrink, HJ; van Delft, Y; Vingerhoets, J, 2011
)
0.37
"After 12 weeks, first-line treatment with etravirine 400 mg once daily with two NRTIs was associated with significantly fewer neuropsychiatric adverse events when compared with efavirenz with two NRTIs."( A comparison of neuropsychiatric adverse events during 12 weeks of treatment with etravirine and efavirenz in a treatment-naive, HIV-1-infected population.
Banhegyi, D; Gazzard, B; Hill, A; Marks, S; Nelson, M; Podzamczer, D; Stark, T; Stellbrink, HJ; van Delft, Y; Vingerhoets, J, 2011
)
0.37
" The incidence of drug-related adverse events was similar in raltegravir recipients with and without hepatitis coinfection in both STARTMRK (50 vs."( Safety and efficacy of raltegravir in patients with HIV-1 and hepatitis B and/or C virus coinfection.
Harvey, C; Leavitt, R; Nguyen, BY; Rockstroh, J; Sklar, P; Strohmaier, K; Teppler, H; Zhao, J, 2012
)
0.38
" Primary outcome was a composite of death, virological failure, default, or serious adverse event (SAE) at 24 weeks."( Efficacy and safety of once-daily nevirapine- or efavirenz-based antiretroviral therapy in HIV-associated tuberculosis: a randomized clinical trial.
Bhavani, PK; Dilip, M; Iliayas, S; Menon, PA; Narendran, G; Padmapriyadarsini, C; Ponnuraja, C; Pooranagangadevi, NP; Ramachandran, R; Ramesh Kumar, S; Selvaraju, S; Swaminathan, S; Venkatesan, P, 2011
)
0.37
"5%) subjects discontinued ART due to this adverse event."( Liver toxicity associated with antiretroviral therapy including efavirenz or ritonavir-boosted protease inhibitors in a cohort of HIV/hepatitis C virus co-infected patients.
Camacho, A; Collado, A; de Los Santos-Gil, I; González-Serrano, M; Macías, J; Merino, D; Mira, JA; Neukam, K; Parra-García, G; Pineda, JA; Rivero, A; Ruiz-Morales, J; Torres-Cornejo, A, 2011
)
0.37
" There were no grade 3 or 4 clinical adverse events."( Safety, tolerability, and pharmacokinetic interactions of the antituberculous agent TMC207 (bedaquiline) with efavirenz in healthy volunteers: AIDS Clinical Trials Group Study A5267.
Allen, R; Aweeka, F; Cramer, Y; Dooley, KE; Flexner, C; Gupta, A; Haas, DW; Lizak, P; Park, JG; Qasba, S; Swindells, S; van Heeswijk, R; Wiggins, I, 2012
)
0.38
" Adverse events, viral load (VL), PK, and reverse transcriptase mutations were assessed and combined for analysis."( Safety and efficacy of GSK2248761, a next-generation nonnucleoside reverse transcriptase inhibitor, in treatment-naive HIV-1-infected subjects.
Dudas, K; Dumont, E; Kim, J; Lou, Y; Mayers, D; Pietropaolo, K; Piscitelli, S; St Clair, M; White, S; Zala, C; Zhou, XJ, 2012
)
0.38
" Rilpivirine compared with efavirenz gave smaller incidences of adverse events leading to discontinuation (3% vs."( Efficacy and safety of rilpivirine (TMC278) versus efavirenz at 48 weeks in treatment-naive HIV-1-infected patients: pooled results from the phase 3 double-blind randomized ECHO and THRIVE Trials.
Boven, K; Cahn, P; Clotet, B; Cohen, CJ; Crauwels, H; Fourie, J; Grinsztejn, B; Johnson, MA; Lefebvre, E; Molina, JM; Rimsky, LT; Saag, M; Supparatpinyo, K; Vanveggel, S; Williams, P; Wu, H, 2012
)
0.38
"Hepatic toxicity and metabolic disorders are major adverse effects elicited during the pharmacological treatment of the human immunodeficiency virus (HIV) infection."( Profile of stress and toxicity gene expression in human hepatic cells treated with Efavirenz.
Apostolova, N; Blas-Garcia, A; Esplugues, JV; Gomez-Sucerquia, LJ; Marti-Cabrera, M, 2012
)
0.38
" Adverse events were mostly mild and no serious adverse events or drug discontinuations were reported."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
" Lipodystrophy accounted for 87 of 96 toxic events."( Frequency of stavudine substitution due to toxicity in children receiving antiretroviral treatment in sub-Saharan Africa.
Chersich, M; Fairlie, L; Kuhn, L; Meyers, T; Moultrie, H; Palmer, M, 2013
)
0.39
" Beyond week 48, the incidence of virologic failure was comparable (3 versus 2%) between treatment groups, rilpivirine resistance-associated mutations were consistent with those observed in year 1, there were few adverse events in both groups and no new safety concerns."( Week 96 efficacy and safety of rilpivirine in treatment-naive, HIV-1 patients in two Phase III randomized trials.
Boven, K; Cassetti, I; Chetchotisakd, P; Cohen, CJ; Crauwels, H; Lazzarin, A; Li, T; Molina, JM; Orkin, C; Rhame, F; Rimsky, L; Stellbrink, HJ; Vanveggel, S; Williams, P, 2013
)
0.39
" Overall incidences of all-causality treatment-related or grade 3/4 adverse events (AEs) or AE-related discontinuations were lower with lersivirine than with efavirenz, and serious AEs occurred at similar rates across treatment groups."( Efficacy and safety of lersivirine (UK-453,061) versus efavirenz in antiretroviral treatment-naive HIV-1-infected patients: week 48 primary analysis results from an ongoing, multicenter, randomized, double-blind, phase IIb trial.
Cooper, DA; Craig, C; Goodrich, J; Kaplan, R; Lazzarin, A; Mori, J; Pozniak, A; Pulik, P; Tawadrous, M; Valdez, H; Vernazza, P; Wang, C; Weil, E, 2013
)
0.39
"We systematically reviewed adverse events among treatment-naive HIV-positive adults and children receiving either NVP or EFV as part of first-line antiretroviral therapy."( Adverse events associated with nevirapine and efavirenz-based first-line antiretroviral therapy: a systematic review and meta-analysis.
Andrieux-Meyer, I; Calmy, A; Ford, N; Hargreaves, S; Mills, EJ; Renaud-Théry, F; Shaffer, N; Shubber, Z; Vitoria, M, 2013
)
0.39
"Compared to NVP, EFV is associated with a lower frequency of severe adverse events, in particular treatment discontinuations."( Adverse events associated with nevirapine and efavirenz-based first-line antiretroviral therapy: a systematic review and meta-analysis.
Andrieux-Meyer, I; Calmy, A; Ford, N; Hargreaves, S; Mills, EJ; Renaud-Théry, F; Shaffer, N; Shubber, Z; Vitoria, M, 2013
)
0.39
"Overall, 71 of 281 raltegravir recipients (25%) and 98 of 282 efavirenz recipients (35%) discontinued the study; discontinuations due to adverse events occurred in 14 (5%) and 28 (10%) patients in the respective groups."( Durable efficacy and safety of raltegravir versus efavirenz when combined with tenofovir/emtricitabine in treatment-naive HIV-1-infected patients: final 5-year results from STARTMRK.
DeJesus, E; DiNubile, MJ; Leavitt, R; Lennox, JL; Miller, M; Nguyen, BY; Rockstroh, JK; Rodgers, AJ; Saag, MS; Sklar, P; Teppler, H; Walker, ML; Wan, H; Yazdanpanah, Y, 2013
)
0.39
" Over the entire study, fewer patients experienced neuropsychiatric and drug-related adverse events in the raltegravir group than in the efavirenz group."( Durable efficacy and safety of raltegravir versus efavirenz when combined with tenofovir/emtricitabine in treatment-naive HIV-1-infected patients: final 5-year results from STARTMRK.
DeJesus, E; DiNubile, MJ; Leavitt, R; Lennox, JL; Miller, M; Nguyen, BY; Rockstroh, JK; Rodgers, AJ; Saag, MS; Sklar, P; Teppler, H; Walker, ML; Wan, H; Yazdanpanah, Y, 2013
)
0.39
" Neuropsychiatric adverse effects are by far the most common reasons for discontinuation."( Discontinuation of efavirenz therapy in HIV patients due to neuropsychiatric adverse effects.
Larsen, CS; Leutscher, PD; Stecher, C; Storgaard, M, 2013
)
0.39
"Cyproheptadine prevention of the neuropsychiatric adverse effects of an antiretroviral regimen including efavirenz has been evaluated in a randomized clinical trial."( Cyproheptadine for prevention of neuropsychiatric adverse effects of efavirenz: a randomized clinical trial.
Akhondzadeh, S; Alimadadi, A; Dabaghzadeh, F; Ghaeli, P; Jafari, S; Khalili, H; Khazaeipour, Z, 2013
)
0.39
"A total of 119 HIV-positive patients, in which 1350 EFV plasma concentrations, 68 SNPs and 14 EFV-related adverse effects (AEs) were analyzed."( Impact of pharmacogenetics on CNS side effects related to efavirenz.
Cabrera Figueroa, S; Carracedo Álvarez, A; Cruz Guerrero, R; Hurlé, AD; Hurtado, LP; Sánchez Martín, A, 2013
)
0.39
" Efavirenz, especially its major metabolite 8-hydroxy-efavirenz, is toxic in neuron cultures at concentrations found in the cerebrospinal fluid."( Neuronal toxicity of efavirenz: a systematic review.
Decloedt, EH; Maartens, G, 2013
)
0.39
" The case illustrates the value of routine monitoring after initiating antiretroviral therapy and the fundamental importance of engaging patients in long-term management to ensure safe treatment."( Liver transplantation for acute liver failure due to efavirenz hepatotoxicity: the importance of routine monitoring.
Bloch, E; Fink, DL, 2013
)
0.39
"Due to ongoing neuropsychiatric adverse events in some efavirenz (EFV)-treated patients, a switch to an alternative non-nucleoside reverse transcriptase inhibitor may be considered."( Efficacy and safety 48 weeks after switching from efavirenz to rilpivirine using emtricitabine/tenofovir disoproxil fumarate-based single-tablet regimens.
Brinson, C; Cheng, AK; Chuck, SK; Cohen, C; Dejesus, E; Mills, AM; Ramanathan, S; Wang, MH; White, K; Williams, S; Yale, KL,
)
0.13
" No subjects discontinued the study due to an adverse event."( Efficacy and safety 48 weeks after switching from efavirenz to rilpivirine using emtricitabine/tenofovir disoproxil fumarate-based single-tablet regimens.
Brinson, C; Cheng, AK; Chuck, SK; Cohen, C; Dejesus, E; Mills, AM; Ramanathan, S; Wang, MH; White, K; Williams, S; Yale, KL,
)
0.13
" This case report indicates the possibility of adverse effects developing when the 2 drugs are used together."( Effect of concomitant use of montelukast and efavirenz on neuropsychiatric adverse events.
Ibarra-Barrueta, O; Mayo-Suarez, J; Mora-Atorrasagasti, O; Palacios-Zabalza, I, 2014
)
0.4
"There is an urgent need for new antituberculosis (anti-TB) drugs, including agents that are safe and effective with concomitant antiretrovirals (ARV) and first-line TB drugs."( Phase I safety, pharmacokinetics, and pharmacogenetics study of the antituberculosis drug PA-824 with concomitant lopinavir-ritonavir, efavirenz, or rifampin.
Allen, R; Aweeka, F; Bao, J; Cramer, Y; Dooley, KE; Haas, DW; Koletar, SL; Luetkemeyer, AF; Marzan, F; Murray, S; Park, JG; Savic, R; Sutherland, D, 2014
)
0.4
" MVC was well tolerated with no grade 3/4 adverse events; all subjects maintained viral suppression to the end of the study."( Switching safely: pharmacokinetics, efficacy and safety of switching efavirenz to maraviroc twice daily in patients on suppressive antiretroviral therapy.
Back, D; Boffito, M; Else, L; Gazzard, B; Jackson, A; Nelson, M; Newell, S; Rockwood, N; Waters, L, 2015
)
0.42
" efavirenz experienced treatment-related adverse events (68."( Efficacy and safety of maraviroc vs. efavirenz in treatment-naive patients with HIV-1: 5-year findings.
Botes, M; Burnside, R; Clumeck, N; Cooper, DA; Dejesus, E; Heera, J; Ive, P; Lazzarin, A; Mukwaya, G; Saag, M; van Der Ryst, E; Walmsley, S, 2014
)
0.4
"Growing evidence associates the non-nucleoside reverse transcriptase inhibitor efavirenz with several adverse events."( Lack of mitochondrial toxicity of darunavir, raltegravir and rilpivirine in neurons and hepatocytes: a comparison with efavirenz.
Alegre, F; Apostolova, N; Blas-García, A; Esplugues, JV; Funes, HA; Martínez, E; Polo, M, 2014
)
0.4
"Darunavir, rilpivirine and raltegravir do not induce toxic effects on Hep3B cells and primary rat neurons, which suggests a safer hepatic and neurological profile than that of efavirenz."( Lack of mitochondrial toxicity of darunavir, raltegravir and rilpivirine in neurons and hepatocytes: a comparison with efavirenz.
Alegre, F; Apostolova, N; Blas-García, A; Esplugues, JV; Funes, HA; Martínez, E; Polo, M, 2014
)
0.4
" Grade 1 or 2 gastrointestinal adverse events were higher among women on lopinavir/ritonavir versus efavirenz."( Efficacy and safety of lopinavir/ritonavir versus efavirenz-based antiretroviral therapy in HIV-infected pregnant Ugandan women.
Achan, J; Ades, V; Charlebois, ED; Clark, TD; Cohan, D; Gandhi, M; Havlir, DV; Kamya, MR; Koss, CA; Luwedde, F; Mwesigwa, J; Natureeba, P; Nzarubara, B; Plenty, A; Ruel, T, 2015
)
0.42
" No serious adverse event related to tenofovir."( Efficacy, safety and pharmacokinetics of tenofovir disoproxil fumarate in virologic-suppressed HIV-infected children using weight-band dosing.
Aurpibul, L; Chokephaibulkit, K; Cressey, TR; Phongsamart, W; Sirisanthana, V; Sricharoenchai, S; Sudjaritruk, T; Wittawatmongkol, O, 2015
)
0.42
"TDF substitution in children and adolescents who were otherwise stable while receiving a first-line nonnucleoside reverse transcriptase inhibitor-based regimen achieved adequate exposure without clinically significant renal or bone adverse events over 96 weeks."( Efficacy, safety and pharmacokinetics of tenofovir disoproxil fumarate in virologic-suppressed HIV-infected children using weight-band dosing.
Aurpibul, L; Chokephaibulkit, K; Cressey, TR; Phongsamart, W; Sirisanthana, V; Sricharoenchai, S; Sudjaritruk, T; Wittawatmongkol, O, 2015
)
0.42
"Efavirenz (EFV) is widely used for the treatment of antiretroviral-naive HIV-positive individuals, but there are concerns about the risk of adverse neuropsychiatric events."( Comparative Safety and Neuropsychiatric Adverse Events Associated With Efavirenz Use in First-Line Antiretroviral Therapy: A Systematic Review and Meta-Analysis of Randomized Trials.
Calmy, A; Doherty, M; Ford, N; Kirby, C; Pozniak, A; Shubber, Z; Vitoria, M, 2015
)
0.42
" The primary outcome was drug discontinuation as a result of any adverse event."( Comparative Safety and Neuropsychiatric Adverse Events Associated With Efavirenz Use in First-Line Antiretroviral Therapy: A Systematic Review and Meta-Analysis of Randomized Trials.
Calmy, A; Doherty, M; Ford, N; Kirby, C; Pozniak, A; Shubber, Z; Vitoria, M, 2015
)
0.42
" A lower relative and absolute risk of discontinuations due to adverse drug reactions was seen with EFV compared to nevirapine."( Comparative Safety and Neuropsychiatric Adverse Events Associated With Efavirenz Use in First-Line Antiretroviral Therapy: A Systematic Review and Meta-Analysis of Randomized Trials.
Calmy, A; Doherty, M; Ford, N; Kirby, C; Pozniak, A; Shubber, Z; Vitoria, M, 2015
)
0.42
" The relative risk of discontinuations due to adverse events was higher for EFV compared with most other first-line options, but absolute differences were less than 5% for all comparisons."( Comparative Safety and Neuropsychiatric Adverse Events Associated With Efavirenz Use in First-Line Antiretroviral Therapy: A Systematic Review and Meta-Analysis of Randomized Trials.
Calmy, A; Doherty, M; Ford, N; Kirby, C; Pozniak, A; Shubber, Z; Vitoria, M, 2015
)
0.42
" Adverse events and serious adverse events were summarised by treatment group."( Efficacy and safety of efavirenz 400 mg daily versus 600 mg daily: 96-week data from the randomised, double-blind, placebo-controlled, non-inferiority ENCORE1 study.
Amin, J; Belloso, W; Carey, D; Cooper, DA; Crabtree-Ramirez, B; Emery, S; Foulkes, S; Jessen, H; Kumar, S; Lee, MP; Losso, M; Mohapi, L; Phanupak, P; Puls, R; Winston, A, 2015
)
0.42
" Adverse events were reported by 291 (91%) of 321 patients in the efavirenz 400 mg group and by 285 (92%) of 309 in the 600 mg group (p=0·48)."( Efficacy and safety of efavirenz 400 mg daily versus 600 mg daily: 96-week data from the randomised, double-blind, placebo-controlled, non-inferiority ENCORE1 study.
Amin, J; Belloso, W; Carey, D; Cooper, DA; Crabtree-Ramirez, B; Emery, S; Foulkes, S; Jessen, H; Kumar, S; Lee, MP; Losso, M; Mohapi, L; Phanupak, P; Puls, R; Winston, A, 2015
)
0.42
" Fewer efavirenz-related adverse events were reported with the 400 mg efavirenz dose than with the 600 mg dose."( Efficacy and safety of efavirenz 400 mg daily versus 600 mg daily: 96-week data from the randomised, double-blind, placebo-controlled, non-inferiority ENCORE1 study.
Amin, J; Belloso, W; Carey, D; Cooper, DA; Crabtree-Ramirez, B; Emery, S; Foulkes, S; Jessen, H; Kumar, S; Lee, MP; Losso, M; Mohapi, L; Phanupak, P; Puls, R; Winston, A, 2015
)
0.42
" Moreover, the possibility of common cellular impacts underlying adverse effects of efavirenz in sperm cells and neurons deserved investigation."( Impaired sperm motility in HIV-infected men: an unexpected adverse effect of efavirenz?
De Almeida, M; Dulioust, E; Frapsauce, C; Gayet, V; Grabar, S; Jouannet, P; Launay, O; Leruez-Ville, M; Sogni, P; Viard, JP, 2015
)
0.42
" We also found no significant differences between the two groups for adverse events and death."( Efficacy and safety of abacavir-containing combination antiretroviral therapy as first-line treatment of HIV infected children and adolescents: a systematic review and meta-analysis.
Adetokunboh, OO; Balogun, TA; Schoonees, A; Wiysonge, CS, 2015
)
0.42
" Additional assessments included CD4 cell counts, genotypic/phenotypic resistance, adverse events, patient-reported outcomes, and quality of life questionnaires."( Rilpivirine vs. efavirenz-based single-tablet regimens in treatment-naive adults: week 96 efficacy and safety from a randomized phase 3b study.
Antinori, A; Arribas, JR; Bloch, M; Bosse, M; Chuck, SK; Cohen, CJ; De-Oertel, S; Garner, W; Piontkowsky, D; Porter, D; Rachlis, A; Rieger, A; Segal-Maurer, S; van Lunzen, J; Wohl, DA, 2016
)
0.43
" Compared with EFV/FTC/TDF, RPV/FTC/TDF was associated with fewer adverse event-related discontinuations (3."( Rilpivirine vs. efavirenz-based single-tablet regimens in treatment-naive adults: week 96 efficacy and safety from a randomized phase 3b study.
Antinori, A; Arribas, JR; Bloch, M; Bosse, M; Chuck, SK; Cohen, CJ; De-Oertel, S; Garner, W; Piontkowsky, D; Porter, D; Rachlis, A; Rieger, A; Segal-Maurer, S; van Lunzen, J; Wohl, DA, 2016
)
0.43
"This combination ART regimen is safe and effective for patients with HIV/HBV co-infection."( Efficacy and Safety of Tenofovir and Lamivudine in Combination with Efavirenz in Patients Co-infected with Human Immunodeficiency Virus and Hepatitis B Virus in China.
Cai, WP; He, HL; Huang, SB; Ling, XM; Liu, YF; Wang, H; Wang, M; Wang, XC; Wei, FL; Wu, H; Wu, YS; Wu, ZY; Yang, L; Zhang, FJ; Zhang, WW, 2016
)
0.43
"WHO recommends tenofovir, efavirenz, and lamivudine or emtricitabine for first-line antiretroviral therapy (ART) in adults, which replaced more toxic regimens using stavudine, zidovudine or nevirapine."( Key toxicity issues with the WHO-recommended first-line antiretroviral therapy regimen.
Cohen, K; Maartens, G; Mouton, JP, 2016
)
0.43
" In sub-Saharan Africa, efavirenz (EFV) forms the preferred first-line ART but adverse drug events have also been reported."( Rolling out Efavirenz for HIV Precision Medicine in Africa: Are We Ready for Pharmacovigilance and Tackling Neuropsychiatric Adverse Effects?
Dandara, C; Leutscher, PD; Masimirembwa, C, 2016
)
0.43
" However, EFV administration has also led to severe adverse effects, several reports highlighted the role of EFV in mitochondrial dysfunction and toxicity but the molecular mechanism has been poorly understood."( Depolarization of mitochondrial membrane potential is the initial event in non-nucleoside reverse transcriptase inhibitor efavirenz induced cytotoxicity.
Chaubey, B; Ganta, KK; Mandal, A, 2017
)
0.46
" We extracted data on trial and patient characteristics, and the following primary outcomes: viral suppression, mortality, AIDS defining illnesses, discontinuations, discontinuations due to adverse events, and serious adverse events."( Comparative efficacy and safety of first-line antiretroviral therapy for the treatment of HIV infection: a systematic review and network meta-analysis.
Bansback, N; Doherty, M; Ford, N; Forrest, JI; Kanters, S; Mills, EJ; Nsanzimana, S; Popoff, E; Socias, ME; Thorlund, K; Vitoria, M, 2016
)
0.43
" Both low-dose efavirenz and integrase strand transfer inhibitors tended to be protective of discontinuations due to adverse events relative to normal-dose efavirenz."( Comparative efficacy and safety of first-line antiretroviral therapy for the treatment of HIV infection: a systematic review and network meta-analysis.
Bansback, N; Doherty, M; Ford, N; Forrest, JI; Kanters, S; Mills, EJ; Nsanzimana, S; Popoff, E; Socias, ME; Thorlund, K; Vitoria, M, 2016
)
0.43
" Of the nine patients excluded from the study, only one was withdrawn due to adverse events."( Effectiveness and safety of generic version of abacavir/lamivudine and efavirenz in treatment naïve HIV-infected patients: a nonrandomized, open-label, phase IV study in Cali-Colombia, 2011-2012.
Amariles, P; Galindo, J; Galindo-Orrego, X; González-Avendaño, S; Hincapié, JA; Mueses-Marín, HF, 2016
)
0.43
" We conducted a thorough review of the reported studies to elucidate the relationship between polymorphisms in CYP2B6 with adverse events and treatment response, including virologic suppression, immunologic response, resistance, and discontinuation of treatment."( Role of Cytochrome P450 2B6 Pharmacogenomics in Determining Efavirenz-Mediated Central Nervous System Toxicity, Treatment Outcomes, and Dosage Adjustments in Patients with Human Immunodeficiency Virus Infection.
Varghese Gupta, S; Vo, TT, 2016
)
0.43
" Relevant articles were hand-searched for renal (Grade 3-4 serum creatinine/estimated glomerular filtration rate elevations, renal adverse events [AEs], discontinuation due to renal AEs, and urinary biomarkers) and bone outcomes (bone mineral density [BMD] reductions, bone turnover markers, and fracture), and results compiled qualitatively."( Systematic review of renal and bone safety of the antiretroviral regimen efavirenz, emtricitabine, and tenofovir disoproxil fumarate in patients with HIV infection.
Bedimo, R; Myers, J; Rosenblatt, L, 2016
)
0.43
"Several neuropsychiatric adverse effects of efavirenz are known."( Effect of Valerian in Preventing Neuropsychiatric Adverse Effects of Efavirenz in HIV-Positive Patients: A Pilot Randomized, Placebo-Controlled Clinical Trial.
Abbasian, L; Ahmadi, M; Ghaeli, P; Khalili, H, 2017
)
0.46
"To evaluate the efficacy and safety of valerian in preventing neuropsychiatric adverse effects of efavirenz in HIV-positive patients."( Effect of Valerian in Preventing Neuropsychiatric Adverse Effects of Efavirenz in HIV-Positive Patients: A Pilot Randomized, Placebo-Controlled Clinical Trial.
Abbasian, L; Ahmadi, M; Ghaeli, P; Khalili, H, 2017
)
0.46
" Nausea was the second common adverse effect that 84% and 76."( Effect of Valerian in Preventing Neuropsychiatric Adverse Effects of Efavirenz in HIV-Positive Patients: A Pilot Randomized, Placebo-Controlled Clinical Trial.
Abbasian, L; Ahmadi, M; Ghaeli, P; Khalili, H, 2017
)
0.46
" Valerian may be considered as a potential option in preventing neuropsychiatric adverse effects of efavirenz in HIV-positive patients."( Effect of Valerian in Preventing Neuropsychiatric Adverse Effects of Efavirenz in HIV-Positive Patients: A Pilot Randomized, Placebo-Controlled Clinical Trial.
Abbasian, L; Ahmadi, M; Ghaeli, P; Khalili, H, 2017
)
0.46
"Efavirenz is an anti-HIV drug that presents relevant short- and long-term central nervous system adverse reactions."( Unmasking efavirenz neurotoxicity: Time matters to the underlying mechanisms.
Antunes, AMM; Cipriano, M; Diogo, LN; Grilo, NM; João Correia, M; Matilde Marques, M; Miranda, JP; Monteiro, EC; Pereira, SA; Serpa, J, 2017
)
0.46
"This study aimed to identify the 516 G>T polymorphism of the CYP2B6 gene and evaluate its influence on central nervous system (CNS) side effect development in HIV-positive individuals undergoing Efavirenz (EFV) treatment in a population from southern Brazil."( CYP2B6 516 G>T polymorphism and side effects of the central nervous system in HIV-positive individuals under Efavirenz treatment: Study of a sample from southern Brazil.
Ellwanger, JH; Matte, MCC; Michita, RT; Müller, TE; Renner, JDP, 2017
)
0.46
" The toxic and genotoxic potential of EFV and TDF alone and in combinations {EFV+combivir [zidovudine (AZT)+lamivudine (3TC)] and TDF+3TC} were assessed using the comet assay and the somatic mutation and recombination test (SMART) in Drosophila melanogaster."( In vivo genotoxicity evaluation of efavirenz (EFV) and tenofovir disoproxil fumarate (TDF) alone and in their clinical combinations in Drosophila melanogaster.
Chen-Chen, L; Cunha, KS; de Jesus Silva Carvalho, C; de Melo E Silva, D; de Moraes Filho, AV; Gonçalves, MW; Rohde, C; Verçosa, CJ, 2017
)
0.46
" Some of its toxic effects on hepatic cells have been reported to display features of mitochondrial dysfunction through bioenergetic stress and autophagy, etc."( Increased MMAB level in mitochondria as a novel biomarker of hepatotoxicity induced by Efavirenz.
Feng, Y; Jia, X; Jin, JO; Liu, L; Lu, H; Ma, F; Tan, Z; Wu, D; Yin, L; Zhang, L, 2017
)
0.46
"Results from nonrandomized cohort studies suggest higher risks of CNS adverse events for dolutegravir, versus other ARVs."( Risks of cardiovascular or central nervous system adverse events and immune reconstitution inflammatory syndrome, for dolutegravir versus other antiretrovirals: meta-analysis of randomized trials.
Hill, AM; Hughes, S; Mitchell, N; Pozniak, AL, 2018
)
0.48
"There was a higher risk of Grade 1-4 insomnia adverse events for DTG (6."( Risks of cardiovascular or central nervous system adverse events and immune reconstitution inflammatory syndrome, for dolutegravir versus other antiretrovirals: meta-analysis of randomized trials.
Hill, AM; Hughes, S; Mitchell, N; Pozniak, AL, 2018
)
0.48
"In this meta-analysis, there was no significant effect of dolutegravir on the risk of cardiac, IRIS or suicide-related serious adverse events."( Risks of cardiovascular or central nervous system adverse events and immune reconstitution inflammatory syndrome, for dolutegravir versus other antiretrovirals: meta-analysis of randomized trials.
Hill, AM; Hughes, S; Mitchell, N; Pozniak, AL, 2018
)
0.48
" The form is designed to obtain information on the demographics of the patients, WHO clinical stage of their HIV infection, HAART regimen for the patients, and suspected adverse events associated with the antiretroviral drugs used by the patients."( A prospective study of adverse events to antiretroviral therapy in HIV- infected adults in Ekiti State, Nigeria.
Awodele, O; Oshikoya, KA; Popoola, TD, 2016
)
0.43
" About half (57%) of the participants reported clinical adverse events; 92% of which were reported within two weeks of HAART initiation."( A prospective study of adverse events to antiretroviral therapy in HIV- infected adults in Ekiti State, Nigeria.
Awodele, O; Oshikoya, KA; Popoola, TD, 2016
)
0.43
"Antiretroviral drugs exposure often presents with adverse events, an observation similar to other studies."( A prospective study of adverse events to antiretroviral therapy in HIV- infected adults in Ekiti State, Nigeria.
Awodele, O; Oshikoya, KA; Popoola, TD, 2016
)
0.43
" EFV is well known to cause neuropsychiatric side-effects on initiation, and a recent adult case series described late-onset neurotoxicity in the form of subacute ataxia and encephalopathy in patients treated with EFV for a median of 2 years, in association with toxic plasma levels of the drug."( A proposed management algorithm for late-onset efavirenz neurotoxicity.
Asukile, MT; Chetty, S; Cross, HM; Hussey, HS; Lee Pan, EB; Tucker, LM, 2018
)
0.48
"We characterized associations between central nervous system (CNS) adverse events and brain neurotransmitter transporter/receptor genomics among participants randomized to efavirenz-containing regimens in AIDS Clinical Trials Group studies in the USA."( Brain neurotransmitter transporter/receptor genomics and efavirenz central nervous system adverse events.
Acosta, EP; Bradford, Y; Daar, ES; Eron, JJ; Gulick, RM; Haas, DW; Morse, GD; Riddler, SA; Ritchie, MD; Sax, PE; Verma, A; Verma, SS, 2018
)
0.48
"Analyses included 167 cases with grade 2 or greater efavirenz-consistent CNS adverse events within 48 weeks of study entry, and 653 efavirenz-tolerant controls."( Brain neurotransmitter transporter/receptor genomics and efavirenz central nervous system adverse events.
Acosta, EP; Bradford, Y; Daar, ES; Eron, JJ; Gulick, RM; Haas, DW; Morse, GD; Riddler, SA; Ritchie, MD; Sax, PE; Verma, A; Verma, SS, 2018
)
0.48
"Efavirenz-related CNS adverse events were not associated with predicted neurotransmitter transporter/receptor gene expression levels in brain or with polymorphisms in these genes."( Brain neurotransmitter transporter/receptor genomics and efavirenz central nervous system adverse events.
Acosta, EP; Bradford, Y; Daar, ES; Eron, JJ; Gulick, RM; Haas, DW; Morse, GD; Riddler, SA; Ritchie, MD; Sax, PE; Verma, A; Verma, SS, 2018
)
0.48
" In a Brazilian cohort, we sought to characterize associations between efavirenz adverse effects (all-cause and CNS) and polymorphisms in seven genes known or suspected to affect efavirenz metabolism and transport."( Drug metabolism and transport gene polymorphisms and efavirenz adverse effects in Brazilian HIV-positive individuals.
Baker, P; Cardoso, CC; da Silva, GAR; de Almeida, TB; de Azevedo, MCVM; de Castro, IJ; Ferry, FRA; Haas, DW; Pinto, JFDC; Tanuri, A, 2018
)
0.48
" Eighty-nine cases had efavirenz adverse effects, including 43 with CNS adverse effects, while 136 controls had no adverse effect of any antiretroviral after treatment for at least 6 months."( Drug metabolism and transport gene polymorphisms and efavirenz adverse effects in Brazilian HIV-positive individuals.
Baker, P; Cardoso, CC; da Silva, GAR; de Almeida, TB; de Azevedo, MCVM; de Castro, IJ; Ferry, FRA; Haas, DW; Pinto, JFDC; Tanuri, A, 2018
)
0.48
" Increased all-cause adverse effects were associated with the CYP2B6 genotype combination 15582CC-516TT-983TT (OR = 7."( Drug metabolism and transport gene polymorphisms and efavirenz adverse effects in Brazilian HIV-positive individuals.
Baker, P; Cardoso, CC; da Silva, GAR; de Almeida, TB; de Azevedo, MCVM; de Castro, IJ; Ferry, FRA; Haas, DW; Pinto, JFDC; Tanuri, A, 2018
)
0.48
"In a highly admixed Brazilian cohort, the CYP2B6 slow metabolizer genotype was associated with an increased risk of efavirenz adverse effects."( Drug metabolism and transport gene polymorphisms and efavirenz adverse effects in Brazilian HIV-positive individuals.
Baker, P; Cardoso, CC; da Silva, GAR; de Almeida, TB; de Azevedo, MCVM; de Castro, IJ; Ferry, FRA; Haas, DW; Pinto, JFDC; Tanuri, A, 2018
)
0.48
" The primary outcomes were the combined endpoints of any adverse outcome (stillbirth, preterm birth [<37 weeks' gestation], small for gestational age [SGA; less than the tenth percentile of birthweight by gestational age], or neonatal death [within 28 days of age]) and severe adverse outcomes (stillbirth, neonatal death, very preterm birth [<32 weeks' gestation], and very SGA [less than the third percentile of birthweight by gestational age])."( Comparative safety of dolutegravir-based or efavirenz-based antiretroviral treatment started during pregnancy in Botswana: an observational study.
Diseko, M; Essex, M; Gaolethe, T; Holmes, LB; Jacobson, DL; Lockman, S; Makhema, J; Mayondi, G; Mmalane, M; Petlo, C; Shapiro, RL; Zash, R, 2018
)
0.48
" The risk for any adverse birth outcome among women on dolutegravir versus efavirenz was similar (33·2% vs 35·0%; aRR 0·95, 95% CI 0·88-1·03), as was the risk of any severe birth outcome (10·7% vs 11·3%; 0·94, 0·81-1·11)."( Comparative safety of dolutegravir-based or efavirenz-based antiretroviral treatment started during pregnancy in Botswana: an observational study.
Diseko, M; Essex, M; Gaolethe, T; Holmes, LB; Jacobson, DL; Lockman, S; Makhema, J; Mayondi, G; Mmalane, M; Petlo, C; Shapiro, RL; Zash, R, 2018
)
0.48
"Our findings suggest that ART drugs are not associated with an increased risk of CMs, yet some may increase adverse birth events."( Comparative safety and effectiveness of perinatal antiretroviral therapies for HIV-infected women and their children: Systematic review and network meta-analysis including different study designs.
Antony, J; Ashoor, HM; Blondal, E; Finkelstein, Y; Ghassemi, M; Gough, K; Hemmelgarn, BR; Hutton, B; Ivory, JD; Khan, PA; Lillie, E; Straus, SE; Tricco, AC; Vafaei, A; Veroniki, AA, 2018
)
0.48
" EFV, relative to GSK3532795, had more serious adverse events (9% versus 5%) and adverse events leading to discontinuation (17% versus 5%)."( Safety, efficacy, and dose response of the maturation inhibitor GSK3532795 (formerly known as BMS-955176) plus tenofovir/emtricitabine once daily in treatment-naive HIV-1-infected adults: Week 24 primary analysis from a randomized Phase IIb trial.
Bogner, JR; DeGrosky, M; Dicker, IB; Gartland, M; Joshi, SR; Lataillade, M; Llamoso, C; Lombaard, J; Min, S; Molina, JM; Morales-Ramirez, J; Pene Dumitrescu, T; Stock, DA, 2018
)
0.48
" Ten CNS toxicities were graded according to the ACTG adverse events scale."( Tryptophan metabolism and its relationship with central nervous system toxicity in people living with HIV switching from efavirenz to dolutegravir.
Boasso, A; Fuchs, D; Higgs, C; Keegan, MR; Nelson, M; Winston, A, 2019
)
0.51
"In this small group of patients, the generic scheme 3TC/TDF/EFV is effective and safe in the treatment of patients with HIV/AIDS naïve, and its effectiveness and safety profile is similar to show by innovator scheme 3TC/TDF/EFV in patients with similar clinical conditions."( [Effectiveness and safety of generic version of lamivudine/tenofovir and efavirenz in treatment naïve HIV-infected patients: a nonrandomized, open-label, phase IV study in Cali-Colombia, 2012-2014].
Amariles, P; Castañeda, C; Galindo, J; Mueses-Marín, HF, 2019
)
0.51
" Day-42 adequate clinical and parasitological response (ACPR) and incidence of adverse events was assessed in HIV-infected individuals on efavirenz-based ART with uncomplicated falciparum malaria treated with AL."( Efficacy and safety of artemether-lumefantrine as treatment for Plasmodium falciparum uncomplicated malaria in adult patients on efavirenz-based antiretroviral therapy in Zambia: an open label non-randomized interventional trial.
Banda, CG; Chaponda, M; Hachizovu, S; Kabuya, JB; Kalilani-Phiri, L; Khoo, SH; Lalloo, DG; Mukaka, M; Mulenga, J; Mulenga, M; Mwapasa, V; Sikalima, J; Terlouw, DJ, 2019
)
0.51
" There were only two cases of grade 3 neutropaenia and one serious adverse event of lobar pneumonia, none of which was judged as probably related to intake of AL."( Efficacy and safety of artemether-lumefantrine as treatment for Plasmodium falciparum uncomplicated malaria in adult patients on efavirenz-based antiretroviral therapy in Zambia: an open label non-randomized interventional trial.
Banda, CG; Chaponda, M; Hachizovu, S; Kabuya, JB; Kalilani-Phiri, L; Khoo, SH; Lalloo, DG; Mukaka, M; Mulenga, J; Mulenga, M; Mwapasa, V; Sikalima, J; Terlouw, DJ, 2019
)
0.51
" Primary outcomes were the proportion of participants with HIV-1 RNA <40 copies/ml at week 24, and central nervous system (CNS) adverse events (AEs) by weeks 8 and 24 (Parts I+II combined)."( Doravirine dose selection and 96-week safety and efficacy versus efavirenz in antiretroviral therapy-naive adults with HIV-1 infection in a Phase IIb trial.
Arastéh, K; Dretler, R; Frobose, C; Gatell, JM; Hagins, DP; Harvey, C; Hoffmann, C; Hwang, C; Kumar, S; Morales-Ramirez, JO; Osiyemi, O; Plettenberg, A; Portilla, J; Raffi, F; Rodgers, A; Rugina, S; Smith, DE; Teppler, H; Thompson, M; Wan, H; Xu, X, 2019
)
0.51
" Proportions of women engaged in care, incidence of DAIDS grade ≥ 2 laboratory toxicity, grade ≥ 3 adverse events (AEs), viral suppression (<1000 copies/mL), birth outcomes and infant HIV infections are reported."( Safety and efficacy of Option B+ ART in Malawi: few severe maternal toxicity events or infant HIV infections among pregnant women initiating tenofovir/lamivudine/efavirenz.
Chagomerana, MB; DiPrete, BL; Harrington, BJ; Hosseinipour, MC; Jumbe, AN; Limarzi, L; Ngongondo, M; Wallie, SD, 2019
)
0.51
" While some women experienced adverse laboratory events, clinical symptom monitoring is likely reasonable."( Safety and efficacy of Option B+ ART in Malawi: few severe maternal toxicity events or infant HIV infections among pregnant women initiating tenofovir/lamivudine/efavirenz.
Chagomerana, MB; DiPrete, BL; Harrington, BJ; Hosseinipour, MC; Jumbe, AN; Limarzi, L; Ngongondo, M; Wallie, SD, 2019
)
0.51
" They received a directly-observed 3-day standard treatment of DPQ and were followed up until day 63 for malaria infection and adverse events."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of Plasmodium falciparum uncomplicated malaria in adult patients on antiretroviral therapy in Malawi and Mozambique: an open label non-randomized interventional trial.
Banda, CG; Kalilani-Phiri, L; Khoo, SH; Lalloo, DG; Macuacua, S; Maculuve, S; Mallewa, J; Mukaka, M; Mwapasa, V; Piqueras, M; Sevene, E; Terlouw, DJ; Vala, A, 2019
)
0.51
"DPQ was highly efficacious and safe for the treatment of malaria in HIV-infected patients concurrently taking efavirenz- or nevirapine-based ART, despite known pharmacokinetic interactions between dihydroartemisinin-piperaquine and efavirenz- or nevirapine-based ART regimens."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of Plasmodium falciparum uncomplicated malaria in adult patients on antiretroviral therapy in Malawi and Mozambique: an open label non-randomized interventional trial.
Banda, CG; Kalilani-Phiri, L; Khoo, SH; Lalloo, DG; Macuacua, S; Maculuve, S; Mallewa, J; Mukaka, M; Mwapasa, V; Piqueras, M; Sevene, E; Terlouw, DJ; Vala, A, 2019
)
0.51
" Both regimens were well-tolerated with no significant differences in frequency of adverse events (two on DTG-ART, one on EFV-ART, all considered unrelated to drug)."( Safety and pharmacokinetics of dolutegravir in pregnant mothers with HIV infection and their neonates: A randomised trial (DolPHIN-1 study).
Amara, A; Byakika-Kibwika, P; Byamugisha, J; Coombs, JA; Else, L; Gini, J; Heiburg, C; Hill, A; Hodel, EM; Kaboggoza, J; Khoo, S; Kintu, K; Lamorde, M; Malaba, T; Mehta, U; Myer, L; Orrell, C; Reynolds, H; Sihlangu, M; Simmons, B; Singh, Y; Waitt, C; Walimbwa, S, 2019
)
0.51
" However, there are several reasons as to why patients may discontinue their antiretroviral therapy, with adverse events being one of the main reasons reported in the literature."( Factors associated to modification of first-line antiretroviral therapy due to adverse events in people living with HIV/AIDS.
Azevedo, LN; Miranda-Filho, DB; Montarroyos, UR; Monteiro, P; Ximenes, RAA,
)
0.13
" Nonetheless, neuropsychiatric adverse events (AE) occur in almost half of the EFV users and it is the main reason for treatment discontinuation."( Predictors of Discontinuation of Efavirenz as Treatment for HIV, Due to Neuropsychiatric Side Effects, in a Multi-Ethnic Sample in the United Kingdom.
Butler, LT; Hamill, MM; Law, JKC, 2020
)
0.56
" Drug-related adverse events occurred more frequently in the participants receiving the standard dose regimen compared with the lower dose one (63."( Efficacy and safety of lower dose tenofovir disoproxil fumarate and efavirenz versus standard dose in HIV-infected, antiretroviral-naive adults: a multicentre, randomized, noninferiority trial.
Chen, J; Chen, R; Hu, Z; Huang, Q; Liu, L; Lu, H; Qi, T; Shen, Y; Song, W; Sun, J; Tang, Y; Wang, J; Wang, X; Wang, Z; Wei, H; Xie, R; Zhang, R, 2020
)
0.56
" Early identification of this uncommon side effect in select patients can prevent irreversible vision loss due to efavirenz-associated retinal toxicity."( Efavirenz-Associated Retinal Toxicity Presenting with Night Vision Defects in Patients with Human Immunodeficiency Virus.
Bhende, M; Biswas, J; Kumar, KD; Selvamuthu, P; Sudharshan, S, 2020
)
0.56
" There were no clinically relevant toxicities nor adverse events in both control and test arms."( Effect of nevirapine, efavirenz and lopinavir/ritonavir on the therapeutic concentration and toxicity of lumefantrine in people living with HIV at Lagos University Teaching Hospital, Nigeria.
Abideen, G; Adeniji, H; Adeuja, O; Agbaje, EO; Akanmu, AS; Akinleye, MO; Akinyede, AA; Busari, AW; Hassan, OO; Ken-Owotor, C; Kogbe, S; Ogunfowokan, T; Onwujuobi, AG; Oreagba, IA; Owolabi, ET; Usman, SO, 2020
)
0.56
" Grade 3/4 adverse events (especially efavirenz-related neuropsychiatric adverse events) leading to regimen discontinuation were also noted."( Efficacy and safety of a single-tablet regimen containing tenofovir disoproxil fumarate 300 mg, lamivudine 300 mg and efavirenz 400 mg as a switch strategy in virologically suppressed HIV-1-infected subjects on nonnucleoside reverse transcriptase inhibito
Betha, TP; Dravid, A; Dravid, M; Gawali, R; Kore, S; Kulkarni, M; Mahajan, U; Rathod, N; Saraf, C; Sharma, AK, 2020
)
0.56
" Grade 3/4 adverse events leading to TLE400 STR discontinuation were seen in 11 (2."( Efficacy and safety of a single-tablet regimen containing tenofovir disoproxil fumarate 300 mg, lamivudine 300 mg and efavirenz 400 mg as a switch strategy in virologically suppressed HIV-1-infected subjects on nonnucleoside reverse transcriptase inhibito
Betha, TP; Dravid, A; Dravid, M; Gawali, R; Kore, S; Kulkarni, M; Mahajan, U; Rathod, N; Saraf, C; Sharma, AK, 2020
)
0.56
"Despite the high efficacy of antiretroviral treatment, no drug is free from adverse events (AEs)."( Discontinuation due to neuropsychiatric adverse events with efavirenz- and dolutegravir-based antiretroviral therapy: a comparative real-life study.
Balboa-Barreiro, V; Castro-Iglesias, Á; Cid-Silva, P; Fernández-Bargiela, N; López-Calvo, S; Margusino-Framiñán, L; Martín-Herranz, I; Mena-De-Cea, Á; Míguez-Rey, E; Rotea-Salvo, S; Vázquez-Rodríguez, P, 2022
)
0.72
"The use of patient-reported outcomes (PROs) to systematically quantify adverse events (AE) will assist in the improvement of medical care and the QoL of patients living with HIV (PLWH)."( Longitudinal trends and determinants of patient-reported side effects on ART-a Swedish national registry study.
Eriksson, LE; Marrone, G; Mellgren, Å; Reinius, M; Svedhem, V, 2020
)
0.56
" Rilpivirine (RPV) is better tolerated, and switching from EFV to RPV in virologically suppressed adults has been safe and efficacious, but data in adolescents are limited."( Switching efavirenz to rilpivirine in virologically suppressed adolescents with HIV: a multi-centre 48-week efficacy and safety study in Thailand.
Anugulruengkitt, S; Chantaratin, S; Chokephaibulkit, K; Jantarabenjakul, W; Kosalaraksa, P; Maleesatharn, A; Phongsamart, W; Sirikutt, P; Suntarattiwong, P, 2022
)
0.72
" HIV RNA viral load, CD4 cell count, fasting total cholesterol (TC), triglyceride, glucose, neuropsychiatric adverse events, depression and QOL were assessed over 48 weeks."( Switching efavirenz to rilpivirine in virologically suppressed adolescents with HIV: a multi-centre 48-week efficacy and safety study in Thailand.
Anugulruengkitt, S; Chantaratin, S; Chokephaibulkit, K; Jantarabenjakul, W; Kosalaraksa, P; Maleesatharn, A; Phongsamart, W; Sirikutt, P; Suntarattiwong, P, 2022
)
0.72
" We also assessed antiretroviral therapy safety, analyzing treatment discontinuation for adverse events."( Brief Report: Efficacy and Safety of Efavirenz, Raltegravir, and Dolutegravir in HIV-1/TB Coinfection. A Multicenter Retrospective Cohort Study in France.
Brun, A; de Castro, N; Hamet, G; Joly, V; Kherabi, Y; Méchaï, F; Molina, JM; Sellier, PO; Yazdanpanah, Y, 2022
)
0.72
" Rate of treatment discontinuation for drug-related adverse events was 10."( Brief Report: Efficacy and Safety of Efavirenz, Raltegravir, and Dolutegravir in HIV-1/TB Coinfection. A Multicenter Retrospective Cohort Study in France.
Brun, A; de Castro, N; Hamet, G; Joly, V; Kherabi, Y; Méchaï, F; Molina, JM; Sellier, PO; Yazdanpanah, Y, 2022
)
0.72
" The safety data analysis of laboratory indicators showed that there was no significant difference in the incidence of adverse events between the 2 groups."( Effectiveness and Safety of Dolutegravir Versus Efavirenz-Based Antiviral Regimen in People Living With HIV-1 in Sichuan Province of China: A Real-World Study.
Chunrong, L; Huanxia, L; Ke, Y; Lin, C; Ruifeng, Z; Shenghua, H; Tongtong, Y; Xiaojing, Y; Yin, W; Yuan, Y; Yuanhong, H, 2022
)
0.72
" DTG + 3TC achieved virological suppression more rapidly and stably versus TDF + 3TC + EFV in ART-naïve HIV-1-infected adults, with better immunological response and less adverse drug effect, and reduced total HIV-1 DNA effectively."( Real-world efficacy and safety of dolutegravir plus lamivudine versus tenofovir plus lamivudine and efavirenz in ART-naïve HIV-1-infected adults.
Chen, D; Du, Y; Huang, Z; Li, J; Wang, Y; Wen, Z; Yin, S; Zhong, H, 2022
)
0.72
" The results of the cytotoxicity assay and drug uptake study showed that PPG4ER was safe and biocompatible up to 12."( Effect of PEGylation on drug uptake, biodistribution, and tissue toxicity of efavirenz-ritonavir loaded PAMAM G4 dendrimers.
Dhobley, A; Kharwade, R; Mahajan, N; Mendhi, S; More, S; Palve, D; Warokar, A, 2023
)
0.91
" Primary safety analyses were pairwise comparisons between ART regimens of the proportion of maternal and infant adverse events of grade 3 or higher up to 50 weeks post partum."( Efficacy and safety of three antiretroviral therapy regimens started in pregnancy up to 50 weeks post partum: a multicentre, open-label, randomised, controlled, phase 3 trial.
Amico, KR; Boyce, C; Brummel, S; Cassim, H; Chakhtoura, N; Chinula, L; Coletti, A; Currier, JS; Fairlie, L; Frenkel, LM; Hoffman, R; Jean-Philippe, P; Johnston, B; Knowles, K; Korutaro, V; Krotje, C; Lockman, S; Masheto, G; McCarthy, K; Mmbaga, BT; Moyo, S; Patel, F; Purdue, L; Rooney, JF; Sax, PE; Shapiro, R; Stranix-Chibanda, L; Stringer, J; van Wyk, J; Ziemba, L, 2023
)
0.91
" Up to the week 50 post-partum visit, the estimated probability of experiencing an adverse event of grade 3 or higher was 25% in the dolutegravir, emtricitabine, and tenofovir alafenamide group; 31% in the dolutegravir, emtricitabine, and tenofovir disoproxil fumarate group; and 28% in the efavirenz, emtricitabine, and tenofovir disoproxil fumarate group (no significant difference between groups)."( Efficacy and safety of three antiretroviral therapy regimens started in pregnancy up to 50 weeks post partum: a multicentre, open-label, randomised, controlled, phase 3 trial.
Amico, KR; Boyce, C; Brummel, S; Cassim, H; Chakhtoura, N; Chinula, L; Coletti, A; Currier, JS; Fairlie, L; Frenkel, LM; Hoffman, R; Jean-Philippe, P; Johnston, B; Knowles, K; Korutaro, V; Krotje, C; Lockman, S; Masheto, G; McCarthy, K; Mmbaga, BT; Moyo, S; Patel, F; Purdue, L; Rooney, JF; Sax, PE; Shapiro, R; Stranix-Chibanda, L; Stringer, J; van Wyk, J; Ziemba, L, 2023
)
0.91
" However, EFV also demonstrates several adverse effects, like hepatotoxicity, altered lipid profile, neuropsychological symptoms, and behavioral effects in children after in utero exposure."( Comparison of Efavirenz and Doravirine Developmental Toxicity in an Embryo Animal Model.
Castelli, F; Ferretti, S; Mignani, L; Monti, E; Quiros-Roldan, E; Tiecco, G; Zanella, I; Zizioli, D, 2023
)
0.91
" Safety endpoints assessed included all the adverse events (AEs) related to the study treatment (TLE400 and TLE600)."( Safety of low dose efavirenz regimen in Indian adults with HIV-1 infection: Insights from a phase 4 interventional randomised trial.
Anuradha, S; Bhrusundi, M; Dravid, AN; Kulkarni, V; Madhukarrao, KM; Morkar, DN; Nageswaramma, S; Naik, KS; Pilawan, AS; Ramapuram, JT; Raveendra, KR, 2023
)
0.91

Pharmacokinetics

A population-based pharmacokinetic (PK) model has been developed for efavirenz based on 16 phase I studies. The data support coadministration of daclatasvir with atazanavir/ritonavir, efvirenz and/or tenofovir.

ExcerptReferenceRelevance
" Higher doses in both species led to disproportionate increases in the AUC and higher Tmax values, suggesting saturation of metabolism and/or prolongation of absorption."( Nonlinear pharmacokinetics of efavirenz (DMP-266), a potent HIV-1 reverse transcriptase inhibitor, in rats and monkeys.
Balani, SK; deLuna, FA; Kauffman, LR; Lin, JH, 1999
)
0.3
"To define the pharmacokinetic profile of efavirenz (EFV) in HIV-1 infected patients, when administered alone or with nelfinavir (NFV)."( Pharmacokinetics of efavirenz (EFV) alone and in combination therapy with nelfinavir (NFV) in HIV-1 infected patients.
Castelli, F; Maserati, R; Regazzi, MB; Seminari, E; Torti, C; Viale, P; Villani, P, 1999
)
0.3
" Blood samples for pharmacokinetic analysis were obtained during a dosage interval."( Pharmacokinetics of efavirenz (EFV) alone and in combination therapy with nelfinavir (NFV) in HIV-1 infected patients.
Castelli, F; Maserati, R; Regazzi, MB; Seminari, E; Torti, C; Viale, P; Villani, P, 1999
)
0.3
"No significant difference was found between the principal pharmacokinetic parameters of EFV when administered alone or in combination with NFV (mean AUC: 57."( Pharmacokinetics of efavirenz (EFV) alone and in combination therapy with nelfinavir (NFV) in HIV-1 infected patients.
Castelli, F; Maserati, R; Regazzi, MB; Seminari, E; Torti, C; Viale, P; Villani, P, 1999
)
0.3
" In this study we analysed the pharmacokinetic profile of nelfinavir after multiple oral doses in 18 HIV-infected patients during a combination regimen of nelfinavir plus efavirenz and stavudine."( Clinical pharmacokinetics of nelfinavir combined with efavirenz and stavudine during rescue treatment of heavily pretreated HIV-infected patients.
Fiocchi, C; Gambarana, E; LoCaputo, F; Maserati, R; Pan, A; Regazzi, MB; Seminari, E; Villani, P, 2000
)
0.31
" The differences between the pharmacokinetic parameters of efavirenz with and without nevirapine were analyzed, and the pharmacokinetics of nevirapine were compared with those in historical control patients."( The steady-state pharmacokinetics of efavirenz and nevirapine when used in combination in human immunodeficiency virus type 1-infected persons.
Beijnen, JH; Carlier, H; Gazzard, B; Harris, M; Hoetelmans, RM; Johnson, M; Kwakkelstein, MO; Lange, JM; Montaner, JS; Moyle, G; Reiss, P; van Leeuwen, R; Veldkamp, AI; Youle, M, 2001
)
0.31
" Although possessing a common mechanism of action, these agents can be differentiated by both molecular and pharmacokinetic characteristics."( Clinical pharmacokinetics of non-nucleoside reverse transcriptase inhibitors.
DiCenzo, R; Morse, GD; Smith, PF, 2001
)
0.31
"To evaluate the pharmacokinetic interactions between efavirenz and rifampicin (rifampin) in patients with HIV infection and tuberculosis."( Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis.
Alarcón-González, A; Gómez-Mateos, J; León-Jimenez, E; López-Cortés, LF; López-Pua, Y; Pachón, J; Ruiz-Valderas, R; Sarasanacenta, M; Viciana, P, 2002
)
0.31
"Nonblind, randomised, pharmacokinetic study."( Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis.
Alarcón-González, A; Gómez-Mateos, J; León-Jimenez, E; López-Cortés, LF; López-Pua, Y; Pachón, J; Ruiz-Valderas, R; Sarasanacenta, M; Viciana, P, 2002
)
0.31
"Plasma concentrations of efavirenz and rifampicin were quantified by using validated high performance liquid chromatography assays, and pharmacokinetic parameter values were determined by noncompartmental methods."( Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis.
Alarcón-González, A; Gómez-Mateos, J; León-Jimenez, E; López-Cortés, LF; López-Pua, Y; Pachón, J; Ruiz-Valderas, R; Sarasanacenta, M; Viciana, P, 2002
)
0.31
"There was a correlation between the pharmacokinetic parameters of efavirenz and the dose/kg administered."( Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis.
Alarcón-González, A; Gómez-Mateos, J; León-Jimenez, E; López-Cortés, LF; López-Pua, Y; Pachón, J; Ruiz-Valderas, R; Sarasanacenta, M; Viciana, P, 2002
)
0.31
"The present population pharmacokinetic (PK) and pharmacodynamic (PD) study modeled the effects of covariates including drug adherence and the coadministration of protease inhibitors (PIs) on the pharmacokinetics of efavirenz (EFV) and the relationship between EFV exposure and virological failure in patients who failed initial PI treatment in Adult AIDS Clinical Trial Group (AACTG) study 398."( Population pharmacokinetics and pharmacodynamics of efavirenz, nelfinavir, and indinavir: Adult AIDS Clinical Trial Group Study 398.
Bennett, KK; Hammer, SM; Labbé, L; Mellors, J; Pfister, M; Rosenkranz, S; Sheiner, LB, 2003
)
0.32
" This study aimed to assess the efavirenz pharmacokinetic profile and interpatient versus intrapatient variability in patients who are positive for human immunodeficiency virus, to explore the relationship between drug exposure, efficacy, and central nervous system toxicity and to build up a Bayesian approach for dosage adaptation."( Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection.
Biollaz, J; Buclin, T; Csajka, C; Décosterd, LA; Fattinger, K; Fellay, J; Marzolini, C; Telenti, A, 2003
)
0.32
"The population pharmacokinetic analysis was performed by use of NONMEM based on plasma samples from a cohort of unselected patients receiving efavirenz."( Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection.
Biollaz, J; Buclin, T; Csajka, C; Décosterd, LA; Fattinger, K; Fellay, J; Marzolini, C; Telenti, A, 2003
)
0.32
"A population-based pharmacokinetic (PK) model has been developed for efavirenz based on 16 phase I studies."( Population pharmacokinetic meta-analysis with efavirenz.
Barrett, JS; Chai, M; Fiske, WD; Joshi, AS; Ludden, TM; Pieniaszek, HJ, 2002
)
0.31
"At week 4 of the study, 12-hour pharmacokinetic profiles for indinavir/ritonavir were obtained for 20 HIV-infected subjects."( Pharmacokinetics of indinavir/ritonavir (800/100 mg) in combination with efavirenz (600 mg) in HIV-1-infected subjects.
Aarnoutse, RE; Boyd, MA; Burger, DM; Cooper, DA; Lange, JM; Phanuphak, P; Ruxrungtham, K; Stek, M; van Heeswijk, RP, 2003
)
0.32
" A >10-fold variation in indinavir Cmin was observed."( Pharmacokinetics of indinavir/ritonavir (800/100 mg) in combination with efavirenz (600 mg) in HIV-1-infected subjects.
Aarnoutse, RE; Boyd, MA; Burger, DM; Cooper, DA; Lange, JM; Phanuphak, P; Ruxrungtham, K; Stek, M; van Heeswijk, RP, 2003
)
0.32
"Despite the known pharmacokinetic interaction between efavirenz and indinavir/ritonavir, the combination of indinavir/ritonavir at 800/100 mg bid and efavirenz at 600 mg qd results in adequate minimum concentrations of both indinavir and efavirenz for treatment-naive patients."( Pharmacokinetics of indinavir/ritonavir (800/100 mg) in combination with efavirenz (600 mg) in HIV-1-infected subjects.
Aarnoutse, RE; Boyd, MA; Burger, DM; Cooper, DA; Lange, JM; Phanuphak, P; Ruxrungtham, K; Stek, M; van Heeswijk, RP, 2003
)
0.32
" The following pharmacokinetic (PK) parameters were determined over 24 h at steady-state after 4 weeks of treatment: area under the plasma concentration vs."( Pharmacokinetics of emtricitabine, didanosine and efavirenz administered once-daily for the treatment of HIV-infected adults (pharmacokinetic substudy of the ANRS 091 trial).
Chene, G; Lascoux-Combes, C; Molina, JM; Perusat, S; Peytavin, G; Rozenbaum, W; Sereni, D, 2004
)
0.32
" EFV Cmax and Cmin were lower than expected, but the data may have been slightly underestimated in this study."( Pharmacokinetics of emtricitabine, didanosine and efavirenz administered once-daily for the treatment of HIV-infected adults (pharmacokinetic substudy of the ANRS 091 trial).
Chene, G; Lascoux-Combes, C; Molina, JM; Perusat, S; Peytavin, G; Rozenbaum, W; Sereni, D, 2004
)
0.32
"To evaluate the safety and pharmacokinetic interaction between GW433908, ritonavir (RTV), and efavirenz (EFV)."( Pharmacokinetics and safety of GW433908 and ritonavir, with and without efavirenz, in healthy volunteers.
Ballow, C; Hendrix, CW; Lou, Y; Piliero, PJ; Preston, SL; Stein, DS; Wire, MB, 2004
)
0.32
" Amprenavir (APV) pharmacokinetic sampling and safety assessments were performed on the last day of each period."( Pharmacokinetics and safety of GW433908 and ritonavir, with and without efavirenz, in healthy volunteers.
Ballow, C; Hendrix, CW; Lou, Y; Piliero, PJ; Preston, SL; Stein, DS; Wire, MB, 2004
)
0.32
" The main pharmacokinetic parameters were calculated using noncompartmental methods."( Effect of efavirenz treatment on the pharmacokinetics of nelfinavir boosted by ritonavir in healthy volunteers.
Burger, DM; Colbers, EP; de Graaff-Teulen, MJ; Hekster, YA; Ibanez, SM; Koopmans, PP; la Porte, CJ; Voncken, DS, 2004
)
0.32
"The aim of this 2NN pharmacokinetic substudy was to investigate the population pharmacokinetics of nevirapine and efavirenz."( Nevirapine and efavirenz pharmacokinetics and covariate analysis in the 2NN study.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, J; MacGregor, TR; van Leth, F, 2005
)
0.33
"The aim of this study was to characterise the pharmacokinetic and pharmacodynamic monitoring of low doses of mycophenolate mofetil (0."( Pharmacokinetics and pharmacodynamics of low dose mycophenolate mofetil in HIV-infected patients treated with abacavir, efavirenz and nelfinavir.
Brunet, M; Gallart, T; García, F; Gatell, JM; Martorell, J; Millán, O; Miró, JM; Plana, M; Pumarola, T; Rojo, I; Vidal, E, 2005
)
0.33
"Mycophenolate mofetil pharmacokinetic profiles in HIV patients under HAART are not significantly different from those found in transplant patients."( Pharmacokinetics and pharmacodynamics of low dose mycophenolate mofetil in HIV-infected patients treated with abacavir, efavirenz and nelfinavir.
Brunet, M; Gallart, T; García, F; Gatell, JM; Martorell, J; Millán, O; Miró, JM; Plana, M; Pumarola, T; Rojo, I; Vidal, E, 2005
)
0.33
" Pharmacokinetic parameters were dose proportional, and the maximum concentration of drug in serum at all doses exceeded the 90% effective concentration for wild-type HIV-1."( Safety, pharmacokinetics, and efficacy of (+/-)-beta-2',3'-dideoxy-5-fluoro-3'-thiacytidine with efavirenz and stavudine in antiretroviral-naïve human immunodeficiency virus-infected patients.
Arastèh, K; Beard, A; Cartee, L; Drauz, D; Herzmann, C; Kreckel, P; Murphy, RL; Otto, MJ; Schinazi, RF; Schulbin, H, 2005
)
0.33
" The influence of patient characteristics on the pharmacokinetic parameters of efavirenz was explored."( Population pharmacokinetics of efavirenz in an unselected cohort of HIV-1-infected individuals.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Meenhorst, PL; Mulder, JW; Prins, JM; Yalvaç, Z, 2005
)
0.33
"From 172 patients, 40 full pharmacokinetic curves and 315 efavirenz plasma concentrations at a single timepoint were available, resulting in a database of 1009 efavirenz plasma concentrations."( Population pharmacokinetics of efavirenz in an unselected cohort of HIV-1-infected individuals.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Meenhorst, PL; Mulder, JW; Prins, JM; Yalvaç, Z, 2005
)
0.33
"The pharmacokinetic parameters of efavirenz were adequately described with the developed population pharmacokinetic model."( Population pharmacokinetics of efavirenz in an unselected cohort of HIV-1-infected individuals.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Meenhorst, PL; Mulder, JW; Prins, JM; Yalvaç, Z, 2005
)
0.33
"Adult AIDS Clinical Trials Group 5043 examined pharmacokinetic (PK) interactions between amprenavir (APV) and efavirenz (EFV) both by themselves and when nelfinavir (NFV), indinavir (IDV), ritonavir (RTV), or saquinavir (SQV) is added."( Amprenavir and efavirenz pharmacokinetics before and after the addition of nelfinavir, indinavir, ritonavir, or saquinavir in seronegative individuals.
Adams, E; Brizz, B; Difrancesco, R; Morse, GD; Para, MF; Reichman, RC; Rosenkranz, S; Segal, Y; Yarasheski, KE, 2005
)
0.33
" Reductions of 25% and 45% were observed in the mean nelfinavir area under the concentration-time curve and minimum concentration of the drug in serum, and there was a 31% more rapid half-life for patients receiving both drugs compared to patients receiving nelfinavir alone."( Pharmacokinetics of nelfinavir and efavirenz in antiretroviral-naive, human immunodeficiency virus-infected subjects when administered alone or in combination with nucleoside analog reverse transcriptase inhibitors.
Fischl, MA; Forrest, A; Hirsch, MS; Merigan, TC; Morse, GD; Park, JG; Robbins, GK; Shafer, RW; Smith, PF; Wu, H; Yu, S, 2005
)
0.33
" The objective was to find cutoff values of the Cmin and AUC24 below which the risk of virologic failure increased."( Pharmacokinetic parameters of nevirapine and efavirenz in relation to antiretroviral efficacy.
Beijnen, JH; Boron-Kaczmarska, A; Hall, DB; Huitema, AD; Johnson, D; Kappelhoff, BS; Lange, JM; Leith, J; Leth, FV; Livrozet, JM; Losso, MH; Saag, MS; Wit, FW, 2006
)
0.33
"A population pharmacokinetic analysis was performed in the context of therapeutic drug monitoring (87 patients, 121 samples)."( Influence of tenofovir, nevirapine and efavirenz on ritonavir-boosted atazanavir pharmacokinetics in HIV-infected patients.
Arvieux, C; Dailly, E; Jolliet, P; Perré, P; Raffi, F; Tattevin, P; Tribut, O, 2006
)
0.33
" The pharmacokinetic profile of saquinavir-SGC was analyzed in a subset of randomly selected patients."( Efficacy, safety and pharmacokinetics of once-daily saquinavir soft-gelatin capsule/ritonavir in antiretroviral-naive, HIV-infected patients.
Burnside, AF; Jayaweera, DT; Montaner, JS; Saag, MS; Schutz, M; Schwartz, R; Walmsley, S, 2006
)
0.33
" Pharmacokinetic profiles in 6 patients showed an observed median Cmin at 24 hours of 429 ng/mL (range, 68-1750 ng/mL)."( Efficacy, safety and pharmacokinetics of once-daily saquinavir soft-gelatin capsule/ritonavir in antiretroviral-naive, HIV-infected patients.
Burnside, AF; Jayaweera, DT; Montaner, JS; Saag, MS; Schutz, M; Schwartz, R; Walmsley, S, 2006
)
0.33
" Both drugs have demonstrated interindividual pharmacokinetic variability."( Efavirenz and nevirapine in HIV-1 infection : is there a role for clinical pharmacokinetic monitoring?
Dahri, K; Ensom, MH, 2007
)
0.34
"Twelve HIV-infected patients were assigned into a one-sequence, two-period pharmacokinetic interaction study."( Effect of efavirenz on the pharmacokinetics of ketoconazole in HIV-infected patients.
Jaruratanasirikul, S; Mahatthanatrakul, W; Ridtitid, W; Sriwiriyajan, S, 2007
)
0.34
" We evaluated the possibility of a pharmacokinetic interaction between TFV and EFV by assessing cross-sectional and longitudinal data in 169 individuals receiving EFV."( Does tenofovir influence efavirenz pharmacokinetics?
Buclin, T; Colombo, S; Décosterd, L; Furrer, H; Rotger, M; Telenti, A, 2007
)
0.34
"Although there is no clear evidence for a pharmacokinetic interaction between TFV and EFV, we cannot rule out an interaction between these drugs restricted to individuals who are slow EFV metabolizers."( Does tenofovir influence efavirenz pharmacokinetics?
Buclin, T; Colombo, S; Décosterd, L; Furrer, H; Rotger, M; Telenti, A, 2007
)
0.34
" EFV levels in plasma were assayed by high-performance liquid chromatography (HLPC) predose (C(trough)) and at 1, 2, 3, 4, 5, 6, 8, 10, 11, 12, 13, 14, 16, 18, 22 and 24 hours post-dose, and pharmacokinetic parameters were determined by non-compartmental methods."( Multiple-dose pharmacokinetics of efavirenz with and without the use of rifampicin in HIV-positive patients.
Caligaris, S; Capone, S; Carosi, G; Carvalho, AC; Cusato, M; De Iaco, G; Manfrin, M; Matteelli, A; Regazzi, M; Tomasoni, L; Villani, P, 2007
)
0.34
" Pharmacokinetic evaluations were performed at weeks 2, 6, and 56."( Pharmacokinetics and pharmacodynamics of efavirenz and nelfinavir in HIV-infected children participating in an area-under-the-curve controlled trial.
Alvero, CG; Brundage, RC; Fenton, T; Fletcher, CV; Mofenson, LM; Powell, C; Spector, SA, 2008
)
0.35
"This open-label, crossover study investigated the pharmacokinetic interaction between TMC114 (darunavir [Prezista]), administered with low-dose ritonavir (TMC114/r) and efavirenz (EFV) in HIV-negative, healthy volunteers."( Pharmacokinetic interaction between TMC114/r and efavirenz in healthy volunteers.
De Pauw, M; Hoetelmans, RM; Lefebvre, E; Mariën, K; Peeters, M; Sekar, VJ, 2007
)
0.34
" TMC114/r and EFV coadministration resulted in TMC114 Cmin, Cmax and AUC12h decreases of 31%, 15% and 13%, respectively."( Pharmacokinetic interaction between TMC114/r and efavirenz in healthy volunteers.
De Pauw, M; Hoetelmans, RM; Lefebvre, E; Mariën, K; Peeters, M; Sekar, VJ, 2007
)
0.34
"The clinical significance of the changes in AUC and Cmin seen with TMC114/r and EFV coadministration has not been established; this combination should be used with caution."( Pharmacokinetic interaction between TMC114/r and efavirenz in healthy volunteers.
De Pauw, M; Hoetelmans, RM; Lefebvre, E; Mariën, K; Peeters, M; Sekar, VJ, 2007
)
0.34
"Fourteen patients participated in the study and seven participated in the intensified pharmacokinetic protocol."( Effect of highly active antiretroviral therapy on tacrolimus pharmacokinetics in hepatitis C virus and HIV co-infected liver transplant recipients in the ANRS HC-08 study.
Abbara, C; Barrail, A; Boissonnas, A; Bonhomme-Faivre, L; Duclos-Vallée, JC; Samuel, D; Taburet, AM; Teicher, E; Vincent, I; Vittecoq, D, 2007
)
0.34
" Coadministration of these drugs might result in complex pharmacokinetic drug-drug interactions."( Amprenavir and lopinavir pharmacokinetics following coadministration of amprenavir or fosamprenavir with lopinavir/ritonavir, with or without efavirenz.
Barditch-Crovo, P; Carson, KA; Flexner, C; Hendrix, CW; Khan, W; Pakes, GE; Parish, M; Parsons, T; Pham, PA; Qaqish, R; Radebaugh, C, 2007
)
0.34
"37) or Cmax (10."( Amprenavir and lopinavir pharmacokinetics following coadministration of amprenavir or fosamprenavir with lopinavir/ritonavir, with or without efavirenz.
Barditch-Crovo, P; Carson, KA; Flexner, C; Hendrix, CW; Khan, W; Pakes, GE; Parish, M; Parsons, T; Pham, PA; Qaqish, R; Radebaugh, C, 2007
)
0.34
"EFV did not appear to significantly alter APV and LPV pharmacokinetic parameters in HIV-infected patients taking APV 750 mg twice daily + LPV 533/133 mg twice daily."( Amprenavir and lopinavir pharmacokinetics following coadministration of amprenavir or fosamprenavir with lopinavir/ritonavir, with or without efavirenz.
Barditch-Crovo, P; Carson, KA; Flexner, C; Hendrix, CW; Khan, W; Pakes, GE; Parish, M; Parsons, T; Pham, PA; Qaqish, R; Radebaugh, C, 2007
)
0.34
" The 400-mg qd efavirenz dose substantially reduced the steady-state mean voriconazole area under the curve over the dosing interval (AUC0-12) by 80% (90% confidence interval [CI], 75%-84%) and peak concentration (Cmax) by 66% (90% CI, 57%-73%)."( Pharmacokinetic interaction between voriconazole and efavirenz at steady state in healthy male subjects.
Foster, G; Gutierrez, MJ; LaBadie, RR; Liu, P; Sharma, A, 2008
)
0.35
" The objective of the present study was to evaluate the potential pharmacokinetic interaction between efavirenz and dual PIs."( Pharmacokinetic interaction between efavirenz and dual protease inhibitors in healthy volunteers.
Forrest, A; Ma, Q; Morse, GD; Para, MF; Reichman, RC; Rosenkranz, SL; Yarasheski, KE, 2008
)
0.35
"The study sought to investigate the relationship between efavirenz exposure and the CYP2B6 516G-->T(*6) genotype in HIV/AIDS outpatients, using pharmacokinetic modelling and simulation."( High prevalence of the CYP2B6 516G-->T(*6) variant and effect on the population pharmacokinetics of efavirenz in HIV/AIDS outpatients in Zimbabwe.
Ashton, M; Chigutsa, E; Chonzi, P; Masimirembwa, C; Nhachi, C; Nyakutira, C; Röshammar, D, 2008
)
0.35
" Population pharmacokinetic modelling and simulation of the data were performed in NONMEM VI."( High prevalence of the CYP2B6 516G-->T(*6) variant and effect on the population pharmacokinetics of efavirenz in HIV/AIDS outpatients in Zimbabwe.
Ashton, M; Chigutsa, E; Chonzi, P; Masimirembwa, C; Nhachi, C; Nyakutira, C; Röshammar, D, 2008
)
0.35
" Pharmacokinetic parameter estimates indicate that a dose reduction to 400 mg efavirenz per day is possible in patients homozygous for the CYP2B6*6 genotype without compromising therapeutic efficacy."( High prevalence of the CYP2B6 516G-->T(*6) variant and effect on the population pharmacokinetics of efavirenz in HIV/AIDS outpatients in Zimbabwe.
Ashton, M; Chigutsa, E; Chonzi, P; Masimirembwa, C; Nhachi, C; Nyakutira, C; Röshammar, D, 2008
)
0.35
"The influence of nevirapine or efavirenz co-administration on ritonavir-boosted amprenavir pharmacokinetics was investigated in HIV-infected patients with a population pharmacokinetic approach."( Impact of nevirapine or efavirenz co-administration on ritonavir-boosted amprenavir pharmacokinetics in HIV-infected patients.
Allavena, C; Biron, C; Dailly, E; Jolliet, P; Raffi, F, 2008
)
0.35
" In summary, a 2-way pharmacokinetic interaction between efavirenz and carbamazepine was demonstrated in this study."( Pharmacokinetic interaction between efavirenz and carbamazepine after multiple-dose administration in healthy subjects.
Damle, B; Grasela, DM; Ji, P; Kaul, S; Unger, SE; Xie, J, 2008
)
0.35
" LPV Cmin was lower than expected in the hemodialysis group."( The pharmacokinetics and pharmacogenomics of efavirenz and lopinavir/ritonavir in HIV-infected persons requiring hemodialysis.
Amorosa, V; Cramer, YS; Gupta, SK; Hall, SD; Koletar, SL; Rosenkranz, SL; Szczech, LA, 2008
)
0.35
" A non-linear mixed effect pharmacokinetic model was developed."( A pharmacokinetic and pharmacogenetic study of efavirenz in children: dosing guidelines can result in subtherapeutic concentrations.
Beijnen, JH; Bekker, V; Crommentuyn, KM; Huitema, AD; Kuijpers, TW; Scherpbier, HJ; ter Heine, R, 2008
)
0.35
" A complete pharmacokinetic study was conducted with 19 HIV-TB patients on two occasions (with and without RMP)."( CYP2B6 G516T polymorphism but not rifampin coadministration influences steady-state pharmacokinetics of efavirenz in human immunodeficiency virus-infected patients in South India.
Anitha, S; Gomathi, C; Hemanth Kumar, AK; Kumar, P; Menon, P; Narendran, G; Rajasekaran, S; Ramachandran, G; Ramesh, K; Swaminathan, S, 2009
)
0.35
" Efavirenz Cmin was not significantly different during vs."( Effect of rifampicin on efavirenz pharmacokinetics in HIV-infected children with tuberculosis.
Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2009
)
0.35
" The substantial proportion of participants with estimated Cmin <1 mg/L could result in the rapid emergence of efavirenz-resistant mutations and treatment failure."( Effect of rifampicin on efavirenz pharmacokinetics in HIV-infected children with tuberculosis.
Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2009
)
0.35
" Plasma samples from 169 human immunodeficiency virus (HIV) patients characterized for CYP2B6, CYP2A6, and CYP3A4/5 allelic diversity were used to build up a population pharmacokinetic model using NONMEM (non-linear mixed effects modeling), the aim being to seek a general approach combining genetic and demographic covariates."( Pharmacogenetics-based population pharmacokinetic analysis of efavirenz in HIV-1-infected individuals.
Arab-Alameddine, M; Biollaz, J; Buclin, T; Cavassini, M; Csajka, C; Décosterd, LA; Di Iulio, J; Eap, CB; Fayet, A; Lubomirov, R; Rotger, M; Telenti, A, 2009
)
0.35
" A 600-mg oral dose of efavirenz was subsequently administered, and pharmacokinetic sampling was repeated."( Associations between CYP2B6 polymorphisms and pharmacokinetics after a single dose of nevirapine or efavirenz in African americans.
Acosta, EP; Floyd, M; Gebretsadik, T; Haas, DW; Mayo, G; Menon, UN; Shintani, A; Stein, CM; Wilkinson, GR, 2009
)
0.35
" As a result of these actions, co-administration of these drugs may result in changes in the pharmacokinetic parameters of one or both of them."( Pharmacokinetic interaction between efavirenz and ketoconazole in rats.
Peris, JE; Saadeddin, A, 2009
)
0.35
" Plasma concentrations of efavirenz were determined by a validated high performance liquid chromatography (HPLC) method with UV detection, and pharmacokinetic parameters were calculated."( Effect of African potato (Hypoxis hemerocallidea) on the pharmacokinetics of efavirenz.
Kanfer, I; Mills, E; Mogatle, S; Skinner, M, 2008
)
0.35
" Pharmacokinetic studies of higher dosages of rifampin are urgently needed in children to assist in placing the dosage of rifampin used in childhood on a more scientific foundation."( Rifampin pharmacokinetics in children, with and without human immunodeficiency virus infection, hospitalized for the management of severe forms of tuberculosis.
Cilliers, K; Donald, PR; Hussey, GD; Labadarios, D; Maritz, JS; McIlleron, H; Schaaf, HS; Smith, P; Willemse, M, 2009
)
0.35
"Small intensive pharmacokinetic (PK) studies of medications in early-phase trials cannot identify the range of factors that influence drug exposure in heterogenous populations."( Nonnucleoside reverse transcriptase inhibitor pharmacokinetics in a large unselected cohort of HIV-infected women.
Anastos, K; Bacchetti, P; Benet, LZ; Cohen, M; Gandhi, M; Gange, SJ; Greenblatt, RM; Kalinowski, A; Minkoff, H; Wolfe, AR; Young, M, 2009
)
0.35
"A population pharmacokinetic model for efavirenz has been developed from therapeutic drug monitoring data in human immunodeficiency virus (HIV)-positive patients by using a nonlinear mixed-effect model."( Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients.
Cabrera, SE; Domínguez-Gil, A; García, MJ; González, F; Luna, G; Santos, D; Valverde, MP, 2009
)
0.35
" Eighteen patients completed the pharmacokinetic study: TT genotype gave the longest half-life (t 1/2), highest plasma EFV concentration, and largest area under the curve."( Pharmacokinetics of plasma efavirenz and CYP2B6 polymorphism in southern Chinese.
Chan, DP; Chan, RC; Cheung, SW; Lee, SS; Liu, ST; To, KW, 2009
)
0.35
" Pharmacokinetic parameters were compared (before and after efavirenz 14-day intake) by determining geometric mean ratios and 90% confidence intervals."( Pharmacokinetics and safety of etravirine administered once or twice daily after 2 weeks treatment with efavirenz in healthy volunteers.
Asboe, D; Back, D; Boffito, M; Gazzard, B; Jackson, A; Lamorde, M; Pozniak, A; Taylor, J; Waters, L; Watson, V, 2009
)
0.35
"A phase 1, open-label, randomized, crossover, drug interaction study was conducted to assess the pharmacokinetic effects of coadministration of posaconazole (400 mg twice daily), with atazanavir (ATV) (300 mg/d alone) and with ritonavir (100 mg/d) or with efavirenz (400 mg/d) in healthy volunteers."( Effects of oral posaconazole on the pharmacokinetics of atazanavir alone and with ritonavir or with efavirenz in healthy adult volunteers.
Krishna, G; Ma, L; Martinho, M; McLeod, J; Moton, A; Seiberling, M, 2009
)
0.35
" Intensive pharmacokinetic (PK) sampling was done on days 10 and 24."( Lack of effect of efavirenz on the pharmacokinetics of tipranavir-ritonavir in healthy volunteers.
Béïque, L; Cameron, DW; la Porte, CJ; Sabo, JP, 2009
)
0.35
"Efavirenz exhibits pharmacokinetic variability causing varied clinical response."( A novel polymorphism in ABCB1 gene, CYP2B6*6 and sex predict single-dose efavirenz population pharmacokinetics in Ugandans.
Aklillu, E; Andersson, M; Fukasawa, T; Gustafsson, LL; Milani, L; Mukonzo, JK; Ogwal-Okeng, J; Röshammar, D; Svensson, JO; Waako, P, 2009
)
0.35
" Use of mixed-effects modelling allowed the analysis and integration of multiple pharmacogenetic and demographic covariates in a pharmacokinetic population model."( A novel polymorphism in ABCB1 gene, CYP2B6*6 and sex predict single-dose efavirenz population pharmacokinetics in Ugandans.
Aklillu, E; Andersson, M; Fukasawa, T; Gustafsson, LL; Milani, L; Mukonzo, JK; Ogwal-Okeng, J; Röshammar, D; Svensson, JO; Waako, P, 2009
)
0.35
" The differences in these pharmacokinetic parameters could possibly be due to differences in body weight and composition, drug-food interactions, metabolism, environmental factors and genetic background."( Pharmacokinetics of low-dose protease inhibitors and efavirenz in low- and middle-income countries.
Burger, D; Gorowara, M; Hill, A; Ruxrungtham, K, 2010
)
0.36
" Six-point pharmacokinetic sampling (0, 2, 4, 6, 8, and 12 h) was undertaken after observed intake with a standardized breakfast."( Pharmacokinetics of lopinavir-ritonavir with and without nonnucleoside reverse transcriptase inhibitors in Ugandan HIV-infected adults.
Dickinson, L; Gibb, DM; Gilks, CF; Kayiwa, J; Khoo, S; Kityo, C; Lutwama, F; Munderi, P; Nalumenya, R; Reid, A; Ssali, F; Tumukunde, D; Walker, AS, 2010
)
0.36
"Efavirenz (EFV) is characterized by interindividual pharmacokinetic variability causing inconsistent clinical responses."( Influence of host genetic factors on efavirenz plasma and intracellular pharmacokinetics in HIV-1-infected patients.
Elens, L; Haufroid, V; Lison, D; Vandercam, B; Wallemacq, P; Yombi, JC, 2010
)
0.36
" The pharmacokinetic parameters were: plasma drug concentration-time profile from 0 to 72 h (AUC0-72), plasma drug concentration-time profile from 0 h to infinity (AUC0-inf), maximal drug concentration (Cmax), time to reach maximal drug concentration (tmax), and time to reach half the initial drug concentration in elimination phase (t1/2)."( Pharmacokinetic interaction between efavirenz and rifampicin in healthy volunteers.
Djoerban, Z; Setiabudy, R, 2011
)
0.37
" However, current pharmacokinetic data are insufficient to guide optimized concurrent dosing."( Modest but variable effect of rifampin on steady-state plasma pharmacokinetics of efavirenz in healthy African-American and Caucasian volunteers.
Court, MH; Dumond, JB; Greenblatt, DJ; Kashuba, AD; Kurpewski, J; Kwara, A; Poethke, P; Tashima, KT, 2011
)
0.37
" We report the pharmacokinetic parameters of tenofovir in combination with efavirenz, darunavir-ritonavir, or atazanavir-ritonavir in HIV-infected children."( Steady-state pharmacokinetics of tenofovir-based regimens in HIV-infected pediatric patients.
Acosta, EP; Britto, P; Carey, V; Graham, B; Hazra, R; Jean-Philippe, P; King, JR; Wiznia, A; Yogev, R, 2011
)
0.37
" The lopinavir/ritonavir dose of 500/125 mg bid administered with efavirenz most closely approximates the pharmacokinetic exposure of lopinavir/ritonavir 400/100 mg bid administered alone."( Pharmacokinetics and safety of the lopinavir/ritonavir tablet 500/125 mg twice daily coadministered with efavirenz in healthy adult participants.
Awni, W; Bernstein, B; Causemaker, SJ; Chiu, YL; Klein, CE; Ng, J, 2012
)
0.38
"To evaluate international pediatric efavirenz dosing recommendations using full pharmacokinetic (PK) information."( Pediatric underdosing of efavirenz: a pharmacokinetic study in Uganda.
Balungi, J; Burger, DM; Bwakura-Dangarembizi, M; Ferrier, A; Fillekes, Q; Gibb, DM; Keishanyu, R; Kendall, L; Lutakome, J; Natukunda, E; Walker, AS, 2011
)
0.37
" NONMEM was used for the population pharmacokinetic modelling."( Influence of CYP2B6 516G>T polymorphism and interoccasion variability (IOV) on the population pharmacokinetics of efavirenz in HIV-infected South African children.
Dandara, C; Gous, H; Karlsson, MO; Meyers, TM; Rheeders, M; Viljoen, M, 2012
)
0.38
"This was a phase 1 pharmacokinetic drug interaction trial."( Safety, tolerability, and pharmacokinetic interactions of the antituberculous agent TMC207 (bedaquiline) with efavirenz in healthy volunteers: AIDS Clinical Trials Group Study A5267.
Allen, R; Aweeka, F; Cramer, Y; Dooley, KE; Flexner, C; Gupta, A; Haas, DW; Lizak, P; Park, JG; Qasba, S; Swindells, S; van Heeswijk, R; Wiggins, I, 2012
)
0.38
" We performed a prospective case-control association study to identify the incidence, pharmacogenetic, pharmacokinetic and biochemical predictors for anti-tubercular and antiretroviral drugs induced liver injury (DILI) in HIV and tuberculosis (TB) co-infected patients."( Pharmacogenetic & pharmacokinetic biomarker for efavirenz based ARV and rifampicin based anti-TB drug induced liver injury in TB-HIV infected patients.
Aderaye, G; Aklillu, E; Amogne, W; Burhenne, J; Habtewold, A; Lindquist, L; Makonnen, E; Riedel, KD; Suda, A; Ueda, N; Yimer, G, 2011
)
0.37
"Healthy HIV-negative subjects underwent 12 hr intensive pharmacokinetic (PK) sampling following single dose LNG alone and after 14 days of EFV."( Pharmacokinetic interactions between the hormonal emergency contraception, levonorgestrel (Plan B), and Efavirenz.
Carten, ML; Cu-Uvin, S; Kiser, JJ; Kwara, A; Mawhinney, S, 2012
)
0.38
"Co-administration of artemether/lumefantrine with antiretroviral therapy has potential for pharmacokinetic drug interactions."( Significant pharmacokinetic interactions between artemether/lumefantrine and efavirenz or nevirapine in HIV-infected Ugandan adults.
Back, D; Byakika-Kibwika, P; de Vries, PJ; Hanpithakpong, W; Katabira, E; Khoo, S; Lamorde, M; Lindegardh, N; Mayanja-Kizza, H; Mayito, J; Merry, C; Nabukeera, L; Namakula, R; Ntale, M; Pakker, N; Ryan, M; Tarning, J, 2012
)
0.38
" Clinical data from population pharmacokinetic and pharmacodynamic trials evaluating the impact of these drug interactions are urgently needed."( Significant pharmacokinetic interactions between artemether/lumefantrine and efavirenz or nevirapine in HIV-infected Ugandan adults.
Back, D; Byakika-Kibwika, P; de Vries, PJ; Hanpithakpong, W; Katabira, E; Khoo, S; Lamorde, M; Lindegardh, N; Mayanja-Kizza, H; Mayito, J; Merry, C; Nabukeera, L; Namakula, R; Ntale, M; Pakker, N; Ryan, M; Tarning, J, 2012
)
0.38
"002) with EFV, but the LR half-life was unchanged."( Concomitant efavirenz reduces pharmacokinetic exposure to the antimalarial drug artemether-lumefantrine in healthy volunteers.
Aweeka, FT; Dorsey, G; Havlir, D; Huang, L; Lizak, P; Marzan, F; Parikh, S; Rosenthal, PJ, 2012
)
0.38
"To determine pharmacokinetic and pharmacogenomic correlates of efavirenz central nervous system (CNS) side effects following a single dose."( Neuropsychometric correlates of efavirenz pharmacokinetics and pharmacogenetics following a single oral dose.
Acosta, EP; Gebretsadik, T; Haas, DW; Johnson, DH; Mayo, G; Shintani, A; Stein, CM, 2013
)
0.39
"001) and Cmax (P = 0."( Neuropsychometric correlates of efavirenz pharmacokinetics and pharmacogenetics following a single oral dose.
Acosta, EP; Gebretsadik, T; Haas, DW; Johnson, DH; Mayo, G; Shintani, A; Stein, CM, 2013
)
0.39
" Strategies that lower Cmax during initial dosing may decrease CNS side effects."( Neuropsychometric correlates of efavirenz pharmacokinetics and pharmacogenetics following a single oral dose.
Acosta, EP; Gebretsadik, T; Haas, DW; Johnson, DH; Mayo, G; Shintani, A; Stein, CM, 2013
)
0.39
"This was a Phase II open-label multiple dose pharmacokinetic and safety study."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"A total of 25 patients (56% male) completed the study; 21 had evaluable pharmacokinetic profiles."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"Coadministration of efavirenz, tenofovir and emtricitabine with a standard first-line TB treatment regimen did not significantly alter the pharmacokinetic parameters of these drugs and was tolerated well by Tanzanian TB patients who are coinfected with HIV."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"This is the first pharmacokinetic modelling of antiretroviral disposition in BP and CVF."( Pharmacokinetic modelling of efavirenz, atazanavir, lamivudine and tenofovir in the female genital tract of HIV-infected pre-menopausal women.
Cohen, MS; Dumond, JB; Forrest, A; Garonzik, SM; Kashuba, AD; Kendrick, RN; Nicol, MR; Patterson, KB, 2012
)
0.38
" Log-transformed trough efavirenz concentrations (Cmin) were previously estimated by population pharmacokinetic modeling."( Genome-wide association study of plasma efavirenz pharmacokinetics in AIDS Clinical Trials Group protocols implicates several CYP2B6 variants.
Acosta, EP; Clifford, DB; Daar, ES; Grady, B; Gulick, RM; Haas, DW; Holzinger, ER; McLaren, P; Morse, GD; Ribaudo, HJ; Ritchie, MD; Robbins, GK, 2012
)
0.38
"Among 856 individuals, CYP2B6 516G→T was associated with efavirenz estimated Cmin (P=8."( Genome-wide association study of plasma efavirenz pharmacokinetics in AIDS Clinical Trials Group protocols implicates several CYP2B6 variants.
Acosta, EP; Clifford, DB; Daar, ES; Grady, B; Gulick, RM; Haas, DW; Holzinger, ER; McLaren, P; Morse, GD; Ribaudo, HJ; Ritchie, MD; Robbins, GK, 2012
)
0.38
"Three CYP2B6 polymorphisms were independently associated with efavirenz estimated Cmin at genome-wide significance, and explained one-third of interindividual variability."( Genome-wide association study of plasma efavirenz pharmacokinetics in AIDS Clinical Trials Group protocols implicates several CYP2B6 variants.
Acosta, EP; Clifford, DB; Daar, ES; Grady, B; Gulick, RM; Haas, DW; Holzinger, ER; McLaren, P; Morse, GD; Ribaudo, HJ; Ritchie, MD; Robbins, GK, 2012
)
0.38
" Noncompartmental pharmacokinetic analysis was used to estimate PK parameters [area under the concentration-time curve over 24 h (AUC0-24h ) and maximal concentration (Cmax )]."( Pharmacokinetics of two common antiretroviral regimens in older HIV-infected patients: a pilot study.
Adams, JL; Corbett, AH; Dumond, JB; Forrest, A; Jennings, SH; Kashuba, AD; Kendrick, RL; Malone, S; Patterson, KB; Prince, HM; Sykes, C; Wang, R; White, N, 2013
)
0.39
" Compared with the general population, these elderly subjects had 8-13% decreased TFV AUC0-24h and Cmax , and 19-78% increased FTC and RTV AUC0-24h and Cmax ."( Pharmacokinetics of two common antiretroviral regimens in older HIV-infected patients: a pilot study.
Adams, JL; Corbett, AH; Dumond, JB; Forrest, A; Jennings, SH; Kashuba, AD; Kendrick, RL; Malone, S; Patterson, KB; Prince, HM; Sykes, C; Wang, R; White, N, 2013
)
0.39
" Pharmacokinetics and drug-drug interaction were simulated using the full physiologically based pharmacokinetic model implemented in the Simcyp™ ADME simulator."( Prediction of drug-drug interactions between various antidepressants and efavirenz or boosted protease inhibitors using a physiologically based pharmacokinetic modelling approach.
Almond, L; Back, D; Khoo, S; Kirov, A; Marzolini, C; Owen, A; Seden, K; Siccardi, M, 2013
)
0.39
" Although the simulated drug-drug interactions with antidepressants were overall weak to moderate according to the classification of the US FDA, fluoxetine and venlafaxine represent better candidates from a pharmacokinetic standpoint for patients on efavirenz and venlafaxine or citalopram for patients on boosted protease inhibitors."( Prediction of drug-drug interactions between various antidepressants and efavirenz or boosted protease inhibitors using a physiologically based pharmacokinetic modelling approach.
Almond, L; Back, D; Khoo, S; Kirov, A; Marzolini, C; Owen, A; Seden, K; Siccardi, M, 2013
)
0.39
" Based on data from a phase I, single-dose pharmacokinetic study, a nonlinear mixed-effects model characterizing BDQ pharmacokinetics and interaction with multiple-dose EFV was developed."( Model-based estimates of the effects of efavirenz on bedaquiline pharmacokinetics and suggested dose adjustments for patients coinfected with HIV and tuberculosis.
Aweeka, F; Dooley, KE; Karlsson, MO; Marzan, F; Park, JG; Svensson, EM, 2013
)
0.39
" We conducted a cross-sectional study of HIV-positive women to determine if protease inhibitor (PI) and non-nucleoside reverse transcriptase inhibitor (NNRTI) C(min) and Cmax values were significantly different than historical general population (predominantly male) averages and to evaluate correlates of higher concentrations."( Factors affecting antiretroviral pharmacokinetics in HIV-infected women with virologic suppression on combination antiretroviral therapy: a cross-sectional study.
Angel, JB; Blitz, SL; Burdge, D; Cohen, J; Conway, B; de Pokomandy, A; Gough, K; Haase, D; Klein, MB; la Porte, CJ; Loemba, H; Loutfy, MR; Pick, N; Raboud, J; Rachlis, AR; Smaill, FM; Trottier, S; Tseng, AL; Walmsley, SL, 2013
)
0.39
" Timed blood samples for C(min) and Cmax were drawn weekly for 3 weeks."( Factors affecting antiretroviral pharmacokinetics in HIV-infected women with virologic suppression on combination antiretroviral therapy: a cross-sectional study.
Angel, JB; Blitz, SL; Burdge, D; Cohen, J; Conway, B; de Pokomandy, A; Gough, K; Haase, D; Klein, MB; la Porte, CJ; Loemba, H; Loutfy, MR; Pick, N; Raboud, J; Rachlis, AR; Smaill, FM; Trottier, S; Tseng, AL; Walmsley, SL, 2013
)
0.39
"Compared to historical control data, C(min) in the women enrolled was significantly higher whereas Cmax was significantly lower."( Factors affecting antiretroviral pharmacokinetics in HIV-infected women with virologic suppression on combination antiretroviral therapy: a cross-sectional study.
Angel, JB; Blitz, SL; Burdge, D; Cohen, J; Conway, B; de Pokomandy, A; Gough, K; Haase, D; Klein, MB; la Porte, CJ; Loemba, H; Loutfy, MR; Pick, N; Raboud, J; Rachlis, AR; Smaill, FM; Trottier, S; Tseng, AL; Walmsley, SL, 2013
)
0.39
" The long terminal elimination half-life of etravirine should support once-daily dosing."( Pharmacokinetics and pharmacodynamics of etravirine 400 mg once daily in treatment-naïve patients.
Bickel, M; Di Perri, G; Faetkenheuer, G; Green, B; Hill, A; Kakuda, T; Kurowski, M; Morrish, G; van Delft, Y,
)
0.13
" Area under the curve over the dosing interval (AUC24h) and trough concentration (C0h) were estimated using a population pharmacokinetic model and compared with previous results using the 200-mg twice-daily dosage."( Pharmacokinetics and pharmacodynamics of etravirine 400 mg once daily in treatment-naïve patients.
Bickel, M; Di Perri, G; Faetkenheuer, G; Green, B; Hill, A; Kakuda, T; Kurowski, M; Morrish, G; van Delft, Y,
)
0.13
" To test the hypothesis that incorporation of mechanism of reduced efavirenz metabolism by the CYP2B6*6 allele can predict the genetic effect on efavirenz pharmacokinetics, in vitro-in vivo extrapolation of efavirenz clearance was performed by physiologically based pharmacokinetic modeling (Simcyp Simulator; Simcyp Ltd."( CYP2B6 pharmacogenetics-based in vitro-in vivo extrapolation of efavirenz clearance by physiologically based pharmacokinetic modeling.
Desta, Z; Guo, Y; Hall, SD; Li, L; Quinney, SK; Xu, C, 2013
)
0.39
"The pharmacokinetic data support coadministration of daclatasvir with atazanavir/ritonavir, efavirenz and/or tenofovir."( Assessment of pharmacokinetic interactions of the HCV NS5A replication complex inhibitor daclatasvir with antiretroviral agents: ritonavir-boosted atazanavir, efavirenz and tenofovir.
Bertz, R; Bifano, M; Grasela, D; Hartstra, J; Hwang, C; Kandoussi, H; Oosterhuis, B; Sevinsky, H; Tiessen, R; Velinova-Donga, M, 2013
)
0.39
" A population pharmacokinetic (PK) model was developed from a randomized, cross-over, drug-interaction study in healthy male Korean subjects (n = 17)."( Population pharmacogenetic-based pharmacokinetic modeling of efavirenz, 7-hydroxy- and 8-hydroxyefavirenz.
Abdelhady, AM; Desta, Z; Jiang, F; Overholser, BR; Shin, JG; Yeo, CW, 2014
)
0.4
" Samples were obtained for pharmacokinetic assessment on day 8 of each study cycle."( Factors associated with variability in rifampin plasma pharmacokinetics and the relationship between rifampin concentrations and induction of efavirenz clearance.
Cao, L; Court, MH; Kurpewski, J; Kwara, A; Mahjoub, BD; Peloquin, CA; Poethke, P; Tashima, KT; Yang, H, 2014
)
0.4
" We evaluated the effect of 2 highly active antiretroviral therapy (HAART) regimens (1 including efavirenz and the other ritonavir-boosted lopinavir) on the pharmacokinetic (PK) parameters of an ENG-releasing implant in HIV-positive women."( Effect of antiretroviral therapy including lopinavir/ritonavir or efavirenz on etonogestrel-releasing implant pharmacokinetics in HIV-positive women.
Amaral, E; Bahamondes, L; Bahamondes, MV; Brito, MB; de Souza, RM; Duarte, G; Ferriani, RA; Quintana, SM; Rocha Prandini, TR; Scaranari, C; Vieira, CS, 2014
)
0.4
" Pharmacokinetic sampling occurred at the end of each dosing period."( Phase I safety, pharmacokinetics, and pharmacogenetics study of the antituberculosis drug PA-824 with concomitant lopinavir-ritonavir, efavirenz, or rifampin.
Allen, R; Aweeka, F; Bao, J; Cramer, Y; Dooley, KE; Haas, DW; Koletar, SL; Luetkemeyer, AF; Marzan, F; Murray, S; Park, JG; Savic, R; Sutherland, D, 2014
)
0.4
" SLNs were prepared and analyzed for physical parameters, stability, and pharmacokinetic profile."( Enhanced oral bioavailability of efavirenz by solid lipid nanoparticles: in vitro drug release and pharmacokinetics studies.
Bajpai, M; Gaur, PK; Mishra, A; Mishra, S, 2014
)
0.4
" Pharmacokinetic sampling was performed at gestation week 37 and during the postpartum period."( Pharmacokinetics of efavirenz and treatment of HIV-1 among pregnant women with and without tuberculosis coinfection.
Castel, S; Chaisson, RE; Cohn, S; Denti, P; Dooley, KE; Haas, DW; Hoffmann, J; Hull, J; Martinson, N; Mashabela, F; McIlleron, H; Msandiwa, R; Wiesner, L, 2015
)
0.42
" A PAS population pharmacokinetic model in two dosing regimens was developed; potential covariates affecting its pharmacokinetics were examined, and Monte Carlo simulations were conducted evaluating the pharmacokinetic-pharmacodynamic index."( Pharmacokinetics of para-aminosalicylic acid in HIV-uninfected and HIV-coinfected tuberculosis patients receiving antiretroviral therapy, managed for multidrug-resistant and extensively drug-resistant tuberculosis.
de Kock, L; Derendorf, H; Diacon, AH; Donald, PR; Hernandez, KR; Prescott, K; Rosenkranz, B; Sy, SK; Yu, M, 2014
)
0.4
" Co-administration with EFV resulted in decreases of 57, 39 and 75% in DTG AUC(0-τ), Cmax and Cτ, respectively."( Effects of enzyme inducers efavirenz and tipranavir/ritonavir on the pharmacokinetics of the HIV integrase inhibitor dolutegravir.
Borland, J; Castellino, S; Chen, S; Guta, P; Hosking, L; Lou, Y; Mosteller, M; Peppercorn, A; Piscitelli, SC; Rubio, JP; Savina, P; Song, I; Wagner, D; Wajima, T; Wilfret, D, 2014
)
0.4
"The drug-drug interactions between pitavastatin and darunavir/ritonavir (DRV/r) as well as pitavastatin and efavirenz (EFV) were examined in an open-label, parallel-arm, pharmacokinetic (PK) study in HIV-uninfected healthy volunteers."( Lack of pharmacokinetic interactions between pitavastatin and efavirenz or darunavir/ritonavir.
Aberg, JA; Ma, Q; Malvestutto, CD; Morse, GD; Underberg, JA, 2014
)
0.4
"In the EFV arm, the geometric mean area under the concentration time curve (AUC0-τ) and Cmax of pitavastatin were 85."( Lack of pharmacokinetic interactions between pitavastatin and efavirenz or darunavir/ritonavir.
Aberg, JA; Ma, Q; Malvestutto, CD; Morse, GD; Underberg, JA, 2014
)
0.4
" When stratified based on CYP2B6 516G>T (n = 29 ; 11 GG, 10 GT and 8 TT), efavirenz pharmacokinetic parameters in plasma and breast milk differed significantly between patient groups."( Breast milk pharmacokinetics of efavirenz and breastfed infants' exposure in genetically defined subgroups of mother-infant pairs: an observational study.
Adejuyigbe, E; Amara, A; Back, D; Bolaji, O; Else, L; Khoo, S; Olagunju, A; Owen, A; Siccardi, M; Waitt, C, 2015
)
0.42
" A pharmacokinetic model was built in a forward and reverse procedure using nonlinear mixed effect modeling in NONMEM VI followed by model-based simulations for optimal doses."( CYP2B6*6, CYP2B6*18, Body weight and sex are predictors of efavirenz pharmacokinetics and treatment response: population pharmacokinetic modeling in an HIV/AIDS and TB cohort in Zimbabwe.
Chonzi, P; Dhoro, M; Kadzirange, G; Masimirembwa, C; Ngara, B; Nhachi, C; Zvada, S, 2015
)
0.42
" The effect of EFV and/or NVP on lumefantrine pharmacokinetic profile among HIV-malaria co-infected patients on ART and treated with AL was investigated."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.42
" Pharmacokinetic analysis of lumefantrine was done using non-linear mixed effect modelling."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.42
"Of the evaluated models, a two-compartment pharmacokinetic model with first order absorption and lag-time described well lumefantrine plasma concentrations time profile."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.42
"Participants receiving daily rifapentine and isoniazid with efavirenz had pharmacokinetic evaluations at baseline and weeks 2 and 4 of concomitant therapy."( Efavirenz Pharmacokinetics and Pharmacodynamics in HIV-Infected Persons Receiving Rifapentine and Isoniazid for Tuberculosis Prevention.
Andersen, JW; Bao, Y; Benson, CA; Chaisson, RE; Fletcher, CV; Gupta, A; Kim, P; Mohapi, L; Mwelase, T; Podany, AT; Supparatpinyo, K; Swindells, S, 2015
)
0.42
"This nonrandomized, parallel group, pharmacokinetic evaluation was conducted in three groups of human immunodeficiency virus-infected Ugandan women: ART-naive (n = 17), efavirenz-based ART (n = 20), and nevirapine-based ART (n = 20)."( Unintended Pregnancies Observed With Combined Use of the Levonorgestrel Contraceptive Implant and Efavirenz-based Antiretroviral Therapy: A Three-Arm Pharmacokinetic Evaluation Over 48 Weeks.
Back, DJ; Buzibye, A; Byakika-Kibwika, P; Cohn, SE; Darin, KM; Dilly Penchala, S; Else, LJ; Lamorde, M; Merry, C; Nakalema, S; Scarsi, KK, 2016
)
0.43
"To study pharmacokinetic effect of Aikeqing Granule (AG) by different medication ways on zidovudine (AZT) in highly active antiretroviral therapy ( HAART) of rats."( [Pharmacokinetic Effect of Aikeqing Granule by Different Medication Ways on Zidovudine in HAART of Rats].
Fu, LC; Lu, ZZ; Ma, JB; Song, C; Su, QJ; Tang, DH, 2015
)
0.42
" Pharmacokinetic parameters [such as t1/2, Tmax, Cmax, AUCo-t, plasma clearance rate (CL)] were calculated by DAS2."( [Pharmacokinetic Effect of Aikeqing Granule by Different Medication Ways on Zidovudine in HAART of Rats].
Fu, LC; Lu, ZZ; Ma, JB; Song, C; Su, QJ; Tang, DH, 2015
)
0.42
"AG combined HAART could enhance the Cmax of AZT."( [Pharmacokinetic Effect of Aikeqing Granule by Different Medication Ways on Zidovudine in HAART of Rats].
Fu, LC; Lu, ZZ; Ma, JB; Song, C; Su, QJ; Tang, DH, 2015
)
0.42
"Population pharmacokinetic (PopPK) analyses often rely on steady state and full adherence to prescribed dosage regimen assumptions from data gathered during therapeutic drug monitoring (TDM)."( Comparison of Population Pharmacokinetics Based on Steady-State Assumption Versus Electronically Monitored Adherence to Lopinavir, Atazanavir, Efavirenz, and Etravirine: A Retrospective Study.
Buclin, T; Bugnon, O; Cavassini, M; Csajka, C; Fuchs, A; Rotzinger, A; Schneider, MP, 2016
)
0.43
" A population pharmacokinetic (PPK) model was developed using data from three studies in HIV-1-infected pediatric subjects (n = 168) and one study in healthy adults (n = 24)."( Population Pharmacokinetics Analysis To Inform Efavirenz Dosing Recommendations in Pediatric HIV Patients Aged 3 Months to 3 Years.
Bertz, R; Chapel, S; Cirincione, B; Luo, M; Roy, A; Savant, I; Sevinsky, H, 2016
)
0.43
"We compared the pharmacokinetic (PK) exposure parameters of efavirenz (EFV) and its major inactive metabolite, 8-hydroxy-efavirenz (8-OH-EFV), in an open-label, single-sequence, and parallel design of HIV-infected and tuberculosis (TB)-HIV-coinfected Ethiopian patients in the HIV-TB Pharmagene study with 20 and 33 patients, respectively."( Long-Term Effect of Rifampicin-Based Anti-TB Regimen Coadministration on the Pharmacokinetic Parameters of Efavirenz and 8-Hydroxy-Efavirenz in Ethiopian Patients.
Aderaye, G; Aklillu, E; Amogne, W; Bertilsson, L; Burhenne, J; Habtewold, A; Makonnen, E; Owen, JS; Yimer, G, 2016
)
0.43
"A physiologically based pharmacokinetic (PBPK) model was developed for cobimetinib using in vitro data."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
0.43
"The PBPK model described cobimetinib pharmacokinetic profiles after both intravenous and oral administration of cobimetinib well and accurately simulated the itraconazole-cobimetinib DDI."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
0.43
"Based on ibrutinib pharmacokinetics and potential sensitivity towards CYP3A4-mediated drug-drug interactions (DDIs), a physiologically based pharmacokinetic approach was developed to mechanistically describe DDI with various CYP3A4 perpetrators in healthy men under fasting conditions."( Ibrutinib Dosing Strategies Based on Interaction Potential of CYP3A4 Perpetrators Using Physiologically Based Pharmacokinetic Modeling.
De Jong, J; de Zwart, L; Mannaert, E; Monshouwer, M; Snoeys, J; Sukbuntherng, J, 2016
)
0.43
"This study predicted the magnitude of the DDI between efavirenz, an inducer of CYP3A4 and inhibitor of CYP2C8, and dual CYP3A4/CYP2C8 substrates (repaglinide, montelukast, pioglitazone, paclitaxel) using a physiologically based pharmacokinetic (PBPK) modeling approach integrating concurrent effects on CYPs."( Physiologically Based Pharmacokinetic Modeling to Predict Drug-Drug Interactions with Efavirenz Involving Simultaneous Inducing and Inhibitory Effects on Cytochromes.
Back, D; Battegay, M; Elzi, L; Marzolini, C; Rajoli, R; Siccardi, M, 2017
)
0.46
" A population-based pharmacokinetic model was developed using 1,132 plasma efavirenz concentrations obtained from 73 HIV-seronegative volunteers administered a single oral dose of 600 mg efavirenz."( Population Pharmacokinetic Modeling To Estimate the Contributions of Genetic and Nongenetic Factors to Efavirenz Disposition.
Bies, RR; Desta, Z; Lu, J; Metzger, IF; Robarge, JD; Skaar, TC; Thong, N, 2017
)
0.46
" The pharmacokinetic studies demonstrated improved pharmacokinetic parameters for the formulation containing SLS and HPC."( Efavirenz dissolution enhancement III: Colloid milling, pharmacokinetics and electronic tongue evaluation.
Bilatto, SE; Cabral, LM; Corrêa, DS; da Costa, MA; Fandaruff, C; Hoffmeister, CR; Pitta, LR; Prado, LD; Rocha, HV; Silva, MA; Tasso, L, 2017
)
0.46
" Simulations of efavirenz clearance after oral administrations in individual cynomolgus monkeys were performed using individual simplified physiologically based pharmacokinetic (PBPK) modeling consisting of gut, liver and central compartments."( Efavirenz clearances in vitro and in vivo in six cynomolgus monkeys associated with polymorphic cytochrome P450 2C9 and simulated by individual physiologically based pharmacokinetic models.
Kusama, T; Miura, T; Shimizu, M; Uehara, S; Uno, Y; Utoh, M; Yamazaki, H, 2017
)
0.46
"Sparse pharmacokinetic sampling of ENG, NVP, or EFV were performed at screening, entry, and then 1, 4, 12, and 24-week postimplant insertion."( Efavirenz decreases etonogestrel exposure: a pharmacokinetic evaluation of implantable contraception with antiretroviral therapy.
Achilles, SL; Chappell, CA; Chen, BA; Cohn, SE; Darin, KM; Lamorde, M; Mackline, H; Nakalema, S; Riddler, SA; Scarsi, KK, 2017
)
0.46
" In addition, a subgroup of patients underwent intensive DBS and plasma sampling (0-24 hours) to provide full-profile data for pharmacokinetic parameters."( Comparison of Dried Blood Spots Versus Conventional Plasma Collection for the Characterization of Efavirenz Pharmacokinetics in a Large-Scale Global Clinical Trial-The ENCORE1 Study.
Amara, AB; Amin, J; Back, DJ; Carey, D; Else, LJ; Emery, S; Khoo, S; Puls, RL, 2017
)
0.46
" Population pharmacokinetic modelling was used to explore pharmacokinetic endpoints at 200, 400 and 600 mg daily doses in pregnant women stratified by CYP2B6 metabolic status."( Evaluation of universal versus genotype-guided efavirenz dose reduction in pregnant women using population pharmacokinetic modelling.
Bolaji, O; Khoo, S; Olagunju, A; Owen, A; Schipani, A, 2018
)
0.48
" The results of clinical pharmacokinetic (PK) studies indicate that guanfacine is sensitive to drug-drug interactions (DDIs) perpetrated by strong inhibitors and inducers of CYP3A4."( Development of Guanfacine Extended-Release Dosing Strategies in Children and Adolescents with ADHD Using a Physiologically Based Pharmacokinetic Model to Predict Drug-Drug Interactions with Moderate CYP3A4 Inhibitors or Inducers.
Li, A; Rong, H; Welty, D; Yeo, K, 2018
)
0.48
"To investigate clinically applicable dose-adjustment strategies to overcome the known drug-drug interaction (DDI) between levonorgestrel and efavirenz, using a physiologically based pharmacokinetic (PBPK) modelling-based approach."( Physiologically based pharmacokinetic modelling prediction of the effects of dose adjustment in drug-drug interactions between levonorgestrel contraceptive implants and efavirenz-based ART.
Back, DJ; Darin, KM; Fletcher, CV; Lamorde, M; Owen, A; Rajoli, RKR; Roberts, O; Scarsi, KK; Siccardi, M, 2018
)
0.48
"We developed a mechanistic population pharmacokinetic model using pooled data from women included in seven studies (1968 samples, 774 collected during pregnancy)."( A Mechanism-Based Population Pharmacokinetic Analysis Assessing the Feasibility of Efavirenz Dose Reduction to 400 mg in Pregnant Women.
Best, BM; Burger, DM; Capparelli, E; Colbers, AC; Cressey, TR; Denti, P; Dooley, KE; Greupink, R; Huitema, ADR; Mirochnick, M; Russel, FGM; Schalkwijk, S; Ter Heine, R, 2018
)
0.48
" Genetic polymorphisms and pharmacokinetic (PK) parameters of EFV400 without (PK1) and with INH/RIF following 4 (PK2) and 12 (PK3) weeks of coadministration were evaluated."( Pharmacokinetics of Efavirenz 400 mg Once Daily Coadministered With Isoniazid and Rifampicin in Human Immunodeficiency Virus-Infected Individuals.
Boffito, M; Cerrone, M; Day-Weber, I; Fedele, S; Hill, A; McClure, M; Neary, M; Owen, A; Wang, X; Weaver, C, 2019
)
0.51
" Weekly therapeutic drug monitoring (TDM), steady-state pharmacokinetic profiles (TT and PP), safety, virological efficacy, and CYP2B6 polymorphisms at positions 516 (C > T) and 938 (T > C) were evaluated."( Pharmacokinetics, Pharmacodynamics, and Pharmacogenetics of Efavirenz 400 mg Once Daily During Pregnancy and Post-Partum.
Bisdomini, E; Boffito, M; Byakika-Kibwika, P; Khan, W; Lamorde, M; McClure, M; Mukonzo, JK; Nakalema, S; Neary, M; Owen, A; Wang, X, 2018
)
0.48
"Although EFV400 pharmacokinetic parameters were slightly lower for TT compared with PP values, efavirenz concentrations exceeded cutoff levels established by the study and those measured in antiretroviral-naive patients receiving EFV400 in ENCORE1."( Pharmacokinetics, Pharmacodynamics, and Pharmacogenetics of Efavirenz 400 mg Once Daily During Pregnancy and Post-Partum.
Bisdomini, E; Boffito, M; Byakika-Kibwika, P; Khan, W; Lamorde, M; McClure, M; Mukonzo, JK; Nakalema, S; Neary, M; Owen, A; Wang, X, 2018
)
0.48
"To describe the pharmacokinetics of isoniazid and acetyl-isoniazid in TB/HIV-coinfected patients, and assess the effects of efavirenz co-administration and a 50% increase in the dose of rifampicin on the pharmacokinetic parameters of isoniazid and acetyl-isoniazid."( Effect of efavirenz-based antiretroviral therapy and high-dose rifampicin on the pharmacokinetics of isoniazid and acetyl-isoniazid.
Affolabi, D; Bah-Sow, O; Chirehwa, MT; Denti, P; McIlleron, H; Merle, C; Wiesner, L, 2019
)
0.51
" Pharmacokinetic samplings were done 16 weeks after initiation of efavirenz-based anti-retroviral therapy and eight weeks after completion of rifampicin-based anti-tuberculosis treatment."( Long-term efavirenz pharmacokinetics is comparable between Tanzanian HIV and HIV/Tuberculosis patients with the same CYP2B6*6 genotype.
Aklillu, E; Bertilsson, L; Burhenne, J; Janabi, M; Kitabi, EN; Minzi, OMS; Mugusi, F; Mugusi, S; Sasi, P, 2018
)
0.48
"This is a pharmacokinetic (PK) substudy of a prospective study that examined the interactions between anti-TB therapy and efavirenz in HIV-infected children with and without TB."( Population pharmacokinetics of efavirenz in HIV and TB/HIV coinfected children: the significance of genotype-guided dosing.
Alghamdi, WA; Antwi, S; Dompreh, A; Enimil, A; Kwara, A; Langaee, T; Peloquin, CA; Wiesner, L; Yang, H, 2019
)
0.51
" Associations between patient genotype and etonogestrel pharmacokinetic parameters were determined through univariate and multivariate linear regression."( Effect of patient genetics on etonogestrel pharmacokinetics when combined with efavirenz or nevirapine ART.
Achilles, SL; Chappell, CA; Chen, BA; Lamorde, M; Matovu, J; Nakalema, S; Neary, M; Owen, A; Scarsi, KK; Siccardi, M, 2019
)
0.51
"Within the control group, CYP2B6 983 T>C was associated with 27% higher etonogestrel Cmax and 28% higher AUC0-24weeks."( Effect of patient genetics on etonogestrel pharmacokinetics when combined with efavirenz or nevirapine ART.
Achilles, SL; Chappell, CA; Chen, BA; Lamorde, M; Matovu, J; Nakalema, S; Neary, M; Owen, A; Scarsi, KK; Siccardi, M, 2019
)
0.51
"We did a parallel, three-group, pharmacokinetic evaluation at HIV clinics in Asia (two sites), South America (five), sub-Saharan Africa (three), and the USA (11) between Dec 30, 2014, and Sept 12, 2016."( Antiretroviral therapy and vaginally administered contraceptive hormones: a three-arm, pharmacokinetic study.
Akelo, V; Aweeka, F; Aziz, M; Berzins, B; Cohn, SE; Coombs, RW; Coughlin, K; Cramer, YS; Friedman, RK; Gingrich, D; Godfrey, C; Moran, LE; Rosenkranz, SL; Scarsi, KK; Swaminathan, S; Zorrilla, CD, 2019
)
0.51
" Further studies designed to examine pharmacodynamic endpoints, such as ovulation, when intravaginal ring hormones are combined with efavirenz are warranted."( Antiretroviral therapy and vaginally administered contraceptive hormones: a three-arm, pharmacokinetic study.
Akelo, V; Aweeka, F; Aziz, M; Berzins, B; Cohn, SE; Coombs, RW; Coughlin, K; Cramer, YS; Friedman, RK; Gingrich, D; Godfrey, C; Moran, LE; Rosenkranz, SL; Scarsi, KK; Swaminathan, S; Zorrilla, CD, 2019
)
0.51
"Maternofoetal physiologically-based pharmacokinetic models integrating multi-compartmental maternal and foetal units were developed using Simbiology® to estimate prenatal drug exposure."( Using mechanistic physiologically-based pharmacokinetic models to assess prenatal drug exposure: Thalidomide versus efavirenz as case studies.
Adejuyigbe, E; Atoyebi, SA; Bolaji, O; Olagunju, A; Owen, A; Rajoli, RKR; Siccardi, M, 2019
)
0.51
" Intensive pharmacokinetic sampling of DTG was undertaken at day 14 and 2wPP following administration of a medium-fat breakfast, with additional paired sampling between maternal plasma and cord blood, breastmilk and infant plasma."( Safety and pharmacokinetics of dolutegravir in pregnant mothers with HIV infection and their neonates: A randomised trial (DolPHIN-1 study).
Amara, A; Byakika-Kibwika, P; Byamugisha, J; Coombs, JA; Else, L; Gini, J; Heiburg, C; Hill, A; Hodel, EM; Kaboggoza, J; Khoo, S; Kintu, K; Lamorde, M; Malaba, T; Mehta, U; Myer, L; Orrell, C; Reynolds, H; Sihlangu, M; Simmons, B; Singh, Y; Waitt, C; Walimbwa, S, 2019
)
0.51
"A simple and rapid ultra-high-performance liquid chromatography (UHPLC) method for determination of efavirenz (EFV) in plasma was developed and applied in a preclinical pharmacokinetic study."( Simple and Rapid Method by Ultra High-Performance Liquid Chromatography (UHPLC) with Ultraviolet Detection for Determination of Efavirenz in Plasma: Application in a Preclinical Pharmacokinetic Study.
Cândido, CD; Dos Santos Martins, E; Franchin, TB; Oliveira, JA; Peccinini, RG; Silva, BCU, 2020
)
0.56
" A physiologically based pharmacokinetic (PBPK) model incorporating the metabolites was developed to predict the effect of other strong and moderate CYP3A4 inhibitors and inducers."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
0.56
" Plasma concentration of each antiretroviral drug was tested for calculation of pharmacokinetic parameters."( Influence of a herbal preparation on the pharmacokinetics of highly active antiretroviral therapy drugs in rats.
Jiang, F; Lu, Z; Su, Q; Tang, Y; Wei, S; Zhou, Z, 2020
)
0.56
" Pharmacokinetic parameters were obtained from intensive plasma concentration-time data."( Influence of selected polymorphisms in disposition genes on lumefantrine pharmacokinetics when coadministered with efavirenz.
Adeagbo, BA; Adegbola, AJ; Bolaji, OO; Bolarinwa, RA; Olagunju, AE; Owen, A; Rana, A; Siccardi, M, 2020
)
0.56
" This study aimed to develop a population model of the pharmacokinetic properties of efavirenz, and to investigate the impact of patients' characteristics and CYP2B6 516G > T polymorphism on the pharmacokinetic properties of efavirenz."( Dosage Optimization of Efavirenz Based on a Population Pharmacokinetic-Pharmacogenetic Model of HIV-infected Patients in Thailand.
Avihingsanon, A; Chaivichacharn, P; Manosuthi, W; Punyawudho, B; Shotelersuk, V; Tongkobpetch, S; Ubolyam, S, 2020
)
0.56
" A 1-compartment model with first-order absorption and elimination was used for describing the pharmacokinetic properties of efavirenz."( Dosage Optimization of Efavirenz Based on a Population Pharmacokinetic-Pharmacogenetic Model of HIV-infected Patients in Thailand.
Avihingsanon, A; Chaivichacharn, P; Manosuthi, W; Punyawudho, B; Shotelersuk, V; Tongkobpetch, S; Ubolyam, S, 2020
)
0.56
" We investigated pregnancy-induced and pharmacogenetic-associated pharmacokinetic changes and drug-drug interactions between isoniazid and efavirenz in pregnant women."( Pharmacokinetics and Drug-Drug Interactions of Isoniazid and Efavirenz in Pregnant Women Living With HIV in High TB Incidence Settings: Importance of Genotyping.
Aaron, L; Aurpibul, L; Bhosale, R; Bradford, S; Browning, R; Chakhtoura, N; Chanaiwa, V; Chipato, T; Costello, D; Denti, P; Gausi, K; Gupta, A; Haas, DW; Hesseling, A; Jean-Philippe, P; Kabugho, E; Masheto, GR; McCarthy, K; Mhembere, T; Mmbaga, BT; Montepiedra, G; Mutambanengwe, M; Nevrekhar, N; Norman, J; Nyati, M; Onyango-Makumbi, C; Rouzier, V; Shin, K; Sterling, TR; Stranix-Chibanda, L; Theron, G; Tongprasert, F; Vhembo, T; Violari, A; Wallis, CL; Weinberg, A; Wiesner, L; Zimmer, B, 2021
)
0.62
" As M9 concentrations have not been quantified in previous clinical studies, a physiologically based pharmacokinetic model was developed to investigate the change in M9 exposure when doravirine is coadministered with CYP3A inducers."( Physiologically Based Pharmacokinetic Modeling of Doravirine and Its Major Metabolite to Support Dose Adjustment With Rifabutin.
Cabalu, TD; Dreyer, D; Fillgrove, KL; Iwamoto, M; Khalilieh, SG; Kuo, Y; Liu, Y; McClain, S; Sanchez, RI; Stoch, SA; Triantafyllou, I; Wenning, L; Yee, KL, 2021
)
0.62
"Population pharmacokinetic (popPK) approaches have spread widely throughout clinical pharmacology research, and every clinician should have some understanding of them."( Parametric Approaches in Population Pharmacokinetics.
Buclin, T; Csajka, C; Guidi, M, 2022
)
0.72
"Population pharmacokinetic (PK) modeling is a widely used approach to analyze PK data obtained from groups of individuals, in both industry and academic research."( Nonparametric Methods in Population Pharmacokinetics.
Bourguignon, L; Goutelle, S; Neely, M; Woillard, JB; Yamada, W, 2022
)
0.72
" The efavirenz population pharmacokinetic profile among HIV-positive smokers is still unknown."( The association between cigarette smoking and efavirenz plasma concentration using the population pharmacokinetic approach.
Chow, NK; Harun, SN; Khan, AH; Low, LL; Sheikh Ghadzi, SM; Wong, EJ, 2021
)
0.62
" The association between smoking and efavirenz pharmacokinetic parameters was determined using the nonlinear mixed-effect model."( The association between cigarette smoking and efavirenz plasma concentration using the population pharmacokinetic approach.
Chow, NK; Harun, SN; Khan, AH; Low, LL; Sheikh Ghadzi, SM; Wong, EJ, 2021
)
0.62
" A pooled population pharmacokinetic analysis with 744 plasma medroxyprogesterone acetate concentrations from 138 women treated with depot medroxyprogesterone and antiretroviral/antituberculosis treatment across three clinical trials was performed."( A Semimechanistic Pharmacokinetic Model for Depot Medroxyprogesterone Acetate and Drug-Drug Interactions With Antiretroviral and Antituberculosis Treatment.
Cohn, SE; Denti, P; Dooley, KE; Firnhaber, C; Francis, J; Godfrey, C; Kendall, MA; McIlleron, H; Mngqibisa, R; Wu, X, 2021
)
0.62
" Minimum duration of nonadherence resulting in a negative drug level test was assessed by simulation of treatment cessation using validated population pharmacokinetic models."( Point-of-Care Detection of Nonadherence to Antiretroviral Treatment for HIV-1 in Resource-Limited Settings Using Drug Level Testing for Efavirenz, Lopinavir, and Dolutegravir: A Validation and Pharmacokinetic Simulation Study.
Burger, DM; Heine, RT; Hermans, LE; Houts, T; Nijhuis, M; Schuurman, R; Tempelman, HA; Wensing, AMJ, 2021
)
0.62
"A total of 769 plasma samples from 376 HIV-infected Han Chinese outpatients were collected to develop a population pharmacokinetic model using NONMEM software."( Effect of albumin and CYP2B6 polymorphisms on exposure of efavirenz: A population pharmacokinetic analysis in Chinese HIV-infected adults.
Li, ZR; Liu, YX; Lu, HZ; Meng, XM; Niu, WJ; Qiu, XY; Zheng, XY, 2021
)
0.62
"Polymorphisms of CYP2B6, along with albumin and weight, resulted as the predictors of efavirenz pharmacokinetic variability, which could be used in prescribing optimal efavirenz doses."( Effect of albumin and CYP2B6 polymorphisms on exposure of efavirenz: A population pharmacokinetic analysis in Chinese HIV-infected adults.
Li, ZR; Liu, YX; Lu, HZ; Meng, XM; Niu, WJ; Qiu, XY; Zheng, XY, 2021
)
0.62
"Pharmacokinetic data were combined in a population pharmacokinetic model."( Impact of CYP2B6 genotype, tuberculosis therapy, and formulation on efavirenz pharmacokinetics in infants and children under 40 months of age.
Benns, A; Bolton Moore, C; Bwakura-Dangarembizi, M; Capparelli, EV; Chadwick, EG; Chakhtoura, N; Frenkel, L; Jean-Philippe, P; Libous, J; Nikanjam, M; Samson, P; Spector, SA; Tran, L; Zimmer, B, 2022
)
0.72
" Median age at the first pharmacokinetic visit was 17."( Impact of CYP2B6 genotype, tuberculosis therapy, and formulation on efavirenz pharmacokinetics in infants and children under 40 months of age.
Benns, A; Bolton Moore, C; Bwakura-Dangarembizi, M; Capparelli, EV; Chadwick, EG; Chakhtoura, N; Frenkel, L; Jean-Philippe, P; Libous, J; Nikanjam, M; Samson, P; Spector, SA; Tran, L; Zimmer, B, 2022
)
0.72
" This study aimed to develop a population pharmacokinetic model to characterize the disposition of maraviroc in neonates to inform dosing regimens and expand available options."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
"Using maraviroc concentrations from neonates who received either a single dose or multiple doses of 8 mg/kg of maraviroc in the first 6 weeks of life, a population pharmacokinetic model was developed to determine the effects of age, sex, maternal efavirenz exposure and concomitant ARV therapy on maraviroc disposition."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
" Levonorgestrel pharmacokinetic parameters were compared between groups using geometric mean ratios (GMR) with 90% confidence intervals."( Pharmacokinetics of dose-adjusted levonorgestrel emergency contraception combined with efavirenz-based antiretroviral therapy or rifampicin-containing tuberculosis regimens.
Badal-Faesen, S; Barr, E; Belaunzaran-Zamudio, PF; Cohn, SE; Gadama, L; Gatechompol, S; Godfrey, C; Jalil, EM; Mawlana, S; Mngqibisa, R; Olefsky, M; Pham, M; Podany, AT; Scarsi, KK; Smeaton, LM; Supparatpinyo, K; Woolley, E, 2023
)
0.91
"5 mg to 3 mg improves levonorgestrel pharmacokinetic exposure in participants receiving either efavirenz-based antiretroviral regimens or rifampicin-containing tuberculosis therapy."( Pharmacokinetics of dose-adjusted levonorgestrel emergency contraception combined with efavirenz-based antiretroviral therapy or rifampicin-containing tuberculosis regimens.
Badal-Faesen, S; Barr, E; Belaunzaran-Zamudio, PF; Cohn, SE; Gadama, L; Gatechompol, S; Godfrey, C; Jalil, EM; Mawlana, S; Mngqibisa, R; Olefsky, M; Pham, M; Podany, AT; Scarsi, KK; Smeaton, LM; Supparatpinyo, K; Woolley, E, 2023
)
0.91
"Despite the potential for efavirenz (EFV) to be an effective alternative antiretroviral agent, its sources of wide inter- and intra-individual pharmacokinetic (PK) variability are not well-characterized in children."( Genetic and non-genetic factors influencing efavirenz population pharmacokinetics among human immunodeficiency virus-1-infected children in Ethiopia.
Ahmed, JH; Aklillu, E; Chaka, TE; Chala, A; Kitabi, EN; Makonnen, E; Tadesse, BT, 2023
)
0.91
" Predicted pharmacokinetic parameters for mothers, breastfeeding infants, and children aged ≥ 3 months were reasonably consistent with observed data, irrespective of CYP2B6 genotype."( Physiologically Based Pharmacokinetic Modeling to Determine the Impact of CYP2B6 Genotype on Efavirenz Exposure in Children, Mothers and Breastfeeding Infants.
Pan, X; Rowland Yeo, K, 2023
)
0.91

Compound-Compound Interactions

Study 903 is a phase 3 trial with a completed 144-week, double-blind phase comparing tenofovir DF (TDF) to stavudine (d4T) in combination with lamivudine and efavirenz (EFV)

ExcerptReferenceRelevance
"Nelfinavir is a novel protease inhibitor that exhibits good inhibitory activity against human immunodeficiency virus type 1 (HIV-1) and is currently used in combination with reverse transcriptase inhibitors for the management of HIV infection."( Clinical pharmacokinetics of nelfinavir combined with efavirenz and stavudine during rescue treatment of heavily pretreated HIV-infected patients.
Fiocchi, C; Gambarana, E; LoCaputo, F; Maserati, R; Pan, A; Regazzi, MB; Seminari, E; Villani, P, 2000
)
0.31
" Efavirenz, DPC082, DPC083, DPC961, and DPC963 used in combination with the NRTIs zidovudine and lamivudine acted synergistically to inhibit RT activity in the HIV-1 RT enzyme assay and additively to slightly synergistically to inhibit HIV-1 (RF) replication in the yield reduction assay."( Potency of nonnucleoside reverse transcriptase inhibitors (NNRTIs) used in combination with other human immunodeficiency virus NNRTIs, NRTIs, or protease inhibitors.
Erickson-Viitanen, SK; King, RW; Klabe, RM; Reid, CD, 2002
)
0.31
"The steady-state pharmacokinetics and pharmacodynamics of two oral doses of lopinavir-ritonavir (lopinavir/r; 400/100 and 533/133 mg) twice daily (BID) when dosed in combination with efavirenz, plus two nucleoside reverse transcriptase inhibitors, were assessed in a phase II, open-label, randomized, parallel arm study in 57 multiple protease inhibitor-experienced but non-nucleoside reverse transcriptase inhibitor-naive human immunodeficiency virus (HIV)-infected subjects."( Pharmacokinetic-pharmacodynamic analysis of lopinavir-ritonavir in combination with efavirenz and two nucleoside reverse transcriptase inhibitors in extensively pretreated human immunodeficiency virus-infected patients.
Bernstein, B; Bertz, R; Brun, S; Foit, C; Granneman, GR; Hsu, A; Isaacson, J; Kempf, DJ; King, M; Lam, W; Richards, B; Rode, R; Rynkiewicz, K; Sun, E, 2003
)
0.32
" This study evaluated the steady-state pharmacokinetics of indinavir/ritonavir at 800/100 mg twice daily (bid) in combination with efavirenz at 600 mg once daily (qd) in HIV-infected Thai subjects who used this nucleoside-sparing combination in The HIV Netherlands Australia Thailand Research Collaboration 009 study."( Pharmacokinetics of indinavir/ritonavir (800/100 mg) in combination with efavirenz (600 mg) in HIV-1-infected subjects.
Aarnoutse, RE; Boyd, MA; Burger, DM; Cooper, DA; Lange, JM; Phanuphak, P; Ruxrungtham, K; Stek, M; van Heeswijk, RP, 2003
)
0.32
"A randomized, double-blind, double-dummy, active-controlled, 2-arm study comparing the antiviral efficacy and safety of atazanavir 400 mg administered once daily with efavirenz 600 mg administered once daily in combination with open-label fixed-dose zidovudine plus lamivudine twice daily."( Comparison of once-daily atazanavir with efavirenz, each in combination with fixed-dose zidovudine and lamivudine, as initial therapy for patients infected with HIV.
Delfraissy, JF; Gatell, JM; Giordano, M; Jemsek, J; Lazzarin, A; Pokrovskiy, V; Powderly, WG; Rivero, A; Rozenbaum, W; Schrader, S; Sension, M; Squires, K; Thiry, A; Vibhagool, A, 2004
)
0.32
"Abacavir provided an effective and durable antiretroviral response that was noninferior to zidovudine, when combined with lamivudine and efavirenz."( Abacavir versus zidovudine combined with lamivudine and efavirenz, for the treatment of antiretroviral-naive HIV-infected adults.
Bonny, T; Brand, JD; Brothers, CH; Buendia, CB; Castillo, SA; DeJesus, E; Gerstoft, J; Hernandez, J; Herrera, G; Lanier, ER; Scott, TR; Teofilo, E, 2004
)
0.32
" A randomized double-blind clinical trial compared the efficacy and safety of 600 mg of ABC administered once daily (n = 384) versus 300 mg of ABC administered twice daily (n = 386) in combination with 300 mg of lamivudine (3TC) and 600 mg of efavirenz (EFV) administered once daily in antiretroviral-naive patients over 48 weeks."( Abacavir once or twice daily combined with once-daily lamivudine and efavirenz for the treatment of antiretroviral-naive HIV-infected adults: results of the Ziagen Once Daily in Antiretroviral Combination Study.
Cahn, P; Castillo, SA; Craig, C; DeJesus, E; Gordon, DN; Moyle, GJ; Scott, TR; Zhao, H, 2005
)
0.33
"Because of drug-drug interactions mediated by hepatic cytochrome P450, tuberculosis treatment guidelines recommend an increase in rifabutin from 300 mg to 450 or 600 mg when combined with efavirenz-based antiretroviral therapy."( Evaluation of the drug interaction between rifabutin and efavirenz in patients with HIV infection and tuberculosis.
Benator, D; Burman, W; Engle, M; Khan, A; Peloquin, CA; Vernon, A; Weiner, M; Zhao, Z, 2005
)
0.33
"Tenofovir disoproxil fumarate (DF) has been studied in combination with efavirenz in healthy volunteers and no interaction was found."( Assessment of drug-drug interactions between tenofovir disoproxil fumarate and the nonnucleoside reverse transcriptase inhibitors nevirapine and efavirenz in HIV-infected patients.
Burger, DM; Droste, JA; Hekster, YA; Kearney, BP, 2006
)
0.33
" Six different groups were studied: 200 mg nevirapine twice daily, 400 mg nevirapine once daily, 600 mg efavirenz once daily, all without tenofovir DF (groups 1, 2, and 3, respectively), and the same groups with the drugs combined with tenofovir 300 mg once daily (groups 4, 5, and 6, respectively)."( Assessment of drug-drug interactions between tenofovir disoproxil fumarate and the nonnucleoside reverse transcriptase inhibitors nevirapine and efavirenz in HIV-infected patients.
Burger, DM; Droste, JA; Hekster, YA; Kearney, BP, 2006
)
0.33
"HIV-positive patients with CD4 cell counts > or = 100 cells/mm3 were randomized to 1 of 2 treatment arms: (1) atazanavir, 400 mg given once daily, plus efavirenz placebo; or (2) efavirenz, 600 mg given once daily, plus atazanavir placebo; each drug was administered with fixed-dose zidovudine (300 mg) and lamivudine (150 mg) given twice daily, and patients were treated for at least 48 weeks."( Body fat and other metabolic effects of atazanavir and efavirenz, each administered in combination with zidovudine plus lamivudine, in antiretroviral-naive HIV-infected patients.
Arathoon, E; Arlotti, M; Giordano, M; Jemsek, JG; Noor, MA; Perez, C; Pokrovskiy, V; Soccodato, M; Sosa, N; Thiry, A, 2006
)
0.33
"Study 903 is a phase 3 trial with a completed 144-week, double-blind phase comparing tenofovir DF (TDF) to stavudine (d4T) in combination with lamivudine (3TC) and efavirenz (EFV) and an ongoing additional 336-week open-label extension phase."( The safety and efficacy of tenofovir DF in combination with lamivudine and efavirenz through 6 years in antiretroviral-naïve HIV-1-infected patients.
Cassetti, I; Cheng, AK; Enejosa, J; Etzel, A; Madruga, JV; Suleiman, JM; Zhong, L,
)
0.13
"Although there is a presumed drug-drug interaction between itraconazole and nonnucleoside reverse-transcriptase inhibitors, the medical literature lacks such documentation."( Drug-drug interaction between itraconazole and efavirenz in a patient with AIDS and disseminated histoplasmosis.
Andrade, RA; Hamill, RJ; Koo, HL, 2007
)
0.34
" We evaluated the effect of preexisting drug-associated resistance mutations to the response in treatment-naive patients to therapy with emtricitabine (FTC) or stavudine (d4T) in combination with didanosine (ddI) and efavirenz (EFV)."( Baseline genotype as a predictor of virological failure to emtricitabine or stavudine in combination with didanosine and efavirenz.
Bae, AS; Borroto-Esoda, K; Harris, JL; Hinkle, JE; Quinn, JB; Rousseau, FS; Waters, JM, 2007
)
0.34
"Study 903 is a phase 3 trial with a completed 144-week, double-blind phase comparing tenofovir DF (TDF) with stavudine (d4T), in combination with lamivudine (3TC) and efavirenz (EFV), and an ongoing 336-week open-label extension phase."( The safety and efficacy of switching stavudine to tenofovir df in combination with lamivudine and efavirenz in hiv-1-infected patients: three-year follow-up after switching therapy.
Cassetti, I; Cheng, AK; Enejosa, J; Etzel, A; Holmes, CB; Madruga, JR; Suleiman, JM; Zhong, L,
)
0.13
" In some patients on the nucleoside-sparing arm, the nucleoside-resistance mutation L74V was selected for in combination with the uncommonly occurring EFV-resistance mutations K103N+L100I; L74V was not detected as a minority variant, using clonal sequence analysis, when the nucleoside-sparing regimen was initiated."( Association of efavirenz hypersusceptibility with virologic response in ACTG 368, a randomized trial of abacavir (ABC) in combination with efavirenz (EFV) and indinavir (IDV) in HIV-infected subjects with prior nucleoside analog experience.
Bettendorf, D; DeGruttola, V; Demeter, LM; Eron, JJ; Eshleman, S; Fischl, M; Hammer, S; Koval, CE; Lustgarten, S; Nguyen, BY; Spreen, W; Squires, K,
)
0.13
" In addition, L74V, when combined with K103N+L100I, may confer a selective advantage to the virus that is independent of its effects on nucleoside resistance."( Association of efavirenz hypersusceptibility with virologic response in ACTG 368, a randomized trial of abacavir (ABC) in combination with efavirenz (EFV) and indinavir (IDV) in HIV-infected subjects with prior nucleoside analog experience.
Bettendorf, D; DeGruttola, V; Demeter, LM; Eron, JJ; Eshleman, S; Fischl, M; Hammer, S; Koval, CE; Lustgarten, S; Nguyen, BY; Spreen, W; Squires, K,
)
0.13
" Pharmacokinetic profiles were also determined in HIV-1-infected patients dosed with raltegravir monotherapy versus raltegravir in combination with TDF and lamivudine."( Lack of a significant drug interaction between raltegravir and tenofovir.
Breidinger, SA; Chen, J; Friedman, EJ; Gottesdiener, KM; Iwamoto, M; Kost, JT; Lasseter, KC; Stek, JE; Stone, JA; Teppler, H; Wagner, JA; Wenning, LA, 2008
)
0.35
" These mt-QSARs offer also a good opportunity to construct drug-drug Complex Networks (CNs) that can be used to explore large and complex drug-viral species databases."( Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks.
Chou, KC; González-Díaz, H; Martinez de la Vega, O; Prado-Prado, FJ; Ubeira, FM; Uriarte, E, 2009
)
0.35
" Because 3'-azido-3'-deoxythymidine (AZT), one of the most current nucleotide reverse transcriptase inhibitors prescribed in combination with EFV, is also conjugated by UGT2B7, the potential metabolic interaction between EFV and AZT has been studied using human liver microsomes."( Glucuronidation of the antiretroviral drug efavirenz by UGT2B7 and an in vitro investigation of drug-drug interaction with zidovudine.
Bélanger, AS; Caron, P; Guillemette, C; Harvey, M; Mehlotra, RK; Zimmerman, PA, 2009
)
0.35
"Similar virological efficacy was observed for efavirenz and lopinavir/r, when administered with Kivexa in antiretroviral-naïve patients, while immunological improvement was slightly superior for efavirenz."( Similar antiviral efficacy and tolerability between efavirenz and lopinavir/ritonavir, administered with abacavir/lamivudine (Kivexa), in antiretroviral-naïve patients: a 48-week, multicentre, randomized study (Lake Study).
Bravo, I; Carosi, G; Clotet, B; del Arco, A; Echeverría, P; Gálvez, J; Gómez, JL; López, JC; López-Blazquez, R; Mariño, A; Moreno, A; Negredo, E; Ocampo, A; Pedrol, E; Pérez-Alvarez, N; Portilla, J; Prieto, A; Rubio, R; Viladés, C, 2010
)
0.36
"Forty-eight-week data are presented from this multicenter, randomized, open-label study comparing the safety profiles of abacavir/lamivudine and tenofovir/emtricitabine, both administered with efavirenz, in HLA-B*5701-negative HIV-1-infected adults."( Randomized comparison of renal effects, efficacy, and safety with once-daily abacavir/lamivudine versus tenofovir/emtricitabine, administered with efavirenz, in antiretroviral-naive, HIV-1-infected adults: 48-week results from the ASSERT study.
Branco, T; Cavassini, M; Domingo, P; Fisher, M; Givens, N; Khuong-Josses, MA; Lim, ML; Moyle, GJ; Norden, AG; Pearce, HC; Podzamczer, D; Post, FA; Rieger, A; Stellbrink, HJ; Vavro, C, 2010
)
0.36
"To determine which NNRTI, EFV or NVP, is more efficacious when given in combination with two NRTIs as part of initial ART for HIV infection in adults and children."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, LC; Rutherford, GW; Siegfried, N; Spaulding, A, 2010
)
0.36
"Both drugs have equivalent efficacies in initial treatment of HIV infection when combined with two NRTIs, but different side effects."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, LC; Rutherford, GW; Siegfried, N; Spaulding, A, 2010
)
0.36
" The lopinavir/ritonavir dose of 500/125 mg bid administered with efavirenz most closely approximates the pharmacokinetic exposure of lopinavir/ritonavir 400/100 mg bid administered alone."( Pharmacokinetics and safety of the lopinavir/ritonavir tablet 500/125 mg twice daily coadministered with efavirenz in healthy adult participants.
Awni, W; Bernstein, B; Causemaker, SJ; Chiu, YL; Klein, CE; Ng, J, 2012
)
0.38
"Eligible patients with HIV-1 RNA (vRNA) levels >5000 copies/mL and without baseline resistance to efavirenz, tenofovir, or emtricitabine were randomized in a double-blind, noninferiority study to receive raltegravir or efavirenz, each combined with tenofovir/emtricitabine."( Long-term treatment with raltegravir or efavirenz combined with tenofovir/emtricitabine for treatment-naive human immunodeficiency virus-1-infected patients: 156-week results from STARTMRK.
Dejesus, E; Dinubile, MJ; Lazzarin, A; Leavitt, R; Lennox, JL; Nguyen, BY; Rockstroh, JK; Rodgers, AJ; Saag, MS; Sklar, P; Teppler, H; Walker, ML; Wan, H; Xu, X; Zhao, J, 2011
)
0.37
"When combined with tenofovir/emtricitabine in treatment-naive patients, raltegravir produced durable viral suppression and immune restoration that was at least equivalent to efavirenz through 156 weeks of therapy."( Long-term treatment with raltegravir or efavirenz combined with tenofovir/emtricitabine for treatment-naive human immunodeficiency virus-1-infected patients: 156-week results from STARTMRK.
Dejesus, E; Dinubile, MJ; Lazzarin, A; Leavitt, R; Lennox, JL; Nguyen, BY; Rockstroh, JK; Rodgers, AJ; Saag, MS; Sklar, P; Teppler, H; Walker, ML; Wan, H; Xu, X; Zhao, J, 2011
)
0.37
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
"To explore the durability of three first-line tenofovir/emtricitabine-based regimens in combination with atazanavir/ritonavir, efavirenz or lopinavir/ritonavir in HIV-1-infected patients."( Duration of first-line antiretroviral therapy with tenofovir and emtricitabine combined with atazanavir/ritonavir, efavirenz or lopinavir/ritonavir in the Italian ARCA cohort.
Borghi, V; Capetti, A; Cicconi, P; Di Biagio, A; Di Giambenedetto, S; Francisci, D; Giacometti, A; Giannarelli, D; Maggiolo, F; Monno, L; Penco, G; Prinapori, R; Sterrantino, G; Zoncada, A, 2013
)
0.39
" For TB drugs, equivalence was suggested for peak plasma concentrations when administered with and without efavirenz/tenofovir/emtricitabine."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"Comprehensive information on the effects of cytochrome P450 2B6 (CYP2B6) polymorphisms, clinical factors, and drug-drug interactions on efavirenz concentrations in HIV/tuberculosis-coinfected (HIV/TB) patients is unavailable."( Impact of pharmacogenetic markers of CYP2B6, clinical factors, and drug-drug interaction on efavirenz concentrations in HIV/tuberculosis-coinfected patients.
Lueangniyomkul, A; Mankatitham, W; Manosuthi, S; Manosuthi, W; Nilkamhang, S; Sukasem, C; Sungkanuparph, S; Thongyen, S, 2013
)
0.39
"Drugs most likely to interact with combined oral contraceptives, transdermal and implant contraceptives include protease inhibitors, the NNRTIs efavirenz and nevirapine, and cobicistat-boosted elvitegravir."( Drug interactions between antiretrovirals and hormonal contraceptives.
Hills-Nieminen, C; Tseng, A, 2013
)
0.39
" Although antidepressants are prescribed to a significant proportion of patients treated with antiretrovirals, there are limited clinical data on drug-drug interactions."( Prediction of drug-drug interactions between various antidepressants and efavirenz or boosted protease inhibitors using a physiologically based pharmacokinetic modelling approach.
Almond, L; Back, D; Khoo, S; Kirov, A; Marzolini, C; Owen, A; Seden, K; Siccardi, M, 2013
)
0.39
" Pharmacokinetics and drug-drug interaction were simulated using the full physiologically based pharmacokinetic model implemented in the Simcyp™ ADME simulator."( Prediction of drug-drug interactions between various antidepressants and efavirenz or boosted protease inhibitors using a physiologically based pharmacokinetic modelling approach.
Almond, L; Back, D; Khoo, S; Kirov, A; Marzolini, C; Owen, A; Seden, K; Siccardi, M, 2013
)
0.39
"Simulated pharmacokinetics and drug-drug interactions were in concordance with available clinical data."( Prediction of drug-drug interactions between various antidepressants and efavirenz or boosted protease inhibitors using a physiologically based pharmacokinetic modelling approach.
Almond, L; Back, D; Khoo, S; Kirov, A; Marzolini, C; Owen, A; Seden, K; Siccardi, M, 2013
)
0.39
" These findings indicate that IVIVE is a useful tool for predicting drug-drug interactions and designing prospective clinical trials, giving insight into the variability of exposure, sample size and time-dependent induction or inhibition."( Prediction of drug-drug interactions between various antidepressants and efavirenz or boosted protease inhibitors using a physiologically based pharmacokinetic modelling approach.
Almond, L; Back, D; Khoo, S; Kirov, A; Marzolini, C; Owen, A; Seden, K; Siccardi, M, 2013
)
0.39
" Finally, observed/predicted drug-drug interactions between antiretrovirals and antifungals are summarized along with clinical recommendations."( Clinically relevant drug-drug interactions between antiretrovirals and antifungals.
Mitra, AK; Pal, D; Patel, M; Paturi, DK; Vadlapatla, RK, 2014
)
0.4
" Posaconazole is contraindicated in combination with either efavirenz or fosamprenavir."( Clinically relevant drug-drug interactions between antiretrovirals and antifungals.
Mitra, AK; Pal, D; Patel, M; Paturi, DK; Vadlapatla, RK, 2014
)
0.4
" Evaluation of a drug-drug interaction (DDI) study and supportive semi-mechanistic population pharmacokinetic (PK) analyses were undertaken to help delineate this issue."( Why did the FDA approve efavirenz 800 mg when co-administered with rifampin?
Arya, V; Chan-Tack, KM; Jadhav, P; Kraft, J; Liu, J; Robertson, SM; Seo, S; Singer, ME; Struble, KA, 2014
)
0.4
" Simulations compared EFV exposure at various doses in combination with RIF to EFV exposures at 600 mg once daily (QD)."( Why did the FDA approve efavirenz 800 mg when co-administered with rifampin?
Arya, V; Chan-Tack, KM; Jadhav, P; Kraft, J; Liu, J; Robertson, SM; Seo, S; Singer, ME; Struble, KA, 2014
)
0.4
"An in vivo study of efavirenz metabolites in rats and human patients with ultra high performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry combined with MetabolitePilot(MT) software is reported for the first time."( Rapid identification of efavirenz metabolites in rats and humans by ultra high performance liquid chromatography combined with quadrupole time-of-flight tandem mass spectrometry.
Deng, Y; Liang, J; Liu, R; Yang, P, 2015
)
0.42
" These predictions were in good agreement with clinical single dose drug-drug interaction studies, but not with reports of imatinib interactions at steady-state."( Human hepatocyte assessment of imatinib drug-drug interactions - complexities in clinical translation.
Beumer, JH; Christner, SM; Kiesel, BF; Parise, RA; Pillai, VC; Rudek, MA; Venkataramanan, R, 2015
)
0.42
" The 3D regimen of 150/100 mg daily paritaprevir/ritonavir, 25 mg daily ombitasvir, and 400 mg twice-daily dasabuvir was administered alone or in combination with 200 mg daily of emtricitabine and 300 mg daily of tenofovir disoproxil fumarate (tenofovir DF), 25 mg daily of rilpivirine, or 400 mg of raltegravir twice daily."( Evaluation of Drug-Drug Interactions between Direct-Acting Anti-Hepatitis C Virus Combination Regimens and the HIV-1 Antiretroviral Agents Raltegravir, Tenofovir, Emtricitabine, Efavirenz, and Rilpivirine.
Awni, W; Dunbar, M; Dutta, S; Khatri, A; Menon, R; Podsadecki, T; Trinh, R, 2016
)
0.43
" A clinical drug-drug interaction (DDI) study with the potent CYP3A4 inhibitor itraconazole resulted in an approximately sevenfold increase in cobimetinib exposure."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
0.43
" Three studies were conducted to evaluate the potential drug-drug interactions between delamanid and antiretroviral drugs, including ritonavir, a strong inhibitor of CYP3A4, and selected anti-TB drugs, including rifampin, a strong inducer of cytochrome P450 (CYP) isozymes."( Delamanid Coadministered with Antiretroviral Drugs or Antituberculosis Drugs Shows No Clinically Relevant Drug-Drug Interactions in Healthy Subjects.
Geiter, L; Mallikaarjun, S; Paccaly, A; Patil, S; Petersen, C; Shoaf, SE; Wells, C, 2016
)
0.43
"Antiretroviral drugs are among the therapeutic agents with the highest potential for drug-drug interactions (DDIs)."( Physiologically Based Pharmacokinetic Modeling to Predict Drug-Drug Interactions with Efavirenz Involving Simultaneous Inducing and Inhibitory Effects on Cytochromes.
Back, D; Battegay, M; Elzi, L; Marzolini, C; Rajoli, R; Siccardi, M, 2017
)
0.46
" Plasma drug-concentration profiles were simulated at steady state in virtual individuals for each drug given alone or in combination with efavirenz."( Physiologically Based Pharmacokinetic Modeling to Predict Drug-Drug Interactions with Efavirenz Involving Simultaneous Inducing and Inhibitory Effects on Cytochromes.
Back, D; Battegay, M; Elzi, L; Marzolini, C; Rajoli, R; Siccardi, M, 2017
)
0.46
"In general, DTG 50 mg given once daily combined with an active background drug is a better choice in terms of both efficacy and safety."( Dolutegravir(DTG, S/GSK1349572) combined with other ARTs is superior to RAL- or EFV-based regimens for treatment of HIV-1 infection: a meta-analysis of randomized controlled trials.
Chen, H; Guo, W; Huang, J; Jiang, J; Liang, B; Liang, H; Liao, Y; Su, J; Xu, X; Ye, L; Zang, N, 2016
)
0.43
"To determine which non-nucleoside reverse transcriptase inhibitor, either EFV or NVP, is more effective in suppressing viral load when given in combination with two nucleoside reverse transcriptase inhibitors as part of initial antiretroviral therapy for HIV infection in adults and children."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside or nucleotide-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, L; Mursleen, S; Rutherford, GW; Siegfried, N; Spaulding, AB, 2016
)
0.43
"Both drugs have similar benefits in initial treatment of HIV infection when combined with two NRTIs."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside or nucleotide-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, L; Mursleen, S; Rutherford, GW; Siegfried, N; Spaulding, AB, 2016
)
0.43
" The results of clinical pharmacokinetic (PK) studies indicate that guanfacine is sensitive to drug-drug interactions (DDIs) perpetrated by strong inhibitors and inducers of CYP3A4."( Development of Guanfacine Extended-Release Dosing Strategies in Children and Adolescents with ADHD Using a Physiologically Based Pharmacokinetic Model to Predict Drug-Drug Interactions with Moderate CYP3A4 Inhibitors or Inducers.
Li, A; Rong, H; Welty, D; Yeo, K, 2018
)
0.48
"To investigate clinically applicable dose-adjustment strategies to overcome the known drug-drug interaction (DDI) between levonorgestrel and efavirenz, using a physiologically based pharmacokinetic (PBPK) modelling-based approach."( Physiologically based pharmacokinetic modelling prediction of the effects of dose adjustment in drug-drug interactions between levonorgestrel contraceptive implants and efavirenz-based ART.
Back, DJ; Darin, KM; Fletcher, CV; Lamorde, M; Owen, A; Rajoli, RKR; Roberts, O; Scarsi, KK; Siccardi, M, 2018
)
0.48
" Conversely, increased-dose levonorgestrel in combination with either 600 or 400 mg of efavirenz was sufficient to restore levonorgestrel concentrations to levels similar to those observed in the 150 mg levonorgestrel control group 48 weeks post-implant-placement (efavirenz:control geometric mean ratio = 0."( Physiologically based pharmacokinetic modelling prediction of the effects of dose adjustment in drug-drug interactions between levonorgestrel contraceptive implants and efavirenz-based ART.
Back, DJ; Darin, KM; Fletcher, CV; Lamorde, M; Owen, A; Rajoli, RKR; Roberts, O; Scarsi, KK; Siccardi, M, 2018
)
0.48
" Therefore, a clinical drug-drug interaction (DDI) study to evaluate the effects of evocalcet on the pharmacokinetics (PKs) of probe substrates for CYP isozymes (CYP1A2, CYP2B6, CYP2C8, CYP2C9, and CYP3A) was conducted in healthy male volunteers using a novel cocktail combination."( Assessment of CYP-Mediated Drug Interactions for Evocalcet, a New Calcimimetic Agent, Based on In Vitro Investigations and a Cocktail Study in Humans.
Akizawa, T; Endo, Y; Fukagawa, M; Kannami, A; Maeda, H; Nagata, Y; Nakamura, H; Narushima, K; Ohtsuka, S; Shimazaki, R; Shiramoto, M; Uchimura, T, 2019
)
0.51
"To investigate the genetic contribution to this previously observed drug-drug interaction through studying SNPs in genes known to be involved in efavirenz, nevirapine or etonogestrel metabolism in the same group of women."( Effect of patient genetics on etonogestrel pharmacokinetics when combined with efavirenz or nevirapine ART.
Achilles, SL; Chappell, CA; Chen, BA; Lamorde, M; Matovu, J; Nakalema, S; Neary, M; Owen, A; Scarsi, KK; Siccardi, M, 2019
)
0.51
"This study demonstrates the influence of pharmacogenetics on the extent of drug-drug interactions between etonogestrel and efavirenz- or nevirapine-based ART."( Effect of patient genetics on etonogestrel pharmacokinetics when combined with efavirenz or nevirapine ART.
Achilles, SL; Chappell, CA; Chen, BA; Lamorde, M; Matovu, J; Nakalema, S; Neary, M; Owen, A; Scarsi, KK; Siccardi, M, 2019
)
0.51
"Open-label Phase 2 drug-drug interaction randomized trial."( Effect of high-dose rifampicin on efavirenz pharmacokinetics: drug-drug interaction randomized trial.
Atwine, D; Barrail-Tran, A; Baudin, E; Bonnet, M; Furlan, V; Gelé, T; K T Nanjebe, D; Kananura, K; Kyohairwe, R; Muyindike, W; Mworozi, K; Nyehangane, D; Orikiriza, P; Taburet, AM; Verstuyft, C, 2020
)
0.56
" This warrants further investigations of other drug-drug interactions for optimising dosing in genetically defined subgroups, particularly during drug development."( Influence of selected polymorphisms in disposition genes on lumefantrine pharmacokinetics when coadministered with efavirenz.
Adeagbo, BA; Adegbola, AJ; Bolaji, OO; Bolarinwa, RA; Olagunju, AE; Owen, A; Rana, A; Siccardi, M, 2020
)
0.56
" We investigated pregnancy-induced and pharmacogenetic-associated pharmacokinetic changes and drug-drug interactions between isoniazid and efavirenz in pregnant women."( Pharmacokinetics and Drug-Drug Interactions of Isoniazid and Efavirenz in Pregnant Women Living With HIV in High TB Incidence Settings: Importance of Genotyping.
Aaron, L; Aurpibul, L; Bhosale, R; Bradford, S; Browning, R; Chakhtoura, N; Chanaiwa, V; Chipato, T; Costello, D; Denti, P; Gausi, K; Gupta, A; Haas, DW; Hesseling, A; Jean-Philippe, P; Kabugho, E; Masheto, GR; McCarthy, K; Mhembere, T; Mmbaga, BT; Montepiedra, G; Mutambanengwe, M; Nevrekhar, N; Norman, J; Nyati, M; Onyango-Makumbi, C; Rouzier, V; Shin, K; Sterling, TR; Stranix-Chibanda, L; Theron, G; Tongprasert, F; Vhembo, T; Violari, A; Wallis, CL; Weinberg, A; Wiesner, L; Zimmer, B, 2021
)
0.62
" Due to its widespread use and CYP3A4-mediated metabolism, there is concern regarding drug-drug interactions (DDIs), particularly a suboptimal LNG exposure when co-administered with CYP3A4 inducers, potentially leading to unintended pregnancies."( Quantitative Assessment of Levonorgestrel Binding Partner Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling.
Chaturvedula, A; Cicali, B; Cristofoletti, R; Hoechel, J; Lingineni, K; Schmidt, S; Vozmediano, V; Wendl, T; Wiesinger, H, 2021
)
0.62
"To assess the pharmacokinetic of itraconazole capsule formulation and its active metabolite, hydroxyitraconazole, in adults with HIV diagnosed with talaromycosis in an endemic area, and to evaluate the drug-drug interaction between itraconazole/hydroxyitraconazole (ITC/OH-ITC) and efavirenz."( Drug-drug interaction between itraconazole capsule and efavirenz in adults with HIV for talaromycosis treatment.
Chaiwarith, R; Chindamporn, A; Cressey, TR; Kaewpoowat, Q; Sirisanthana, T; Worasilchai, N; Yasri, S, 2021
)
0.62
" The clinical impact of this drug-drug interaction on talaromycosis treatment or prophylaxis in the era of potent ART needs further evaluation."( Drug-drug interaction between itraconazole capsule and efavirenz in adults with HIV for talaromycosis treatment.
Chaiwarith, R; Chindamporn, A; Cressey, TR; Kaewpoowat, Q; Sirisanthana, T; Worasilchai, N; Yasri, S, 2021
)
0.62
"To evaluate the effect of methadone maintenance treatment (MMT) combined with rilpivirine (RPV)-based regimens on drug use of HIV individuals."( Outcomes of Methadone Maintenance Therapy Combined with Rilpivirine/Efavirenz in Treatment-Naive HIV-Infected Patients.
Dong, X; Hong, L; Huang, S; Lei, S; Li, H; Li, X; Xie, R; Xin, J; Yang, C; Yang, X; Zhang, B; Zhang, R, 2021
)
0.62
"This study was a prospective, open-label, controlled, drug-drug interaction trial at a single center for 24 weeks."( Outcomes of Methadone Maintenance Therapy Combined with Rilpivirine/Efavirenz in Treatment-Naive HIV-Infected Patients.
Dong, X; Hong, L; Huang, S; Lei, S; Li, H; Li, X; Xie, R; Xin, J; Yang, C; Yang, X; Zhang, B; Zhang, R, 2021
)
0.62
" As medroxyprogesterone acetate is a cytochrome P450 (CYP3A4) substrate, drug-drug interactions (DDIs) with antiretroviral or antituberculosis treatment may lead to subtherapeutic medroxyprogesterone acetate concentrations (< 0."( A Semimechanistic Pharmacokinetic Model for Depot Medroxyprogesterone Acetate and Drug-Drug Interactions With Antiretroviral and Antituberculosis Treatment.
Cohn, SE; Denti, P; Dooley, KE; Firnhaber, C; Francis, J; Godfrey, C; Kendall, MA; McIlleron, H; Mngqibisa, R; Wu, X, 2021
)
0.62
"To determine if double-dose levonorgestrel emergency contraception (EC) in combination with efavirenz or rifampicin, 2 drugs known to decrease levonorgestrel exposure, resulted in similar pharmacokinetics compared to standard-dose levonorgestrel EC without drug-drug interactions."( Pharmacokinetics of dose-adjusted levonorgestrel emergency contraception combined with efavirenz-based antiretroviral therapy or rifampicin-containing tuberculosis regimens.
Badal-Faesen, S; Barr, E; Belaunzaran-Zamudio, PF; Cohn, SE; Gadama, L; Gatechompol, S; Godfrey, C; Jalil, EM; Mawlana, S; Mngqibisa, R; Olefsky, M; Pham, M; Podany, AT; Scarsi, KK; Smeaton, LM; Supparatpinyo, K; Woolley, E, 2023
)
0.91
"The predictive performance of the PBPK model to simulate dolutegravir and raltegravir pharmacokinetics and to reproduce the strength of induction was verified using clinical drug-drug interaction studies (steady-state induction) and switch studies (residual induction)."( Management of Drug Interactions with Inducers: Onset and Disappearance of Induction on Cytochrome P450 3A4 and Uridine Diphosphate Glucuronosyltransferase 1A1 Substrates.
Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023
)
0.91
" To this end, the drug-drug interaction between efavirenz and the uridine 5'-diphospho-glucuronosyltransferase 1A1 substrates dolutegravir and raltegravir was first simulated in nonpregnant subjects."( Mechanistic Modeling of the Drug-Drug Interaction Between Efavirenz and Dolutegravir: Is This Interaction Clinically Relevant When Switching From Efavirenz to Dolutegravir During Pregnancy?
Ahmadzia, HK; Dallmann, A; Rakhmanina, N; van den Anker, J, 2023
)
0.91

Bioavailability

Efavirenz (EFV; aqueous solubility 4 microg/ml, bioavailability 40-45%) is a first-line agent in the pediatric therapeutic cocktail. HIV/AIDS disease is associated with reduced relative bioavailability of efavirensz. The current study was aimed to prepare SNEDDS to augmentsolubility, release rate, and oral bioavailability.

ExcerptReferenceRelevance
" Studies of L-743, 726 in rats, monkeys, and a chimpanzee demonstrated the compound's potential for good oral bioavailability and pharmacokinetics in humans."( L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase.
Anderson, PS; Britcher, SF; Carroll, SS; Huff, JR; Lumma, WC; Lyle, TA; Olsen, DB; Payne, LS; Tran, LO; Young, SD, 1995
)
0.29
" After oral dosing, the bioavailability of EFV in rats (10 mg/kg) and monkeys (2 mg/kg) was 16% and 42%, respectively."( Nonlinear pharmacokinetics of efavirenz (DMP-266), a potent HIV-1 reverse transcriptase inhibitor, in rats and monkeys.
Balani, SK; deLuna, FA; Kauffman, LR; Lin, JH, 1999
)
0.3
" Preliminary pharmacokinetics in rats showed that compound 18 is orally bioavailable and penetrates well into the brain."( Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
Bäckbro, K; Engelhardt, P; Fridborg, K; Högberg, M; Johansson, NG; Kangasmetsä, J; Lövgren, S; Noréen, R; Oberg, B; Sahlberg, BL; Sahlberg, C; Unge, T; Vrang, L; Zhang, H, 1999
)
0.3
" The best compounds are potent orally bioavailable inhibitors of both wild-type HIV-1 and its clinically relevant K103N mutant virus, but are highly protein-bound in human plasma."( 4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
Bacheler, LT; Chidester, DR; Cocuzza, AJ; Cordova, BC; Diamond, S; Erickson-Viitanen, SK; Jeffrey, S; Klabe, RM; Ko, SS; Rodgers, JD; Weigelt, CA, 2001
)
0.31
" Through an integrated effort involving synthesis, docking studies, and biological and pharmacokinetic evaluation, we investigated the structural dependence of the poor bioavailability and rapid clearance within the thioureidic series of antivirals."( Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
Aiello, F; Armaroli, S; Bergamini, A; Bolacchi, F; Bongiovanni, B; Caccia, S; Campiani, G; Capozzi, M; Coletta, M; Fabbrini, M; Garofalo, A; Greco, G; Guiso, G; Maga, G; Marini, S; Morelli, E; Nacci, V; Novellino, E; Ramunno, A; Spadari, S; Ventura, L, 2001
)
0.31
" Volume of distribution and absorption rate constant were 77."( Nevirapine and efavirenz pharmacokinetics and covariate analysis in the 2NN study.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, J; MacGregor, TR; van Leth, F, 2005
)
0.33
"Ideally, an anti-HIV drug should (1) be highly active against wild-type and mutant HIV without allowing breakthrough; (2) have high oral bioavailability and long elimination half-life, allowing once-daily oral treatment at low doses; (3) have minimal adverse effects; and (4) be easy to synthesize and formulate."( In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
Andries, K; Arnold, E; Bohets, H; Clark, AD; Daeyaert, F; Das, K; de Béthune, MP; De Clerck, F; de Jonge, M; De Knaep, F; Frenkel, YV; Guillemont, J; Heeres, J; Hughes, SH; Janssen, PA; Koymans, L; Kukla, M; Lampo, A; Lewi, PJ; Ludovici, D; Medaer, B; Pasquier, E; Pauwels, R; Stoffels, P; Vinkers, M; Williams, P, 2005
)
0.33
" Asian race and baseline total bilirubin (TBR) increased the relative bioavailability of efavirenz by 56% and 57%, respectively."( Population pharmacokinetics of efavirenz in an unselected cohort of HIV-1-infected individuals.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Meenhorst, PL; Mulder, JW; Prins, JM; Yalvaç, Z, 2005
)
0.33
" Asian race and baseline TBR were found to be significantly correlated with the bioavailability of efavirenz."( Population pharmacokinetics of efavirenz in an unselected cohort of HIV-1-infected individuals.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Meenhorst, PL; Mulder, JW; Prins, JM; Yalvaç, Z, 2005
)
0.33
"0%, suggesting that the two capsule formulations resulted in similar rate and extent of bioavailability under fasting conditions."( Comparative bioavailability of a generic capsule formulation of the reverse transcriptase inhibitor efavirenz and the innovator product.
Al-Numani, D; Di Marco, M; Garg, M; Marier, JF; Monif, T; Morelli, G; Morin, I; Singla, AK; Stiles, M; Tippabhotla, SK; Vijan, T, 2006
)
0.33
" Pharmacokinetic studies of 5a in rat and dog demonstrated that this compound has good oral bioavailability in animal species."( Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Dunn, JP; Dunten, P; Elworthy, TR; Han, X; Harris, SF; Heilek, G; Hirschfeld, DR; Hogg, JH; Huber, W; Kaiser, AC; Kertesz, DJ; Kim, W; Klumpp, K; Li, Y; Mirzadegan, T; Roepel, MG; Saito, YD; Silva, TM; Swallow, S; Sweeney, ZK; Tracy, JL; Villasenor, A; Vora, H; Zhou, AS, 2008
)
0.35
" Further refinement of key compounds in this series to optimize physical properties and pharmacokinetics has resulted in the identification of 8e (MK-4965), which has high levels of potency against wild-type and key mutant viruses, excellent oral bioavailability and overall pharmacokinetics, and a clean ancillary profile."( Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
Felock, PJ; Flynn, JA; Lai, MT; Liang, Y; Liu, M; McGaughey, G; Miller, M; Moyer, G; Munshi, V; Perlow-Poehnelt, R; Prasad, S; Reid, JC; Sanchez, R; Sisko, JT; Torrent, M; Tucker, TJ; Tynebor, RM; Vacca, JP; Wan, BL; Williams, TM; Yan, Y, 2008
)
0.35
" Efavirenz relative bioavailability was 26% higher in subjects homozygous for ABCB1 (rs3842)."( A novel polymorphism in ABCB1 gene, CYP2B6*6 and sex predict single-dose efavirenz population pharmacokinetics in Ugandans.
Aklillu, E; Andersson, M; Fukasawa, T; Gustafsson, LL; Milani, L; Mukonzo, JK; Ogwal-Okeng, J; Röshammar, D; Svensson, JO; Waako, P, 2009
)
0.35
" Efavirenz (EFV; aqueous solubility 4 microg/ml, bioavailability 40-45%) is a first-line agent in the pediatric therapeutic cocktail."( Efavirenz-loaded polymeric micelles for pediatric anti-HIV pharmacotherapy with significantly higher oral bioavailability [corrected].
Chiappetta, DA; Hocht, C; Sosnik, A; Taira, C, 2010
)
0.36
"To encapsulate EFV in polymeric micelles to improve the aqueous solubility and the the oral bioavailability of the drug."( Efavirenz-loaded polymeric micelles for pediatric anti-HIV pharmacotherapy with significantly higher oral bioavailability [corrected].
Chiappetta, DA; Hocht, C; Sosnik, A; Taira, C, 2010
)
0.36
"This work demonstrates that the encapsulation of EFV, which is poorly water soluble, into polymeric micelles of different poly(ethylene oxide)-poly(propylene oxide) block copolymers significantly improves the oral bioavailability of the drug, and reduces the interindividual variability."( Efavirenz-loaded polymeric micelles for pediatric anti-HIV pharmacotherapy with significantly higher oral bioavailability [corrected].
Chiappetta, DA; Hocht, C; Sosnik, A; Taira, C, 2010
)
0.36
"The effect of mixing the contents of efavirenz capsules (sprinkles) with a small amount of food on the bioavailability and pharmacokinetics of efavirenz in healthy adults was evaluated."( Bioavailability in healthy adults of efavirenz capsule contents mixed with a small amount of food.
Grasela, D; Ji, P; Kaul, S; Lu, M; Nguyen, KL; Shangguan, T, 2010
)
0.36
" To assure therapeutic plasma concentrations, the low oral bioavailability demands the administration of relatively high EFV doses."( A highly concentrated and taste-improved aqueous formulation of efavirenz for a more appropriate pediatric management of the anti-HIV therapy.
Chiappetta, DA; Hocht, C; Sosnik, A, 2010
)
0.36
" A two-compartment model in which the slope of distribution is assumed to be equal to the absorption rate constant adequately described the data."( Is the recommended once-daily dose of lamivudine optimal in West African HIV-infected children?
Bardin, C; Blanche, S; Bouazza, N; Diagbouga, S; Hien, H; Hirt, D; Msellati, P; Nacro, B; Ouiminga, A; Rouet, F; Tréluyer, JM; Urien, S; Van De Perre, P; Zoure, E, 2010
)
0.36
" The aqueous solubility of the drug was increased more than 8400 times (up to 34mg/mL) and preliminary preclinical data suggested the significantly greater oral bioavailability with respect to an extemporaneous suspension and an oleous solution (similar to the only "commercially available" pediatric formulation)."( Oral pharmacokinetics of the anti-HIV efavirenz encapsulated within polymeric micelles.
Chiappetta, DA; Hocht, C; Sosnik, A; Taira, C, 2011
)
0.37
" This study evaluated efavirenz bioavailability after rifampicin administration to healthy volunteers."( Pharmacokinetic interaction between efavirenz and rifampicin in healthy volunteers.
Djoerban, Z; Setiabudy, R, 2011
)
0.37
"Co-administration of a single dose of efavirenz 600 mg/day with 1-week rifampicin 450 mg/day significantly reduced efavirenz bioavailability in healthy volunteers."( Pharmacokinetic interaction between efavirenz and rifampicin in healthy volunteers.
Djoerban, Z; Setiabudy, R, 2011
)
0.37
"63), while HIV/AIDS patients were found to have 30% lower relative bioavailability (95% CI 18."( HIV/AIDS patients display lower relative bioavailability of efavirenz than healthy subjects.
Aklillu, E; Ashton, M; Gustafsson, LL; Mukonzo, JK; Nanzigu, S; Ogwal-Okeng, J; Rekić, D; Röshammar, D; Waako, P, 2011
)
0.37
" HIV/AIDS disease is associated with reduced relative bioavailability of efavirenz."( HIV/AIDS patients display lower relative bioavailability of efavirenz than healthy subjects.
Aklillu, E; Ashton, M; Gustafsson, LL; Mukonzo, JK; Nanzigu, S; Ogwal-Okeng, J; Rekić, D; Röshammar, D; Waako, P, 2011
)
0.37
"The oral bioavailability of the antiretroviral efavirenz (EFV) undergoes high inter and intra-individual variability, this fact supporting its therapeutic drug monitoring."( Efavirenz is a substrate and in turn modulates the expression of the efflux transporter ABCG2/BCRP in the gastrointestinal tract of the rat.
Bramuglia, GF; Chiappetta, DA; Di Gennaro, SS; Hocht, C; Peroni, RN; Rubio, MC; Sosnik, A, 2011
)
0.37
" Bioavailability decreased."( Mechanism of efavirenz influence on methadone pharmacokinetics and pharmacodynamics.
Bedynek, PS; Campbell, S; Crafford, A; Ensign, D; Hoffer, C; Kharasch, ED; Kim, T; London, A; Stubbert, K; Whittington, D, 2012
)
0.38
" The developed EFV-loaded particles appear as a useful platform to investigate the intranasal administration to increase the bioavailability in the CNS."( Poly(ε-caprolactone), Eudragit® RS 100 and poly(ε-caprolactone)/Eudragit® RS 100 blend submicron particles for the sustained release of the antiretroviral efavirenz.
Chiappetta, DA; Seremeta, KP; Sosnik, A, 2013
)
0.39
"The bioavailability of the drug in the CNS was increased fourfold and the relative exposure index (ratio between the area under the curve in the CNS and plasma) was increased fivefold with respect to the same system administered intravenously."( Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV.
Chiappetta, DA; Hocht, C; Opezzo, JA; Sosnik, A, 2013
)
0.39
"The purpose of this study was to develop NS of efavirenz (EFV) and to investigate its potential in enhancing the oral bioavailability of EFV."( Nanosuspension of efavirenz for improved oral bioavailability: formulation optimization, in vitro, in situ and in vivo evaluation.
Patel, GV; Patel, VB; Pathak, A; Rajput, SJ, 2014
)
0.4
"Thus, it can be concluded that NS formulation of EFV can provide improved oral bioavailability due to enhanced solubility, dissolution velocity, permeability and hence absorption."( Nanosuspension of efavirenz for improved oral bioavailability: formulation optimization, in vitro, in situ and in vivo evaluation.
Patel, GV; Patel, VB; Pathak, A; Rajput, SJ, 2014
)
0.4
" The simulation of gastrointestinal bioavailability and IVIVC obtained from immediate-release tablet formulations suggests that GastroPlus™ is a valuable in silico method for IVIVC and for studies directed at developing formulations of class II drugs."( In vitro-in vivo correlation of efavirenz tablets using GastroPlus®.
Cabral, LM; Castro, HC; de Sousa, VP; dos Santos, TC; Esteves, VS; Honório, Tda S; Pinto, EC; Rocha, HV; Rodrigues, CR, 2013
)
0.39
" In vivo studies confirm bioavailability benefits with an approximately four-fold higher pharmacokinetic exposure after oral administration to rodents, and predictive modeling suggests dose reduction with the new formulation may be possible."( Antiretroviral solid drug nanoparticles with enhanced oral bioavailability: production, characterization, and in vitro-in vivo correlation.
Curley, P; Foster, AJ; Giardiello, M; Khoo, SH; Liptrott, NJ; Long, J; Martin, P; McDonald, TO; Owen, A; Rannard, SP; Roberts, P; Schipani, A; Siccardi, M; Smith, D, 2014
)
0.4
" Subjects taking concomitant PIs exhibited increases in CsA and TAC exposure (AUC/dose) due to the increased apparent oral bioavailability and decreased apparent oral clearance."( Changes in clearance, volume and bioavailability of immunosuppressants when given with HAART in HIV-1 infected liver and kidney transplant recipients.
Barin, B; Benet, L; Browne, M; Carlson, L; Christians, U; Floren, L; Frassetto, L; Roland, M; Stock, P; Wolfe, A, 2013
)
0.39
"The aim of the present study was to prepare surface stabilized nanoparticles for oral bioavailability enhancement of efavirenz (EFZ)."( Surface stabilized efavirenz nanoparticles for oral bioavailability enhancement.
Agrawal, AK; Jain, S; Mahajan, RR; Sharma, JM, 2013
)
0.39
" The liquid formulation bioavailability relative to the capsule was found to increase with age to reach 90% of its mature value by the age of 8 years."( Pharmacometric characterization of efavirenz developmental pharmacokinetics and pharmacogenetics in HIV-infected children.
Brundage, RC; Fletcher, CV; Salem, AH, 2014
)
0.4
"The objective of the present work is to develop a dose adjustable nanotechnology based liquid formulation of efavirenz with improved bioavailability for HIV therapy."( Anti HIV nanoemulsion formulation: optimization and in vitro-in vivo evaluation.
Ali, J; Ansari, SH; Khan, AW; Kotta, S; Sharma, RK, 2014
)
0.4
"The EFV-based HAART regimen was associated with a reduction in the bioavailability of ENG, which showed decreases of 63."( Effect of antiretroviral therapy including lopinavir/ritonavir or efavirenz on etonogestrel-releasing implant pharmacokinetics in HIV-positive women.
Amaral, E; Bahamondes, L; Bahamondes, MV; Brito, MB; de Souza, RM; Duarte, G; Ferriani, RA; Quintana, SM; Rocha Prandini, TR; Scaranari, C; Vieira, CS, 2014
)
0.4
"The coadministration of EFV decreased the bioavailability of ENG released from the implant, which could impair contraceptive efficacy."( Effect of antiretroviral therapy including lopinavir/ritonavir or efavirenz on etonogestrel-releasing implant pharmacokinetics in HIV-positive women.
Amaral, E; Bahamondes, L; Bahamondes, MV; Brito, MB; de Souza, RM; Duarte, G; Ferriani, RA; Quintana, SM; Rocha Prandini, TR; Scaranari, C; Vieira, CS, 2014
)
0.4
"Solid lipid nanoparticle is an efficient lipid based drug delivery system which can enhance the bioavailability of poorly water soluble drugs."( Enhanced oral bioavailability of efavirenz by solid lipid nanoparticles: in vitro drug release and pharmacokinetics studies.
Bajpai, M; Gaur, PK; Mishra, A; Mishra, S, 2014
)
0.4
"Due to the differences between bioavailability of efavirenz (EFV) and tenofovir (TDF), the single-tablet regimen of EFV/emtricitabine (FTC)/TDF is not approved as initial antiretroviral therapy (ART) in Europe by the European Medical Agency."( Safety and efficacy of coformulated efavirenz/emtricitabine/tenofovir single-tablet regimen in treatment-naive patients infected with HIV-1.
De Castro, N; Delaugerre, C; Flandre, P; Gallien, S; Molina, JM; Nguyen, N, 2015
)
0.42
" A 30 mg/mL solution in a medium-chain triglyceride vehicle is the only pediatric formulation available with an oral bioavailability 20% lower than the solid form."( Formulation and development of bicontinuous nanostructured liquid crystalline particles of efavirenz.
Avachat, AM; Parpani, SS, 2015
)
0.42
"Polymorphism and particle size distribution can impact the dissolution behaviour and, as a consequence, bioavailability and bioequivalence of poorly soluble drugs, such as Efavirenz (EFV)."( Correlation between microstructure and bioequivalence in anti-HIV drug efavirenz.
Azanza Ricardo, CL; Cuffini, SL; de Santana, DP; Fandaruff, C; Galindo Bedor, DC; Rebuffi, L; Rocha, HV; Scardi, P; Segatto Silva, MA, 2015
)
0.42
" Its erratic oral absorption and poor bioavailability make it a potential candidate for being formulated as a nanosuspension."( Formulation and optimization of efavirenz nanosuspensions using the precipitation-ultrasonication technique for solubility enhancement.
Khatri, K; Shilpi, S; Taneja, S, 2016
)
0.43
" Compared to RRC, Ugandan children exhibited reduced bioavailability of EFV and LPV; 11% (P=0."( The effect of malnutrition on the pharmacokinetics and virologic outcomes of lopinavir, efavirenz and nevirapine in food insecure HIV-infected children in Tororo, Uganda.
Achan, J; Aweeka, F; Bartelink, IH; Capparelli, E; Charlebois, E; Dorsey, G; Gingrich, D; Havlir, D; Jullien, V; Kamya, M; Plenty, A; Ruel, T; Savic, RM; Scherpbier, HJ; Young, SL, 2015
)
0.42
" Patients in the EFV-arm but not in the NVP-arm had significantly lower lumefantrine bioavailability compared to that in the control-arm."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.42
"Co-treatment of AL with EFV-based ART but not NVP-based ART significantly reduces lumefantrine bioavailability and consequently total exposure."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.42
" Thus, PA-SLN improved the EFV bioavailability and maintained therapeutic levels in the brain for an extended period of time that can result in significant eradication of the viral load therein."( Targeting of AIDS related encephalopathy using phenylalanine anchored lipidic nanocarrier.
Hurkat, P; Jain, A; Jain, SK; Vyas, A, 2015
)
0.42
"Over the past few decades, nanocrystal formulations have evolved as promising drug delivery systems owing to their ability to enhance the bioavailability and maintain the stability of poorly water-soluble drugs."( Conjugation of Hot-Melt Extrusion with High-Pressure Homogenization: a Novel Method of Continuously Preparing Nanocrystal Solid Dispersions.
Feng, X; Gryczke, A; Kolter, K; Langley, N; Lu, J; Majumdar, S; Mishra, SR; Neupane, D; Patil, H; Repka, MA; Tiwari, RV; Ye, X, 2016
)
0.43
"70%) of the EFV reaching to liver indicates that major amount of EFV bypasses the liver and thereby, enhances the oral bioavailability of the EFV."( Solid lipid nanoparticles (SLN) of Efavirenz as lymph targeting drug delivery system: Elucidation of mechanism of uptake using chylomicron flow blocking approach.
Jain, R; Joshi, A; Makwana, V; Nivsarkar, M; Patel, K, 2015
)
0.42
" The current study was aimed to prepare SNEDDS to augment solubility, release rate, and oral bioavailability of BCS class II drug, efavirenz (EFV)."( Efavirenz Self-Nano-Emulsifying Drug Delivery System: In Vitro and In Vivo Evaluation.
Kamble, RN; Kumar, A; Mehta, PP, 2016
)
0.43
"Although sex-related differences in gastrointestinal physiology have been vastly reported, its impact on drug oral bioavailability and bioequivalence (product discrimination) is often ignored."( Sex-by-formulation interaction assessed through a bioequivalence study of efavirenz tablets.
Fagiolino, P; Ibarra, M; Lorier, M; Magallanes, L; Vázquez, M, 2016
)
0.43
" Body weight was identified as a significant predictor of efavirenz apparent clearance (CL), oral central volume of distribution (VC), and absorption rate constant (Ka)."( Population Pharmacokinetics Analysis To Inform Efavirenz Dosing Recommendations in Pediatric HIV Patients Aged 3 Months to 3 Years.
Bertz, R; Chapel, S; Cirincione, B; Luo, M; Roy, A; Savant, I; Sevinsky, H, 2016
)
0.43
"This study aims to develop a self-nanoemulsifying drug delivery system (SNEDDS) based on non-ionic surfactant mixtures to improve the oral bioavailability of efavirenz (EFZ) categorized as a class II according to the BCS, for HIV- therapy."( Mixed surfactant based (SNEDDS) self-nanoemulsifying drug delivery system presenting efavirenz for enhancement of oral bioavailability.
Sahoo, SK; Sahu, AN; Senapati, PC, 2016
)
0.43
" In conclusion, ECNPs are significantly safe and exhibit higher bioavailability thus constitute an effective MPT against HIV."( Triple combination MPT vaginal microbicide using curcumin and efavirenz loaded lactoferrin nanoparticles.
Bhaskar, C; Kishore, G; Kondapi, AK; Kumar, P; Lakshmi, YS, 2016
)
0.43
" Co-administration with some antiretroviral therapies (ART) changes the bioavailability of the etonogestrel (ENG)-releasing contraceptive implant, possibly affecting the bleeding pattern."( Bleeding patterns of HIV-infected women using an etonogestrel-releasing contraceptive implant and efavirenz-based or lopinavir/ritonavir-based antiretroviral therapy.
Amaral, E; Bahamondes, L; Bahamondes, MV; Brito, MB; Duarte, G; Ferriani, RA; Prandini, TR; Quintana, SM; Ragazini, CS; Vieira, CS, 2016
)
0.43
" It is poorly soluble and exhibits variable bioavailability hence, a high oral dose is recommended for therapy."( Engineered nanoparticles of Efavirenz using methacrylate co-polymer (Eudragit-E100) and its biological effects in-vivo.
Dhevendaran, K; Hari, BNV; Narayanan, N; Ramyadevi, D, 2016
)
0.43
" This study investigated the differences in bioavailability between WHO-prequalified first-line antiretroviral generics by means of adjusted indirect comparisons to ensure interchangeability between these generics."( Interchangeability between first-line generic antiretroviral products prequalified by WHO using adjusted indirect comparisons.
García-Arieta, A; Gordon, J; Gwaza, L; Leufkens, H; Potthast, H; Stahl, M; Welink, J, 2017
)
0.46
" Ternary nanosponge complexes were found to have 2-fold increase in oral bioavailability of efavirenz as compared to plain drug."( Enhancement of Bioavailability of Non-nucleoside Reverse Transciptase Inhibitor Using Nanosponges.
Rao, MRP; Shirsath, C, 2017
)
0.46
"To enhance efficacy, bioavailability and reduce toxicity of first-line highly active anti-retroviral regimen, zidovudine + efavirenz + lamivudine loaded lactoferrin nanoparticles were prepared (FLART-NP) and characterized for physicochemical properties, bioactivity and pharmacokinetic profile."( Triple Drug Combination of Zidovudine, Efavirenz and Lamivudine Loaded Lactoferrin Nanoparticles: an Effective Nano First-Line Regimen for HIV Therapy.
Kondapi, AK; Kumar, P; Lakshmi, YS, 2017
)
0.46
" Decreased bioavailability and increased toxicity limit its use."( An oral formulation of efavirenz-loaded lactoferrin nanoparticles with improved biodistribution and pharmacokinetic profile.
Kondapi, AK; Kumar, P; Lakshmi, YS, 2017
)
0.46
"Compared with free EFV, lacto-EFV-nano is a promising oral nanoformulation with enhanced bioavailability and efficacy of EFV and improved safety."( An oral formulation of efavirenz-loaded lactoferrin nanoparticles with improved biodistribution and pharmacokinetic profile.
Kondapi, AK; Kumar, P; Lakshmi, YS, 2017
)
0.46
"The nonnucleoside reverse transcriptase inhibitors, used for the treatment of HIV infections, are reported to have low bioavailability pertaining to high first-pass metabolism, high protein binding, and enzymatic metabolism."( Systematic Approach for the Formulation and Optimization of Solid Lipid Nanoparticles of Efavirenz by High Pressure Homogenization Using Design of Experiments for Brain Targeting and Enhanced Bioavailability.
Chotai, N; Gupta, S; Kesarla, R; Misra, A; Omri, A, 2017
)
0.46
" Enhanced CNS bioavailability (12."( Intranasal chitosan-g-HPβCD nanoparticles of efavirenz for the CNS targeting.
Belgamwar, A; Khan, S; Yeole, P, 2018
)
0.48
"Efavirenz is a fundamental drug in the HIV therapy; however, it has a low bioavailability due to low water solubility."( Efavirenz Dissolution Enhancement IV-Antisolvent Nanocrystallization by Sonication, Physical Stability, and Dissolution.
Prado, LD; Rocha, HVA; Sartori, GJ, 2017
)
0.46
" The modeled hepatic intrinsic clearances were also significantly associated with the P450 2C9 genotypes, however, absorption rate constants or volumes of the systemic circulation were not likely determining factors for the individual efavirenz clearance variations in the six cynomolgus monkeys."( Efavirenz clearances in vitro and in vivo in six cynomolgus monkeys associated with polymorphic cytochrome P450 2C9 and simulated by individual physiologically based pharmacokinetic models.
Kusama, T; Miura, T; Shimizu, M; Uehara, S; Uno, Y; Utoh, M; Yamazaki, H, 2017
)
0.46
" We hypothesized that the presence of multiple drugs would reduce crystallization tendency, thereby providing stable, supersaturating formulations for bioavailability enhancement."( Multidrug, Anti-HIV Amorphous Solid Dispersions: Nature and Mechanisms of Impacts of Drugs on Each Other's Solution Concentrations.
Arca, HÇ; Dahal, D; Edgar, KJ; Mosquera-Giraldo, LI; Taylor, LS, 2017
)
0.46
"Recent work has developed solid drug nanoparticles (SDNs) of efavirenz that have been demonstrated, preclinically, improved oral bioavailability and the potential to enable up to a 50% dose reduction, and is currently being studied in a healthy volunteer clinical trial."( Assessment of interactions of efavirenz solid drug nanoparticles with human immunological and haematological systems.
Giardiello, M; Liptrott, NJ; McDonald, TO; Owen, A; Rannard, SP, 2018
)
0.48
" The versatile HA-PQ10 entrapped all drugs and achieved an enhanced relative bioavailability of EFV, TDF, and FTC compared to the market formulation for potentially enhanced HIV treatment."( 3D printed, controlled release, tritherapeutic tablet matrix for advanced anti-HIV-1 drug delivery.
Choonara, YE; du Toit, LC; Kondiah, PPPD; Kumar, P; Pillay, V; Siyawamwaya, M, 2019
)
0.51
" The effect of the mechanical activation on the dissolution behavior and bioavailability was investigated revealing possible correlations with the grinding action, in terms of crystallinity, particle size and morphology."( Mechanical activation of Efavirenz: the effects on the dissolution and inhibitory behavior.
Cappelletto, E; Firrito, C; Pizzato, M; Rebuffi, L; Scardi, P, 2018
)
0.48
"Present investigation aimed to prepare, optimise, and characterise lipid nanocapsules (LNCs) for improving the solubility and bioavailability of efavirenz (EFV)."( Efavirenz oral delivery via lipid nanocapsules: formulation, optimisation, and ex-vivo gut permeation study.
Alizadeh, A; Jahanian-Najafabadi, A; Taymouri, S; Varshosaz, J, 2018
)
0.48
" Recent studies indicate that the bioavailability is higher for antiretroviral drugs delivered by LFNPs than when the drugs are administered alone."( Evaluation of the reproductive toxicity of antiretroviral drug loaded lactoferrin nanoparticles.
Kondapi, AK; Madugulla, L; Ravula, AR; Yenugu, S, 2019
)
0.51
" male and female subjects exhibiting different discriminatory potential to detect bioavailability differences between formulations."( Sex-by-formulation interaction in bioequivalence studies: the importance of formulations and experimental conditions.
Fagiolino, P; Ibarra, M; Vázquez, M, 2019
)
0.51
"" The objective of this study was to improve solubility and oral bioavailability by formulating liquid-SNEDDS and to mask bitter taste and minimize BMS."( Taste Evaluation by Electronic Tongue and Bioavailability Enhancement of Efavirenz.
Bhutada, K; Kaushal, P; Rao, MRP, 2019
)
0.51
" To improve solubility and bioavailability of highly potent anti-retroviral drugs, we explored the use of a nanoparticle (NP) for formulating a combination of two water-insoluble HIV inhibitors."( Antiretroviral Hydrophobic Core Graft-Copolymer Nanoparticles: The Effectiveness against Mutant HIV-1 Strains and in Vivo Distribution after Topical Application.
Alfaro, J; Bogdanov, AA; Bolotin, E; Castillo, G; Gottikh, MB; Gupta, S; Leporati, A, 2019
)
0.51
"Amorphous solid dispersions (ASDs) are found to be a well-established strategy for overcoming limited aqueous solubility and poor oral bioavailability of active pharmaceutical ingredients (APIs)."( Determination of drug-polymer solubility from supersaturated spray-dried amorphous solid dispersions: A case study with Efavirenz and Soluplus®.
Costa, BLA; Del Confetto, S; Ré, MI; Sauceau, M; Sescousse, R, 2019
)
0.51
" Thus, quality evaluation of different crystal forms should be assessed especially the solubility and dissolution behaviors among polymorphic forms, which correlate to bioavailability and therapy efficacy."( Polymorphic properties and dissolution profile of efavirenz due to solvents recrystallization.
Soewandhi, SN; Suendo, V; Wardhana, YW; Wikarsa, S, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" Both sex and CD4 cell count affected the bioavailability of isoniazid."( Model-Based Assessment of Variability in Isoniazid Pharmacokinetics and Metabolism in Patients Co-Infected With Tuberculosis and HIV: Implications for a Novel Dosing Strategy.
Äbelö, A; Ashton, M; Bienvenu, E; Birgersson, S; Janzén, D; Sundell, J, 2020
)
0.56
" An absolute bioavailability study informed the hepatic and gastric availability."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
0.56
"The aim of the study was to evaluate organogel nanoparticles as a lipophilic vehicle to increase the oral bioavailability of poorly soluble compounds."( Organogel Nanoparticles as a New Way to Improve Oral Bioavailability of Poorly Soluble Compounds.
Beyssac, E; Franceschi, S; Garrait, G; Goudouneche, D; Martin, B; Perez, E, 2020
)
0.56
" Various parameters have been investigated in the current study such as (i) the release profile of organogel assessed by USP 4 cell flow dialysis, (ii) the impact of organogel on intestinal absorption, using Caco-2 cells as in vitro model and jejunum segments as ex vivo assay and (iii) the bioavailability of organogel following oral pharmacokinetic study."( Organogel Nanoparticles as a New Way to Improve Oral Bioavailability of Poorly Soluble Compounds.
Beyssac, E; Franceschi, S; Garrait, G; Goudouneche, D; Martin, B; Perez, E, 2020
)
0.56
"Organogel nanoparticles increase the bioavailability of BCS Class II drugs."( Organogel Nanoparticles as a New Way to Improve Oral Bioavailability of Poorly Soluble Compounds.
Beyssac, E; Franceschi, S; Garrait, G; Goudouneche, D; Martin, B; Perez, E, 2020
)
0.56
" The immission distributional kinetics model is applied in projecting bioavailability (F = 0."( Modelling the influx and efflux waves in drug movement: a basis for Pharmacokinetic-Pharmacodynamic link of efavirenz.
Nemaura, T, 2019
)
0.51
" Rifampicin bioavailability was also lower in patients on concomitant ART."( Effect of efavirenz-based ART on the pharmacokinetics of rifampicin and its primary metabolite in patients coinfected with TB and HIV.
Äbelö, A; Ashton, M; Bienvenu, E; Sundell, J, 2021
)
0.62
" Liquid formulation led to a 42% decrease in bioavailability compared with opened capsules."( Impact of CYP2B6 genotype, tuberculosis therapy, and formulation on efavirenz pharmacokinetics in infants and children under 40 months of age.
Benns, A; Bolton Moore, C; Bwakura-Dangarembizi, M; Capparelli, EV; Chadwick, EG; Chakhtoura, N; Frenkel, L; Jean-Philippe, P; Libous, J; Nikanjam, M; Samson, P; Spector, SA; Tran, L; Zimmer, B, 2022
)
0.72
"Efavirenz (EFV) is an anti-HIV drug with high dose and 40% oral bioavailability (BA)."( Cationic Solid SMEDDS of Efavirenz for Improved Oral Delivery: Development by Central Composite Design, In Vitro and In Vivo Evaluation.
Dudhipala, N; Katla, V; Thota, SK; Veerabrahma, K, 2023
)
0.91
" The typical estimates of oral clearance, volume of distribution, and absorption rate constant for typical 22 kg children with CYP2B6 *1/*1 and ABCB1c."( Genetic and non-genetic factors influencing efavirenz population pharmacokinetics among human immunodeficiency virus-1-infected children in Ethiopia.
Ahmed, JH; Aklillu, E; Chaka, TE; Chala, A; Kitabi, EN; Makonnen, E; Tadesse, BT, 2023
)
0.91
" Age affected the bioavailability of rifampicin and isoniazid; at birth, children had 48."( Evaluating pediatric tuberculosis dosing guidelines: A model-based individual data pooled analysis.
Aarnoutse, R; Chabala, C; Cotton, MF; Denti, P; Galileya, LT; Gibb, D; Hesseling, A; Lee, J; McIlleron, H; Njahira Mukui, I; Rabie, H; Turkova, A; Wasmann, RE; Zar, H, 2023
)
0.91
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Fasting efavirenz concentrations at 12 h after dosing (C12) were monitored. Dosing efvirenz in children based only on weight results in a large variability in drug exposure.

ExcerptRelevanceReference
" An increase in dosage of indinavir from 800 to 1000 mg 3 times daily is recommended during coadministration with efavirenz."( Efavirenz.
Adkins, JC; Noble, S, 1998
)
0.3
" The delayed gastric emptying in monkeys also was observed when the animals dosed at 160 mg/kg exhibited emesis, 8 h postdose, which was found to contain a substantial portion of the dose."( Nonlinear pharmacokinetics of efavirenz (DMP-266), a potent HIV-1 reverse transcriptase inhibitor, in rats and monkeys.
Balani, SK; deLuna, FA; Kauffman, LR; Lin, JH, 1999
)
0.3
" Electrospray ionization-liquid chromatography/mass spectrometry analyses of bile samples from rats dosed with either efavirenz or with 8-OH efavirenz revealed three polar metabolites, M9, M12, and M13, with pseudomolecular ions [M-H](-) at m/z 733, 602, and 749, respectively."( Liquid chromatography/mass spectrometry and high-field nuclear magnetic resonance characterization of novel mixed diconjugates of the non-nucleoside human immunodeficiency virus-1 reverse transcriptase inhibitor, efavirenz.
Chen, H; Christ, DD; Gan, LS; Mutlib, AE; Nemeth, G, 1999
)
0.3
" Blood samples for pharmacokinetic analysis were obtained during a dosage interval."( Pharmacokinetics of efavirenz (EFV) alone and in combination therapy with nelfinavir (NFV) in HIV-1 infected patients.
Castelli, F; Maserati, R; Regazzi, MB; Seminari, E; Torti, C; Viale, P; Villani, P, 1999
)
0.3
" EFV exhibits a relatively low interindividual variability and a dosing regimen of 600 mg day-1 assures plasma concentrations that are adequate for inhibition of viral replication."( Pharmacokinetics of efavirenz (EFV) alone and in combination therapy with nelfinavir (NFV) in HIV-1 infected patients.
Castelli, F; Maserati, R; Regazzi, MB; Seminari, E; Torti, C; Viale, P; Villani, P, 1999
)
0.3
" The pharmacokinetics of efavirenz allow for once daily dosing without regard to meals of normal composition."( Clinical history of efavirenz.
Ruiz, N, 1999
)
0.3
" Although protease inhibitor (PI) containing therapies are very potent, many problems have now been identified that reduce quality of life such as a high pill burden, multiple daily dosing and dietary constraints."( Review of NNRTIs: 'today and tomorrow'.
Katlama, C, 1999
)
0.3
"25 mg/L and the mean AUC during the dosing interval was 17."( Clinical pharmacokinetics of nelfinavir combined with efavirenz and stavudine during rescue treatment of heavily pretreated HIV-infected patients.
Fiocchi, C; Gambarana, E; LoCaputo, F; Maserati, R; Pan, A; Regazzi, MB; Seminari, E; Villani, P, 2000
)
0.31
" Oral dosing is administered three times daily for delavirdine (DLV), twice daily for nevirapine (NVP), and once daily for efavirenz (EFV)."( Clinical uses of non-nucleoside reverse transcriptase inhibitors.
Harris, M; Montaner, JS,
)
0.13
" The spectrum of mutations observed in cases of virological treatment failure was similar for patients initially dosed with efavirenz at 200, 400, or 600 mg once a day and for patients treated with efavirenz in combination with indinavir, stavudine, or ZDV-3TC."( Human immunodeficiency virus type 1 mutations selected in patients failing efavirenz combination therapy.
Abremski, K; Anton, ED; Aujay, M; Bacheler, LT; Baker, D; Becker, MF; Bolling, L; Bunville, J; Ellis, D; George, HJ; Hollis, G; Krakowski, K; Kudish, P; Lasut, AL; Spalding, DR; Wang, XV, 2000
)
0.31
" Further processing of this glutathione adduct was also important in producing the lesion and was demonstrated by inhibiting gamma-glutamyltranspeptidase with acivicin pretreatment (10 mg/kg, IV) prior to dosing with efavirenz."( The species-dependent metabolism of efavirenz produces a nephrotoxic glutathione conjugate in rats.
Chen, H; Christ, DD; Davies, MH; Gan, LS; Gemzik, B; Gerson, RJ; Haley, PJ; Krahn, DF; Markwalder, JA; Meunier, PC; Miwa, GT; Mutlib, AE; Robertson, RT; Seitz, SP, 2000
)
0.31
" Combining d4T/ddI with protease inhibitors presents problems, such as a complicated dosing schedule and harsh gastrointestinal side effects."( Dethroning AZT.
Falkenberg, J; Gilden, D; Torres, G, 1997
)
0.3
" Situations to avoid include using dosing schedules that do not sufficiently suppress the virus, waiting for viral load to return to pre-treatment levels before switching drugs, and not switching drugs to at least two new potent compounds when changing combination therapy."( Update on antivirals.
, 1997
)
0.3
" All three drugs are currently available through expanded access programs, are dosed either once or twice daily, and can be taken with or without food."( I want a new drug. An overview of three new anti-HIV drugs.
Simmons, P, 1998
)
0.3
" The dosage regimens and limitations are described for each drug."( Four new antiretroviral medications will soon offer more options to HIV patients.
Murphy, MJ,
)
0.13
" Abacavir is also attracting attention due to its potency and dosing convenience."( Dupont pharmaceuticals study 006 for Sustiva.
Bartlett, JG, 1998
)
0.3
" Food and Drug Administration (FDA) has approved Sustiva (efavirenz) as the first HIV drug to have a once-daily dosing schedule."( FDA approves Sustiva (efavirenz) capsules, first once-daily anti-HIV drug. Food and Drug Administration.
, 1998
)
0.3
" Clinical trial results indicate that the low dosage and efficacy of Sustiva make it a good treatment option for many patients."( New drug approved.
, 1998
)
0.3
"Efavirenz (Sustiva) is the first once-daily dosing anti-HIV drug approved by the Food and Drug Administration."( First once-daily drug simplifies dosing, offers new options in HIV-1 treatment.
, 1998
)
0.3
"DuPont Pharmaceuticals' Sustiva (efavirenz) was approved by the FDA as the first once-daily- dosing anti-HIV drug."( Now approved: Sustiva in combination offers patients a new first-line therapy.
,
)
0.13
"Information is provided on efavirenz (Sustiva, formerly DMP-266), including dosage information, resistance and clinical trial results, and pharmacology."( Product information.
Bartlett, JG, 1999
)
0.3
" Information on each drug, such as the name of the drug, the dosage normally prescribed, and cost of treatment is listed."( What they say about: non-nucleoside drugs.
,
)
0.13
" The studies showed twice-daily dosing is inferior to taking the drug every 8 hours."( No more twice-a-day Crixivan.
Vazquez, E,
)
0.13
" Dosing is recommended at bedtime to avert side effects, which are described."( Sustiva (efavirenz) is approved.
Vazquez, E,
)
0.13
" Common side effects and dosing information are described."( Efavirenz (Sustiva) receives FDA approval. Food and Drug Administration.
, 1998
)
0.3
" Dosage and cost data are included."( What they say about non-nucleoside drugs.
,
)
0.13
" Progress is also highlighted about dosing regimens, antiretroviral resistance, and reconstitution of the immune system."( Moving forward: a treatment overview from the 12th World AIDS Conference.
Agosto, M, 1998
)
0.3
" In addition, the favorable side-effect profile, diminished pill burden for clients, and daily dosing have contributed to its popularity."( Evidence of hypertriglyceridemia in managing HIV patients on efavirenz.
Cohen, DM; James, CW; Miller, JL; Perlada, DE; Savini, CJ; Wilson, SA,
)
0.13
" For levofloxacin, plasma samples were obtained at steady state during a 24-h dosing interval."( Pharmacokinetic evaluation of oral levofloxacin in human immunodeficiency virus-infected subjects receiving concomitant antiretroviral therapy.
Cadeo, B; Carosi, G; Fiocchi, C; Marchetti, F; Regazzi, MB; Signorini, L; Viale, P; Villani, A; Villani, P, 2001
)
0.31
" In addition to a potent antiretroviral activity, efavirenz is an easy-to-take drug with once-daily dosing and is usually well tolerated."( [Apropos of atypical melancholia with Sustiva (efavirenz)].
Danion, JM; Halleguen, O; Lang, JM; Lang, JP; Picard, A,
)
0.13
" More conveniently dosed and patient-friendly regimens are needed."( Virological and immunological responses to a once-a-day antiretroviral regimen with didanosine, lamivudine and efavirenz.
Maggiolo, F; Maserati, R; Migliorino, M; Pan, A; Provettoni, G; Rizzi, L; Rizzi, M; Suter, F, 2001
)
0.31
"Although the minimal effective efavirenz plasma concentration that assures virological success is not currently known, it may be advisable to increase the dosage of efavirenz to 800 mg once daily when it is coadministered with rifampicin."( Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis.
Alarcón-González, A; Gómez-Mateos, J; León-Jimenez, E; López-Cortés, LF; López-Pua, Y; Pachón, J; Ruiz-Valderas, R; Sarasanacenta, M; Viciana, P, 2002
)
0.31
" Discontinuation of atenolol, and nifedipine dosage reduction by 50% were effective in managing his orthostatic changes."( Symptomatic orthostasis with extended-release nifedipine and protease inhibitors.
Rathbun, RC; Rossi, DR; Slater, LN, 2002
)
0.31
" During the dosing interval, no single SPrcolon;BP EFV-concentration ratio was significantly predictive of the absolute measure of exposure in SP."( Pharmacokinetic and pharmacodynamic investigation of efavirenz in the semen and blood of human immunodeficiency virus type 1-infected men.
Cohen, MS; Eron, JJ; Fiscus, SA; Fiske, WD; Gotzkowsky, SK; Kashuba, AD; Kim, JY; Petch, L; Reddy, YS, 2002
)
0.31
"The protease inhibitor (PI) ritonavir is used as a strong inhibitor of cytochrome P450 3A4, which boosts the activities of coadministered PIs, resulting in augmented plasma PI levels, simplification of the dosage regimen, and better efficacy against resistant viruses."( Steady-state pharmacokinetics of amprenavir coadministered with ritonavir in human immunodeficiency virus type 1-infected patients.
Bidault, R; Bollens, D; Choudet, N; Demarles, D; Gillotin, C; Goujard, C; Meynard, JL; Rousseau, C; Taburet, AM; Vincent, I, 2003
)
0.32
"The steady-state pharmacokinetics and pharmacodynamics of two oral doses of lopinavir-ritonavir (lopinavir/r; 400/100 and 533/133 mg) twice daily (BID) when dosed in combination with efavirenz, plus two nucleoside reverse transcriptase inhibitors, were assessed in a phase II, open-label, randomized, parallel arm study in 57 multiple protease inhibitor-experienced but non-nucleoside reverse transcriptase inhibitor-naive human immunodeficiency virus (HIV)-infected subjects."( Pharmacokinetic-pharmacodynamic analysis of lopinavir-ritonavir in combination with efavirenz and two nucleoside reverse transcriptase inhibitors in extensively pretreated human immunodeficiency virus-infected patients.
Bernstein, B; Bertz, R; Brun, S; Foit, C; Granneman, GR; Hsu, A; Isaacson, J; Kempf, DJ; King, M; Lam, W; Richards, B; Rode, R; Rynkiewicz, K; Sun, E, 2003
)
0.32
" However, dosage individualization based on plasma concentration monitoring might be indicated."( Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection.
Biollaz, J; Buclin, T; Csajka, C; Décosterd, LA; Fattinger, K; Fellay, J; Marzolini, C; Telenti, A, 2003
)
0.32
" The average drug exposure during 1 dosing interval was estimated for each patient and correlated with markers of efficacy and toxicity."( Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection.
Biollaz, J; Buclin, T; Csajka, C; Décosterd, LA; Fattinger, K; Fellay, J; Marzolini, C; Telenti, A, 2003
)
0.32
" This enabled the derivation of a dosing adaptation strategy suitable to bring the average concentration into a therapeutic target from 1000 to 4000 microg/L to optimize viral load suppression and to minimize central nervous system toxicity."( Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection.
Biollaz, J; Buclin, T; Csajka, C; Décosterd, LA; Fattinger, K; Fellay, J; Marzolini, C; Telenti, A, 2003
)
0.32
" However, further evaluation is needed before individualization of an efavirenz dosage regimen based on routine drug level monitoring should be recommended for optimal patient management."( Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection.
Biollaz, J; Buclin, T; Csajka, C; Décosterd, LA; Fattinger, K; Fellay, J; Marzolini, C; Telenti, A, 2003
)
0.32
"37) were similar regardless of the dosing regimen."( Indinavir, efavirenz, and abacavir pharmacokinetics in human immunodeficiency virus-infected subjects.
Cha, R; DiCenzo, R; Fischl, MA; Forrest, A; Hammer, SM; Morse, GD; Squires, KE; Wu, H, 2003
)
0.32
" For efavirenz, the concentrations at 12 hours and 24 hours (Cmin) after dosing were assessed."( Pharmacokinetics of indinavir/ritonavir (800/100 mg) in combination with efavirenz (600 mg) in HIV-1-infected subjects.
Aarnoutse, RE; Boyd, MA; Burger, DM; Cooper, DA; Lange, JM; Phanuphak, P; Ruxrungtham, K; Stek, M; van Heeswijk, RP, 2003
)
0.32
"When EFV is coadministered with the GW433908 700 mg + RTV 100 mg BID regimen, no dosage adjustment is recommended."( Pharmacokinetics and safety of GW433908 and ritonavir, with and without efavirenz, in healthy volunteers.
Ballow, C; Hendrix, CW; Lou, Y; Piliero, PJ; Preston, SL; Stein, DS; Wire, MB, 2004
)
0.32
" PI-based therapies often fail due to poor adherence caused by heavy pill burden, complex dosing schedules and undesirable side effects."( Clinical utility of current NNRTIs and perspectives of new agents in this class under development.
Hamatake, R; Hong, Z; Zhang, Z, 2004
)
0.32
" HIV type 1 (HIV-1)-infected patients receiving EFV or lopinavir-ritonavir (LPV/r) had 9 or 10 blood samples drawn over 8 to 24 h of a dosing interval at steady state before and after receiving 250 mg of VPA twice daily for 7 days."( Effects of valproic acid coadministration on plasma efavirenz and lopinavir concentrations in human immunodeficiency virus-infected adults.
Cruttenden, K; DiCenzo, R; Gelbard, H; Morse, G; Peterson, D; Riggs, G; Schifitto, G, 2004
)
0.32
" Blood samples were collected up to 24 h after dosing on days 10 (period 1) and 20 (period 2)."( Effect of efavirenz treatment on the pharmacokinetics of nelfinavir boosted by ritonavir in healthy volunteers.
Burger, DM; Colbers, EP; de Graaff-Teulen, MJ; Hekster, YA; Ibanez, SM; Koopmans, PP; la Porte, CJ; Voncken, DS, 2004
)
0.32
" After the dosage of efavirenz was lowered, all neuropsychiatric symptoms subsided."( Efavirenz intoxication due to slow hepatic metabolism.
Bleiber, G; Günthard, HF; Hasse, B; Krause, M, 2005
)
0.33
" ABC administered once daily in combination with 3TC and EFV administered once daily was non-inferior to the ABC twice-daily dosing schedule when combined with 3TC and EFV over 48 weeks."( Abacavir once or twice daily combined with once-daily lamivudine and efavirenz for the treatment of antiretroviral-naive HIV-infected adults: results of the Ziagen Once Daily in Antiretroviral Combination Study.
Cahn, P; Castillo, SA; Craig, C; DeJesus, E; Gordon, DN; Moyle, GJ; Scott, TR; Zhao, H, 2005
)
0.33
"No adequate substitute for collecting blood 24 hours after dosing emerged from this analysis, which might explain the weak association observed between EFV plasma levels and treatment outcomes in the studies available."( Therapeutic drug monitoring of efavirenz: trough levels cannot be estimated on the basis of earlier plasma determinations.
López-Cortés, LF; Lucero-Muñoz, MJ; Marín-Niebla, A; Pascual-Carrasco, R; Rodríguez-Díez, M; Ruiz-Valderas, R, 2005
)
0.33
" Plasma efavirenz levels can be reduced by rifampicin, but the appropriate daily dosage of efavirenz is unclear."( Efavirenz levels and 24-week efficacy in HIV-infected patients with tuberculosis receiving highly active antiretroviral therapy and rifampicin.
Kiertiburanakul, S; Mahanontharit, A; Manosuthi, W; Prasithsirikul, W; Rattanasiri, S; Ruxrungtham, K; Sankote, J; Sungkanuparph, S; Thakkinstian, A; Vibhagool, A, 2005
)
0.33
" Plasma efavirenz levels were measured (at 12 h after dosing and on day 14) by high-performance liquid chromatography."( Efavirenz levels and 24-week efficacy in HIV-infected patients with tuberculosis receiving highly active antiretroviral therapy and rifampicin.
Kiertiburanakul, S; Mahanontharit, A; Manosuthi, W; Prasithsirikul, W; Rattanasiri, S; Ruxrungtham, K; Sankote, J; Sungkanuparph, S; Thakkinstian, A; Vibhagool, A, 2005
)
0.33
"Venous blood samples from 10 HIV-infected patients receiving efavirenz (600 mg once a day plus two nucleoside reverse transcriptase inhibitors) were collected over the 24 h dosing interval."( Intracellular and plasma pharmacokinetics of efavirenz in HIV-infected individuals.
Almond, LM; Back, DJ; Edirisinghe, D; Hoggard, PG; Khoo, SH, 2005
)
0.33
" When atazanavir 300 mg was coadministered with ritonavir 100 mg on a once-daily dosage regimen, atazanavir AUC from 0 to 24 hours and minimum plasma concentration were increased by 3- to 4-fold and approximately 10-fold, respectively, compared with atazanavir 300 mg alone."( Clinical pharmacokinetics and summary of efficacy and tolerability of atazanavir.
Barrail, A; Goujard, C; Le Tiec, C; Taburet, AM, 2005
)
0.33
" The optimal efavirenz dosage is still unclear."( Efavirenz 600 mg/day versus efavirenz 800 mg/day in HIV-infected patients with tuberculosis receiving rifampicin: 48 weeks results.
Kiertiburanakul, S; Manosuthi, W; Rattanasiri, S; Ruxrungtham, K; Sungkanuparph, S; Thakkinstian, A; Vibhagool, A, 2006
)
0.33
" Despite therapeutic drug monitoring and subsequent efavirenz dosage reductions, side-effects did not resolve completely and lopinavir concentrations remained relatively low."( Genotyping of CYP2B6 and therapeutic drug monitoring in an HIV-infected patient with high efavirenz plasma concentrations and severe CNS side-effects.
Hansen, AB; Justesen, US; Mathiesen, S; Von Lüttichau, HR, 2006
)
0.33
"For moderately pre-treated HIV-infected patients with few mutations who switched to efavirenz from previous successful HAART, the proposed plasma efficacy-threshold was reached without any dosage adaptation."( Intracellular and plasma efavirenz concentrations in HIV-infected patients switching from successful protease inhibitor-based highly active antiretroviral therapy (HAART) to efavirenz-based HAART (SUSTIPHAR Study).
Breilh, D; Camou, F; Caubet, O; Djabarouti, S; Fleury, H; Lavit, M; Pellegrin, I; Pellegrin, JL; Saux, MC, 2006
)
0.33
"The data show insufficient plasma concentrations for some children despite efavirenz dosing according to recommendations."( Need for therapeutic drug monitoring in HIV-1 infected children receiving efavirenz doses according to international guidelines.
Dunsch, D; Elanjikal, S; Funk, MB; Koenigs, C; Kreuz, W; Linde, R; von Hentig, N, 2006
)
0.33
"Efavirenz is dosed once daily, and is generally administered in the evening owing to its central nervous system side-effects."( Can efavirenz be taken in the morning?
Maeland, A; Skeie, L, 2006
)
0.33
" Individually, these agents have long half-lifes that allow for once-daily dosing and may provide a pharmacologic bridge for the occasional missed dose."( Efavirenz/emtricitabine/tenofovir disoproxil fumarate fixed-dose combination: first-line therapy for all?
Best, B; Goicoechea, M, 2007
)
0.34
"Most antiretrovirals are metabolized in the liver, and lower dosing could be advisable in patients with severe liver insufficiency."( Influence of liver fibrosis stage on plasma levels of antiretroviral drugs in HIV-infected patients with chronic hepatitis C.
Barreiro, P; Gonzalez-Lahoz, J; Jiménez-Nácher, I; Labarga, P; Martín-Carbonero, L; Rodríguez-Novoa, S; Ruiz, A; Soriano, V, 2007
)
0.34
" The method quantitates BUP and NBUP plasma concentrations within the range of expected values from current BUP dosing guidelines."( Buprenorphine assay and plasma concentration monitoring in HIV-infected substance users.
DiFrancesco, R; Donnelly, J; Fischl, MA; Gripshover, B; McCance-Katz, EF; Moody, DE; Morse, GD; Reichman, RC; Zingman, BS, 2007
)
0.34
"Efavirenz-containing regimens using concentration-controlled dosing have been shown to provide potent antiretroviral activity in children."( High prevalence of subtherapeutic plasma concentrations of efavirenz in children.
Egbers, C; Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2007
)
0.34
"Three consecutive blood samples were drawn between 12 and 24 hours after dosing in 15 HIV-infected children receiving the recommended daily doses of efavirenz."( High prevalence of subtherapeutic plasma concentrations of efavirenz in children.
Egbers, C; Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2007
)
0.34
"Our findings, together with those of previous studies, indicate that many children dosed according to the current guidelines do not achieve adequate efavirenz exposure."( High prevalence of subtherapeutic plasma concentrations of efavirenz in children.
Egbers, C; Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2007
)
0.34
" Efavirenz is administered once-daily and its simple dosing schedule improves adherence to therapy allowing for durability of the virologic and clinical responses."( Efavirenz.
Maggiolo, F, 2007
)
0.34
" Although in vivo dosage form disintegration was faster for Tablet A as compared to Tablet B and was similar between Tablet A and the capsule, Tablet A showed a slower rate and extent of drug absorption than Tablet B and the capsule."( Investigation of human pharmacoscintigraphic behavior of two tablets and a capsule formulation of a high dose, poorly water soluble/highly permeable drug (efavirenz).
Benedek, IH; Digenis, GA; Doll, WJ; Fiske, WD; Gao, JZh; Gray, DA; Hussain, MA; Motheram, R; Page, RC; Sandefer, E, 2007
)
0.34
"A novel, once-daily dosing regimen of 3 antiretroviral drugs, emtricitabine, didanosine, and efavirenz, was tested in 37 therapy-naive HIV-infected children and adolescents between 3 and 21 years of age (inclusive)."( Long-term safety and efficacy of a once-daily regimen of emtricitabine, didanosine, and efavirenz in HIV-infected, therapy-naive children and adolescents: Pediatric AIDS Clinical Trials Group Protocol P1021.
Abrams, E; Blum, MR; Britto, P; Chittick, GE; Cunningham, C; Dickover, R; Draper, L; Flynn, P; Hu, C; Hughes, M; Kraimer, J; McKinney, RE; Ortiz, AA; Rathore, M; Reynolds, L; Rodman, J; Scites, M; Serchuck, LK; Smith, ME; Spector, S; Tran, P; Weinberg, A; Yogev, R, 2007
)
0.34
" This study evaluated the pharmacokinetics (PK) and bioequivalence of an investigational coformulation of EFV/FTC/TDF (test) single-tablet regimen compared with the commercially available individual dosage forms (EFV+FTC+TDF; reference treatment) in healthy subjects."( Bioequivalence of efavirenz/emtricitabine/tenofovir disoproxil fumarate single-tablet regimen.
Hinkle, J; Hui, J; Kaul, S; Kearney, BP; Mathias, AA; Menning, M, 2007
)
0.34
" EFV dose was reduced in CYP2B6 516G-->T carriers who had high plasma EFV concentrations while receiving the standard dosage (600 mg)."( Successful efavirenz dose reduction in HIV type 1-infected individuals with cytochrome P450 2B6 *6 and *26.
Fujimoto, K; Gatanaga, H; Gejyo, F; Hamaguchi, M; Hayashida, T; Horiba, M; Kimura, A; Kimura, S; Koike, T; Kuwahara, T; Matsushita, S; Oka, S; Sato, I; Shirasaka, T; Takata, N; Tsuchiya, K; Tsukada, H; Ueda, M; Yamamoto, M; Yoshino, M, 2007
)
0.34
" When efavirenz (four patients) or a nucleoside analogue combination (one patient) was added, very little change in tacrolimus dosing was required."( Effect of highly active antiretroviral therapy on tacrolimus pharmacokinetics in hepatitis C virus and HIV co-infected liver transplant recipients in the ANRS HC-08 study.
Abbara, C; Barrail, A; Boissonnas, A; Bonhomme-Faivre, L; Duclos-Vallée, JC; Samuel, D; Taburet, AM; Teicher, E; Vincent, I; Vittecoq, D, 2007
)
0.34
" Tacrolimus dosing must be optimised according to therapeutic drug monitoring and the antiretroviral drug combination."( Effect of highly active antiretroviral therapy on tacrolimus pharmacokinetics in hepatitis C virus and HIV co-infected liver transplant recipients in the ANRS HC-08 study.
Abbara, C; Barrail, A; Boissonnas, A; Bonhomme-Faivre, L; Duclos-Vallée, JC; Samuel, D; Taburet, AM; Teicher, E; Vincent, I; Vittecoq, D, 2007
)
0.34
" The 400-mg qd efavirenz dose substantially reduced the steady-state mean voriconazole area under the curve over the dosing interval (AUC0-12) by 80% (90% confidence interval [CI], 75%-84%) and peak concentration (Cmax) by 66% (90% CI, 57%-73%)."( Pharmacokinetic interaction between voriconazole and efavirenz at steady state in healthy male subjects.
Foster, G; Gutierrez, MJ; LaBadie, RR; Liu, P; Sharma, A, 2008
)
0.35
" The results of the calculations revealed that the variant that survives in patients dosed with either nevirapine or efavirenz had a more positive Delta Delta G value than other variants that were not observed in patients."( Energetic effects for observed and unobserved HIV-1 reverse transcriptase mutations of residues L100, V106, and Y181 in the presence of nevirapine and efavirenz.
Franklin, AM; Jorgensen, WL; Rader, LH; Smith, KD; Smith, MB; Smith, RH; Taylor, EV; Tirado-Rives, J, 2008
)
0.35
" TDM is useful to determine the best dosage regimen adapted to each patient."( Determination of abacavir, amprenavir, didanosine, efavirenz, nevirapine, and stavudine concentration in human plasma by MALDI-TOF/TOF.
Alonzi, T; Ascenzi, P; Mancone, C; Narciso, P; Notari, S; Tripodi, M, 2008
)
0.35
" Sometimes literature references are submitted to the FDA to support dosing recommendations."( Are literature references sufficient for dose recommendations? An FDA case study of efavirenz and rifampin.
Chan-Tack, KM; DiGiacinto, JL; Reynolds, KS; Robertson, SM; Struble, KA, 2008
)
0.35
"HIV-1-infected children received efavirenz capsules or tablets in accordance with manufacturer's dosing recommendations."( Antiviral efficacy, tolerability and pharmacokinetics of efavirenz in an unselected cohort of HIV-infected children.
Burger, D; Hoffmann, F; Huss, K; Jansson, A; Kurowski, M; Notheis, G; Wintergerst, U, 2008
)
0.35
"In antiretroviral (ARV) therapy, pill burden, dosing frequency, and regimen complexity adversely affect adherence."( Randomization to once-daily stavudine extended release/lamivudine/efavirenz versus a more frequent regimen improves adherence while maintaining viral suppression.
Boyle, BA; Grimm, K; Jayaweera, D; Maa, JF; Seekins, DW; Witt, MD,
)
0.13
" Pharmacokinetic profiles were also determined in HIV-1-infected patients dosed with raltegravir monotherapy versus raltegravir in combination with TDF and lamivudine."( Lack of a significant drug interaction between raltegravir and tenofovir.
Breidinger, SA; Chen, J; Friedman, EJ; Gottesdiener, KM; Iwamoto, M; Kost, JT; Lasseter, KC; Stek, JE; Stone, JA; Teppler, H; Wagner, JA; Wenning, LA, 2008
)
0.35
" This case raises several significant questions regarding the adverse effects and dosing of this medication, including which patient characteristics predispose to efavirenz toxicity, the relevance of the CYP2B6 mutation, and indications for therapeutic drug monitoring."( Status epilepticus resulting from severe efavirenz toxicity in an HIV-infected patient.
Kwara, A; Nijhawan, AE; Venna, N; Zachary, KC, 2008
)
0.35
"The pharmacokinetics of EFV and LPV/RTV in hemodialysis suggests that no dosing adjustments are necessary in treatment-naive patients."( The pharmacokinetics and pharmacogenomics of efavirenz and lopinavir/ritonavir in HIV-infected persons requiring hemodialysis.
Amorosa, V; Cramer, YS; Gupta, SK; Hall, SD; Koletar, SL; Rosenkranz, SL; Szczech, LA, 2008
)
0.35
"Our main objectives were to study the population pharmacokinetics of efavirenz and to explore the adequacy of dosing guidelines."( A pharmacokinetic and pharmacogenetic study of efavirenz in children: dosing guidelines can result in subtherapeutic concentrations.
Beijnen, JH; Bekker, V; Crommentuyn, KM; Huitema, AD; Kuijpers, TW; Scherpbier, HJ; ter Heine, R, 2008
)
0.35
" Current dosing guidelines can result in subtherapeutic concentrations in children carrying the CYP2B6-516-G/G genotype and with the liquid formulation."( A pharmacokinetic and pharmacogenetic study of efavirenz in children: dosing guidelines can result in subtherapeutic concentrations.
Beijnen, JH; Bekker, V; Crommentuyn, KM; Huitema, AD; Kuijpers, TW; Scherpbier, HJ; ter Heine, R, 2008
)
0.35
" The pharmacokinetic profile of GS-9160 in healthy human volunteers revealed that once-daily dosing was not likely to achieve antiviral efficacy; hence, the clinical development of this compound was discontinued."( Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
Chen, J; Chen, X; Geleziunas, R; Hesselgesser, J; Jin, H; Jones, GS; Kim, CU; Tsiang, M; Wright, M; Yu, F; Zeynalzadegan, A, 2009
)
0.35
" In addition, the detection and determination limits, reproducibility and applicability of the analysis to pharmaceutical dosage forms were also investigated."( Voltammetric studies on the HIV-1 inhibitory drug Efavirenz: the interaction between dsDNA and drug using electrochemical DNA biosensor and adsorptive stripping voltammetric determination on disposable pencil graphite electrode.
Dogan-Topal, B; Ozkan, SA; Uslu, B, 2009
)
0.35
" Therefore, dosage adjustment in accordance with the type of polymorphism (CYP2B6, CYP2A6, or CYP3A4) is required in order to maintain EFV within the therapeutic target levels."( Pharmacogenetics-based population pharmacokinetic analysis of efavirenz in HIV-1-infected individuals.
Arab-Alameddine, M; Biollaz, J; Buclin, T; Cavassini, M; Csajka, C; Décosterd, LA; Di Iulio, J; Eap, CB; Fayet, A; Lubomirov, R; Rotger, M; Telenti, A, 2009
)
0.35
" Pharmacokinetic studies of higher dosages of rifampin are urgently needed in children to assist in placing the dosage of rifampin used in childhood on a more scientific foundation."( Rifampin pharmacokinetics in children, with and without human immunodeficiency virus infection, hospitalized for the management of severe forms of tuberculosis.
Cilliers, K; Donald, PR; Hussey, GD; Labadarios, D; Maritz, JS; McIlleron, H; Schaaf, HS; Smith, P; Willemse, M, 2009
)
0.35
" The population model can be implemented in pharmacokinetic clinical software for dosage optimization by using the Bayesian approach."( Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients.
Cabrera, SE; Domínguez-Gil, A; García, MJ; González, F; Luna, G; Santos, D; Valverde, MP, 2009
)
0.35
" Efavirenz and nevirapine concentrations at 12 h after dosing (C12) were monitored at weeks 6 and 12."( A randomized trial comparing plasma drug concentrations and efficacies between 2 nonnucleoside reverse-transcriptase inhibitor-based regimens in HIV-infected patients receiving rifampicin: the N2R Study.
Burapatarawong, S; Likanonsakul, S; Lueangniyomkul, A; Mankatitham, W; Manosuthi, W; Prasithsirskul, W; Prommool, V; Ruxrungtham, K; Sungkanuparph, S; Tantanathip, P; Thawornwa, U; Thongyen, S, 2009
)
0.35
"Concerns have been raised about the possibility of subtherapeutic efavirenz (EFV) plasma levels in children with the current dosing guideline."( Plasma efavirenz concentrations and the association with CYP2B6-516G >T polymorphism in HIV-infected Thai children.
Aurpibul, L; Cressey, TR; Puthanakit, T; Sirisanthana, V; Tanpaiboon, P, 2009
)
0.35
"Current EFV dosing guidelines provide adequate plasma drug concentrations in Thai HIV-infected children."( Plasma efavirenz concentrations and the association with CYP2B6-516G >T polymorphism in HIV-infected Thai children.
Aurpibul, L; Cressey, TR; Puthanakit, T; Sirisanthana, V; Tanpaiboon, P, 2009
)
0.35
"To assess whether stepwise dosing of efavirenz decreases the incidence and severity of NPAEs while maintaining virologic efficacy."( Stepped-dose versus full-dose efavirenz for HIV infection and neuropsychiatric adverse events: a randomized trial.
Gutiérrez-Valencia, A; López-Cortés, LF; Lozano, F; Palacios, R; Rivero, A; Ruiz-Valderas, R; Terrón, A; Viciana, P, 2009
)
0.35
" An optimized dosing schedule that would place the highest percentage of children in the interval of effective and nontoxic concentrations was simulated."( Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
Diagbouga, S; Hien, H; Hirt, D; Msellati, P; Nacro, B; Olivier, M; Peyrière, H; Rouet, F; Tréluyer, JM; Urien, S; Van De Perre, P; Zoure, E, 2009
)
0.35
"Multicenter, double-blind, randomized study of raltegravir (100, 200, 400, or 600 mg twice a day) vs efavirenz (600 mg every day), both with tenofovir/lamivudine (TDF/3TC), for 48 weeks, after which raltegravir arms were combined and all dosed at 400 mg twice a day."( Sustained antiretroviral effect of raltegravir after 96 weeks of combination therapy in treatment-naive patients with HIV-1 infection.
Campbell, H; Crumpacker, CS; Danovich, RM; Gotuzzo, E; Isaacs, RD; Kovacs, C; Markowitz, M; Mendo, F; Morales-Ramirez, JO; Nguyen, BY; Prada, G; Ratanasuwan, W; Strohmaier, KM; Teppler, H; Wan, H, 2009
)
0.35
" Fasting efavirenz concentrations at 12 h after dosing (C12) were monitored."( Body weight cutoff for daily dosage of efavirenz and 60-week efficacy of efavirenz-based regimen in human immunodeficiency virus and tuberculosis coinfected patients receiving rifampin.
Eampokarap, B; Kaewsaard, S; Lueangniyomkul, A; Mankatitham, W; Manosuthi, W; Ruxrungtham, K; Sungkanuparph, S; Suwanvattana, P; Tantanathip, P; Thongyen, S; Uttayamakul, S, 2009
)
0.35
" After dosing with TPV/r for 10 days, EFV 600 mg once a day was added to the regimen."( Lack of effect of efavirenz on the pharmacokinetics of tipranavir-ritonavir in healthy volunteers.
Béïque, L; Cameron, DW; la Porte, CJ; Sabo, JP, 2009
)
0.35
" Dosing convenience predicts adherence, and studies have demonstrated that patients can be switched from PI-based therapy to simplified, once-daily efavirenz-based regimens without losing virological control."( Efavirenz: a decade of clinical experience in the treatment of HIV.
Maggiolo, F, 2009
)
0.35
"To determine the impact of once-nightly versus twice-daily dosing and beliefs about highly active antiretroviral therapy (HAART) on adherence to efavirenz-based HAART in antiretroviral-naive patients."( The impact of once-nightly versus twice-daily dosing and baseline beliefs about HAART on adherence to efavirenz-based HAART over 48 weeks: the NOCTE study.
Cooper, V; Fisher, M; Gellaitry, G; Horne, R; Lange, AC; Vrijens, B; White, D, 2010
)
0.36
"The difference in adherence observed between once-nightly and twice-daily dosing was driven by a difference in persistence with treatment."( The impact of once-nightly versus twice-daily dosing and baseline beliefs about HAART on adherence to efavirenz-based HAART over 48 weeks: the NOCTE study.
Cooper, V; Fisher, M; Gellaitry, G; Horne, R; Lange, AC; Vrijens, B; White, D, 2010
)
0.36
" These data suggest that 2 tablets of lopinavir-ritonavir BD may be inadequate when dosed with NNRTIs in Ugandan adults, and the dosage should be increased by the addition of an additional adult tablet or a half-dose tablet (100/25 mg), where available."( Pharmacokinetics of lopinavir-ritonavir with and without nonnucleoside reverse transcriptase inhibitors in Ugandan HIV-infected adults.
Dickinson, L; Gibb, DM; Gilks, CF; Kayiwa, J; Khoo, S; Kityo, C; Lutwama, F; Munderi, P; Nalumenya, R; Reid, A; Ssali, F; Tumukunde, D; Walker, AS, 2010
)
0.36
" Measurement of the patient's efavirenz plasma concentrations revealed a mean minimum steady-state concentration during a dosage interval (C(min,ss)) of 12."( Long-term efficacy and safety of efavirenz dose reduction to 200 mg once daily in a Caucasian patient with HIV.
Cabrera Figueroa, S; Cordero Sánchez, M; de la Paz Valverde Merino, M; Domínguez-Gil Hurlé, A; Iglesias Gómez, A; Sánchez Martín, A, 2010
)
0.36
" Pharmacogenetic testing together with TDM links genotype to phenotypic differences in drug concentrations and adverse events, providing additional support for dosage adjustment and a more efficient use of both approaches."( The convergence of therapeutic drug monitoring and pharmacogenetic testing to optimize efavirenz therapy.
Bustos Bernal, C; Cabrera Figueroa, S; Domínguez-Gil Hurlé, A; Fernández de Gatta, M; García Sánchez, MJ; Hernández García, L; Sepúlveda Correa, R, 2010
)
0.36
" After receiving the standard efavirenz dosage of 600 mg daily, the patient had subtherapeutic plasma efavirenz concentrations."( Decreased plasma efavirenz concentrations in a patient receiving rifabutin.
Hill, CJ; Hsu, O; Kim, M; O'Brien, JG; Tan, B, 2010
)
0.36
" These findings may have relevance to pharmacokinetics and dosing of efavirenz in African populations."( Tribal ethnicity and CYP2B6 genetics in Ugandan and Zimbabwean populations in the UK: implications for efavirenz dosing in HIV infection.
Andrews, S; Holt, DW; Jamshidi, Y; McKeown, DA; Moreton, M; Nithiyananthan, T; Sadiq, ST; Tinworth, L, 2010
)
0.36
"Lersivirine appeared to be well tolerated after 28 days of continuous dosing in this small, selected group of young, healthy male volunteers."( Safety and tolerability of lersivirine, a nonnucleoside reverse transcriptase inhibitor, during a 28-day, randomized, placebo-controlled, Phase I clinical study in healthy male volunteers.
Choo, H; Davis, J; Goodrich, J; Hackman, F; Langdon, G; Lewis, D; Ndongo, MN; Tawadrous, M, 2010
)
0.36
" In turn, ART commonly requires complex dosing schedules and leads to the emergence of viral resistance and treatment failures."( Analyses of nanoformulated antiretroviral drug charge, size, shape and content for uptake, drug release and antiviral activities in human monocyte-derived macrophages.
Balkundi, S; Bronich, T; Gendelman, HE; Kabanov, AV; Kanmogne, G; Martinez-Skinner, A; McMillan, J; Mosley, RL; Nowacek, AS; Roy, U, 2011
)
0.37
"No data on once-daily dosing of nucleoside analogues in African children currently exist."( Pharmacokinetics and acceptability of once- versus twice-daily lamivudine and abacavir in HIV type-1-infected Ugandan children in the ARROW Trial.
Adkison, K; Bakeera-Kitaka, S; Burger, D; Gibb, DM; Kekitiinwa, A; Kendall, L; Mugyenyi, P; Musiime, V; Musoke, P; Odongo, F; Snowden, WB; Thomason, M; Walker, AS, 2010
)
0.36
" For both children and caregivers, once-daily dosing of lamivudine plus abacavir was highly acceptable and strongly preferred over twice-daily."( Pharmacokinetics and acceptability of once- versus twice-daily lamivudine and abacavir in HIV type-1-infected Ugandan children in the ARROW Trial.
Adkison, K; Bakeera-Kitaka, S; Burger, D; Gibb, DM; Kekitiinwa, A; Kendall, L; Mugyenyi, P; Musiime, V; Musoke, P; Odongo, F; Snowden, WB; Thomason, M; Walker, AS, 2010
)
0.36
" Once-daily dosing of abacavir and lamivudine could provide an alternative dosing strategy for HIV-1-infected children, with high acceptability and strong preference suggesting the potential for improved adherence."( Pharmacokinetics and acceptability of once- versus twice-daily lamivudine and abacavir in HIV type-1-infected Ugandan children in the ARROW Trial.
Adkison, K; Bakeera-Kitaka, S; Burger, D; Gibb, DM; Kekitiinwa, A; Kendall, L; Mugyenyi, P; Musiime, V; Musoke, P; Odongo, F; Snowden, WB; Thomason, M; Walker, AS, 2010
)
0.36
"All randomised controlled trials comparing EFV to NVP in HIV-infected individuals without prior exposure to ART, irrespective of the dosage or NRTI backbone."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, LC; Rutherford, GW; Siegfried, N; Spaulding, A, 2010
)
0.36
" Data were analysed on an intention-to-treat basis and reported as per dosage of NVP."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, LC; Rutherford, GW; Siegfried, N; Spaulding, A, 2010
)
0.36
"The trials were pooled as per dosage of NVP."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, LC; Rutherford, GW; Siegfried, N; Spaulding, A, 2010
)
0.36
"This study aimed to test whether a pharmacokinetic simulation model could extrapolate nonclinical drug data to predict human efavirenz exposure after single and continuous dosing as well as the effects of concomitant rifampicin and further to evaluate the weight-based dosage recommendations used to counteract the rifampicin-efavirenz interaction."( In silico prediction of efavirenz and rifampicin drug-drug interaction considering weight and CYP2B6 phenotype.
Ashton, M; Mukonzo, J; Rekić, D; Röshammar, D, 2011
)
0.37
" Decreases in estimated glomerular filtration rate occurred within the first few weeks of dosing in participants receiving EVG/COBI/FTC/TDF, remained within the normal range and did not progress at week 24 or 48; no participant experienced a clinical adverse event or discontinued study drug due to changes in serum creatinine or renal function."( Randomized, phase 2 evaluation of two single-tablet regimens elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate versus efavirenz/emtricitabine/tenofovir disoproxil fumarate for the initial treatment of HIV infection.
Chuck, SL; Cohen, C; DeJesus, E; Elion, R; Kearney, BP; Liu, HC; Ramanathan, S; Rashbaum, B; Ruane, P; Shamblaw, D; Warren, DR; Yale, K, 2011
)
0.37
" The peak plasma concentration (C(max)), area under the concentration-time curve for a dosing interval (AUC([τ])), and lowest plasma concentration (C(min)) for EE and NGMN during cycles of treatment with Ortho Cyclen with and without coadministration of efavirenz were compared."( The effect of efavirenz on the pharmacokinetics of an oral contraceptive containing ethinyl estradiol and norgestimate in healthy HIV-negative women.
Bertz, R; Eley, T; Garner, D; Krantz, K; Nettles, R; Persson, A; Sevinsky, H; Yones, C; Zhang, J, 2011
)
0.37
"There are potential benefits to individualizing dosage in patients treated with efavirenz (EFV)."( Successful efavirenz dose reduction guided by therapeutic drug monitoring.
Buclin, T; Calmy, A; Cavassini, M; Decosterd, LA; Delhumeau, C; di Iulio, J; Fayet Mello, A; Fleurent, A; Hirschel, B; Schneider, MP; Telenti, A, 2011
)
0.37
" All consenting participants with EFV concentrations above P75 on standard dosage were included in a dose-reduction cycle."( Successful efavirenz dose reduction guided by therapeutic drug monitoring.
Buclin, T; Calmy, A; Cavassini, M; Decosterd, LA; Delhumeau, C; di Iulio, J; Fayet Mello, A; Fleurent, A; Hirschel, B; Schneider, MP; Telenti, A, 2011
)
0.37
"Among the 3 trials, 522 subjects were treated with FTC dosed once daily and 841 subjects were treated with 3TC dosed twice daily."( Reduced emergence of the M184V/I resistance mutation when antiretroviral-naïve subjects use emtricitabine versus lamivudine in regimens composed of two NRTIs plus the NNRTI efavirenz.
Borroto-Esoda, K; Chen, SS; Harris, J; Margot, N; McColl, DJ; Miller, MD,
)
0.13
" Body weight and genetic factors will be important covariates in dosing algorithms."( Modest but variable effect of rifampin on steady-state plasma pharmacokinetics of efavirenz in healthy African-American and Caucasian volunteers.
Court, MH; Dumond, JB; Greenblatt, DJ; Kashuba, AD; Kurpewski, J; Kwara, A; Poethke, P; Tashima, KT, 2011
)
0.37
"Individuals from the CIPRA-South Africa cohort taking EFV-based antiretroviral therapy with concomitant tuberculosis (TB) were dosed with either increased (800 mg) or standard (600 mg) dose EFV during TB treatment."( Efavirenz and rifampicin in the South African context: is there a need to dose-increase efavirenz with concurrent rifampicin therapy?
Cohen, K; Conradie, F; Ive, P; Orrell, C; Sanne, I; Wood, R; Zeinecker, J, 2011
)
0.37
" Lopinavir was active at levels well below those achieved with standard dosing of coformulated lopinavir-ritonavir."( In vitro activity of antiretroviral drugs against Plasmodium falciparum.
Nsanzabana, C; Rosenthal, PJ, 2011
)
0.37
"To evaluate international pediatric efavirenz dosing recommendations using full pharmacokinetic (PK) information."( Pediatric underdosing of efavirenz: a pharmacokinetic study in Uganda.
Balungi, J; Burger, DM; Bwakura-Dangarembizi, M; Ferrier, A; Fillekes, Q; Gibb, DM; Keishanyu, R; Kendall, L; Lutakome, J; Natukunda, E; Walker, AS, 2011
)
0.37
"African children aged 3-12 years, on efavirenz dosed according to 2006 WHO/manufacturer's recommendations, had lower and highly variable efavirenz PK parameters compared with adult data from manufacturer's leaflet."( Pediatric underdosing of efavirenz: a pharmacokinetic study in Uganda.
Balungi, J; Burger, DM; Bwakura-Dangarembizi, M; Ferrier, A; Fillekes, Q; Gibb, DM; Keishanyu, R; Kendall, L; Lutakome, J; Natukunda, E; Walker, AS, 2011
)
0.37
" Information on how polymorphisms influence drug metabolism and transport to target sites is important in guiding dosage or selection of appropriate alternative therapies."( Prevalence of MDR1 C3435T and CYP2B6 G516T polymorphisms among HIV-1 infected South African patients.
Bessong, PO; Masebe, TM; Meyer, D; Ndip, RN; Nwobegahay, J, 2012
)
0.38
" Because a dose-response relationship was not identified, a second study examined a lower, 30-mg QD dose in 8 subjects (6 active and 2 placebo)."( Safety and efficacy of GSK2248761, a next-generation nonnucleoside reverse transcriptase inhibitor, in treatment-naive HIV-1-infected subjects.
Dudas, K; Dumont, E; Kim, J; Lou, Y; Mayers, D; Pietropaolo, K; Piscitelli, S; St Clair, M; White, S; Zala, C; Zhou, XJ, 2012
)
0.38
" The significant reduction in the AUC of 5-hydroxyomeprazole after repeated efavirenz dosing suggests induction of sequential metabolism and mixed inductive/inhibitory effects of efavirenz on CYP2C19."( Induction of CYP2C19 and CYP3A activity following repeated administration of efavirenz in healthy volunteers.
Aregbe, AO; Desta, Z; Flockhart, DA; Michaud, V; Ogburn, E; Quigg, TC; Thong, N, 2012
)
0.38
" Observed ART dosing took place for at least 2 weeks."( Untreated HIV infection is associated with higher blood alcohol levels.
Beatty, G; Gruber, VA; Lum, PJ; McCance-Katz, EF; Peters, M; Rainey, PM, 2012
)
0.38
" Adherence by type of ART and dosing frequency were compared by Brown-Mood median tests."( Impact of antiretroviral dosing frequency and pill burden on adherence among newly diagnosed, antiretroviral-naive HIV patients.
Buscher, A; Giordano, TP; Hartman, C; Kallen, MA, 2012
)
0.38
"We determined the pharmacokinetics of efavirenz in plasma and cerebrospinal fluid (CSF) over a 24-h dosing interval in a patient who had undergone a lumbar drain because of cryptococcal meningitis."( Efavirenz pharmacokinetics in cerebrospinal fluid and plasma over a 24-hour dosing interval.
Back, D; Dickinson, L; Watson, V; Yilmaz, A, 2012
)
0.38
" To identify risk factors for nonoptimal anticoagulation and to determine if warfarin dosing is differentially affected by specific antiretroviral agents."( Warfarin therapy in the HIV medical home model: low rates of therapeutic anticoagulation despite adherence and differences in dosing based on specific antiretrovirals.
Anderson, AM; Chane, T; Chen, S; Easley, KA; Patel, M; Xue, W, 2012
)
0.38
" RPV is dosed once daily with food and has been coformulated into a single tablet containing tenofovir and emtricitabine."( Rilpivirine, a novel non-nucleoside reverse transcriptase inhibitor for the management of HIV-1 infection: a systematic review.
Schafer, JJ; Short, WR, 2012
)
0.38
" However, the observed modest changes probably do not warrant dosage adjustment during co-administration of AL with EFV."( Concomitant efavirenz reduces pharmacokinetic exposure to the antimalarial drug artemether-lumefantrine in healthy volunteers.
Aweeka, FT; Dorsey, G; Havlir, D; Huang, L; Lizak, P; Marzan, F; Parikh, S; Rosenthal, PJ, 2012
)
0.38
" Neuropsychometric testing with drowsiness visual analogue scale, grooved pegboard and letter digit substitution tests was done the day prior to dosing and at 1, 2, 3, 4 and 6 h post-dose."( Neuropsychometric correlates of efavirenz pharmacokinetics and pharmacogenetics following a single oral dose.
Acosta, EP; Gebretsadik, T; Haas, DW; Johnson, DH; Mayo, G; Shintani, A; Stein, CM, 2013
)
0.39
" Strategies that lower Cmax during initial dosing may decrease CNS side effects."( Neuropsychometric correlates of efavirenz pharmacokinetics and pharmacogenetics following a single oral dose.
Acosta, EP; Gebretsadik, T; Haas, DW; Johnson, DH; Mayo, G; Shintani, A; Stein, CM, 2013
)
0.39
" Model-predicated area under the concentration-time curve during the dosing interval (AUC(τ)) and exposure ratios of CVF AUC(τ):BP AUC(τ) were calculated for each drug."( Pharmacokinetic modelling of efavirenz, atazanavir, lamivudine and tenofovir in the female genital tract of HIV-infected pre-menopausal women.
Cohen, MS; Dumond, JB; Forrest, A; Garonzik, SM; Kashuba, AD; Kendrick, RN; Nicol, MR; Patterson, KB, 2012
)
0.38
" Through dose-response experiments, we established relative inhibitory potencies of NRTIs on in vitro telomerase activity as compared to the inhibitory potencies of the corresponding dideoxynucleotide triphosphates."( In vitro and ex vivo inhibition of human telomerase by anti-HIV nucleoside reverse transcriptase inhibitors (NRTIs) but not by non-NRTIs.
Côté, HC; Hukezalie, KR; Thumati, NR; Wong, JM, 2012
)
0.38
"Timed plasma samples obtained throughout the dosing interval were analyzed for efavirenz concentrations with liquid chromatography/tandem mass spectrometry."( Correlates of efavirenz exposure in Chilean patients affected with human immunodeficiency virus reveals a novel association with a polymorphism in the constitutive androstane receptor.
Chaikan, A; Cortes, CP; la Porte, CJ; Owen, A; Siccardi, M; Zhang, G, 2013
)
0.39
"Literature data pertaining to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate-release (IR) solid oral dosage forms containing efavirenz as the only active pharmaceutical ingredient (API) are reviewed."( Biowaiver monographs for immediate release solid oral dosage forms: efavirenz.
Abrahamsson, B; Cristofoletti, R; Dressman, JB; Groot, DW; Kopp, S; Langguth, P; Nair, A; Polli, JE; Shah, VP, 2013
)
0.39
" Using available pharmacokinetic data, an EFV dosing schedule was developed for young co-infected children and implemented as the standard of care at Macha Hospital in Southern Province, Zambia."( Effectiveness of efavirenz-based regimens in young HIV-infected children treated for tuberculosis: a treatment option for resource-limited settings.
Bositis, C; Hamangaba, F; Moss, WJ; Sutcliffe, CG; van Dijk, JH; Watson, DC, 2013
)
0.39
" Blood plasma (for TFV, FTC, EFV, ATV and RTV concentrations) and peripheral blood mononuclear cells [PBMCs; for tenofovir diphosphate (TFV-DP) and emtricitabine triphosphate (FTC-TP) concentrations] were collected at 11 time-points over a 24-hour dosing interval."( Pharmacokinetics of two common antiretroviral regimens in older HIV-infected patients: a pilot study.
Adams, JL; Corbett, AH; Dumond, JB; Forrest, A; Jennings, SH; Kashuba, AD; Kendrick, RL; Malone, S; Patterson, KB; Prince, HM; Sykes, C; Wang, R; White, N, 2013
)
0.39
" Evaluation in clinical trials of adjusted regimens is necessary to ensure appropriate dosing for HIV-infected TB patients on an EFV-based regimen."( Model-based estimates of the effects of efavirenz on bedaquiline pharmacokinetics and suggested dose adjustments for patients coinfected with HIV and tuberculosis.
Aweeka, F; Dooley, KE; Karlsson, MO; Marzan, F; Park, JG; Svensson, EM, 2013
)
0.39
" These data do not support weight-based dosing of EFV with RIF."( Relationship between weight, efavirenz exposure, and virologic suppression in HIV-infected patients on rifampin-based tuberculosis treatment in the AIDS Clinical Trials Group A5221 STRIDE Study.
Aweeka, F; Benson, CA; Grinsztejn, B; Havlir, DV; Hogg, E; Ive, P; Lu, D; Luetkemeyer, AF; Marzan, F; Rosenkranz, SL; Sanne, IM; Swindells, S, 2013
)
0.39
"Regimen simplification can be defined as a change in established effective therapy to reduce pill burden and dosing frequency, to enhance tolerability, or to decrease specific food and fluid requirements."( Abacavir-based triple nucleoside regimens for maintenance therapy in patients with HIV.
Bosco, O; Cruciani, M; Malena, M; Mengoli, C; Parisi, SG; Serpelloni, G, 2013
)
0.39
" SJS can occur in children at any age, with any level of immunosuppression, and can occur during the lead-in dosing period of NVP."( Stevens-Johnson syndrome and HIV in children in Swaziland.
Blank, DA; Draper, HR; Dziuban, EJ; Hughey, AB; Kochelani, D; Schutze, GE; Stewart, DA, 2013
)
0.39
" However, the clinical utility or validity of introducing genotype-assisted dosing is not known."( High predictive value of CYP2B6 SNPs for steady-state plasma efavirenz levels in South African HIV/AIDS patients.
Dandara, C; Ren, Y; Skelton, M; Smith, P; Swart, M; Takuva, S, 2013
)
0.39
"Screening for CYP2B6 516G>T SNP has a high specificity and positive predictive value for efavirenz levels above 4 µg/ml and could be used in deciding on efavirenz dosage among individuals homozygous for this variant, which could lead to better precision medication."( High predictive value of CYP2B6 SNPs for steady-state plasma efavirenz levels in South African HIV/AIDS patients.
Dandara, C; Ren, Y; Skelton, M; Smith, P; Swart, M; Takuva, S, 2013
)
0.39
" Area under the curve over the dosing interval (AUC24h) and trough concentration (C0h) were estimated using a population pharmacokinetic model and compared with previous results using the 200-mg twice-daily dosage."( Pharmacokinetics and pharmacodynamics of etravirine 400 mg once daily in treatment-naïve patients.
Bickel, M; Di Perri, G; Faetkenheuer, G; Green, B; Hill, A; Kakuda, T; Kurowski, M; Morrish, G; van Delft, Y,
)
0.13
"In the SENSE trial, etravirine 400 mg once daily achieved similar exposures to historical reference data on etravirine when dosed at 200 mg twice daily."( Pharmacokinetics and pharmacodynamics of etravirine 400 mg once daily in treatment-naïve patients.
Bickel, M; Di Perri, G; Faetkenheuer, G; Green, B; Hill, A; Kakuda, T; Kurowski, M; Morrish, G; van Delft, Y,
)
0.13
" No clinically relevant interactions between daclatasvir and tenofovir disoproxil fumarate were observed for either drug, and no dosing adjustments were indicated."( Assessment of pharmacokinetic interactions of the HCV NS5A replication complex inhibitor daclatasvir with antiretroviral agents: ritonavir-boosted atazanavir, efavirenz and tenofovir.
Bertz, R; Bifano, M; Grasela, D; Hartstra, J; Hwang, C; Kandoussi, H; Oosterhuis, B; Sevinsky, H; Tiessen, R; Velinova-Donga, M, 2013
)
0.39
" However, no orally dosed HIV nanomedicines are available clinically to patients."( Antiretroviral solid drug nanoparticles with enhanced oral bioavailability: production, characterization, and in vitro-in vivo correlation.
Curley, P; Foster, AJ; Giardiello, M; Khoo, SH; Liptrott, NJ; Long, J; Martin, P; McDonald, TO; Owen, A; Rannard, SP; Roberts, P; Schipani, A; Siccardi, M; Smith, D, 2014
)
0.4
" The developed model may serve as the foundation for further exploration of pharmacogenetic-based dosing of EFV."( Population pharmacogenetic-based pharmacokinetic modeling of efavirenz, 7-hydroxy- and 8-hydroxyefavirenz.
Abdelhady, AM; Desta, Z; Jiang, F; Overholser, BR; Shin, JG; Yeo, CW, 2014
)
0.4
"At weeks 12 and 24, all 49 dosed subjects remained suppressed on RPV/FTC/TDF."( Efficacy and safety 48 weeks after switching from efavirenz to rilpivirine using emtricitabine/tenofovir disoproxil fumarate-based single-tablet regimens.
Brinson, C; Cheng, AK; Chuck, SK; Cohen, C; Dejesus, E; Mills, AM; Ramanathan, S; Wang, MH; White, K; Williams, S; Yale, KL,
)
0.13
" Plasma efavirenz concentrations 12 h after dosing were measured using a validated high-performance liquid chromatography."( Low level of efavirenz in HIV-1-infected Thai adults is associated with the CYP2B6 polymorphism.
Chamnanphol, M; Jantararoungtong, T; Koomdee, N; Manosuthi, W; Prommas, S; Puangpetch, A; Santon, S; Sukasem, C; Sungkanuparph, S, 2014
)
0.4
" At 12 weeks after ART, plasma efavirenz concentrations at 12h after dosing were measured."( CYP2B6 haplotype and biological factors responsible for hepatotoxicity in HIV-infected patients receiving efavirenz-based antiretroviral therapy.
Lueangniyomkul, A; Mankatitham, W; Manosuthi, S; Manosuthi, W; Nilkamhang, S; Sukasem, C; Sungkanuparph, S; Thongyen, S, 2014
)
0.4
"Differences in drug metabolism due to cytochrome P450 (CYP) polymorphisms may be significant enough to warrant different dosing strategies in carriers of specific cytochrome P450 (CYP) polymorphisms, especially for drugs with a narrow therapeutic index."( Impact of CYP polymorphisms, ethnicity and sex differences in metabolism on dosing strategies: the case of efavirenz.
Chetty, M; Chetty, VV; Naidoo, P, 2014
)
0.4
" The corresponding dosing strategies developed for carriers of specific CYP2B6 genotypes were also reviewed."( Impact of CYP polymorphisms, ethnicity and sex differences in metabolism on dosing strategies: the case of efavirenz.
Chetty, M; Chetty, VV; Naidoo, P, 2014
)
0.4
" Ethnic differences and the associated prevalence of CYP2B6 polymorphisms result in significant differences in the PKPD associated with a standard 600 mg per day dose of EFV, warranting dosage reduction in carriers of specific CYP2B6 polymorphisms."( Impact of CYP polymorphisms, ethnicity and sex differences in metabolism on dosing strategies: the case of efavirenz.
Chetty, M; Chetty, VV; Naidoo, P, 2014
)
0.4
"Using EFV as an example of a drug with a narrow therapeutic index and a high inter-patient variability in plasma concentrations corresponding to a standard dose of the drug, this review demonstrates how genotyping of the primary metabolising enzyme can be useful for appropriate dosage adjustments in individuals."( Impact of CYP polymorphisms, ethnicity and sex differences in metabolism on dosing strategies: the case of efavirenz.
Chetty, M; Chetty, VV; Naidoo, P, 2014
)
0.4
" At 12 and 24 weeks after antiretroviral therapy, plasma efavirenz concentrations at 12 h after dosing were measured."( CYP2B6 18492T->C polymorphism compromises efavirenz concentration in coinfected HIV and tuberculosis patients carrying CYP2B6 haplotype *1/*1.
Manosuthi, S; Manosuthi, W; Nilkamhang, S; Sukasem, C; Sungkanuparph, S; Thongyen, S, 2014
)
0.4
"The individualization of EFV dosage guided by genotyping 516G>T CYP2B6 and therapeutic drug monitoring could increase the efficiency of EFV use in antiretroviral treatment."( Dose reduction of efavirenz: an observational study describing cost-effectiveness, pharmacokinetics and pharmacogenetics.
Calvo Hernández, MV; Figueroa, SC; García-Berrocal, B; Gómez, AI; Gonzalez-Buitrago, JM; Isidoro-García, M; Martín, AF; Martín, AS; Sánchez, MC; Tovar, CB; Valverde Merino, MP, 2014
)
0.4
" Pharmacokinetic sampling occurred at the end of each dosing period."( Phase I safety, pharmacokinetics, and pharmacogenetics study of the antituberculosis drug PA-824 with concomitant lopinavir-ritonavir, efavirenz, or rifampin.
Allen, R; Aweeka, F; Bao, J; Cramer, Y; Dooley, KE; Haas, DW; Koletar, SL; Luetkemeyer, AF; Marzan, F; Murray, S; Park, JG; Savic, R; Sutherland, D, 2014
)
0.4
" A PAS population pharmacokinetic model in two dosing regimens was developed; potential covariates affecting its pharmacokinetics were examined, and Monte Carlo simulations were conducted evaluating the pharmacokinetic-pharmacodynamic index."( Pharmacokinetics of para-aminosalicylic acid in HIV-uninfected and HIV-coinfected tuberculosis patients receiving antiretroviral therapy, managed for multidrug-resistant and extensively drug-resistant tuberculosis.
de Kock, L; Derendorf, H; Diacon, AH; Donald, PR; Hernandez, KR; Prescott, K; Rosenkranz, B; Sy, SK; Yu, M, 2014
)
0.4
" EFV concentrations from DBS were approximately 42% lower than the paired plasma values, and the ratio of blood/plasma did not change over the dosing interval."( A validated method for quantification of efavirenz in dried blood spots using high-performance liquid chromatography-mass spectrometry.
Amara, AB; Back, DJ; Else, LJ; Khoo, S; Olagunju, A; Puls, RL; Tjia, J, 2015
)
0.42
" This modelling technique is able to inform the design of clinical studies, and allows assessment of pragmatic dosing strategies under complex therapeutic scenarios."( Use of in vitro to in vivo extrapolation to predict the optimal strategy for patients switching from efavirenz to maraviroc or nevirapine.
Back, D; Davies, G; Khoo, S; Owen, A; Schipani, A; Siccardi, M, 2015
)
0.42
" Therefore, no efavirenz dosage adjustment during rifampicin cotreatment is required in Ugandans."( CYP2B6 genotype, but not rifampicin-based anti-TB cotreatments, explains variability in long-term efavirenz plasma exposure.
Aklillu, E; Gustafson, LL; Mukonzo, JK; Nanzigu, S; Ogwal-Okeng, J; Waako, P, 2014
)
0.4
" Polymorphisms in important drug metabolizing enzymes and the implications for EFV dosing were investigated."( Efavirenz dosing: influence of drug metabolizing enzyme polymorphisms and concurrent tuberculosis treatment.
Abdool Karim, SS; Botha, JH; Gengiah, TN; Naidoo, K; Yende-Zuma, N, 2015
)
0.42
" Whether standard antiretroviral drug dosage is adequate in heavy individuals remains unresolved."( Impact of body weight on virological and immunological responses to efavirenz-containing regimens in HIV-infected, treatment-naive adults.
Ammassari, A; Battegay, M; Bonora, S; Burger, D; Chêne, G; Dauchy, FA; Fehr, J; Ghosn, J; Gianotti, N; Gogos, C; Grarup, J; Launay, O; Marzolini, C; Mocroft, A; Mussini, C; Obel, N; Raffi, F; Roca, B; Sabin, C; Siccardi, M; Torti, C; Zangerle, R, 2015
)
0.42
"Virological and immunological responses to initial EFV-containing regimens were not impaired in heavy individuals, suggesting that the standard 600 mg EFV dosage is appropriate across a wide weight range."( Impact of body weight on virological and immunological responses to efavirenz-containing regimens in HIV-infected, treatment-naive adults.
Ammassari, A; Battegay, M; Bonora, S; Burger, D; Chêne, G; Dauchy, FA; Fehr, J; Ghosn, J; Gianotti, N; Gogos, C; Grarup, J; Launay, O; Marzolini, C; Mocroft, A; Mussini, C; Obel, N; Raffi, F; Roca, B; Sabin, C; Siccardi, M; Torti, C; Zangerle, R, 2015
)
0.42
" Geometric mean CSF efavirenz, 7OH-, and 8OH-efavirenz concentrations (with 90% confidence intervals [CIs]) for the 400-mg and 600-mg dosing groups were 16."( Cerebrospinal fluid exposure of efavirenz and its major metabolites when dosed at 400 mg and 600 mg once daily: a randomized controlled trial.
Amara, A; Amin, J; Avihingsanon, A; Avinghsanon, A; Barber, T; Chetchotisakd, P; Clarke, A; Cooper, DA; Else, L; Emery, S; Jessen, H; Khoo, S; Owen, A; Puls, R; Winston, A, 2015
)
0.42
" In conclusion, this genotypic resistance analysis strongly suggests that the latest NNRTI, rilpivirine, may retain activity in a large proportion of HIV-1 patients in whom resistance failed while they were on an efavirenz- or nevirapine-containing regimen, and may present an attractive option for second-line treatment given its good safety profile and dosing convenience."( Predicted residual activity of rilpivirine in HIV-1 infected patients failing therapy including NNRTIs efavirenz or nevirapine.
Camacho, RJ; Gomes, P; Rhee, SY; Theys, K; Vandamme, AM, 2015
)
0.42
" Here, we used mass spectrometry imaging with infrared matrix-assisted laser desorption-electrospray ionization to quantify the distribution of efavirenz within tissues from a macaque dosed orally to a steady state."( Mass spectrometry imaging reveals heterogeneous efavirenz distribution within putative HIV reservoirs.
Adamson, L; Bokhart, MT; Fedoriw, Y; Kashuba, AD; Luciw, PA; Muddiman, DC; Rosen, EP; Sykes, C; Thompson, CG, 2015
)
0.42
" Infant plasma concentrations did not change significantly during the dosing interval, 157 ng/mL (28."( Breast milk pharmacokinetics of efavirenz and breastfed infants' exposure in genetically defined subgroups of mother-infant pairs: an observational study.
Adejuyigbe, E; Amara, A; Back, D; Bolaji, O; Else, L; Khoo, S; Olagunju, A; Owen, A; Siccardi, M; Waitt, C, 2015
)
0.42
" This study used population pharmacokinetics modeling to explore the influence of demographic and pharmacogenetic factors including efavirenz-rifampicin interaction on EFV pharmacokinetics, towards safer dosing of EFV."( CYP2B6*6, CYP2B6*18, Body weight and sex are predictors of efavirenz pharmacokinetics and treatment response: population pharmacokinetic modeling in an HIV/AIDS and TB cohort in Zimbabwe.
Chonzi, P; Dhoro, M; Kadzirange, G; Masimirembwa, C; Ngara, B; Nhachi, C; Zvada, S, 2015
)
0.42
" Optimal lumefantrine dosage regimen for patients on EFV-based ART was determined by population pharmacokinetics and simulation."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.42
" The predictive model through simulation of lumefantrine exposure at different dosage regimen scenarios for patients on EFV-based ART, suggest that AL taken twice daily for five days using the current dose could improve lumefantrine exposure and consequently malaria treatment outcomes."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.42
" The impact of HAART on imatinib may depend on whether it is being initiated or has already been dosed chronically in patients."( Human hepatocyte assessment of imatinib drug-drug interactions - complexities in clinical translation.
Beumer, JH; Christner, SM; Kiesel, BF; Parise, RA; Pillai, VC; Rudek, MA; Venkataramanan, R, 2015
)
0.42
" Simulations for a normalized population receiving US Food and Drug Administration weight-band dosing predicted that 15% of children would have a C12 below target threshold (<1."( Efavirenz Concentrations and Probability of HIV Replication in Children.
Aurpibul, L; Bouazza, N; Chanta, C; Cressey, TR; Homkham, N; Ingsrisawang, L; Jourdain, G; Kamonpakorn, N; Krikajornkitti, S; Lallemant, M; Narkbunnam, T; Salvadori, N; Treluyer, JM; Urien, S, 2015
)
0.42
" EFV area under the plasma concentration-time curve over 1 dosing interval from time 0 to 24 hours postdose values were generally suboptimal (<110 μM × h) in subjects younger than 3 years treated with oral solution; these subjects switched to capsule sprinkle."( Efavirenz Capsule Sprinkle and Liquid Formulations With Didanosine and Emtricitabine in HIV-1-infected Infants and Children 3 Months to 6 Years of Age: Study AI266-922.
Biguenet, S; Bunupuradah, T; Krystal, M; Lataillade, M; Pavia-Ruz, N; Rossouw, M; Sáez-Llorens, X; Seekins, D; Sevinsky, H; Taylor, M; Yang, R, 2015
)
0.42
" Absence of hypersensitivity reactions, superior resistance profile and once-daily dosing favours abacavir for African children, supporting WHO 2013 guidelines."( Abacavir, zidovudine, or stavudine as paediatric tablets for African HIV-infected children (CHAPAS-3): an open-label, parallel-group, randomised controlled trial.
Abongomera, G; Asiimwe, A; Burger, D; Chabala, C; Chintu, C; Cook, AD; Gibb, DM; Kekitiinwa, A; Kenny, J; Kityo, C; Klein, N; McIlleron, H; Mirembe, G; Mulenga, V; Musiime, V; Owen-Powell, E; Thomason, MJ; Walker, AS, 2016
)
0.43
" The erosion and drug release kinetics from organogels under conventional (filling gelatin capsules) or multiparticulate (beads obtained by prilling) dosage forms were measured in simulated gastric and intestinal fluids."( Factors influencing the erosion rate and the drug release kinetics from organogels designed as matrices for oral controlled release of a hydrophobic drug.
Franceschi, S; Girod Fullana, S; Pereira Camelo, SR; Perez, E; Ré, MI, 2016
)
0.43
"To assess the cost-effectiveness of CYP2B6 genotyping to guide efavirenz dosing for initial HIV therapy in the USA."( Cost-effectiveness of CYP2B6 genotyping to optimize efavirenz dosing in HIV clinical practice.
Freedberg, KA; Haas, DW; Li, XC; Park, SS; Schackman, BR, 2015
)
0.42
"Current care without CYP2B6 genotyping has an incremental cost-effectiveness ratio >$100,000/QALY compared with genotype-guided dosing, even if lower dosing reduces efficacy."( Cost-effectiveness of CYP2B6 genotyping to optimize efavirenz dosing in HIV clinical practice.
Freedberg, KA; Haas, DW; Li, XC; Park, SS; Schackman, BR, 2015
)
0.42
"CYP2B6 genotyping can inform efavirenz dosing and decrease HIV therapy cost."( Cost-effectiveness of CYP2B6 genotyping to optimize efavirenz dosing in HIV clinical practice.
Freedberg, KA; Haas, DW; Li, XC; Park, SS; Schackman, BR, 2015
)
0.42
"9% for the GG genotype (reduced dosage required), 36."( Prevalence of CYP2B6 polymorphisms in Argentinians: the role of genetic testing.
Argibay, PF; Belloso, WH; Cajal, AR; Scibona, P; Vazquez, C, 2015
)
0.42
" The population pharmacokinetic-pharmacodynamic (PK-PD) model shows that favorable HDL cholesterol changes can be expected in children with current efavirenz dosing guidelines over 5 years of treatment."( A Population Pharmacokinetic/Pharmacodynamic Model Predicts Favorable HDL Cholesterol Changes Over the First 5 Years in Children Treated With Current Efavirenz-Based Regimens.
Bhakeecheep, S; Bouazza, N; Coeur, SL; Cressey, TR; Homkham, N; Hongsiriwon, S; Ingsrisawang, L; Jourdain, G; Kanjanavanit, S; Ngampiyaskul, C; Salvadori, N; Srirojana, S; Treluyer, JM; Urien, S, 2016
)
0.43
"Twenty-nine subjects completed both dosing cohorts."( Efavirenz but Not Atazanavir/Ritonavir Significantly Reduces Atovaquone Concentrations in HIV-Infected Subjects.
Alfaro, RM; Calderón, MM; Kovacs, JA; Kumar, P; McManus, M; Pau, AK; Penzak, SR, 2016
)
0.43
"Population pharmacokinetic (PopPK) analyses often rely on steady state and full adherence to prescribed dosage regimen assumptions from data gathered during therapeutic drug monitoring (TDM)."( Comparison of Population Pharmacokinetics Based on Steady-State Assumption Versus Electronically Monitored Adherence to Lopinavir, Atazanavir, Efavirenz, and Etravirine: A Retrospective Study.
Buclin, T; Bugnon, O; Cavassini, M; Csajka, C; Fuchs, A; Rotzinger, A; Schneider, MP, 2016
)
0.43
"Published PopPK models for lopinavir, atazanavir, efavirenz, and etravirine were applied to estimate PK parameters and individual concentrations in 140 HIV patients taking part in a medication adherence program using 2 dosing data sets."( Comparison of Population Pharmacokinetics Based on Steady-State Assumption Versus Electronically Monitored Adherence to Lopinavir, Atazanavir, Efavirenz, and Etravirine: A Retrospective Study.
Buclin, T; Bugnon, O; Cavassini, M; Csajka, C; Fuchs, A; Rotzinger, A; Schneider, MP, 2016
)
0.43
"Clearance estimates and likewise predicted concentrations did not markedly differ between the 2 dosing histories."( Comparison of Population Pharmacokinetics Based on Steady-State Assumption Versus Electronically Monitored Adherence to Lopinavir, Atazanavir, Efavirenz, and Etravirine: A Retrospective Study.
Buclin, T; Bugnon, O; Cavassini, M; Csajka, C; Fuchs, A; Rotzinger, A; Schneider, MP, 2016
)
0.43
"PopPK analysis assuming steady state with full adherence produced similar results to those based on detailed electronic dosing history reconciled with patients' allegations."( Comparison of Population Pharmacokinetics Based on Steady-State Assumption Versus Electronically Monitored Adherence to Lopinavir, Atazanavir, Efavirenz, and Etravirine: A Retrospective Study.
Buclin, T; Bugnon, O; Cavassini, M; Csajka, C; Fuchs, A; Rotzinger, A; Schneider, MP, 2016
)
0.43
"Around 450 and 250 mg daily doses might meet EFV dosing needs of HIV-TB infected Ugandans in general and CYP2B6*6/*6 genotypes, respectively."( CYP2B6 genotype-based efavirenz dose recommendations during rifampicin-based antituberculosis cotreatment for a sub-Saharan Africa population.
Aklillu, E; Bisaso, RK; Gustafsson, LL; Mukonzo, JK; Ogwal-Okeng, J; Owen, JS, 2016
)
0.43
" Further evaluation of the impact of CYP2B6 polymorphisms on EFV PK showed that the identification of CYP2B6 genetic status is not predictive of EFV exposure and thus not informative to guide pediatric dosing regimens."( Population Pharmacokinetics Analysis To Inform Efavirenz Dosing Recommendations in Pediatric HIV Patients Aged 3 Months to 3 Years.
Bertz, R; Chapel, S; Cirincione, B; Luo, M; Roy, A; Savant, I; Sevinsky, H, 2016
)
0.43
" The DDI risk for cobimetinib with other CYP3A4 inhibitors and inducers needs to be assessed in order to provide dosing instructions."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
0.43
"This study demonstrates the value of using PBPK simulation to assess the clinical DDI risk inorder to provide dosing instructions with other CYP3A4 perpetrators."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
0.43
" Coadministration of Kaletra (lopinavir/ritonavir) with delamanid resulted in an approximately 25% higher delamanid area under the concentration-time curve from time 0 to the end of the dosing interval (AUCτ)."( Delamanid Coadministered with Antiretroviral Drugs or Antituberculosis Drugs Shows No Clinically Relevant Drug-Drug Interactions in Healthy Subjects.
Geiter, L; Mallikaarjun, S; Paccaly, A; Patil, S; Petersen, C; Shoaf, SE; Wells, C, 2016
)
0.43
"The first-generation integrase inhibitors (INIs) raltegravir (RAL) and elvitegravir (EVG) have shown efficacy against HIV infection, but they have the limitations of once-more daily dosing and extensive cross-resistance."( Dolutegravir(DTG, S/GSK1349572) combined with other ARTs is superior to RAL- or EFV-based regimens for treatment of HIV-1 infection: a meta-analysis of randomized controlled trials.
Chen, H; Guo, W; Huang, J; Jiang, J; Liang, B; Liang, H; Liao, Y; Su, J; Xu, X; Ye, L; Zang, N, 2016
)
0.43
"According to simulations, a paediatric efavirenz/lamivudine/abacavir fixed-dose formulation of 150 mg efavirenz, 75 mg lamivudine and 150 mg abacavir provided the most effective and safe concentrations across WHO weight bands, with the flexibility of dosage required across the paediatric population."( Optimization of the strength of the efavirenz/lamivudine/abacavir fixed-dose combination for paediatric patients.
Bienczak, A; Bouazza, N; Burger, D; Capparelli, EV; Cressey, TR; Denti, P; Foissac, F; Lallemant, M; McIlleron, H; Penazzato, M; Treluyer, JM; Urien, S, 2017
)
0.46
"We included all randomized controlled trials (RCTs) that compared EFV to NVP in people with HIV without prior exposure to ART, irrespective of the dosage or NRTI's given in combination."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside or nucleotide-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, L; Mursleen, S; Rutherford, GW; Siegfried, N; Spaulding, AB, 2016
)
0.43
" We performed subgroup analyses for concurrent treatment for tuberculosis and dosage of NVP."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside or nucleotide-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, L; Mursleen, S; Rutherford, GW; Siegfried, N; Spaulding, AB, 2016
)
0.43
" The powders obtained, which present enhanced dissolution properties, can be incorporated in a solid dosage form for treatment of AIDS in paediatric patients with promising results."( Efavirenz dissolution enhancement III: Colloid milling, pharmacokinetics and electronic tongue evaluation.
Bilatto, SE; Cabral, LM; Corrêa, DS; da Costa, MA; Fandaruff, C; Hoffmeister, CR; Pitta, LR; Prado, LD; Rocha, HV; Silva, MA; Tasso, L, 2017
)
0.46
"We compared the pharmacokinetics of moxifloxacin during rifampicin co-treatment or when dosed alone in African patients with drug-susceptible recurrent TB."( Effect of rifampicin and efavirenz on moxifloxacin concentrations when co-administered in patients with drug-susceptible TB.
Adamson, J; Chirehwa, M; Denti, P; Essack, S; Govender, K; Kimba-Phongi, E; McIlleron, H; Naidoo, A; Naidoo, K; Padayatchi, N; Yende-Zuma, N, 2017
)
0.46
" Genotype-directed dosing yields therapeutic EFV concentrations and appears to outperform other dosing approaches."( CYP2B6 genotype-directed dosing is required for optimal efavirenz exposure in children 3-36 months with HIV infection.
Benns, A; Bolton Moore, C; Borkowsky, W; Bwakura-Dangarembizi, M; Capparelli, EV; Chadwick, EG; Hawkins, E; Heckman, B; Jean-Philippe, P; Loftis, A; Purdue, L; Samson, P; Spector, SA; Wallis, C; Worrell, C, 2017
)
0.46
" It is desirable for multidrug combinations to be coformulated into single dosage forms where possible, to promote patient convenience and adherence to dosage regimens, for which amorphous solid dispersion (ASD) is particularly well-suited."( Multidrug, Anti-HIV Amorphous Solid Dispersions: Nature and Mechanisms of Impacts of Drugs on Each Other's Solution Concentrations.
Arca, HÇ; Dahal, D; Edgar, KJ; Mosquera-Giraldo, LI; Taylor, LS, 2017
)
0.46
" There are concerns about the appropriateness of current EFV dosing and it has been discussed whether EFV dosing should be adapted according to genotype in children as suggested for adults."( Genetic variants in CYP2B6 and CYP2A6 explain interindividual variation in efavirenz plasma concentrations of HIV-infected children with diverse ethnic origin.
Dahl, ML; Eriksen, J; Gustafsson, LL; Navér, L; Österberg, E; Rubin, J; Soeria-Atmadja, S, 2017
)
0.46
"To investigate if pediatric EFV dosing should be guided by genetic variation in drug metabolizing enzymes rather than by body weight."( Genetic variants in CYP2B6 and CYP2A6 explain interindividual variation in efavirenz plasma concentrations of HIV-infected children with diverse ethnic origin.
Dahl, ML; Eriksen, J; Gustafsson, LL; Navér, L; Österberg, E; Rubin, J; Soeria-Atmadja, S, 2017
)
0.46
" Knowledge about individual variants in key drug metabolizing enzyme genes could improve clinical safety and genotype directed dosing could achieve more predictable EFV plasma concentrations in HIV-infected children."( Genetic variants in CYP2B6 and CYP2A6 explain interindividual variation in efavirenz plasma concentrations of HIV-infected children with diverse ethnic origin.
Dahl, ML; Eriksen, J; Gustafsson, LL; Navér, L; Österberg, E; Rubin, J; Soeria-Atmadja, S, 2017
)
0.46
"For HIV-infected pregnant women receiving efavirenz, low daily DHA-PQ dosing was predicted to improve protection against parasitemia and reduce risk of toxicity compared to monthly dosing."( Predicting Optimal Dihydroartemisinin-Piperaquine Regimens to Prevent Malaria During Pregnancy for Human Immunodeficiency Virus-Infected Women Receiving Efavirenz.
Aweeka, F; Dorsey, G; Havlir, D; Huang, L; Jagannathan, P; Kakuru, A; Kamya, M; Muhindo, M; Nakalembe, M; Natureeba, P; Rosenthal, PJ; Savic, RM; Vucicevic, K; Wallender, E, 2018
)
0.48
" According to the World Health Organization, a similar dosing strategy for all patient populations is desirable for universal roll-out; however, it remains unknown whether the 400 mg daily dose is adequate during pregnancy."( A Mechanism-Based Population Pharmacokinetic Analysis Assessing the Feasibility of Efavirenz Dose Reduction to 400 mg in Pregnant Women.
Best, BM; Burger, DM; Capparelli, E; Colbers, AC; Cressey, TR; Denti, P; Dooley, KE; Greupink, R; Huitema, ADR; Mirochnick, M; Russel, FGM; Schalkwijk, S; Ter Heine, R, 2018
)
0.48
" CYP2B6 genotyping but not anti-tuberculosis co-treatment should guide efavirenz dosing to optimize treatment outcomes."( Long-term efavirenz pharmacokinetics is comparable between Tanzanian HIV and HIV/Tuberculosis patients with the same CYP2B6*6 genotype.
Aklillu, E; Bertilsson, L; Burhenne, J; Janabi, M; Kitabi, EN; Minzi, OMS; Mugusi, F; Mugusi, S; Sasi, P, 2018
)
0.48
" Adult rhesus macaques were dosed daily with 200 mg EFV (as part of a four-drug regimen) for 10 days."( Predicting Efavirenz Concentrations in the Brain Tissue of HIV-Infected Individuals and Exploring their Relationship to Neurocognitive Impairment.
Adamson, L; Blake, KH; Eron, JJ; Forrest, A; Joseph, SB; Kashuba, ADM; Kincer, LP; Luciw, P; Menezes, P; Price, RW; Robertson, K; Schauer, AP; Spudich, S; Srinivas, N; Swanstrom, R; Sykes, C; White, N, 2019
)
0.51
"Pharmacokinetics studies recommend increasing efavirenz dosage in tuberculosis/HIV patients using rifampicin."( Daily 800 mg versus 600 mg Efavirenz for HIV Patients Treating Tuberculosis with a Rifampicin-Based Regimen: An Open Label Randomized Controlled Trial.
do Brasil, PEAA; Hadad, DJ; Maia, IR; Rolla, V; Sant'anna, FM; Schmaltz, CAS; Trajman, A; Xavier, MS, 2018
)
0.48
"CYP2B6 516 genotype-directed dosing improves efavirenz (EFV) exposures in HIV-infected children younger than 36 months, but such data are lacking in those with tuberculosis (TB) coinfection."( Establishing Dosing Recommendations for Efavirenz in HIV/TB-Coinfected Children Younger Than 3 Years.
Benns, A; Bwakura Dangarembizi, M; Capparelli, EV; Chadwick, EG; Chakhtoura, N; Jackson, C; Jean-Philippe, P; Libous, JL; Moore, CB; Purdue, L; Samson, P; Spector, SA; Wallis, C; Zimmer, B, 2019
)
0.51
"Genotype-directed dosing safely achieved therapeutic EFV concentrations and virologic suppression in HIV/TB-coinfected children younger than 24 months, but further study is needed to confirm appropriate dosing in those aged 24-36 months."( Establishing Dosing Recommendations for Efavirenz in HIV/TB-Coinfected Children Younger Than 3 Years.
Benns, A; Bwakura Dangarembizi, M; Capparelli, EV; Chadwick, EG; Chakhtoura, N; Jackson, C; Jean-Philippe, P; Libous, JL; Moore, CB; Purdue, L; Samson, P; Spector, SA; Wallis, C; Zimmer, B, 2019
)
0.51
"The current WHO weight-based dosing recommendations for efavirenz result in a wide variability of drug exposure in children."( Population pharmacokinetics of efavirenz in HIV and TB/HIV coinfected children: the significance of genotype-guided dosing.
Alghamdi, WA; Antwi, S; Dompreh, A; Enimil, A; Kwara, A; Langaee, T; Peloquin, CA; Wiesner, L; Yang, H, 2019
)
0.51
" In addition, dosing efavirenz in children based only on weight results in a large variability in drug exposure."( Population pharmacokinetics of efavirenz in HIV and TB/HIV coinfected children: the significance of genotype-guided dosing.
Alghamdi, WA; Antwi, S; Dompreh, A; Enimil, A; Kwara, A; Langaee, T; Peloquin, CA; Wiesner, L; Yang, H, 2019
)
0.51
" Therefore, the physicochemical properties of polymorphic forms from active pharmaceutical ingredients (APIs) should be carefully considered in dosage forms pre-formulation approaches."( Polymorphic properties and dissolution profile of efavirenz due to solvents recrystallization.
Soewandhi, SN; Suendo, V; Wardhana, YW; Wikarsa, S, 2019
)
0.51
" Additionally, we observe additive inhibitory activity against pseudotyped viruses when B#24 is dosed in competition with the clinically used non-nucleoside reverse transcriptase inhibitor (NNRTI) efavirenz."( Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
Banerjee, S; Blakemore, PR; Brack-Werner, R; Herrmann, A; Loesgen, S; Milicevic Sephton, S; Neuhaus, GF; Overacker, RD; Strother, JA, 2019
)
0.51
" To promote the tolerance of efavirenz, it is better to adjust the dosage of efavirenz according to the polymorphisms of CYP2B6-516 in HIV-infected adults."( Meta-analysis of the associations of CYP2B6-516G>T polymorphisms with efavirenz-induced central nervous system side effects and virological outcome in HIV-infected adults.
Cheng, L; Feng, W; Li, X; Sun, F; Wang, Y; Weng, B; Xia, P; Yuan, Q, 2020
)
0.56
" Lopinavir TDM excluded pharmacokinetic reasons for failure in patients failing treatment when lopinavir dosing was supervised."( Pediatric Antiretroviral Therapeutic Drug Monitoring: A Five and a Half Year Experience from a South African Tertiary Hospital.
Decloedt, EH; Engelbrecht, AE; Norman, J; Rabie, H; Wiesner, L, 2020
)
0.56
" These data suggest that malaria and HIV coinfected pregnant women may require adjustments in AL dosage or treatment duration to achieve exposure comparable with HIV-uninfected pregnant women."( Efavirenz-Based Antiretroviral Therapy Reduces Artemether-Lumefantrine Exposure for Malaria Treatment in HIV-Infected Pregnant Women.
Aweeka, F; Huang, L; Hughes, E; Kajubi, R; Mwebaza, N; Mwima, MW; Nguyen, V; Nyunt, MM; Orukan, F; Parikh, S, 2020
)
0.56
" A novel dosing strategy that has the potential to reduce isoniazid-related toxicity and treatment failure is presented."( Model-Based Assessment of Variability in Isoniazid Pharmacokinetics and Metabolism in Patients Co-Infected With Tuberculosis and HIV: Implications for a Novel Dosing Strategy.
Äbelö, A; Ashton, M; Bienvenu, E; Birgersson, S; Janzén, D; Sundell, J, 2020
)
0.56
" The current PBPK model, which considers changes in unbound potency-adjusted active species, can be used to inform dosing recommendations when abemaciclib is coadministered with CYP3A4 perpetrators."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
0.56
" This warrants further investigations of other drug-drug interactions for optimising dosing in genetically defined subgroups, particularly during drug development."( Influence of selected polymorphisms in disposition genes on lumefantrine pharmacokinetics when coadministered with efavirenz.
Adeagbo, BA; Adegbola, AJ; Bolaji, OO; Bolarinwa, RA; Olagunju, AE; Owen, A; Rana, A; Siccardi, M, 2020
)
0.56
" However, dosage recommendations incorporating CYP2B6 516G > T polymorphism have not been investigated in the Thai population."( Dosage Optimization of Efavirenz Based on a Population Pharmacokinetic-Pharmacogenetic Model of HIV-infected Patients in Thailand.
Avihingsanon, A; Chaivichacharn, P; Manosuthi, W; Punyawudho, B; Shotelersuk, V; Tongkobpetch, S; Ubolyam, S, 2020
)
0.56
" Vaginal film is becoming more acceptable and a convenient dosage form compared to cream, gel and suppository."( Efavirenz nanomicelles loaded vaginal film (EZ film) for preexposure prophylaxis (PrEP) of HIV.
Cetindag, E; Dave, R; Fu, Y; Gandhi, T; Jablonski, J; Mediouni, S; Patel, K; Patki, M; Valente, ST; Vartak, R, 2020
)
0.56
" It has several advantages for pediatric patients, as the dosage form disintegrates quickly in the mouth and does not require water for administration, thereby improving patient compliance with the treatment."( Development of Pediatric Orodispersible Tablets Based on Efavirenz as a New Therapeutic Alternative.
Ângelos, MA; da Silva, RMF; de Freitas Neto, JL; de Melo, CG; do Nascimento Gomes Barbosa, I; Dos Santos Mendes, LM; Ferreira, MRA; Neto, PJR; Rolim, LA; Soares, LAL, 2020
)
0.56
"Supersaturable SMEDDS, a versatile dosage form, was investigated for improving the biopharmaceutical attributes and eradicating the food effect of poorly water soluble drug efavirenz."( Polymeric Precipitation Inhibitor Assisted Supersaturable SMEDDS of Efavirenz Based on Experimental Observations and Molecular Mechanics.
Bedi, N; Mahajan, S; Sheikh, BA; Singh, D; Singh, M, 2021
)
0.62
"Findings will provide timely information on the safety, efficacy, and optimal dosing of t-PA to treat moderate/severe COVID-19-induced ARDS, which can be rapidly adapted to a phase III trial (NCT04357730; FDA IND 149634)."(
Abbasi, S; Abd El-Wahab, A; Abdallah, M; Abebe, G; Aca-Aca, G; Adama, S; Adefegha, SA; Adidigue-Ndiome, R; Adiseshaiah, P; Adrario, E; Aghajanian, C; Agnese, W; Ahmad, A; Ahmad, I; Ahmed, MFE; Akcay, OF; Akinmoladun, AC; Akutagawa, T; Alakavuklar, MA; Álava-Rabasa, S; Albaladejo-Florín, MJ; Alexandra, AJE; Alfawares, R; Alferiev, IS; Alghamdi, HS; Ali, I; Allard, B; Allen, JD; Almada, E; Alobaid, A; Alonso, GL; Alqahtani, YS; Alqarawi, W; Alsaleh, H; Alyami, BA; Amaral, BPD; Amaro, JT; Amin, SAW; Amodio, E; Amoo, ZA; Andia Biraro, I; Angiolella, L; Anheyer, D; Anlay, DZ; Annex, BH; Antonio-Aguirre, B; Apple, S; Arbuznikov, AV; Arinsoy, T; Armstrong, DK; Ash, S; Aslam, M; Asrie, F; Astur, DC; Atzrodt, J; Au, DW; Aucoin, M; Auerbach, EJ; Azarian, S; Ba, D; Bai, Z; Baisch, PRM; Balkissou, AD; Baltzopoulos, V; Banaszewski, M; Banerjee, S; Bao, Y; Baradwan, A; Barandika, JF; Barger, PM; Barion, MRL; Barrett, CD; Basudan, AM; Baur, LE; Baz-Rodríguez, SA; Beamer, P; Beaulant, A; Becker, DF; Beckers, C; Bedel, J; Bedlack, R; Bermúdez de Castro, JM; Berry, JD; Berthier, C; Bhattacharya, D; Biadgo, B; Bianco, G; Bianco, M; Bibi, S; Bigliardi, AP; Billheimer, D; Birnie, DH; Biswas, K; Blair, HC; Bognetti, P; Bolan, PJ; Bolla, JR; Bolze, A; Bonnaillie, P; Borlimi, R; Bórquez, J; Bottari, NB; Boulleys-Nana, JR; Brighetti, G; Brodeur, GM; Budnyak, T; Budnyk, S; Bukirwa, VD; Bulman, DM; Burm, R; Busman-Sahay, K; Butcher, TW; Cai, C; Cai, H; Cai, L; Cairati, M; Calvano, CD; Camacho-Ordóñez, A; Camela, E; Cameron, T; Campbell, BS; Cansian, RL; Cao, Y; Caporale, AS; Carciofi, AC; Cardozo, V; Carè, J; Carlos, AF; Carozza, R; Carroll, CJW; Carsetti, A; Carubelli, V; Casarotta, E; Casas, M; Caselli, G; Castillo-Lora, J; Cataldi, TRI; Cavalcante, ELB; Cavaleiro, A; Cayci, Z; Cebrián-Tarancón, C; Cedrone, E; Cella, D; Cereda, C; Ceretti, A; Ceroni, M; Cha, YH; Chai, X; Chang, EF; Chang, TS; Chanteux, H; Chao, M; Chaplin, BP; Chaturvedi, S; Chaturvedi, V; Chaudhary, DK; Chen, A; Chen, C; Chen, HY; Chen, J; Chen, JJ; Chen, K; Chen, L; Chen, Q; Chen, R; Chen, SY; Chen, TY; Chen, WM; Chen, X; Chen, Y; Cheng, G; Cheng, GJ; Cheng, J; Cheng, YH; Cheon, HG; Chew, KW; Chhoker, S; Chiu, WN; Choi, ES; Choi, MJ; Choi, SD; Chokshi, S; Chorny, M; Chu, KI; Chu, WJ; Church, AL; Cirrincione, A; Clamp, AR; Cleff, MB; Cohen, M; Coleman, RL; Collins, SL; Colombo, N; Conduit, N; Cong, WL; Connelly, MA; Connor, J; Cooley, K; Correa Ramos Leal, I; Cose, S; Costantino, C; Cottrell, M; Cui, L; Cundall, J; Cutaia, C; Cutler, CW; Cuypers, ML; da Silva Júnior, FMR; Dahal, RH; Damiani, E; Damtie, D; Dan-Li, W; Dang, Z; Dasa, SSK; Davin, A; Davis, DR; de Andrade, CM; de Jong, PL; de Oliveira, D; de Paula Dorigam, JC; Dean, A; Deepa, M; Delatour, C; Dell'Aiera, S; Delley, MF; den Boer, RB; Deng, L; Deng, Q; Depner, RM; Derdau, V; Derici, U; DeSantis, AJ; Desmarini, D; Diffo-Sonkoue, L; Divizia, M; Djenabou, A; Djordjevic, JT; Dobrovolskaia, MA; Domizi, R; Donati, A; Dong, Y; Dos Santos, M; Dos Santos, MP; Douglas, RG; Duarte, PF; Dullaart, RPF; Duscha, BD; Edwards, LA; Edwards, TE; Eichenwald, EC; El-Baba, TJ; Elashiry, M; Elashiry, MM; Elashry, SH; Elliott, A; Elsayed, R; Emerson, MS; Emmanuel, YO; Emory, TH; Endale-Mangamba, LM; Enten, GA; Estefanía-Fernández, K; Estes, JD; Estrada-Mena, FJ; Evans, S; Ezra, L; Faria de, RO; Farraj, AK; Favre, C; Feng, B; Feng, J; Feng, L; Feng, W; Feng, X; Feng, Z; Fernandes, CLF; Fernández-Cuadros, ME; Fernie, AR; Ferrari, D; Florindo, PR; Fong, PC; Fontes, EPB; Fontinha, D; Fornari, VJ; Fox, NP; Fu, Q; Fujitaka, Y; Fukuhara, K; Fumeaux, T; Fuqua, C; Fustinoni, S; Gabbanelli, V; Gaikwad, S; Gall, ET; Galli, A; Gancedo, MA; Gandhi, MM; Gao, D; Gao, K; Gao, M; Gao, Q; Gao, X; Gao, Y; Gaponenko, V; Garber, A; Garcia, EM; García-Campos, C; García-Donas, J; García-Pérez, AL; Gasparri, F; Ge, C; Ge, D; Ge, JB; Ge, X; George, I; George, LA; Germani, G; Ghassemi Tabrizi, S; Gibon, Y; Gillent, E; Gillies, RS; Gilmour, MI; Goble, S; Goh, JC; Goiri, F; Goldfinger, LE; Golian, M; Gómez, MA; Gonçalves, J; Góngora-García, OR; Gonul, I; González, MA; Govers, TM; Grant, PC; Gray, EH; Gray, JE; Green, MS; Greenwald, I; Gregory, MJ; Gretzke, D; Griffin-Nolan, RJ; Griffith, DC; Gruppen, EG; Guaita, A; Guan, P; Guan, X; Guerci, P; Guerrero, DT; Guo, M; Guo, P; Guo, R; Guo, X; Gupta, J; Guz, G; Hajizadeh, N; Hamada, H; Haman-Wabi, AB; Han, TT; Hannan, N; Hao, S; Harjola, VP; Harmon, M; Hartmann, MSM; Hartwig, JF; Hasani, M; Hawthorne, WJ; Haykal-Coates, N; Hazari, MS; He, DL; He, P; He, SG; Héau, C; Hebbar Kannur, K; Helvaci, O; Heuberger, DM; Hidalgo, F; Hilty, MP; Hirata, K; Hirsch, A; Hoffman, AM; Hoffmann, JF; Holloway, RW; Holmes, RK; Hong, S; Hongisto, M; Hopf, NB; Hörlein, R; Hoshino, N; Hou, Y; Hoven, NF; Hsieh, YY; Hsu, CT; Hu, CW; Hu, JH; Hu, MY; Hu, Y; Hu, Z; Huang, C; Huang, D; Huang, DQ; Huang, L; Huang, Q; Huang, R; Huang, S; Huang, SC; Huang, W; Huang, Y; Huffman, KM; Hung, CH; Hung, CT; Huurman, R; Hwang, SM; Hyun, S; Ibrahim, AM; Iddi-Faical, A; Immordino, P; Isla, MI; Jacquemond, V; Jacques, T; Jankowska, E; Jansen, JA; Jäntti, T; Jaque-Fernandez, F; Jarvis, GA; Jatt, LP; Jeon, JW; Jeong, SH; Jhunjhunwala, R; Ji, F; Jia, X; Jia, Y; Jian-Bo, Z; Jiang, GD; Jiang, L; Jiang, W; Jiang, WD; Jiang, Z; Jiménez-Hoyos, CA; Jin, S; Jobling, MG; John, CM; John, T; Johnson, CB; Jones, KI; Jones, WS; Joseph, OO; Ju, C; Judeinstein, P; Junges, A; Junnarkar, M; Jurkko, R; Kaleka, CC; Kamath, AV; Kang, X; Kantsadi, AL; Kapoor, M; Karim, Z; Kashuba, ADM; Kassa, E; Kasztura, M; Kataja, A; Katoh, T; Kaufman, JS; Kaupp, M; Kehinde, O; Kehrenberg, C; Kemper, N; Kerr, CW; Khan, AU; Khan, MF; Khan, ZUH; Khojasteh, SC; Kilburn, S; Kim, CG; Kim, DU; Kim, DY; Kim, HJ; Kim, J; Kim, OH; Kim, YH; King, C; Klein, A; Klingler, L; Knapp, AK; Ko, TK; Kodavanti, UP; Kolla, V; Kong, L; Kong, RY; Kong, X; Kore, S; Kortz, U; Korucu, B; Kovacs, A; Krahnert, I; Kraus, WE; Kuang, SY; Kuehn-Hajder, JE; Kurz, M; Kuśtrowski, P; Kwak, YD; Kyttaris, VC; Laga, SM; Laguerre, A; Laloo, A; Langaro, MC; Langham, MC; Lao, X; Larocca, MC; Lassus, J; Lattimer, TA; Lazar, S; Le, MH; Leal, DB; Leal, M; Leary, A; Ledermann, JA; Lee, JF; Lee, MV; Lee, NH; Leeds, CM; Leeds, JS; Lefrandt, JD; Leicht, AS; Leonard, M; Lev, S; Levy, K; Li, B; Li, C; Li, CM; Li, DH; Li, H; Li, J; Li, L; Li, LJ; Li, N; Li, P; Li, T; Li, X; Li, XH; Li, XQ; Li, XX; Li, Y; Li, Z; Li, ZY; Liao, YF; Lin, CC; Lin, MH; Lin, Y; Ling, Y; Links, TP; Lira-Romero, E; Liu, C; Liu, D; Liu, H; Liu, J; Liu, L; Liu, LP; Liu, M; Liu, T; Liu, W; Liu, X; Liu, XH; Liu, Y; Liuwantara, D; Ljumanovic, N; Lobo, L; Lokhande, K; Lopes, A; Lopes, RMRM; López-Gutiérrez, JC; López-Muñoz, MJ; López-Santamaría, M; Lorenzo, C; Lorusso, D; Losito, I; Lu, C; Lu, H; Lu, HZ; Lu, SH; Lu, SN; Lu, Y; Lu, ZY; Luboga, F; Luo, JJ; Luo, KL; Luo, Y; Lutomski, CA; Lv, W; M Piedade, MF; Ma, J; Ma, JQ; Ma, JX; Ma, N; Ma, P; Ma, S; Maciel, M; Madureira, M; Maganaris, C; Maginn, EJ; Mahnashi, MH; Maierhofer, M; Majetschak, M; Malla, TR; Maloney, L; Mann, DL; Mansuri, A; Marelli, E; Margulis, CJ; Marrella, A; Martin, BL; Martín-Francés, L; Martínez de Pinillos, M; Martínez-Navarro, EM; Martinez-Quintanilla Jimenez, D; Martínez-Velasco, A; Martínez-Villaseñor, L; Martinón-Torres, M; Martins, BA; Massongo, M; Mathew, AP; Mathews, D; Matsui, J; Matsumoto, KI; Mau, T; Maves, RC; Mayclin, SJ; Mayer, JM; Maynard, ND; Mayr, T; Mboowa, MG; McEvoy, MP; McIntyre, RC; McKay, JA; McPhail, MJW; McVeigh, AL; Mebazaa, A; Medici, V; Medina, DN; Mehmood, T; Mei-Li, C; Melku, M; Meloncelli, S; Mendes, GC; Mendoza-Velásquez, C; Mercadante, R; Mercado, MI; Merenda, MEZ; Meunier, J; Mi, SL; Michels, M; Mijatovic, V; Mikhailov, V; Milheiro, SA; Miller, DC; Ming, F; Mitsuishi, M; Miyashita, T; Mo, J; Mo, S; Modesto-Mata, M; Moeller, S; Monte, A; Monteiro, L; Montomoli, J; Moore, EE; Moore, HB; Moore, PK; Mor, MK; Moratalla-López, N; Moratilla Lapeña, L; Moreira, R; Moreno, MA; Mörk, AC; Morton, M; Mosier, JM; Mou, LH; Mougharbel, AS; Muccillo-Baisch, AL; Muñoz-Serrano, AJ; Mustafa, B; Nair, GM; Nakanishi, I; Nakanjako, D; Naraparaju, K; Nawani, N; Neffati, R; Neil, EC; Neilipovitz, D; Neira-Borrajo, I; Nelson, MT; Nery, PB; Nese, M; Nguyen, F; Nguyen, MH; Niazy, AA; Nicolaï, J; Nogueira, F; Norbäck, D; Novaretti, JV; O'Donnell, T; O'Dowd, A; O'Malley, DM; Oaknin, A; Ogata, K; Ohkubo, K; Ojha, M; Olaleye, MT; Olawande, B; Olomo, EJ; Ong, EWY; Ono, A; Onwumere, J; Ortiz Bibriesca, DM; Ou, X; Oza, AM; Ozturk, K; Özütemiz, C; Palacio-Pastrana, C; Palaparthi, A; Palevsky, PM; Pan, K; Pantanetti, S; Papachristou, DJ; Pariani, A; Parikh, CR; Parissis, J; Paroul, N; Parry, S; Patel, N; Patel, SM; Patel, VC; Pawar, S; Pefura-Yone, EW; Peixoto Andrade, BCO; Pelepenko, LE; Peña-Lora, D; Peng, S; Pérez-Moro, OS; Perez-Ortiz, AC; Perry, LM; Peter, CM; Phillips, NJ; Phillips, P; Pia Tek, J; Piner, LW; Pinto, EA; Pinto, SN; Piyachaturawat, P; Poka-Mayap, V; Polledri, E; Poloni, TE; Ponessa, G; Poole, ST; Post, AK; Potter, TM; Pressly, BB; Prouty, MG; Prudêncio, M; Pulkki, K; Pupier, C; Qian, H; Qian, ZP; Qiu, Y; Qu, G; Rahimi, S; Rahman, AU; Ramadan, H; Ramanna, S; Ramirez, I; Randolph, GJ; Rasheed, A; Rault, J; Raviprakash, V; Reale, E; Redpath, C; Rema, V; Remucal, CK; Remy, D; Ren, T; Ribeiro, LB; Riboli, G; Richards, J; Rieger, V; Rieusset, J; Riva, A; Rivabella Maknis, T; Robbins, JL; Robinson, CV; Roche-Campo, F; Rodriguez, R; Rodríguez-de-Cía, J; Rollenhagen, JE; Rosen, EP; Rub, D; Rubin, N; Rubin, NT; Ruurda, JP; Saad, O; Sabell, T; Saber, SE; Sabet, M; Sadek, MM; Saejio, A; Salinas, RM; Saliu, IO; Sande, D; Sang, D; Sangenito, LS; Santos, ALSD; Sarmiento Caldas, MC; Sassaroli, S; Sassi, V; Sato, J; Sauaia, A; Saunders, K; Saunders, PR; Savarino, SJ; Scambia, G; Scanlon, N; Schetinger, MR; Schinkel, AFL; Schladweiler, MC; Schofield, CJ; Schuepbach, RA; Schulz, J; Schwartz, N; Scorcella, C; Seeley, J; Seemann, F; Seinige, D; Sengoku, T; Seravalli, J; Sgromo, B; Shaheen, MY; Shan, L; Shanmugam, S; Shao, H; Sharma, S; Shaw, KJ; Shen, BQ; Shen, CH; Shen, P; Shen, S; Shen, Y; Shen, Z; Shi, J; Shi-Li, L; Shimoda, K; Shoji, Y; Shun, C; Silva, MA; Silva-Cardoso, J; Simas, NK; Simirgiotis, MJ; Sincock, SA; Singh, MP; Sionis, A; Siu, J; Sivieri, EM; Sjerps, MJ; Skoczen, SL; Slabon, A; Slette, IJ; Smith, MD; Smith, S; Smith, TG; Snapp, KS; Snow, SJ; Soares, MCF; Soberman, D; Solares, MD; Soliman, I; Song, J; Sorooshian, A; Sorrell, TC; Spinar, J; Staudt, A; Steinhart, C; Stern, ST; Stevens, DM; Stiers, KM; Stimming, U; Su, YG; Subbian, V; Suga, H; Sukhija-Cohen, A; Suksamrarn, A; Suksen, K; Sun, J; Sun, M; Sun, P; Sun, W; Sun, XF; Sun, Y; Sundell, J; Susan, LF; Sutjarit, N; Swamy, KV; Swisher, EM; Sykes, C; Takahashi, JA; Talmor, DS; Tan, B; Tan, ZK; Tang, L; Tang, S; Tanner, JJ; Tanwar, M; Tarazi, Z; Tarvasmäki, T; Tay, FR; Teketel, A; Temitayo, GI; Thersleff, T; Thiessen Philbrook, H; Thompson, LC; Thongon, N; Tian, B; Tian, F; Tian, Q; Timothy, AT; Tingle, MD; Titze, IR; Tolppanen, H; Tong, W; Toyoda, H; Tronconi, L; Tseng, CH; Tu, H; Tu, YJ; Tung, SY; Turpault, S; Tuynman, JB; Uemoto, AT; Ugurlu, M; Ullah, S; Underwood, RS; Ungell, AL; Usandizaga-Elio, I; Vakonakis, I; van Boxel, GI; van den Beucken, JJJP; van der Boom, T; van Slegtenhorst, MA; Vanni, JR; Vaquera, A; Vasconcellos, RS; Velayos, M; Vena, R; Ventura, G; Verso, MG; Vincent, RP; Vitale, F; Vitali, S; Vlek, SL; Vleugels, MPH; Volkmann, N; Vukelic, M; Wagner Mackenzie, B; Wairagala, P; Waller, SB; Wan, J; Wan, MT; Wan, Y; Wang, CC; Wang, H; Wang, J; Wang, JF; Wang, K; Wang, L; Wang, M; Wang, S; Wang, WM; Wang, X; Wang, Y; Wang, YD; Wang, YF; Wang, Z; Wang, ZG; Warriner, K; Weberpals, JI; Weerachayaphorn, J; Wehrli, FW; Wei, J; Wei, KL; Weinheimer, CJ; Weisbord, SD; Wen, S; Wendel Garcia, PD; Williams, JW; Williams, R; Winkler, C; Wirman, AP; Wong, S; Woods, CM; Wu, B; Wu, C; Wu, F; Wu, P; Wu, S; Wu, Y; Wu, YN; Wu, ZH; Wurtzel, JGT; Xia, L; Xia, Z; Xia, ZZ; Xiao, H; Xie, C; Xin, ZM; Xing, Y; Xing, Z; Xu, S; Xu, SB; Xu, T; Xu, X; Xu, Y; Xue, L; Xun, J; Yaffe, MB; Yalew, A; Yamamoto, S; Yan, D; Yan, H; Yan, S; Yan, X; Yang, AD; Yang, E; Yang, H; Yang, J; Yang, JL; Yang, K; Yang, M; Yang, P; Yang, Q; Yang, S; Yang, W; Yang, X; Yang, Y; Yao, JC; Yao, WL; Yao, Y; Yaqub, TB; Ye, J; Ye, W; Yen, CW; Yeter, HH; Yin, C; Yip, V; Yong-Yi, J; Yu, HJ; Yu, MF; Yu, S; Yu, W; Yu, WW; Yu, X; Yuan, P; Yuan, Q; Yue, XY; Zaia, AA; Zakhary, SY; Zalwango, F; Zamalloa, A; Zamparo, P; Zampini, IC; Zani, JL; Zeitoun, R; Zeng, N; Zenteno, JC; Zepeda-Palacio, C; Zhai, C; Zhang, B; Zhang, G; Zhang, J; Zhang, K; Zhang, Q; Zhang, R; Zhang, T; Zhang, X; Zhang, Y; Zhang, YY; Zhao, B; Zhao, D; Zhao, G; Zhao, H; Zhao, Q; Zhao, R; Zhao, S; Zhao, T; Zhao, X; Zhao, XA; Zhao, Y; Zhao, Z; Zheng, Z; Zhi-Min, G; Zhou, CL; Zhou, HD; Zhou, J; Zhou, W; Zhou, XQ; Zhou, Z; Zhu, C; Zhu, H; Zhu, L; Zhu, Y; Zitzmann, N; Zou, L; Zou, Y, 2022
)
0.72
" The objectives of this article are to present an overview of nonparametric methods used in population pharmacokinetic modeling and to explain their specific characteristics to inform scientists and clinicians about their potential value for data analysis, simulation, dosage design, and therapeutic drug monitoring (TDM)."( Nonparametric Methods in Population Pharmacokinetics.
Bourguignon, L; Goutelle, S; Neely, M; Woillard, JB; Yamada, W, 2022
)
0.72
" "Untimed" EFV concentrations with unknown dosing and collection time were assessed using a validated liquid chromatography-tandem mass spectrometry method."( Untimed Efavirenz Drug Levels After Switching From Brand to Generic Formulations: A Short Communication.
Atkinson, K; Auyeung, K; Barrios, R; Baynes, KA; Brumme, CJ; Lepik, KJ; Sereda, P; Toy, J; Watson, BE, 2021
)
0.62
"The present study endeavors quality by design (QbD) assisted chromatographic method for the quantification of Efavirenz (ERZ) in bulk and tablet dosage form."( Quantification and Validation of Stability-Indicating RP-HPLC Method for Efavirenz in Bulk and Tablet Dosage Form using Quality by Design (QbD): A Shifting Paradigm.
Bari, SB; Gurumukhi, VC, 2022
)
0.72
"1 ng/mL), resulting in contraception failure, when depot medroxyprogesterone is dosed at 12-week intervals."( A Semimechanistic Pharmacokinetic Model for Depot Medroxyprogesterone Acetate and Drug-Drug Interactions With Antiretroviral and Antituberculosis Treatment.
Cohn, SE; Denti, P; Dooley, KE; Firnhaber, C; Francis, J; Godfrey, C; Kendall, MA; McIlleron, H; Mngqibisa, R; Wu, X, 2021
)
0.62
"Study A5338 suggested that more frequent depot MPA dosing may be appropriate for women receiving rifampicin, isoniazid, and efavirenz."( Pharmacogenetics of interaction between depot medroxyprogesterone acetate and efavirenz, rifampicin, and isoniazid during treatment of HIV and tuberculosis.
Angira, F; Badal-Faesen, S; Baker, P; Cohn, SE; Denti, P; Francis, J; Haas, DW; Kendall, MA; Mawlana, S; McIlleron, H; Mngqibisa, R; Omoz-Oarhe, A; Robinson, JA; Samaneka, WP, 2022
)
0.72
" TB therapy (isoniazid and rifampin) led to a 29% decreased clearance, however Monte Carlo simulations demonstrated the majority of participants on TB therapy receiving standard EFV dosing to be in the target area under the curve range."( Impact of CYP2B6 genotype, tuberculosis therapy, and formulation on efavirenz pharmacokinetics in infants and children under 40 months of age.
Benns, A; Bolton Moore, C; Bwakura-Dangarembizi, M; Capparelli, EV; Chadwick, EG; Chakhtoura, N; Frenkel, L; Jean-Philippe, P; Libous, J; Nikanjam, M; Samson, P; Spector, SA; Tran, L; Zimmer, B, 2022
)
0.72
"EFV dosing should account for CYP2B6 516 genotype and formulation, but does not require adjustment for concurrent TB therapy."( Impact of CYP2B6 genotype, tuberculosis therapy, and formulation on efavirenz pharmacokinetics in infants and children under 40 months of age.
Benns, A; Bolton Moore, C; Bwakura-Dangarembizi, M; Capparelli, EV; Chadwick, EG; Chakhtoura, N; Frenkel, L; Jean-Philippe, P; Libous, J; Nikanjam, M; Samson, P; Spector, SA; Tran, L; Zimmer, B, 2022
)
0.72
" There are only 200 mg and 600 mg dosage forms of EFV in China."( Efficacy and safety of Efavirenz 400 mg-based regimens switching from 600 mg-based regimens in people living with HIV with virological suppression in China: a randomized, open-label, non-inferiority study.
Han, J; Li, B; Liu, Y; Xiao, J; Zhang, L; Zhao, H, 2022
)
0.72
" This study aimed to develop a population pharmacokinetic model to characterize the disposition of maraviroc in neonates to inform dosing regimens and expand available options."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
" The final model was used in Monte Carlo simulations to generate expected exposures with recommended dosing regimens."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
" Monte Carlo simulations with FDA-approved weight band dosing resulted in the majority of simulated patients (84."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
"While maraviroc apparent clearance is decreased in the first few days of life, the current FDA-approved maraviroc weight band dosing provides maraviroc exposures for neonates in the first 6 weeks of life, which were consistent with adult maraviroc exposure range."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
"Dolutegravir concentrations are reduced by efavirenz induction effect necessitating twice-daily dolutegravir dosing when coadministered."( Initial Supplementary Dose of Dolutegravir in Second-Line Antiretroviral Therapy: A Noncomparative, Double-Blind, Randomized Placebo-Controlled Trial.
Griesel, R; Hill, A; Keene, C; Maartens, G; Meintjes, G; Omar, Z; Simmons, B; van Zyl, G; Zhao, Y, 2023
)
0.91
" Therefore, in addition to body weight, pediatric dosing of EFV should consider pharmacogenetic variability, duration of therapy, and individual treatment outcomes."( Genetic and non-genetic factors influencing efavirenz population pharmacokinetics among human immunodeficiency virus-1-infected children in Ethiopia.
Ahmed, JH; Aklillu, E; Chaka, TE; Chala, A; Kitabi, EN; Makonnen, E; Tadesse, BT, 2023
)
0.91
" A verified PBPK model for efavirenz describing the CYP3A4- and CYP2B6-mediated auto-induction during multiple dosing was reported previously and was applied in this study to predict the exposure of efavirenz in vulnerable populations, including children (down to the age of 3 months), mothers, and breastfeeding infants, accounting for the various CYP2B6 genotypes."( Physiologically Based Pharmacokinetic Modeling to Determine the Impact of CYP2B6 Genotype on Efavirenz Exposure in Children, Mothers and Breastfeeding Infants.
Pan, X; Rowland Yeo, K, 2023
)
0.91
"Our simulations support the common practice of maintaining the adjusted dosage of a drug for another 2 weeks after stopping an inducer."( Management of Drug Interactions with Inducers: Onset and Disappearance of Induction on Cytochrome P450 3A4 and Uridine Diphosphate Glucuronosyltransferase 1A1 Substrates.
Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023
)
0.91
" Due to their long dosing interval, clinical studies with IM CAB/RPV are challenging."( Intramuscular cabotegravir and rilpivirine concentrations after switching from efavirenz-containing regimen.
Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023
)
0.91
"The current World Health Organization (WHO) pediatric tuberculosis dosing guidelines lead to suboptimal drug exposures."( Evaluating pediatric tuberculosis dosing guidelines: A model-based individual data pooled analysis.
Aarnoutse, R; Chabala, C; Cotton, MF; Denti, P; Galileya, LT; Gibb, D; Hesseling, A; Lee, J; McIlleron, H; Njahira Mukui, I; Rabie, H; Turkova, A; Wasmann, RE; Zar, H, 2023
)
0.91
" The importance of the drug-drug interactions with lopinavir/ritonavir and efavirenz should be evaluated further and considered in future dosing guidance."( Evaluating pediatric tuberculosis dosing guidelines: A model-based individual data pooled analysis.
Aarnoutse, R; Chabala, C; Cotton, MF; Denti, P; Galileya, LT; Gibb, D; Hesseling, A; Lee, J; McIlleron, H; Njahira Mukui, I; Rabie, H; Turkova, A; Wasmann, RE; Zar, H, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
HIV-1 reverse transcriptase inhibitorAn entity which inhibits the activity of HIV-1 reverse transcriptase.
antiviral drugA substance used in the prophylaxis or therapy of virus diseases.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
benzoxazine
acetylenic compoundAny organic molecule containing a C#C bond.
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
cyclopropanesCyclopropane and its derivatives formed by substitution.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (87)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency31.62285.623417.292931.6228AID485281
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency26.83253.189029.884159.4836AID1224846
RAR-related orphan receptor gammaMus musculus (house mouse)Potency26.60320.006038.004119,952.5996AID1159523
SMAD family member 2Homo sapiens (human)Potency13.44810.173734.304761.8120AID1346924
PPM1D proteinHomo sapiens (human)Potency44.07830.00529.466132.9993AID1347411
SMAD family member 3Homo sapiens (human)Potency13.44810.173734.304761.8120AID1346924
TDP1 proteinHomo sapiens (human)Potency23.32220.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency15.60400.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency19.10520.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743054; AID743063
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency29.84930.013326.981070.7614AID1346978
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency23.71010.000657.913322,387.1992AID1259378
progesterone receptorHomo sapiens (human)Potency15.60400.000417.946075.1148AID1346784; AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency8.89200.01237.983543.2770AID1346984; AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency25.37350.000214.376460.0339AID720691; AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.28740.003041.611522,387.1992AID1159552; AID1159555
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency23.01810.001530.607315,848.9004AID1224841; AID1224848; AID1224849; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency33.48890.375827.485161.6524AID743217
pregnane X nuclear receptorHomo sapiens (human)Potency23.12530.005428.02631,258.9301AID1346982; AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency27.03980.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743078; AID743079; AID743080; AID743091
GVesicular stomatitis virusPotency17.37680.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency27.54040.00108.379861.1304AID1645840
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency33.48890.001019.414170.9645AID743191
caspase-3Homo sapiens (human)Potency29.84930.013326.981070.7614AID1346978
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency23.71010.001723.839378.1014AID743083
thyroid stimulating hormone receptorHomo sapiens (human)Potency12.23520.001628.015177.1139AID1224843; AID1224895
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency26.832519.739145.978464.9432AID1159509
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency15.59610.057821.109761.2679AID1159526; AID1159528
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency28.18380.10009.191631.6228AID1346983
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency26.60320.000323.4451159.6830AID743065; AID743067
heat shock protein beta-1Homo sapiens (human)Potency33.48890.042027.378961.6448AID743210; AID743228
mitogen-activated protein kinase 1Homo sapiens (human)Potency15.84890.039816.784239.8107AID1454
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency15.55540.000627.21521,122.0200AID743202; AID743219
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency12.58930.00798.23321,122.0200AID2546
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.00000.015812.3113615.5000AID1461
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency21.13170.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency40.26380.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency17.37680.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency33.49150.002319.595674.0614AID651631; AID720552
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency21.13170.001551.739315,848.9004AID1259244
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency28.18380.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency17.37680.01238.964839.8107AID1645842
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency29.84930.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency29.84930.011912.222168.7989AID651632
cytochrome P450 2C9, partialHomo sapiens (human)Potency17.37680.01238.964839.8107AID1645842
Chain A, Ferritin light chainEquus caballus (horse)Potency11.22025.623417.292931.6228AID485281
glp-1 receptor, partialHomo sapiens (human)Potency19.95260.01846.806014.1254AID624417
Fumarate hydrataseHomo sapiens (human)Potency37.22120.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency56.23410.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency23.26260.000811.382244.6684AID686978; AID686979
Smad3Homo sapiens (human)Potency15.84890.00527.809829.0929AID588855
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency13.45040.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency24.91780.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency11.22020.28189.721235.4813AID2326
GVesicular stomatitis virusPotency11.98770.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency16.93300.00108.379861.1304AID1645840
polyproteinZika virusPotency37.22120.00308.794948.0869AID1347053
IDH1Homo sapiens (human)Potency32.64270.005210.865235.4813AID686970
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency32.64270.00419.984825.9290AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency5.01193.548119.542744.6684AID743266
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency28.18380.00798.23321,122.0200AID2546
gemininHomo sapiens (human)Potency27.89220.004611.374133.4983AID624296
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency36.12540.005612.367736.1254AID624032
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency112.20206.309660.2008112.2020AID720707
Interferon betaHomo sapiens (human)Potency11.98770.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
TAR DNA-binding protein 43Homo sapiens (human)Potency35.48131.778316.208135.4813AID652104
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency31.62283.981146.7448112.2020AID720708
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, POL POLYPROTEINHuman immunodeficiency virus 1IC50 (µMol)0.26120.00250.26120.5200AID977608
Chain A, POL POLYPROTEINHuman immunodeficiency virus 1IC50 (µMol)0.26120.00250.26120.5200AID977608
Chain B, POL POLYPROTEINHuman immunodeficiency virus 1IC50 (µMol)0.26120.00250.26120.5200AID977608
Chain A, POL POLYPROTEINHuman immunodeficiency virus 1IC50 (µMol)0.26120.00250.26120.5200AID977608
Chain B, POL POLYPROTEINHuman immunodeficiency virus 1IC50 (µMol)0.26120.00250.26120.5200AID977608
Chain A, Pol PolyproteinHuman immunodeficiency virus 1IC50 (µMol)0.26120.00250.26120.5200AID977608
Chain B, Pol PolyproteinHuman immunodeficiency virus 1IC50 (µMol)0.26120.00250.26120.5200AID977608
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Prothrombin Bos taurus (cattle)IC50 (µMol)0.02200.00890.88576.0000AID1191671
Gag-Pol polyproteinHIV-1 M:B_HXB2RIC50 (µMol)2.17780.00060.91418.3200AID1795395; AID1795423; AID1795433; AID1795434; AID1795435; AID1795436; AID1795437; AID1795438; AID1795727; AID1795743; AID1798815; AID1801910; AID1802513; AID1802514; AID1802605
Gag-Pol polyproteinHIV-1 M:B_HXB2RKi0.14000.00000.51449.0000AID1798816
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (NEW YORK-5 ISOLATE)IC50 (µMol)0.02000.00020.10421.7000AID1801804
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.01800.00030.71237.0700AID573468
Cannabinoid receptor 1Mus musculus (house mouse)Ki0.01000.00060.72467.2000AID736440
Microsomal triglyceride transfer protein large subunitHomo sapiens (human)IC50 (µMol)0.05400.00000.72635.7500AID266346
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)IC50 (µMol)0.00400.00021.014010.0000AID299022
Envelope glycoprotein gp160 [Cleaved into: Surface protein gp120 Human immunodeficiency virus 1IC50 (µMol)0.00350.00352.70228.7000AID1624241
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)1.36530.00011.076810.0000AID104448; AID1059142; AID1069710; AID1126511; AID1141975; AID1141976; AID1165079; AID1171593; AID1171594; AID1171595; AID1171596; AID1171598; AID1191404; AID1191671; AID1198749; AID1198752; AID1198754; AID1206939; AID1231487; AID1235381; AID1248227; AID1249724; AID1272056; AID1298247; AID1298248; AID1298249; AID1298250; AID1298251; AID1298253; AID1304407; AID1316359; AID1320869; AID1352323; AID1373153; AID1379964; AID1391076; AID1391088; AID1410405; AID1410486; AID1418468; AID143393; AID1457063; AID1457064; AID1457065; AID1485966; AID1485969; AID1485970; AID1485971; AID1485972; AID1485973; AID1485974; AID1485975; AID1520066; AID1535529; AID1558858; AID1565088; AID1572530; AID1594861; AID1596756; AID1609110; AID1627029; AID1687691; AID1693803; AID1705194; AID1705195; AID1729163; AID1731753; AID1750722; AID1767116; AID1811038; AID1815396; AID1822283; AID1847040; AID1880369; AID1884230; AID1884494; AID197777; AID197783; AID197931; AID197932; AID197933; AID197934; AID198099; AID198237; AID198385; AID198399; AID198563; AID199102; AID200153; AID241471; AID241472; AID241533; AID241665; AID266345; AID266346; AID266347; AID266348; AID267644; AID279321; AID279324; AID279325; AID282736; AID282737; AID282738; AID282739; AID282740; AID299022; AID342718; AID347085; AID347086; AID347087; AID360705; AID386493; AID391221; AID391222; AID391223; AID397176; AID404605; AID430054; AID457955; AID457959; AID457960; AID457961; AID518734; AID518735; AID518737; AID518738; AID557019; AID557043; AID557044; AID573464; AID573465; AID573466; AID573468; AID573469; AID573470; AID583849; AID583863; AID620437; AID649485; AID649486; AID649488; AID698145; AID698146; AID757621; AID779524; AID82961
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Ki0.29390.00031.552310.0000AID1594861; AID198768; AID198769; AID198911; AID198912; AID198913; AID198915; AID198916; AID198917; AID302259; AID302260; AID368564; AID368565; AID368566; AID368567; AID368568; AID368569; AID370724; AID370725; AID370726; AID370727; AID605176; AID605177; AID605178; AID622047; AID622049; AID622052; AID736038; AID736040; AID736041; AID736438; AID736439; AID736440
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)20.60000.00401.966610.0000AID1873200
Reverse transcriptase Human immunodeficiency virus 1IC50 (µMol)0.06430.01000.53567.1300AID1815391; AID1815397; AID1815398; AID1815399; AID1815400; AID1815401; AID1815402
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1EC50 (µMol)0.09000.00040.61539.7000AID1326646; AID1326647; AID1373152; AID1373158; AID1373159; AID1373160; AID1373161; AID1373162; AID1373163; AID1407642; AID1410481; AID1410482; AID1421325; AID1456307; AID1456308; AID1483271; AID1483272; AID1483273; AID1483274; AID1483275; AID1483276; AID1483277; AID1750717; AID1750718; AID1750719; AID240140; AID267854; AID267855; AID267856; AID267858; AID366548; AID366549; AID366550
Reverse transcriptase Human immunodeficiency virus 1EC50 (µMol)0.10530.00021.16839.0740AID1731746; AID1731747; AID1731749; AID1731750; AID1731751; AID1741393; AID1741394; AID1741395; AID1741396; AID1741397
Cholesterol 24-hydroxylaseHomo sapiens (human)Kd5.33330.05002.00005.0000AID1653622; AID1653623; AID1653636
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)ID500.40000.40000.40000.4000AID298089
Cytochrome P450 2B6Homo sapiens (human)Km0.45000.45000.45000.4500AID1168819
AcetylcholinesteraseRattus norvegicus (Norway rat)ID500.08000.08000.08000.0800AID650690
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Activity0.23940.00091.30738.0000AID199980
Reverse transcriptase/RNaseH Human immunodeficiency virus 1C907.30007.30007.30007.3000AID141362
Reverse transcriptase/RNaseH Human immunodeficiency virus 1ED500.05520.00020.99359.8000AID105535; AID105537; AID105539; AID105543
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC90 (µMol)0.04930.00170.03850.3100AID1272056; AID141361; AID141363; AID143399; AID1594861; AID198577; AID198578; AID216433; AID81627; AID81765; AID81766; AID82967; AID94447
Reverse transcriptase/RNaseH Human immunodeficiency virus 1ID501.92480.00602.18989.0000AID1155813; AID1155814; AID1155815; AID1574384; AID1574385; AID1574386; AID242820; AID253490; AID253492; AID253493; AID253494; AID253495; AID257163; AID257164; AID257165; AID267851; AID267862; AID267863; AID298087; AID298088; AID298089; AID366526; AID366527; AID366529; AID368555; AID368556; AID368557; AID650689; AID650690; AID650691; AID663305; AID663306; AID663308
Protease Human immunodeficiency virus 1IC90 (µMol)3.72600.00200.67847.3000AID143396; AID143398; AID143402; AID94449
Fructose-1,6-bisphosphatase 1 Mus musculus (house mouse)ID500.40000.40004.20008.0000AID368556
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (339)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
proteolysisProthrombin Bos taurus (cattle)
acute-phase responseProthrombin Bos taurus (cattle)
positive regulation of blood coagulationProthrombin Bos taurus (cattle)
protein polymerizationProthrombin Bos taurus (cattle)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
viral life cycleGag-Pol polyproteinHIV-1 M:B_HXB2R
establishment of integrated proviral latencyGag-Pol polyproteinHIV-1 M:B_HXB2R
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2B6Homo sapiens (human)
steroid metabolic processCytochrome P450 2B6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2B6Homo sapiens (human)
cellular ketone metabolic processCytochrome P450 2B6Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2B6Homo sapiens (human)
lipid metabolic processMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
triglyceride metabolic processMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
circadian rhythmMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein secretionMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phospholipid transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
sterol transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
triglyceride transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
low-density lipoprotein particle remodelingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
plasma lipoprotein particle assemblyMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
chylomicron assemblyMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
very-low-density lipoprotein particle assemblyMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
lipoprotein transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
response to calcium ionMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
establishment of localization in cellMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
intermembrane lipid transferMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
ceramide 1-phosphate transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
lipoprotein metabolic processMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
cholesterol homeostasisMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to hypoxiaDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
neutrophil mediated immunityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
germinal center formationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of leukocyte chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane protein ectodomain proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch receptor processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell population proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to xenobiotic stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of T cell chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
signal releaseDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
B cell differentiationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell growthDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to lipopolysaccharideDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of chemokine productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
regulation of mast cell apoptotic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
T cell differentiation in thymusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesion mediated by integrinDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
wound healing, spreading of epidermal cellsDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
spleen developmentDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell motilityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
defense response to Gram-positive bacteriumDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cellular response to high density lipoprotein particle stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
commissural neuron axon guidanceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of cold-induced thermogenesisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein localization to membrane raftCholesterol 24-hydroxylaseHomo sapiens (human)
bile acid biosynthetic processCholesterol 24-hydroxylaseHomo sapiens (human)
cholesterol catabolic processCholesterol 24-hydroxylaseHomo sapiens (human)
xenobiotic metabolic processCholesterol 24-hydroxylaseHomo sapiens (human)
nervous system developmentCholesterol 24-hydroxylaseHomo sapiens (human)
sterol metabolic processCholesterol 24-hydroxylaseHomo sapiens (human)
progesterone metabolic processCholesterol 24-hydroxylaseHomo sapiens (human)
regulation of long-term synaptic potentiationCholesterol 24-hydroxylaseHomo sapiens (human)
angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 3Homo sapiens (human)
signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 3Homo sapiens (human)
associative learningRap guanine nucleotide exchange factor 3Homo sapiens (human)
Rap protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of actin cytoskeleton organizationRap guanine nucleotide exchange factor 3Homo sapiens (human)
negative regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
intracellular signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of GTPase activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of protein export from nucleusRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of stress fiber assemblyRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
establishment of endothelial barrierRap guanine nucleotide exchange factor 3Homo sapiens (human)
cellular response to cAMPRap guanine nucleotide exchange factor 3Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 3Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (129)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
serine-type endopeptidase activityProthrombin Bos taurus (cattle)
calcium ion bindingProthrombin Bos taurus (cattle)
protein bindingProthrombin Bos taurus (cattle)
fibrinogen bindingProthrombin Bos taurus (cattle)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptidase activityGag-Pol polyproteinHIV-1 M:B_HXB2R
integrase activityGag-Pol polyproteinHIV-1 M:B_HXB2R
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
monooxygenase activityCytochrome P450 2B6Homo sapiens (human)
iron ion bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-alpha-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
heme bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-beta-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2B6Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2B6Homo sapiens (human)
lipid transporter activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
lipid bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
apolipoprotein bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein-containing complex bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein heterodimerization activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phospholipid transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phosphatidylcholine transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
cholesterol transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
triglyceride transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
ceramide 1-phosphate transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phosphatidylethanolamine transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phospholipid transporter activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
endopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
interleukin-6 receptor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
integrin bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
peptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metallopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
SH3 domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytokine bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
PDZ domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
tumor necrosis factor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metal ion bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
iron ion bindingCholesterol 24-hydroxylaseHomo sapiens (human)
steroid hydroxylase activityCholesterol 24-hydroxylaseHomo sapiens (human)
heme bindingCholesterol 24-hydroxylaseHomo sapiens (human)
cholesterol 24-hydroxylase activityCholesterol 24-hydroxylaseHomo sapiens (human)
testosterone 16-beta-hydroxylase activityCholesterol 24-hydroxylaseHomo sapiens (human)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein domain specific bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (77)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneCytochrome P450 2B6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2B6Homo sapiens (human)
cytoplasmCytochrome P450 2B6Homo sapiens (human)
endoplasmic reticulumMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
endoplasmic reticulum lumenMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
Golgi apparatusMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
cytosolMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
brush border membraneMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
microvillus membraneMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
vesicleMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
receptor complexMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
Golgi apparatusMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
endoplasmic reticulumMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
basolateral plasma membraneMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
cell-cell junctionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
focal adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
ruffle membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Golgi membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
endoplasmic reticulum lumenDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell surfaceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
actin cytoskeletonDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
apical plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane raftDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
endoplasmic reticulumCholesterol 24-hydroxylaseHomo sapiens (human)
endoplasmic reticulum membraneCholesterol 24-hydroxylaseHomo sapiens (human)
dendriteCholesterol 24-hydroxylaseHomo sapiens (human)
presynapseCholesterol 24-hydroxylaseHomo sapiens (human)
postsynapseCholesterol 24-hydroxylaseHomo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
cortical actin cytoskeletonRap guanine nucleotide exchange factor 3Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
microvillusRap guanine nucleotide exchange factor 3Homo sapiens (human)
endomembrane systemRap guanine nucleotide exchange factor 3Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
lamellipodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
filopodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
extracellular exosomeRap guanine nucleotide exchange factor 3Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2857)

Assay IDTitleYearJournalArticle
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID1798816Reverse Transcriptase Assay from Article 10.1021/jm801395v: \\Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.\\2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID1795395HIV-1 RT Assay from Article 10.1021/jm0211063: \\Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.\\2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.
AID1795743HIV-1 RT Assay from Article 10.1016/j.bmc.2004.08.050: \\Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.\\2004Bioorganic & medicinal chemistry, Dec-01, Volume: 12, Issue:23
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.
AID1795423HIV-1 RT Assay from Article 10.1021/jm990095j: \\Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.\\1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID1802513DNA Polymerase Assay from Article 10.1002/cbic.201600592: \\Natural Product Kuwanon-L Inhibits HIV-1 Replication through Multiple Target Binding.\\2017Chembiochem : a European journal of chemical biology, 02-16, Volume: 18, Issue:4
Natural Product Kuwanon-L Inhibits HIV-1 Replication through Multiple Target Binding.
AID1801910HIV-1 RT Colorimetric Assay from Article 10.1016/j.bioorg.2016.05.009: \\Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives.\\2016Bioorganic chemistry, 08, Volume: 67Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives.
AID1795438HIV-1 RT Assay from Article 10.1016/S0960-894X(01)00331-6: \\Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.\\2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
AID1795433HIV-1 RT Assay from Article 10.1021/jm990580e: \\Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.\\2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1802514RNAse H-Polymerase-Independent Cleavage Assay from Article 10.1002/cbic.201600592: \\Natural Product Kuwanon-L Inhibits HIV-1 Replication through Multiple Target Binding.\\2017Chembiochem : a European journal of chemical biology, 02-16, Volume: 18, Issue:4
Natural Product Kuwanon-L Inhibits HIV-1 Replication through Multiple Target Binding.
AID1795727HIV-1 RT Assay from Article 10.1016/j.bmc.2004.11.045: \\Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.\\2005Bioorganic & medicinal chemistry, Feb-15, Volume: 13, Issue:4
Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.
AID1795435HIV-1 RT Assay from Article 10.1016/s0960-894x(99)00486-2: \\Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.\\1999Bioorganic & medicinal chemistry letters, Oct-04, Volume: 9, Issue:19
Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.
AID1795437HIV-1 RT Assay from Article 10.1016/s0960-894x(00)00321-8: \\Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.\\2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.
AID1798815Reverse Transcriptase Assay from Article 10.1021/jm801322h: \\Novel Indazole Non-Nucleoside Reverse Transcriptase Inhibitors Using Molecular Hybridization Based on Crystallographic Overlays (dagger).\\2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
AID1795436HIV-1 RT Assay from Article 10.1016/s0960-894x(99)00565-x: \\Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).\\1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).
AID1801530In-vitro HIV-1 RT Screening from Article 10.1016/j.bioorg.2015.12.005: \\Design, synthesis and in-vitro evaluation of novel tetrahydroquinoline carbamates as HIV-1 RT inhibitor and their antifungal activity.\\2016Bioorganic chemistry, Feb, Volume: 64Design, synthesis and in-vitro evaluation of novel tetrahydroquinoline carbamates as HIV-1 RT inhibitor and their antifungal activity.
AID1801804RNA-dependent DNA Polymerase (RDDP) Assay from Article 10.1002/cbic.201500668: \\Inhibition of HIV-1 Reverse Transcriptase Dimerization by Small Molecules.\\2016Chembiochem : a European journal of chemical biology, Apr-15, Volume: 17, Issue:8
Inhibition of HIV-1 Reverse Transcriptase Dimerization by Small Molecules.
AID1802605HIV-1 RT In-Vitro Assay from Article 10.1016/j.bioorg.2017.03.013: \\Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives.\\2017Bioorganic chemistry, 06, Volume: 72Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives.
AID1795434HIV-1 RT Assay from Article 10.1016/s0960-894x(01)00239-6: \\4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.\\2001Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID586360Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1292013Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells2016European journal of medicinal chemistry, Jun-10, Volume: 115Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID248880Inhibitory concentration against human immunodeficiency virus type 1 (with K103N/Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID587749Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as inhibition of 2 mins magnetic nanopartials-medated infectiv2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID342718Inhibition of HIV1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as incorporation of radioactive dTTP into poly(rA)/oligo(DT)2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
AID1212882Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID1457056Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1884225Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1729149Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID557040Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1435502Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID416758Antiviral activity against HIV1 with reverse transcriptase Y181I mutation in human CEM cells assessed as protection against virus-induced cytopathicity2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID586486Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138A/S147G/Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunod2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1348220Antiviral activity against HIV1 pNL4-3 infected in HEK293 cells assessed as reduction in viral transcription by measuring decrease in luciferase activity at 1 uM after 20 hrs by luciferase reporter gene assay2017Journal of natural products, 12-22, Volume: 80, Issue:12
Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities.
AID279397Antiviral activity against HIV1 isolate with RT 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1157592Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-in2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1171588Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-32014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID522368Antiviral activity against wild type HIV1 infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1069710Inhibition of GST-tagged recombinant wild type HIV-1 reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli JM109 using dTTP as substrate after 40 mins by spectrofluorometric analysis2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID198563The compound was evaluated for the inhibition of HIV-1 reverse transcriptase2000Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.
AID709836Ratio of EC50 for HIV1 expressing wild type reverse transcriptase in presence of human serum albumin and human alpha-1 acid glycoprotein to EC50 for HIV1 expressing wild type reverse transcriptase2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1784586Inhibition of HIV-1 reverse transcriptase using Cy5-CAGGAAACAGCTATGAC/3'-GTCCTTTGTCGATACTGTTTTTTT-5' as primer/template at 5 to 50 uM preincubated for 20 min followed by dATP addition measured after 5 to 10 mins by gel electrophoresis analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Exploring the dNTP -binding site of HIV-1 reverse transcriptase for inhibitor design.
AID1059143Cytotoxicity against human MT4 cells after 5 days by MTT assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID496630Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase Y181C/V35T, V60I, I135V, S162A, K173T, Q174K, N175Y, D177E, T200A, Q207E, R211K, H221Y mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID523481Antiviral activity against HIV1 with RT connection domain G190S/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1574388Resistance index, ratio of ID50 for recombinant HIV-1 His-tagged reverse transcriptase p66/p51 K103N mutant to ID50 for recombinant wild type HIV-1 reverse transcriptase His-tagged p66/p512019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID557019Inhibition of HIV1 isolate R8 reverse transcriptase after 90 mins2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID248261In vitro inhibitory concentration against HIV L100I mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1197832Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID266347Inhibition of HIV1 reverse transcriptase Y181C mutant in 293T cells2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.
AID293563Antiviral activity against HIV1 LAI with RT L100I and K103N mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID279472Antiviral activity against HIV1 isolate with RT 103S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID247500Inhibitory activity against HIV-1 mutant strain 179E2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID527562Antiviral activity against HIV1 NL4-3 containing reverse transcriptase K103N mutation infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1057040Antiviral activity against wild-type HIV1 3B infected in MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID508752Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID141359Potency of second-generation NNRTIs against Mutant HIV-1 sV179D/L100I/Y181C free drug2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1572525Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID1457069Downregulation of iNOS mRNA levels in C57BL/6 mouse BV2 cells at 1000 nM after 24 hrs by RT-PCR assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID698299Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-32012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID199980Inhibitory activity against human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.
AID1750721Inhibition of HIV-1 p66/p51 reverse transcriptase E138K mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID443680Antiviral activity against HIV with reverse transcriptase Y188L mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID1059146Antiviral activity against HIV1 3B infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID443684Antiviral activity against HIV with reverse transcriptase K103N/Y181C double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID519866Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1729153Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1884223Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against wildtype HIV-1 3B infected in human MT4 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1435505Antiviral activity against HIV1 expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID541171Selectivity ratio of EC50 for antiviral activity against HIV1 harboring L74M and E92V mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1198749Inhibition of HIV1 reverse transcriptase-associated RNA-dependent DNA polymerase activity after 30 mins2015European journal of medicinal chemistry, Mar-26, Volume: 93(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.
AID361920Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase P225H mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1773458Resistance factor, ratio of EC50 for HIV1 harboring K103N mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID1456310Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID361924Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/V108I mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID496624Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/A33E, V35T, T39A, D123E, S162A, Q174G, T200E, I202V, Q207E mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID241472Inhibitory concentration against HIV-1 mutant reverse transcriptase (Y181C)2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.
AID1561717Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenesulfonamide assessed as protection ag
AID446239Cytotoxicity against human SupT1 cells2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID698300Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-32012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1815390Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 of Anti-HIV activity against HIV-1 IIIB infected in human MT42021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID279480Antiviral activity against HIV1 isolate with RT 100F mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1750719Inhibition of HIV-1 p66/p51 reverse transcriptase Y181C mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1264550Selectivity ratio for antiviral activity against HIV-1 expressing reverse transcriptase K101P mutant to HIV-1 expressing wild-type reverse transcriptase2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1750723Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase L100I mutant2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID541167Selectivity ratio of EC50 for antiviral activity against HIV1 harboring Q148K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID519891Selectivity ratio of EC50 for 0.02 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.02 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID619638Antiviral activity against HIV-1 3B harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID519876Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID508768Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID386492Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate.
AID665272Antiviral activity against HIV1 RES056 harboring K103N/Y181C RT mutant infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1884489Antiviral activity against drug-resistant HIV-1 L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID490362Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect in presence of 10 % fetal bovine serum2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID1880374Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID573246Cmin in HIV-1 infected children at 10 to 15 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID508769Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase H221Y mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID253493Dose required to inhibit HIV-1 reverse transcriptase activity (Y181I mutant) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID347607Antiviral activity against wild type HIV HXB2 in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay in presence of 40% human serum2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID448395Inhibition of wild type HIV reverse transcriptase in presence of poly(rA) 300 template, (dT) 16 primer2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 3: optimisation of physicochemical properties.
AID1157580Cytotoxicity against human MT4 cells after 96 hrs by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1171593Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in enzyme activity2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1736361Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase V108I/K103N double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr
AID508758Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1316335Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1583022Selectivity index, ratio of CC50 for cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection 2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1815400Inhibition of HIV1 reverse transcriptase Y188L mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1212918Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID279464Antiviral activity against HIV1 isolate with RT 101Q, 103N, 225H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1379964Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 assessed as reduction in biotin-dUTP incorporation incubated for 40 mins using poly(rA) template and oligo(dT)16 primer by picogreen dye based spectrofluorometry2017European journal of medicinal chemistry, Nov-10, Volume: 140Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID82272Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected wild type cells2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID523356Antiviral activity against HIV1 with RT connection domain Y181C/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID302270Resistance index, ratio of Ki for HIV1 reverse transcriptase Y181I mutant to Ki for wild type HIV1 3B reverse transcriptase2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID82141Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected K103N strain2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID1069707Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1435504Antiviral activity against HIV1 expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID1316336Antiviral activity against HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID586367Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase F121Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1731747Inhibition of reverse transcriptase K103N mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID368569Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-DNA-dNTP ternary complex expressed in Escherichia coli BL212009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID562698Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as decrease in virus production at 2 times EC90 after 72 hrs by beta-galactosidase reporter gene assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation.
AID698303Cytotoxicity against mock-infected human MT4 cells measured after 5 days by MTT assay2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID464767Binding affinity to human serum albumin2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1352318Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID293176Antiviral activity against HIV1 RT 181C mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity.
AID391224Antiviral activity against wild type HIV1 infected in human MT4 cells after 72 hrs in presence of 10% fetal bovine serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID152959Antiviral activity of Protein Binding of compound was evaluated for Thai 9466 virus expressed PBMC by P242000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1171597Inhibition of wild type HIV1 reverse transcriptase V106A mutant assessed as reduction in enzyme activity2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1186000Antiviral activity against HIV1 harboring reverse transcriptase K103N/P225H double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID650690Inhibition of HIV 1 reverse transcriptase Y181I mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1261312Antiviral activity against BVDV infected in MDBK cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1165074Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1736349Inhibition of RNase H activity of HIV-1 reverse transcriptase using DNA/RNA hybrid as substrate incubated for 30 mins by fluorescence based analysis
AID464765Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1653628Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) F416A mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID476471Cytotoxicity against human MT2 cells infected with HIV1 harboring reverse transcriptase Y181C mutation by MTT assay2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1457057Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID240140Concentration required to inhibit HIV-1 reverse transcriptase activity (wild-type) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID572179Antiviral activity against HIV-1 subtype O V029524 harboring NNRTI A98G, V179E and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1157581Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID665549Cytotoxicity against human MT4 cells after 5 days by MTT assay2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
AID1773459Resistance factor, ratio of EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID298079Antiviral activity against HIV1 RT 112 mutant in lymphocytes assessed as reduction of p24 antigen production2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID263513Antiviral activity against HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID279488Antiviral activity against HIV1 isolate with RT G190S mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID82271Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C strain2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID279402Antiviral activity against HIV1 isolate with RT 103N, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID508658Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF03 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1880380Antiviral activity against HIV-1 IIIB harboring reverse transcriptase E138K mutant infected in human MT4 cells by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID1736348Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infect
AID279414Antiviral activity against HIV1 isolate with RT 108I, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1750716Selectivity index, ratio of CC50 for human MT-4 cells to EC50 for HIV-1 infected in MT-4 cells2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1773446Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1609105Selectivity index, ratio of CC50 for human MT4 cells to EC50 of antiviral activity against HIV-1 IIIB infected in human MT4 cells2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID508756Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID576026Half life in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID465423Volume of distribution at steady state in Beagle dog at 0.5 mg/kg, iv or. 5 mg/kg, po2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID519874Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID573982Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Simian immunodeficiency virus MAC 2512008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID247501Inhibitory activity against HIV-1 mutant strain 181C2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID523482Antiviral activity against HIV1 with RT connection domain G190S/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID226236Fold resistance (L100I/ WT) (as per ref 10 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID576048Reduction in ABCC1 mRNA expression in healthy human at 400 mg, po qd for 14 days by RT-PCR2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID519962Selectivity ratio of EC50 for 0.05 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.05 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID586384Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155S mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1379961Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by measuring virus-induced syncytium formation by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID293558Antiviral activity against HIV1 LAI with RT L100I mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID269686Antiviral activity against HIV1 NNTRI resistant Y188L mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269686Antiviral activity against HIV1 NNTRI resistant Y188L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269686Antiviral activity against HIV1 NNTRI resistant Y188L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1731745Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB
AID267859Cytotoxicity against MT4 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1773449Antiviral activity against wild type HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID464772Oral bioavailability in Beagle dog at 4 mg/kg, po2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID366557Antiviral activity against HIV1 with reverse transcriptase G190A mutation in human MT4 cells assessed as reduction of virus-induced cytopathic effect2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1596751Antiviral activity against wild type HIV-1 3B infected in MT4 cells measured after 5 days by MTT assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID508830Antiviral activity against Human immunodeficiency virus 1 subtype B isolate WEJO infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1357795Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID443699Antiviral activity against HIV with reverse transcriptase G190S mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID1212893Drug metabolism in human liver microsomes harboring CYP2B6*1/*1 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID449492Selective index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1435509Antiviral activity against HIV1 RES056 expressing reverse transcriptase mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID1457058Antiviral activity against HIV1 harboring reverse transcriptase K103N /Y1881C double mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1126506Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1558855Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1653620Inhibition of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli at 60 to 100 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-ma2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID298081Selectivity index, ratio of TC50 for lymphocytes to ED50 for HIV1 3B2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID1435516Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase E138K mutant
AID508782Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138Q mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1609110Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based spectrofluorometric assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID607875Cytotoxic activity against human MT4 cells assessed as viability of mock-infected cells after 5 days by MTT assay2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1736357Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr
AID541170Selectivity ratio of EC50 for antiviral activity against HIV1 harboring N155S mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1212915Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID1736346Selectivity index, ratio of CC50 for human HEK 293T cells to EC50 for VSVG/wild type HIV1 infected in human HEK 293T cells
AID573985Antiviral activity against Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID557025Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and G190A mutant relative to drug-sensitive HIV1 CNDO2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443704Antiviral activity against HIV with reverse transcriptase K103N/P225H double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID587739Cytotoxicity against human HeLaT4 cells by WST-1 assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID675390Antiviral activity against HIV1 infected in human MT4 cells assessed as virus-induced cytopathogenicity after 4 days by MTT assay2012European journal of medicinal chemistry, Sep, Volume: 55Disubstituted thiourea derivatives and their activity on CNS: synthesis and biological evaluation.
AID556525Antiviral activity against Human immunodeficiency virus 1 clone 38086 harboring K49R, V60I, I135V, Q145M, Q174H, G196E, Q207E, R211K, V245K mutation in reverse transcriptase by phenosense assay relative to wild type2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility.
AID1390711Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID1220368Drug metabolism in human seminal plasma assessed as formation of N- and O-linked glucuronidated metabolite at 100 mg administered every 4 hrs by UPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID1815402Inhibition of HIV1 reverse transcriptase F227L/V106A double mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1736367Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase G190A/K103N double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel
AID519877Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID622058Ratio of Ki for HIV1 RT p66/p66 homodimer K103N/Y181C double mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID82967Inhibitory activity against HIV-1 reverse transcriptase1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).
AID1750726Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase Y188L mutant2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1754639Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Antiviral activity against HIV-1 IIIB infected in human MT4 cells2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1884486Antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1418468Inhibition of recombinant wild-type HIV1 GST-fused reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in biotin-dUTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 2018Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22
Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine.
AID658566Resistance factor, ratio of EC50 for multidrug-resistant HIV1 695-RT infected in HEK293T cells to wildtype HIV1 infected in HEK293T cells2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium.
AID370724Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID82461Antiviral activity against K103N/L100I strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1316346Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID583847Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, E138K mutant infected in human SupT1 cells derived from 9 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to drug sensitive HIV2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1163230Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei brucei Squib427 assessed as reduction in parasite growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID738333Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID1057036Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID1457065Inhibition of HIV1 reverse transcriptase p66 Y181I mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation counting 2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1212895Drug metabolism in human liver microsomes harboring CYP2B6*6/*6 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID279407Antiviral activity against HIV1 isolate with RT 98G, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID572176Antiviral activity against HIV-1 subtype H V022827 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1168820Activity of CYP2B6 (unknown origin) assessed as maximum depletion rate constant pre-incubated for 5 mins in presence of NADPH by uHPLC-MS/MS based substrate depletion kinetics assay2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Structure-Activity Studies Reveal the Oxazinone Ring Is a Determinant of Cytochrome P450 2B6 Activity Toward Efavirenz.
AID635346Cytotoxicity against human MT4 cells measured by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID1212894Drug metabolism in human liver microsomes harboring CYP2B6*1/*6 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID523350Antiviral activity against HIV1 with RT connection domain K103N/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1763906Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID738334Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID586371Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Y143C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID263518Antiviral activity against HIV1 V179E mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID1198753Inhibition of HIV1 reverse transcriptase Lys103Asn mutant-associated DNA polymerase-independent RNase H activity after 1 hr2015European journal of medicinal chemistry, Mar-26, Volume: 93(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.
AID313876Antiviral activity against HIV1 in MT4 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase--structure-activity relationships and crystallographic analysis.
AID1483285Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase F227L/V106A double mutant in human MT4 cells infected HIV1 3B2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1077223Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID328844Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID361918Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K101E mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID527376Toxicity in human CEM-SS cells2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1155819Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase L100I mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1565090Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1572530Inhibition of HIV1 reverse transcriptase p66/p51 using poly(rA)/oligo(dT)16 as template/primer measured after 40 mins by pico-green based spectrofluorometric analysis
AID1357798Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1156488Selectivity index, ratio of CC50 for human MT4 cells to IC50 for wild type HIV1 3B2014European journal of medicinal chemistry, Jul-23, Volume: 82Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors.
AID279466Antiviral activity against HIV1 isolate with RT 103N, 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID293565Antiviral activity against HIV1 LAI with RT F227C and V106A mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID246343Effective concentration of the compound to inhibit HIV-1 mutant K103N+Y181C replication in HIV-infected MT-4 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID584046Ratio of IC50 for HIV1 reverse transcriptase F227C mutant to IC50 for wild type HIV1 reverse transcriptase2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1435503Antiviral activity against HIV1 expressing reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID279438Antiviral activity against HIV1 isolate with RT 98G, 103N, 108I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1741390Inhibition of reverse transcriptase in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1327987Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells after 48 hrs by luciferase reporter gene assay2016Journal of natural products, 09-23, Volume: 79, Issue:9
Eremophilane Sesquiterpenes from an Endophytic Fungus Periconia Species.
AID613687Antitumor activity against human A375 cells xenografted in athymic nude Harlan mouse assessed as reduced tumor growth at 20 mg/kg, ip administered daily 5 days pre week measured every day2011Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors.
AID1157598Antiviral activity against HIV1 MP1308 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID576041Drug concentration in PBMCs of healthy human at 400 mg, po measured after 5 hrs on day 1 post dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID269797Antiviral activity against HIV1 I135V mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269797Antiviral activity against HIV1 I135V mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269797Antiviral activity against HIV1 I135V mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID279453Antiviral activity against HIV1 isolate with RT 98G, 100I, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID440082Antiviral activity against HIV1 HXB2 harboring 190S mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1705188Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1594861Inhibition of HIV1 reverse transcriptase2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.
AID573989Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 12008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID522374Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106A mutant clone to EC50 for wild type HIV12010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1653636Binding affinity to recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli in absence of substrate at 24 degC by stopped-flow spectrophotometric method2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID279460Antiviral activity against HIV1 isolate with RT 103N, 108I, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1483269Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID263507Antiviral activity against HIV1 in HEK293T cells2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID663313Resistance ratio of ID50 for HIV1 reverse transcriptase Y181I mutant to ID50 HIV1 wild type reverse transcriptase2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1884230Inhibition of wild type HIV-1 reverse transcriptase assessed as reduction of biotin-dUTP incorporation into protein using ABTS as substrate incubated for 1 hrs by ELISA analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID766431Cytotoxicity against human MT2 cells by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.
AID246244Effective concentration against human immunodeficiency virus type 1 wild type srtain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID279509Antiviral activity against HIV1 isolate with RT F227L mutation in Hela-JC-53 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1059145Antiviral activity against drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID263517Antiviral activity against HIV1 E138K mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID368556Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-mediated RNA-dependent DNA polymerase activity expressed in Escherichia coli BL21 assessed as [3H]dTTP incorporation by cell free-based scintillation counting2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID1763900Antiviral activity against HIV-1 IIIB harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID82470Antiviral activity against V106I strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID105693Anti-HIV-1 activity against K1001 strain was determined in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1784587Inhibition of HIV-1 reverse transcriptase using 5'-Cy5CAGGAAACAGCTATGAC/3'-GTCCTTTGTCGATACTGTTTTTTT-5' as primer/template at 0.5 uM preincubated for 20 min followed by dATP addition measured after 5 to 10 mins by gel electrophoresis analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Exploring the dNTP -binding site of HIV-1 reverse transcriptase for inhibitor design.
AID88370Antiviral activity against K103N/Y181C mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1773840Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1331267Inhibition of HIV-1 reverse transcriptase assessed as reduction in biotin-labeled dNTP incorporation using streptavidine bound template measured after 1 hr by ELISA2017Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1
Design, synthesis and anti-HIV-1 RT evaluation of 2-(benzyl(4-chlorophenyl)amino)-1-(piperazin-1-yl)ethanone derivatives.
AID88377Antiviral activity against V106A mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1687686Cytotoxicity against human MT4 cells assessed as inhibition of cell viability by measuring reduction in absorbance at OD540 by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID586379Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase I151L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1316338Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1171411Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1705194Inhibition of RNA-dependent DNA polymerase activity of wild type recombinant HIV-1 His-tagged p66/p51 reverse transcriptase assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintilla2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID523483Antiviral activity against HIV1 with RT connection domain L100I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID302253Antiviral activity against HIV1 with reverse transcriptase K103N mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1264540Antiviral activity against HIV-1 X4 expressing reverse transcriptase K103N mutant infected in human CD4+ T cells for 3 days by FACS analysis2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1884490Antiviral activity against drug-resistant HIV-1 K103 N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID253490Dose required to inhibit HIV-1 reverse transcriptase activity (K103N mutant) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID246393Effective concentration against human immunodeficiency virus type 1 mutated at 103N+181C2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID366517Antiviral activity against HIV1 NL4-3 in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1165079Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(rA)-oligo(dT) as template/primer and digoxigenin-/biotin-labeled dUTP nucleotides incubated for 1 hr2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1691436Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cell death incubated for 5 days by MTT assay2020European journal of medicinal chemistry, May-01, Volume: 193In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID105543Inhibition of wild type HIV-1 in MT-4 cell culture (human T cell line)1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID1888691Toxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay
AID1163255Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1286670Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1572522Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells
AID1761018Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1157599Antiviral activity against NRTI-resistant HIV1 MP1315 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID198385Inhibitory concentration for 50% inhibition of HIV-1 reverse transcriptase2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.
AID1191668Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenic effect2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
AID541159Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 8 passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1335213Antiviral activity against HIV-1 NL4-3 harboring RT-Y188L mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID523357Antiviral activity against HIV1 with RT connection domain G190A mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID248491In vitro inhibitory concentration against HIV F227L and V106A mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1206935Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection from virus-induced cytopathicity after 4 days by MTT assay2015European journal of medicinal chemistry, Jun-05, Volume: 97Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1750717Inhibition of HIV-1 p66/p51 reverse transcriptase L100I mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID586376Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Q148H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1729151Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1761014Antiviral activity against HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1743618Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID279479Antiviral activity against HIV1 isolate with RT 179D, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID419085Inhibition of HIV1 replication in human 293T cells preincubated 15 mins prior to infection measured after 48 hrs postinfection by luciferase reporter gene assay2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
Synthesis and biological evaluation of N4-(hetero)arylsulfonylquinoxalinones as HIV-1 reverse transcriptase inhibitors.
AID573975Antiretroviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1636930Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against viral infection by MTT method2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Computer-aided discovery of anti-HIV agents.
AID1847040Inhibition of HIV-1 reverse transcriptase associated RNA-dependent DNA polymerase activity using poly(A)-oligo(dT) as template/primer incubated for 30 mins by multilabel counter plate reader analysis2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase.
AID490368Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID508648Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, T386A mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID619636Antiviral activity against HIV-1 3B harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID1357790Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID614139Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 IIIB infected in human MT4 cells2011Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
AID227244The compound was evaluated for antiviral activity using whole cell assay2000Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.
AID1220370Blood plasma protein binding in human at 100 mg administered every 4 hrs by ultrafiltration method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID1574374Antiviral activity against HIV-1 IRLL98 harboring reverse transcriptase M41L, D67N, Y181C, M184V, R211K, and T215Y mutants infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1888697Antiviral activity against HIV1 with RT Y188L mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1773830Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 infected in human MT4 cells2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1335201Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/V108I double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID541164Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1627029Inhibition of HIV1 RT using 17-mer DNA/Alexa Fluor 488 5'-end labeled DNA/Alexa Fluor 555-aha-dUTP as primer/template/substrate preincubated for 10 mins followed substarte addition measured after 30 mins by FRET assay2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID279446Antiviral activity against HIV1 isolate with RT 101Q, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1126511Inhibition of wild-type HIV1 reverse transcriptase p66/p51 after 40 mins by spectrophotometry2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID82276Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C+K103N strain2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID1457066Inhibition of HIV1 reverse transcriptase p66 K103N/Y1881C double mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintilla2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID198237Inhibitory activity against HIV-1 reverse transcriptase2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz.
AID1773835Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID541156Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 5 passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID496620Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase K101E/K30E, I31P, V35Q, T39S, E44G, E53G, A62G, N81H, Q91H,I135V,S162A, K173S, Q174R, D177E, V179I, T200I, Q207N, R211K, F214L mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID247620Inhibitory activity against HIV-1 double mutants strain 227L and 106A2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID448401Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y188C mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 3: optimisation of physicochemical properties.
AID1316334Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1456307Inhibition of HIV-1 reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID1731748Inhibition of reverse transcriptase Y183C mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1888696Antiviral activity against HIV1 with RT Y181C mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1357804Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y188L mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1069709Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID586478Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G140S/Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1596755Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in MT4 cells2019European journal of medicinal chemistry, Aug-15, Volume: 176Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID257165Inhibition of Y181I mutant HIV1 reverse transcriptase by [3H]-dTTP poly(rA)/oligo(dT) incorporation2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID591356Antiviral activity against wild type HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced cytopathicity after 4 days by microscopic analysis2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
AID247498Inhibitory activity against HIV-1 mutant strain 106A2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID518734Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by filter-based filtration assay2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1653619Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mass spec2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID508831Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 92BR025 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID279427Antiviral activity against HIV1 isolate with RT 103R, 179D, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID619635Antiviral activity against HIV-1 3B harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID492278Antiviral activity against HIV1 with reverse transcriptase K103N, Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID257164Inhibition of K103N mutant HIV1 reverse transcriptase by [3H]-dTTP poly(rA)/oligo(dT) incorporation2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID1326644Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by cell titer glo based luciferase reporter gene assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.
AID619639Antiviral activity against HIV-1 3B harboring RT F227L and V106A mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID443705Antiviral activity against HIV with reverse transcriptase K101E/G190A double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID583854Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1220363Drug level in human cerebrospinal fluid2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID576031AUC (0 to 24 hrs) in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID1185996Antiviral activity against HIV1 harboring reverse transcriptase L1001/K103N double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID446410Fold resistance, ratio of IC50 for HIV reverse transcriptase with L234I mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID1637393Antiviral activity against human HIV-1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID519873Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1773439Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID446256Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y188C mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID508784Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138G mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID616199Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus 1 NL4-3 infected in human MT2 cells assessed as inhibition of viral replication after 48 hrs by luciferase activity reporter gene assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis of new 2'-deoxy-2'-fluoro-4'-azido nucleoside analogues as potent anti-HIV agents.
AID1212897Drug metabolism in human liver microsomes harboring CYP2B6*1/*6 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by LC/MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID298062Antiviral activity against HIV2 ROD in human MT4 cells by XTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID573475Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5331 by cell based assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1069122Antiviral activity against HIV harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum2014Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID152958Antiviral activity of Protein Binding of compound was evaluated for A 018C virus expressed PBMC by P242000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1736354Antiviral activity against VSVG/wild-type HIV-1 infected in human HEK 293T cells assessed as time during which compound exhibits 50% virologic failure at 1 uM treated at post-viral infection and measured at 48 hrs post-infection by luciferase reporter gen
AID718372Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
AID88382Antiviral activity against Y188C mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1157596Antiviral activity against HIV1 W5269 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID271413Antiviral activity against wild type HIV1 in HeLa-JC53 cells2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID279398Antiviral activity against HIV1 isolate with RT 103N, 108I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1741398Inhibition of reverse transcriptase F227L and V106A mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1379962Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID82463Antiviral activity against K103N/V108I strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1421325Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured 5 days post infection by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1446811Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1141964Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1298247Inhibition of HIV1 wild type reverse transcriptase p66/p51 using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1627027Cytotoxicity against HIV1 infected human CEM cells assessed as reduction in cell viability after 7 days by MTT assay2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID508792Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID541166Selectivity ratio of EC50 for antiviral activity against HIV1 harboring G140S mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID523349Antiviral activity against HIV1 with RT connection domain K103N mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1161107Cytotoxicity against human MT4 cells by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID1503321Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation.
AID541152Selectivity ratio of EC50 for antiviral activity against EFV-resistant HIV1 selected after 3 passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID431619Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1811038Inhibition of recombinant wild-type HIV1 p66/p51 reverse transcriptase assessed as inhibition of [3H]dGTP incorporation using poly (rA) as templates incubated for 40 mins by spectrofluorometer2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1168821Activity of CYP2B6 (unknown origin) assessed per pmol protein pre-incubated for 5 mins in presence of NADPH by uHPLC-MS/MS based substrate depletion kinetics assay2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Structure-Activity Studies Reveal the Oxazinone Ring Is a Determinant of Cytochrome P450 2B6 Activity Toward Efavirenz.
AID279473Antiviral activity against HIV1 isolate with RT 230L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1882468Antiviral activity against wild type HIV-1 IIIB infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID584084Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase Y181C mutant infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type HIV1 NL4-32010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID279515Antiviral activity against HIV1 isolate with RT V106I, D123G, Y181C, F227L, T369I mutation in Hela-JC-53 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1141969Ratio of EC50 for HIV1 harboring reverse transcriptase K103N/Y181C double mutant to EC50 for wild type HIV1 NL4.32014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1157593Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1884228Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1206934Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathicity after 4 days by MTT assay2015European journal of medicinal chemistry, Jun-05, Volume: 97Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1286671Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1572520Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
AID1773453Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells
AID246780Compound concentration required to reduce the amount of p24 by 90% in wtIIIBinfected C8166 cells2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID650541Resistance ratio of EC50 for multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID143396Compound was evaluated for its ability to inhibit the mutant K103N L1001 NNRTI HIV-1 enzyme2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID508653Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID771796Cytotoxicity against human MT4 cells after 96 hrs by MTT assay2014Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 23Synthesis and structure evaluation of new complex butylarylpiperazin-1-yl derivatives.
AID347796Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 181I mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID632796Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral infection2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID299022Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID1574378Antiviral activity against HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1335219Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/Y181C double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID371906Antiviral activity against HIV1 NL4-3 with K103N/V108I double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1141959Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID235444Selective index as the ratio of CD50 to that of ED50 against HIV-1 HxB2 strain.2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID508826Antiviral activity against Human immunodeficiency virus 1 subtype B isolate 93BR021 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID198768Binding affinity towards L100I mutant HIV-1 reverse transcriptase (as per ref 10 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID1168819Activity of CYP2B6 (unknown origin) pre-incubated for 5 mins in presence of NADPH by uHPLC-MS/MS based substrate depletion kinetics assay2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Structure-Activity Studies Reveal the Oxazinone Ring Is a Determinant of Cytochrome P450 2B6 Activity Toward Efavirenz.
AID368561Antiviral activity against HIV1 reverse transcriptase Y188L mutant infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID197777Compound was evaluated for its ability to inhibit HIV-1 Reverse Transcriptase in an in vitro enzyme assay2001Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
AID1884222Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 to 7 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID88367Antiviral activity against K103N/L100I mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID623214Antiviral activity against HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID282738Inhibition of HIV1 RT V106A mutant2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID347619Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 138K mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID508645Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, G190S mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1561721Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide to EC
AID496632Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, T39L, K122E, D123N, S162A, E169T, K173E, Q174E, D177E,T200A, I202V, Q207E mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID730232Antiviral activity Vesicular stomatitis virus pseudotype2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p
AID1222793Dissociation constant, pKa of the compound2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Which metabolites circulate?
AID562697Antiviral activity against HIV1 NL4-3 infected in human HeLa cells assessed as decrease in single-cycle viral infection after 72 hrs by beta-galactosidase reporter gene assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation.
AID269685Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269685Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269685Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID416755Antiviral activity against HIV1 with reverse transcriptase L100I mutation in human CEM cells assessed as protection against virus-induced cytopathicity2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID279491Antiviral activity against HIV1 isolate with RT K101E mutant2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1457061Ratio of EC50 for HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID519875Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1157586Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID508640Antiviral activity against Human immunodeficiency virus 1 subtype BG infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID370732Cytotoxicity against human C8166 cells by MTT method2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID571979Antiviral activity against HIV-1 subtype B V022811 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1373161Inhibition of reverse transcriptase E138K mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID235446Selective index (CD50 compared to ED50 against HIV-1 IIIB strain).2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID293178Antiviral activity against HIV1 RT 100I mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity.
AID293175Antiviral activity against HIV1 with RT 103N mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity.
AID279410Antiviral activity against HIV1 isolate with RT 179E mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1298253Inhibition of HIV1 3B reverse transcriptase p66/p51 K103N/Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID586370Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G140S mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID709868Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID94445Potency of second-generation NNRTIs against Mutant HIV-1 K103N plasma; Vlaue ranges from 3400-81002000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID246344Effective concentration of the compound to inhibit HIV-1 mutant L100I+K103N replication in HIV-infected MT-4 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID587740Selectivity index, ratio of CC50 for human HeLa-T4 cells to EC50 for single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID457956Antiviral activity against HIV1 3B infected in human MT4 cells assessed inhibition of viral-induced cytopathic effect after 5 days2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID586901Activity at MRP12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID441314Fold resistance, ratio of IC50 for HIV reverse transcriptase with K101E mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
AID1212884Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID1326643Inhibition of wild type HIV-1 3B reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 5 days by cell titer glo based luciferase reporter gene assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.
AID1561718Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against virus-indu
AID1304409Antiviral activity against HIV-1 3B expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID1157582Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID508798Ratio of EC50 for HIV1 in presence of 50% human serum to EC50 for HIV1 in absence of serum proteins by GFP assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1060628Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.
AID1186328Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Antiviral activity of benzimidazole derivatives. III. Novel anti-CVB-5, anti-RSV and anti-Sb-1 agents.
AID366524Antiviral activity against HIV1 isolates with reverse transcriptase Y188L mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID368557Inhibition of HIV1 recombinant reverse transcriptase Y181I mutant-mediated RNA-dependent DNA polymerase activity assessed as [3H]dTTP incorporation by cell free-based scintillation counting2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID279393Antiviral activity against HIV1 isolate with RT 106I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID522577Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106I mutant clone to EC50 for wild type HIV12010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID263152Antiviral activity against HIV1 in HEK293T cells2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID263152Antiviral activity against HIV1 in HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID263152Antiviral activity against HIV1 in HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1157595Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID361912Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190A mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID267650Antiviral activity against HIV1 K103N/L100I mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID586378Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1335209Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/V108I double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1565098Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID508763Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID557022Antiviral activity against HIV1 CRF01_AE harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1884226Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1379959Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by measuring virus-induced syncytium formation by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID1884539Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 K103 N mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID302256Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT K103N mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID650543Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID440079Antiviral activity against HIV1 HXB2 harboring 138K mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID279498Antiviral activity against HIV1 isolate with RT K103N-V108I-A98G mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1212896Drug metabolism in human liver microsomes harboring CYP2B6*1/*1 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by LC/MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID1574380Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV-1 NL4-32019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID465421Binding affinity to human serum albumin2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID666972Cytotoxicity against human MT4 cells after 5 days by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors.
AID541157Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 6 low passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1572526Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID88381Antiviral activity against Y181C mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID328845Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID573254Apparent oral clearance in HIV-1 infected children at 12 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID279523Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID665274Cytotoxicity against human MT4 cells after 5 days by MTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID279404Antiviral activity against HIV1 isolate with RT 103N, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID106069Inhibitory activity against 188L strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID698306Antiviral activity against HIV1 containing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1357803Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y181C mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID508650Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID279318Inhibition of HIV1 RT assessed as natural endogenous reverse transcription at 50 nM2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID457955Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase using poly(rA)/pligo(dT) template2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID613677Antiproliferative activity against human A375 cells assessed as cell growth at 15 uM after 96 hrs by trypan blue assay2011Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors.
AID299025Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV12007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID443676Antiviral activity against HIV with reverse transcriptase CNDO mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID718370Cytotoxicity against HIV1 3B infected in human MT4 cells by MTT assay2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
AID1773461Resistance factor, ratio of EC50 for HIV1 harboring E138K mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID443702Antiviral activity against HIV with reverse transcriptase K103N/G190A double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID299026Antiviral activity against HIV1 3B in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID106049Inhibitory activity against 100I strain and 103N strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1609107Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1574383Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase K103N/Y181C double mutant to EC50 for wild type HIV-1 NL4-32019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID271415Antiviral activity against HIV1 Y188L mutant in HeLa-JC53 cells2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase.
AID342719Antiviral activity against HIV1 3B in human MT4 cells assessed as virus-induced cytopathogenicity after 5 days2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
AID248016Inhibitory concentration against wild-type HIV-1 LAI Virus was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.
AID1483279Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1767121Ratio of antiviral activity against HIV1 NL4-3 Env-deficient VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production when host cells were infected with compound pretreated viral particles to antiviral a2021European journal of medicinal chemistry, Aug-05, Volume: 220Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.
AID302254Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID605181Antiviral activity against HIV1 R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral spread in presence of 10% fetal bovine serum2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
AID496627Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K32R, V35E, T39S, S48T, V60I, D121Y, K122E, I135T, S162A, K173A, Q174K, D177E, V179I, T200E, Q207D, R211K mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID279411Antiviral activity against HIV1 isolate with RT 103N, 108I, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID519967Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells by phenosense assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID269690Antiviral activity against HIV1 NNTRI resistant K103N/L100I mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269690Antiviral activity against HIV1 NNTRI resistant K103N/L100I mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269690Antiviral activity against HIV1 NNTRI resistant K103N/L100I mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1736364Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel
AID586479Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Y143H/N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID449489Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus induced cytotoxicity after 5 days by MTT assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID541169Selectivity ratio of EC50 for antiviral activity against HIV1 harboring N155H mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1141968Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1574371Therapeutic index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 NL4-3 infected in human MT4 cells2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1059144Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID105325Inhibition of Efavirenz resistant HIV-1 (Y181C) induced cytopathicity in MT-4 cells.2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID557044Inhibition of HIV1 isolate R8 reverse transcriptase K103N mutant after 90 mins by electrochemiluminescence analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID257173Cytotoxicity against MT4 cells by MTT method2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID267851Inhibition of wild type HIV1 reverse transcriptase2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID81591Antiviral activity against HIV-1 using antiinfectivity assay2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
AID1231486Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID492046Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
AID366559Antiviral activity against HIV1 with reverse transcriptase K103N/Y181C mutation in human MT4 cells assessed as reduction of virus-induced cytopathic effect2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID508766Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230V mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID105202Antiviral activity against MT-4 cells infected with Nev-R strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1457071Effect on CD163 mRNA levels in C57BL/6 mouse BV2 cells at 1000 nM after 24 hrs by RT-PCR assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1485966Inhibition of recombinant wild-type HIV-1 reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli JM109 assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by Pi2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID1743637Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID586910Induction of BCRP activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID279443Antiviral activity against HIV1 isolate with RT 106A, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID368567Inhibition of HIV1 recombinant free reverse transcriptase K103N mutant expressed in Escherichia coli BL212009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID269799Antiviral activity against HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269799Antiviral activity against HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269799Antiviral activity against HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1763904Antiviral activity against HIV-1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1212919Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as intrinsic clearance for enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID83552Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr188Leu2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID541131Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RT-6TAMs mutant gene to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID313877Selectivity index, ratio of EC50 for MT4 cells to EC50 for HIV12008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase--structure-activity relationships and crystallographic analysis.
AID82460Antiviral activity against K103N/G190A strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID440086Antiviral activity against HIV1 HXB2 harboring K103N and Y181C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID573998Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for CHI/1043-resistant Human immunodeficiency virus harboring T66I and Q146K mutations in integrase2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID583853Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID88378Antiviral activity against V106A/Y181C mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1304400Antiviral activity against HIV-1 RF infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID1171578Cytotoxic activity against human MT4 cells by MTT assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID663905Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2012European journal of medicinal chemistry, Jul, Volume: 535-acetyl-2-arylbenzimidazoles as antiviral agents. Part 4.
AID611909Antiviral activity against Human immunodeficiency virus 1 NL 4.3 harboring reverse transcriptase Y181C mutant pseudotyped with VSV-G envelope co-transfected with luciferase gene infected in 293T cells assessed as inhibition of HIV1 replication administere2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Lindenane disesquiterpenoids with anti-HIV-1 activity from Chloranthus japonicus.
AID622049Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer Y181C mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID448402Fold resistance, ratio of IC50 for HIV reverse transcriptase with K101E mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 3: optimisation of physicochemical properties.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID263512Antiviral activity against HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID269794Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269794Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269794Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID519871Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID370727Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID562703Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation.
AID1245795Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 96 hrs by MTT assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Isolation and anticancer, anthelminthic, and antiviral (HIV) activity of acylphloroglucinols, and regioselective synthesis of empetrifranzinans from Hypericum roeperianum.
AID279490Antiviral activity against HIV1 isolate with RT Y188L mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1884487Cytotoxicity against human MT4 cells assessed as cell growth inhibition incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID476473Cytotoxicity against human MT2 cells infected with HIV1 harboring reverse transcriptase K103N/Y181C mutation by MTT assay2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1637399Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring L100I mutant infected in human MT4 cells2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID279507Antiviral activity against HIV1 isolate with RT D123G mutation in Hela-JC-53 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID767497Cytotoxicity against human MT2 cells assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID572173Antiviral activity against HIV-1 subtype CRF05_DF V022824 harboring NNRTI V106I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID248846Inhibitory concentration against human immunodeficiency virus type 1 (with Y188C resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID366518Cytotoxicity against human MT4 cells by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1731749Inhibition of reverse transcriptase Y188L mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID371901Antiviral activity against HIV1 NL4-3 with Y181C mutant in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by multiple round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID457957Cytotoxicity in human MT4 cells assessed as reduction in cell viability2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1574386Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1637389Antiviral activity against human HIV-1 3B harboring RES056 mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID386498Antiviral activity against HIV1 with reverse transcriptase K103N/Y181C mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate.
AID302263Inhibition of HIV1 reverse transcriptase V179D mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID279527Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 30% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1811034Anti-viral activity against HIV1 harboring RT E138K mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1565097Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID279448Antiviral activity against HIV1 isolate with RT 101H, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1637395Antiviral activity against human HIV-1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID508636Antiviral activity against Human immunodeficiency virus 1 subtype G infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508629Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR029 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID443695Antiviral activity against HIV with reverse transcriptase K103N mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID698144Inhibition of HIV1 reverse transcriptase L100I mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID441316Fold resistance, ratio of IC50 for HIV reverse transcriptase with V108I mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
AID1763898Antiviral activity against HIV-1 IIIB harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID443678Antiviral activity against HIV with reverse transcriptase K103N mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID508647Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, E138G mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID519884Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID621981Resistance index, ratio of EC50 for HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant to EC50 for wild-type HIV1 3B2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID508773Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181V mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID492045Cytotoxicity against human MT4 cells after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
AID267651Selectivity for wild type HIV1 virus over HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID302250Selectivity index, ratio of CC50 for MT4 cells to EC50 for HIV1 NL43 infected MT4 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID293556Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1636146Antiviral activity against wild type HIV1 NL4-32016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID255644Effective concentration required to inhibit HTLV-III B induced cytopathicity in human CEM cells2005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives.
AID253494Dose required to inhibit HIV-1 reverse transcriptase activity (Y188L mutant) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID347089Metabolic stability in human liver microsomes assessed as half life2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
AID571982Antiviral activity against HIV-1 subtype B V022814 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID427975Antiviral activity against HIV1 infected in human HeLa cells expressing CD4-LTR assessed as inhibition of viral entry-related beta galactosidase expression treated for 2 hrs measured after 48 hrs by MAGI assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID1171579Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1348212Antiviral activity against wild-type VSV-G pseudotyped HIV1 infected in HEK293 cells at 10 uM pretreated for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay relative to control2017Journal of natural products, 12-22, Volume: 80, Issue:12
Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities.
AID82457Antiviral activity against G190A strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1348214Antiviral activity against VSV-G pseudotyped HIV1 infected in human MT2 cells pretreated for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay2017Journal of natural products, 12-22, Volume: 80, Issue:12
Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities.
AID1435511Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase
AID279493Antiviral activity against HIV1 isolate V106I-Y188L mutant2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID330489Antiviral activity against HIV1 RES056 infected in MT4 cells by MTT2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID302257Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT Y181C mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID621980Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID141362Ratio of Inhibitory activity against mutant K103N HIV-1 Reverse transcriptase to mutant L1001 HIV-1 Reverse transcriptase2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
AID685335Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B2012Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.
AID1815393Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1249723Antiviral activity against HIV1 expressing reverse transcriptase F227L + V106A mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID143398Compound was evaluated for its ability to inhibit the mutant K103N NNRTI HIV-1 enzyme2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID1552555Antiviral activity against HIV1 YU2 pseudovirus infected in human TZM-bl cells assessed as inhibition of viral infection incubated for 20 mins prior to infection and measured after 48 hrs post infection by bright Glo-luciferase reporter gene assay2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID1552557Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID1736359Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y188L mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infect
AID473115Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
AID573481Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8117 harboring A98S, G190A mutation in reverse transcriptase to wild-type2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1261813Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 4 days by MTT assay2015European journal of medicinal chemistry, Nov-13, Volume: 105Synthesis, cytotoxicity and antiviral evaluation of new series of imidazo[4,5-g]quinoline and pyrido[2,3-g]quinoxalinone derivatives.
AID523346Antiviral activity against HIV1 with RT connection domain T369V mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID665273Antiviral activity against HIV2 ROD mutant infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID665552Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
AID632799Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of viral infection2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID541154Selectivity ratio of EC50 for antiviral activity against APV-resistant HIV1 selected after 2 passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID586481Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155H/G163K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1761020Antiviral activity against HIV-1 harboring reverse transcriptase RES056 mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID665275Selectivity index ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2012European journal of medicinal chemistry, Jul, Volume: 53Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1773451Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells
AID366550Inhibition of HIV1 reverse transcriptase Y181C mutant by scintillation counting assay2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1171415Aqueous solubility of the compound at pH 6.5 after 48 hrs by shake-flask method2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID430054Inhibition of HIV1 recombinant RNA-dependent DNA polymerase activity of reverse transcriptase assessed as incorporation of radioactive dTTP into poly(rA)/oligo(dT)2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
AID279451Antiviral activity against HIV1 isolate with RT 101E, 108I, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID508641Antiviral activity against Human immunodeficiency virus 1 subtype AG infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID492287Antiviral activity against HIV1 with reverse transcriptase F227L, V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID197932HIV-1 reverse transcriptase inhibitory activity against Cys181 mutant using (poly)rC600*(oligo)dGT as template primer.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID605176Inhibition of wild type HIV1 reverse transcriptase by SPA assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
AID573997Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for MK-0518-resistant Human immunodeficiency virus harboring G140S and Q148H mutations in integrase2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID246265Effective concentration against human immunodeficiency virus type 1 G190S mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID440670Antiviral activity against NNRTI-resistant HIV1 N119 with reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.
AID496633Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, K43R, V60I, K101R, K122E, D123S, I135V, S162A, K173T, Q174K, D177E, V179I, G196E, T200A, Q207E mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID88368Antiviral activity against K103N/P225H mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID246359Protection of infected MT-4 cells from wtIIIB-HIV-1-induced cytopathogenicity2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID226171Compound was evaluated for the inhibition of wilde-type RF strain of HIV-12000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1141975Inhibition of HIV1 wild-type reverse transcriptase using [3H]dTTP by scintillation counting2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1155813Inhibition of wild type HIV-1 recombinant reverse transcriptase assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:12014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID718369Selectivity index, ratio of CC50 for HIV1 3B infected in human MT4 cells to EC50 for HIV1 3B2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
AID1750725Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase Y181C mutant2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID508635Antiviral activity against Human immunodeficiency virus 1 subtype (H) infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1352322Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID523484Antiviral activity against HIV1 with RT connection domain L100I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1750715Cytotoxicity against in human MT-4 cells after 5 days by MTT assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID279431Antiviral activity against HIV1 isolate with RT 103S, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1773455Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring E138K mutant infected in human MT4 cells
AID666973Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-32012European journal of medicinal chemistry, Aug, Volume: 54Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors.
AID1815380Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID368562Cytotoxicity against human MT4 cells by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID1320867Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1483280Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase L100I mutant in human MT4 cells infected HIV1 3B2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1743629Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID675389Cytotoxicity against human MT4 cells after 96 hrs by MTT assay2012European journal of medicinal chemistry, Sep, Volume: 55Disubstituted thiourea derivatives and their activity on CNS: synthesis and biological evaluation.
AID1391085Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID766430Aqueous solubility of the compound at pH 6.5 by shake-flask method2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.
AID279482Antiviral activity against HIV1 isolate with RT K103N mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID508796Ratio of EC50 for HIV1 in presence of 1 mg/ml alpha-1 acid-glycoprotein to EC50 for HIV1 in absence of serum proteins by GFP assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1435517Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase F227L/V106A double mutant
AID82467Antiviral activity against P236L strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID490372Antiviral activity against HIV1 expressing reverse transcriptase V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID496616Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, T39M, K46Q, V60I, S68G, D123E, I135V, S162A, K173A, Q174K,D177E, T200A, Q207E, R211K mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID252950Selectivity index of cytotoxic activity (CC50) to inhibitory activity (IC50) relative to LAI cell line2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID1565099Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1693799Antiviral activity against HIV-3B infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID1485967Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID465422Half life in Beagle dog at 0.5 mg/kg, iv or. 5 mg/kg, po2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID757624Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID267647Antiviral activity against HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID1335204Ratio of IC50 for HIV-1 NL4-3 harboring RT-Y188L mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1152370Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1285844Antiviral activity against HIV1 A17 infected in human C8166 cells assessed as reduction in p24 antigen level incubated for 4 hrs followed by cell plating for 72 hrs by ELISA method2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Design, synthesis and anti-HIV-1 evaluation of hydrazide-based peptidomimetics as selective gelatinase inhibitors.
AID1736345Cytotoxicity against human HEK 293T cells assessed as reduction in cell viability measured after 48 hrs by Celltiter-glo assay
AID1443670Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID557041Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1687691Inhibition of HIV-1BH10 reverse transcriptase expressed in Escherichia coli assessed as polymerization by real time FRET assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase.
AID279391Antiviral activity against HIV1 isolate with RT 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1248226Antiviral activity against wild type HIV 2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1220383Antiviral activity against HIV12013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID1483273Inhibition of HIV1 3B reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID279522Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells in the presence of 50% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID541162Selectivity ratio of EC50 for antiviral activity against HIV1 harboring L74M mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID263508Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID541133Selectivity ratio of EC50 for antiviral activity against NNRTI-resistant HIV1 harboring RTY181C mutant gene to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID571977Antiviral activity against HIV-1 subtype B V022809 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID508639Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1729163Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template incubated for 1 hr by ELISA2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1763897Antiviral activity against HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID279324Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells after dialysis2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID519861Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID586483Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155H/D232N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1352314Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1565088Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into template incubated for 1 hr by ELISA
AID779524Inhibition of recombinant wild type HIV-1 reverse transcriptase p66/p51 expressed in Escherichia coli JM109 using poly(rA)/oligo(dT)16 (1:1.2) as template/primer after 40 mins by spectrofluorometric analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.
AID1298252Inhibition of HIV1 reverse transcriptase p66/p51 G190A mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID584083Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase K103N mutant infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type HIV1 NL4-32010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1705186Antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1743620Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1261315Antiviral activity against human CVB5 infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity after 3 days by plaque reduction assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID106609Cytotoxic concentration that reduces the MT-4 cell viability by 50%2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
AID366529Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase Y181I mutant2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID519859Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID572169Antiviral activity against HIV-1 subtype D V022832 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID508624Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 92TH006 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1743631Antiviral activity against HIV1 harboring RT F227L/V106Amutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1741397Inhibition of reverse transcriptase E138K mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID416757Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in human CEM cells assessed as protection against virus-induced cytopathicity2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID248069Inhibitory concentration against 103N and 181C mutant strains was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.
AID508656Antiviral activity against Human immunodeficiency virus 1 subtype O misolate BCF01 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID523477Antiviral activity against HIV1 with RT connection domain G190A/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID586373Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Y143R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID571986Antiviral activity against HIV-1 subtype C V022829 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1212914Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID1446819Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1435508Antiviral activity against HIV1 expressing reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID508764Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K101E mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID82606The effect of protein binding on the antiviral activity versus wild type virus strain K103N was tested in the presence of acid glycoprotein in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID562704Selectivity ratio of EC50 for HIV1 harboring capsid I201V mutant protein infected in human HeLa cells to EC50 for wild type HIV1 infected in human HeLa cells2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation.
AID1637402Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring Y188L mutant infected in human MT4 cells2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID508634Antiviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773443Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV-1 3B infected in MT4 cells
AID620437Inhibition of wild type HIV1 reverse transcriptase2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID1653618Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mass spectrometry2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID583863Inhibition of HIV1 HXB2 reverse transcriptase K103N mutant activity by primer extension assay2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID726438Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID279435Antiviral activity against HIV1 isolate with RT 101Q, 103R mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID573480Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase to wild-type2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1220380Drug metabolism of the compound assessed as CYP2B6 (unknown origin)-mediated formation of metabolites with retention time of 1.92 mins at 5 uM by UPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID573472Antiviral activity of wild-type Human immunodeficiency virus 1 infected in human TZM-bl cells human assessed as inhibition of viral replication by luciferase reporter gene assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID276232Cytotoxicity against MT2 cells2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID82277Inhibition of HIV-1 IIIB replication in MT-4-infected wild type cells.2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID1743638Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1822283Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID509268Inhibition of HIV1 RT by ELISA2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Antiviral efficacy of the novel compound BIT225 against HIV-1 release from human macrophages.
AID492044Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
AID253492Dose required to inhibit HIV-1 reverse transcriptase activity (V179D mutant) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID698146Inhibition of wild type HIV1 reverse transcriptase RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID476472Antiviral activity against HIV1 reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as inhibition of viral replication by MTT assay2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1320866Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1754637Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID648424Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1261308Cytotoxicity against human MT4 cells assessed as cell viability after 96 hrs by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID370730Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 Y188L mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID572178Antiviral activity against HIV-1 subtype H V029523 harboring NNRTI K101Q and V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1761015Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1884493Antiviral activity against drug-resistant HIV-1 E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1754647Antiviral activity against HIV1 harboring RT RES056 mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID573996Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for L-870,810-resistant Human immunodeficiency virus harboring L74M, E92Q and S230N mutations in integrase2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1141973Ratio of EC50 for HIV1 harboring reverse transcriptase L1001 mutant to EC50 for wild type HIV1 NL4.32014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID247504Inhibitory activity against HIV-1 mutant strain 190S2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID82462Antiviral activity against K103N/P225H strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID508630Antiviral activity against Human immunodeficiency virus 1 subtype G isolate G3 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1822282Antiviral activity against HIV-1 harboring RES056 mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID430055Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
AID443433Cytotoxicity against human MT4 cells assessed as reduction of cell viability after 96 hrs by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis, pharmacological and antiviral activity of 1,3-thiazepine derivatives.
AID573976Antiretroviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID328842Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID572189Antiviral activity against HIV-1 SM058 harboring NNTRI 227L and 106A mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1320865Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID650696Ratio of ID50 for HIV 1 reverse transcriptase K103N mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID371911Antiviral activity against HIV1 NL4-3 with Y181C mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID443683Antiviral activity against HIV with reverse transcriptase L100I/K103N double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID508637Antiviral activity against Human immunodeficiency virus 1 subtype D infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1348217Antiviral activity against wild-type VSV-G pseudotyped HIV1 infected in HEK293 cells assessed as time of 50% failure at 1 uM measured at 48 hrs post infection by luciferase reporter gene assay2017Journal of natural products, 12-22, Volume: 80, Issue:12
Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities.
AID571983Antiviral activity against HIV-1 subtype B V022815 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID464771Volume of distribution at steady state in Beagle dog at 0.5 mg/kg, iv or 0.5 mg/kg, po2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID622050Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer Y188L mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID519023Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as increase in viral two-LTR circles2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID279477Antiviral activity against HIV1 isolate with RT 181V mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID576032AUC (0 to infinity) in healthy human plasma at 400 mg, measured on day 1 post dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID1811045Cytotoxicity against mock infected human MT4 cells by MTT assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1185992Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID571967Antiviral activity against HIV-1 subtype CRF02_AG V022808 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1653637Binding affinity to substrate bound recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli assessed as Kon rate of cholesterol by stopped-flow spectrophotometric method2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID1171587Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase K103N-Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID366530Resistance index, ratio of ID50 for reverse transcriptase Y181I mutant to IC50 for wild-type HIV1 reverse transcriptase2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID279458Antiviral activity against HIV1 isolate with RT 103Q mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID347612Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 225H mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID573474Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5269 by cell based assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID508623Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG035 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1316332Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID279481Antiviral activity against HIV1 isolate with RT 101E mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1335214Antiviral activity against HIV-1 NL4-3 harboring RT-L100I/K103N double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID368559Antiviral activity against HIV1 reverse transcriptase K103N mutant infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID440087Antiviral activity against HIV1 HXB2 harboring 227L and 106A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID440072Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV-1 LAI harboring wild type reverse transcriptase infected in human MT4 cells2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1880369Inhibition of HIV-1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorometric analysis2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID1773447Antiviral activity against wild type HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID94449Inhibitory concentration against wild-type virus K103N/L1001 and HIV-1 RT double mutant in whole cell antiviral assay2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.
AID586474Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138K/Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID96295Potency of second-generation NNRTIs against Mutant HIV-1 sL100I plasma; Value ranges from 6600-157002000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1637390Cytotoxicity against mock-infected human MT4 cells assessed as reduction of cell viability after 5 days by MTT assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID248354Concentration required to inhibit 50% viral production of human immunodeficiency virus type 1 (HIV-1-IIIB)2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Hierarchical database screenings for HIV-1 reverse transcriptase using a pharmacophore model, rigid docking, solvation docking, and MM-PB/SA.
AID1653622Binding affinity to recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli in absence of substrate by UV-spectrophotometric method2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID267653Selectivity for wild type HIV1 virus over HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID1261313Antiviral activity against YFV infected in BHK-21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID347618Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 236L mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID573477Antiviral activity of Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase by cell based assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID443703Antiviral activity against HIV with reverse transcriptase Y181C/G190A double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID1443667Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1773442Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
AID328846Inhibition of human MRP1 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID368565Inhibition of wild type HIV1 reverse transcriptase-DNA binary complex2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID83554Potency evaluated against wild type HIV-1 strain IIIB2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID94314Antiviral activity against HIV-1 K103N mutant virus.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID508628Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR020 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID440077Antiviral activity against HIV1 HXB2 harboring 101E mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID519868Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID571972Antiviral activity against HIV-1 subtype CRF01_AE V022821 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID541126Cytotoxicity against human SupT1 cells infected with HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1198751Inhibition of HIV1 reverse transcriptase Tyr181Cys mutant-associated DNA polymerase-independent RNase H activity after 1 hr2015European journal of medicinal chemistry, Mar-26, Volume: 93(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.
AID557043Inhibition of HIV1 isolate R8 reverse transcriptase Y181C mutant after 90 mins by electrochemiluminescence analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID267854Antiviral activity against wild type HIV1 NL4-3 in MT4 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID709870Antiviral activity against HIV1 expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID366549Inhibition of HIV1 reverse transcriptase K103N mutant by scintillation counting assay2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1220367Drug metabolism in human blood plasma assessed as formation of N- and O-linked glucuronidated metabolite at 100 mg administered every 4 hrs by UPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID302255Antiviral activity against HIV1 with reverse transcriptase Y188L mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID82603The effect of protein binding on the antiviral activity versus wild type virus strain HXB2 was tested in the presence of acid glycoprotein in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID443686Antiviral activity against HIV with reverse transcriptase Y181C/G190A double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID279437Antiviral activity against HIV1 isolate with RT 103N, 108I, 225H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID106769Cytotoxic dose required to reduce the viability of normal uninfected MT-4 cells by 50%2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID1535529Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(A)/oligo(dT)15 as template/primer after 1 hr by ELISA2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
AID298089Inhibition of HIV1 RT Y181I mutant2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID279454Antiviral activity against HIV1 isolate with RT 100I, 103N, 108I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID105535Inhibitory activity against HIV-1 Asn 103 mutant in MT-4 cells.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID586386Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66I/L74M mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficienc2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1373163Inhibition of reverse transcriptase K103N/Y181C double mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID298059Inhibition of HIV1 reverse transcriptase2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID1275552Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1729157Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID465420Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT2 cells2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID279471Antiviral activity against HIV1 isolate with RT 103N, 238N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID571981Antiviral activity against HIV-1 subtype B V022813 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID576038Ratio of drug concentration in PBMCs to plasma of healthy human administered at 400 mg, po measured after 24 hrs on day 1 post dose2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID299029Antiviral activity against HIV1 with reverse transcriptase E138K mutation in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID649488Inhibition of ribonuclease H activity of wild type Human immunodeficiency virus 1 reverse transcriptase2012European journal of medicinal chemistry, Apr, Volume: 50Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach.
AID508777Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1572518Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID299030Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID200153Inhibition of HIV-1 reverse transcriptase.2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
AID247618Inhibitory activity against HIV-1 double mutants strain 101E and 103N2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID441313Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y188C mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
AID1165076Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1535527Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 RES056 containing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
AID1298245Cytotoxicity against human MT4 cells after 5 days MTT assay2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID279470Antiviral activity against HIV1 isolate with RT 238T mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID256325Percentage inhibition of proliferation against alive human A-375 cells treated with DMSO (control) at a concentration of 15 uM2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
6-[1-(2,6-difluorophenyl)ethyl]pyrimidinones antagonize cell proliferation and induce cell differentiation by inhibiting (a nontelomeric) endogenous reverse transcriptase.
AID1245796Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Isolation and anticancer, anthelminthic, and antiviral (HIV) activity of acylphloroglucinols, and regioselective synthesis of empetrifranzinans from Hypericum roeperianum.
AID709867Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID440076Antiviral activity against HIV1 HXB2 harboring 100I mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID83550Potency evaluated against NNRTI-Resistant HIV-1 strain Lys103Asn2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1069123Antiviral activity against HIV harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum2014Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID1357805Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID573473Antiviral activity of wild-type Human immunodeficiency virus 1 harboring Y181C mutation in reverse transcriptase infected in human TZM-bl cells human assessed as inhibition of viral replication by luciferase reporter gene assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1880379Antiviral activity against HIV-1 IIIB harboring reverse transcriptase Y188L mutant infected in human MT4 cells by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
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AID1558848Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1357784Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID508649Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, V179L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1815384Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1687682Antiviral activity against HIV-1 Y181C mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID242820Dose required to inhibit HIV-1 reverse transcriptase activity (wild-type) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID256475Ratio of CC50 required to reduce the viability of mock-infected human CEM cells to EC50 required to inhibit HTLV-III B induced cytopathicity in that cells2005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives.
AID573977Antiretroviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID508762Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E, K103N mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID517493Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 40% human serum2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1407645Cytotoxicity against human CEM-GFP cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors.
AID1320869Inhibition of recombinant wild type HIV1 p66/p51 using poly(rA) template/oligo(dT)16 primer after 40 mins by PicoGreen-based spectrofluorometric method2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1729161Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID246799Compound concentration required to reduce the amount of p24 by 90% in C8166 cells infected with an efavirenz-resistant strain EFVR carrying mutations K103R, V179D, and P225H2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID279450Antiviral activity against HIV1 isolate with RT 98G, 103N, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID586475Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G140C/Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID82465Antiviral activity against L100I strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID658564Antiviral activity against multidrug-resistant HIV1 695-RT infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium.
AID1198752Inhibition of HIV1 reverse transcriptase Tyr181Cys mutant-associated RNA-dependent DNA polymerase activity after 30 mins2015European journal of medicinal chemistry, Mar-26, Volume: 93(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.
AID198911Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution K103N2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID279474Antiviral activity against HIV1 isolate with RT 101R, 103N, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID586473Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138K/Q148K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID448399Fold resistance, ratio of IC50 for HIV reverse transcriptase with F227L mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 3: optimisation of physicochemical properties.
AID298078Antiviral activity against wild type HIV1 3B in lymphocytes assessed as reduction of p24 antigen production2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID198106Inhibitory activity against R172A mutant reverse transcriptase2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.
AID508770Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190S mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1249714Antiviral activity against HIV1 3B expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1653634Binding affinity to recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli at 50 uM in presence of substrate by UV-spectrophotometric method2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID1687684Antiviral activity against HIV-1 RES056 mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID508787Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106M mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID293560Antiviral activity against HIV1 LAI with RT K103N mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1750724Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase K103N mutant2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1815392Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID279399Antiviral activity against HIV1 isolate with RT 179D mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1057039Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID361910Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase Y188L mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID726436Cytotoxicity in human MT2 cells assessed as inhibition of cell growth2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID1212898Drug metabolism in human liver microsomes harboring CYP2B6*6/*6 genotype assessed as CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by LC/MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID767495Aqueous solubility of the compound in Britton-Robinson buffer at pH 6.5 after 48 hrs by shake-flask method2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1157587Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID361914Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190E mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID82456Antiviral activity against E138K strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1407641Inhibition of recombinant HIV-1 reverse transcriptase RNA-dependent DNA polymerase activity at 1 ug/ml using poly(rA)/oligo(dT)16 as template/primer preincubated for 5 to 10 mins followed by template/primer addition and measured after 16 hrs by colorimetr2018European journal of medicinal chemistry, Sep-05, Volume: 157Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors.
AID427973Antiviral activity against HIV1 infected in human HeLa cells expressing CD4-LTR assessed as inhibition of viral entry-related beta galactosidase expression at 0.2 to 0.4 uM followed by drug wash out and viral infection measured after 48 hrs by MAGI assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID517492Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1637404Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring F227L/V106A double mutant infected in human MT4 cells2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID241471Inhibitory concentration against HIV-1 mutant reverse transcriptase (K103R)2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.
AID247497Inhibitory activity against HIV-1 mutant strain 103N2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID143402Compound was evaluated for its ability to inhibit the mutant K103N V1081NNRTI HIV-1 enzyme2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID1888693Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID1183081Antiviral activity against HIV-13B infected in MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT method2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and antiviral activity of new phenylimidazopyridines and N-benzylidenequinolinamines derived by molecular simplification of phenylimidazo[4,5-g]quinolines.
AID1736365Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase L100I/K103N double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel
AID1741396Inhibition of reverse transcriptase Y188L mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1261324Antiviral activity against HIV-1 infected in MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1457063Inhibition of HIV1 NL4-3 reverse transcriptase His-tagged p66/p51 associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation c2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID269800Antiviral activity against HIV1 V106A mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269800Antiviral activity against HIV1 V106A mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269800Antiviral activity against HIV1 V106A mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID88369Antiviral activity against K103N/V108I mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID293557Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 LAI2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID404605Inhibition of HIV1 virion-associated reverse transcriptase2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID247619Inhibitory activity against HIV-1 double mutants strain 103N and 181C2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID519881Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID557038Antiviral activity against HIV1 isolate R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID279424Antiviral activity against HIV1 isolate with RT 103N, 106A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID371914Antiviral activity against HIV1 NL4-3 with double K103N/L100I mutant in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by multiple round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1736363Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y181C mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cells
AID1248223Cytotoxicity against uninfected human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1446813Cytotoxicity against human MT4 cells after 5 days by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1457062Ratio of EC50 for HIV-1 harboring reverse transcriptase K103N/Y1881C double mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1636147Antiviral activity against NNRTI resistant HIV1 harboring reverse transcriptase V106I/Y181C/G190A/H221Y mutant assessed as inhibition of viral infection in human TZM-bl cells after 48 hrs by luciferase reporter gene assay2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID576028Volume of distribution in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID279423Antiviral activity against HIV1 isolate with RT 106I, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1773452Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring K103N mutant infected in human MT4 cells
AID302259Inhibition of wild type HIV1 3B reverse transcriptase2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID313193Antiviral activity against HIV1 Y181C mutant2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and antiviral activity of new dimeric inhibitors against HIV-1.
AID1815382Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1171586Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID658571Antiviral activity against wild type Human immunodeficiency virus 1 NL4-3 pseudotyped with VSV envelope infected in human HeLa-SxR5 cells assessed as inhibition of viral replication at 65 nM after 3 days by beta-galactosidase assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium.
AID473117Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
AID519858Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1741392Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID576039Ratio of drug concentration in PBMCs to plasma of healthy human administered at 400 mg, po measured after 5 hrs on day 1 post dose2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID1320864Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1304405Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human MT4 cells to EC50 for antiviral activity against HIV-1 3B2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID1391077Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID361906Antiviral activity against wild type HIV1 in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID370731Antiviral activity against HIV1 3B infected human C8166 cells assessed as inhibition of syncytia formation by p24 antigen based assay2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID1763902Antiviral activity against HIV-1 IIIB harboring RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID665553Fold resistance, ratio of EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant to EC50 for wild type HIV1 3B2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
AID1457060Ratio of EC50 for HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1815381Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1357797Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID663308Inhibition of HIV1 recombinant reverse transcriptase Y181I mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1880372Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID82605The effect of protein binding on the antiviral activity versus wild type virus strain HXB2 was tested in the presence of human serum in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1231487Inhibition of wild-type HIV1 Reverse transcriptase p66/p51 assessed as relative fluorescence signal after 40 mins2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID1457073Cytotoxicity against C57BL/6 mouse BV2 cells assessed as effect on cell proliferation rate at 10 to 10000 nM up to 48 hrs by MTT assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID557049Antiviral activity against HIV1 clade G harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1457055Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1056584Antiviral activity against wild-type HIV-1 infected in HEK293T cells co-transfected with VSVG protein assessed as time required for 50% failure of viral replication at 10 uM by luciferase reporter gene assay2013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID718368Cytotoxicity against HIV2 ROD infected in human MT4 cells by MTT assay2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
AID279440Antiviral activity against HIV1 isolate with RT 101R, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID735081Antiviral activity against HIV harboring reverse transcriptase Y181C mutant by cell based assay2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and biological evaluation of phosphonate analogues of nevirapine.
AID573245Cmin in HIV-1 infected children at 13.9 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID1750722Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID541174Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V, G140S and V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1261309Cytotoxicity against MDBK cells assessed as cell viability after 48 to 96 hrs by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1565095Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID541134Selectivity ratio of EC50 for antiviral activity against PI-resistant HIV1 harboring RTI84V, L90M mutant gene to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID622048Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer V106A mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID246283Effective concentration of the compound to inhibit HIV-1 mutant LAI replication in HIV-infected MT-4 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID736038Inhibition of HIV1 reverse transcriptase p66/p51 K103N/Y181C mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID523353Antiviral activity against HIV1 with RT connection domain Y181C mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID583865Inhibition of HIV1 histidine-tagged reverse transcriptase L100I mutant activity by primer extension assay2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID586385Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155T mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID241665Inhibitory concentration against HIV-1 mutant reverse transcriptase (K103N+Y181C)2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.
AID1750718Inhibition of HIV-1 p66/p51 reverse transcriptase K103N mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID584081Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, H221Y, F227F/L, M230M/I mutant infected in human SupT1 cells derived from 11 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID586387Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66I/E92Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficienc2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID586466Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase L74M/N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficien2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1057038Antiviral activity against HIV2 ROD infected in MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID1754644Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID255623Concentration required to reduce the viability of mock-infected human CEM cells2005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives.
AID1316342Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1884494Inhibition of recombinant wild-type p66/p51 HIV-1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID279436Antiviral activity against HIV1 isolate with RT 103R, 179D mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID105704Anti-HIV-1 activity against Y181C strain, in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID508757Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K, M230L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID106053Inhibitory activity against 100I strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID587738Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID607876Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type Human immunodeficieny virus 1 3B infected in human MT4 cells2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID88366Antiviral activity against K103N mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID586383Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1326646Inhibition of HIV-1 3B reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by cell titer glo based luciferase reporter gene assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.
AID141361Inhibitory activity against mutant K103N HIV-1 Reverse transcriptase2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
AID576027Apparent oral clearance in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID313189Protection against HIV1 HTLV 3B-induced cytopathogenicity in human MT4 cells by MTT assay2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and antiviral activity of new dimeric inhibitors against HIV-1.
AID1736362Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cells
AID404607Antiviral activity against HIV1 with reverse transcriptase K103R mutation2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID279499Antiviral activity against HIV1 isolate with RT A98G mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID269802Antiviral activity against HIV1 Y188L mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269802Antiviral activity against HIV1 Y188L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269802Antiviral activity against HIV1 Y188L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID416759Antiviral activity against HIV1 with reverse transcriptase Y188L mutation in human CEM cells assessed as protection against virus-induced cytopathicity2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID1483281Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase K103N mutant in human MT4 cells infected HIV1 3B2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1574376Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID522378Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106I/V179D mutant clone to EC50 for wild type HIV12010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID443688Antiviral activity against HIV with reverse transcriptase K101E/G190A double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID279447Antiviral activity against HIV1 isolate with RT 236L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID105203Antiviral activity against MT-4 cells infected with wild-type HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID573978Antiretroviral activity against Human immunodeficiency virus 2 EHO infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1186001Antiviral activity against HIV1 harboring reverse transcriptase K103N/P225H double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1161106Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID1815389Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID305058Cytotoxicity against HEK293T cells after 48 hrs2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
4-Aminopyrimidines as novel HIV-1 inhibitors.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID632804Cytotoxicity against human MT2 cells infected with HIV1 NL4.3 by MTT assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID1186008Antiviral activity against HIV1 infected in 293T cells assessed as time of 50% failure2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID279508Antiviral activity against HIV1 isolate with RT Y181C mutation in Hela-JC-53 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1822273Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1155812Fold resistance, ratio of EC50 for HIV-1 harboring NNTRI-resistant reverse transcriptase Y188L mutant infected in human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID368558Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID279444Antiviral activity against HIV1 isolate with RT 101Q, 181C, 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID448398Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y181C mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 3: optimisation of physicochemical properties.
AID1736366Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y188L mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cells
AID1729156Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1186002Antiviral activity against HIV1 harboring reverse transcriptase K103N/G190A double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID81765Compound was evaluated for its ability to inhibit a virus containing the clinically relevant K103N mutation2001Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
AID1483271Inhibition of HIV1 3B reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1763901Antiviral activity against HIV-1 IIIB harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1157601Antiviral activity against HIV1 CRF02 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID247499Inhibitory activity against HIV-1 mutant strain 138K2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID257167Antiviral activity against HIV1 IRLL98 mutant strain infected MT4 cells by MTT method2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID1335205Ratio of IC50 for HIV-1 NL4-3 harboring RT-L100I/K103N double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID282737Inhibition of HIV1 RT K103N mutant2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID1483277Inhibition of HIV1 3B reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID508832Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93IN101 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID361915Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106M mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID562701Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation.
AID519890Selectivity ratio of EC50 for 0.01 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.01 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID649487Inhibition of RNA-dependent DNA polymerase activity of Human immunodeficiency virus 1 reverse transcriptase Tyr181Cys mutant2012European journal of medicinal chemistry, Apr, Volume: 50Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach.
AID1335210Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/G190A double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1884542Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 E138K mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID105326Inhibition of HIV-1 (IIIB) induced cytopathicity in MT-4 cells.2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID389379Cytotoxicity against human MT4 cells2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID397177Antiviral activity against HIV1 3B expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID279518Antiviral activity against HIV1 NL4-3 in Hela-JC53 cells in the presence of 10% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID106065Inhibitory activity against 181C strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID440081Antiviral activity against HIV1 HXB2 harboring 190A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID586369Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID302258Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT Y188L mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1583021Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID276231Antiviral activity against HIV1 3B in MT2 cells2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1191401Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1191404Inhibition of wild type HIV1 p66/p51 reverse transcriptase by spectrofluorometry2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID88380Antiviral activity against V108I/Y181C mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID348906Antiviral activity against drug-resistant HIV1 with reverse transcriptase Y181C mutant infected in human MT4 cells assessed as virus-induced cell death by MTT method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies.
AID572182Antiviral activity against HIV-1 SM012 harboring NNTRI 108I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1379963Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2017European journal of medicinal chemistry, Nov-10, Volume: 140Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID611907Antiviral activity against wild type Human immunodeficiency virus 1 NL 4.3 pseudotyped with VSV-G envelope co-transfected with luciferase gene infected in human 293T cells assessed as inhibition of HIV1 replication administered 15 mins prior to infection 2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Lindenane disesquiterpenoids with anti-HIV-1 activity from Chloranthus japonicus.
AID508772Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y188L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1485969Inhibition of HIV-1 reverse transcriptase L100I mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID508774Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1249722Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID298074Antiviral activity against HIV1 3B in MT4 cells by MTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID279325Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells before dialysis2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID299027Antiviral activity against HIV1 with reverse transcriptase L100I mutation in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID649486Inhibition of RNA-dependent DNA polymerase activity of Human immunodeficiency virus 1 reverse transcriptase Lys103Asn mutant2012European journal of medicinal chemistry, Apr, Volume: 50Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach.
AID279452Antiviral activity against HIV1 isolate with RT 103N, 108I, 238T mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID605178Inhibition of HIV1 reverse transcriptase Y181C mutant by SPA assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
AID104802In vitro cytotoxicity against mock infected MT-4 cells.2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID666971Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days2012European journal of medicinal chemistry, Aug, Volume: 54Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors.
AID642209Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Quinoline tricyclic derivatives. Design, synthesis and evaluation of the antiviral activity of three new classes of RNA-dependent RNA polymerase inhibitors.
AID105700Anti-HIV-1 activity against K103N+Y181C strain was determined in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID573479Antiviral activity of Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase by cell based assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID105701Anti-HIV-1 activity against LAI strain in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID573464Inhibition of RNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase by filter-based filtration assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID443706Antiviral activity against HIV with reverse transcriptase K101E/Y181C/G190A mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID347610Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 100I mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID650545Antiviral activity against HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1815385Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID508621Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID572180Antiviral activity against HIV-1 SM002 harboring NNTRI 181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1691437Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2020European journal of medicinal chemistry, May-01, Volume: 193In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID391221Inhibition of wild type HIV1 RT polymerase by SPA2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID105537Inhibitory activity against HIV-1 Cys 181 mutant in MT-4 cells.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID541127Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of late RT products after 12 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID573249Cmax in HIV-1 infected children at 10 to 15 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID1731751Inhibition of reverse transcriptase F227L/V106A double mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1743619Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID279419Antiviral activity against HIV1 isolate with RT 101Q, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID508755Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID247617Inhibitory activity against HIV-1 double mutants strain 100I and 103N2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID371909Antiviral activity against HIV1 NL4-3 with L100I mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1552560Antiviral activity against HIV1 LAI infected in human LC5 cells expressing DsRed1 reporter gene assessed as inhibition of viral infection measured after 48 hrs post infection by reporter gene based luminescence assay2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID1822278Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID248068Inhibitory concentration against 100I and 103N mutant strains was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.
AID519965Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1483282Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase Y181C mutant in human MT4 cells infected HIV1 3B2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID279468Antiviral activity against HIV1 isolate with RT 98G, 108I, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1637396Antiviral activity against human HIV-1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID649489Inhibition of ribonuclease H activity of Human immunodeficiency virus 1 reverse transcriptase Lys103Asn mutant2012European journal of medicinal chemistry, Apr, Volume: 50Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach.
AID279320Inhibition of reverse transcriptase assessed as decrease in ssDNA level in cell free virion HIV1 by NERT-based real-time PCR at 250 uM2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID1204077Cytotoxicity against human MT4 cells assessed as cell viability after 96 hrs by MTT method2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-((1,3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents.
AID361928Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V108I/Y181C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID557035Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1888692Selectivity index, ratio of CC50 for toxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells cells assessed as protection against viral-induc
AID557047Antiviral activity against HIV1 clade D harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1535523Antiviral activity against HIV1 RES056 containing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
AID496615Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, K64R, K102Q, D123E, S162A, K173T, Q174K, D177E, G196E,T200A, Q207E, R211K mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1069126Antiviral activity against wild-type HIV infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum2014Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID1624241Binding affinity to HIV1 cYTA48P envelope glycoprotein gp120 infected in human TZM-b1 cells assessed as induction of conformational changes measured after 48 hrs2019Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5
Soluble-type small-molecule CD4 mimics as HIV entry inhibitors.
AID476469Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus replication by MTT assay2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1729159Antiviral activity against HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID584237Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I mutant derived from 17 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type HIV1 NL4-2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID269689Antiviral activity against HIV1 NNTRI resistant L100I mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269689Antiviral activity against HIV1 NNTRI resistant L100I mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269689Antiviral activity against HIV1 NNTRI resistant L100I mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1348213Antiviral activity against wild-type VSV-G pseudotyped HIV1 infected in HEK293 cells pretreated for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay2017Journal of natural products, 12-22, Volume: 80, Issue:12
Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities.
AID83547Potency evaluated against NNRTI-Resistant HIV-1 strain Gly190Ala2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID279528Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 40% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1457054Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID635302Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID298061Antiviral activity against HIV1 3B in human MT4 cells by XTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID1191402Cytotoxicity against human MT4 cells after 5 days MTT assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID465424Oral bioavailability in Beagle dog at 4 mg/kg2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1171595Inhibition of wild type HIV1 reverse transcriptase Y181I/Y181C mutant assessed as reduction in enzyme activity2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1180486Antiviral activity against VSV-G protein pseudotyped HIV1 infected in 293T cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter assay2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Uralsaponins M-Y, antiviral triterpenoid saponins from the roots of Glycyrrhiza uralensis.
AID1888704Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT F227L + V106A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID586482Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase N155H/G163R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1773450Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID619637Antiviral activity against HIV-1 3B harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID1126508Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1171412Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1822281Antiviral activity against HIV-1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1261812Cytotoxicity against human MT4 cells assessed as reduction in cell proliferation after 96 hrs by MTT assay2015European journal of medicinal chemistry, Nov-13, Volume: 105Synthesis, cytotoxicity and antiviral evaluation of new series of imidazo[4,5-g]quinoline and pyrido[2,3-g]quinoxalinone derivatives.
AID557039Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID279525Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 10% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID361913Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190S mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID650548Resistance ratio of EC50 for HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1165078Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1231485Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID440669Cytotoxicity against human MT4 cells assessed as reduction of cell viability after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.
AID1316341Antiviral activity against HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID583869Inhibition of HIV1 histidine-tagged reverse transcriptase V108I mutant activity by primer extension assay2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID370728Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 V106A mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID523479Antiviral activity against HIV1 with RT connection domain G190S mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID508754Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1373162Inhibition of reverse transcriptase F227L/V106A double mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID265471Activity against HIV1 3B assessed by inhibition of p24 production in human lymphocytes2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID573248Cmax in HIV-1 infected children at 12 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID366527Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase K103N mutant2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID492286Antiviral activity against HIV1 with reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID523354Antiviral activity against HIV1 with RT connection domain Y181C/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID583852Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID576029Apparent oral clearance in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID586382Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase M154I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID650688Inhibition of HIV 1 reverse transcriptase L100I mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1815387Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID267652Selectivity for wild type HIV1 virus over HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID1126507Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID576037Half life in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID1320863Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1235381Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 assessed as reduction in biotin deoxyuridine triphosphate (biotin-dUTP) incorporation using poly(rA)/oligo (dT)16 template and primer by spectrofluorometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1888694Antiviral activity against HIV1 with RT L100I mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID586467Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E92Q/N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficien2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1272056Inhibition of HIV1 reverse transcriptase2016European journal of medicinal chemistry, Jan-27, Volume: 108Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry.
AID1627026Cytotoxicity against HIV1 infected human PBMC cells assessed as reduction in cell viability after 7 days by MTT assay2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID519961Selectivity ratio of EC50 for 0.02 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.02 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID496742Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/V35T, K122E, I135V, T139A, S162A, K173T, Q174K, N175Y, D177E, T200A, Q207E, R211K mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1220382Antiviral activity against HIV1 expressing Env-green fluorescent fusion protein infected in PBMC assessed as inhibition of viral activity after 72 hrs by flow cytometry analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID464768Half life in human microsomes2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1171585Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID573468Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase DNA-dependent DNA polymerase activity by gel-based primer extension assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1822279Antiviral activity against HIV-1 harboring Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID247505Inhibitory activity against HIV-1 mutant strain 227C2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID1743634Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID698302Antiviral activity against HIV1 containing reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1391086Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1888703Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID1410483Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID1155816Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase L100I mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:12014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID586363Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E92Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID508797Ratio of EC50 for HIV1 in presence of 45 mg/ml HSA to EC50 for HIV1 in absence of serum proteins by GFP assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1220372Seminal plasma protein binding in human at 100 mg administered every 4 hrs by ultrafiltration method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID1705189Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1558857Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID252955Ratio of CC50 and EC50 against wild type human immunodeficiency virus type 1 LAI strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID198917Inhibition of HIV-1 wild-type RT2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID573469Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1335220Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/Y188L double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1357792Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1185995Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay relative HIV12014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID248258In vitro inhibitory concentration against HIV G190S mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1637403Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring E138K mutant infected in human MT4 cells2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID347085Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 reverse transcriptase2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
AID508827Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG037 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID88364Antiviral activity against E138K mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID361926Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106A/Y181C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1390715Resistance index, ratio of EC50 for HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID1636148Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase A98G/K101E/Y181C/G190A mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID269798Antiviral activity against HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269798Antiviral activity against HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269798Antiviral activity against HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1815397Inhibition of HIV1 reverse transcriptase L100I mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1767116Inhibition of wild type HIV-1 NL4-3 reverse transcriptase using random mRNA as template and GADPH as primer measured at 42 degreeC for 5 mins, 95 degreeC for 10sec and 60 degreeC for 60 sec by qRT-PCR analysis2021European journal of medicinal chemistry, Aug-05, Volume: 220Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.
AID650546Antiviral activity against HIV 1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1197833Resistance index, ratio of EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant to EC50 for wild type HIV1 3B2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID1535525Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
AID1410482Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID371897Selectivity index, ratio of CC50 for human TZM-b1 cells to EC50 for HIV1 NL4-32009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID348904Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as virus-induced cell death by MTT method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies.
AID1059141Selectivity index, ratio of CC50 for human MT4 cells to EC50 for drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID366558Antiviral activity against HIV1 with reverse transcriptase K103N/L100I mutation in human MT4 cells assessed as reduction of virus-induced cytopathic effect2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID571975Antiviral activity against HIV-1 subtype CRF01_AE V029525 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID347617Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 227L mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1609108Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID263153Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID263153Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID263153Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1583023Selectivity index, ratio of CC50 for cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay to EC50 for antiviral activity against NNRTI-resistant HIV1 RES056 containing reverse transcriptas2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID279465Antiviral activity against HIV1 isolate with RT 98G, 103N, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1565093Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB
AID698294Antiviral activity against HIV1 IRLL98 containing reverse transcriptase K101Q, Y181C and G190A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID767498Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1163234Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID648422Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1197830Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID279412Antiviral activity against HIV1 isolate with RT 103N, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1705190Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID105205Potency against non nucleoside reverse transcriptor was determined in MT-4 cells2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Threshold interaction energy of NRTI's (2'-deoxy 3'-substituted nucleosidic analogs of reverse transcriptase inhibitors) to undergo competitive inhibition.
AID1286677Aqueous solubility of the compound at pH 72016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID584047Ratio of IC50 for HIV1 reverse transcriptase Y181C, Y188C mutant to IC50 for wild type HIV1 reverse transcriptase2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID248648Inhibitory concentration against wild type human immunodeficiency virus type 1 was determined by recombinant virus assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID572170Antiviral activity against HIV-1 subtype D V022818 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1171413Antiviral activity against wild type HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1558847Antiviral activity against HIV1 3B infected in human MT4 cells incubated assessed as reduction in virus-induced cytopathic effect for 5 days by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1171589Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-32014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1335211Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/Y188L double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1198754Inhibition of HIV1 reverse transcriptase Lys103Asn mutant-associated RNA-dependent DNA polymerase activity after 30 mins2015European journal of medicinal chemistry, Mar-26, Volume: 93(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.
AID1627030Antiviral activity against HIV-1 LAI infected in human PBM cells after 7 days2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1565091Antiviral activity against drug resistant HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID106949Anti-HIV-1 activity against WTIIIB HIV-1 strain in MT-4 cells2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID143395Antiviral activity against HIV-1 in MT-2 (human leukemia) cells in vitro.2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID1316339Antiviral activity against HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1352312Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID279430Antiviral activity against HIV1 isolate with RT 103N, 106I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1373158Inhibition of reverse transcriptase L100I mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID263516Antiviral activity against HIV1 I135V mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1275550Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID298090Inhibition of HIV1 RT L100I mutant2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID441311Fold resistance, ratio of IC50 for HIV reverse transcriptase with F227L mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
AID508785Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138A mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID279511Antiviral activity against HIV1 isolate with RT V106I, Y181C mutation in Hela-JC-53 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1693802Inhibition of recombinant HIV-1 BH10 reverse transcriptase using D38/[32P]25PGA as template-primer at 100 uM incubated for 5 mins followed by dTTP addition and measured after 15 to 30 sec by nucleotide incorporation assay relative to control2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID247503Inhibitory activity against HIV-1 mutant strain 190A2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID496618Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, V60I, K122E, D123S, I135V, E138D, S162A, K173T,Q174S, D177E, I178M, V189I, T200A, I202V, Q207E, F214L, V245Q mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID279517Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells in the presence of 5% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID371903Antiviral activity against HIV1 NL4-3 with L100I/V108I double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID82961Inhibitory activity against HIV-1 reverse transcriptase1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).
AID621974Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1242376Resistance index, ratio of EC50 for NRTI-resistant HIV containing reverse transcriptase K103N/Y181C mutation to EC50 for wild type HIV2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase.
AID571978Antiviral activity against HIV-1 subtype B V022810 harboring NNRTI A98S andK101R mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1249715Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID698145Inhibition of HIV1 reverse transcriptase K103N mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID248494In vitro inhibitory concentration against HIV L100I and K103N mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1736344Antiviral activity against VSVG/wild-type HIV-1 infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infection by luciferase reporter gene ass
AID650542Antiviral activity against multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant infected in human MT4 cells assessed as virus-induced cytopathic effect after 5 days by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1443660Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID591355Antiviral activity against HIV2 isolate ROD infected in human CEM cells assessed as inhibition of virus-induced cytopathicity after 4 days by microscopic analysis2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
AID621978Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID366556Antiviral activity against HIV1 in human MT4 cells assessed as reduction of viral-induced cytopathic effect in presence of human serum2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID592540Cytotoxicity against human CEM cells by coulter counter analysis2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
AID1316337Antiviral activity against HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1165077Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1815398Inhibition of HIV1 reverse transcriptase K103N mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1773456Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells
AID508644Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773839Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID279489Antiviral activity against HIV1 isolate with RT K103N-V108I-P225H mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1483283Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase Y188L mutant in human MT4 cells infected HIV1 3B2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID265470Cytotoxicity against human lymphocytes2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID562119Apparent oral clearance in patient with HIV infection at 600 mg/kg, iv QD2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients.
AID541132Selectivity ratio of EC50 for antiviral activity against NNRTI-resistant HIV1 harboring RTK103N mutant gene to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID576040Ratio of drug concentration in PBMCs to plasma of healthy human administered at 400 mg, po qd for 14 days measured after 5 hrs post last dose2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID265474Selectivity index, TC50 for human lymphocytes/EC50 for HIV1 3B2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID267862Inhibition of HIV1 reverse transcriptase K103N mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID1165075Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1316340Antiviral activity against HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1884488Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against NNRTI resistant HIV-1 infected in human MT4 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID635347Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID522373Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106I/V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1485973Inhibition of HIV-1 reverse transcriptase Y181C mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID1141963Antiviral activity against HIV-2 ROD infected in human CEM cells assessed as protection of cells monitored by giant cell formation by microscopy2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID386493Inhibition of HIV1 recombinant wild type reverse transcriptase2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate.
AID82474Antiviral activity against Y181C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID717257Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID1352315Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1391076Inhibition of wild type HIV1 reverse transcriptase using poly (A)/oligo (dT)15 as template/primer assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID508783Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID519863Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID573482Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase to wild-type2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1335216Antiviral activity against HIV-1 NL4-3 harboring RT-K103N mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1212900Drug metabolism in human liver microsomes harboring CYP2B6*1/*6 genotype assessed as intrinsic clearance for CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID269687Antiviral activity against HIV1 NNTRI resistant Y181C mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269687Antiviral activity against HIV1 NNTRI resistant Y181C mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269687Antiviral activity against HIV1 NNTRI resistant Y181C mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID573247Cmin in HIV-1 infected children at 14.4 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID106950Anti-HIV-1 activity against Y181C HIV-1 strain in MT-4 cells2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID82604The effect of protein binding on the antiviral activity versus wild type virus strain HXB2 was tested in the presence of both acid glycoprotein and human serum in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID247495Inhibitory activity against HIV-1 mutant strain 100I2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID241533Inhibitory concentration against HIV-1 wild type reverse transcriptase (IIIB)2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.
AID573478Antiviral activity of Human immunodeficiency virus 1 isolate 8117 harboring A98S, G190A mutation in reverse transcriptase by cell based assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1761019Antiviral activity against HIV-1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID246394Effective concentration against human immunodeficiency virus type 1 mutated at 227L+106A2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1636931Aqueous solubility of compound in pH 6.5 solution by shake flask method2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Computer-aided discovery of anti-HIV agents.
AID757622Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1636149Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase K103N/V179F/Y181C mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID1316344Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID607873Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID198769Binding affinity towards wild type HIV-1 reverse transcriptase (as per ref 10 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID105540Inhibitory activity against HIV-1 Wild Type in MT-4 cell culture (human T-cell line with 50% human AB serum)1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID1304401Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID374090Antiviral activity against HIV1 3B Y181C resistant mutant in human MT4 cells assessed as protection against viral induced cytopathogenicity by MTT assay2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Novel modifications in the series of O-(2-phthalimidoethyl)-N-substituted thiocarbamates and their ring-opened congeners as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID446236Inhibition of HIV reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID279426Antiviral activity against HIV1 isolate with RT 227L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID508825Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG029 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID246351Effective concentration against human immunodeficiency virus type 1 mutated at 188L2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID44797In vitro reduction of p24 by 90% in Efavirenz resistant HIV-1 (K103R, V179D, P225H) infected C8166 cells.2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID508788Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106A mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508793Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID105698Anti-HIV-1 activity against K103N+K1001 strain was determined in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID96294Potency of second-generation NNRTIs against Mutant HIV-1 sL100I free drug2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID328843Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID1457052Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
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A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID586485Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase L101I/T124A/S153F mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunod2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID632795Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT2 cells assessed as inhibition of viral infection2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID663300Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 NL4-32012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1596754Cytotoxicity against human MT4 cells measured after 5 days by MTT assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID216433Activity against whole cell using anti-infectivity assay1999Bioorganic & medicinal chemistry letters, Oct-04, Volume: 9, Issue:19
Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.
AID648421Cytotoxicity against human MT4 cells after 5 days by MTT assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID446409Fold resistance, ratio of IC50 for HIV reverse transcriptase with L100I mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID1558854Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1391079Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID279461Antiviral activity against HIV1 isolate with RT 179D, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1206938Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015European journal of medicinal chemistry, Jun-05, Volume: 97Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID279439Antiviral activity against HIV1 isolate with RT 101P, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1320868Solubility of the compound2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID446255Fold resistance, ratio of IC50 for HIV reverse transcriptase with V106A mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID1335203Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/P225H double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1335212Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/P225H double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID298075Antiviral activity against HIV1 RT Y181C mutant in MT4 cells by MTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID614140Cytotoxicity against human MT4 cells after 4 days by MTT assay2011Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
AID1815394Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A double mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID298087Inhibition of wild type HIV1 RT2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID573979Antiretroviral activity against Simian immunodeficiency virus MAC 251 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1574382Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV-1 NL4-32019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID347086Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase K103N mutant2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
AID519964Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID293559Antiviral activity against HIV1 LAI with RT Y188L mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1141976Inhibition of HIV1 wild-type reverse transcriptase K103N mutant using [3H]dTTP by scintillation counting2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1200844Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID1761012Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID141360Potency of second-generation NNRTIs against Mutant HIV-1 sV179D/L100I/Y181C plasma; value ranges from 130000-3095002000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1884229Antiviral activity against HIV-1 RES056 infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID266346Inhibition of HIV1 reverse transcriptase K103N mutant in 293T cells2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.
AID253332Cytotoxic concentration against wild type human immunodeficiency virus type 1 LA1 strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID611908Antiviral activity against Human immunodeficiency virus 1 NL 4.3 harboring reverse transcriptase K103N mutant pseudotyped with VSV-G envelope co-transfected with luciferase gene infected in 293T cells assessed as inhibition of HIV1 replication administere2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Lindenane disesquiterpenoids with anti-HIV-1 activity from Chloranthus japonicus.
AID465418Antiviral activity against wild type HIV1 infected in human MT2 cells2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID508790Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID269804Antiviral activity against HIV1 Y181H mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269804Antiviral activity against HIV1 Y181H mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269804Antiviral activity against HIV1 Y181H mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID198070Inhibitory activity against E138K mutant reverse transcriptase2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.
AID1352323Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 using poly (rA)/anoligo (dT)16 as template/primer assessed as inhibition of biotin-dUTP incorporation after 40 mins by Pico-Green staining based fluorescence assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1272057Tmax in human plasma after the first dose of drug2016European journal of medicinal chemistry, Jan-27, Volume: 108Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry.
AID361927Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106I/Y181C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1264541Antiviral activity against HIV-1 X4 expressing reverse transcriptase Y181C mutant infected in human CD4+ T cells for 3 days by FACS analysis2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1811035Anti-viral activity against HIV1 harboring RT Y188L mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID557021Antiviral activity against HIV1 CRF02_AG harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID347608Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 190A mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID509269Inhibition of HIV1 RT at 20 to 0.625 uM by ELISA2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Antiviral efficacy of the novel compound BIT225 against HIV-1 release from human macrophages.
AID279422Antiviral activity against HIV1 isolate with RT 190E mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID508781Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138R mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID517495Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1316360Fold resistance, ratio of IC50 for recombinant HIV1 reverse transcriptase K103N/Y181C double mutant to IC50 for wild type HIV1 reverse transcriptase2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1888695Antiviral activity against HIV1 with RT K103N mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1636150Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase L100I/K103N/H221Y mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID1200847Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID1691435Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cell death incubated for 5 days by MTT assay2020European journal of medicinal chemistry, May-01, Volume: 193In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID1141971Ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4.32014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1687681Antiviral activity against HIV-1 K103N mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1880373Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
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AID508626Antiviral activity against Human immunodeficiency virus 1 subtype E isolate CMU08 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1316328Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID348907Ratio of ED50 for drug resistant HIV1 with reverse transcriptase K103N mutant to wild type HIV1 NL4-32008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies.
AID1705193Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID573253AUC (0 to t) in HIV-1 infected children at 14.4 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID82476Antiviral activity against wild-type HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID767501Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID106074Inhibitory activity against LAI strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID574002Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for wild-type Human immunodeficiency virus 2 ROD2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1773445Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID386489Antiviral activity against HIV1 with reverse transcriptase K103N/Y181C mutation in human MT4 cells assessed as reduction of virus-induced cytopathogenicity by MTT assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Parallel synthesis, molecular modelling and structure-activity relationship studies on O-[2-(hetero)arylethyl]-N-phenylthiocarbamates.
AID496626Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K22N, V35T, T39A, K122E, I135V, T139A, S162A, K173T, Q174A, D177E, T200A, Q207E, R211K, F214L mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1248225Antiviral activity against HIV 1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID619642Ratio of EC50 for HIV-1 3B harboring RT E138K mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID557037Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID518741Antiviral activity against HIV 1 subtype B harboring reverse transcriptase M230L mutant infected in human TZM-bl cells assessed as inhibition of viral growth by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID366523Resistance index, ratio of EC50 for drug-resistant HIV1 isolate with reverse transcriptase Y181C mutation to EC50 for wild type HIV1 NL4-32008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID492043Inhibition of HIV1 reverse transcriptase2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
AID440074Antiviral activity against HIV1 HXB2 harboring Y181C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1171582Antiviral activity against HIV2 ROD infected in human CEM cells assessed as protection against virus-induced cytopathicity by giant cell formation assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1191399Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID622053Ratio of Ki for HIV1 RT p66/p66 homodimer L100I mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID361919Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase E138K mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID104408Antiviral activity of Protein Binding of compound was evaluated for HIV-2 virus expressed MT-2 by yield2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID246511Compound concentration required to achieve 50% protection of infected MT-4 cells from K103N-Y181C strain was determined by the MTT method2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID371902Antiviral activity against wild type HIV1 NL4-3 in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by multiple round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID519860Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID443677Antiviral activity against HIV with reverse transcriptase L100I mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443675Antiviral activity against HIV with reverse transcriptase MDRC4 mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID1168822Inhibition of CYP2B6 (unknown origin) assessed as reduction in hydroxybupropion formation at 10 uM incubated for 10 mins by uHPLC-MS/MS method2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Structure-Activity Studies Reveal the Oxazinone Ring Is a Determinant of Cytochrome P450 2B6 Activity Toward Efavirenz.
AID1156487Cytotoxicity against human MT4 cells after 5 days by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors.
AID248257In vitro inhibitory concentration against HIV G190A mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID476468Cytotoxicity against human MT2 cells by MTT assay2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1212885Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID1574372Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1391080Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID397176Inhibition of wild-type HIV1 reverse transcriptase2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1561720Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenes
AID1687683Antiviral activity against HIV-1 E138K mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID557048Antiviral activity against HIV1 clade F1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID347090Metabolic stability in human hepatocytes assessed as half life2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
AID1736360Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase G190A/K103N double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr
AID557068Plasma protein binding in healthy human at 200 mg/kg2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1298249Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1155809Antiviral activity against HIV-1 harboring NNTRI-resistant reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID586477Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G140S/Q148K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1220381Drug metabolism of the compound assessed as CYP2C8 (unknown origin)-mediated formation of dihydroxylated metabolites with retention time of 1.92 mins at 5 uM by UPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID257166Antiviral activity against wild type HIV1 NL4-3 infected MT4 cells by MTT method2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1456306Inhibition of HIV-1 3B wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID366519Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-32008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1186005Antiviral activity against HIV1 harboring reverse transcriptase K103N/V108I double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID736440Non-competitive inhibition of wild type HIV1 reverse transcriptase p66/p51 after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID267648Antiviral activity against HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID443691Antiviral activity against HIV with reverse transcriptase V106A/G190A/F227L mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID757625Antiviral activity against HIV1 RES056 expressing RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID81627Antiviral activity was evaluated against K103N mutant HIV-1 virus2001Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9
Synthesis and evaluation of efavirenz (Sustiva) analogues as HIV-1 reverse transcriptase inhibitors: replacement of the cyclopropylacetylene side chain.
AID313190Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV12008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and antiviral activity of new dimeric inhibitors against HIV-1.
AID496622Antiviral activity against HIV-1 subtype CRF06_cpx ontaining reverse transcriptase V106I/V21I, V35T, V60I, K122T, D123R, I135V, S162A, K173T, Q174K, D177E, I178L, T200A, Q207D, R211K, V245Q, E248D mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID370726Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID1357785Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID508753Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID279455Antiviral activity against HIV1 isolate with RT 103N, 188H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID620429Antiviral activity against wild type HIV1 BaL in human TZM-b1 cells after 48 hrs by luciferase assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID1352317Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1731752Inhibition of reverse transcriptase RES056 mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1261316Antiviral activity against human RSV infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by plaque reduction assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1811037Anti-viral activity against HIV1 harboring RT K103N mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1687687Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells reduction in cell viability by MTT assay to EC50 for antiviral activity against wild type HIV-1 strain IIIB infected in human MT4 cells assessed as reduction in virus-induced cytopa2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID573466Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID556524Antiviral activity against Human immunodeficiency virus 1 clone pNL4-3-Q145M harboring K102Q, Q145M, S162C, K277R, I293V mutation in reverse transcriptase by phenosense assay relative to wild type2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility.
AID508642Antiviral activity against Human immunodeficiency virus 1 subtype AE infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1410405Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as decrease in biotin-dUTP incorporation using DIG-labeled dUTP/biotin-labeled dUTP and dTTP as template and viral nucleotides after 1 hr by ELISA2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.
AID105539Inhibitory activity against HIV-1 Ile 100 mutant in MT-4 cells.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID1653625Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) R415A mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID248316In vitro inhibitory concentration against HIV-1 Y181C mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID279462Antiviral activity against HIV1 isolate with RT 103N, 108I, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1155814Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase K103N mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:12014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1535522Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
AID279418Antiviral activity against HIV1 isolate with RT 98G, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1558853Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1763903Antiviral activity against HIV-1 IIIB harboring RT F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID519867Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID244633Selective index value (ratio of CC50 to IC50 value)against HIV LAI cell line2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID304872Antiviral activity against HIV1 with reverse transcriptase IRLL98 mutation in MT4 cells after 5 days by MTT method relative to wild type NL4-32007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.
AID1483286Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID522377Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106A/V179D mutant clone to EC50 for wild type HIV12010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID663301Resistance ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-32012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID347615Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 108I mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID440073Antiviral activity against HIV1 HXB2 harboring K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1206937Cytotoxicity against human MT4 cells assessed as reduction of cell viability after 4 days by MTT assay2015European journal of medicinal chemistry, Jun-05, Volume: 97Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1637391Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B infected in human MT4 cells2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1304406Inhibition of wild type HIV-1 BH10 recombinant reverse transcriptase expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rA)/oligo(dT) as template primer2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID104412Antiviral activity of Protein Binding of compound was evaluated for RF virus expressed MT-2 by yield2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID650694Ratio of ID50 for HIV 1 reverse transcriptase Y181I mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID508771Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190A mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID389378Antiviral activity against HIV1 3B in human MT4 cells assessed as protection of cell against virus-induced cytopathogenicity2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID573990Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for non nucleoside Protease inhibitor-resistant Human immunodeficiency virus 12008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1483276Inhibition of HIV1 3B reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1373155Cytotoxicity against human MT4 cells after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID1637397Antiviral activity against human HIV-1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID246267Effective concentration against human immunodeficiency virus type 1 L100I mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1558856Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1767118Antiviral activity against HIV1 NL4-3 Env-deficient VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production when host cells were infected with compound pretreated viral particles at 10 uM measured after2021European journal of medicinal chemistry, Aug-05, Volume: 220Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.
AID508631Antiviral activity against Human immunodeficiency virus 1 subtype G isolate JV1083 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1292010Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells assessed as cell viability after 4 days by MTT assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1503322Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 4 days by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation.
AID269801Antiviral activity against HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269801Antiviral activity against HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269801Antiviral activity against HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID265473Activity against HIV-AB1 assessed by inhibition of p24 production in human lymphocytes2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID1298251Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1743626Antiviral activity against HIV1 harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID717258Cytotoxicity against human MT4 cells by MTT assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID1691438Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, May-01, Volume: 193In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID1316359Inhibition of recombinant HIV1 reverse transcriptase K103N/Y181C double mutant using DIG-dUTP/biotin-dUTP/dTTP assessed as suppression of biotin-dUTP incorporation after 1 hr by ELISA2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1155807Antiviral activity against HIV-1 harboring NNTRI-resistant reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID663295Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1731743Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID279417Antiviral activity against HIV1 isolate with RT 106A, F227L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID572171Antiviral activity against HIV-1 subtype D V022819 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID198913Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution V106A2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID1773838Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID298080Antiviral activity against HIV1 RT AB1 mutant in lymphocytes assessed as reduction of p24 antigen production2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID1880378Antiviral activity against HIV-1 IIIB harboring reverse transcriptase Y181C mutant infected in human MT4 cells by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID347614Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 106A mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID246482Effective concentration for the inhibition of wild type human immunodeficiency virus type 1 LAI strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID293564Antiviral activity against HIV1 LAI with RT K103N and Y181C mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID279526Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 20% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1485968Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID279513Antiviral activity against HIV1 isolate with RT V106I, Y181C, F227L, T369I mutation in Hela-JC-53 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1624242Cytotoxicity against human TZM-b1 cells assessed as reduction in cell viability by CCK8 assay2019Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5
Soluble-type small-molecule CD4 mimics as HIV entry inhibitors.
AID1574377Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1653638Binding affinity to substrate bound recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli assessed as Koff rate of cholesterol by stopped-flow spectrophotometric method2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID1731753Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into wild type RT measured after 1 hr by ELISA
AID298076Antiviral activity against HIV1 RT K103N-Y181C mutant in MT4 cells by MTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID1155805Cytotoxicity against human MT4 cells assessed as induction of cell death by MTT method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1446820Antiviral activity against HIV1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1457053Antiviral activity against HIV1 NL4-3 infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1693803Inhibition of recombinant HIV-1 BH10 reverse transcriptase using D38/[32P]25PGA as template-primer incubated for 5 mins in presence of DTT followed by dTTP addition and measured after 15 to 30 sec by nucleotide incorporation assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID1882476Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID279395Antiviral activity against HIV1 isolate with RT 101Q mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID342720Cytotoxicity against human MT4 cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
AID1352319Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1529939Inhibition of recombinant HIV-1 M:B reverse transcriptase RNA-dependent DNA polymerase activity expressed in Escherichia coli M15 using poly(A)/oligo(dT)16 as template/primer measured after 30 mins by picogreen dye based assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Novel natural non-nucleoside inhibitors of HIV-1 reverse transcriptase identified by shape- and structure-based virtual screening techniques.
AID767499Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID650691Inhibition of wild type HIV1 NL4-3 reverse transcriptase assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1773826Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID572174Antiviral activity against HIV-1 subtype CRF05_DF V022833 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1060626Fold resistance, ratio of EC50 for HIV1 RES056 expressing K103N/Y181C mutant infected in human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.
AID584080Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, E138K, F227F/L mutant infected in human SupT1 cells derived from 11 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to drug sen2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID508651Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID605180Antiviral activity against HIV1 R8 harboring reverse transcriptase infected in human MT4 cells assessed as inhibition of viral spread in presence of 50% normal human serum2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
AID1298243Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID279433Antiviral activity against HIV1 isolate with RT 179T mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID443682Antiviral activity against HIV with reverse transcriptase G190S mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID104410Antiviral activity of Protein Binding of compound was evaluated for PB shift virus expressed MT-2 by RNA2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1741399Inhibition of reverse transcriptase RES056 mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID391226Antiviral activity against HIV1 with reverse transcriptase Y181C mutant infected in human MT4 cells after 72 hrs in presence of 10% fetal bovine serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID1729150Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1261314Antiviral activity against Reo-1 virus infected in BHK-21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID198916Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution Y188L2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID1565094Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV RES056
AID347088Antiviral activity against HIV1 NL4-3 in HeLaP4 reporter cell assessed as virus replication by FluorAceTM beta-galactosidase reporter assay2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
AID523347Antiviral activity against HIV1 with RT connection domain N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1141960Antiviral activity against HIV1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID508791Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101Q mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID771795Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 23Synthesis and structure evaluation of new complex butylarylpiperazin-1-yl derivatives.
AID143399Compound was evaluated for its ability to inhibit the mutant K103N P225H NNRTI HIV-1 enzyme2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1574381Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV-1 NL4-32019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID257917Antiviral activity against HIV1 Y181C mutant using HeLa MAGI assay2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor.
AID586374Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase P145S mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID736039Inhibition of HIV1 reverse transcriptase p66/p51 G190A mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID1161104Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID1357796Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID663306Inhibition of HIV1 recombinant reverse transcriptase K103N mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID197783Compound was evaluated for the inhibition of HIV-1 Reverse transcriptase2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1561719Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against v
AID1264539Antiviral activity against HIV-1 X4 expressing reverse transcriptase K101P mutant infected in human CD4+ T cells for 3 days by FACS analysis2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID257916Antiviral activity against HIV1 K103N mutant using HeLa MAGI assay2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor.
AID106061Inhibitory activity against 103N strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID248263In vitro inhibitory concentration against HIV V179E mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID247724Inhibitory concentration against 103N mutant was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.
AID440084Antiviral activity against HIV1 HXB2 harboring 100I and K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1485975Inhibition of HIV-1 reverse transcriptase G190A mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID1163232Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID698301Antiviral activity against HIV1 containing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID302261Inhibition of HIV1 reverse transcriptase L100I mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID446254Fold resistance, ratio of IC50 for HIV reverse transcriptase with F227L mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID518736Selectivity ratio of IC50 for RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant to IC50 for RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID557050Antiviral activity against HIV1 clade H harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID279478Antiviral activity against HIV1 isolate with RT 106L, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID519022Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as decrease in the integrated viral DNA2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID583848Antiviral activity against HIV1 NL4-3 infected in human SupT1 cells derived from 11 viral passages assessed as inhibition of viral replication after 21 days relative to drug sensitive HIV1 NL4-32010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID588996Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, MRP22010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1729160Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID82464Antiviral activity against K103N/Y181C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID82275Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C strain2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID279409Antiviral activity against HIV1 isolate with RT 101P, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1485965Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID1483284Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase E138K mutant in human MT4 cells infected HIV1 3B2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID166688Antiviral activity of Protein Binding of compound was evaluated for RF virus expressed plasma; value ranges from 92-2202000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID141358Potency of second-generation NNRTIs against Mutant HIV-1 sV179D/L100I/Y181C2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1754645Antiviral activity against HIV1 harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1446872Inhibition of recombinant HIV-1 group M subtype B RT-RNase H activity expressed in Escherichia coli M15 using 18-nucleotide 3'-fluorescein-labeled RNA annealed to a complementary 18-nucleotide 5'-dabsyl-labeled DNA as substrate measured after 1 hr2017European journal of medicinal chemistry, Apr-21, Volume: 130Natural product-inspired esters and amides of ferulic and caffeic acid as dual inhibitors of HIV-1 reverse transcriptase.
AID685330Antiviral activity against HIV-1 RES056 harboring RT K103N/Y181C mutant gene infected human MT4 cells assessed as inhibition in viral syncytium formation by MTT assay2012Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.
AID279389Antiviral activity against HIV1 isolate with RT 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1200846Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID82475Antiviral activity against Y188C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1888705Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID1457074Neuroprotective activity against glutamate-induced excitotoxicity in C57BL/6 mouse BV2 cells assessed as increase in cell viability at 1000 nM preincubated for 30 mins followed by reincubation in conditioned culture media for 18 hrs in presence of glutama2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID508652Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P, K103N, V108I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1435515Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase Y188L mutant
AID1391087Antiviral activity against HIV1 harboring reverse transcriptase RES056 double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1157603Antiviral activity against HIV1 MP411 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID279497Antiviral activity against HIV1 isolate with RT K103N-K101Q-P225H mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID298060Antiviral activity against HIV1 RF in human CEM-SS cells by XTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID1446812Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID248882Inhibitory concentration against human immunodeficiency virus type 1 (with V108I/Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID347611Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 101E mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID519882Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID557023Antiviral activity against HIV1 clade A harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1161105Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID1574375Antiviral activity against HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID330488Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID457959Inhibition of HIV1 reverse transcriptase L100I mutant by RNA-dependent DNA polymerase activity assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID492279Cytotoxicity against human MT4 cells after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID302252Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT IRLL98 mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1141970Ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4.32014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID293181Selectivity index, ratio of CC50 for MT4 cells to IC50 for HIV1 LAI2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity.
AID1637401Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring Y181C mutant infected in human MT4 cells2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1275548Antiviral activity against HIV1 3B expressing reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID197931HIV-1 reverse transcriptase inhibitory activity against Asn103 mutant using (poly)rC600*(oligo)dGT as template primer.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID366521Resistance index, ratio of EC50 for drug-resistant HIV1 isolate with reverse transcriptase K103N mutation to EC50 for wild type HIV1 NL4-32008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID576035Cmax in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID82608The effect of protein binding on the antiviral activity versus wild type virus strain K103N was tested in the presence of human serum in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1357800Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase L100I mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1446818Antiviral activity against HIV1 harboring Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1822277Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1275545Antiviral activity against HIV1 3B expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1815399Inhibition of HIV1 reverse transcriptase Y181C mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID622055Ratio of Ki for HIV1 RT p66/p66 homodimer Y181C mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID247502Inhibitory activity against HIV-1 mutant strain 188L2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID1200845Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID635301Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID779529Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.
AID1212917Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID1077219Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells2014European journal of medicinal chemistry, Apr-09, Volume: 76Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID541135Selectivity ratio of EC50 for antiviral activity against PI-resistant HIV1 harboring RTG48V, V82A and L90M mutant gene to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID650549Resistance ratio of EC50 for HIV 1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1191403Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID509270Inhibition of HIV1 protease assessed as substrate cleavage by cell free assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Antiviral efficacy of the novel compound BIT225 against HIV-1 release from human macrophages.
AID508767Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1884491Antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID519960Selectivity ratio of EC50 for 0.01 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.01 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID246340Effective concentration against human immunodeficiency virus type 1 K103N and Y181C mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID248492In vitro inhibitory concentration against HIV K101E and K103N mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID293180Antiviral activity against HIV1 RT 103N/181C mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity.
AID1391083Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1335208Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/Y181C double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1185991Cytotoxicity against HEK293T cells at 10 uM after 48 hrs2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID440671Antiviral activity against NNRTI-resistant HIV1 A17 with reverse transcriptase K103N, Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.
AID82607The effect of protein binding on the antiviral activity versus wild type virus strain K103N was tested in the presence of both acid glycoprotein and human serum in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1743636Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1357794Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1761011Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1261340Antiviral activity against HSV12015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1653623Binding affinity to recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli in presence of substrate by UV-spectrophotometric method2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID562702Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation.
AID361921Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase P236L mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1391084Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1811046Selectivity index, ratio of CC50 for mock infected human MT4 cells to IC50 for HIV1 IIIB infected human MT4 cells2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID492276Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID717256Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID1884492Antiviral activity against drug-resistant HIV-1 Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1220361Total blood plasma concentration in human2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID586365Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase L101I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID717844Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation at 20 uM after 45 mins by spectrophotometric analysis relative to control2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2.
AID279506Antiviral activity against HIV1 isolate with RT V106I mutation in Hela-JC-53 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID650692Inhibition of HIV 1 reverse transcriptase Y188L mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID518739Selectivity ratio of IC50 for DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant to IC50 for DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1653624Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase and L-Glu by gas chromatography2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID1220362Total seminal plasma concentration in human2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID541172Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V and V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID279529Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 50% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID473116Cytotoxicity against human MT4 cells after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
AID443681Antiviral activity against HIV with reverse transcriptase G190A mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID1156484Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors.
AID663296Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1163231Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei rhodesiense STIB-900 assessed as reduction in parasite growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID246266Effective concentration against human immunodeficiency virus type 1 K103N mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1077220Cytotoxicity against human MT4 cells assessed as growth inhibition after 5 days by MTT assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID1520066Inhibition of recombinant wild type HIV-1 His-tagged reverse transcriptase p66/p51 expressed in Escherichia coli JM109 using poly(rA)/oligo(dT)16 as template/primer incubated for 40 mins by pico-green based spectrofluorometric analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID247526Inhibitory activity against wild type HIV-1 LAI cell line2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID735082Antiviral activity against wild type HIV by cell based assay2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and biological evaluation of phosphonate analogues of nevirapine.
AID1773454Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y188L mutant infected in human MT4 cells
AID279429Antiviral activity against HIV1 isolate with RT 103N, 106M mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID299028Antiviral activity against HIV1 with reverse transcriptase K103N mutation in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID1352316Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID371899Antiviral activity against HIV1 NL4-3 with L100I mutant in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by multiple round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID663298Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID541150Selectivity ratio of EC50 for antiviral activity against 3TC-resistant HIV1 selected after 4 passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1249719Antiviral activity against HIV1 expressing reverse transcriptase K103N mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID496629Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K20R, V35T, E36D, T39N, V60I, D123N, I135V, S162A, K173T, Q174K, D177E, T200A, Q207E, R211K mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1352168Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 48 to 96 hrs by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Quinoxaline derivatives as new inhibitors of coxsackievirus B5.
AID279432Antiviral activity against HIV1 isolate with RT 181I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID279510Antiviral activity against HIV1 isolate with RT T369I mutation in Hela-JC-53 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID496631Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I,Y181C/V35T, T39M, P119S, D123E, S162A, E169D, K173T, Q174K, D177E, T200A, Q207E, K219N, V245Q, E248D mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1141966Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1249720Antiviral activity against HIV1 expressing reverse transcriptase E138K mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID391225Antiviral activity against HIV1 with reverse transcriptase K103N mutant infected in human MT4 cells after 72 hrs in presence of 10% fetal bovine serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID348905Antiviral activity against drug-resistant HIV1 with reverse transcriptase K103N mutant infected in human MT4 cells assessed as virus-induced cell death by MTT method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies.
AID541161Selectivity ratio of EC50 for antiviral activity against HIV1 harboring T66I mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1171592Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase K103N-Y181C mutant to EC50 for wild type HIV1 NL4-32014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID366531Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase L100I mutant2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID430057Selectivity index, CC50 for human MT4 cells to EC50 for HIV1 3B2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
AID265467Antiviral activity against HIV1 3B in MT4 cell line2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID366520Antiviral activity against HIV1 isolates with reverse transcriptase K103N mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID282735Inhibition of HIV1 RT2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID576033Tmax in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID614141Antiviral activity against wild type Human immunodeficiency virus 1 3B bearing reverse transcriptase K103N and Y181C double mutation infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2011Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
AID1155811Fold resistance, ratio of EC50 for HIV-1 harboring NNTRI-resistant reverse transcriptase Y181C mutant infected in human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID248259In vitro inhibitory concentration against HIV K101E mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1483272Inhibition of HIV1 3B reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID104448Concentration required to protect the cell against HIV-1 strain IIIB viral cytopathogenicity by 50% in MT-4 cells2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
AID1558858Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1574379Resistance index, ratio of EC50 for HIV-1 IRLL98 harboring reverse transcriptase M41L, D67N, Y181C, M184V, R211K, and T215Y mutants to EC50 for wild type HIV-1 NL4-32019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID572181Antiviral activity against HIV-1 SM007 harboring NNTRI 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID166708Inhibitory activity against RNA2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz.
AID1456308Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID665551Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
AID1815383Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1653626Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) F405A mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID586359Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID222294Effect of human plasma protein binding on antiviral efficacy.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID650540Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID443679Antiviral activity against HIV with reverse transcriptase Y181C mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID231368Ratio of wild type IIIB to that of Y181C HIV-1 induced cytopathogenicity2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C varia
AID361904Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/L100I mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID736041Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1191671Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 pre-incubated with compound before enzyme addition using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
AID1446814Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID622047Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer K103N mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID583864Ratio of IC50 for HIV1 HXB2 reverse transcriptase K103N mutant to IC50 for wild type HIV1 reverse transcriptase2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1316343Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID571984Antiviral activity against HIV-1 subtype C V022816 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1304408Antiviral activity against HIV-1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID1750720Inhibition of HIV-1 p66/p51 reverse transcriptase Y188L mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID247725Inhibitory concentration against 181C mutant was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.
AID1609103Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by MTT assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID279469Antiviral activity against HIV1 isolate with RT 238N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID88371Antiviral activity against P236L mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1773836Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1743635Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1163233Antiviral activity against HIV1 infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hrs by2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID361911Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase L100I mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID347616Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 179D mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID104450Concentration required to protect the cell against HIV-2 strain ROD viral cytopathogenicity by 50% in MT-4 cells; NA denotes not active2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
AID279413Antiviral activity against HIV1 isolate with RT 106A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1750727Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase E138K mutant2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID279400Antiviral activity against HIV1 isolate with RT 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1186003Antiviral activity against HIV1 harboring reverse transcriptase K103N/G190A double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1204078Antiviral activity against HIV1 infected in human MT4 cells assessed as protection against viral-induced cytopathogenecity after 4 days by MTT method2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-((1,3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents.
AID1873200Inhibition of human ABCG2 expressed in dog MDCK-II-BCRP cells mediated pheophorbide A efflux preincubated with PhA followed by compound addition and measured after 60 mins by flow cytometry2022European journal of medicinal chemistry, Jul-05, Volume: 237Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
AID1155808Antiviral activity against HIV-1 harboring NNTRI-resistant reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID573981Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Human immunodeficiency virus 2 EHO2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID632801Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID1212881Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as enzyme-mediated 8-hydroxyefavirenz metabolite formation after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID586909Induction of MRP3 activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID96290In vitro antiviral activity against HIV-1 (L100I).2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1304407Inhibition of HIV-1 BH10 recombinant reverse transcriptase K103N mutant expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rA)/oligo(dT) as template primer2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID1316333Cytotoxicity against human mock-infected MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID269793Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269793Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269793Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID522369Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106A mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID663299Cytotoxicity against human MT4 cells after 5 days by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID246299Effective concentration of the compound to inhibit HIV-1 mutant L100I replication in HIV-infected MT-4 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1264543Cytotoxicity against human CD4-positive T cells2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1316330Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID576045Fraction unbound in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID404606Antiviral activity against HIV1 with reverse transcriptase Y181C mutation2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID523345Antiviral activity against HIV1 with RT connection domain T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID635345Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID1197829Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID1246228Cytotoxicity against human MT4 cells2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, cytotoxicity and antimicrobial activity of thiourea derivatives incorporating 3-(trifluoromethyl)phenyl moiety.
AID650547Resistance ratio of EC50 for HIV 1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID576044Drug concentration in PBMCs of healthy human at 400 mg, po ad for 14 days measured after 24 hrs post last dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID82459Antiviral activity against K103N strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID586377Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Q148K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID279457Antiviral activity against HIV1 isolate with RT 98G, 101E, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1811044Antiviral activity against HIV1 IIIB infected human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1231488Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID1822280Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID446257Fold resistance, ratio of IC50 for HIV reverse transcriptase with K101E mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID1171414Cytotoxicity against human MT2 cells assessed as reduction in cell viability by MTT assay2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID83549Potency evaluated against NNRTI-Resistant HIV-1 strain Leu100Ile2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID586388Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66K/L74M mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficienc2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1261311Cytotoxicity against african green monkey Vero 76 cells assessed as cell viability after 48 to 96 hrs by crystal violet staining method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID330485Antiviral activity against HIV1 3B infected in MT4 cells by MTT2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID541163Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92Q mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1197831Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID619640Antiviral activity against HIV-1 3B harboring RT K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID464764Antiviral activity against wild type HIV1 infected in human MT2 cells2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1163254Antileishmanial activity against Leishmania infantum MHOM/MA (BE)/67 infected in primary peritoneal mouse macrophages assessed as reduction in parasite burdun2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID279463Antiviral activity against HIV1 isolate with RT 108I, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID492280Selectivity index, CC50 for human MT4 cells to EC50 for wild type HIV1 3B2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID279401Antiviral activity against HIV1 isolate with RT 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID508795Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V090I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID464766Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT2 cells2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID492284Antiviral activity against HIV1 with reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID347087Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase Y181C mutant2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
AID1316345Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1520060Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1741395Inhibition of reverse transcriptase Y181C mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID279521Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells in the presence of 40% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID279467Antiviral activity against HIV1 isolate with RT 106A, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID302621Cytotoxicity against human MT2 cells by MTT assay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
From docking false-positive to active anti-HIV agent.
AID1197834Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID1773828Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1272058Half life in human administered as single dose2016European journal of medicinal chemistry, Jan-27, Volume: 108Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry.
AID366526Inhibition of RNA dependent DNA polymerase activity of wild-type HIV1 reverse transcriptase2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID738332Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for wild type HIV1 3B2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID440085Antiviral activity against HIV1 HXB2 harboring 101E and K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1171598Inhibition of wild type HIV1 reverse transcriptase Y181I mutant assessed as reduction in enzyme activity2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1754638Cytotoxicity against mock-infected human MT4 cells incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID279459Antiviral activity against HIV1 isolate with RT 101H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID246392Effective concentration against human immunodeficiency virus type 1 mutated at 100I+103N2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID556526Antiviral activity against Human immunodeficiency virus 1 clone Q9016 harboring K122E, Q145M, I202V, F214L mutation in reverse transcriptase by phenosense assay relative to wild type2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility.
AID779528Antiviral activity against HIV-1 RESO56 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.
AID267855Antiviral activity against HIV1 IRLL98 in MT4 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID508780Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138S mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID88379Antiviral activity against V108I mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID557024Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase L100I mutant relative to drug-sensitive HIV1 CNDO2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID571969Antiviral activity against HIV-1 subtype CRF02_AG V022826 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID576042Drug concentration in PBMCs of healthy human at 400 mg, po ad for 14 days measured after 5 hrs post last dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID508833Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93MW959 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1693801Antiviral activity against HIV2 ROD infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID1729158Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID571973Antiviral activity against HIV-1 subtype CRF01_AE V022822 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1410397Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.
AID508622Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG024 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID361923Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/G190A mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1705192Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1457064Inhibition of HIV1 reverse transcriptase p66 K103N mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation counting 2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID279494Antiviral activity against HIV1 isolate with RT G190A mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1731746Inhibition of reverse transcriptase L100I mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID571968Antiviral activity against HIV-1 subtype CRF02_AG V022825 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1743630Antiviral activity against HIV1 harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1520061Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B harbouring NNRTI K103N mutant infected in human MT4 cells2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1141972Ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4.32014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID441309Fold resistance, ratio of IC50 for HIV reverse transcriptase with K103N mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
AID441315Fold resistance, ratio of IC50 for HIV reverse transcriptase with P236L mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
AID508829Antiviral activity against Human immunodeficiency virus 1 subtype B isolate JR-CSF infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID541168Selectivity ratio of EC50 for antiviral activity against HIV1 harboring V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID443701Antiviral activity against HIV with reverse transcriptase K103N/Y181C double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID519888Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1126510Selectivity index, ratio of CC50 for mock-infected human MT4 cells to IC50 for HIV1 3B infected in human MT4 cells2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1069708Cytotoxicity against human MT4 cells assessed as cell viability2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID571987Antiviral activity against HIV-1 subtype C V022831 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID448403Fold resistance, ratio of IC50 for HIV reverse transcriptase with P236L mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 3: optimisation of physicochemical properties.
AID457961Inhibition of HIV1 reverse transcriptase K103N mutant by RNA-dependent DNA polymerase activity assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID573987Antiviral activity against Protease inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID508633Cytotoxicity against human MT4 cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID519870Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1390710Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID1773457Resistance factor, ratio of EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID282740Inhibition of HIV1 RT Y188L mutant2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID572186Antiviral activity against HIV-1 SM034 harboring NNTRI 188L mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID443689Antiviral activity against HIV with reverse transcriptase K101E/Y181C/G190A mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID105324Inhibition of Efavirenz resistant HIV-1 (K103N-Y181C) induced cytopathicity in MT-4 cells.2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID519856Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID541175Selectivity ratio of EC50 for antiviral activity against HIV1 harboring G140S and Q148H mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID440083Antiviral activity against HIV1 HXB2 harboring 227C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID576034Tmax in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID1155815Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase Y181I mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:12014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID517497Antiviral activity against HIV1 harboring reverse transcriptase V106A mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID490370Antiviral activity against HIV1 expressing reverse transcriptase K103N/L100I double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID523478Antiviral activity against HIV1 with RT connection domain G190A/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1773837Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1171584Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1292011Cytotoxicity against mock infected human MT4 cells after 4 days by MTT assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1261317Antiviral activity against Human poliovirus 1 Sabin infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity by plaque reduction assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1316329Inhibition of recombinant wild type HIV1 reverse transcriptase using DIG-dUTP/biotin-dUTP/dTTP assessed as suppression of biotin-dUTP incorporation after 1 hr by ELISA2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID519883Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1884220Antiviral activity against HIV-1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID279476Antiviral activity against HIV1 isolate with RT 101N, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID82469Antiviral activity against V106A/Y181C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1126509Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1574373Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID263515Antiviral activity against HIV1 I135T mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID508775Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1457072Effect on fizz mRNA levels in C57BL/6 mouse BV2 cells at 1000 nM after 24 hrs by RT-PCR assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID584029Inhibition of HIV1 histidine-tagged reverse transcriptase E233V mutant activity by primer extension assay2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1191669Cytotoxicity against human MT4 cells assessed as reduction in cell viability2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
AID573988Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 12008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID738335Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID571970Antiviral activity against HIV-1 subtype CRF02_AG V022830 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID443692Antiviral activity against HIV with reverse transcriptase MDRC4 mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID726437Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase K103N and Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID519865Antiviral activity against HIV1 subtype B-NL4-3 infected in 3 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID541153Selectivity ratio of EC50 for antiviral activity against EFV-resistant HIV1 selected after 7 passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541151Selectivity ratio of EC50 for antiviral activity against 3TC-resistant HIV1 selected after 8 passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1552563Antiviral activity against HIV1 V13-03413B infected in human LC5 cells expressing DsRed1 reporter gene assessed as inhibition of viral infection measured after 48 hrs post infection by reporter gene based luminescence assay2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID571980Antiviral activity against HIV-1 subtype B V022812 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID519892Selectivity ratio of EC50 for 0.05 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.05 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID750863Antiviral activity against HIV1 infected in human 293T cells assessed as inhibition of viral replication incubated for 15 mins prior to infection measured after 48 hrs by luciferase reporter gene assay2013Journal of natural products, Jun-28, Volume: 76, Issue:6
Diterpenoids with diverse skeletons from the roots of Euphorbia micractina.
AID1171596Inhibition of wild type HIV1 reverse transcriptase L100I mutant assessed as reduction in enzyme activity2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1069124Antiviral activity against HIV harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum2014Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID392513Antiviral activity against HIV12009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks.
AID371904Antiviral activity against HIV1 NL4-3 with K103N/L100I double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID368555Inhibition of wild type HIV1 reverse transcriptase-mediated RNA-dependent DNA polymerase activity assessed as [3H]dTTP incorporation by cell free-based scintillation counting2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID246349Effective concentration against human immunodeficiency virus type 1 mutated at 103N2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1212916Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as intrinsic clearance for enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in absence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID663311Resistance ratio of ID50 for HIV1 reverse transcriptase K103N mutant to ID50 HIV1 wild type reverse transcriptase2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID735080Ratio of EC50 for HIV harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and biological evaluation of phosphonate analogues of nevirapine.
AID1155804Antiviral activity against wild type HIV-1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1220376Drug metabolism in human liver microsomes assessed as formation of metabolites with retention time of 1.92 mins at 20 uM by UPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
AID573257Antiviral activity against HIV1 infected in children assessed as decrease in viral burden at 14.4 mg/kg once daily measured after 3 months2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID279321Inhibition of reverse transcriptase activity in HIV1 infected HeLa-MAGI cells at 37 deg C after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID541130Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RTM184V mutant gene to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID151310percentage in tissue culture medium2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID586472Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138K/Q148H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID253495Dose required to inhibit HIV-1 reverse transcriptase activity ( L100I mutant) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID576030Volume of distribution in healthy human plasma at 400 mg, po measured on day 1 post dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID248841Inhibitory concentration against human immunodeficiency virus type 1 (with G190A resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID1761009Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID279500Antiviral activity against HIV1 isolate with RT V106I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID81628Antiviral activity was evaluated against wild-type HIV-1 virus2001Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9
Synthesis and evaluation of efavirenz (Sustiva) analogues as HIV-1 reverse transcriptase inhibitors: replacement of the cyclopropylacetylene side chain.
AID328841Inhibition of human MRP1 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID572183Antiviral activity against HIV-1 SM024 harboring NNTRI 190A mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1443663Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID508786Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V108I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID572187Antiviral activity against HIV-1 SM051 harboring NNTRI 100I and 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1435513Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase K103N mutant
AID1152373Cytotoxicity against human MT4 cells by MTT assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1171583Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID573986Antiviral activity against non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1435514Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase Y181C mutant
AID523486Antiviral activity against HIV1 with RT connection domain L100I/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID263514Antiviral activity against HIV1 V106A mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID1443669Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID366522Antiviral activity against HIV1 isolates with reverse transcriptase Y181C mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID586480Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Q148R/N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID105707Anti-HIV-1 activity against Y188L strain was determined in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1653627Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) K358A mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID1815388Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID572184Antiviral activity against HIV-1 SM026 harboring NNTRI 103N and 181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1884540Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1077222Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID1572523Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID557046Antiviral activity against HIV1 clade C harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1773829Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID586484Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase V72I/F121Y/T125K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunode2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID605183Antiviral activity against HIV1 R8 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as concentration required to inhibit >95% viral spread in presence of 10% FBS2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
AID632797Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT2 cells assessed as inhibition of viral infection2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID246203Concentration required to achieve 50% protection of infected MT-4 cells from Y181C-HIV-1 strain2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID446238Antiviral activity against HIV RF infected in human SupT1 cells2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID1141967Antiviral activity against HIV1 harboring reverse transcriptase L1001 mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1455949Antiviral activity against VSV pseudotyped HIV1 infected in SupT1 cells after 48 hrs by luciferase reporter gene assay2017Journal of natural products, 02-24, Volume: 80, Issue:2
Griseofulvin Derivative and Indole Alkaloids from Penicillium griseofulvum CPCC 400528.
AID1754640Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID279392Antiviral activity against HIV1 isolate with RT 100I, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID576046Fraction unbound in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID446408Fold resistance, ratio of IC50 for HIV reverse transcriptase with V108I mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID1736358Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase L100I/K103N double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr
AID269688Antiviral activity against HIV1 NNTRI resistant K103N mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269688Antiviral activity against HIV1 NNTRI resistant K103N mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269688Antiviral activity against HIV1 NNTRI resistant K103N mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID518737Inhibition of DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by gel-based primer extension assay2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID247726Inhibitory concentration against 188L mutant was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.
AID473114Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
AID267856Antiviral activity against HIV1 K103N mutant in MT4 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID735083Inhibition of HIV reverse transcriptase2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and biological evaluation of phosphonate analogues of nevirapine.
AID492281Antiviral activity against wild type HIV1 LAI infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID519893Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.005 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID82458Antiviral activity against K101E strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1773460Resistance factor, ratio of EC50 for HIV1 harboring Y188L mutant mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID465419Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID269796Antiviral activity against HIV1 F227L mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269796Antiviral activity against HIV1 F227L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269796Antiviral activity against HIV1 F227L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1705183Antiviral activity against HIV-1 NL4-3 infected in human MT-4 cells assessed as virus induced cytopathic effect by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID573256Apparent oral clearance in HIV-1 infected children at 14.4 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID508765Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M236L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID541160Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 9 passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID517494Selectivity ratio of IC50 for wild type HIV1 in presence of 40% human serum to IC50 for wild type HIV1 in presence of 10% FBS2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1736347Inhibition of HIV-1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT) as template/primer incubated for 1 hr followed by transferring into streptavidin plate for 1 hr by absorba
AID360704Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA/DNAM duplex primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID517496Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1520057Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1443668Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID368560Antiviral activity against HIV1 reverse transcriptase Y181C mutant infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID1705185Selectivity ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 NL4-3 infected in human MT4 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1596756Inhibition of recombinant wild-type HIV1 3B reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(rA)/oligo(dT)16 as template primer incubated for 1 hr followed by the addition of (DIG)-dUTP and biotin-labeled dNTPs by ELISA2019European journal of medicinal chemistry, Aug-15, Volume: 176Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID263519Antiviral activity against HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID1446873Inhibition of wild-type HIV1 RT associated RNA dependent DNA polymerase activity using poly(A) template/oligo(dT) primer after 30 mins by picogreen staining based method2017European journal of medicinal chemistry, Apr-21, Volume: 130Natural product-inspired esters and amides of ferulic and caffeic acid as dual inhibitors of HIV-1 reverse transcriptase.
AID523355Antiviral activity against HIV1 with RT connection domain Y181C/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID361925Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/Y181C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1503175Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells at 100 uM after 48 hrs by luciferase reporter gene assay relative to control2017Journal of natural products, 10-27, Volume: 80, Issue:10
Metabolites from the Plant Endophytic Fungus Aspergillus sp. CPCC 400735 and Their Anti-HIV Activities.
AID586380Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase S153F mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1191400Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1410481Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID584239Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase Y181C, V179V/D mutant derived from 17 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type 2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1815386Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID248012In vitro inhibitory concentration against HIV LAI cell line2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1761007Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability measured after 1 day by CytoTox-Glo assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID232750Selectivity index is the ratio between CC50 for MT-4 cells and IC50 against HIV-1 infection2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
AID293174Antiviral activity against HIV1 LAI assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity.
AID557042Antiviral activity against HIV1 isolate R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID527375Antiviral activity against wild type HIV1 NL4-3 infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID222921percentage in human serum; value ranges from -0.2-0.52000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID94447Inhibitory concentration against wild-type virus K103N and HIV-1 RT mutant in a whole cell antiviral assay2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.
AID313194Antiviral activity against HIV1 K103N/Y181C mutant2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and antiviral activity of new dimeric inhibitors against HIV-1.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1261310Cytotoxicity against BHK cells assessed as cell viability after 48 to 96 hrs by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1552554Antiviral activity against HIV1 HXB2 pseudovirus infected in human TZM-bl cells assessed as inhibition of viral infection incubated for 20 mins prior to infection and measured after 48 hrs by bright Glo-luciferase reporter gene assay2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID431622Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID622057Ratio of Ki for HIV1 RT p66/p66 homodimer G190A mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID440078Antiviral activity against HIV1 HXB2 harboring 106A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1407647Therapeutic index, ratio of CC50 for human CEM-GFP cells to IC50 for HIV-1 NL4-3 infected in human CEM-GFP cells2018European journal of medicinal chemistry, Sep-05, Volume: 157Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors.
AID663309Inhibition of HIV1 recombinant reverse transcriptase V106A mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1335218Antiviral activity against wild-type HIV-1 NL4-3 harboring vesicular stomatitis virus glycoprotein infected in HEK293T cells pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID279445Antiviral activity against HIV1 isolate with RT 101E, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1185997Antiviral activity against HIV1 harboring reverse transcriptase L1001/K103N double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1376906Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells after 48 hrs by firefly luciferase reporter gene assay2017Journal of natural products, 06-23, Volume: 80, Issue:6
Stachybotrysins A-G, Phenylspirodrimane Derivatives from the Fungus Stachybotrys chartarum.
AID1335206Ratio of IC50 for HIV-1 NL4-3 harboring RT-Y181C mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1435506Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID508638Antiviral activity against Human immunodeficiency virus 1 subtype F1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID441303Inhibition of wild type HIV reverse transcriptase in presence of poly(rA) 300 template, (dT) 16 primer2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
AID1888702Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID279512Antiviral activity against HIV1 isolate with RT V106I, Y181C, F227L mutation in Hela-JC-53 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID94443Potency of second-generation NNRTIs against Mutant HIV-1 K103N2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID279420Antiviral activity against HIV1 isolate with RT 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1249718Antiviral activity against HIV1 expressing reverse transcriptase L100I mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID519885Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID622054Ratio of Ki for HIV1 RT p66/p66 homodimer K103N mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1596753Antiviral activity against HIV-1 3B harboring reverse transcriptase RES056 mutant infected in MT4 cells measured after 5 days by MTT assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID586471Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E138A/Q148R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1483278Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1410484Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B reverse transcriptase infected in human MT4 cells2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID1574389Resistance index, ratio of ID50 for recombinant HIV-1 His-tagged reverse transcriptase p66/p51 Y181I mutant to ID50 for recombinant wild type HIV-1 reverse transcriptase His-tagged p66/p512019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1741400Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based fluorescence assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID490371Antiviral activity against HIV1 expressing reverse transcriptase G190A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID508627Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR019 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1741393Inhibition of reverse transcriptase L100I mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1761017Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID779525Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.
AID83551Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr181Cys2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID1535526Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
AID106057Inhibitory activity against 103N strain and 181C strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID347613Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 103N mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID430056Cytotoxicity against human MT4 cells after 5 days2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
AID198399Tested for inhibitory concentration against HIV-1 non-nucleoside reverse transcriptase2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.
AID1822276Antiviral activity against HIV-1 harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1705191Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID266345Inhibition of wild type HIV1 reverse transcriptase in 293T cells2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.
AID1443662Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1171590Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-32014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID347609Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 190S mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID650544Antiviral activity against HIV 1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1761016Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1407642Inhibition of recombinant HIV-1 reverse transcriptase RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)16 as template/primer preincubated for 5 to 10 mins followed by template/primer addition and measured after 16 hrs by colorimetric assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors.
AID586476Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G140S/Q148H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1373160Inhibition of reverse transcriptase Y188L mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID584241Ratio of EC50 for wild type HIV1 NL4-3 to EC50 for HIV1 NL4-3 harboring reverse transcriptase V179V/D mutant2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID299031Antiviral activity against HIV1 with reverse transcriptase Y188H mutation in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID1157585Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID279484Antiviral activity against HIV1 isolate with RT K103N-P225H mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID757623Cytotoxicity against human MT4 cells after 5 days by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1186327Cytotoxicity against mock-infected human MT4 cells after 96 hrs by MTT assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Antiviral activity of benzimidazole derivatives. III. Novel anti-CVB-5, anti-RSV and anti-Sb-1 agents.
AID1060630Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.
AID232055Selectivity index (Ratio of CC50/EC50).2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID198912Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution L10012001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID586902Activity at MRP22011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID105905Effective dose required to achieve protection of MT-4 cells from Y181C HIV-1 induced cytopathogenicity2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C varia
AID347621Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 181C mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1171580Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1155818Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase Y181I mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID572185Antiviral activity against HIV-1 SM030 harboring NNTRI 100I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1503177Cytotoxicity against human SupT1 cells assessed as decrease in cell viability after 48 hrs by CCK-8 assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
Metabolites from the Plant Endophytic Fungus Aspergillus sp. CPCC 400735 and Their Anti-HIV Activities.
AID267645Antiviral activity against wild type HIV1 virus2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID293555Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1741394Inhibition of reverse transcriptase K103N mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID293562Antiviral activity against HIV1 LAI with RT F227C mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID248881Inhibitory concentration against human immunodeficiency virus type 1 (with V106A/Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID685333Cytotoxicity against mock-infected human MT4 cells by MTT assay2012Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.
AID1059142Inhibition of recombinant HIV1 reverse transcriptase using poly rA:dT as template/primer after 1 hr by ELISA2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1705195Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV-1 p66/p51 reverse transcriptase K103N mutant assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintillation cou2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1637398Antiviral activity against human HIV-1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1057037Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in MT4 cells2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID226250Y181C/WTIIIB ratio of the compound2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1574384Inhibition of recombinant wild type HIV-1 His-tagged reverse transcriptase p66/p51 expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysis2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID246350Effective concentration against human immunodeficiency virus type 1 mutated at 181C2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID94313Antiviral activity toward K103N mutant HIV-1 virus as protein binding adjusted (PB adj).2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID313191Antiviral activity against HIV1 HTLV-3B2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and antiviral activity of new dimeric inhibitors against HIV-1.
AID576050Effect on P-gp activity in PBMCs isolated from healthy human receiving compound dose at 400 mg, po qd for 14 days by rhodamine -123 efflux assay2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID1773444Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV1 RES056 infected in MT4 cells
AID527563Antiviral activity against HIV1 NL4-3 containing reverse transcriptase Y181C mutation infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1335207Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1754646Antiviral activity against HIV1 harboring RT F227L/V106A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID440075Antiviral activity against HIV1 HXB2 harboring Y188L mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1705187Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID586470Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase F121Y/T125K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID541129Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RTK65R mutant gene to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1292009Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as cell viability after 4 days by MTT assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1880376Antiviral activity against HIV-1 IIIB harboring reverse transcriptase L1001 mutant infected in human MT4 cells by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID1304399Inhibition of HIV-1 BH10 recombinant reverse transcriptase expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rC)/oligo(dG) as template primer2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID779526Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.
AID622056Ratio of Ki for HIV1 RT p66/p66 homodimer Y188L mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1880377Antiviral activity against HIV-1 IIIB harboring reverse transcriptase K103N mutant infected in human MT4 cells by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID371907Antiviral activity against HIV1 NL4-3 with Y181L mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID448400Fold resistance, ratio of IC50 for HIV reverse transcriptase with V106A mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 3: optimisation of physicochemical properties.
AID1261341Antiviral activity against VSV2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1352320Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID371908Antiviral activity against HIV1 NL4-3 with V108I mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID518738Inhibition of DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by gel-based primer extension assay2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1572521Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells
AID1248224Selectivity index, ratio of CC50 for uninfected human MT4 cells to EC50 for wild type HIV 1 3B infected in human MT4 cells2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1298248Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1264542Aqueous solubility of compound2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1304404Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human CEM-SS cells to EC50 for antiviral activity against HIV-1 RF2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID248878Inhibitory concentration against human immunodeficiency virus type 1 (with K103N/G190A resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID1155817Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase K103N mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID717260Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID1410486Inhibition of wild-type HIV1 reverse transcriptase infected in human MT4 cells assessed as reduction in biotin-dUTP incorporation2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID605175Antiviral activity against HIV1 R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral spread in presence of 10% fetal bovine serum2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
AID642208Cytotoxicity against human MT4 cells after 96 hrs by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Quinoline tricyclic derivatives. Design, synthesis and evaluation of the antiviral activity of three new classes of RNA-dependent RNA polymerase inhibitors.
AID1186004Antiviral activity against HIV1 harboring reverse transcriptase K103N/V108I double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID361916Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V108I mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1583019Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1653631Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) K358L mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID246352Effective concentration against human immunodeficiency virus type 1 mutated at 227C2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID457960Inhibition of HIV1 reverse transcriptase Y181I mutant by RNA-dependent DNA polymerase activity assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID248493In vitro inhibitory concentration value against HIV K103N and Y181C mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID632800Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID518735Inhibition of RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by filter-based filtration assay2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1357799Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID496634Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I,A98G/V35T, E36D, T39K, S48A, I50V, V60I, S68G, I135V, S162A, K173T, Q174K, D177E, G196E, T200A, E203G, Q207D, R211K, Q222P mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1171581Antiviral activity against HIV1 3B infected in human CEM cells assessed as protection against virus-induced cytopathicity by giant cell formation assay2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID293179Antiviral activity against HIV1 RT 100I/103N mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity.
AID198230Inhibitory activity against wild-type HIV-1 reverse transcriptase2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.
AID541155Selectivity ratio of EC50 for antiviral activity against APV-resistant HIV1 selected after 4 passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID440664Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.
AID492283Antiviral activity against HIV1 with reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID347620Antiviral activity against NNRTI-resistant HIV HXB2 with reverse transcriptase 188H mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID446258Fold resistance, ratio of IC50 for HIV reverse transcriptase with P236L mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID88384Antiviral activity against wild-type HIV-1 in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1357783Antiviral activity against wild-type HIV-1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1161103Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID584238Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase K103N, V108V/I mutant derived from 10 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type 2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID279416Antiviral activity against HIV1 isolate with RT 179A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1552578Selectivity ratio of IC50 for HIV1 V13-03413B infected in human LC5 cells to IC50 for HIV1 LAI infected in human LC5 cells2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID441312Fold resistance, ratio of IC50 for HIV reverse transcriptase with V106A mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
AID279501Antiviral activity against HIV1 isolate with RT Y181C mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1077218Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2014European journal of medicinal chemistry, Apr-09, Volume: 76Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID1503176Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells after 48 hrs by luciferase reporter gene assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
Metabolites from the Plant Endophytic Fungus Aspergillus sp. CPCC 400735 and Their Anti-HIV Activities.
AID248844Inhibitory concentration against human immunodeficiency virus type 1 (with V108I resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID583849Inhibition of HIV1 reverse transcriptase activity by primer extension assay2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1231489Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID1435518Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase mutant
AID572188Antiviral activity against HIV-1 SM052 harboring NNTRI 101E and 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1773440Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID302265Inhibition of HIV1 reverse transcriptase Y188L mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1754643Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID522372Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106A/V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1731750Inhibition of reverse transcriptase E138K mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1191670Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
AID586908Induction of MRP1 activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID519887Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1335202Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/G190A double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1326647Inhibition of reverse transcriptase Y181C mutant in HIV-1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by cell titer glo based luciferase reporter gene assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.
AID1275543Antiviral activity against HIV1 RES056 expressing reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1888701Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID82468Antiviral activity against V106A strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1391088Inhibition of HIV1 reverse transcriptase K103N/Y181C double mutant using poly (A)/oligo (dT)15 as template/primer assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID557067Plasma protein binding in HIV1 infected patient2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1594858Half life in human serum at 600 mg, qd2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.
AID248260In vitro inhibitory concentration against HIV K103N mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID736439Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID397178Ratio of EC50 for HIV1 3B expressing reverse transcriptase Y181C mutant to EC50 for HIV1 3B2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1572527Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID665550Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
AID586468Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T97A/N155H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficien2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID361908Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID105906Effective dose required to achieve protection of MT-4 cells from wild type IIIB HIV-1 induced cytopathogenicity2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C varia
AID541173Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E138K and Q148K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID583842Ratio of IC50 for HIV1 reverse transcriptase Y181I, Y188L mutant to IC50 for wild type HIV1 reverse transcriptase2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID496628Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K20R, V35T, E36A, T39D, V60I, I135V, T139I, K173A, Q174K, T200E, Q207A, R211K, F214L mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID508828Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92RW020 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1520058Antiviral activity against HIV1 3B harbouring NNRTI K103N mutant infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1357788Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID371910Antiviral activity against HIV1 NL4-3 with K103N mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID779527Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.
AID523352Antiviral activity against HIV1 with RT connection domain K103N/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1763899Antiviral activity against HIV-1 IIIB harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1185994Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID246786Concentration required to reduce the amount of p24 by 90% in C8166 cells infected with an efavirenz-resistant strain EFVR2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID1572524Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID492285Antiviral activity against HIV1 with reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID299024Cytotoxicity against MT4 cells assessed as reduction of cell viability2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID199102Inhibitory concentration against wild-type reverse transcriptase of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1636927Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against viral infection by MTT method2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Computer-aided discovery of anti-HIV agents.
AID1446817Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID298088Inhibition of HIV1 RT K103N mutant2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID1565100Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID279514Antiviral activity against HIV1 isolate with RT V106I, D123G, Y181C, F227L mutation in Hela-JC-53 cells2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID586906Inhibition of BCRP activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID1212886Drug metabolism in microsomes expressing CYP2B6.6 (unknown origin) assessed as intrinsic clearance for enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID1884541Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1882469Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID279492Antiviral activity against HIV1 isolate with RT K103N-F227L mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID766432Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.
AID576043Drug concentration in PBMCs of healthy human at 400 mg, po measured after 24 hrs on day 1 post dose by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID443687Antiviral activity against HIV with reverse transcriptase K103N/P225H double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443693Antiviral activity against HIV with reverse transcriptase CNDO mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID698305Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1373156Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID663310Inhibition of HIV1 recombinant reverse transcriptase Y188L mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID267863Inhibition of HIV1 reverse transcriptase Y181I mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID416431Antiviral activity against HIV1 bearing VSV envelope infected in human HeLa CD4 cells coexpressing LTR/beta-Gal gene assessed as reduction in virus-induced beta-galactosidase reporter gene activity after 72 hrs by single-cycle infection assay2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Identification and characterization of UK-201844, a novel inhibitor that interferes with human immunodeficiency virus type 1 gp160 processing.
AID573252AUC (0 to t) in HIV-1 infected children at 10 to 15 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID360705Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID269795Antiviral activity against HIV1 E138K mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269795Antiviral activity against HIV1 E138K mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269795Antiviral activity against HIV1 E138K mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID623217Cytotoxicity against human MT4 cells after 4 days by MTT assay2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1348215Antiviral activity against HIV1 NL4-3 infected in human MT2 cells measured after 72 hrs post infection by fluorAce beta-galactosidase reporter gene assay2017Journal of natural products, 12-22, Volume: 80, Issue:12
Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities.
AID1198748Inhibition of HIV1 reverse transcriptase-associated DNA polymerase-independent RNase H activity after 1 hr2015European journal of medicinal chemistry, Mar-26, Volume: 93(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.
AID508657Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF02 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1357786Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID573255Apparent oral clearance in HIV-1 infected children at 13.3 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID738331Cytotoxicity against mock-infected human MT4 cells assessed as cell viability after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID523480Antiviral activity against HIV1 with RT connection domain G190S/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID416756Antiviral activity against HIV1 with reverse transcriptase K103N mutation in human CEM cells assessed as protection against virus-induced cytopathicity2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID476470Antiviral activity against HIV1 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral replication by MTT assay2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1811036Anti-viral activity against HIV1 harboring RT Y181C mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID246348Effective concentration against human immunodeficiency virus type 1 mutated at 100I2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID267858Antiviral activity against HIV1 Y188L mutant in MT4 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID279406Antiviral activity against HIV1 isolate with RT 103N, 238T mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1275544Antiviral activity against HIV1 3B expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID572175Antiviral activity against HIV-1 subtype F V029522 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID96293Potency of second-generation NNRTIs against Mutant HIV-1 sL100I2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID248843Inhibitory concentration against human immunodeficiency virus type 1 (with V106A resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID523351Antiviral activity against HIV1 with RT connection domain K103N/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID605182Antiviral activity against HIV1 R8 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral spread in presence of 10% fetal bovine serum2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
AID1157597Antiviral activity against HIV1 MP582 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID279396Antiviral activity against HIV1 isolate with RT 103N, 225H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1152372Antiviral activity against HIV1 RES056 harboring RT K103N,Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1882470Antiviral activity against HIV-1 harboring K103N/Y181C mutant infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1352169Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 3 to 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Quinoxaline derivatives as new inhibitors of coxsackievirus B5.
AID1743628Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1185990Antiviral activity against wild type HIV1 infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID573476Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5512 by cell based assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID293177Antiviral activity against HIV1 RT 188L mutant assessed as inhibition of viral-induced cytopathicity in MT4 cells by MTT method2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity.
AID361907Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase Y181C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1286669Antiviral activity against HIV1 BH10 harboring wild type reverse transcriptase infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID279415Antiviral activity against HIV1 isolate with RT 101E, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1767120Antiviral activity against HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of early stage viral production at 10 uM measured after 48 hrs by luciferase assay relative to control2021European journal of medicinal chemistry, Aug-05, Volume: 220Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.
AID586364Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E92V mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID619641Ratio of EC50 for HIV-1 3B harboring RT K103N mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID1483274Inhibition of HIV1 3B reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID246556Concentration required for 50% protection of infected MT-4 cells from wtIIIB-HIV-1-induced cytopathogenicity was determined by the MTT method2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID586907Induction of ABCB1 activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID508778Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1357791Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID517499Antiviral activity against HIV1 harboring reverse transcriptase K103N/L100I double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID313192Antiviral activity against efavirenz-resistant HIV12008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and antiviral activity of new dimeric inhibitors against HIV-1.
AID519966Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells by phenosense assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID726439Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID370729Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 V179D mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID443697Antiviral activity against HIV with reverse transcriptase Y188L mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID1705196Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV-1 p66/p51 reverse transcriptase Y188L mutant assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintillation cou2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1326645Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B reverse transcriptase infected in human MT4 cells2016European journal of medicinal chemistry, Oct-21, Volume: 122Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.
AID1822274Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID592539Selectivity index, CC50 for human CEM cells to IC50 for HIV1 3B2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
AID1888690Antiviral activity against HIV1 3B infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1637400Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring K103N mutant infected in human MT4 cells2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID649490Inhibition of ribonuclease H activity of Human immunodeficiency virus 1 reverse transcriptase Tyr181Cys mutant2012European journal of medicinal chemistry, Apr, Volume: 50Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach.
AID1705184Cytotoxicity against human MT-4 cells assessed as reduction in cell viability by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID269805Antiviral activity against HIV1 Y181S mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269805Antiviral activity against HIV1 Y181S mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269805Antiviral activity against HIV1 Y181S mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1435507Antiviral activity against HIV1 expressing reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID648420Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1249724Inhibition of HIV1 reverse transcriptase p66/p51 assessed as inhibition of biotin-dUTP incorporation using poly (rA)/oligo(dT)16 as template/primer incubated for 40 mins2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID522371Antiviral activity against recombinant HIV1 harboring reverse transcriptase V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1212901Drug metabolism in human liver microsomes harboring CYP2B6*6/*6 genotype assessed as intrinsic clearance for CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID1155806Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID257163Inhibition of wild type HIV1 reverse transcriptase by [3H]dTTP poly(rA)/oligo(dT) incorporation2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID557051Antiviral activity against PI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID583846Ratio of IC50 for HIV1 reverse transcriptase V106A, F227L mutant to IC50 for wild type HIV1 reverse transcriptase2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1060632Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as inhibition of viral cytopathicity after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.
AID1157583Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1275554Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV2 ROD infected in human MT4 cells2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID279483Antiviral activity against HIV1 isolate with RT K103N-Y181C mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID650689Inhibition of HIV 1 reverse transcriptase K103N mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID508646Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, Y188L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1691439Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 RES056 infected in human MT4 cells2020European journal of medicinal chemistry, May-01, Volume: 193In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID279495Antiviral activity against HIV1 isolate with RT K103N-Y188L mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID663303Resistance ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-32012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID586911Induction of SLCO1B1 activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID440672Antiviral activity against HIV1 EFV with reverse transcriptase K103R, V179D, P225H mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.
AID572172Antiviral activity against HIV-1 subtype CRF05_DF V022823 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID584240Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase Y181C, V108V/I, V179V/D mutant derived from 17 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to w2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1373154Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID1882473Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytopathicity by MTT assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID446252Fold resistance, ratio of IC50 for HIV reverse transcriptase with K103N mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID1264538Antiviral activity against HIV-1 X4 expressing wild-type reverse transcriptase infected in human CD4+ T cells for 3 days by FACS analysis2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1457068Antineuroinflammatory activity in C57BL/6 mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production at 1 to 10 uM after 24 hrs by Griess assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID443696Antiviral activity against HIV with reverse transcriptase Y181C mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391223Inhibition of HIV1 RT polymerase Y181C mutant by SPA2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID82473Antiviral activity against V108I/Y181C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1249721Antiviral activity against HIV1 expressing reverse transcriptase Y181C mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID605177Inhibition of HIV1 reverse transcriptase K103N mutant by SPA assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
AID523348Antiviral activity against HIV1 with RT connection domain T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID448404Fold resistance, ratio of IC50 for HIV reverse transcriptase with V108I mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 3: optimisation of physicochemical properties.
AID508789Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103S mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID586368Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T124A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID366525Resistance index, ratio of EC50 for drug-resistant HIV1 isolate with reverse transcriptase Y188L mutation to EC50 for wild type HIV1 NL4-32008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1457059Ratio of EC50 for HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID685331Antiviral activity against HIV-1 3B infected human MT4 cells assessed as inhibition in viral syncytium formation by MTT assay2012Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.
AID1185999Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay relative HIV12014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID267654Selectivity for wild type HIV1 virus over HIV1 K103N/L100I mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID446253Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y181C mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
AID586375Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Q146R mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1636928Cytotoxicity against human MT2 cells assessed as growth inhibition by MTT method2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Computer-aided discovery of anti-HIV agents.
AID586904Activity at BCRP2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID1888689Antiviral activity against HIV1 with RT F227L + V106A mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1693800Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID1304402Cytotoxicity against mock-infected human CEM-SS cells2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID562870Selectivity ratio of EC50 for HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells to EC50 for wild type HIV1 infected in human HeLa cells2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation.
AID663302Resistance ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-32012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID269803Antiviral activity against HIV1 V179E mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269803Antiviral activity against HIV1 V179E mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269803Antiviral activity against HIV1 V179E mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID496621Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase K101E/V35T, E36D, K49R, V60I, K122P, I135R, S162A, E169R, K173T, Q174E,D177E, V189I, T200A, I202V, Q207E, R211K, V245Q mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID663307Inhibition of HIV1 recombinant reverse transcriptase L100I mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID298064Cytotoxicity against human MT4 cells by MTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID1485974Inhibition of HIV-1 reverse transcriptase Y188L mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID282739Inhibition of HIV1 RT Y181I mutant2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID1183080Cytotoxicity against mock-infected human MT4 cells assessed as reduction in proliferation after 96 hrs by MTT method2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and antiviral activity of new phenylimidazopyridines and N-benzylidenequinolinamines derived by molecular simplification of phenylimidazo[4,5-g]quinolines.
AID279487Antiviral activity against HIV1 isolate with RT K103N-L100I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1731744Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
AID1897020Antiviral activity against HIV-1 KP-5mvcR infected in human TZM-bl cells assessed as inhibition of viral entry by measuring reduction in RLU by single round assay2022Bioorganic & medicinal chemistry, 12-15, Volume: 76Hybrids of small CD4 mimics and gp41-related peptides as dual-target HIV entry inhibitors.
AID519872Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1487425Aqueous solubility of the compound in buffer at pH 6.4 after 48 hrs UV spectroscopy based shake flask method2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Discovery of novel dengue virus entry inhibitors via a structure-based approach.
AID1636929Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against viral infection by MTT method2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Computer-aided discovery of anti-HIV agents.
AID1272059Half life in human administered as multiple doses2016European journal of medicinal chemistry, Jan-27, Volume: 108Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry.
AID348908Ratio of ED50 for drug resistant HIV1 with reverse transcriptase Y181C mutant to wild type HIV1 NL4-32008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies.
AID267644Inhibition of HIV1 reverse transcriptase2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID1882474Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathicity by MTT assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID698298Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-32012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1693805Inhibition of recombinant HIV-1 BH10 reverse transcriptase Y181C mutant using D38/[32P]25PGA as template-primer incubated for 60 mins in absence of DTT followed by dTTP addition and measured after 15 to 30 sec by nucleotide incorporation assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID1736368Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase V108I/K103N double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel
AID1060631Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of viral cytopathicity after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.
AID492282Antiviral activity against HIV1 with reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID1882471Cytotoxicity against human MT2 cells assessed as cell viability by MTT assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1141961Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4.3 infected in human MT4 cells2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1141962Antiviral activity against HIV1 3B infected in human CEM cells assessed as protection of cells monitored by giant cell formation by microscopy2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID248879Inhibitory concentration against human immunodeficiency virus type 1 (with K103N/V108I resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID1888700Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID523485Antiviral activity against HIV1 with RT connection domain L100I/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1888698Antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1754642Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID443700Antiviral activity against HIV with reverse transcriptase L100I/K103N double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID1152371Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID266348Inhibition of HIV1 reverse transcriptase Y188C mutant in 293T cells2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.
AID1653630Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) K358R mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID1884227Antiviral activity against HIV-1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1410410Fold resistance, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.
AID619634Antiviral activity against HIV-1 3B harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID370725Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 L100I mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID1292012Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2016European journal of medicinal chemistry, Jun-10, Volume: 115Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID519862Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1565092Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
AID571974Antiviral activity against HIV-1 subtype CRF01_AE V029521 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID342721Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
AID1483275Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID571971Antiviral activity against HIV-1 subtype CRF01_AE V022820 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID611888Antiviral activity against Human immunodeficiency virus 1 assessed as inhibition of viral replication at 0.001 uM2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Bioactive neolignans and lignans from the bark of Machilus robusta.
AID298077Cytotoxicity against lymphocytes2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID541158Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 6 passages to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1741391Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1141977Inhibition of HIV1 wild-type reverse transcriptase Y181I/Y181C mutant using [3H]dTTP by scintillation counting2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1743622Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 RES056 infected in human MT4 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID246298Effective concentration of the compound to inhibit HIV-1 mutant K103N replication in HIV-infected MT-4 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID263522Antiviral activity against HIV1 F227L mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID1157600Antiviral activity against HIV1 CRF01 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID248262In vitro inhibitory concentration against HIV V106A mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1171591Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase L100I mutant to EC50 for wild type HIV1 NL4-32014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1373159Inhibition of reverse transcriptase K103N mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID279516Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID299023Antiviral activity against HIV1 assessed as reduction of virus-induced cytopathic effect in MT4 cells2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID279405Antiviral activity against HIV1 isolate with RT 101E, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID519864Antiviral activity against HIV1 subtype B-NL4-3 infected in 2 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID366528Resistance index, ratio of ID50 for reverse transcriptase K103N mutant to IC50 for wild-type HIV1 sreverse transcriptase2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID279390Antiviral activity against HIV1 isolate with RT 103N, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID371896Antiviral activity against wild type HIV1 NL4-3 in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID665547Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
AID576036Cmax in healthy human plasma at 400 mg, po qd for 14 days by liquid chromatography-tandem mass spectrometry2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID586469Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase L101I/S153F mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficie2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID586362Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase E92I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID519021Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as effect on total viral DNA2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID1572519Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID508794Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID391227Antiviral activity against wild type HIV1 infected in human MT4 cells after 72 hrs in presence of 50% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID1390713Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID586487Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase V72I/F121Y/T125K/I151V mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human im2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1407646Antiviral activity against Human immunodeficiency virus 1 NL4-3 infected in human CEM-GFP cells after 7 days by p24 ELISA2018European journal of medicinal chemistry, Sep-05, Volume: 157Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors.
AID584082Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase L100I, K103Q, H221H/Y mutant infected in human SupT1 cells derived from 11 viral passages with efavirenz assessed as inhibition of viral replication after 21 days relative to drug sensi2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1754641Antiviral activity against HIV1 harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID302249Antiviral activity against HIV1 NL43 in MT4 cells assessed as inhibition of viral induced cytopathic effect after 4 days by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID279519Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells in the presence of 20% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1736356Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y181C mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infect
AID1246230Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity by MTT assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, cytotoxicity and antimicrobial activity of thiourea derivatives incorporating 3-(trifluoromethyl)phenyl moiety.
AID441310Fold resistance, ratio of IC50 for HIV reverse transcriptase with Y181C mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
AID1357801Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase K103N mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID496619Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase A98G/V35T, V60I, I135L, S162A, K173A, Q174K, D177E, I178M, T200A,Q207E, R211K, V245Q, D250E mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID263521Antiviral activity against HIV1 F227C mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID263520Antiviral activity against HIV1 Y188L mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID583871Inhibition of HIV1 histidine-tagged reverse transcriptase Y181C mutant activity by primer extension assay2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID198577Inhibitory concentration for 90% inhibition of HIV-1 reverse transcriptase, whole cell based antiviral assay2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.
AID573467Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID508632Antiviral activity against Human immunodeficiency virus 1 subtype G isolate RU132 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1446815Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1815401Inhibition of HIV1 reverse transcriptase E138K mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID361909Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106A mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1815391Inhibition of HIV1 reverse transcriptase K103N/Y181C double mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID573465Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1847042Antiviral activity against HIV 1 infected in human HeLa-MAGI cells assessed as inhibition of viral replication measured 24 hrs post infection by fluorescence based analysis2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase.
AID105695Anti-HIV-1 activity against K103N strain in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1155810Fold resistance, ratio of EC50 for HIV-1 harboring NNTRI-resistant reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID492047Antiviral activity against HIV1 bearing reverse transcriptase K103N and Y181C double mutation infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
AID1249713Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID508654Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID279421Antiviral activity against HIV1 isolate with RT 101E, 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1443661Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID573999Ratio of EC50 for Human immunodeficiency virus in presence of 10% FCS to EC50 for Human immunodeficiency virus in presence of 50% human serum2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID709869Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID658572Antiviral activity against wild type Human immunodeficiency virus 1 NL4-3 pseudotyped with HIV envelope infected in human HeLa-SxR5 cells assessed as inhibition of viral replication at 65 nM after 3 days by beta-galactosidase assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium.
AID279434Antiviral activity against HIV1 isolate with RT 101E, 181C, 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1275547Antiviral activity against HIV1 3B expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID557052Antiviral activity against NRTI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1884221Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID279524Antiviral activity against HIV1 NL4-3 with Y188L mutation in Hela-JC53 cells in the presence of 5% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1069125Inhibition of HIV wild-type reverse transcriptase by electrochemiluminescence assay2014Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID361922Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase Y188C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID588997Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, MPR32010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID257169Antiviral activity against HIV1 Y188L mutant strain infected MT4 cells by MTT method2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID717261Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID1693804Inhibition of recombinant HIV-1 BH10 reverse transcriptase Y181C mutant using D38/[32P]25PGA as template-primer incubated for 5 mins in presence of DTT followed by dTTP addition and measured after 15 to 30 sec by nucleotide incorporation assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID663904Cytotoxicity against human MT4 cells after 96 hrs by MTT assay2012European journal of medicinal chemistry, Jul, Volume: 535-acetyl-2-arylbenzimidazoles as antiviral agents. Part 4.
AID416432Antiviral activity against HIV1 bearing HIV1 NL4-3 envelope infected in human HeLa CD4 cells coexpressing LTR/beta-Gal gene assessed as reduction in virus-induced beta-galactosidase reporter gene activity after 72 hrs by single-cycle infection assay2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Identification and characterization of UK-201844, a novel inhibitor that interferes with human immunodeficiency virus type 1 gp160 processing.
AID1815395Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID522370Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106I mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID302260Inhibition of HIV1 reverse transcriptase K103N mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID302248Cytotoxicity against MT4 cells after 4 days by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID496617Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, T39K, I50V, V60I, S68G, I135V, S162A, K173V, Q174K,D177E, T200A, E203Q, Q207D, R211K mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID397179Antiviral activity against HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID508761Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, F227L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508779Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID573250Cmax in HIV-1 infected children at 14.4 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID82466Antiviral activity against P225H strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID573470Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1357793Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID279485Antiviral activity against HIV1 isolate with RT K103N-V108I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1609109Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1060627Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.
AID665271Antiviral activity against HIV1 3B harboring wild type RT infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID443694Antiviral activity against HIV with reverse transcriptase L100I mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID1888699Antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID279408Antiviral activity against HIV1 isolate with RT 101Q, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1298250Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1750714Antiviral activity against HIV-1 infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID246779Concentration required to reduce the amount of p24 by 90% in wtIIIB-HIV-1-infected C8166 cells2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID443708Antiviral activity against HIV with reverse transcriptase V106A/G190A/F227L mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID1773462Resistance factor, ratio of EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID197934HIV-1 reverse transcriptase inhibitory activity against Wild Type Reverse transcriptase using (poly)rC600*(oligo)dGT as template primer.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID1609106Antiviral activity against HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1249717Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1882475Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathicity by MTT assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID361917Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106I mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1348216Antiviral activity against wild-type VSV-G pseudotyped MLV infected in HEK293 cells pretreated for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay2017Journal of natural products, 12-22, Volume: 80, Issue:12
Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities.
AID1248222Antiviral activity against wild type HIV 1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID265472Activity against HIV-112 assessed by inhibition of p24 production in human lymphocytes2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID279441Antiviral activity against HIV1 isolate with RT 101Q, 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID573471Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID279442Antiviral activity against HIV1 isolate with RT 98G, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1773448Antiviral activity against wild type HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1264544Ratio of EC50 for HIV-1 expressing reverse transcriptase K101P mutant to EC50 for HIV-1 X4 expressing wild-type reverse transcriptase2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID248255In vitro inhibitory concentration against HIV E138K mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID279428Antiviral activity against HIV1 isolate with RT 101E, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID586903Activity at MRP32011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID143393Inhibition of the NNRTI HIV-1 enzyme by 50% using enzyme assay.2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID248842Inhibitory concentration against human immunodeficiency virus type 1 (with K103N resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID302262Inhibition of HIV1 reverse transcriptase V106A mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1141965Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID302251Antiviral activity against HIV1 with reverse transcriptase IRLL98 mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1561722Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonam
AID1637394Antiviral activity against human HIV-1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID519886Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID457958Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID257918Antiviral activity against HIV1 V106A mutant using HeLa MAGI assay2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor.
AID1761006Antiviral activity against wild type HIV1 NL4-3 infected in human TZM-bl cells assessed as reduction in viral infection measured after 1 day by luciferase reporter gene assay based luminiscence assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID293561Antiviral activity against HIV1 LAI with RT Y181C mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID391222Inhibition of HIV1 RT polymerase K103N mutant by SPA2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID141363Inhibitory activity against mutant L1001 HIV-1 Reverse transcriptase2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
AID1572528Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID246300Effective concentration of the compound to inhibit HIV-1 mutant Y181C replication in HIV-infected MT-4 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1811039Anti-viral activity against HIV1 harboring RT L100I mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID271414Antiviral activity against HIV1 K103N-Y181C mutant in HeLa-JC53 cells2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase.
AID1248227Inhibition of recombinant HIV1 Reverse transcriptase p66/p51 using poly (rA)-oligo (dT) as template primer after 40 mins by spectrofluorometric analysis2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID371905Antiviral activity against HIV1 NL4-3 with K103N/Y181C double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID518740Antiviral activity against HIV 1 subtype B harboring wild type reverse transcriptase infected in human TZM-bl cells assessed as inhibition of viral growth by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1212899Drug metabolism in human liver microsomes harboring CYP2B6*1/*1 genotype assessed as intrinsic clearance for CYP2B6 variant-mediated 8-hydroxyefavirenz metabolite formation measured per mg protein after 15 mins by LC/MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID279520Antiviral activity against wild type HIV1 NL4-3 in Hela-JC53 cells in the presence of 30% human serum after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID248264In vitro inhibitory concentration against HIV Y188L mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID246323Effective concentration against human immunodeficiency virus type 1 Y181C mutant was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID298065Metabolic stability in rat plasma2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID443423Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus induced cytopathogenicity after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis, pharmacological and antiviral activity of 1,3-thiazepine derivatives.
AID622052Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer K103N/Y181C mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID698304Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID623212Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1373153Inhibition of recombinant wild-type HIV-1 3B reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli JM109 assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID440071Antiviral activity against HIV-1 LAI harboring wild type reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID576049Reduction in ABCC2 mRNA expression in healthy human at 400 mg, po qd for 14 days by RT-PCR2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID449491Cytotoxicity against human MT4 cells as reduction in cell viability after 5 days by MTT assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID282736Inhibition of HIV1 RT L100I mutant2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID1485972Inhibition of HIV-1 reverse transcriptase E138K mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID279486Antiviral activity against HIV1 isolate with RT K103N-K101Q mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID522376Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V179D mutant clone to EC50 for wild type HIV12010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID246269Effective concentration against human immunodeficiency virus type 1 Y188L mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1171594Inhibition of wild type HIV1 reverse transcriptase K103N mutant assessed as reduction in enzyme activity2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID556527Antiviral activity against Human immunodeficiency virus 1 clone 14682 harboring 122E, 135V, Q145V, 200A mutation in reverse transcriptase by phenosense assay relative to wild type2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility.
AID541124Antiviral activity against HIV1 3B infected in SupT1 cells assessed as fold decrease in viral 2-LTR circles accumulation after 3 hrs postinfection by TaqMan real-time PCR2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1391081Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID519869Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID736040Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID1435510Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay
AID427967Antiviral activity against HIV1 infected in human HeLa cells expressing CD4-LTR assessed as inhibition of viral entry-related beta galactosidase expression treated for 2 hrs followed by drug wash out measured after 48 hrs by MAGI assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID443690Antiviral activity against HIV with reverse transcriptase K103N/Y181C/G190A mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557053Antiviral activity against NRTI-, PI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID736438Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID82472Antiviral activity against V108I strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID508643Antiviral activity against Human immunodeficiency virus 1 subtype A1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID440080Antiviral activity against HIV1 HXB2 harboring 179E mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID83553Potency evaluated against NNRTI-Resistant HIV-1 strain Val106Ala2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID622051Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer G190A mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID279475Antiviral activity against HIV1 isolate with RT 101E, 103N, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID248845Inhibitory concentration against human immunodeficiency virus type 1 (with Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID305057Antiviral activity against HIV in HEK293T cells after 48 hrs2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
4-Aminopyrimidines as novel HIV-1 inhibitors.
AID257168Antiviral activity against HIV1 K103N mutant strain infected MT4 cells by MTT method2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID573244Cmin in HIV-1 infected children at 12 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID1335215Antiviral activity against HIV-1 NL4-3 harboring RT-Y181C mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1435512Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase L100I mutant
AID198915Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution Y181I2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID279403Antiviral activity against HIV1 isolate with RT 108I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1352321Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103 N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID279394Antiviral activity against HIV1 isolate with RT 98G mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID198578Inhibitory concentration against HIV-1 reverse transcriptase2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.
AID389380Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1574387Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 L100I mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1773827Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID82471Antiviral activity against V106I/Y181C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID279425Antiviral activity against HIV1 isolate with RT 179G mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID649485Inhibition of RNA-dependent DNA polymerase activity of wild type Human immunodeficiency virus 1 reverse transcriptase2012European journal of medicinal chemistry, Apr, Volume: 50Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach.
AID1157584Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID246301Effective concentration of the compound to inhibit HIV-1 mutant Y188L replication in HIV-infected MT-4 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1884538Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 L100I mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID614142Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2011Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
AID1157594Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1884224Antiviral activity against HIV-1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID573251AUC (0 to t) in HIV-1 infected children at 12 mg/kg, po administered once daily by HPLC2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Is the recommended dose of efavirenz optimal in young West African human immunodeficiency virus-infected children?
AID1391082Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID496623Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/G18V, Q23P, V35T, E40D, V60I, S68G, D123E, I135V, S162A, K173T, Q174N, T200A, Q207E, R211K, F214L mutant relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1304403Cytotoxicity against mock-infected human MT4 cells2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID1200843Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID1286672Antiviral activity against HIV1 harboring reverse transcriptase Y181C/K103N double mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID431621Cytotoxicity against human MT4 cells by MTT assay2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID663305Inhibition of HIV1 wild type recombinant reverse transcriptase assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID44798In vitro concentration required to reduce the amount of p24 by 90% in WTIIIB infected C8166 cells2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID1185998Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID248256In vitro inhibitory concentration against HIV F227C mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID576047Reduction in ABCB1 mRNA expression in healthy human at 400 mg, po qd for 14 days by RT-PCR2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID1249716Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by MTT assay2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID368564Inhibition of wild type HIV1 free reverse transcriptase2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID1687685Antiviral activity against HIV-2 ROD strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID650687Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV 1 NL4-32011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID490369Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect in presence of 40 % human serum2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID1152374Selectivity index, ratio CC50 for human MT4 cells to EC50 for HIV 1 3B2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID198099Inhibitory activity against HIV-1 reverse transcriptase enzyme1999Bioorganic & medicinal chemistry letters, Oct-04, Volume: 9, Issue:19
Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.
AID518742Selectivity ratio of EC50 for antiviral activity against HIV 1 subtype B harboring reverse transcriptase M230L mutant to EC50 for antiviral activity against HIV 1 subtype B harboring wild type reverse transcriptase2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1446816Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID541128Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of integrated junction products after 48 hrs by Alu-PCR assay2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID368568Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-DNA binary complex expressed in Escherichia coli BL212009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID1583020Antiviral activity against NNRTI-resistant HIV1 RES056 containing reverse transcriptase K103N+Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID557036Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1212883Drug metabolism in microsomes expressing CYP2B6.1 (unknown origin) assessed as intrinsic clearance for enzyme-mediated 8-hydroxyefavirenz metabolite formation measured per pmol of P450 after 15 mins by HPLC/UV system in presence of Cyt b5 coexpression2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
AID508776Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179T mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID557045Antiviral activity against HIV1 CRF17_BF harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557020Antiviral activity against HIV1 clade B harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1561716Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in absence of test compound assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID279449Antiviral activity against HIV1 isolate with RT 98G, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID541109Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID197933HIV-1 reverse transcriptase inhibitory activity against Ile 100 mutant using (poly)rC600*(oligo)dGT as template primer.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID371900Antiviral activity against HIV1 NL4-3 with K103N mutant in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by multiple round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID246463Compound concentration required to achieve 50% protection of infected MT-4 cells from Y181C strain was determined by the MTT method2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID571976Antiviral activity against HIV-1 subtype B V022807 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID267649Antiviral activity against HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID508625Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 93TH073 infected in human PBMC cells by cell based assay2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID619643Ratio of EC50 for HIV-1 3B harboring RT L100I mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID94444Potency of second-generation NNRTIs against Mutant HIV-1 K103N free drug2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID572177Antiviral activity against HIV-1 subtype H V022828 harboring NNRTI K101Q and V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1390714Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID1456311Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B wild type reverse transcriptase infected in human MT4 cells2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID1206939Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 assessed as reduction in biotin-labeled dUTP incorporation into DNA using polyr(A) x oligo(dT)16 template/primer hybrid2015European journal of medicinal chemistry, Jun-05, Volume: 97Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID246153Concentration required to achieve 50% protection of infected MT-4 cells from K103N-Y181C2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID330487Cytotoxicity against human MT4 cells2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID541165Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E138K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1609104Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID586900Activity at ABCB12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID1261342Antiviral activity against Vaccinia virus2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1157604Antiviral activity against HIV1 MP1033 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID88365Antiviral activity against G190A mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID247723Inhibitory concentration against 100I mutant was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.
AID1520059Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1390712Cytotoxicity against human MT4 cells after 5 days by MTT assay2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID247496Inhibitory activity against HIV-1 mutant strain 101E2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID1485970Inhibition of HIV-1 reverse transcriptase K103N mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID508751Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID104411Antiviral activity of Protein Binding of compound was evaluated for RF virus expressed MT-2 by RNA2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID586366Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase G118S mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1815396Inhibition of wild type HIV1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID586905Inhibition of ABCB1 activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID576051Ratio of drug concentration in PBMCs to plasma of healthy human administered at 400 mg, po qd for 14 days measured after 24 hrs post last dose2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.
AID1298246Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1743639Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT F227L/V106A mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID584030Inhibition of HIV1 histidine-tagged reverse transcriptase L234I mutant activity by primer extension assay2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1687688Antiviral activity against wild type HIV1 assessed as inhibitory effect on virus producing cells at 10 uM by cell based inhibition assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase.
AID361905Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/P225H mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1357789Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID443707Antiviral activity against HIV with reverse transcriptase K103N/Y181C/G190A mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID1637388Antiviral activity against human HIV-1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1443664Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1743621Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID573995Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for L-708,906-resistant Human immunodeficiency virus harboring T66I, L74M and S230R mutations in integrase2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1443666Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1743627Antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1565096Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID571985Antiviral activity against HIV-1 subtype C V022817 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID464770Half life in Beagle dog at 0.5 mg/kg, iv or 0.5 mg/kg, po2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID279496Antiviral activity against HIV1 isolate with RT K103N-G190A mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID386490Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in human MT4 cells assessed as reduction of virus-induced cytopathogenicity by MTT assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Parallel synthesis, molecular modelling and structure-activity relationship studies on O-[2-(hetero)arylethyl]-N-phenylthiocarbamates.
AID104409Antiviral activity of Protein Binding of compound was evaluated for E virus expressed MT-2 by yield2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1729152Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV 3B infected in human MT4 cells2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID448397Fold resistance, ratio of IC50 for HIV reverse transcriptase with K103N mutant to IC50 for HIV wild type reverse transcriptase2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Pyrazole NNRTIs 3: optimisation of physicochemical properties.
AID302264Inhibition of HIV1 reverse transcriptase Y1811 mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1653629Activation of recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) Y427A mutant expressed in Escherichia coli at 20 uM using cholesterol as substrate measured after 30 mins in presence of cytochrome P450 oxidoreductase by gas chromatography-mas2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID562120Apparent oral volume of distribution in patient with HIV infection at 600 mg/kg QD2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients.
AID1574385Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1410485Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells2018ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID443685Antiviral activity against HIV with reverse transcriptase K103N/G190A double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID519971Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT to EC50 for 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID1687680Antiviral activity against wild type HIV-1 strain 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1627028Cytotoxicity against HIV1 infected African green monkey Vero cells assessed as reduction in cell viability after 7 days by MTT assay2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1596752Antiviral activity against HIV-1 3B harboring reverse transcriptase E138K mutant infected in MT4 cells measured after 5 days by MTT assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID1815377Anti-HIV activity against HIV-1 IIIB infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1157602Antiviral activity against HIV1 MP634 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1357802Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase E138K mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1773441Antiviral activity against wild type HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID757626Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID368566Inhibition of wild type HIV1 reverse transcriptase-DNA-dNTP ternary complex2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID1485971Inhibition of HIV-1 reverse transcriptase V106A mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID443698Antiviral activity against HIV with reverse transcriptase G190A mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID757621Inhibition of recombinant wild type HIV1 RT using poly(rA)/oligo(dT)16 as template after 40 mins by spectrofluorometric analysis2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1761008Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID519889Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.005 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge.
AID508760Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V108I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID523358Antiviral activity against HIV1 with RT connection domain G190A/N348Ib mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID508759Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1163253Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID586381Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase S153Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1653633Binding affinity to recombinant human C-terminal 4His-tagged CYP46A1 delta(2 to 50) mutant expressed in Escherichia coli at 15 to 30 uM in absence of substrate by UV-spectrophotometric method2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
AID1558849Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells incubated for 5 days by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID663297Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID370733Therapeutic index, ratio of IC50 for HIV1 3B to TC50 for human C8166 cells2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID1373152Inhibition of reverse transcriptase Y181C mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID330490Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES0532008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID279456Antiviral activity against HIV1 isolate with RT 188H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID302266Resistance index, ratio of Ki for HIV1 RT K103N mutant to Ki for wild type HIV1 3B reverse transcriptase2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID586361Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase T66K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vir2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID366548Inhibition of HIV1 wild-type reverse transcriptase by scintillation counting assay2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID621982Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer L100I mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1822275Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV-1 IIIB infected in human MT4 cells2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID586372Antiviral activity against Human immunodeficiency virus 1 NL432 harboring integrase Y143H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 2 to 3 days by PCR relative to wild type Human immunodeficiency vi2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
AID1275546Antiviral activity against HIV1 3B expressing reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID81766Compound was evaluated for its ability to inhibit the wild type RF strain of HIV-12001Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2002European journal of biochemistry, Mar, Volume: 269, Issue:6
Structural basis for the inhibitory efficacy of efavirenz (DMP-266), MSC194 and PNU142721 towards the HIV-1 RT K103N mutant.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,956)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's131 (4.43)18.2507
2000's1071 (36.23)29.6817
2010's1416 (47.90)24.3611
2020's338 (11.43)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 83.44

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index83.44 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index141.33 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (83.44)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials631 (20.29%)5.53%
Trials0 (0.00%)5.53%
Reviews204 (6.56%)6.00%
Reviews0 (0.00%)6.00%
Case Studies201 (6.46%)4.05%
Case Studies0 (0.00%)4.05%
Observational64 (2.06%)0.25%
Observational0 (0.00%)0.25%
Other2,010 (64.63%)84.16%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (317)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Open Label, Randomized Trial of TDF/FTC+Raltegravir Vs. TDF/FTC+Efavirenz in HIV-1-Infected Women: Differential Effects on Viral Suppression/Reservoir, & Immune Parameters in Different Compartments, Including Gut & Genital Tract [NCT00984152]Phase 30 participants (Actual)Interventional2011-06-30Withdrawn(stopped due to Decision not to go forth with study.)
Comparison of Virological and Immunological Results of Efavirenz-based Regimen in HIV-infected Patients With or Without Allergic Reactions to Nevirapine [NCT01044810]559 participants (Actual)Observational2010-01-31Completed
An Open-label Study of Liquid and Sprinkled Formulations of Efavirenz Administered in Combination With Didanosine and Emtricitabine in HIV-infected Infants and Children 3 Months to 6 Years of Age. [NCT00364793]Phase 1/Phase 256 participants (Actual)Interventional2007-02-28Completed
A Multicenter, Double-Blind, Randomized, Active-Controlled Study to Evaluate the Safety and Antiretroviral Activity of MK-0518 Versus Efavirenz in Treatment Naive HIV-Infected Patients, Each in Combination With TRUVADA™ [NCT00369941]Phase 3566 participants (Actual)Interventional2006-08-31Completed
Bioavailability Mechanistic Study of Hot-Melt-Extruded Amorphous Solid Dispersions [NCT03886766]16 participants (Actual)Interventional2019-04-30Completed
Clinical Trial of CNS Penetrating ART to Prevent NeuroAIDS in China [NCT01340950]Phase 4250 participants (Actual)Interventional2010-07-31Completed
A Randomized, Pilot Estimation Study to Compare the Safety and Efficacy of Raltegravir+TDF+3TC Versus TDF+3TC+EFV in HBV/HIV Co-infected Patients [NCT01318096]60 participants (Anticipated)Interventional2011-03-31Not yet recruiting
Pharmacokinetics of Tenofovir and Tenofovir-diphosphate, Emtricitabine and Emtricitabine-triphosphate, and Efavirenz Once Daily Over 10 Days Following Drug Intake Cessation in Healthy Volunteers [NCT01108926]Phase 119 participants (Actual)Interventional2010-06-30Completed
An Open-label, Parallel Drug Interaction Study to Evaluate the Effect of a CYP3A Moderate Inducer Efavirenz on the Pharmacokinetics of Quizartinib in Healthy Subjects [NCT04459598]Phase 132 participants (Actual)Interventional2020-08-19Completed
Phase 2 Comparison of Low-Dose Naltrexone vs ARV Effectiveness in HIV+ Progression [NCT01174914]Phase 2171 participants (Actual)Interventional2008-03-31Completed
"Single-center, Randomized, Five-way Crossover Study to Investigate Low-dose Combinations of Caffeine, Efavirenz, Losartan, Omeprazole, Metoprolol, Chlorzoxazone and Midazolam (Basel Cocktail) for Simultaneous Phenotyping of CYP1A2, CYP2B6, CYP2C9, CYP2C1 [NCT01187862]Phase 116 participants (Actual)Interventional2010-07-31Completed
A Study to Evaluate the Potential Drug-Drug Interaction Between Efavirenz and Danoprevir With Low Dose Ritonavir When Administered Together in Healthy Adult Volunteers [NCT01588002]Phase 140 participants (Actual)Interventional2012-04-30Completed
The Effects of Maraviroc Versus Efavirenz in Combination With Zidovudine/Abacavir on the CD4/CD8 Ratio in Treatment-naïve HIV-infected Individuals [NCT03178084]Phase 3721 participants (Actual)Interventional2014-10-15Completed
The Risk of Cardiovascular Events Among HIV Patients Initiating Efavirenz-containing Versus Efavirenz-free Antiretroviral Regimens [NCT02426866]29,612 participants (Actual)Observational2014-12-31Completed
Impact of a Dolutegravir-based Regimen on Early Mortality of Severely Immunocompromised AIDS Patients [NCT01837277]Phase 2/Phase 3186 participants (Actual)Interventional2017-12-15Completed
A Phase I, Open-label, Fixed-sequence, Two-period, Crossover, Drug-drug Interaction Study to Investigate the Effect of Efavirenz on the Pharmacokinetics of Ganaplacide and Lumefantrine Combination in Healthy Participants [NCT05330273]Phase 114 participants (Actual)Interventional2022-04-28Completed
Efavirenz Pharmacokinetics and Pharmacogenomics in Older HIV-infected Patients [NCT01886404]30 participants (Actual)Observational [Patient Registry]2013-12-01Completed
"Safeguard the Household - A Study of HIV Antiretroviral Therapy Treatment Strategies Appropriate for a Resource Poor Country" [NCT00255840]812 participants (Actual)Interventional2006-07-31Completed
A PHASE 1, RANDOMIZED, OPEN LABEL, 2-WAY CROSSOVER STUDY TO ESTIMATE THE EFFECT OF MULTIPLE DOSE PF-06651600 ON THE PHARMACOKINETICS OF SINGLE DOSE MIDAZOLAM AND EFAVIRENZ IN HEALTHY PARTICIPANTS [NCT03762928]Phase 112 participants (Actual)Interventional2018-12-07Completed
A Phase IIIB, Randomized Trial of Open-Label Efavirenz or Atazanavir With Ritonavir in Combination With Double-Blind Comparison of Emtricitabine/Tenofovir or Abacavir/Lamivudine in Antiretroviral-Naive Subjects [NCT00118898]Phase 31,864 participants (Actual)Interventional2005-09-30Completed
A Phase 3, Randomized, Multicenter Study of the Treatment of Antiretroviral-Naive HIV-1 Infected Subjects Comparing Tenofovir Disoproxil Fumarate and Emtricitabine in Combination With Efavirenz vs Combivir (Lamivudine/Zidovudine) and Efavirenz [NCT00112047]Phase 3517 participants (Actual)Interventional2003-07-31Completed
An Evaluation of the Uptake and Safety of, and Adherence to Antiretroviral Treatment Among Individuals With CD4 ≥ 250 Cells/mm3 and HIV Virus Load ≥ 50,000 cp/mL [NCT01583439]11 participants (Actual)Interventional2012-09-30Terminated(stopped due to Low Accrual.)
Bioequivalence Study of Efavirenz, Emtricitabine and Tenofovir in Healthy Volunteers, After Administering a Single Dose of a Fixed Dose Combination of the Test Formulation With Respect to the Reference Product, Atripla ® From Gador S.A [NCT03309566]Phase 424 participants (Actual)Interventional2016-09-04Completed
PI or NNRTI as First-line Treatment of HIV in a West African Population With Low Adherence - the PIONA Trial [NCT01192035]Phase 4400 participants (Actual)Interventional2011-05-31Completed
Reverse Triple Negative Immune Resistant Breast Cancer [NCT05076682]Phase 230 participants (Anticipated)Interventional2022-06-30Recruiting
Switching Tenofovir/Emtricitabine/Efavirenz to Tenofovir/Emtricitabine/Rilpivirine Versus Continuing Tenofovir/Emtricitabine/Efavirenz in HIV1-infected Patients With Complete Virological Suppression [NCT03251690]246 participants (Actual)Interventional2016-10-27Completed
Daily Antiretroviral Therapy (DART 1): An Open-Label, Single-Arm, Prospective, Multicenter Clinical Trial to Evaluate the Efficacy and Safety of Didanosine Enteric Coated (Ddl-EC) in Combination With Lamivudine (3TC) and Efavirenz (EFV) Once Daily in Anti [NCT00116415]65 participants Interventional2002-03-31Completed
A Phase 3 Study Switching HIV-1 Infected Subjects With an Undetectable Viral Load From a HAART Regimen Dosed Twice Daily or More Frequently to a Once-Daily HAART Regimen [NCT00135369]Phase 3300 participants Interventional2002-09-30Completed
Efficacy of Simultaneous Versus Sequential Antiretroviral Therapy and Antituberculosis Treatment in Patients With AIDS and Active Tuberculosis. Open, Randomized and Controlled, Multisite Clinical Trial. [NCT00737724]63 participants (Actual)Interventional2008-03-31Terminated(stopped due to Other published trials showed definitive expected superiority of Group 1)
[NCT00523458]Phase 45 participants (Actual)Interventional2007-07-31Terminated(stopped due to A delay in protocol approval and approval of laboratory sites in Salvador, Brazil left too little time for completion of enrollment into the study.)
Systematic Empirical vs. Test-guided Anti-tuberculosis Treatment Impact in Severely Immunosuppressed HIV-infected Adults Initiating Antiretroviral Therapy With CD4 Cell Counts <100/mm3: the STATIS Randomized Controlled Trial [NCT02057796]Phase 41,050 participants (Actual)Interventional2014-09-30Completed
INFLAMMATION AND DRUG METABOLISM - Does the Effect of Drugs Decrease When Patients With Type 2 Diabetes Initiate Antidiabetic Treatment? [NCT04504045]Phase 110 participants (Actual)Interventional2020-09-01Terminated(stopped due to Slow recruitment due to COVID-19, the study was stopped when recruited numbers fulfilled the pre-defined lower sample size.)
A Phase IIb Randomized, Controlled, Partially Blinded Clinical Trial to Investigate Safety, Efficacy and Dose-response of BMS-986001 in Treatment-naive HIV-1-infected Subjects, Followed by an Open-label Period on the Recommended Dose [NCT01489046]Phase 2297 participants (Actual)Interventional2011-02-28Terminated
The Safety and Antiviral Efficacy of Stavudine Extended Release Formulation as Compared to Stavudine Immediate Release Formulation, Each as Part of Potent Antiretroviral Combination Therapy [NCT00005918]Phase 3730 participants Interventional2000-06-30Completed
A Single-centre, Single-dose, Open-label and Self-control Study to Evaluate the Effect of Efavirenz on Pharmacokinetic of SHR6390 in Healthy Chinese Subjects [NCT04973020]Phase 120 participants (Actual)Interventional2021-09-01Completed
Intensive Pharmacokinetic Studies of Antiretroviral Drug Combinations in Children [NCT00260078]Phase 1/Phase 275 participants (Actual)Interventional2006-02-28Completed
A Phase III, Randomized, Open-Label Trial to Evaluate Strategies for Providing Antiretroviral Therapy to Infants Shortly After Primary Infection in a Resource Poor Setting [NCT00102960]Phase 3377 participants (Actual)Interventional2005-07-31Completed
A Study to Determine the Concentration-Electrocardiographic Effects of Efavirenz in Healthy Subjects Enriched for CYP2B6 Polymorphisms [NCT02164812]Phase 158 participants (Actual)Interventional2014-07-31Completed
A Phase 1, 3-Part, Open-label, Drug-Drug Interaction Study to Evaluate the Effect of a Moderate CYP3A4 Inhibitor, and of Strong and Moderate CYP3A4 Inducers on the Pharmacokinetics of TAK-279 in Healthy Subjects [NCT05995249]Phase 148 participants (Anticipated)Interventional2023-08-11Recruiting
Change in Sleep Architecture and Neuropsychological Performance Following Switch From Atripla to Stribild. [NCT02283060]Phase 430 participants (Anticipated)Interventional2014-09-30Recruiting
A Study to Compare Long-Term Safety and Tolerability of Stavudine (d4T) Extended Release (ER) Versus Conventional (Immediate Release, IR) Formulations, Each In Combination With Lamivudine (3TC) and Efavirenz (EFV) in Subjects Who Have Completed BMS Studie [NCT00116298]Phase 3900 participants Interventional2001-01-31Completed
Peking Union Medical College Hospital [NCT04463784]500 participants (Anticipated)Interventional2018-04-01Active, not recruiting
Multicenter, Double-Blind, Randomized, Dose Ranging Study to Compare the Safety and Activity of MK0518 Plus Tenofovir and Lamivudine (3TC) Versus Efavirenz Plus Tenofovir and Lamivudine (3TC) in ART-Naive, HIV-Infected Patients [NCT00100048]Phase 2206 participants (Actual)Interventional2005-01-31Completed
Role of Pharmacogenetics in Efavirenz and Nevirapine Pharmacokinetics, Efficacy and Safety in Mother-infant Pairs During Pregnancy and Lactation [NCT02269462]460 participants (Actual)Observational2012-12-31Completed
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289]1,578 participants (Actual)Observational2003-06-09Completed
Daily Antiretroviral Therapy (DART-II): An Open-Label, Single-Arm, Prospective, Multicenter Clinical Trial To Evaluate the Efficacy and Safety fo Stavudine Extended Release (d4T XR) in Combination With Lamivudine (3TC) and Efavirenz (EFV) Once Daily in An [NCT00116116]Phase 470 participants Interventional2002-03-31Completed
A Phase IV Open-label, Multi-centre, Randomised, Dual-arm, Pilot Study to Assess the Feasibility of Switching Individuals Receiving Efavirenz With Continuing Central Nervous System (CNS) Toxicity, to Dolutegravir [NCT02285374]Phase 440 participants (Anticipated)Interventional2014-11-30Not yet recruiting
A Phase 3 Study Switching HIV-1 Infected Patients With an Undetectable Viral Load on a First Protease Inhibitor-Based Regimen to an Efavirenz-Based Regimen [NCT00135382]Phase 3254 participants Interventional2002-06-30Completed
A Phase I, Open-label Trial to Explore the Pharmacokinetics, Safety and Tolerability of TMC278 25 mg Once Daily Following a 2-week Period Receiving Efavirenz, in Healthy Male and Female Subjects [NCT01268839]Phase 120 participants (Actual)Interventional2010-01-31Completed
Tenofovir, Emtricitabine, Efavirenz and Atazanavir Pharmacokinetics in the Aging HIV-Infected Population [NCT01180075]85 participants (Actual)Observational2010-05-31Completed
A Pilot Evaluation of the Pharmacokinetics, Efficacy and Safety of Switching From Efavirenz to Maraviroc Administered at 600mg Then 300mg Twice-daily in Patients Suppressed on an Efavirenz-containing Regimen as Initial Therapy [NCT01190293]Phase 412 participants (Actual)Interventional2010-01-31Completed
The Effect of Dolutegravir-based ART on Plasma Etonogestrel Levels in HIV-infected Women Using Contraceptive Implants in Botswana [NCT03336346]148 participants (Actual)Observational2017-11-15Completed
Pharmacokinetics of EFV 400mg Once Daily During Pregnancy in HIV+ Women [NCT02499874]Phase 126 participants (Actual)Interventional2015-08-31Completed
Phase III Study of the Virologic Efficacy and Safety of Dolutegravir-Containing Versus Efavirenz-Containing Antiretroviral Therapy Regimens in HIV-1-Infected Pregnant Women and Their Infants [NCT03048422]Phase 3643 participants (Actual)Interventional2018-01-19Completed
Raltegravir Cerebrospinal Fluid Pharmacodynamic Study in HIV-Infected Individuals [NCT01293123]2 participants (Actual)Interventional2011-12-31Terminated(stopped due to Did not meet enrollment goals)
Protease Inhibitors to Reduce Malaria Morbidity in HIV-Infected Pregnant Women [NCT00993031]Phase 3389 participants (Actual)Interventional2009-12-15Completed
A Randomized Open Label Trial of HIV Protease Inhibitors for the Prevention of Malaria in HIV-Infected Children [NCT00978068]Phase 3176 participants (Actual)Interventional2009-09-30Completed
Pharmacokinetics of Rifabutin Combined With Antiretroviral Therapy in the Treatment of Tuberculosis Patient With HIV Infection in South Africa: A Phase II Trial [NCT00640887]Phase 248 participants (Anticipated)Interventional2009-02-28Completed
Effects of CYP2B6 Genetic Polymorphisms on Efavirenz Pharmacokinetics, Autoinduction and Drug Interactions in Healthy Volunteers. [NCT00668395]73 participants (Actual)Interventional2007-05-31Completed
A Single-centre, Open-label Study to Assess the Effects of Steady-state Efavirenz 600 mg QD (Sustiva®) on Tipranavir Concentration When Tipranavir/Ritonavir Are Administered at Doses 500 mg/200 mg BID to Steady-state in Healthy Adult Volunteers [NCT02226991]Phase 134 participants (Actual)Interventional2006-04-30Completed
A Phase 2b Randomized, Double-Blind, Double-Dummy Trial of 100 or 200 mg Once-Daily Doses of Cenicriviroc (CVC, TBR 652) or Once-Daily EFV, Each With Open-Label FTC/TDF, in HIV 1-Infected, Antiretroviral Treatment-Naïve, Adult Patients With Only CCR5-Trop [NCT01338883]Phase 2143 participants (Actual)Interventional2011-06-30Completed
Evaluation of the Capacity of a Weekly Strategy of 4 Consecutive Days on Treatment Followed by 3 Days Off Treatment, in HIV-1 Infected Patients With Undetectable Viral Load for at Least 12 Months, to Maintain a Virological Success With This Intermittent M [NCT02157311]Phase 3100 participants (Actual)Interventional2014-07-31Completed
A Randomized Study to Compare the Efficacy of Vorinostat/Hydroxychloroquine/Maraviroc (VHM) in Controlling HIV After Treatment Interruption in Subjects Who Initiated ART During Acute HIV Infection [NCT02475915]Phase 1/Phase 215 participants (Actual)Interventional2015-01-31Completed
Study of Once-Daily Abacavir/Lamivudine Versus Tenofovir/Emtricitabine, Administered With Efavirenz in Antiretroviral-Naive, HIV-1 Infected Adult Subjects [NCT00549198]Phase 4392 participants (Actual)Interventional2007-06-30Completed
Genetic Determinants of the Metabolism of Non-nucleoside Reverse Transcriptase Inhibitors [NCT00730223]Phase 133 participants (Actual)Interventional2004-03-31Completed
A Phase IIb Randomized, Partially Blinded, Dose-Finding Trial of TMC278 in Antiretroviral-Naive HIV-1 Infected Subjects [NCT00110305]Phase 2368 participants (Actual)Interventional2005-06-30Completed
A Phase I, Double-blind, Double-dummy, Randomized, Placebo Controlled and Active Controlled Trial to Evaluate the Effect of TMC278 25 mg Daily at Steady-state and the Effect of Efavirenz (EFV) 600 mg Daily at Steady-state on the QT/QTc Interval, in 2 Rand [NCT00744809]Phase 1120 participants (Actual)Interventional2008-08-31Completed
A Multicenter, Randomized, Double-Blind, Comparative Trial Of A Novel CCR5 Antagonist, UK-427,857, In Combination With Zidovudine/Lamivudine Versus Efavirenz In Combination With Zidovudine/Lamivudine For The Treatment Of Antiretroviral-Naive HIV-1 Infecte [NCT00098293]Phase 3916 participants (Actual)Interventional2004-11-30Completed
Adherence to a One Pill, Once-a-day Antiretroviral Regimen [NCT00990600]Phase 3212 participants (Actual)Interventional2008-04-30Completed
A Randomized Trial to Evaluate the Effectiveness of Antiretroviral Therapy Plus HIV Primary Care Versus HIV Primary Care Alone to Prevent the Sexual Transmission of HIV-1 in Serodiscordant Couples [NCT00074581]Phase 33,526 participants (Actual)Interventional2005-02-28Completed
The Effect of Rifampicin on the Pharmacokinetics of Intracellular Tenofovir-diphosphate and Tenofovir When Coadministered With Tenofovir Alafenamide Fumarate During the Maintenance Phase of Tuberculosis Treatment in TB/HIV-1 Coinfected Participants [NCT04424264]Phase 118 participants (Actual)Interventional2019-12-05Completed
Mecahnisms of Lipodystrophy in HIV-Infected Patients [NCT00457665]Phase 456 participants (Actual)Interventional2002-02-28Completed
A Phase 1, Open Label, Single Sequence, Three Period Study to Evaluate the Single Dose Pharmacokinetics of GSK1349572 100mg Versus 50mg and the Effect of Efavirenz 600mg Once Daily on the Pharmacokinetics, Safety and Tolerability of GSK1349572 50mg Once D [NCT01098526]Phase 112 participants (Actual)Interventional2010-03-16Completed
A Phase 4, Open Label, Randomized, Controlled Study to Assess the Effect on Lipid Profile of Switching From a Stable HAART Regimen of Fixed Dose Abacavir/Lamivudine (Kivexa) Plus Efavirenz, to Once Daily Atripla in Adult HIV-1 Infected Subjects With Raise [NCT00615810]Phase 4159 participants (Actual)Interventional2008-03-31Completed
A Prospective Longitudinal Pilot Study to Measure the Effect of Intensification With Raltegravir +/- a Protease Inhibitor (PI) or Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) on HIV-1 Levels in the Gut [NCT00884793]8 participants (Actual)Interventional2008-09-30Completed
Pharmacokinetic Interaction Between Coartem® and Either Nevirapine, Efavirenz or Rifampicin in HIV Positive Ugandan Patients [NCT00620438]Phase 490 participants (Anticipated)Interventional2008-02-29Active, not recruiting
A Single Sequence, 2-Period, Open-label Crossover Study in Healthy Subjects to Determine the Effect of a Moderate CYP3A4 Inducer on the Pharmacokinetics of Omaveloxolone [NCT05909644]Phase 120 participants (Actual)Interventional2023-07-05Completed
A Phase II Trial to Assess the Efficacy of Efavirenz as Second-line Monotherapy for the Treatment of Advanced Pancreatic Adenocarcinomas. [NCT00964171]Phase 272 participants (Anticipated)Interventional2008-08-31Recruiting
A Randomized, Double-Blind, Equivalence Trial Comparing Emtricitabine to Stavudine Within a Triple Drug Combination Containing Didanosine Plus Efavirenz in Antiretroviral-Drug Naive HIV-1 Infected Patients [NCT00006208]Phase 30 participants Interventional2000-08-31Active, not recruiting
Patient Preference, Sleep Quality, and Anxiety/Depression: Comparison of Raltegravir and Efavirenz [NCT00944957]60 participants (Anticipated)Interventional2009-11-30Recruiting
A Study Comparing Efficacy and Tolerance of Two Maintenance Strategies : a Monotherapy With Lopinavir/Ritonavir or a Single-tablet Triple Therapy by Efavirenz/Emtricitabin/Tenofovir in HIV-1 Infected Patients With HIV RNA Below 50 cp/mL [NCT00946595]Phase 2/Phase 3420 participants (Anticipated)Interventional2009-11-30Completed
Cellular Pharmacology of Tenofovir and Emtricitabine for HIV Prophylaxis (Cell Prep) [NCT01040091]Phase 134 participants (Actual)Interventional2009-12-31Completed
"The Effect of Prior Short Course Combination Antiretroviral Therapy Administered for the Prevention of Mother-to-Child Transmission (pMTCT) of HIV-1 on Subsequent Treatment Efficacy in Treatment-Nearly Naive Participants" [NCT00442962]Phase 454 participants (Actual)Interventional2007-05-31Completed
A Phase III, Randomized, Double-blind Trial of TMC278 25mg q.d. Versus Efavirenz 600mg q.d. in Combination With a Background Regimen Containing 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors in Antiretroviral-naive HIV-1 Infected Subjects. [NCT00543725]Phase 3680 participants (Actual)Interventional2008-06-30Completed
A Phase III, Randomized, Double-blind Trial of TMC278 25 mg q.d. Versus Efavirenz 600mg q.d. in Combination With a Fixed Background Regimen Consisting of Tenofovir Disoproxil Fumarate and Emtricitabine in Antiretroviral-naive HIV-1 Infected Subjects. [NCT00540449]Phase 3694 participants (Actual)Interventional2008-05-31Completed
A Phase I, Safety, Tolerability, and Pharmacokinetic Interaction Study of Single-Dose TMC207 and Efavirenz in Healthy Volunteers [NCT00992069]Phase 137 participants (Actual)Interventional2009-12-31Completed
The Stability and Bioequivalence of Tenofovir, Emtricitabine and Efavirenz (Atripla) in an Extemporaneously Prepared Oral Liquid Formulation Compared With the Commercially Available Tablet Formulation [NCT00862823]Phase 414 participants (Actual)Interventional2009-02-28Completed
Initiation of a Once Daily Regimen of Tenofovir, Lamivudine and Efavirenz After 4 Weeks Versus 12 Weeks of Tuberculosis Treatment in HIV-1 Infected Patients (Time Study) [NCT01014481]Phase 4156 participants (Actual)Interventional2009-10-31Terminated(stopped due to this study was ended prematurely by ethical committees with a reason of the final outcome was achieved with no longer recruitment was needed.)
Pharmacokinetic Interactions Between Antiretroviral Agents, Lopinavir/Ritonavir and Efavirenz and Antimalarial Drug Combinations, Artesunate/Amodiaquine and Artemether/Lumefantrine. [NCT00697892]Phase 138 participants (Actual)Interventional2005-07-31Completed
Nucleoside-Sparing Combination Therapy With Lopinavir/Ritonavir (LPV/r) + Raltegravir (RAL) vs. Efavirenz (EFV) + Tenofovir Disoproxil Fumarate + Emtricitabine (TDF/FTC) in Antiretroviral-Naïve Patients [NCT00752856]Phase 251 participants (Actual)Interventional2008-08-26Completed
Pharmacokinetics of Efavirenz and Lopinavir Nano-formulations in HIV Negative Healthy Volunteers: an Adaptive Design Study [NCT02631473]Phase 150 participants (Anticipated)Interventional2015-11-30Suspended(stopped due to Study is on hold whilst a grant application for further funding is put together)
Effects of 2 Initial Standard Antiretroviral Combinations Therapies on Lipid Metabolism in ARV-naive HIV-infected Subjects [NCT00759070]Phase 450 participants (Anticipated)Interventional2008-09-30Active, not recruiting
TBTC Study 23C: Intensive Pharmacokinetic Study of Intermittent Rifabutin and Isoniazid With Daily Efavirenz in Combination With Two Nucleoside Analogs for Treatment of HIV and Tuberculosis Co-infections [NCT00023413]Phase 220 participants Interventional1999-11-30Completed
CID 0805 - Treatment of Acute HIV Infection With a Once Daily Regimen of Emtricitabine, Tenofovir and Efavirenz - A Pilot Study of Response to Therapy and HIV Pathogenesis [NCT00924898]Phase 492 participants (Actual)Interventional2005-01-31Completed
Adjusting Antiretroviral Therapy Dosage Using Therapeutic Drug Monitoring [NCT00836212]Phase 412 participants (Anticipated)Interventional2008-03-31Recruiting
Open Randomized Study to Assess the Evolution of Plasma Lipid Profile by Lipidomic in Patients Infected With Human Immunodeficiency Virus (HIV-1) With Viral Suppression That Change Atripla® to Eviplera® Compared to Continue With Atripla® [NCT02547844]Phase 430 participants (Actual)Interventional2015-09-30Completed
Pharmacokinetics and Safety of Antiretroviral Drugs in Lactating Women and Breastmilk Fed Infants [NCT04862975]200 participants (Anticipated)Observational2024-01-08Not yet recruiting
Decay Kinetics of HIV With the Integrase Inhibitor Raltegravir [NCT00863668]0 participants (Actual)Interventional2009-03-31Withdrawn
CID 0708 - Sex, Aging and Antiretroviral Pharmacokinetics [NCT00666055]11 participants (Actual)Observational2008-03-31Completed
Steady-state Pharmacokinetics of Efavirenz (Sustiva/Stocrin) 400 mg Once Daily in the Presence of Rifampicin and Isoniazid (Rifinah or the Local Generics) [NCT02832778]Phase 135 participants (Anticipated)Interventional2016-11-21Recruiting
A Phase IIb Study to Select a Once Daily Dose of GSK1349572 Administered With Either Abacavir/Lamivudine or Tenofovir/Emtricitabine in HIV-1 Infected Antiretroviral Therapy Naive Adult Subjects [NCT00951015]Phase 2208 participants (Actual)Interventional2009-07-30Completed
[NCT00525239]60 participants (Anticipated)Interventional2004-03-31Recruiting
A Phase I, Open-label, Randomized, Crossover Trial in 20 Healthy Subjects to Investigate the Pharmacokinetic Interactions Between the Combination of Efavirenz and Tenofovir Disoproxil Fumarate and Different Dosages of Telaprevir. [NCT00828789]Phase 120 participants (Actual)Interventional2009-02-28Completed
Antiretroviral Therapy and the Hepatitis C Virus [NCT00545558]Phase 118 participants (Actual)Interventional2006-04-30Completed
Phase 3, Single Center, Controlled, Investigator-blinded, Randomized Matched Pair Design Study of CD4 Cell Recovery in HIV-1 Patients With Sustained Virologic Response Comparing Protease Inhibitor and Non-nucleoside Reverse Transcriptase Inhibitor Based T [NCT00966160]Phase 3215 participants (Actual)Interventional1999-01-31Completed
CCR5 Antagonism to Decrease the Incidence of the Immune Reconstitution Inflammatory Syndrome in HIV-Infected Patients [NCT00988780]276 participants (Anticipated)Interventional2009-12-31Active, not recruiting
A Phase III, Double Blind, Mulit-centre, Randomised Placebo Controlled, Pilot Study to Assess the Feasibility of Switching Individuals Receiving Efavirez With Continuing Central Nervous System (CNS) Toxicity to TMC125. [NCT00792324]Phase 324 participants (Actual)Interventional2008-06-30Completed
A Phase 1, Open-label, 2-part Study to Evaluate the Effect of Rifampin and Efavirenz on the Pharmacokinetics of Fedratinib in Healthy Adult Subjects [NCT03983239]Phase 132 participants (Actual)Interventional2019-06-21Completed
A Phase III Randomized, Open Label Trial to Evaluate Dolutegravir Versus Efavirenz 400 mg, Both Combined With Tenofovir Disoproxil Fumarate + Lamivudine for the Initial Management of HIV Infected Adults in Resource-limited Settings [NCT02777229]Phase 3616 participants (Actual)Interventional2016-07-31Completed
A Phase 4 Study of the Effect on Immune Reconstitution of a Lopinavir/Ritonavir-Based Versus an Efavirenz-based HAART (Highly Active Antiretroviral Therapy) Regimen in Antiretroviral-Naïve Subjects With Advanced HIV Disease [NCT00775606]Phase 415 participants (Actual)Interventional2008-10-31Terminated(stopped due to Study stopped 12/2010 due to poor enrollment. Only 15 of 60 needed enrolled.)
Changes in Liver Steatosis After Switching From Efavirenz to Raltegravir Among HIV/HCV-Coinfected Patients Receiving Two Nucleoside Analogs Plus Efavirenz: The Steral Study [NCT01900015]Phase 445 participants (Actual)Interventional2014-02-03Completed
Efavirenz and Ritonavir Influence on Human Brain Levo-acetylmethadol (LAAM) Disposition Assessed Using PET Imaging [NCT01935830]Early Phase 110 participants (Actual)Interventional2013-08-31Completed
Patient Preference, Sleep Quality, and Anxiety/Depression: A Randomized Comparison of Etravirine and Efavirenz [NCT00792584]50 participants (Anticipated)Interventional2008-11-30Completed
Study of Protease Inhibitor and/or Non-Nucleoside Reverse Transcriptase Inhibitor With Dual Nucleosides in Initial Therapy of HIV Infection [NCT00000919]900 participants InterventionalCompleted
A Randomized, Open-Label Study of the Long-Term Effectiveness of Three Initial Highly Active Antiretroviral Therapy (HAART) Strategies in HAART-Niave, HIV-Infected Persons [NCT00000922]1,710 participants InterventionalCompleted
A Phase III Randomized, Controlled Trial of Efavirenz (EFV) or Nelfinavir (NFV) in Combination With Fixed-Dose Combination Lamivudine/Zidovudine (3TC/ZDV) and Indinavir (IDV) in HIV-Infected Subjects With Less Than or Equal to 200 CD4 Cells/mm3 or Greater [NCT00000903]Phase 3444 participants InterventionalCompleted
Continued Salvage Anti-Retroviral Therapy With Abacavir, Amprenavir, and Efavirenz [NCT00001758]Phase 225 participants Interventional1997-11-30Completed
Once-daily Antiretroviral Therapy in HIV-1 Infected Patients With CD4+ Cell Counts Below 100 Cells/Mcl. A Prospective, Randomized, Multicentre, Open Clinical Study. [NCT00532168]Phase 4108 participants (Actual)Interventional2007-09-30Completed
Optimization of Antiretroviral Therapy [NCT02935075]Phase 4184 participants (Actual)Interventional2018-03-05Completed
Optimizing Malaria Treatment for HIV-Malaria Co-Infected Individuals by Addressing Drug Interactions Between Artemether-Lumefantrine and Efavirenz; a Randomized Controlled Trial [NCT04708496]Phase 4888 participants (Anticipated)Interventional2021-01-18Recruiting
Pharmacokinetics of Efavirenz During Treatment of HIV-1 Infected Subjects With Hepatic Impairment. [NCT00162097]Phase 121 participants (Actual)Interventional2004-11-30Completed
Multicentric Randomised Controlled Trial Assessing the Efficacy of Two Strategies of Structured Treatment Interruption of Highly Active Antiretroviral Therapy (HAART) Compared With a Continuous HAART in HIV- Infected Adults in Abidjan [NCT00158405]Phase 3840 participants (Actual)Interventional2002-12-31Completed
A Randomised, Open-label, 96-week Study Comparing the Safety and Efficacy of Three Different Combination Antiretroviral Regimens as Initial Therapy for HIV Infection. [NCT00335322]Phase 4329 participants (Actual)Interventional2007-02-28Completed
Randomized, Open-Label Evaluation of Efficacy of Once-Daily Protease Inhibitor and Once-Daily Non-Nucleoside Reverse Transcriptase Inhibitor-Containing Therapy Combinations for Initial Treatment of HIV-1 Infected Persons From Resource-Limited Settings (PE [NCT00084136]Phase 41,571 participants (Actual)Interventional2005-05-31Completed
A Pilot Study of Atazanavir/Ritonavir/Efavirenz as a Nucleoside Sparing Regimen [NCT00135343]Phase 360 participants Interventional2004-04-30Completed
A Single-Center, Single-Arm, Open-Label, Fixed-Sequence Phase I Drug-Drug Interaction Clinical Study of the Effect of Efavirenz on Pharmacokinetics of Maleate Pyrotinib in Chinese Healthy Subjects. [NCT04680091]Phase 120 participants (Actual)Interventional2020-11-12Active, not recruiting
Phase 3 Randomized Trial Evaluating the Virological Efficacy and the Tolerance of 4 New Simplified Antiretroviral Treatments in Naive HIV-1 Infected Patients in Dakar and Yaounde [NCT00573001]Phase 3120 participants (Actual)Interventional2008-07-31Completed
Hepatic Safety of Raltegravir-based and Efavirenz-based Antiretroviral Regimens in Antiretroviral-Naïve HIV-infected Subjects Co-Infected With Hepatitis C [NCT01147107]Phase 480 participants (Actual)Interventional2014-02-28Completed
A Randomized, Pilot Study on the Antiviral Activity and Immunological Effects of Lopinavir/Ritonavir vs. Efavirenz in Treatment-naïve HIV-Infected Patients With CD4 Cell Counts Below 100 Cells/mm3 [NCT00386659]Phase 460 participants InterventionalTerminated
Randomized, Controlled, Open Label, Multi-Center Phase III Trial Comparing the Safety and Antiviral Activity of a Protease-Containing Regimen (d4T/ddI/IDV/RTV) Versus a Protease-Sparing Regimen (d4T/ddI/EFV) and the Ability of Interleukin-2 to Purge HIV F [NCT00006154]Phase 3165 participants (Anticipated)InterventionalCompleted
The Study of Mechanisms of Lipodystrophy in HIV-Infected Patients [NCT00006190]Phase 40 participants Interventional2000-11-30Completed
Comparison of the Virologic Efficacy of Nelfinavir and/or DMP 266 (Efavirenz, EFV) in Combination With One or Two New Nucleoside Analogs in Nucleoside Experienced Subjects: A Roll-Over Study to ACTG 302/303 [NCT00001087]Phase 2300 participants InterventionalCompleted
Pharmacodynamics of Efavirenz 400mg in Treatment-naïve Chinese HIV-infected Patients in a Prospective Cohort Study [NCT04596488]25 participants (Actual)Interventional2017-06-01Completed
Treatment Outcome of Children With HIV Infection [NCT00476606]1,000 participants (Anticipated)Observational2003-03-31Active, not recruiting
Effect of Encapsulation Upon Efavirenz Pharmacokinetics [NCT01087814]Phase 416 participants (Actual)Interventional2010-02-28Completed
Effect of CYP2B6 Genotype and Efavirenz on the Disposition and Pharmacodynamic of Methadone and Tizanidine in Healthy Volunteers [NCT05789173]Early Phase 160 participants (Anticipated)Interventional2023-10-06Recruiting
Phase III Open-label Randomized Multicenter Trial to Assess the Non-inferiority of Raltegravir Compared With EFavirenz, Both in Combination With LAmivudine and TEnofovir, in ART-naïve HIV-1-infected Patients Receiving Rifampin for Active TuBerculosis [NCT02273765]Phase 3460 participants (Actual)Interventional2015-09-11Completed
Reducing Early Mortality and Early Morbidity by Empiric Tuberculosis Treatment Regimens (REMEMBER) [NCT01380080]Phase 4851 participants (Actual)Interventional2011-10-31Completed
Effect of Cytochrome P450 2B6 Genetic Polymorphism and Voriconazole on CYP2B6 Activity in Healthy Volunteers [NCT01104376]61 participants (Actual)Interventional2010-03-31Completed
Phase II Open-label Randomized Multicenter Trial to Compare the Efficacy and Safety of Two Different Doses of Raltegravir and Efavirenz, All in Combination With Tenofovir and Lamivudine, in Naive HIV-1-infected Patients Receiving Rifampin for Active Tuber [NCT00822315]Phase 2155 participants (Actual)Interventional2009-07-31Completed
Safety and Efficacy of the Universal Use of EFV-TDF-FTC and AZT-3TC-LPV/r Combinations in Pregnant and Breastfeeding Women to Prevent mother-to Child Transmission of HIV-1 o, Resource-limited Settings: A Multicentre Randomized Phase 3 Clinical Trial [NCT00936195]Phase 30 participants (Actual)Interventional2010-01-31Withdrawn(stopped due to faillure to obtain insurance because of refusal from insurance companies)
Dose-Finding and Pharmacogenetic Study of Efavirenz in HIV-infected and HIV/TB Co-infected Infants and Children 3 Months to Less Than 36 Months of Age [NCT00802802]Phase 167 participants (Actual)Interventional2010-02-10Completed
Adjunctive Therapy With Telmisartan Instituted With ART During Acute HIV Infection to Reduce the Establishment of CNS Reservoirs of HIV and Lymph Node Fibrosis [NCT02750059]Phase 221 participants (Actual)Interventional2015-01-31Completed
A Phase IIb, Multi-centre, Randomised, Double-blind, Active-controlled Trial Comparing the Neuropsychiatric Adverse Event Profile of Etravirine 400mg qd Versus Efavirenz 600mg qd in Combination With 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors [NCT00903682]Phase 2157 participants (Actual)Interventional2009-06-30Completed
Trial for the Optimal Timing of HIV Therapy After Cryptococcal Meningitis [NCT01075152]Phase 4177 participants (Actual)Interventional2010-11-30Completed
A Long Term Open-Label Extension Study Of Lersivirine For The Treatment Of HIV-1 Infection [NCT01254656]Phase 2108 participants (Actual)Interventional2011-02-28Terminated(stopped due to See termination reason in detailed description.)
A Randomized, Phase II, Placebo Controlled Trial of Abacavir (ABC, 1592U89) in Combination With Open-Label Indinavir Sulfate (IDV) and Efavirenz (EFV, DMP-266) in HIV-Infected Subjects With Nucleoside Analog Experience: A Rollover Study for ACTG 320 [NCT00001086]Phase 2300 participants InterventionalCompleted
ART Drug Dosage Adjustment Using FSCII in Chinese HIV-infected Population [NCT02632474]Phase 410 participants (Actual)Interventional2015-04-30Completed
A Phase II, Randomized, Open-Label Study of Maximally Assisted Therapy (MAT) Compared to Self-Administered Therapy (SAT) for the Treatment of HIV Infection in Antiretroviral Naive Subjects With CD4 Greater Than or Equal to 200 Cells/mm3 [NCT00001122]Phase 274 participants InterventionalCompleted
An Open-Label Drug Interaction Study to Investigate the Effects of Steady State Fenofibric Acid on the Single-Dose Pharmacokinetics of Efavirenz in Healthy Volunteers [NCT00960570]Phase 130 participants (Actual)Interventional2008-02-29Completed
Pharmacokinetics and Pharmacodynamics of the Etonogestrel Contraceptive Implant When Co-administered With Efavirenz [NCT01980342]Phase 41 participants (Actual)Interventional2014-10-31Terminated(stopped due to loss of funding)
Anti-retroviral Efficacy, Tolerance and Other Pharmacologic Interactions of the Non Nucleoside Analog Efavirenz in Association With Rifampicin to Treat Tuberculosis and AIDS [NCT00533390]Phase 4130 participants (Actual)Interventional2007-01-31Terminated(stopped due to Lack of financial support and low inclusion rate)
Efficacy and Safety of Concomitant Use of Nevirapine and Rifampicin in Antiretroviral Naive Patients Co-infected With HIV and Tuberculosis in India. [NCT01805258]Phase 3135 participants (Actual)Interventional2007-06-30Completed
A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE, 2-PERIOD STUDY TO ESTIMATE THE EFFECT OF MULTIPLE DOSE ABROCITINIB ON THE PHARMACOKINETICS OF SINGLE DOSES OF CAFFEINE, EFAVIRENZ, AND OMEPRAZOLE IN HEALTHY PARTICIPANTS [NCT05067439]Phase 113 participants (Actual)Interventional2021-10-21Completed
US Sustiva Oral Liquid Expanded Access Program: an Open-label, Multicenter Expanded Access Study of the Liquid Formulation of Sustiva (Efavirenz, DMP 266) [NCT00162227]0 participants Expanded Access2000-09-30No longer available
Analysis of Lipodystrophy in HIV-Infected Individuals A Prospective, Non-randomised, 48 Week Study of the Effect of PI Containing and Non-PI Containing Antiretroviral Regimens on the Expression of Adipocyte Specific Genes, Protein Levels and Cellular Stru [NCT00192660]Phase 480 participants (Actual)Interventional2003-02-28Completed
Implementing Anti-Retroviral Therapy in Resource-Constrained Settings: A Randomized Controlled Trial to Assess the Effect of Integrated Tuberculosis and HIV Care on the Incidence of AIDS-Defining Conditions or Mortality in Subjects Co-Infected With Tuberc [NCT00091936]592 participants (Anticipated)Interventional2009-08-31Completed
The Adult Antiretroviral Treatment and Resistance Study (Tshepo) [NCT00197613]Phase 3650 participants Interventional2002-12-31Completed
Disulfiram Interactions With HIV Medications: Clinical Implications [NCT00878306]Phase 140 participants (Actual)Interventional2008-11-30Completed
A Randomized, Double-blind, Double-simulated, Active-controlled,Phase III Clinical Study Evaluating the Efficacy and Safety of Azvudine Combined With Tenofovir Fumarate and Efavirenz in Hiv-infected Treatment Naive Patients [NCT04303598]Phase 3720 participants (Anticipated)Interventional2020-04-01Not yet recruiting
Pilot Trial to Evaluate the Efficacy and Tolerance of a Simple Once Daily Combined Regimen Including Tenofovir (TDF), Emtricitabine (FTC) and Efavirenz (EFV) in HIV-1 Infected Patients Naive to Prior Antiretroviral Treatment in Senegal [NCT00158457]Phase 340 participants (Actual)Interventional2004-06-30Completed
The Optimization of HAART for Chinese--a RCT Study [NCT02945163]Phase 4184 participants (Actual)Interventional2018-03-05Completed
Phase 2b Study to Select a Once Daily Oral Dose of GSK2248761 Administered With Tenofovir/Emtricitabine or Abacavir/Lamivudine in HIV-1 Infected Antiretroviral Therapy Naive Adult Subjects [NCT01231555]Phase 223 participants (Actual)Interventional2010-11-18Terminated
A Phase II Trial to Assess the Efficacy of Efavirenz in Metastatic Patients With Androgen-independent Prostate Cancer [NCT00964002]Phase 261 participants (Actual)Interventional2008-05-31Completed
A Phase II, Randomized, Open-Label Comparative Trial of Salvage Antiretroviral Therapies for HIV-Infected Individuals With Virological Evidence of Nelfinavir Treatment Failure as Reflected by Plasma HIV RNA Concentration of >= 1,000 Copies/ml [NCT00000918]Phase 2300 participants InterventionalCompleted
Early Antiretroviral Therapy in Resource Limited Settings in Patients With High CD4+ Cell Counts (EARLI) [NCT01479634]279 participants (Actual)Interventional2011-10-31Completed
The Pharmacokinetics of Co-formulated Emtricitabine/Tenofovir/Efavirenz in HIV-infected Patients With Smear-positive Pulmonary Tuberculosis in the Kilimanjaro Region, Tanzania [NCT00474435]Phase 230 participants (Anticipated)Interventional2008-11-30Recruiting
A Pharmacokinetic Study of Once Daily Efavirenz 400 mg Versus 600 mg in Thai HIV-1 Infected Subjects [NCT00476424]Phase 228 participants (Actual)Interventional2007-06-30Completed
Efavirenz-based Versus Nevirapine-based Antiretroviral Therapy Among HIV-infected Patients Receiving Rifampin [NCT00483054]Phase 3142 participants (Actual)Interventional2007-01-31Completed
Randomized Non-inferiority Trial Comparing the Nevirapine-based Antiretroviral Therapy Versus the Standard Efavirenz-based ART for the Treatment of HIV-TB Co-infected Patients on Rifampicin-based Therapy (ANRS 12146 CARINEMO) [NCT00495326]Phase 2/Phase 3570 participants (Actual)Interventional2007-12-31Completed
Randomized, Non-inferiority Trial Comparing a Dual Maintenance Therapy Strategy With Dolutegravir + Lamivudine (DTG/3TC) or Atazanavir/Ritonavir + Lamivudine (ATV/r+3TC) Versus the Standard WHO First Line Triple Therapy Tenofovir + Lamivudine + Efavirenz [NCT04022967]Phase 3480 participants (Actual)Interventional2020-09-21Active, not recruiting
Randomized, Double-Blinded Clinical Trial to Evaluate the Incidence and Severity of Neuropsychiatric Side Effects and Antiviral Efficacy of Efavirenz Given as a Stepped Dosage Over 2 Weeks Versus the Usual Dosage in HIV-Infected Patients. [NCT00556634]Phase 4114 participants (Actual)Interventional2006-04-30Completed
A Randomized Study to Evaluate the Effect of Switching From Efavirenz to Atazanavir/ Ritonavir on Lipoatrophy and Mitochondrial Dysfunction in HIV-infected Subjects With Good Virologic Suppression [NCT01194856]Phase 41 participants (Actual)Interventional2010-10-31Terminated(stopped due to Closed due to low enrollment)
A Pharmacokinetic Evaluation of Levonorgestrel Implant and Non-nucleoside Reverse Transcriptase Inhibitor (NNRTI)-Based Antiretroviral Therapy in HIV-infected Ugandan Women [NCT01789879]Phase 260 participants (Actual)Interventional2014-03-04Completed
A Pilot Project of Virologic, Pharmacologic and Immunologic Correlates of Gastrointestinal-Associated Lymphoid Tissue Immune Reconstitution Following Maraviroc Therapy [NCT00870363]Phase 444 participants (Actual)Interventional2009-04-30Completed
[NCT00810303]Phase 112 participants (Actual)Interventional2009-03-31Completed
A Phase II, Randomized Trial of Amprenavir as Part of Dual Protease Inhibitor Regimens (Placebo-Controlled) in Combination With Abacavir, Efavirenz, and Adefovir Dipivoxil Versus Amprenavir Alone in HIV-Infected Subjects With Prior Exposure to Approved Pr [NCT00000912]Phase 2475 participants InterventionalCompleted
Multi-Center, Open-Label Study of the Effect of Indinavir, Efavirenz, and Adefovir Dipivoxil Combination Therapy in Patients Who Have Failed Nelfinavir [NCT00002220]Phase 3120 participants InterventionalCompleted
Evaluation of Immune Reconstitution in HIV Infected Patients Treated With Fortovase (Saquinavir) SGC QD Plus Ritonavir QD Plus 2 NRTIs Vs Efavirenz QD Plus 2 NRTIs [NCT00002448]Phase 340 participants Interventional1999-10-31Completed
An Open Label, Randomized Study to Compare Antiretroviral Therapy (ART) Initiation When CD4 is Between 15% to 24% to ART Initiation When CD4 Falls Below 15% in Children With HIV Infection and Moderate Immune Suppression [NCT00234091]Phase 3300 participants (Actual)Interventional2006-04-30Completed
An Open-Label, Randomized Study to Determine the Impact of Antiretroviral Treatment in HCV/HIV-Coinfected Subjects With High CD4+ Cell Count on the Efficacy of Hepatitis C Treatment With Pegylated Interferon Alfa-2A and Ribavirin [NCT00100581]2 participants (Actual)InterventionalCompleted
A Multicenter, Randomized, Open Label, Clinical Trial Comparing a QD Regimen of Didanosine, Lamivudine and Efavirenz With a Standard BID Regimen of Zidovudine, Lamivudine and Efavirenz in the Starting Treatment of Human Immunodeficiency Virus Infection (G [NCT00256828]Phase 4360 participants Interventional2004-06-30Completed
Open-label Randomized Multicenter Study of Once Daily Antiretroviral Treatment Regimen Comparing Ritonavir Boosted Atazanavir to Efavirenz [NCT00280969]Phase 371 participants (Actual)Interventional2005-09-30Completed
Safeguard the Household: A Study of HIV Antiretroviral Therapy Treatment Strategies Appropriate for a Resource Poor Country [NCT00080522]813 participants Interventional2005-02-28Completed
A Randomized Clinical Trial to Determine the Efficacy of Early Versus Standard Antiretroviral Therapy in HIV Infected Adults With CD4+ T Cell Counts Between 200 and 350 Cells/mm3 [NCT00120510]816 participants (Actual)Interventional2007-07-31Completed
A Randomized, Open-Label Study Assessing Safety, Tolerability and Efficacy of an Induction-Maintenance Treatment Strategy Including Lopinavir/Ritonavir Plus Tenofovir Disoproxil Fumarate and Emtricitabine Versus Efavirenz Plus Tenofovir Disoproxil Fumarat [NCT00121017]Phase 2200 participants InterventionalWithdrawn
HAART Regimen Comprising 3TC + ddI + EFV in Once-daily Administration in HIV-1 Infected Children in Burkina Faso [NCT00122538]Phase 252 participants (Actual)Interventional2006-02-28Completed
Multicentre, Open Label, Prospective, Randomised Clinical Trial of an Antiretroviral Simplification Treatment With Efavirenz + Abacavir + 3TC Once Daily [NCT00314626]Phase 399 participants (Actual)Interventional2004-11-30Completed
Virological and Clinical Anti-HBV Efficacy of Tenofovir and Emtricitabine in Antiretroviral Naïve Patients With HIV/HBV co-Infection [NCT00127959]Phase 424 participants Interventional2004-03-31Completed
A Pilot Study of Safety, Effectiveness, and Adherence of Lamivudine/Zidovudine and Efavirenz (3TC/ZDV + EFV) to Treat HIV-1 Infection in Senegal [NCT00100568]44 participants (Actual)Interventional2006-07-31Completed
A Randomized Comparison of Protease Inhibitor-based Versus Non-nucleoside Reverse Transcriptase Inhibitor-based Antiretroviral Therapy for Initial Treatment of Individuals With AIDS-related Kaposi's Sarcoma in Sub-Saharan Africa [NCT00444379]Phase 4224 participants (Actual)Interventional2007-04-30Completed
A Phase I, 2-panel, Open-label, Randomized, Crossover Trial in Healthy Subjects to Investigate the Pharmacokinetic Interaction Between TMC435 and Antiretroviral Agents, Efavirenz and Raltegravir, at Steady State [NCT01241773]Phase 148 participants (Actual)Interventional2010-10-31Completed
A Single-centre, Single-arm, Open-label and Fixed-sequence Drug-drug Interaction Study to Evaluate the Effect of Efavirenz on the Pharmacokinetics of SHR2150 in Healthy Chinese Subjects [NCT05141422]Phase 120 participants (Actual)Interventional2021-12-13Active, not recruiting
A Phase III, Double-Blind, Placebo-Controlled, Multicenter Study to Determine the Effectiveness and Tolerability of the Combination of DMP 266 and Indinavir Versus Indinavir in HIV-Infected Patients Receiving Nucleoside Analogue (NRTI) Therapy [NCT00002393]Phase 3300 participants InterventionalCompleted
A Study of the Effects of Combination Antiretroviral Therapy in Acute HIV-1 Infection With an Emphasis on Immunological Responses [NCT00001119]288 participants Interventional1999-10-31Completed
The Effect of Efavirenz and Nelfinavir on the Pharmacokinetics of Hydroxymethylglutaryl Coenzyme A Reductase Inhibitors [NCT00017758]Phase 156 participants InterventionalCompleted
Canadian Sustiva Oral Liquid Expanded Access Program: An Open-Label, Multicenter Expanded Access Study of the Liquid Formulation of Sustiva (Efavirenz, DMP266) [NCT00162188]0 participants Expanded Access2001-05-31No longer available
Pilot Study on Efficacy and Safety of a Once Daily FTC, ddI, Efavirenz Combination in Antiretroviral Naive HIV Infected Adults. ANRS 091 MONTANA [NCT00196599]Phase 239 participants Interventional1999-02-28Completed
Treatment Options for Protease Inhibitor-exposed Children [NCT01146873]Phase 3300 participants (Actual)Interventional2010-07-31Completed
Randomised Controlled Trial of Immediate Versus Deferred Antiretroviral Therapy for HIV-Associated Tuberculous Meningitis [NCT00433719]253 participants (Actual)Interventional2005-09-30Active, not recruiting
Evaluation of Safety and Efficacy of Two Different Once Daily Anti Retroviral Treatment Regimens Along With Anti-tuberculosis Treatment in Patients With HIV-1 and Tuberculosis [NCT00332306]Phase 3180 participants (Anticipated)Interventional2006-06-30Active, not recruiting
A Pilot Study of the Pharmacokinetic Interactions Between the Hormonal Emergency Contraception, Plan B, and Efavirenz [NCT00482963]Phase 124 participants (Actual)Interventional2007-05-31Completed
Efficacy and Safety of 400 mg Efavirenz Versus Standard 600 mg Dose in HIV/TB Co-infected Patients Receiving Rifampicin Based Anti-TB Therapy [NCT04513379]Phase 380 participants (Anticipated)Interventional2020-11-01Not yet recruiting
A Randomized Controlled Trial to Compare the Effects of Highly Active Antiretroviral Therapy (HAART) Versus Statin Therapy on Endothelial Function and Markers of Inflammation/Coagulation In HIV-Infected Individuals With High CD4 Cell Counts [NCT01515813]Phase 20 participants (Actual)Interventional2011-11-30Withdrawn(stopped due to On 05/08/12, team working on revising protocol and re-open study under version 2.0)
The Neurocognitive Sub Study of Encore1:A Randomised, Double-Blind, Placebo-Controlled, Clinical Trial to Compare the Safety and Efficacy of Reduced Dose Efavirenz (EFV) With Standard Dose EFV Plus 2N(t)RTI in Antiretroviral-naïve HIV-Infected Individuals [NCT01516060]Phase 371 participants (Actual)Interventional2012-01-31Completed
Ex Vivo Study of Immune-Reconstitution Kinetics in HIV-infected ARV-naive Subjects, With Advanced Disease, Starting a Darunavir/Ritonavir or Efavirenz Based HAART (IMMUNO Study) [NCT01541085]33 participants (Actual)Observational2011-12-31Completed
A Feasibility Study of Lamivudine/Zidovudine (3TC/ZDV) Plus Efavirenz (EFV) as Initial Therapy of HIV-1 Infected Patients in a Rural Area of China [NCT00100594]100 participants (Anticipated)Interventional2005-05-31Completed
Pilot Trial Evaluating Once Daily Triple Combination Antiretroviral Therapy With Tenofovir-Emtricitabine and Efavirenz in HIV-1 Infected Patients With Mycobacterium Tuberculosis Infection ANRS129 BKVIR [NCT00115609]Phase 370 participants (Actual)Interventional2006-01-31Completed
Phase II, Randomized, Open-Label Study of Switching to Protease Inhibitor-Sparing Regimens for Improvement of Metabolic Abnormalities [NCT00021463]Phase 2342 participants InterventionalCompleted
Effect of Change to a Nucleoside Reverse Transcriptase Inhibitor (NRTI)-Sparing Regimen of Efavirenz (EFV) and Lopinavir/Ritonavir (LPV/r) on Liver Histology in HIV-1-Infected Individuals With Lactic Acidemia and Persistent Alanine Aminotransferase (ALT) [NCT00023218]0 participants (Actual)InterventionalWithdrawn
A Phase IV Multicenter Study of the Efficacy and Safety of 48-Week Induction Treatment With TRIZIVIR (Abacavir 300 Mg/Lamivudine 150 Mg/Zidovudine 300 Mg Combination Tablet BID) With Efavirenz (600 Mg QD) Followed by 48-Week Randomized, Open-Label, Mainte [NCT00011895]Phase 4400 participants Interventional2001-02-28Active, not recruiting
Randomized Study to Evaluate Immediate Potent Antiretroviral Therapy for HIV-Infected Subjects With CD4 Cell Counts Less Than 350 Cells/mm3 Admitted to Intensive Care Areas With an AIDS-Defining Illness, Pneumonia, or Sepsis [NCT00028327]Phase 3250 participants InterventionalCompleted
A Phase I/II, Open-Label, AUC-Controlled Study to Determine the Pharmacokinetics, Safety, Tolerability, and Antiviral Activity of DMP 266 (Efavirenz) in Combination With Nelfinavir in Children [NCT00000893]Phase 1103 participants (Actual)Interventional1997-10-31Completed
A Randomized, Controlled Trial of Two Potent, Simplified Regimens Utilizing A Protease Inhibitor-Sparing Regimen Versus A Nucleoside-Sparing Regimen for HIV-Infected Subjects Who Participated in ACTG 388 or Who Responded to A First Potent Combination Regi [NCT00014937]240 participants InterventionalCompleted
Pharmacokinetic Interactions Between Ritonavir, Amprenavir and Efavirenz and Nelfinavir, Amprenavir, and Efavirenz in People Infected With HIV [NCT00001766]Phase 122 participants Interventional1998-08-31Completed
A Phase III, Randomized, Open-label, Multicenter Study of the Safety and Efficacy of Efavirenz Versus Tenofovir When Administered in Combination With the Abacavir/Lamivudine Fixed-dose Combination Tablet as a Once-daily Regimen in Antiretroviral-naive HIV [NCT00053638]Phase 3345 participants Interventional2003-02-28Completed
A Comparative Trial of Protease-Containing and Protease-Sparing HAART Regimens in HIV-Infected Adolescents With an Evaluation of Therapeutic Drug Monitoring [NCT00075907]Phase 3240 participants Interventional2004-07-31Completed
Study to Evaluate the Effect of Efavirenz Coadministration on the Pharmacokinetics of the Active Moieties of a Combined Oral Contraceptive Containing Ethinyl Estradiol and Norgestimate in Healthy Female Subjects [NCT00399685]Phase 128 participants (Actual)Interventional2006-12-31Completed
Phase III, Randomized, Double-Blind Comparison of Three Protease Inhibitor-Sparing Regimens for the Initial Treatment of HIV Infection [NCT00013520]Phase 31,125 participants InterventionalCompleted
An Open-Label, Non-Randomized Study of Pharmacokinetic Interactions Between Depo-Medroxyprogesterone Acetate (DMPA, Depo-Provera) and Selected Protease Inhibitor (PI) and Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI) Therapies Among HIV-Infected W [NCT00016601]76 participants Interventional2001-06-30Completed
Intensive Pharmacokinetics of the Nelfinavir-Rifabutin Interaction in Patients With HIV-Related Tuberculosis Treated With a Rifabutin-Based Regimen [NCT00018083]0 participants InterventionalRecruiting
A Phase I/II, Open Label Study to Evaluate the Ability of Combination Therapy With ABT-378/Ritonavir (Kaletra), Lamivudine (Epivir), Efavirenz (Sustiva)and Tenofovir DF to Completely Suppress Viral Replication in Subjects Infected With HIV-1 [NCT00038220]Phase 240 participants Interventional2000-07-31Completed
An Open Label, Phase II Study of Amprenavir/Ritonavir, Saquinavir/Ritonavir or Efavirenz in HIV-Infected Subjects Following Failure With Kaletra (ABT-378/Ritonavir) as Their First Protease Inhibitor Based HAART [NCT00038532]Phase 224 participants Interventional2001-04-30Completed
A Phase III, Randomized, Open-Label Comparison of Lopinavir/Ritonavir Plus Efavirenz Versus Lopinavir/Ritonavir Plus 2 NRTIs Versus Efavirenz Plus 2 NRTIs as Initial Therapy for HIV-1 Infection [NCT00050895]Phase 3775 participants InterventionalCompleted
Multicenter, Pilot Study of Telbivudine (LdT) Anti-HBV Treatment Prior to the Initiation of Highly Active Antiretroviral Therapy Containing Lamivudine in Subjects Coinfected With HBV and HIV [NCT00051090]0 participants (Actual)InterventionalWithdrawn
Augmenting the Magnitude of HAART-Induced Immune Restoration With the Use of Cyclosporine [NCT00031070]Phase 240 participants InterventionalCompleted
A Retrospective Study to Compare the 3-Year Antiviral Efficacy of Nevirapine and Efavirenz in Combination With D4t and 3tc in 2NN Patients and of Trizivir Versus Trizivir Plus Nevirapine in CHARM Patients [NCT00127972]Phase 4763 participants (Actual)Interventional2004-02-29Completed
A Randomized, Open-Label Study Exploring a Simplified Kaletra® (Lopinavir/Ritonavir)-Based Therapy Versus a Sustiva® (Efavirenz)-Based Standard of Care in Previously Non-Treated HIV-Infected Subjects [NCT00075231]Phase 2150 participants Interventional2003-12-31Completed
Feasibility Study of a Once Daily Antiretroviral Regimen for HIV-Infected Patients With CD4 Below 200/mm3, in Hô Chi Minh City, Vietnam [NCT00158470]Phase 3100 participants (Actual)Interventional2003-09-30Completed
A Phase 3, Randomized, Double-Blind, Multicenter Study of the Treatment of Antiretroviral-naive, HIV-1-Infected Patients Comparing Tenofovir Disoproxil Fumarate Administered in Combination With Lamivudine and Efavirenz vs. Stavudine, Lamivudine and Efavir [NCT00158821]Phase 3180 participants (Anticipated)Interventional2000-03-31Completed
Boosted PI VS. NNRTI Based Therapy as Initial Treatment for HIV-1 Infected Patients With Advanced Disease [NCT00162643]Phase 4300 participants Interventional2004-12-31Recruiting
Virological and Clinical Anti-HBV Efficacy of Tenofovir in Antiretroviral naïve Patients With HIV/HBV Co-infection [NCT00192595]Phase 436 participants (Actual)Interventional2004-01-31Completed
Phase II Randomized Trial Comparing Efficacy and Safety of the Maintenance of a HAART Association Protease Inhibitor Containing Versus a Once Daily Antiretroviral Triple Association, in HIV Adult Patients With Undetectable Viral Load.ANRS 099 ALIZE [NCT00196612]Phase 3350 participants Interventional2001-04-30Completed
Combination of Efavirenz & Truvada (COMET Study): Phase 4 Evaluation of Switching Twice Daily Combivir to Once-Daily Regimen Co-Formulated Truvada in Virologically Suppressed HIV Infected Patients Taking Efavirenz. [NCT00224458]Phase 4400 participants Interventional2004-09-30Completed
Randomized, Open-Label 2x2 Factorial Study to Compare the Safety and Efficacy of Different Combination Antiretroviral Therapy Regimens in Treatment Naive Patients With Advanced HIV Disease and/or CD4+ Cell Counts Less Than 200 Cells/MicroL [NCT00342355]Phase 41,771 participants (Actual)Interventional2004-01-31Completed
A Phase IV 48-Week, Randomized, Open-Label, Multicenter Trial of Abacavir (300mg BID)/Efavirenz (600mg QD)/Didanosine (400mg QD) +/- Hydroxyurea (500mg BID) in HIV-1 Infected Subjects Failing Initial Therapy With 3TC/ZDV (or d4T) +/- Protease Inhibitor(s) [NCT00005018]Phase 4150 participants Interventional1999-07-31Completed
Optimizing Pediatric HIV-1 Treatment in Infants With Prophylactic Exposure to Nevirapine, Nairobi, Kenya (6-12 Month RCT) [NCT00427297]Phase 334 participants (Actual)Interventional2007-09-30Terminated(stopped due to There is no longer equipoise. DSMB recommended termination.)
Open Label Randomized Controlled Trial to Assess the Impact of Prophylactic Exposure to Tenofovir Gel on the Efficacy of Subsequent Tenofovir-containing Antiretroviral Therapy on Viral Suppression [NCT01387022]59 participants (Actual)Interventional2011-06-30Completed
A Study in Underrepresented Patient Population or Regimen Tolerability: SUPPoRT [NCT00727597]Phase 3101 participants (Actual)Interventional2008-07-31Completed
Influence of Nevirapine on HCV Viral Load Among HIV/HCV-coinfected Patients [NCT01277627]60 participants (Anticipated)Interventional2011-01-31Not yet recruiting
Pharmacokinetic Interactions Between Antiretroviral Agents, Lopinavir/Ritonavir and Efavirenz and Antimalarial Drug Combination, Artemether/Lumefantrine [NCT00266058]Phase 133 participants (Actual)Interventional2005-12-31Completed
Molecular, Biochemical and Clinical Differences Between Stavudine and Tenofovir, Each Combined With Lamivudine and Efavirenz in South African HIV-infected Patients [NCT01601899]Phase 460 participants (Actual)Interventional2008-10-31Terminated(stopped due to DSMB decision to begin closeout process in view of April 2010 SA HAART guideline)
Open, Parallel and Randomised Pilot Clinical Trial to Evaluate the Utility of the Therapeutic Monitoring of Plasma Levels of Efavirenz in Hiv-Infected Patients Initiating an Antiretroviral Treatment Regimen With Sustiva [NCT00299091]Phase 431 participants (Actual)Interventional2006-09-30Completed
Single-center, Randomized, Open-label Study to Investigate the Effect of Single-dose Famotidine and Multiple-dose Efavirenz on the Pharmacokinetics of Daridorexant in Healthy Male Subjects [NCT04390334]Phase 124 participants (Actual)Interventional2020-05-13Completed
Enfuvirtide for the Initial Phase of Antiretroviral Therapy in HIV-infected Patients With High Risk of Clinical Progression : ANRS 130 APOLLO [NCT00302822]Phase 3195 participants (Actual)Interventional2006-04-30Completed
Cross-sectional Study for the Characterisation of the Pharmacokinetic Parameters of Protease Inhibitors and Non-nucleoside Analog Reverse Transcriptase Inhibitors in the Spanish Population of HIV-infected Subjects [NCT00307502]Phase 1675 participants (Actual)Interventional2005-01-31Completed
Viral Decay Kinetics During Induction Therapy With or Without the Use of Enfuvirtide in HAART-naÃ-ve Patients With Advanced HIV [NCT00344760]Phase 42 participants (Anticipated)Interventional2005-01-31Completed
BREATHER (PENTA 16) Short-Cycle Therapy (SCT) (5 Days on/2 Days Off) in Young People With Chronic HIV-infection [NCT01641016]Phase 2/Phase 3160 participants (Anticipated)Interventional2011-04-30Active, not recruiting
Comparative Bioavailability Study of Two Efavirenz 600 mg Formulations in Healthy Volunteers. [NCT01704898]Phase 412 participants (Actual)Interventional2013-04-30Completed
A Prospective, Multicenter, Open, Randomized Phase 2a Trial to Confirm a Sustained Virological Suppression Defined as HIV-RNA <50 Copies/ml of 3 Different Doses of Fozivudine in Context to a Standard Zidovudine Based Antiretroviral Therapy Regimen After 2 [NCT01714414]Phase 2120 participants (Actual)Interventional2012-12-31Completed
Influence of Efavirenz and Ritonavir on Human Brain P-Glycoprotein Activity Using PET Imaging [NCT01668147]Phase 1/Phase 213 participants (Actual)Interventional2012-08-31Completed
Virological and Immunological Safety of a Dose Reduction Strategy Antiretroviral Regimen With Efavirenz / Tenofovir / Emtricitabine [NCT01778413]Phase 460 participants (Actual)Interventional2013-05-31Completed
The Efficacy and Safety of Biktarvy in Treatment-Naïve Late Presenters With HIV-1 Infection [NCT04296695]Phase 4250 participants (Anticipated)Interventional2021-07-14Active, not recruiting
A Phase II Study of the Prolongation of Virologic Success (ACTG 372A) and Options for Virologic Failure (ACTG B/C/D) in HIV-Infected Subjects Receiving Indinavir in Combination With Nucleoside Analogs: A Rollover Study for ACTG 320 [NCT00000885]Phase 2440 participants InterventionalCompleted
Phase II Randomized, Open-Label Study of Maintenance of HIV RNA Suppression After Switching to ddI/d4T/HU vs. ddI/d4T/EFV vs. Continuing the Pre-Entry Protease Inhibitor Regimen [NCT00000939]Phase 2150 participants InterventionalCompleted
A Phase II, 48-Week, Open-Label Study Designed to Evaluate the Safety, Tolerability, and Efficacy of a Simplified Dosing Regimen of Viracept (Nelfinavir Mesylate) 1250 Mg BID, Crixivan (Indinavir Sulfate) 1200mg q12h, and Sustiva (Efavirenz; DMP-266) 600 [NCT00002235]Phase 26 participants InterventionalCompleted
A Randomized Evaluation of Antiretroviral Therapy Alone or With Delayed Chemotherapy Versus Antiretroviral Therapy With Immediate Adjunctive Chemotherapy for Treatment of Limited Stage AIDS-KS in Resource-Limited Settings (REACT-KS) AMC 067 [NCT01352117]Phase 3192 participants (Actual)Interventional2011-11-18Completed
A Study on ART Naïve Patients On Different Regimens to Treat Hiv (a Phase 4 Study) [NCT01445223]Phase 4242 participants (Actual)Interventional2004-04-30Completed
A Randomised, Double-blind, Placebo-controlled, Trial to Compare the Safety and Efficacy of Reduced Dose Versus Standard Dose EFV Plus Two Nucleotides (N(t)RTI) in Antiretroviral-naïve HIV-infected Adults Over 96 Weeks [NCT01011413]Phase 3636 participants (Actual)Interventional2011-08-31Completed
A Randomized, Open-Label Superiority Trial Comparing Emtricitabine to Abacavir Within a Triple Drug Combination in Antiretroviral-Drug Naive HIV-1 Infected Patients [NCT00002362]Phase 30 participants Interventional1999-08-31Suspended
A Randomized, Placebo-Controlled Study of the Safety and Efficacy of Efavirenz, Didanosine, and Stavudine in Combination With or Without Hydroxyurea in Antiretroviral Naive or Experienced HIV-Infected Patients [NCT00002230]Phase 3100 participants InterventionalCompleted
A Phase II/III 48-Week, Randomized, Double-Blind, Controlled, Multicenter Study to Evaluate the Efficacy and Safety of Lamivudine 300mg Once Daily Vs. Lamivudine 150mg BID in Combination With Zidovudine 300mg BID and Efavirenz 600mg Once Daily in Antiretr [NCT00004852]Phase 20 participants Interventional1999-09-30Completed
An Open-Label Study to Evaluate the Safety, Tolerance, Antiviral Activity, and Pharmacokinetics of Emtricitabine in Combination With Efavirenz and Didanosine in a Once-Daily Regimen in HIV Infected, Antiretroviral Therapy Naive or Very Limited Antiretrovi [NCT00016718]Phase 1/Phase 243 participants (Actual)Interventional2001-08-31Completed
A Phase II Study of ABT-378/Ritonavir and Efavirenz in Multiple Protease Inhibitor-Experienced Subjects [NCT00004582]Phase 20 participants InterventionalCompleted
A Phase III, Open-label, Single Centre, Single-arm, Pilot Study to Assess the Feasibility of Switching, Individuals Receiving Efavirenz With Continuing Central Nervous System (CNS) Toxicity, to Raltegravir [NCT01195467]Phase 340 participants (Actual)Interventional2010-10-31Completed
The EFV Central Nervous System Exposure Sub-study of Encore1: A Randomised, Double-blind, Placebo-controlled, Clinical Trial to Compare the Safety and Efficacy of Reduced Dose Efavirenz (EFV) With Standard Dose EFV Plus Two Nucleotide Reverse Transcriptas [NCT01451333]Phase 332 participants (Actual)Interventional2011-09-30Completed
Effect of Moringa Oleifera (Moringa, Drumstick/Horseradish Tree) on The Pharmacokinetics of Efavirenz and Nevirapine In-vivo. [NCT01410058]19 participants (Actual)Observational2013-01-31Completed
A Proof-of-Concept Clinical Research Study of Efavirenz in Patients With Alzheimer's Disease [NCT03706885]Phase 15 participants (Actual)Interventional2018-05-05Completed
A Phase III Study Comparing the Antiviral Efficacy and Safety of BMS-232632 With Efavirenz; Each in Combination With Fixed Dose Zidovudine-Lamivudine [NCT00013897]Phase 30 participants Interventional2001-02-28Completed
A Phase I, Three-Arm Safety, Tolerability, and Pharmacokinetic Interaction Study of PA-824, an Investigational Nitroimidazole for the Treatment of Tuberculosis, Together With Efavirenz, Ritonavir-Boosted Lopinavir, or Rifampin [NCT01571414]Phase 152 participants (Actual)Interventional2012-05-31Completed
A Randomized Study of the Virologic Efficacy of Different Antiretroviral (AR) Treatment Strategies in HIV-Infected Individuals With Detectable Plasma HIV RNA Measurements After at Least 16 Weeks on Their Initial Protease Inhibitor-Containing AR Regimens [NCT00000914]800 participants InterventionalCompleted
A Phase II, 48 Week, Open-Label Study Designed to Evaluate the Efficacy, Safety, Tolerability, and Pharmacokinetics of a Simplified Dosing Regimen of Preveon (Adefovir Dipivoxil; bis-POM PMEA), Videx (Didanosine; ddI), Sustiva (Efavirenz; DMP-266), and Ep [NCT00002234]Phase 225 participants InterventionalCompleted
A Phase II, 24-Week, Open-Label Study Designed to Evaluate the Safety, Tolerability, and Efficacy of Novel Quadruple-Combination Therapy With Preveon (Adefovir Dipivoxil; Bis-POM PMEA), Abacavir (1592U89), Sustiva (Efavirenz; DMP-266), and Amprenavir (141 [NCT00002419]Phase 225 participants InterventionalCompleted
A Phase II, Open-Label, Multicenter Study to Characterize the Effectiveness and Safety of Efavirenz in Combination With Stavudine and Lamivudine in Antiretroviral Therapy-Naive HIV-Infected Patients [NCT00002227]Phase 260 participants InterventionalCompleted
A Controlled Phase 2 Trial Assessing Three Doses of T-20 in Combination With Abacavir, Amprenavir, Ritonavir, and Efavirenz in HIV-1 Infected Adults [NCT00002239]Phase 268 participants Interventional1999-05-31Completed
An Open-Label, Proof of Concept, Randomized Trial Comparing a LPV/r-Based to an nNRTI-Based Antiretroviral Therapy Regimen for Clearance of Plasmodium Falciparum Subclinical Parasitemia in HIV-infected Adults With CD4+ Counts >200 and <500 Cells/mm^3 [NCT01632891]Phase 1/Phase 252 participants (Actual)Interventional2014-01-10Completed
A Randomized, Open-Label, Study of Nelfinavir or Efavirenz in HIV-1 Infected, Antiretroviral Naive Patients [NCT00005000]Phase 4200 participants Interventional1999-12-31Active, not recruiting
Pharmacokinetic Interaction Studies of Amprenavir (APV), Efavirenz (EFV), and a Second Protease Inhibitor in HIV-Seronegative Volunteers [NCT00005762]90 participants Interventional2001-03-31Completed
A Phase IV, Open-Label, Randomized Study to Compare the Efficacy and Safety of Epivir/Ziagen/Zerit (3TC/ABC/d4T) Versus Epivir/Ziagen/Sustiva (3TC/ABC/EFV) Versus Epivir/Ziagen/Agenerase/Norvir (3TC/ABC/APV/RTV) for 96 Weeks in the Treatment of HIV-1 Infe [NCT00005017]Phase 4300 participants InterventionalActive, not recruiting
A Phase IV, Open-Label, Multicenter Study of the Efficacy and Safety of Quadruple Combination Antiretroviral Therapy With Combivir (Lamivudine 150mg/Zidovudine 300mg) BID, Ziagen (Abacavir) 300mg BID, and Sustiva (Efavirenz) 600mg QD for 24 Weeks, Followe [NCT00004585]Phase 440 participants Interventional1999-10-31Completed
A Multicenter, Open, Randomized, Forty-Eight-Week, Pilot Study to Evaluate the Activity, Safety, and Pharmacokinetics of Indinavir Sulfate, 1200 Mg q 12h and DMP 266, 300 Mg q 12h Versus Indinavir Sulfate, 1000 Mg q 8h and DMP 266, 600 Mg q.h.s. [NCT00002387]80 participants InterventionalCompleted
An Open Label, Randomized, Multicenter Study to Evaluate Fortovase (Saquinavir) SGC QD, Norvir (Ritonavir) QD Plus Two NRTIs Vs Sustiva (Efavirenz) QD Plus Two NRTIs in HIV Infected Patients [NCT00002447]Phase 3146 participants Interventional1999-10-31Completed
A Phase II Study Evaluating the Safety and Antiviral Activity of Combination Therapy With 1592U89, 141W94 and DMP 266 in HIV-1 Infected Subjects With Detectable HIV-1 Plasma RNA Despite Treatment With a Protease Inhibitor Containing Regimen [NCT00002213]Phase 280 participants InterventionalCompleted
A Phase II, Open-Label, Multicenter Study to Characterize the Effectiveness and Safety of Efavirenz in Combination With Stavudine and Didanosine in Antiretroviral Therapy-Naive HIV-Infected Patients [NCT00002225]Phase 260 participants InterventionalCompleted
Open-Label, Multiple Dose Study to Determine the Relative Bioavailability of Atazanavir (ATV) 400 mg Administered With Ritonavir (RTV) and Efavirenz (EFV) Compared to Atazanavir 300 mg Administered With Ritonavir Alone in Healthy Subjects [NCT00357188]Phase 122 participants Interventional2006-07-31Completed
Phase IV, Open-Label, Randomized, Multicenter Study Evaluating Efficacy and Tolerability of Single Tablet Regimen of Efavirenz/Emtricitabine/Tenofovir DF Compared to Unmodified HAART in HIV-1 Infected Subjects Who Have Achieved Virological Suppression on [NCT00365612]Phase 4300 participants (Anticipated)Interventional2006-07-31Completed
Neuropsychiatric Adverse Effects of Efavirenz in Children Living With HIV in Kilimanjaro, Tanzania [NCT03227653]144 participants (Actual)Observational2017-06-19Completed
Investigating Influence of Pregnancy-induced Changes in Antiretroviral Pharmacokinetics, Together With Polymorphisms in Drug Disposition Genes, on Viral Decay Dynamics in HIV Positive Women Starting Therapy Late in Pregnancy and Postpartum [NCT03284645]194 participants (Actual)Observational2017-12-22Completed
Pharmacokinetics Study of Tenofovir in HIV-infected Thai Children Using Tenofovir-based Regimen [NCT02404259]32 participants (Actual)Interventional2010-06-30Completed
Influence of Cytochrome P2B6 on Efavirenz Dose in HIV-infected Thai Patients in a Prospective Randomized Controlled Trial: a Proof-of-concept Study [NCT02421289]Phase 1190 participants (Anticipated)Interventional2013-04-30Recruiting
A Randomized Controlled Trial Comparing Efavirenz With Rilpivirine on Changes in Endothelial Function, Inflammatory Markers, and Oxidative Stress in HIV-uninfected Healthy Volunteers [NCT01585038]Phase 440 participants (Actual)Interventional2012-07-31Completed
HIV Postexposure Prophylaxis With Darunavir/r (PEPDar) [NCT01516970]Phase 3312 participants (Actual)Interventional2011-11-25Completed
An Open-Label, Randomized Comparison of Elvitegravir-Cobicistat-Tenofovir Alafenamide-Emtricitabine Versus Efavirenz-Tenofovir Disoproxil Fumarate-Lamivudine in Patients Starting Antiretroviral Therapy on the Day of HIV Diagnosis [NCT03405194]0 participants (Actual)Interventional2018-05-01Withdrawn(stopped due to Haiti gained access to dolutegravir as first-line ART, so we cancelled the study before any patient was enrolled (we didn't want SOC group to receive EFV))
Safety and Pharmacokinetics of Dolutegravir in Pregnant HIV Mothers and Their Neonates: A Pilot Study [NCT02245022]Phase 2/Phase 360 participants (Actual)Interventional2017-03-14Completed
Multicenter, Double-Blind, Randomized, 2-Part, Dose Ranging Study to Compare the Safety, and Antiretroviral Activity of MK-1439 Plus TRUVADA Versus Efavirenz Plus TRUVADA in Antiretroviral Treatment-Naive, HIV-1 Infected Patients [NCT01632345]Phase 2342 participants (Actual)Interventional2012-10-12Completed
Phase I Dose Escalation Trial of Efavirenz for Patients With Solid Tumours or Non-Hodgkin Lymphoma in Therapeutic Failure. [NCT01878890]Phase 125 participants (Actual)Interventional2011-09-05Completed
A Randomized, Blinded, 12-week Comparison of Elvucitabine/Efavirenz/Tenofovir Versus Lamivudine/Efavirenz/Tenofovir in HIV-1 Infected Treatment-naive Participants. There is a 36 Week, Open-label, Extension Phase for Eligible Participants. [NCT00350272]Phase 276 participants (Actual)Interventional2006-05-31Completed
A Pharmacokinetic Evaluation of Increased Dose Levonorgestrel Implant and Efavirenz-Based Antiretroviral Therapy In HIV-Infected Ugandan Women [NCT02722421]Phase 228 participants (Actual)Interventional2017-04-06Completed
A Pilot Project of Virologic, Pharmacologic and Immunologic Correlates of Gastrointestinal-Associated Lymphoid Tissue Immune Reconstitution Following Raltegravir Therapy [NCT00661960]25 participants (Actual)Interventional2008-03-31Completed
Pilot Study of Raltegravir/Tenofovir/Emtricitabine Versus Efavirenz/Tenofovir/Emtricitabine for Adults With Acute HIV-1 Infection: Exploring the Role of Integrase Inhibition in Early HIV Pathogenesis [NCT00734344]18 participants (Actual)Interventional2008-09-30Completed
A Phase 3b, Randomized, Open-label Clinical Study to Demonstrate Non-inferiority in Virologic Response Rates of HIV-1 RNA Suppression <400 Copies/mL of TDF/FTC/RPV Versus TDF/FTC/EFV in First-line Antiretroviral NNRTI-based Suppressed Patients. Switching [NCT01709084]Phase 3426 participants (Actual)Interventional2013-10-02Completed
Evaluating Pharmacokinetic Interactions With Vaginal Ring Contraceptives and Antiretroviral Therapy (ART) [NCT01903031]Phase 284 participants (Actual)Interventional2014-12-30Completed
The Intensive Pharmacokinetics Sub-study of Encore1: A Randomised, Double-blind, Placebo-controlled, Clinical Trial to Compare the Safety and Efficacy of Reduced Dose Efavirenz (EFV) With Standard Dose EFV Plus Two Nucleotide Reverse Transcriptase Inhibit [NCT01271894]Phase 340 participants (Actual)Interventional2011-09-30Completed
A Randomized Controlled Pilot Trial Comparing Continued Antiretroviral Therapy With Tenofovir/Emtricitabine/Efavirenz (TDF/FTC/EFV) With Switch to Tenofovir/Emtricitabine/Raltegravir (TDF/FTC/RAL) on Changes in Endothelial Function and Markers of Bone Met [NCT01270802]Phase 430 participants (Actual)Interventional2011-04-30Completed
A Randomized Comparison of Three Regimens of Chemotherapy With Compatible Antiretroviral Therapy for Treatment of Advanced AIDS-KS in Resource-Limited Settings [NCT01435018]Phase 3334 participants (Actual)Interventional2013-10-01Completed
Study of the Pharmacokinetic Effects of Efavirenz on the Pharmacokinetics of SHR1459 in Healthy Subjects [NCT05560360]Phase 120 participants (Actual)Interventional2022-11-04Completed
Flucloxacillin as an Inducer of CYP-enzymes [NCT04840641]Phase 114 participants (Actual)Interventional2021-03-25Completed
An Open Label, Randomized, Parallel Design Estimation Pilot Study to Compare the Efficacy and Safety of Raltegravir-based Versus Efavirenz-based Combination Therapy in Treatment-naïve Patients With HIV-1 Infection [NCT01989910]Phase 4107 participants (Actual)Interventional2013-09-30Completed
The Effect of Efavirenz and Ritonavir-boosted Darunavir on the Pharmacokinetics of the HMG CoA Reductase Inhibitor Pitavastatin [NCT01695954]Phase 134 participants (Actual)Interventional2012-05-31Completed
Randomized Clinical Trial to Evaluate the Interest of a Down-scaled Treatment Strategy Using Dual Therapy (Nucleoside Analogs) in HIV Infected Patients Already Being Treated Using Triple Therapy, Who Present With a Successful Virological Control and for W [NCT02302547]Phase 3224 participants (Actual)Interventional2014-12-31Completed
A Phase IV Randomized Trial to Evaluate the Virologic Response and Pharmacokinetics of Two Different Potent Regimens in HIV Infected Women Initiating Triple Antiretroviral Regimens Between 20 and 36 Weeks of Pregnancy for the Prevention of Mother-to-Child [NCT01618305]Phase 4408 participants (Actual)Interventional2013-09-05Completed
An Open-label, Drug Interaction Study to Investigate the Effects of Steady-State Fenofibric Acid on the Single-Dose Pharmacokinetics of Efavirenz in Healthy Subjects [NCT01472380]Phase 130 participants (Actual)Interventional2011-11-30Completed
International, Multicenter, Randomized, Partially Blind Study to Evaluate Efficacy, Safety and Selection of the Optimal Dose for VM-1500 in Comparison to Efavirenz in Combination With Two NRTIs in Treatment-naïve, HIV-1 Infected Patients [NCT02489461]Phase 2/Phase 3150 participants (Actual)Interventional2014-08-05Completed
Influence of Autoinhibition/Autoinduction and CYP2B6 Genetic Variations on CYP2B6 Activity and Drug Interactions in Healthy Volunteers [NCT02401256]Phase 470 participants (Actual)Interventional2013-07-31Completed
A Randomised Trial of Monitoring Practice and Induction Maintenance Drug Regimens in the Management of Antiretroviral Therapy in Children With HIV Infection in Africa [NCT02028676]Phase 41,206 participants (Actual)Interventional2007-03-31Completed
Decrease of Neuropsychiatric and Neurocognitive Side Effects Prevalence [NCT02447016]Phase 425 participants (Actual)Interventional2015-05-31Terminated(stopped due to no more participants taking atripla)
A Phase IIb, Dose Ranging Study of Oral GSK1265744 in Combination With Nucleoside Reverse Transcriptase Inhibitors for Induction of Human Immunodeficiency Virus -1 (HIV-1) Virologic Suppression Followed by an Evaluation of Maintenance of Virologic Suppres [NCT01641809]Phase 2244 participants (Actual)Interventional2012-08-06Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00016718 (3) [back to overview]Proportion of Participants With Suppression of HIV Viral Load to Less Than 50 Copies/ml at Week 16
NCT00016718 (3) [back to overview]Proportion of Participants With Suppression of HIV Viral Load to Less Than 400 Copies/ml at Week 16
NCT00016718 (3) [back to overview]Proportion of Participants Who Developed Grade 3 or 4 Adverse Events Attributed to the Study Treatment.
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Plasma Concentration for Contraceptives
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00074581 (2) [back to overview]Linked Partner HIV Infection Rates in Early-ART and Delayed-ART Arms
NCT00074581 (2) [back to overview]All Partner HIV Infection Rates in Early-ART and Delayed-ART Arms
NCT00084136 (18) [back to overview]Time to Loss of Virologic Response by Week 48 (Defined by FDA TLOVR Algorithm - Excluding Study Allowed ARV Substitutions)(PI Comparison)
NCT00084136 (18) [back to overview]Time to Treatment Failure (NRTI Comparison)
NCT00084136 (18) [back to overview]Time to Treatment Failure (PI Comparison)
NCT00084136 (18) [back to overview]Change in CD4 Count From Screening to Weeks 24, 48, 96 (NRTI Comparison)
NCT00084136 (18) [back to overview]Change in CD4 Count From Screening to Weeks 24, 48, 96 (PI Comparison)
NCT00084136 (18) [back to overview]Plasma HIV-1 Viral Load Fewer Than 400 Copies/ml (NRTI Comparison)
NCT00084136 (18) [back to overview]Plasma HIV-1 Viral Load Fewer Than 400 Copies/ml (PI Comparison)
NCT00084136 (18) [back to overview]Time to Discontinuation of Initial Antiretroviral (ARV) Therapy (NRTI Comparison)
NCT00084136 (18) [back to overview]Time to Discontinuation of Initial Antiretroviral (ARV) Therapy (PI Comparison)
NCT00084136 (18) [back to overview]Time to First Dose Modification or Grade 3 or 4 Adverse Event (NRTI Comparison)
NCT00084136 (18) [back to overview]Time to First Dose Modification or Grade 3 or 4 Adverse Event (PI Comparison)
NCT00084136 (18) [back to overview]Time to Immunologic Failure (PI Comparison)
NCT00084136 (18) [back to overview]Time to Loss of Virologic Response at Week 48 (Defined by FDA TLOVR Algorithm - Excluding Study Allowed ARV Substitutions)(NRTI Comparison)
NCT00084136 (18) [back to overview]Time to Loss of Virologic Response at Week 48 (Defined by FDA TLOVR Algorithm - Including All ARV Substitutions)(NRTI Comparison)
NCT00084136 (18) [back to overview]Time to Loss of Virologic Response at Week 48 (Defined by FDA TLOVR Algorithm - Including All ARV Substitutions)(PI Comparison)
NCT00084136 (18) [back to overview]Time to Immunologic Failure (NRTI Comparison)
NCT00084136 (18) [back to overview]Time to Loss of Virologic Response at Week 96 (Defined by FDA TLOVR Algorithm - Excluding Study Allowed ARV Substitutions)(NRTI Comparison)
NCT00084136 (18) [back to overview]Time to Loss of Virologic Response at Week 96 (Defined by FDA TLOVR Algorithm - Including All ARV Substitutions)(NRTI Comparison)
NCT00098293 (17) [back to overview]Time-Averaged Difference (TAD) in log10-transformed HIV-1 RNA Levels
NCT00098293 (17) [back to overview]Percentage of Participants With HIV-1 RNA Levels of Less Than 400 Copies/mL and Less Than 50 Copies/mL at Week 96 for Enhanced Sensitivity Trofile Assay (ESTA) R5 Participants
NCT00098293 (17) [back to overview]Percentage of Participants With HIV-1 RNA Levels of Less Than 400 Copies/mL and Less Than 50 Copies/mL at Week 96 Analyzed Using Logistic Regression
NCT00098293 (17) [back to overview]Percentage of Participants With HIV-1 RNA Levels of Less Than 400 Copies/mL and Less Than 50 Copies/mL at Week 48 for Enhanced Sensitivity Trofile Assay (ESTA) R5 Participants
NCT00098293 (17) [back to overview]Percentage of Participants With HIV-1 RNA Levels of Less Than 400 Copies/mL and Less Than 50 Copies/mL at Week 48 Analyzed Using Logistic Regression
NCT00098293 (17) [back to overview]Number of Participants With Phenotypic Resistance at Time of Treatment Failure Through Week 48 and 96
NCT00098293 (17) [back to overview]Number of Participants With NRTI Associated Mutations at Time of Treatment Failure Through Week 48 and 96
NCT00098293 (17) [back to overview]Time to Virologic Failure
NCT00098293 (17) [back to overview]Percentage of Participants With Viral Load of Less Than 400 Copies/Milliliter [Copies/mL] and Less Than 50 Copies/mL of Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) at Week 48 for Full Analysis Set (FAS) Population
NCT00098293 (17) [back to overview]Number of Participants Per Tropism Status at Baseline and at the Time of Treatment Failure Through Week 96
NCT00098293 (17) [back to overview]Number of Participants Per Tropism Status at Baseline and at the Time of Treatment Failure Through Week 48
NCT00098293 (17) [back to overview]Change From Baseline in Lymphocyte Cluster of Differentiation 8 (CD8) Count at Week 48 and 96
NCT00098293 (17) [back to overview]Change From Baseline in Lymphocyte Cluster of Differentiation 4 (CD4) Count at Week 48 and 96
NCT00098293 (17) [back to overview]Change From Baseline in Log 10-transformed Plasma Viral Load (HIV-1 RNA) Levels at Week 48 and 96
NCT00098293 (17) [back to overview]Percentage of Participants With Viral Load of Less Than 400 Copies/mL and Less Than 50 Copies/mL of HIV-1 RNA at Week 96
NCT00098293 (17) [back to overview]Percentage of Participants With Viral Load of Less Than 400 Copies/mL and Less Than 50 Copies/mL of HIV-1 RNA at Week 48 for Per Protocol (PP) Population
NCT00098293 (17) [back to overview]Number of Participants With Efavirenz Associated Mutations at Time of Treatment Failure Through Week 48 and 96
NCT00100048 (26) [back to overview]Number of Participants With HIV RNA Levels Below 400 Copies/mL at Week 48
NCT00100048 (26) [back to overview]Number of Participants With HIV RNA Levels Below 50 Copies/mL at Week 24 (Cohort II)
NCT00100048 (26) [back to overview]Number of Participants With Clinical Adverse Experiences (AEs)and Serious Adverse Experiences (SAEs)
NCT00100048 (26) [back to overview]Number of Patients That Discontinued With CAEs
NCT00100048 (26) [back to overview]Number of Patients That Discontinued With LAEs
NCT00100048 (26) [back to overview]Number of Patients With Clinical Adverse Experiences (CAEs)
NCT00100048 (26) [back to overview]Number of Patients With Clinical Adverse Experiences (CAEs) and Number of Patients With Serious CAEs at Day 10 (Cohort I)
NCT00100048 (26) [back to overview]Number of Patients With Drug-related CAEs
NCT00100048 (26) [back to overview]Number of Patients With Drug-related LAEs
NCT00100048 (26) [back to overview]Number of Patients With HIV RNA Level Below 50 Copies/mL and HIV RNA Level Below 400 Copies/mL at Week 96
NCT00100048 (26) [back to overview]Number of Patients With Laboratory Adverse Experiences (LAEs)
NCT00100048 (26) [back to overview]Number of Patients With Serious CAEs (Cohort I and II Combined)
NCT00100048 (26) [back to overview]Number of Patients With Serious CAEs and Non-serious CAEs at Week 144
NCT00100048 (26) [back to overview]Number of Patients With Serious Drug-related CAEs
NCT00100048 (26) [back to overview]Number of Patients With Serious LAEs
NCT00100048 (26) [back to overview]Change From Baseline in CD4 (T-helper) Cell Count at Week 240
NCT00100048 (26) [back to overview]Change From Baseline in CD4 Cell Count at Week 96
NCT00100048 (26) [back to overview]Change From Baseline in Cluster of Differentiation 4 (CD4) Cell Count at Week 24 (Cohort II)
NCT00100048 (26) [back to overview]Change From Baseline in Plasma HIV RNA at Week 24 (Cohort II)
NCT00100048 (26) [back to overview]Change From Baseline in Plasma HIV RNA at Week 240
NCT00100048 (26) [back to overview]Number of Patients With Serious Drug-related LAEs
NCT00100048 (26) [back to overview]Change From Baseline in Plasma HIV RNA at Week 96
NCT00100048 (26) [back to overview]Change From Baseline in Plasma Human Immunodeficiency Virus (HIV) Ribonucleic Acid (RNA) on Day 10 (Cohort I)
NCT00100048 (26) [back to overview]Number of Participants With HIV RNA (Human Immunodeficiency Virus Ribonucleic Acid) Levels Below 50 Copies/mL at Week 240
NCT00100048 (26) [back to overview]Number of Participants With HIV RNA Levels Below 400 Copies/mL at Week 24 (Cohort II)
NCT00100048 (26) [back to overview]Number of Participants With HIV RNA Levels Below 400 Copies/mL at Week 240
NCT00102960 (13) [back to overview]Number of Children Experiencing Severe CDC Stage B or Stage C Disease or Death (Cumulative After 3.5 Years)
NCT00102960 (13) [back to overview]Hospitalization Rates
NCT00102960 (13) [back to overview]Time to Failure of First Line Therapy or Death
NCT00102960 (13) [back to overview]Number of Participants Who Experienced Regimen-limiting ART Drug Toxicity
NCT00102960 (13) [back to overview]Total Occurrence of Grade 3 or 4 Laboratory Events
NCT00102960 (13) [back to overview]Total Occurrence of Grade 3 or 4 Clinical Events
NCT00102960 (13) [back to overview]Time From Randomization to Starting or Needing to Start Continuous Therapy
NCT00102960 (13) [back to overview]Number of Participants Who Experienced Virological Failure Defined as Confirmed HIV-1 RNA Value of at Least 10,000 Copies Per/ml Recorded on Two Consecutive Separate Occasions After 24 Weeks of Treatment (Initial Therapy or Restart)
NCT00102960 (13) [back to overview]Number of Participants Who Experienced Immunological Failure Defined as Failure of CD4% to Reach 20% or CD4% Falls Below 20% on Two Occasions, Within 4 Weeks, at Any Time After the First 24 Weeks of Therapy (Initial Therapy or Restart)
NCT00102960 (13) [back to overview]Number of Participants Who Experienced Clinical Failure (Defined as Development of Severe CDC Stage B or Stage C Disease.) on Therapy.
NCT00102960 (13) [back to overview]Time to First Hospitalization
NCT00102960 (13) [back to overview]Time to Death Alone or Death Plus Life Threatening Stage C Events or HIV Events Associated With Permanent End-organ Damage.
NCT00102960 (13) [back to overview]Duration of Hospitalisation
NCT00110305 (14) [back to overview]Change From Baseline in CD4+ Cell Count (Relative) at Week 96
NCT00110305 (14) [back to overview]Number of Participants With Virologic Response (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm, by Area Under the Plasma Concentration Time Curve From Time 0 to 24 Hours (AUC24h) Quartiles
NCT00110305 (14) [back to overview]Number of Participants With Virologic Response at Week 240 (Viral Load Less Than 400 Copies/mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00110305 (14) [back to overview]Number of Participants With Virologic Response at Week 240 (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00110305 (14) [back to overview]Number of Participants With Virologic Response at Week 240 (Viral Load Less Than 50 Copies Per mL) - Snapshot Analysis
NCT00110305 (14) [back to overview]Number of Participants With Virologic Response at Week 96 (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00110305 (14) [back to overview]Trough Plasma Concentration (Ctrough) for TMC278
NCT00110305 (14) [back to overview]Number of Participants With Virologic Failure for the Resistance Determinations by Developing Mutations: First Available On-Treatment Genotypic Data After Failure
NCT00110305 (14) [back to overview]Number of Participants With Virologic Response at Week 48 (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00110305 (14) [back to overview]Number of Participants With Virologic Response at Week 96 (Viral Load Less Than 50 Copies Per mL) - Snapshot Analysis
NCT00110305 (14) [back to overview]Area Under the Plasma Concentration Time Curve From Time 0 to 24 Hours (AUC24h) for TMC278
NCT00110305 (14) [back to overview]Change From Baseline in CD4+ Cell Count (Absolute) at Week 240
NCT00110305 (14) [back to overview]Change From Baseline in CD4+ Cell Count (Absolute) at Week 96
NCT00110305 (14) [back to overview]Change From Baseline in CD4+ Cell Count (Relative) at Week 240
NCT00112047 (53) [back to overview]Percentage of Participants With Pure Virologic Failure (HIV-1 RNA < 50 c/mL) at Week 96
NCT00112047 (53) [back to overview]Percentage of Participants With Pure Virological Failure (HIV-1 RNA < 400 c/mL) at Week 144
NCT00112047 (53) [back to overview]Percentage of Participants With Pure Virological Failure (HIV-1 RNA < 400 c/mL) Through Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Percentage of Participants With Pure Virological Failure (HIV-1 RNA < 50 c/mL) at Week 144
NCT00112047 (53) [back to overview]Percentage of Participants With Pure Virological Failure (HIV-1 RNA < 50 c/mL) Through Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Quality of Life (SF-12v2 Health Survey: Mental Component Summary) Change From Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Quality of Life (SF-12v2 Health Survey: Physical Component Summary) Change From Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Treatment Satisfaction Questionnaire (General Satisfaction With Current Treatment Regimen): Change From Week 144 to Week 240 in the Category Shift From Atripla Baseline.
NCT00112047 (53) [back to overview]Treatment Satisfaction Questionnaire (Satisfaction With Convenience and Simplicity of Current Treatment Regimen): Change From Week 144 to Week 240 in the Category Shift From Atripla Baseline.
NCT00112047 (53) [back to overview]Treatment Satisfaction Questionnaire (Satisfaction With Current Treatment Regimen to Control HIV): Change From Week 144 to Week 240 in the Category Shift From Atripla Baseline.
NCT00112047 (53) [back to overview]Treatment Satisfaction Questionnaire (Satisfaction With Tolerability of Current Treatment Regimen) Change From Week 144 to Week 240 in the Category Shift From Atripla Baseline.
NCT00112047 (53) [back to overview]Treatment Satisfaction Questionnaire (Bothered With the Side Effects of Current Treatment Regimen): Change From Week 144 to Week 240 in the Category Shift From Atripla Baseline.
NCT00112047 (53) [back to overview]Percentage of Participants With Plasma HIV-1 RNA < 50 c/mL at Week 144
NCT00112047 (53) [back to overview]Percentage of Participants With Pure Virologic Failure (HIV-1 RNA < 400 c/mL) at Week 48
NCT00112047 (53) [back to overview]Percentage of Participants With Pure Virologic Failure (HIV-1 RNA < 400 c/mL) at Week 96
NCT00112047 (53) [back to overview]Change From Baseline in CD4 Cell Count (Cells/mm^3) at Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Change From Study Baseline in CD4 Cell Count (Cells/mm^3) at Week 144
NCT00112047 (53) [back to overview]Change From Study Baseline in CD4 Cell Count (Cells/mm^3) at Week 48
NCT00112047 (53) [back to overview]Change From Study Baseline in CD4 Cell Count (Cells/mm^3) at Week 96
NCT00112047 (53) [back to overview]Change From Study Baseline in HIV-1 RNA (Log10 c/mL) at Week 144
NCT00112047 (53) [back to overview]Change From Study Baseline in HIV-1 RNA (Log10 c/mL) at Week 48
NCT00112047 (53) [back to overview]Change From Study Baseline in HIV-1 RNA (Log10 c/mL) at Week 96
NCT00112047 (53) [back to overview]Change in Limb Fat (kg) From Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Change in Limb Fat (kg) From Week 48 to Week 144
NCT00112047 (53) [back to overview]Change in Limb Fat (kg) From Week 48 to Week 96
NCT00112047 (53) [back to overview]Change in Total Body Fat (kg) From Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Change in Total Body Fat (kg) From Week 48 to Week 144
NCT00112047 (53) [back to overview]Change in Total Body Fat (kg) From Week 48 to Week 96
NCT00112047 (53) [back to overview]Change in Trunk Fat (kg) From Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Change in Trunk Fat (kg) From Week 48 to Week 144
NCT00112047 (53) [back to overview]Change in Trunk Fat (kg) From Week 48 to Week 96
NCT00112047 (53) [back to overview]Percentage of Participants With Confirmed Plasma HIV-1 RNA < 400 c/mL at Week 144 (Defined by FDA TLOVR Algorithm)
NCT00112047 (53) [back to overview]Percentage of Participants With Confirmed Plasma HIV-1 RNA < 400 c/mL at Week 240 (Atripla Week 96) Defined by the FDA TLOVR Algorithm
NCT00112047 (53) [back to overview]Percentage of Participants With Confirmed Plasma HIV-1 RNA < 400 c/mL at Week 48 (Defined by the Food and Drug Administration [FDA] Time-to-Loss-of Virologic Response [TLOVR] Algorithm
NCT00112047 (53) [back to overview]Percentage of Participants With Confirmed Plasma HIV-1 RNA < 400 c/mL at Week 96 (Defined by FDA TLOVR Algorithm)
NCT00112047 (53) [back to overview]Percentage of Participants With Confirmed Plasma HIV-1 RNA < 50 c/mL at Week 144 (Defined by FDA TLOVR Algorithm)
NCT00112047 (53) [back to overview]Percentage of Participants With Confirmed Plasma HIV-1 RNA < 50 c/mL at Week 240 (Atripla Week 96) Defined by the FDA TLOVR Algorithm
NCT00112047 (53) [back to overview]Percentage of Participants With Confirmed Plasma HIV-1 RNA < 50 c/mL at Week 48 (Defined by FDA TLOVR Algorithm)
NCT00112047 (53) [back to overview]Percentage of Participants With Confirmed Plasma HIV-1 RNA < 50 c/mL at Week 96 (Defined by FDA TLOVR Algorithm)
NCT00112047 (53) [back to overview]Percentage of Participants With HIV-1 RNA < 50 c/mL at Week 48
NCT00112047 (53) [back to overview]Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 400 c/mL) at Week 144
NCT00112047 (53) [back to overview]Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 400 c/mL) at Week 48
NCT00112047 (53) [back to overview]Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 400 c/mL) at Week 96
NCT00112047 (53) [back to overview]Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 400 c/mL) From Week 144 (Atripla Baseline) Through Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 50 c/mL) at Week 144
NCT00112047 (53) [back to overview]Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 50 c/mL) at Week 48
NCT00112047 (53) [back to overview]Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 50 c/mL) at Week 96
NCT00112047 (53) [back to overview]Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 50 c/mL) From Week 144 (Atripla Baseline) Through Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Percentage of Participants With Plasma HIV-1 RNA < 400 c/mL at Week 144
NCT00112047 (53) [back to overview]Percentage of Participants With Plasma HIV-1 RNA < 400 c/mL at Week 240 (Atripla Week 96)
NCT00112047 (53) [back to overview]Percentage of Participants With Plasma HIV-1 RNA < 400 c/mL at Week 48.
NCT00112047 (53) [back to overview]Percentage of Participants With Pure Virologic Failure (HIV-1 RNA < 50 c/mL) at Week 48
NCT00112047 (53) [back to overview]Percentage of Participants With Plasma HIV-1 RNA < 50 c/mL at Week 240 (Atripla Week 96)
NCT00118898 (22) [back to overview]Cumulative Probability of Not Experiencing Regimen Failure
NCT00118898 (22) [back to overview]Cumulative Probability of Not Experiencing Treatment Modification
NCT00118898 (22) [back to overview]Cumulative Probability of Not Experiencing Virologic Failure
NCT00118898 (22) [back to overview]Number of Participants Experiencing Certain Targeted Clinical Events, Including Death, AIDS-defining Illness, and HIV-1 Related Events.
NCT00118898 (22) [back to overview]Number of Participants With HIV-1 RNA Levels Less Than 200 Copies/mL
NCT00118898 (22) [back to overview]The Number of Participants With HIV-1 RNA Levels Less Than 50 Copies/mL
NCT00118898 (22) [back to overview]Time From Randomization to Virologic Failure
NCT00118898 (22) [back to overview]Time From Treatment Dispensation to a Grade 3/4 Safety Event
NCT00118898 (22) [back to overview]Time From Treatment Dispensation to Regimen Failure (First Occurrence of Virologic Failure or Treatment Modification)
NCT00118898 (22) [back to overview]Time From Treatment Dispensation to Treatment Modification
NCT00118898 (22) [back to overview]Amount of Study Follow-up
NCT00118898 (22) [back to overview]Number of Participants With a Grade 3/4 Safety Event
NCT00118898 (22) [back to overview]Number of Participants With Regimen Failure
NCT00118898 (22) [back to overview]Number of Participants With Treatment Modification
NCT00118898 (22) [back to overview]Number of Participants With Virologic Failure
NCT00118898 (22) [back to overview]Number of Participants With Virologic Failure and Emergence of Major Resistance
NCT00118898 (22) [back to overview]Change in CD4 Count (Cells/mm3) From Baseline
NCT00118898 (22) [back to overview]Change in Fasting High-density Lipoprotein (HDL) Cholesterol Level From Baseline
NCT00118898 (22) [back to overview]Change in Fasting Non-high Density Lipoprotein (Non-HDL) Cholesterol Level From Baseline
NCT00118898 (22) [back to overview]Change in Fasting Total Cholesterol Level From Baseline
NCT00118898 (22) [back to overview]Change in Fasting Triglyceride Level From Baseline
NCT00118898 (22) [back to overview]Cumulative Probability of Not Experiencing a Grade 3/4 Safety Event
NCT00162097 (13) [back to overview]Number of Participants With Identified Electrocardiogram (ECG) Abnormalities
NCT00162097 (13) [back to overview]Number of Participants Who Experienced AEs Leading to Study Drug Discontinuation
NCT00162097 (13) [back to overview]Number of Participants With Abnormal Physical Examination Findings at Baseline (Screening and/or Day 1)
NCT00162097 (13) [back to overview]Number of Participants With Clinically Meaningful Vital Signs Measures
NCT00162097 (13) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax)
NCT00162097 (13) [back to overview]Number of Participants Who Experienced AEs
NCT00162097 (13) [back to overview]Number of Participants Who Died or Experienced Other Serious Adverse Events (SAEs)
NCT00162097 (13) [back to overview]Number of Participants With Marked Abnormalities (MAs) in Hematology Measurements
NCT00162097 (13) [back to overview]Number of Participants With Serum Chemistry MAs
NCT00162097 (13) [back to overview]Number of Participants With Urinalysis MAs
NCT00162097 (13) [back to overview]Area Under the Plasma Concentration-time Curve Over the Dosing Interval of 24 Hours (AUC[TAU])
NCT00162097 (13) [back to overview]Maximum Plasma Concentration (Cmax)
NCT00162097 (13) [back to overview]Minimum Plasma Concentration (Cmin)
NCT00255840 (1) [back to overview]Cumulative Treatment Failure Rate of Participants on First Line Antiretroviral Therapy Monitored by Primary Health Care Nurses (Investigative Arm)is Not Inferior to the Cumulative Treatment Failure Rate of Participants Monitored by Doctors (Control Arm).
NCT00335322 (2) [back to overview]Time Weighted Mean Change From Baseline Plasma HIV-RNA
NCT00335322 (2) [back to overview]Time-weighted Mean Change From Baseline Plasma HIV-RNA.
NCT00342355 (2) [back to overview]Serious Adverse Events
NCT00342355 (2) [back to overview]Progression to AIDS or Death in tx naïve Pts With Adv HIV dx in the Four Randomly Assigned Regimens.
NCT00350272 (2) [back to overview]The Proportion Of Participants With Virologic Response For 10 mg/Day Elvucitabine In HIV-1-Infected Participants By 12 Weeks Compared With The Proportion Of Participants With Lamivudine 300 mg/Day
NCT00350272 (2) [back to overview]The Safety Profile Of Elvucitabine.
NCT00364793 (28) [back to overview]Percent of CD4 Cells Change From Baseline at Weeks 60, 72, 84, and 96 - Treated Participants
NCT00364793 (28) [back to overview]The Number of Participants With Plasma HIV RNA < 400 Copies Per Milliliter (c/mL) at Week 48 as Analyzed by Different Algorithms - All Treated Participants
NCT00364793 (28) [back to overview]The Number of Participants With Plasma HIV RNA Levels < 400 c/mL at Week 24 as Analyzed by Different Algorithms - All Treated Participants
NCT00364793 (28) [back to overview]The Number of Participants With Plasma HIV RNA Levels < 400 c/mL at Weeks 60, 72, 84 and 96 (Observed Cases) - All Treated Participants
NCT00364793 (28) [back to overview]CD4 Cell Count Change From Baseline at Weeks 24 and 48 - Treated Participants
NCT00364793 (28) [back to overview]The Number of Participants With Plasma HIV RNA Levels < 50 c/mL at Week 48 as Analyzed by Different Algorithms - All Treated Participants
NCT00364793 (28) [back to overview]The Number of Participants With Plasma HIV RNA Levels < 50 c/mL at Weeks 60, 72, 84 and 96 (Observed Cases) - All Treated Participants
NCT00364793 (28) [back to overview]Apparent Oral Clearance Adjusted for Body Weight (CLT/F/kg) of EFV at Week 2 - Pharmacokinetic Evaluable Population
NCT00364793 (28) [back to overview]Area Under the Plasma Concentration Time Curve (AUC) Over One Dosing Interval From Time Zero to 24 Hours Post-dose(TAU) at Week 2 - Pharmacokinetic Evaluable Population
NCT00364793 (28) [back to overview]AUC (TAU) of Didanosine (ddI) at Week 2 - Pharmacokinetic Evaluable Population
NCT00364793 (28) [back to overview]The Number of Participants With Plasma HIV RNA Levels < 50 c/mL at Week 24 as Analyzed by Different Algorithms - All Treated Participants
NCT00364793 (28) [back to overview]CLT/F of Didanosine (ddI) at Week 2 - Pharmacokinetic Evaluable Population
NCT00364793 (28) [back to overview]CLT/F/kg of Didanosine (ddI) at Week 2 - Pharmacokinetic Evaluable Population
NCT00364793 (28) [back to overview]Apparent Oral Clearance (CLT/F) of EFV at Week 2 - Pharmacokinetic Evaluable Population
NCT00364793 (28) [back to overview]Terminal Phase Elimination Half-life (T-HALF) in Didanosine (ddI) at Week 2 - Pharmacokinetic Evaluable Population
NCT00364793 (28) [back to overview]CD4 Cell Count Change From Baseline at Weeks 60, 72, 84, and 96 - Treated Participants
NCT00364793 (28) [back to overview]Cmax and Cmin of Didanosine (ddI) at Week 2 - Pharmacokinetic Evaluable Population
NCT00364793 (28) [back to overview]Log10 c/mL HIV RNA Changes From Baseline at Weeks 60, 72, 84 and 96 - Treated Participants
NCT00364793 (28) [back to overview]Log10 c/mL HIV RNA Changes From Baseline Through Week 48 - Treated Participants
NCT00364793 (28) [back to overview]Maximum Observed Plasma Concentration (Cmax) and Plasma Concentration 24 Hours Post-dose (Cmin) of EFV at Week 2 - Pharmacokinetic Evaluable Population
NCT00364793 (28) [back to overview]Number of Participants With Acquisition of Resistance to EFV Categorized by AUC Relationship - Evaluable Pharmacokinetic Population
NCT00364793 (28) [back to overview]Number of Treated Participants With Resistance Associated Genotypic and Phenotypic Changes in Viruses - Participants With Virologic Failure, Lack of Suppression or Viral Load Rebound
NCT00364793 (28) [back to overview]Number of Participants With Hematologic Abnormalities - Treated Participants
NCT00364793 (28) [back to overview]Number of Participants With Lipid and Glucose Laboratory Abnormalities - Treated Participants
NCT00364793 (28) [back to overview]Number of Participants With Liver Function Test Laboratory Abnormalities - Treated Population
NCT00364793 (28) [back to overview]Number of Participants With On-Treatment Adverse Events (AEs), Related Adverse Events, Serious Adverse Events (SAEs), Death, Discontinuation Due to Adverse Events, and CDC Class C AIDS Events
NCT00364793 (28) [back to overview]Number of Participants With Serum Chemistry Abnormalities - Treated Participants
NCT00364793 (28) [back to overview]Percent of CD4 Cells Change From Baseline at Weeks 24 and 48 - Treated Participants
NCT00369941 (73) [back to overview]Change From Baseline in CD4 Cell Count at Week 156
NCT00369941 (73) [back to overview]Change From Baseline in CD4 Cell Count at Week 240
NCT00369941 (73) [back to overview]Change From Baseline in CD4 Cell Count at Week 96
NCT00369941 (73) [back to overview]Change From Baseline in Cluster of Differentiation Antigen 4 (CD4) Cell Count at Week 48
NCT00369941 (73) [back to overview]Number of Participants Who Achieved HIV RNA <400 Copies/mL at Week 156
NCT00369941 (73) [back to overview]Number of Participants Who Achieved HIV RNA <400 Copies/mL at Week 240
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Drug-related CAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants Discontinued With Drug-related LAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants Discontinued With Drug-related LAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants Who Achieved Human Immunodeficiency Virus (HIV) Ribonucleic Acid (RNA) <50 Copies/mL at Week 48
NCT00369941 (73) [back to overview]Number of Participants Who Achieved HIV RNA <50 Copies/mL at Week 96
NCT00369941 (73) [back to overview]Number of Participants Who Achieved HIV RNA <50 Copies/mL at Week 240
NCT00369941 (73) [back to overview]Number of Participants Who Achieved HIV RNA <50 Copies/mL at Week 156
NCT00369941 (73) [back to overview]Number of Participants Who Achieved HIV RNA <400 Copies/mL at Week 96
NCT00369941 (73) [back to overview]Number of Participants Who Achieved HIV RNA <400 Copies/mL at Week 48
NCT00369941 (73) [back to overview]Number of Participants With Drug-related CAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants With Drug-related LAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants With Serious LAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants With Serious LAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants With Serious LAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants With Serious LAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants With Serious Drug-related LAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants With Serious Drug-related LAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants With Serious Drug-related LAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants With Serious Drug-related LAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants With Serious Drug-related CAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants With Serious Drug-related CAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants With Serious Drug-related CAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants With Serious Drug-related CAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants With Drug-related CAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants With Drug-related CAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants With Drug-related CAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants With Clinical Adverse Experiences (CAEs) at Week 48
NCT00369941 (73) [back to overview]Number of Participants With CAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants With CAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants With CAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Serious Drug-related CAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Serious Drug-related CAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Serious Drug-related CAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Serious Drug-related CAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Serious CAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Serious CAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Serious CAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Serious CAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Drug-related CAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Drug-related CAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With Drug-related CAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With CAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With CAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With CAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants With Serious CAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants With Serious CAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants With Serious CAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants That Discontinued With CAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants That Died by Week 96
NCT00369941 (73) [back to overview]Number of Participants That Died by Week 48
NCT00369941 (73) [back to overview]Number of Participants That Died by Week 240
NCT00369941 (73) [back to overview]Number of Participants That Died by Week 156
NCT00369941 (73) [back to overview]Number of Participants Discontinued With LAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants With Serious CAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants With Nervous System Symptoms Assessed by Review of Accumulated Safety Data up to Week 8
NCT00369941 (73) [back to overview]Number of Participants With LAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants With LAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants With LAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants With Laboratory Adverse Experiences (LAEs) at Week 48
NCT00369941 (73) [back to overview]Number of Participants With Drug-related LAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants With Drug-related LAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants With Drug-related LAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants Discontinued With LAEs at Week 48
NCT00369941 (73) [back to overview]Number of Participants Discontinued With LAEs at Week 240
NCT00369941 (73) [back to overview]Number of Participants Discontinued With LAEs at Week 156
NCT00369941 (73) [back to overview]Number of Participants Discontinued With Drug-related LAEs at Week 96
NCT00369941 (73) [back to overview]Number of Participants Discontinued With Drug-related LAEs at Week 48
NCT00427297 (4) [back to overview]Incidence of Severe Adverse Events (Excluding Mortality)
NCT00427297 (4) [back to overview]Viral Failure
NCT00427297 (4) [back to overview]Incidence of Mortality
NCT00427297 (4) [back to overview]Immunologic Failure
NCT00442962 (11) [back to overview]Late Change in CD4 Count From Baseline
NCT00442962 (11) [back to overview]Time to Initial Virological Failure
NCT00442962 (11) [back to overview]Time to Loss of Virologic Response by Week 48 (Defined by FDA TLOVR Algorithm)
NCT00442962 (11) [back to overview]Time to Initial Virologic Response
NCT00442962 (11) [back to overview]Time to First Safety Event
NCT00442962 (11) [back to overview]Time to First Dose Modification
NCT00442962 (11) [back to overview]Early Changes in CD4 Count From Baseline
NCT00442962 (11) [back to overview]Percentage of Participants With Late Virologic Response
NCT00442962 (11) [back to overview]Percentage of Participants With Early Virologic Suppression
NCT00442962 (11) [back to overview]Percentage of Participants With Early Virologic Response
NCT00442962 (11) [back to overview]Percentage of Participants With Late Virologic Suppression
NCT00457665 (1) [back to overview]Effect of Drug Regimens on Serum Triglycerides.
NCT00540449 (9) [back to overview]The Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies/ml) at Week 96
NCT00540449 (9) [back to overview]The Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies/ml) at Week 48
NCT00540449 (9) [back to overview]Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies/ml) at Week 96
NCT00540449 (9) [back to overview]Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies/ml) at Week 48
NCT00540449 (9) [back to overview]Number of Participants With Virologic Failure for the Resistance Determination by Emerging Resistance Associated Mutations: First Available On-Treatment Genotypic Data After Failure
NCT00540449 (9) [back to overview]Mean Change From Baseline to Week 48 and Week 96 in Absolute and Relative CD4+ Cell Counts (Using Imputed Data)
NCT00540449 (9) [back to overview]Number of Participants With Virological Response (Observed, <50 Copies/ml) at Last On-Treatment Visit (Post-Week 96).
NCT00540449 (9) [back to overview]Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies/ml) at Week 96
NCT00540449 (9) [back to overview]Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies/ml) at Week 48
NCT00543725 (9) [back to overview]Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies Per mL) at Week 96
NCT00543725 (9) [back to overview]Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies Per mL) at Week 48
NCT00543725 (9) [back to overview]Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies Per mL) at Week 96
NCT00543725 (9) [back to overview]Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies Per mL) at Week 48
NCT00543725 (9) [back to overview]Number of Participants With Virologic Failure for the Resistance Determinations by Developing Mutations: First Available On-Treatment Genotypic Data After Failure
NCT00543725 (9) [back to overview]Mean Change From Baseline to Week 48 and Week 96 in Absolute and Relative CD4+ Cell Counts (Using Imputed Data)
NCT00543725 (9) [back to overview]Number of Participants With Virological Response (Observed, <50 Copies/mL) at Last On-Treatment Visit (Post-Week 96).
NCT00543725 (9) [back to overview]Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies Per mL) at Week 96
NCT00543725 (9) [back to overview]Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies Per mL) at Week 48
NCT00549198 (58) [back to overview]Mean Change From Baseline in Estimated Glomerular Filtration Rate (GFR), Calculated by Modification of Diet in Renal Disease (MDRD) Equation, at Week 96
NCT00549198 (58) [back to overview]Mean Change From Baseline in Estimated Glomerular Filtration Rate (GFR), Calculated by Modification of Diet in Renal Disease (MDRD) Equation, at Week 48
NCT00549198 (58) [back to overview]Mean Change From Baseline in Estimated Glomerular Filtration Rate (GFR), Calculated by Modification of Diet in Renal Disease (MDRD) Equation, at Week 24
NCT00549198 (58) [back to overview]Mean Change From Baseline in Estimated GFR, Calculated by Cockcroft-Gault Equation, at Week 96
NCT00549198 (58) [back to overview]Mean Change From Baseline in Estimated GFR, Calculated by Cockcroft-Gault Equation, at Week 48
NCT00549198 (58) [back to overview]Number of Participants With National Kidney Foundation Chronic Kidney Disease Stage 1, 2, 3, 4, or 5 Categories of Renal Function at Week 24
NCT00549198 (58) [back to overview]Change From Baseline in Cluster Difference 4 (CD4+) Cell Count at Week 24
NCT00549198 (58) [back to overview]Change From Baseline in Cluster Difference 4 (CD4+) Cell Count at Week 48
NCT00549198 (58) [back to overview]Change From Baseline in Cluster Difference 4 (CD4+) Cell Count at Week 96
NCT00549198 (58) [back to overview]Exploratory Analysis of Change From Baseline in Albumin as a Ratio to Urine Creatinine at Week 96
NCT00549198 (58) [back to overview]Exploratory Analysis of Change From Baseline in Beta 2 Microglobulin (B2M) as a Ratio to Urine Creatinine at Week 96
NCT00549198 (58) [back to overview]Exploratory Analysis of Change From Baseline in Bone Specific Alkaline Phosphatase (BSAP) at Week 96
NCT00549198 (58) [back to overview]Exploratory Analysis of Change From Baseline in N-acetyl-B-glucosaminidase (NAG) as a Ratio to Urine Creatinine at Week 96
NCT00549198 (58) [back to overview]Exploratory Analysis of Change From Baseline in Osteocalcin at Week 96
NCT00549198 (58) [back to overview]Exploratory Analysis of Change From Baseline in Procollagen Type 1 Amino-terminal Propeptide (P1NP) at Week 96
NCT00549198 (58) [back to overview]Exploratory Analysis of Change From Baseline in Retinol Binding Protein (RBP) as a Ratio to Urine Creatinine at Week 96
NCT00549198 (58) [back to overview]Exploratory Analysis of Change From Baseline in Type 1 Collagen Cross-linked C-telopeptide at Week 96
NCT00549198 (58) [back to overview]Mean Change From Baseline in Estimated GFR, Calculated by Cockcroft-Gault Equation, at Week 24
NCT00549198 (58) [back to overview]Number of Participants With HIV-1 RNA <50 Copies/Milliliter (c/mL) and 400 c/mL at Week 48
NCT00549198 (58) [back to overview]Number of Participants With HIV-1 RNA <50 Copies/Milliliter (c/mL) and 400 c/mL at Week 96
NCT00549198 (58) [back to overview]Number of Participants With National Kidney Foundation Chronic Kidney Disease Stage 1, 2, 3, 4, or 5 Categories of Renal Function at Week 48
NCT00549198 (58) [back to overview]Number of Participants With National Kidney Foundation Chronic Kidney Disease Stage 1, 2, 3, 4, or 5 Categories of Renal Function at Week 96
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting High-density Lipoprotein (HDL) at Week 24
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting High-density Lipoprotein (HDL) at Week 96
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Total Cholesterol at Week 24
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Total Cholesterol at Week 48
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Total Cholesterol at Week 96
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Triglycerides at Week 24
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Triglycerides at Week 48
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Triglycerides at Week 96
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Low-density Lipoprotein (LDL) at Week 24
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Low-density Lipoprotein (LDL) at Week 48
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Low-density Lipoprotein (LDL) at Week 96
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Treatment-emergent Division of AIDS (DAIDS) Toxicities at Week 24
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Treatment-emergent Division of AIDS (DAIDS) Toxicities at Week 48
NCT00549198 (58) [back to overview]Percent Change From Baseline in Lumbar Spine Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 48
NCT00549198 (58) [back to overview]Number of Participants Meeting World Health Organization (WHO) Criteria for Osteopenia (T-score of -2.5 to -1.0) and Osteoporosis (T-score of <-2.5) at Week 24
NCT00549198 (58) [back to overview]Number of Participants Experiencing an Adverse Event (AE) Leading to Discontinuation by Week 96
NCT00549198 (58) [back to overview]Number of Participants Meeting World Health Organization (WHO) Criteria for Osteopenia (T-score of -2.5 to -1.0) and Osteoporosis (T-score of <-2.5) at Week 48
NCT00549198 (58) [back to overview]Number of Participants Meeting World Health Organization (WHO) Criteria for Osteopenia (T-score of -2.5 to -1.0) and Osteoporosis (T-score of <-2.5) at Week 96
NCT00549198 (58) [back to overview]Number of Participants With a Decline From Baseline in Lumbar Spine and Hip Bone Mineral Density (BMD) >=2.0% and >=6.0% at Week 24
NCT00549198 (58) [back to overview]Number of Participants With a Decline From Baseline in Lumbar Spine and Hip Bone Mineral Density (BMD) >=2.0% and >=6.0% at Week 48
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting High-density Lipoprotein (HDL) at Week 48
NCT00549198 (58) [back to overview]Number of Participants With the Indicated Treatment-emergent Division of AIDS (DAIDS) Toxicities at Week 96
NCT00549198 (58) [back to overview]Number of Participants With a Decline From Baseline in Lumbar Spine and Hip Bone Mineral Density (BMD) >=2.0% and >=6.0% at Week 96
NCT00549198 (58) [back to overview]Number of Participants With Decline From Baseline in Estimated GFR, Calculated by MDRD and Cockcroft-Gault Equations, of >=10 mL/Min/1.73 m^2 (mL/Min for Cockcroft-Gault), >=20 mL/Min/1.72 m^2, >=10%, and >=20% at Week 24
NCT00549198 (58) [back to overview]Number of Participants With Decline From Baseline in Estimated GFR, Calculated by MDRD and Cockcroft-Gault Equations, of >=10 mL/Min/1.73m^2 (mL/Min for Cockcroft-Gault), >=20 mL/Min/1.72m^2, >=10%, and >=20% at Week 48
NCT00549198 (58) [back to overview]Number of Participants With Decline From Baseline in Estimated GFR, Calculated by MDRD and Cockcroft-Gault Equations, of >=10 mL/Min/1.73m^2 (mL/Min for Cockcroft-Gault), >=20 mL/Min/1.72m^2, >=10%, and >=20% at Week 96
NCT00549198 (58) [back to overview]Number of Participants With HIV-1 RNA <50 Copies/Milliliter (c/mL) and 400 c/mL at Week 24
NCT00549198 (58) [back to overview]Number of Participants Experiencing an Adverse Event (AE) Leading to Discontinuation by Week 48
NCT00549198 (58) [back to overview]Number of Participants Experiencing an Adverse Event (AE) Leading to Discontinuation by Week 24
NCT00549198 (58) [back to overview]Number of Participants Classified as Protocol-defined Failures With Treatment-emergent Resistance to Study Drug in the Indicated Viruses at Week 96
NCT00549198 (58) [back to overview]"Number of Participants Who Indicated Yes or No to the Question of Whether Unplanned Healthcare Resources Were Utilized"
NCT00549198 (58) [back to overview]Percent Change From Baseline in Lumbar Spine Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 96
NCT00549198 (58) [back to overview]Percent Change From Baseline in Lumbar Spine Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 24
NCT00549198 (58) [back to overview]Percent Change From Baseline in Hip Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 96
NCT00549198 (58) [back to overview]Percent Change From Baseline in Hip Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 48
NCT00549198 (58) [back to overview]Percent Change From Baseline in Hip Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 24
NCT00661960 (1) [back to overview]the Percentage of CD3+/CD4+ Cells Per Cubic Millimeter at the Effector Sites in the Duodenal Tissues Obtained From Volunteers to the Antiretroviral Therapy Regimen Over Time.
NCT00668395 (1) [back to overview]Effect of CYP2B6 Genotype on Efavirenz Clearance
NCT00727597 (2) [back to overview]Number of Subjects Developing Any Treatment-related Grade 3-4 Adverse Events
NCT00727597 (2) [back to overview]Number of Subjects Needing to Switch Comparator Drugs (FPV/r or EFV)
NCT00734344 (32) [back to overview]Mean Platelet Count Between Treatment Groups at 2 Months
NCT00734344 (32) [back to overview]Mean Platelet Count Between Treatment Groups at 4 Months
NCT00734344 (32) [back to overview]Mean Platelet Count Between Treatment Groups at 6 Months
NCT00734344 (32) [back to overview]Mean Platelet Count Between Treatment Groups at 8 Months
NCT00734344 (32) [back to overview]Mean White Blood Cell Count Between Treatment Groups at 10 Months
NCT00734344 (32) [back to overview]Mean Hematocrit Between Treatment Groups at 4 Months
NCT00734344 (32) [back to overview]Mean Hematocrit Between Treatment Groups at 6 Months
NCT00734344 (32) [back to overview]Mean Hematocrit Between Treatment Groups at 8 Months
NCT00734344 (32) [back to overview]Mean Platelet Count Between Treatment Groups at 10 Months
NCT00734344 (32) [back to overview]Mean Platelet Count Between Treatment Groups at 12 Months
NCT00734344 (32) [back to overview]Mean White Blood Cell Count Between Treatment Groups at 4 Months
NCT00734344 (32) [back to overview]Mean White Blood Cell Count Between Treatment Groups at 2 Months
NCT00734344 (32) [back to overview]Mean White Blood Cell Count Between Treatment Groups at 14 Months
NCT00734344 (32) [back to overview]Mean White Blood Cell Count Between Treatment Groups at 12 Months
NCT00734344 (32) [back to overview]Mean Hematocrit Between Treatment Groups at 2 Months
NCT00734344 (32) [back to overview]Mean White Blood Cell Count Between Treatment Groups at 8 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 10 Months
NCT00734344 (32) [back to overview]Mean White Blood Cell Count Between Treatment Groups at 6 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 1 Months
NCT00734344 (32) [back to overview]Mean Platelet Count Between Treatment Groups at 14 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 11 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 2 Months
NCT00734344 (32) [back to overview]Mean Hematocrit Between Treatment Groups at 12 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 3 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 4 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 5 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 6 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 7 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 8 Months
NCT00734344 (32) [back to overview]Mean CD4 Count Between Treatment Groups at 9 Months
NCT00734344 (32) [back to overview]Mean Hematocrit Between Treatment Groups at 10 Months
NCT00734344 (32) [back to overview]Mean Hematocrit Between Treatment Groups at 14 Months
NCT00752856 (4) [back to overview]Compare Early Activated CD4+ T-cell Recovery Rates From Baseline to Week 4.
NCT00752856 (4) [back to overview]Compare Late Activated CD4+ T-cell Recovery Rates Between Treatment Regimens From Baseline to Week 48
NCT00752856 (4) [back to overview]Viral Suppression Efficacy at 48 Weeks
NCT00752856 (4) [back to overview]To Compare the Phase 1 Viral Decay Rates Between LPV/r + RAL vs. EFV/TDF/FTC Treatment Combinations.
NCT00775606 (6) [back to overview]Naive, Central Memory, Effector Memory, and T Reg CD4+ T-cell Frequency
NCT00775606 (6) [back to overview]Activated and Regulatory CD4+ and CD8+ T-cell Frequencies
NCT00775606 (6) [back to overview]CD4+ T-cell Change
NCT00775606 (6) [back to overview]CD4+ (Cluster of Differentiation 4) T-cell Apoptosis
NCT00775606 (6) [back to overview]Naive, Central Memory, Effector Memory, and T Reg CD4+ T-cell Frequency
NCT00775606 (6) [back to overview]Activation and Proliferation of CD4+ and CD8+ T-cell Frequencies
NCT00810303 (18) [back to overview]AUC of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz) on Study Days 1-5
NCT00810303 (18) [back to overview]AUC0-24h of Efavirenz (Steady State Pharmacokinetic After Chronic Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Day 30
NCT00810303 (18) [back to overview]AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30
NCT00810303 (18) [back to overview]AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15
NCT00810303 (18) [back to overview]AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30
NCT00810303 (18) [back to overview]AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16
NCT00810303 (18) [back to overview]AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15
NCT00810303 (18) [back to overview]Cmax of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Days 16-20
NCT00810303 (18) [back to overview]Cmax of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz) on Study Days 1-5
NCT00810303 (18) [back to overview]Cmax of Efavirenz (Steady State Pharmacokinetic After Chronic Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Day 30
NCT00810303 (18) [back to overview]Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30
NCT00810303 (18) [back to overview]Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16
NCT00810303 (18) [back to overview]Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15
NCT00810303 (18) [back to overview]Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30
NCT00810303 (18) [back to overview]Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16
NCT00810303 (18) [back to overview]Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15
NCT00810303 (18) [back to overview]AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16
NCT00810303 (18) [back to overview]AUC of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Days 16-20
NCT00862823 (2) [back to overview]Maximum Concentration for Tenofovir, Emtricitabine and Efavirenz
NCT00862823 (2) [back to overview]Area Under the Concentration Time Curve for Tenofovir, Emtricitabine and Efavirenz
NCT00870363 (4) [back to overview]Trough Plasma and Tissue Drug Levels in Volunteers at the Time of the Upper Endoscopy
NCT00870363 (4) [back to overview]Change in the Density of CD3+/CD4+ Cells Per Cubic Millimeter at the Effector Sites in the Duodenal Tissues Following Antiretroviral Therapy Regimen
NCT00870363 (4) [back to overview]Changes in CD4+ T-cell Numbers by Treatment Regimen
NCT00870363 (4) [back to overview]Change in HIV DNA Per 10^6 Cells in Duodenal Tissue Versus PBMC by Drug Regimen Received
NCT00884793 (4) [back to overview]Number of Subjects Who Had a Decrease in HIV RNA Per Million CD4+ T Cells in the Ileum
NCT00884793 (4) [back to overview]Number of Subjects Who Experienced an Increase in CD4+ T Cells (as a % of All Cells) in the Ileum.
NCT00884793 (4) [back to overview]Number of Subjects Who Experienced an Increase in CD4% in the Ileum.
NCT00884793 (4) [back to overview]"Average Change in Activated (CD38+HLADR+) CD8+ T Cells in the Ileum"
NCT00903682 (7) [back to overview]Resistance Determinations
NCT00903682 (7) [back to overview]Mean Change From Baseline in CD4+ Cell Count
NCT00903682 (7) [back to overview]Proportion of Patients With at Least 1 Treatment-emergent Grade 1-4 Central Nervous System or Psychiatric Adverse Event
NCT00903682 (7) [back to overview]Neuropsychiatric Adverse Events by Week 48
NCT00903682 (7) [back to overview]Antiviral Activity of ETR vs. EFV
NCT00903682 (7) [back to overview]Antiviral Activity of ETR vs. EFV
NCT00903682 (7) [back to overview]Mean Change From Baseline in Neuropsychiatric and Total Tolerabililty Score
NCT00924898 (6) [back to overview]Time to HIV RNA Suppression <50 Copies/mL
NCT00924898 (6) [back to overview]Number of Participants Without Virologic Failure at Week 48
NCT00924898 (6) [back to overview]Number of Participants Without Virologic Failure at Week 24
NCT00924898 (6) [back to overview]Number of Participants With HIV RNA Suppression at Week 96
NCT00924898 (6) [back to overview]Number of Participants With Baseline Genotypic Resistance to One or More Antiretroviral Drugs in the Study Treatment
NCT00924898 (6) [back to overview]Number of Participants With Baseline Genotypic Resistance to Antiretroviral Medications
NCT00951015 (22) [back to overview]Relationship Between the Change From Baseline in CD4+ Cell Counts at Week 96 and the Indicated Plasma DTG PK Parameters
NCT00951015 (22) [back to overview]Number of Participants With Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) <50 Copies/Milliliter (c/mL) at Week 16
NCT00951015 (22) [back to overview]Relationship Between the Change From Baseline in Plasma HIV-1 RNA at Week 2 and the Indicated Plasma DTG PK Parameters
NCT00951015 (22) [back to overview]Relationship Between the Indicated Safety Parameters at Week 96 and the Indicated Plasma DTG PK Parameters
NCT00951015 (22) [back to overview]Pre-dose Concentration (C0) and C0 Avg of DTG
NCT00951015 (22) [back to overview]Relationship Between Gastrointestinal System Organ Class AEs of Special Interest at Week 96 and the Indicated Plasma DTG PK Parameters
NCT00951015 (22) [back to overview]Plasma DTG Concentration
NCT00951015 (22) [back to overview]Number of Participants With the Indicated Type of HIV-1 Disease Progression (AIDS or Death)
NCT00951015 (22) [back to overview]Number of Participants With the Indicated Treatment-emergent Integrase (IN) Mutations Detected at the Time of Protocol-defined Virologic Failure (PDVF), as a Measure of Genotypic Resistance
NCT00951015 (22) [back to overview]Number of Participants With the Indicated Grade 1 to Grade 4 Treatment-emergent Clinical Chemistry and Hematology Toxicities
NCT00951015 (22) [back to overview]Time to Maximal Drug Concentration (Tmax) of DTG
NCT00951015 (22) [back to overview]Number of Participants With the Indicated Treatment-emergent Major Mutations of Other Classes Detected at the Time of Protocol-defined Virologic Failure (PDVF), as a Measure of Genotypic Resistance
NCT00951015 (22) [back to overview]Number of Participants With the Indicated Fold Increase in DTG FC (Fold Change in IC50 Relative to Wild-type Virus) at the Time of PDVF, as a Measure of Post-Baseline Phenotypic Resistance
NCT00951015 (22) [back to overview]Viral Change Over the Initial 2 Weeks of Treatment
NCT00951015 (22) [back to overview]Change From Baseline in Cluster of Differentiation 4+ (CD4+) Cell Counts at the Indicated Time Points
NCT00951015 (22) [back to overview]AUC(0-tau) of DTG
NCT00951015 (22) [back to overview]Change From Baseline in HIV-1 RNA at the Indicated Time Points
NCT00951015 (22) [back to overview]Number of Participants With Any Adverse Event (AE) and Any Serious Adverse Events (SAE)
NCT00951015 (22) [back to overview]Number of Participants With New HIV-associated Conditions of the Indicated Class
NCT00951015 (22) [back to overview]Number of Participants With Plasma HIV-1 RNA <400 c/mL
NCT00951015 (22) [back to overview]Number of Participants With Plasma HIV-1 RNA <50 c/mL
NCT00951015 (22) [back to overview]Maximal Concentration (Cmax), Minimal Concentration (Cmin), and Concentration at the End of Dosing Interval (Ctau) of DTG
NCT00960570 (3) [back to overview]Area Under the Concentration Versus Time Curve From Time 0 to Time t [AUC(0-t)]
NCT00960570 (3) [back to overview]Maximum Plasma Concentration (Cmax) of Efavirenz
NCT00960570 (3) [back to overview]Area Under the Concentration Versus Time Curve From Time 0 Extrapolated to Infinity [AUC(0-∞)]
NCT00964002 (2) [back to overview]Percentage of Participants Without Prostate-specific Antigen Progression at 3 Months
NCT00964002 (2) [back to overview]Percentage of Participants Without Prostate-specific Antigen Progression at 6 Months
NCT00978068 (6) [back to overview]Incidence-density of Malaria Defined as the Number of Incident Episodes of Malaria Per Time at Risk.
NCT00978068 (6) [back to overview]Percentage of Uncomplicated Malaria Episodes With Accompanying Adverse Events That Occurred in the 28 Days Following Antimalarial Therapy
NCT00978068 (6) [back to overview]28-day Risk of Recurrent Parasitemia
NCT00978068 (6) [back to overview]63-day Risk of Recurrent Malaria
NCT00978068 (6) [back to overview]Estimates of the 6-month Risk of a First Episode of Malaria
NCT00978068 (6) [back to overview]Incidence-density of Malaria Defined as the Number of Incident Episodes of Complicated Malaria Per Time at Risk.
NCT00993031 (14) [back to overview]Prevalence of Malaria Defined as Positive Placental Blood Smear
NCT00993031 (14) [back to overview]Prevalence of Malaria Defined as Positive Placental Blood PCR
NCT00993031 (14) [back to overview]Prevalence of Composite Clinical Outcome Defined by LBW, Stillbirth(Intrauterine Fetal Demise >20wks GA), Late Spontaneous Abortion(Miscarriage 12-20wks GA), Preterm Delivery(<37wks Gestation), Neonatal Death(Death of Liveborn Infant Within First 28days)
NCT00993031 (14) [back to overview]Number of Participants With Grade 3 or 4 Toxicity in the Two Treatment Groups in Women
NCT00993031 (14) [back to overview]Maternal Malaria Defined as the Number of Treatments for New Episodes of Malaria Per Time at Risk After Pregnancy
NCT00993031 (14) [back to overview]Incidence of Pre-eclampsia Defined by Hypertension > 140/90 on Two Occasions Measured > 6 Hours Apart With ≥1+ Proteinuria on Clean Catch Urine Dipstick
NCT00993031 (14) [back to overview]Change in Maternal CD4 Cell Counts
NCT00993031 (14) [back to overview]ART Levels in Hair Samples at Delivery
NCT00993031 (14) [back to overview]Maternal Malaria Defined as the Number of Treatments for New Episodes of Malaria Per Time at Risk During Pregnancy
NCT00993031 (14) [back to overview]Placental Malaria Defined Placental Histopathologic Analysis
NCT00993031 (14) [back to overview]Placental Malaria Defined as Positive Placental RDT
NCT00993031 (14) [back to overview]Number of Participants With Severe Maternal Anemia Defined by Hemoglobin < 8g/dl at Any Point During the Trial in Each Treatment Group
NCT00993031 (14) [back to overview]Number of Participants With Maternal to Child Transmission of HIV, Measured by Infant HIV DNA PCR
NCT00993031 (14) [back to overview]Number of Participants With Maternal HIV RNA Suppression of <400 Copies/mL
NCT01011413 (8) [back to overview]Percentage of Participants With Plasma HIV-1 RNA <400 Copies/mL and <50 Copies/mL at 48 and 96 Weeks After Randomisation
NCT01011413 (8) [back to overview]Change From Baseline in Estimate Creatinine Clearance
NCT01011413 (8) [back to overview]Mean Change From Baseline in CD4+ T-cell Count
NCT01011413 (8) [back to overview]Change From Baseline in Fasted Insulin Levels
NCT01011413 (8) [back to overview]Percentage of Participants With Plasma HIV-1 RNA <200 Copies/mL 48 Weeks After Randomisation
NCT01011413 (8) [back to overview]Change in Selected Serum Biochemical Parameters
NCT01011413 (8) [back to overview]Change From Baseline in Metabolic Endpoints
NCT01011413 (8) [back to overview]Steady-state Efavirenz Concentrations
NCT01075152 (10) [back to overview]Safety of ART Initiation
NCT01075152 (10) [back to overview]Percentage of Participants, Per CSF WBC Subgroup, Who Died by Week 26
NCT01075152 (10) [back to overview]Microbiologic Clearance
NCT01075152 (10) [back to overview]Karnofsky Functional Status
NCT01075152 (10) [back to overview]46-week Survival
NCT01075152 (10) [back to overview]Antiretroviral Therapy Tolerability
NCT01075152 (10) [back to overview]HIV-1 Viral Suppression
NCT01075152 (10) [back to overview]Incidence of Cryptococcal-relapse
NCT01075152 (10) [back to overview]Incidence of Immune Reconstitution Inflammatory Syndrome
NCT01075152 (10) [back to overview]Mortality
NCT01087814 (1) [back to overview]Serum Levels of Efavirenz
NCT01104376 (1) [back to overview]Measure Efavirenz Clearance
NCT01146873 (5) [back to overview]Percentage of Participants With Elevated Total Cholesterol, Elevated LDL, Abnormal HDL, or Abnormal Triglycerides at 40 Weeks After Randomization
NCT01146873 (5) [back to overview]Highest Grade ALT After Randomization
NCT01146873 (5) [back to overview]Viral Rebound
NCT01146873 (5) [back to overview]Viral Failure
NCT01146873 (5) [back to overview]CD4 Cell Percentage at 48 Weeks After Randomization
NCT01147107 (1) [back to overview]Rates of Grade 2 and Higher Alanine Aminotransferase (ALT) Elevations
NCT01195467 (2) [back to overview]The Rate of Neuropsychiatric and Central Nervous System (CNS) Toxicity of Raltegravir Therapy After 12 Weeks on Treatment
NCT01195467 (2) [back to overview]The Rate of Neuropsychiatric and Central Nervous System (CNS) Toxicity of Raltegravir Therapy After 4 Weeks on Treatment
NCT01231555 (13) [back to overview]Change From Baseline (Day 1) in Plasma HIV-1 RNA Over Period
NCT01231555 (13) [back to overview]Number of Participants Discontinuing the Study Drugs Due to AEs
NCT01231555 (13) [back to overview]Change From Baseline (Day 1) in Plasma HIV-1 RNA Over Period
NCT01231555 (13) [back to overview]Number of Participants With HIV Disease Progression
NCT01231555 (13) [back to overview]Minimum and Maximum Plasma GSK2248761 Concentration at Week 2
NCT01231555 (13) [back to overview]Number of Participants With Serious Adverse Events (SAEs) and Adverse Events (AEs)
NCT01231555 (13) [back to overview]Number of Participants With Plasma HIV-1 RNA Below 50 Copies/mL as a Function of Viral Load
NCT01231555 (13) [back to overview]Number of Participants With HIV Associated Conditions
NCT01231555 (13) [back to overview]Number of Participants With Plasma HIV-1 RNA Below 50 Copies/mL as a Function of Viral Load
NCT01231555 (13) [back to overview]Number of Participants With Changes in Electrocardiogram (ECG) From Baseline (Day 1) Over 16 Weeks
NCT01231555 (13) [back to overview]Number of Participants With Changes in Electrocardiogram (ECG) From Baseline (Day 1) Over 16 Weeks
NCT01231555 (13) [back to overview]Change From Baseline (Day 1) in Plasma HIV-1 RNA Over Period
NCT01231555 (13) [back to overview]Number of Participants With Plasma HIV-1 RNA Below 50 Copies/mL as a Function of Viral Load
NCT01254656 (7) [back to overview]Change From Baseline in CD4+ Lymphocyte Counts (Absolute) at 192 Weeks From Day 1 of the Parent Protocol
NCT01254656 (7) [back to overview]Change From Baseline in CD4+ Lymphocyte Counts (Absolute) at 144 Weeks From Day 1 of the Parent Protocol
NCT01254656 (7) [back to overview]Change From Baseline in CD4+ Lymphocyte Counts (Percentage) at 144 Weeks From Day 1 of the Parent Protocol
NCT01254656 (7) [back to overview]Change From Baseline in CD4+ Lymphocyte Counts (Percentage) at 192 Weeks From Day 1 of the Parent Protocol
NCT01254656 (7) [back to overview]Number of Participants With Plasma HIV-1 RNA Level <50 Copies/mL up to Week 208
NCT01254656 (7) [back to overview]Number of Participants With Plasma Human Immunodeficiency Virus - 1 (HIV-1) Ribonucleic Acid (RNA) Level <50 Copies/mL at 144 Weeks From Day 1 of the Parent Protocol
NCT01254656 (7) [back to overview]Virology Analysis Participant Accountability From Week 96 Through Study Termination
NCT01270802 (2) [back to overview]Change in Flow-mediated Dilation (FMD) of the Brachial Artery
NCT01270802 (2) [back to overview]Change in Serum Levels of Vitamin D
NCT01352117 (12) [back to overview]Percentage of Participants With Etoposide Dose Modification
NCT01352117 (12) [back to overview]Percentage of Participants With HIV-1 RNA Suppression
NCT01352117 (12) [back to overview]Percentage of Participants With HIV-1 RNA Suppression
NCT01352117 (12) [back to overview]Cumulative Incidence of Initial KS Partial or Complete Response by Week 96
NCT01352117 (12) [back to overview]Cumulative Incidence of Initial KS Progressive Disease by Week 96
NCT01352117 (12) [back to overview]Cumulative Incidence of KS Progressive Disease After Initiation of Delayed Etoposide in Arm A
NCT01352117 (12) [back to overview]Cumulative Incidence of KS Response After Initiation of Delayed Etoposide in Arm A
NCT01352117 (12) [back to overview]Cumulative Incidence of KS-IRIS
NCT01352117 (12) [back to overview]Number of Participants With Grade 3 or Higher Adverse Events
NCT01352117 (12) [back to overview]Change in Peripheral Blood CD4+ Lymphocyte Cell Count
NCT01352117 (12) [back to overview]Change in Peripheral Blood CD4+ Lymphocyte Cell Count
NCT01352117 (12) [back to overview]Percentage of Participants With ARV Dose Modification
NCT01380080 (16) [back to overview]Cumulative Probability of Death by Week 24
NCT01380080 (16) [back to overview]Cumulative Probability of Death or AIDS Progression by Week 24
NCT01380080 (16) [back to overview]Cumulative Probability of Death or AIDS Progression by Week 48
NCT01380080 (16) [back to overview]CD4+ T-cell Count Change From Baseline
NCT01380080 (16) [back to overview]Proportion of Participants With HIV-1 RNA Level <400 Copies/mL
NCT01380080 (16) [back to overview]CD4+ T-cell Count
NCT01380080 (16) [back to overview]Time to Initiation of TB Treatment by Week 96
NCT01380080 (16) [back to overview]Proportion of Participants With TB Diagnosis by Week 96
NCT01380080 (16) [back to overview]Proportion of Participants With Reportable Hospitalization by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants With Immune Reconstitution Inflammatory Syndrome (IRIS) by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants With at Least One New Grade 3 or 4 Targeted Laboratory Value That is at Least a One-grade Increase From Baseline by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants With at Least One New Grade 3 or 4 Adverse Event That is at Least a One-grade Increase From Baseline by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants Who Prematurely Discontinued Antiretroviral Therapy by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants Who Prematurely Discontinued Any Component of TB Treatment by Week 48
NCT01380080 (16) [back to overview]Cumulative Probability of First AIDS Progression by Week 96
NCT01380080 (16) [back to overview]Cumulative Probability of Death or Unknown Vital Status by Week 24
NCT01387022 (4) [back to overview]The Antiretroviral Treatment Failure Rate at 12 Months.
NCT01387022 (4) [back to overview]Tenofovir Resistance, Defined as Presence of K65R, K70E or Any of the TAMS Mutations
NCT01387022 (4) [back to overview]Reported Adverse Events With Severity Grades 3 and 4 Based on the DAIDS Toxicity Grading Tables
NCT01387022 (4) [back to overview]Change in CD4+ Cell Count From Randomisation to 12 Months Post-randomisation
NCT01410058 (3) [back to overview]AUC
NCT01410058 (3) [back to overview]C12h
NCT01410058 (3) [back to overview]Cmax
NCT01435018 (37) [back to overview]Cumulative Rate of KS Progression, Death, AIDS Defining Event, or Virologic Failure by Week 48 for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of KS Progression, Death, AIDS Defining Event, or Virologic Failure by Week 48 for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of IERC-confirmed KS Progression by Week 48 for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of HIV-1 RNA Virologic Failure by Week 48 for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of HIV-1 RNA Virologic Failure by Week 48 for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of Death for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of Death for BV+ART vs PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of KS Progression, Death, or AIDS Defining Event by Week 48 for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of IERC-confirmed KS Progression by Week 48 for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of Death by Week 48 for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of Change in KS Treatment by Week 48 for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of Change in KS Treatment by Week 48 for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of AIDS-defining Event by Week 48 for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of AIDS-defining Event by Week 48 for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of KS Progression, Death, or AIDS Defining Event by Week 48 for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of Death by Week 48 for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of KS Progression, Death, AIDS Defining Event, Virologic Failure, or KS-IRIS by Week 48 for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of KS Progression, Death, AIDS Defining Event, Virologic Failure, or KS-IRIS by Week 48 for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Self-reported Adherence to ART Therapy
NCT01435018 (37) [back to overview]Number of Participants With Treatment-related Toxicities and Adverse Events (AEs)
NCT01435018 (37) [back to overview]Number of Participants With Symptomatic Peripheral Neuropathy (SPN)
NCT01435018 (37) [back to overview]Number of Participants With Peripheral Neuropathy (PN)
NCT01435018 (37) [back to overview]Number of Participants With IERC-Confirmed KS Disease Progression, Dose-Limiting Toxicity, Death, AIDS-Defining Events, Virologic Failure and Objective Response in Step 4
NCT01435018 (37) [back to overview]Number of Participants With IERC-Confirmed KS Disease Progression, Dose-Limiting Toxicity, Death, AIDS-Defining Events, Virologic Failure and Objective Response in Step 3
NCT01435018 (37) [back to overview]Number of Participants With IERC-Confirmed KS Disease Progression, Dose-Limiting Toxicity, Death, AIDS-Defining Events, Virologic Failure and Objective Response in Step 2
NCT01435018 (37) [back to overview]Changes in CD4+ Lymphocyte Cell Count for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Changes in CD4+ Lymphocyte Cell Count for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Time to IERC-confirmed KS Progression or Death for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Time to IERC-confirmed KS Progression or Death for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Number of Participants With Objective Response for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Number of Participants With Objective Response for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Number of Participants With Kaposi's Sarcoma-Immune Reconstitution Inflammatory Syndrome (KS-IRIS) for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Number of Participants With Kaposi's Sarcoma-Immune Reconstitution Inflammatory Syndrome (KS-IRIS) for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Duration of Objective Response for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Duration of Objective Response for BV+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of Progression-Free Survival by Week 48 for ET+ART vs. PTX+ART
NCT01435018 (37) [back to overview]Cumulative Rate of Progression-Free Survival by Week 48 for BV+ART vs. PTX+ART
NCT01472380 (3) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time 0 to Time t[AUC(0-t)]
NCT01472380 (3) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time 0 Extrapolated to Infinity [AUC(0-infinity]
NCT01472380 (3) [back to overview]Pharmacokinetics: Maximum Plasma Concentration (Cmax)
NCT01516970 (4) [back to overview]Percentage of Participants Who Developed Detectable HIV Antibodies
NCT01516970 (4) [back to overview]Worst Sheehan Disability Scale (SDS) Score for the Safety Population
NCT01516970 (4) [back to overview]Number of Participants With Early Discontinuation From Randomized Human Immunodeficiency Virus Postexposure Prophylaxis (HIV PEP)
NCT01516970 (4) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT01585038 (4) [back to overview]Oxidative Stress Markers
NCT01585038 (4) [back to overview]Change in Flow-mediated Dilation of the Brachial Artery
NCT01585038 (4) [back to overview]Endothelial Activation Markers
NCT01585038 (4) [back to overview]Inflammatory Markers
NCT01618305 (17) [back to overview]Proportion of Women With HIV-1 Drug Resistance Mutations at Screening, 2-4 Weeks Postpartum in Women Who Stopped Antiretroviral Therapy, and at the Time of Inadequate Virologic Response Using Standard and Ultrasensitive Methods.
NCT01618305 (17) [back to overview]Proportion of Women Who Achieved HIV-1 RNA Virologic Suppression Below the Lower Limit of Quantification of the Assay at Delivery
NCT01618305 (17) [back to overview]Proportion of Women With 1) Successful Viral Load (Plasma HIV-1 RNA VL) Decrease From Entry to Week 2 and VL Less Than 1,000 Copies/ml at All Time Points After 4 Weeks on Study Drugs, Until Delivery; and 2) Who Remain on the Assigned Study Regimen
NCT01618305 (17) [back to overview]Proportion of Women With HIV-1 Drug Resistance Mutations at Screening, 2-4 Weeks Postpartum in Women Who Stopped Antiretroviral Therapy, and at the Time of Inadequate Virologic Response Using Standard and Ultrasensitive Methods.
NCT01618305 (17) [back to overview]Proportion of Women With HIV-1 RNA Plasma Viral Load Less Than 200 Copies/mL at Weeks 4 and 6 From Treatment Initiation
NCT01618305 (17) [back to overview]Proportion of Women With HIV-1 RNA Vaginal Viral Load Less Than 1200 Copies/mL at Weeks 4 and 6 From Treatment Initiation
NCT01618305 (17) [back to overview]Proportion of Deliveries With a Low Birth Weight (Less Than 2,500 Grams)
NCT01618305 (17) [back to overview]Proportion of Deliveries That Had an Outcome of a Stillbirth/Fetal Demise.
NCT01618305 (17) [back to overview]Proportion of Deliveries That Were Extremely Premature (Less Than 34 Weeks Gestation).
NCT01618305 (17) [back to overview]Proportion of Deliveries That Were Premature (Less Than 37 Weeks Gestation)
NCT01618305 (17) [back to overview]Proportion of Women Who Experienced at Least One New Adverse Event of Greater Than or Equal to Grade 3 as Defined in the Division of AIDS (DAIDS) Toxicity Table
NCT01618305 (17) [back to overview]Proportion of Deliveries With an Extremely Low Birth Weight (<1,500 Grams).
NCT01618305 (17) [back to overview]Proportion of Infants Who Experienced at Least One Adverse Event of Greater Than or Equal to Grade 3.
NCT01618305 (17) [back to overview]Proportion of Participants Who Discontinued Randomized Study Drug Prior to Labor and Delivery.
NCT01618305 (17) [back to overview]Proportion of Women With Plasma HIV-1 RNA Viral Load Less Than 200 Copies/mL at Delivery
NCT01618305 (17) [back to overview]Log10 Change in Viral Load From Entry to Each Time Point Prior to Delivery
NCT01618305 (17) [back to overview]Proportion of HIV-infected Infants With Genotypic Resistance to Study Drugs
NCT01632345 (19) [back to overview]Change From Baseline in CD4 Cell Count at Week 24: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Change From Baseline in CD4 Cell Count at Week 48: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Change From Baseline in CD4 Cell Count at Week 96: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Change From Baseline in CD4 T Lymphocyte Cell Count at Week 24: Doravirine (All Doses) vs Efavirenz (Part I)
NCT01632345 (19) [back to overview]Percentage of Participants Who Discontinued Study Therapy Due to AEs in Weeks 0-24: Doravirine (All Doses) vs Efavirenz (Part I)
NCT01632345 (19) [back to overview]Percentage of Participants With At Least 1 AE in Weeks 0-24: Doravirine (All Doses) vs Efavirenz (Part I)
NCT01632345 (19) [back to overview]Percentage of Participants With At Least 1 AE in Weeks 0-24: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With CNS Events by Week 24: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With Virologic Response (HIV-1 RNA <200 Copies/mL) at Week 24: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With CNS Events by Week 8: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With At Least 1 AE in Weeks 0-96: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With At Least 1 AE in Weeks 0-48: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With Virologic Response (HIV-1 RNA) < 40 Copies/mL) at Week 24: Doravirine (All Doses) vs Efavirenz (Part I)
NCT01632345 (19) [back to overview]Percentage of Participants With Virologic Response (HIV-1 RNA <40 Copies/mL) at Week 96: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With Virologic Response (HIV-1 RNA <40 Copies/mL) at Week 48: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With Virologic Response (HIV-1 RNA <40 Copies/mL) at Week 24: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With Virologic Response (HIV-1 RNA <200 Copies/mL) at Week 96: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With Virologic Response (HIV-1 RNA <200 Copies/mL) at Week 48: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)
NCT01632345 (19) [back to overview]Percentage of Participants With Virologic Response (HIV-1 RNA <200 Copies/mL) at Week 24: Doravirine (All Doses) vs Efavirenz (Part I)
NCT01632891 (7) [back to overview]Change in log10(Pf Parasite Density) From Entry to Day 30
NCT01632891 (7) [back to overview]Number of Participants With Uncomplicated Clinical Malaria
NCT01632891 (7) [back to overview]Time to First Pf SCP Clearance
NCT01632891 (7) [back to overview]Log10(Pf Parasite Density)
NCT01632891 (7) [back to overview]Proportion of Participants With Plasmodium Falciparum (Pf) Subclinical Parasitemia (SCP) Clearance
NCT01632891 (7) [back to overview]Number of Participants With Detectable Pf Gametocyte Density
NCT01632891 (7) [back to overview]Change in log10(Pf Gametocyte Density) From Entry to Day 30
NCT01641809 (57) [back to overview]Number of Participants With Adherence to Study Treatment
NCT01641809 (57) [back to overview]Number of Participants With Adherence to Study Treatment
NCT01641809 (57) [back to overview]Change From Baseline in Total Neutrophils, Platelet Count and WBC Count Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in Total Neutrophils, Platelet Count and WBC Count Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in Plasma log10 HIV-1 RNA Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in Plasma log10 HIV-1 RNA Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in Hemoglobin Level Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in Hemoglobin Level Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in Estimated Creatinine Clearance Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in Estimated Creatinine Clearance Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in Estimated Creatinine Clearance Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in Creatinine and Total Bilirubin Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in Creatinine and Total Bilirubin Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in CD4+ Cell Count Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in CD4+ Cell Count Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in ALT, AST and CK Over Time by Visit
NCT01641809 (57) [back to overview]Change From Baseline in ALT, AST and CK Over Time by Visit
NCT01641809 (57) [back to overview]Absolute Values for Platelet Count, Total Neutrophils and WBC Count During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]Absolute Values for Plasma Logarithm to the Base 10 (log10) HIV-1 RNA Over Time by Visit
NCT01641809 (57) [back to overview]Absolute Values for Plasma Logarithm to the Base 10 (log10) HIV-1 RNA Over Time by Visit
NCT01641809 (57) [back to overview]Absolute Values for Hemoglobin During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]Absolute Values for Creatinine and Total Bilirubin During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]Absolute Values for Cluster of Differentiation 4+ (CD4+) Cell Count During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]Absolute Values for ALT, AST, CK During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]Percentage of Participants With HIV-1 Ribonucleic Acid (RNA) <50 Copies/Milliliter (mL) at Week 48 Using the Missing, Switch, Discontinuation Equals Failure (MSDF) Algorithm
NCT01641809 (57) [back to overview]Percentage of Participants Who Discontinued Treatment Due to Adverse Events-Maintenance Phase
NCT01641809 (57) [back to overview]Percentage of Participants Who Discontinued Treatment Due to Adverse Events-Induction Phase
NCT01641809 (57) [back to overview]Percentage of Participants Who Discontinued Investigational Product Due to Adverse Events
NCT01641809 (57) [back to overview]Number of Participants With Clinically Significant Electrocardiogram (ECG) Findings
NCT01641809 (57) [back to overview]Percentage of Participants With Plasma HIV-1 RNA <50 Copies/mL Over Time by Visit Using Observed Case Analysis
NCT01641809 (57) [back to overview]Area Under the Concentration Time Curve Over the Dosing Interval (AUC[0-tau]) for GSK1265744 at Week 2
NCT01641809 (57) [back to overview]Percentage of Participants With Plasma HIV-1 RNA <50 Copies/mL Over Time by Visit Using Observed Case Analysis
NCT01641809 (57) [back to overview]Percentage of Participants With Plasma HIV-1 RNA <400 Copies/mL Until Week 96 Using the Observed Case Analysis
NCT01641809 (57) [back to overview]Percentage of Participants With Plasma HIV-1 RNA <400 Copies/mL Until Week 96 Using the MSDF Algorithm
NCT01641809 (57) [back to overview]Percentage of Participants With HIV-1 RNA <50 Copies/mL From Week 24 Through Week 96 by Visit Using MSDF Algorithm-Maintenance Phase
NCT01641809 (57) [back to overview]Percentage of Participants With HIV-1 RNA <50 Copies/mL at Week 16 and Week 24 Using MSDF Algorithm-Induction Phase
NCT01641809 (57) [back to overview]Number of Participants With Treatment Emergent Phenotypic Resistance
NCT01641809 (57) [back to overview]Number of Participants With Treatment Emergent Genotypic Mutations Associated With Development of Resistance
NCT01641809 (57) [back to overview]Number of Participants With Post-Baseline HIV-1 Associated Conditions Progression of Disease
NCT01641809 (57) [back to overview]Number of Participants With Maximum Treatment-emergent Hematology Toxicities-Maintenance Phase
NCT01641809 (57) [back to overview]Change From Baseline in Estimated Creatinine Clearance Over Time by Visit
NCT01641809 (57) [back to overview]Maximum Observed Concentration (Cmax) for GSK1265744 at Week 2
NCT01641809 (57) [back to overview]Concentration at the End of a Dosing Interval (Ctau) for GSK1265744 at Week 2
NCT01641809 (57) [back to overview]Number of Participants With Maximum Treatment-emergent Hematology Toxicities-Induction Phase
NCT01641809 (57) [back to overview]Number of Participants With Maximum Treatment-emergent Hematology Toxicities Over Time
NCT01641809 (57) [back to overview]Number of Participants With Maximum Treatment-emergent Clinical Chemistry Toxicity-Induction Phase
NCT01641809 (57) [back to overview]Number of Participants With Maximum Treatment-emergent Clinical Chemistry Toxicities-Maintenance Phase
NCT01641809 (57) [back to overview]Number of Participants With Maximum Treatment-emergent Clinical Chemistry Toxicities Over Time
NCT01641809 (57) [back to overview]Number of Participants With AEs and SAEs-Induction Phase
NCT01641809 (57) [back to overview]Number of Participants With AEs and SAEs Over Time
NCT01641809 (57) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)-Maintenance Phase
NCT01641809 (57) [back to overview]Number of Participants With Adherence to Study Treatment
NCT01641809 (57) [back to overview]Percentage of Participants With Plasma HIV-1 RNA <50 Copies/mL Over Time by Visit Using the MSDF Algorithm
NCT01695954 (3) [back to overview]GMR of Cmax of Pitavastatin When Coadministered With Efavirenz or With Darunavir/Ritonavir
NCT01695954 (3) [back to overview]GMR of 24- Hour AUC of Pitavastatin When Coadministered With Efavirenz or With Darunavir/Ritonavir Over 24 Hour AUC of Pitavastatin
NCT01695954 (3) [back to overview]AUC
NCT01709084 (6) [back to overview]Percentage of Participants With Plasma HIV-1 RNA Levels < 50 Copies/mL at Week 48
NCT01709084 (6) [back to overview]Percentage of Participants With Plasma HIV-1 RNA Levels >= 50 Copies Per Milliliter (Copies/mL) at Week 48 Based on Time to Loss of Virologic Response (TLOVR) [Non-virologic Failure Censored] Imputation Method.
NCT01709084 (6) [back to overview]Percentage of Participants With Plasma Human Immunodeficiency Virus - Type 1 Ribonucleic Acid (HIV-1 RNA) Levels Less Than (<) 400 Copies Per Milliliter (Copies/mL) at Week 48
NCT01709084 (6) [back to overview]Percentage of Participants With Plasma HIV-1 RNA Levels More Than or Equal to (>=) 400 Copies/mL at Week 48 Based on Time to Loss of Virologic Response (TLOVR) [Non-virologic Failure Censored] Imputation Method.
NCT01709084 (6) [back to overview]Number of Participants With Treatment-Emergent Nucleoside Reverse Transcriptase Inhibitor (N[t]RTI) or Nucleoside/Nucleotide Reverse Transcriptase Inhibitor (NNRTI) Mutations
NCT01709084 (6) [back to overview]Percentage of Participant With Treatment Adherence Based on Tablet Count
NCT01837277 (1) [back to overview]Early Mortality
NCT01878890 (4) [back to overview]Number of Participants Who Experienced Dose-Limiting Toxicities (DLTs)
NCT01878890 (4) [back to overview]Maximum Tolerated Dose (MTD) of Efavirenz
NCT01878890 (4) [back to overview]12-week Objective Response Rate
NCT01878890 (4) [back to overview]12-week Non-progression Rate
NCT01903031 (21) [back to overview]EFV PK Parameter Minimum Plasma Concentration (Cmin) Determined Based on EFV Levels From Individual Participants Enrolled in Arm B
NCT01903031 (21) [back to overview]RTV PK Parameter Tmax Determined Based on RTV Levels From Individual Participants Enrolled in Arm C
NCT01903031 (21) [back to overview]RTV PK Parameter Cmin Determined Based on RTV Levels From Individual Participants Enrolled in Arm C
NCT01903031 (21) [back to overview]RTV PK Parameter Cmax Determined Based on RTV Levels From Individual Participants Enrolled in Arm C
NCT01903031 (21) [back to overview]RTV PK Parameter CLss/F Determined Based on RTV Levels From Individual Participants Enrolled in Arm C
NCT01903031 (21) [back to overview]Ritonavir (RTV) PK Parameter AUC(0-24h) Calculated Based on Intensive RTV PK Samples Obtained From Individual Participants Enrolled in Arm C
NCT01903031 (21) [back to overview]Proportion of Participants With Progesterone Levels Greater Than 5 ng/mL.
NCT01903031 (21) [back to overview]Proportion of Participants With Plasma HIV-1 RNA Levels <40 Copies/mL
NCT01903031 (21) [back to overview]Etonogestrel Concentrations Obtained on Study Days 7 and 14
NCT01903031 (21) [back to overview]Ethinyl Estradiol Concentrations Obtained on Study Days 7 and 14.
NCT01903031 (21) [back to overview]EFV PK Parameter Maximum Plasma Concentration (Cmax) Determined Based on EFV Levels From Individual Participants Enrolled in Arm B
NCT01903031 (21) [back to overview]EFV PK Parameter Clearance (CLss/F) Determined Based on EFV Levels From Individual Participants Enrolled in Arm B
NCT01903031 (21) [back to overview]EFV PK Parameter Area Under the Concentration-Time Curve (AUC0-24hours) Calculated Based on Intensive EFV PK Samples Obtained From Individual Participants Enrolled in Arm B
NCT01903031 (21) [back to overview]ATV PK Parameter Time to Cmax (Tmax) Determined Based on ATV Levels From Individual Participants Enrolled in Arm C
NCT01903031 (21) [back to overview]ATV PK Parameter Cmin Determined Based on ATV Levels From Individual Participants Enrolled in Arm C
NCT01903031 (21) [back to overview]ATV PK Parameter Cmax Determined Based on ATV Levels From Individual Participants Enrolled in Arm C
NCT01903031 (21) [back to overview]ATV PK Parameter CLss/F Determined Based on ATV Levels From Individual Participants Enrolled in Arm C
NCT01903031 (21) [back to overview]ATV PK Parameter AUC(0-24h) Calculated Based on Intensive Atazanavir (ATV) PK Samples Obtained From Individual Participants Enrolled in Arm C
NCT01903031 (21) [back to overview]Percentage of Participants With Signs and Symptoms of Grade 2 or Higher Deemed Possibly, Probably or Definitely Related to Study Treatment
NCT01903031 (21) [back to overview]Etonogestrel Concentrations at Study Day 21
NCT01903031 (21) [back to overview]Ethinyl Estradiol Concentrations at Study Day 21
NCT01989910 (3) [back to overview]The Proportion of Treatment Failure at Week 48 for Both Arms.
NCT01989910 (3) [back to overview]The Proportion of Patients Who Can Achieve of Less Than 20 HIV RNA Copies Per ml at Week 48 of Both Arms.
NCT01989910 (3) [back to overview]The Proportion of Patients With Achievement of Less Than 400 HIV RNA Copies Per ml at Week 48 for Both Arms.
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Body Mass Index-for-age Z-score
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Cessation of First-line Regimen for Clinical/Immunological Failure
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Change From Baseline in Absolute CD4 to Week 72
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Height-for-age Z-score
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: New ART-modifying Adverse Event
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: New Grade 3 or 4 Adverse Event Definitely/Probably or Uncertainly Related to ART
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: New or Recurrent WHO Stage 3 or 4 Event or Death
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: New Serious Adverse Events Not Solely Related to HIV
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: New WHO Stage 3 or 4 Event or Death
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Weight-for-age Z-score
NCT02028676 (58) [back to overview]LCM vs CDM: Change From Baseline in CD4% to Week 144
NCT02028676 (58) [back to overview]LCM vs CDM: Change From Baseline in CD4% to Week 72
NCT02028676 (58) [back to overview]LCM vs CDM: Disease Progression to a New WHO Stage 4 Event or Death
NCT02028676 (58) [back to overview]LCM vs CDM: New Grade 3 or 4 Adverse Event (AE), Not Solely Related to HIV
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks) at 48 Weeks
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks) at 96 Weeks
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: All-cause Mortality
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Body Mass Index-for-age Z-score
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 48
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 72
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 96
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 48
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 72
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 96
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Height-for-age Z-score
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: New Grade 3 or 4 Adverse Event (AE), Not Solely Related to HIV
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: New Grade 3 or 4 Adverse Event (AE), Not Solely Related to HIV, Judged Definitely/Probably or Uncertain Whether Related to Lamivudine or Abacavir
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: New Serious Adverse Events Not Solely Related to HIV
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: New WHO Stage 3 or 4 Event or Death
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: New WHO Stage 4 Event or Death
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Suppressed HIV RNA Viral Load 48 Weeks After Randomisation
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Weight-for-age Z-score
NCT02028676 (58) [back to overview]Cotrimoxazole: Change From Baseline in CD4% to Week 72
NCT02028676 (58) [back to overview]Cotrimoxazole: New Hospitalisation or Death
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Suppression of HIV RNA Viral Load 96 Weeks After Randomisation
NCT02028676 (58) [back to overview]CDM vs LCM, Induction ART: Suppression of HIV RNA Viral Load 144 Weeks After Baseline
NCT02028676 (58) [back to overview]CDM vs LCM, Induction ART: Suppression of HIV RNA Viral Load 72 Weeks After Baseline
NCT02028676 (58) [back to overview]Cotrimoxazole: All-cause Mortality
NCT02028676 (58) [back to overview]Cotrimoxazole: Body Mass Index-for-age Z-score
NCT02028676 (58) [back to overview]Cotrimoxazole: Change From Baseline in Absolute CD4 to Week 72
NCT02028676 (58) [back to overview]Cotrimoxazole: Height-for-age Z-score
NCT02028676 (58) [back to overview]Cotrimoxazole: New Clinical and Diagnostic Positive Malaria
NCT02028676 (58) [back to overview]Cotrimoxazole: New Grade 3 or 4 Adverse Event (AE), Not Solely Related to HIV
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Change From Baseline in Absolute CD4 to Week 144
NCT02028676 (58) [back to overview]Cotrimoxazole: New Serious Adverse Events Not Solely Related to HIV
NCT02028676 (58) [back to overview]Cotrimoxazole: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)
NCT02028676 (58) [back to overview]Cotrimoxazole: New Severe Pneumonia
NCT02028676 (58) [back to overview]Cotrimoxazole: New WHO Stage 3 or 4 Event or Death
NCT02028676 (58) [back to overview]Cotrimoxazole: New WHO Stage 3 Severe Recurrent Pneumonia or Diarrhoea
NCT02028676 (58) [back to overview]Cotrimoxazole: New WHO Stage 4 Event or Death
NCT02028676 (58) [back to overview]Cotrimoxazole: Weight-for-age Z-score
NCT02028676 (58) [back to overview]Induction ART: Change From Baseline in CD4% 72 Weeks After ART Initiation
NCT02028676 (58) [back to overview]Induction ART: Change From Baseline in CD4% to 144 Weeks From ART Initiation
NCT02028676 (58) [back to overview]Induction ART: New Grade 3 or 4 Adverse Event (AE), Not Solely Related to HIV
NCT02028676 (58) [back to overview]Induction ART: New WHO Stage 4 Event or Death
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: All-cause Mortality
NCT02401256 (1) [back to overview]Efavirenz AUC0-inf (Single Dose) and AUC0-24(Multiple Dose)
NCT03048422 (23) [back to overview]Cumulative Probability of Infant Deaths
NCT03048422 (23) [back to overview]Count of Infants With HIV-1 Antiretroviral Drug Resistance Mutations at the Time of Infant HIV Diagnosis
NCT03048422 (23) [back to overview]Maternal Change in Creatinine Clearance
NCT03048422 (23) [back to overview]Change in Maternal Weight Overall
NCT03048422 (23) [back to overview]Change in Maternal Weight Antepartum
NCT03048422 (23) [back to overview]Cumulative Probability of Women Experiencing Grade 3 or Higher Adverse Event
NCT03048422 (23) [back to overview]Cumulative Probability of Infants Experiencing Grade 3 or Higher Adverse Event
NCT03048422 (23) [back to overview]Cumulative Probability of Infants Experiencing Grade 3 or Higher Adverse Event
NCT03048422 (23) [back to overview]Cumulative Probability of Infant HIV-infection
NCT03048422 (23) [back to overview]Percentage of Mothers With HIV-1 RNA Viral Load Less Than 200 Copies/mL at Delivery
NCT03048422 (23) [back to overview]Infant Creatinine Clearance
NCT03048422 (23) [back to overview]Time to First HIV-1 RNA Less Than 200 Copies/mL Through Delivery
NCT03048422 (23) [back to overview]Percentage of Mothers With Virologic Success of HIV-1 RNA Less Than 200 Copies/mL at Delivery Based on FDA Snapshot Algorithm
NCT03048422 (23) [back to overview]Percentage of Mothers With Virologic Success of HIV-1 RNA Less Than 200 Copies/mL at 50 Weeks Postpartum Based on FDA Snapshot Algorithm
NCT03048422 (23) [back to overview]Percentage of Mothers With HIV-1 RNA Less Than 50 Copies/mL at Delivery Measured at Central Laboratory
NCT03048422 (23) [back to overview]Change in Maternal Weight Postpartum
NCT03048422 (23) [back to overview]Percentage of Mothers With HIV-1 RNA Less Than 200 Copies/mL at 50 Weeks Postpartum
NCT03048422 (23) [back to overview]Percentage of Mothers With HIV-1 ARV Drug Resistance Mutations at the Time of Maternal Virologic Failure
NCT03048422 (23) [back to overview]Percentage of Mother-Infant Pairs With Preterm Deliveries
NCT03048422 (23) [back to overview]Percentage of Mother-infant Pairs With an Adverse Pregnancy Outcome or Major Congenital Anomaly
NCT03048422 (23) [back to overview]Percentage of Mother-Infant Pairs With an Adverse Pregnancy Outcome
NCT03048422 (23) [back to overview]Percentage of Mother-infant Pairs With an Adverse Pregnancy Outcome
NCT03048422 (23) [back to overview]Percentage of Infants Born Small for Gestational Age
NCT04459598 (9) [back to overview]Total Apparent Clearance (CL/F) for Quizartinib Following Single Dose of Quizartinib With or Without Efavirenz
NCT04459598 (9) [back to overview]Area Under the Plasma Concentration-Time Curve up to the Last Quantifiable Concentration Post-Dose (AUClast) Following Single Dose of Quizartinib With or Without Efavirenz
NCT04459598 (9) [back to overview]Time to Maximum Plasma Concentration (Tmax) Following Single Dose of Quizartinib With or Without Efavirenz
NCT04459598 (9) [back to overview]Volume of Distribution in the Terminal Phase (Vz/F) for Quizartinib Following Single Dose of Quizartinib With or Without Efavirenz
NCT04459598 (9) [back to overview]Area Under the Plasma Concentration-Time Curve up to Infinity (AUCinf) Following Single Dose of Quizartinib With or Without Efavirenz
NCT04459598 (9) [back to overview]Terminal Half-Life (t1/2) Following Single Dose of Quizartinib With or Without Efavirenz
NCT04459598 (9) [back to overview]Metabolite to Parent Ratio (MPR) Based on Area Under the Curve for Active Metabolite AC886 Following Single Dose of Quizartinib With or Without Efavirenz
NCT04459598 (9) [back to overview]Number of Participants With Treatment-emergent Adverse Events Following Single Dose of Quizartinib With or Without Efavirenz
NCT04459598 (9) [back to overview]Maximum Plasma Concentration (Cmax) Following Single Dose of Quizartinib With or Without Efavirenz

Proportion of Participants With Suppression of HIV Viral Load to Less Than 50 Copies/ml at Week 16

Proportion was calculated as number of participants with HIV-1 RNA <= 50 copies/ml relative to the number of participants with HIV-1 RNA measured at that time point. (NCT00016718)
Timeframe: At week 16

Interventionproportion of participants (Number)
Age Group 10.50
Age Group 20.76
Age Group 30.75

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Proportion of Participants With Suppression of HIV Viral Load to Less Than 400 Copies/ml at Week 16

Proportion was calculated as number of participants with HIV-1 RNA <= 400 copies/ml relative to the number of participants with HIV-1 RNA measured at that time point. (NCT00016718)
Timeframe: At week 16

Interventionproportion of participants (Number)
Age Group 10.83
Age Group 20.86
Age Group 30.81

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Proportion of Participants Who Developed Grade 3 or 4 Adverse Events Attributed to the Study Treatment.

"Adverse events were graded using the Division of AIDS (DAIDS) Table for Grading the Severity of Adult and Pediatric Adverse Events (DAIDS AE Grading Table), Version 1.0, December 2004, Clarification August 2009, which is available on the RCC website at (http://rcc.tech-res.com/). Adverse Events of Grade 3 or 4 laboratory abnormalities or signs and symptoms that were judged by the study team to be possibly or probably related to the study treatment.~Comparisons between age groups were not required as per protocol." (NCT00016718)
Timeframe: At study entry, weeks 2 and 4, every 4 weeks up to week 96 and every 6 weeks thereafter for Group 1 participants and at study entry, weeks 2 and 4, every 4 weeks up to week 144 and every 12 weeks thereafter for Groups 2 and 3

Interventionproportion of participants (Number)
Age Group 10.17
Age Group 20.1
Age Group 30.19

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PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.1.602.05

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.701.010.63
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.8.410.714.6
RAL 400mg b.i.d.2.2501.7703.035
RPV 25mg q.d.0.1450.1340.134

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Interventionng/mL (Median)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.448647

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,
Interventionng/mL (Median)
2nd Trimester3rd TrimesterPostpartum
EVG/COBI 150/150mg q.d.1447.11432.81713.1
TAF 10mg q.d. w/COBI80.491.298.2
TAF 25mg q.d.69.796133
TAF 25mg q.d. w/COBI or RTV Boosting87.8107141

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PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

Interventionng/mL (Geometric Mean)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.108128

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PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.2.842.524.51
DRV/RTV 600/100mg b.i.d.2.122.222.51
FPV/RTV 700/100mg b.i.d.2.121.642.87
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA0.470.52

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PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.360.480.38
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.130.130.28
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.3.75.17.2
RAL 400mg b.i.d.0.06210.0640.0797

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PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs

"Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose.~For the TAF 25 mg q.d., 10 mg q.d. w/COBI, and 25 mg q.d. w/COBI or RTV boosting arms, samples were all below the limit of quantification and statistical analyses were not conducted." (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.0.210.210.61
ATV/RTV Arm 1: 300/100mg q.d.2.00.71.2
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.490.710.90
DRV/COBI 800/150 mg q.d.0.330.271.43
DRV/RTV 800/100mg q.d.0.991.172.78
DTG 50mg q.d.0.730.931.28
EFV 600 mg q.d. (Outside THA)1.491.481.94
EVG/COBI 150/150mg q.d.0.02580.04870.3771
TAF 10mg q.d. w/COBI0.001950.001950.00195
TAF 25mg q.d.0.001950.001950.00195
TAF 25mg q.d. w/COBI or RTV Boosting0.001950.001950.00195
TFV 300mg q.d.0.0390.0540.061
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.0.30.50.8
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.440.571.26

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Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs

Infant plasma concentrations were collected and measured during the first 9 days of life. Half-life is defined as 0.693/k, where k, the elimination rate constant, is the slope of the decline in concentrations. (NCT00042289)
Timeframe: Infant plasma samples at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

Interventionhour (Median)
DTG 50mg q.d.32.8
EVG/COBI 150/150mg q.d.7.6
DRV/COBI 800/150 mg q.d.NA
EFV 600 mg q.d. (Outside THA)65.6

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PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.0.0630.0560.081

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Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs

Infant plasma concentrations were collected and measured during the first 9 days of life. (NCT00042289)
Timeframe: Blood samples were collected at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

,,,
Interventionmcg/mL (Median)
2-10 hours after birth18-28 hours after birth36-72 hours after birth5-9 days after birth
DRV/COBI 800/150 mg q.d.0.351.431.871.72
DTG 50mg q.d.1.731.531.000.06
EFV 600 mg q.d. (Outside THA)1.11.00.90.4
EVG/COBI 150/150mg q.d.0.1320.0320.0050.005

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs

Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

Interventionng*hour/mL (Geometric Mean)
2nd Trimester3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.NA27173645

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.55.151.879.6
DRV/RTV 600/100mg b.i.d.45.845.961.7
FPV/RTV 700/100mg b.i.d.43.5032.1551.60
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA34.233.5

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.4.58.35.3
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)14.916.127.1
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.7296133
RAL 400mg b.i.d.6.65.411.6

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24 (area under the curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

,,,,,,,,,,,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.25.3318.8536.20
ATV/RTV Arm 1: 300/100mg q.d.88.241.957.9
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.30.645.748.8
DRV/COBI 800/150 mg q.d.50.0042.0595.55
DRV/RTV 800/100mg q.d.64.663.5103.9
DTG 50mg q.d.47.649.265.0
EFV 600 mg q.d. (Outside THA)47.3060.0262.70
EVG/COBI 150/150mg q.d.15.314.021.0
TAF 10mg q.d. w/COBI0.1970.2060.216
TAF 25mg q.d.0.1710.2120.271
TAF 25mg q.d. w/COBI or RTV Boosting0.1810.2570.283
TFV 300mg q.d.1.92.43.0
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.14.528.839.6
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.26.237.758.7

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PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.0.15
DTG 50mg q.d.1.25
EVG/COBI 150/150mg q.d.0.91
DRV/COBI 800/150 mg q.d.0.07
ATV/COBI 300/150 mg q.d.0.07
TFV 300mg q.d.0.88

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PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. For arms with zero overall participants analyzed, samples were below the limit of quantification and ratios could not be calculated. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
TAF 10mg q.d. w/COBI0.97
EFV 600 mg q.d. (Outside THA)0.67
EFV 600mg q.d.0.49
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.0.2
RAL 400mg b.i.d.1.5
ETR 200mg b.i.d.0.52
MVC 150 or 300mg b.i.d.0.33
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.14
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.16
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.0.19
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.12
RPV 25mg q.d.0.55
ATV/RTV 300/100mg q.d. or TFV/ATV/RTV 300/300/100mg q.d.0.18
DRV/RTV 800/100mg q.d. or DRV/RTV 600/100mg b.i.d.0.18

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Plasma Concentration for Contraceptives

Serum concentrations of the contraceptives. Note that no historical controls were provided by team pharmacologists and thus no comparisons were done for contraceptive concentrations in women using hormonal contraceptives and selected ARV drugs as compared to historical controls not using those ARV drugs. (NCT00042289)
Timeframe: Measured at 6-7 weeks after contraceptive initiation postpartum

Interventionpg/mL (Median)
ATV/RTV/TFV 300/100/300mg q.d. With ENG604
LPV/RTV 400/100 b.i.d. With ENG428
EFV 600mg q.d. With ENG125

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Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12h (area-under-the-curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8 and 12 hours post dosing.

Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
LPV/RTV 400/100 b.i.d. With ENG115.97100.20

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Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,,,,,,,,,,,,,,,,,,,,,,
InterventionParticipants (Count of Participants)
2nd Trimester3rd TrimesterPostpartum
ATV/RTV Arm 1: 300/100mg q.d.11212
DRV/COBI 800/150 mg q.d.3414
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.71622
DRV/RTV 600/100mg b.i.d.71922
DRV/RTV 800/100mg q.d.91922
DTG 50mg q.d.92023
EFV 600 mg q.d. (Outside THA)123334
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.82927
ETR 200mg b.i.d.5137
EVG/COBI 150/150mg q.d.81018
FPV/RTV 700/100mg b.i.d.82622
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)101926
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.93027
ATV/COBI 300/150 mg q.d.125
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA1514
RAL 400mg b.i.d.113330
RPV 25mg q.d.142625
TAF 10mg q.d. w/COBI152322
TAF 25mg q.d.132324
TAF 25mg q.d. w/COBI or RTV Boosting102418
TFV 300mg q.d.22727
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.11112
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.72332

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Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8, 12, and 24 hours post dosing.

,
Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
ATV/RTV/TFV 300/100/300mg q.d. With ENG53.9655.25
EFV 600mg q.d. With ENG53.6456.65

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Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,
InterventionParticipants (Count of Participants)
3rd TrimesterPostpartum
EFV 600mg q.d.2021
MVC 150 or 300mg b.i.d.87

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

Interventionmg*hour/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.55.458.3

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.1.9691.6692.387

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.5.445.10

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.2.822.203.90
ATV/RTV Arm 1: 300/100mg q.d.NA3.64.1
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.3.114.514.52
DRV/COBI 800/150 mg q.d.4.593.677.04
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.6.226.558.96
DRV/RTV 600/100mg b.i.d.5.645.537.78
DRV/RTV 800/100mg q.d.6.775.788.11
DTG 50mg q.d.3.623.544.85
EFV 600 mg q.d. (Outside THA)3.875.134.41
FPV/RTV 700/100mg b.i.d.5.615.126.75
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)3.893.625.37
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA5.15.0
TFV 300mg q.d.0.2500.2450.298
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.1.22.54.1
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.2.733.565.43

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Linked Partner HIV Infection Rates in Early-ART and Delayed-ART Arms

incident HIV infections occurring in the partners (HIV-negative at enrollment) of randomized HIV-infected index (HIV-positive at enrollment) cases are assessed, by arm. Only acquisition from the index partner were included in the primary analysis, therefore, each endpoint was required to be confirmed (by genotyping) such that the viral envelop sequence in the index case matched that of the partner. (NCT00074581)
Timeframe: Throughout study

Interventionevent rate per 100 person-yr (Number)
Early-ART0.07
Delayed-ART1.03

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All Partner HIV Infection Rates in Early-ART and Delayed-ART Arms

All Incident HIV infections occurring in the partners (HIV-negative at enrollment) of randomized HIV-infected index (HIV-positive at enrollment) cases are assessed, by arm. (NCT00074581)
Timeframe: Throughout study

Interventionevent rate per 100 person-yr (Number)
Early-ART0.44
Delayed-ART1.41

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Time to Loss of Virologic Response by Week 48 (Defined by FDA TLOVR Algorithm - Excluding Study Allowed ARV Substitutions)(PI Comparison)

Time from randomization to any of the following events occurring prior to week 48: discontinued ARV regimen (see time to discontinuation of initial ARV therapy above); discontinued study follow-up or died; absence of virologic suppression defined as 2 consecutive plasma HIV-1 RNA values < 400 copies/mL; two consecutive plasma HIV-1 RNA values > 400 copies/mL following virologic suppression. (NCT00084136)
Timeframe: Week 48 (using follow-up only until closing of ddI+FTV+ATV arm on May 22,2008)

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
ddI+FTC+ATV0048
ZDV/3TC+EFV016NA

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Time to Treatment Failure (NRTI Comparison)

Time from randomization to the earliest of: scheduled week of first plasma sample meeting virologic failure (two consecutive plasma HIV-1 RNA values 1,000 copies/mL or higher, regardless of whether ARV medications being taken at the time); scheduled week of first AIDS defining diagnosis (WHO Stage 4 (2005) plus microsporidiosis, cyclospora gastroenteritis and Chaga's disease), not attributed to Immune Reconstitution Inflammatory Syndrome (reviewed by chairs); date of death (due to any cause). Plasma drawn every 8 weeks (except confirmation samples could be drawn earlier). (NCT00084136)
Timeframe: Virologic failure starting 14 weeks following randomization; disease progression starting 12 weeks following randomization; and death occurring at any time following randomization. Follow-up through study closure (May 31, 2010).

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
TDF/FTC+EFV1640NA
ZDV/3TC+EFV1640NA

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Time to Treatment Failure (PI Comparison)

Time from randomization to the earliest of: scheduled week of first plasma sample meeting virologic failure (two consecutive plasma HIV-1 RNA values 1,000 copies/mL or higher, regardless of whether ARV medications being taken at the time); scheduled week of first AIDS defining diagnosis (WHO Stage 4 (2005), plus microsporidiosis, cyclospora gastroenteritis and Chaga's disease), not attributed to Immune Reconstitution Inflammatory Syndrome (reviewed by chairs); date of death (due to any cause). Plasma drawn every 8 weeks (except confirmation samples could be drawn earlier). (NCT00084136)
Timeframe: Virologic failure starting 14 weeks following randomization; disease progression starting 12 weeks following randomization; and death occurring at any time following randomization. Follow-up until ddI+FTC+ATV arm closed (May 22, 2008).

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
ddI+FTC+ATV1624120
ZDV/3TC+EFV1640NA

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Change in CD4 Count From Screening to Weeks 24, 48, 96 (NRTI Comparison)

Available pre-randomization CD4 cell counts were limited to the single CD4 cell count used for study eligibility (and therefore must have been fewer than 300 cells/mm3). (NCT00084136)
Timeframe: weeks 24, 48 and 96 (including all follow-up through to study closure on May 31, 2010)

,
Interventioncells/mm^3 (Median)
Change from screening to week 24 (N=490; N=498)Change from screening to week 48 (N=480; N=485)Change from screening to week 96 (N=458; N=471)
TDF/FTC+EFV120.5159226
ZDV/3TC+EFV112.5151.5220.5

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Change in CD4 Count From Screening to Weeks 24, 48, 96 (PI Comparison)

Available pre-randomization CD4 cell counts were limited to the single CD4 cell count used for study eligibility (and therefore must have been fewer than 300 cells/mm3). (NCT00084136)
Timeframe: weeks 24, 48 and 96 (including follow-up until ddI+FTC+ARV arm closed - May 22, 2008)

,
Interventioncells/mm^3 (Median)
Change from screening to week 24 (N=490; N=502)Change from screening to week 48 (N=474; N=477)Change from screening to week 96 (N= 188; N=188)
ddI+FTC+ATV146.5187.0256.0
ZDV/3TC+EFV112.5152.0216.0

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Plasma HIV-1 Viral Load Fewer Than 400 Copies/ml (NRTI Comparison)

Number of participants with plasma HIV-1 Viral load fewer than 400 copies/mL at study visit weeks 24 and 48. Closest observed result between 20 and up to 28 weeks (for week 24), and between 44 and up to 52 (for week 48) used if multiple results available. Missing values excluded, and both study treatment status and history ignored. (NCT00084136)
Timeframe: At Weeks 24 and 48 (including follow-up through to study closure on May 31, 2010)

,
Interventionparticipants (Number)
Week 24: Number with RNA <400 c/mL (N=495; N=500)Week 48: Number with RNA <400 c/mL (N=482; N=487)
TDF/FTC+EFV448455
ZDV/3TC+EFV459442

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Plasma HIV-1 Viral Load Fewer Than 400 Copies/ml (PI Comparison)

Number of participants with plasma HIV-1 Viral load fewer than 400 copies/mL at study visit weeks 24 and 48. Closest observed result between 20 and up to 28 weeks (for week 24), and between 44 and up to 52 (for week 48) used if multiple results available. Missing values excluded, and both study treatment status and history ignored. (NCT00084136)
Timeframe: At Weeks 24 and 48 (including only follow-up until ddI+FTC+ARV arm closed - May 22, 2008)

,
Interventionparticipants (Number)
Week 24: Number with RNA <400 c/mL (N=495; N=506)Week 48: Number with RNA <400 c/mL (N=476; N=478)
ddI+FTC+ATV431424
ZDV/3TC+EFV459437

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Time to Discontinuation of Initial Antiretroviral (ARV) Therapy (NRTI Comparison)

Time is measured from date of treatment initiation to earliest of the following: date of last participant contact (premature discontinuation of study follow-up); date all ARV medications were held (if all medications held for at least 8 weeks, for any reason); date that any ARV medication was changed (excluding the following single ARV substitutions: stavudine or tenofovir for zidovudine, nevirapine for efavirenz, or didanosine for tenofovir). (NCT00084136)
Timeframe: Throughout follow-up until study closed (May 31,2010)

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
TDF/FTC+EFV1836201
ZDV/3TC+EFV1634163

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Time to Discontinuation of Initial Antiretroviral (ARV) Therapy (PI Comparison)

Time is measured from date of treatment initiation to earliest of the following: date of last participant contact (premature discontinuation of study follow-up); date all ARV medications were held (if all medications held for at least 8 weeks, for any reason); date that any ARV medication was changed (excluding the following single ARV substitutions: stavudine or tenofovir for zidovudine, nevirapine for efavirenz, or didanosine for tenofovir). (NCT00084136)
Timeframe: Throughout follow-up until ddI+FTC+ATV arm closed (May 22,2008)

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
ddI+FTC+ATV71876
ZDV/3TC+EFV1634NA

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Time to First Dose Modification or Grade 3 or 4 Adverse Event (NRTI Comparison)

Time from treatment dispensation to the first occurring of the following: week of first ARV medication change; week of first grade 3 or higher sign/symptom or laboratory abnormality (total bilirubin was excluded) that was at least one grade higher than baseline. Grading used the Division of AIDS (DAIDS) 2004 Severity of Adverse Events Tables. (NCT00084136)
Timeframe: Throughout study follow-up until study closure (May 31, 2010)

,
Interventionweeks (Number)
10th percentile25th percentile50th percentile
TDF/FTC+EFV432224
ZDV/3TC+EFV412112

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Time to First Dose Modification or Grade 3 or 4 Adverse Event (PI Comparison)

Time from treatment dispensation to the first occurring of the following: week of first ARV medication change; week of first grade 3 or higher sign/symptom or laboratory abnormality (total bilirubin was excluded) that was at least one grade higher than baseline. Grading used the Division of AIDS (DAIDS) 2004 Severity of Adverse Events Tables. (NCT00084136)
Timeframe: Throughout study follow-up until ddI+FTC+ATV arm closed (May 22, 2008)

,
Interventionweeks (Number)
10th percentile25th percentile50th percentile
ddI+FTC+ATV432144
ZDV/3TC+EFV41296

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Time to Immunologic Failure (PI Comparison)

Time from randomization to the first scheduled study visit (week 48 or later) with a CD4+ cell count fewer than 100 cells/mm3. (NCT00084136)
Timeframe: At or after Week 48 (including only follow-up until ddI+FTV+ATV arm closed - May 22,2008)

,
Interventionweeks (Number)
1st percentile5th percentile
ddI+FTC+ATV48NA
ZDV/3TC+EFV48112

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Time to Loss of Virologic Response at Week 48 (Defined by FDA TLOVR Algorithm - Excluding Study Allowed ARV Substitutions)(NRTI Comparison)

Time from randomization to any of the following events occurring prior to week 48: discontinued ARV regimen (see time to discontinuation of initial ARV therapy above); discontinued study follow-up or died; absence of virologic suppression defined as 2 consecutive plasma HIV-1 RNA values < 400 copies/mL; two consecutive plasma HIV-1 RNA values > 400 copies/mL following virologic suppression. (NCT00084136)
Timeframe: Week 48 (using follow-up through study closure on May 31,2010)

,
Interventionweeks (Number)
5th percentile10th percentile
TDF/FTC+EFV024
ZDV/3TC+EFV016

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Time to Loss of Virologic Response at Week 48 (Defined by FDA TLOVR Algorithm - Including All ARV Substitutions)(NRTI Comparison)

Time from randomization to any of the following events occurring prior to week 48: changed any ARV medication (including permanent discontinuation of all medications); discontinued study follow-up or died; absence of virologic suppression defined as 2 consecutive plasma HIV-1 RNA values < 400 copies/mL; two consecutive plasma HIV-1 RNA values > 400 copies/mL following virologic suppression. (NCT00084136)
Timeframe: Week 48 using follow-up through study closure on May 31,2010

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
TDF/FTC+EFV00NA
ZDV/3TC+EFV0032

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Time to Loss of Virologic Response at Week 48 (Defined by FDA TLOVR Algorithm - Including All ARV Substitutions)(PI Comparison)

Time from randomization to any of the following events occurring prior to week 48: changed any ARV medication (including permanent discontinuation of all medications); discontinued study follow-up or died; absence of virologic suppression defined as 2 consecutive plasma HIV-1 RNA values < 400 copies/mL; two consecutive plasma HIV-1 RNA values > 400 copies/mL following virologic suppression. (NCT00084136)
Timeframe: Week 48 (using follow-up only until closing of ddI+FTV+ATV arm on May 22,2008)

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
ddI+FTC+ATV0048
ZDV/3TC+EFV0032

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Time to Immunologic Failure (NRTI Comparison)

Time from randomization to the first scheduled study visit (week 48 or later) with a CD4+ cell count fewer than 100 cells/mm3. (NCT00084136)
Timeframe: At or after Week 48 (including all follow-up through study closure - May 31,2010)

,
Interventionweeks (Number)
1st percentile5th percentile10th percentile
TDF/FTC+EFV48104NA
ZDV/3TC+EFV48128NA

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Time to Loss of Virologic Response at Week 96 (Defined by FDA TLOVR Algorithm - Excluding Study Allowed ARV Substitutions)(NRTI Comparison)

Time from randomization to any of the following events occurring prior to week 96: discontinued ARV regimen (see time to discontinuation of initial ARV therapy above); discontinued study follow-up or died; absence of virologic suppression defined as 2 consecutive plasma HIV-1 RNA values < 400 copies/mL; two consecutive plasma HIV-1 RNA values > 400 copies/mL following virologic suppression. (NCT00084136)
Timeframe: Week 96 (using follow-up through to study closure on May 31,2010)

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
TDF/FTC+EFV024NA
ZDV/3TC+EFV016NA

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Time to Loss of Virologic Response at Week 96 (Defined by FDA TLOVR Algorithm - Including All ARV Substitutions)(NRTI Comparison)

Time to any of the following events occurring prior to week 96: changed any ARV medication (including permanent discontinuation of all medications); discontinued study follow-up or died; absence of virologic suppression defined as 2 consecutive plasma HIV-1 RNA values < 400 copies/mL; two consecutive plasma HIV-1 RNA values > 400 copies/mL following virologic suppression. (NCT00084136)
Timeframe: Week 96 using follow-up through study closure on May 31,2010

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
TDF/FTC+EFV00NA
ZDV/3TC+EFV0032

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Time-Averaged Difference (TAD) in log10-transformed HIV-1 RNA Levels

TAD from baseline was calculated as area under the curve (AUC) of HIV-1 RNA load (log10 copies/mL) divided by time period minus baseline HIV-1 RNA load (log10 copies/mL). Baseline value calculated as average of pre-dose measurements collected at screening, randomization, and immediately pre-dose. Data not analyzed for participants originally randomized to maraviroc once daily arm since after termination, focus was shifted from efficacy and safety to only safety as reflected in the abbreviated set of efficacy measures noted in the amended planned analysis. (NCT00098293)
Timeframe: Baseline up to Week 48 and Week 96

,
Interventionlog10 copies/mL (Least Squares Mean)
Week 48Week 96
Efavirenz Once Daily + CBV (DB)-2.262-2.034
Maraviroc Twice Daily + CBV (DB)-2.152-1.945

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Percentage of Participants With HIV-1 RNA Levels of Less Than 400 Copies/mL and Less Than 50 Copies/mL at Week 96 for Enhanced Sensitivity Trofile Assay (ESTA) R5 Participants

Percentage of participants with HIV-1 RNA levels of less than 400 copies/mL and less than 50 copies/mL were not analyzed for maraviroc once daily, then twice daily arm in order to avoid misinterpretation due to possible bias due to the fact that only a non-random sample of participants in the terminated arm were re-assayed with ESTA. (NCT00098293)
Timeframe: Week 96

,
InterventionPercentage of participants (Number)
Less than 400 copies/mLLess than 50 copies/mL
Efavirenz Once Daily + CBV (DB)64.462.7
Maraviroc Twice Daily + CBV (DB)64.058.8

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Percentage of Participants With HIV-1 RNA Levels of Less Than 400 Copies/mL and Less Than 50 Copies/mL at Week 96 Analyzed Using Logistic Regression

(NCT00098293)
Timeframe: Week 96

,,
InterventionPercentage of participants (Number)
Less than 400 copies/mLLess than 50 copies/mL
Efavirenz Once Daily + CBV (DB)64.562.6
Maraviroc Once Daily + CBV (DB), Then Twice Daily + CBV (OL)52.948.3
Maraviroc Twice Daily + CBV (DB)61.456.9

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Percentage of Participants With HIV-1 RNA Levels of Less Than 400 Copies/mL and Less Than 50 Copies/mL at Week 48 for Enhanced Sensitivity Trofile Assay (ESTA) R5 Participants

Percentage of participants with HIV-1 RNA levels of less than 400 copies/mL and less than 50 copies/mL were not analyzed for maraviroc once daily, then twice daily arm in order to avoid misinterpretation due to possible bias due to the fact that only a non-random sample of participants in the terminated arm were re-assayed with ESTA. (NCT00098293)
Timeframe: Week 48

,
InterventionPercentage of participants (Number)
Less than 400 copies/mLLess than 50 copies/mL
Efavirenz Once Daily + CBV (DB)72.368.3
Maraviroc Twice Daily + CBV (DB)73.368.5

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Percentage of Participants With HIV-1 RNA Levels of Less Than 400 Copies/mL and Less Than 50 Copies/mL at Week 48 Analyzed Using Logistic Regression

(NCT00098293)
Timeframe: Week 48

,,
InterventionPercentage of participants (Number)
Less than 400 copies/mLLess than 50 copies/mL
Efavirenz Once Daily + CBV (DB)73.169.3
Maraviroc Once Daily + CBV (DB), Then Twice Daily + CBV (OL)61.555.8
Maraviroc Twice Daily + CBV (DB)70.665.3

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Number of Participants With Phenotypic Resistance at Time of Treatment Failure Through Week 48 and 96

Phenotypic resistance to nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs) assessed at screening by Monogram Bioscience PhenoSense genotype (MBPSGT) assay, repeated if viral load >500 copies/mL at treatment failure through week 48, 96. Phenotypic resistance to maraviroc was assumed in maraviroc treatment failures with X4-using virus and in R5 maraviroc treatment failures using Monogram Bioscience PhenoSense Entry Assay. Phenotypic resistance to zidovudine, lamivudine, efavirenz and maraviroc at time of failure was summarized. (NCT00098293)
Timeframe: Screening, time of failure through Week 48, Week 96

,,
Interventionparticipants (Number)
Resistance to Zidovudine: Week 48 (n= 20, 43, 15)Resistance to Lamivudine: Week 48 (n= 20, 43, 15)Resistance to Efavirenz: Week 48 (n= 20, 43, 15)Resistance to Maraviroc: Week 48 (n= 20, 43, 15)Resistance to Zidovudine: Week 96 (n= 27, 55, 23)Resistance to Lamivudine: Week 96 (n= 27, 55, 23)Resistance to Efavirenz: Week 96 (n= 27, 55, 23)Resistance to Maraviroc: Week 96 (n= 27, 55, 23)
Efavirenz Once Daily + CBV (DB)037NA0813NA
Maraviroc Once Daily + CBV (DB), Then Twice Daily + CBV (OL)0140NA0200NA
Maraviroc Twice Daily + CBV (DB)0270120330NA

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Number of Participants With NRTI Associated Mutations at Time of Treatment Failure Through Week 48 and 96

Genotypic resistance to NRTIs was assessed by identification of relevant mutations at screening using MBPSGT assay and repeated for all participants with HIV-1 viral load more than 500 copies/mL at treatment failure through week 48 and week 96. Following mutations associated with NRTIs were summarized at time of failure: Any zidovudine/lamivudine (Zid/Lam), Any thymidine analogue-associated mutation (TAM), methionine (M) to valine/isoleucine (V/I) substitution at residue (r) 184 (M184V/I), lysine (K) to arginine (R) substitution at residue 65 (K65R) and any other NRTI mutations. (NCT00098293)
Timeframe: Screening, time of failure through Week 48, Week 96

,,
Interventionparticipants (Number)
Any Zid/Lam Mutation: Week 48 (n= 20, 43, 15)Any TAM Mutation: Week 48 (n= 20, 43, 15)K65R Mutation: Week 48 (n= 20, 43, 15)M184V/I Mutation: Week 48 (n= 20, 43, 15)Other NRTI Mutation: Week 48 (n= 20, 43, 15)Any Zid/Lam Mutation: Week 96 (n= 27, 55, 23)Any TAM Mutation: Week 96 (n= 27, 55, 23)K65R Mutation: Week 96 (n= 27, 55, 23)M184V/I Mutation: Week 96 (n= 27, 55, 23)Other NRTI Mutation: Week 96 (n= 27, 55, 23)
Efavirenz Once Daily + CBV (DB)3003082080
Maraviroc Once Daily + CBV (DB), Then Twice Daily + CBV (OL)14101402030200
Maraviroc Twice Daily + CBV (DB)27612713361331

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Time to Virologic Failure

Time to virologic failure based on observed HIV-1 RNA levels and failure events (death;permanent discontinuation of drug;lost to follow-up [LTFU];new anti-retroviral drug added [except background drug change to drug of same class];or on open label for early non-response or rebound). Failure:at Time 0 if level not <400 copies/mL(2 consecutive visits) before events or last available visit;at time of earliest event if level <400 copies/mL(2 consecutive visits);failure if level >=400 copies/mL(2 consecutive visits) or 1 visit >=400 copies/mL followed by permanent discontinuation of drug or LTFU. (NCT00098293)
Timeframe: Week 48, Week 96

,
Interventiondays (Median)
Week 48Week 96
Efavirenz Once Daily + CBV (DB)NANA
Maraviroc Twice Daily + CBV (DB)NANA

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Percentage of Participants With Viral Load of Less Than 400 Copies/Milliliter [Copies/mL] and Less Than 50 Copies/mL of Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) at Week 48 for Full Analysis Set (FAS) Population

(NCT00098293)
Timeframe: Week 48

,,
InterventionPercentage of participants (Number)
Less than 400 copies/mLLess than 50 copies/mL
Efavirenz Once Daily + CBV (DB)73.169.3
Maraviroc Once Daily + CBV (DB), Then Twice Daily + CBV (OL)61.555.8
Maraviroc Twice Daily + CBV (DB)70.665.3

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Number of Participants Per Tropism Status at Baseline and at the Time of Treatment Failure Through Week 96

Number of participants per tropism status (R5, X4, DM, or NR/NP) at baseline and time of treatment failure analyzed through week 96 visit. Treatment failure defined as insufficient clinical response. Tropism result was censored for participants with viral load <500 copies/mL at time of treatment failure categorized as BLQ. The assessment for time of treatment failure was defined as last on treatment assessment. (NCT00098293)
Timeframe: Baseline, time of failure through Week 96

,,
Interventionparticipants (Number)
Baseline: R5; Treatment failure: R5Baseline: R5; Treatment failure: X4Baseline: R5; Treatment failure: DMBaseline: R5; Treatment failure: NR/NPBaseline: DM; Treatment failure: R5Baseline: DM; Treatment failure: X4Baseline: DM; Treatment failure: DMBaseline: DM; Treatment failure: NR/NPBaseline: NR/NP; Treatment failure: R5Baseline: NR/NP; Treatment failure: X4Baseline: NR/NP; Treatment failure: DMBaseline: NR/NP; Treatment failure: NR/NP
Efavirenz Once Daily + CBV (DB)1000510000000
Maraviroc Once Daily + CBV (DB), Then Twice Daily + CBV (OL)904600500000
Maraviroc Twice Daily + CBV (DB)14111712401001

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Number of Participants Per Tropism Status at Baseline and at the Time of Treatment Failure Through Week 48

Number of participants per tropism status (C-X-C chemokine receptor 5 {CCR5} [R5], C-X-C chemokine receptor type 4 {CXCR4} [X4], Dual/mixed [DM], or Non-reportable/Non-phenotypable [NR/NP]) at baseline and time of treatment failure analyzed through week 48 visit. Treatment failure: discontinuation due to insufficient clinical response. Tropism result was censored for participants with viral load <500 copies/mL at time of treatment failure categorized as below lower limit of quantification (BLQ). The assessment for time of treatment failure was defined as last on treatment assessment. (NCT00098293)
Timeframe: Baseline, time of failure through Week 48

,,
Interventionparticipants (Number)
Baseline: R5; Treatment failure: R5Baseline: R5; Treatment failure: X4Baseline: R5; Treatment failure: DMBaseline: R5; Treatment failure: NR/NPBaseline: DM; Treatment failure: R5Baseline: DM; Treatment failure: X4Baseline: DM; Treatment failure: DMBaseline: DM; Treatment failure: NR/NP
Efavirenz Once Daily + CBV (DB)60040000
Maraviroc Once Daily + CBV (DB), Then Twice Daily + CBV (OL)50350050
Maraviroc Twice Daily + CBV (DB)1101051240

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Change From Baseline in Lymphocyte Cluster of Differentiation 8 (CD8) Count at Week 48 and 96

Baseline value calculated as the average of pre-dose measurements collected at screening and immediately pre-dose. Change from baseline in lymphocyte CD8 count at Week 48 and 96 was not analyzed for participants originally randomized to maraviroc once daily arm since after termination, focus was shifted from efficacy and safety to only safety as reflected in the abbreviated set of efficacy measures noted in the amended planned analysis. (NCT00098293)
Timeframe: Baseline, Week 48, Week 96

,
Interventioncells/µL (Mean)
BaselineChange at Week 48Change at Week 96
Efavirenz Once Daily + CBV (DB)935.78-126.83-150.27
Maraviroc Twice Daily + CBV (DB)938.8038.3420.74

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Change From Baseline in Lymphocyte Cluster of Differentiation 4 (CD4) Count at Week 48 and 96

Baseline value calculated as the average of pre-dose measurements collected at screening and immediately pre-dose. (NCT00098293)
Timeframe: Baseline, Week 48, Week 96

,,
Interventioncells per microliter (cells/µL) (Mean)
BaselineChange at Week 48Change at Week 96
Efavirenz Once Daily + CBV (DB)271.87143.52171.50
Maraviroc Once Daily + CBV (DB), Then Twice Daily + CBV (OL)274.1172.50183.75
Maraviroc Twice Daily + CBV (DB)264.70169.53206.31

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Change From Baseline in Log 10-transformed Plasma Viral Load (HIV-1 RNA) Levels at Week 48 and 96

Change from baseline in log 10-transformed plasma viral load (HIV-1 RNA) levels (log10 copies/mL). Baseline value calculated as average of pre-dose measurements collected at screening, randomization, and immediately pre-dose. (NCT00098293)
Timeframe: Baseline, Week 48, Week 96

,,
Interventionlog10 copies/mL (Mean)
BaselineChange at Week 48Change at Week 96
Efavirenz Once Daily + CBV (DB)4.857-2.347-2.053
Maraviroc Once Daily + CBV (DB), Then Twice Daily + CBV (OL)4.899-2.665-2.565
Maraviroc Twice Daily + CBV (DB)4.851-2.240-1.961

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Percentage of Participants With Viral Load of Less Than 400 Copies/mL and Less Than 50 Copies/mL of HIV-1 RNA at Week 96

(NCT00098293)
Timeframe: Week 96

,,
InterventionPercentage of participants (Number)
Less than 400 copies/mLLess than 50 copies/mL
Efavirenz Once Daily + CBV (DB)64.562.6
Maraviroc Once Daily + CBV (DB), Then Twice Daily + CBV (OL)52.948.3
Maraviroc Twice Daily + CBV (DB)61.456.9

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Percentage of Participants With Viral Load of Less Than 400 Copies/mL and Less Than 50 Copies/mL of HIV-1 RNA at Week 48 for Per Protocol (PP) Population

Percentage of participants with viral load of less than 400 copies/mL and less than 50 copies/mL of HIV-1 RNA were not analyzed for participants originally randomized to maraviroc once daily arm since after termination, focus was shifted from efficacy and safety to only safety as reflected in the abbreviated set of efficacy measures noted in the amended planned analysis. (NCT00098293)
Timeframe: Week 48

,
InterventionPercentage of participants (Number)
Less than 400 copies/mLLess than 50 copies/mL
Efavirenz Once Daily + CBV (DB)78.2774.44
Maraviroc Twice Daily + CBV (DB)75.0070.00

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Number of Participants With Efavirenz Associated Mutations at Time of Treatment Failure Through Week 48 and 96

Genotypic resistance: mutations at screening by MBPSGT assay, repeated if viral load >500 copies/mL at treatment failure through week 48, 96. Efavirenz mutation:lysine to aspargine at r103(K103N);tyrosine to cysteine/isoleucine at r181(Y181C/I);tyrosine to cysteine/leucine/histidine at r188(Y188C/L/H);glycine to alanine/serine at r190(G190A/S);valine to alanine to r106(V106A);leucine to isoleucine at r100(L100I);alanine to glycine at r98(A98G);lysine to glutamic acid at r101(K101E);valine to isoleucine at r108(V108I);proline to histidine at r225(P225H);methionine to leucine at r230(M230L). (NCT00098293)
Timeframe: Screening, time of failure through Week 48, Week 96

,
Interventionparticipants (Number)
L100I Mutation: Week 48 (n= 43, 15)K103N Mutation: Week 48 (n= 43, 15)V106M Mutation: Week 48 (n= 43, 15)V108I Mutation: Week 48 (n= 43, 15)Y181C/I Mutation: Week 48 (n= 43, 15)Y188L Mutation: Week 48 (n= 43, 15)G190S/A Mutation: Week 48 (n= 43, 15)P225H Mutation: Week 48 (n= 43, 15)L100I Mutation: Week 96 (n= 55, 23)K103N Mutation: Week 96 (n= 55, 23)V106M Mutation: Week 96 (n= 55, 23)V108I Mutation: Week 96 (n= 55, 23)Y181C/I Mutation: Week 96 (n= 55, 23)Y188L Mutation: Week 96 (n= 55, 23)G190S/A Mutation: Week 96 (n= 55, 23)P225H Mutation: Week 96 (n= 55, 23)
Efavirenz Once Daily + CBV (DB)06000010012110021
Maraviroc Twice Daily + CBV (DB)0001000000010000

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Number of Participants With HIV RNA Levels Below 400 Copies/mL at Week 48

(NCT00100048)
Timeframe: 48 weeks

Interventionparticipants (Number)
MK0518 100 mg b.i.d.38
MK0518 200 mg b.i.d34
MK0518 400 mg b.i.d.40
MK0518 600 mg b.i.d.36
EFV Combo Therapy33

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Number of Participants With HIV RNA Levels Below 50 Copies/mL at Week 24 (Cohort II)

(NCT00100048)
Timeframe: Week 24

Interventionparticipants (Number)
MK0518 100 mg b.i.d.28
MK0518 200 mg b.i.d27
MK0518 400 mg b.i.d.33
MK0518 600 mg b.i.d.32
EFV Combo Therapy31

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Number of Participants With Clinical Adverse Experiences (AEs)and Serious Adverse Experiences (SAEs)

"An AE was defined as any unfavorable & unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to its use. Any worsening of a preexisting condition which was temporally associated with the use of the study drug, was also an AE.~A SAE was any AE that resulted in death, was life threatening, resulted in a persistent or significant disability/incapacity, resulted in or prolonged an existing inpatient hospitalization, was a congenital anomaly/birth defect, was cancer, or was an overdose." (NCT00100048)
Timeframe: Week 240

,
InterventionParticipants (Number)
Adverse experiencesSerious adverse experiences
EVF Combo Therapy354
MK-0518 b.i.d.15425

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Number of Patients That Discontinued With CAEs

(NCT00100048)
Timeframe: 48 Weeks

,,,,
Interventionparticipants (Number)
Discontinued with CAEsDid Not Discontinue with CAEs
EFV Combo Therapy038
MK0518 100 mg b.i.d.039
MK0518 200 mg b.i.d040
MK0518 400 mg b.i.d.041
MK0518 600 mg b.i.d.040

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Number of Patients That Discontinued With LAEs

(NCT00100048)
Timeframe: 48 Weeks

,,,,
Interventionparticipants (Number)
Discontinued With LAEsDid Not Discontinue With LAEs
EFV Combo Therapy038
MK0518 100 mg b.i.d.039
MK0518 200 mg b.i.d040
MK0518 400 mg b.i.d.041
MK0518 600 mg b.i.d.139

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Number of Patients With Clinical Adverse Experiences (CAEs)

An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product. (NCT00100048)
Timeframe: 48 weeks

,,,,
Interventionparticipants (Number)
With CAEsWithout CAEs
EFV Combo Therapy344
MK0518 100 mg b.i.d.318
MK0518 200 mg b.i.d.355
MK0518 400 mg b.i.d.365
MK0518 600 mg b.i.d.355

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Number of Patients With Clinical Adverse Experiences (CAEs) and Number of Patients With Serious CAEs at Day 10 (Cohort I)

"An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product.~Serious CAEs are any AEs occurring at any dose that; Results~in death; or Is life threatening; or Results in a persistent or significant disability/incapacity; or Results in or~prolongs an existing inpatient hospitalization; or Is a congenital anomaly/birth defect; or Is a cancer; or Is an~overdose." (NCT00100048)
Timeframe: 10 days

,,,,
Interventionparticipants (Number)
With CAEsWithout CAEsWith Serious CAEsWithout Serious CAEs
MK0518 100 mg b.i.d.4307
MK0518 200 mg b.i.d.2507
MK0518 400 mg b.i.d.3306
MK0518 600 mg b.i.d.5308
Placebo5207

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Number of Patients With HIV RNA Level Below 50 Copies/mL and HIV RNA Level Below 400 Copies/mL at Week 96

(NCT00100048)
Timeframe: 96 Weeks

,
Interventionparticipants (Number)
HIV RNA <50 copies/mLHIV RNA <400 copies/mL
EFV Combo Therapy3232
MK0518 b.i.d.133135

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Number of Patients With Laboratory Adverse Experiences (LAEs)

A laboratory adverse experience (LAE) is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product (NCT00100048)
Timeframe: 48 Weeks

,,,,
Interventionparticipants (Number)
With LAEsWithout LAEs
EFV Combo Therapy830
MK0518 100 mg b.i.d.831
MK0518 200 mg b.i.d.733
MK0518 400 mg b.i.d.1130
MK0518 600 mg b.i.d.535

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Number of Patients With Serious CAEs (Cohort I and II Combined)

Serious CAEs are any AEs occurring at any dose that; Results in death; or Is life threatening; or Results in a persistent or significant disability/incapacity; or Results in or prolongs an existing inpatient hospitalization; or Is a congenital anomaly/birth defect; or Is a cancer; or Is an overdose (NCT00100048)
Timeframe: 48 weeks

,,,,
Interventionparticipants (Number)
With Serious CAEsWithout Serious CAEs
EFV Combo Therapy236
MK0518 100 mg b.i.d.237
MK0518 200 mg b.i.d.535
MK0518 400 mg b.i.d.041
MK0518 600 mg b.i.d.238

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Number of Patients With Serious CAEs and Non-serious CAEs at Week 144

"An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product~An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product" (NCT00100048)
Timeframe: 144 Weeks

,
Interventionparticipants (Number)
With CAEsWithout CAEsWith serious CAEsWithout serious CAEs
EFV Combo Therapy353434
MK0518 b.i.d.153718142

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Number of Patients With Serious LAEs

Serious LAEs are any LAEs occurring at any dose that; Results in death; or Is life threatening; or Results in a persistent or significant disability/incapacity; or Results in or prolongs an existing inpatient hospitalization; or Is a congenital anomaly/birth defect; or Is a cancer; or Is an overdose (NCT00100048)
Timeframe: 48 Weeks

,,,,
Interventionparticipants (Number)
With serious LAEsWithout serious LAEs
EFV Combo Therapy038
MK0518 100 mg b.i.d.039
MK0518 200 mg b.i.d.040
MK0518 400 mg b.i.d.041
MK0518 600 mg b.i.d.040

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Change From Baseline in CD4 (T-helper) Cell Count at Week 240

Change in number of CD4 cells/mm^3 from baseline to Week 240. (NCT00100048)
Timeframe: Baseline and Week 240

Interventioncells/mm^3 (Mean)
MK-0518 b.i.d.301.7
EVF Combo Therapy275.6

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Change From Baseline in CD4 Cell Count at Week 96

(NCT00100048)
Timeframe: Baseline and Week 96

Interventioncells/mm3 (Mean)
MK0518 b.i.d.221.2
EFV Combo Therapy232.4

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Change From Baseline in Cluster of Differentiation 4 (CD4) Cell Count at Week 24 (Cohort II)

Mean change from baseline at Week 24 in CD4 Cell Count (cells/mm3) (NCT00100048)
Timeframe: Baseline and Week 24

Interventioncells/mm3 (Mean)
MK0518 100 mg b.i.d.184
MK0518 200 mg b.i.d122
MK0518 400 mg b.i.d.147
MK0518 600 mg b.i.d.134
EFV Combo Therapy101

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Change From Baseline in Plasma HIV RNA at Week 24 (Cohort II)

Mean change from baseline at Week 24 in plasma HIV RNA (copies/mL) (NCT00100048)
Timeframe: Baseline and Week 24

Interventioncopies/mL (Mean)
MK0518 100 mg b.i.d.-2.39
MK0518 200 mg b.i.d-2.20
MK0518 400 mg b.i.d.-2.33
MK0518 600 mg b.i.d.-2.49
EFV Combo Therapy-2.44

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Change From Baseline in Plasma HIV RNA at Week 240

HIV RNA levels were determined by AMPLICOR HIV-1 Monitor™ Standard Assay. (NCT00100048)
Timeframe: Baseline and Week 240

InterventionLog10Copies/mL (Mean)
MK-0518 b.i.d.-2.29
EVF Combo Therapy-2.07

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Change From Baseline in Plasma HIV RNA at Week 96

(NCT00100048)
Timeframe: Baseline and Week 96

Interventioncopies/mL (Mean)
MK0518 b.i.d.-2.30
EFV Combo Therapy-2.28

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Change From Baseline in Plasma Human Immunodeficiency Virus (HIV) Ribonucleic Acid (RNA) on Day 10 (Cohort I)

Mean change from baseline on Day 10 in plasma Human Immunodeficiency Virus (HIV) Ribonucleic acid (RNA) (copies/mL) (NCT00100048)
Timeframe: Baseline and Day 10

Interventioncopies/mL (Mean)
MK0518 100 mg b.i.d.-1.93
MK0518 200 mg b.i.d-1.98
MK0518 400 mg b.i.d.-1.66
MK0518 600 mg b.i.d.-2.16
Placebo-0.17

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Number of Participants With HIV RNA (Human Immunodeficiency Virus Ribonucleic Acid) Levels Below 50 Copies/mL at Week 240

HIV RNA levels were determined by AMPLICOR HIV-1 Monitor™ UltraSensitive Assay. (NCT00100048)
Timeframe: Week 240

InterventionParticipants (Number)
MK-0518 b.i.d.110
EFV Combo Therapy24

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Number of Participants With HIV RNA Levels Below 400 Copies/mL at Week 24 (Cohort II)

(NCT00100048)
Timeframe: Week 24

Interventionparticipants (Number)
MK0518 100 mg b.i.d.31
MK0518 200 mg b.i.d27
MK0518 400 mg b.i.d.35
MK0518 600 mg b.i.d.32
EFV Combo Therapy32

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Number of Participants With HIV RNA Levels Below 400 Copies/mL at Week 240

HIV RNA levels were determined by AMPLICOR HIV-1 Monitor™ Standard Assay. (NCT00100048)
Timeframe: Week 240

InterventionParticipants (Number)
MK-0518 b.i.d.115
EVF Combo Therapy25

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Number of Children Experiencing Severe CDC Stage B or Stage C Disease or Death (Cumulative After 3.5 Years)

The outcome measure is defined as a number because it represents the number of children that experienced severe CDC Stage B or Stage C disease or death as defined in the outcome measure title above (NCT00102960)
Timeframe: Occurrence of severe CDC Stage B or Stage C disease or death (cumulative after 3.5 years), whichever came first, was assessed from randomization up to at least 3.5 years.

InterventionParticipants (Count of Participants)
Deferred Therapy41
Early Therapy 40 Weeks28
Early Therapy 96 Weeks21

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Hospitalization Rates

Hospitalisation rates in the three arms enrolled in the CHER study (NCT00102960)
Timeframe: 4.8 years

InterventionEvents per 100 person years (Number)
Deferred Therapy27.6
Early Therapy 40 Weeks16.4
Early Therapy 96 Weeks14.2

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Time to Failure of First Line Therapy or Death

To compare time to failure of first line ART (due to clinical, virological or immunological disease progression, or regimen-limiting ART toxicities) or death among three randomized arms (infants who receive early ART in Arms 2 and 3 and infants in whom ART is deferred until clinical or immunological disease progression in Arm 1) during the study (up to 4.8 years). The number of participants experiencing the events did not reach the 50% survival and thus median time-to-event is not be presented. Therefore we report the number of participants experiencing the events per Arm. (NCT00102960)
Timeframe: From date of randomization up to failure of first-line therapy or death from any cause, whichever came first, assessed up to 4.8 years

InterventionParticipants (Count of Participants)
Deferred Therapy48
Early Therapy up to 40 Weeks32
Early Therapy up to 96 Weeks26

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Number of Participants Who Experienced Regimen-limiting ART Drug Toxicity

Development of toxicity requiring more than one drug substitution within the same class or a switch to a new class of drugs (regimen-limiting toxicity failure) or requiring a permanent treatment discontinuation. This was part of the primary outcome measure that was a composite endpoint. (NCT00102960)
Timeframe: Regimen limiting drug toxicity was monitored from randomization up to the entire study duration of 4.8 years.

InterventionParticipants (Count of Participants)
Deferred Therapy0
Early Therapy 40 Weeks0
Early Therapy 96 Weeks0

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Total Occurrence of Grade 3 or 4 Laboratory Events

(NCT00102960)
Timeframe: From randomization up to 4.8 years

InterventionCount of events (Number)
Deferred Therapy35
Early Therapy 40 Weeks44
Early Therapy 96 Weeks33

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Total Occurrence of Grade 3 or 4 Clinical Events

This was a secondary outcome measure that assessed the total count of Grade 3 or 4 (clinical or laboratory) adverse events. (NCT00102960)
Timeframe: 4.8 years

InterventionCount of events (Number)
Deferred Therapy170
Early Therapy 40 Weeks118
Early Therapy 96 Weeks88

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Time From Randomization to Starting or Needing to Start Continuous Therapy

Time from randomization to starting (deferred therapy Arm) or needing to start continuous therapy (early therapy 40 or 96 weeks) (NCT00102960)
Timeframe: 4.8 years

InterventionWeeks (Median)
Deferred Therapy20
Early Therapy 40 Weeks33
Early Therapy 96 Weeks70

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Number of Participants Who Experienced Virological Failure Defined as Confirmed HIV-1 RNA Value of at Least 10,000 Copies Per/ml Recorded on Two Consecutive Separate Occasions After 24 Weeks of Treatment (Initial Therapy or Restart)

This was part of the primary outcome measure that was a composite endpoint that included confirmed HIV-1 RNA value of at least 10,000 copies per/ml recorded on two consecutive separate occasions after 24 weeks of treatment (initial therapy or restart). (NCT00102960)
Timeframe: Virological failure was assessed from randomization through the entire study duration of 4.8 years.

InterventionParticipants (Count of Participants)
Deferred Therapy10
Early Therapy 40 Weeks1
Early Therapy 96 Weeks1

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Number of Participants Who Experienced Immunological Failure Defined as Failure of CD4% to Reach 20% or CD4% Falls Below 20% on Two Occasions, Within 4 Weeks, at Any Time After the First 24 Weeks of Therapy (Initial Therapy or Restart)

This was part of the primary outcome measure above. The primary outcome was a composite endpoint. The primary outcome analysis only considered the initially enrolled children that were 377 in total (ART-Deferred n=125, Early therapy 40 weeks n=126 and Early therapy 96 weeks n=126). This was part of the primary outcome measure that was a composite endpoint. (NCT00102960)
Timeframe: This outcome was assessed from the date of randomization to immunological failure. Immunological failure was assessed in the entire study duration of 4.8 years.

InterventionParticipants (Count of Participants)
Deferred Therapy9
Early ART for 40 Weeks14
Early Therapy for 96 Weeks11

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Number of Participants Who Experienced Clinical Failure (Defined as Development of Severe CDC Stage B or Stage C Disease.) on Therapy.

This included development of severe CDC Stage B or Stage C disease.This was part of the primary outcome measure that was a composite endpoint (NCT00102960)
Timeframe: Clinical failure on therapy was assessed at each visit for the entire study duration of 4.8 years.

InterventionParticipants (Count of Participants)
Deferred Therapy8
Early Therapy 40 Weeks6
Early Therapy 96 Weeks5

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Time to First Hospitalization

To compare time to first hospitalization in the three randomized arms (infants who received early ART in Arms 2 and 3 and those who received deferred ART in Arm 1). Not all participants were hospitalized and thus the upper limits could not be evaluated. (NCT00102960)
Timeframe: From randomization up to 4.8 years

InterventionWeeks (Median)
Deferred Therapy73.1
Early Therapy 40 WeeksNA
Early Therapy 96 WeeksNA

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Time to Death Alone or Death Plus Life Threatening Stage C Events or HIV Events Associated With Permanent End-organ Damage.

This was a composite endpoint in which the number of children experiencing the events is reported. The number of participants experiencing the events did not reach the 50% survival and thus median time-to-event is not be presented. Therefore, we report the number of participants experiencing the events per Arm. (NCT00102960)
Timeframe: 4.8 years

InterventionParticipants (Count of Participants)
Deferred Therapy34
Early Therapy 40 Weeks18
Early Therapy 96 Weeks13

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Duration of Hospitalisation

This is the total number of days spent in hospital by the participants and is reported per arm (NCT00102960)
Timeframe: 4.8 years, the study duration

InterventionDays (Number)
Deferred Therapy1018
Early Therapy 40 Weeks533
Early Therapy 96 Weeks414

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Change From Baseline in CD4+ Cell Count (Relative) at Week 96

Change from baseline in CD4+ cell count was imputed in case of missing values: in case of premature discontinuation, data were imputed with the baseline value after discontinuation (i.e. change=0, Non-Completer [NC] = Failure); otherwise last observation carried forward was applied. (NCT00110305)
Timeframe: Baseline (Day 1 of Week 0) to Week 96

InterventionPercentage of CD4+ Cells (Mean)
TMC278 25mg8.6
TMC278 75 mg9.9
TMC278 150 mg9.3
All TMC2789.3
Efavirenz9.6

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Number of Participants With Virologic Response (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm, by Area Under the Plasma Concentration Time Curve From Time 0 to 24 Hours (AUC24h) Quartiles

Quartile 1, 2, 3 and 4 of AUC24h means the quartile with the lowest 25%, 26-50%, 51-75% and the highest 25% of AUC24h values, respectively, irrespective of the different doses of TMC278. For each participant, a single value for area under the plasma concentration-time curve from time of administration up to 24 hours post dosing (AUC24h) of TMC278 was estimated from a population pharmacokinetic model, based on all samples collected throughout the trial up to Week 96. Virologic response was calculated by time to loss of virologic response (TLOVR) algorithm. (NCT00110305)
Timeframe: Up to Week 96

InterventionParticipants (Number)
AUC24h Quartile 148
AUC24h Quartile 250
AUC24h Quartile 355
AUC24h Quartile 451

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Number of Participants With Virologic Response at Week 240 (Viral Load Less Than 400 Copies/mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm

The TLOVR algorithm was used to derive response, ie, response and loss of response needed to be confirmed at 2 consecutive visits and participants who permanently discontinued were considered nonresponders. Participants with intermittent missing viral load values were considered responders if the preceeding and succeeding visits indicated response. In all other cases, intermittent values were imputed with nonresponse. Resuppression after confirmed virologic failure was considered as failure in this algorithm. (NCT00110305)
Timeframe: Week 240

InterventionParticipants (Number)
All TMC278166
Efavirenz54

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Number of Participants With Virologic Response at Week 240 (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm

The TLOVR algorithm was used to derive response, ie, response and loss of response needed to be confirmed at 2 consecutive visits and participants who permanently discontinued were considered nonresponders. Participants with intermittent missing viral load values were considered responders if the preceeding and succeeding visits indicated response. In all other cases, intermittent values were imputed with nonresponse. Resuppression after confirmed virologic failure was considered as failure in this algorithm. (NCT00110305)
Timeframe: Week 240

InterventionParticipants (Number)
All TMC278152
Efavirenz51

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Number of Participants With Virologic Response at Week 240 (Viral Load Less Than 50 Copies Per mL) - Snapshot Analysis

The analysis is based on the last observed viral load data within the Week 240 window. Virologic response is defined as a viral load less than 50 copies/mL. Missing viral load was considered as non-response. (NCT00110305)
Timeframe: Week 240

InterventionParticipants (Number)
All TMC278150
Efavirenz51

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Number of Participants With Virologic Response at Week 96 (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm

The TLOVR algorithm was used to derive response, ie, response and loss of response needed to be confirmed at 2 consecutive visits and participants who permanently discontinued were considered nonresponders. Participants with intermittent missing viral load values were considered responders if the preceeding and succeeding visits indicated response. In all other cases, intermittent values were imputed with nonresponse. Resuppression after confirmed virologic failure was considered as failure in this algorithm. (NCT00110305)
Timeframe: Week 96

InterventionParticipants (Number)
TMC278 25 mg71
TMC278 75 mg68
TMC278 150 mg65
All TMC278204
Efavirenz63

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Trough Plasma Concentration (Ctrough) for TMC278

For each participant, a single value for trough (i.e. predose) plasma concentration (Ctrough) of TMC278 was estimated from a population pharmacokinetic model, based on samples collected throughout the trial up to Week 96. (NCT00110305)
Timeframe: Up to Week 96

Interventionng/mL (Mean)
TMC278 25 mg92.7
TMC278 75 mg196.0
TMC278 150 mg342.0

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Number of Participants With Virologic Failure for the Resistance Determinations by Developing Mutations: First Available On-Treatment Genotypic Data After Failure

Virologic failure for the resistance determinations was defined as a viral load greater than 0.5 log10 copies /mL above the nadir with a minimum of 500 copies/mL. For this study, treatment-emergent mutations (for at least one treatment) are presented as Resistance associated mutation (RAMs): i) Non-nucleotide reverse transcriptase inhibitor (NNRTI) RAMs, ii) Nucleoside/tide reverse transcriptase inhibitor (N[t]RTI RAMs). (NCT00110305)
Timeframe: Week 240

,
InterventionParticipants (Number)
Treatment-emergent NNRTI RAME138KK101EK103NTreatment-emergent N(t)RTI RAMM184V
All TMC278177611310
Efavirenz400300

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Number of Participants With Virologic Response at Week 48 (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm

The TLOVR algorithm was used to derive response, ie, response and loss of response needed to be confirmed at 2 consecutive visits and participants who permanently discontinued were considered nonresponders. Participants with intermittent missing viral load values were considered responders if the preceeding and succeeding visits indicated response. In all other cases, intermittent values were imputed with nonresponse. Resuppression after confirmed virologic failure was considered as failure in this algorithm. (NCT00110305)
Timeframe: Week 48

InterventionParticipants (Number)
TMC278 25 mg74
TMC278 75 mg76
TMC278 150 mg70
All TMC278220
Efavirenz72

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Number of Participants With Virologic Response at Week 96 (Viral Load Less Than 50 Copies Per mL) - Snapshot Analysis

The analysis is based on the last observed viral load data within the Week 96 window. Virologic response is defined as a viral load less than 50 copies/mL. Missing viral load was considered as non-response. (NCT00110305)
Timeframe: Week 96

InterventionParticipants (Number)
TMC278 25 mg71
TMC278 75 mg70
TMC278 150 mg66
All TMC278207
Efavirenz64

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Area Under the Plasma Concentration Time Curve From Time 0 to 24 Hours (AUC24h) for TMC278

For each participant, a single value for area under the plasma concentration-time curve from time of administration up to 24 hours post dosing (AUC24h) of TMC278 was estimated from a population pharmacokinetic model, based on all samples collected throughout the trial up to Week 96. (NCT00110305)
Timeframe: Up to Week 96

Interventionng*h/mL (Mean)
TMC278 25 mg2767
TMC278 75 mg5906
TMC278 150 mg10281

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Change From Baseline in CD4+ Cell Count (Absolute) at Week 240

Change from baseline in CD4+ cell count was imputed in case of missing values: in case of premature discontinuation, data were imputed with the baseline value after discontinuation (i.e. change=0, Non-Completer [NC] = Failure); otherwise last observation carried forward was applied. (NCT00110305)
Timeframe: Baseline (Day 1 of Week 0) to Week 240

InterventionCells per microliter (Mean)
All TMC278221.0
Efavirenz217.9

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Change From Baseline in CD4+ Cell Count (Absolute) at Week 96

Change from baseline in CD4+ cell count was imputed in case of missing values: in case of premature discontinuation, data were imputed with the baseline value after discontinuation (i.e. change=0, Non-Completer [NC] = Failure); otherwise last observation carried forward was applied. (NCT00110305)
Timeframe: Baseline (Day 1 of Week 0) to Week 96

InterventionCells per microliter (Mean)
TMC278 25mg145.9
TMC278 75 mg172.0
TMC278 150 mg158.9
All TMC278159.0
Efavirenz159.8

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Change From Baseline in CD4+ Cell Count (Relative) at Week 240

Change from baseline in CD4+ cell count was imputed in case of missing values: in case of premature discontinuation, data were imputed with the baseline value after discontinuation (i.e. change=0, Non-Completer [NC] = Failure); otherwise last observation carried forward was applied. (NCT00110305)
Timeframe: Baseline (Day 1 of week 0) to Week 240

InterventionPercentage of CD4+ cells (Mean)
All TMC2788.7
Efavirenz9.7

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Percentage of Participants With Pure Virologic Failure (HIV-1 RNA < 50 c/mL) at Week 96

Participants who achieved confirmed HIV-1 RNA < 50 c/mL but had not experienced a confirmed relapse were considered censored at the last HIV-1 RNA collection date. (NCT00112047)
Timeframe: Week 96

InterventionPercentage of Participants (Number)
EFV+FTC+TDF20
CBV+EFV23

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Percentage of Participants With Pure Virological Failure (HIV-1 RNA < 400 c/mL) at Week 144

Participants who achieved confirmed HIV-1 RNA < 400 c/mL but had not experienced a confirmed relapse were considered censored at the last HIV-1 RNA collection date. (NCT00112047)
Timeframe: Week 144

InterventionPercentage of participants (Number)
EFV+FTC+TDF11
CBV+EFV17

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Percentage of Participants With Pure Virological Failure (HIV-1 RNA < 400 c/mL) Through Week 240 (Atripla Week 96)

Participants who achieved confirmed HIV-1 RNA < 400 c/mL but had not experienced a confirmed relapse were considered censored at the last HIV-1 RNA collection date. (NCT00112047)
Timeframe: Week 240 (Atripla Week 96)

InterventionPercentage of Participants (Number)
EFV+FTC+TDF/Atripla (From Study Baseline)11
All Atripla (From Atripla Baseline)2

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Percentage of Participants With Pure Virological Failure (HIV-1 RNA < 50 c/mL) at Week 144

Participants who achieved confirmed HIV-1 RNA < 50 c/mL but had not experienced a confirmed relapse were considered censored at the last HIV-1 RNA collection date. (NCT00112047)
Timeframe: Week 144

InterventionPercentage of Participants (Number)
EFV+FTC+TDF21
CBV+EFV25

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Percentage of Participants With Pure Virological Failure (HIV-1 RNA < 50 c/mL) Through Week 240 (Atripla Week 96)

Participants who achieved confirmed HIV-1 RNA < 50 c/mL but had not experienced a confirmed relapse were considered censored at the last HIV-1 RNA collection date. (NCT00112047)
Timeframe: Week 240 (Atripla Week 96)

InterventionPercentage of Participants (Number)
EFV+FTC+TDF/Atripla (From Study Baseline)22
All Atripla (From Atripla Baseline)4

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Quality of Life (SF-12v2 Health Survey: Mental Component Summary) Change From Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

The change from Week 144 (Atripla baseline) to Week 240 (Atripla Week 96) in the SF-12v2 Health Survey MCS. The SF-12v2 includes 8 concepts commonly represented in health surveys: physical functioning, role functioning physical, bodily pain, general health, vitality, social functioning, role functioning emotional, and mental health. Results are expressed in terms of 2 composite scores: the PCS and the MCS. PCS and MCS values can range from 0 to 100 and are designed to have a mean value of 50 and a SD of 10 (in the general population). (NCT00112047)
Timeframe: Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

InterventionComposite Score (Mean)
All Atripla0.9

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Quality of Life (SF-12v2 Health Survey: Physical Component Summary) Change From Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

The change from Week 144 (Atripla baseline) to Week 240 (Atripla Week 96) in the SF-12v2 Health Survey: Physical Component Summary (PCS). The SF-12v2 includes 8 concepts commonly represented in health surveys: physical functioning, role functioning physical, bodily pain, general health, vitality, social functioning, role functioning emotional, and mental health. Results are expressed in terms of 2 composite scores: the PCS and the Mental Component Summary (MCS). PCS and MCS values can range from 0 to 100 and are designed to have a mean value of 50 and SD of 10 (in the general population). (NCT00112047)
Timeframe: Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

InterventionComposite Score (Mean)
All Atripla0.0

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Treatment Satisfaction Questionnaire (General Satisfaction With Current Treatment Regimen): Change From Week 144 to Week 240 in the Category Shift From Atripla Baseline.

"Participants were asked: In general, how satisfied are you with your current treatment regimen? Possible responses were on a 4-category scale: very satisfied; somewhat satisfied; somewhat dissatisfied; and very dissatisfied. For the evaluation of changes in treatment satisfaction from Week 144 (Atripla baseline) to Week 240 (Atripla Week 96) responses were dichotomized into very satisfied and not very satisfied (not very satisfied included very dissatisfied; somewhat dissatisfied; and somewhat satisfied)." (NCT00112047)
Timeframe: Week 144 ([W 144]; Atripla baseline) to Week 240 ([W 240]; Atripla Week 96)

InterventionParticipants (Number)
Very satisfied (W 144 and W 240)Not very satisfied (W 144 and W 240)Very satisfied (W 144); not very satisfied (W 240)Not very satisfied (W 144); very satisfied (W 240)
All Atripla18010923

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Treatment Satisfaction Questionnaire (Satisfaction With Convenience and Simplicity of Current Treatment Regimen): Change From Week 144 to Week 240 in the Category Shift From Atripla Baseline.

"Participants were asked: In general, how satisfied are you with the convenience and simplicity of your current treatment regimen? Possible responses were on a 4-category scale: very satisfied; somewhat satisfied; somewhat dissatisfied; and very dissatisfied. For the evaluation of changes in treatment satisfaction from Week 144 (Atripla baseline) to Week 240 (Atripla Week 96) responses were dichotomized into very satisfied and not very satisfied (not very satisfied included very dissatisfied; somewhat dissatisfied; and somewhat satisfied)." (NCT00112047)
Timeframe: Week 144 ([W 144]; Atripla baseline) to Week 240 ([W 240]; Atripla Week 96)

InterventionParticipants (Number)
Very satisfied (W 144 and W 240)Not very satisfied (W 144 and W 240)Very satisfied (W 144); not very satisfied (W 240)Not very satisfied (W 144); very satisfied (W 240)
All Atripla1826829

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Treatment Satisfaction Questionnaire (Satisfaction With Current Treatment Regimen to Control HIV): Change From Week 144 to Week 240 in the Category Shift From Atripla Baseline.

"Participants were asked: In general, how satisfied are you with the ability of your current treatment regimen to control your HIV infection? Possible responses were on a 4-category scale: very satisfied; somewhat satisfied; somewhat dissatisfied; and very dissatisfied. For the evaluation of changes in treatment satisfaction from Week 144 (Atripla baseline) to Week 240 (Atripla Week 96) responses were dichotomized into very satisfied and not very satisfied (not very satisfied included very dissatisfied; somewhat dissatisfied; and somewhat satisfied)." (NCT00112047)
Timeframe: Week 144 ([W 144]; Atripla baseline) to Week 240 ([W 240]; Atripla Week 96)

InterventionParticipants (Number)
Very satisfied (W 144 and W 240)Not very satisfied (W 144 and W 240)Very satisfied (W 144); not very satisfied (W 240)Not very satisfied (W 144); very satisfied (W 240)
All Atripla1928917

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Treatment Satisfaction Questionnaire (Satisfaction With Tolerability of Current Treatment Regimen) Change From Week 144 to Week 240 in the Category Shift From Atripla Baseline.

"Participants were asked: In general, how satisfied are you with your ability to tolerate your current treatment regimen? Possible responses were on a 4-category scale: very satisfied; somewhat satisfied; somewhat dissatisfied; and very dissatisfied. For the evaluation of changes in treatment satisfaction from Week 144 (Atripla baseline) to Week 240 (Atripla Week 96) responses were dichotomized into very satisfied and not very satisfied (not very satisfied included very dissatisfied; somewhat dissatisfied; and somewhat satisfied)." (NCT00112047)
Timeframe: Week 144 ([W 144]; Atripla baseline) to Week 240 ([W 240]; Atripla Week 96)

InterventionParticipants (Number)
Very satisfied (W 144 and W 240)Not very satisfied (W 144 and W 240)Very satisfied (W 144); not very satisfied (W 240)Not very satisfied (W 144); very satisfied (W 240)
All Atripla166211326

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Treatment Satisfaction Questionnaire (Bothered With the Side Effects of Current Treatment Regimen): Change From Week 144 to Week 240 in the Category Shift From Atripla Baseline.

"Participants were asked: How bothered are you with the side effects of your current treatment regimen? Possible responses were on a 4-category scale: does not bother me; bothers me a little bit; bothers me a lot; and bothers me terribly. For the evaluation of the change in treatment satisfaction from Week 144 (Atripla baseline) to Week 240 (Atripla Week 96) responses were dichotomized into does not bother me and bothers me (bothers me included bothers me a little bit; bothers me a lot; bothers me terribly)." (NCT00112047)
Timeframe: Week 144 ([W 144]; Atripla baseline) to Week 240 ([W 240]; Atripla Week 96)

InterventionParticipants (Number)
Bothers me (W 144 and W 240)Does not bother me (W 144 and W 240)Bothers me (W 144); does not bother me (W 240)Does not bother me (W 144); bothers me (W 240)
All Atripla411263128

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Percentage of Participants With Plasma HIV-1 RNA < 50 c/mL at Week 144

The percentage of participants with plasma HIV-1 RNA < 50 c/mL at Week 144. Participants with missing observations/changes in ART were considered to have HIV-1 RNA ≥ 50 c/mL (i.e., ITT missing or switch=failure analysis). (NCT00112047)
Timeframe: Week 144

InterventionPercentage of Participants (Number)
EFV+FTC+TDF60.8
CBV+EFV50.4

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Percentage of Participants With Pure Virologic Failure (HIV-1 RNA < 400 c/mL) at Week 48

Participants who achieved confirmed HIV-1 RNA < 400 c/mL but had not experienced a confirmed relapse were considered censored at the last HIV-1 RNA collection date. (NCT00112047)
Timeframe: Baseline to 48 Weeks

InterventionPercentage of Participants (Number)
EFV+FTC+TDF9
CBV+EFV16

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Percentage of Participants With Pure Virologic Failure (HIV-1 RNA < 400 c/mL) at Week 96

Participants who achieved confirmed HIV-1 RNA < 400 c/mL but had not experienced a confirmed relapse were considered censored at the last HIV-1 RNA collection date. (NCT00112047)
Timeframe: Week 96

InterventionPercentage of Participants (Number)
EFV+FTC+TDF9
CBV+EFV17

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Change From Baseline in CD4 Cell Count (Cells/mm^3) at Week 240 (Atripla Week 96)

Change from baseline to Week 240 (Atripla Week 96) in CD4 cell count = Week 240 (Atripla Week 96) CD4 cell count value minus baseline CD4 cell count value (NCT00112047)
Timeframe: Study/Atripla baseline to Week 240 (Atripla Week 96)

InterventionCD4 Cell count (Cells/mm^3) (Mean)
EFV+FTC+TDF/Atripla (From Study Baseline)346
All Atripla (From Atripla Baseline)42

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Change From Study Baseline in CD4 Cell Count (Cells/mm^3) at Week 144

Change from study baseline to Week 144 in CD4 cell count = Week 144 CD4 cell count value minus study baseline CD4 cell count value (NCT00112047)
Timeframe: Baseline to Week 144

InterventionCD4 Cell Count (cells/mm^3) (Mean)
EFV+FTC+TDF312
CBV+EFV271

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Change From Study Baseline in CD4 Cell Count (Cells/mm^3) at Week 48

Change from study baseline to Week 48 in CD4 cell count = Week 48 CD4 cell count value minus study baseline CD4 cell count value (NCT00112047)
Timeframe: Study baseline to Week 48

InterventionCD4 Cell Count (cells/mm^3) (Mean)
EFV+FTC+TDF190
CBV+EFV158

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Change From Study Baseline in CD4 Cell Count (Cells/mm^3) at Week 96

Change from study baseline to Week 96 in CD4 cell count = Week 96 CD4 cell count value minus study baseline CD4 cell count value (NCT00112047)
Timeframe: Baseline to Week 96

InterventionCD4 Cell Count (cells/mm^3) (Mean)
EFV+FTC+TDF270
CBV+EFV237

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Change From Study Baseline in HIV-1 RNA (Log10 c/mL) at Week 144

Change from study baseline to Week 144 in HIV-1 RNA in log10 scale (Week 144 HIV-1 RNA value in log10 scale minus study baseline HIV-1 RNA value in log10 scale). (NCT00112047)
Timeframe: Study baseline to Week 144

InterventionLog10 c/mL (Mean)
EFV+FTC+TDF-3.32
CBV+EFV-3.30

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Change From Study Baseline in HIV-1 RNA (Log10 c/mL) at Week 48

Change from study baseline to Week 48 in HIV-1 RNA in log10 scale (Week 48 HIV-1 RNA value in log10 scale minus study baseline HIV-1 RNA value in log10 scale). (NCT00112047)
Timeframe: Study baseline to Week 48

InterventionLog10 c/mL (Mean)
EFV+FTC+TDF-3.31
CBV+EFV-3.26

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Change From Study Baseline in HIV-1 RNA (Log10 c/mL) at Week 96

Change from study baseline to Week 96 in HIV-1 RNA in log10 scale (Week 96 HIV-1 RNA value in log10 scale minus study baseline HIV-1 RNA value in log10 scale). (NCT00112047)
Timeframe: Study baseline to Week 96

InterventionLog10 c/mL (Mean)
EFV+FTC+TDF-3.30
CBV+EFV-3.25

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Change in Limb Fat (kg) From Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

Change from Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96) in limb fat = Week 240 (Atripla Week 96) limb fat value minus Week 144 (Atripla Baseline) limb fat value (NCT00112047)
Timeframe: Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

Interventionlimb fat (kg) (Mean)
All Atripla0.12

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Change in Limb Fat (kg) From Week 48 to Week 144

Change from Week 48 to Week 144 in limb fat = Week 144 limb fat value minus Week 48 limb fat value (NCT00112047)
Timeframe: Week 48 to Week 144

Interventionlimb fat (kg) (Mean)
EFV+FTC+TDF1.13
CBV+EFV-1.09

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Change in Limb Fat (kg) From Week 48 to Week 96

Change from Week 48 to Week 96 in limb fat = Week 96 limb fat value minus Week 48 limb fat value. (NCT00112047)
Timeframe: Week 48 to Week 96

Interventionlimb fat (kg) (Mean)
EFV+FTC+TDF0.74
CBV+EFV-0.77

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Change in Total Body Fat (kg) From Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

Change from Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96) in total body fat = Week 240 (Atripla Week 96) total body fat value minus Week 144 (Atripla Baseline) total body fat value (NCT00112047)
Timeframe: Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

Interventiontotal body fat (kg) (Mean)
All Atripla0.37

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Change in Total Body Fat (kg) From Week 48 to Week 144

Change from Week 48 to Week 144 in total body fat = Week 144 total body fat value minus Week 48 total body fat value (NCT00112047)
Timeframe: Week 48 to Week 144

Interventiontotal body fat (kg) (Mean)
EFV+FTC+TDF2.47
CBV+EFV-1.18

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Change in Total Body Fat (kg) From Week 48 to Week 96

Change from Week 48 to Week 96 in total body fat = Week 96 total body fat value minus Week 48 total body fat value (NCT00112047)
Timeframe: 48 weeks to 96 weeks

Interventiontotal body fat (kg) (Mean)
EFV+FTC+TDF1.69
CBV+EFV-0.82

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Change in Trunk Fat (kg) From Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

Change from Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96) in trunk fat = Week 240 (Atripla Week 96) trunk fat value minus Week 144 (Atripla Baseline) trunk fat value (NCT00112047)
Timeframe: Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

Interventiontrunk fat (kg) (Mean)
All Atripla0.27

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Change in Trunk Fat (kg) From Week 48 to Week 144

Change from Week 48 to Week 144 in trunk fat = Week 144 trunk fat value minus Week 48 trunk fat value (NCT00112047)
Timeframe: Week 48 to Week 144

Interventiontrunk fat (kg) (Mean)
EFV+FTC+TDF1.30
CBV+EFV-0.10

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Change in Trunk Fat (kg) From Week 48 to Week 96

Change from Week 48 to Week 96 in trunk fat = Week 96 trunk fat value minus Week 48 trunk fat value (NCT00112047)
Timeframe: Week 48 to Week 96

Interventiontrunk fat (kg) (Mean)
EFV+FTC+TDF0.94
CBV+EFV-0.04

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Percentage of Participants With Confirmed Plasma HIV-1 RNA < 400 c/mL at Week 144 (Defined by FDA TLOVR Algorithm)

Participants who achieved/maintained confirmed HIV-1 RNA < 400 c/mL had to satisfy the following: 1) not experienced death, permanent study drug discontinuation, or addition of new antiretroviral drug, except nevirapine in place of EFV, prior to Week 144 visit; 2) achieved confirmed HIV-1 RNA < 400 c/mL on 2 consecutive visits prior to Week 144 visit (i.e., the first of the 2 consecutive HIV-1 RNA < 400 c/mL occurred prior to the Week 144 visit; 3) not had confirmed HIV-1 RNA > 400 c/mL after achievement of confirmed HIV-1 RNA levels < 400 c/mL prior to Week 144 visit. (NCT00112047)
Timeframe: 144 weeks

InterventionPercentage of Participants (Number)
EFV+FTC+TDF70.9
CBV+EFV58.1

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Percentage of Participants With Confirmed Plasma HIV-1 RNA < 400 c/mL at Week 240 (Atripla Week 96) Defined by the FDA TLOVR Algorithm

Participants who achieved/maintained confirmed HIV-1 RNA < 400 c/mL had to satisfy the following criteria: 1) not experienced death, permanent study drug discontinuation, or addition of new antiretroviral drug except nevirapine in place of EFV prior to Week 240 visit; 2) achieved confirmed HIV-1 RNA < 400 c/mL on 2 consecutive visits prior to Week 240 visit (that is, the first of the 2 consecutive HIV-1 RNA < 400 c/mL occurred prior to the Week 240 visit; 3) not had confirmed HIV-1 RNA > 400 c/mL after achievement of confirmed HIV RNA levels < 400 c/mL prior to Week 240 visit. (NCT00112047)
Timeframe: Week 144 (Atripla baseline) to Week 240 (Atripla Week 96)

InterventionPercentage of Participants (Number)
All Atripla87

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Percentage of Participants With Confirmed Plasma HIV-1 RNA < 400 c/mL at Week 48 (Defined by the Food and Drug Administration [FDA] Time-to-Loss-of Virologic Response [TLOVR] Algorithm

Participants who achieved/maintained confirmed HIV-1 RNA < 400 c/mL had to satisfy the following criteria: 1) not experienced death, permanent study drug discontinuation, or addition of new antiretroviral drug except nevirapine in place of EFV prior to Week 48 visit; 2) achieved confirmed HIV-1 RNA < 400 c/mL on 2 consecutive visits prior to Week 48 visit (ie, the first of the 2 consecutive HIV-1 RNA < 400 c/mL occurred prior to the Week 48 visit; 3) not had confirmed HIV-1 RNA > 400 c/mL after achievement of confirmed HIV RNA levels < 400 c/mL prior to Week 48 visit. (NCT00112047)
Timeframe: 48 weeks

InterventionPercentage of participants (Number)
EFV+FTC+TDF84.4
CBV+EFV72.8

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Percentage of Participants With Confirmed Plasma HIV-1 RNA < 400 c/mL at Week 96 (Defined by FDA TLOVR Algorithm)

Participants who achieved/maintained confirmed HIV-1 RNA < 400 c/mL had to satisfy the following criteria: 1) not experienced death, permanent study drug discontinuation, or addition of new antiretroviral drug except nevirapine in place of EFV prior to Week 96 visit; 2) achieved confirmed HIV-1 RNA < 400 c/mL on 2 consecutive visits prior to Week 96 visit (that is, the first of the 2 consecutive HIV-1 RNA < 400 c/mL occurred prior to the Week 96 visit; 3) not had confirmed HIV-1 RNA > 400 c/mL after achievement of confirmed HIV RNA levels < 400 c/mL prior to Week 96 visit. (NCT00112047)
Timeframe: 96 Weeks

InterventionPercentage of Participants (Number)
EFV+FTC+TDF74.6
CBV+EFV61.9

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Percentage of Participants With Confirmed Plasma HIV-1 RNA < 50 c/mL at Week 144 (Defined by FDA TLOVR Algorithm)

Participants who achieved/maintained confirmed HIV-1 RNA < 50 c/mL (c/mL) had to satisfy the following criteria: 1) not experienced death, permanent study drug discontinuation, or addition of new antiretroviral drug, except nevirapine in place of EFV, prior to Week 144 visit; 2) achieved confirmed HIV-1 RNA < 50 c/mL on 2 consecutive visits prior to Week 144 visit (that is, the first of the 2 consecutive HIV-1 RNA < 50 c/mL occurred prior to the Week 144 visit; 3) not had confirmed HIV-1 RNA > 50 c/mL after achievement of confirmed HIV-1 RNA levels < 50 c/mL prior to Week 144 visit. (NCT00112047)
Timeframe: Week 144

InterventionPercentage of participants (Number)
EFV+FTC+TDF64.3
CBV+EFV56.3

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Percentage of Participants With Confirmed Plasma HIV-1 RNA < 50 c/mL at Week 240 (Atripla Week 96) Defined by the FDA TLOVR Algorithm

Participants who achieved/maintained confirmed HIV-1 RNA < 50 c/mL had to satisfy the following criteria: 1) not experienced death, permanent study drug discontinuation, or addition of new antiretroviral drug except nevirapine in place of EFV prior to Week 240 visit; 2) achieved confirmed HIV-1 RNA < 50 c/mL on 2 consecutive visits prior to Week 240 visit (that is, the first of the 2 consecutive HIV-1 RNA < 50 c/mL occurred prior to the Week 240 visit; 3) not had confirmed HIV-1 RNA > 50 c/mL after achievement of confirmed HIV RNA levels < 50 c/mL prior to Week 240 visit. (NCT00112047)
Timeframe: Week 144 (Atripla baseline) to Week 240 (Atripla Week 96)

InterventionPercentage of Participants (Number)
All Atripla85

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Percentage of Participants With Confirmed Plasma HIV-1 RNA < 50 c/mL at Week 48 (Defined by FDA TLOVR Algorithm)

Participants who achieved/maintained confirmed HIV-1 RNA < 50 c/mL had to satisfy the following criteria: 1) not experienced death, permanent study drug discontinuation, or addition of new antiretroviral drug except nevirapine in place of EFV prior to Week 48 visit; 2) achieved confirmed HIV-1 RNA < 50 c/mL on 2 consecutive visits prior to Week 48 visit (that is, the first of the 2 consecutive HIV-1 RNA < 50 c/mL occurred prior to the Week 48 visit; 3) not had confirmed HIV-1 RNA > 50 c/mL after achievement of confirmed HIV RNA levels < 50 c/mL prior to Week 48 visit. (NCT00112047)
Timeframe: Week 48

InterventionPercentage of Participants (Number)
EFV+FTC+TDF79.5
CBV+EFV70.4

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Percentage of Participants With Confirmed Plasma HIV-1 RNA < 50 c/mL at Week 96 (Defined by FDA TLOVR Algorithm)

Participants who achieved/maintained confirmed HIV-1 RNA < 50 c/mL had to satisfy the following criteria: 1) not experienced death, permanent study drug discontinuation, or addition of new antiretroviral drug except nevirapine in place of EFV prior to Week 96 visit; 2) achieved confirmed HIV-1 RNA < 50 c/mL on 2 consecutive visits prior to Week 96 visit (that is, the first of the 2 consecutive HIV-1 RNA < 50 c/mL occurred prior to the Week 96 visit; 3) not had confirmed HIV-1 RNA > 50 c/mL after achievement of confirmed HIV RNA levels < 50 c/mL prior to Week 96 visit. (NCT00112047)
Timeframe: Week 96

InterventionPercentage of Participants (Number)
EFV+FTC+TDF67.2
CBV+EFV60.9

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Percentage of Participants With HIV-1 RNA < 50 c/mL at Week 48

The percentage of participants with plasma HIV-1 RNA < 50 c/mL at Week 48. Participants with missing observations/changes in ART were considered to have HIV-1 RNA ≥ 50 c/mL (i.e., ITT missing or switch=failure analysis). (NCT00112047)
Timeframe: 48 Weeks

InterventionPercentage of Participants (Number)
EFV+FTC+TDF74.5
CBV+EFV66.9

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Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 400 c/mL) at Week 144

"TLOVR for participants who achieved a confirmed virologic response was the time to the earliest of: premature study regimen discontinuation or the first of 2 consecutive HIV-1 RNA ≥ 400 c/mL or last HIV-1 RNA ≥ 400 c/mL followed by loss to follow-up. If the time to HIV-1 RNA ≥ 400 c/mL was immediately preceded by missing scheduled visits then the time of virologic failure was replaced by the first such missing visit. Participants who had not achieved a confirmed virologic response before regimen discontinuation were considered non-responders on Study Day 1." (NCT00112047)
Timeframe: Week 144

InterventionPercentage of Participants (Number)
EFV+FTC+TDF28
CBV+EFV41

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Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 400 c/mL) at Week 48

"TLOVR for participants who achieved a confirmed virologic response was the time to the earliest of: premature study regimen discontinuation or the first of 2 consecutive HIV-1 RNA ≥ 400 c/mL or last HIV-1 RNA ≥ 400 c/mL followed by loss to follow-up. If the time to HIV-1 RNA ≥ 400 c/mL was immediately preceded by missing scheduled visits then the time of virologic failure was replaced by the first such missing visit. Participants who had not achieved a confirmed virologic response before regimen discontinuation were considered non-responders on Study Day 1." (NCT00112047)
Timeframe: Baseline to 48 weeks

InterventionPercentage of Participants (Number)
EFV+FTC+TDF19
CBV+EFV30

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Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 400 c/mL) at Week 96

TLOVR for participants with confirmed virologic response (2 consecutive HIV-1 RNA < 400 c/mL) prior to study drug discontinuation, was the time to the earliest of premature study regimen discontinuation, or confirmed HIV-1 RNA > 400 c/mL (2 consecutive HIV-1 RNA ≥ 400 c/mL, or the last HIV-1 RNA ≥ 400 c/mL followed by premature study regimen discontinuation due to loss to follow-up). Participants who did not achieve confirmed virologic response before premature study regimen discontinuation or last HIV-1 RNA, were assumed to have lost virologic response on Study Day 1. (NCT00112047)
Timeframe: Week 96

InterventionPercentage of Participants (Number)
EFV+FTC+TDF25
CBV+EFV37

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Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 400 c/mL) From Week 144 (Atripla Baseline) Through Week 240 (Atripla Week 96)

"TLOVR for participants who achieved a confirmed virologic response was the time to the earliest of: premature study regimen discontinuation or the first of 2 consecutive HIV-1 RNA ≥ 400 c/mL or last HIV-1 RNA ≥ 400 c/mL followed by loss to follow-up. If the time to HIV-1 RNA ≥ 400 c/mL was immediately preceded by missing scheduled visits then the time of virologic failure was replaced by the first such missing visit. Participants who had not achieved a confirmed virologic response before regimen discontinuation were considered non-responders on Study Day 1." (NCT00112047)
Timeframe: Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

InterventionPercentage of Participants (Number)
All Atripla13

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Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 50 c/mL) at Week 144

"TLOVR for participants who achieved a confirmed virologic response was the time to the earliest of: premature study regimen discontinuation or the first of 2 consecutive HIV-1 RNA ≥ 50 c/mL or last HIV-1 RNA ≥ 50 c/mL followed by loss to follow-up. If the time to HIV-1 RNA ≥ 50 c/mL was immediately preceded by missing scheduled visits then the time of virologic failure was replaced by the first such missing visit. Participants who had not achieved a confirmed virologic response before regimen discontinuation were considered non-responders on Study Day 1." (NCT00112047)
Timeframe: Week 144

InterventionPercentage of Participants (Number)
EFV+FTC+TDF34
CBV+EFV43

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Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 50 c/mL) at Week 48

"TLOVR for participants who achieved a confirmed virologic response was the time to the earliest of: premature study regimen discontinuation or the first of 2 consecutive HIV-1 RNA ≥ 50 c/mL or last HIV-1 RNA ≥ 50 c/mL followed by loss to follow-up. If the time to HIV-1 RNA ≥ 50 c/mL was immediately preceded by missing scheduled visits then the time of virologic failure was replaced by the first such missing visit. Participants who had not achieved a confirmed virologic response before regimen discontinuation were considered non-responders on Study Day 1." (NCT00112047)
Timeframe: Baseline to 48 Weeks

InterventionPercentage of Participants (Number)
EFV+FTC+TDF23
CBV+EFV32

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Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 50 c/mL) at Week 96

"TLOVR for participants who achieved a confirmed virologic response was the time to the earliest of: premature study regimen discontinuation or the first of 2 consecutive HIV-1 RNA ≥ 50 c/mL or last HIV-1 RNA ≥ 50 c/mL followed by loss to follow-up. If the time to HIV-1 RNA ≥ 50 c/mL was immediately preceded by missing scheduled visits then the time of virologic failure was replaced by the first such missing visit. Participants who had not achieved a confirmed virologic response before regimen discontinuation were considered non-responders on Study Day 1." (NCT00112047)
Timeframe: Week 96

InterventionPercentage of Participants (Number)
EFV+FTC+TDF32
CBV+EFV38

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Percentage of Participants With Loss of Virologic Response (HIV-1 RNA < 50 c/mL) From Week 144 (Atripla Baseline) Through Week 240 (Atripla Week 96)

"TLOVR for participants who achieved a confirmed virologic response was the time to the earliest of: premature study regimen discontinuation or the first of 2 consecutive HIV-1 RNA ≥ 50 c/mL or last HIV-1 RNA ≥ 50 c/mL followed by loss to follow-up. If the time to HIV-1 RNA ≥ 50 c/mL was immediately preceded by missing scheduled visits then the time of virologic failure was replaced by the first such missing visit. Participants who had not achieved a confirmed virologic response before regimen discontinuation were considered non-responders on Study Day 1." (NCT00112047)
Timeframe: Week 144 (Atripla Baseline) to Week 240 (Atripla Week 96)

InterventionPercentage of Participants (Number)
All Atripla15

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Percentage of Participants With Plasma HIV-1 RNA < 400 c/mL at Week 144

The percentage of participants with plasma HIV-1 RNA < 400 c/mL at Week 144. Participants with missing observations/changes in ART were considered to have HIV-1 RNA ≥ 400 c/mL (i.e., ITT missing or switch=failure analysis). (NCT00112047)
Timeframe: Week 144

InterventionPercentage of Participants (Number)
EFV+FTC+TDF63.1
CBV+EFV51.6

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Percentage of Participants With Plasma HIV-1 RNA < 400 c/mL at Week 240 (Atripla Week 96)

The percentage of participants with plasma HIV-1 RNA < 400 c/mL at Week 240. Participants with missing observations/changes in ART were considered to have HIV-1 RNA ≥ 400 c/mL (i.e., ITT missing or switch=failure analysis). (NCT00112047)
Timeframe: Week 240 (Atripla Week 96)

InterventionPercentage of Participants (Number)
EFV+FTC+TDF/Atripla (From Study Baseline)87
All Atripla (From Atripla Baseline)85

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Percentage of Participants With Plasma HIV-1 RNA < 400 c/mL at Week 48.

The percentage of participants with plasma HIV-1 RNA < 400 c/mL at Week 48. Participants with missing observations/changes in ART were considered to have HIV-1 RNA ≥ 400 c/mL (i.e., ITT missing or switch=failure analysis). (NCT00112047)
Timeframe: 48 weeks

InterventionPercentage of Participants (Number)
EFV+FTC+TDF80.4
CBV+EFV69.3

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Percentage of Participants With Pure Virologic Failure (HIV-1 RNA < 50 c/mL) at Week 48

Participants who achieved confirmed HIV-1 RNA < 50 c/mL but had not experienced a confirmed relapse were considered censored at the last HIV-1 RNA collection date. (NCT00112047)
Timeframe: Baseline to 48 Weeks

InterventionPercentage of participants (Number)
EFV+FTC+TDF16
CBV+EFV24

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Percentage of Participants With Plasma HIV-1 RNA < 50 c/mL at Week 240 (Atripla Week 96)

The percentage of participants with plasma HIV-1 RNA < 50 c/mL at Week 240. Participants with missing observations/changes in ART were considered to have HIV-1 RNA ≥ 50 c/mL (i.e., ITT missing or switch=failure analysis). (NCT00112047)
Timeframe: Week 240 (Atripla Week 96)

InterventionPercentage of Participants (Number)
EFV+FTC+TDF/Atripla (From Study Baseline)84
All Atripla (From Atripla Baseline)82

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Cumulative Probability of Not Experiencing Regimen Failure

Kaplan-Meier estimate of the cumulative survival probability at week 48 and 96. Blood samples for determining virologic failure were obtained at 16 and 24 weeks, and every 12 weeks thereafter. Virologic failure was defined as a confirmed plasma HIV-1 RNA level >= 1000 copies/mL at or after 16 weeks and before 24 weeks or >=200 copies/mL at or after 24 weeks. Treatment modification was defined as the 1st modification of the regimen, including a permanent discontinuation, switch, or substitution. (NCT00118898)
Timeframe: At week 48 and 96

,,,
Interventionpercentage of participants (Number)
Week 48Week 96
EFV, FTC/TDF, and Placebo ABC/3TC7970
EFV, Placebo FTC/TDF, and ABC/3TC6454
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC8073
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC6657

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Cumulative Probability of Not Experiencing Treatment Modification

Kaplan-Meier estimate of the cumulative survival probability at week 48 and 96. Treatment modification is defined as the 1st modification of the regimen, including a permanent discontinuation, switch, or substitution. (NCT00118898)
Timeframe: At week 48 and 96

,,,
Interventionpercentage of participants (Number)
Week 48Week 96
EFV, FTC/TDF, and Placebo ABC/3TC8073
EFV, Placebo FTC/TDF, and ABC/3TC6756
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC8677
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC7362

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Cumulative Probability of Not Experiencing Virologic Failure

Kaplan-Meier estimate of the cumulative survival probability at week 48 and 96. Blood samples for determining virologic failure were obtained at 16 and 24 weeks, and every 12 weeks thereafter. Virologic failure was defined as a confirmed plasma HIV-1 RNA level >= 1000 copies/mL at or after 16 weeks and before 24 weeks or >=200 copies/mL at or after 24 weeks. (NCT00118898)
Timeframe: At week 48 and 96

,,,
Interventionpercentage of participants (Number)
Week 48Week 96
EFV, FTC/TDF, and Placebo ABC/3TC9490
EFV, Placebo FTC/TDF, and ABC/3TC8885
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC9289
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC8883

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Number of Participants With HIV-1 RNA Levels Less Than 200 Copies/mL

(NCT00118898)
Timeframe: At Weeks 48 and 96

,,,
InterventionParticipants (Number)
Number of Participants with RNA data at Week 48Number with HIV-1 RNA <200 copies/ml at Week 48Number of Participants with RNA data at Week 96Number with HIV-1 RNA <200 copies/ml at Week 96
EFV, FTC/TDF, and Placebo ABC/3TC415398379362
EFV, Placebo FTC/TDF, and ABC/3TC400377361342
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC416391384368
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC411372374346

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The Number of Participants With HIV-1 RNA Levels Less Than 50 Copies/mL

(NCT00118898)
Timeframe: At Weeks 48 and 96

,,,
InterventionParticipants (Number)
Number of Participants with RNA data at Week 48Number with HIV-1 RNA <50 copies/ml at Week 48Number of Participants with RNA data at Week 96Number with HIV-1 RNA <50 copies/ml at Week 96
EFV, FTC/TDF, and Placebo ABC/3TC415372379345
EFV, Placebo FTC/TDF, and ABC/3TC400346361328
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC416348384345
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC411322374317

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Time From Randomization to Virologic Failure

Blood samples for determining virologic failure were obtained at visit weeks 16 and 24 , and every 12 weeks thereafter. Virologic failure was defined as a confirmed plasma HIV-1 RNA level >= 1000 copies/mL at or after 16 weeks after randomization and before 24 weeks, or >=200 copies/mL at or after 24 weeks. The 5th percentile for time to virologic failure is the time (in weeks) at which 5% of the participants have experienced virologic failure. (NCT00118898)
Timeframe: Follow-up time was variable,median follow-up was 138 weeks; see 'Amount of study follow-up' outcome for details

,,,
InterventionWeeks (Number)
5th percentile time to virologic failure10th percentile time to virologic failure
EFV, FTC/TDF, and Placebo ABC/3TC3696
EFV, Placebo FTC/TDF, and ABC/3TC2436
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC2484
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC2436

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Time From Treatment Dispensation to a Grade 3/4 Safety Event

Grade 3/4 safety event is defined as a grade 3 or 4 sign, symptom, or laboratory abnormality that is at least one grade higher than at baseline, total bilirubin and creatine kinase (CPK) were excluded. Grading used the Division of AIDS (DAIDS) 2004 Severity of Adverse Events Tables. (NCT00118898)
Timeframe: All follow-up while on initially assigned regimen; the median (25th, 75th percentile) follow-up while on initial regimen was 120 (54, 156) weeks and the range was 0 to 205 weeks.

,,,
InterventionWeeks (Number)
5th percentile time to a grade 3/4 safety event10th percentile time to a grade 3/4 safety event25th percentile time to a grade 3/4 safety event
EFV, FTC/TDF, and Placebo ABC/3TC2.67.959.3
EFV, Placebo FTC/TDF, and ABC/3TC1.32.016.0
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC3.08.181.4
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC1.33.944.4

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Time From Treatment Dispensation to Regimen Failure (First Occurrence of Virologic Failure or Treatment Modification)

Blood samples for determining virologic failure were obtained at 16 and 24 weeks, and every 12 weeks thereafter. Virologic failure was defined as a confirmed plasma HIV-1 RNA level >= 1000 copies/mL at or after 16 weeks and before 24 weeks or >=200 copies/mL at or after 24 weeks. Treatment modification was defined as the 1st modification of the regimen, including a permanent discontinuation, switch, or substitution. (NCT00118898)
Timeframe: Follow-up time was variable,median follow-up was 138 weeks; see 'Amount of study follow-up' outcome for details

,,,
InterventionWeeks (Number)
5th percentile time to regimen failure10th percentile time to regimen failure25th percentile time to regimen failure
EFV, FTC/TDF, and Placebo ABC/3TC41672
EFV, Placebo FTC/TDF, and ABC/3TC4424
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC41684
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC4436

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Time From Treatment Dispensation to Treatment Modification

Treatment modification is defined as the 1st modification of the regimen, including a permanent discontinuation, switch, or substitution. (NCT00118898)
Timeframe: Follow-up time was variable,median follow-up was 138 weeks; see 'Amount of study follow-up' outcome for details

,,,
InterventionWeeks (Number)
5th percentile time to treatment modification10th percentile time to treatment modification25th percentile time to treatment modification
EFV, FTC/TDF, and Placebo ABC/3TC3.415.083.7
EFV, Placebo FTC/TDF, and ABC/3TC1.42.127.4
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC7.924.9108.9
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC1.65.043.6

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Amount of Study Follow-up

Participants were to be followed for 96 weeks after the last enrollment. Accrual was expected to take 96 weeks, thus the planned follow-up time was 96 to 192 weeks, dependent on when in the study the participant enrolled. This outcome summarizes that total amount of actual follow-up in weeks from randomization to last contact. (NCT00118898)
Timeframe: Follow-up time was variable, median follow-up was 138 weeks

InterventionWeeks (Median)
EFV, FTC/TDF, and Placebo ABC/3TC141.4
EFV, Placebo FTC/TDF, and ABC/3TC133.3
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC141.6
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC137.3

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Number of Participants With a Grade 3/4 Safety Event

Grade 3/4 safety event is defined as a grade 3 or 4 sign, symptom, or laboratory abnormality that is at least one grade higher than at baseline, total bilirubin and creatine kinase (CPK) were excluded. Grading used the Division of AIDS (DAIDS) 2004 Severity of Adverse Events Tables. As-treated analysis censored at 1st modification of initially assigned regimen, participants who never started treatment were excluded. (NCT00118898)
Timeframe: Over all study follow-up while on initially assigned treatment, median follow-up was 120 weeks

Interventionparticipants (Number)
EFV, FTC/TDF, and Placebo ABC/3TC145
EFV, Placebo FTC/TDF, and ABC/3TC182
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC137
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC156

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Number of Participants With Regimen Failure

Blood samples for determining virologic failure were obtained at 16 and 24 weeks, and every 12 weeks thereafter. Virologic failure was defined as a confirmed plasma HIV-1 RNA level >= 1000 copies/mL at or after 16 weeks and before 24 weeks or >=200 copies/mL at or after 24 weeks. Treatment modification was defined as the 1st modification of the regimen, including a permanent discontinuation, switch, or substitution. (NCT00118898)
Timeframe: Follow-up time was variable, median follow-up was 138 weeks; see 'Amount of study follow-up' outcome for details

Interventionparticipants (Number)
EFV, FTC/TDF, and Placebo ABC/3TC162
EFV, Placebo FTC/TDF, and ABC/3TC246
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC157
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC233

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Number of Participants With Treatment Modification

Treatment modification is defined as the 1st modification of the regimen, including a permanent discontinuation, switch, or substitution. (NCT00118898)
Timeframe: Follow-up time was variable, median follow-up was 138 weeks; see 'Amount of study follow-up' outcome for details

Interventionparticipants (Number)
EFV, FTC/TDF, and Placebo ABC/3TC152
EFV, Placebo FTC/TDF, and ABC/3TC239
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC138
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC216

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Number of Participants With Virologic Failure

Blood samples for determining virologic failure were obtained at 16 and 24 weeks, and every 12 weeks thereafter. Virologic failure was defined as a confirmed plasma HIV-1 RNA level >= 1000 copies/mL at or after 16 weeks and before 24 weeks or >=200 copies/mL at or after 24 weeks. (NCT00118898)
Timeframe: Follow-up time was variable, median follow-up was 138 weeks; see 'Amount of study follow-up' outcome for details

Interventionparticipants (Number)
EFV, FTC/TDF, and Placebo ABC/3TC57
EFV, Placebo FTC/TDF, and ABC/3TC72
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC57
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC83

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Number of Participants With Virologic Failure and Emergence of Major Resistance

Emergence of resistant virus was assessed by genotypic testing performed at Stanford University for all participants who met criteria for virologic failure and retrospectively on baseline samples from these participants. Major mutations were defined by International AIDS Society-United States of America (2008), as well as T69D, L74I, G190C/E/Q/T/V for reverse transcriptase and L24I, F53L, I54V/A/T/S, G73C/S/T/A, N88D for protease. (NCT00118898)
Timeframe: Follow-up time was variable,median follow-up was 138 weeks; see 'Amount of study follow-up' outcome for details

Interventionparticipants (Number)
EFV, FTC/TDF, and Placebo ABC/3TC27
EFV, Placebo FTC/TDF, and ABC/3TC41
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC5
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC12

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Change in CD4 Count (Cells/mm3) From Baseline

Change was calculated as the CD4 count at Week 48 (or at Week 96) minus the baseline CD4 count (mean of pre-entry and entry values). (NCT00118898)
Timeframe: At Weeks 48 and 96

,,,
InterventionCells/mm3 (Median)
Week 48Week 96
EFV, FTC/TDF, and Placebo ABC/3TC163220.5
EFV, Placebo FTC/TDF, and ABC/3TC188250.5
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC175251.5
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC177.5250.3

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Change in Fasting High-density Lipoprotein (HDL) Cholesterol Level From Baseline

Only fasting results are included. The protocol did not require that samples be collected fasting. (NCT00118898)
Timeframe: At Weeks 48 and 96

,,,
Interventionmg/dL (Median)
Week 48Week 96
EFV, FTC/TDF, and Placebo ABC/3TC89
EFV, Placebo FTC/TDF, and ABC/3TC1011
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC54
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC87

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Change in Fasting Non-high Density Lipoprotein (Non-HDL) Cholesterol Level From Baseline

Only fasting results are included. The protocol did not require that samples be collected fasting. (NCT00118898)
Timeframe: At Weeks 48 and 96

,,,
Interventionmg/dL (Median)
Week 48Week 96
EFV, FTC/TDF, and Placebo ABC/3TC1413.5
EFV, Placebo FTC/TDF, and ABC/3TC2318
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC810
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC2018

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Change in Fasting Total Cholesterol Level From Baseline

Only fasting results are included. The protocol did not require that samples be collected fasting. (NCT00118898)
Timeframe: At Weeks 48 and 96

,,,
Interventionmg/dL (Median)
Week 48Week 96
EFV, FTC/TDF, and Placebo ABC/3TC2223
EFV, Placebo FTC/TDF, and ABC/3TC3533
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC1114
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC3025

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Change in Fasting Triglyceride Level From Baseline

Only fasting results are included. The protocol did not require that samples be collected fasting. (NCT00118898)
Timeframe: At Weeks 48 and 96

,,,
Interventionmg/dL (Median)
Week 48Week 96
EFV, FTC/TDF, and Placebo ABC/3TC109
EFV, Placebo FTC/TDF, and ABC/3TC1514
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC1411
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC2433

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Cumulative Probability of Not Experiencing a Grade 3/4 Safety Event

Kaplan-Meier estimate of the cumulative survival probability at week 48 and 96. Grade 3/4 safety event is defined as a grade 3 or 4 sign, symptom, or laboratory abnormality that is at least one grade higher than at baseline, total bilirubin and creatine kinase (CPK) were excluded. Grading used the Division of AIDS (DAIDS) 2004 Severity of Adverse Events Tables. As-treated analysis censored at 1st modification of initially assigned regimen, participants who never started treatment were excluded. (NCT00118898)
Timeframe: At week 48 and 96

,,,
Interventionpercentage of participants (Number)
Week 48Week 96
EFV, FTC/TDF, and Placebo ABC/3TC7870
EFV, Placebo FTC/TDF, and ABC/3TC6458
RTV-boosted ATV, FTC/TDF, and Placebo ABC/3TC7973
RTV-boosted ATV, Placebo FTC/TDF, and ABC/3TC7366

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Number of Participants With Identified Electrocardiogram (ECG) Abnormalities

ECG abnormalities are findings that are clinically meaningful by the judgment of the investigator. A 12-lead ECG was performed and all ECG recordings were evaluated by the investigator. Abnormalities, if present at any study time point, were listed. (NCT00162097)
Timeframe: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing)

Interventionparticipants (Number)
EFV600mg Participants With Mild Hepatic Impairment3
EFV600mg Participants With Moderate Hepatic Impairment1
EFV600mg Participants With Severe Hepatic Impairment0
EFV600mg Participants With Normal Hepatic Function5

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Number of Participants Who Experienced AEs Leading to Study Drug Discontinuation

AEs were defined as any new untoward medical occurrences or worsening of a pre-existing medical condition in a participant administered a medicinal product, whether or not considered related to the medicinal product. Participants who discontinued the study due to an AE were recorded. (NCT00162097)
Timeframe: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing).

Interventionparticipants (Number)
EFV600mg Participants With Mild Hepatic Impairment0
EFV600mg Participants With Moderate Hepatic Impairment0
EFV600mg Participants With Severe Hepatic Impairment0
EFV600mg Participants With Normal Hepatic Function0

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Number of Participants With Abnormal Physical Examination Findings at Baseline (Screening and/or Day 1)

The physical examination included an evaluation of the participant's height and body mass index (BMI) (at screening only), and weight. Abnormal physical examination are findings that are clinically meaningful by the judgment of the investigator (NCT00162097)
Timeframe: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing)

Interventionparticipants (Number)
EFV600mg Participants With Mild Hepatic Impairment5
EFV600mg Participants With Moderate Hepatic Impairment2
EFV600mg Participants With Severe Hepatic Impairment1
EFV600mg Participants With Normal Hepatic Function5

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Number of Participants With Clinically Meaningful Vital Signs Measures

Vital signs were recorded throughout the study and included investigations related to body temperature, respiratory rate, seated blood pressure (systolic and diastolic), and heart rate. The investigator used his/her clinical judgement to decide whether or not abnormalities in vital signs were clinically meaningful. (NCT00162097)
Timeframe: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing)

Interventionparticipants (Number)
EFV600mg Participants With Mild Hepatic Impairment0
EFV600mg Participants With Moderate Hepatic Impairment0
EFV600mg Participants With Severe Hepatic Impairment0
EFV600mg Participants With Normal Hepatic Function0

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Time to Reach Maximum Observed Plasma Concentration (Tmax)

Tmax was obtained directly from the concentration-time data. (NCT00162097)
Timeframe: Blood samples were collected at time 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose, relative to administration of PM or AM dose.

Interventionhours (Median)
EFV600mg Participants With Mild Hepatic Impairment1.765
EFV600mg Participants With Moderate Hepatic Impairment4.500
EFV600mg Participants With Severe Hepatic Impairment1.000
EFV600mg Participants With Normal Hepatic Function3.500

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Number of Participants Who Experienced AEs

AEs were defined as any new untoward medical occurrences or worsening of a pre-existing medical condition in a participant administered a medicinal product, whether or not considered related to the medicinal product. (NCT00162097)
Timeframe: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing).

Interventionparticipants (Number)
EFV600mg Participants With Mild Hepatic Impairment1
EFV600mg Participants With Moderate Hepatic Impairment0
EFV600mg Participants With Severe Hepatic Impairment0
EFV600mg Participants With Normal Hepatic Function0

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Number of Participants Who Died or Experienced Other Serious Adverse Events (SAEs)

An SAE was defined as any adverse event (AE) occurring at any dose that; resulted in death; was life threatening; resulted in a persistent or significant disability/incapacity; resulted in/prolonged an existing in-patient hospitalization; was a congenital anomaly/birth defect; was a cancer; or was an overdose. (NCT00162097)
Timeframe: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing). Participants were monitored for SAEs up to 30 days after study discharge.

,,,,
InterventionParticipants (Number)
DeathsOther Serious Adverse Events
Participants Not Dosed11
Participants With Mild Hepatic Impairment00
Participants With Moderate Hepatic Impairment00
Participants With Normal Hepatic Function00
Participants With Severe Hepatic Impairment00

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Number of Participants With Marked Abnormalities (MAs) in Hematology Measurements

MAs are laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following hematology MA definitions specify the criteria for the data presented. Low platelet count: <0.85 x lower limit of normal (LLN) (or if pre-treatment value upper limit of normal [ULN], then NCT00162097)
Timeframe: Throughout study, from screening (within 21 days of Day 1 dosing) through Day 3.

,,,
Interventionparticipants (Number)
Low platelet countLow leukocytesLow neutrophils+bands (absolute)Low lymphocytes (absolute)
EFV600mg Participants With Mild Hepatic Impairment0110
EFV600mg Participants With Moderate Hepatic Impairment1020
EFV600mg Participants With Normal Hepatic Function0100
EFV600mg Participants With Severe Hepatic Impairment0011

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Number of Participants With Serum Chemistry MAs

MAs are laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following serum chemistry MA definitions specify the criteria for MAs in the data presented. High bilirubin (total): >1.1 x ULN (or if pre-treatment value >ULN, then >1.25 x pre-treatment value). High creatinine: >1.33 x pre-treatment value. Low albumin: <0.9 x LLN (or if pre-treatment value 2 x pre-treatment value. (NCT00162097)
Timeframe: Throughout study, from screening (within 21 days of Day 1 dosing) through Day 3.

,,,
Interventionparticipants (Number)
High bilirubin (total) (n = 5, 1, 1, 7)High creatinine (n = 5, 1, 1, 7)Low albumin (n = 5, 1, 1, 7)High amylase (total) (n = 5, 1, 0, 7)
EFV600mg Participants With Mild Hepatic Impairment1000
EFV600mg Participants With Moderate Hepatic Impairment0010
EFV600mg Participants With Normal Hepatic Function0101
EFV600mg Participants With Severe Hepatic Impairment0000

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Number of Participants With Urinalysis MAs

"MAs are laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following urinalysis MA definitions specify the criteria for MAs in the data presented. The presence of white blood cells (WBCs) and red blood cells (RBCs) in the urine was graded on a scale: 0 = no cells present (negative); trace =a small number of cells present; then 1+, 2+, 3+ and 4+, denoting increasingly positive urine results (ie, WBCs/RBCs present in the urine). The MA for both WBCs and RBCs was >= 2+ (or, if pre-treatment value >=2+, then >= 4+)." (NCT00162097)
Timeframe: Throughout study, from screening (within 21 days of Day 1 dosing) through Day 3.

,,,
Interventionparticipants (Number)
White blood cells (WBCs)Red blood cells (RBCs)
EFV600mg Participants With Mild Hepatic Impairment11
EFV600mg Participants With Moderate Hepatic Impairment00
EFV600mg Participants With Normal Hepatic Function00
EFV600mg Participants With Severe Hepatic Impairment00

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Area Under the Plasma Concentration-time Curve Over the Dosing Interval of 24 Hours (AUC[TAU])

The AUC(TAU), from time 0 to the time of the last measurable concentration (t), was calculated by the linear trapezoidal rule. (NCT00162097)
Timeframe: Blood samples were collected at time 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose, relative to administration of PM or AM dose.

Interventionmcg*h/mL (Geometric Mean)
EFV600mg Participants With Mild Hepatic Impairment83.422
EFV600mg Participants With Moderate Hepatic Impairment75.425
EFV600mg Participants With Severe Hepatic Impairment101.912
EFV600mg Participants With Normal Hepatic Function93.516

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Maximum Plasma Concentration (Cmax)

Cmax was obtained directly from the concentration-time data. (NCT00162097)
Timeframe: Blood samples were collected at time 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose, relative to administration of PM or AM dose.

Interventionmicrograms (mcg)/mL (Geometric Mean)
EFV600mg Participants With Mild Hepatic Impairment5.303
EFV600mg Participants With Moderate Hepatic Impairment8.964
EFV600mg Participants With Severe Hepatic Impairment6.750
EFV600mg Participants With Normal Hepatic Function6.515

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Minimum Plasma Concentration (Cmin)

Cmin was obtained directly from the concentration-time data. (NCT00162097)
Timeframe: Blood samples were collected at time 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose, relative to administration of PM or AM dose.

Interventionmcg/mL (Geometric Mean)
EFV600mg Participants With Mild Hepatic Impairment2.599
EFV600mg Participants With Moderate Hepatic Impairment4.885
EFV600mg Participants With Severe Hepatic Impairment3.780
EFV600mg Participants With Normal Hepatic Function2.405

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Cumulative Treatment Failure Rate of Participants on First Line Antiretroviral Therapy Monitored by Primary Health Care Nurses (Investigative Arm)is Not Inferior to the Cumulative Treatment Failure Rate of Participants Monitored by Doctors (Control Arm).

Cumulative treatment failure is a composite endpoint made up of death, virological failure, toxicity failure and protocol-defined loss to follow-up failure. (NCT00255840)
Timeframe: 96 weeks

InterventionPercentage of participants (Number)
Antiretroviral Therapy Monitored by Medical Officer44
Antiretroviral Therapy Managed by Primary Health Care Nurse48

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Time Weighted Mean Change From Baseline Plasma HIV-RNA

(NCT00335322)
Timeframe: 144 weeks

Interventionlog copies/mL (Mean)
TDF/FTC+EFV-2.77
TDF/FTC+ r/ATV-2.88
TDF/FTC + AZT+ABC-2.54

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Time-weighted Mean Change From Baseline Plasma HIV-RNA.

(NCT00335322)
Timeframe: 48 weeks

Interventionlog copies/mL (Mean)
TDF/FTC+EFV-2.59
TDF/FTC+r/ATV-2.69
TDF/FTC+AZT+ABC-2.39

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Serious Adverse Events

Safety outcomes in four different randomly assigned regimens (NCT00342355)
Timeframe: January 2004 until March 31, 2008

Interventionparticipant (Number)
AZT+ddI+EFV73
AZT + ddI + r/LPV69
d4T + 3TC + EFV64
d4T + 3TC + r/LPV60

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Progression to AIDS or Death in tx naïve Pts With Adv HIV dx in the Four Randomly Assigned Regimens.

Progression of disease, AIDS, or death in treatment naive patients with advanced HIV diagnosis will be evaluated in the four randomly assigned regimens. (NCT00342355)
Timeframe: January 2004 until March 31 2008

Interventionparticipants (Number)
AZT+ddI+EFV93
AZT + ddI + r/LPV77
d4T + 3TC + EFV70
d4T + 3TC + r/LPV80

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The Proportion Of Participants With Virologic Response For 10 mg/Day Elvucitabine In HIV-1-Infected Participants By 12 Weeks Compared With The Proportion Of Participants With Lamivudine 300 mg/Day

The proportion of participants having achieved a virologic response for elvucitabine 10 mg/day in combination with efavirenz and tenofovir in HIV-1-infected participants over 12 weeks compared with the proportion of participants having achieved a virologic response for lamivudine 300 mg/day in combination with efavirenz and tenofovir. Virologic response was defined as having achieved undetectable (<50 copies/mL) HIV-1 RNA levels from baseline assessment. (NCT00350272)
Timeframe: 12 weeks

,
Interventionpercentage of participants (Number)
Week 2Week 4Week 6Week 8Week 10Week 12
Elvucitabine13.516.227.035.154.156.8
Lamivudine8.110.835.154.156.870.3

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The Safety Profile Of Elvucitabine.

Determination of the safety profile of elvucitabine as defined by the frequency, type and severity of treatment-emergent adverse events (AEs) and the frequency of Grade 3 and Grade 4 laboratory abnormalities. (NCT00350272)
Timeframe: 12 weeks

,
Interventionparticipants (Number)
Treatment emergent adverse eventsTreatment emergent severe adverse eventsTreatment related serious adverse eventsDiscontinuations due to adverse eventsTreatment emergent Grade 3/4 lab abnormalities
Elvucitabine, Efavirenz,Tenofovir363026
Lamivudine,Efavirenz,Tenofovir352005

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Percent of CD4 Cells Change From Baseline at Weeks 60, 72, 84, and 96 - Treated Participants

A CD4 cell is an antigenic marker of helper/inducer T cells. These cells were counted during the hematology cell counts performed during a Complete Blood Cell count (CBC) performed by the Central Laboratory. CD4 are measured as number of cells per millimeter to the third power (cells/mm^3). Percent of CD4 cells is the number of CD4 cells per total number of cells measured*100. An increase in the percent of CD4 cells is an improvement. The Baseline visit was within 50 days after the screening visit and was prior to start of study medication (Week 1). (NCT00364793)
Timeframe: Baseline to Weeks 60, 72, 84, and 96

,,,,
Interventionpercentage of CD4 cells (Median)
Baseline (n=7,9,3,5,24)Week 60 (n=3,6,2,3,14)Week 72 (n=2,7,1,3,13)Week 84 (n=3,7,1,3,14)Week 96 (n=3,6,1,3,13)
EFV+ddI+FTC in All Participants247177
EFV+ddI+FTC in Children >= 2 Years to < 3 Years127-1215
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years713121214
EFV+ddI+FTC in Infants >=3 Months to < 6 Months2810-14-3-2
EFV+ddI+FTC in Infants >=6 Months to < 2 Years263187

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The Number of Participants With Plasma HIV RNA < 400 Copies Per Milliliter (c/mL) at Week 48 as Analyzed by Different Algorithms - All Treated Participants

Algorithms: Confirmed Virologic Response (CVR) non-completer = failure (NC = F): participants were responders if they achieved confirmed HIV RNA < 400 c/mL at Week 48; participants were failures if virologic rebound occurred at or before Week 48; therapy discontinued before Week 48; no response by Week 48, or missing HIV RNA at Week 48 and beyond. Virologic Response - Observed Cases (VR-OC): participants were responders according to a single on-treatment HIV RNA < 400 c/mL closest to the planned Week 48 visit and within the predefined Week 48 visit window; those on treatment and missing their Week 48 measurement were responders only if previous and subsequent measurements to the Week 48 visit window were < 400 c/mL; denominator was all who remained on treatment through Week 48. Snapshot: participants were responders according to the last on-treatment HIV RNA < 400 c/mL in the predefined Week 48 visit window; denominator was all treated participants. (NCT00364793)
Timeframe: Week 48

,,,,
Interventionparticipants (Number)
CVR (NC=F) n=15, 10, 4, 8, 37VR-OC n=9, 9, 3, 6, 27SNAPSHOT n=15, 10, 4, 8, 37
EFV+ddI+FTC in Children >= 2 Years to < 3 Years333
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years555
EFV+ddI+FTC in Infants >=3 Months to < 6 Months777
EFV+ddI+FTC in Infants >=6 Months to < 2 Years666
Total Participants212121

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The Number of Participants With Plasma HIV RNA Levels < 400 c/mL at Week 24 as Analyzed by Different Algorithms - All Treated Participants

Algorithms: Confirmed Virologic Response (CVR) non-completer = failure (NC = F): participants were responders if they achieved confirmed HIV RNA < 400 c/mL at Week 24; participants were failures if virologic rebound occurred at or before Week 24; therapy discontinued before Week 24; no response by Week 24, or missing HIV RNA at Week 24 and beyond. Virologic Response - Observed Cases (VR-OC): participants were responders according to a single on-treatment HIV RNA < 400 c/mL closest to the planned Week 24 visit and within the predefined Week 24 visit window; those on treatment and missing their Week 24 measurement were responders only if previous and subsequent measurements to the Week 24 visit window were < 400 c/mL; denominator was all who remained on treatment through Week 24. (NCT00364793)
Timeframe: Week 24

,,,,
Interventionparticipants (Number)
CVR (n=15, 10, 4, 8, 37)VR-OC(n=11,10 ,4, 7, 32)
EFV+ddI+FTC in All Participants2625
EFV+ddI+FTC in Children >= 2 Years to < 3 Years44
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years76
EFV+ddI+FTC in Infants >=3 Months to < 6 Months88
EFV+ddI+FTC in Infants >=6 Months to < 2 Years77

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The Number of Participants With Plasma HIV RNA Levels < 400 c/mL at Weeks 60, 72, 84 and 96 (Observed Cases) - All Treated Participants

Virologic Response - Observed Cases (VR-OC): participants were responders at a specific week according to a single on-treatment HIV RNA < 400 c/mL closest to the planned visit and within the predefined visit window; those on treatment and missing their specific week measurement were responders only if previous and subsequent measurements to that week visit window were < 400 c/mL; denominator was all who remained on treatment through the specific week. (NCT00364793)
Timeframe: Weeks 60, 72, 84, and 96

,,,,
Interventionparticipants (Number)
Week 60 (n=7, 8, 3, 4, 22)Week 72 (n=7, 7, 2, 4, 20)Week 84 (n=7, 7, 2, 4, 20)Week 96 (n=7, 6, 2, 4, 19)
EFV+ddI+FTC in All Participants19171717
EFV+ddI+FTC in Children >= 2 Years to < 3 Years2111
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years4444
EFV+ddI+FTC in Infants >=3 Months to < 6 Months7777
EFV+ddI+FTC in Infants >=6 Months to < 2 Years6555

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CD4 Cell Count Change From Baseline at Weeks 24 and 48 - Treated Participants

A CD4 cell is an antigenic marker of helper/inducer T cells. These cells were counted during the hematology cell counts performed during a Complete Blood Cell count (CBC) performed by the Central Laboratory. CD4 are measured as number of cells per millimeters to the third power (cells/mm^3). An increase from baseline in the number of CD4 cells is an improvement. The Baseline visit was within 50 days after the screening visit and was prior to start of study medication (Week 1). (NCT00364793)
Timeframe: Baseline to Weeks 24 and 48

,,,,
Interventioncells/mm^3 (Median)
Baseline (n=10, 9, 3, 6, 28)Week 24 (n=6, 7, 3, 6, 22)Week 48 (n=7, 8, 2, 5, 22)
EFV+ddI+FTC in All Participants1144177196
EFV+ddI+FTC in Children >= 2 Years to < 3 Years51731971
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years413283284
EFV+ddI+FTC in Infants >=3 Months to < 6 Months1518259-258
EFV+ddI+FTC in Infants >=6 Months to < 2 Years156982346

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The Number of Participants With Plasma HIV RNA Levels < 50 c/mL at Week 48 as Analyzed by Different Algorithms - All Treated Participants

Algorithms: Confirmed Virologic Response (CVR) non-completer = failure (NC = F): participants were responders if they achieved confirmed HIV RNA < 50 c/mL at Week 48; participants were failures if virologic rebound occurred at or before Week 48; therapy discontinued before Week 48; no response by Week 48, or missing HIV RNA at Week 48 and beyond. Virologic Response - Observed Cases (VR-OC): participants were responders according to a single on-treatment HIV RNA < 50 c/mL closest to the planned Week 48 visit and within the predefined Week 48 visit window; those on treatment and missing their Week 48 measurement were responders only if previous and subsequent measurements to the Week 48 visit window were < 50 c/mL; denominator was all who remained on treatment through Week 48. Snapshot: participants were responders according to the last on-treatment HIV RNA < 50 c/mL in the predefined Week 48 visit window; denominator was all treated participants. (NCT00364793)
Timeframe: Week 48

,,,,
Interventionparticipants (Number)
CVR (NC=F) n=15, 10, 4, 8, 37VR-OC n=9, 9, 3, 6, 27SNAPSHOT n=15, 10, 4, 8, 37
EFV+ddI+FTC in All Participants181717
EFV+ddI+FTC in Children >= 2 Years to < 3 Years222
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years444
EFV+ddI+FTC in Infants >=3 Months to < 6 Months666
EFV+ddI+FTC in Infants >=6 Months to < 2 Years655

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The Number of Participants With Plasma HIV RNA Levels < 50 c/mL at Weeks 60, 72, 84 and 96 (Observed Cases) - All Treated Participants

Virologic Response - Observed Cases (VR-OC): participants were responders at a specific week according to a single on-treatment HIV RNA < 50 c/mL closest to the planned visit and within the predefined visit window; those on treatment and missing their specific week measurement were responders only if previous and subsequent measurements to that week visit window were < 50 c/mL; denominator was all who remained on treatment through the specific week. (NCT00364793)
Timeframe: Weeks 60, 72, 84, and 96

,,,,
Interventionparticipants (Number)
Week 60 (n=7, 8, 3, 4, 22)Week 72 (n=7, 7, 2, 4, 20)Week 84 (n=7, 7, 2, 4, 20)Week 96 (n=7, 6, 2, 4, 19)
EFV+ddI+FTC in All Participants14171615
EFV+ddI+FTC in Children >= 2 Years to < 3 Years2110
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years3434
EFV+ddI+FTC in Infants >=3 Months to < 6 Months4776
EFV+ddI+FTC in Infants >=6 Months to < 2 Years5555

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Apparent Oral Clearance Adjusted for Body Weight (CLT/F/kg) of EFV at Week 2 - Pharmacokinetic Evaluable Population

Plasma concentrations of EFV were determined using a validated liquid chromatography tandem mass spectrometry method (LC-MS/MS). The lower limit of quantification (LLOQ) for EFV was 10.0 nanograms per milliliter (ng/mL) and the upper limit of quantification (ULOQ) was 8,000 ng/mL. CLT/F/kg was calculated by dividing CLT/F by body weight in kilograms (kg). Blood samples were collected before study drug administration and at 0.5, 1, 3, 5, 8, and 24 hours after study drug administration from an indwelling catheter or by direct venipuncture and the pharmacokinetic parameters were summarized using geometric means. CLT/F/kg was measured in liters per hour per kilogram (L/h/kg). (NCT00364793)
Timeframe: Week 2

InterventionL/h/kg (Geometric Mean)
EFV+ddI+FTC in Infants >=3 Months to < 6 Months2.07
EFV+ddI+FTC in Infants >=6 Months to < 2 Years2.36
EFV+ddI+FTC in Children >= 2 Years to < 3 Years1.44
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years0.66

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Area Under the Plasma Concentration Time Curve (AUC) Over One Dosing Interval From Time Zero to 24 Hours Post-dose(TAU) at Week 2 - Pharmacokinetic Evaluable Population

Plasma concentrations were obtained using a validated liquid chromatography tandem mass spectrometry method (LC-MS/MS). The lower limit of quantification (LLOQ) for EFV was 10.0 nanograms per milliliter (ng/mL) and the upper limit of quantification (ULOQ) was 8,000 ng/mL. AUC(TAU) was calculated by log- and linear trapezoidal summations. If a concentration was < LLOQ at time TAU, the value of the concentration at time TAU was estimated using the quotient of the last quantifiable concentration and λ. Blood samples were collected before study drug administration and at 0.5, 1, 3, 5, 8, and 24 hours after study drug administration from an indwelling catheter or by direct venipuncture and the pharmacokinetic parameters summarized using geometric means. AUC(TAU) was measured in micromolars*time (µM•h). (NCT00364793)
Timeframe: Week 2

InterventionµM•h (Geometric Mean)
EFV+ddI+FTC in Infants >=3 Months to < 6 Months129.5
EFV+ddI+FTC in Infants >=6 Months to < 2 Years71.4
EFV+ddI+FTC in Children >= 2 Years to < 3 Years93.8
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years130.8

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AUC (TAU) of Didanosine (ddI) at Week 2 - Pharmacokinetic Evaluable Population

Plasma concentrations were obtained using a validated LC-MS/MS at Week 2. The lower limit of quantification (LLOQ) for ddI was 2.50 nanograms per milliliter (ng/mL). AUC(TAU) was calculated by log- and linear trapezoidal summations. If a concentration was < LLOQ at time TAU, the value of the concentration at time TAU was estimated using the quotient of the last quantifiable concentration and λ. Blood samples were collected before study drug administration and at 0.5, 1, 3, 5, 8, and 24 hours after study drug administration from an indwelling catheter or by direct venipuncture and the pharmacokinetic parameters summarized using geometric means. AUC(TAU) was measured in nanograms*time per milliliter (ng•h/mL). (NCT00364793)
Timeframe: Week 2

Interventionng•h/mL (Geometric Mean)
EFV+ddI+FTC in Infants >=3 Months to < 6 Months1445
EFV+ddI+FTC in Infants >=6 Months to < 2 Years2848
EFV+ddI+FTC in Children >= 2 Years to < 3 Years1038
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years1000

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The Number of Participants With Plasma HIV RNA Levels < 50 c/mL at Week 24 as Analyzed by Different Algorithms - All Treated Participants

Algorithms: Confirmed Virologic Response (CVR) non-completer = failure (NC = F): participants were responders if they achieved confirmed HIV RNA < 50 c/mL at Week 24; participants were failures if virologic rebound occurred at or before Week 24; therapy discontinued before Week 24; no response by Week 24, or missing HIV RNA at Week 24 and beyond. Virologic Response - Observed Cases (VR-OC): participants were responders according to a single on-treatment HIV RNA < 50 c/mL closest to the planned Week 24 visit and within the predefined Week 24 visit window; those on treatment and missing their Week 24 measurement were responders only if previous and subsequent measurements to the Week 24 visit window were < 50 c/mL; denominator was all who remained on treatment through Week 24. (NCT00364793)
Timeframe: Week 24

,,,,
Interventionparticipants (Number)
CVR (n=15, 10, 4, 8, 37)VR-OC (n=11, 10, 4, 7, 32)
EFV+ddI+FTC in All Participants1516
EFV+ddI+FTC in Children >= 2 Years to < 3 Years32
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years44
EFV+ddI+FTC in Infants >=3 Months to < 6 Months45
EFV+ddI+FTC in Infants >=6 Months to < 2 Years45

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CLT/F of Didanosine (ddI) at Week 2 - Pharmacokinetic Evaluable Population

Plasma concentrations for ddI were determined using a validated LC/MS/MS assay. The LLOQ for ddI was 2.50 nanograms per milliliter (ng/mL). CLT/F was calculated by dividing the dose of ddI by AUC(TAU) of ddI. Blood samples were collected before study drug administration and at 0.5, 1, 3, 5, 8, and 24 hours after study drug administration from an indwelling catheter or by direct venipuncture and the pharmacokinetic parameters were summarized using geometric means. CLT/F was measured in liters per hour (L/h). (NCT00364793)
Timeframe: Week 2

InterventionL/h (Geometric Mean)
EFV+ddI+FTC in Infants >=3 Months to < 6 Months40.7
EFV+ddI+FTC in Infants >=6 Months to < 2 Years35.6
EFV+ddI+FTC in Children >= 2 Years to < 3 Years113.9
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years143.0

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CLT/F/kg of Didanosine (ddI) at Week 2 - Pharmacokinetic Evaluable Population

Plasma concentrations for ddI were determined using a validated LC/MS/MS assay. The LLOQ for ddI was 2.50 nanograms per milliliter (ng/mL). CLT/F/kg was calculated by dividing CLT/F by body weight in kilograms (kg). Blood samples were collected before study drug administration and at 0.5, 1, 3, 5, 8, and 24 hours after study drug administration from an indwelling catheter or by direct venipuncture and the pharmacokinetic parameters were summarized using geometric means. CLT/F/kg was measured in liters per hour per kilogram (L/h/kg). (NCT00364793)
Timeframe: Week 2

InterventionL/h/kg (Geometric Mean)
EFV+ddI+FTC in Infants >=3 Months to < 6 Months7.88
EFV+ddI+FTC in Infants >=6 Months to < 2 Years4.26
EFV+ddI+FTC in Children >= 2 Years to < 3 Years11.36
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years10.34

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Apparent Oral Clearance (CLT/F) of EFV at Week 2 - Pharmacokinetic Evaluable Population

Plasma concentrations of EFV were obtained using a validated liquid chromatography tandem mass spectrometry method (LC-MS/MS). The lower limit of quantification (LLOQ) for EFV was 10.0 nanograms per milliliter (ng/mL) and the upper limit of quantification (ULOQ) was 8,000 ng/mL. CLT/F was calculated by dividing the dose of EFV by AUC(TAU) of EFV. Blood samples were collected before study drug administration and at 0.5, 1, 3, 5, 8, and 24 hours after study drug administration from an indwelling catheter or by direct venipuncture and the pharmacokinetic parameters were summarized using geometric means. CLT/F was measured in liters per hour (L/h). (NCT00364793)
Timeframe: Week 2

InterventionL/h (Geometric Mean)
EFV+ddI+FTC in Infants >=3 Months to < 6 Months9.54
EFV+ddI+FTC in Infants >=6 Months to < 2 Years19.69
EFV+ddI+FTC in Children >= 2 Years to < 3 Years13.16
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years9.11

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Terminal Phase Elimination Half-life (T-HALF) in Didanosine (ddI) at Week 2 - Pharmacokinetic Evaluable Population

Plasma concentrations for ddI were determined using a validated LC/MS/MS assay. The LLOQ for ddI was 2.50 nanograms per milliliter (ng/mL). Blood samples were collected before study drug administration and at 0.5, 1, 3, 5, 8, and 24 hours after study drug administration from an indwelling catheter or by direct venipuncture and the T-HALF was summarized using a mean. Terminal elimination plasma half-life=ln2 divided by K where K is the absolute value of the slope of the terminal phase of the plasma profile as determined by log-linear regression of at least three data points. T-HALF was measured in hours (h). (NCT00364793)
Timeframe: Week 2

Interventionh (Mean)
EFV+ddI+FTC in Infants >=3 Months to < 6 Months0.92
EFV+ddI+FTC in Infants >=6 Months to < 2 Years1.41
EFV+ddI+FTC in Children >= 2 Years to < 3 Years1.73
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years1.14

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CD4 Cell Count Change From Baseline at Weeks 60, 72, 84, and 96 - Treated Participants

A CD4 cell is an antigenic marker of helper/inducer T cells. These cells were counted during the hematology cell counts performed during a Complete Blood Cell count (CBC) performed by the Central Laboratory. CD4 are measured as number of cells per millimeters to the third power (cells/mm^3). An increase from baseline in the number of CD4 cells is an improvement. The Baseline visit was within 50 days after the screening visit and was prior to start of study medication (Week 1). (NCT00364793)
Timeframe: Baseline to Weeks 60, 72, 84, and 96

,,,,
Interventioncells/mm^3 (Median)
Baseline (n=10,9,3,6,28)Week 60 (n=6, 6, 2,3,17)Week 72 (n=5, 7, 1, 3, 16)Week 84 (n=6, 7, 1, 3, 17)Week 96 (n=6, 6, 1, 3, 16)
EFV+ddI+FTC in All Participants1144-3159259-40
EFV+ddI+FTC in Children >= 2 Years to < 3 Years517580-50101402
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years413676620497744
EFV+ddI+FTC in Infants >=3 Months to < 6 Months1518-870-1178-937-834
EFV+ddI+FTC in Infants >=6 Months to < 2 Years1569-91423459-43

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Cmax and Cmin of Didanosine (ddI) at Week 2 - Pharmacokinetic Evaluable Population

Cmax and Cmin were derived from plasma concentration versus time. Plasma concentrations for ddI were determined using a validated LC/MS/MS assay. All reportable Cmin values were =6 months to < 2 years (Group 2); LLOQ/2 was imputed for those summary statistics;in Group 2, 9 of 10 Cmin values were NCT00364793)
Timeframe: Week 2

,,,
Interventionng/mL (Geometric Mean)
Cmax (n=12, 10, 4, 6)Cmin (n=4, 10, 4, 3)
EFV+ddI+FTC in Children >= 2 Years to < 3 Years3561.25
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years3761.25
EFV+ddI+FTC in Infants >=3 Months to < 6 Months8501.25
EFV+ddI+FTC in Infants >=6 Months to < 2 Years11931.54

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Log10 c/mL HIV RNA Changes From Baseline at Weeks 60, 72, 84 and 96 - Treated Participants

HIV RNA measured as log10 copies per milliliter (c/mL) plasma. HIV RNA values ≥ 1,000 c/mL were considered evidence of infection. A decrease in number of c/mL is an improvement for the participant. HIV RNA was first measured using the ultrasensitive and standard Roche Amplicor PCR, version 1.5, and then the method of measurement was switched to the COBAS AmpliPrep/COBAS TaqMan HIV IVD method. The Baseline visit was within 50 days after the screening visit and was prior to start of study medication (Week 1). (NCT00364793)
Timeframe: Baseline through Weeks 60, 72, 84, and 96

,,,,
Interventionlog10 c/mL (Median)
Baseline (n=13,10,4,7,34)Week 60 (n=7, 8, 3, 4, 22)Week 72 (n=7, 6, 1, 3, 17)Week 84 (n=7, 7, 2, 4, 20)Week 96 (n=7, 6, 2, 4, 19)
EFV+ddI+FTC in All Participants5.88-3.50-3.45-3.37-3.45
EFV+ddI+FTC in Children >= 2 Years to < 3 Years5.88-3.26-3.20-2.18-2.15
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years5.50-3.48-4.18-3.51-3.57
EFV+ddI+FTC in Infants >=3 Months to < 6 Months5.88-3.92-4.08-4.08-3.82
EFV+ddI+FTC in Infants >=6 Months to < 2 Years5.88-3.44-2.75-3.28-3.73

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Log10 c/mL HIV RNA Changes From Baseline Through Week 48 - Treated Participants

HIV RNA measured as log10 copies per milliliter (c/mL) plasma. HIV RNA values ≥ 1,000 c/mL were considered evidence of infection. A decrease in number of c/mL is an improvement for the participant. HIV RNA was first measured using the ultrasensitive and standard Roche Amplicor PCR, version 1.5, and then the method of measurement was switched to the COBAS AmpliPrep/COBAS TaqMan HIV IVD method. The Baseline visit was within 50 days after the screening visit and was prior to start of study medication (Week 1). (NCT00364793)
Timeframe: Baseline through Week 48

,,,,
Interventionlog10 c/mL (Median)
Baseline (n=13,10,4,7,34)Week 2 (n=12, 9, 4, 5, 30)Week 4 (n=11, 8, 4, 6, 29)Week 8 (n=11, 10, 3, 7, 31)Week 12 (n=10, 10, 3, 6, 29)Week 16 (n=10, 10, 4, 7, 31)Week 24 (n=10, 9, 3, 7, 29)Week 32 (n=9, 9, 4, 6, 28)Week 40 (n=7, 9, 4 ,6, 26)Week 48 (n=9, 9, 3, 6, 27)
EFV+ddI+FTC in All Participants5.88-2.11-2.63-2.92-3.14-3.27-3.28-3.27-3.93-3.18
EFV+ddI+FTC in Children >= 2 Years to < 3 Years5.88-2.42-2.86-2.92-4.02-4.11-4.18-3.73-4.02-3.27
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years5.50-1.93-3.04-3.27-3.31-3.44-2.95-2.93-2.93-2.93
EFV+ddI+FTC in Infants >=3 Months to < 6 Months5.88-1.89-2.18-2.73-2.48-2.72-3.46-2.75-4.01-2.92
EFV+ddI+FTC in Infants >=6 Months to < 2 Years5.88-2.26-2.49-2.91-3.19-3.17-3.92-3.28-4.17-3.27

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Maximum Observed Plasma Concentration (Cmax) and Plasma Concentration 24 Hours Post-dose (Cmin) of EFV at Week 2 - Pharmacokinetic Evaluable Population

Cmax and Cmin were derived from plasma concentrations versus time using a validated liquid chromatography tandem mass spectrometry method (LC-MS/MS). The lower limit of quantification (LLOQ) for EFV was 10.0 nanograms per milliliter (ng/mL) and the upper limit of quantification (ULOQ) was 8,000 ng/mL. Cmax and Cmin were recorded directly from experimental observations. Blood samples were collected before study drug administration and at 0.5, 1, 3, 5, 8, and 24 hours after study drug administration from an indwelling catheter or by direct venipuncture and the pharmacokinetic parameters were summarized using geometric means. Cmax and Cmin were measured in ng/mL. (NCT00364793)
Timeframe: Week 2

,,,
Interventionng/mL (Geometric Mean)
CmaxCmin
EFV+ddI+FTC in Children >= 2 Years to < 3 Years2167648
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years26321185
EFV+ddI+FTC in Infants >=3 Months to < 6 Months3790391
EFV+ddI+FTC in Infants >=6 Months to < 2 Years1998445

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Number of Participants With Acquisition of Resistance to EFV Categorized by AUC Relationship - Evaluable Pharmacokinetic Population

PK parameters were evaluated 2 weeks post start of dosing. Based on observed AUC, measured in micromoles (μM)*h, dosing was increased, remained the same, or decreased at next visit to achieve the desired AUC (110-380 μM*h). Number of participants who became resistant was categorized by those who required additional dosing after Week 2 (AUC<110 μM*h) and those who did not. AUC: derived from plasma concentration of EFV versus time. Plasma concentrations for determination of AUC were obtained using a validated LC-MS/MS method. LLOQ for EFV = 10.0 ng/mL and ULOQ = 8,000 ng/mL. AUC calculated by log- and linear trapezoidal summations. Genotypic resistance=presence of substitutions in the RT gene and/or presence of mutations that confer resistance to entire nucleoside reverse transcriptase inhibitor class. Phenotypic resistance=EFV: > 3.3* IC50 of control strain. Assays: Monogram Biosciences Phenosense™ GT (EFV biologic cutoff=3) and VircoTYPE™ HIV-1 v 4.3.01( EFV biologic cutoff=3.3). (NCT00364793)
Timeframe: Baseline to Week 48

,,,,
Interventionparticipants (Number)
Resistant; AUC<110 µM•h(n=2,7,2,3,14)Resistant; AUC>=110 µM•h(n=10,3,2,4,19)
EFV+ddI+FTC in All Participants64
EFV+ddI+FTC in Children >= 2 Years to < 3 Years10
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years10
EFV+ddI+FTC in Infants >=3 Months to < 6 Months12
EFV+ddI+FTC in Infants >=6 Months to < 2 Years32

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Number of Treated Participants With Resistance Associated Genotypic and Phenotypic Changes in Viruses - Participants With Virologic Failure, Lack of Suppression or Viral Load Rebound

At baseline, treatment-naïve screened by genotype; treatment-experienced screened by genotype and phenotype. Genotypic resistance: presence of substitutions in reverse transcriptase (RT) gene and/or presence of mutations that confer resistance to nucleoside reverse transcriptase inhibitor class. Phenotype resistance: FTC: > 3.1* the 50% inhibitory concentration (IC50) of the control strain; EFV: > 3.3* IC50 ; ddI: > 2.6*IC50. Virologic failure: <1 log10 decrease in HIV RNA from Week 16 on; confirmatory HIV RNA within 14-35 days; HIV RNA > 10,000 c/mL with prior value < 400 c/mL; confirmatory HIV RNA 14-35 days. Monogram Biosciences Phenosense™ assay ( EFV and FTC: biologic cutoffs=3 and 3.5, respectively; ddI: clinical cutoff: lower limit=1.39; upper limit = 2.2.); VircoTYPE™ HIV-1 v 4.3.01( EFV, FTC: biologic cutoffs=3.3 and 3.1, respectively;ddI: clinical cutoff: lower limit = 0.9; upper limit = 2.6. No genotypic/phenotypic changes in presence of virologic failure=no resistance. (NCT00364793)
Timeframe: Baseline to Week 48

,,,,
Interventionparticipants (Number)
Lack of suppression with Changes (PP)Viral Load Rebound with Changes(PP)Viral Failure with Changes (outside 35 day limit)
EFV+ddI+FTC in All Participants325
EFV+ddI+FTC in Children >= 2 Years to < 3 Years001
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years001
EFV+ddI+FTC in Infants >=3 Months to < 6 Months210
EFV+ddI+FTC in Infants >=6 Months to < 2 Years113

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Number of Participants With Hematologic Abnormalities - Treated Participants

Abnormalities were determined from laboratory measurements analyzed at the central or local laboratory. DAIDS DAIDS Grading Severity of Adult and Pediatric AEs v Dec 2004. Hemoglobin Gr 1: 8.5-10.0 g/dL; Gr 2: 7.5-8.4 g/dL; Gr 3: 6.50-7.4 g/dL; Gr 4: <6.5 g/dL; Platelets, decreased: Gr 1: 100.000-124.999*10^9/L; Gr 2: 50.000-99.999*10^9/L; Gr 3: 25.000-49.999*10^9/L; Gr 4: <25.000*10^9/L; White blood cell count (WBC) decreased Gr 1: 2.000-2.500*10^9/L; Gr 2: 1.500-1.999*10^9/L; Gr 3: 1.000-1.499*10^9/L; Gr 4: <1.000*10^9/L. Baseline visit was within 50 days post screening and was prior to start of study drug (Week 1). (NCT00364793)
Timeframe: Baseline to Week 96

,,,,
Interventionparticipants (Number)
Hemoglobin (n=11, 10, 4, 7, 32)Platelet (n=11, 10, 4, 7, 32)Neutrophils (n=11, 10, 4, 7, 32)
EFV+ddI+FTC in All Participants12210
EFV+ddI+FTC in Children >= 2 Years to < 3 Years200
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years101
EFV+ddI+FTC in Infants >=3 Months to < 6 Months417
EFV+ddI+FTC in Infants >=6 Months to < 2 Years512

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Number of Participants With Lipid and Glucose Laboratory Abnormalities - Treated Participants

Abnormalities were determined from measurements analyzed at central or local laboratory. DAIDS Grading Severity of Adult and Pediatric AEs v Dec 2004. Total Cholesterol (fasting) Gr 1: 170 - 199 mg/dL; Gr 2: 200 - 300 mg/dL; Gr 3 >300 mg/dL; Gr 4 Not Applicable(NA). LDL cholesterol, fasting: Gr 1: 110-129 mg/dL; Gr 2: 130-189 mg/dL; Gr 3 >=190 mg/dL; Gr 4 NA. Triglycerides, fasting: Gr 1: NA; Gr 2 500-750 mg/dL; Gr 3: 751-1,200 mg/dL; Gr 4: >1,200 mg/dL. Glucose, serum, high, fasting and (non-fasting): Gr 1: 110 - 125 (116-160) mg/dL; Gr 2: 126-250 (161- 250) mg/dL; Gr 3: 251-500 (251-500) mg/dL; Gr 4: >500 (> 500) mg/dL. Glucose, serum, low, >=1 month of age (<1 month): Gr 1: 55-64 (50-54) mg/dL; Gr 2: 40-54 (40-49) mg/dL; Gr 3: 30-39 (30-39) mg/dL; Gr 4: <30 (<30) mg/dL. Baseline: within 50 days after the screening visit and was prior to start of study medication (Week 1). Only those in 4th arm were old enough to fast prior to testing; other arms did not have fasting samples taken. (NCT00364793)
Timeframe: Baseline to Week 96

,,,,
Interventionparticipants (Number)
Total Cholesterol (n=9,10,4,0,23)Total Cholesterol Fasting (n=0,0,0,7,7)Glucose High (n=11,10,3,0,24)Glucose Low (n=11,10,3,0,24)Glucose High Fasting (n=0,0,0,7,7)LDL cholesterol (n=9,10,4,0,23)LDL cholesterol fasting (n=0,0,0,7,7)
EFV+ddI+FTC in All Participants7113141
EFV+ddI+FTC in Children >= 2 Years to < 3 Years1NA00NA0NA
EFV+ddI+FTC in Children >= 3 Years to <= 6 YearsNA1NANA1NA1
EFV+ddI+FTC in Infants >=3 Months to < 6 Months2NA12NA0NA
EFV+ddI+FTC in Infants >=6 Months to < 2 Years4NA01NA4NA

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Number of Participants With Liver Function Test Laboratory Abnormalities - Treated Population

Abnormalities were determined from laboratory measurements analyzed at the central or local laboratory. Division of AIDS Table (DAIDS) for Grading Severity of Adult and Pediatric AEs version (v) Dec 2004. Upper limit of normal (ULN): lower limit of normal (LLN), alanine transaminase (ALT); aspartate aminotransferase (AST); alkaline phosphatase (ALP). ALT Grade (Gr) 1: 1.25 to 2.5*ULN; Gr 2: 2.6 to 5.0*ULN; Gr 3: 5.1 to 10.0*ULN; Gr 4: >10.0*ULN. AST Gr 1: 1.25 to 2.5*ULN; Gr 2: 2.6 to 5.0*ULN; Gr 3: 5.1 to 10.0*ULN; Gr 4: >10.0*ULN. Total bilirubin Gr 1: 1.25 to 1.5*ULN; Gr 2: 1.6 to 2.5*ULN; Gr 3: 2.6 to 5.0*ULN; Gr 4: >5.0*ULN. ALP (U/L) Gr 1: 1.25 to 2.5*ULN, Gr 2: 2.6 to 5.0*ULN, Gr 3: 5.1 to 10.0*ULN, Gr 4: >10.0*ULN. Albumin (low) Gr 1: 3 grams per deciliter (g/dL) to NCT00364793)
Timeframe: Baseline to Week 96

,,,,
Interventionparticipants (Number)
Albumin (n=12, 10, 4, 7, 33)ALP (n=12, 10, 4, 7, 33)ALT (n=12, 10, 4, 7, 33)AST (n=12, 10, 4, 7, 33)
EFV+ddI+FTC in All Participants1171210
EFV+ddI+FTC in Children >= 2 Years to < 3 Years1221
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years0500
EFV+ddI+FTC in Infants >=3 Months to < 6 Months0878
EFV+ddI+FTC in Infants >=6 Months to < 2 Years0231

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Number of Participants With Serum Chemistry Abnormalities - Treated Participants

Central/local laboratory. DAIDS v 2004. Bicarbonate, low: Gr 1: 16 milliequivalents per liter (mEq/L) - < LLN; Gr 2: 11.0-15.9 mEq/L; Gr 3: 8.0-10.9 mEq/L; Gr 4: <8.0 mEq/L; calcium, high Gr 1: 10.6-11.5 mg/dL; Gr 2: 11.6-12.5 mg/dL; Gr 3 12.6-13.5 mg/dL; Gr 4: >13.5 mg/dL; calcium, low Gr1: 7.8-8.4 mg/dL; Gr2: 7.0-7.7 mg/dL; Gr3: 6.1-6.9 mg/dL; Gr 4: <6.1 mg/dL; creatinine Gr1: 1.1-1.3*ULN; Gr 2: 1.4-1.8*ULN; Gr 3: 1.9-3.4*ULN; Gr 4: >=3.5*ULN; lipase Gr 1: 1.1-1.5*ULN; Gr 2: 1.6-3.0*ULN; Gr 3: 3.1-5.0*ULN; Gr 4: >5.0*ULN; potassium high (low) Gr 1: 5.6-6.0 (3.0-3.4) mEq/L; Gr 2: 6.1-6.5 (2.5-2.9) mEq/L; Gr 3: 6.6-7.0 (2.0-2.4) mEq/L; Gr 4: >7.0 (<2.0) mEq/L; sodium, high (low) Gr 1: 146-150 (130-135) mEq/L; Gr 2: 151-154 (125-129) mEq/L; Gr 3: 155-159 (121-124) mEq/L; Gr 4: >=160 (<=120) mEq/L; uric acid Gr 1: 7.5-10.0 mg/dL; Gr 2: 10.1-12.0 mg/dL; Gr 3: 12.1-15.0 mg/dL; Gr 4: >15.0 mg/dL. Baseline within 50 days post screening, prior to start of study medication. (NCT00364793)
Timeframe: Baseline to Week 96

,,,,
Interventionparticipants (Number)
Bicarbonate, low (n=12, 10, 4, 7, 33)Sodium, low (n=12, 10, 4, 7, 33)Sodium High (n=12, 10, 4, 7, 33)Uric Acid (n=12, 10, 4, 7, 33)Calcium High (n= 12, 10, 4, 7, 33)Calcium Low (n= 12, 10, 4, 7, 33)Potassium High (n= 12, 10, 4, 7, 33)Potassium Low (n= 12, 10, 4, 7, 33)Lipase Total (n= 12, 10, 4, 7, 33)
EFV+ddI+FTC in All Participants28153236933
EFV+ddI+FTC in Children >= 2 Years to < 3 Years420101010
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years541011012
EFV+ddI+FTC in Infants >=3 Months to < 6 Months1051000511
EFV+ddI+FTC in Infants >=6 Months to < 2 Years941124400

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Percent of CD4 Cells Change From Baseline at Weeks 24 and 48 - Treated Participants

A CD4 cell is an antigenic marker of helper/inducer T cells. These cells were counted during the hematology cell counts performed during a Complete Blood Cell count (CBC) performed by the Central Laboratory. CD4 are measured as number of cells per millimeter to the third power (cells/mm^3). Percent of CD4 cells is the number of CD4 cells per total number of cells measured*100. An increase in the percent of CD4 cells is an improvement. The Baseline visit was within 50 days after the screening visit and was prior to start of study medication (Week 1). (NCT00364793)
Timeframe: Baseline to Weeks 24 and 48

,,,,
Interventionpercentage of CD4 cells (Median)
Baseline (n=7, 9, 3, 5, 24)Week 24 (n=3, 7, 3, 5, 18)Week 48 (n=5, 8, 2, 5, 20)
EFV+ddI+FTC in All Participants2496
EFV+ddI+FTC in Children >= 2 Years to < 3 Years1298
EFV+ddI+FTC in Children >= 3 Years to <= 6 Years71011
EFV+ddI+FTC in Infants >=3 Months to < 6 Months28145
EFV+ddI+FTC in Infants >=6 Months to < 2 Years2624

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Change From Baseline in CD4 Cell Count at Week 156

Mean change from baseline at Week 156 in CD4 cell count (cells/mm3) (NCT00369941)
Timeframe: Baseline and Week 156

InterventionCD4 Cell Count (cells/mm3) (Mean)
MK-0518 400 mg b.i.d.331.7
Efavirenz 600 mg q.h.s.295.2

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Change From Baseline in CD4 Cell Count at Week 240

Mean change from baseline at Week 240 in CD4 cell count (cells/mm3) (NCT00369941)
Timeframe: Baseline and Week 240

InterventionCD4 Cell Count (cells/mm3) (Mean)
MK-0518 400 mg b.i.d.373.7
Efavirenz 600 mg q.h.s.311.6

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Change From Baseline in CD4 Cell Count at Week 96

Mean change from baseline at Week 96 in CD4 cell count (cells/mm3) (NCT00369941)
Timeframe: Baseline and Week 96

InterventionCD4 Cell Count (cells/mm3) (Mean)
MK-0518 400 mg b.i.d.239.6
Efavirenz 600 mg q.h.s.224.8

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Change From Baseline in Cluster of Differentiation Antigen 4 (CD4) Cell Count at Week 48

Mean change from baseline at Week 48 in CD4 cell count (cells/mm3) (NCT00369941)
Timeframe: Baseline and Week 48

InterventionCD4 Cell Count (cells/mm3) (Mean)
MK-0518 400 mg b.i.d.189.1
Efavirenz 600 mg q.h.s.163.3

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Number of Participants Who Achieved HIV RNA <400 Copies/mL at Week 156

Antiretroviral activity was evaluated for participants who achieved HIV RNA level <400 copies/mL at Week 156. (NCT00369941)
Timeframe: 156 Weeks

InterventionParticipants (Number)
MK-0518 400 mg b.i.d.224
Efavirenz 600 mg q.h.s.203

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Number of Participants Who Achieved HIV RNA <400 Copies/mL at Week 240

Antiretroviral activity was evaluated for participants who achieved HIV RNA level <400 copies/mL at Week 240. (NCT00369941)
Timeframe: 240 Weeks

InterventionParticipants (Number)
MK-0518 400 mg b.i.d.206
Efavirenz 600 mg q.h.s.181

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Number of Participants Who Achieved Human Immunodeficiency Virus (HIV) Ribonucleic Acid (RNA) <50 Copies/mL at Week 48

Antiretroviral activity was evaluated for participants who achieved HIV RNA level <50 copies/mL at Week 48. (NCT00369941)
Timeframe: 48 Weeks

InterventionParticipants (Number)
MK-0518 400 mg b.i.d.241
Efavirenz 600 mg q.h.s.230

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Number of Participants Who Achieved HIV RNA <50 Copies/mL at Week 96

Antiretroviral activity was evaluated for participants who achieved HIV RNA level <50 copies/mL at Week 96. (NCT00369941)
Timeframe: 96 Weeks

InterventionParticipants (Number)
MK-0518 400 mg b.i.d.228
Efavirenz 600 mg q.h.s.222

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Number of Participants Who Achieved HIV RNA <50 Copies/mL at Week 240

Antiretroviral activity was evaluated for participants who achieved HIV RNA level <50 copies/mL at Week 240. (NCT00369941)
Timeframe: 240 Weeks

InterventionParticipants (Number)
MK-0518 400 mg b.i.d.198
Efavirenz 600 mg q.h.s.171

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Number of Participants Who Achieved HIV RNA <50 Copies/mL at Week 156

Antiretroviral activity was evaluated for participants who achieved HIV RNA level <50 copies/mL at Week 156. (NCT00369941)
Timeframe: 156 Weeks

InterventionParticipants (Number)
MK-0518 400 mg b.i.d.212
Efavirenz 600 mg q.h.s.192

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Number of Participants Who Achieved HIV RNA <400 Copies/mL at Week 96

Antiretroviral activity was evaluated for participants who achieved HIV RNA level <400 copies/mL at Week 96. (NCT00369941)
Timeframe: 96 Weeks

InterventionParticipants (Number)
MK-0518 400 mg b.i.d.240
Efavirenz 600 mg q.h.s.229

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Number of Participants Who Achieved HIV RNA <400 Copies/mL at Week 48

Antiretroviral activity was evaluated for participants who achieved HIV RNA level <400 copies/mL at Week 48. (NCT00369941)
Timeframe: 48 Weeks

InterventionParticipants (Number)
MK-0518 400 mg b.i.d.252
Efavirenz 600 mg q.h.s.241

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Number of Participants With Serious LAEs at Week 96

"A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product.~Serious AEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose." (NCT00369941)
Timeframe: 96 Weeks

,
InterventionParticipants (Number)
With Serious LAEsWithout Serious LAEs
Efavirenz 600 mg q.h.s.1281
MK-0518 400 mg b.i.d.0281

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Number of Participants With Serious LAEs at Week 48

"A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product.~Serious AEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose." (NCT00369941)
Timeframe: 48 Weeks

,
InterventionParticipants (Number)
With Serious LAEsWithout Serious LAEs
Efavirenz 600 mg q.h.s.1281
MK-0518 400 mg b.i.d.0281

[back to top]

Number of Participants With Serious LAEs at Week 240

"A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product.~Serious AEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose." (NCT00369941)
Timeframe: 240 Weeks

,
InterventionParticipants (Number)
With Serious LAEsWithout Serious LAEs
Efavirenz 600 mg q.h.s.2280
MK-0518 400 mg b.i.d.0281

[back to top]

Number of Participants With Serious LAEs at Week 156

"A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product.~Serious AEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose." (NCT00369941)
Timeframe: 156 Weeks

,
InterventionParticipants (Number)
With Serious LAEsWithout Serious LAEs
Efavirenz 600 mg q.h.s.2280
MK-0518 400 mg b.i.d.0281

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Number of Participants With Clinical Adverse Experiences (CAEs) at Week 48

An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 48 Weeks

,
InterventionParticipants (Number)
With CAEsWithout CAEs
Efavirenz 600 mg q.h.s.27210
MK-0518 400 mg b.i.d.25328

[back to top]

Number of Participants With CAEs at Week 96

An adverse event (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 96 Weeks

,
InterventionParticipants (Number)
With CAEsWithout CAEs
Efavirenz 600 mg q.h.s.2748
MK-0518 400 mg b.i.d.26516

[back to top]

Number of Participants With CAEs at Week 240

An adverse event (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 240 Weeks

,
InterventionParticipants (Number)
With CAEsWithout CAEs
Efavirenz 600 mg q.h.s.2766
MK-0518 400 mg b.i.d.27110

[back to top]

Number of Participants With CAEs at Week 156

An adverse event (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 156 Weeks

,
InterventionParticipants (Number)
With CAEsWithout CAEs
Efavirenz 600 mg q.h.s.2766
MK-0518 400 mg b.i.d.26714

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Number of Participants That Discontinued With Serious CAEs at Week 96

Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. (NCT00369941)
Timeframe: 96 Weeks

,
InterventionParticipants (Number)
Discontinued With Serious CAEsDid Not Discontinue With Serious CAEs
Efavirenz 600 mg q.h.s.5277
MK-0518 400 mg b.i.d.8273

[back to top]

Number of Participants That Discontinued With Serious CAEs at Week 48

Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. (NCT00369941)
Timeframe: 48 Weeks

,
InterventionParticipants (Number)
Discontinued with Serious CAEsDid Not Discontinue with Serious CAEs
Efavirenz 600 mg q.h.s.4278
MK-0518 400 mg b.i.d.7274

[back to top]

Number of Participants That Discontinued With Serious CAEs at Week 240

Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. (NCT00369941)
Timeframe: 240 Weeks

,
InterventionParticipants (Number)
Discontinued With Serious CAEsDid Not Discontinue With Serious CAEs
Efavirenz 600 mg q.h.s.10272
MK-0518 400 mg b.i.d.11270

[back to top]

Number of Participants That Discontinued With Serious CAEs at Week 156

Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. (NCT00369941)
Timeframe: 156 Weeks

,
InterventionParticipants (Number)
Discontinued With Serious CAEsDid Not Discontinue With Serious CAEs
Efavirenz 600 mg q.h.s.6276
MK-0518 400 mg b.i.d.10271

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Number of Participants That Discontinued With CAEs at Week 96

An adverse event (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 96 Weeks

,
InterventionParticipants (Number)
Discontinued With CAEsDid Not Discontinue With CAEs
Efavirenz 600 mg q.h.s.17265
MK-0518 400 mg b.i.d.10271

[back to top]

Number of Participants That Discontinued With CAEs at Week 48

An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 48 Weeks

,
InterventionParticipants (Number)
Discontinued with CAEsDid Not Discontinue with CAEs
Efavirenz 600 mg q.h.s.17265
MK-0518 400 mg b.i.d.9272

[back to top]

Number of Participants That Discontinued With CAEs at Week 240

An adverse event (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 240 Weeks

,
InterventionParticipants (Number)
Discontinued With CAEsDid Not Discontinue With CAEs
Efavirenz 600 mg q.h.s.25257
MK-0518 400 mg b.i.d.14267

[back to top]

Number of Participants With Serious CAEs at Week 96

Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. (NCT00369941)
Timeframe: 96 Weeks

,
InterventionParticipants (Number)
With Serious CAEsWithout Serious CAEs
Efavirenz 600 mg q.h.s.33249
MK-0518 400 mg b.i.d.37244

[back to top]

Number of Participants With Serious CAEs at Week 48

Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. (NCT00369941)
Timeframe: 48 Weeks

,
InterventionParticipants (Number)
With Serious CAEsWithout Serious CAEs
Efavirenz 600 mg q.h.s.27255
MK-0518 400 mg b.i.d.28253

[back to top]

Number of Participants With Serious CAEs at Week 240

Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. (NCT00369941)
Timeframe: 240 Weeks

,
InterventionParticipants (Number)
With Serious CAEsWithout Serious CAEs
Efavirenz 600 mg q.h.s.57225
MK-0518 400 mg b.i.d.57224

[back to top]

Number of Participants That Discontinued With CAEs at Week 156

An adverse event (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 156 Weeks

,
InterventionParticipants (Number)
Discontinued With CAEsDid Not Discontinue With CAEs
Efavirenz 600 mg q.h.s.21261
MK-0518 400 mg b.i.d.13268

[back to top]

Number of Participants That Died by Week 96

All participant deaths in the span of 96 weeks on study were recorded. (NCT00369941)
Timeframe: 96 Weeks

,
InterventionParticipants (Number)
DiedDid Not Die
Efavirenz 600 mg q.h.s.0282
MK-0518 400 mg b.i.d.3278

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Number of Participants That Died by Week 48

All participant deaths in the span of 48 weeks on study were recorded. (NCT00369941)
Timeframe: 48 Weeks

,
InterventionParticipants (Number)
DiedDid Not Die
Efavirenz 600 mg q.h.s.0282
MK-0518 400 mg b.i.d.2279

[back to top]

Number of Participants That Died by Week 240

All participant deaths in the span of 240 weeks on study were recorded. (NCT00369941)
Timeframe: 240 Weeks

,
InterventionParticipants (Number)
DiedDid Not Die
Efavirenz 600 mg q.h.s.5277
MK-0518 400 mg b.i.d.5276

[back to top]

Number of Participants That Died by Week 156

All participant deaths in the span of 156 weeks on study were recorded. (NCT00369941)
Timeframe: 156 Weeks

,
InterventionParticipants (Number)
DiedDid Not Die
Efavirenz 600 mg q.h.s.1281
MK-0518 400 mg b.i.d.4277

[back to top]

Number of Participants Discontinued With LAEs at Week 96

A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 96 Weeks

,
InterventionParticipants (Number)
Discontinued With LAEsDid Not Discontinue With LAEs
Efavirenz 600 mg q.h.s.2280
MK-0518 400 mg b.i.d.0281

[back to top]

Number of Participants With Serious CAEs at Week 156

Serious CAEs are any AEs occurring at any dose that: results in death; or is life threatening; or results in a persistent or significant disability/incapacity; or results in or prolongs an existing inpatient hospitalization; or is a congenital anomaly/birth defect; or is a cancer; or is an overdose. (NCT00369941)
Timeframe: 156 Weeks

,
InterventionParticipants (Number)
With Serious CAEsWithout Serious CAEs
Efavirenz 600 mg q.h.s.46236
MK-0518 400 mg b.i.d.46235

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Number of Participants With Nervous System Symptoms Assessed by Review of Accumulated Safety Data up to Week 8

Participants with dizziness, insomnia, somnolence, concentration impaired, depression, nightmare, confusional state, suicidal ideation, nervous system disorder, psychotic disorder, abnormal dreams, suicide attempt, acute psychosis, delirium, depressed level of consciousness, hallucination, auditory hallucination, completed suicide, and major depression (NCT00369941)
Timeframe: 8 Weeks

,
InterventionParticipants (Number)
With Nervous System SymptomsWithout Nervous System Symptoms
Efavirenz 600 mg q.h.s.147135
MK-0518 400 mg b.i.d.57224

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Number of Participants With LAEs at Week 96

A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 96 Weeks

,
InterventionParticipants (Number)
With LAEsWithout LAEs
Efavirenz 600 mg q.h.s.53229
MK-0518 400 mg b.i.d.33248

[back to top]

Number of Participants With LAEs at Week 240

A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 240 Weeks

,
InterventionParticipants (Number)
With LAEsWithout LAEs
Efavirenz 600 mg q.h.s.77205
MK-0518 400 mg b.i.d.56225

[back to top]

Number of Participants With LAEs at Week 156

A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 156 Weeks

,
InterventionParticipants (Number)
With LAEsWithout LAEs
Efavirenz 600 mg q.h.s.63219
MK-0518 400 mg b.i.d.41240

[back to top]

Number of Participants With Laboratory Adverse Experiences (LAEs) at Week 48

A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 48 Weeks

,
InterventionParticipants (Number)
With LAEsWithout LAEs
Efavirenz 600 mg q.h.s.41241
MK-0518 400 mg b.i.d.27254

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Number of Participants Discontinued With LAEs at Week 48

A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 48 Weeks

,
InterventionParticipants (Number)
Discontinued with LAEsDid Not Discontinue with LAEs
Efavirenz 600 mg q.h.s.1281
MK-0518 400 mg b.i.d.0281

[back to top]

Number of Participants Discontinued With LAEs at Week 240

A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 240 Weeks

,
InterventionParticipants (Number)
Discontinued With LAEsDid Not Discontinue With LAEs
Efavirenz 600 mg q.h.s.3279
MK-0518 400 mg b.i.d.0281

[back to top]

Number of Participants Discontinued With LAEs at Week 156

A laboratory AE is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the study product, whether or not considered related to the use of the product. (NCT00369941)
Timeframe: 156 Weeks

,
InterventionParticipants (Number)
Discontinued With LAEsDid Not Discontinue With LAEs
Efavirenz 600 mg q.h.s.3279
MK-0518 400 mg b.i.d.0281

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Incidence of Severe Adverse Events (Excluding Mortality)

(NCT00427297)
Timeframe: 2 years

Interventionevent (Number)
NVP-containing21
NVP-sparing6

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Viral Failure

Virologic treatment failure was defined as follow-up (at least 24 weeks after enrollment date) viral load > 400 copies. (NCT00427297)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
NVP-containing2
NVP-sparing2

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Incidence of Mortality

Death during follow-up (NCT00427297)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
NVP-containing4
NVP-sparing5

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Immunologic Failure

Immunologic treatment failure was defined as CD4% dropping below 15%, after a previous result greater than or equal to 15% (following along WHO Guidelines). (NCT00427297)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
NVP-containing2
NVP-sparing1

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Late Change in CD4 Count From Baseline

Change in CD4+ lymphocyte counts between week 48 study visit and baseline. (NCT00442962)
Timeframe: At week 48

Interventioncells/mm^3 (Mean)
EFV + FTC/TDF194

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Time to Initial Virological Failure

Virologic failure defined as two consecutive measurements of plasma HIV-1 RNA at least 400 copies/mL at or after the week 16 study visit. Time measured from enrollment. (NCT00442962)
Timeframe: Throughout study

Interventionweeks (Number)
5th percentile10th percentile15th percentile
EFV + FTC/TDF161624

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Time to Loss of Virologic Response by Week 48 (Defined by FDA TLOVR Algorithm)

(NCT00442962)
Timeframe: Throughout study

Interventionweeks (Number)
10th percentile15th percentile20th percentile
EFV + FTC/TDF162424

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Time to Initial Virologic Response

Time from enrollment to scheduled week of first plasma HIV-1 RNA viral load fewer than 400 copies/mL. (NCT00442962)
Timeframe: Throughout study

Interventionweeks (Number)
50th percentile75th percentile95th percentile
EFV + FTC/TDF2824

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Time to First Safety Event

Time from starting study treatment to first grade 3 or 4 sign/symptom or laboratory abnormality and at least one grade higher than baseline. Grading used the Division of AIDS (DAIDS) 2004 Severity of Adverse Events Tables. (NCT00442962)
Timeframe: Throughout study

Interventionweeks (Number)
5th percentile10th percentile15th percentile
EFV + FTC/TDF4.124.433.1

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Time to First Dose Modification

Time from starting study treatment to first dose/drug modification. (NCT00442962)
Timeframe: Throughout study

Interventionweeks (Number)
10th percentile15th percentile20th percentile
EFV + FTC/TDF1.924.925.7

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Early Changes in CD4 Count From Baseline

Changes in CD4+ lymphocyte counts between study visit weeks 4, 8 16 and 24 and baseline. (NCT00442962)
Timeframe: At weeks 0(baseline), 4, 8, 16, 24

Interventioncells/mm^3 (Mean)
Change from baseline to week 4Change from baseline to week 8Change from baseline to week 16Change from baseline to week 24
EFV + FTC/TDF105118138147

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Percentage of Participants With Late Virologic Response

Plasma HIV-1 Viral Load Fewer Than 400 Copies/ml (NCT00442962)
Timeframe: At Week 48

Interventionpercentage (Number)
EFV + FTC/TDF80.43

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Percentage of Participants With Early Virologic Suppression

Plasma HIV-1 Viral Load Fewer Than 50 Copies/ml (NCT00442962)
Timeframe: At Weeks 24

Interventionpercentage of participants (Number)
EFV + FTC/TDF72.0

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Percentage of Participants With Early Virologic Response

Plasma HIV-1 Viral Load Fewer Than 400 Copies/ml (NCT00442962)
Timeframe: At Week 24

Interventionpercentage of participants (Number)
EFV + FTC/TDF80.8

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Percentage of Participants With Late Virologic Suppression

Plasma HIV-1 Viral Load Fewer Than 50 Copies/ml (NCT00442962)
Timeframe: At Week 48

Interventionpercentage (Number)
EFV + FTC/TDF70.5

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Effect of Drug Regimens on Serum Triglycerides.

(NCT00457665)
Timeframe: 12 and 24 months

,
Interventionmg/dL (Mean)
At 12 monthsAt 24 months
Efavirenz (Sustiva)230.4290.0
Nelfinavir (Viracept)228.0293.4

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The Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies/ml) at Week 96

(NCT00540449)
Timeframe: Week 96

,
InterventionParticipants (Number)
Virologic Response, <50 copies/mlVirologic failureNo viral load data in the 96 week window
Efavirenz2682749
TMC2782655427

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The Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies/ml) at Week 48

The analysis is based on the last observed viral load (VL) data within the Week 48 window. Virologic response is defined as a VL<50 copies/ml (observed case). Missing VL was considered as non-response. Virologic Failure includes subjects who had VL>=50 copies/ml in the Wk48 window, subjects who discontinued early due to lack or loss of efficacy, subjects who discontinued for reasons other than an adverse event, death or lack or loss of efficacy and at the time of discontinuation had a VL>=50 copies/ml and subjects who had a switch in background regimen that was not permitted by the protocol. (NCT00540449)
Timeframe: Week 48

,
InterventionParticipants (Number)
Virologic Response HIV RNA <50 copies/mL at Wk 48Virologic FailureNo Viral Load Data in 48 week window
Efavirenz2812439
TMC2782854714

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Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies/ml) at Week 96

(NCT00540449)
Timeframe: Week 96

,
InterventionParticipants (Number)
ResponderVirologic failureDeathDiscontinued due to AEDiscontinued due to other reason than AE
Efavirenz2711632925
TMC2782634501028

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Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies/ml) at Week 48

Virological response is defined as confirmed plasma viral load less than (<) 50 human immunodeficiency virus-1 (HIV-1) (ribonucleic acid [RNA]) copies/milliliter (ml) at Week 48. The TLOVR algorithm was used to derive response. Response needed to be confirmed at 2 consecutive visits and participants who permanently discontinued were considered nonresponders after discontinuation. Resuppression after confirmed virologic failure was considered as failure. Virologic Failure includes participants who were rebounder (confirmed viral load >= 50 copies/ml after being responder) or who were never suppressed (no confirmed viral load <50 copies/ml). (NCT00540449)
Timeframe: Week 48

,
InterventionParticipants (Number)
ResponderVirologic failureDiscontinued due to Adverse Event (AE)Discontinued due to other reason than AE
Efavirenz285152519
TMC27828738615

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Number of Participants With Virologic Failure for the Resistance Determination by Emerging Resistance Associated Mutations: First Available On-Treatment Genotypic Data After Failure

Virologic failure for the resistance determinations was defined as lack of virologic response (never having had 2 consecutive plasma viral load <50 copies/mL) and plasma viral load increase of >=0.5 log 10 copies/mL above nadir (i.e., never suppressed), or confirmed loss of virologic response (2 consecutive plasma viral load >=50 copies/mL after having had 2 consecutive plasma viral load <50 copies/mL; i.e., rebounder), or discontinued with a last observed on-treatment plasma viral load >=50 copies/mL after having had 2 consecutive plasma viral load <50 copies/mL. For this study, treatment-emergent reverse transcriptase (RT) resistance associated mutations (RAMs) occurring in at least 2 virologic failures (for at least one treatment group) for the following lists are presented: i) Extended list of Non-nucleoside reverse transcriptase inhibitor (NNRTI RAMs) ii) IAS-USA list of Nucleoside/tide reverse transcriptase inhibitor (N[t]RTI RAMs). (NCT00540449)
Timeframe: Week 96

,
InterventionParticipants (Number)
Any RAM from Extended NNRTI RAMs listNNRTI RAM: E138KNNRTI RAM: K101ENNRTI RAM: Y181CNNRTI RAM: V90INNRTI RAM: V189INNRTI RAM: H221YNNRTI RAM: E138QNNRTI RAM: K103NAny RAM from IAS-USA N(t)RTI RAMs listN(t)RTI RAM: M184IN(t)RTI RAM: M184VN(t)RTI RAM: K065RN(t)RTI RAM: K219EN(t)RTI RAM: Y115F
Efavirenz900000008533000
TMC2782918554443131247332

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Mean Change From Baseline to Week 48 and Week 96 in Absolute and Relative CD4+ Cell Counts (Using Imputed Data)

Change from baseline in CD4+ cell count was imputed in case of missing values: in case of premature discontinuation, data were imputed with the baseline value after discontinuation (i.e. change=0, Non-Completer [NC] = Failure); otherwise last observation carried forward was applied. (NCT00540449)
Timeframe: Baseline, Week 48, and Week 96

,
Interventioncells per microliter (Mean)
Absolute cell count, Week 48Absolute cell count, Week 96Relative cell count, Week 48Relative cell count, Week 96
Efavirenz181.6226.78.710.2
TMC278195.5220.78.610.1

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Number of Participants With Virological Response (Observed, <50 Copies/ml) at Last On-Treatment Visit (Post-Week 96).

Virological response is defined as (observed) plasma viral load less than 50 human immunodeficiency virus-type 1 (HIV-1) ribonucleic acid (RNA) copies per ml at the last on-treatment visit (post-Week 96). (NCT00540449)
Timeframe: Variable, ranging from 3 months up to maximum 15 months for TMC278 and 12 months for Efavirenz after the 96-week visit

InterventionParticipants (Number)
TMC278245
Efavirenz261

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Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies/ml) at Week 96

(NCT00540449)
Timeframe: Week 96

InterventionParticipants (Number)
TMC278273
Efavirenz278

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Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies/ml) at Week 48

(NCT00540449)
Timeframe: Week 48

InterventionParticipants (Number)
TMC278297
Efavirenz293

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Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies Per mL) at Week 96

(NCT00543725)
Timeframe: Week 96

,
InterventionParticipants (Number)
ResponderVirologic failureDeathDiscontinued due to AEDiscontinued due to other reason than AE
Efavirenz2582432330
TMC2782693411620

[back to top]

Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies Per mL) at Week 48

Virological response is defined as confirmed plasma viral load less than (<) 50 human immunodeficiency virus-1 (HIV-1) (ribonucleic acid [RNA]) copies/milliliter (ml) at Week 48. The TLOVR algorithm was used to derive response. Response needed to be confirmed at 2 consecutive visits and participants who permanently discontinued were considered nonresponders after discontinuation. Resuppression after confirmed virologic failure was considered as failure. Virologic Failure includes participants who were rebounder (confirmed viral load >= 50 copies/ml after being responder) or who were never suppressed (no confirmed viral load <50 copies/ml). (NCT00543725)
Timeframe: Week 48

,
InterventionParticipants (Number)
ResponderVirologic failureDeathDiscontinued due to AEDiscontinued due to other reason than AE
Efavirenz2761832120
TMC278291241816

[back to top]

Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies Per mL) at Week 96

(NCT00543725)
Timeframe: Week 96

,
InterventionParticipants (Number)
Virologic response (<50 copies/mL)Virologic failureNo plasma viral load data in 96-Week window
Efavirenz2543846
TMC2782595328

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Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies Per mL) at Week 48

The analysis is based on the last observed viral load (VL) data within the Week 48 window. Virologic response is defined as a VL<50 copies/mL (observed case). Missing VL was considered as non-response. Virologic Failure includes subjects who had VL>=50 copies/mL in the Wk 48 window, subjects who discontinued early due to lack or loss of efficacy, subjects who discontinued for reasons other than an adverse event, death or lack or loss of efficacy and at the time of discontinuation had a VL>=50 copies/mL and subjects who had a switch in background regimen that was not permitted by the protocol. (NCT00543725)
Timeframe: Week 48

,
InterventionParticipants (Number)
Virologic Response (<50 copies/mL)Virologic failureNo plasma viral load data in 48-week window
Efavirenz2653835
TMC2782814118

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Number of Participants With Virologic Failure for the Resistance Determinations by Developing Mutations: First Available On-Treatment Genotypic Data After Failure

Virologic failure for the resistance determinations was defined as lack of virologic response (never having had 2 consecutive plasma viral load <50 copies/mL) and plasma viral load increase of >=0.5 log 10 copies/mL above nadir (i.e., never suppressed), or confirmed loss of virologic response (2 consecutive plasma viral load >=50 copies/mL after having had 2 consecutive plasma viral load <50 copies/mL; i.e., rebounder), or discontinued with a last observed on-treatment plasma viral load >=50 copies/mL after having had 2 consecutive plasma viral load <50 copies/mL. For this study, treatment-emergent reverse transcriptase (RT) resistance associated mutations (RAMs) occurring in at least 2 virologic failures (for at least one treatment group) for the following lists are presented: i) Extended list of Non-nucleoside reverse transcriptase inhibitor (NNRTI RAMs) ii) IAS-USA list of Nucleoside/tide reverse transcriptase inhibitor (N[t]RTI RAMs). (NCT00543725)
Timeframe: Week 96

,
InterventionParticipants (Number)
Treatment-emergent NNRTI RAME138KH221YK101EK103NV90IV106MV189IY188CTreatment-emergent N(t)RTI RAMK65RK219EM184IM184V
Efavirenz111026120262013
TMC278171333020201702810

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Mean Change From Baseline to Week 48 and Week 96 in Absolute and Relative CD4+ Cell Counts (Using Imputed Data)

Change from baseline in CD4+ cell count was imputed in case of missing values: in case of premature discontinuation, data were imputed with the baseline value after discontinuation (i.e. change=0, Non-Completer [NC] = Failure); otherwise last observation carried forward was applied. (NCT00543725)
Timeframe: Baseline, Week 48, and Week 96

,
Interventioncells per microliter (Mean)
Absolute cell count, Week 48Absolute cell count, Week 96Relative cell count, Week 48Relative cell count, Week 96
Efavirenz170.7212.08.09.7
TMC278188.6234.58.310.1

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Number of Participants With Virological Response (Observed, <50 Copies/mL) at Last On-Treatment Visit (Post-Week 96).

Virological response is defined as (observed) plasma viral load less than 50 human immunodeficiency virus-type 1 (HIV-1) ribonucleic acid (RNA) copies per mL at the last on-treatment post-Week 96 visit. (NCT00543725)
Timeframe: Variable, ranging from 3 months up to maximum 18 months for TMC278 and 12 months for Efavirenz

InterventionParticipants (Number)
TMC278260
Efavirenz246

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Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies Per mL) at Week 96

Virological response is defined as confirmed plasma viral load < 400 HIV-1 (RNA) copies/mL at Week 96. The TLOVR algorithm was used to derive response. Response needed to be confirmed at 2 consecutive visits and participants who permanently discontinued were considered nonresponders after discontinuation. Resuppression after confirmed virologic failure was considered as failure. Virologic Failure includes participants who were rebounder (confirmed viral load >= 400 copies/mL after being responder) or who were never suppressed (no confirmed viral load <400 copies/mL). (NCT00543725)
Timeframe: Week 96

InterventionParticipants (Number)
TMC278283
Efavirenz270

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Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies Per mL) at Week 48

Virological response is defined as confirmed plasma viral load < 400 HIV-1 (RNA) copies/mL at Week 48. The TLOVR algorithm was used to derive response. Response needed to be confirmed at 2 consecutive visits and participants who permanently discontinued were considered nonresponders after discontinuation. Resuppression after confirmed virologic failure was considered as failure. Virologic Failure includes participants who were rebounder (confirmed viral load >= 400 copies/mL after being responder) or who were never suppressed (no confirmed viral load <400 copies/mL). (NCT00543725)
Timeframe: Week 48

InterventionParticipants (Number)
TMC278300
Efavirenz286

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Mean Change From Baseline in Estimated Glomerular Filtration Rate (GFR), Calculated by Modification of Diet in Renal Disease (MDRD) Equation, at Week 96

Change from baseline was calculated as the Week 96 value minus the baseline value. GFR is a measure of the rate at which blood is filtered by the kidney. MDRD is an equation (calculation) used to estimate GFR in participants with impaired renal function based on serum creatinine, age, race, and gender. GFR (mL/min/1.73 m^2) = 175 * (Scr)^-1.154 * (Age)^-0.203 * (0.742 if female) * (1.212 if African American) (conventional units). mL, milliliters; min, minute; m^s, meters squared; Scr, serum creatinine. (NCT00549198)
Timeframe: Baseline, Week 96

InterventionmL/min/1.73m^2 (Mean)
ABC/3TC FDC1.48
TDF/FTC FDC-1.15

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Mean Change From Baseline in Estimated Glomerular Filtration Rate (GFR), Calculated by Modification of Diet in Renal Disease (MDRD) Equation, at Week 48

Change from baseline was calculated as the Week 48 value minus the baseline value. GFR is a measure of the rate at which blood is filtered by the kidney. MDRD is an equation (calculation) used to estimate GFR in participants with impaired renal function based on serum creatinine, age, race, and gender. GFR (mL/min/1.73 m^2) = 175 * (Scr)^-1.154 * (Age)^-0.203 * (0.742 if female) * (1.212 if African American) (conventional units). mL, milliliters; min, minute; m^2, meters squared; Scr, serum creatinine; BMI, body mass index. (NCT00549198)
Timeframe: Baseline, Week 48

Interventionmilliliters per minute (mL/min)/1.73 m^2 (Mean)
ABC/3TC FDC0.22
TDF/FTC FDC1.18

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Mean Change From Baseline in Estimated Glomerular Filtration Rate (GFR), Calculated by Modification of Diet in Renal Disease (MDRD) Equation, at Week 24

Change from baseline was calculated as the Week 24 value minus the baseline value. GFR is a measure of the rate at which blood is filtered by the kidney. MDRD is an equation (calculation) used to estimate GFR in participants with impaired renal function based on serum creatinine, age, race, and gender. GFR (mL/min/1.73 m^2) = 175 * (Scr)^-1.154 * (Age)^-0.203 * (0.742 if female) * (1.212 if African American) (conventional units). mL, milliliters; min, minute; m^2, meters squared; Scr, serum creatinine. (NCT00549198)
Timeframe: Baseline, Week 24

InterventionmL/min/1.73m^2 (Mean)
ABC/3TC FDC2.78
TDF/FTC FDC0.43

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Mean Change From Baseline in Estimated GFR, Calculated by Cockcroft-Gault Equation, at Week 96

Change from baseline was calculated as the Week 96 value minus the baseline value. Cockcroft-Gault is an equation (calculation) used to estimate GFR based on serum creatinine, weight, and gender. GFR = (140 - age) * (mass in kg) * (0.85 if female) divided by 72 * serum creatinine in mg/dL. mg, milligram; dL, deciliter; kg, kilogram. (NCT00549198)
Timeframe: Baseline, Week 96

InterventionmL/min (Mean)
ABC/3TC FDC4.37
TDF/FTC FDC2.68

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Mean Change From Baseline in Estimated GFR, Calculated by Cockcroft-Gault Equation, at Week 48

Change from baseline was calculated as the Week 48 value minus the baseline value. Cockcroft-Gault is an equation (calculation) used to estimate GFR based on serum creatinine, weight, and gender. GFR = (140 - age) * (mass in kg) * (0.85 if female) divided by 72 * serum creatinine in mg/dL. mg, milligram; dL, deciliter; kg, kilogram. (NCT00549198)
Timeframe: Baseline, Week 48

InterventionmL/min (Mean)
ABC/3TC FDC2.66
TDF/FTC FDC3.80

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Number of Participants With National Kidney Foundation Chronic Kidney Disease Stage 1, 2, 3, 4, or 5 Categories of Renal Function at Week 24

Normal: GFR >=60 mL/min/1.73 m^2 and creatinine ratio <=200 mg/g GFR; Stage 1: GFR >=90 mL/min/1.73 m^2 and creatinine ratio >200 mg/g; Stage 2: GFR >=60-<90 mL/min/1.73 m^2 and creatinine ratio >200 mg/g; Stage 3: GFR >=30-<60 mL/min/1.73 m^2; Stage 4: GFR >=15-<30 mL/min/1.73 m^2; Stage 5: GFR <15 mL/min/1.73 m^2. mL, milliliter; min, minute; m^2, meters squared; mg, milligram; g, gram. (NCT00549198)
Timeframe: Baseline, Week 24

,
Interventionparticipants (Number)
NormalStage 1Stage 2Stage 3Stage 4Stage 5
ABC/3TC FDC97115100
TDF/FTC FDC114155100

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Change From Baseline in Cluster Difference 4 (CD4+) Cell Count at Week 24

CD4+ counts are used to monitor the progression of HIV disease and the strength of the immune system. The number of CD4+ cells decreases as HIV disease progresses. Cell counts were measured from participant blood samples taken throughout the study. (NCT00549198)
Timeframe: Baseline, Week 24

Interventioncells/millimeters cubed (mm^3) (Median)
ABC/3TC FDC110.0
TDF/FTC FDC100.0

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Change From Baseline in Cluster Difference 4 (CD4+) Cell Count at Week 48

CD4+ counts are used to monitor the progression of HIV disease and the strength of the immune system. The number of CD4+ cells decreases as HIV disease progresses. Cell counts were measured from participant blood samples taken throughout the study. (NCT00549198)
Timeframe: Baseline, Week 48

Interventioncells/mm^3 (Median)
ABC/3TC FDC150.0
TDF/FTC FDC150.0

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Change From Baseline in Cluster Difference 4 (CD4+) Cell Count at Week 96

CD4+ counts are used to monitor the progression of HIV disease and the strength of the immune system. The number of CD4+ cells decreases as HIV disease progresses. Cell counts were measured from participant blood samples taken throughout the study. (NCT00549198)
Timeframe: Baseline, Week 96

Interventioncells/mm^3 (Median)
ABC/3TC FDC235.0
TDF/FTC FDC220.0

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Exploratory Analysis of Change From Baseline in Albumin as a Ratio to Urine Creatinine at Week 96

Renal biomarkers were analyzed using urine samples collected from participants at baseline and Week 96. Renal biomarkers may be an indicator of various aspects of kidney function. The ratio was calculated by dividing the change from baseline albumin value by the urine creatinine value. Albumin is measured in milligrams per millimole (mg/mmol). (NCT00549198)
Timeframe: Baseline, Week 96

Interventionratio (Geometric Mean)
ABC/3TC FDC0.872
TDF/FTC FDC0.973

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Exploratory Analysis of Change From Baseline in Beta 2 Microglobulin (B2M) as a Ratio to Urine Creatinine at Week 96

Renal biomarkers were analyzed using urine samples collected from participants at baseline and Week 96. Renal biomarkers may be an indicator of various aspects of kidney function. The ratio was calculated by dividing the change from baseline B2M value by the urine creatinine value. B2M, beta 2 microglobulin (measured in mg/mmol). (NCT00549198)
Timeframe: Baseline, Week 96

Interventionratio (Geometric Mean)
ABC/3TC FDC0.542
TDF/FTC FDC0.984

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Exploratory Analysis of Change From Baseline in Bone Specific Alkaline Phosphatase (BSAP) at Week 96

Bone biomarkers were analyzed using blood samples collected from participants at baseline and Week 96. Bone biomarkers may be an indicator of bone turnover. (NCT00549198)
Timeframe: Baseline, Week 96

Interventionug/L (Geometric Mean)
ABC/3TC FDC1.111
TDF/FTC FDC2.542

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Exploratory Analysis of Change From Baseline in N-acetyl-B-glucosaminidase (NAG) as a Ratio to Urine Creatinine at Week 96

Renal biomarkers were analyzed using urine samples collected from participants at baseline and Week 96. Renal biomarkers may be an indicator of various aspects of kidney function. The ratio was calculated by dividing the change from baseline NAG value by the urine creatinine value. NAG, N-acetyl-B-glucosaminidase (measured in micromoles per hour per millimole [umol/h/mmol]). (NCT00549198)
Timeframe: Baseline, Week 96

Interventionratio (Geometric Mean)
ABC/3TC FDC0.868
TDF/FTC FDC0.939

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Exploratory Analysis of Change From Baseline in Osteocalcin at Week 96

Bone biomarkers were analyzed using blood samples collected from participants at baseline and Week 96. Bone biomarkers may be an indicator of bone turnover. (NCT00549198)
Timeframe: Baseline, Week 96

Interventionug/L (Geometric Mean)
ABC/3TC FDC3.01
TDF/FTC FDC5.79

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Exploratory Analysis of Change From Baseline in Procollagen Type 1 Amino-terminal Propeptide (P1NP) at Week 96

P1NP is a bone biomarker that was analyzed using blood samples collected from participants at baseline and Week 96. Bone biomarkers may be an indicator of bone turnover. (NCT00549198)
Timeframe: Baseline, Week 96

Interventionmicrograms per Liter (ug/L) (Geometric Mean)
ABC/3TC FDC1.2
TDF/FTC FDC1.4

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Exploratory Analysis of Change From Baseline in Retinol Binding Protein (RBP) as a Ratio to Urine Creatinine at Week 96

Renal biomarkers were analyzed using urine samples collected from participants at baseline and Week 96. Renal biomarkers may be an indicator of various aspects of kidney function. The ratio was calculated by dividing the change from baseline RBP value by the urine creatinine value. RBP, retinol binding protein (measured in micrograms per millimole [ug/mmol]). (NCT00549198)
Timeframe: Baseline, Week 96

Interventionratio (Geometric Mean)
ABC/3TC FDC1.099
TDF/FTC FDC1.550

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Exploratory Analysis of Change From Baseline in Type 1 Collagen Cross-linked C-telopeptide at Week 96

Bone biomarkers were analyzed using blood samples collected from participants at baseline and Week 96. Bone biomarkers may be an indicator of bone turnover. (NCT00549198)
Timeframe: Baseline, Week 96

Interventionnanograms per Liter (ng/L) (Geometric Mean)
ABC/3TC FDC89.9
TDF/FTC FDC203.6

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Mean Change From Baseline in Estimated GFR, Calculated by Cockcroft-Gault Equation, at Week 24

Change from baseline was calculated as the Week 24 value minus the baseline value. Cockcroft-Gault is an equation (calculation) used to estimate GFR based on serum creatinine, weight, and gender. GFR = (140 - age) * (mass in kg) * (0.85 if female) divided by 72 * serum creatinine in mg/dL. mg, milligram; dL, deciliter; kg, kilogram; CG, Cockcroft-Gault. (NCT00549198)
Timeframe: Baseline, Week 24

InterventionmL/min (Mean)
ABC/3TC FDC4.27
TDF/FTC FDC2.54

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Number of Participants With HIV-1 RNA <50 Copies/Milliliter (c/mL) and 400 c/mL at Week 48

HIV-1 RNA level (viral load) is a strong predictor of the rate of HIV disease progression. It was measured from plasma (participant blood samples) taken at all visits throughout the study. HIV, human immunodeficiency virus; RNA, ribonucleic acid. Viral load is a measure of the severity of the HIV infection. (NCT00549198)
Timeframe: Week 48

,
Interventionparticipants (Number)
<50 copies/mL<400 copies/mL
ABC/3TC FDC121130
TDF/FTC FDC145151

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Number of Participants With HIV-1 RNA <50 Copies/Milliliter (c/mL) and 400 c/mL at Week 96

HIV-1 RNA level (viral load) is a strong predictor of the rate of HIV disease progression. It was measured from plasma (participant blood samples) taken at all visits throughout the study. HIV, human immunodeficiency virus; RNA, ribonucleic acid. Viral load is a measure of the severity of the HIV infection. (NCT00549198)
Timeframe: Week 96

,
Interventionparticipants (Number)
<50 copies/mL<400 copies/mL
ABC/3TC FDC98110
TDF/FTC FDC113126

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Number of Participants With National Kidney Foundation Chronic Kidney Disease Stage 1, 2, 3, 4, or 5 Categories of Renal Function at Week 48

Normal: GFR >=60 mL/min/1.73 m^2 and creatinine ratio <=200 mg/g GFR; Stage 1: GFR >=90 mL/min/1.73 m^2 and creatinine ratio >200 mg/g; Stage 2: GFR >=60-<90 mL/min/1.73 m^2 and creatinine ratio >200 mg/g; Stage 3: GFR >=30-<60 mL/min/1.73 m^2; Stage 4: GFR >=15-<30 mL/min/1.73 m^2; Stage 5: GFR <15 mL/min/1.73 m^2. mL, milliliter; min, minute; m^2, meters squared; mg, milligram; g, gram. (NCT00549198)
Timeframe: Baseline, Week 48

,
Interventionparticipants (Number)
MissingNormalStage 1Stage 2Stage 3Stage 4Stage 5
ABC/3TC FDC129073000
TDF/FTC FDC1910653000

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Number of Participants With National Kidney Foundation Chronic Kidney Disease Stage 1, 2, 3, 4, or 5 Categories of Renal Function at Week 96

Normal: GFR >=60 mL/min/1.73 m^2 and creatinine ratio <=200 mg/g GFR; Stage 1: GFR >=90 mL/min/1.73 m^2 and creatinine ratio >200 mg/g; Stage 2: GFR >=60-<90 mL/min/1.73 m^2 and creatinine ratio >200 mg/g; Stage 3: GFR >=30-<60 mL/min/1.73 m^2; Stage 4: GFR >=15-<30 mL/min/1.73 m^2; Stage 5: GFR <15 mL/min/1.73 m^2. mL, milliliter; min, minute; m^2, meters squared; mg, milligram; g, gram. (NCT00549198)
Timeframe: Baseline, Week 96

,
Interventionparticipants (Number)
MissingNormalStage 1Stage 2Stage 3Stage 4Stage 5
ABC/3TC FDC117534000
TDF/FTC FDC188344000

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting High-density Lipoprotein (HDL) at Week 24

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <40 mg/dL, low; 40-<60 mg/dL, normal; >=60 mg/dL, high. (NCT00549198)
Timeframe: Baseline, Week 24

,
Interventionparticipants (Number)
Low to lowLow to normalLow to highNormal to lowNormal to normalNormal to highHigh to lowHigh to normalHigh to high
ABC/3TC FDC197210012260010
TDF/FTC FDC3666913012035

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting High-density Lipoprotein (HDL) at Week 96

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <40 mg/dL, low; 40-<60 mg/dL, normal; >=60 mg/dL, high. (NCT00549198)
Timeframe: Baseline, Week 96

,
Interventionparticipants (Number)
Low to lowLow to normalLow to highNormal to lowNormal to normalNormal to highHigh to lowHigh to normalHigh to high
ABC/3TC FDC11662508300010
TDF/FTC FDC23751301727017

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Total Cholesterol at Week 24

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <200 mg/dL, desirable; 200-<240 mg/dL, borderline high; >=240 mg/dL, high. mg, milligram; dL, deciliter. (NCT00549198)
Timeframe: Baseline, Week 24

,
Interventionparticipants (Number)
Desirable to desirableDesirable to borderline highDesirable to highBorderline high to desirableBorderline high to borderline highBorderline high to highHigh to desirableHigh to borderline highHigh to high
ABC/3TC FDC5447321210003
TDF/FTC FDC104299396002

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Total Cholesterol at Week 48

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <200 mg/dL, desirable; 200-<240 mg/dL, borderline high; >=240 mg/dL, high. mg, milligram; dL, deciliter. (NCT00549198)
Timeframe: Baseline, Week 48

,
Interventionparticipants (Number)
Desirable to desirableDesirable to borderline highDesirable to highBorderline high to desirableBorderline high to borderline highBorderline high to highHigh to desirableHigh to borderline highHigh to high
ABC/3TC FDC4652361210003
TDF/FTC FDC96379198002

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Total Cholesterol at Week 96

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <200 mg/dL, desirable; 200-<240 mg/dL, borderline high; >=240 mg/dL, high. mg, milligram; dL, deciliter. (NCT00549198)
Timeframe: Baseline, Week 96

,
Interventionparticipants (Number)
Desirable to desirableDesirable to borderline highDesirable to highBorderline high to desirableBorderline high to borderline highBorderline high to highHigh to desirableHigh to borderline highHigh to high
ABC/3TC FDC3949461210003
TDF/FTC FDC864710198002

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Triglycerides at Week 24

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <150 mg/dL, normal; 150-<200 mg/dL, borderline high; 200-<500 mg/dL, high; >=500 mg/dL, very high. (NCT00549198)
Timeframe: Baseline, Week 24

,
Interventionparticipants (Number)
Normal to normalNormal to borderline highNormal to highNormal to very highBorderline high to normalBorderline high to borderline highBorderline high to highBorderline high to very highHigh to normalHigh to borderline highHigh to highHigh to very highVery high to normalVery high to borderline highVery high to highVery high to very high
ABC/3TC FDC63212305590251230001
TDF/FTC FDC781990710150631500010

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Triglycerides at Week 48

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <150 mg/dL, normal; 150-<200 mg/dL, borderline high; 200-<500 mg/dL, high; >=500 mg/dL, very high. (NCT00549198)
Timeframe: Baseline, Week 48

,
Interventionparticipants (Number)
Normal to normalNormal to borderline highNormal to highNormal to very highBorderline high to normalBorderline high to borderline highBorderline high to highBorderline high to very highHigh to normalHigh to borderline highHigh to highHigh to very highVery high to normalVery high to borderline highVery high to highVery high to very high
ABC/3TC FDC552230045110241240001
TDF/FTC FDC702312167190531500010

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting Triglycerides at Week 96

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <150 mg/dL, normal; 150->200 mg/dL, borderline high; 200-<500 mg/dL, high;>= 500 mg/dL, very high. (NCT00549198)
Timeframe: Baseline, Week 96

,
Interventionparticipants (Number)
Normal to normalNormal to borderline highNormal to highNormal to very highBorderline high to normalBorderline high to borderline highBorderline high to highBorderline high to very highHigh to normalHigh to borderline highHigh to highHigh to very highVery high to normalVery high to borderline highVery high to highVery high to very high
ABC/3TC FDC472534144111241150001
TDF/FTC FDC553120158190521600010

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Low-density Lipoprotein (LDL) at Week 24

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <100 mg/dL, optimal; 100-<130 mg/dL, near/above optimal; 130-<160 mg/dL, borderline high; 160-<190 mg/dL, high; >=190 mg/dL, very high. (NCT00549198)
Timeframe: Baseline, Week 24

,
Interventionparticipants (Number)
Optimal to optimalOptimal to near or above optimalOptimal to borderline highOptimal to highOptimal to very highNear or above optimal to optimalNear or above optimal to near or above optimalNear or above optimal to borderline highNear or above optimal to highNear or above optimal to very highBorderline high to optimalBorderline high to near or above optimalBorderline high to borderline highBorderline high to highBorderline high to very highHigh to optimalHigh to near or above optimalHigh to borderline highHigh to highHigh to very highVery high to optimalVery high to near or above optimalVery high to borderline highVery high to highVery high to very high
ABC/3TC FDC224122610617124012430001000101
TDF/FTC FDC464311105221151063320001000001

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Low-density Lipoprotein (LDL) at Week 48

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <100 mg/dL, optimal; 100-<130 mg/dL, near/above optimal; 130-<160 mg/dL, borderline high; 160-<190 mg/dL, high; >=190 mg/dL, very high. (NCT00549198)
Timeframe: Baseline, Week 48

,
Interventionparticipants (Number)
Optimal to optimalOptimal to near or above optimalOptimal to borderline highOptimal to highOptimal to very highNear or above optimal to optimalNear or above optimal to near or above optimalNear or above optimal to borderline highNear or above optimal to highNear or above optimal to very highBorderline high to optimalBorderline high to near or above optimalBorderline high to borderline highBorderline high to highBorderline high to very highHigh to optimalHigh to near or above optimalHigh to borderline highHigh to highHigh to very highVery high to optimalVery high to near or above optimalVery high to borderline highVery high to highVery high to very high
ABC/3TC FDC203827810419124012340001000101
TDF/FTC FDC424612103211361035420001000001

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Low-density Lipoprotein (LDL) at Week 96

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <100 mg/dL, optimal; 100-<130 mg/dL, near/above optimal; 130-<160 mg/dL, borderline high; 160-<190 mg/dL, high; >=190 mg/dL, very high. (NCT00549198)
Timeframe: Baseline, Week 96

,
Interventionparticipants (Number)
Optimal to optimalOptimal to near or above optimalOptimal to borderline highOptimal to highOptimal to very highNear or above optimal to optimalNear or above optimal to near or above optimalNear or above optimal to borderline highNear or above optimal to highNear or above optimal to very highBorderline high to optimalBorderline high to near or above optimalBorderline high to borderline highBorderline high to highBorderline high to very highHigh to optimalHigh to near or above optimalHigh to borderline highHigh to highHigh to very highVery high to optimalVery high to near or above optimalVery high to borderline highVery high to highVery high to very high
ABC/3TC FDC183529930417126012340001000101
TDF/FTC FDC374617101191672035330001000001

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Number of Participants With the Indicated Treatment-emergent Division of AIDS (DAIDS) Toxicities at Week 24

The DAIDS toxicity table provides descriptive terminology for grading the severity of adult adverse events. Laboratory grades also provide ranges for each parameter. Grade 1: mild, Grade 2: moderate, Grade 3: severe, Grade 4: potentially life-threatening. LDL, low-density lipid; HDL, high-density lipid. Treatment emergent refers to any toxicity that was not present prior to the start of study drug treatment. (NCT00549198)
Timeframe: Week 24

,
Interventionparticipants (Number)
Cholesterol, Grade 3Cholesterol, Grade 4LDL cholesterol, Grade 3LDL cholesterol, Grade 4Non-HDL cholesterol, Grade 3Non-HDL cholesterol, Grade 4Triglycerides, Grade 3Triglycerides, Grade 4Alanine aminotransferase, Grade 3Alanine aminotransferase, Grade 4Aspartate aminotransferase, Grade 3Aspartate aminotransferase, Grade 4Alkaline phosphatase, Grade 3Alkaline phosphatase, Grade 4Creatinine kinase, Grade 3Creatinine kinase, Grade 4Phosphorus inorganic, Grade 3Phosphorus inorganic, Grade 4Lipase, Grade 3Lipase, Grade 4Hyperkalaemia, Grade 3Hyperkalaemia, Grade 4Glomerular filtration rate, MDRD, Grade 3Glomerular filtration rate, MDRD, Grade 4Total neutrophils, Grade 3Total neutrophils, Grade 4Thrombocytopenia, Grade 3Thrombocytopenia, Grade 4
ABC/3TC FDC60801902011110001103201101110
TDF/FTC FDC1030500031021011101001100200

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Number of Participants With the Indicated Treatment-emergent Division of AIDS (DAIDS) Toxicities at Week 48

The DAIDS toxicity table provides descriptive terminology for grading the severity of adult adverse events. Laboratory grades also provide ranges for each parameter. Grade 1: mild, Grade 2: moderate, Grade 3: severe, Grade 4: potentially life-threatening. LDL, low-density lipid; HDL, high-density lipid. Treatment emergent refers to any toxicity that was not present prior to the start of study drug treatment. (NCT00549198)
Timeframe: Week 48

,
Interventionparticipants (Number)
Cholesterol, Grade 3Cholesterol, Grade 4LDL cholesterol, Grade 3LDL cholesterol, Grade 4Non-HDL cholesterol, Grade 3Non-HDL cholesterol, Grade 4Triglycerides, Grade 3Triglycerides, Grade 4Alanine aminotransferase, Grade 3Alanine aminotransferase, Grade 4Aspartate aminotransferase, Grade 3Aspartate aminotransferase, Grade 4Alkaline phosphatase, Grade 3Alkaline phosphatase, Grade 4Total bilirubin Grade 3Total bilirubin, Grade 4Creatinine kinase, Grade 3Creatinine kinase, Grade 4Phosphorus inorganic, Grade 3Phosphorus inorganic, Grade 4Lipase, Grade 3Lipase, Grade 4Hyperkalaemia, Grade 3Hyperkalaemia, Grade 4Glomerular filtration rate, MDRD, Grade 3Glomerular filtration rate, MDRD, Grade 4Total neutrophils, Grade 3Total neutrophils, Grade 4Thrombocytopenia, Grade 4
ABC/3TC FDC7090200302222001001305202102310
TDF/FTC FDC103060004102100021101002100200

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Percent Change From Baseline in Lumbar Spine Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 48

BMD is a measure (grams per cm^3) of the mineral content of bone in a particular skeletal area. DXA scans use low energy x-rays to measure the density of bones. The standard error (SE) of both treatment groups was based on the model on the log scale. (NCT00549198)
Timeframe: Baseline, Week 48

Interventionpercent change (Mean)
ABC/3TC FDC-1.59
TDF/FTC FDC-2.41

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Number of Participants Meeting World Health Organization (WHO) Criteria for Osteopenia (T-score of -2.5 to -1.0) and Osteoporosis (T-score of <-2.5) at Week 24

"The T-score is a radiographic diagnosis that compares bone mineral density (BMD) to that of a normal, healthy, 30-year-old female. The lower the T-score, the lower the BMD. A T-score of +1 to -1 is normal. A T-score decrease of -1 indicates a 10%-15% decrease in BMD." (NCT00549198)
Timeframe: Week 24

,
Interventionparticipants (Number)
Osteopenia, spine, n=147, 173Osteporosis, spine, n=147, 173Osteopenia, hip, n=149, 170Osteoporosis, hip, n=149, 170
ABC/3TC FDC4116384
TDF/FTC FDC689541

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Number of Participants Experiencing an Adverse Event (AE) Leading to Discontinuation by Week 96

An adverse event was any untoward medical occurrence in a participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Adverse events occurring in two or more participants are presented. (NCT00549198)
Timeframe: Baseline to Week 96

,
Interventionparticipants (Number)
Any eventDrug hypersensitivityBone density decreasedRashDizzinessHypersensitivityAbnormal dreamsDrug eruptionDepression
ABC/3TC FDC33110213310
TDF/FTC FDC2818330012

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Number of Participants Meeting World Health Organization (WHO) Criteria for Osteopenia (T-score of -2.5 to -1.0) and Osteoporosis (T-score of <-2.5) at Week 48

"The T-score is a radiographic diagnosis that compares bone mineral density (BMD) to that of a normal, healthy, 30-year-old female. The lower the T-score, the lower the BMD. A T-score of +1 to -1 is normal. A T-score decrease of -1 indicates a 10%-15% decrease in BMD." (NCT00549198)
Timeframe: Week 48

,
Interventionparticipants (Number)
Osteopenia, spine, n=132, 147Osteporosis, spine, n=132, 147Osteopenia, hip, n=130, 147Osteoporosis, hip, n=130, 147
ABC/3TC FDC4115374
TDF/FTC FDC575500

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Number of Participants Meeting World Health Organization (WHO) Criteria for Osteopenia (T-score of -2.5 to -1.0) and Osteoporosis (T-score of <-2.5) at Week 96

"The T-score is a radiographic diagnosis that compares bone mineral density (BMD) to that of a normal, healthy, 30-year-old female. The lower the T-score, the lower the BMD. A T-score of +1 to -1 is normal. A T-score decrease of -1 indicates a 10%-15% decrease in BMD." (NCT00549198)
Timeframe: Week 96

,
Interventionparticipants (Number)
Osteopenia, spine, n=64, 82Osteporosis, spine, n=64, 82Osteopenia, hip, n=65, 80Osteoporosis, hip, n=65, 80
ABC/3TC FDC215200
TDF/FTC FDC343310

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Number of Participants With a Decline From Baseline in Lumbar Spine and Hip Bone Mineral Density (BMD) >=2.0% and >=6.0% at Week 24

BMD is a measure of the mineral content of bone in a particular skeletal area. DXA scans use low energy x-rays to measure the density of bones. (NCT00549198)
Timeframe: Baseline, Week 24

,
Interventionparticipants (Number)
>=2%, spine, n=142, 165>=6%, spine, n=142, 165>=2%, hip, n=137, 160>=6%, hip, n=137, 160
ABC/3TC FDC7310381
TDF/FTC FDC11517936

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Number of Participants With a Decline From Baseline in Lumbar Spine and Hip Bone Mineral Density (BMD) >=2.0% and >=6.0% at Week 48

BMD is a measure of the mineral content of bone in a particular skeletal area. DXA scans use low energy x-rays to measure the density of bones. (NCT00549198)
Timeframe: Baseline, Week 48

,
Interventionparticipants (Number)
>=2%, spine, n=125, 141>=6%, spine, n=125, 141>=2%, hip, n=119, 140>=6%, hip, n=119, 140
ABC/3TC FDC515543
TDF/FTC FDC841311117

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Number of Participants With the Indicated Change From Baseline in National Cholesterol Education Program (NCEP) Thresholds for Fasting High-density Lipoprotein (HDL) at Week 48

Blood samples were collected from participants for analysis of their lipid profile. Data are categorized by the maximum post-baseline threshold reached. <40 mg/dL, low; 40-<60 mg/dL, normal; >=60 mg/dL, high. (NCT00549198)
Timeframe: Baseline, Week 48

,
Interventionparticipants (Number)
Low to lowLow to normalLow to highNormal to lowNormal to normalNormal to highHigh to lowHigh to normalHigh to high
ABC/3TC FDC176718011270010
TDF/FTC FDC28731002320035

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Number of Participants With the Indicated Treatment-emergent Division of AIDS (DAIDS) Toxicities at Week 96

The DAIDS toxicity table provides descriptive terminology for grading the severity of adult adverse events. Laboratory grades also provide ranges for each parameter. Grade 1: mild, Grade 2: moderate, Grade 3: severe, Grade 4: potentially life-threatening. LDL, low-density lipid; HDL, high-density lipid. Treatment emergent refers to any toxicity that was not present prior to the start of study drug therapy. (NCT00549198)
Timeframe: Week 96

,
Interventionparticipants (Number)
Cholesterol, Grade 3Cholesterol, Grade 4LDL cholesterol, Grade 3LDL cholesterol, Grade 4Non-HDL cholesterol, Grade 3Non-HDL cholesterol, Grade 4Triglycerides, Grade 3Triglycerides, Grade 4Alanine aminotransferase, Grade 3Alanine aminotransferase, Grade 4Aspartate aminotransferase, Grade 3Aspartate aminotransferase, Grade 4Alkaline phosphatase, Grade 3Alkaline phosphatase, Grade 4Total bilirubin, Grade 3Total bilirubin, Grade 4Creatinine kinase, Grade 3Creatinine kinase, Grade 4Phosphorus inorganic, Grade 3Phosphorus inorganic, Grade 4Lipase, Grade 3Lipase, Grade 4Hyperkalaemia, Grade 3Hyperkalaemia, Grade 4Glomerular filtration rate, MDRD, Grade 3Glomerular filtration rate, MDRD, Grade 4Total neutrophils, Grade 3Total neutrophils, Grade 4Thrombocytopenia, Grade 3Thrombocytopenia, Grade 4
ABC/3TC FDC90130220212222001001406402103510
TDF/FTC FDC105050004112100022302200101300

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Number of Participants With a Decline From Baseline in Lumbar Spine and Hip Bone Mineral Density (BMD) >=2.0% and >=6.0% at Week 96

BMD is a measure of the mineral content of bone in a particular skeletal area. DXA scans use low energy x-rays to measure the density of bones. (NCT00549198)
Timeframe: Baseline, Week 96

,
Interventionparticipants (Number)
>=2%, spine, n=59, 79>=6%, spine, n=59, 79>=2%, hip, n=58, 76>=6%, hip, n=58, 76
ABC/3TC FDC213331
TDF/FTC FDC3985213

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Number of Participants With Decline From Baseline in Estimated GFR, Calculated by MDRD and Cockcroft-Gault Equations, of >=10 mL/Min/1.73 m^2 (mL/Min for Cockcroft-Gault), >=20 mL/Min/1.72 m^2, >=10%, and >=20% at Week 24

mL, milliliter; min, minute; m^2, meters squared (NCT00549198)
Timeframe: Baseline, Week 24

,
Interventionparticipants (Number)
>=10 mL/min, MDRD>=10 mL/min, Cockcroft-Gault>=20 mL/min, MDRD>=20 mL/min, Cockcroft-Gault>=10%, MDRD>=10%, Cockcroft-Gault>=20%, MDRD>=20%, Cockcroft-Gault
ABC/3TC FDC161643151022
TDF/FTC FDC262064241733

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Number of Participants With Decline From Baseline in Estimated GFR, Calculated by MDRD and Cockcroft-Gault Equations, of >=10 mL/Min/1.73m^2 (mL/Min for Cockcroft-Gault), >=20 mL/Min/1.72m^2, >=10%, and >=20% at Week 48

mL, milliliter; min, minute; m^2, meters squared (NCT00549198)
Timeframe: Baseline, Week 48

,
Interventionparticipants (Number)
>=10 mL/min, MDRD>=10 mL/min, Cockcroft-Gault>=20 mL/min, MDRD>=20 mL/min, Cockcroft-Gault>=10%, MDRD>=10%, Cockcroft-Gault>=20%, MDRD>=20%, Cockcroft-Gault
ABC/3TC FDC231544211143
TDF/FTC FDC21143221920

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Number of Participants With Decline From Baseline in Estimated GFR, Calculated by MDRD and Cockcroft-Gault Equations, of >=10 mL/Min/1.73m^2 (mL/Min for Cockcroft-Gault), >=20 mL/Min/1.72m^2, >=10%, and >=20% at Week 96

mL, milliliter; min, minute; m^2, meters squared (NCT00549198)
Timeframe: Baseline, Week 96

,
Interventionparticipants (Number)
>=10 mL/min, MDRD>=10 mL/min, Cockcroft-Gault>=20 mL/min, MDRD>=20 mL/min, Cockcroft-Gault>=10%, MDRD>=10%, Cockcroft-Gault>=20%, MDRD>=20%, Cockcroft-Gault
ABC/3TC FDC151144151233
TDF/FTC FDC381975271664

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Number of Participants With HIV-1 RNA <50 Copies/Milliliter (c/mL) and 400 c/mL at Week 24

HIV-1 RNA level (viral load) is a strong predictor of the rate of HIV disease progression. It was measured from plasma (participant blood samples) taken at all visits throughout the study. HIV, human immunodeficiency virus; RNA, ribonucleic acid. Viral load is a measure of the severity of the HIV infection. (NCT00549198)
Timeframe: Week 24

,
Interventionparticipants (Number)
<50 copies/mL<400 copies/mL
ABC/3TC FDC126147
TDF/FTC FDC144168

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Number of Participants Experiencing an Adverse Event (AE) Leading to Discontinuation by Week 48

An adverse event was any untoward medical occurrence in a participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Adverse events occurring in two or more participants are presented. (NCT00549198)
Timeframe: Baseline to Week 48

,
Interventionparticipants (Number)
Any eventDrug hypersensitivityBone density decreasedRashDizzinessHypersensitivityDrug eruption
ABC/3TC FDC291102131
TDF/FTC FDC21123301

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Number of Participants Experiencing an Adverse Event (AE) Leading to Discontinuation by Week 24

An adverse event was any untoward medical occurrence in a participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Adverse events occurring in two or more participants are presented. (NCT00549198)
Timeframe: Baseline to Week 24

,
Interventionparticipants (Number)
Any eventDrug hypersensitivityRashDizzinessHypersensitivityDrug eruption
ABC/3TC FDC26112031
TDF/FTC FDC1413201

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Number of Participants Classified as Protocol-defined Failures With Treatment-emergent Resistance to Study Drug in the Indicated Viruses at Week 96

Viral resistance was measured using blood samples collected from participants throughout the study. NRTI, nucleoside reverse transcriptase inhibitor; NNRTI, non-nucleoside reverse transcriptase inhibitor. Virological failure was defined as any one of: participant does not achieve a 1 log10 copies (cop)/mL decrease in plasma HIV-1 RNA by Week (Wk) 4, or has two consecutive plasma HIV-1 RNA measures >=400 cop/mL separated by at least 2-4 wk after being previously <=400 cop/mL on/after Wk 4, or has two consecutive plasma HIV-1 RNA measures >400 cop/mL separated by at least 2-4 wk on/after Wk 24. (NCT00549198)
Timeframe: Week 96

,
Interventionparticipants (Number)
Any treatment-emergent mutationNRTINNRTI
ABC/3TC FDC442
TDF/FTC FDC000

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"Number of Participants Who Indicated Yes or No to the Question of Whether Unplanned Healthcare Resources Were Utilized"

Participants were asked at each visit whether or not they utilized unplanned healthcare resources. (NCT00549198)
Timeframe: Baseline to Week 96

,
Interventionparticipants (Number)
Week 4, Yes, n=178, 183Week 4, No, n=178, 183Week 12, Yes, n=162, 177Week 12, No, n=162, 177Week 24, Yes, n=156, 173Week 24, No, n=156, 173Week 36, Yes, n=148, 169Week 36, No, n=148, 169Week 48, Yes, n=137, 161Week 48, No, n=137, 161Week 60, Yes, n=129, 148Week 60, No, n=129, 148Week 72, Yes, n=126, 139Week 72, No, n=126, 139Week 84, Yes, n=121, 136Week 84, No, n=121, 136Week 96, Yes, n=113, 135Week 96, No, n=113, 135
ABC/3TC FDC601185610670864810044934782487834873083
TDF/FTC FDC49134471305911450119361254410440992410817118

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Percent Change From Baseline in Lumbar Spine Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 96

BMD is a measure (grams per cm^3) of the mineral content of bone in a particular skeletal area. DXA scans use low energy x-rays to measure the density of bones. The standard error (SE) of both treatment groups was based on the model on the log scale. (NCT00549198)
Timeframe: Baseline, Week 96

Interventionpercent change (Mean)
ABC/3TC FDC-0.87
TDF/FTC FDC-1.70

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Percent Change From Baseline in Lumbar Spine Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 24

BMD is a measure (grams [g] per centimeters cubed [cm^3]) of the mineral content of bone in a particular skeletal area. DXA scans use low energy x-rays to measure the density of bones. The standard error (SE) of both treatment groups was based on the model on the log scale. (NCT00549198)
Timeframe: Baseline, Week 24

Interventionpercent change (Mean)
ABC/3TC FDC-2.12
TDF/FTC FDC-3.30

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Percent Change From Baseline in Hip Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 96

BMD is a measure (grams per cm^3) of the mineral content of bone in a particular skeletal area. DXA scans use low energy x-rays to measure the density of bones. The standard error (SE) of both treatment groups was based on the model on the log scale. (NCT00549198)
Timeframe: Baseline, Week 96

Interventionpercent change (Mean)
ABC/3TC FDC-2.17
TDF/FTC FDC-3.55

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Percent Change From Baseline in Hip Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 48

BMD is a measure (grams per cm^3) of the mineral content of bone in a particular skeletal area. DXA scans use low energy x-rays to measure the density of bones. The standard error (SE) of both treatment groups was based on the model on the log scale. (NCT00549198)
Timeframe: Baseline, Week 48

Interventionpercent change (Mean)
ABC/3TC FDC-1.90
TDF/FTC FDC-3.56

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Percent Change From Baseline in Hip Bone Mineral Density (BMD), Measured by Dual-energy X-ray Absorptiometry (DXA), at Week 24

BMD is a measure (grams per cm^3) of the mineral content of bone in a particular skeletal area. DXA scans use low energy x-rays to measure the density of bones. The standard error (SE) of both treatment groups was based on the model on the log scale. (NCT00549198)
Timeframe: Baseline, Week 24

Interventionpercent change (Mean)
ABC/3TC FDC-1.19
TDF/FTC FDC-2.73

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the Percentage of CD3+/CD4+ Cells Per Cubic Millimeter at the Effector Sites in the Duodenal Tissues Obtained From Volunteers to the Antiretroviral Therapy Regimen Over Time.

Duodenal tissue immune cell subsets were measured by flow cytometry. (NCT00661960)
Timeframe: nine months

Intervention% CD3/CD4 T-cells in GALT tissue (Median)
Negative Volunteers55.3
HIV-postive Randomized to Raltegravir11.7
HIV-postive Randomized to NNRTI9.9

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Effect of CYP2B6 Genotype on Efavirenz Clearance

Efavirenz clearance is a measure of rate of elimination of the drug from the body. We used this measure to evaluate differences in rate of elimination of efavirenz at a single dose and after multiple dosing within three CYP2B6 genotypes (CYP2B6*1/*1, *1/*6 and CYP2B6*6/*6). Efavirenz clearance was measured in normal metabolizer of CYP2B6 (CYP2B6*1/*1 genotype), intermediate metabolizer (CYP2B6*1/*6) and slow metabolizer (CYP2B6*6/*6) at a single 600 mg oral dose of efavirenz and then after multiple dosing (autoinduction), i.e., the administration of efavirenz (600 mg/day) for 17 days. Single and multiple dose efavirenz clearance was measured and compared to determine the extent of autoinduction within this genotype group. (NCT00668395)
Timeframe: Efavirenz clearance at single dose and multiple dose stratified by CYP2B6 genotypes

,,
Interventionml/h/kg (Mean)
Single efavirenz doseMultiple efavirenz dose
CYP2B6*1/*193.3550.05
CYP2B6*1/*676.08119.90
CYP2B6*6/*651.0380.12

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Number of Subjects Needing to Switch Comparator Drugs (FPV/r or EFV)

"Subjects were randomized and initiated treatment on one of the antiretroviral arms(FPV/r or EFV) at study Entry visit. Subjects would be switched for the follwing reasons:~To resolve a Grade 3 or 4 Adverse Event~The subject experienced a virologic failure (as defined in section 3.6.2)~The investigator believes the subject is at a significant risk for failing to comply with the protocol AND the investigator believes a regimen substitution is likely to resolve the compliance issue~The investigator believes there is any other significant safety concern for the subject associated with remaining on the current regimen (e.g., hypersensitivity reaction, increased risk of suicide)" (NCT00727597)
Timeframe: 96 weeks

Interventionparticipants (Number)
Once Daily (QD) Regimen of Lexiva1
QD Regimen of Sustiva2

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Mean Platelet Count Between Treatment Groups at 2 Months

The mean platelet count between treament groups at 2 months after starting study drug. The calculated number of platelets in a volume of blood, usually expressed as platelets per cubic millimeter (cmm) of whole blood. Platelets are the smallest cell-like structures in the blood and are important for blood clotting and plugging damaged blood vessels. Platelet counts are usually done by laboratory machines that also count other blood elements such as the white and red cells. They can also be counted by use of a microscope. Normal platelet counts are in the range of 150,000 to 400,000 per microliter (or 150 - 400 x 100 per liter). (NCT00734344)
Timeframe: 2 months after baseline

Interventioncount per microliter (Mean)
Raltegravir Plus Truvada232600
Efavirenz Plus Truvada225600

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Mean Platelet Count Between Treatment Groups at 4 Months

The mean platelet count between treatment groups at 4 months after starting study drug. The calculated number of platelets in a volume of blood, usually expressed as platelets per cubic millimeter (cmm) of whole blood. Platelets are the smallest cell-like structures in the blood and are important for blood clotting and plugging damaged blood vessels. Platelet counts are usually done by laboratory machines that also count other blood elements such as the white and red cells. They can also be counted by use of a microscope. Normal platelet counts are in the range of 150,000 to 400,000 per microliter (or 150 - 400 x 109 per liter). (NCT00734344)
Timeframe: 4 months after baseline

Interventioncount per microliter (Mean)
Raltegravir Plus Truvada210800
Efavirenz Plus Truvada197300

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Mean Platelet Count Between Treatment Groups at 6 Months

The mean platelet count between treatment groups at 6 months after starting study drug. The calculated number of platelets in a volume of blood, usually expressed as platelets per cubic millimeter (cmm) of whole blood. Platelets are the smallest cell-like structures in the blood and are important for blood clotting and plugging damaged blood vessels. Platelet counts are usually done by laboratory machines that also count other blood elements such as the white and red cells. They can also be counted by use of a microscope. Normal platelet counts are in the range of 150,000 to 400,000 per microliter (or 150 - 400 x 109 per liter). (NCT00734344)
Timeframe: 6 months after baseline

Interventioncount per microliter (Mean)
Raltegravir Plus Truvada230000
Efavirenz Plus Truvada224800

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Mean Platelet Count Between Treatment Groups at 8 Months

The mean platelet count between treatment groups at 8 months after starting study drug. The calculated number of platelets in a volume of blood, usually expressed as platelets per cubic millimeter (cmm) of whole blood. Platelets are the smallest cell-like structures in the blood and are important for blood clotting and plugging damaged blood vessels. Platelet counts are usually done by laboratory machines that also count other blood elements such as the white and red cells. They can also be counted by use of a microscope. Normal platelet counts are in the range of 150,000 to 400,000 per microliter (or 150 - 400 x 109 per liter). (NCT00734344)
Timeframe: 8 months after baseline

Interventioncount per microliter (Mean)
Raltegravir Plus Truvada215700
Efavirenz Plus Truvada208100

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Mean White Blood Cell Count Between Treatment Groups at 10 Months

Mean WBC count of all subjects as determined by standard lab procedures at 10 months after starting study drug as well as range. The normal number of WBCs in the blood is 4,500-10,000 white blood cells per microliter (mcL). (NCT00734344)
Timeframe: 10 months after baseline

Interventionwhite blood cells per microliter (mcL). (Mean)
Raltegravir Plus Truvada5230
Efavirenz Plus Truvada4615

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Mean Hematocrit Between Treatment Groups at 4 Months

Mean hematocrit of all subjects at 4 months after starting study drug. The hematocrit, also known as packed cell volume (PCV) or erythrocyte volume fraction (EVF), is the volume percentage (%) of red blood cells in blood. It is normally 45% for men and 40% for women. (NCT00734344)
Timeframe: 4 months after baseline

Interventionpercentage (Mean)
Raltegravir Plus Truvada41.4
Efavirenz Plus Truvada43

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Mean Hematocrit Between Treatment Groups at 6 Months

Mean hematocrit of all subjects at 6 months after starting study drug. The hematocrit, also known as packed cell volume (PCV) or erythrocyte volume fraction (EVF), is the volume percentage (%) of red blood cells in blood. It is normally 45% for men and 40% for women. (NCT00734344)
Timeframe: 6 months after baseline

Interventionpercentage (Mean)
Raltegravir Plus Truvada42.1
Efavirenz Plus Truvada39.8

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Mean Hematocrit Between Treatment Groups at 8 Months

Mean hematocrit of all subjects at 8 months after starting study drug. The hematocrit, also known as packed cell volume (PCV) or erythrocyte volume fraction (EVF), is the volume percentage (%) of red blood cells in blood. It is normally 45% for men and 40% for women. (NCT00734344)
Timeframe: 8 months after baseline

Interventionpercentage (Mean)
Raltegravir Plus Truvada40.3
Efavirenz Plus Truvada41.2

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Mean Platelet Count Between Treatment Groups at 10 Months

The mean platelet count between treatment groups at 10 months after starting study drug. The calculated number of platelets in a volume of blood, usually expressed as platelets per cubic millimeter (cmm) of whole blood. Platelets are the smallest cell-like structures in the blood and are important for blood clotting and plugging damaged blood vessels. Platelet counts are usually done by laboratory machines that also count other blood elements such as the white and red cells. They can also be counted by use of a microscope. Normal platelet counts are in the range of 150,000 to 400,000 per microliter (or 150 - 400 x 109 per liter). (NCT00734344)
Timeframe: 10 months after baseline

Interventioncount per microliter (Mean)
Raltegravir Plus Truvada193500
Efavirenz Plus Truvada243300

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Mean Platelet Count Between Treatment Groups at 12 Months

The mean platelet count between treatment groups at 12 months after starting study drug. The calculated number of platelets in a volume of blood, usually expressed as platelets per cubic millimeter (cmm) of whole blood. Platelets are the smallest cell-like structures in the blood and are important for blood clotting and plugging damaged blood vessels. Platelet counts are usually done by laboratory machines that also count other blood elements such as the white and red cells. They can also be counted by use of a microscope. Normal platelet counts are in the range of 150,000 to 400,000 per microliter (or 150 - 400 x 109 per liter). (NCT00734344)
Timeframe: 12 months after baseline

Interventioncount per microliter (Mean)
Raltegravir Plus Truvada255600
Efavirenz Plus Truvada185500

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Mean White Blood Cell Count Between Treatment Groups at 4 Months

Mean WBC count of all subjects as determined by standard lab procedures at 4 months after starting study drug as well as range. The normal number of WBCs in the blood is 4,500-10,000 white blood cells per microliter (mcL). (NCT00734344)
Timeframe: 4 months post baseline

Interventionwhite blood cells per microliter (mcL). (Mean)
Raltegravir Plus Truvada5850
Efavirenz Plus Truvada4948

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Mean White Blood Cell Count Between Treatment Groups at 2 Months

Mean WBC count for all subjects as determined by standard lab procedures at 2 months after starting study drug as well as range. The normal number of WBCs in the blood is 4,500-10,000 white blood cells per microliter (mcL). (NCT00734344)
Timeframe: baseline to 2 months

Interventionwhite blood cells per microliter (mcL). (Mean)
Raltegravir Plus Truvada5904
Efavirenz Plus Truvada4918

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Mean White Blood Cell Count Between Treatment Groups at 14 Months

Mean WBC count of all subjects as determined by standard lab procedures at 14 months after starting study drug as well as range. The normal number of WBCs in the blood is 4,500-10,000 white blood cells per microliter (mcL). (NCT00734344)
Timeframe: 14 months after baseline

Interventionwhite blood cells per microliter (mcL). (Mean)
Raltegravir Plus Truvada3180
Efavirenz Plus Truvada4903

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Mean White Blood Cell Count Between Treatment Groups at 12 Months

Mean WBC count of all subjects as determined by standard lab procedures at 12 months after starting study drug as well as range. The normal number of WBCs in the blood is 4,500-10,000 white blood cells per microliter (mcL). (NCT00734344)
Timeframe: 12 months after baseline

Interventionwhite blood cells per microliter (mcL). (Mean)
Raltegravir Plus Truvada6320
Efavirenz Plus Truvada4868

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Mean Hematocrit Between Treatment Groups at 2 Months

Mean hematocrit of all subjects at 2 months after starting study drug. The hematocrit, also known as packed cell volume (PCV) or erythrocyte volume fraction (EVF), is the volume percentage (%) of red blood cells in blood. It is normally 45% for men and 40% for women. (NCT00734344)
Timeframe: 2 months after baseline

Interventionpercentage (Mean)
Raltegravir Plus Truvada41.5
Efavirenz Plus Truvada41.8

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Mean White Blood Cell Count Between Treatment Groups at 8 Months

Mean WBC count of all subjects as determined by standard lab procedures at 8 months after starting study drug as well as range. The normal number of WBCs in the blood is 4,500-10,000 white blood cells per microliter (mcL). (NCT00734344)
Timeframe: 8 months after baseline

Interventionwhite blood cells per microliter (mcL). (Mean)
Raltegravir Plus Truvada6240
Efavirenz Plus Truvada4607

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Mean CD4 Count Between Treatment Groups at 10 Months

Mean CD4 count between groups 10 months after starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3 in adults and teens. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 10 months after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada469
Efavirenz Plus Truvada571.5

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Mean White Blood Cell Count Between Treatment Groups at 6 Months

Mean WBC count of all subjects as determined by standard lab procedures at 6 months after starting study drug as well as range. The normal number of WBCs in the blood is 4,500-10,000 white blood cells per microliter (mcL). (NCT00734344)
Timeframe: 6 months after baseline

Interventionwhite blood cells per microliter (mcL). (Mean)
Raltegravir Plus Truvada5219
Efavirenz Plus Truvada4522

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Mean CD4 Count Between Treatment Groups at 1 Months

Mean CD4 count between groups 1 month after starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 1 month after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada629.1
Efavirenz Plus Truvada535

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Mean Platelet Count Between Treatment Groups at 14 Months

The mean platelet count between treatment groups at 14 months after starting study drug. The calculated number of platelets in a volume of blood, usually expressed as platelets per cubic millimeter (cmm) of whole blood. Platelets are the smallest cell-like structures in the blood and are important for blood clotting and plugging damaged blood vessels. Platelet counts are usually done by laboratory machines that also count other blood elements such as the white and red cells. They can also be counted by use of a microscope. Normal platelet counts are in the range of 150,000 to 400,000 per microliter (or 150 - 400 x 109 per liter). (NCT00734344)
Timeframe: 4 months after baseline

Interventioncount per microliter (Mean)
Raltegravir Plus Truvada217400
Efavirenz Plus Truvada216800

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Mean CD4 Count Between Treatment Groups at 11 Months

Mean CD4 count between groups 11 months after of starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3 in adults and teens. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 11 months after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada495

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Mean CD4 Count Between Treatment Groups at 2 Months

Mean CD4 count between groups 2 months after starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3 in adults and teens. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 2 months after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada703.1
Efavirenz Plus Truvada527.2

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Mean Hematocrit Between Treatment Groups at 12 Months

Mean hematocrit of all subjects at 12 months after starting study drug. The hematocrit, also known as packed cell volume (PCV) or erythrocyte volume fraction (EVF), is the volume percentage (%) of red blood cells in blood. It is normally 45% for men and 40% for women. (NCT00734344)
Timeframe: 12 months after baseline

Interventionpercentage (Mean)
Raltegravir Plus Truvada41
Efavirenz Plus Truvada43.5

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Mean CD4 Count Between Treatment Groups at 3 Months

Mean CD4 count between groups 3 months after starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3 in adults and teens. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 3 months after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada716.4
Efavirenz Plus Truvada671.7

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Mean CD4 Count Between Treatment Groups at 4 Months

Mean CD4 count between groups 4 months after starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3 in adults and teens. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 4 months after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada617.2
Efavirenz Plus Truvada646.5

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Mean CD4 Count Between Treatment Groups at 5 Months

Mean CD4 count between groups 5 months after starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3 in adults and teens. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 5 months after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada805.7
Efavirenz Plus Truvada539.6

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Mean CD4 Count Between Treatment Groups at 6 Months

Mean CD4 count between groups 6 months after starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3 in adults and teens. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 6 months after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada652.2
Efavirenz Plus Truvada673.5

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Mean CD4 Count Between Treatment Groups at 7 Months

Mean CD4 count between groups 7 months after starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3 in adults and teens. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 7 months after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada504
Efavirenz Plus Truvada552.5

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Mean CD4 Count Between Treatment Groups at 8 Months

Mean CD4 count between groups 8 months after starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3 in adults and teens. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 8 months after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada464.5
Efavirenz Plus Truvada586.5

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Mean CD4 Count Between Treatment Groups at 9 Months

Mean CD4 count between groups 9 months after starting study drug. CD4 cells are types of white blood cells called T lymphocytes or T cells that fight infection. CD4 counts are most often used to evaluate the immune system of a person diagnosed with a human immunodeficiency virus (HIV) infection to help stage and monitor progression of the disease and monitor effectiveness of antiretroviral treatment. A CD4 count is typically reported as an absolute level or count of cells (expressed as cells per cubic millimeter of blood). A normal CD4 count ranges from 410-1,590 cells/mm3 in adults and teens. Sometimes results are expressed as a percent of total lymphocytes (CD4 percent). (NCT00734344)
Timeframe: 9 months after baseline

Interventioncells/mm3 (Mean)
Raltegravir Plus Truvada306
Efavirenz Plus Truvada571

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Mean Hematocrit Between Treatment Groups at 10 Months

Mean hematocrit of all subjects at 10 months after starting study drug. The hematocrit, also known as packed cell volume (PCV) or erythrocyte volume fraction (EVF), is the volume percentage (%) of red blood cells in blood. It is normally 45% for men and 40% for women. (NCT00734344)
Timeframe: 10 months after baseline

Interventionpercentage (Mean)
Raltegravir Plus Truvada45
Efavirenz Plus Truvada38

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Mean Hematocrit Between Treatment Groups at 14 Months

Mean hematocrit of all subjects at 14 months after starting study drug. The hematocrit, also known as packed cell volume (PCV) or erythrocyte volume fraction (EVF), is the volume percentage (%) of red blood cells in blood. It is normally 45% for men and 40% for women. (NCT00734344)
Timeframe: 14 months after baseline

Interventionpercentage (Mean)
Raltegravir Plus Truvada36
Efavirenz Plus Truvada39.7

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Compare Early Activated CD4+ T-cell Recovery Rates From Baseline to Week 4.

To compare early (baseline to Week 4) activated CD4+ T-cell recovery rates between treatment regimens. (NCT00752856)
Timeframe: Baseline to Week 4

Interventioncells/mm^3 (Mean)
1 - Kaletra + Isentress Taken Twice Daily-3.81
2 - Atripla Taken Once Daily-1.18

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Compare Late Activated CD4+ T-cell Recovery Rates Between Treatment Regimens From Baseline to Week 48

To compare late (baseline to Week 48) activated CD4+ T-cell recovery rates between treatment regimens. (NCT00752856)
Timeframe: 48 weeks

Interventioncells/mm^3 (Mean)
1 - Kaletra + Isentress Taken Twice Daily-2.24
2 - Atripla Taken Once Daily-5.65

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Viral Suppression Efficacy at 48 Weeks

To determine the antiviral efficacy of LPV/r + RAL compared to EFV/TDF/FTC after 48 weeks of treatment by achieving undetectable viral load (NCT00752856)
Timeframe: 48 weeks

Interventionpercentage of participants (Number)
1 - Kaletra + Isentress Taken Twice Daily86
2 - Atripla Taken Once Daily87.5

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To Compare the Phase 1 Viral Decay Rates Between LPV/r + RAL vs. EFV/TDF/FTC Treatment Combinations.

Repeated HIV RNA measured at different time points (baseline, days 2, 7, 10, 14) will be treated as the outcome variable in a linear mixed-effects model. The primary fixed effects will include time, treatment group, treatment group-by-time interaction; random effects will include both intercept and slope allowing each subject to have individual baseline viral load and viral decay (rate of decrease in viral load following initiation of antiretroviral therapy). The treatment group-by- time interaction term in the model will indicate the difference in viral decay rates between the two treatment groups. Baseline covariate adjustment will be included if necessary. (NCT00752856)
Timeframe: Baseline, days 2, 7, 10, 14

Interventionlog(10)/day (Median)
1 - Kaletra + Isentress Taken Twice Daily0.47
2 - Atripla Taken Once Daily0.55

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Naive, Central Memory, Effector Memory, and T Reg CD4+ T-cell Frequency

Naive, central memory and effector memory, and T reg CD4+ T-cell frequency at week 24 (NCT00775606)
Timeframe: week 24 measurements

,
Interventionpercentage of cells (Mean)
Mean percentage of naive CD4+ T cells at week 24Mean percentage of central memory CD4+ T cells at week 24Mean percentage of effector memory CD4+ T cells at week 24Mean percentage of CD4+ Treg cells at week 24
ARM A Lopinavir/Ritonavir29.0810.8934.985.58
ARM B Efavirenz25.738.2844.825.51

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Activated and Regulatory CD4+ and CD8+ T-cell Frequencies

Activation of CD4+ and CD8+ T cells were measured at week 24 (NCT00775606)
Timeframe: week 24 measurements

,
Interventionpercentage of cells (Mean)
Activation of CD4+ T cells at week 24Activation of CD8+ T cells at week 24Proliferation of CD4+ T cells at week 24Proliferation of CD8+ T cells at week 24
ARM A Lopinavir-ritonavir8.7020.920.470.81
ARM B Efavirenz7.3917.170.520.48

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CD4+ T-cell Change

This measures the change in CD4+ T-cells from baseline to week 24 of treatment. (NCT00775606)
Timeframe: 24 weeks after treatment initiation (baseline and week 24)

Interventioncells/mm3 (Mean)
ARM A/Lopinavir-ritonavir176.83
ARM B/Efavirenz102.6

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CD4+ (Cluster of Differentiation 4) T-cell Apoptosis

Change in the percentage of naive CD4 T-cells undergoing apoptosis as measured by propidium iodide staining. This is a lab test that measures the percentage of naive CD4 T-cells that are undergoing cell death. The change in this measure is obtained by determining the difference between the percentage of naive CD4 T-cells undergoing apoptosis at week 24 of treatment and the percentage undergoing apoptosis at baseline. (NCT00775606)
Timeframe: 24 weeks from treatment initiation (baseline and week 24)

Interventionper cent (Mean)
ARM A/Lopinavir-ritonavir-12.33
ARM B/Efavirenz-8.01

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Naive, Central Memory, Effector Memory, and T Reg CD4+ T-cell Frequency

Naive, central memory, effector memory, and T reg CD4+ T-cell frequency at baseline (NCT00775606)
Timeframe: baseline measurements

,
Interventionpercentage of cells (Mean)
Mean percentage of naive CD4+ T cells at baselineMean percentage of central memory CD4+ T cells at baselineMean percentage of effector memory CD4+ T cells at baselineMean percentage of CD4+ Treg cells at baseline
ARM A Lopinavir/Ritonavir32.6711.5436.447.35
ARM B Efavirenz24.709.0247.326.96

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Activation and Proliferation of CD4+ and CD8+ T-cell Frequencies

Activation and proliferation of CD4+ and CD8+ T cells were measured at baseline (NCT00775606)
Timeframe: baseline measurements

,
Interventionpercentage of cells (Mean)
Activation of CD4+ T cells at baselineActivation of CD8+ T cells at baselineProliferation of CD4+ T cells at baselineProliferation of CD8+ T cells at baseline
ARM A Lopinavir-ritonavir12.8534.611.211.39
ARM B Efavirenz12.3533.571.251.25

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AUC of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz) on Study Days 1-5

The area under the concentrations-time curve (AUC) was calculated with the measured data points from the time of administration until the last quantificable concentration by the trapezoidal formula and the extrapolation to infinity. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study days 1-5

Interventionng*h/ml (Mean)
Study Group29.7

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AUC0-24h of Efavirenz (Steady State Pharmacokinetic After Chronic Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Day 30

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng*h/ml (Mean)
Study Group11.4

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AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng*h/ml (Mean)
Study Group325

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AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 15

Interventionng*h/ml (Mean)
Study Group466

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AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng*h/ml (Mean)
Study Group51.2

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AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 16

Interventionng*h/ml (Mean)
Study Group58.6

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AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 15

Interventionng*h/ml (Mean)
Study Group51.9

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Cmax of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Days 16-20

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study days 16-20

Interventionng/ml (Mean)
Study Group0.659

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Cmax of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz) on Study Days 1-5

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study days 1-5

Interventionng/ml (Mean)
Study Group0.622

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Cmax of Efavirenz (Steady State Pharmacokinetic After Chronic Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Day 30

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng/ml (Mean)
Study Group0.918

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Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng/ml (Mean)
Study Group45.3

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Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 16

Interventionng/ml (Mean)
Study Group60.9

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Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 15

Interventionng/ml (Mean)
Study Group79.0

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Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng/ml (Mean)
Study Group4.46

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Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 16

Interventionng/ml (Mean)
Study Group5.54

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Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 15

Interventionng/ml (Mean)
Study Group4.82

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AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 16

Interventionng*h/ml (Mean)
Study Group411

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AUC of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Days 16-20

The area under the concentrations-time curve (AUC) was calculated with the measured data points from the time of administration until the last quantificable concentration by the trapezoidal formula and the extrapolation to infinity. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study days 16-20

Interventionng*h/ml (Mean)
Study Group27.0

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Maximum Concentration for Tenofovir, Emtricitabine and Efavirenz

The maximum concentration for tenofovir, emtricitabine and efavirenz (NCT00862823)
Timeframe: 17 days

,
Interventionmg/L (Geometric Mean)
Efavirenz CmaxEmtricitabine CmaxTenofovir Cmax
Atripla Liquid1.32.10.2
Atripla Tablet1.51.80.3

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Area Under the Concentration Time Curve for Tenofovir, Emtricitabine and Efavirenz

The area under the concentration time curve for tenofovir, emtricitabine and efavirenz (NCT00862823)
Timeframe: 17 days

,
Interventionmg*hr/mL (Geometric Mean)
Efavirenz AUCEmtricitabine AUCTenofovir AUC
Atripla Liquid56.710.82.2
Atripla Tablet58.710.91.8

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Trough Plasma and Tissue Drug Levels in Volunteers at the Time of the Upper Endoscopy

The reported drug level is for the primary ART agent for that cohort. For the maraviroc arm, maraviroc plasma and tissue levels are reported. For the maraviroc plus raltegravir arm, the raltegravir plasma and tissue levels are reported. For the efavirenz arm, the efavirenz plasma and tissue levels are reported. HIV negative controls were not on ART and did not have drug levels measured. (NCT00870363)
Timeframe: nine months

,,
Interventionng/mL (Median)
plasma primary ARTduodenal tissue primary ART
Efavirenz or Other NNRTI With 2 NRTIs245911.1
Maraviroc in Combination With 2 NRTIs94.50.7
Maraviroc PLUS Raltegravir in Combination With 2 NRTIs3970.1

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Change in the Density of CD3+/CD4+ Cells Per Cubic Millimeter at the Effector Sites in the Duodenal Tissues Following Antiretroviral Therapy Regimen

immunohistochemistry for CD3+/CD4+ cells counted manually within the lamina propria (NCT00870363)
Timeframe: Baseline and nine months for 3 treatment cohorts and Baseline for the control group, which was only assessed at one time point

Interventioncells/mm^2 (Mean)
Maraviroc in Combination With 2 NRTIs24
Maraviroc PLUS Raltegravir in Combination With 2 NRTIs89
Efavirenz or Other NNRTI With 2 NRTIs119
HIV Negative Controls Not on ART566

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Changes in CD4+ T-cell Numbers by Treatment Regimen

peripheral absolute CD4+ T-cell counts increase from baseline to 9 months of cART by commercial assay (NCT00870363)
Timeframe: Baseline and nine months

Interventioncells/mL (Mean)
Maraviroc in Combination With 2 NRTIs221
Maraviroc PLUS Raltegravir in Combination With 2 NRTIs231
Efavirenz or Other NNRTI With 2 NRTIs194

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Change in HIV DNA Per 10^6 Cells in Duodenal Tissue Versus PBMC by Drug Regimen Received

single-cell suspension of digested duodenal tissue and Ficol-Hypaque separated PBMC underwent HIV-DNA PCR (NCT00870363)
Timeframe: Baseline and nine months

,,
Interventioncopies/10^6 cells (Mean)
PBMC HIV-DNADuodenal HIV-DNA
Efavirenz or Other NNRTI With 2 NRTIs-1330-325
Maraviroc in Combination With 2 NRTIs-1709-16
Maraviroc PLUS Raltegravir in Combination With 2 NRTIs-2500-846

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Number of Subjects Who Had a Decrease in HIV RNA Per Million CD4+ T Cells in the Ileum

Number of subjects who had a decrease from week 0 to week 12 in unspliced cell-associated HIV RNA per million CD4+ T cells in the ileum (NCT00884793)
Timeframe: 12 weeks

Interventionparticipants (Number)
Intensification Arm5

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Number of Subjects Who Experienced an Increase in CD4+ T Cells (as a % of All Cells) in the Ileum.

Number of subjects who experienced an increase in CD4+ T cells (as a % of all cells) in the ileum (by flow cytometry) from week 0 to week 12. (NCT00884793)
Timeframe: 12 weeks

Interventionparticipants (Number)
Intensification Arm6

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Number of Subjects Who Experienced an Increase in CD4% in the Ileum.

Number of subjects who experienced an increase from week 0 to week 12 in CD4+ T cells (as a % of T cells, by flow cytometry) in the ileum (NCT00884793)
Timeframe: 12 weeks

Interventionparticipants (Number)
Intensification Arm5

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"Average Change in Activated (CD38+HLADR+) CD8+ T Cells in the Ileum"

Average of changes(week 0-week 12) in the % of CD8+ T cells that are CD38+HLA-DR+, by flow cytometry (NCT00884793)
Timeframe: 12 weeks

Interventionpercentage change (Mean)
Intensification Arm-5.4

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Resistance Determinations

The evolution of viral genotype and phenotype was assessed by the number of patients with resistance-associated mutations emerging at the endpoint. A mutation was considered emerging if it was present at endpoint and not present at baseline or any pre-baseline assessment. (NNRTI = non-nucleoside reverse transcriptase inhibitor; NRTI = nucleoside reverse transcriptase inhibitor; RAM = resistance-associated mutation, IAS-USA = International AIDS Society - USA) (NCT00903682)
Timeframe: at baseline and all subsequent visits until week 48 in case if virologic failure

,
Interventionnumber of participants (Number)
>= 1 successful genotype after baseline>= 1 IAS-USA NRTI RAMs>= 1 NRTI Surveillance Drug Resistance Mutation>= 1 NNRTI RAMsno NRTI or NNRTI RAMs
Efavirenz92236
Etravirine110029

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Mean Change From Baseline in CD4+ Cell Count

The mean change in CD4+ cell count from baseline was calculated with a last observation carried forward method; i.e. the last observed value was carried forward, irrespective of the reason for discontinuation. (NCT00903682)
Timeframe: at baseline and week 2, 6, 12, 24, 36 and 48

,
Interventionnumber of cells/L (x10^6) (Mean)
Week 2Week 6Week 12Week 24Week 36Week 48
Efavirenz72.45121.62151.46174.08180.18221.39
Etravirine69.96128.14143.24182.01213.45205.11

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Proportion of Patients With at Least 1 Treatment-emergent Grade 1-4 Central Nervous System or Psychiatric Adverse Event

"Proportion of patients with at least 1 treatment-emergent Grade 1-4 Central Nervous System or psychiatric Adverse Event, observed between Baseline through Week 12 and judged by investigator to be at least possibly related to the study drug in ETR group versus EFV group. All Adverse Events were graded according to the Division of AIDS Table for Grading the Severity of Adult and Pediatric Adverse Events (DAIDS AE grading table). Grade 1-4 covers all severities." (NCT00903682)
Timeframe: between baseline and 12 weeks

Interventionpercentage of patients (Number)
Etravirine16.5
Efavirenz46.2

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Neuropsychiatric Adverse Events by Week 48

The percentage of patients with at least 1 treatment emergent Grade 1 -4 neurologic or psychiatric adverse event, judged by the investigator to be at least possibly related to the study drug. (NCT00903682)
Timeframe: from baseline to week 48

Interventionpercentage of patients (Number)
Etravirine20.3
Efavirenz52.6

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Antiviral Activity of ETR vs. EFV

The proportion of patients with confirmed plasma viral load <50 copies/mL at Week 48 as assessed by Time to Loss of Virologic Response (TLOVR) (NCT00903682)
Timeframe: between baseline and week 48

InterventionNumber of participants (Number)
Etravirine60
Efavirenz58

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Antiviral Activity of ETR vs. EFV

The proportion of patients with confirmed plasma viral load <200 copies/mL at Week 48 as assessed by Time to Loss of Virologic Response (TLOVR) (NCT00903682)
Timeframe: between baseline and week 48

InterventionNumber of participants (Number)
Etravirine64
Efavirenz62

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Mean Change From Baseline in Neuropsychiatric and Total Tolerabililty Score

"The HIV Patient Symptoms Profile measures the tolerability of HIV treatment from the patient's perspective, using 14 concept scales in maximum 84 questions. The response options include a no or yes answer to Did symptom occur?. If yes, there is a problem scale which ranges from 1 = I had this symptom and it was not a problem to 5 = I had this symptom and it was a severe problem. A neuropsychiatric tolerability score is composed as the sum of 21 items and ranges from 0 (best) to 105 (worse). A total Tolerability score (ie, the sum of all items) ranges from 0 (best) to 420 (worse)" (NCT00903682)
Timeframe: between baseline and week 48

,
Interventionpoints on a scale (Mean)
Total Tolerability ScoreNeuropsychiatric Tolerability Score
Efavirenz-0.01-0.07
Etravirine-0.04-0.04

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Time to HIV RNA Suppression <50 Copies/mL

Number of days from ART initiation to HIV RNA suppression <50 copies/mL (NCT00924898)
Timeframe: Number of days from start of study treatment until HIV RNA suppression, assessed through week 96

Interventiondays (Median)
Acute HIV Infection Treatment Group105

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Number of Participants Without Virologic Failure at Week 48

HIV RNA level <50 copies/mL at week 48 (NCT00924898)
Timeframe: HIV RNA level at week 48 following enrollment

InterventionParticipants (Count of Participants)
Acute HIV Infection Treatment Group71

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Number of Participants Without Virologic Failure at Week 24

Number of participants with a HIV RNA level <200 copies/mL at week 24 (NCT00924898)
Timeframe: HIV RNA level prior to or at week 24 following enrollment

InterventionParticipants (Count of Participants)
Acute HIV Infection Treatment Group81

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Number of Participants With HIV RNA Suppression at Week 96

Number of participants wtih HIV RNA level <50 copies/mL at week 96 (NCT00924898)
Timeframe: HIV RNA level at 96 weeks following enrollment

InterventionParticipants (Count of Participants)
Acute HIV Infection Treatment Group65

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Number of Participants With Baseline Genotypic Resistance to One or More Antiretroviral Drugs in the Study Treatment

Baseline genotypic resistance defined as presence of any surveillance drug resistance mutation to any drug in the study treatment listed by the World Health Organization (NCT00924898)
Timeframe: At enrollment

InterventionParticipants (Count of Participants)
Acute HIV Infection Treatment Group71

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Number of Participants With Baseline Genotypic Resistance to Antiretroviral Medications

Prevalence of any of the surveillance drug resistance mutations associated with resistance to antiretroviral medications listed by the World Health Organization (NCT00924898)
Timeframe: At enrollment

InterventionParticipants (Count of Participants)
Acute HIV Infection Treatment Group17

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Relationship Between the Change From Baseline in CD4+ Cell Counts at Week 96 and the Indicated Plasma DTG PK Parameters

Relationships between plasma DTG PK parameters (AUC[0-tau] [area under the time concentration curve over the dosing interval], Cmax [maximal concentration], C0avg [average pre-dose concentration], and Ctau [concentration at the end of the dosing interval]) and the change from Baseline in CD4+ cell counts at Week 96 (calculated as the post-Baseline value minus the value at Baseline) was assessed using Pearson's correlation analyses. The Pearson's correlation coefficient is a measure of the correlation between CD4+ cell counts and plasma DTG PK parameters and ranges from -1 to 1. A value of 0 indicates no statistical association; a value close to -1 or 1 indicates a higher association.Because PK was assessed for DTG, no participants in the EFV treatment group were analyzed.Only those participants available at the specified time points were analyzed (represented by n=X in the category titles) (NCT00951015)
Timeframe: Week 96

,,,
InterventionPearson's correlation coefficient (Number)
AUC(0-tau), n=13, 14, 15, 0Cmax, n=13, 14, 15, 0C0avg, n=43, 40, 42, 0Ctau, n=13, 14, 15, 0
DTG 10 mg QD-0.100-0.047-0.009-0.289
DTG 25 mg QD0.3790.332-0.0130.299
DTG 50 mg QD0.0080.2340.206-0.074
Overall DTG-0.0050.037-0.011-0.055

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Number of Participants With Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) <50 Copies/Milliliter (c/mL) at Week 16

Plasma samples were collected for quantitative HIV-1 RNA analysis at Week 16. The analysis was performed using the time to loss of virological response (TLOVR) dataset. In the TLOVR dataset, participant responses at a specified threshold of HIV-1 RNA (<50 copies/mL) are determined by using the Food and Drug Administration's TLOVR algorithm. Using the TLOVR algorithm, participants are considered to have failed on therapy if they never achieved confirmed RNA levels below the threshold, if they had confirmed rebound of RNA above the threshold, if they made a non-permitted change in background regimen, or if they permanently discontinued investigational product for any reason. Data are reported per the Week 16 report. In later cuts of the data, the Week 16 values may have changed (because of the nature of the TLOVR algorithm).ITT-E Population included all randomized participants who received at least one dose of study medication (NCT00951015)
Timeframe: Week 16

Interventionparticipants (Number)
DTG 10 mg QD51
DTG 25 mg QD47
DTG 50 mg QD46
EFV 600 mg QD29

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Relationship Between the Change From Baseline in Plasma HIV-1 RNA at Week 2 and the Indicated Plasma DTG PK Parameters

Relationships between Week 2 plasma DTG PK parameters (AUC[0-tau] [area under the time concentration curve over the dosing interval], Cmax [maximal concentration], and Ctau [concentration at the end of the dosing interval]) and the change from Baseline in plasma HIV-1 RNA at Week 2 (calculated as the post-Baseline value minus the value at Baseline) was assessed using Pearson's correlation analyses. The Pearson's correlation coefficient is a measure of the correlation between plasma HIV-1 RNA and plasma DTG PK parameters and ranges from -1 to 1. A value of 0 indicates no statistical association; a value close to -1 or 1 indicates a higher association. Because PK was assessed for DTG, no participants in the EFV treatment group were analyzed. PK/Pharmacodynamic (PD) Analysis Population: all participants with available PD measures (e.g., safety and/or efficacy data) and with evaluable DTG plasma concentration data considered suitable for investigation of relationship with the PD measures (NCT00951015)
Timeframe: Week 2

,,,
InterventionPearson's correlation coefficient (Number)
AUC(0-tau)CmaxCtau
DTG 10 mg QD0.4260.4520.273
DTG 25 mg QD-0.018-0.051-0.100
DTG 50 mg QD-0.258-0.150-0.263
Overall DTG-0.086-0.055-0.129

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Relationship Between the Indicated Safety Parameters at Week 96 and the Indicated Plasma DTG PK Parameters

Relationships between log-transformed plasma DTG PK parameters (AUC[0-tau], Cmax, C0, C0avg, Ctau, and Cmin) and safety parameters (AE occurrence, maximum AE intensity, alanine aminotransferase [ALT], change from Baseline [CFB] in ALT, total bilirubin, CFB in total bilirubin, creatine kinase, CFB in creatine kinase, triglycerides, CFB in triglycerides, lipase, CFB in lipase, total cholesterol [TC], CFB in TC) was assessed using Pearson's correlation analyses. The Pearson's correlation coefficient is a measure of the correlation between safety parameters and plasma DTG PK parameters and ranges from -1 to 1. A value of 0 indicates no statistical association; a value close to -1 or 1 indicates a higher association. The presence of >=1 AE was used for AE occurrence. The most severe AE grade/intensity was used for maximum AE intensity. Maximum laboratory values per participant were used for safety parameters. CFB was calculated as the post-Baseline value minus the value at Baseline. (NCT00951015)
Timeframe: Week 96

InterventionPearson's correlation coefficient (Number)
AUC(0-tau) versus AE occurrence, n=45AUC(0-tau) versus maximum AE intensity, n=45AUC(0-tau) versus ALT, n=45AUC(0-tau) versus CFB in ALT, n=45AUC(0-tau) versus total bilirubin, n=45AUC(0-tau) versus CFB in total bilirubin, n=45AUC(0-tau) versus creatine kinase, n=45AUC(0-tau) versus CFB in creatine kinase, n=45AUC(0-tau) vs Triglycerides, n=45AUC(0-tau) versus CFB in triglycerides, n=45AUC(0-tau) versus lipase, n=45AUC(0-tau) versus CFB in lipase, n=45AUC(0-tau) versus total cholesterol, n=45AUC(0-tau) versus CFB in total cholesterol, n=45Cmax versus AE occurrence, n=45Cmax versus maximum AE intensity, n=45Cmax versus ALT, n=45Cmax versus CFB in ALT, n=45Cmax versus total bilirubin, n=45Cmax versus CFB in total bilirubin, n=45Cmax versus creatine kinase, n=45Cmax versus CFB in creatine kinase, n=45Cmax versus triglycerides, n=45Cmax versus CFB in triglycerides, n=45Cmax versus lipase, n=45Cmax versus CFB in lipase, n=45Cmax versus total cholesterol, n=45Cmax versus CFB in total cholesterol, n=45C0 versus AE occurrence, n=133C0 versus maximum AE intensity, n=133C0 versus ALT, n=133C0 versus CFB in ALT, n=133C0 versus total bilirubin, n=133C0 versus CFB in total bilirubin, n=133C0 versus creatine kinase, n=133C0 versus CFB in creatine kinase, n=133C0 versus triglycerides, n=133C0 versus CFB in triglycerides, n=133C0 versus lipase, n=133C0 versus CFB in lipase, n=133C0 versus total cholesterol, n=133C0 versus CFB in total cholesterol, n=133C0avg versus AE occurrence, n=140C0avg versus maximum AE intensity, n=140C0avg versus ALT, n=140C0avg versus CFB in ALT, n=140C0avg versus total bilirubin, n=140C0avg versus CFB in total bilirubin, n=140C0avg versus creatine kinase, n=140C0avg versus CFB in creatine kinase, n=140C0avg versus triglycerides, n=140C0avg versus CFB in triglycerides, n=140C0avg versus lipase, n=140C0avg versus CFB in lipase, n=140C0avg versus total cholesterol, n=140C0avg versus CFB in total cholesterol, n=140Ctau versus AE occurrence, n=45Ctau versus maximum AE intensity, n=45Ctau versus ALT, n=45Ctau versus CFB in ALT, n=45Ctau versus total bilirubin, n=45Ctau versus CFB in total bilirubin, n=45Ctau versus creatine kinase, n=45Ctau versus CFB in creatine kinase, n=45Ctau versus triglycerides, n=45Ctau versus CFB in triglycerides, n=45Ctau versus lipase, n=45Ctau versus CFB in lipase, n=45Ctau versus total cholesterol, n=45Ctau versus CFB in total cholesterol, n=45Cmin versus AE occurrence, n=45Cmin versus maximum AE intensity, n=45Cmin versus ALT, n=45Cmin versus CFB in ALT, n=45Cmin versus total bilirubin, n=45Cmin versus CFB in total bilirubin, n=45Cmin versus creatine kinase, n=45Cmin versus CFB in creatine kinase, n=45Cmin versus triglycerides, n=45Cmin versus CFB in triglycerides, n=45Cmin versus lipase, n=45Cmin versus CFB in lipase, n=45Cmin versus total cholesterol, n=45Cmin versus CFB in total cholesterol, n=45
Overall DTG0.1140.171-0.196-0.2010.3640.147-0.168-0.1450.1040.216-0.0660.092-0.097-0.1530.0610.110-0.135-0.1350.2650.033-0.188-0.1610.1340.244-0.0340.115-0.101-0.192-0.080-0.003-0.196-0.2370.2980.120-0.094-0.093-0.058-0.012-0.187-0.137-0.179-0.125-0.0280.036-0.166-0.1770.3190.109-0.114-0.1100.0570.092-0.164-0.120-0.170-0.0830.1900.205-0.281-0.2850.4460.237-0.143-0.1250.0610.172-0.1310.056-0.039-0.1080.1560.193-0.236-0.2530.4300.171-0.132-0.124-0.0420.057-0.1350.032-0.194-0.208

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Pre-dose Concentration (C0) and C0 Avg of DTG

The plasma DTG C0 of DTG was determined using limited/sparse PK sampling at Week 2, Week 12, and Week 24. C0 avg was calculated at Week 24 as the mean of the C0 of DTG at Week 2, Week 12, and Week 24. Because PK was assessed for DTG, no participants in the EFV treatment group were analyzed. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X in the category titles). Different participants may have been analyzed at different time points, so the overall number of participants analyzed reflects everyone in the PK Summary Population. (NCT00951015)
Timeframe: Week 2, Week 12, and Week 24

,,
InterventionMicrogram per milliliter (µg/mL) (Geometric Mean)
C0, Week 2, n=46, 44, 43, 0C0, Week 12, n=46, 45, 44, 0C0, Week 24, n=45, 44, 44, 0C0 avg, n=48, 46, 46, 0
DTG 10 mg QD0.310.330.330.34
DTG 25 mg QD0.570.470.570.56
DTG 50 mg QD1.201.131.201.25

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Relationship Between Gastrointestinal System Organ Class AEs of Special Interest at Week 96 and the Indicated Plasma DTG PK Parameters

Logistic regressions were performed to examine the correlation between plasma DTG PK parameters (AUC[0-tau] [area under the time concentration curve over the dosing interval], Cmax [maximal concentration], Ctau [concentration at the end of the dosing interval], and C0avg [average pre-dose concentration]) on log scales and the presence of gastrointestinal system organ class AEs (abdominal pain, diarrhea, nausea, and vomiting) at Week 96. Data are presented as estimates from logistic regression, which is a measure of the association between AEs of special interest and plasma DTG PK parameters. A value of 0 indicates no statistical association; a large absolute value of the estimate indicates higher association. Because PK was assessed for DTG, no participants in the EFV treatment group were analyzed. Results are presented for participants in any DTG group (overall DTG).Only those participants available at the specified time points were analyzed represented by n=X in the category titles (NCT00951015)
Timeframe: Week 96

Interventionestimated effect (Number)
Abdominal pain versus AUC(0-tau), n=45Abdominal pain versus Cmax, n=45Abdominal pain versus Ctau, n=45Abdominal pain versus C0avg, n=140Diarrhoea versus AUC(0-tau), n=45Diarrhoea versus Cmax, n=45Diarrhoea versus Ctau, n=45Diarrhoea versus C0avg, n=140Nausea versus AUC(0-tau), n=45Nausea versus Cmax, n=45Nausea versus Ctau, n=45Nausea versus C0avg, n=140Vomiting versus AUC(0-tau), n=45Vomiting versus Cmax, n=45Vomiting versus Ctau, n=45Vomiting versus C0avg, n=140
Overall DTG-2.49-2.98-1.72-0.41-0.62-0.98-0.290.13-0.31-0.720.03-0.32-1.29-1.61-1.15-0.89

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Plasma DTG Concentration

Blood samples for the determination of plasma DTG concentration were collected from the participants randomized to receive DTG, at the following time points: pre-dose and 2-4 hours post-dose at Weeks 2, Week 12, and Week 24. Because PK was assessed for DTG, no participants in the EFV treatment group were analyzed. The Pharmacokinetic (PK) Summary Population is comprised of all participants who received DTG and underwent intensive PK sampling or limited PK sampling during the study and provided evaluable DTG PK parameters. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X in the category titles).Different participants may have been analyzed at different time points, so the overall number of participants analyzed reflects everyone in the PK Summary Population. (NCT00951015)
Timeframe: Week 2, Week 12, and Week 24

,,
InterventionMicrograms per milliliter (µg/mL) (Mean)
Week 2, Pre-dose, n=46, 44, 43, 0Week 2, 2-4 hours post-dose, n=31, 29, 29, 0Week 12, Pre-dose, n= 46, 45, 44, 0Week 12, 2-4 hours post-dose, n=48, 45, 45, 0Week 24, Pre-dose, n=45, 44, 44, 0Week 24, 2-4 hours post-dose, n=45, 45, 45, 0
DTG 10 mg QD0.35801.01210.36481.03740.37661.0113
DTG 25 mg QD0.67791.97160.57591.79070.66361.9021
DTG 50 mg QD1.40443.84141.41693.60561.45343.5397

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Number of Participants With the Indicated Type of HIV-1 Disease Progression (AIDS or Death)

Clinical disease progression (CDP) was assessed according to the Centers for Disease Control and Prevention (CDC) HIV-1 classification system. Category (CAT) A: one or more of the following conditions (CON), without any CON listed in Categories B and C: asymptomatic HIV infection, persistent generalized lymphadenopathy, acute (primary) HIV infection with accompanying illness or history of acute HIV infection. CAT B: symptomatic CON that are attributed to HIV infection or are indicative of a defect in cell-mediated immunity; or that are considered by physicians to have a clinical course or to require management that is complicated by HIV infection; and not included among CON listed in clinical CAT C. CAT C: the clinical CON listed in the AIDS surveillance case definition. Indicators of CDP were defined as: CAT A at Baseline (BS) to CAT B event (EV), CAT A at BS to a CAT C EV; CAT B at BS to a CAT C EV; CAT C at BS to a new CAT C EV; or CAT A, B, or C at BS to death. (NCT00951015)
Timeframe: From Baseline up to Week 96

,,,
InterventionParticipants (Number)
CAT A at Baseline to a CAT C eventCAT B at Baseline to a CAT C eventCAT C at Baseline to a new CAT C eventCAT A, B, or C at Baseline to death
DTG 10 mg QD0001
DTG 25 mg QD0000
DTG 50 mg QD0100
EFV 600 mg QD0000

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Number of Participants With the Indicated Treatment-emergent Integrase (IN) Mutations Detected at the Time of Protocol-defined Virologic Failure (PDVF), as a Measure of Genotypic Resistance

For participants meeting one of the criteria for PDVF, plasma samples collected at the time point of virologic failure were tested to evaluate any potential genotypic and/or phenotypic evolution of resistance. PDVF was defined as (A) Virologic Non-response: a decrease in plasma HIV-1 RNA of <1 log10 copies/mL by Week 4, with subsequent confirmation, unless plasma HIV-1 RNA is <400 copies/mL; confirmed plasma HIV-1 RNA levels >=400 copies/mL on or after Week 24 without evidence of prior suppression to <400copies/mL or (B) Virologic Rebound: confirmed rebound in plasma HIV-1 RNA levels to >=400 copies/mL after prior confirmed suppression to <400 copies/mL; confirmed plasma HIV-1 RNA levels >0.5 log10 copies/mL above the nadir value, where nadir is the lowest HIV-1 value >=400 copies/mL.On-treatment Genotypic Resistance Population: all participants in the ITT-E Population with available on-treatment genotypic data, excluding participants who were not protocol-defined virologic failures. (NCT00951015)
Timeframe: From Baseline up to Week 96/Early Withdrawal

,,
InterventionParticipants (Number)
A23A/VS255N
DTG 10 mg QD11
DTG 25 mg QD00
EFV 600 mg QD00

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Number of Participants With the Indicated Grade 1 to Grade 4 Treatment-emergent Clinical Chemistry and Hematology Toxicities

Blood samples were collected for the measurement of clinical chemistry and hematology parameters. Toxicities were graded for severity according to the Division of AIDS (DAIDS) toxicity scales as: Grade 1 (mild), Grade 2 (moderate), Grade 3 (severe), or Grade 4 (potentially life threatening). (NCT00951015)
Timeframe: From Baseline up to Week 96/Early Withdrawal

,,,
InterventionParticipants (Number)
Alanine amino transferaseCholesterolCreatinine kinaseLipaseTriglyceridesAlkaline phosphataseAmylaseAspartate amino transferaseCarbon dioxide content/bicarbonateCreatinineHypercalcemiaHyperglycaemiaHyperkalemiaHypernatremiaHypocalcemiaHypoglycaemiaHypokalemiaHyponatremiaLow-density lipoprotein cholesterolMagnesiumPhosphate, inorganicTotal bilirubinActivated partial thromboplastin timeHemoglobinInternational normalized ratioPlatelet countProthrombin timeTotal neutrophilsWhite blood cell count
DTG 10 mg QD718171101212280016014346147937061791
DTG 25 mg QD11166131038244015015311215615412194871
DTG 50 mg QD31371121162300171155371151436061761
EFV 600 mg QD19245911049300117108431320411051514101

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Time to Maximal Drug Concentration (Tmax) of DTG

Tmax of DTG was determined using non-compartmental analysis based on intensive PK sampling at the following time points: pre-dose; 2, 3, 4, 8, and 24 hours post-dose at Week 2. Because PK was assessed for DTG, no participants in the EFV treatment group were analyzed. (NCT00951015)
Timeframe: Pre-dose and 2, 3, 4, 8, and 24 hours post-dose at Week 2

InterventionHours (Median)
DTG 10 mg QD2.0
DTG 25 mg QD2.0
DTG 50 mg QD2.0

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Number of Participants With the Indicated Treatment-emergent Major Mutations of Other Classes Detected at the Time of Protocol-defined Virologic Failure (PDVF), as a Measure of Genotypic Resistance

For participants meeting one of the criteria for PDVF, plasma samples collected at the time point of virologic failure were tested to evaluate any potential genotypic and/or phenotypic evolution of resistance. PDVF was defined as (A) Virologic Non-response: a decrease in plasma HIV-1 RNA of <1 log10 copies/mL by Week 4, with subsequent confirmation, unless plasma HIV-1 RNA is <400 copies/mL; confirmed plasma HIV-1 RNA levels >=400 copies/mL on or after Week 24 without evidence of prior suppression to <400copies/mL or (B) Virologic Rebound: confirmed rebound in plasma HIV-1 RNA levels to >=400 copies/mL after prior confirmed suppression to <400 copies/mL; confirmed plasma HIV-1 RNA levels >0.5 log10 copies/mL above the nadir value, where nadir is the lowest HIV-1 value >=400 copies/mL. (NCT00951015)
Timeframe: From Baseline up to Week 96/Early Withdrawal

InterventionParticipants (Number)
DTG 10 mg QD1
DTG 25 mg QD0
EFV 600 mg QD0

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Number of Participants With the Indicated Fold Increase in DTG FC (Fold Change in IC50 Relative to Wild-type Virus) at the Time of PDVF, as a Measure of Post-Baseline Phenotypic Resistance

The FC in IC50 (50% inhibitory concentration) for DTG relative to wild-type virus was determined for virus isolated at Baseline and at the time of PDVF. Fold increase in DTG FC at the time of PDVF was derived as the PDVF FC/Baseline FC ratio. PDVF was defined as (A) Virologic Non-response: a decrease in plasma HIV-1 RNA of <1 log10 copies/mL by Week 4, with subsequent confirmation, unless plasma HIV-1 RNA is <400 copies/mL; confirmed plasma HIV-1 RNA levels >=400 copies/mL on or after Week 24 without evidence of prior suppression to <400copies/mL or (B) Virologic Rebound: confirmed rebound in plasma HIV-1 RNA levels to >=400 copies/mL after prior confirmed suppression to <400 copies/mL; confirmed plasma HIV-1 RNA levels >0.5 log10 copies/mL above the nadir value, where nadir is the lowest HIV-1 value >=400 copies/mL.On-treatment Phenotypic Resistance Population: all participants in the ITT-E Population with available on-treatment phenotypic data (NCT00951015)
Timeframe: From Baseline up to Week 96/Early Withdrawal

,
InterventionParticipants (Number)
<1 fold1-<2 fold2-<4 fold4-<8 fold>=8 fold
DTG 10 mg QD02000
DTG 25 mg QD10000

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Viral Change Over the Initial 2 Weeks of Treatment

Plasma samples were collected for quantitative HIV-1 RNA analysis at Baseline and Week 2. Viral change is defined as the change in plasma HIV-1 RNA over the initial 2 weeks of treatment, calculated as the value at Week 2 minus the value at Baseline. Only those participants available at the specified time point were analyzed. (NCT00951015)
Timeframe: Baseline and Week 2

InterventionLog10 c/mL (Mean)
DTG 10 mg QD-2.387
DTG 25 mg QD-2.365
DTG 50 mg QD-2.392
EFV 600 mg QD-1.930

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Change From Baseline in Cluster of Differentiation 4+ (CD4+) Cell Counts at the Indicated Time Points

Blood samples were collected for lymphocyte subset assessment by flow cytometry at Baseline (Day 1), Week 1, Week 2, Week 4, Week 8, Week 12, Week 16, Week 20, Week 24, Week 32, Week 40, Week 48, Week 60, Week 72, Week 84, and Week 96. Change from Baseline was calculated as the post-Baseline value minus the value at Baseline. Only those participants available at the specified time points were analyzed (represented by n=X, X, X, X in the category titles). Different participants may have been analyzed at different time points, so the overall number of participants analyzed reflects everyone in the ITT-E Population. (NCT00951015)
Timeframe: Baseline (Day 1), Week 1, Week 2, Week 4, Week 8, Week 12, Week 16, Week 20, Week 24, Week 32, Week 40, Week 48, Week 60, Week 72, Week 84, and Week 96

,,,
InterventionCells per cubic millimeter (Median)
Week 1, n=53, 50, 48, 50Week 2, n=53, 50, 50, 47Week 4, n=53, 50, 50, 45Week 8, n=52, 50, 49, 44Week 12, n=53, 48, 48, 45Week 16, n=52, 49, 49, 44Week 20, n=52, 48, 49, 44Week 24, n=51, 49, 47, 44Week 32, n=50, 48, 47, 44Week 40, n=50, 48, 47, 44Week 48, n=51, 47, 47, 45Week 60, n=51, 48, 47, 43Week 72, n=51, 47, 48, 44Week 84, n=51, 47, 46, 42Week 96, n=48, 44, 46, 39
DTG 10 mg QD85.075.075.0118.5139.0153.0163.5159.0221.5205.0204.0265.0236.0292.0335.0
DTG 25 mg QD94.579.089.0156.5137.5176.0200.0206.0195.5204.5249.0278.0285.0313.0391.5
DTG 50 mg QD75.599.5110.0129.0171.5160.0139.0167.0203.0224.0223.0229.0220.0280.0326.0
EFV 600 mg QD42.555.089.0104.5127.0115.5136.0109.5146.5171.5174.0221.0195.0296.5301.0

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AUC(0-tau) of DTG

The area under the time concentration curve over the dosing interval (AUC[0-tau]) of DTG was determined using non-compartmental analysis based on intensive PK sampling at the following time points: pre-dose; 2, 3, 4, 8, and 24 hours post-dose at Week 2. Because PK was assessed for DTG, no participants in the EFV treatment group were analyzed. Only those participants available at the specified time points were analyzed. (NCT00951015)
Timeframe: Pre-dose and 2, 3, 4, 8, and 24 hours post-dose at Week 2

InterventionHours*µg/mL (Geometric Mean)
DTG 10 mg QD16.0
DTG 25 mg QD23.1
DTG 50 mg QD48.1

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Change From Baseline in HIV-1 RNA at the Indicated Time Points

Plasma samples were collected for quantitative HIV-1 RNA analysis at Baseline (Day 1), Week 1, Week 2, Week 4, Week 8, Week 12, Week 16, Week 20, Week 24, Week 32, Week 40, Week 48, Week 60, Week 72, Week 84, and Week 96. Change from Baseline was calculated as the post-Baseline value minus the value at Baseline. (NCT00951015)
Timeframe: Baseline (Day 1), Week 1, Week 2, Week 4, Week 8, Week 12, Week 16, Week 20, Week 24, Week 32, Week 40, Week 48, Week 60, Week 72, Week 84, and Week 96

,,,
InterventionLog10 c/mL (Mean)
Week 1, n=53, 50, 48, 50Week 2, n=53, 50, 50, 48Week 4, n=53, 50, 50, 45Week 8, n=52, 50, 49, 45Week 12, n=53, 49, 49, 45Week 16, n=52, 49, 49, 45Week 20, n=52, 48, 49, 44Week 24, n=52, 49, 48, 45Week 32, n=52, 49, 47, 45Week 40, n=51, 48, 47, 44Week 48, n=51, 48, 48, 45Week 60, n=50, 48, 48, 44Week 72, n=51, 47, 48, 44Week 84, n=51, 47, 47, 43Week 96, n=48, 44, 46, 39
DTG 10 mg QD-1.815-2.387-2.629-2.657-2.685-2.718-2.701-2.700-2.717-2.647-2.723-2.741-2.742-2.725-2.728
DTG 25 mg QD-1.773-2.365-2.583-2.666-2.671-2.668-2.662-2.657-2.658-2.665-2.667-2.675-2.622-2.670-2.680
DTG 50 mg QD-1.738-2.392-2.713-2.848-2.860-2.859-2.869-2.853-2.855-2.855-2.850-2.825-2.860-2.855-2.854
EFV 600 mg QD-1.562-1.930-2.162-2.450-2.603-2.698-2.745-2.773-2.772-2.795-2.711-2.765-2.757-2.743-2.807

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Number of Participants With Any Adverse Event (AE) and Any Serious Adverse Events (SAE)

An adverse event (AE) is defined as any untoward medical occurrence in a participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. A serious adverse event (SAE) is defined as any untoward medical occurrence that, at any dose: results in death; is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity; or is a congenital anomaly/birth defect. All clinically suspected cases of hypersensitivity reaction to abacavir in participants receiving abacavir/lamivudine were reported as SAEs. Medical or scientific judgment was to have been exercised in other situations. Refer to the general AE/SAE module for a list of AEs (occuring at a frequency threshold >=3%) and SAEs. (NCT00951015)
Timeframe: From Baseline up to Week 96/Early Withdrawal

,,,
InterventionParticipants (Number)
Any AEAny SAE
DTG 10 mg QD505
DTG 25 mg QD465
DTG 50 mg QD467
EFV 600 mg QD467

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Number of Participants With New HIV-associated Conditions of the Indicated Class

HIV-associated conditions were assessed according to the Centers for Disease Control and Prevention (CDC) HIV-1 classification system. Category (CAT) A: one or more of the following conditions (CON), without any CON listed in Categories B and C: asymptomatic HIV infection, persistent generalized lymphadenopathy, acute (primary) HIV infection with accompanying illness or history of acute HIV infection. CAT B: symptomatic CON that are attributed to HIV infection or are indicative of a defect in cell-mediated immunity; or that are considered by physicians to have a clinical course or to require management that is complicated by HIV infection; and not included among CON listed in clinical CAT C. CAT C: the clinical CON listed in the acquired immunodeficiency syndrome (AIDS) surveillance case definition. (NCT00951015)
Timeframe: From Baseline up to Week 96

,,,
InterventionParticipants (Number)
Category BCategory CDeath
DTG 10 mg QD201
DTG 25 mg QD000
DTG 50 mg QD110
EFV 600 mg QD100

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Number of Participants With Plasma HIV-1 RNA <400 c/mL

Plasma samples were collected for quantitative HIV-1 RNA analysis at Baseline (Day 1), Week 1, Week 2, Week 4, Week 8, Week 12, Week 16, Week 20, Week 24, Week 32, Week 40, Week 48, Week 60, Week 72, Week 84, and Week 96. The analysis was performed using the time to loss of virological response (TLOVR) dataset. In the TLOVR dataset, participant responses at a specified threshold of HIV-1 RNA (<400 c/mL) are determined by using the Food and Drug Administration's TLOVR algorithm. Using the TLOVR algorithm, participants are considered to have failed on therapy if they never achieved confirmed RNA levels below the threshold, if they had confirmed rebound of RNA above the threshold, if they made a non-permitted change in background regimen, or if they permanently discontinued investigational product for any reason. (NCT00951015)
Timeframe: Baseline (Day 1), Week 1, Week 2, Week 4, Week 8, Week 12, Week 16, Week 20, Week 24, Week 32, Week 40, Week 48, Week 60, Week 72, Week 84, and Week 96

,,,
InterventionParticipants (Number)
BaselineWeek 1Week 2Week 4Week 8Week 12Week 16Week 20Week 24Week 32Week 40Week 48Week 60Week 72Week 84Week 96
DTG 10 mg QD0254552525252525252505050505046
DTG 25 mg QD0204549494948484747474746464543
DTG 50 mg QD0164148494949494848484848474746
EFV 600 mg QD0152332414545454545454444434239

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Number of Participants With Plasma HIV-1 RNA <50 c/mL

Plasma samples were collected for quantitative HIV-1 RNA analysis at Baseline (Day 1), Week 1, Week 2, Week 4, Week 8, Week 12, Week 16, Week 20, Week 24, Week 32, Week 40, Week 48, Week 60, Week 72, Week 84, and Week 96. The analysis was performed using the time to loss of virological response (TLOVR) dataset. In the TLOVR dataset, participant responses at a specified threshold of HIV-1 RNA (<50 copies/mL) are determined by using the Food and Drug Administration's TLOVR algorithm. Using the TLOVR algorithm, participants are considered to have failed on therapy if they never achieved confirmed RNA levels below the threshold, if they had confirmed rebound of RNA above the threshold, if they made a non-permitted change in background regimen, or if they permanently discontinued investigational product for any reason. (NCT00951015)
Timeframe: Baseline (Day 1), Week 1, Week 2, Week 4, Week 8, Week 12, Week 16, Week 20, Week 24, Week 32, Week 40, Week 48, Week 60, Week 72, Week 84, and Week 96

,,,
InterventionParticipants (Number)
BaselineWeek 1Week 2Week 4Week 8Week 12Week 16Week 20Week 24Week 32Week 40Week 48Week 60Week 72Week 84Week 96
DTG 10 mg QD062237465051515150494848484742
DTG 25 mg QD041935454646474645454544444340
DTG 50 mg QD041131434547474746464646454645
EFV 600 mg QD0369182529384143424041403836

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Maximal Concentration (Cmax), Minimal Concentration (Cmin), and Concentration at the End of Dosing Interval (Ctau) of DTG

The Cmax, Cmax, and Ctau of DTG were determined using non-compartmental analysis based on intensive PK sampling at the following time points: pre-dose; 2, 3, 4, 8, and 24 hours post-dose at Week 2. Because PK was assessed for DTG, no participants in the EFV treatment group were analyzed. (NCT00951015)
Timeframe: Pre-dose and 2, 3, 4, 8, and 24 hours post-dose at Week 2

,,
Interventionµg/mL (Geometric Mean)
CmaxCminCtau
DTG 10 mg OD1.100.330.37
DTG 25 mg OD1.710.440.45
DTG 50 mg OD3.400.941.05

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Area Under the Concentration Versus Time Curve From Time 0 to Time t [AUC(0-t)]

The area under the plasma concentration versus time curve from time 0 to the time of the last measurable concentration (t), as calculated by the linear trapezoidal rule for efavirenz. (NCT00960570)
Timeframe: serial pharmacokinetic blood samples drawn prior to dosing on Days 1 and 31 and then 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 48, 72, 96 and 120 hours after dose administration

Interventionng-hr/mL (Mean)
Efavirenz Alone70,144.35
Efavirenz With Fenofibric Acid63,313.23

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Maximum Plasma Concentration (Cmax) of Efavirenz

The maximum or peak concentration that efavirenz reaches in the plasma. (NCT00960570)
Timeframe: serial pharmacokinetic blood samples drawn prior to dosing on Days 1 and 31 and then 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 48, 72, 96 and 120 hours after dose administration.

Interventionng/mL (Mean)
Efavirenz Alone2,461.58
Efavirenz With Fenofibric Acid2,384.79

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Area Under the Concentration Versus Time Curve From Time 0 Extrapolated to Infinity [AUC(0-∞)]

The area under the plasma concentration versus time curve from time 0 to infinity. [AUC(0-∞)] was calculated as the sum of AUC(0-t) plus the ratio of the last measurable plasma concentration to the elimination rate constant for efavirenz. (NCT00960570)
Timeframe: serial pharmacokinetic blood samples drawn immediately prior to dosing on Days 1 and 31 and then 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 48, 72, 96 and 120 hours after dose administration

Interventionng-hr/mL (Mean)
Efavirenz Alone106,689.60
Efavirenz With Fenofibric Acid96,382.08

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Percentage of Participants Without Prostate-specific Antigen Progression at 3 Months

"Prostate-specific antigen (PSA) non-progression rate is defined as the rate of patients with the absence of PSA progression.~PSA progression is defined as follows :~In patients whose PSA has not decreased, progressive disease is a 25% increase over the baseline (on-study) and an increase in the absolute-value PSA level by at least 5 ng/mL, which is confirmed by a second value.~In patients whose PSA has decreased but has not reached response criteria, progressive disease would be considered to have occurred when PSA increases 25% over the nadir, provided that the increase is a minimum of 5 ng/mL and is confirmed.~For the 3-month evaluation, patients who died within the 3 first months will be considered as progressions.~PSA assessment is to be performed every 28 days in the first 6 months after inclusion then every 3 months until progression or end of treatment. PSA assessment to establish eligibility is to be obtained from the same local laboratory using the same PSA assay." (NCT00964002)
Timeframe: 3 months

Interventionpercentage of participants (Number)
Efavirenz28.3

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Percentage of Participants Without Prostate-specific Antigen Progression at 6 Months

"Prostate-specific antigen (PSA) non-progression rate is defined as the rate of patients with the absence of PSA progression.~PSA progression is defined as follows :~In patients whose PSA has not decreased, progressive disease is a 25% increase over the baseline (on-study) and an increase in the absolute-value PSA level by at least 5 ng/mL, which is confirmed by a second value.~In patients whose PSA has decreased but has not reached response criteria, progressive disease would be considered to have occurred when PSA increases 25% over the nadir, provided that the increase is a minimum of 5 ng/mL and is confirmed.~For the 6-month evaluation, patients who died within the 6 first months will be considered as progressions.~PSA assessment is to be performed every 28 days in the first 6 months after inclusion then every 3 months until progression or end of treatment. PSA assessment to establish eligibility is to be obtained from the same local laboratory using the same PSA assay." (NCT00964002)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Efavirenz11.3

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Incidence-density of Malaria Defined as the Number of Incident Episodes of Malaria Per Time at Risk.

(NCT00978068)
Timeframe: Time from randomization to at least 24 months of follow up or until end of the study

InterventionEpisodes/ Person-Yr at Risk (Number)
Group 1: LPV/r + 2 NRTIs1.32
Group 2: Nevirapine (NVP) or Efavirenz (EFV) + 2 NRTIs2.25

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Percentage of Uncomplicated Malaria Episodes With Accompanying Adverse Events That Occurred in the 28 Days Following Antimalarial Therapy

The rates of adverse events, defined as severity grade 2 or higher that are possibly, probably or definitely related to study drugs over the course of the 28-day period after antimalarial therapy with artemether-lumefantrine (AL). (NCT00978068)
Timeframe: 28 days after antimalarial therapy

Intervention% uncomplicated malaria episodes w/ AEs (Number)
LPV/r + 2 NRTIs71.0
NVP or EFV + 2 NRTIs79.3

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28-day Risk of Recurrent Parasitemia

To assess the effect of potential interactions between ART and artemether-lumefantrine, the risks of recurrent parasitemia at 28 days were compared between the two groups. (NCT00978068)
Timeframe: 28 days after antimalarial therapy

InterventionCummulative Risk Percentage (Number)
LPV/r + 2 NRTIs14.0
NVP or EFV + 2 NRTIs40.8

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63-day Risk of Recurrent Malaria

To assess the effect of potential interactions between ART and artemether-lumefantrine, the risks of recurrent malaria at 63 days were compared between the two groups. (NCT00978068)
Timeframe: 28 days after antimalarial therapy

InterventionCumulative Risk Percentage (Number)
LPV/r + 2 NRTIs28.1
NVP or EFV + 2 NRTIs54.2

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Estimates of the 6-month Risk of a First Episode of Malaria

To assess the effect of ART independently of potential interactions with antimalarial therapy after treatment for malaria, we compared the two groups with respect to the time to the first episode of malaria. Cumulative risk was estimated using the Kaplan-Meier product-limit formula. (NCT00978068)
Timeframe: Enrollment to 6 months follow up

InterventionCumulative Risk Percentage (Number)
LPV/r + 2 NRTIs40.7
NVP or EFV + 2 NRTIs52.5

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Incidence-density of Malaria Defined as the Number of Incident Episodes of Complicated Malaria Per Time at Risk.

(NCT00978068)
Timeframe: Time from randomization to at least 24 months of follow up or until end of the study

InterventionEpisodes/ Person-Yr at Risk (Number)
Group 10.024
Group 20.026

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Prevalence of Malaria Defined as Positive Placental Blood Smear

Number of participants with positive placental blood smear for malaria (NCT00993031)
Timeframe: Delivery

Interventionparticipants (Number)
With Protease Inhibitor5
Without Protease Inhibitor6

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Prevalence of Malaria Defined as Positive Placental Blood PCR

Number of participants with positive placental blood PCR for malaria (NCT00993031)
Timeframe: Delivery

Interventionparticipants (Number)
With Protease Inhibitor6
Without Protease Inhibitor7

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Prevalence of Composite Clinical Outcome Defined by LBW, Stillbirth(Intrauterine Fetal Demise >20wks GA), Late Spontaneous Abortion(Miscarriage 12-20wks GA), Preterm Delivery(<37wks Gestation), Neonatal Death(Death of Liveborn Infant Within First 28days)

Percent of evaluated participants with composite clinical outcome defined by LBW, stillbirth (intrauterine fetal demise >20wks GA), late spontaneous abortion(miscarriage 12-20wks GA), preterm delivery(<37wks gestation), neonatal death(death of live-born infant within first 28 days) (NCT00993031)
Timeframe: Time from randomization until 24 months postpartum or cessation of breastfeeding

Intervention% of evaluated participants with outcome (Number)
With Protease Inhibitor33.9
Without Protease Inhibitor27.8

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Number of Participants With Grade 3 or 4 Toxicity in the Two Treatment Groups in Women

(NCT00993031)
Timeframe: Randomization to one month postpartum

InterventionParticipants (Count of Participants)
Without Protease Inhibitor12
With Protease Inhibitor8

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Maternal Malaria Defined as the Number of Treatments for New Episodes of Malaria Per Time at Risk After Pregnancy

(NCT00993031)
Timeframe: Number of treatments given for clinical malaria based on postive blood smear from time from delivery until 24 months after delivery or cessation of breastfeeding

Interventiontreatments (Number)
Group A21
Group B13

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Incidence of Pre-eclampsia Defined by Hypertension > 140/90 on Two Occasions Measured > 6 Hours Apart With ≥1+ Proteinuria on Clean Catch Urine Dipstick

Pre-eclampsia Defined by Hypertension > 140/90 on Two Occasions Measured > 6 Hours Apart With ≥1+ Proteinuria on Clean Catch Urine Dipstick (NCT00993031)
Timeframe: Time from randomization until delivery

InterventionParticipants (Count of Participants)
Without Protease Inhibitor0
With Protease Inhibitor0

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Change in Maternal CD4 Cell Counts

CD4 cell count recovery efavirenz at delivery (NCT00993031)
Timeframe: Time of randomization to delivery, an average of 20 weeks

InterventionCD4 cell count (Median)
Without Protease Inhibitor-7
With Protease Inhibitor57

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ART Levels in Hair Samples at Delivery

antiretroviral hair concentrations (per doubling) (NCT00993031)
Timeframe: delivery

Interventionantiretroviral hair concentration(ng/mg) (Mean)
Without Protease Inhibitor5.7
With Protease Inhibitor6.6

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Maternal Malaria Defined as the Number of Treatments for New Episodes of Malaria Per Time at Risk During Pregnancy

(NCT00993031)
Timeframe: Number of treatments given for clinical malaria based on postive blood smear from time from randomization until 24 months after delivery or cessation of breastfeeding

Interventiontreatments (Number)
With Protease Inhibitor17
Without Protease Inhibitor17

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Placental Malaria Defined Placental Histopathologic Analysis

Number of participants with positive placental histopathology slide for malaria (NCT00993031)
Timeframe: Delivery

Interventionparticipants (Number)
With Protease Inhibitor62
Without Protease Inhibitor47

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Placental Malaria Defined as Positive Placental RDT

Number of participants with positive placental RDT for malaria. Malaria rapid diagnostic tests (RDTs) assist in the diagnosis of malaria by detecting evidence of malaria parasites (antigens) in human blood. RDTs permit a reliable detection of malaria infections particularly in remote areas with limited access to good quality microscopy services. (NCT00993031)
Timeframe: Delivery

Interventionparticipants (Number)
With Protease Inhibitor6
Without Protease Inhibitor7

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Number of Participants With Severe Maternal Anemia Defined by Hemoglobin < 8g/dl at Any Point During the Trial in Each Treatment Group

Proportion of women with severe maternal Anemia (hemoglobin < 8g/dl by hemacue or CBC) at any point during the trial in Each Treatment Group (NCT00993031)
Timeframe: Time from randomization until one year follow up

InterventionParticipants (Count of Participants)
Without Protease Inhibitor11
With Protease Inhibitor11

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Number of Participants With Maternal to Child Transmission of HIV, Measured by Infant HIV DNA PCR

HIV tested by DNA PCR (NCT00993031)
Timeframe: Delivery to 48 weeks postpartum

InterventionParticipants (Count of Participants)
Without Protease Inhibitor0
With Protease Inhibitor2

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Number of Participants With Maternal HIV RNA Suppression of <400 Copies/mL

Virologic suppression was defined as plasma HIV-1 RNA 400 copies/ml or less based on the lower limit of detection of the available test. (NCT00993031)
Timeframe: Time from randomization until delivery, an average of 20 weeks

InterventionParticipants (Count of Participants)
Without Protease Inhibitor166
With Protease Inhibitor153

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Percentage of Participants With Plasma HIV-1 RNA <400 Copies/mL and <50 Copies/mL at 48 and 96 Weeks After Randomisation

Percentage of participants in each of the two treatment arms with plasma HIV-1 RNA <400 copies/mL and <50 copies/mL at 48 and 96 weeks after randomisation (NCT01011413)
Timeframe: Baseline and 2 years

,
Interventionparticipants (Number)
HIV-1 RNA <50cp/mLHIV-1 RNA <400cp/mL
600 mg Efavirenz268280
Efavirenz 400 mg277291

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Change From Baseline in Estimate Creatinine Clearance

Change from baseline to week 96 in estimate creatinine clearance between randomised treatment arms (NCT01011413)
Timeframe: Baseline and 2 years

Interventionmillilitres per minute (Mean)
600mg Efavirenz-0.17
400mg Efavirenz1.59

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Mean Change From Baseline in CD4+ T-cell Count

Mean change from baseline to week 96 in CD4+ T-cell count/mm3 between the two treatment arms (NCT01011413)
Timeframe: Baseline and 2 years

Interventioncells per mm3 (Mean)
600mg Efavirenz209
400mg Efavirenz235

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Change From Baseline in Fasted Insulin Levels

Change from baseline to week 96 in fasted insulin levels (NCT01011413)
Timeframe: Baseline and 2 years

InterventionmU per litre (Mean)
600mg Efavirenz-0.11
400mg Efavirenz0.3

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Percentage of Participants With Plasma HIV-1 RNA <200 Copies/mL 48 Weeks After Randomisation

Percentage of participants in each of the treatment arms with centrally quantified plasma HIV-1 RNA viral load <200 copies/mL 48 weeks after randomisation. (NCT01011413)
Timeframe: 48 weeks

Interventionpercentage of participants (Number)
600mg Efavirenz92.2
400mg Efavirenz94.1

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Change in Selected Serum Biochemical Parameters

Change from baseline to week 96 in alanine aminotransferase, aspartate aminotransferase and alkaline phosphatase levels between randomised treatment arms (NCT01011413)
Timeframe: Baseline and 2 years

,
InterventionUnits per Litre (Mean)
Alanine aminotransferaseAspartate aminotransferaseAlkaline phosphatase
600 mg Efavirenz6.531.7126.75
Efavirenz 400 mg0.64-1.2321.23

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Change From Baseline in Metabolic Endpoints

Change from baseline to week 96 in fasted total cholesterol, high density cholesterol and low density cholesterol, and glucose between randomised treatment arms (NCT01011413)
Timeframe: Baseline and 2 years

,
Interventionmmol per Litre (Mean)
Total cholesterol mmol/LHDL mmol/LLDL mmol/LBlood glucose mmol/L
400mg Efavirenz0.540.300.160.40
600mg Efavirenz0.620.350.210.24

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Steady-state Efavirenz Concentrations

Steady-state efavirenz mid-dosing interval plasma concentrations (NCT01011413)
Timeframe: Week 4

Interventionmilligram per Litre (Geometric Mean)
600mg Efavirenz2.85
400mg Efavirenz2.10

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Safety of ART Initiation

Incidence of Adverse Events (Grade 3,4,5) through 46-weeks, as defined by the National Institute of Allergy and Infectious Diseases, Division of AIDS toxicity classification scale, version 2009. (NCT01075152)
Timeframe: 46 weeks

Interventionparticipants (Number)
Earlier HIV Therapy73
Deferred HIV Therapy75

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Percentage of Participants, Per CSF WBC Subgroup, Who Died by Week 26

Percentage of Participants who died by week 26 based on CSF white blood cell (WBC) count at study entry (time of randomization at a median of 8 days of anti-fungal therapy). (NCT01075152)
Timeframe: 26 weeks

,
Interventionpercentage of participants (Number)
CSF WBC <5 /mcl (n=33, 31)CSF WBC >5/mcL (n=42, 40)
Deferred HIV Therapy16.145
Earlier HIV Therapy48.540.5

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Microbiologic Clearance

Microbiologic clearance of cryptococcus as measured by serial quantitative cryptococcal cultures collected at diagnosis through 14 days of amphotericin therapy. The early fungicidal activity (EFA) of the rate of clearance is expressed as log10 colony forming units (CFU) of Cryptococcus neoformans per mL of CSF per day. (NCT01075152)
Timeframe: 4 weeks

,
Interventionlog10 CFU/mL/day (Mean)
EFA by mixed effects modelEFA by linear regression
Deferred HIV Therapy-0.31-0.35
Earlier HIV Therapy-0.31-0.39

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Karnofsky Functional Status

"Functional status via Karnofsky performance status score at 4, 26, 46 weeks.~Karnofsky Scale:~100 - Normal; no complaints; no evidence of disease. 90 - Able to carry on normal activity; minor signs or symptoms of disease. 80 - Normal activity with effort; some signs or symptoms of disease. 70 - Cares for self; unable to carry on normal activity or to do active work. 60 - Requires occasional assistance, but is able to care for most of his personal needs.~50 - Requires considerable assistance and frequent medical care. 40 - Disabled; requires special care and assistance. 30 - Severely disabled; hospital admission is indicated although death not imminent.~20 - Very sick; hospital admission necessary; active supportive treatment necessary.~10 - Moribund; fatal processes progressing rapidly. 0 - Dead" (NCT01075152)
Timeframe: 46 weeks

,
InterventionScores on a scale (Mean)
4 weeks26 weeks46 weeks
Deferred HIV Therapy709395
Earlier HIV Therapy709392

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46-week Survival

46-week survival by time-to-event analysis of all subjects enrolled (NCT01075152)
Timeframe: 46 weeks

Interventionparticipants (Number)
Earlier HIV Therapy41
Deferred HIV Therapy29

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Antiretroviral Therapy Tolerability

Incidence of antiretroviral therapy interruption by >=3 consecutive days (NCT01075152)
Timeframe: 26 weeks

Interventionparticipants (Number)
Earlier HIV Therapy5
Deferred HIV Therapy1

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HIV-1 Viral Suppression

HIV-1 virologic suppression to <400 copies/mL at 26-weeks after enrollment (NCT01075152)
Timeframe: 26 weeks

Interventionparticipants (Number)
Earlier HIV Therapy43
Deferred HIV Therapy49

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Incidence of Cryptococcal-relapse

Incidence of culture positive cryptococcal meningitis relapse (NCT01075152)
Timeframe: 46 weeks

Interventionparticipants (Number)
Earlier HIV Therapy2
Deferred HIV Therapy8

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Incidence of Immune Reconstitution Inflammatory Syndrome

Incidence of cryptococcal-related immune reconstitution inflammatory syndrome through 46 weeks after enrollment. (NCT01075152)
Timeframe: 46 weeks

Interventionparticipants (Number)
Earlier HIV Therapy17
Deferred HIV Therapy9

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Mortality

Intention to treat analysis of 26 week survival of all subjects enrolled. Reported below are the numbers of participants who died by Week 26. (NCT01075152)
Timeframe: 26 weeks from study entry

Interventionparticipants (Number)
Earlier HIV Therapy40
Deferred HIV Therapy27

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Serum Levels of Efavirenz

Serum levels of efavirenz were measured on the fifth day of taking efavirenz (tablet) and the fifth day of taking an overencapsulated efavirenz. (NCT01087814)
Timeframe: 5th day of taking drug

Interventionng/mL (Mean)
Efavirenz (Tablet)5151.11
Over-encapsulated Efavirenz4965.08

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Measure Efavirenz Clearance

Effect of steady-state voriconazole on efavirenz Clearance in healthy volunteers (n=61) administered a single 100 mg oral dose of efavirenz at baseline (control phase) and after treatment with voriconazole to steady-state. (NCT01104376)
Timeframe: Baseline, 30 min, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 and 24h after efavirenz

Interventionml/min/kg (Mean)
ControlVericonazole
CYP2B645.5120.03

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Percentage of Participants With Elevated Total Cholesterol, Elevated LDL, Abnormal HDL, or Abnormal Triglycerides at 40 Weeks After Randomization

Percentage of participants with elevated total cholesterol, elevated LDL, abnormal HDL, or abnormal triglycerides at 40 weeks after randomization (NCT01146873)
Timeframe: 40 weeks

,
Interventionpercentage of participants (Number)
Elevated total cholesterolElevated LDLAbnormal HDLAbnormal triglycerides
Group 1: Lopinavir/Ritonavir (LPV/r)24.818.64.822.8
Group 2: Efavirenz (EFV)13.39.84.210.5

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Highest Grade ALT After Randomization

Highest grade ALT after randomization. Grading was determined based on the Division of AIDS (2004) Toxicity Tables to grade adverse reactions. Grading scale: 0 (none), 1 (mild), 2 (moderate), 3 (severe), 4 (potentially life-threatening). (NCT01146873)
Timeframe: through 48 weeks post randomization

,
Interventionnumber of participants (Number)
Grade 0Grade 1Grade 2Grade 3Grade 4
Group 1: Lopinavir/Ritonavir (LPV/r)1398010
Group 2: Efavirenz (EFV)120161031

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Viral Rebound

Probability of viral rebound defined as >=1 HIV RNA measurements >50 copies/ml using survival analysis by 48 weeks post-randomization. (NCT01146873)
Timeframe: 48 weeks

Interventionprobability of viral rebound (Mean)
Group 1: Lopinavir/Ritonavir (LPV/r)0.284
Group 2: Efavirenz (EFV)0.176

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Viral Failure

Probability of viral failure defined as >= 2 HIV RNA measurements >1000 copies/ml using survival analysis by 48 weeks post-randomization. (NCT01146873)
Timeframe: 48 weeks

Interventionprobability of viral failure (Mean)
Group 1: Lopinavir/Ritonavir (LPV/r)0.020
Group 2: Efavirenz (EFV)0.027

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CD4 Cell Percentage at 48 Weeks After Randomization

CD4 Cell Percentage at 48 Weeks After Randomization (NCT01146873)
Timeframe: 48 weeks

Interventionpercentage of cells (Mean)
Group 1: Lopinavir/Ritonavir (LPV/r)34.7
Group 2: Efavirenz (EFV)37.5

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Rates of Grade 2 and Higher Alanine Aminotransferase (ALT) Elevations

To estimate the rates of grade 2*and higher ALT elevations in the two regimens. (NCT01147107)
Timeframe: over week 72

InterventionParticipants (Count of Participants)
Raltegravir Based Therapy24
Efavirenz Based Therapy30

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The Rate of Neuropsychiatric and Central Nervous System (CNS) Toxicity of Raltegravir Therapy After 12 Weeks on Treatment

"The rate of neuropsychiatric and central nervous system (CNS) toxicity as measured after 12 weeks of raltegravir therapy as measured by :~Sleep questionnaire~CNS toxicity (as determined by questionnaire based on efavirenz SPC and graded based on the ACTG adverse event scale)" (NCT01195467)
Timeframe: baseline to week 12

Interventionpercentage of improvement in sleep score (Number)
Single Arm25

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The Rate of Neuropsychiatric and Central Nervous System (CNS) Toxicity of Raltegravir Therapy After 4 Weeks on Treatment

To assess the rate of neuropsychiatric and central nervous system (CNS) toxicity as measured from baseline to 4 weeks of raltegravir therapy as measured by sleep questionnaire & CNS toxicity (as determined by questionnaire based on efavirenz SPC and graded based on the ACTG adverse event scale) (NCT01195467)
Timeframe: 4 weeks

Interventionpercentage improvement in CNS score (Number)
Single Arm26

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Change From Baseline (Day 1) in Plasma HIV-1 RNA Over Period

For summaries and analyses which use HIV-1 RNA level as a continuous measure, the logarithm to base 10 of the value was used. In cases where a sample was retested, the retest value was used. Baseline was defined as the value recorded on Day 1. Change from Baseline is the value at indicated time point minus the Baseline value. Data for participants prior to switch and after the switch has been presented. (NCT01231555)
Timeframe: Baseline (Day 1) up to Week 16

Interventionlog10 copies per milliliter (Mean)
Before switch, Week 2Before switch, Week 4Before switch, Week 8Baseline switchAfter switch, Week 1After switch, Week 2After switch, Week 4
GSK2248761 200 mg Once Daily-2.018-2.134-2.712-2.170-2.287-2.235-2.482

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Number of Participants Discontinuing the Study Drugs Due to AEs

Adverse event (AE) is an unfavorable change in the health of a participant, including abnormal laboratory findings, that happens during a clinical study or within a certain time period after the study has ended. This change may or may not be caused by the intervention being studied. Number of participants quitting/ prematurely discontinuing the use of study drug(s) were recorded. (NCT01231555)
Timeframe: Up to 20 weeks

InterventionParticipants (Count of Participants)
GSK2248761 100 mg Once Daily0
GSK2248761 200 mg Once Daily0
EFV 600 mg Once Daily0

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Change From Baseline (Day 1) in Plasma HIV-1 RNA Over Period

For summaries and analyses which use HIV-1 RNA level as a continuous measure, the logarithm to base 10 of the value was used. In cases where a sample was retested, the retest value was used. Baseline was defined as the value recorded on Day 1. Change from Baseline is the value at indicated time point minus the Baseline value. Data for participants prior to switch and after the switch has been presented. (NCT01231555)
Timeframe: Baseline (Day 1) up to Week 16

Interventionlog10 copies per milliliter (Mean)
Before switch, Week 2Before switch, Week 4Before switch, Week 8Before switch, Week 12
EFV 600 mg Once Daily-2.131-2.334-2.723-2.866

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Number of Participants With HIV Disease Progression

Number of participants acquiring clinical disease progression or death during the treatment period were presented. Clinical disease progression was defined as the progression from Baseline (Day 1) HIV disease status in either of these categories; CDC Category A at baseline to CDC Category B event, CDC Category A at baseline to CDC Category C event, CDC Category B at baseline to CDC Category C event, CDC Category C at baseline to new CDC Category C event, CDC Category A, B or C at baseline to death. If no change occurs, it was termed as no disease progression. (NCT01231555)
Timeframe: Up to 20 Weeks

InterventionParticipants (Count of Participants)
GSK2248761 100 mg Once Daily0
GSK2248761 200 mg Once Daily0
EFV 600 mg Once Daily0

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Minimum and Maximum Plasma GSK2248761 Concentration at Week 2

"Maximum observed plasma concentration and minimum observed plasma concentration of GSK2248761 was recorded on Week 2. The PK parameters were calculated by standard non-compartmental analysis according to current working practices and using WinNonlin Pro 4.1 or higher. Log transformed values have been presented.~All calculations of non-compartmental parameters were based on actual sampling times." (NCT01231555)
Timeframe: At Week 2

,
Interventionmicrograms per milliliter (Geometric Mean)
CminCmax
GSK2248761 100 mg Once Daily0.151.78
GSK2248761 200 mg Once Daily0.493.70

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Number of Participants With Serious Adverse Events (SAEs) and Adverse Events (AEs)

Adverse event (AE) is an unfavorable change in the health of a participant, including abnormal laboratory findings, that happens during a clinical study or within a certain time period after the study has ended. This change may or may not be caused by the intervention being studied. Serious adverse event (SAE) is an adverse event that results in death, is life-threatening, requires inpatient hospitalization or extends a current hospital stay, results in an ongoing or significant incapacity or interferes substantially with normal life functions, or causes a congenital anomaly or birth defect. Medical events that do not result in death, are not life-threatening, or do not require hospitalization may be considered serious adverse events if they put the participant in danger or require medical or surgical intervention to prevent one of the results listed above. (NCT01231555)
Timeframe: Up to 20 Weeks

,,
InterventionParticipants (Count of Participants)
Any SAEAny AE
EFV 600 mg Once Daily18
GSK2248761 100 mg Once Daily18
GSK2248761 200 mg Once Daily05

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Number of Participants With Plasma HIV-1 RNA Below 50 Copies/mL as a Function of Viral Load

"This analysis was based on the Missing, Switch or Discontinuation equals Failure (MSDF) algorithm (as codified by the FDA's snapshot algorithm) and was adjusted for stratification factors and stage of recruitment. Dose selection was based primarily on antiviral activity and tolerability in conjunction with immunologic, safety, virologic resistance and pharmacokinetic (PK) measures. The efficacy decision criteria was based on an observed difference of >=8% between the two GSK2248761 dosage arms." (NCT01231555)
Timeframe: Up to Week 16

InterventionParticipants (Count of Participants)
Before switch, Week 4Before switch, Week 8After switch, Baseline switchAfter switch, Week 1After switch, Week 2After switch, Week 4
GSK2248761 200 mg Once Daily011111

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Number of Participants With HIV Associated Conditions

HIV associated condition included recurrence of previous conditions. Centre for disease control (CDC) associated conditions and non-CDC associated conditions were planned to be monitored. (NCT01231555)
Timeframe: Up to 20 Weeks

InterventionParticipants (Count of Participants)
GSK2248761 100 mg Once Daily0
GSK2248761 200 mg Once Daily0
EFV 600 mg Once Daily0

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Number of Participants With Plasma HIV-1 RNA Below 50 Copies/mL as a Function of Viral Load

"This analysis was based on the Missing, Switch or Discontinuation equals Failure (MSDF) algorithm (as codified by the FDA's snapshot algorithm) and was adjusted for stratification factors and stage of recruitment. Dose selection was based primarily on antiviral activity and tolerability in conjunction with immunologic, safety, virologic resistance and pharmacokinetic (PK) measures. The efficacy decision criteria was based on an observed difference of >=8% between the two GSK2248761 dosage arms." (NCT01231555)
Timeframe: Up to Week 16

InterventionParticipants (Count of Participants)
Before switch, Week 4Before switch, Week 8Before switch, Week 12
EFV 600 mg Once Daily332

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Number of Participants With Changes in Electrocardiogram (ECG) From Baseline (Day 1) Over 16 Weeks

The QTc interval was assessed by two methods Bazzette's method (QTc[b]) and Federica's method (QTc[f]). Baseline value was recorded at Day 1. Change from Baseline is the value at indicated time point minus the Baseline value. Change from Baseline values were categorized into <30 milliseconds (msec), >=30 but <60 msec, and >=60 msec. The data has been presented for QTcB and QTcF for participants prior to switching the therapy. (NCT01231555)
Timeframe: Baseline (Day 1) to 16 weeks

InterventionParticipants (Count of Participants)
QTcB, Week 2, <30 msecQTcB, Week 2, >=30 to <60 msecQTcB, Week 4, <30 msecQTcB, Week 12, <30 msecQTcF, Week 2, <30 msecQTcF, Week 4, <30 msecQTcF, Week 12, <30 msecQTcF, Week 12, >=30 to <60
EFV 600 mg Once Daily71638621

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Number of Participants With Changes in Electrocardiogram (ECG) From Baseline (Day 1) Over 16 Weeks

The QTc interval was assessed by two methods Bazzette's method (QTc[b]) and Federica's method (QTc[f]). Baseline value was recorded at Day 1. Change from Baseline is the value at indicated time point minus the Baseline value. Change from Baseline values were categorized into <30 milliseconds (msec), >=30 but <60 msec, and >=60 msec. The data has been presented for QTcB and QTcF for participants prior to switching the therapy. (NCT01231555)
Timeframe: Baseline (Day 1) to 16 weeks

,
InterventionParticipants (Count of Participants)
QTcB, Week 2, <30 msecQTcB, Week 2, >=30 to <60 msecQTcB, Week 4, <30 msecQTcF, Week 2, <30 msecQTcF, Week 4, <30 msec
GSK2248761 100 mg Once Daily60464
GSK2248761 200 mg Once Daily50454

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Change From Baseline (Day 1) in Plasma HIV-1 RNA Over Period

For summaries and analyses which use HIV-1 RNA level as a continuous measure, the logarithm to base 10 of the value was used. In cases where a sample was retested, the retest value was used. Baseline was defined as the value recorded on Day 1. Change from Baseline is the value at indicated time point minus the Baseline value. Data for participants prior to switch and after the switch has been presented. (NCT01231555)
Timeframe: Baseline (Day 1) up to Week 16

Interventionlog10 copies per milliliter (Mean)
Before switch, Week 2Before switch, Week 4Baseline switchAfter switch, Week 1After switch, Week 2After switch, Week 4
GSK2248761 100 mg Once Daily-1.863-2.140-2.046-2.218-2.307-2.380

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Number of Participants With Plasma HIV-1 RNA Below 50 Copies/mL as a Function of Viral Load

"This analysis was based on the Missing, Switch or Discontinuation equals Failure (MSDF) algorithm (as codified by the FDA's snapshot algorithm) and was adjusted for stratification factors and stage of recruitment. Dose selection was based primarily on antiviral activity and tolerability in conjunction with immunologic, safety, virologic resistance and pharmacokinetic (PK) measures. The efficacy decision criteria was based on an observed difference of >=8% between the two GSK2248761 dosage arms." (NCT01231555)
Timeframe: Up to Week 16

InterventionParticipants (Count of Participants)
Before switch, Week 4After switch, Baseline switchAfter switch, Week 1After switch, Week 2After switch, Week 4
GSK2248761 100 mg Once Daily11332

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Change From Baseline in CD4+ Lymphocyte Counts (Absolute) at 192 Weeks From Day 1 of the Parent Protocol

Participant's immunological status assessed by CD4+ lymphocyte count (absolute and percentage) at 192 weeks from Day 1 of the parent protocol. (NCT01254656)
Timeframe: 192 Weeks from Day 1 of the parent protocol

Interventioncells/uL (Mean)
Lersivirine (LRV) 500 mg308
LRV 750 mg304
Efavirenz (EFV) 600 mg300

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Change From Baseline in CD4+ Lymphocyte Counts (Absolute) at 144 Weeks From Day 1 of the Parent Protocol

Participant's immunological status assessed by CD4+ lymphocyte count (absolute and percentage) at 48 weeks (ie, 144 weeks from Day 1 of the parent protocol) (NCT01254656)
Timeframe: 144 Weeks from Day 1 of the parent protocol

Interventioncells/uL (Mean)
Lersivirine (LRV) 500 mg293
LRV 750 mg302
Efavirenz (EFV) 600 mg303

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Change From Baseline in CD4+ Lymphocyte Counts (Percentage) at 144 Weeks From Day 1 of the Parent Protocol

Participant's immunological status assessed by CD4+ lymphocyte count (absolute and percentage) at 48 weeks (ie, 144 weeks from Day 1 of the parent protocol) (NCT01254656)
Timeframe: 144 Weeks from Day 1 of the parent protocol

InterventionPercentage (Mean)
Lersivirine (LRV) 500 mg13
LRV 750 mg13
Efavirenz (EFV) 600 mg13

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Change From Baseline in CD4+ Lymphocyte Counts (Percentage) at 192 Weeks From Day 1 of the Parent Protocol

Participant's immunological status assessed by CD4+ lymphocyte count (absolute and percentage) at 192 weeks from Day 1 of the parent protocol. (NCT01254656)
Timeframe: 192 Weeks from Day 1 of the parent protocol

InterventionPercentage (Mean)
Lersivirine (LRV) 500 mg13
LRV 750 mg15
Efavirenz (EFV) 600 mg12

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Number of Participants With Plasma HIV-1 RNA Level <50 Copies/mL up to Week 208

Number of participants with HIV-1 RNA level <50 copies/mL plasma was summarized at last visit. Abbott RealTime HIV-1 assay was used to measure the HIV-1 RNA level. (NCT01254656)
Timeframe: Up to Week 208

InterventionParticipants (Number)
Lersivirine (LRV) 500 mg39
LRV 750 mg38
Efavirenz (EFV) 600 mg13

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Number of Participants With Plasma Human Immunodeficiency Virus - 1 (HIV-1) Ribonucleic Acid (RNA) Level <50 Copies/mL at 144 Weeks From Day 1 of the Parent Protocol

Number of participants with HIV-1 RNA level <50 copies/mL plasma was summarized at 48 weeks i.e. 144 weeks from Day 1 of the parent protocol. Roche Amplicor HIV-1 Monitor assay was used to measure the HIV-1 RNA level. (NCT01254656)
Timeframe: 144 Weeks from Day 1 of the parent protocol

InterventionParticipants (Number)
Lersivirine (LRV) 500 mg40
LRV 750 mg40
Efavirenz (EFV) 600 mg16

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Virology Analysis Participant Accountability From Week 96 Through Study Termination

"Virology analysis included virus susceptibility (phenotype and genotype)to a standard panel of approved antiretrovirals as determined by the Monogram Biosciences PhenoSense GT assay. Below analysis table included the following parameters: 1. protocol-defined treatment failure was defined as an increase in HIV-1 RNA to detectable levels (≥50 copies/mL) on 2 consecutive measurements, the second measurement taken no more than 14 days after the first measurement); 2. Treatment failure: treatment failure (both virologic and non-virologic) was defined as a subject who met the protocol-defined treatment failure criterion or discontinued from the study; 3. NRTI or NNRTI resistance mutations: nucleoside reverse transcriptase inhibitor or lersivirine-associated resistance-associated mutations (RAM) based on the International AIDS Society-USA (IAS-USA) RAM guidelines; 4. 'with result' meant an analyzed sample returned genotypic result or phenotypic result or both." (NCT01254656)
Timeframe: Week 96 through study termination

,,
InterventionParticipants (Number)
Treatment failure (TF)Protocol defined treatment failureTF analysed - HIV-1 RNA >500 c/mLTF analysed - HIV-1 RNA >500 c/mL with resultTF analysed - HIV-1 RNA <= 500 c/mLTF analysed - HIV-1 RNA <= 500 c/mL with resultNRTI or NNRTI resistance mutations
Efavirenz (EFV) 600 mg5000200
Lersivirine (LRV) 500 mg8411520
LRV 750 mg5300210

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Change in Flow-mediated Dilation (FMD) of the Brachial Artery

Change in FMD is a measure of change in endothelial function (NCT01270802)
Timeframe: Baseline and 24 weeks

Intervention% change from baseline (Mean)
Continued Tenofovir/Emtricitabine/Efavirenz-0.67
Switch to Tenofovir/Emtricitabine Plus Raltegravir-0.1

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Change in Serum Levels of Vitamin D

Change in serum levels of 24-OH-vitamin D provide a measure of the amount of change in vitamin D in the body (NCT01270802)
Timeframe: Baseline and 24 weeks

Interventionng/mL (Mean)
Continued Tenofovir/Emtricitabine/Efavirenz0.06
Switch to Tenofovir/Emtricitabine Plus Raltegravir0.14

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Percentage of Participants With Etoposide Dose Modification

Etoposide (ET) was administered for a maximum of 8 cycles (16 weeks) from study entry (Arm B) or from Step 2 entry (Arm A). Dose modifications were reported as temporarily held, resumed at a different dose, deferred, prematurely discontinued and underdosed. The percentage of participants who experienced each dose modification is provided in the data table below. The categories are not mutually exclusive. A participant may have experienced multiple dose modifications and may be counted in more than one category. Each participant is counted at most once within category. (NCT01352117)
Timeframe: From ET dispensation to ET discontinuation (total duration of ET was up to 16 weeks)

,
Interventionpercentage of participants (Number)
Temporarily heldResumed at a different doseDeferredDiscontinuedUnderdosed
Arm A: ART With Delayed ET (Step 2)015.637.56.30
Arm B: ART With Immediate ET5.29.424.010.41.0

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Percentage of Participants With HIV-1 RNA Suppression

HIV-1 RNA suppression was defined as plasma HIV-1 RNA <400 copies/mL. Only Arm A participants could enter Step 2 to initiate delayed ET. (NCT01352117)
Timeframe: Entry and Weeks 12, 24, 32, 48, 72, 96; Step 2 entry and Weeks 12, 24, 32, 48 and 72.

Interventionpercentage of participants (Number)
Entry: HIV-1 RNA suppressionWeek 12: HIV-1 RNA suppressionWeek 24: HIV-1 RNA suppressionWeek 32: HIV-1 RNA suppressionWeek 48: HIV-1 RNA suppressionWeek 72: HIV-1 RNA suppressionWeek 96: HIV-1 RNA suppressionStep 2 entry: HIV-1 RNA suppressionStep 2 Week 12: HIV-1 RNA suppressionStep 2 Week 24: HIV-1 RNA suppressionStep 2 Week 32: HIV-1 RNA suppressionStep 2 Week 48: HIV-1 RNA suppressionStep 2 Week 72: HIV-1 RNA suppression
Arm A: ART Alone or With Delayed ET4.390.394.592.095.391.292.993.3100.095.896.0100.0100.0

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Percentage of Participants With HIV-1 RNA Suppression

HIV-1 RNA suppression was defined as plasma HIV-1 RNA <400 copies/mL. Only Arm A participants could enter Step 2 to initiate delayed ET. (NCT01352117)
Timeframe: Entry and Weeks 12, 24, 32, 48, 72, 96; Step 2 entry and Weeks 12, 24, 32, 48 and 72.

Interventionpercentage of participants (Number)
Entry: HIV-1 RNA suppressionWeek 12: HIV-1 RNA suppressionWeek 24: HIV-1 RNA suppressionWeek 32: HIV-1 RNA suppressionWeek 48: HIV-1 RNA suppressionWeek 72: HIV-1 RNA suppressionWeek 96: HIV-1 RNA suppression
Arm B: ART With Immediate ET4.290.697.594.798.696.693.8

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Cumulative Incidence of Initial KS Partial or Complete Response by Week 96

KS partial response (PR) or complete response (CR) compared to study entry based on clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). Cumulative incidence was estimated with death and initiation of delayed KS treatment (alternate KS treatment or delayed ET in Arm A) as competing risks. Time at risk was censored at the end of Step 1 (Week 96 or premature study discontinuation) or on the date when the DSMB's recommendation to close the study became public, whichever occurred earlier. (NCT01352117)
Timeframe: From entry through 96 weeks

Interventioncumulative events per 100 participants (Number)
Arm A: ART Alone Period (Step 1)39.89
Arm B: ART With Immediate ET64.08

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Cumulative Incidence of Initial KS Progressive Disease by Week 96

KS progressive disease (PD) compared to study entry or best response based on clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). Cumulative incidence was estimated with death and initiation of alternate KS treatment as competing risks. Time at risk was censored at the end of Step 1 (Week 96 or premature study discontinuation) or on the date when the DSMB's recommendation to close the study became public, whichever occurred earlier. (NCT01352117)
Timeframe: From entry through 96 weeks

Interventioncumulative events per 100 participants (Number)
Arm A: ART Alone Period (Step 1)60.61
Arm B: ART With Immediate ET52.73

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Cumulative Incidence of KS Progressive Disease After Initiation of Delayed Etoposide in Arm A

KS progressive disease (PD) compared to Step 2 entry (prior to initiation of delayed ET) or Step 2 best response based on clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). Cumulative incidence was estimated with death and initiation of alternate KS treatment as competing risks. Time at risk was censored at the end of Step 2 (at up to 84 weeks or premature study discontinuation) or on the date when the DSMB's recommendation to close the study became public, whichever occurred earlier. (NCT01352117)
Timeframe: From initiation of etoposide (Step 2 entry) to up to 84 weeks (end of Step 2)

Interventioncumulative events per 100 participants (Number)
Arm A: ART With Delayed ET Period (Step 2)35.78

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Cumulative Incidence of KS Response After Initiation of Delayed Etoposide in Arm A

KS response, partial or complete (PR or CR) compared to Step 2 entry (prior to initiation of delayed ET) based on clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). Cumulative incidence was estimated with death and initiation of alternate KS treatment as competing risks. Time at risk was censored at the end of Step 2 (at up to 84 weeks or premature study discontinuation) or on the date when the DSMB's recommendation to close the study became public, whichever occurred earlier. (NCT01352117)
Timeframe: From initiation of etoposide (Step 2 entry) to up to 84 weeks (end of Step 2)

Interventioncumulative events per 100 participants (Number)
Arm A: ART With Delayed ET Period (Step 2)62.57

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Cumulative Incidence of KS-IRIS

KS-IRIS was defined as KS progressive disease that occurs within 12 weeks of initiation of ART that is associated with an increase in peripheral blood CD4+ lymphocyte cell count of at least 50 cells/mm^3 above the study screening value and/or a decrease in the HIV RNA level by at least 0.5 log10 below the study entry value prior to, or at the time of, documented KS progressive disease. Cumulative incidence was estimated with death and initiation of alternate KS treatment as competing risks. Time at risk was censored (1) when lost to follow-up, (2) at the study visit following Week 12 or (3) on the date when the DSMB's recommendation to close the study became public, whichever occurred earlier. Time of KS-IRIS was defined as the time of the initial KS progressive disease. (NCT01352117)
Timeframe: From study entry to Week 12

Interventioncumulative events per 100 participants (Number)
Arm A: ART Alone or With Delayed ET23.14
Arm B: ART With Immediate ET7.40

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Number of Participants With Grade 3 or Higher Adverse Events

Number of participants who experienced an AE (sign/symptom or laboratory abnormality) of Grade 3 or higher. The AEs were graded by the clinicians according to the Division of AIDS (DAIDS) AE Grading Table (see reference in the Protocol Section) as follows: Grade 1=Mild, Grade 2=Moderate, Grade 3=Severe, Grade 4=Potentially Life-Threatening. (NCT01352117)
Timeframe: From study treatment dispensation through up to Week 96, until long-term follow-up began in Step 3 or until study discontinuation.

InterventionParticipants (Count of Participants)
Arm A: ART Alone or With Delayed ET47
Arm B: ART With Immediate ET42

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Change in Peripheral Blood CD4+ Lymphocyte Cell Count

Absolute change in CD4+ cell count was calculated as value at a given visit minus the value at study screening in Step 1, and as value at a given visit minus Step 2 entry in Step 2. Only participants in Arm A could enter Step 2 to initiate delayed ET. (NCT01352117)
Timeframe: Screening and Weeks 12, 24, 32, 48, 72, 96; Step 2 entry and Weeks 12, 24, 32, 48 and 72.

Interventioncells/mm^3 (Median)
Week 12: CD4 changeWeek 24: CD4 changeWeek 32: CD4 changeWeek 48: CD4 changeWeek 72: CD4 changeWeek 96: CD4 changeStep 2 Week 12: CD4 changeStep 2 Week 24: CD4 changeStep 2 Week 32: CD4 changeStep 2 Week 48: CD4 changeStep 2 Week 72: CD4 change
Arm A: ART Alone or With Delayed ET405790125143149-13-1528251

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Change in Peripheral Blood CD4+ Lymphocyte Cell Count

Absolute change in CD4+ cell count was calculated as value at a given visit minus the value at study screening in Step 1, and as value at a given visit minus Step 2 entry in Step 2. Only participants in Arm A could enter Step 2 to initiate delayed ET. (NCT01352117)
Timeframe: Screening and Weeks 12, 24, 32, 48, 72, 96; Step 2 entry and Weeks 12, 24, 32, 48 and 72.

Interventioncells/mm^3 (Median)
Week 12: CD4 changeWeek 24: CD4 changeWeek 32: CD4 changeWeek 48: CD4 changeWeek 72: CD4 changeWeek 96: CD4 change
Arm B: ART With Immediate ET67121119121125206

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Percentage of Participants With ARV Dose Modification

ARV dose modifications were reported as temporarily held, prematurely discontinued and increased. The percentage of participants who experienced each dose modification is provided in the data table below. The categories are not mutually exclusive. A participant may have experienced multiple dose modifications and may be counted in more than one category. Each participant is counted at most once within category. (NCT01352117)
Timeframe: From treatment dispensation to Week 96

,
Interventionpercentage of participants (Number)
Temporarily heldPrematurely discontinuedIncreased
Arm A: ART Alone or With Delayed ET7.426.61.1
Arm B: ART With Immediate ET11.521.90

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Cumulative Probability of Death by Week 24

The Kaplan-Meier estimate of cumulative probability of death by week 24 (NCT01380080)
Timeframe: From study entry to week 24

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric4.8
Arm B: IPT5.2

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Cumulative Probability of Death or AIDS Progression by Week 24

The Kaplan-Meier estimate of the cumulative probability of death or AIDS progression by week 24. AIDS progression was defined as new WHO stage 3 or 4 conditions occurred after study entry. (NCT01380080)
Timeframe: From study entry to week 24

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric17.1
Arm B: IPT12.5

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Cumulative Probability of Death or AIDS Progression by Week 48

The Kaplan-Meier estimate of the cumulative probability of death or AIDS progression by week 48. AIDS progression was defined as new WHO stage 3 or 4 conditions occurred after study entry. (NCT01380080)
Timeframe: From study entry to week 48

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric19.3
Arm B: IPT15.3

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CD4+ T-cell Count Change From Baseline

Change was calculated as the CD4+ T-cell count at the later weeks (4, 24 and 48) minus the baseline (week 0) CD4+ T-cell count. (NCT01380080)
Timeframe: Weeks 0, 4, 24 and 48

,
Interventioncells/ mm^3 (Median)
Week 4Week 24Week 48
Arm A: Empiric4996158
Arm B: IPT54102146

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Proportion of Participants With HIV-1 RNA Level <400 Copies/mL

Proportion of participants with HIV-1 RNA level <400 copies/mL. (NCT01380080)
Timeframe: At weeks 0, 4, 24, and 48

,
InterventionProportion of participants (Number)
Week 0Week 4Week 24Week 48
Arm A: Empiric00.460.840.87
Arm B: IPT0.010.490.850.89

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CD4+ T-cell Count

The absolute levels of CD4+ T-cell counts (cells/mm^3) (NCT01380080)
Timeframe: At weeks 0, 4, 24, and 48

,
Interventioncells/ mm^3 (Median)
Week 0Week 4Week 24Week 48
Arm A: Empiric1874121176
Arm B: IPT1976121172

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Time to Initiation of TB Treatment by Week 96

Median time to TB treatment initiation since study entry (NCT01380080)
Timeframe: From study entry to week 96

InterventionDays (Median)
Arm A: Empiric0
Arm B: IPT0

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Proportion of Participants With TB Diagnosis by Week 96

Proportion of participants with TB diagnosis per current ACTG Diagnosis Appendix 60 by week 96 (NCT01380080)
Timeframe: From study entry to week 96

InterventionProportion of participants (Number)
Arm A: Empiric0.08
Arm B: IPT0.05

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Proportion of Participants With Reportable Hospitalization by Week 48

Proportion of participants with reportable hospitalization reported by Week 48 (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.10
Arm B: IPT0.12

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Proportion of Participants With Immune Reconstitution Inflammatory Syndrome (IRIS) by Week 48

Proportion of participants with IRIS (using current ACTG definition Appendix 60, see References) by Week 48. IRIS in participants with TB and other opportunistic infections may occur shortly after the initiation of potent combination ART, particularly in participants with advanced HIV disease. (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.04
Arm B: IPT0.05

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Proportion of Participants With at Least One New Grade 3 or 4 Targeted Laboratory Value That is at Least a One-grade Increase From Baseline by Week 48

"Proportion of participants with at least one new Grade 3 or 4 that is at least a one-grade increase from baseline for the following targeted laboratory values by Week 48~The targeted laboratory events include hemoglobin, serum creatinine, ALT and AST" (NCT01380080)
Timeframe: From study entry to week 48. The lab events were collected at study entry, weeks 2, 4, 8, 12, 16, 20, 24, and 48.

InterventionProportion of participants (Number)
Arm A: Empiric0.11
Arm B: IPT0.13

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Proportion of Participants With at Least One New Grade 3 or 4 Adverse Event That is at Least a One-grade Increase From Baseline by Week 48

Proportion of participants with at least one new Grade 3 or 4 laboratory or sign or symptom that is at least a one-grade increase from baseline by Week 48. Grade 3=Severe, Grade 4=Life-Threatening according to DAIDS AE Grading Table (see references). (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.32
Arm B: IPT0.30

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Proportion of Participants Who Prematurely Discontinued Antiretroviral Therapy by Week 48

Proportion of participants with premature discontinuation of antiretroviral therapy (ART) by Week 48 (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.19
Arm B: IPT0.21

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Proportion of Participants Who Prematurely Discontinued Any Component of TB Treatment by Week 48

Proportion of participants with premature discontinuation of any component of TB treatment by Week 48 (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.13
Arm B: IPT0.05

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Cumulative Probability of First AIDS Progression by Week 96

The Kaplan-Meier estimate of the cumulative probability of first AIDS progression which was defined as the identification of a new World Health Organization (WHO) stage 3 or 4 condition (NCT01380080)
Timeframe: From study entry to week 96

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric16.6
Arm B: IPT11.3

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Cumulative Probability of Death or Unknown Vital Status by Week 24

"The Kaplan-Meier estimate of the cumulative probability of death or unknown vital status by week 24.~The vital status was considered unknown at week 24 if a participant prematurely discontinued from the study before week 24 and no vital status was obtained at week 48." (NCT01380080)
Timeframe: From study entry to week 24

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric5.2
Arm B: IPT5.2

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The Antiretroviral Treatment Failure Rate at 12 Months.

Treatment failure is defined as viral load > 50 copies/ml, antiretroviral regimen changes for treatment failure or death (NCT01387022)
Timeframe: 12 months post ART intiation or until time of death

Interventionparticipants (Number)
Tenofovir-containing Regimen4
Tenofovir-sparing Regimen5

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Tenofovir Resistance, Defined as Presence of K65R, K70E or Any of the TAMS Mutations

(NCT01387022)
Timeframe: From randomisation until either time of termination or time of death

InterventionParticipants (Count of Participants)
Tenofovir-containing Regimen1
Tenofovir-sparing Regimen1

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Reported Adverse Events With Severity Grades 3 and 4 Based on the DAIDS Toxicity Grading Tables

(NCT01387022)
Timeframe: From randomisation until either time of termination or time of death

InterventionParticipants (Count of Participants)
Tenofovir-containing Regimen7
Tenofovir-sparing Regimen12

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Change in CD4+ Cell Count From Randomisation to 12 Months Post-randomisation

Difference between 12 months and randomisation CD4+ count was calculated and then summarised (NCT01387022)
Timeframe: Measured at 12 months post ART initiation

Interventioncells/uL (Median)
Tenofovir-containing Regimen217
Tenofovir-sparing Regimen174

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AUC

Area under the plasma concentration time curve, determined using a non-compartmental approach by means of the Phoenix WinNonlin software application. Time points for sample collection were 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 h (NCT01410058)
Timeframe: Baseline (day 22), Post-moringa (day 35)

,
Interventionh*microgram/mL (Geometric Mean)
Baseline (Day 22)Post-moringa (Day 35)
Efavirenz34.6732.58
Nevirapine94.17100.44

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C12h

plasma concentration 12h post dose, determined using a non-compartmental approach by means of the Phoenix WinNonlin software application. Time points for sample collection were 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 h (NCT01410058)
Timeframe: Baseline (Day 22); Post-moringa (Day 35)

,
Interventionmicrogram/mL (Geometric Mean)
Baseline (Day 22)Post-moringa (Day 35)
Efavirenz2.962.53
Nevirapine7.307.55

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Cmax

Maximum plasma concentration post does, determined using a non-compartmental approach by means of the Phoenix WinNonlin software application. Time points for sample collection were 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 h (NCT01410058)
Timeframe: Baseline (day 22), Post-moringa (day 35)

,
Interventionmicrogram/mL (Geometric Mean)
Baseline (Day 22)Post-moringa (Day 35)
Efavirenz5.085.51
Nevirapine9.9210.57

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Cumulative Rate of KS Progression, Death, AIDS Defining Event, or Virologic Failure by Week 48 for ET+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of KS progression, death, AIDS defining event, or virologic failure by week 48 (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
ET+ART77.5
PTX+ART54.6

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Cumulative Rate of KS Progression, Death, AIDS Defining Event, or Virologic Failure by Week 48 for BV+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of KS progression, death, AIDS defining event, or virologic failure by week 48 (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
BV+ART60.9
PTX+ART42.0

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Cumulative Rate of IERC-confirmed KS Progression by Week 48 for BV+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of IERC-confirmed KS progression by week 48. IERC-confirmed KS progression was defined as KS disease progression confirmed by the IERC based on comparing follow-up KS response to study entry or best KS response with respect to clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
BV+ART43.9
PTX+ART25.7

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Cumulative Rate of HIV-1 RNA Virologic Failure by Week 48 for ET+ART vs. PTX+ART

Virologic failure is defined as two successive measurements of plasma HIV-1 RNA >=1000 copies/mL at week 12 to week 24 or RNA >=400 copies/mL at week 24 or later. (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
ET+ART7.8
PTX+ART0.0

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Cumulative Rate of HIV-1 RNA Virologic Failure by Week 48 for BV+ART vs. PTX+ART

Virologic failure is defined as two successive measurements of plasma HIV-1 RNA >=1000 copies/mL at week 12 to week 24 or RNA >=400 copies/mL at week 24 or later. (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
BV+ART7.4
PTX+ART1.8

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Cumulative Rate of Death for ET+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of death. Time to death was computed as the number of weeks between study entry and date of death. For participants who did not have the event, time to death was censored at the week of last contact with the participant or at the participant's off study week, whichever is later. (NCT01435018)
Timeframe: From study entry to week 240

InterventionCumulative events per 100 persons (Number)
ET+ART25.6
PTX+ART10.7

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Cumulative Rate of Death for BV+ART vs PTX+ART

The Kaplan-Meier estimate of the cumulative rate of death. Time to death was computed as the number of weeks between study entry and date of death. For participants who did not have the event, time to death was censored at the week of last contact with the participant or at the participant's off study week, whichever is later. (NCT01435018)
Timeframe: From study entry to week 240

InterventionCumulative events per 100 persons (Number)
BV+ART18.5
PTX+ART10.3

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Cumulative Rate of KS Progression, Death, or AIDS Defining Event by Week 48 for ET+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of KS progression, death, or AIDS defining event by week 48 (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
ET+ART72.4
PTX+ART54.6

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Cumulative Rate of IERC-confirmed KS Progression by Week 48 for ET+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of IERC-confirmed KS progression by week 48. IERC-confirmed KS progression was defined as KS disease progression confirmed by the IERC based on comparing follow-up KS response to study entry or best KS response with respect to clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
ET+ART69.8
PTX+ART41.2

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Cumulative Rate of Death by Week 48 for BV+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of death by week 48. Time to death was computed as the number of weeks from study entry to the death date. For participants who did have the event, time to death was censored at the week of last contact with the participant. Time to death above 48 were censored at week 48. (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
BV+ART18.5
PTX+ART10.3

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Cumulative Rate of Change in KS Treatment by Week 48 for ET+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of change in KS treatment by week 48. Change in KS treatment was defined as stopping Step 1 randomized chemotherapy and initiating a different chemotherapy. (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
ET+ART59.5
PTX+ART26.0

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Cumulative Rate of Change in KS Treatment by Week 48 for BV+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of change in KS treatment by week 48. Change in KS treatment was defined as stopping Step 1 randomized chemotherapy and initiating a different chemotherapy. (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
BV+ART32.5
PTX+ART18.9

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Cumulative Rate of AIDS-defining Event by Week 48 for ET+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of AIDS-defining events by week 48. AIDS-defining events refer to non-KS AIDS-defining diagnosis (WHO Stage 4 (2007), plus microsporidiosis, cyclospora gastroenteritis, Chagas disease and visceral leishmaniasis). Time to event was computed as the number of weeks from study entry to the first AIDS-defining event. For participants who did not have any of the events, event time was censored at the week of last contact with the participant. Follow-up time beyond 48 was censored at week 48. (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
ET+ART15.2
PTX+ART28.6

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Cumulative Rate of AIDS-defining Event by Week 48 for BV+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of AIDS-defining events by week 48. AIDS-defining events refer to non-KS AIDS-defining diagnosis (WHO Stage 4 (2007), plus microsporidiosis, cyclospora gastroenteritis, Chagas disease and visceral leishmaniasis). Time to event was computed as the number of weeks from study entry to the first AIDS-defining event. For participants who did not have any of the events, event time was censored at the week of last contact with the participant. Follow-up time beyond 48 was censored at week 48. (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
BV+ART17.9
PTX+ART19.6

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Cumulative Rate of KS Progression, Death, or AIDS Defining Event by Week 48 for BV+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of KS progression, death, or AIDS defining event by week 48 (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
BV+ART56.7
PTX+ART42.1

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Cumulative Rate of Death by Week 48 for ET+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of death by week 48. Time to death was computed as the number of weeks from study entry to date of death. For participants who did have the event, time to death was censored at the week of last contact with the participant. Time to death above 48 were censored at week 48. (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
ET+ART25.6
PTX+ART10.7

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Cumulative Rate of KS Progression, Death, AIDS Defining Event, Virologic Failure, or KS-IRIS by Week 48 for ET+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of KS progression, death, AIDS defining event, virologic failure, or KS-IRIS. (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
ET+ART57.6
PTX+ART33.9

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Cumulative Rate of KS Progression, Death, AIDS Defining Event, Virologic Failure, or KS-IRIS by Week 48 for BV+ART vs. PTX+ART

The Kaplan-Meier estimate of the cumulative rate of KS progression, death, AIDS defining event, virologic failure, or KS-IRIS. (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
BV+ART54.5
PTX+ART36.2

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Self-reported Adherence to ART Therapy

ART adherence is based on participant's recall of the number of missed ART doses for the past month. Perfect adherence is defined as having zero missed ART doses. (NCT01435018)
Timeframe: At Weeks 6, 12, 18, 30 and 48

,,
InterventionParticipants (Count of Participants)
Week 6 Perfect AdherenceWeek 12 Perfect AdherenceWeek 18 Perfect adherenceWeek 30 Perfect adherenceWeek 48 Perfect adherence
BV+ART101101856613
ET+ART433629130
PTX+ART106103978520

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Number of Participants With Symptomatic Peripheral Neuropathy (SPN)

"SPN consists of three assessments: (1) pain, aching or burning in feet, legs, (2) pins and needles in feet, legs, and (3) numbness (lack of feeling) in feet, legs. SPN is graded on a severity scale from 0 (not present), 1 (mild) to 10 (severe). Presence of SPN is defined as having grade >=1 in at least one of the three assessments." (NCT01435018)
Timeframe: Screening, Weeks 3, 6, 9, 12, 15, 18, 21. Assessment of SPN for ET+ART was only done at screening, weeks 9 and 21.

,,
InterventionParticipants (Count of Participants)
ScreeningWeek 3Week 6Week 9Week 12Week 15Week 18Week 21
BV+ART7662464036262530
ET+ART2400140004
PTX+ART5934322723161520

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Number of Participants With Peripheral Neuropathy (PN)

Presence of PN is defined as having all of the following results: presence of symptomatic PN, abnormal perception of vibrations, and absent or hypoactive deep tendon reflexes. (NCT01435018)
Timeframe: Screening, Weeks 3, 6, 9, 12, 15, 18, 21. Assessment of PN for ET+ART was only done at screening, weeks 9 and 21.

,,
InterventionParticipants (Count of Participants)
ScreeningWeek 3Week 6Week 9Week 12Week 15Week 18Week 21
BV+ART71133265
ET+ART10000000
PTX+ART00224312

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Number of Participants With IERC-Confirmed KS Disease Progression, Dose-Limiting Toxicity, Death, AIDS-Defining Events, Virologic Failure and Objective Response in Step 4

IERC-confirmed KS progression refers to KS disease progression confirmed by the IERC based on comparing follow-up KS response to study entry or best KS response with respect to clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). AIDS-defining events refer to non-KS AIDS-defining diagnosis (WHO Stage 4 (2007), plus microsporidiosis, cyclospora gastroenteritis, Chagas disease and visceral leishmaniasis). Virologic failure is defined as two successive measurements of plasma HIV-1 RNA >=1000 copies/mL at week 12 to week 24 or RNA >=400 copies/mL at week 24 or later. Objective response refers to complete response or partial response as best overall KS response. Results are presented by Step 4 treatment arm. (NCT01435018)
Timeframe: From Step 4 study entry to Step 4 discontinuation, up to 96 weeks

,
InterventionParticipants (Count of Participants)
With IERC-confirmed KS progressionWith dose-limiting toxicityDiedWith AIDS-defining eventsWith virologic failureWith objective response
BV+ART203013
PTX+ART302003

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Number of Participants With IERC-Confirmed KS Disease Progression, Dose-Limiting Toxicity, Death, AIDS-Defining Events, Virologic Failure and Objective Response in Step 3

IERC-confirmed KS progression refers to KS disease progression confirmed by the IERC based on comparing follow-up KS response to study entry or best KS response with respect to clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). AIDS-defining events refer to non-KS AIDS-defining diagnosis (WHO Stage 4 (2007), plus microsporidiosis, cyclospora gastroenteritis, Chagas disease and visceral leishmaniasis). Virologic failure is defined as two successive measurements of plasma HIV-1 RNA >=1000 copies/mL at week 12 to week 24 or RNA >=400 copies/mL at week 24 or later. Objective response refers to complete response or partial response as best overall KS response. Results are presented by Step 3 treatment arm. (NCT01435018)
Timeframe: From Step 3 study entry to Step 3 discontinuation, up to 144 weeks

,,
InterventionParticipants (Count of Participants)
With IERC-confirmed KS progressionWith dose-limiting toxicityDiedWith AIDS-defining eventsWith virologic failureWith objective response
BV+ART6035218
ET+ART200025
PTX+ART8077129

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Number of Participants With IERC-Confirmed KS Disease Progression, Dose-Limiting Toxicity, Death, AIDS-Defining Events, Virologic Failure and Objective Response in Step 2

IERC-confirmed KS progression refers to KS disease progression confirmed by the IERC based on comparing follow-up KS response to study entry or best KS response with respect to clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). AIDS-defining events refer to non-KS AIDS-defining diagnosis (WHO Stage 4 (2007), plus microsporidiosis, cyclospora gastroenteritis, Chagas disease and visceral leishmaniasis). Virologic failure is defined as two successive measurements of plasma HIV-1 RNA >=1000 copies/mL at week 12 to week 24 or RNA >=400 copies/mL at week 24 or later. Objective response refers to complete response or partial response as best overall KS response. Results are presented by Step 2 treatment arm. (NCT01435018)
Timeframe: From Step 2 study entry to Step 2 discontinuation, up to 144 weeks

,,
InterventionParticipants (Count of Participants)
With IERC-confirmed KS progressionWith dose-limiting toxicityDiedWith AIDS-defining eventsWith virologic failureWith objective response
BV+ART101127
ET+ART100010
PTX+ART105015

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Changes in CD4+ Lymphocyte Cell Count for ET+ART vs. PTX+ART

Baseline CD4 lymphocyte cell count is the mean of screening and Step 1 entry CD4 values. Absolute change in CD4+ lymphocyte cell count was calculated as value at a given visit minus the baseline CD4 lymphocyte cell count. (NCT01435018)
Timeframe: Baseline, weeks 12, 24, 48

,
Interventioncells/mm^3 (Median)
Week 12 CD4 changeWeek 24 CD4 changeWeek 48 CD4 change
ET+ART3710669
PTX+ART4795157

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Changes in CD4+ Lymphocyte Cell Count for BV+ART vs. PTX+ART

Baseline CD4 lymphocyte cell count is the mean of screening and Step 1 entry CD4 values. Absolute change in CD4+ lymphocyte cell count was calculated as value at a given visit minus the baseline CD4 lymphocyte cell count. (NCT01435018)
Timeframe: Baseline, weeks 12, 24, 48

,
Interventioncells/mm^3 (Median)
Week 12 CD4 changeWeek 24 CD4 changeWeek 48 CD4 change
BV+ART2143112
PTX+ART3765105

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Time to IERC-confirmed KS Progression or Death for ET+ART vs. PTX+ART

Time to IERC-confirmed KS progression or death was computed as the number of weeks between study entry and the earlier between date of IERC-confirmed KS progression or date of death. For participants who did not have the event, event time was censored at the week of last contact with the participant or the participant's off study week, whichever is later. The 25-th percentile and hazard ratio are presented. (NCT01435018)
Timeframe: From study entry to week 240

Interventionweeks (Number)
ET+ART17.9
PTX+ART30.0

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Time to IERC-confirmed KS Progression or Death for BV+ART vs. PTX+ART

Time to IERC-confirmed KS progression or death was computed as the number of weeks between study entry and the earlier between date of IERC-confirmed KS progression or date of death. For participants who did not have the event, event time was censored at the week of last contact with the participant or at the participant's off study week, whichever is later.The 25-th percentile and hazard ratio are presented. (NCT01435018)
Timeframe: From study entry to week 240

Interventionweeks (Number)
BV+ART24.7
PTX+ART38.6

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Number of Participants With Objective Response for ET+ART vs. PTX+ART

The number of participants with objective response (complete response or partial response) as best overall KS response in Step 1. Overall KS response status (complete response, partial response, stable, disease progression) was based on comparing follow-up KS response to study entry or best KS response with respect to clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). (NCT01435018)
Timeframe: From study entry up to week 144

InterventionParticipants (Count of Participants)
ET+ART18
PTX+ART34

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Number of Participants With Objective Response for BV+ART vs. PTX+ART

The number of participants with objective response (complete response or partial response) as best overall KS response in Step 1. Overall KS response status (complete response, partial response, stable, disease progression) was based on comparing follow-up KS response to study entry or best KS response with respect to clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). (NCT01435018)
Timeframe: From study entry up to week 144

InterventionParticipants (Count of Participants)
BV+ART80
PTX+ART91

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Number of Participants With Kaposi's Sarcoma-Immune Reconstitution Inflammatory Syndrome (KS-IRIS) for ET+ART vs. PTX+ART

KS-IRIS is defined as any IERC-confirmed KS-progression that occurs within 12 weeks of ART-initiation that is associated with an increase in CD4 cell count of at least 50 cells/mm^3 above the study entry value and/or a decrease in the HIV-1 RNA level by at least 0.5 log below the study entry value prior to or at the time of documented KS progression. (NCT01435018)
Timeframe: From study entry to week 12

InterventionParticipants (Count of Participants)
ET+ART6
PTX+ART0

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Number of Participants With Kaposi's Sarcoma-Immune Reconstitution Inflammatory Syndrome (KS-IRIS) for BV+ART vs. PTX+ART

KS-IRIS is defined as any IERC-confirmed KS-progression that occurs within 12 weeks of ART-initiation that is associated with an increase in CD4 cell count of at least 50 cells/mm^3 above the study entry value and/or a decrease in the HIV-1 RNA level by at least 0.5 log below the study entry value prior to or at the time of documented KS progression. (NCT01435018)
Timeframe: From study entry to week 12

InterventionParticipants (Count of Participants)
BV+ART2
PTX+ART0

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Duration of Objective Response for ET+ART vs. PTX+ART

Duration of objective response is the number of weeks from first complete or partial response to the earliest among progression, death or off study week. The 25th percentile duration is presented. (NCT01435018)
Timeframe: From study entry up to week 144

Interventionweeks (Number)
ET+ART10.1
PTX+ART19.9

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Duration of Objective Response for BV+ART vs. PTX+ART

Duration of objective response is the number of weeks from first complete or partial response to the earliest among progression, death or off study week. The 25th percentile duration is presented. (NCT01435018)
Timeframe: From study entry up to week 144

Interventionweeks (Number)
ET+ART21.0
PTX+ART45.7

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Cumulative Rate of Progression-Free Survival by Week 48 for ET+ART vs. PTX+ART

Progression-free survival (PFS) by week 48 is defined as a lack of the following events: (a) Independent Endpoint Review Committee (IERC)-confirmed KS progression, (b) death, (c) entry into an additional step, or (d) loss to follow-up, prior to week 48. PFS rate was estimated by the Kaplan-Meier survival probability at week 48. Time to event was computed as the number of weeks from study entry to the first among these events. For participants who did not have any of the events, event time was censored at the week of last contact with the participant. Follow-up time beyond 48 was censored at week 48. Overall KS outcome status (complete response, partial response, stable, disease progression) was based on comparing follow-up to study entry or best KS response with respect to clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
ET+ART19.7
PTX+ART49.8

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Cumulative Rate of Progression-Free Survival by Week 48 for BV+ART vs. PTX+ART

Progression-free survival (PFS) by week 48 is defined as a lack of the following events: (a) Independent Endpoint Review Committee (IERC)-confirmed KS progression, (b) death, (c) entry into an additional step, or (d) loss to follow-up, prior to week 48. PFS rate was estimated by the Kaplan-Meier survival probability at week 48. Time to event was computed as the number of weeks from study entry to the first among these events. For participants who did not have any of the events, event time was censored at the week of last contact with the participant. Follow-up time beyond 48 was censored at week 48. Overall KS outcome status (complete response, partial response, stable, disease progression) was based on comparing follow-up to study entry or best KS response with respect to clinical assessment of KS cutaneous lesions (count, character and marker lesion area), oral KS, visceral KS and tumor-associated edema and as described in the publications (Krown et al 1989, Cianfrocca et al 2002). (NCT01435018)
Timeframe: From study entry to week 48

InterventionCumulative events per 100 persons (Number)
BV+ART44.1
PTX+ART64.2

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Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time 0 to Time t[AUC(0-t)]

The area under the plasma concentration versus time curve from time 0 to the time of the last measurable concentration (t), as calculated by the linear trapezoidal rule for efavirenz (NCT01472380)
Timeframe: serial pharmacokinetic blood samples drawn immediately prior to dosing on Days 1 and 31 and then 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 48, 72, 96, and 120 hours after dose administration

Interventionh*ug/mL (Mean)
Efavirenz Alone70.58
Efavirenz With Fenofibric Acid64.62

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Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time 0 Extrapolated to Infinity [AUC(0-infinity]

The area under the plasma concentration versus time curve from time 0 to infinity. [AUC(0 to infinity)] was calculated as the sum of AUC (0-t) plus the ratio of the last measurable plasma concentration to the elimination rate constant for efavirenz. (NCT01472380)
Timeframe: serial pharmacokinetic blood samples drawn immediately prior to dosing on Days 1 and 31 and then 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 48, 72, 96, and 120 hours after dose administration

Interventionh*ug/mL (Mean)
Efavirenz Alone121
Efavirenz With Fenofibric Acid112

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Pharmacokinetics: Maximum Plasma Concentration (Cmax)

The maximum or peak concentration that the drug reaches in the plasma for efavirenz (NCT01472380)
Timeframe: serial pharmacokinetic blood samples drawn immediately prior to dosing on Days 1 and 31 and then 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 48, 72, 96, and 120 hours after dose administration

Interventionug/mL (Mean)
Efavirenz Alone2.62
Efavirenz With Fenofibric Acid2.63

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Percentage of Participants Who Developed Detectable HIV Antibodies

Seroconversion rate of HIV antibodies while receiving HIV PEP evaluated as the percentage of participants who developed detectable HIV antibodies (defined as positive) and percentage of participants who had not developed detectable HIV antibodies (defined as negative). Per protocol (PP) population included all participants in mITT (defined as all participants who were assigned to receive randomized HIV PEP and were not discontinued due to confirmation of the negative HIV infection status of the index person) excluding participants with: No indication for HIV PEP; Initiation of PEP >72 hours after injury; Discontinuation of HIV PEP due to confirmation of HIV negative status of index person and if index person bears resistant virus against HIV PEP components prescribed; incorrect HIV PEP; no intake of medication. (NCT01516970)
Timeframe: At Month 3

,
Interventionpercentage of participants (Number)
NegativePositive
Darunavir/Ritonavir Postexposure Prophylaxis (DRV/r PEP)99.30.7
Standard of Care Postexposure Prophylaxis (SOCPEP)1000

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Worst Sheehan Disability Scale (SDS) Score for the Safety Population

The Sheehan Disability Scale (SDS) assesses functional impairment in 3 inter-related domains: work/school, social and family life, using a rating scale for each item ranging from 0 (not at all) to 10 (extremely). (NCT01516970)
Timeframe: Month 3

,
Interventionunits on a scale (Mean)
Impairment in work/school/studiesImpairment in social lifeImpairment in family life
Darunavir/Ritonavir Postexposure Prophylaxis (DRV/r PEP)2.5662.4652.226
Standard of Care Postexposure Prophylaxis (SOCPEP)3.5033.4642.954

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Number of Participants With Early Discontinuation From Randomized Human Immunodeficiency Virus Postexposure Prophylaxis (HIV PEP)

Number of participants with early discontinuation from randomized HIV PEP for any reason other than confirmation of the negative HIV infection status of the index person in participants receiving HIV PEP for at least 28 days and a maximum of 30 days was assessed. Per protocol (PP) population included all participants in modified intention-to-treat (mITT [defined as all participants who were assigned to receive randomized HIV PEP and were not discontinued due to confirmation of the negative HIV infection status of the index person]) excluding participants with: No indication for HIV PEP; Initiation of PEP >72 hours after injury; Discontinuation of HIV PEP due to confirmation of HIV negative status of index person and if index person bears resistant virus against HIV PEP components prescribed; incorrect HIV PEP; no intake of medication. (NCT01516970)
Timeframe: Up to 30 days

Interventionparticipants (Number)
Darunavir/Ritonavir Postexposure Prophylaxis (DRV/r PEP)10
Standard of Care Postexposure Prophylaxis (SOCPEP)15

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

An adverse event (AE) is defined to be non-treatment-emergent if the onset date of the AE was clearly before the date of first HIV PEP administration, otherwise it is considered treatment-emergent. (NCT01516970)
Timeframe: Up to Month 3

Interventionparticipants (Number)
Darunavir/Ritonavir Postexposure Prophylaxis (DRV/r PEP)131
Standard of Care Postexposure Prophylaxis (SOCPEP)125

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Oxidative Stress Markers

Change in F2-isoprostane levels (NCT01585038)
Timeframe: Change from baseline to 4 weeks

Interventionpg/mL (Mean)
Efavirenz92.7
Rilpivirine-101.4

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Change in Flow-mediated Dilation of the Brachial Artery

This is a measure of in vivo endothelial function (NCT01585038)
Timeframe: Change from baseline to 4 weeks

Interventionabsolute percentage change (Mean)
Efavirenz0.089
Rilpivirine0.63

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Endothelial Activation Markers

Change in soluble vascular cell adhesion molecule-1 levels (NCT01585038)
Timeframe: Change from baseline to 4 weeks

Interventionpg/mL (Mean)
Efavirenz-27.62
Rilpivirine-20.92

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Inflammatory Markers

Change in high sensitivity C-reactive protein levels (NCT01585038)
Timeframe: Change from baseline to 4 weeks

Interventionmg/L (Mean)
Efavirenz0.80
Rilpivirine-0.41

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Proportion of Women With HIV-1 Drug Resistance Mutations at Screening, 2-4 Weeks Postpartum in Women Who Stopped Antiretroviral Therapy, and at the Time of Inadequate Virologic Response Using Standard and Ultrasensitive Methods.

"Consensus sequencing was performed on a sample from screening. Women were evaluated for integrase and reverse transcriptase resistance mutations separately.~Additionally, consensus sequencing was performed among women who had an inadequate virologic response (defined in the protocol) on a sample taken at that time of inadequate virologic response.~Genotypic resistance among women who stopped antiretroviral therapy was not assessed. Because World Health Organization guidelines have been updated to indicate all people living with HIV should remain on antiretroviral therapy, even postpartum women, no women stopped antiretroviral therapy after delivery. Therefore, this aspect of the outcome measure is no longer relevant and was not assessed." (NCT01618305)
Timeframe: Measured at screening and at the time of inadequate virologic response (from Week 2 antepartum through participants' last study visit 24 weeks after delivery).

InterventionProportion (Number)
Reverse transcriptase resistance at screeningIntegrase resistance at screeningReverse transcriptase resistance at viral failure
Arm A (Women).07.00.60

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Proportion of Women Who Achieved HIV-1 RNA Virologic Suppression Below the Lower Limit of Quantification of the Assay at Delivery

"A successful outcome was defined as maternal HIV-1 RNA plasma viral load less than the lower limit of quantification (LLQ) for the testing assay, which could vary. Most (99%) women had their viral load measured using an assay with LLQ equal to 40 or 20 copies/mL.~If the viral load at delivery was missing, the last observed viral load within 21 days prior to the delivery date was considered." (NCT01618305)
Timeframe: Measured at participants' delivery visit (or last visit within three weeks prior to delivery)

InterventionProportion (Number)
Arm A (Women).58
Arm B (Women).86

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Proportion of Women With 1) Successful Viral Load (Plasma HIV-1 RNA VL) Decrease From Entry to Week 2 and VL Less Than 1,000 Copies/ml at All Time Points After 4 Weeks on Study Drugs, Until Delivery; and 2) Who Remain on the Assigned Study Regimen

A successful viral load decrease was defined as follows: for women having HIV-1 RNA viral load greater than or equal to 10,000 copies/mL at entry, a viral load <200 copies/mL; for women with VL less than 10,000 copies/mL at entry, a Log10 viral load decrease of at least 2.0 from entry. (NCT01618305)
Timeframe: Measured from entry through delivery (approximately 36 to 40 weeks gestation).

InterventionProportion (Number)
Arm A (Women).63
Arm B (Women).89

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Proportion of Women With HIV-1 Drug Resistance Mutations at Screening, 2-4 Weeks Postpartum in Women Who Stopped Antiretroviral Therapy, and at the Time of Inadequate Virologic Response Using Standard and Ultrasensitive Methods.

"Consensus sequencing was performed on a sample from screening. Women were evaluated for integrase and reverse transcriptase resistance mutations separately.~Additionally, consensus sequencing was performed among women who had an inadequate virologic response (defined in the protocol) on a sample taken at that time of inadequate virologic response.~Genotypic resistance among women who stopped antiretroviral therapy was not assessed. Because World Health Organization guidelines have been updated to indicate all people living with HIV should remain on antiretroviral therapy, even postpartum women, no women stopped antiretroviral therapy after delivery. Therefore, this aspect of the outcome measure is no longer relevant and was not assessed." (NCT01618305)
Timeframe: Measured at screening and at the time of inadequate virologic response (from Week 2 antepartum through participants' last study visit 24 weeks after delivery).

InterventionProportion (Number)
Reverse transcriptase resistance at screeningIntegrase resistance at screeningReverse transcriptase resistance at viral failureIntegrase resistance at viral failure
Arm B (Women).11.00.30.00

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Proportion of Women With HIV-1 RNA Plasma Viral Load Less Than 200 Copies/mL at Weeks 4 and 6 From Treatment Initiation

The Week 4 and 6 participant viral loads were the viral load results obtained closest to (within four days of) the target date for that visit from initiation of treatment (for Week 4, day 24-32 after first dose; for Week 6, day 38-46 after first dose). (NCT01618305)
Timeframe: Measured at Weeks 4 and 6 from first dose of randomized treatment, prior to delivery

,
InterventionProportion (Number)
Week 4Week 6
Arm A (Women).75.85
Arm B (Women).95.96

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Proportion of Women With HIV-1 RNA Vaginal Viral Load Less Than 1200 Copies/mL at Weeks 4 and 6 From Treatment Initiation

"The Week 4 and 6 participant viral loads were the viral load results obtained closest to (within four days of) the target date for that visit from initiation of treatment (for Week 4, day 24-32 after first dose; for Week 6, day 38-46 after first dose).~Vaginal swabs produce much less testable sample volume than blood plasma draws. Each vaginal swab specimen had to be diluted, and this dilution factor raised the lower limit of quantification (LLQ). The most commonly observed LLQs were 300 and 1200. For consistency, the higher LLQ was considered the threshold for this outcome measure." (NCT01618305)
Timeframe: Measured at Weeks 4 and 6 from first dose of randomized treatment, prior to delivery

,
InterventionProportion (Number)
Week 4Week 6
Arm A (Women).97.98
Arm B (Women).95.94

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Proportion of Deliveries With a Low Birth Weight (Less Than 2,500 Grams)

The unit of analysis was the mother-infant pair or set; in the case of multiple gestation, the worst outcome was considered in analysis (e.g. if two twins were delivered to one mother, one at 2,000 grams and one at 3,000 grams, this mother-infant set would count as one instance of low birth weight in analysis because at least one of the infants had the outcome). (NCT01618305)
Timeframe: Measured within 72 hours after delivery

InterventionProportion (Number)
Arm A (Women).124
Arm B (Women).127

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Proportion of Deliveries That Had an Outcome of a Stillbirth/Fetal Demise.

The unit of analysis was the mother-infant set. All sets where the woman received at least one dose of study treatment and remained on study through delivery were eligible. In the case of twins, the worst outcome (i.e. a stillbirth) was used. (NCT01618305)
Timeframe: Measured at delivery (approximately 36 to 40 weeks gestation)

InterventionProportion (Number)
Arm A (Women).005
Arm B (Women).015

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Proportion of Deliveries That Were Extremely Premature (Less Than 34 Weeks Gestation).

"The unit of analysis for this outcome measure was the mother-infant set. A mother-infant set was counted as having an extremely premature delivery if any infant in the mother-infant set was delivered prior to 34 weeks gestation (i.e. in the case of twins, if either of the twins was delivered prior to 34 weeks gestation then this set would count as one extremely premature delivery outcome).~Only women who enrolled prior to 34 weeks gestation were included in this analysis. Those that enrolled from 34 to less than 37 weeks gestation were excluded because they were already past the gestational age where this outcome could have occurred at entry." (NCT01618305)
Timeframe: At delivery (within 72 hours).

InterventionProportion (Number)
Arm A (Women).036
Arm B (Women).023

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Proportion of Deliveries That Were Premature (Less Than 37 Weeks Gestation)

"The unit of analysis for this outcome measure was the mother-infant set. A mother-infant set was counted as having a premature delivery if any infant in the mother-infant set was delivered prior to 37 weeks gestation (i.e. in the case of twins, if either of the twins was delivered prior to 37 weeks gestation then this set would count as one premature delivery outcome).~All mother-infant sets that delivered at least one live birth on study were eligible for this outcome." (NCT01618305)
Timeframe: Measured at delivery (within 72 hours).

InterventionProportion (Number)
Arm A (Women).105
Arm B (Women).123

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Proportion of Women Who Experienced at Least One New Adverse Event of Greater Than or Equal to Grade 3 as Defined in the Division of AIDS (DAIDS) Toxicity Table

"New adverse events were those with an onset date on or after randomization. Adverse events present at baseline would only be considered New if they increased in grade on or after randomization.~All women who received at least one dose of study drug were eligible for this analysis." (NCT01618305)
Timeframe: Measured from entry through participants' last study visit, approximately 24 weeks after delivery

InterventionPropotion (Number)
Arm A (Women).30
Arm B (Women).30

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Proportion of Deliveries With an Extremely Low Birth Weight (<1,500 Grams).

The unit of analysis was the mother-infant pair or set; in the case of multiple gestation, the worst outcome was considered in analysis (e.g. if two twins were delivered to one mother, one at 2,000 grams and one at 1,000 grams, this mother-infant set would count as one instance of extremely low birth weight in analysis because at least one of the infants had the outcome). (NCT01618305)
Timeframe: Measured within 72 hours after delivery

InterventionProportion (Number)
Arm A (Women).000
Arm B (Women).005

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Proportion of Infants Who Experienced at Least One Adverse Event of Greater Than or Equal to Grade 3.

All infants who were live births on study were eligible for this analysis. Adverse event grades were defined based on the DAIDS toxicity table. (NCT01618305)
Timeframe: Measured from birth through infants' last study visit, approximately 24 weeks after delivery

InterventionProportion (Number)
Arm A (Infants).25
Arm B (Infants).25

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Proportion of Participants Who Discontinued Randomized Study Drug Prior to Labor and Delivery.

Only women who initiated (i.e. received at least one dose of) their randomized treatment were eligible for this outcome measure. Women were considered to have discontinued study drug if they stopped receiving efavirenz or raltegravir (whichever was assigned) prior to labor and delivery for any reason, including loss to follow-up. (NCT01618305)
Timeframe: Measured from entry through participants' delivery visit (approximately 36 to 40 weeks gestation)

InterventionProportion (Number)
Arm A (Women).05
Arm B (Women).03

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Proportion of Women With Plasma HIV-1 RNA Viral Load Less Than 200 Copies/mL at Delivery

If there was no viral load measurement at the delivery visit, the last viral load within three weeks prior to delivery was considered. (NCT01618305)
Timeframe: Measured at participants' delivery visit (or last visit within three weeks prior to delivery)

InterventionProportion (Number)
Arm A (Women).84
Arm B (Women).94

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Log10 Change in Viral Load From Entry to Each Time Point Prior to Delivery

"Change in viral load from entry (or screening, if there was no entry viral load) to each study week prior to delivery, calculated on the log10 scale as log10(week X RNA) - log10(baseline RNA).~For this analysis, HIV-1 RNA values that were censored below the lower limit of quantification (LLQ) were imputed to be equal to the LLQ - 1." (NCT01618305)
Timeframe: Measured at antepartum Weeks 1, 2, 4, 6, 8, 10, 12, 14, and 16.

,
InterventionLog10 copies/mL (Median)
Week 1Week 2Week 4Week 6Week 8Week 10Week 12Week 14Week 16
Arm A (Women)-1.4-1.8-2.0-2.1-2.2-2.3-2.4-2.5-2.5
Arm B (Women)-1.5-2.1-2.4-2.4-2.4-2.3-2.5-2.5-2.7

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Proportion of HIV-infected Infants With Genotypic Resistance to Study Drugs

Genotypic resistance to each class of study drug (reverse transcriptase inhibitors and integrase inhibitors) was assessed separately among HIV infected infants. (NCT01618305)
Timeframe: Measured on or after confirmation of HIV-infection up to the infants' last study visit at Week 24

,
InterventionProportion (Number)
Reverse transcriptase resistanceIntegrase resistance
Arm A (Infants).20.00
Arm B (Infants).00.00

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Change From Baseline in CD4 Cell Count at Week 24: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Assessment of the change from baseline in the CD4 cell count at Week 24 in participants receiving doravirine at 100 mg, compared with participants receiving efavirenz 600 mg. The OF approach was used to handle missing data, and the Baseline CD4 cell count was carried forward for participants who discontinued assigned treatment due to lack of efficacy. (NCT01632345)
Timeframe: Baseline, Week 24

Interventioncells/mm^3 (Mean)
Doravirine 100 mg: Part I/II (Combined)152.3
Efavirenz 600 mg: Part I/II (Combined)146.0

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Change From Baseline in CD4 Cell Count at Week 48: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Assessment of the change from baseline in the CD4 count at Week 48 in participants receiving doravirine at 100 mg, compared with participants receiving efavirenz 600 mg. The OF approach was used to handle missing data, and the Baseline CD4 cell count was carried forward for subjects who discontinued assigned treatment due to lack of efficacy. (NCT01632345)
Timeframe: Baseline, Week 48

Interventioncells/mm^3 (Mean)
Doravirine 100 mg: Part I/II (Combined)191.9
Efavirenz 600 mg: Part I/II (Combined)194.5

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Change From Baseline in CD4 Cell Count at Week 96: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

A secondary endpoint in Part I/II combined was the change from baseline in the CD4 count at Week 96 in participants receiving doravirine at 100 mg, compared with participants receiving efavirenz 600 mg. The OF approach was used to handle missing data, and the Baseline CD4 cell count was carried forward for subjects who discontinued assigned treatment due to lack of efficacy. (NCT01632345)
Timeframe: Baseline, Week 96

Interventioncells/mm^3 (Mean)
Doravirine 100 mg: Part I/II (Combined)259.2
Efavirenz 600 mg: Part I/II (Combined)263.6

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Change From Baseline in CD4 T Lymphocyte Cell Count at Week 24: Doravirine (All Doses) vs Efavirenz (Part I)

Evaluation of the change from baseline in the CD4 cell count at Week 24 in participants receiving doravirine at all doses (25 mg, 50 mg, 100 mg, and 200 mg), compared with participants receiving efavirenz 600 mg. The Observed Failure (OF) approach was used to handle missing data, and the Baseline CD4 cell count was carried forward for participants who discontinued assigned treatment due to lack of efficacy. (NCT01632345)
Timeframe: Baseline, Week 24

Interventioncells/mm^3 (Mean)
Doravirine 25 mg: Part I154.1
Doravirine 50 mg: Part I112.9
Doravirine 100 mg: Part I133.6
Doravirine 200 mg: Part I140.7
Efavirenz 600 mg: Part I121.1

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Percentage of Participants Who Discontinued Study Therapy Due to AEs in Weeks 0-24: Doravirine (All Doses) vs Efavirenz (Part I)

Assessment of the percentage of participants receiving doravirine at all doses (25 mg, 50 mg, 100 mg, or 200 mg), compared with participants receiving efavirenz 600 mg, who discontinued therapy due to an AE over 24 weeks of treatment. An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR's product, whether or not considered related to the use of the product.The percentage of participants in any treatment group who discontinued therapy due to an AE was primarily assessed for Weeks 0-24. (NCT01632345)
Timeframe: Up to Week 24

InterventionPercentage of participants (Number)
Doravirine 25 mg: Part I2.5
Doravirine 50 mg: Part I7.0
Doravirine 100 mg: Part I2.4
Doravirine 200 mg: Part I0.0
Efavirenz 600 mg: Part I4.8

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Percentage of Participants With At Least 1 AE in Weeks 0-24: Doravirine (All Doses) vs Efavirenz (Part I)

Assessment of the percentage of participants receiving doravirine at all doses (25 mg, 50 mg, 100 mg, or 200 mg), compared with participants receiving efavirenz 600 mg, who had at least 1 AE over 24 weeks of treatment. An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR's product, whether or not considered related to the use of the product.The percentage of participants in any treatment group with at least 1 AE was primarily assessed for Weeks 0-24. (NCT01632345)
Timeframe: Up to Week 24

InterventionPercentage of participants (Number)
Doravirine 25 mg: Part I90.0
Doravirine 50 mg: Part I93.0
Doravirine 100 mg : Part I71.4
Doravirine 200 mg: Part I85.4
Efavirenz 600 mg: Part I83.3

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Percentage of Participants With At Least 1 AE in Weeks 0-24: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Assessment of the percentage of participants receiving doravirine at 100 mg, compared with participants receiving efavirenz 600 mg, who had at least 1 AE over 24 weeks of treatment. An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR's product, whether or not considered related to the use of the product.The percentage of participants in any treatment group with at least 1 AE was assessed for Weeks 0-24. (NCT01632345)
Timeframe: Up to Week 24

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)75.0
Efavirenz 600 mg: Part I/II (Combined)85.2

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Percentage of Participants With CNS Events by Week 24: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Assessment of the percentage of participants receiving doravirine at 100 mg, compared with participants receiving efavirenz 600 mg, who had CNS events over 24 weeks of treatment. CNS events were pooled and evaluated as pre-specified by the protocol (depression, nightmare, confusional state, suicidal ideation, nervous system disorder, psychotic disorder, abnormal dreams, suicide attempt, acute psychosis, delirium, depressed level of consciousness, hallucination, hallucination auditory, hallucination visual, completed suicide, suicidal behavior, major depression, depressed mood, depressive symptom, insomnia, disturbance in attention, somnolence, dizziness, or concentration impaired). The percentage of participants in either treatment group with CNS events was assessed over Weeks 0-24. (NCT01632345)
Timeframe: Up to Week 24

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)26.9
Efavirenz 600 mg: Part I/II (Combined)47.2

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Percentage of Participants With Virologic Response (HIV-1 RNA <200 Copies/mL) at Week 24: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Assessment of the virologic response to doravirine at 100 mg, compared to efavirenz, each in combination with TRUVADA, as measured by the percentage of participants with plasma HIV-1 RNA <200 copies/mL at Week 24. HIV RNA levels were determined using the Abbott RealTime HIV-1 Assay. The percentage of participants in any treatment group with a virologic response was primarily assessed for Weeks 0-24. The NC=F approach was used as the primary approach to handle missing data for this analysis of efficacy. This secondary outcome was analyzed for HIV-1 RNA <200 copies/mL in Part I & Part II combined. (NCT01632345)
Timeframe: Week 24

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)89.7
Efavirenz 600 mg: Part I/II (Combined)87.0

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Percentage of Participants With CNS Events by Week 8: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Assessment of the percentage of participants receiving doravirine at 100 mg, compared with participants receiving efavirenz 600 mg, who had CNS events over 8 weeks of treatment. CNS events were pooled and evaluated as pre-specified by the protocol (depression, nightmare, confusional state, suicidal ideation, nervous system disorder, psychotic disorder, abnormal dreams, suicide attempt, acute psychosis, delirium, depressed level of consciousness, hallucination, hallucination auditory, hallucination visual, completed suicide, suicidal behavior, major depression, depressed mood, depressive symptom, insomnia, disturbance in attention, somnolence, dizziness, or concentration impaired). The percentage of participants in either treatment group with CNS events was assessed over Weeks 0-8. (NCT01632345)
Timeframe: Up to Week 8

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)24.1
Efavirenz 600 mg: Part I/II (Combined)44.4

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Percentage of Participants With At Least 1 AE in Weeks 0-96: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

A secondary outcome in Part I/II combined was the percentage of participants receiving doravirine at 100 mg, compared with participants receiving efavirenz 600 mg, who had at least 1 AE over 96 weeks of treatment. The percentage of participants in any treatment group with at least 1 AE was primarily assessed for Weeks 0-96. (NCT01632345)
Timeframe: Up to Week 96

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)89.8
Efavirenz 600 mg: Part I/II (Combined)96.3

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Percentage of Participants With At Least 1 AE in Weeks 0-48: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

A secondary outcome in Part I/II combined was the percentage of participants receiving doravirine at 100 mg, compared with participants receiving efavirenz 600 mg, who had at least 1 AE over 48 weeks of treatment. The percentage of participants in any treatment group with at least 1 AE was primarily assessed for Weeks 0-48. (NCT01632345)
Timeframe: Up to Week 48

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)87.0
Efavirenz 600 mg: Part I/II (Combined)89.8

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Percentage of Participants With Virologic Response (HIV-1 RNA) < 40 Copies/mL) at Week 24: Doravirine (All Doses) vs Efavirenz (Part I)

Assessment of the virologic response to doravirine at all studied doses (25 mg, 50 mg, 100 mg, and 200 mg), compared to efavirenz, each in combination with TRUVADA, as measured by the percentage of participants with plasma HIV-1 RNA <40 copies/mL at Week 24. HIV RNA levels were determined using the Abbott RealTime HIV-1 Assay, which has a limit of reliable quantification of 40 copies/mL. The percentage of participants in any treatment group with a virologic response was assessed at Week 24. The Non-Completer = Failure (NC=F) approach, in which participants who prematurely discontinued assigned treatment for any reason and were considered as failures thereafter, was used as the primary approach to handle missing data this analysis of efficacy.This primary outcome was analyzed for HIV-1 RNA <40 copies/mL in Part I. (NCT01632345)
Timeframe: Week 24

InterventionPercentage of participants (Number)
Doravirine 25 mg: Part I80.0
Doravirine 50 mg: Part I74.4
Doravirine 100 mg: Part I71.4
Doravirine 200 mg: Part I80.5
Efavirenz 600 mg: Part I64.3

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Percentage of Participants With Virologic Response (HIV-1 RNA <40 Copies/mL) at Week 96: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Assessment of the virologic response to doravirine at 100 mg, compared to efavirenz, each in combination with TRUVADA, as measured by the percentage of participants with HIV-1 RNA <40 copies/mL at Week 96. HIV RNA levels were determined using the Abbott RealTime HIV-1 Assay. The percentage of participants in any treatment group with a virologic response was primarily assessed for Weeks 0-24. The NC=F approach was used as the primary approach to handle missing data this analysis of efficacy. This primary outcome was analyzed for HIV-1 RNA <40 copies/mL in Part I & Part II combined. (NCT01632345)
Timeframe: Week 96

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)75.0
Efavirenz 600 mg: Part I/II (Combined)75.9

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Percentage of Participants With Virologic Response (HIV-1 RNA <40 Copies/mL) at Week 48: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Assessment of the virologic response to doravirine at 100 mg, compared to efavirenz, each in combination with TRUVADA, as measured by the percentage of participants with HIV-1 RNA <40 copies/mL at Week 48. HIV RNA levels were determined using the Abbott RealTime HIV-1 Assay. The percentage of participants in any treatment group with a virologic response was primarily assessed for Weeks 0-24. The NC=F approach was used as the primary approach to handle missing data this analysis of efficacy. This primary outcome was analyzed for HIV-1 RNA <40 copies/mL in Part I & Part II combined. (NCT01632345)
Timeframe: Week 48

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)77.8
Efavirenz 600 mg: Part I/II (Combined)79.4

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Percentage of Participants With Virologic Response (HIV-1 RNA <40 Copies/mL) at Week 24: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Assessment of the virologic response to doravirine at 100 mg, compared to efavirenz, each in combination with TRUVADA, as measured by the percentage of participants with HIV-1 RNA <40 copies/mL at Week 24. HIV RNA levels were determined using the Abbott RealTime HIV-1 Assay, which has a limit of reliable quantification of 40 copies/mL. The percentage of participants in any treatment group with a virologic response was assessed at Week 24. The NC=F approach was used as the primary approach to handle missing data this analysis of efficacy. This primary outcome was analyzed for HIV-1 RNA <40 copies/mL in Part I & Part II combined. (NCT01632345)
Timeframe: Week 24

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)72.9
Efavirenz 600 mg: Part I/II (Combined)73.1

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Percentage of Participants With Virologic Response (HIV-1 RNA <200 Copies/mL) at Week 96: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Assessment of the virologic response to doravirine at 100 mg, compared to efavirenz, each in combination with TRUVADA, as measured by the percentage of participants with plasma HIV-1 RNA <200 copies/mL at Week 96. HIV RNA levels were determined using the Abbott RealTime HIV-1 Assay. The percentage of participants in any treatment group with a virologic response was primarily assessed for Weeks 0-96. The Non-Completer = Failure (NC=F) approach, in which participants who prematurely discontinued assigned treatment for any reason and were considered as failures thereafter, was used as the primary approach to handle missing data this analysis of efficacy. This primary outcome was analyzed for HIV-1 RNA <200 copies/mL in Part I & Part II combined. (NCT01632345)
Timeframe: Week 96

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)79.6
Efavirenz 600 mg: Part I/II (Combined)75.9

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Percentage of Participants With Virologic Response (HIV-1 RNA <200 Copies/mL) at Week 48: Doravirine 100 mg vs Efavirenz (Part I & Part II Combined)

Evaluation of the antiretroviral activity of doravirine at 100 mg, compared to efavirenz, each in combination with TRUVADA for 24 weeks, as measured by the percentage of participants with HIV-1 RNA <200 copies/mL at Week 48. HIV RNA levels were determined using the Abbott RealTime HIV-1 Assay. This primary outcome was analyzed for RNA <200 copies/mL in Part I & Part II combined. (NCT01632345)
Timeframe: Week 48

InterventionPercentage of participants (Number)
Doravirine 100 mg: Part I/II (Combined)85.2
Efavirenz 600 mg: Part I/II (Combined)85.0

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Percentage of Participants With Virologic Response (HIV-1 RNA <200 Copies/mL) at Week 24: Doravirine (All Doses) vs Efavirenz (Part I)

Assessment of the virologic response to doravirine at all studied doses (25 mg, 50 mg, 100 mg, and 200 mg), compared to efavirenz, each in combination with TRUVADA, as measured by the percentage of participants with plasma HIV-1 RNA <200 copies/mL at Week 24. HIV RNA levels were determined using the Abbott RealTime HIV-1 Assay.The percentage of participants in any treatment group with a virologic response was assessed at Week 24. The NC=F approach was used as the primary approach to handle missing data for this analysis of efficacy. This primary outcome was analyzed for HIV-1 RNA <200 copies/mL in Part I. (NCT01632345)
Timeframe: Week 24

InterventionPercentage of participants (Number)
Doravirine 25 mg: Part I85.0
Doravirine 50 mg: Part I83.7
Doravirine 100 mg: Part I92.9
Doravirine 200 mg: Part I90.2
Efavirenz 600 mg: Part I81.0

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Change in log10(Pf Parasite Density) From Entry to Day 30

"Change is evaluated as log10(Pf parasite density) at day 30 minus log10(Pf parasite density) at entry.~Change is evaluated in four groups:~Randomized to nNRTI-based ART with continued Pf SCP at day 15~Randomized to nNRTI-based ART with clearance of Pf SCP at day 15~Randomized to LPV/r-based ART with continued Pf SCP at day 15~Randomized to LPV/r-based ART with clearance of Pf SCP at day 15" (NCT01632891)
Timeframe: Entry, Day 30

Interventionlog10(parasites/µL) (Median)
nNRTI-based ART, Not Cleared-2.26
nNRTI-based ART, Cleared-1.65
LPV/R-based ART, Not Cleared-1.82
LPV/R-based ART, Cleared-3.61

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Number of Participants With Uncomplicated Clinical Malaria

Uncomplicated clinical malaria is defined as the presence of non-severe fever/symptoms and parasitemia without organ complication. (NCT01632891)
Timeframe: From study entry to day 30

InterventionParticipants (Count of Participants)
LPV/R-based ART2
nNRTI-based ART1

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Time to First Pf SCP Clearance

Time to clearance is defined by time to first measurement with PCR < 10 parasites/µL, and is evaluated as the point estimate and 95% CI for the day when 50% of participants cleared parasite. (NCT01632891)
Timeframe: From study entry up to day 30

InterventionDays (Median)
LPV/R-based ART12
nNRTI-based ART14

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Log10(Pf Parasite Density)

Pf parasite density was determined by PCR. If parasite density equals 0, the value is set to 0.01 before log10 transformation. The value 0.01 was chosen based on the smallest observed parasite density value of 0.017. (NCT01632891)
Timeframe: Entry, days 3, 6, 9, 12, 15, 20, 25, 30

,
Interventionlog10(parasites/µL) (Mean)
EntryDay 3Day 6Day 9Day 12Day 15Day 20Day 25Day 30
LPV/R-based ART2.481.921.771.651.591.590.650.280.14
nNRTI-based ART2.091.571.491.631.561.430.670.490.30

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Proportion of Participants With Plasmodium Falciparum (Pf) Subclinical Parasitemia (SCP) Clearance

"Pf SCP clearance defined by polymerase chain reaction (PCR) < 10 parasites/µL on three consecutive occasions within a 24-hour period.~If a participant had missing data on day 15, they were considered as not having clearance." (NCT01632891)
Timeframe: Day 15 (3 samples collected, separated by at least 5 hours and all three collected within 24-hours)

,
InterventionProportion of participants (Number)
Proportion ClearedProportion Not Cleared
LPV/R-based ART0.230.77
nNRTI-based ART0.270.73

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Number of Participants With Detectable Pf Gametocyte Density

Number of participants with detectable Pf gametocyte density as determined by PCR. Due to the large number of undetectable results, this outcome was measured as dichotomous. (NCT01632891)
Timeframe: Entry, days 3, 6, 9, 12, 15, 20, 25, 30

,
InterventionParticipants (Count of Participants)
EntryDay 3Day 6Day 9Day 12Day 15Day 20Day 25Day 30
LPV/R-based ART1110911610111211
nNRTI-based ART121512131114141613

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Change in log10(Pf Gametocyte Density) From Entry to Day 30

"Change in log10(Pf gametocyte density) as evaluated using a Hodges-Lehmann estimate from entry to day 30 is evaluated in two groups:~Randomized to nNRTI-based ART with continued Pf SCP at day 15~Randomized to LPV/r-based ART with continued Pf SCP at day 15~Analysis was not conducted in either group with clearance at day 15 due to the small sample size and high number of undetectable samples in both clearance groups at entry and day 30." (NCT01632891)
Timeframe: Entry, Day 30

Interventionlog10(gametocyte/µL) (Number)
nNRTI-based ART, Not Cleared-0.46
LPV/R-based ART, Not Cleared0.17

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Number of Participants With Adherence to Study Treatment

Number of participants with >=90% adherence to study treatment based on pill count is summarized. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300 and 312

InterventionParticipants (Count of Participants)
Baseline; n=57, 55, 56, 52Week 4; n=54, 52, 53, 50Week 8; n=53, 50, 56, 48Week 12; n=55, 48, 53, 48Week 16; n=53, 51, 53, 44Week 20; n=51, 49, 55, 44Week 24; n=51, 46, 51, 43Week 28; n=49, 48, 53, 41Week 32; n=47, 48, 55, 41Week 36; n=46, 48, 50, 41Week 40; n=38, 35, 45, 39Week 48; n=33, 37, 45, 35Week 60; n=38, 38, 40, 37Week 72; n=35, 37, 44, 32Week 84; n=36, 39, 42, 33Week 96; n=31, 36, 33, 0Week 108; n=23, 23, 29, 0Week 120; n=30, 38, 41, 0Week 132; n=29, 32, 40, 0Week 144; n=33, 34, 43, 0Week 156; n=31, 28, 39, 0Week 168; n=29, 33, 41, 0Week 180; n=26, 29, 39, 0Week 192; n=30, 30, 39, 0Week 204; n=29, 32, 38, 0Week 216; n=29, 30, 37, 0Week 228; n=27, 34, 40, 0Week 240; n=28, 26, 41, 0Week 252; n=23, 26, 33, 0Week 264; n=15, 18, 24, 0Week 276; n=14, 14, 21, 0Week 288; n=12, 14, 18, 0Week 300; n=12, 13, 20, 0
GSK1265744 60 mg555253465051484852484141374139302739354135353435333135352921181718

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Number of Participants With Adherence to Study Treatment

Number of participants with >=90% adherence to study treatment based on pill count is summarized. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300 and 312

InterventionParticipants (Count of Participants)
Baseline; n=57, 55, 56, 52Week 4; n=54, 52, 53, 50Week 8; n=53, 50, 56, 48Week 12; n=55, 48, 53, 48Week 16; n=53, 51, 53, 44Week 20; n=51, 49, 55, 44Week 24; n=51, 46, 51, 43Week 28; n=49, 48, 53, 41Week 32; n=47, 48, 55, 41Week 36; n=46, 48, 50, 41Week 40; n=38, 35, 45, 39Week 48; n=33, 37, 45, 35Week 60; n=38, 38, 40, 37Week 72; n=35, 37, 44, 32Week 84; n=36, 39, 42, 33
Efavirenz 600 mg484447434241393537363433352729

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Change From Baseline in Total Neutrophils, Platelet Count and WBC Count Over Time by Visit

Blood samples were collected for the analysis of total neutrophils, platelet count and WBC count. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

InterventionGiga cells per liter (Mean)
T. neutrophils; Week 2; n=57, 56, 59, 59T. neutrophils; Week 4; n=57, 57, 59, 57T. neutrophils; Week 8; n=58, 56, 56, 55T. neutrophils; Week 12; n=58, 53, 57, 51T. neutrophils; Week 16; n=57, 54, 57, 52T. neutrophils; Week 20; n=56, 54, 55, 49T. neutrophils; Week 24; n=56, 53, 56, 47T. neutrophils; Week 26; n=48, 50, 53, 45T. neutrophils; Week 28; n=50, 52, 52, 45T. neutrophils; Week 32; n=51, 53, 55, 45T. neutrophils; Week 36; n=52, 53, 55, 44T. neutrophils; Week 40; n=51, 53, 55, 45T. neutrophils; Week 48; n=51, 53, 54, 44T. neutrophils; Week 60; n=48, 47, 52, 44T. neutrophils; Week 72; n=47, 48, 52, 42T. neutrophils; Week 84; n=46, 48, 51, 42T. neutrophils; Week 96; n=46, 46, 52, 41Platelet count; Week 2; n=57, 56, 59, 59Platelet count; Week 4; n=57, 57, 59, 57Platelet count; Week 8; n=58, 56, 56, 55Platelet count; Week 12; n=58, 53, 57, 51Platelet count; Week 16; n=57, 54, 57, 52Platelet count; Week 20; n=56, 54, 55, 49Platelet count; Week 24; n=56, 53, 56, 47Platelet count; Week 26; n=48, 50, 53, 45Platelet count; Week 28; n=50, 52, 52, 45Platelet count; Week 32; n=51, 52, 55, 45Platelet count; Week 36; n=52, 53, 55, 44Platelet count; Week 40; n=51, 53, 54, 45Platelet count; Week 48; n=51, 52, 53, 44Platelet count; Week 60; n=48, 47, 51, 44Platelet count; Week 72; n=47, 48, 52, 42Platelet count; Week 84; n=46, 48, 51, 42Platelet count; Week 96; n=46, 45, 51, 41WBC count; Week 2; n=57, 56, 59, 59WBC count; Week 4; n=57, 57, 59, 57WBC count; Week 8; n=58, 56, 56, 55WBC; Week 12; n=58, 53, 57, 51WBC count; Week 16; n=57, 54, 57, 52WBC count; Week 20; n=56, 54, 55, 49WBC count; Week 24; n=56, 53, 56, 47WBC count; Week 26; n=48, 50, 53, 45WBC count; Week 28; n=50, 52, 52, 45WBC count; Week 32; n=51, 53, 55, 45WBC count; Week 36; n=52, 53, 55, 44WBC count; Week 40; n=51, 53, 55, 45WBC count; Week 48; n=51, 53, 54, 44WBC count; Week 60; n=48, 47, 52, 44WBC count; Week 72; n=47, 48, 52, 42WBC count; Week 84; n=46, 48, 51, 42WBC count; Week 96; n=46, 46, 52, 41
Efavirenz 600 mg0.7160.3750.2730.5250.3670.7400.6370.4490.4460.7170.4140.7300.6650.8000.8920.7900.83117.115.610.311.29.317.123.917.517.213.812.318.920.630.828.318.917.50.690.290.270.540.360.780.550.350.390.710.360.750.730.951.020.950.92

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Change From Baseline in Total Neutrophils, Platelet Count and WBC Count Over Time by Visit

Blood samples were collected for the analysis of total neutrophils, platelet count and WBC count. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

,,
InterventionGiga cells per liter (Mean)
T. neutrophils; Week 2; n=57, 56, 59, 59T. neutrophils; Week 4; n=57, 57, 59, 57T. neutrophils; Week 8; n=58, 56, 56, 55T. neutrophils; Week 12; n=58, 53, 57, 51T. neutrophils; Week 16; n=57, 54, 57, 52T. neutrophils; Week 20; n=56, 54, 55, 49T. neutrophils; Week 24; n=56, 53, 56, 47T. neutrophils; Week 26; n=48, 50, 53, 45T. neutrophils; Week 28; n=50, 52, 52, 45T. neutrophils; Week 32; n=51, 53, 55, 45T. neutrophils; Week 36; n=52, 53, 55, 44T. neutrophils; Week 40; n=51, 53, 55, 45T. neutrophils; Week 48; n=51, 53, 54, 44T. neutrophils; Week 60; n=48, 47, 52, 44T. neutrophils; Week 72; n=47, 48, 52, 42T. neutrophils; Week 84; n=46, 48, 51, 42T. neutrophils; Week 96; n=46, 46, 52, 41T. neutrophils; Week 108; n=43, 46, 49, 0T. neutrophils; Week 120; n=41, 46, 49, 0T. neutrophils; Week 132; n=40, 46, 49, 0T. neutrophils; Week 144; n=37, 45, 46, 0T. neutrophils; Week 156; n=37, 42, 49, 0T. neutrophils; Week 168; n=35, 43, 47, 0T. neutrophils; Week 180; n=36, 41, 47, 0T. neutrophils; Week 192; n=35, 40, 47, 0T. neutrophils; Week 204; n=34, 39, 47, 0T. neutrophils; Week 216; n=32, 39, 43, 0T. neutrophils; Week 228; n=30, 39, 47, 0T. neutrophils; Week 240; n=32, 39, 47, 0T. neutrophils; Week 252; n=31, 36, 45, 0T. neutrophils; Week 264; n=32, 38, 46, 0T. neutrophils; Week 276; n=31, 38, 45, 0T. neutrophils; Week 288; n=30, 38, 44, 0T. neutrophils; Week 300; n=30, 37, 43, 0T. neutrophils; Week 312; n=31, 33, 41, 0T. neutrophils; Week 324; n=3, 4, 2, 0Platelet count; Week 2; n=57, 56, 59, 59Platelet count; Week 4; n=57, 57, 59, 57Platelet count; Week 8; n=58, 56, 56, 55Platelet count; Week 12; n=58, 53, 57, 51Platelet count; Week 16; n=57, 54, 57, 52Platelet count; Week 20; n=56, 54, 55, 49Platelet count; Week 24; n=56, 53, 56, 47Platelet count; Week 26; n=48, 50, 53, 45Platelet count; Week 28; n=50, 52, 52, 45Platelet count; Week 32; n=51, 52, 55, 45Platelet count; Week 36; n=52, 53, 55, 44Platelet count; Week 40; n=51, 53, 54, 45Platelet count; Week 48; n=51, 52, 53, 44Platelet count; Week 60; n=48, 47, 51, 44Platelet count; Week 72; n=47, 48, 52, 42Platelet count; Week 84; n=46, 48, 51, 42Platelet count; Week 96; n=46, 45, 51, 41Platelet count; Week 108; n=43, 46, 49, 0Platelet count; Week 120; n=41, 46, 49, 0Platelet count; Week 132; n=40, 46, 48, 0Platelet count; Week 144; n=37, 45, 44, 0Platelet count; Week 156; n=37, 42, 47, 0Platelet count; Week 168; n=35, 43, 46, 0Platelet count; Week 180; n=36, 41, 46, 0Platelet count; Week 192; n=35, 40, 46, 0Platelet count; Week 204; n=34, 39, 45, 0Platelet count; Week 216; n=32, 39, 44, 0Platelet count; Week 228; n=31, 39, 46, 0Platelet count; Week 240; n=32, 39, 47, 0Platelet count; Week 252; n=31, 36, 44, 0Platelet count; Week 264; n=32, 38, 45, 0Platelet count; Week 276; n=31, 38, 45, 0Platelet count; Week 288; n=30, 38, 43, 0Platelet count; Week 300; n=30, 37, 40, 0Platelet count; Week 312; n=31, 33, 41, 0Platelet count; Week 324; n=3, 4, 2, 0WBC count; Week 2; n=57, 56, 59, 59WBC count; Week 4; n=57, 57, 59, 57WBC count; Week 8; n=58, 56, 56, 55WBC; Week 12; n=58, 53, 57, 51WBC count; Week 16; n=57, 54, 57, 52WBC count; Week 20; n=56, 54, 55, 49WBC count; Week 24; n=56, 53, 56, 47WBC count; Week 26; n=48, 50, 53, 45WBC count; Week 28; n=50, 52, 52, 45WBC count; Week 32; n=51, 53, 55, 45WBC count; Week 36; n=52, 53, 55, 44WBC count; Week 40; n=51, 53, 55, 45WBC count; Week 48; n=51, 53, 54, 44WBC count; Week 60; n=48, 47, 52, 44WBC count; Week 72; n=47, 48, 52, 42WBC count; Week 84; n=46, 48, 51, 42WBC count; Week 96; n=46, 46, 52, 41WBC count; Week 108; n=43, 46, 49, 0WBC count; Week 120; n=41, 46, 49, 0WBC count; Week 132; n=40, 46, 49, 0WBC count; Week 144; n=37, 45, 46, 0WBC count; Week 156; n=37, 42, 49, 0WBC count; Week 168; n=35, 43, 47, 0WBC count; Week 180; n=36, 41, 47, 0WBC count; Week 192; n=35, 40, 47, 0WBC count; Week 204; n=34, 39, 47, 0WBC count; Week 216; n=32, 39, 43, 0WBC count; Week 228; n=31, 39, 47, 0WBC count; Week 240; n=32, 39, 47, 0WBC count; Week 252; n=31, 36, 45, 0WBC count; Week 264; n=32, 38, 46, 0WBC count; Week 276; n=31, 38, 45, 0WBC count; Week 288; n=30, 38, 44, 0WBC count; Week 300; n=30, 37, 43, 0WBC count; Week 312; n=31, 33, 41, 0WBC count; Week 324; n=3, 4, 2, 0
GSK1265744 10 mg0.0420.0380.2510.1380.3880.2700.4620.1200.4960.0710.4200.4300.3860.3740.3830.4100.6310.6230.3720.7770.6720.7620.5880.7690.4900.6180.5430.7800.5080.2680.4750.4000.4560.1390.2430.86011.09.910.313.716.517.212.08.36.67.75.211.112.520.923.713.625.924.523.816.827.126.634.928.434.733.928.128.727.215.927.948.444.128.527.331.70.190.160.370.320.450.360.470.190.670.250.560.570.430.600.630.710.950.890.590.920.911.050.971.070.610.980.880.980.790.660.620.920.920.580.571.97
GSK1265744 30 mg-0.084-0.083-0.0660.040-0.1560.0320.1090.0520.2130.1490.0290.1780.2450.4580.2740.5280.6980.5700.6500.4050.4680.4180.5340.4050.5940.6480.5880.7890.8130.7610.7610.6270.6730.4550.4170.31516.620.125.914.611.314.518.411.215.811.610.88.920.018.722.817.220.824.626.921.023.230.636.427.624.626.425.227.126.215.423.234.535.526.830.98.30.130.020.150.280.020.230.340.260.420.450.300.420.530.760.560.961.010.901.010.710.820.750.970.690.890.951.011.131.151.101.211.041.130.770.700.53
GSK1265744 60 mg0.1040.1550.3410.3590.2030.5250.4060.3750.5020.6920.5350.5750.5340.7110.6661.0060.9971.0060.7690.6710.8311.0951.0110.8400.7220.8210.9140.8191.0830.8121.1761.1060.9130.6990.5640.96014.314.118.417.717.913.719.310.317.815.411.87.817.626.622.721.121.733.120.432.233.541.240.045.427.937.633.529.127.430.832.845.846.745.435.32.00.310.300.480.730.360.770.640.660.690.930.920.810.781.041.091.431.381.351.161.021.221.641.581.331.111.241.371.311.531.171.661.571.321.020.95-0.05

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Change From Baseline in Plasma log10 HIV-1 RNA Over Time by Visit

Plasma samples for quantitative analysis of HIV-1 RNA were collected at indicated time points. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

,,
InterventionLog10 copies per milliliter (Mean)
Week 2; n=57, 56, 59, 59Week 4; n=58, 57, 59, 57Week 8; n=59, 56, 57, 55Week 12; n=58, 52, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 56, 47Week 24; n=56, 53, 56, 48Week 26; n=48, 50, 53, 44Week 28; n=51, 52, 52, 45Week 32; n=52, 53, 55, 45Week 36; n=52, 53, 55, 45Week 40; n=52, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 48, 53, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 52, 42Week 96; n=45, 48, 52, 40Week 108; n=43, 46, 49, 0Week 120; n=41, 46, 49, 0Week 132; n=40, 46, 49, 0Week 144; n=37, 45, 47, 0Week 156; n=37, 42, 49, 0Week 168; n=35, 43, 47, 0Week 180; n=36, 41, 47, 0Week 192; n=36, 40, 47, 0Week 204; n=34, 39, 47, 0Week 216; n=33, 39, 47, 0Week 228; n=32, 39, 47, 0Week 240; n=31, 39, 45, 0Week 252; n=31, 38, 47, 0Week 264; n=32, 38, 47, 0Week 276; n=31, 38, 45, 0Week 288; n=30, 38, 45, 0Week 300; n=31, 37, 44, 0Week 312; n=31, 33, 43, 0Week 324; n=3, 4, 3, 0
GSK1265744 10 mg-2.534-2.731-2.733-2.793-2.823-2.823-2.831-2.788-2.784-2.763-2.768-2.760-2.682-2.729-2.745-2.722-2.670-2.723-2.712-2.705-2.690-2.737-2.680-2.747-2.671-2.750-2.787-2.770-2.798-2.787-2.780-2.786-2.768-2.776-2.780-2.488
GSK1265744 30 mg-2.306-2.550-2.611-2.634-2.659-2.665-2.659-2.662-2.663-2.636-2.646-2.638-2.602-2.613-2.514-2.568-2.608-2.632-2.650-2.610-2.555-2.645-2.592-2.628-2.641-2.632-2.636-2.636-2.627-2.601-2.659-2.659-2.659-2.664-2.569-2.215
GSK1265744 60 mg-2.504-2.718-2.741-2.790-2.815-2.834-2.830-2.792-2.791-2.781-2.792-2.790-2.799-2.787-2.783-2.782-2.778-2.743-2.717-2.743-2.703-2.716-2.700-2.767-2.667-2.718-2.718-2.726-2.736-2.758-2.734-2.764-2.775-2.730-2.789-2.438

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Change From Baseline in Plasma log10 HIV-1 RNA Over Time by Visit

Plasma samples for quantitative analysis of HIV-1 RNA were collected at indicated time points. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

InterventionLog10 copies per milliliter (Mean)
Week 2; n=57, 56, 59, 59Week 4; n=58, 57, 59, 57Week 8; n=59, 56, 57, 55Week 12; n=58, 52, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 56, 47Week 24; n=56, 53, 56, 48Week 26; n=48, 50, 53, 44Week 28; n=51, 52, 52, 45Week 32; n=52, 53, 55, 45Week 36; n=52, 53, 55, 45Week 40; n=52, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 48, 53, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 52, 42Week 96; n=45, 48, 52, 40
Efavirenz 600 mg-1.875-2.092-2.344-2.533-2.602-2.666-2.694-2.733-2.714-2.672-2.679-2.679-2.676-2.615-2.738-2.739-2.731

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Change From Baseline in Hemoglobin Level Over Time by Visit

Blood samples were collected for the analysis of hemoglobin level. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

,,
InterventionGrams per liter (Mean)
Week 2; n=57, 56, 59, 59Week 4; n=57, 57, 59, 57Week 8; n=58, 56, 56, 55Week 12; n=58, 53, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 55, 49Week 24; n=56, 53, 56, 47Week 26; n=48, 50, 53, 45Week 28; n=50, 52, 52, 45Week 32; n=51, 53, 55, 45Week 36; n=52, 53, 55, 44Week 40; n=51, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 47, 52, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 51, 42Week 96; n=46, 46, 52, 41Week 108; n=43, 46, 49, 0Week 120; n=41, 46, 49, 0Week 132; n=40, 46, 49, 0Week 144; n=37, 45, 46, 0Week 156; n=37, 42, 49, 0Week 168; n=35, 43, 47, 0Week 180; n=36, 41, 47, 0Week 192; n=35, 40, 47, 0Week 204; n=34, 39, 47, 0Week 216; n=32, 39, 44, 0Week 228; n=31, 39, 47, 0Week 240; n=32, 39, 47, 0Week 252; n=31, 36, 45, 0Week 264; n=32, 38, 46, 0Week 276; n=31, 38, 46, 0Week 288; n=30, 38, 44, 0Week 300; n=30, 37, 43, 0Week 312; n=31, 33, 42, 0Week 324; n=3, 4, 2, 0
GSK1265744 10 mg0.1-0.22.72.01.12.12.61.81.71.60.30.51.22.61.83.32.74.04.23.54.04.06.35.53.34.54.75.16.26.26.36.67.34.67.04.3
GSK1265744 30 mg0.00.54.83.93.53.84.83.44.03.12.92.22.74.74.54.03.33.44.73.02.65.16.04.03.54.74.14.85.86.46.05.56.85.16.110.0
GSK1265744 60 mg-0.70.62.02.62.33.13.62.51.53.52.72.1-0.52.22.43.03.63.02.12.52.32.74.82.73.03.23.43.12.15.85.55.46.95.58.020.5

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Change From Baseline in Hemoglobin Level Over Time by Visit

Blood samples were collected for the analysis of hemoglobin level. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

InterventionGrams per liter (Mean)
Week 2; n=57, 56, 59, 59Week 4; n=57, 57, 59, 57Week 8; n=58, 56, 56, 55Week 12; n=58, 53, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 55, 49Week 24; n=56, 53, 56, 47Week 26; n=48, 50, 53, 45Week 28; n=50, 52, 52, 45Week 32; n=51, 53, 55, 45Week 36; n=52, 53, 55, 44Week 40; n=51, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 47, 52, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 51, 42Week 96; n=46, 46, 52, 41
Efavirenz 600 mg0.70.72.02.81.10.81.92.20.10.6-0.8-0.20.02.32.41.71.9

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Change From Baseline in Estimated Creatinine Clearance Over Time by Visit

Blood samples were collected for the analysis of estimated creatinine clearance. Estimated creatinine clearance was calculated using Cockcroft-Gault formula. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 16, 20, 24, 26, 40, 48, 60, 96, 180, 204, 252 and 264

InterventionMilliliters per minute (Mean)
Week 2; n=1, 1, 0, 3Week 4; n=58, 57, 59, 57Week 8; n=2, 1, 1, 1Week 16; n=55, 53, 56, 49Week 20; n=2, 0, 0, 1Week 24; n=52, 53, 55, 46Week 48; n=51, 50, 54, 44Week 96; n=45, 48, 52, 40Week 180; n=1, 0, 0, 0
GSK1265744 10 mg-3.0-1.45.52.28.0-2.7-2.62.21.0

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Change From Baseline in Estimated Creatinine Clearance Over Time by Visit

Blood samples were collected for the analysis of estimated creatinine clearance. Estimated creatinine clearance was calculated using Cockcroft-Gault formula. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 16, 20, 24, 26, 40, 48, 60, 96, 180, 204, 252 and 264

InterventionMilliliters per minute (Mean)
Week 4; n=58, 57, 59, 57Week 8; n=2, 1, 1, 1Week 16; n=55, 53, 56, 49Week 24; n=52, 53, 55, 46Week 48; n=51, 50, 54, 44Week 96; n=45, 48, 52, 40Week 264; n=0, 0, 1, 0
GSK1265744 60 mg-4.97.0-2.7-5.8-4.5-9.0-143.0

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Change From Baseline in Estimated Creatinine Clearance Over Time by Visit

Blood samples were collected for the analysis of estimated creatinine clearance. Estimated creatinine clearance was calculated using Cockcroft-Gault formula. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 16, 20, 24, 26, 40, 48, 60, 96, 180, 204, 252 and 264

InterventionMilliliters per minute (Mean)
Week 2; n=1, 1, 0, 3Week 4; n=58, 57, 59, 57Week 8; n=2, 1, 1, 1Week 16; n=55, 53, 56, 49Week 24; n=52, 53, 55, 46Week 26; n=0, 1, 0, 0Week 40; n=0, 1, 0, 0Week 48; n=51, 50, 54, 44Week 96; n=45, 48, 52, 40Week 204; n=0, 1, 0, 0Week 252; n=0, 1, 0, 0
GSK1265744 30 mg-10.0-3.7-1.00.2-6.4-7.0-95.0-1.1-2.4-23.00.0

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Change From Baseline in Creatinine and Total Bilirubin Over Time by Visit

Blood samples were collected for the analysis of creatinine and total bilirubin. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

,,
InterventionMicromoles per liter (Mean)
Creatinine; Week 2; n=58, 56, 58, 58Creatinine; Week 4; n=58, 57, 59, 57Creatinine; Week 8; n=58, 55, 57, 54Creatinine; Week 12; n=58, 53, 57, 51Creatinine; Week 16; n=57, 54, 57, 52Creatinine; Week 20; n=56, 54, 55, 49Creatinine; Week 24; n=56, 53, 56, 47Creatinine; Week 26; n=48, 50, 53, 45Creatinine; Week 28; n=51, 52, 52, 45Creatinine; Week 32; n=52, 53, 55, 45Creatinine; Week 36; n=52, 52, 55, 45Creatinine; Week 40; n=52, 53, 55, 44Creatinine; Week 48; n=51, 53, 54, 44Creatinine; Week 60; n=48, 47, 53, 44Creatinine; Week 72; n=47, 47, 52, 42Creatinine; Week 84; n=46, 48, 52, 42Creatinine; Week 96; n=45, 48, 52, 40Creatinine; Week 108; n=43, 46, 48, 0Creatinine; Week 120; n=40, 45, 48, 0Creatinine; Week 132; n=40, 46, 49, 0Creatinine; Week 144; n=37, 45, 47, 0Creatinine; Week 156; n=37, 42, 49, 0Creatinine; Week 168; n=35, 43, 47, 0Creatinine; Week 180; n=36, 41, 47, 0Creatinine; Week 192; n=36, 39, 47, 0Creatinine; Week 204; n=34, 39, 47, 0Creatinine; Week 216; n=33, 39, 46, 0Creatinine; Week 228; n=32, 39, 47, 0Creatinine; Week 240; n=30, 39, 46, 0Creatinine; Week 252; n=31, 38, 46, 0Creatinine; Week 264; n=32, 38, 47, 0Creatinine; Week 276; n=31, 38, 45, 0Creatinine; Week 288; n=31, 38, 45, 0Creatinine; Week 300; n=30, 37, 44, 0Creatinine; Week 312; n=31, 34, 43, 0Creatinine; Week 324; n=3, 4, 3, 0T. Bilirubin; Week 2; n=58, 56, 58, 58T. Bilirubin; Week 4; n=58, 57, 59, 57T. Bilirubin; Week 8; n=58, 55, 57, 54T. Bilirubin; Week 12; n=58, 53, 57, 51T. Bilirubin; Week 16; n=57, 54, 57, 52T. Bilirubin; Week 20; n=56, 54, 55, 49T. Bilirubin; Week 24; n=56, 53, 56, 47T. Bilirubin; Week 26; n=48, 50, 53, 45T. Bilirubin; Week 28; n=51, 52, 52, 45T. Bilirubin; Week 32; n=52, 53, 55, 45T. Bilirubin; Week 36; n=52, 52, 55, 45T. Bilirubin; Week 40; n=52, 53, 55, 44T. Bilirubin; Week 48; n=51, 53, 54, 44T. Bilirubin; Week 60; n=48, 47, 53, 44T. Bilirubin; Week 72; n=47, 47, 52, 42T. Bilirubin; Week 84; n=46, 48, 52, 42T. Bilirubin; Week 96; n=45, 48, 52, 40T. Bilirubin; Week 108; n=43, 46, 48, 0T. Bilirubin; Week 120; n=40, 45, 48, 0T. Bilirubin; Week 132; n=40, 46, 49, 0T. Bilirubin; Week 144; n=37, 45, 47, 0T. Bilirubin; Week 156; n=37, 42, 49, 0T. Bilirubin; Week 168; n=35, 43, 47, 0T. Bilirubin; Week 180; n=36, 41, 47, 0T. Bilirubin; Week 192; n=36, 39, 47, 0T. Bilirubin; Week 204; n=34, 39, 47, 0T. Bilirubin; Week 216; n=33, 39, 46, 0T. Bilirubin; Week 228; n=32, 39, 47, 0T. Bilirubin; Week 240; n=30, 39, 46, 0T. Bilirubin; Week 252; n=31, 38, 46, 0T. Bilirubin; Week 264; n=32, 38, 47, 0T. Bilirubin; Week 276; n=31, 38, 45, 0T. Bilirubin; Week 288; n=31, 38, 45, 0T. Bilirubin; Week 300; n=30, 37, 44, 0T. Bilirubin; Week 312; n=31, 34, 43, 0T. Bilirubin; Week 324; n=3, 4, 3, 0
GSK1265744 10 mg3.362.242.383.392.912.542.522.742.223.363.112.832.753.283.894.581.905.874.413.765.995.286.575.896.906.218.347.168.486.965.977.898.8110.497.9815.900.00.10.00.40.4-0.10.51.11.10.71.21.60.91.91.52.31.00.70.91.00.71.61.11.10.71.10.51.61.21.40.40.70.51.11.45.3
GSK1265744 30 mg2.582.502.061.591.100.852.441.802.801.693.412.362.182.304.713.805.345.184.154.025.806.365.625.087.916.469.317.197.337.527.105.847.849.167.869.75-0.3-0.3-0.5-0.9-1.2-0.70.20.50.70.20.61.70.10.00.10.10.01.41.12.01.11.00.80.00.30.70.80.50.92.02.92.81.91.71.15.5
GSK1265744 60 mg4.154.083.443.792.095.294.456.035.015.006.004.764.474.466.596.537.767.266.784.995.075.166.825.915.905.167.426.617.087.646.996.196.208.197.105.03-0.4-0.8-0.6-0.5-0.2-0.4-0.71.00.50.91.41.5-0.30.90.61.21.70.81.31.10.41.01.41.00.90.60.3-0.3-0.10.2-0.10.90.00.90.80.7

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Change From Baseline in Creatinine and Total Bilirubin Over Time by Visit

Blood samples were collected for the analysis of creatinine and total bilirubin. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

InterventionMicromoles per liter (Mean)
Creatinine; Week 2; n=58, 56, 58, 58Creatinine; Week 4; n=58, 57, 59, 57Creatinine; Week 8; n=58, 55, 57, 54Creatinine; Week 12; n=58, 53, 57, 51Creatinine; Week 16; n=57, 54, 57, 52Creatinine; Week 20; n=56, 54, 55, 49Creatinine; Week 24; n=56, 53, 56, 47Creatinine; Week 26; n=48, 50, 53, 45Creatinine; Week 28; n=51, 52, 52, 45Creatinine; Week 32; n=52, 53, 55, 45Creatinine; Week 36; n=52, 52, 55, 45Creatinine; Week 40; n=52, 53, 55, 44Creatinine; Week 48; n=51, 53, 54, 44Creatinine; Week 60; n=48, 47, 53, 44Creatinine; Week 72; n=47, 47, 52, 42Creatinine; Week 84; n=46, 48, 52, 42Creatinine; Week 96; n=45, 48, 52, 40T. Bilirubin; Week 2; n=58, 56, 58, 58T. Bilirubin; Week 4; n=58, 57, 59, 57T. Bilirubin; Week 8; n=58, 55, 57, 54T. Bilirubin; Week 12; n=58, 53, 57, 51T. Bilirubin; Week 16; n=57, 54, 57, 52T. Bilirubin; Week 20; n=56, 54, 55, 49T. Bilirubin; Week 24; n=56, 53, 56, 47T. Bilirubin; Week 26; n=48, 50, 53, 45T. Bilirubin; Week 28; n=51, 52, 52, 45T. Bilirubin; Week 32; n=52, 53, 55, 45T. Bilirubin; Week 36; n=52, 52, 55, 45T. Bilirubin; Week 40; n=52, 53, 55, 44T. Bilirubin; Week 48; n=51, 53, 54, 44T. Bilirubin; Week 60; n=48, 47, 53, 44T. Bilirubin; Week 72; n=47, 47, 52, 42T. Bilirubin; Week 84; n=46, 48, 52, 42T. Bilirubin; Week 96; n=45, 48, 52, 40
Efavirenz 600 mg0.65-0.32-0.92-1.42-2.92-3.26-2.03-2.67-3.42-3.50-3.26-2.83-2.73-3.87-4.48-2.48-2.28-3.0-3.4-3.4-2.4-2.4-2.6-2.9-2.7-2.8-2.6-2.7-2.9-2.6-2.2-2.7-2.6-2.5

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Change From Baseline in CD4+ Cell Count Over Time by Visit

CD4+ cell counts were assessed by flow cytometry. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

,,
InterventionCells per cubic millimeter (Mean)
Week 2; n=57, 56, 59, 59Week 4; n=58, 57, 59, 57Week 8; n=58, 56, 57, 55Week 12; n=58, 53, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 56, 49Week 24; n=56, 53, 56, 47Week 26; n=48, 50, 53, 45Week 28; n=49, 52, 52, 45Week 32; n=52, 53, 55, 45Week 36; n=52, 53, 55, 45Week 40; n=52, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 47, 53, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 52, 42Week 96; n=46, 46, 52, 41Week 108; n=43, 46, 49, 0Week 120; n=41, 46, 49, 0Week 132; n=40, 46, 49, 0Week 144; n=37, 45, 46, 0Week 156; n=37, 42, 49, 0Week 168; n=35, 43, 47, 0Week 180; n=36, 41, 47, 0Week 192; n=35, 40, 47, 0Week 204; n=34, 39, 47, 0Week 216; n=33, 39, 47, 0Week 228; n=32, 39, 47, 0Week 240; n=32, 39, 47, 0Week 252; n=31, 38, 47, 0Week 264; n=32, 38, 47, 0Week 276; n=31, 38, 46, 0Week 288; n=30, 38, 45, 0Week 300; n=30, 37, 44, 0Week 312; n=30, 34, 43, 0Week 324; n=3, 4, 3, 0
GSK1265744 10 mg92.6136.4129.9140.5159.3165.2172.5186.4205.0191.4192.0203.6235.1217.7232.0261.5269.4296.2266.1297.1330.7334.5338.1338.0300.8369.5397.0331.8356.5400.3344.4398.3411.0437.7335.0402.0
GSK1265744 30 mg79.576.9117.8140.8142.2153.8180.9177.7188.1205.2213.0212.8241.6269.4201.4287.0267.5304.3279.3305.2308.9319.2332.4348.6351.0332.9373.4366.5395.9343.7365.0350.3383.5404.4433.0276.0
GSK1265744 60 mg91.788.290.5145.2148.3182.6204.0194.7193.3209.9265.0212.3259.0266.1254.0278.1286.2288.4307.2313.2322.4320.4361.3384.2342.3340.0357.8383.7408.4383.1391.8362.2337.1353.5407.0272.0

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Change From Baseline in CD4+ Cell Count Over Time by Visit

CD4+ cell counts were assessed by flow cytometry. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

InterventionCells per cubic millimeter (Mean)
Week 2; n=57, 56, 59, 59Week 4; n=58, 57, 59, 57Week 8; n=58, 56, 57, 55Week 12; n=58, 53, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 56, 49Week 24; n=56, 53, 56, 47Week 26; n=48, 50, 53, 45Week 28; n=49, 52, 52, 45Week 32; n=52, 53, 55, 45Week 36; n=52, 53, 55, 45Week 40; n=52, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 47, 53, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 52, 42Week 96; n=46, 46, 52, 41
Efavirenz 600 mg24.846.065.6103.4135.5149.0143.4166.4178.2197.4185.2221.5262.5263.8257.1279.4281.7

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Change From Baseline in ALT, AST and CK Over Time by Visit

Blood samples were collected for the analysis of ALT, AST and CK. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

InterventionInternational Units per Liter (Mean)
ALT; Week 2; n=58, 56, 58, 58ALT; Week 4; n=58, 57, 59, 57ALT; Week 8; n=58, 55, 57, 54ALT; Week 12; n=58, 53, 57, 51ALT; Week 16; n=57, 54, 57, 52ALT; Week 20; n=56, 54, 55, 49ALT; Week 24; n=56, 53, 56, 47ALT; Week 26; n=48, 50, 53, 45ALT; Week 28; n=51, 52, 52, 45ALT; Week 32; n=52, 53, 55, 45ALT; Week 36; n=52, 52, 55, 45ALT; Week 40; n=52, 53, 55, 44ALT; Week 48; n=51, 53, 54, 44ALT; Week 60; n=48, 47, 53, 44ALT; Week 72; n=47, 47, 52, 42ALT; Week 84; n=46, 48, 52, 42ALT; Week 96; n=45, 48, 52, 40AST; Week 2; n=58, 56, 58, 58AST; Week 4; n=58, 57, 59, 57AST; Week 8; n=58, 55, 57, 54AST; Week 12; n=58, 53, 57, 50AST; Week 16; n=57, 54, 57, 52AST; Week 20; n=56, 54, 55, 49AST; Week 24; n=56, 53, 56, 47AST; Week 26; n=48, 50, 53, 45AST; Week 28; n=51, 52, 52, 45AST; Week 32; n=52, 53, 55, 45AST; Week 36; n=52, 52, 55, 45AST; Week 40; n=52, 53, 55, 44AST; Week 48; n=51, 53, 54, 44AST; Week 60; n=48, 47, 53, 44AST; Week 72; n=47, 47, 52, 42AST; Week 84; n=46, 48, 52, 42AST; Week 96; n=45, 48, 52, 40CK; Week 2; n=58, 56, 58, 58CK; Week 4; n=58, 57, 59, 57CK; Week 8; n=58, 55, 57, 54CK; Week 12; n=58, 53, 57, 51CK; Week 16; n=57, 54, 57, 52CK; Week 20; n=56, 54, 55, 49CK; Week 24; n=56, 53, 56, 47CK; Week 26; n=48, 50, 53, 45CK; Week 28; n=51, 52, 52, 45CK; Week 32; n=52, 53, 55, 45CK; Week 36; n=52, 52, 55, 45CK; Week 40; n=52, 53, 55, 44CK; Week 48; n=51, 53, 54, 44CK; Week 60; n=48, 47, 53, 44CK; Week 72; n=47, 47, 52, 42CK; Week 84; n=46, 48, 52, 42CK; Week 96; n=45, 48, 52, 40
Efavirenz 600 mg-1.30.1-6.3-6.3-1.6-4.8-6.0-3.7-8.1-8.6-8.2-8.0-8.6-6.3-8.5-4.0-7.60.9-2.9-7.3-7.94.4-3.6-2.1-2.6-5.1-2.8-1.9-5.1-4.4-3.2-4.62.3-0.3159.8-120.3-212.8-220.1269.7135.3103.921.24.1110.3158.73.82.824.5-14.3123.9143.9

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Change From Baseline in ALT, AST and CK Over Time by Visit

Blood samples were collected for the analysis of ALT, AST and CK. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

,,
InterventionInternational Units per Liter (Mean)
ALT; Week 2; n=58, 56, 58, 58ALT; Week 4; n=58, 57, 59, 57ALT; Week 8; n=58, 55, 57, 54ALT; Week 12; n=58, 53, 57, 51ALT; Week 16; n=57, 54, 57, 52ALT; Week 20; n=56, 54, 55, 49ALT; Week 24; n=56, 53, 56, 47ALT; Week 26; n=48, 50, 53, 45ALT; Week 28; n=51, 52, 52, 45ALT; Week 32; n=52, 53, 55, 45ALT; Week 36; n=52, 52, 55, 45ALT; Week 40; n=52, 53, 55, 44ALT; Week 48; n=51, 53, 54, 44ALT; Week 60; n=48, 47, 53, 44ALT; Week 72; n=47, 47, 52, 42ALT; Week 84; n=46, 48, 52, 42ALT; Week 96; n=45, 48, 52, 40ALT; Week 108; n=43, 46, 48, 0ALT; Week 120; n=40, 45, 48, 0ALT; Week 132; n=40, 46, 49, 0ALT; Week 144; n=37, 45, 47, 0ALT; Week 156; n=37, 42, 49, 0ALT; Week 168; n=35, 43, 47, 0ALT; Week 180; n=36, 41, 47, 0ALT; Week 192; n=36, 39, 47, 0ALT; Week 204; n=34, 39, 47, 0ALT; Week 216; n=33, 39, 46, 0ALT; Week 228; n=32, 39, 47, 0ALT; Week 240; n=30, 39, 46, 0ALT; Week 252; n=31, 38, 46, 0ALT; Week 264; n=32, 38, 47, 0ALT; Week 276; n=31, 38, 45, 0ALT; Week 288; n=31, 38, 45, 0ALT; Week 300; n=30, 37, 44, 0ALT; Week 312; n=31, 34, 43, 0ALT; Week 324; n=3, 4, 3, 0AST; Week 2; n=58, 56, 58, 58AST; Week 4; n=58, 57, 59, 57AST; Week 8; n=58, 55, 57, 54AST; Week 12; n=58, 53, 57, 50AST; Week 16; n=57, 54, 57, 52AST; Week 20; n=56, 54, 55, 49AST; Week 24; n=56, 53, 56, 47AST; Week 26; n=48, 50, 53, 45AST; Week 28; n=51, 52, 52, 45AST; Week 32; n=52, 53, 55, 45AST; Week 36; n=52, 52, 55, 45AST; Week 40; n=52, 53, 55, 44AST; Week 48; n=51, 53, 54, 44AST; Week 60; n=48, 47, 53, 44AST; Week 72; n=47, 47, 52, 42AST; Week 84; n=46, 48, 52, 42AST; Week 96; n=45, 48, 52, 40AST; Week 108; n=43, 46, 48, 0AST; Week 120; n=40, 45, 48, 0AST; Week 132; n=40, 46, 49, 0AST; Week 144; n=37, 45, 47, 0AST; Week 156; n=37, 42, 49, 0AST; Week 168; n=35, 43, 47, 0AST; Week 180; n=36, 41, 47, 0AST; Week 192; n=36, 39, 47, 0AST; Week 204; n=34, 39, 47, 0AST; Week 216; n=33, 39, 46, 0AST; Week 228; n=32, 39, 47, 0AST; Week 240; n=30, 39, 46, 0AST; Week 252; n=31, 38, 46, 0AST; Week 264; n=32, 38, 47, 0AST; Week 276; n=31, 38, 45, 0AST; Week 288; n=31, 38, 45, 0AST; Week 300; n=30, 37, 44, 0AST; Week 312; n=31, 34, 43, 0AST; Week 324; n=3, 4, 3, 0CK; Week 2; n=58, 56, 58, 58CK; Week 4; n=58, 57, 59, 57CK; Week 8; n=58, 55, 57, 54CK; Week 12; n=58, 53, 57, 51CK; Week 16; n=57, 54, 57, 52CK; Week 20; n=56, 54, 55, 49CK; Week 24; n=56, 53, 56, 47CK; Week 26; n=48, 50, 53, 45CK; Week 28; n=51, 52, 52, 45CK; Week 32; n=52, 53, 55, 45CK; Week 36; n=52, 52, 55, 45CK; Week 40; n=52, 53, 55, 44CK; Week 48; n=51, 53, 54, 44CK; Week 60; n=48, 47, 53, 44CK; Week 72; n=47, 47, 52, 42CK; Week 84; n=46, 48, 52, 42CK; Week 96; n=45, 48, 52, 40CK; Week 108; n=43, 46, 48, 0CK; Week 120; n=40, 45, 48, 0CK; Week 132; n=40, 46, 49, 0CK; Week 144; n=37, 45, 47, 0CK; Week 156; n=37, 42, 49, 0CK; Week 168; n=35, 43, 47, 0CK; Week 180; n=36, 41, 47, 0CK; Week 192; n=36, 39, 47, 0CK; Week 204; n=34, 39, 47, 0CK; Week 216; n=33, 39, 46, 0CK; Week 228; n=32, 39, 47, 0CK; Week 240; n=30, 39, 46, 0CK; Week 252; n=31, 38, 46, 0CK; Week 264; n=32, 38, 47, 0CK; Week 276; n=31, 38, 45, 0CK; Week 288; n=31, 38, 45, 0CK; Week 300; n=30, 37, 44, 0CK; Week 312; n=31, 34, 43, 0CK; Week 324; n=3, 4, 3, 0
GSK1265744 10 mg0.1-0.72.21.22.1-0.7-2.11.1-2.3-3.10.80.1-4.1-1.0-2.8-2.4-0.40.54.44.30.1-0.52.31.74.91.91.736.85.32.03.33.36.64.85.517.70.7-1.04.21.3-0.71.3-1.43.3-2.0-2.74.60.1-3.3-0.9-2.7-2.2-0.8-1.00.1-0.2-3.4-3.0-0.8-1.9-1.5-1.7-2.713.5-1.0-2.2-1.6-1.5-1.4-2.011.72.740.0-2.3216.9120.6-2.0144.227.5133.79.83.1325.957.1-1.3115.4-19.8-0.7335.464.211.530.610.6-5.327.722.45.279.143.264.01.224.61.939.921.625.3727.5-1.3
GSK1265744 30 mg-2.1-2.60.52.70.1-3.6-1.2-2.6-2.3-1.7-4.2-4.1-3.8-2.62.71.920.6-2.7-2.6-3.0-3.4-1.8-1.1-2.8-3.3-1.7-3.0-1.1-0.12.80.72.91.2-1.47.61.3-1.3-2.81.51.61.9-3.1-0.3-0.9-0.2-1.0-2.1-2.9-3.2-2.03.72.020.5-4.0-2.5-3.9-4.3-3.2-3.4-4.2-5.3-4.8-4.9-5.9-5.3-2.1-4.3-3.3-3.6-5.3-2.3-5.3-32.2-82.0115.839.8156.3-68.932.4-16.374.1-25.1-33.6-48.6-54.7-80.153.833.6-22.8-88.5-48.9-41.3-72.4-87.9-60.7-16.4-98.5-101.8-74.4-129.0-108.1-110.1-31.3-126.5-98.5-100.7-141.3-195.0
GSK1265744 60 mg-1.51.78.0-0.6-0.33.01.4-1.7-2.9-4.0-3.0-1.4-2.40.5-0.9-2.0-1.7-0.7-3.7-3.8-1.8-2.2-3.6-1.21.3-3.4-2.70.5-0.7-1.62.01.11.9-1.80.01.0-1.60.15.3-1.7-0.64.61.5-1.7-1.9-1.4-0.6-0.5-3.03.0-0.5-1.8-1.00.6-2.40.7-3.9-4.1-3.8-2.90.1-4.5-4.3-2.8-3.4-3.9-2.9-1.4-2.2-4.1-0.3-6.70.4-2.9266.727.128.6298.955.954.496.8122.166.1103.528.6206.267.614.919.6100.361.4649.668.773.374.462.898.648.341.940.492.062.538.9146.443.456.0209.4102.7

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Absolute Values for Platelet Count, Total Neutrophils and WBC Count During Double-blind Randomized Treatment Until Week 96

Blood samples were collected for the analysis of platelet count, total neutrophils (T. neutrophils) and WBC count. Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84 and 96

,,,
InterventionGiga cells per liter (Mean)
T. neutrophils; Baseline; n=60, 60, 61, 62T. neutrophils; Week 2; n=57, 56, 59, 59T. neutrophils; Week 4; n=57, 57, 59, 57T. neutrophils; Week 8; n=58, 56, 56, 55T. neutrophils; Week 12; n=58, 53, 57, 51T. neutrophils; Week 16; n=57, 54, 57, 52T. neutrophils; Week 20; n=56, 54, 55, 49T. neutrophils; Week 24; n=56, 53, 56, 47T. neutrophils; Week 26; n=48, 50, 53, 45T. neutrophils; Week 28; n=50, 52, 52, 45T. neutrophils; Week 32; n=51, 53, 55, 45T. neutrophils; Week 36; n=52, 53, 55, 44T. neutrophils; Week 40; n=51, 53, 55, 45T. neutrophils; Week 48; n=51, 53, 54, 44T. neutrophils; Week 60; n=48, 47, 52, 44T. neutrophils; Week 72; n=47, 48, 52, 42T. neutrophils; Week 84; n=46, 48, 51, 42T. neutrophils; Week 96; n=46, 46, 52, 41Platelet count; Baseline; n=60, 60, 61, 62Platelet count; Week 2; n=57, 56, 59, 59Platelet count; Week 4; n=57, 57, 59, 57Platelet count; Week 8; n=58, 56, 56, 55Platelet count; Week 12; n=58, 53, 57, 51Platelet count; Week 16; n=57, 54, 57, 52Platelet count; Week 20; n=56, 54, 55, 49Platelet count; Week 24; n=56, 53, 56, 47Platelet count; Week 26; n=48, 50, 53, 45Platelet count; Week 28; n=50, 52, 52, 45Platelet count; Week 32; n=51, 52, 55, 45Platelet count; Week 36; n=52, 53, 55, 44Platelet count; Week 40; n=51, 53, 54, 45Platelet count; Week 48; n=51, 52, 53, 44Platelet count; Week 60; n=48, 47, 51, 44Platelet count; Week 72; n=47, 48, 52, 42Platelet count; Week 84; n=46, 48, 51, 42Platelet count; Week 96; n=46, 45, 51, 41WBC count; Baseline; n=60, 60, 61, 62WBC count; Week 2; n=57, 56, 59, 59WBC count; Week 4; n=57, 57, 59, 57WBC count; Week 8; n=58, 56, 56, 55WBC count; Week 12; n=58, 53, 57, 51WBC count; Week 16; n=57, 54, 57, 52WBC count; Week 20; n=56, 54, 55, 49WBC count; Week 24; n=56, 53, 56, 47WBC count; Week 26; n=48, 50, 53, 45WBC count; Week 28; n=50, 52, 52, 45WBC count; Week 32; n=51, 53, 55, 45WBC count; Week 36; n=52, 53, 55, 44WBC count; Week 40; n=51, 53, 55, 45WBC count; Week 48; n=51, 53, 54, 44WBC count; Week 60; n=48, 47, 52, 44WBC count; Week 72; n=47, 48, 52, 42WBC count; Week 84; n=46, 48, 51, 42WBC count; Week 96; n=46, 46, 52, 41
Efavirenz 600 mg2.4413.2072.8482.7462.9792.8583.1873.1422.8862.9163.1742.9143.1873.1343.2693.3613.2593.297200.1216.2216.0209.8213.7211.4214.9220.9214.4215.4212.6209.8217.7220.3230.5225.9216.5214.04.705.455.025.025.275.135.505.345.085.145.485.175.515.535.755.845.785.75
GSK1265744 10 mg2.6432.7232.6852.8992.8123.0782.9583.1512.8853.1832.7973.1623.1553.1383.1643.1973.2453.466212.5225.0225.2224.5227.2230.0231.3226.1224.9223.3220.5220.0224.9225.6232.5234.0224.8237.15.065.325.245.445.415.565.465.575.305.715.305.645.635.515.735.805.916.14
GSK1265744 30 mg2.8912.7762.7712.8022.9332.7162.9042.9962.9583.0053.0362.9163.0653.1323.3333.1313.3853.540202.3222.0222.4228.4216.4212.4215.5219.7215.5217.0214.0212.1210.1221.2219.8224.4218.8221.85.195.305.175.305.505.205.415.535.505.535.635.485.615.725.935.716.116.15
GSK1265744 60 mg2.4872.5982.6492.7382.8222.6652.9892.8842.8302.9893.1673.0103.0503.0043.2003.1633.5123.494190.0204.8204.6211.5209.2209.5205.4210.9199.4209.8207.8204.2199.3209.9212.2212.2210.1210.64.725.025.025.045.344.975.395.285.295.385.575.565.455.415.635.736.056.01

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Absolute Values for Plasma Logarithm to the Base 10 (log10) HIV-1 RNA Over Time by Visit

Plasma samples for quantitative analysis of HIV-1 RNA were collected at indicated time points. Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

,,
InterventionLog10 copies per milliliter (Mean)
Baseline; n=60, 60, 61, 62Week 2; n=57, 56, 59, 59Week 4; n=58, 57, 59, 57Week 8; n=59, 56, 57, 55Week 12; n=58, 52, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 56, 47Week 24; n=56, 53, 56, 48Week 26; n=48, 50, 53, 44Week 28; n=51, 52, 52, 45Week 32; n=52, 53, 55, 45Week 36; n=52, 53, 55, 45Week 40; n=52, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 48, 53, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 52, 42Week 96; n=45, 48, 52, 40Week 108; n=43, 46, 49, 0Week 120; n=41, 46, 49, 0Week 132; n=40, 46, 49, 0Week 144; n=37, 45, 47, 0Week 156; n=37, 42, 49, 0Week 168; n=35, 43, 47, 0Week 180; n=36, 41, 47, 0Week 192; n=36, 40, 47, 0Week 204; n=34, 39, 47, 0Week 216; n=33, 39, 47, 0Week 228; n=32, 39, 47, 0Week 240; n=31, 39, 45, 0Week 252; n=31, 38, 47, 0Week 264; n=32, 38, 47, 0Week 276; n=31, 38, 45, 0Week 288; n=30, 38, 45, 0Week 300; n=31, 37, 44, 0Week 312; n=31, 33, 43, 0Week 324; n=3, 4, 3, 0
GSK1265744 10 mg4.4241.8831.7061.6951.6431.6191.6231.6151.5951.5911.6091.6041.6121.6861.6481.6251.6451.6811.6341.6381.6461.6821.6341.6651.6131.6891.6281.5911.5911.5961.5911.5911.5911.5911.6011.5971.591
GSK1265744 30 mg4.2701.9841.7311.6661.6181.6021.5961.5971.6021.6071.6201.6101.6181.6541.5981.6971.6431.6031.6091.5911.6311.6981.6031.6421.5911.5911.5951.5921.5911.6011.5991.5911.5911.5921.5911.6001.591
GSK1265744 60 mg4.4281.9391.7251.6661.6411.6161.5991.6031.5941.5911.6181.6061.6081.5981.5941.5911.5921.5961.5911.6181.5911.6301.6191.6031.6001.6991.6341.6341.6251.5911.5931.6171.6181.5911.6251.5911.591

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Absolute Values for Plasma Logarithm to the Base 10 (log10) HIV-1 RNA Over Time by Visit

Plasma samples for quantitative analysis of HIV-1 RNA were collected at indicated time points. Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

InterventionLog10 copies per milliliter (Mean)
Baseline; n=60, 60, 61, 62Week 2; n=57, 56, 59, 59Week 4; n=58, 57, 59, 57Week 8; n=59, 56, 57, 55Week 12; n=58, 52, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 56, 47Week 24; n=56, 53, 56, 48Week 26; n=48, 50, 53, 44Week 28; n=51, 52, 52, 45Week 32; n=52, 53, 55, 45Week 36; n=52, 53, 55, 45Week 40; n=52, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 48, 53, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 52, 42Week 96; n=45, 48, 52, 40
Efavirenz 600 mg4.2902.4152.2011.9501.7581.6971.6491.6101.6101.6001.6141.6071.6071.5961.6571.5921.5911.598

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Absolute Values for Hemoglobin During Double-blind Randomized Treatment Until Week 96

Blood samples were collected for the analysis of hemoglobin level. Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84 and 96

,,,
InterventionGrams per liter (Mean)
Baseline; n=60, 60, 61, 62Week 2; n=57, 56, 59, 59Week 4; n=57, 57, 59, 57Week 8; n=58, 56, 56, 55Week 12; n=58, 53, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 55, 49Week 24; n=56, 53, 56, 47Week 26; n=48, 50, 53, 45Week 28; n=50, 52, 52, 45Week 32; n=51, 53, 55, 45Week 36; n=52, 53, 55, 44Week 40; n=51, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 47, 52, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 51, 42Week 96; n=46, 46, 52, 41
Efavirenz 600 mg145.4146.4146.6148.1149.2147.6147.2148.5148.2145.9145.9145.0145.1145.4147.6147.7147.0147.0
GSK1265744 10 mg141.9142.0141.9144.9144.3143.5144.3144.8144.4143.7144.6142.3142.2142.9144.5143.9145.6144.9
GSK1265744 30 mg143.2142.8143.5147.7147.4146.5146.9147.8145.8146.8146.1145.9145.2145.7148.3148.1147.7147.1
GSK1265744 60 mg146.6145.9147.3148.6149.1148.7149.8150.4149.8149.3150.5149.8149.2146.5149.8149.6150.3150.8

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Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96

Blood samples were collected for the analysis of estimated creatinine clearance. Estimated creatinine clearance was calculated using Cockcroft-Gault formula. Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 16, 20, 24, 26, 40, 48, 60 and 96

InterventionMilliliters per minute (Mean)
Baseline; n=60, 60, 61, 62Week 2; n=1, 1, 0, 3Week 4; n=58, 57, 59, 57Week 8; n=2, 1, 1, 1Week 16; n=55, 53, 56, 49Week 20; n=2, 0, 0, 1Week 24; n=52, 53, 55, 46Week 48; n=51, 50, 54, 44Week 96; n=45, 48, 52, 40
GSK1265744 10 mg131.096.0129.3125.0132.4137.0127.9127.0130.8

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Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96

Blood samples were collected for the analysis of estimated creatinine clearance. Estimated creatinine clearance was calculated using Cockcroft-Gault formula. Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 16, 20, 24, 26, 40, 48, 60 and 96

InterventionMilliliters per minute (Mean)
Baseline; n=60, 60, 61, 62Week 4; n=58, 57, 59, 57Week 8; n=2, 1, 1, 1Week 16; n=55, 53, 56, 49Week 24; n=52, 53, 55, 46Week 48; n=51, 50, 54, 44Week 96; n=45, 48, 52, 40
GSK1265744 60 mg128.3122.4143.0123.9120.7122.3116.6

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Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96

Blood samples were collected for the analysis of estimated creatinine clearance. Estimated creatinine clearance was calculated using Cockcroft-Gault formula. Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 16, 20, 24, 26, 40, 48, 60 and 96

InterventionMilliliters per minute (Mean)
Baseline; n=60, 60, 61, 62Week 2; n=1, 1, 0, 3Week 4; n=58, 57, 59, 57Week 8; n=2, 1, 1, 1Week 16; n=55, 53, 56, 49Week 24; n=52, 53, 55, 46Week 26; n=0, 1, 0, 0Week 40; n=0, 1, 0, 0Week 48; n=51, 50, 54, 44Week 96; n=45, 48, 52, 40
GSK1265744 30 mg135.2106.0132.5124.0139.4132.8147.0180.0139.2137.7

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Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96

Blood samples were collected for the analysis of estimated creatinine clearance. Estimated creatinine clearance was calculated using Cockcroft-Gault formula. Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 16, 20, 24, 26, 40, 48, 60 and 96

InterventionMilliliters per minute (Mean)
Baseline; n=60, 60, 61, 62Week 2; n=1, 1, 0, 3Week 4; n=58, 57, 59, 57Week 8; n=2, 1, 1, 1Week 16; n=55, 53, 56, 49Week 20; n=2, 0, 0, 1Week 24; n=52, 53, 55, 46Week 48; n=51, 50, 54, 44Week 60; n=0, 0, 0, 1Week 96; n=45, 48, 52, 40
Efavirenz 600 mg125.699.0127.0101.0132.3122.0135.1131.0144.0134.8

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Absolute Values for Creatinine and Total Bilirubin During Double-blind Randomized Treatment Until Week 96

Blood samples were collected for the analysis of creatinine and total bilirubin (T. bilirubin). Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84 and 96

,,,
InterventionMicromoles per liter (Mean)
Creatinine; Baseline; n=60, 60, 61, 62Creatinine; Week 2; n=58, 56, 58, 58Creatinine; Week 4; n=58, 57, 59, 57Creatinine; Week 8; n=58, 55, 57, 54Creatinine; Week 12; n=58, 53, 57, 51Creatinine; Week 16; n=57, 54, 57, 52Creatinine; Week 20; n=56, 54, 55, 49Creatinine; Week 24; n=56, 53, 56, 47Creatinine; Week 26; n=48, 50, 53, 45Creatinine; Week 28; n=51, 52, 52, 45Creatinine; Week 32; n=52, 53, 55, 45Creatinine; Week 36; n=52, 52, 55, 45Creatinine; Week 40; n=52, 53, 55, 44Creatinine; Week 48; n=51, 53, 54, 44Creatinine; Week 60; n=48, 47, 53, 44Creatinine; Week 72; n=47, 47, 52, 42Creatinine; Week 84; n=46, 48, 52, 42Creatinine; Week 96; n=45, 48, 52, 40T. Bilirubin; Baseline; n=60, 60, 61, 62T. Bilirubin; Week 2; n=58, 56, 58, 58T. Bilirubin; Week 4; n=58, 57, 59, 57T. Bilirubin; Week 8; n=58, 55, 57, 54T. Bilirubin; Week 12; n=58, 53, 57, 51T. Bilirubin; Week 16; n=57, 54, 57, 52T. Bilirubin; Week 20; n=56, 54, 55, 49T. Bilirubin; Week 24; n=56, 53, 56, 47T. Bilirubin; Week 26; n=48, 50, 53, 45T. Bilirubin; Week 28; n=51, 52, 52, 45T. Bilirubin; Week 32; n=52, 53, 55, 45T. Bilirubin; Week 36; n=52, 52, 55, 45T. Bilirubin; Week 40; n=52, 53, 55, 44T. Bilirubin; Week 48; n=51, 53, 54, 44T. Bilirubin; Week 60; n=48, 47, 53, 44T. Bilirubin; Week 72; n=47, 47, 52, 42T. Bilirubin; Week 84; n=46, 48, 52, 42T. Bilirubin; Week 96; n=45, 48, 52, 40
Efavirenz 600 mg83.183.883.182.481.179.679.580.078.678.578.178.479.279.077.977.779.781.09.76.86.46.37.07.06.86.66.86.46.66.56.36.67.06.56.66.8
GSK1265744 10 mg80.483.882.982.983.883.483.283.283.483.083.883.583.383.483.984.585.082.09.29.29.49.39.59.69.09.610.610.39.810.310.810.011.210.811.710.3
GSK1265744 30 mg80.583.383.082.282.782.382.083.382.683.882.684.683.283.183.086.184.886.49.49.19.39.08.98.59.09.89.910.29.810.111.29.69.810.09.99.9
GSK1265744 60 mg79.984.684.283.584.182.486.185.287.085.685.786.785.485.085.287.387.388.510.510.09.810.110.210.410.410.012.011.411.712.212.310.411.611.412.012.5

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Absolute Values for Cluster of Differentiation 4+ (CD4+) Cell Count During Double-blind Randomized Treatment Until Week 96

CD4+ cell counts were assessed by flow cytometry. Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84 and 96

,,,
InterventionCells per cubic millimeter (Mean)
Baseline; n=60, 60, 61, 62Week 2; n=57, 56, 59, 59Week 4; n=58, 57, 59, 57Week 8; n=58, 56, 57, 55Week 12; n=58, 53, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 56, 49Week 24; n=56, 53, 56, 47Week 26; n=48, 50, 53, 45Week 28; n=49, 52, 52, 45Week 32; n=52, 53, 55, 45Week 36; n=52, 53, 55, 45Week 40; n=52, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 47, 53, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 52, 42Week 96; n=46, 46, 52, 41
Efavirenz 600 mg456.5487.0509.9531.4564.3594.4607.7599.5625.7635.7663.8651.5687.9732.6733.9722.5744.7747.8
GSK1265744 10 mg445.5544.0580.5576.6588.4608.3607.3614.6632.8652.2638.1638.7650.2677.3668.1683.2718.3726.2
GSK1265744 30 mg444.9525.1522.0555.2599.0595.8607.4626.5629.5635.9650.8658.6658.5687.2720.9651.3736.9722.9
GSK1265744 60 mg459.0549.3545.8544.3596.6599.7636.6658.0645.8653.3665.2720.3667.6713.8719.8710.9735.0743.1

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Absolute Values for ALT, AST, CK During Double-blind Randomized Treatment Until Week 96

Blood samples were collected for the analysis of ALT, AST and CK. Baseline value is the last pre-treatment value observed. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84 and 96

,,,
InterventionInternational Units per Liter (Mean)
ALT; Baseline; n=60, 60, 61, 62ALT; Week 2; n=58, 56, 58, 58ALT; Week 4; n=58, 57, 59, 57ALT; Week 8; n=58, 55, 57, 54ALT; Week 12; n=58, 53, 57, 51ALT; Week 16; n=57, 54, 57, 52ALT; Week 20; n=56, 54, 55, 49ALT; Week 24; n=56, 53, 56, 47ALT; Week 26; n=48, 50, 53, 45ALT; Week 28; n=51, 52, 52, 45ALT; Week 32; n=52, 53, 55, 45ALT; Week 36; n=52, 52, 55, 45ALT; Week 40; n=52, 53, 55, 44ALT; Week 48; n=51, 53, 54, 44ALT; Week 60; n=48, 47, 53, 44ALT; Week 72; n=47, 47, 52, 42ALT; Week 84; n=46, 48, 52, 42ALT; Week 96; n=45, 48, 52, 40AST; Baseline; n=60, 60, 61, 62AST; Week 2; n=58, 56, 58, 58AST; Week 4; n=58, 57, 59, 57AST; Week 8; n=58, 55, 57, 54AST; Week 12; n=58, 53, 57, 51AST; Week 16; n=57, 54, 57, 52AST; Week 20; n=56, 54, 55, 49AST; Week 24; n=56, 53, 56, 47AST; Week 26; n=48, 50, 53, 45AST; Week 28; n=51, 52, 52, 45AST; Week 32; n=52, 53, 55, 45AST; Week 36; n=52, 52, 55, 45AST; Week 40; n=52, 53, 55, 44AST; Week 48; n=51, 53, 54, 44AST; Week 60; n=48, 47, 53, 44AST; Week 72; n=47, 47, 52, 42AST; Week 84; n=46, 48, 52, 42AST; Week 96; n=45, 48, 52, 40CK; Baseline; n=60, 60, 61, 62CK; Week 2; n=58, 56, 58, 58CK; Week 4; n=58, 57, 59, 57CK; Week 8; n=58, 55, 57, 54CK; Week 12; n=58, 53, 57, 51CK; Week 16; n=57, 54, 57, 52CK; Week 20; n=56, 54, 55, 49CK; Week 24; n=56, 53, 56, 47CK; Week 26; n=48, 50, 53, 45CK; Week 28; n=51, 52, 52, 45CK; Week 32; n=52, 53, 55, 45CK; Week 36; n=52, 52, 55, 45CK; Week 40; n=52, 53, 55, 44CK; Week 48; n=51, 53, 54, 44CK; Week 60; n=48, 47, 53, 44CK; Week 72; n=47, 47, 52, 42CK; Week 84; n=46, 48, 52, 42CK; Week 96; n=45, 48, 52, 40
Efavirenz 600 mg30.530.031.425.025.730.427.025.728.324.223.123.523.422.624.922.727.124.331.532.829.024.424.436.728.726.125.823.725.426.323.023.724.922.929.927.7349.8512.1236.2152.9161.2646.5528.2247.4163.5154.7254.7303.1150.2146.3168.0120.5258.6281.1
GSK1265744 10 mg23.924.023.125.425.026.022.320.924.220.419.523.422.718.421.419.920.122.025.025.624.028.726.324.226.023.328.422.621.929.224.721.423.421.822.323.6197.3237.9196.7413.3316.1195.1342.7226.0344.1213.4205.6528.4259.5203.5315.7182.5204.3542.7
GSK1265744 30 mg28.126.325.629.331.428.524.927.526.626.526.924.724.624.825.930.729.948.727.526.625.029.529.029.224.227.226.926.726.525.424.524.325.331.029.247.7295.9276.1221.8427.2314.7427.3202.1306.3267.7276.8248.8242.9225.4219.3215.5354.0329.2272.8
GSK1265744 60 mg28.527.230.335.926.626.930.328.623.524.823.224.225.824.828.126.325.325.528.126.828.332.825.526.531.728.624.525.525.626.426.524.230.426.425.225.9181.2184.8180.5451.7211.8213.3485.3243.0242.5290.4311.3255.2292.6219.8399.6247.7195.0199.7

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Percentage of Participants With HIV-1 Ribonucleic Acid (RNA) <50 Copies/Milliliter (mL) at Week 48 Using the Missing, Switch, Discontinuation Equals Failure (MSDF) Algorithm

Plasma samples were collected for quantitative analysis of HIV-1 RNA. Percentage of participants with HIV-1 RNA <50 copies/mL at Week 48 was determined using the MSDF algorithm based on the current US Food and Drug Administration (FDA) definition of Snapshot algorithm. This algorithm treats all participants without HIV-1 RNA data at the visit of interest (due to missing data or discontinuation of investigational product prior to visit window) as well as participants who switch their concomitant antiretroviral therapy prior to the visit of interest as non-responders. Virological response within an analysis window was determined by the last available HIV-1 RNA measurement in that window while the participant was on-treatment. MSDF response rate was calculated as number of responders in the analysis window divided by the number of participants in the analysis population. ITT-E Population comprised of all randomized participants who received at least one dose of investigational product. (NCT01641809)
Timeframe: Week 48

InterventionPercentage of participants (Number)
GSK1265744 10 mg80
GSK1265744 30 mg80
GSK1265744 60 mg87
Efavirenz 600 mg71

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Percentage of Participants Who Discontinued Treatment Due to Adverse Events-Maintenance Phase

AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. The percentage of participants with adverse events leading to withdrawal/permanent discontinuation of investigational product is presented. (NCT01641809)
Timeframe: Week 24 to Week 96

InterventionPercentage of participants (Number)
GSK1265744 10 mg2
GSK1265744 30 mg4
GSK1265744 60 mg2
Efavirenz 600 mg2

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Percentage of Participants Who Discontinued Treatment Due to Adverse Events-Induction Phase

AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. The percentage of participants with adverse events leading to withdrawal/permanent discontinuation of investigational product is presented. (NCT01641809)
Timeframe: Up to Week 24

InterventionPercentage of participants (Number)
GSK1265744 10 mg0
GSK1265744 30 mg2
GSK1265744 60 mg5
Efavirenz 600 mg13

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Percentage of Participants Who Discontinued Investigational Product Due to Adverse Events

AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. The percentage of participants with adverse events leading to withdrawal/permanent discontinuation of investigational product is presented. (NCT01641809)
Timeframe: Up to Week 324

InterventionPercentage of participants (Number)
GSK1265744 10 mg7
GSK1265744 30 mg7
GSK1265744 60 mg7
Efavirenz 600 mg15

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Number of Participants With Clinically Significant Electrocardiogram (ECG) Findings

Twelve lead ECG was performed after the participants had rested in a semi-supine position for at least 5 minutes using an ECG machine that automatically calculated the heart rate and measured PR, QRS, QT, and corrected QT (QTc) intervals. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for worst case results at any time on-treatment is presented. (NCT01641809)
Timeframe: Up to Week 324

InterventionParticipants (Count of Participants)
GSK1265744 10 mg25
GSK1265744 30 mg19
GSK1265744 60 mg15
Efavirenz 600 mg10

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Percentage of Participants With Plasma HIV-1 RNA <50 Copies/mL Over Time by Visit Using Observed Case Analysis

Plasma samples were collected for quantitative analysis of HIV-1 RNA. Percentage of participants with HIV-1 RNA <50 copies/mL over time was determined using the observed case analysis, which did not impute for any missing assessments. Observed case response rate was calculated as the number of participants with a positive response at the time point where the participant is on therapy divided by the number of participants in the analysis population with an assessment in the scheduled visit window during the randomized period or open-label phase. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

,,
InterventionPercentage of participants (Number)
Baseline; n=60, 60, 61, 62Week 2; n=57, 56, 59, 59Week 4; n=58, 57, 59, 57Week 8; n=59, 56, 57, 55Week 12; n=58, 52, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 56, 47Week 24; n=56, 53, 56, 48Week 26; n=48, 50, 53, 44Week 28; n=51, 52, 52, 45Week 32; n=52, 53, 55, 45Week 36; n=52, 53, 55, 45Week 40; n=52, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 48, 53, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 52, 42Week 96; n=45, 48, 52, 40Week 108; n=43, 46, 49, 0Week 120; n=41, 46, 49, 0Week 132; n=40, 46, 49, 0Week 144; n=37, 45, 47, 0Week 156; n=37, 42, 49, 0Week 168; n=35, 43, 47, 0Week 180; n=36, 41, 47, 0Week 192; n=36, 40, 47, 0Week 204; n=34, 39, 47, 0Week 216; n=33, 39, 47, 0Week 228; n=32, 39, 47, 0Week 240; n=31, 39, 45, 0Week 252; n=31, 38, 47, 0Week 264; n=32, 38, 47, 0Week 276; n=31, 38, 45, 0Week 288; n=30, 38, 45, 0Week 300; n=31, 37, 44, 0Week 312; n=31, 33, 43, 0Week 324; n=3, 4, 3, 0
GSK1265744 10 mg0518392959591939810096989692949191899595959295949794971001009710010010010097100100
GSK1265744 30 mg05482898894989894949496969296929498961009693959510010097100100979710010010010097100
GSK1265744 60 mg0537393919398959810096959598981001009810098100989898989698989810098989610095100100

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Area Under the Concentration Time Curve Over the Dosing Interval (AUC[0-tau]) for GSK1265744 at Week 2

Blood samples for pharmacokinetic (PK) analysis were collected at the indicated time points. The PK parameters were calculated by standard non-compartmental analysis. The PK Summary Population comprised of all participants who received GSK1265744 or with Rilpivirine, underwent intensive and/or limited/sparse PK sampling during the study, and provided evaluable GSK1265744 and Rilpivirine plasma concentration data (NCT01641809)
Timeframe: pre-dose, 1, 2, 3, 4, 8 and 24 hours post-dose at Week 2

InterventionHours*micrograms per milliliter (Geometric Mean)
GSK1265744 10 mg45.69
GSK1265744 30 mg133.74
GSK1265744 60 mg227.58

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Percentage of Participants With Plasma HIV-1 RNA <50 Copies/mL Over Time by Visit Using Observed Case Analysis

Plasma samples were collected for quantitative analysis of HIV-1 RNA. Percentage of participants with HIV-1 RNA <50 copies/mL over time was determined using the observed case analysis, which did not impute for any missing assessments. Observed case response rate was calculated as the number of participants with a positive response at the time point where the participant is on therapy divided by the number of participants in the analysis population with an assessment in the scheduled visit window during the randomized period or open-label phase. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300, 312 and 324

InterventionPercentage of participants (Number)
Baseline; n=60, 60, 61, 62Week 2; n=57, 56, 59, 59Week 4; n=58, 57, 59, 57Week 8; n=59, 56, 57, 55Week 12; n=58, 52, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 56, 47Week 24; n=56, 53, 56, 48Week 26; n=48, 50, 53, 44Week 28; n=51, 52, 52, 45Week 32; n=52, 53, 55, 45Week 36; n=52, 53, 55, 45Week 40; n=52, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 48, 53, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 52, 42Week 96; n=45, 48, 52, 40
Efavirenz 600 mg0142655768791969396969893989510010098

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Percentage of Participants With Plasma HIV-1 RNA <400 Copies/mL Until Week 96 Using the Observed Case Analysis

Plasma samples were collected for quantitative analysis of HIV-1 RNA. Percentage of participants with HIV-1 RNA <400 copies/mL over time was determined using the observed case analysis, which did not impute for any missing assessments. Observed case response rate was calculated as the number of participants with a positive response at the time point where the participant is on randomized therapy divided by the number of participants in the analysis population with an assessment in the scheduled visit window during the randomized period. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 20, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84 and 96

,,,
InterventionPercentage of participants (Number)
Baseline; n=60, 60, 61, 62Week 2; n=57, 56, 59, 59Week 4; n=58, 57, 59, 57Week 8; n=59, 56, 57, 55Week 12; n=58, 52, 57, 51Week 16; n=57, 54, 57, 52Week 20; n=56, 54, 56, 47Week 24; n=56, 53, 56, 48Week 26; n=48, 50, 53, 44Week 28; n=51, 52, 52, 45Week 32; n=52, 53, 55, 45Week 36; n=52, 53, 55, 45Week 40; n=52, 53, 55, 45Week 48; n=51, 53, 54, 44Week 60; n=48, 48, 53, 44Week 72; n=47, 48, 52, 42Week 84; n=46, 48, 52, 42Week 96; n=45, 48, 52, 40
Efavirenz 600 mg0717491929610010010010010010010010098100100100
GSK1265744 10 mg0919795979810010010010010010010098969810096
GSK1265744 30 mg0869898100100100100100100100100100981009698100
GSK1265744 60 mg08697989810010010010010098100100100100100100100

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Percentage of Participants With Plasma HIV-1 RNA <400 Copies/mL Until Week 96 Using the MSDF Algorithm

Plasma samples were collected for quantitative analysis of HIV-1 RNA. The percentage of participants with HIV-1 RNA <400 copies/mL over time was determined using the MSDF algorithm based on the current US FDA definition of the Snapshot algorithm. This algorithm treats all participants without HIV-1 RNA data at the visit of interest (due to missing data or discontinuation of investigational product prior to visit window) as well as participants who switch their concomitant antiretroviral therapy prior to the visit of interest as non-responders. Virological response within an analysis window was determined by the last available HIV-1 RNA measurement in that window while the participant was on-treatment. MSDF response rate was calculated as number of responders in the analysis window divided by the number of participants in the analysis population. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84 and 96

,,,
InterventionPercentage of participants (Number)
BaselineWeek 2Week 4Week 8Week 12Week 16Week 24Week 26Week 28Week 32Week 36Week 40Week 48Week 60Week 72Week 84Week 96
Efavirenz 600 mg068687973817971737373737371686865
GSK1265744 10 mg087939390939380858787878380777775
GSK1265744 30 mg080939285878780838585858577757777
GSK1265744 60 mg084939289939287858990908987858585

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Percentage of Participants With HIV-1 RNA <50 Copies/mL From Week 24 Through Week 96 by Visit Using MSDF Algorithm-Maintenance Phase

Plasma samples were collected for quantitative analysis of HIV-1 RNA. The end point was determined using MSDF algorithm based on the current US FDA definition of Snapshot algorithm. This algorithm treats all participants without HIV-1 RNA data at the visit of interest (due to missing data or discontinuation of investigational product prior to visit window) as well as participants who switch their concomitant antiretroviral therapy prior to the visit of interest as non-responders. Virological response within an analysis window was determined by the last available HIV-1 RNA measurement in that window while the participant was on-treatment. MSDF response rate was calculated as number of responders in the analysis window divided by the number of participants in the analysis population. ITT-Maintenance Exposed (ME) Population comprised of all participants randomized to GSK1265744 and who received at least one dose of investigational product during maintenance phase of the study. (NCT01641809)
Timeframe: Weeks 24, 26, 28, 32, 36, 40, 48, 60, 72, 84 and 96

,,,
InterventionPercentage of participants (Number)
Week 24Week 26Week 28Week 32Week 36Week 40Week 48Week 60Week 72Week 84Week 96
Efavirenz 600 mg9687919194899489898983
GSK1265744 10 mg9690989698969290838379
GSK1265744 30 mg9485899192929183838585
GSK1265744 60 mg9695959695959695959593

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Percentage of Participants With HIV-1 RNA <50 Copies/mL at Week 16 and Week 24 Using MSDF Algorithm-Induction Phase

Plasma samples were collected for quantitative analysis of HIV-1 RNA. Percentage of participants with HIV-1 RNA <50 copies/mL over time was determined using the MSDF algorithm based on the current US FDA definition of the Snapshot algorithm. This algorithm treats all participants without HIV-1 RNA data at the visit of interest (due to missing data or discontinuation of investigational product prior to visit window) as well as participants who switch their concomitant antiretroviral therapy prior to the visit of interest as non-responders. Virological response within an analysis window was determined by the last available HIV-1 RNA measurement in that window while the participant was on-treatment. MSDF response rate was calculated as number of responders in the analysis window divided by the number of participants in the analysis population. (NCT01641809)
Timeframe: Week 16 and Week 24

,,,
InterventionPercentage of participants (Number)
Week 16Week 24
Efavirenz 600 mg7474
GSK1265744 10 mg9087
GSK1265744 30 mg8385
GSK1265744 60 mg8787

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Number of Participants With Treatment Emergent Phenotypic Resistance

Plasma samples were collected for drug resistance testing. Phenotypic resistance data for the following drugs under integrase inhibitor (INI), non-nucleoside reverse transcriptase inhibitor (NNRTI), NRTI and proteasome inhibitor drug classes is presented for participants with confirmed virologic failure: GSK1265744, Raltegravir [RAL], Delavirdine [DLV], Efavirenz [EFV], Etravirine [ETR], Nevirapine (NVP), RPV, 3TC, ABC, FTC, TDF, Zidovudine [ZDV], Stavudine [d4T], Didanosine [ddI], Atazanavir/ritonavir [ATV/r], Darunavir (DRV)/r, Fosamprenavir/r [FPV/r], Indinavir/r [IDV/r], Lopinavir/r [LPV/r], Nelfinavir [NFV], Ritonavir [RTV], Saquinavir/r [SQV/r], Tipranavir/r [TPV/r]. On-treatment Phenotypic Resistance population comprised of all participants in the ITT-E Population with available on-treatment phenotypic resistance data, excluding participants who are not protocol-defined virologic failures. (NCT01641809)
Timeframe: Up to Week 324

,,,
InterventionParticipants (Count of Participants)
INI, GSK1265744; Resistant; n=5, 1, 2, 2INI, GSK1265744; Sensitive; n=5, 1, 2, 2INI, RAL; Resistant; n=5, 1, 2, 2INI, RAL; Sensitive; n=5, 1, 2, 2NNRTI, DLV; Resistant; n=6, 2, 2, 5NNRTI, DLV; Sensitive; n=6, 2, 2, 5NNRTI, EFV; Resistant; n=6, 2, 2, 5NNRTI, EFV; Sensitive; n=6, 2, 2, 5NNRTI, ETR; Resistant; n=6, 2, 2, 5NNRTI, ETR; Partially sensitive; n=6, 2, 2, 5NNRTI, ETR; Sensitive; n=6, 2, 2, 5NNRTI, NVP; Resistant; n=6, 2, 2, 5NNRTI, NVP; Sensitive; n=6, 2, 2, 5NNRTI, RPV; Resistant; n=6, 2, 2, 5NNRTI, RPV; Sensitive; n=6, 2, 2, 5NRTI, 3TC; Resistant; n=6, 2, 2, 5NRTI, 3TC; Sensitive; n=6, 2, 2, 5NRTI, ABC; Resistant; n=6, 2, 2, 5NRTI, ABC; Partially sensitive; n=6, 2, 2, 5NRTI, ABC; Sensitive; n=6, 2, 2, 5NRTI, FTC; Resistant; n=6, 2, 2, 5NRTI, FTC; Sensitive; n=6, 2, 2, 5NRTI, TDF; Resistant; n=6, 2, 2, 5NRTI, TDF; Partially sensitive; n=6, 2, 2, 5NRTI, TDF; Sensitive; n=6, 2, 2, 5NRTI, ZDV; Resistant; n=6, 2, 2, 5NRTI, ZDV; Sensitive; n=6, 2, 2, 5NRTI, d4T; Resistant; n=6, 2, 2, 5NRTI, d4T; Sensitive; n=6, 2, 2, 5NRTI, ddI; Resistant; n=6, 2, 2, 5NRTI, ddI; Partially sensitive; n=6, 2, 2, 5NRTI, ddI; Sensitive; n=6, 2, 2, 5PI, ATV/r; Resistant; n=6, 2, 2, 5PI, ATV/r; Sensitive; n=6, 2, 2, 5PI, DRV/r; Resistant; n=6, 2, 2, 5PI, DRV/r; Partially sensitive; n=6, 2, 2, 5PI, DRV/r; Sensitive; n=6, 2, 2, 5PI, FPV/r; Resistant; n=6, 2, 2, 5PI, FPV/r; Partially sensitive; n=6, 2, 2, 5PI, FPV/r; Sensitive; n=6, 2, 2, 5PI, IDV/r; Resistant; n=6, 2, 2, 5PI, IDV/r; Sensitive; n=6, 2, 2, 5PI, LPV/r; Resistant; n=6, 2, 2, 5PI, LPV/r; Partially sensitive; n=6, 2, 2, 5PI, LPV/r; Sensitive; n=6, 2, 2, 5PI, NFV; Resistant; n=6, 2, 2, 5PI, NFV; Sensitive; n=6, 2, 2, 5PI, RTV; Resistant; n=6, 2, 2, 5PI, RTV; Sensitive; n=6, 2, 2, 5PI, SQV/r; Resistant; n=6, 2, 2, 5PI, SQV/r; Partially sensitive; n=6, 2, 2, 5PI, SQV/r; Sensitive; n=6, 2, 2, 5PI, TPV/r; Resistant; n=6, 2, 2, 5PI, TPV/r; Partially sensitive; n=6, 2, 2, 5PI, TPV/r; Sensitive; n=6, 2, 2, 5
Efavirenz 600 mg0202050500505050500505005050500505005005050050505005005
GSK1265744 10 mg2332333330333330600606015240600606006006060060606006006
GSK1265744 30 mg0101020200202020200202002020200202002002020020202002002
GSK1265744 60 mg1111020200202020200202002020200202002002020020202002002

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Number of Participants With Treatment Emergent Genotypic Mutations Associated With Development of Resistance

Plasma samples were collected for drug resistance testing. The treatment emergent INI mutations associated with development of resistance to RAL, ELV, dolutegravir (DTG) or GSK1265744 and major resistance mutations to other classes (NRTI, NNRTI, PI) as defined by International AIDS society (IAS)-United States of America (USA) are presented. On-treatment Genotypic Resistance population comprised of all participants in the ITT-E Population with available on-treatment genotypic resistance data, excluding participants who are not protocol-defined virologic failures. (NCT01641809)
Timeframe: Up to Week 324

,,,
InterventionParticipants (Count of Participants)
Any INI mutationAny mutation to other classes
Efavirenz 600 mg00
GSK1265744 10 mg34
GSK1265744 30 mg00
GSK1265744 60 mg11

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Number of Participants With Post-Baseline HIV-1 Associated Conditions Progression of Disease

HIV-1 associated conditions were assessed according to the 1993 Centers for Disease Control and Prevention (CDC) Revised Classification System for HIV Infection in Adults. The clinical categories of HIV infection as per CDC system are class A=Asymptomatic HIV infection or lymphadenopathy or acute HIV infection; class B=symptomatic non-acquired immunodeficiency syndrome (AIDS) conditions and class C=AIDS indicator conditions. Number of participants experiencing disease progression is presented, where disease progression is defined as the progression from Baseline HIV disease status as follows: CDC class A at Baseline to CDC class C event; CDC Class B at Baseline to CDC Class C event; CDC Class C at Baseline to new CDC Class C event; and CDC class A, B or C at Baseline to death. (NCT01641809)
Timeframe: Up to Week 324

,,,
InterventionParticipants (Count of Participants)
CDC Class A to CDC Class CCDC Class B to CDC Class CCDC Class C to new CDC Class CCDC Class A, B or C to Death
Efavirenz 600 mg0000
GSK1265744 10 mg1000
GSK1265744 30 mg1001
GSK1265744 60 mg0001

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Number of Participants With Maximum Treatment-emergent Hematology Toxicities-Maintenance Phase

Blood samples were collected for the analysis of following hematology parameters: Activated Partial Thromboplastin Time (APTT), hemoglobin, international normalized ratio (INR), platelet count, prothrombin time (PT), total neutrophils and white blood cell (WBC) count. A toxicity is considered treatment emergent if it developed or increased in intensity from Baseline while on-treatment. Laboratory toxicities were graded using the DAIDS Table for Grading the Severity of Adult and Pediatric Adverse Events, where Grade 1=Mild, Grade 2=moderate, Grade 3=severe and Grade 4=potentially life-threatening. (NCT01641809)
Timeframe: Week 24 to Week 96

,,,
InterventionParticipants (Count of Participants)
APTT; Grade 1APTT; Grade 2APTT; Grade 3APTT; Grade 4Hemoglobin; Grade 1Hemoglobin; Grade 2Hemoglobin; Grade 3Hemoglobin; Grade 4INR; Grade 1INR; Grade 2INR; Grade 3INR; Grade 4Platelet count; Grade 1Platelet count; Grade 2Platelet count; Grade 3Platelet count; Grade 4PT; Grade 1PT; Grade 2PT; Grade 3PT; Grade 4Total neutrophils; Grade 1Total neutrophils; Grade 2Total neutrophils; Grade 3Total neutrophils; Grade 4WBC count; Grade 1WBC count; Grade 2WBC count; Grade 3WBC count; Grade 4
Efavirenz 600 mg5001000031001000310023113000
GSK1265744 10 mg5001010020104000100075112100
GSK1265744 30 mg5101000041010000301192015100
GSK1265744 60 mg50010000010041110010103132110

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Change From Baseline in Estimated Creatinine Clearance Over Time by Visit

Blood samples were collected for the analysis of estimated creatinine clearance. Estimated creatinine clearance was calculated using Cockcroft-Gault formula. Baseline value is the last pre-treatment value observed. Change from Baseline is calculated as value at indicated time point minus Baseline value. (NCT01641809)
Timeframe: Baseline (Day 1) and Weeks 2, 4, 8, 16, 20, 24, 26, 40, 48, 60, 96, 180, 204, 252 and 264

InterventionMilliliters per minute (Mean)
Week 2; n=1, 1, 0, 3Week 4; n=58, 57, 59, 57Week 8; n=2, 1, 1, 1Week 16; n=55, 53, 56, 49Week 20; n=2, 0, 0, 1Week 24; n=52, 53, 55, 46Week 48; n=51, 50, 54, 44Week 60; n=0, 0, 0, 1Week 96; n=45, 48, 52, 40
Efavirenz 600 mg-0.7-0.10.03.44.04.80.416.05.1

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Maximum Observed Concentration (Cmax) for GSK1265744 at Week 2

Blood samples for PK analysis were collected at the indicated time points. The PK parameters were calculated by standard non-compartmental analysis. (NCT01641809)
Timeframe: pre-dose, 1, 2, 3, 4, 8 and 24 hours post-dose at Week 2

InterventionMicrograms per milliliter (Geometric Mean)
GSK1265744 10 mg2.77
GSK1265744 30 mg7.49
GSK1265744 60 mg13.12

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Concentration at the End of a Dosing Interval (Ctau) for GSK1265744 at Week 2

Blood samples for PK analysis were collected at the indicated time points. The PK parameters were calculated by standard non-compartmental analysis. (NCT01641809)
Timeframe: pre-dose, 1, 2, 3, 4, 8 and 24 hours post dose at Week 2

InterventionMicrograms per milliliter (Geometric Mean)
GSK1265744 10 mg1.45
GSK1265744 30 mg4.34
GSK1265744 60 mg5.83

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Number of Participants With Maximum Treatment-emergent Hematology Toxicities-Induction Phase

Blood samples were collected for the analysis of following hematology parameters: APTT, basophils, eosinophils, hematocrit, hemoglobin, INR, lymphocytes, mean corpuscle volume (MCV), monocytes, platelet count, PT, red blood cell (RBC) count, total neutrophils and WBC count. A toxicity was considered treatment emergent if it developed or increased in intensity from Baseline while on-treatment. Laboratory toxicities were graded using the DAIDS Table for Grading the Severity of Adult and Pediatric Adverse Events, where Grade 1=Mild, Grade 2=moderate, Grade 3=severe and Grade 4=potentially life-threatening. (NCT01641809)
Timeframe: Up to Week 24

,,,
InterventionParticipants (Count of Participants)
APTT; Grade 1APTT; Grade 2APTT; Grade 3APTT; Grade 4Basophils; Grade 1Basophils; Grade 2Basophils; Grade 3Basophils; Grade 4Eosinophils; Grade 1Eosinophils; Grade 2Eosinophils; Grade 3Eosinophils; Grade 4Hematocrit; Grade 1Hematocrit; Grade 2Hematocrit; Grade 3Hematocrit; Grade 4Hemoglobin; Grade 1Hemoglobin; Grade 2Hemoglobin; Grade 3Hemoglobin; Grade 4INR; Grade 1INR; Grade 2INR; Grade 3INR; Grade 4Lymphocytes; Grade 1Lymphocytes; Grade 2Lymphocytes; Grade 3Lymphocytes; Grade 4MCV; Grade 1MCV; Grade 2MCV; Grade 3MCV; Grade 4Monocytes; Grade 1Monocytes; Grade 2Monocytes; Grade 3Monocytes; Grade 4Platelet count; Grade 1Platelet count; Grade 2Platelet count; Grade 3Platelet count; Grade 4PT; Grade 1PT; Grade 2PT; Grade 3PT; Grade 4RBC; Grade 1RBC; Grade 2RBC; Grade 3RBC; Grade 4Total neutrophils; Grade 1Total neutrophils; Grade 2Total neutrophils; Grade 3Total neutrophils; Grade 4WBC count; Grade 1WBC count; Grade 2WBC count; Grade 3WBC count; Grade 4
Efavirenz 600 mg30000000000000000000100000000000000010001000000022111000
GSK1265744 10 mg10000000000000000100000000000000000020000000000083000000
GSK1265744 30 mg00010000000000000000200100000000000000001001000062002100
GSK1265744 60 mg10010000000000000000000000000000000020000000000083012000

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Number of Participants With Maximum Treatment-emergent Hematology Toxicities Over Time

Blood samples were collected for the analysis of following hematology parameters: APTT, hemoglobin, INR, platelet count, PT, total neutrophils and WBC count. Laboratory toxicities were graded using the DAIDS Table for Grading the Severity of Adult and Pediatric Adverse Events, where Grade 1=Mild, Grade 2=moderate, Grade 3=severe and Grade 4=potentially life-threatening. (NCT01641809)
Timeframe: Up to Week 324

,,,
InterventionParticipants (Count of Participants)
APTT; Grade 1APTT; Grade 2APTT; Grade 3APTT; Grade 4Hemoglobin; Grade 1Hemoglobin; Grade 2Hemoglobin; Grade 3Hemoglobin; Grade 4INR; Grade 1INR; Grade 2INR; Grade 3INR; Grade 4Platelet count; Grade 1Platelet count; Grade 2Platelet count; Grade 3Platelet count; Grade 4PT; Grade 1PT; Grade 2PT; Grade 3PT; Grade 4Total neutrophils; Grade 1Total neutrophils; Grade 2Total neutrophils; Grade 3Total neutrophils; Grade 4WBC count; Grade 1WBC count; Grade 2WBC count; Grade 3WBC count; Grade 4
Efavirenz 600 mg5001000031001000310023113000
GSK1265744 10 mg5001010020104000100075112100
GSK1265744 30 mg5101000041010000301192015100
GSK1265744 60 mg50010000010041110010103132110

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Number of Participants With Maximum Treatment-emergent Clinical Chemistry Toxicity-Induction Phase

Blood samples were collected for the analysis of following clinical chemistry parameters: ALT, albumin, ALP, AST, CO2/bicarbonate, chloride, cholesterol, CK, creatinine, glucose, high density lipoprotein (HDL) cholesterol, LDL cholesterol, lipase, inorganic phosphorus, potassium, sodium, total bilirubin, triglycerides and urea/blood urea nitrogen (BUN). A toxicity was considered treatment emergent if it developed or increased in intensity from Baseline while on-treatment. Laboratory toxicities were graded using the DAIDS Table for Grading the Severity of Adult and Pediatric Adverse Events, where Grade 1=Mild, Grade 2=moderate, Grade 3=severe and Grade 4=potentially life-threatening. (NCT01641809)
Timeframe: Up to Week 24

,,,
InterventionParticipants (Count of Participants)
ALT; Grade 1ALT; Grade 2ALT; Grade 3ALT; Grade 4Albumin; Grade 1Albumin; Grade 2Albumin; Grade 3Albumin; Grade 4ALP; Grade 1ALP; Grade 2ALP; Grade 3ALP; Grade 4AST; Grade 1AST; Grade 2AST; Grade 3AST; Grade 4CO2/bicarbonate; Grade 1CO2/bicarbonate; Grade 2CO2/bicarbonate; Grade 3CO2/bicarbonate; Grade 4Chloride; Grade 1Chloride; Grade 2Chloride; Grade 3Chloride; Grade 4Cholesterol; Grade 1Cholesterol; Grade 2Cholesterol; Grade 3Cholesterol; Grade 4CK; Grade 1CK; Grade 2CK; Grade 3CK; Grade 4Creatinine; Grade 1Creatinine; Grade 2Creatinine; Grade 3Creatinine; Grade 4Glucose; Grade 1Glucose; Grade 2Glucose; Grade 3Glucose; Grade 4HDL cholesterol; Grade 1HDL cholesterol; Grade 2HDL cholesterol; Grade 3HDL cholesterol; Grade 4LDL cholesterol; Grade 1LDL cholesterol; Grade 2LDL cholesterol; Grade 3LDL cholesterol; Grade 4Lipase; Grade 1Lipase; Grade 2Lipase; Grade 3Lipase; Grade 4Inorganic phosphorus; Grade 1Inorganic phosphorus; Grade 2Inorganic phosphorus; Grade 3Inorganic phosphorus; Grade 4Potassium; Grade 1Potassium; Grade 2Potassium; Grade 3Potassium; Grade 4Sodium; Grade 1Sodium; Grade 2Sodium; Grade 3Sodium; Grade 4Total bilirubin; Grade 1Total bilirubin; Grade 2Total bilirubin; Grade 3Total bilirubin; Grade 4Triglycerides; Grade 1Triglycerides; Grade 2Triglycerides; Grade 3Triglycerides; Grade 4Urea/BUN; Grade 1Urea/BUN; Grade 2Urea/BUN; Grade 3Urea/BUN; Grade 4
Efavirenz 600 mg8400000030006120600000004960412411006501000048206510682021008100000002010000
GSK1265744 10 mg31000000000062101000000073007232010010500000054009620561070007000020000000000
GSK1265744 30 mg4500000011008500500000008200521400008300000091003110221010004000110001000000
GSK1265744 60 mg1300200004000713010000000123206312000013120000085305741722020007000410003100000

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Number of Participants With Maximum Treatment-emergent Clinical Chemistry Toxicities-Maintenance Phase

Blood samples were collected for the analysis of following clinical chemistry parameters: alanine aminotranferase (ALT), albumin, alkaline phosphatase (ALP), aspartate aminotransferase (AST), carbon dioxide(CO2)/bicarbonate, cholesterol, creatine kinase (CK), creatinine, glucose, low density lipoprotein (LDL) cholesterol, lipase, inorganic phosphorus, potassium, sodium, total bilirubin and triglycerides. A toxicity is considered treatment emergent if it developed or increased in intensity from Baseline while on-treatment. Laboratory toxicities were graded using the Division of AIDS (DAIDS) Table for Grading the Severity of Adult and Pediatric Adverse Events, where Grade 1=Mild, Grade 2=moderate, Grade 3=severe and Grade 4=potentially life-threatening. (NCT01641809)
Timeframe: Week 24 to Week 96

,,,
InterventionParticipants (Count of Participants)
ALT; Grade 1ALT; Grade 2ALT; Grade 3ALT; Grade 4Albumin; Grade 1Albumin; Grade 2Albumin; Grade 3Albumin; Grade 4ALP; Grade 1ALP; Grade 2ALP; Grade 3ALP; Grade 4AST; Grade 1AST; Grade 2AST; Grade 3AST; Grade 4CO2/bicarbonate; Grade 1CO2/bicarbonate; Grade 2CO2/bicarbonate; Grade 3CO2/bicarbonate; Grade 4Cholesterol; Grade 1Cholesterol; Grade 2Cholesterol; Grade 3Cholesterol; Grade 4CK; Grade 1CK; Grade 2CK; Grade 3CK; Grade 4Creatinine; Grade 1Creatinine; Grade 2Creatinine; Grade 3Creatinine; Grade 4Glucose; Grade 1Glucose; Grade 2Glucose; Grade 3Glucose; Grade 4LDL cholesterol; Grade 1LDL cholesterol; Grade 2LDL cholesterol; Grade 3LDL cholesterol; Grade 4Lipase; Grade 1Lipase; Grade 2Lipase; Grade 3Lipase; Grade 4Inorganic phosphorus; Grade 1Inorganic phosphorus; Grade 2Inorganic phosphorus; Grade 3Inorganic phosphorus; Grade 4Potassium; Grade 1Potassium; Grade 2Potassium; Grade 3Potassium; Grade 4Sodium; Grade 1Sodium; Grade 2Sodium; Grade 3Sodium; Grade 4Total bilirubin; Grade 1Total bilirubin; Grade 2Total bilirubin; Grade 3Total bilirubin; Grade 4Triglycerides; Grade 1Triglycerides; Grade 2Triglycerides; Grade 3Triglycerides; Grade 4
Efavirenz 600 mg630100004000523281009104050351000115008640970079204100710000000110
GSK1265744 10 mg96010000200055226100176308236110017140014640995251020120001420072000110
GSK1265744 30 mg126111000110013801140001712009426100017100016112098103111070001210013100400
GSK1265744 60 mg175000000400013520900019153011445200020112013147081162955080001600084000331

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Number of Participants With Maximum Treatment-emergent Clinical Chemistry Toxicities Over Time

Blood samples were collected for the analysis of following clinical chemistry parameters: ALT, albumin, ALP, AST, CO2/bicarbonate, cholesterol, CK, creatinine, glucose, LDL cholesterol, lipase, inorganic phosphorus, potassium, sodium, total bilirubin and triglycerides. Laboratory toxicities were graded using the DAIDS Table for Grading the Severity of Adult and Pediatric Adverse Events, where Grade 1=Mild, Grade 2=moderate, Grade 3=severe and Grade 4=potentially life-threatening. (NCT01641809)
Timeframe: Up to Week 324

,,,
InterventionParticipants (Count of Participants)
ALT; Grade 1ALT; Grade 2ALT; Grade 3ALT; Grade 4Albumin; Grade 1Albumin; Grade 2Albumin; Grade 3Albumin; Grade 4ALP; Grade 1ALP; Grade 2ALP; Grade 3ALP; Grade 4AST; Grade 1AST; Grade 2AST; Grade 3AST; Grade 4CO2/bicarbonate; Grade 1CO2/bicarbonate; Grade 2CO2/bicarbonate; Grade 3CO2/bicarbonate; Grade 4Cholesterol; Grade 1Cholesterol; Grade 2Cholesterol; Grade 3Cholesterol; Grade 4CK; Grade 1CK; Grade 2CK; Grade 3CK; Grade 4Creatinine; Grade 1Creatinine; Grade 2Creatinine; Grade 3Creatinine; Grade 4Glucose; Grade 1Glucose; Grade 2Glucose; Grade 3Glucose; Grade 4LDL cholesterol; Grade 1LDL cholesterol; Grade 2LDL cholesterol; Grade 3LDL cholesterol; Grade 4Lipase; Grade 1Lipase; Grade 2Lipase; Grade 3Lipase; Grade 4Inorganic phosphorus; Grade 1Inorganic phosphorus; Grade 2Inorganic phosphorus; Grade 3Inorganic phosphorus; Grade 4Potassium; Grade 1Potassium; Grade 2Potassium; Grade 3Potassium; Grade 4Sodium; Grade 1Sodium; Grade 2Sodium; Grade 3Sodium; Grade 4Total bilirubin; Grade 1Total bilirubin; Grade 2Total bilirubin; Grade 3Total bilirubin; Grade 4Triglycerides; Grade 1Triglycerides; Grade 2Triglycerides; Grade 3Triglycerides; Grade 4
Efavirenz 600 mg84010000500072328100910605045110012601874010710892041001110000000111
GSK1265744 10 mg960100002000762261001773092371100191400147401195251120140001420072000110
GSK1265744 30 mg1261110001100138011400017120010426100018100017112098203111070001210013100400
GSK1265744 60 mg1950200004000155409000191530124452000211120131470911621065080001600084000331

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Number of Participants With AEs and SAEs-Induction Phase

An AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose: results in death; is life-threatening; requires hospitalization or prolongation of existing hospitalization; results in disability/incapacity; is a congenital anomaly/birth defect; other medical events that may jeopardize the participant or may require medical or surgical intervention to prevent one of the outcomes mentioned before; all events of possible drug-induced liver injury with hyperbilirubinemia. (NCT01641809)
Timeframe: Up to Week 24

,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
Efavirenz 600 mg592
GSK1265744 10 mg542
GSK1265744 30 mg540
GSK1265744 60 mg552

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Number of Participants With AEs and SAEs Over Time

An AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose: results in death; is life-threatening; requires hospitalization or prolongation of existing hospitalization; results in disability/incapacity; is a congenital anomaly/birth defect; other medical events that may jeopardize the participant or may require medical or surgical intervention to prevent one of the outcomes mentioned before; all events of possible drug-induced liver injury with hyperbilirubinemia. Safety Population comprised of all randomized participants who were exposed to investigational products with the exception of any participants with documented evidence of not having consumed any amount of investigational product. (NCT01641809)
Timeframe: Up to Week 324

,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
Efavirenz 600 mg604
GSK1265744 10 mg5713
GSK1265744 30 mg5712
GSK1265744 60 mg6011

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Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)-Maintenance Phase

An AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose: results in death; is life-threatening; requires hospitalization or prolongation of existing hospitalization; results in disability/incapacity; is a congenital anomaly/birth defect; other medical events that may jeopardize the participant or may require medical or surgical intervention to prevent one of the outcomes mentioned before; all events of possible drug-induced liver injury with hyperbilirubinemia. Maintenance Safety Population comprised of all participants randomized to GSK1265744 and who were exposed to investigational products during the maintenance phase of the study with the exception of any participants with documented evidence of not having consumed any amount of investigational product. (NCT01641809)
Timeframe: Week 24 to Week 96

,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
Efavirenz 600 mg352
GSK1265744 10 mg405
GSK1265744 30 mg505
GSK1265744 60 mg505

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Number of Participants With Adherence to Study Treatment

Number of participants with >=90% adherence to study treatment based on pill count is summarized. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300 and 312

,
InterventionParticipants (Count of Participants)
Baseline; n=57, 55, 56, 52Week 4; n=54, 52, 53, 50Week 8; n=53, 50, 56, 48Week 12; n=55, 48, 53, 48Week 16; n=53, 51, 53, 44Week 20; n=51, 49, 55, 44Week 24; n=51, 46, 51, 43Week 28; n=49, 48, 53, 41Week 32; n=47, 48, 55, 41Week 36; n=46, 48, 50, 41Week 40; n=38, 35, 45, 39Week 48; n=33, 37, 45, 35Week 60; n=38, 38, 40, 37Week 72; n=35, 37, 44, 32Week 84; n=36, 39, 42, 33Week 96; n=31, 36, 33, 0Week 108; n=23, 23, 29, 0Week 120; n=30, 38, 41, 0Week 132; n=29, 32, 40, 0Week 144; n=33, 34, 43, 0Week 156; n=31, 28, 39, 0Week 168; n=29, 33, 41, 0Week 180; n=26, 29, 39, 0Week 192; n=30, 30, 39, 0Week 204; n=29, 32, 38, 0Week 216; n=29, 30, 37, 0Week 228; n=27, 34, 40, 0Week 240; n=28, 26, 41, 0Week 252; n=23, 26, 33, 0Week 264; n=15, 18, 24, 0Week 276; n=14, 14, 21, 0Week 288; n=12, 14, 18, 0Week 300; n=12, 13, 20, 0Week 312; n=1, 1, 0, 0
GSK1265744 10 mg5346494444454745464033323732342521282832302924282729252818121312111
GSK1265744 30 mg514945404540414642433033353536322036302925242427262728222116131071

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Percentage of Participants With Plasma HIV-1 RNA <50 Copies/mL Over Time by Visit Using the MSDF Algorithm

Plasma samples were collected for quantitative analysis of HIV-1 RNA. Percentage of participants with HIV-1 RNA <50 copies/mL over time was determined using the MSDF algorithm based on the current US FDA definition of the Snapshot algorithm. This algorithm treats all participants without HIV-1 RNA data at the visit of interest (due to missing data or discontinuation of investigational product prior to visit window) as well as participants who switch their concomitant antiretroviral therapy prior to the visit of interest as non-responders. Virological response within an analysis window was determined by the last available HIV-1 RNA measurement in that window while the participant was on-treatment. MSDF response rate was calculated as number of responders in the analysis window divided by the number of participants in the analysis population. (NCT01641809)
Timeframe: Baseline (Day 1), Weeks 2, 4, 8, 12, 16, 24, 26, 28, 32, 36, 40, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 180, 192, 204, 216, 228, 240, 252, 264, 276, 288, 300 and 312

,,,
InterventionPercentage of participants (Number)
BaselineWeek 2Week 4Week 8Week 12Week 16Week 24Week 26Week 28Week 32Week 36Week 40Week 48Week 60Week 72Week 84Week 96Week 108Week 120Week 132Week 144Week 156Week 168Week 180Week 192Week 204Week 216Week 228Week 240Week 252Week 264Week 276Week 288Week 300Week 312
Efavirenz 600 mg013244861747466696971687168686863000000000000000000
GSK1265744 10 mg048809088908778858385838078727268686562585857585755555350525352505252
GSK1265744 30 mg050788375838575788082828073737575727370676365676562636362626262626052
GSK1265744 60 mg051708782878785858785858785858584808080778075757475777574757570747070

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GMR of Cmax of Pitavastatin When Coadministered With Efavirenz or With Darunavir/Ritonavir

Geometric Mean Ratio (GMR) of Cmax for pitavastatin with Efavirenz vs. alone and GMR of Cmax for pitavastatin with darunavir/ritonavir vs. alone was reported. (NCT01695954)
Timeframe: Day 18

Interventionng/mL (Geometric Mean)
Arm A: (Pitavastatin and Efavirenz)1.20
Arm B: (Pitavastatin and Ritonavir-boosted Darunavir)0.93

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GMR of 24- Hour AUC of Pitavastatin When Coadministered With Efavirenz or With Darunavir/Ritonavir Over 24 Hour AUC of Pitavastatin

Geometric Mean Ratio (GMR) of 24- Hour Area under the plasma drug concentration-time curve (AUC) of pitavastatin when coadministered with efavirenz or with darunavir/ritonavir over 24 Hour (AUC) of pitavastatin (NCT01695954)
Timeframe: 0 to 24 hours

,
InterventionRatio (Geometric Mean)
GMR of Pitavastatin with (EFV or DRV)/PitavastatinGMR of (EFV or DRV) with Pitavastatin/(EFV or DRV)
Arm A: (Pitavastatin and Efavirenz).89.90
Arm B: (Pitavastatin and Darunavir).911.08

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AUC

24-hour area under the curve (AUC) for pitavastatin when coadministered with efavirenz and with darunavir/ritonavir and 24-hour AUC for efavirenz or darunavir when coadministered with pitavastatin (NCT01695954)
Timeframe: 0 to 24 hours

Interventionng*hr/mL (Mean)
Arm A: (Pitavastatin and Efavirenz)85.3
Arm B: (Pitavastatin and Darunavir)62.8

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Percentage of Participants With Plasma HIV-1 RNA Levels < 50 Copies/mL at Week 48

Percentage of Participants with plasma HIV-1 RNA <50 copies/mL, obtained by the modified Food and Drug Administration (FDA) Snapshot method. (NCT01709084)
Timeframe: Week 48

InterventionPercentage of Participants (Number)
TDF/FTC/RPV93.9
TDF/FTC/EFV96.2

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Percentage of Participants With Plasma HIV-1 RNA Levels >= 50 Copies Per Milliliter (Copies/mL) at Week 48 Based on Time to Loss of Virologic Response (TLOVR) [Non-virologic Failure Censored] Imputation Method.

Percentage of participants with plasma HIV-1 RNA levels analysed based on TLOVR imputation method which is defined as confirmed plasma HIV-1 RNA >=50 copies/mL, excluding participants who discontinued the study with HIV-1 RNA suppression <50 copies/mL. (NCT01709084)
Timeframe: Week 48

InterventionPercentage of Participants (Number)
TDF/FTC/RPV1.5
TDF/FTC/EFV1.0

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Percentage of Participants With Plasma Human Immunodeficiency Virus - Type 1 Ribonucleic Acid (HIV-1 RNA) Levels Less Than (<) 400 Copies Per Milliliter (Copies/mL) at Week 48

Percentage of Participants with viral load (plasma HIV-1 RNA levels) less than 400 copies per mL at Week 48, obtained by the modified Food and Drug Administration (FDA) Snapshot method. (NCT01709084)
Timeframe: Week 48

InterventionPercentage of Participants (Number)
TDF/FTC/RPV93.9
TDF/FTC/EFV96.2

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Percentage of Participants With Plasma HIV-1 RNA Levels More Than or Equal to (>=) 400 Copies/mL at Week 48 Based on Time to Loss of Virologic Response (TLOVR) [Non-virologic Failure Censored] Imputation Method.

Percentage of participants with plasma HIV-1 RNA levels analysed based on time to loss of virologic response (TLOVR) imputation method which is defined as confirmed plasma HIV-1 RNA >=400 copies/mL, excluding participants who discontinued the study with HIV-1 RNA suppression <400 copies/mL. (NCT01709084)
Timeframe: Week 48

InterventionPercentage of Participants (Number)
TDF/FTC/RPV0.5
TDF/FTC/EFV0.5

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Number of Participants With Treatment-Emergent Nucleoside Reverse Transcriptase Inhibitor (N[t]RTI) or Nucleoside/Nucleotide Reverse Transcriptase Inhibitor (NNRTI) Mutations

To compare the loss of treatment options, the number of participants with treatment-emergent N[t]RTI or NNRTI mutations, as defined by IAS-USA (2014), after virologic failure were compared between the treatment groups. (NCT01709084)
Timeframe: Up to Week 48

InterventionParticipants (Number)
TDF/FTC/RPV0
TDF/FTC/EFV0

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Percentage of Participant With Treatment Adherence Based on Tablet Count

In both treatment groups adherence rates assessed by tablet count, the majority of participants had an adherence of >95% (97% and 98% in RPV and EFV treated treatment groups respectively). (NCT01709084)
Timeframe: Up to 48 Weeks

InterventionPercentage of Participants (Number)
TDF/FTC/RPV97.2
TDF/FTC/EFV97.6

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Early Mortality

Proportion of deaths in each group (NCT01837277)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
Dolutegravir9
Efavirenz13

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Number of Participants Who Experienced Dose-Limiting Toxicities (DLTs)

A DLT was any drug-related toxicity with grade ≥ 3 according to NCI-CTCAE v4.0 (except alopecia, nausea and vomiting, regardless of grade), any drug-related toxicity, regardless of grade, who led a treatment delay> 14 days, a score ≥ 19 for the Hospital Anxiety And Depression Scale (HAD) during treatment. (NCT01878890)
Timeframe: Up to 28 days for each dosing cohort

InterventionParticipants (Count of Participants)
Efavirenz: 600 mg0
Efavirenz: 1200 mg3
Efavirenz: 1800 mg1
Efavirenz: 2200 mg3

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Maximum Tolerated Dose (MTD) of Efavirenz

"MTD was determined by testing increasing doses up to 3000 mg (oral daily intake).~The dose escalation scheme is the continual reassessment method likehood approach (CRML) described by O'Quigley and Shen [O'Quigley et al. Biometrics 1996].~MTD reflects the highest dose of drug that did not cause a Dose-Limiting Toxicity (DLT) in > 25% of participants.~A DLT was any drug-related toxicity with grade ≥ 3 according to NCI-CTCAE v4.0 (except alopecia, nausea and vomiting, regardless of grade), any drug-related toxicity, regardless of grade, who led a treatment delay> 14 days, a score ≥ 19 for the Hospital Anxiety And Depression Scale (HAD) during treatment." (NCT01878890)
Timeframe: Up to 28 days for each dosing cohort

Interventionmg (Number)
All Participants1200

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12-week Objective Response Rate

Objective response is defined as complete or partial response (CR, PR) using the Response Evaluation Criteria in Solid Tumors (RECIST v1.1). Objective reponse rate is calculated as the number of patients with objective reponse divided by the number of alive patients. (NCT01878890)
Timeframe: up to 3 months after first adminitration of Efavirenz

InterventionParticipants (Count of Participants)
All Participants0

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12-week Non-progression Rate

Non progression is defined as complete or partial response (CR, PR) or stable disease (SD), using the Response Evaluation Criteria in Solid Tumors (RECIST v1.1). Non-progression rate is calculated as the number of alive and progression free patients divided by the number of patients. (NCT01878890)
Timeframe: Evaluated up to 3 months after first administration of Efavirenz

InterventionParticipants (Count of Participants)
All Participants0

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EFV PK Parameter Minimum Plasma Concentration (Cmin) Determined Based on EFV Levels From Individual Participants Enrolled in Arm B

This evaluates the effect of NuvaRing on the EFV PK parameter Cmin obtained from both sampling periods, before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. Cmin defines minimum concentration observed within the first 8 hours of the 24 hour dosing interval. (NCT01903031)
Timeframe: Intensive EFV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement).

Interventionng/mL (Median)
Cmin day 0Cmin day 21
NuvaRing With EFV Plus ≥2 NRTIs2121.51766.0

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RTV PK Parameter Tmax Determined Based on RTV Levels From Individual Participants Enrolled in Arm C

This evaluates the effect of NuvaRing on the PK parameter Tmax of RTV before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. Tmax defines time to maximum concentration since dose is initiated. (NCT01903031)
Timeframe: Intensive RTV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement)

Interventionhour (Median)
Tmax day 0Tmax day 21
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs3.03.0

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RTV PK Parameter Cmin Determined Based on RTV Levels From Individual Participants Enrolled in Arm C

This evaluates the effect of NuvaRing on the PK parameter Cmin of RTV before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. Cmin defines minimum concentration observed within the first 8 hours of the 24 hour dosing interval. (NCT01903031)
Timeframe: Intensive RTV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement)

Interventionng/mL (Median)
Cmin day 0Cmin day 21
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs70.051.9

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RTV PK Parameter Cmax Determined Based on RTV Levels From Individual Participants Enrolled in Arm C

This evaluates the effect of NuvaRing on the PK parameter Cmax of RTV before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. Cmax defines maximum concentration observed within the first 8 hours of the 24 hour dosing interval. (NCT01903031)
Timeframe: Intensive RTV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement)

Interventionng/mL (Median)
Cmax day 0Cmax day 21
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs1437.01063.0

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RTV PK Parameter CLss/F Determined Based on RTV Levels From Individual Participants Enrolled in Arm C

This evaluates the effect of NuvaRing on the PK parameter CLss/F of RTV before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. CLss/F defines apparent oral clearance. (NCT01903031)
Timeframe: Intensive RTV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement)

Interventionhour (Median)
CLss/F day 0CLss/F day 21
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs9.313.9

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Ritonavir (RTV) PK Parameter AUC(0-24h) Calculated Based on Intensive RTV PK Samples Obtained From Individual Participants Enrolled in Arm C

This evaluates the effect of NuvaRing on the PK parameter AUC(0-24h) of RTV before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. AUC(0-24h) defines area under the concentration-time curve over the period of 24 hours (pre-dose concentration was used to impute concentration at 24h). (NCT01903031)
Timeframe: Intensive RTV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement)

Interventionh*ng/mL (Median)
AUC0-24h day 0AUC0-24h day 21
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs10740.07210.7

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Proportion of Participants With Progesterone Levels Greater Than 5 ng/mL.

This evaluates alterations in progesterone levels due to the potential PK interaction between NuvaRing and the ARVs EFV and ATV/r by examining progesterone levels at study days 0 (before vaginal ring placement), 7, 14, and 21 (before vaginal ring removal), and study day 28, without regard to menstrual cycle status at study entry. (NCT01903031)
Timeframe: Study days 0, 7, 14, 21 and 28

,,
Interventionproportion of participants (Number)
Proportion with progesterone >5 at day 0Proportion with progesterone >5 at day 7Proportion with progesterone >5 at day 14Proportion with progesterone >5 at day 21Proportion with progesterone >5 at day 28
NuvaRing and no ART0.080.080.000.000.00
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs0.250.080.000.000.00
NuvaRing With EFV Plus ≥2 NRTIs0.040.240.040.000.00

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Proportion of Participants With Plasma HIV-1 RNA Levels <40 Copies/mL

This evaluates the short-term impact of Nuvaring on virologic suppression in participants who have been administered Nuvaring alone or together with EFV or ATV/r by measuring proportion of participants with plasma HIV-1 RNA levels <40 copies/mL at study day 0 (before vaginal ring placement) and study day 21 (three weeks after vaginal ring placement). An FDA-approved HIV-1 RNA assay was required. (NCT01903031)
Timeframe: Study day 0 and study day 21

,,
Interventionproportion of participants (Number)
Proportion with HIV-1 RNA <40 copies/mL at day 0Proportion with HIV-1 RNA <40 copies/mL at day 21
NuvaRing and no ART0.220.17
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs0.890.85
NuvaRing With EFV Plus ≥2 NRTIs0.930.85

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Etonogestrel Concentrations Obtained on Study Days 7 and 14

This evaluates the effect of EFV and ATV/r on etonogestrel by measuring etonogestrel concentrations on all three study arms 7 and 14 days after NuvaRing administration. The assay lower limit of quantification for etonogestrel was 250 pg/mL; values < 250 were assigned a value of half the lower limit (ie, 125 pg/mL). (NCT01903031)
Timeframe: Study days 7 and 14

,,
Interventionpg/mL (Median)
Concentration at Day 7Concentration at Day 14
NuvaRing and no ART1970.002070.00
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs3250.003530.00
NuvaRing With EFV Plus ≥2 NRTIs427.00437.00

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Ethinyl Estradiol Concentrations Obtained on Study Days 7 and 14.

This evaluates the effect of EFV and ATV/r on ethinyl estradiol by measuring ethinyl estradiol concentrations on all three study arms 7 and 14 days after NuvaRing administration. The assay lower limit of quantification for ethinyl estradiol was 5 pg/mL; values < 5 were assigned a value of half the lower limit (ie, 2.5 pg/mL). (NCT01903031)
Timeframe: Study days 7 and 14

,,
Interventionpg/mL (Median)
Concentration at Day 7Concentration at Day 14
NuvaRing and no ART18.0519.70
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs15.7016.55
NuvaRing With EFV Plus ≥2 NRTIs9.9810.50

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EFV PK Parameter Maximum Plasma Concentration (Cmax) Determined Based on EFV Levels From Individual Participants Enrolled in Arm B

This evaluates the effect of NuvaRing on the EFV PK parameter Cmax obtained from both sampling periods, before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. Cmax defines maximum concentration observed within the first 8 hours of the 24 hour dosing interval. (NCT01903031)
Timeframe: Intensive EFV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement).

Interventionng/mL (Median)
Cmax day 0Cmax day 21
NuvaRing With EFV Plus ≥2 NRTIs4541.03786.0

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EFV PK Parameter Clearance (CLss/F) Determined Based on EFV Levels From Individual Participants Enrolled in Arm B

This evaluates the effect of NuvaRing on the EFV PK parameter CLss/F obtained from both sampling periods, before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. CLss/F defines apparent oral clearance (NCT01903031)
Timeframe: Intensive EFV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement).

InterventionL/h (Median)
CLss/F day 0CLss/F day 21
NuvaRing With EFV Plus ≥2 NRTIs8.710.4

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EFV PK Parameter Area Under the Concentration-Time Curve (AUC0-24hours) Calculated Based on Intensive EFV PK Samples Obtained From Individual Participants Enrolled in Arm B

This evaluates the effect of NuvaRing on the PK parameter AUC(0-24h) of EFV before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. AUC(0-24h) defines area under the concentration-time curve over the period of 24 hours (pre-dose concentration was used to impute concentration at 24h). (NCT01903031)
Timeframe: Intensive EFV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement).

Interventionh*ng/mL (Median)
AUC0-24h day 0AUC0-24h day 21
NuvaRing With EFV Plus ≥2 NRTIs68949.157795.9

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ATV PK Parameter Time to Cmax (Tmax) Determined Based on ATV Levels From Individual Participants Enrolled in Arm C

This evaluates the effect of NuvaRing on the ATV PK parameter Tmax obtained from both sampling periods, before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. Tmax defines time to maximum concentration since dose is initiated. (NCT01903031)
Timeframe: Intensive ATV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement).

Interventionhour (Median)
Tmax day 0Tmax day 21
NuvaRing With ATV/r Plus TDF ≥1 NRTIs2.93.0

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ATV PK Parameter Cmin Determined Based on ATV Levels From Individual Participants Enrolled in Arm C

This evaluates the effect of NuvaRing on the ATV PK parameter Cmin obtained from both sampling periods, before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. Cmin defines minimum concentration observed within the first 8 hours of the 24 hour dosing interval. (NCT01903031)
Timeframe: Intensive ATV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement).

Interventionng/mL (Median)
Cmin day 0Cmin day 21
NuvaRing With ATV/r Plus TDF ≥1 NRTIs796.7599.4

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ATV PK Parameter Cmax Determined Based on ATV Levels From Individual Participants Enrolled in Arm C

This evaluates the effect of NuvaRing on the ATV PK parameter Cmax obtained from both sampling periods, before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. Cmax defines maximum concentration observed within the first 8 hours of the 24 hour dosing interval. (NCT01903031)
Timeframe: Intensive ATV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement).

Interventionng/mL (Median)
Cmax day 0Cmax day 21
NuvaRing With ATV/r Plus TDF ≥1 NRTIs4291.03583.0

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ATV PK Parameter CLss/F Determined Based on ATV Levels From Individual Participants Enrolled in Arm C

This evaluates the effect of NuvaRing on the ATV PK parameter CLss/F obtained from both sampling periods, before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. CLss/f defines apparent oral clearance. (NCT01903031)
Timeframe: Intensive ATV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement).

InterventionL/h (Median)
CLss/F day 0CLss/F day 21
NuvaRing With ATV/r Plus TDF ≥1 NRTIs6.88.2

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ATV PK Parameter AUC(0-24h) Calculated Based on Intensive Atazanavir (ATV) PK Samples Obtained From Individual Participants Enrolled in Arm C

This evaluates the effect of NuvaRing on the PK parameter AUC(0-24h) of ATV before NuvaRing placement (at study day 0) and three weeks later (on study day 21), prior to NuvaRing removal. AUC(0-24h) defines area under the concentration-time curve over the period of 24 hours (pre-dose concentration was used to impute concentration at 24h). (NCT01903031)
Timeframe: Intensive ATV PK samples at pre-dose, 1, 3, 4, 5, and 8 hours post-dose on study day 0 (before vaginal ring placement) and on study day 21 (3 weeks after vaginal ring placement)

Interventionh*ng/mL (Median)
AUC0-24h day 0AUC0-24h day 21
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs44313.736764.7

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Etonogestrel Concentrations at Study Day 21

This evaluates the effect of EFV and ATV/r on etonogestrel by measuring etonogestrel concentrations on all three study arms 21 days after NuvaRing administration. The pharmacokinetic (PK) blood sample for measurement of etonogestrel on study day 21 was taken before the NuvaRing was removed. The assay lower limit of quantification for etonogestrel was 250 pg/mL; values < 250 were assigned a value of half the lower limit (ie, 125 pg/mL). (NCT01903031)
Timeframe: Day 21

Interventionpg/mL (Median)
NuvaRing and no ART1860.00
NuvaRing With EFV Plus ≥2 NRTIs429.00
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs3290.00

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Ethinyl Estradiol Concentrations at Study Day 21

This evaluates the effect of EFV and ATV/r on ethinyl estradiol by measuring ethinyl estradiol concentrations on all three study arms 21 days after NuvaRing administration. The PK blood sample for measurement of ethinyl estradiol on study day 21 was taken before the NuvaRing was removed. The assay lower limit of quantification for ethinyl estradiol was 5 pg/mL ; values < 5 were assigned a value of half the lower limit (ie, 2.5 pg/mL). (NCT01903031)
Timeframe: Day 21

Interventionpg/mL (Median)
NuvaRing and no ART21.30
NuvaRing With EFV Plus ≥2 NRTIs11.40
NuvaRing With ATV/r Plus TDF and ≥1 NRTIs16.05

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The Proportion of Treatment Failure at Week 48 for Both Arms.

The proportion of treatment failure, defined as detectable HIV RNA copies copies/mL, at week 48 for both arms. (NCT01989910)
Timeframe: At week 48 of both arms

InterventionParticipants (Count of Participants)
Raltegravir2
Efavirenz2

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The Proportion of Patients Who Can Achieve of Less Than 20 HIV RNA Copies Per ml at Week 48 of Both Arms.

Virological response to achieve HIV RNA copies <20 copies/mL at week 48 of both arms. (NCT01989910)
Timeframe: At week 48 of both arms

InterventionParticipants (Count of Participants)
Raltegravir41
Efavirenz36

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The Proportion of Patients With Achievement of Less Than 400 HIV RNA Copies Per ml at Week 48 for Both Arms.

Virological response to achieve HIV RNA copies <400 copies/mL at week 48 of both arms. (NCT01989910)
Timeframe: At week 48 of both arms

InterventionParticipants (Count of Participants)
Raltegravir41
Efavirenz36

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LCM vs CDM, Induction ART: Body Mass Index-for-age Z-score

Age-adjusted change in body mass index-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 4 years (maximum 5 years)

Interventionage-adjusted z-score (Mean)
Clinically Driven Monitoring (CDM)0.65
Laboratory Plus Clinical Monitoring (LCM)0.61
Arm A: ABC+3TC+NNRTI0.56
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance0.64
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance0.69

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LCM vs CDM, Induction ART: Cessation of First-line Regimen for Clinical/Immunological Failure

Number of participants stopping their first-line regimen for clinical/immunological failure, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)28
Laboratory Plus Clinical Monitoring (LCM)35

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LCM vs CDM, Induction ART: Change From Baseline in Absolute CD4 to Week 72

Estimated in those >5 years at enrolment, in whom absolute CD4 is meaningful. (In uninfected children, CD4 decreases with age during early childhood.) (NCT02028676)
Timeframe: Baseline, week 72

Interventionabsolute cells per mm3 (Mean)
Clinically Driven Monitoring (CDM)408
Laboratory Plus Clinical Monitoring (LCM)385
Arm A: ABC+3TC+NNRTI402
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance447
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance336

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LCM vs CDM, Induction ART: Height-for-age Z-score

Age-adjusted change in weight-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 4 years (maximum 5 years)

Interventionage-adjusted z-score (Mean)
Clinically Driven Monitoring (CDM)0.36
Laboratory Plus Clinical Monitoring (LCM)0.43
Arm A: ABC+3TC+NNRTI0.40
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance0.40
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance0.38

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LCM vs CDM, Induction ART: New ART-modifying Adverse Event

Number of participants with a new ART-modifying adverse event, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)31
Laboratory Plus Clinical Monitoring (LCM)32
Arm A: ABC+3TC+NNRTI8
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance30
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance25

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LCM vs CDM, Induction ART: New or Recurrent WHO Stage 3 or 4 Event or Death

Number of participants with a new or recurrent WHO stage 3 or 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)91
Laboratory Plus Clinical Monitoring (LCM)79
Arm A: ABC+3TC+NNRTI64
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance53
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance53

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LCM vs CDM, Induction ART: New WHO Stage 3 or 4 Event or Death

Number of participants with a new WHO stage 3 or 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)77
Laboratory Plus Clinical Monitoring (LCM)73
Arm A: ABC+3TC+NNRTI73
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance61
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance54

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LCM vs CDM, Induction ART: Weight-for-age Z-score

Age-adjusted change in weight-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 4 years (maximum 5 years)

Interventionage-adjusted z-score (Mean)
Clinically Driven Monitoring (CDM)0.76
Laboratory Plus Clinical Monitoring (LCM)0.78
Arm A: ABC+3TC+NNRTI0.72
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance0.79
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance0.80

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LCM vs CDM: Change From Baseline in CD4% to Week 144

(NCT02028676)
Timeframe: Baseline, week 144

Interventionpercentage of total lymphocytes (Mean)
Clinically Driven Monitoring (CDM)19.7
Laboratory Plus Clinical Monitoring (LCM)19.4

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LCM vs CDM: Change From Baseline in CD4% to Week 72

(NCT02028676)
Timeframe: Baseline, week 72

Interventionpercentage of total lymphocytes (Mean)
Clinically Driven Monitoring (CDM)17.2
Laboratory Plus Clinical Monitoring (LCM)16.7

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LCM vs CDM: Disease Progression to a New WHO Stage 4 Event or Death

Number of participants with disease progression to a new WHO stage 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)47
Laboratory Plus Clinical Monitoring (LCM)39

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Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)

Binary outcome measure: missed any doses of ART in the last 4 weeks by self-report. Mean calculated across all 12-weekly visits attended over the whole follow-up (no specific timepoint prespecified), giving the percentage of visits attended where the carer/participant reported missing any pills in the last 4 weeks. (NCT02028676)
Timeframe: Mean over median 2 years (from once vs twice daily randomization to 16 March 2012; maximum 2.6 years)

Intervention% of visits reporting missed pills (Mean)
Once-daily ABC+3TC8
Twice-daily ABC+3TC8

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Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks) at 48 Weeks

Number of participants reporting missing any doses of ART in the last 4 weeks by self-report at 48 weeks. (NCT02028676)
Timeframe: 48 weeks after randomization to once- versus twice-daily

Interventionparticipants (Number)
Once-daily ABC+3TC32
Twice-daily ABC+3TC29

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Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks) at 96 Weeks

Number of participants reporting missing any doses of ART in the last 4 weeks by self-report at 96 weeks. (NCT02028676)
Timeframe: 96 weeks after randomization to once- versus twice-daily

Interventionparticipants (Number)
Once-daily ABC+3TC26
Twice-daily ABC+3TC25

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Once Versus Twice Daily Abacavir+Lamivudine: All-cause Mortality

Number of participants who died, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from randomization to 16 March 2012; maximum 2.6 years)

Interventionparticipants (Number)
Once-daily ABC+3TC1
Twice-daily ABC+3TC4

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Once Versus Twice Daily Abacavir+Lamivudine: Body Mass Index-for-age Z-score

Age-adjusted change in body mass index-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from once vs twice daily randomization to 16 March 2012; maximum 2.6 years)

Interventionage-adjusted z-score (Mean)
Once-daily ABC+3TC-0.29
Twice-daily ABC+3TC-0.35

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 48

Estimated in those >5 years at enrolment, in whom absolute CD4 is meaningful. (In uninfected children, CD4 decreases with age during early childhood.) (NCT02028676)
Timeframe: Randomisation to once vs twice daily, week 48

Interventioncells per mm3 (Mean)
Once-daily ABC+3TC3
Twice-daily ABC+3TC-3

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 72

All participants aged >5 years at randomization to once versus twice daily alive in follow-up with CD4 measured (NCT02028676)
Timeframe: Baseline, week 72

Interventioncells per mm3 (Mean)
Once-daily ABC+3TC-6
Twice-daily ABC+3TC27

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 96

All participants aged >5 years at randomization to once versus twice daily alive in follow-up with CD4 measured (NCT02028676)
Timeframe: Randomisation to once vs twice daily, week 96

Interventioncells per mm3 (Mean)
Once-daily ABC+3TC-26
Twice-daily ABC+3TC60

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 48

(NCT02028676)
Timeframe: Randomisation to once vs twice daily, week 48

Interventionpercentage of total lymphocytes (Mean)
Once-daily ABC+3TC0.9
Twice-daily ABC+3TC1.3

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 72

(NCT02028676)
Timeframe: Baseline, week 72

Interventionpercentage of total lymphocytes (Mean)
Once-daily ABC+3TC1.9
Twice-daily ABC+3TC1.9

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 96

(NCT02028676)
Timeframe: Randomisation to once vs twice daily, week 96

Interventionpercentage of lymphocytes (Mean)
Once-daily ABC+3TC1.6
Twice-daily ABC+3TC2.5

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Once Versus Twice Daily Abacavir+Lamivudine: Height-for-age Z-score

Age-adjusted change in height-for-age Z-score over all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from once vs twice daily randomization to 16 March 2012; maximum 2.6 years)

Interventionage-adjusted z-score (Mean)
Once-daily ABC+3TC0.28
Twice-daily ABC+3TC0.32

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Once Versus Twice Daily Abacavir+Lamivudine: New WHO Stage 3 or 4 Event or Death

Number of participants with a new WHO stage 3 or 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from randomization to 16 March 2012; maximum 2.6 years)

Interventionparticipants (Number)
Once-daily ABC+3TC9
Twice-daily ABC+3TC12

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Once Versus Twice Daily Abacavir+Lamivudine: New WHO Stage 4 Event or Death

Number of participants with a new WHO stage 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from randomization to 16 March 2012; maximum 2.6 years)

Interventionparticipants (Number)
Once-daily ABC+3TC3
Twice-daily ABC+3TC7

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Once Versus Twice Daily Abacavir+Lamivudine: Suppressed HIV RNA Viral Load 48 Weeks After Randomisation

Number of participants with HIV RNA viral load <80 copies/ml at 48 weeks. Measured retrospectively on stored plasma specimens: due to low stored volumes from some children, samples had to be diluted and therefore a threshold of <80 copies/ml was used to indicate suppression. (NCT02028676)
Timeframe: 48 weeks

Interventionparticipants (Number)
Once-daily ABC+3TC236
Twice-daily ABC+3TC242

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Once Versus Twice Daily Abacavir+Lamivudine: Weight-for-age Z-score

Age-adjusted change in weight-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from once vs twice daily randomization to 16 March 2012; maximum 2.6 years)

Interventionage-adjusted z-score (Mean)
Once-daily ABC+3TC0.01
Twice-daily ABC+3TC-0.00

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Cotrimoxazole: Change From Baseline in CD4% to Week 72

(NCT02028676)
Timeframe: Baseline, week 72

Interventionpercentage of total lymphocytes (Mean)
Continued Cotrimoxazole Prophylaxis1.7
Stopped Cotrimoxazole Prophylaxis1.1

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Cotrimoxazole: New Hospitalisation or Death

Number of participants with a new hospitalisation or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis48
Stopped Cotrimoxazole Prophylaxis72

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Once Versus Twice Daily Abacavir+Lamivudine: Suppression of HIV RNA Viral Load 96 Weeks After Randomisation

Number of participants with HIV RNA viral load <80 copies/ml at 96 weeks. Threshold for suppression <80 copies/ml as samples had to be diluted due to low volumes. (NCT02028676)
Timeframe: 96 weeks

Interventionparticipants (Number)
Once-daily ABC+3TC230
Twice-daily ABC+3TC234

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CDM vs LCM, Induction ART: Suppression of HIV RNA Viral Load 144 Weeks After Baseline

Number of participants with HIV RNA viral load <80 copies/ml 144 weeks after baseline. Threshold for suppression <80 copies/ml as samples had to be diluted due to low volumes. (NCT02028676)
Timeframe: 144 weeks

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)192
Laboratory Plus Clinical Monitoring (LCM)193
Arm A: ABC+3TC+NNRTI127
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance135
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance124

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CDM vs LCM, Induction ART: Suppression of HIV RNA Viral Load 72 Weeks After Baseline

Number of participants with HIV RNA viral load <80 copies/ml 72 weeks after baseline. Threshold for suppression <80 copies/ml as samples had to be diluted due to low volumes. (NCT02028676)
Timeframe: 72 weeks

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)76
Laboratory Plus Clinical Monitoring (LCM)78
Arm A: ABC+3TC+NNRTI56
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance72
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance26

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Cotrimoxazole: All-cause Mortality

Number of participants who died, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis3
Stopped Cotrimoxazole Prophylaxis2

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Cotrimoxazole: Body Mass Index-for-age Z-score

Age-adjusted change in body mass index-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionage-adjusted z-score (Mean)
Continued Cotrimoxazole Prophylaxis-0.24
Stopped Cotrimoxazole Prophylaxis-0.28

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Cotrimoxazole: Change From Baseline in Absolute CD4 to Week 72

Estimated in those >5 years at randomization to stop vs continue, in whom absolute CD4 is meaningful. (In uninfected children, CD4 decreases with age during early childhood.) (NCT02028676)
Timeframe: Baseline, week 72

Interventioncells per mm3 (Mean)
Continued Cotrimoxazole Prophylaxis7
Stopped Cotrimoxazole Prophylaxis-2

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Cotrimoxazole: Height-for-age Z-score

Age-adjusted change in height-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionage-adjusted z-score (Mean)
Continued Cotrimoxazole Prophylaxis0.22
Stopped Cotrimoxazole Prophylaxis0.19

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Cotrimoxazole: New Clinical and Diagnostic Positive Malaria

Number of participants with a new clinical and diagnostic positive malaria, to be analysed using time-to-event methods. Diagnostic positive by either microscopy (thick film) or rapid diagnostic test (RDT) (NCT02028676)
Timeframe: Median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis39
Stopped Cotrimoxazole Prophylaxis77

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LCM vs CDM, Induction ART: Change From Baseline in Absolute CD4 to Week 144

Estimated in those >5 years at enrolment, in whom absolute CD4 is meaningful. (In uninfected children, CD4 decreases with age during early childhood.) (NCT02028676)
Timeframe: Baseline, week 144

Interventionabsolute cells per mm3 (Mean)
Clinically Driven Monitoring (CDM)418
Laboratory Plus Clinical Monitoring (LCM)420
Arm A: ABC+3TC+NNRTI446
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance450
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance360

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Cotrimoxazole: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)

Binary outcome measure: missed any doses of ART in the last 4 weeks by self-report. Mean calculated across all 12-weekly visits attended over the whole follow-up (no specific timepoint prespecified), giving the percentage of visits attended where the carer/participant reported missing any pills in the last 4 weeks. (NCT02028676)
Timeframe: Mean over median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Intervention% of visits reporting missed pills (Mean)
Continued Cotrimoxazole Prophylaxis9
Stopped Cotrimoxazole Prophylaxis8

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Cotrimoxazole: New Severe Pneumonia

Number of participants with a new severe pneumonia, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis7
Stopped Cotrimoxazole Prophylaxis10

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Cotrimoxazole: New WHO Stage 3 or 4 Event or Death

Number of participants with a new WHO stage 3 or 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis8
Stopped Cotrimoxazole Prophylaxis19

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Cotrimoxazole: New WHO Stage 3 Severe Recurrent Pneumonia or Diarrhoea

Number of participants with a new WHO stage 3 severe recurrent pneumonia or diarrhoea, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis1
Stopped Cotrimoxazole Prophylaxis4

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Cotrimoxazole: New WHO Stage 4 Event or Death

Number of participants with a new WHO stage 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis4
Stopped Cotrimoxazole Prophylaxis7

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Cotrimoxazole: Weight-for-age Z-score

Age-adjusted change in weight-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionage-adjusted z-score (Mean)
Continued Cotrimoxazole Prophylaxis-0.01
Stopped Cotrimoxazole Prophylaxis-0.05

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Induction ART: Change From Baseline in CD4% 72 Weeks After ART Initiation

(NCT02028676)
Timeframe: Baseline, 72 weeks

Interventionpercentage of total lymphocytes (Mean)
Arm A: ABC+3TC+NNRTI16.4
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance17.1
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance17.3

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Induction ART: Change From Baseline in CD4% to 144 Weeks From ART Initiation

(NCT02028676)
Timeframe: Baseline, 144 weeks

Interventionpercentage of total lymphocytes (Mean)
Arm A: ABC+3TC+NNRTI19.8
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance19.6
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance19.2

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Induction ART: New WHO Stage 4 Event or Death

Number of participants with a new WHO stage 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Arm A: ABC+3TC+NNRTI30
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance28
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance28

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LCM vs CDM, Induction ART: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)

Binary outcome measure: missed any doses of ART in the last 4 weeks by self-report. Mean calculated across all 12-weekly visits attended over the whole follow-up (no specific timepoint prespecified), giving the percentage of visits attended where the carer/participant reported missing any pills in the last 4 weeks. (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Intervention% of visits reporting missed pills (Mean)
Clinically Driven Monitoring (CDM)8.5
Laboratory Plus Clinical Monitoring (LCM)9.4
Arm A: ABC+3TC+NNRTI8.3
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance9.5
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance9.1

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LCM vs CDM, Induction ART: All-cause Mortality

Number of participants who died from any cause, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)25
Laboratory Plus Clinical Monitoring (LCM)29
Arm A: ABC+3TC+NNRTI20
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance14
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance20

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Efavirenz AUC0-inf (Single Dose) and AUC0-24(Multiple Dose)

After the samples collection, blood from phase 2 and phase 4 were used to perform the quantification of Efavirenz in plasma. The composite of the efavirenz concentration (blood collection between 0 to 120 hrs) were used to calculate the area under the plasma concentration time curve (AUC0-inf for single dose and AUC0-24 for multiple dose) of efavirenz. (NCT02401256)
Timeframe: Single dose pharmacokinetics (PK) versus multiple doses (after 17 day pretreatment) PK (total 38 days for each subject)

,,
Interventionh*uM (Mean)
Efavirenz AUC0-inf (Single Dose)Efavirenz AUC0-24 (Multiple Dose)
CYP2B6*1/*1411.53183.97
CYP2B6*1/*6620.36254.40
CYP2B6*6/*6522.42321.86

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Cumulative Probability of Infant Deaths

The Kaplan-Meier estimate of the cumulative probability of infant deaths from birth through 50 weeks after birth. (NCT03048422)
Timeframe: Birth through 50 weeks after birth

InterventionCumulative probability per 100 persons (Number)
Arm 1 Infants1.0
Arm 2 Infants2.0
Arm 3 Infants6.9

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Count of Infants With HIV-1 Antiretroviral Drug Resistance Mutations at the Time of Infant HIV Diagnosis

Count of infants with HIV-1 antiretroviral drug resistance mutations (to any antiretroviral drug) at the time of infant HIV diagnosis, based on laboratory blood test results. (NCT03048422)
Timeframe: From birth through 50 weeks postpartum

InterventionParticipants (Count of Participants)
Arm 1 Infants1
Arm 2 Infants0
Arm 3 Infants1

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Maternal Change in Creatinine Clearance

Maternal change in creatinine clearance per week based on generalized estimating equations (NCT03048422)
Timeframe: Baseline to 50 weeks postpartum

InterventionmL/min (Mean)
Arm 1: Maternal DTG+FTC/TAF-0.980
Arm 2: Maternal DTG+FTC/TDF-0.887
Arm 3: Maternal EFV/FTC/TDF-0.935

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Change in Maternal Weight Overall

Change in maternal weight per week based on generalized estimating equations (NCT03048422)
Timeframe: Baseline to 50 weeks postpartum

Interventionkg/week (Mean)
Arm 1: Maternal DTG+FTC/TAF-0.027
Arm 2: Maternal DTG+FTC/TDF-0.050
Arm 3: Maternal EFV/FTC/TDF-0.084

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Change in Maternal Weight Antepartum

Change in maternal antepartum weight per week based on generalized estimating equations (NCT03048422)
Timeframe: Baseline through before delivery (up to one day prior)

Interventionkg/week (Mean)
Arm 1: Maternal DTG+FTC/TAF0.378
Arm 2: Maternal DTG+FTC/TDF0.319
Arm 3: Maternal EFV/FTC/TDF0.291

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Cumulative Probability of Women Experiencing Grade 3 or Higher Adverse Event

"The Kaplan-Meier estimate of the cumulative probability of women experiencing grade 3 or higher adverse events, including events resulting in death due to any cause.~Time to first maternal grade 3 or higher adverse event was defined as the first grade 3 or higher adverse event that occurred after randomization and before 74 weeks of follow-up. The timeframe of 74 weeks was determined by adding up 56 weeks of postpartum follow-up to the mean duration of antepartum follow-up, which was 18 weeks." (NCT03048422)
Timeframe: From randomization up to 74 weeks

,
InterventionCumulative probability per 100 persons (Number)
Arm 1: Maternal DTG+FTC/TAF25.1
Arm 2: Maternal DTG+FTC/TDF30.8
Arm 3: Maternal EFV/FTC/TDF27.9
Arms 1 and 2: Maternal DTG+FTC/TAF and DTG+FTC/TDF27.9
Arm 3: Maternal EFV/FTC/TDF27.9

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Cumulative Probability of Infants Experiencing Grade 3 or Higher Adverse Event

The Kaplan-Meier estimate of the cumulative probability of infants experiencing grade 3 or higher adverse events, including events resulting in death due to any cause. (NCT03048422)
Timeframe: From birth through Week 50 postpartum

InterventionCumulative probability per 100 persons (Number)
Arm 1 Infants25.3
Arm 2 Infants28.6
Arm 3 Infants30.9

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Cumulative Probability of Infants Experiencing Grade 3 or Higher Adverse Event

The Kaplan-Meier estimate of the cumulative probability of infants experiencing grade 3 or higher adverse events, including events resulting in death due to any cause. (NCT03048422)
Timeframe: Birth through Week 50 postpartum

InterventionCumulative probability per 100 persons (Number)
Arms 1 and 2 Infants26.8
Arm 3 Infants30.9

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Cumulative Probability of Infant HIV-infection

The Kaplan-Meier estimate of the cumulative probability of infants acquiring HIV-1 infection from birth through 50 weeks after birth based on nucleic acid test results. (NCT03048422)
Timeframe: Birth through 50 weeks after birth

InterventionCumulative probability per 100 persons (Number)
Arm 1 Infants0.98
Arm 2 Infants0.50
Arm 3 Infants0.55

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Percentage of Mothers With HIV-1 RNA Viral Load Less Than 200 Copies/mL at Delivery

Percentage of mothers with plasma HIV-1 RNA viral load less than 200 copies/mL at delivery determined using real-time test results obtained at site laboratories. This outcome was evaluated in the non-inferiority (primary outcome) and superiority (secondary outcome) analyses. The intention-to-treat analysis included all randomized women who had viral load data available. The per-protocol analysis excluded women who modified randomized treatment (stopped, paused, switched, added any treatment) before viral load evaluation at delivery, with the exception of women who modified randomized treatment for use of a concomitant medication. (NCT03048422)
Timeframe: Delivery

,
InterventionPercentage of participants (Number)
Intention-to-Treat AnalysisPer-Protocol Analysis
Arm 3: Maternal EFV/FTC/TDF91.091.4
Arms 1 and 2: Maternal DTG+FTC/TAF and DTG+FTC/TDF97.597.5

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Infant Creatinine Clearance

Infant creatinine clearance based on Schwartz formula (NCT03048422)
Timeframe: Delivery and 26 weeks postpartum

,,
InterventionmL/min (Mean)
Delivery26 Weeks Postpartum
Arm 1 Infants52.7134.8
Arm 2 Infants53.1123.6
Arm 3 Infants49.0135.0

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Time to First HIV-1 RNA Less Than 200 Copies/mL Through Delivery

Time to first viral HIV-1 RNA less than 200 copies/mL through delivery, determined using real-time results obtained from site laboratories (NCT03048422)
Timeframe: Randomization to delivery

Interventionweeks (Mean)
Arms 1 and 2: Maternal DTG+FTC/TAF and DTG+FTC/TDF4.26
Arm 3: Maternal EFV/FTC/TDF6.49

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Percentage of Mothers With Virologic Success of HIV-1 RNA Less Than 200 Copies/mL at Delivery Based on FDA Snapshot Algorithm

Percentage of mothers with virologic success of HIV-1 RNA less than 200 copies/mL at delivery based on FDA snapshot algorithm using real-time test results obtained from site laboratories (NCT03048422)
Timeframe: Delivery

Interventionpercentage of participants (Number)
Arm 1: Maternal DTG+FTC/TAF88.9
Arm 2: Maternal DTG+FTC/TDF92.6
Arm 3: Maternal EFV/FTC/TDF81.0

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Percentage of Mothers With Virologic Success of HIV-1 RNA Less Than 200 Copies/mL at 50 Weeks Postpartum Based on FDA Snapshot Algorithm

Percentage of mothers with virologic success of HIV-1 RNA less than 200 copies/mL at 50 weeks postpartum based on FDA snapshot algorithm using real-time test results obtained from site laboratories (NCT03048422)
Timeframe: 50 weeks postpartum

Interventionpercentage of participants (Number)
Arm 1: Maternal DTG+FTC/TAF75.6
Arm 2: Maternal DTG+FTC/TDF77.7
Arm 3: Maternal EFV/FTC/TDF76.3

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Percentage of Mothers With HIV-1 RNA Less Than 50 Copies/mL at Delivery Measured at Central Laboratory

Percentage of mothers with HIV-1 RNA less than 50 copies/mL at delivery using batched test results obtained from central laboratory (NCT03048422)
Timeframe: Delivery

Interventionpercentage of participants (Number)
Arms 1 and 2: Maternal DTG+FTC/TAF and DTG+FTC/TDF94.4
Arm 3: Maternal EFV/FTC/TDF78.8

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Change in Maternal Weight Postpartum

Change in maternal postpartum weight per week based on generalized estimating equations (NCT03048422)
Timeframe: Delivery to 50 weeks postpartum

Interventionkg/week (Mean)
Arm 1: Maternal DTG+FTC/TAF0.014
Arm 2: Maternal DTG+FTC/TDF-0.008
Arm 3: Maternal EFV/FTC/TDF-0.032

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Percentage of Mothers With HIV-1 RNA Less Than 200 Copies/mL at 50 Weeks Postpartum

Percentage of mothers with HIV-1 RNA less than 200 copies/mL at 50 weeks postpartum using real-time test results obtained from site laboratories (NCT03048422)
Timeframe: 50 weeks postpartum

Interventionpercentage of participants (Number)
Arms 1 and 2: Maternal DTG+FTC/TAF and DTG+FTC/TDF96.3
Arm 3: Maternal EFV/FTC/TDF96.4

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Percentage of Mothers With HIV-1 ARV Drug Resistance Mutations at the Time of Maternal Virologic Failure

Percentage of mothers with HIV-1 antiretroviral (ARV) drug resistance mutations at the time of maternal virologic failure. Virologic failure was defined as two consecutive plasma HIV-1 RNA viral loads <200 copies/mL on or after 24 weeks on study. Drug resistance mutations were assessed using the Stanford algorithm, and all ARV regimens were assessed for mutations. (NCT03048422)
Timeframe: From 24 weeks after randomization through Week 50 postpartum

Interventionpercentage of participants (Number)
Arm 1: Maternal DTG+FTC/TAF0.92
Arm 2: Maternal DTG+FTC/TDF1.86
Arm 3: Maternal EFV/FTC/TDF6.16

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Percentage of Mother-Infant Pairs With Preterm Deliveries

Percentage of mother-infant pairs with preterm deliveries (<37 weeks gestation) resulting in live born infant (NCT03048422)
Timeframe: Delivery

Interventionpercentage of participants (Number)
Arm 1: Maternal DTG+FTC/TAF5.8
Arm 2: Maternal DTG+FTC/TDF9.4
Arm 3: Maternal EFV/FTC/TDF12.1

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Percentage of Mother-infant Pairs With an Adverse Pregnancy Outcome or Major Congenital Anomaly

Percentage of mother-infant pairs with an adverse pregnancy outcome or major congenital anomaly. Adverse pregnancy outcomes include spontaneous abortions (<20 weeks gestation), stillbirths (≥20 weeks gestation), preterm deliveries (<37 weeks gestation), and infants small for gestational age (<10th percentile per INTERGROWTH 21st Standards). Major congenital anomaly was defined consistent with the definition of malformation provided by Holmes and Westgate (i.e., a structural abnormality with surgical, medical, or cosmetic importance) and evaluated by an internal study team blinded to treatment arm. (NCT03048422)
Timeframe: Delivery through 50 weeks postpartum

Interventionpercentage of mother-infant pairs (Number)
Arm 1: Maternal DTG+FTC/TAF24.1
Arm 2: Maternal DTG+FTC/TDF32.9
Arm 3: Maternal EFV/FTC/TDF33.2

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Percentage of Mother-Infant Pairs With an Adverse Pregnancy Outcome

Percentage of mother-infant pairs with an adverse pregnancy outcome. Adverse pregnancy outcome includes spontaneous abortion (<20 weeks gestation), stillbirth (≥20 weeks gestation), preterm delivery (<37 completed weeks), or small for gestational age (<10th percentile per INTERGROWTH 21st Standards) (NCT03048422)
Timeframe: Delivery

Interventionpercentage of mother-infant pairs (Number)
Arms 1 and 2: Maternal DTG+FTC/TAF and DTG+FTC/TDF28.4
Arm 3: Maternal EFV/FTC/TDF32.7

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Percentage of Mother-infant Pairs With an Adverse Pregnancy Outcome

Percentage of mother-infant pairs with an adverse pregnancy outcome. Adverse pregnancy outcome includes spontaneous abortion (<20 weeks gestation), stillbirth (≥20 weeks gestation), preterm delivery (<37 completed weeks), or small for gestational age (<10th percentile by INTERGROWTH 21st Standards) (NCT03048422)
Timeframe: Delivery

Interventionpercentage of mother-infant pairs (Number)
Arm 1: Maternal DTG+FTC/TAF24.1
Arm 2: Maternal DTG+FTC/TDF32.9
Arm 3: Maternal EFV/FTC/TDF32.7

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Percentage of Infants Born Small for Gestational Age

Percentage of infants born small for gestational age (<10th percentile adjusted for sex assigned at birth) based on Intergrowth 21st Standards (NCT03048422)
Timeframe: Birth

Interventionpercentage of participants (Number)
Arm 1 Infants16.3
Arm 2 Infants22.5
Arm 3 Infants20.5

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Total Apparent Clearance (CL/F) for Quizartinib Following Single Dose of Quizartinib With or Without Efavirenz

Total Apparent Clearance (CL/F) is defined as total apparent clearance and was calculated using non-compartmental analysis. (NCT04459598)
Timeframe: Predose, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 144, 216, 288, 360, 432, and 504 hours post-quizartinib dose

InterventionL/h (Mean)
Efavirenz 600 mg + Quizartinib 60 mg12.210
Quizartinib 60 mg1.1849

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Area Under the Plasma Concentration-Time Curve up to the Last Quantifiable Concentration Post-Dose (AUClast) Following Single Dose of Quizartinib With or Without Efavirenz

Area Under the Plasma Concentration-Time Curve up to the Last Quantifiable Concentration Post-Dose (AUClast) is defined as AUC from time 0 to the last measurable concentration, as calculated by the linear up-log down trapezoidal method and was calculated using non-compartmental analysis. AUClast was assessed for Quizartinib and active metabolite AC886. (NCT04459598)
Timeframe: Predose, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 144, 216, 288, 360, 432, and 504 hours post-quizartinib dose

,
Interventionng*h/mL (Mean)
QuizartinibAC886
Efavirenz 600 mg + Quizartinib 60 mg2730185
Quizartinib 60 mg236004110

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Time to Maximum Plasma Concentration (Tmax) Following Single Dose of Quizartinib With or Without Efavirenz

Time of Maximum Plasma Concentration (Tmax) is defined as time of maximum observed plasma concentration and was an observed value from the study. Tmax was assessed for Quizartinib and active metabolite AC886. (NCT04459598)
Timeframe: Predose, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 144, 216, 288, 360, 432, and 504 hours post-quizartinib dose

,
Interventionhours (Median)
QuizartinibAC886
Efavirenz 600 mg + Quizartinib 60 mg2.04.0
Quizartinib 60 mg4.04.0

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Volume of Distribution in the Terminal Phase (Vz/F) for Quizartinib Following Single Dose of Quizartinib With or Without Efavirenz

Volume of Distribution in the Terminal Phase (Vz/F) is defined as volume of distribution in the terminal phase and was calculated using non-compartmental analysis. (NCT04459598)
Timeframe: Predose, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 144, 216, 288, 360, 432, and 504 hours post-quizartinib dose

InterventionL (Mean)
Efavirenz 600 mg + Quizartinib 60 mg359.9
Quizartinib 60 mg214.9

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Area Under the Plasma Concentration-Time Curve up to Infinity (AUCinf) Following Single Dose of Quizartinib With or Without Efavirenz

Area Under the Plasma Concentration-Time Curve up to Infinity (AUCinf) is defined as area under the plasma concentration-time curve from the time of dosing extrapolated to infinity and was calculated using non-compartmental analysis. AUCinf was assessed for Quizartinib and active metabolite AC886. (NCT04459598)
Timeframe: Predose, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 144, 216, 288, 360, 432, and 504 hours post-quizartinib dose

,
Interventionng*h/mL (Mean)
QuizartinibAC886
Efavirenz 600 mg + Quizartinib 60 mg2760208
Quizartinib 60 mg260004540

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Terminal Half-Life (t1/2) Following Single Dose of Quizartinib With or Without Efavirenz

Terminal Elimination Half-Life (t1/2) is defined as terminal elimination half-life and was calculated using non-compartmental analysis. AUClast was assessed for Quizartinib and active metabolite AC886. Half-life (t1/2) was assessed for Quizartinib and active metabolite AC886. (NCT04459598)
Timeframe: Predose, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 144, 216, 288, 360, 432, and 504 hours post-quizartinib dose

,
Interventionhours (Mean)
QuizartinibAC886
Efavirenz 600 mg + Quizartinib 60 mg23.811.9
Quizartinib 60 mg136135

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Metabolite to Parent Ratio (MPR) Based on Area Under the Curve for Active Metabolite AC886 Following Single Dose of Quizartinib With or Without Efavirenz

AUCinf is defined as area under the plasma concentration-time curve from the time of dosing extrapolated to infinity and AUClast is defined as AUC from time 0 to the last measurable concentration, as calculated by the linear up-log down trapezoidal method. MPR is defined as a metabolite to parent ratio with metabolite as the numerator and the parent as the denominator. MPR corrected for molecular weight of AC886 of AUCinf and AUClast are reported and were calculated using non-compartmental analysis. (NCT04459598)
Timeframe: Predose, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 144, 216, 288, 360, 432, and 504 hours post-quizartinib dose

,
Interventionratio (Mean)
MPR AUClastMPR AUCinf
Efavirenz 600 mg + Quizartinib 60 mg0.06750.0762
Quizartinib 60 mg0.1860.1880

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Number of Participants With Treatment-emergent Adverse Events Following Single Dose of Quizartinib With or Without Efavirenz

A Treatment-Emergent Adverse Events (TEAE) is defined as any event not present prior to the initiation of the drug treatment of the drug treatment or any event already present that worsens in either intensity or frequency following exposure to the drug treatment. Number of any TEAE that is related and unrelated to study medication is presented. (NCT04459598)
Timeframe: Baseline up to 30 days post last dose, up to approximately 2 months

InterventionParticipants (Count of Participants)
Efavirenz 600 mg + Quizartinib 60 mg13
Quizartinib 60 mg5

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Maximum Plasma Concentration (Cmax) Following Single Dose of Quizartinib With or Without Efavirenz

Maximum Plasma Concentration (Cmax) is defined as the maximum observed plasma concentration and was an observed value for the study. Cmax was assessed for Quizartinib and active metabolite AC886. (NCT04459598)
Timeframe: Predose, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 144, 216, 288, 360, 432, and 504 hours post-quizartinib dose

,
Interventionng/mL (Mean)
QuizartinibAC886
Efavirenz 600 mg + Quizartinib 60 mg130.011.0
Quizartinib 60 mg238.034.4

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