Page last updated: 2024-12-07

lopinavir

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Lopinavir is a protease inhibitor medication used to treat HIV infection. It works by blocking the activity of the HIV protease enzyme, which is necessary for the virus to replicate. Lopinavir is typically taken in combination with ritonavir, another protease inhibitor, which helps to increase the levels of lopinavir in the blood. Lopinavir is available as both oral and intravenous formulations. It was developed by Abbott Laboratories and approved by the Food and Drug Administration (FDA) in 1999. Lopinavir is a synthetic compound, and its chemical name is (2S)-N-[(2R)-2-hydroxy-1-(phenylmethyl)-2-(2-[[(2S)-2-(2-quinolyl)acetyl]amino]phenyl)ethyl]-3,3-dimethylbutanamide. Lopinavir is effective in treating HIV infection, and it has been shown to reduce the risk of death and AIDS-related illnesses in people living with HIV. However, lopinavir can have side effects, such as diarrhea, nausea, and vomiting. It is important to note that lopinavir is not a cure for HIV, and it is not effective in preventing HIV transmission. It is also important to note that lopinavir should only be taken under the supervision of a healthcare provider. Lopinavir has been extensively studied for its antiviral activity against HIV, and it is one of the most commonly used antiretroviral medications. Research on lopinavir has focused on its mechanism of action, pharmacokinetics, efficacy, safety, and potential resistance development. Lopinavir is an important medication for people living with HIV, and it has significantly improved the quality of life for many individuals.'

Cross-References

ID SourceID
PubMed CID92727
CHEMBL ID729
CHEBI ID31781
SCHEMBL ID21775
MeSH IDM0558541

Synonyms (123)

Synonym
a-157378.0
1(2h)-pyrimidineacetamide, n-((1s,3s,4s)-4-(((2,6-dimethylphenoxy)acetyl)amino)-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl)tetrahyrdo-alpha-1-methylethyl)-2-oxo-, (alphas)-
(1s-(1r*(r*),3r*,4r*))-n-(4-(((2,6-dimethylphenoxy)acetyl)amino)-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl)tetrahydro-alpha-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetamide
c37h48n4o5
lopinavir ,
n-{1-benzyl-4-[2-(2,6-dimethyl-phenoxy)-acetylamino]-3-hydroxy-5-phenyl-pentyl}-3-methyl-2-(2-oxo-tetrahydro-pyrimidin-1-yl)-butyramide
1(2h)-pyrimidineacetamide, n-[(1s,3s,4s)-4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-alpha-(1-methylethyl)-2-oxo-, (alphas)- (9ci)
1(2h)-pyrimidineacetamide, n-[4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-alpha-(1-methylethyl)-2-oxo-, [1s-[1r*(r*),3r*,4r*]]-
(alphas)-tetrahydro-n-((alphas)-alpha-((2s,3s)-2-hydroxy-4-phenyl-3-(2-(2,6-xylyloxy)acetamido)butyl)phenethyl)-alpha-isopropyl-2-oxo-1(2h)-pyrimidineacetamide
aids032937
1(2h)-pyrimidineacetamide, n-[(1s,3s,4s)-4-[[2-(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-alpha-(1-methylethyl)-2-oxo-, (alphas)-
koletra
abt 378
aluviran
a 157378
a 157378.0
abt-378
lpv ,
(2s)-n-[(1s,3s,4s)-1-benzyl-4-[[2-(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-pentyl]-3-methyl-2-(2-oxohexahydropyrimidin-1-yl)butanamide
rs-346
1(2h)-pyrimidineacetamide, n-[(1s,3s,4s)-4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-.alpha.-(1-methylethyl)-2-oxo-, (as)-
1MUI
DB01601
D01425
lopinavir (jan/usp/inn)
NCGC00164576-01
NCGC00164576-02
2Q5K
2O4S
2RKF
2RKG
lopinavir, (s-(2s,4s,5s))-
lopinavir-
lopinavirum
CHEMBL729
a-157378-0
chebi:31781 ,
NCGC00164576-03
dtxcid6026456
dtxsid8046456 ,
tox21_112204
cas-192725-17-0
(2s)-n-[(2r,4s,5s)-5-[[2-(2,6-dimethylphenoxy)acetyl]amino]-4-hydroxy-1,6-diphenyl-hexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
A813594
abt378
MLS004774152
lopinavir [usan:usp:inn:ban]
unii-2494g1jf75
2494g1jf75 ,
hsdb 8138
BCP9000857
lpv & aag
lopinavir & alpha1-acid glycoprotein
BCPP000184
smr002529581
MLS003915624
lopinavir [ema epar]
(1s-(1r*(r*),3r*,4r*))-n-(4-(((2,6-dimethylphenoxy)acetyl)amino)-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl)tetrahydro-.alpha.-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetamide
lopinavir [usp monograph]
lopinavir [who-ip]
lopinavir [vandf]
lopinavir [mart.]
lopinavirum [who-ip latin]
lopinavir [mi]
kaletra component lopinavir
lopinavir [usan]
lopinavir [ep monograph]
lopinavir [usp-rs]
lopinavir component of kaletra
(s)-n-((2s,4s,5s)-5-(2-(2,6-dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenylhexan-2-yl)-3-methyl-2-(2-oxotetrahydropyrimidin-1(2h)-yl)butanamide
(alphas)-tetrahydro-n-[(alphas)-alpha-[(2s,3s)-2-hydroxy-4-phenyl-3-[2-(2,6-xylyloxy)acetamido]butyl]phenethyl]-alpha-isopropyl-2-oxo-1(2h)-pyrimidineacetamide
lopinavir [jan]
lopinavir [inn]
lopinavir [orange book]
lopinavir [who-dd]
S1380
AB01274785-01
HY-14588
CS-2077
lopinavir & plga
MLS006011206
SCHEMBL21775
2QHC
tox21_112204_1
NCGC00164576-04
3OGQ
(2s)-n-((1s,3s,4s)-1-benzyl-4-{[(2,6-dimethylphenoxy)acetyl]amino}-3-hydroxy-5-phenylpentyl)-3-methyl-2-(2-oxotetrahydropyrimidin-1(2h)-yl)butanamide
KJHKTHWMRKYKJE-SUGCFTRWSA-N
AKOS025243115
(2s)-n-[(2s,4s,5s)-5-{[(2,6-dimethylphenoxy)acetyl]amino}-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxotetrahydropyrimidin-1(2h)-yl)butanamide
KS-1436
AB01274785_02
4L1A
lopinavir (abt-378)
(2s)-n-[(2s,4s,5s)-5-[2-(2,6-dimethylphenoxy)acetamido]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
J-521653
SR-01000931910-2
sr-01000931910
(alphas)-n-[(1s,3s,4s)-4-[[2-(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-alpha-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetamide
bdbm50180655
SW219767-1
abt-378; lopinavir
(2s)-n-[(1s,3s,4s)-1-benzyl-4-{[(2,6-dimethylphenoxy)acetyl]amino}-3-hydroxy-5-phenylpentyl]-3-methyl-2-(2-oxotetrahydropyrimidin-1(2h)-yl)butanamide
Q422585
EX-A4008
BRD-K99451608-001-02-4
CCG-270285
kaletra (lpv+rtv)
a-1573780
gtpl11504
lopinavir 100 microg/ml in acetonitrile
BL164636
lopinavir, bio-x
HB7108
EN300-7402887
L0377
Z2235801862
lopinavir (mart.)
lopinavir (ep monograph)
lopinavir (usp monograph)
abt-378/r
lopinavir (usp-rs)
j05ae06

Research Excerpts

Overview

Lopinavir (LPV) is a second-generation HIV protease inhibitor (PI) designed to overcome resistance development in patients undergoing long-term antiviral therapy. The drug has low aqueous solubility leading to poor oral bioavailability and thus frequent dosing.

ExcerptReferenceRelevance
"Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers (IC50 1.7 microM)."( Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein.
Greenblatt, DJ; Moltke, LL; Richert, C; Vishnuvardhan, D, 2003
)
2.48
"Lopinavir (LPV) is a second-generation HIV protease inhibitor (PI) designed to overcome resistance development in patients undergoing long-term antiviral therapy. "( Enzymatic and structural analysis of the I47A mutation contributing to the reduced susceptibility to HIV protease inhibitor lopinavir.
Brynda, J; Kagan, RM; Konvalinka, J; Kozísek, M; Lepsík, M; Machala, L; Rezácová, P; Sasková, KG; Václavíková, J, 2008
)
2
"Lopinavir (LPV) is a second generation HIV-1 protease inhibitor. "( Crystallographic study of multi-drug resistant HIV-1 protease lopinavir complex: mechanism of drug recognition and resistance.
Brunzelle, JS; Dewdney, TG; Kovari, IA; Kovari, LC; Liu, Z; Reiter, SJ; Wang, Y; Yedidi, RS, 2013
)
2.07
"Lopinavir/ritonavir is an important protease inhibitor for treating HIV-1 infection in patients aged >2 years in combination with other antiretrovirals. "( Pharmacokinetics, Safety, and Bioequivalence of 2 Lopinavir/Ritonavir (200/50 mg) Tablets in Healthy Chinese Volunteers: Effect of Food on Absorption.
Bao, D; Fu, W; Hu, W; Lin, L; Liu, Y; Zhang, Q; Zhang, W; Zheng, L, 2023
)
2.61
"Lopinavir (LPV) is an effective agent that inhibits the protease activity of coronavirus."( A systematic review of lopinavir therapy for SARS coronavirus and MERS coronavirus-A possible reference for coronavirus disease-19 treatment option.
Qian, JD; Wang, GQ; Wang, Y; Yao, TT; Zhu, WY, 2020
)
1.59
"Lopinavir is an HIV-1 protease inhibitor with low aqueous solubility leading to poor oral bioavailability and thus frequent dosing."( Central composite design-based optimization of lopinavir vitamin E-TPGS micelle: In vitro characterization and in vivo pharmacokinetic study.
Mahajan, HS; Patil, PH, 2020
)
1.54
"Lopinavir/ritonavir is a licensed antiviral treatment against HIV and has shown activity against other coronaviruses."( Efficacy of Lopinavir/Ritonavir Compared With Standard Care for Treatment of Coronavirus Disease 2019 (COVID-19): A Systematic Review.
Hariyanto, TI; Jillian Hardi, C; Kristine, E; Kurniawan, A, 2021
)
1.72
"Lopinavir-ritonavir is a repurposed drug for coronavirus disease-2019 (COVID-19). "( Efficacy and safety of lopinavir-ritonavir in COVID-19: A systematic review of randomized controlled trials.
Barvaliya, M; Bhalla, HL; Khosla, PP; Patel, PB; Patel, TK; Saurabh, MK, 2021
)
2.37
"Lopinavir/ritonavir is a potent coformulation of protease inhibitors used against HIV infection. "( Lopinavir/Ritonavir: A Review of Analytical Methodologies for the Drug Substances, Pharmaceutical Formulations and Biological Matrices.
Cabral, LM; de Sousa, VP; Pinto, EC; Velozo, CT, 2022
)
3.61
"Lopinavir is a BCS Class IV drug exhibiting poor bioavailability due to P-gp efflux and limited permeation. "( Improvement of Oral Bioavailability of Lopinavir Without Co-administration of Ritonavir Using Microspheres of Thiolated Xyloglucan.
Bhalekar, MR; Kadam, AA; Madgulkar, AR, 2018
)
2.19
"Lopinavir is a specific reversible inhibitor of the enzyme HIV protease with mean oral bioavailability of less than 20 % due to extensive hepatic metabolism by cytochrome P450 3A4. "( Formulation and in-vivo Evaluation of Novel Topical Gel of Lopinavir for Targeting HIV.
Ansari, H; Singh, P, 2018
)
2.17
"Lopinavir is a highly potent protease inhibitors commonly used in treatment of HIV infection. "( Compartmental pharmacokinetic modeling of lopinavir in humans.
Duangchaemkarn, K; Lohitnavy, M, 2013
)
2.1
"Lopinavir is an HIV protease inhibitor with high protein binding (98-99%) in human plasma. "( Determination of total and unbound concentrations of lopinavir in plasma using liquid chromatography-tandem mass spectrometry and ultrafiltration methods.
Benaboud, S; Hirt, D; Illamola, SM; Labat, L; Tréluyer, JM; Tubiana, R; Warszawski, J, 2014
)
2.09
"Lopinavir is a protease inhibitor with high specificity for HIV-1 protease formulated with ritonavir. "( Lopinavir/ritonavir: a protease inhibitor for HIV-1 treatment.
Barragan, P; Podzamczer, D, 2008
)
3.23
"Lopinavir is a protease inhibitor indicated for the treatment of HIV infection. "( Simultaneous population pharmacokinetic model for lopinavir and ritonavir in HIV-infected adults.
Barbanoj, MJ; Blanco, A; Clotet, B; Costa, J; Domingo, P; Miranda, C; Moltó, J; Negredo, E; Santos, JR; Valle, M, 2008
)
2.04
"Lopinavir/ritonavir is a common protease inhibitor (PI) used for second-line regimens in children. "( Pharmacokinetics and 48 week efficacy of low-dose lopinavir/ritonavir in HIV-infected children.
Ananworanich, J; Boonrak, P; Bunupuradah, T; Burger, D; Gorowara, M; Jupimai, T; Pancharoen, C; Phasomsap, C; Puthanakit, T; Ruxrungtham, K; van der Lugt, J, 2009
)
2.05
"Lopinavir (LPV) is a potent protease inhibitor used in combination with low doses of ritonavir in the treatment of HIV-infected patients. "( Association between ABCC2 polymorphism and lopinavir accumulation in peripheral blood mononuclear cells of HIV-infected patients.
Elens, L; Haufroid, V; Lison, D; Vandercam, B; Wallemacq, P; Yombi, JC, 2009
)
2.06
"Lopinavir is a potent protease inhibitor (PI) used for the treatment of HIV infection. "( A population analysis of weight-related differences in lopinavir pharmacokinetics and possible consequences for protease inhibitor-naive and -experienced patients.
Bouillon-Pichault, M; Chhun, S; Dupin, N; Jullien, V; Krivine, A; Launay, O; Lortholary, O; Morini, JP; Piketty, C; Pons, G; Salmon, D; Treluyer, JM; Viard, JP; Weiss, L, 2009
)
2.04
"Lopinavir-ritonavir is a human immunodeficiency virus 1 (HIV-1) protease inhibitor boosted by ritonavir, a cytochrome p450 inhibitor. "( Association of prenatal and postnatal exposure to lopinavir-ritonavir and adrenal dysfunction among uninfected infants of HIV-infected mothers.
Bavoux, F; Benhammou, V; Blanche, S; Czernichow, P; Firtion, G; Foissac, F; Kariyawasam, D; Laborde, K; Layouni, I; Le Chenadec, J; Munzer, M; Polak, M; Simon, A; Tréluyer, JM; Warszawski, J, 2011
)
2.07
"Lopinavir is a potent inducer of methadone metabolism, and treatment with L/R requires clinical monitoring and increased methadone doses in some patients, whereas ritonavir has no significant effect on methadone metabolism."( The protease inhibitor lopinavir-ritonavir may produce opiate withdrawal in methadone-maintained patients.
Friedland, G; Jatlow, P; McCance-Katz, EF; Rainey, PM, 2003
)
1.35
"Lopinavir/ritonavir is a protease inhibitor (PI) that has shown great effectiveness as salvage therapy in PI-experienced HIV-infected children."( Mutations at codons 54 and 82 of HIV protease predict virological response of HIV-infected children on salvage lopinavir/ritonavir therapy.
Angeles Muñoz-Fernández, M; Bellón, JM; Luis Jiménez, J; Martinez-Colom, A; Resino, S, 2005
)
1.98
"Lopinavir is an HIV protease inhibitor that is co-formulated with ritonavir. "( Pharmacokinetics of a once-daily regimen of lopinavir/ritonavir in HIV-1-infected children.
Burger, D; de Groot, R; van der Lee, M; Verweel, G, 2006
)
2.04
"Lopinavir-ritonavir is a preferred protease inhibitor co-formulation for initial HIV-1 treatment. "( The KLEAN study of fosamprenavir-ritonavir versus lopinavir-ritonavir, each in combination with abacavir-lamivudine, for initial treatment of HIV infection over 48 weeks: a randomised non-inferiority trial.
DeJesus, E; Eron, J; Estrada, V; Gathe, J; Katlama, C; Lackey, P; Patel, L; Shaefer, M; Staszewski, S; Sutherland-Phillips, D; Vavro, C; Wannamaker, P; Yau, L; Yeni, P; Yeo, J; Young, B, 2006
)
2.03
"Lopinavir/ritonavir is a highly cost-effective regimen relative to atazanavir for the treatment of HIV. "( Cost effectiveness of lopinavir/ritonavir compared with atazanavir in antiretroviral-naive patients: modelling the combined effects of HIV and heart disease.
Brun, S; Chumney, EC; King, MS; Luo, MP; Simpson, KN, 2007
)
2.1
"Lopinavir is a protease inhibitor (PI) for the treatment of HIV infection that was specifically designed to overcome the shortcomings of earlier agents in this class. "( Lopinavir plus ritonavir: a novel protease inhibitor combination for HIV infections.
Tan, D; Walmsley, S, 2007
)
3.23
"Lopinavir is a protease inhibitor with high specificity for HIV-1 protease. "( Lopinavir.
Faulds, D; Hurst, M, 2000
)
3.19
"Lopinavir is a new protease inhibitor that is structurally related to ritonavir. "( Lopinavir-Ritonavir: a new protease inhibitor.
Graham, KK; Mangum, EM, 2001
)
3.2
"Lopinavir/ritonavir is a fixed-dose protease inhibitor (PI) combination used for the treatment of HIV-1 infection. "( Kaletra (lopinavir/ritonavir).
Corbett, AH; Kashuba, AD; Lim, ML,
)
1.99
"Lopinavir/ritonavir is an effective option for the treatment of HIV-1-infected individuals when used in combination with other antiretroviral agents. "( Kaletra (lopinavir/ritonavir).
Corbett, AH; Kashuba, AD; Lim, ML,
)
1.99
"Lopinavir is a newly developed inhibitor of human immunodeficiency virus (HIV) protease that, when formulated with ritonavir, yields mean trough plasma lopinavir concentrations that are at least 75 times as high as that needed to inhibit replication of wild-type HIV by 50 percent."( Lopinavir-ritonavir versus nelfinavir for the initial treatment of HIV infection.
Arribas, J; Beall, G; Bernstein, B; Brun, S; Japour, A; Johnson, D; Johnson, M; King, M; Lalonde, R; Ruane, P; Sun, E; Walmsley, S, 2002
)
3.2

Effects

Lopinavir/ritonavir has been approved for once-daily dosing in antiretroviral-naive patients. The drug has shown no improvement in time to clinical improvement which is seen in our meta-analyses (P=0.1). Lopinavirs and Ritonavir have been reported to be able to induce intracellular oxidative stress in diverse cellular models.

ExcerptReferenceRelevance
"Lopinavir has the highest binding affinities to the pocket site of SARS-CoV spike glycoprotein/ACE-2 complex, cyclic AMP-dependent protein kinase A and 3-Chymotrypsin like protease while redemsivir has the highest binding affinities for vacuolar proton-translocating ATPase (V-ATPase) and papain-like proteins."( Repurposing of chloroquine and some clinically approved antiviral drugs as effective therapeutics to prevent cellular entry and replication of coronavirus.
Adebayo, AI; Adeoye, AO; Olaoye, IF; Oso, BJ; Tijjani, H, 2021
)
1.34
"Lopinavir/ritonavir has modest antiviral activity against severe acute respiratory syndrome coronavirus 2. "( Viral kinetics and factors associated with rapid viral clearance during lopinavir/ritonavir-based combination therapy in non-severe COVID-19 patients.
Chen, L; Ding, JG; Hong, L; Li, J; Sun, GQ; Sun, QF; Ye, EL; Yu, XQ; Zhang, XX, 2020
)
2.23
"Lopinavir/ritonavir has been used for the treatment of Severe Acute Respiratory Syndrome (SARS) and Middle East Respiratory Syndrome (MERS) coronavirus infections. "( Lopinavir/ritonavir for the treatment of SARS, MERS and COVID-19: a systematic review.
Einav, S; Servillo, G; Vargas, M, 2020
)
3.44
"Lopinavir-ritonavir has been proposed as a treatment for COVID-19 on the basis of in vitro activity, preclinical studies, and observational studies. "( Lopinavir-ritonavir in patients admitted to hospital with COVID-19 (RECOVERY): a randomised, controlled, open-label, platform trial.
, 2020
)
3.44
"Lopinavir-ritonavir has shown no improvement in time to clinical improvement which is seen in our meta-analyses (P=0.1)."( Repurposing of drugs for COVID-19: a systematic review and meta-analysis.
Amparore, D; Checcucci, E; Dasgupta, P; Elhage, O; Fiori, C; Kotecha, P; Light, A; Porpiglia, F, 2022
)
1.44
"Lopinavir/ritonavir has no more treatment effects than other therapeutic agents used herein in COVID-19 patients."( Lopinavir/Ritonavir for COVID-19: a Systematic Review and Meta-Analysis.
Amani, B; Hashemi, P; Khanijahani, A, 2021
)
3.51
"Lopinavir and Ritonavir have been reported to be able to induce intracellular oxidative stress in diverse cellular models, however scarce informations are available about protease inhibitor effects of in the central nervous system (CNS)."( HIV Protease Inhibitors Apoptotic Effect in SH-SY5Y Neuronal Cell Line.
Ceglia, V; Celsi, F; Crovella, S; de Oliveira Franca, RF; Pacor, S; Tricarico, PM, 2016
)
1.16
"Lopinavir/ritonavir has served as a well established benchmark comparator for the noninferiority of other ritonavir-boosted PI regimens."( Lopinavir/Ritonavir: a review of its use in the management of HIV-1 infection.
Croxtall, JD; Perry, CM, 2010
)
2.52
"Lopinavir/ritonavir has demonstrated antiviral activity in the HIV-infected adult."( Forty-eight-week evaluation of lopinavir/ritonavir, a new protease inhibitor, in human immunodeficiency virus-infected children.
Allen, U; Arpadi, S; Bernstein, B; Bertz, RJ; Cahn, P; Castrejón, MM; Chadwick, E; Deetz, CO; Gomez, P; Handelsman, E; Heuser, RS; Hsu, AF; Kempf, DJ; Pelton, S; Ramilo, O; Renz, CL; Rode, RA; Sáez-Llorens, X; Sun, E; Violari, A, 2003
)
2.05
"Lopinavir/ritonavir has demonstrated antiviral activity in the HIV-infected patient."( Positive virological outcome after lopinavir/ritonavir salvage therapy in protease inhibitor-experienced HIV-1-infected children: a prospective cohort study.
Bellón, JM; Cabrero, E; de José, MI; González, MI; Gonzalez-Rivera, M; Gurbindo, D; Mellado, MJ; Muñoz-Fernández, MA; Ramos, JT; Resino, S, 2004
)
2.04
"Lopinavir/ritonavir has recently been approved for once-daily dosing in antiretroviral-naive patients."( Lopinavir/ritonavir in the treatment of human immunodeficiency virus infection.
Hicks, CB; Kaplan, SS, 2005
)
2.49

Actions

Lopinavir induced an increase in the fluorescence of pZsProSensor-1 transfected SiHa cells, indicative of proteasomal inhibition.

ExcerptReferenceRelevance
"Lopinavir/ritonavir may increase the risk of diarrhoea and nausea and/or vomiting."( Adverse effects of remdesivir, hydroxychloroquine and lopinavir/ritonavir when used for COVID-19: systematic review and meta-analysis of randomised trials.
Agoritsas, T; Bartoszko, JJ; Brignardello-Petersen, R; Chu, DK; Ge, L; Izcovich, A; Khamis, AM; Kum, E; McLeod, SL; Mustafa, RA; Qasim, A; Rochwerg, B; Siemieniuk, RA; Vandvik, P; Zeraatkar, D, 2022
)
1.69
"Lopinavir induced an increase in the fluorescence of pZsProSensor-1 transfected SiHa cells, indicative of proteasomal inhibition. "( Lopinavir up-regulates expression of the antiviral protein ribonuclease L in human papillomavirus-positive cervical carcinoma cells.
Batman, G; Hampson, IN; Hampson, L; Oliver, AW; Richard, C; Zehbe, I, 2011
)
3.25

Treatment

Treatment with lopinavir-ritonavir (adjusted hazard ratio [aHR], 2.28; 95% confidence interval [CI], 1.24 to 4.21) and younger age was associated with negative conversion of viral RNA. LopinavIR-rit onavir treatment was stopped early in 13 patients (13.8%) because of adverse events.

ExcerptReferenceRelevance
"Lopinavir-ritonavir treatment was stopped early in 13 patients (13.8%) because of adverse events."( A Trial of Lopinavir-Ritonavir in Adults Hospitalized with Severe Covid-19.
Bai, T; Cai, Y; Cao, B; Chen, H; Chen, N; Cheng, F; Dong, C; Dong, X; Fan, G; Ge, Q; Gong, F; Gu, X; Guo, L; Hayden, FG; He, J; Horby, PW; Hu, X; Huang, C; Huang, H; Jaki, T; Jia, C; Li, C; Li, H; Li, K; Li, X; Liu, W; Liu, X; Liu, Y; Liu, Z; Lu, S; Luo, S; Pan, L; Peng, L; Qiu, F; Qu, Z; Ruan, L; Ruan, S; Shang, L; Song, B; Tu, S; Wang, C; Wang, J; Wang, K; Wang, S; Wang, Y; Wei, M; Wei, Y; Wen, D; Wu, J; Wu, X; Xia, J; Xiang, J; Xie, X; Xu, J; Yu, T; Yuan, Y; Zhan, H; Zhang, D; Zhang, L; Zhang, Y; Zhou, F; Zhou, X; Zou, J, 2020
)
1.67
"Lopinavir-cART treatment was also associated with selective depletion of uNK cells, reduced trophoblast migration and defective placentation."( Periconceptional exposure to lopinavir, but not darunavir, impairs decidualization: a potential mechanism leading to poor birth outcomes in HIV-positive pregnancies.
Acosta, S; Dunk, C; Kala, S; Serghides, L, 2020
)
1.57
"Lopinavir/ritonavir treatment resulted in an unfavourable modulation of such markers compared with atazanavir/ritonavir treatment."( Evaluation of adhesion molecules and immune parameters in HIV-infected patients treated with an atazanavir/ritonavir- compared with a lopinavir/ritonavir-based regimen.
Bandera, A; Clerici, M; Fenizia, C; Giannattasio, C; Gori, A; Maloberti, A; Masetti, M; Muscatello, A; Sabbatini, F; Soria, A; Squillace, N; Trabattoni, D, 2018
)
1.41
"The lopinavir/ritonavir-treated and interferon-β1b-treated animals had better outcome than the untreated animals, with improved clinical (mean clinical scores ↓50.9%-95.0% and ↓weight loss than the untreated animals), radiological (minimal pulmonary infiltrates), and pathological (mild bronchointerstitial pneumonia) findings, and lower mean viral loads in necropsied lung (↓0.59-1.06 log10 copies/glyceraldehyde 3-phosphate dehydrogenase [GAPDH]; P < .050) and extrapulmonary (↓0.11-1.29 log10 copies/GAPDH; P < .050 in kidney) tissues."( Treatment With Lopinavir/Ritonavir or Interferon-β1b Improves Outcome of MERS-CoV Infection in a Nonhuman Primate Model of Common Marmoset.
Bao, L; Cai, JP; Chan, JF; Chen, H; Chu, H; Deng, W; Gao, H; Jia, L; Li, F; Qin, C; Xiao, C; Yao, Y; Yeung, ML; Yu, P; Yuen, KY; Zhou, J, 2015
)
1.25
"Lopinavir treatment of erythrocytes from healthy volunteers is followed by cell shrinkage and phospholipid scrambling of the erythrocyte cell membrane, an effect in part due to stimulation of ROS formation and Ca2+ entry."( Enhanced Eryptosis Following Exposure to Lopinavir.
Abbès, S; Al Mamun Bhuyan, A; Bissinger, R; Bouguerra, G; Lang, F; Waibel, S, 2015
)
2.13
"Lopinavir/ritonavir-treated subjects demonstrating 3 consecutive monthly HIV-1 RNA levels <50 copies/mL started lopinavir/ritonavir monotherapy."( A 96-week comparison of lopinavir-ritonavir combination therapy followed by lopinavir-ritonavir monotherapy versus efavirenz combination therapy.
Arribas, JR; Bellos, NC; Bernstein, BM; Brun, SC; Cameron, DW; da Silva, BA; Gilmore, N; Hanna, GJ; King, MS; Myers, RA, 2008
)
1.37
"Lopinavir treatment for 24 h had no effect on basal Rb phosphorylation but reduced Rb phosphorylation in all four meningioma cultures."( Lopinavir inhibits meningioma cell proliferation by Akt independent mechanism.
Johnson, MD; O'Connell, M; Pilcher, W, 2011
)
2.53
"Lopinavir/ritonavir treatments drastically inhibited the growth of gingival epithelium when the drug was present throughout the growth period of the tissue. "( The HIV protease inhibitor lopinavir/ritonavir (Kaletra) alters the growth, differentiation and proliferation of primary gingival epithelium.
Alam, S; Dinello, D; Israr, M; Kishel, JJ; Meyers, C; Mitchell, D, 2011
)
2.11
"Lopinavir/ritonavir treatment was associated with a better outcome even when adjusted for baseline lactate dehydrogenase level."( Role of lopinavir/ritonavir in the treatment of SARS: initial virological and clinical findings.
Chan, KH; Chan, KS; Cheng, VC; Chu, CM; Guan, Y; Hung, IF; Kao, RY; Peiris, JS; Poon, LL; Wong, CL; Wong, MM; Yuen, KY, 2004
)
1.48
"Lopinavir/ritonavir-treated children presented lower viral loads than nelfinavir-treated children at week 4 (P=0.020) and week 24 (P<0.0001)."( Different kinetics of immunologic recovery using nelfinavir or lopinavir/ritonavir-based regimens in children with perinatal HIV-1 infection.
Chiappini, E; De Luca, M; De Martino, M; Galli, L; Miccinesi, G; Zappa, M,
)
1.09
"In lopinavir-naive, treatment-experienced patients, darunavir-ritonavir was non-inferior to lopinavir-ritonavir treatment in terms of our virological endpoint, and should therefore be considered as a treatment option for this population."( Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in treatment-experienced, HIV-infected patients in TITAN: a randomised controlled phase III trial.
Banhegyi, D; Berger, D; de Béthune, MP; De Pauw, M; Lefebvre, E; Madruga, JV; McMurchie, M; Norris, D; Ruxrungtham, K; Spinosa-Guzman, S; Suter, F; Tomaka, F; Vangeneugden, T, 2007
)
1.2
"Treatment with lopinavir-ritonavir was not associated with a difference from standard care in the time to clinical improvement (hazard ratio for clinical improvement, 1.31; 95% confidence interval [CI], 0.95 to 1.80)."( A Trial of Lopinavir-Ritonavir in Adults Hospitalized with Severe Covid-19.
Bai, T; Cai, Y; Cao, B; Chen, H; Chen, N; Cheng, F; Dong, C; Dong, X; Fan, G; Ge, Q; Gong, F; Gu, X; Guo, L; Hayden, FG; He, J; Horby, PW; Hu, X; Huang, C; Huang, H; Jaki, T; Jia, C; Li, C; Li, H; Li, K; Li, X; Liu, W; Liu, X; Liu, Y; Liu, Z; Lu, S; Luo, S; Pan, L; Peng, L; Qiu, F; Qu, Z; Ruan, L; Ruan, S; Shang, L; Song, B; Tu, S; Wang, C; Wang, J; Wang, K; Wang, S; Wang, Y; Wei, M; Wei, Y; Wen, D; Wu, J; Wu, X; Xia, J; Xiang, J; Xie, X; Xu, J; Yu, T; Yuan, Y; Zhan, H; Zhang, D; Zhang, L; Zhang, Y; Zhou, F; Zhou, X; Zou, J, 2020
)
1.29
"Treatment with lopinavir/ritonavir showed signs of autophagy."( In vitro effectivity of three approved drugs and their synergistic interaction against Leishmania infantum.
Abou-El-Naga, IF; Fawzy Hussien Mogahed, NM; Mady, RF, 2020
)
0.9
"Treatment with lopinavir-ritonavir (adjusted hazard ratio [aHR], 2.28; 95% confidence interval [CI], 1.24 to 4.21) and younger age (aHR, 2.64; 95% CI 1.43 to 4.87) was associated with negative conversion of viral RNA."( Lopinavir-ritonavir versus hydroxychloroquine for viral clearance and clinical improvement in patients with mild to moderate coronavirus disease 2019.
Choe, JY; Hong, HL; Jung, CY; Kim, EJ; Kim, JW; Kim, KC; Kwon, HH, 2021
)
2.4
"A treatment with lopinavir/ritonavir and hydroxychloroquine twice daily was started."( Clinical characteristics and management of a liver transplanted patient admitted with SARS-CoV-2 infection.
Bernasconi, E; Bertoli, R; Cerny, A; Ceschi, A; De Gottardi, A; Fratila, C; Gianella, P; Magenta, L; Majno-Hurst, P; Vanini, G, 2020
)
0.89
"Treatment of lopinavir-ritonavir combined with arbidol did not significantly accelerate main symptom improvement and promote the image absorption of pulmonary inflammation."( Lopinavir-ritonavir alone or combined with arbidol in the treatment of 73 hospitalized patients with COVID-19: A pilot retrospective study.
Lan, X; Shao, C; Wu, Z; Xu, Y; Zeng, X, 2021
)
2.42
"Treatment with lopinavir-NO induced only a transient activation of Akt and inhibition of P70S6 kinase."( Lopinavir-NO, a nitric oxide-releasing HIV protease inhibitor, suppresses the growth of melanoma cells in vitro and in vivo.
Al-Abed, Y; Basile, MS; Cavalli, E; He, M; Maksimovic-Ivanic, D; Mazzon, E; Mijatovic, S; Nicoletti, F; Paskas, S; Rakocevic, S, 2019
)
2.3
"Dual treatment with lopinavir-ritonavir plus lamivudine has non-inferior therapeutic efficacy and is similarly tolerated to triple treatment."( Dual treatment with lopinavir-ritonavir plus lamivudine versus triple treatment with lopinavir-ritonavir plus lamivudine or emtricitabine and a second nucleos(t)ide reverse transcriptase inhibitor for maintenance of HIV-1 viral suppression (OLE): a random
Arribas, JR; Cabié, A; Crespo, M; Domingo, P; Dronda, F; Estrada, V; Gatell, JM; Girard, PM; Iribarren, JA; Knobel, H; Landman, R; Mallolas, J; Martínez-Rebollar, M; Montero, M; Pich, J; Podzamczer, D; Portilla, J; Pulido, F; Weiss, L; Zamora, FX, 2015
)
1.06
"Treatment with lopinavir/ritonavir (LPV/r) monotherapy has been shown to be an effective alternative, especially in the maintenance of patients previously treated with combination therapy and prolonged virological suppression. "( [Lopinavir/ritonavir monotherapy for the treatment of HIV-1 infection: the emergence of resistance].
Delgado, R, 2008
)
1.61
"Treatment with lopinavir and ritonavir, but not amprenavir, induced ER stress, as indicated by a decrease in secreted alkaline phosphatase activities and an increase in the unfolded protein response. "( HIV protease inhibitors induce endoplasmic reticulum stress and disrupt barrier integrity in intestinal epithelial cells.
Chen, J; Chen, L; Gurley, E; Hylemon, PB; Pandak, WM; Sanyal, AJ; Studer, E; Sun, L; Wang, G; Wang, JY; Wang, X; Wu, X; Zha, W; Zhang, L; Zhou, H, 2010
)
0.71
"Treatment with lopinavir/ritonavir is significantly associated with elevated BP, an effect that appears to be mediated through an increase in BMI. "( Antiretroviral medications associated with elevated blood pressure among patients receiving highly active antiretroviral therapy.
Crane, HM; Kitahata, MM; Van Rompaey, SE, 2006
)
0.69
"The treatment with lopinavir+ritonavir caused discrete, yet significant, alterations of aspartate aminotransferase activity, blood urea nitrogen and creatinine plasma levels."( Effects of lopinavir-ritonavir combined therapy during the rat pregnancy. Morphological and biochemical aspects.
Amed, AA; Cunha, AM; Hagemann, CC; Kulay, L; Maciel, GA; Oliveira, FH; Oliveira-Filho, RM; Simões, MJ; Simões, RS; Soares, JM, 2007
)
1.05

Toxicity

Study showed a high incidence of adverse events when a higher than standard dose of the new lopinavir/ritonavir tablets was combined with rifampicin. Grade 1 or 2 gastrointestinal adverse events were higher amon. It remains unclear whether a safe and effective rifabutin dose exists for treatment of TB.

ExcerptReferenceRelevance
" Three patients discontinued therapy for drug-related adverse events."( Safety and antiviral activity at 48 weeks of lopinavir/ritonavir plus nevirapine and 2 nucleoside reverse-transcriptase inhibitors in human immunodeficiency virus type 1-infected protease inhibitor-experienced patients.
Benson, CA; Brun, SC; Deeks, SG; Eron, JJ; Feinberg, J; Gulick, RM; Hicks, C; Hsu, A; Japour, AJ; Kempf, D; Kessler, HA; King, M; Murphy, RL; Real, K; Riddler, S; Sax, PE; Stryker, R; Sun, E; Thompson, M; Wheeler, D, 2002
)
0.57
" In our clinical setting IDV/r showed to be less effective and more toxic than LPV/RTV as first-line HAART."( Lopinavir/ritonavir vs. indinavir/ritonavir in antiretroviral naive HIV-infected patients: immunovirological outcome and side effects.
Adorni, F; Bini, T; Bongiovanni, M; Chiesa, E; Cicconi, P; Monforte d'Arminio, A, 2004
)
1.77
" Discontinuation due to adverse events is infrequent."( Safety, efficacy and development of resistance under the new protease inhibitor lopinavir/ritonavir: 48-week results.
Kaiser, R; Mauss, S; Rockstroh, JK; Schmutz, G; Vogel, M; Voigt, E; Wasmuth, JC, 2004
)
0.55
" Twenty-eight patients discontinued therapy prior to week 204 because of adverse events (n = 10), lost to follow-up (n = 9), or other reasons (n = 9)."( Long-term safety and durable antiretroviral activity of lopinavir/ritonavir in treatment-naive patients: 4 year follow-up study.
Benson, C; Brun, SC; Eron, JJ; Gulick, RM; Hicks, C; Kessler, HA; King, KR; King, MS; Murphy, RL; White, AC, 2004
)
0.57
"Liver toxicity is a common side effect of antiretroviral therapy, particularly in subjects coinfected with the hepatitis C virus (HCV)."( Short communication: liver toxicity of lopinavir-containing regimens in HIV-infected patients with or without hepatitis C coinfection.
González-Lahoz, J; González-Requena, D; Jiménez-Nacher, I; Núñez, M; Soriano, V, 2004
)
0.59
" 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
" Parameters studied were HIV RNA, CD4+ cell counts, metabolic parameters and drug-related adverse events."( Predictive factors of lopinavir/ritonavir discontinuation for drug-related toxicity: results from a cohort of 416 multi-experienced HIV-infected individuals.
Bini, T; Bongiovanni, M; Chiesa, E; Cicconi, P; Di Biagio, A; Landonio, S; Meraviglia, P; Monforte, Ad; Testa, L; Tordato, F, 2005
)
0.64
"The SCOLTA project (Surveillance Cohort Long-term Toxicity Antiretrovirals) is a system for online surveying of adverse reactions to recently commercialized antiretroviral drugs and a "sentinel" for unexpected and late adverse reactions arising during any antiretroviral treatment (available at: http://www."( An Italian approach to postmarketing monitoring: preliminary results from the SCOLTA (Surveillance Cohort Long-Term Toxicity Antiretrovirals) project on the safety of lopinavir/ritonavir.
Armignacco, O; Bonfanti, P; Carradori, S; Magnani, C; Martinelli, C; Parruti, G; Quirino, T; Ricci, E, 2005
)
0.52
" Adverse events were described in 18 children."( Safety and antiviral response at 12 months of lopinavir/ritonavir therapy in human immunodeficiency virus-1-infected children experienced with three classes of antiretrovirals.
Cabrero, E; De José, MI; Dueñas, J; Fortuny, C; González-Montero, R; Mellado, MJ; Muñoz-Fernández, MA; Mur, A; Navarro, M; Otero, C; Pocheville, I; Ramos, JT, 2005
)
0.59
" Treatment was not discontinued in any patient because of adverse effects."( Atazanavir and lopinavir/ritonavir: pharmacokinetics, safety and efficacy of a promising double-boosted protease inhibitor regimen.
Azuaje, C; Crespo, M; Curran, A; Diaz, M; Feijoo, M; Lopez, RM; Ocaña, I; Pahissa, A; Pou, L; Ribera, E, 2006
)
0.69
" Subsequently, the patient developed a possible adverse skin reaction to his antiretrovirals and was hospitalized."( Carbamazepine toxicity induced by lopinavir/ritonavir and nelfinavir.
Bates, DE; Herman, RJ, 2006
)
0.61
" Together, these in vitro results indicate that combination with other antiretrovirals does not significantly increase the toxic potential of TFV in RPTECs."( In vitro cytotoxicity and mitochondrial toxicity of tenofovir alone and in combination with other antiretrovirals in human renal proximal tubule cells.
Alvarez, ML; Cihlar, T; Cordobilla, B; Domingo, JC; Domingo, P; Giralt, M; Guallar, J; López-Dupla, M; Sánchez de la Rosa, R; Saumoy, M; Torres, F; Vidal, F; Villarroya, F, 2006
)
0.33
" Safety data were generally similar between the groups; grade 3 or 4 adverse events occurred in 80 (27%) darunavir-ritonavir and 89 (30%) lopinavir-ritonavir patients."( Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in treatment-experienced, HIV-infected patients in TITAN: a randomised controlled phase III trial.
Banhegyi, D; Berger, D; de Béthune, MP; De Pauw, M; Lefebvre, E; Madruga, JV; McMurchie, M; Norris, D; Ruxrungtham, K; Spinosa-Guzman, S; Suter, F; Tomaka, F; Vangeneugden, T, 2007
)
0.78
" No statistically significant differences in adverse event incidence occurred between treatment groups, except for a higher vomiting rate in the 400/300 mg dose group."( High-dose lopinavir/ritonavir in highly treatment-experienced HIV-1 patients: efficacy, safety, and predictors of response.
Bernstein, B; Brun, SC; Eron, JJ; Flexner, C; Havlir, DV; Katlama, C; King, MS; Klein, CE; Letendre, SL; Podzamczer, D,
)
0.53
" A saquinavir C(min) > 2000 ng/ml was associated with an increased risk of gastrointestinal grade 3 or 4 adverse events and higher total cholesterol."( Pharmacokinetics of two randomized trials evaluating the safety and efficacy of indinavir, saquinavir and lopinavir in combination with low-dose ritonavir: the MaxCmin1 and 2 trials.
Cahn, P; Castagna, A; Clumeck, N; Dragsted, UB; Fox, Z; Gerstoft, J; Justesen, US; Losso, M; Lundgren, JD; Obel, N; Pedersen, C; Peters, B, 2007
)
0.55
" Three infants (14%) had transient adverse events of grade 3 or more that were possibly related to study treatment but did not require permanent treatment discontinuation."( Pharmacokinetics, safety and efficacy of lopinavir/ritonavir in infants less than 6 months of age: 24 week results.
Capparelli, EV; Chadwick, EG; Chen, J; Hughes, M; Palumbo, P; Pinto, JA; Robbins, B; Rodman, JH; Serchuck, L; Smith, E; Yogev, R, 2008
)
0.61
" Data regarding demographics, clinical disease and antiretroviral treatment history, HIV-1 RNA copies/mL, CD4 T-cell counts [absolute (cells/microL) and percentages (%)], adverse events, clinical laboratory values, reasons for discontinuation of PIs, and concomitant medications were extracted from the database for PI-naive (first-line) and PI-experienced (second- or higher-line) PI use."( Long-term safety and effectiveness of ritonavir, nelfinavir, and lopinavir/ritonavir in antiretroviral-experienced HIV-infected children.
Burri, M; Nadal, D; Rode, R; Rudin, C; Shen, Y, 2008
)
0.58
"Long-term PI-based therapy seems to be safe and to result in durable virologic and immunologic effectiveness in HIV-1-infected antiretroviral-experienced children."( Long-term safety and effectiveness of ritonavir, nelfinavir, and lopinavir/ritonavir in antiretroviral-experienced HIV-infected children.
Burri, M; Nadal, D; Rode, R; Rudin, C; Shen, Y, 2008
)
0.58
"The study showed a high incidence of adverse events when a higher than standard dose of the new lopinavir/ritonavir tablets was combined with rifampicin."( High incidence of adverse events in healthy volunteers receiving rifampicin and adjusted doses of lopinavir/ritonavir tablets.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Koopmans, PP; L'homme, RF; Nijland, HM; Rongen, GA; van Crevel, R; van Uden, P, 2008
)
0.78
" DRV/r had a lower incidence of possibly treatment-related grade 2-4 gastrointestinal-related adverse events (7 versus 14%) and treatment-related moderate-to-severe diarrhea (4 versus 10%) than LPV/r."( Efficacy and safety of once-daily darunavir/ritonavir versus lopinavir/ritonavir in treatment-naive HIV-1-infected patients at week 48.
Andrade-Villanueva, J; De Meyer, S; De Pauw, M; Dejesus, E; Fourie, J; Khanlou, H; Lefebvre, E; Ortiz, R; Spinosa-Guzman, S; van Lunzen, J; Vangeneugden, T; Voronin, E, 2008
)
0.59
" Serious adverse events were noted in 51 (12%) of 441 patients in the atazanavir/ritonavir group and in 42 (10%) of 437 patients in the lopinavir/ritonavir group."( Once-daily atazanavir/ritonavir versus twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 48 week efficacy and safety results of the CASTLE study.
Andrade-Villanueva, J; Chetchotisakd, P; Corral, J; David, N; Echevarria, J; Mancini, M; McGrath, D; Molina, JM; Moyle, G; Percival, L; Thiry, A; Yang, R, 2008
)
0.8
" Twenty-five patients (62%) experienced at least one adverse event."( Three-year outcome data of second-line antiretroviral therapy in Ugandan adults: good virological response but high rate of toxicity.
Bates, M; Castelnuovo, B; Colebunders, R; John, L; Kamya, MR; Lutwama, F; Ronald, A; Spacek, LA,
)
0.13
" In the studies performed to date, darunavir has been well tolerated, with a better profile than that of the PIs used in control groups in terms of adverse effects such as diarrhea, gastrointestinal tolerability and lipid alterations."( [Safety and tolerability of darunavir].
Antela López, A, 2008
)
0.35
" Common clinical adverse events (AEs) were diarrhoea, nausea, fatigue and headache."( Antiviral activity and safety of aplaviroc, a CCR5 antagonist, in combination with lopinavir/ritonavir in HIV-infected, therapy-naïve patients: results of the EPIC study (CCR100136).
Adkison, KK; Berger, D; Bonny, T; Cimoch, P; Lamarca, A; Lazzarin, A; Madison, SJ; McCarty, D; Millard, J; Nichols, WG; Salvato, P; Smaill, FM; Teofilo, E; Yeni, P, 2009
)
0.58
" Adverse events were limited to transient grade 3 neutropenia in 3 subjects."( Early initiation of lopinavir/ritonavir in infants less than 6 weeks of age: pharmacokinetics and 24-week safety and efficacy.
Alvero, CG; Browning, R; Capparelli, E; Chadwick, EG; Hazra, R; Heckman, BE; Hughes, MD; Luzuriaga, K; Palumbo, P; Pinto, J; Purdue, L; Robbins, B; Rodman, J; Serchuck, L; Yogev, R, 2009
)
0.68
" Rates of discontinuation and adverse events, including diarrhea, were similar between arms."( A once-daily lopinavir/ritonavir-based regimen is noninferior to twice-daily dosing and results in similar safety and tolerability in antiretroviral-naive subjects through 48 weeks.
Bernstein, B; Cohen, DE; da Silva, BA; Fredrick, L; Gathe, J; Gibbs, S; Loutfy, MR; Marsh, T; Naylor, C; Podzamczer, D; Rubio, R, 2009
)
0.72
" Adverse event rate leading to study drug discontinuation was 5% in both arms."( Efficacy and safety of switching from boosted lopinavir to boosted atazanavir in patients with virological suppression receiving a LPV/r-containing HAART: the ATAZIP study.
Aranda, M; Arranz, JA; Blanco, JL; Clotet, B; Cosin, J; Cruceta, A; Dalmau, D; Domingo, P; Ferrer, E; García, I; Gatell, JM; Gutiérrez, F; Knobel, H; Lazzari, Ed; Llibre, JM; Mallolas, J; Martínez, E; Milinkovic, A; Murillas, J; Pedrol, E; Pich, J; Podzamczer, D; Ribera, E; Roca, V; Vidal, F, 2009
)
0.61
"Double-boosted SQV+LPV/r was an effective and safe alternative for a second-line regimen in children."( Safety and efficacy of a double-boosted protease inhibitor combination, saquinavir and lopinavir/ritonavir, in pretreated children at 96 weeks.
Ananworanich, J; Boonrak, P; Bunupuradah, T; Burger, D; Engchanil, C; Kosalaraksa, P; Lumbiganon, P; Mahanontharit, A; Mengthaisong, T; Puthanakit, T; Ruxrungtham, K; Tompkins, E; van der Lugt, J, 2009
)
0.58
"Primary endpoints were time to virologic failure (confirmed HIV-1 RNA > or = 1,000 copies/mL at 16-24 weeks or > or = 200 copies/mL at > or = 24 weeks) and time to first grade 3 or 4 adverse event or laboratory abnormality that was at least one grade higher than at baseline."( Virologic response and safety of the abacavir/lamivudine fixed-dose formulation as part of highly active antiretroviral therapy: analyses of six clinical studies.
Dix, LP; Ha, B; Liao, QM; Pappa, KA,
)
0.13
" Few subjects treated with ABC/3TC developed grade 3 or 4 adverse events, laboratory toxicities, or changes in lipid levels."( Virologic response and safety of the abacavir/lamivudine fixed-dose formulation as part of highly active antiretroviral therapy: analyses of six clinical studies.
Dix, LP; Ha, B; Liao, QM; Pappa, KA,
)
0.13
" Diarrhea was the most frequently reported adverse event."( Long-term efficacy and safety of fosamprenavir plus ritonavir versus lopinavir/ritonavir in combination with abacavir/lamivudine over 144 weeks.
Baril, JG; Duiculescu, D; Estrada, V; Lim, ML; Logue, K; Pharo, C; Plettenberg, A; Pulido, F; Schewe, K; Vavro, C; Yau, L,
)
0.37
" Treatment-related gastrointestinal adverse events were greater in patients taking lopinavir/ritonavir."( Once-daily atazanavir/ritonavir compared with twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 96-week efficacy and safety results of the CASTLE study.
Absalon, J; Andrade-Villanueva, J; Chetchotisakd, P; Corral, J; David, N; Echevarria, J; Lataillade, M; Mancini, M; McGrath, D; Molina, JM; Moyle, G; Percival, L; Wirtz, V; Yang, R, 2010
)
0.83
" Atazanavir/ritonavir had a better lipid profile and fewer gastrointestinal adverse events than lopinavir/ritonavir."( Once-daily atazanavir/ritonavir compared with twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 96-week efficacy and safety results of the CASTLE study.
Absalon, J; Andrade-Villanueva, J; Chetchotisakd, P; Corral, J; David, N; Echevarria, J; Lataillade, M; Mancini, M; McGrath, D; Molina, JM; Moyle, G; Percival, L; Wirtz, V; Yang, R, 2010
)
0.82
" The occurrence of treatment-related moderate/severe adverse events was comparable for all events except nausea, which was reported more frequently among BID-treated subjects."( Similar safety and efficacy of once- and twice-daily lopinavir/ritonavir tablets in treatment-experienced HIV-1-infected subjects at 48 weeks.
Andrade-Villanueva, J; Badal-Faesen, S; Bernstein, BM; Fredrick, LM; Gathe, J; Gaultier, IA; Mingrone, H; Podsadecki, TJ; Woodward, WC; Zajdenverg, R, 2010
)
0.61
"Long-term treatment with LPV/r-based cART is safe and effective in HIV-1-infected children."( Long-term safety and effectiveness of lopinavir/ritonavir in antiretroviral-experienced HIV-1-infected children.
Bucher, HC; Nadal, D; Rickenbach, M; Rudin, C; Wolbers, M, 2010
)
0.63
" Through 96 weeks, 77 subjects from each group discontinued prematurely; adverse or HIV-related events contributed to discontinuation of 36 subjects overall, with no significant differences between treatment groups."( Short communication: Comparable safety and efficacy with once-daily versus twice-daily dosing of lopinavir/ritonavir tablets with emtricitabine + tenofovir DF in antiretroviral-naïve, HIV type 1-infected subjects: 96 week final results of the randomized t
Bernstein, B; Cohen, D; da Silva, B; Fredrick, L; González-García, J; Johnson, M; Naylor, C; Sloan, L, 2010
)
0.58
" Safety was assessed with the incidence of treatment-emergent adverse events (AE)."( Pilot, randomized study assessing safety, tolerability and efficacy of simplified LPV/r maintenance therapy in HIV patients on the 1 PI-based regimen.
Ackad, N; Andrade-Villanueva, J; Bortolozzi, R; Cahn, P; Casiró, AD; Cassetti, I; Junod, P; Krolewiecki, A; Longo, N; Lupo, SH; Montaner, J; Patterson, P; Rampakakis, E; Sampalis, JS; Sierra-Madero, J, 2011
)
0.37
" Three patients allocated elvitegravir had serious adverse events related to study drugs compared with seven assigned raltegravir; two and eight patients died, respectively."( Efficacy and safety of once daily elvitegravir versus twice daily raltegravir in treatment-experienced patients with HIV-1 receiving a ritonavir-boosted protease inhibitor: randomised, double-blind, phase 3, non-inferiority study.
Andrade-Villanueva, J; Cheng, AK; Chuck, SL; Clotet, B; Clumeck, N; Lamarca, A; Liu, YP; Margot, N; Molina, JM; Zhong, L, 2012
)
0.38
" The occurrence of treatment-related, moderate/severe adverse events was similar between treatment groups through 48 weeks of treatment."( Examination of noninferiority, safety, and tolerability of lopinavir/ritonavir and raltegravir compared with lopinavir/ritonavir and tenofovir/ emtricitabine in antiretroviral-naïve subjects: the progress study, 48-week results.
Fredrick, LM; Gathe, J; Lawal, A; Nilius, AM; Podsadecki, TJ; Pulido, F; Reynes, J; Soto-Malave, R; Tian, M,
)
0.37
" There were no serious adverse events (AEs) in either arm."( A switch in therapy to a reverse transcriptase inhibitor sparing combination of lopinavir/ritonavir and raltegravir in virologically suppressed HIV-infected patients: a pilot randomized trial to assess efficacy and safety profile: the KITE study.
Del Rio, C; Easley, KA; Eaton, ME; Lennox, JL; Ofotokun, I; Sanford, SE; Shenvi, N; Sheth, AN; White, K, 2012
)
0.61
" None of 9 severe adverse events were LPV/r- or liver-related."( A pilot, prospective, open-label simplification study to evaluate the safety, efficacy, and pharmacokinetics of once-daily lopinavir-ritonavir monotherapy in HIV-HCV coinfected patients: the MONOCO study.
Ackad, N; Conway, B; Cooper, C; la Porte, C; Sampalis, J; Tossonian, H,
)
0.34
"Once-daily LPV/r monotherapy in HIV-HCV coinfected individuals offers a safe and effective approach to the management of the HIV infection, with a predictable pharmacokinetic profile."( A pilot, prospective, open-label simplification study to evaluate the safety, efficacy, and pharmacokinetics of once-daily lopinavir-ritonavir monotherapy in HIV-HCV coinfected patients: the MONOCO study.
Ackad, N; Conway, B; Cooper, C; la Porte, C; Sampalis, J; Tossonian, H,
)
0.34
" Four grade 3 and no grade 4 adverse events were reported."( Pharmacokinetics and 48-week safety and efficacy of generic lopinavir/ritonavir in Thai HIV-infected patients.
Ananworanich, J; Avihingsanon, A; Burger, DM; Gorowara, M; Lange, JM; Phanuphak, P; Ramautarsing, RA; Ruxthungtham, K; Sophonphan, J; van der Lugt, J, 2013
)
0.63
" Significantly fewer discontinuations because of adverse events were observed with DRV/r (4."( Final 192-week efficacy and safety of once-daily darunavir/ritonavir compared with lopinavir/ritonavir in HIV-1-infected treatment-naïve patients in the ARTEMIS trial.
DeJesus, E; Khanlou, H; Lathouwers, E; Lefebvre, E; Opsomer, M; Orkin, C; Stoehr, A; Supparatpinyo, K; Tomaka, F; Van de Casteele, T, 2013
)
0.61
" Efficacy (HIV-1 RNA levels, CD4+ T-cell counts) and safety and tolerability (treatment discontinuation, treatment-related adverse events [AE], and clinical laboratory abnormalities) at 48 weeks were assessed for total women, women by age (≥50, <50 years) and body mass index (BMI; <25, ≥25 to <30, ≥30 kg/m2), and sex."( Meta-analysis of the safety, tolerability, and efficacy of lopinavir/ritonavir-containing antiretroviral therapy in HIV-1-infected women.
Fredrick, L; Hermes, A; Martinez, M; Norton, M; Pasley, M; Squires, K; Trinh, R,
)
0.37
"2% receiving the increased dose, discontinued treatment because of adverse events (p=0."( A randomized controlled trial to assess safety, tolerability, and antepartum viral load with increased lopinavir/ritonavir dosage in pregnancy.
Bonafe, SM; Castelo, A; Costa, DA; Machado, RH; Pott-Junior, H; Senise, JF; Vaz, MJ, 2013
)
0.6
" Both ACT regimens were safe and well tolerated."( Artemisinin-based combination therapies are efficacious and safe for treatment of uncomplicated malaria in HIV-infected Ugandan children.
Achan, J; Arinaitwe, E; Charlebois, E; Clark, TD; Dorsey, G; Havlir, D; Ikilezi, G; Kakuru, A; Kamya, MR; Muhindo, MK; Mwangwa, F; Rosenthal, PJ; Ruel, T; Tappero, JW, 2014
)
0.4
"Treatment of uncomplicated malaria with AL or DP was efficacious and safe in HIV-infected children taking ART."( Artemisinin-based combination therapies are efficacious and safe for treatment of uncomplicated malaria in HIV-infected Ugandan children.
Achan, J; Arinaitwe, E; Charlebois, E; Clark, TD; Dorsey, G; Havlir, D; Ikilezi, G; Kakuru, A; Kamya, MR; Muhindo, MK; Mwangwa, F; Rosenthal, PJ; Ruel, T; Tappero, JW, 2014
)
0.4
"Protease inhibitor (PI) monotherapy for treatment could avoid the adverse events, drug resistance, and additional costs associated with other antiretrovirals that are normally used, particularly the nucleoside analogues."( Is there a higher risk of CNS adverse events for PI monotherapy versus triple therapy? A review of results from randomized clinical trials.
Hill, A; Moecklinghoff, C; Powderly, W,
)
0.13
"There was no clear difference in the risk of central nervous system (CNS) adverse events between PI monotherapy (either DRV/r or LPV/r) and standard triple drug treatment."( Is there a higher risk of CNS adverse events for PI monotherapy versus triple therapy? A review of results from randomized clinical trials.
Hill, A; Moecklinghoff, C; Powderly, W,
)
0.13
" However, the information on CNS adverse events has not been reported using standardized definitions in the studies."( Is there a higher risk of CNS adverse events for PI monotherapy versus triple therapy? A review of results from randomized clinical trials.
Hill, A; Moecklinghoff, C; Powderly, W,
)
0.13
"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
)
0.61
"The most frequent clinical side effect was fatigue (in 23 cases, 88."( Side effects and tolerability of post-exposure prophylaxis with zidovudine, lamivudine, and lopinavir/ritonavir: a comparative study with HIV/AIDS patients.
Cai, J; Xiao, J; Zhang, Q, 2014
)
0.62
" Bayesian fixed-effect network meta-analysis models adjusting for the type of nucleoside reverse transcriptase inhibitor backbone (tenofovir disoproxil fumarate/emtricitabine [TDF/FTC] or abacavir/lamivudine [ABC/3TC]) were used to evaluate week 48 efficacy (HIV-RNA suppression to <50 copies/mL and change in CD4+ cells/µL) and safety (lipid changes, adverse events, and discontinuations due to adverse events) of DTG relative to all other treatments."( 48-week efficacy and safety of dolutegravir relative to commonly used third agents in treatment-naive HIV-1-infected patients: a systematic review and network meta-analysis.
Camejo, RR; Cuffe, R; Gilchrist, KA; Lim, JW; Nichols, G; Patel, DA; Pulgar, S; Snedecor, SJ; Stephens, J; Sudharshan, L; Tang, WY, 2014
)
0.4
" Dolutegravir had better or equivalent changes in total cholesterol, LDL, triglycerides, and lower odds of adverse events and discontinuation due to adverse events compared to all treatments."( 48-week efficacy and safety of dolutegravir relative to commonly used third agents in treatment-naive HIV-1-infected patients: a systematic review and network meta-analysis.
Camejo, RR; Cuffe, R; Gilchrist, KA; Lim, JW; Nichols, G; Patel, DA; Pulgar, S; Snedecor, SJ; Stephens, J; Sudharshan, L; Tang, WY, 2014
)
0.4
" The Division of AIDS 2004, clarification 2009, table for grading severity of adverse events was used to classify drug toxicities."( Pharmacokinetics and safety of rifabutin in young HIV-infected children receiving rifabutin and lopinavir/ritonavir.
Gous, H; Kellermann, T; Kindra, G; McIlleron, H; Moultrie, H; Sawry, S; Van Rie, A; Wiesner, L, 2015
)
0.64
" It remains unclear whether a safe and effective rifabutin dose exists for treatment of TB in children receiving lopinavir/ritonavir."( Pharmacokinetics and safety of rifabutin in young HIV-infected children receiving rifabutin and lopinavir/ritonavir.
Gous, H; Kellermann, T; Kindra, G; McIlleron, H; Moultrie, H; Sawry, S; Van Rie, A; Wiesner, L, 2015
)
0.85
" 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
)
0.96
" 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
"0% discontinued treatment due to adverse events."( Short Communication: Efficacy and Safety of Treatment Simplification to Lopinavir/Ritonavir or Darunavir/Ritonavir Monotherapy: A Randomized Clinical Trial.
Bravo, I; Cañadas, MP; Clotet, B; García-Rosado, D; Llibre, JM; Moltó, J; Paredes, R; Pérez-Álvarez, N; Santos, JR, 2016
)
0.67
" To investigate safety, we compared adverse events (AE) among infants exposed to different maternal cART regimens."( Maternal Lopinavir/Ritonavir Is Associated with Fewer Adverse Events in Infants than Nelfinavir or Atazanavir.
Barr, E; Davies, J; Forster, JE; Kinzie, K; Levin, MJ; McFarland, EJ; Pappas, J; Paul, S; Smith, C; Weinberg, A, 2016
)
0.85
" Outcomes of interest were viral suppression, mortality, AIDS-defining illnesses or WHO stage 3-4 disease, discontinuations, discontinuations due to adverse events, and serious adverse events."( Comparative efficacy and safety of second-line antiretroviral therapy for treatment of HIV/AIDS: a systematic review and network meta-analysis.
Ayers, D; Calmy, A; Chan, K; Cooper, DA; Doherty, M; Ford, N; Kanters, S; Mills, EJ; Nsanzimana, S; Paton, NI; Popoff, E; Socias, ME; Vitoria, M; Wiens, MO, 2017
)
0.46
" Secondary endpoints included treatment adherence, patient satisfaction, incidence of adverse events and differences in plasma HIV-1 RNA viral load (VL) and CD4 cell counts."( High quality of life, treatment tolerability, safety and efficacy in HIV patients switching from triple therapy to lopinavir/ritonavir monotherapy: A randomized clinical trial.
Aguirrebengoa, K; de Jesus, SE; de Los Santos, I; Fariñas, MC; Flores, J; Galindo, MJ; García-Mercé, I; García-Vallecillos, C; Hernández-Quero, J; Hidalgo-Tenorio, C; Imaz, A; Lozano, F; Montes, ML; Orihuela, F; Pasquau, J; Ríos-Villegas, MJ; Romero-Palacios, A; Sanjoaquín, I; Vázquez, P; Vergas, J, 2018
)
0.69
" There were also no differences in the incidence and severity of adverse events, even though 22."( High quality of life, treatment tolerability, safety and efficacy in HIV patients switching from triple therapy to lopinavir/ritonavir monotherapy: A randomized clinical trial.
Aguirrebengoa, K; de Jesus, SE; de Los Santos, I; Fariñas, MC; Flores, J; Galindo, MJ; García-Mercé, I; García-Vallecillos, C; Hernández-Quero, J; Hidalgo-Tenorio, C; Imaz, A; Lozano, F; Montes, ML; Orihuela, F; Pasquau, J; Ríos-Villegas, MJ; Romero-Palacios, A; Sanjoaquín, I; Vázquez, P; Vergas, J, 2018
)
0.69
" Adverse events (grade 1-4) were more common at baseline (27%) than during rifabutin treatment (15%) (P = 0."( Safety and efficacy of rifabutin among HIV/TB-coinfected children on lopinavir/ritonavir-based ART.
Akanmu, S; Brown, B; Chang, C; Darin, KM; David, N; Kanki, PJ; Ogunbosi, B; Okonkwo, P; Oladokun, R; Olaitan, O; Rawizza, HE; Scarsi, KK, 2019
)
0.75
"With clinical and laboratory monitoring, our data suggest that rifabutin is a safe option for TB therapy among children on PI-based ART."( Safety and efficacy of rifabutin among HIV/TB-coinfected children on lopinavir/ritonavir-based ART.
Akanmu, S; Brown, B; Chang, C; Darin, KM; David, N; Kanki, PJ; Ogunbosi, B; Okonkwo, P; Oladokun, R; Olaitan, O; Rawizza, HE; Scarsi, KK, 2019
)
0.75
" 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
" Secondary outcomes were duration of hospital stay, length of intensive care unit stay, 28-day mortality, effect of early or late administration of IFN on mortality, adverse effects, and complications during the hospitalization."( A Randomized Clinical Trial of the Efficacy and Safety of Interferon β-1a in Treatment of Severe COVID-19.
Abbasian, L; Davoudi-Monfared, E; Hajiabdolbaghi, M; Kazemzadeh, H; Khalili, H; Rahmani, H; Salehi, M; Yekaninejad, MS, 2020
)
0.56
"3%) in the arbidol group experienced adverse events during the follow-up period."( Efficacy and Safety of Lopinavir/Ritonavir or Arbidol in Adult Patients with Mild/Moderate COVID-19: An Exploratory Randomized Controlled Trial.
Cai, W; Chen, X; Deng, X; Guan, Y; Hong, W; Hu, F; Li, F; Li, L; Li, Y; Lin, W; Liu, J; Mo, X; Peng, P; Wang, J; Wang, Y; Wen, C; Xiao, G; Xie, Z; Zhang, F; Zhang, L, 2020
)
0.87
" 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
)
0.83
"To find effective and safe treatments for COVID-19, the WHO recommended to systemically evaluate experimental therapeutics in collaborative randomised clinical trials."( Protocol for the DisCoVeRy trial: multicentre, adaptive, randomised trial of the safety and efficacy of treatments for COVID-19 in hospitalised adults.
Ader, F, 2020
)
0.56
" In this context, intensive pharmacovigilance allows early detection of adverse events, and thereby infer the safety profile of the indication."( [Adverse effects of lopinavir/ritonavir in critically ill patients with COVID-19].
Carboni Bisso, I; Catanzariti, A; Las Heras, M; Vecchio, G; Zapico, V, 2020
)
0.88
" Its empirical use has been associated with multiple cardiac adverse reactions pertaining to its ancillary multi-channel blocking properties, vaguely characterized until now."( Spontaneous reported cardiotoxicity induced by lopinavir/ritonavir in COVID-19. An alleged past-resolved problem.
Drici, MD; Fresse, A; Gérard, A; Lepelley, M; Rocher, F; Romani, S; Salem, JE; Viard, D, 2021
)
0.88
" Regarding adverse effects, except occurrence of diarrhea (higher in the L/R group), safety was comparable to SOC."( Safety and efficacy of lopinavir/ritonavir combination in COVID-19: A systematic review, meta-analysis, and meta-regression analysis.
Avti, P; Bansal, S; Bhattacharyya, A; Hazarika, M; Kaur, H; Kumar, S; Mahendru, D; Medhi, B; Prajapat, M; Prakash, A; Sarma, P; Sharma, S; Shekhar, N,
)
0.44
" Secondary Endpoints: All causes mortality, Frequency of respiratory progression (defined as SPO2≤ 94% on room air or PaO2/FiO2 <300mmHg and requirement for supplemental oxygen or more advanced ventilator support), time to defervescence (in those with fever at enrolment), frequency of requirement for supplemental oxygen or non-invasive ventilation, frequency of requirement for mechanical ventilation, frequency of serious adverse events as per DAIDS table grade of severity."( Safety and efficacy of antiviral combination therapy in symptomatic patients of Covid-19 infection - a randomised controlled trial (SEV-COVID Trial): A structured summary of a study protocol for a randomized controlled trial.
Bahurupi, YA; Bandyopadhyay, A; Chikara, G; Moirangthem, B; Panda, PK; Saha, S; Singh, BC, 2020
)
0.56
"Lopinavir plasma concentrations in patients with moderate-to-severe COVID-19 were higher than expected, and they were associated with the occurrence of hepatic or gastrointestinal adverse drug reactions."( Plasma Concentrations and Safety of Lopinavir/Ritonavir in COVID-19 Patients.
Azoulay, C; Batista, R; Benaboud, S; Boujaafar, S; Canouï, E; Carlier, N; Chouchana, L; Gana, I; Kernéis, S; Legendre, P; Preta, LH; Regard, L; Terrier, B; Treluyer, JM; Zerbit, J; Zheng, Y, 2021
)
2.34
" The secondary outcome is the incidence of serious adverse drug reactions within seven days of randomization."( The efficacy and safety of Ivermectin in patients with mild and moderate COVID-19: A structured summary of a study protocol for a randomized controlled trial.
Dadvand, H; Davoodian, P; Fathalipour, M; Ghazizadeh, S; Hassaniazad, M; Hassanipour, S; Hosseini, FS; Kahoori, S; Malektojari, A; Nikoofal-Sahlabadi, S; Nikpoor, AR; Sepandi, M, 2021
)
0.62
" Grade ≥3 adverse events were compared between cohorts."( Pharmacokinetics and Safety of Zidovudine, Lamivudine, and Lopinavir/Ritonavir in HIV-infected Children With Severe Acute Malnutrition in Sub-Saharan Africa: IMPAACT Protocol P1092.
Aweeka, F; Bradford, S; Browning, R; Coletti, A; Costello, D; Graham, B; Hughes, E; Kamthunzi, P; Kawalazira, R; Mmbaga, BT; Moye, J; Musoke, P; Nathoo, K; Norman, J; Owor, M; Purdue, L; Reding, C; Tierney, C; Whalen, ME; Wiesner, L; Ziemba, L, 2021
)
0.86
"For children with mild COVID-19, LPR is inferior to conventional treatment in reducing virus shedding time and hospitalization duration and is associated with increased adverse reactions."( Safety and efficacy of oral lopinavir/ritonavir in pediatric patients with coronavirus disease: a nationwide comparative analysis.
Chen, RJ; Cui, YX; He, YL; Li, XY; Li, ZP; Lu, JM; Ma, SL; Shang, FN; Wang, XF; Xu, H; Ye, QF; Zhai, XW; Zhang, XB; Zhou, AF, 2021
)
0.92
" The scientific community is studying and testing numerous compounds that can be effective and safe for treating people with covid-19."( [The praise of uncertainty: a systematic living review to evaluate the efficacy and safety of drug treatments for patients with covid-19.]
Amato, L; Cruciani, F; Davoli, M; De Crescenzo, F; Mitrova, Z; Saulle, R; Vecchi, S, 2021
)
0.62
" No differences for the risk of any adverse events are observed between convalescent plasma and remdesivir compared to standard treatment."( [The praise of uncertainty: a systematic living review to evaluate the efficacy and safety of drug treatments for patients with covid-19.]
Amato, L; Cruciani, F; Davoli, M; De Crescenzo, F; Mitrova, Z; Saulle, R; Vecchi, S, 2021
)
0.62
"08) or incidence of adverse events (P=0."( Comprehensive evaluation of the efficacy and safety of LPV/r drugs in the treatment of SARS and MERS to provide potential treatment options for COVID-19.
Li, X; Liu, J; Luo, R; Wu, D; Wu, L; Xu, P; Zheng, Y, 2021
)
0.62
" The virological cure, radiological improvement and adverse events were pooled as risk ratio (RR) with 95% CI."( Efficacy and safety of lopinavir-ritonavir in COVID-19: A systematic review of randomized controlled trials.
Barvaliya, M; Bhalla, HL; Khosla, PP; Patel, PB; Patel, TK; Saurabh, MK, 2021
)
0.93
" Methods We conducted a disproportionality analysis of US Food and Drug Administration Adverse Event Reporting System (FAERS) between 2020Q1 and 2021Q1 to evaluate the association between lopinavir-ritonavir and risk of drug-induced liver injury (or severe drug-induced liver injury) and calculated their reporting odds ratios (RORs) with 95% confidence intervals (CIs)."( Drug-induced liver injury associated with lopinavir-ritonavir in patients with COVID-19: a disproportionality analysis of U.S. food and drug administration adverse event reporting system (FAERS) data.
Barnes, EL; Kinlaw, AC; Li, X; Moon, AM; Tang, H; Wang, T; Yang, JY; Zhou, L, 2021
)
1.08
" No adverse events were related to study drugs."( Pharmacokinetics and Safety of the Abacavir/Lamivudine/Lopinavir/Ritonavir Fixed-Dose Granule Formulation (4-in-1) in Neonates: PETITE Study.
Andrieux-Meyer, I; Bekker, A; Capparelli, E; Cotton, MF; Cressey, R; Cressey, TR; du Toit, S; Groenewald, M; Kumar, M; Lallemant, M; Nielsen, J; Rabie, H; Salvadori, N; Than-In-At, K, 2022
)
0.97
" In addition to the ongoing research and development of vaccines, there is still a dire need for safe and effective drugs for the control and treatment against the SARS-CoV-2 virus infection."( Safety profile of COVID-19 drugs in a real clinical setting.
Bhardwaj, M; Chiu, MN; Sah, SP, 2022
)
0.72
"Through a literature search conducted on PubMed and Google Scholar database, various adverse events suspected to be induced by eight drugs, including dexamethasone, hydroxychloroquine, chloroquine, remdesivir, favipiravir, lopinavir/ritonavir, ivermectin, and tocilizumab, administered in COVID-19 patients in clinical practice and studies were identified in 30 case reports, 3 case series, and 10 randomized clinical trials."( Safety profile of COVID-19 drugs in a real clinical setting.
Bhardwaj, M; Chiu, MN; Sah, SP, 2022
)
0.91
"Mild, moderate, or severe adverse events of numerous repurposed and investigational drugs caused by various factors and mechanisms were observed."( Safety profile of COVID-19 drugs in a real clinical setting.
Bhardwaj, M; Chiu, MN; Sah, SP, 2022
)
0.72
"To summarise specific adverse effects of remdesivir, hydroxychloroquine and lopinavir/ritonavir in patients with COVID-19."( Adverse effects of remdesivir, hydroxychloroquine and lopinavir/ritonavir when used for COVID-19: systematic review and meta-analysis of randomised trials.
Agoritsas, T; Bartoszko, JJ; Brignardello-Petersen, R; Chu, DK; Ge, L; Izcovich, A; Khamis, AM; Kum, E; McLeod, SL; Mustafa, RA; Qasim, A; Rochwerg, B; Siemieniuk, RA; Vandvik, P; Zeraatkar, D, 2022
)
1.2
" For most interventions and outcomes the certainty of the evidence was very low to low except for gastrointestinal adverse effects from hydroxychloroquine, which was moderate certainty."( Adverse effects of remdesivir, hydroxychloroquine and lopinavir/ritonavir when used for COVID-19: systematic review and meta-analysis of randomised trials.
Agoritsas, T; Bartoszko, JJ; Brignardello-Petersen, R; Chu, DK; Ge, L; Izcovich, A; Khamis, AM; Kum, E; McLeod, SL; Mustafa, RA; Qasim, A; Rochwerg, B; Siemieniuk, RA; Vandvik, P; Zeraatkar, D, 2022
)
0.97
" ICU admission, length of stay (LOS) in hospital, in-hospital mortality, and the incidence of adverse events were also measured."( Efficacy and safety of favipiravir plus interferon-beta versus lopinavir/ritonavir plus interferon-beta in moderately ill patients with COVID-19: A randomized clinical trial.
Bazram, A; Farshidi, H; Fathalipour, M; Gharibzadeh, A; Hassaniazad, M; Khalili, E; Noormandi, A, 2022
)
0.96
" The primary endpoints here considered were any adverse events observed or reported during the treatment cycle with estimates of odds ratio (OR) and 95% confidence interval (CI), until November 6, 2021."( A systematic review and Bayesian network meta-analysis for comparative safety assessment of favipiravir interventions in hospitalized COVID-19 patients.
Chen, M; Dai, W; Yang, F; Yang, K; Zeng, J, 2022
)
0.72
" We extracted data on trials and patient characteristics, and the following primary outcomes: all-cause mortality (ACM), and treatment-emergent adverse events (TEAEs)."( Comparative efficacy and safety of pharmacological interventions for severe COVID-19 patients: An updated network meta-analysis of 48 randomized controlled trials.
Chen, J; Cheng, Q; Fang, Z; Jia, Q; Zhao, G, 2022
)
0.72
" We found that most medications were safe in treating severe COVID-19."( Comparative efficacy and safety of pharmacological interventions for severe COVID-19 patients: An updated network meta-analysis of 48 randomized controlled trials.
Chen, J; Cheng, Q; Fang, Z; Jia, Q; Zhao, G, 2022
)
0.72
" Moreover, adverse events were more frequent in the fed state, but all were mild."( Pharmacokinetics, Safety, and Bioequivalence of 2 Lopinavir/Ritonavir (200/50 mg) Tablets in Healthy Chinese Volunteers: Effect of Food on Absorption.
Bao, D; Fu, W; Hu, W; Lin, L; Liu, Y; Zhang, Q; Zhang, W; Zheng, L, 2023
)
1.16

Pharmacokinetics

Lopinavir Cmax and AUC12 were increased 20% to 30% when combined with ritonavir. 32 HIV-infected children received treatment with combinations of high-dose isoniazid, pyrazinamide, ethambutol, ethionamide, terizidone, a fluoroquinolone, and amikacin and 1.

ExcerptReferenceRelevance
"The response to regimens including lopinavir-ritonavir (LPV/r) in patients who have received multiple protease (PR) inhibitors (PI) can be analyzed in terms of human immunodeficiency virus type 1 (HIV-1) genotypic and pharmacokinetic (pK) determinants."( Human immunodeficiency virus type 1 genotypic and pharmacokinetic determinants of the virological response to lopinavir-ritonavir-containing therapy in protease inhibitor-experienced patients.
Breilh, D; Dabis, F; Dupon, M; Fleury, H; Lavignolle, V; Lawson-Ayayi, S; Masquelier, B; Morlat, P; Neau, D; Ragnaud, JM, 2002
)
0.8
" Pharmacokinetic curves were obtained for lopinavir and saquinavir."( Lopinavir/ritonavir plus saquinavir in salvage therapy; pharmacokinetics, tolerability and efficacy.
Burger, DM; la Porte, CJ; Rockstroh, JK; Schneider, K; Wasmuth, JC, 2003
)
2.03
"The pharmacokinetic parameters of lopinavir (LPV) were examined by administering Kaletra (LPV+ritonavir) to 8 healthy Japanese volunteers both in the fasting and postprandial conditions."( Pharmacokinetics of lopinavir after administration of Kaletra in healthy Japanese volunteers.
Ito, H; Kaneda, T; Mamiya, N; Nagaoka, K; Nakai, M; Oki, T; Sagisaka, M; Usami, Y; Utsumi, M; Yamanaka, K, 2004
)
0.93
" Patients receiving the same doses of lopinavir/ritonavir (n = 10) or amprenavir with ritonavir (n = 8) were chosen as controls for pharmacokinetic analyses."( Deep salvage with amprenavir and lopinavir/ritonavir: correlation of pharmacokinetics and drug resistance with pharmacodynamics.
Baldini, F; Cauda, R; Cingolani, A; De Luca, A; Di Giambenedetto, S; Hoetelmans, RM, 2004
)
0.88
"Coadministration of lopinavir-ritonavir, an antiretroviral protease inhibitor, at the standard dose (400/100 mg twice a day [BID]) with the antituberculous agent rifampin is contraindicated because of a significant pharmacokinetic interaction due to induction of cytochrome P450 3A by rifampin."( Pharmacokinetics of adjusted-dose lopinavir-ritonavir combined with rifampin in healthy volunteers.
Bertz, R; Boeree, MJ; Burger, DM; Colbers, EP; Hekster, YA; Koopmans, PP; la Porte, CJ; Voncken, DS; Wikstrom, K, 2004
)
0.93
" The median pharmacokinetic parameters of lopinavir were as follows: area under the concentration-time curve from 0 to 12 h (AUC(0-12)), 85."( Steady-state pharmacokinetics of a double-boosting regimen of saquinavir soft gel plus lopinavir plus minidose ritonavir in human immunodeficiency virus-infected adults.
Azuaje, C; Clotet, B; Crespo, M; Diaz, M; Falcó, V; Lopez, RM; Ocaña, I; Pahissa, A; Pou, L; Ribera, E; Ruiz, I; Ruiz, L, 2004
)
0.81
" In contrast, the sparse sampling done in population pharmacokinetic studies relies on patient-reported times of dosing, the accuracy of which the authors sought to assess by adding electronic monitoring to the usual patient reporting of dosing times."( Successful projection of the time course of drug concentration in plasma during a 1-year period from electronically compiled dosing-time data used as input to individually parameterized pharmacokinetic models.
Bertz, R; Mayer, S; Rode, R; Tousset, E; Urquhart, J; Vrijens, B, 2005
)
0.33
" LPV/r concentrations were measured by LC-MS/MS, and the data were analyzed by noncompartmental pharmacokinetic analysis."( Absence of circadian variation in the pharmacokinetics of lopinavir/ritonavir given as a once daily dosing regimen in HIV-1-infected patients.
Bourbeau, M; Cameron, DW; Garber, GE; Giguere, P; Seguin, I; van Heeswijk, RP, 2005
)
0.57
"To develop a population pharmacokinetic model for lopinavir in combination with ritonavir, in which the interaction between both drugs was characterized, and in which relationships between patient characteristics and pharmacokinetics were identified."( Population pharmacokinetics of lopinavir in combination with ritonavir in HIV-1-infected patients.
Beijnen, JH; Crommentuyn, KM; Huitema, AD; Kappelhoff, BS; Mairuhu, AT; Meenhorst, PL; Mulder, JW; van Gorp, EC, 2005
)
0.87
" First, ritonavir data were fitted to a previously developed model to obtain individual Bayesian estimates of pharmacokinetic parameters."( Population pharmacokinetics of lopinavir in combination with ritonavir in HIV-1-infected patients.
Beijnen, JH; Crommentuyn, KM; Huitema, AD; Kappelhoff, BS; Mairuhu, AT; Meenhorst, PL; Mulder, JW; van Gorp, EC, 2005
)
0.61
"We have developed a model that has defined a time-independent inverse relationship between the exposure to ritonavir and the CL/F of lopinavir, and provided an adequate description of the pharmacokinetic parameters for the latter."( Population pharmacokinetics of lopinavir in combination with ritonavir in HIV-1-infected patients.
Beijnen, JH; Crommentuyn, KM; Huitema, AD; Kappelhoff, BS; Mairuhu, AT; Meenhorst, PL; Mulder, JW; van Gorp, EC, 2005
)
0.82
"Samples were collected for a 12-hour pharmacokinetic profile in all children."( Pharmacokinetics and 24-week efficacy/safety of dual boosted saquinavir/lopinavir/ritonavir in nucleoside-pretreated children.
Ananworanich, J; Bergshoeff, A; Burger, D; Engchanil, C; Hill, A; Kosalaraksa, P; Pancharoen, C; Ruxrungtham, K; Siangphoe, U, 2005
)
0.56
" Median area under the concentration curve at 0-12 hours and Cmin were 39."( Pharmacokinetics and 24-week efficacy/safety of dual boosted saquinavir/lopinavir/ritonavir in nucleoside-pretreated children.
Ananworanich, J; Bergshoeff, A; Burger, D; Engchanil, C; Hill, A; Kosalaraksa, P; Pancharoen, C; Ruxrungtham, K; Siangphoe, U, 2005
)
0.56
"Six HIV-positive antiretroviral experienced patients initiating therapy with a regimen including lopinavir/ritonavir (400/100 mg twice per day) and indinavir (800 mg twice per day) underwent steady-state pharmacokinetic analysis."( Steady-state pharmacokinetics and tolerability of indinavir-lopinavir/r combination therapy in antiretroviral-experienced patients.
Antoniou, T; Giguere, P; Phillips, EJ; Tseng, AL; van Heeswijk, RP; Walker, SE, 2005
)
0.79
"The influence of saquinavir hard-gel capsules on lopinavir pharmacokinetic parameters was investigated using a population approach."( No significant influence of saquinavir hard-gel capsule administration on pharmacokinetics of lopinavir in combination with ritonavir: a population approach.
Allavena, C; Dailly, E; Gagnieu, MC; Jolliet, P; Raffi, F, 2005
)
0.8
" When the 2 hepatic impairment groups were combined, lopinavir Cmax and AUC12 were increased 20% to 30% compared to the controls."( Pharmacokinetics of lopinavir/ritonavir in HIV/hepatitis C virus-coinfected subjects with hepatic impairment.
Arribas, J; Brun, SC; Causemaker, SJ; Cepeda, C; DaSilva, B; García Cabanillas, JA; Li, J; Lorenzo, A; Peng, JZ; Pulido, F, 2006
)
0.91
"To assess potential pharmacokinetic (PK) interactions between atazanavir (ATV, 300 mg, once daily) and lopinavir (LPV, 400 mg, twice daily), both boosted by ritonavir (RTV, 100 mg)."( Ritonavir-boosted atazanavir-lopinavir combination: a pharmacokinetic interaction study of total, unbound plasma and cellular exposures.
Biollaz, J; Buclin, T; Cavassini, M; Colombo, S; Decosterd, LA; Franc, C; Guignard, N; Khonkarly, M; Rochat, B; Tarr, PE; Telenti, A, 2006
)
0.84
" Minimum and maximum concentrations (C subsetmin, C subsetmax), area under the concentration-time curve (AUC subset0-12h), total clearance (CL subsettot) and half-life (t1/2) were calculated."( Pharmacokinetics and tolerability of a combination of indinavir, lopinavir and ritonavir in multiply pretreated HIV-1 infected adults.
Harder, S; Klauke, S; Kurowski, M; Lutz, T; Müller, A; Rottmann, C; Staszewski, S; von Hentig, N, 2006
)
0.57
" 3,467 ng*h/mL; Cmin 220 ng/mL vs."( Pharmacokinetics and tolerability of a combination of indinavir, lopinavir and ritonavir in multiply pretreated HIV-1 infected adults.
Harder, S; Klauke, S; Kurowski, M; Lutz, T; Müller, A; Rottmann, C; Staszewski, S; von Hentig, N, 2006
)
0.57
" The mean (standard deviation) AUC0-24, Cmax and Cmin of lopinavir were 149."( Pharmacokinetics of a once-daily regimen of lopinavir/ritonavir in HIV-1-infected children.
Burger, D; de Groot, R; van der Lee, M; Verweel, G, 2006
)
0.84
"Our findings indicate that 460/115 mg/m2 lopinavir/ritonavir once daily leads to mean pharmacokinetic parameters comparable to data of 800/200 mg lopinavir/ritonavir once daily in adults, although the variability observed in the trough levels is much higher in children."( Pharmacokinetics of a once-daily regimen of lopinavir/ritonavir in HIV-1-infected children.
Burger, D; de Groot, R; van der Lee, M; Verweel, G, 2006
)
0.86
" Pharmacokinetic sampling was performed on day 8 of each treatment, and samples were analyzed for FPV, amprenavir (APV), LPV, and RTV concentrations by high-performance liquid chromatography-tandem mass spectrometry."( Dose separation does not overcome the pharmacokinetic interaction between fosamprenavir and lopinavir/ritonavir.
Corbett, AH; Eron, JJ; Kalvass, LA; Kashuba, AD; Lim, ML; Ngo, LT; Patterson, KB; Tien, HC, 2006
)
0.55
" A pre-dose to 6 h post-dose steady-state pharmacokinetic analysis (n = 35) of the drugs on the day of the scheduled Caesarean section was performed."( Placental transfer and pharmacokinetics of lopinavir and other protease inhibitors in combination with nevirapine at delivery.
Belohradsky, BH; Eberle, J; Friese, K; Gingelmaier, A; Grubert, TA; Kästner, R; Kurowski, M; Mylonas, I, 2006
)
0.6
" The consequences of these pharmacokinetic discrepancies and the necessity to modify the currently recommended dosage regimen should be further investigated."( Population analysis of weight-, age-, and sex-related differences in the pharmacokinetics of lopinavir in children from birth to 18 years.
Blanche, S; Chaix, ML; Delaugerre, C; Firtion, G; Hirt, D; Jullien, V; Macassa, E; Pons, G; Rey, E; Rouzioux, C; Teglas, JP; Tréluyer, JM; Urien, S; Vaz, P, 2006
)
0.55
" Thus, for ritonavir AUC12, Cmax and Cmin in HCV+/FIB+patients were 63%, 86% and 100% higher, respectively, when compared with those parameters in HCV-patients (p=0."( Lopinavir/ritonavir pharmacokinetics in HIV and hepatitis C virus co-infected patients without liver function impairment: influence of liver fibrosis.
Barbanoj, MJ; Blanco, A; Clotet, B; Costa, J; DelaVarga, M; Domingo, P; Miranda, C; Miranda, J; Moltó, J; Negredo, E; Tural, C; Valle, M; Vilaró, J, 2007
)
1.78
" Lopinavir and ritonavir pharmacokinetic parameters were evaluated."( Lack of effect of gastric acid-reducing agents on the pharmacokinetics of lopinavir/ritonavir in HIV-infected patients.
Awni, W; Brun, S; Chiu, YL; King, KR; Klein, CE; Naylor, C; Woodward, WC, 2007
)
1.48
" Pharmacokinetic parameters estimated by noncompartmental method were reported as 90% confidence intervals (CIs) about the geometric mean ratio (GMR)."( Lopinavir/Ritonavir pharmacokinetic profile: impact of sex and other covariates following a change from twice-daily to once-daily therapy.
Acosta, EP; Binongo, JN; Chuck, SK; Lennox, JL; Ofotokun, I; Palau, M, 2007
)
1.78
"HIV-infected subjects on abacavir (600 mg once daily) plus two nucleoside reverse transcriptase inhibitors (NRTIs) (excluding tenofovir) underwent a 24 h pharmacokinetic assessment for plasma abacavir concentrations."( Abacavir plasma pharmacokinetics in the absence and presence of atazanavir/ritonavir or lopinavir/ritonavir and vice versa in HIV-infected patients.
Back, D; Boffito, M; Bonora, S; D'Avolio, A; Else, L; Gazzard, B; Mandalia, S; Moyle, G; Nelson, M; Pozniak, A; Waters, LJ, 2007
)
0.56
" The clinical consequences of these substantial pharmacokinetic changes should be investigated."( Lopinavir-ritonavir dramatically affects the pharmacokinetics of irinotecan in HIV patients with Kaposi's sarcoma.
Corona, G; Innocenti, F; Sandron, S; Sartor, I; Tirelli, U; Toffoli, G; Vaccher, E, 2008
)
1.79
" Data originated from pre-defined pharmacokinetic substudies within two randomized 48-week trials evaluating the safety and efficacy of three protease inhibitor regimens."( Pharmacokinetics of two randomized trials evaluating the safety and efficacy of indinavir, saquinavir and lopinavir in combination with low-dose ritonavir: the MaxCmin1 and 2 trials.
Cahn, P; Castagna, A; Clumeck, N; Dragsted, UB; Fox, Z; Gerstoft, J; Justesen, US; Losso, M; Lundgren, JD; Obel, N; Pedersen, C; Peters, B, 2007
)
0.55
"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
)
0.69
"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
)
0.69
"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
)
0.69
" Intensive pharmacokinetic sampling was performed at 2 weeks and predose concentrations were collected every 8 weeks; safety and plasma HIV-1 RNA were monitored every 4-12 weeks for 24 weeks."( Pharmacokinetics, safety and efficacy of lopinavir/ritonavir in infants less than 6 months of age: 24 week results.
Capparelli, EV; Chadwick, EG; Chen, J; Hughes, M; Palumbo, P; Pinto, JA; Robbins, B; Rodman, JH; Serchuck, L; Smith, E; Yogev, R, 2008
)
0.61
" Lopinavir pharmacokinetic measures (median [interquartile range]) for children with and without rifampicin, respectively, were maximum concentration (Cmax) of 10."( Effect of rifampicin on lopinavir pharmacokinetics in HIV-infected children with tuberculosis.
Egbers, C; Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2008
)
1.56
" Although the median Cmax and AUC0-12 were lowered by 26% and 31%."( Effect of rifampicin on lopinavir pharmacokinetics in HIV-infected children with tuberculosis.
Egbers, C; Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2008
)
0.65
"Studies on the pharmacokinetic interaction between atazanavir and lopinavir with ritonavir (lopinavir/ritonavir) report contradictory results."( Atazanavir and lopinavir with ritonavir alone or in combination: analysis of pharmacokinetic interaction and predictors of drug exposure.
Bacarelli, A; Cauda, R; De Luca, A; Di Giambenedetto, S; Navarra, P; Ragazzoni, E; Regazzi, M; Villani, P, 2008
)
0.94
" Total (n = 56) and unbound (n = 36) LPV pharmacokinetic parameters were determined at steady-state using validated high-performance liquid chromatography with ultraviolet detection and high-performance liquid chromatography-tandem mass spectrometry methods, respectively."( Lopinavir/ritonavir pharmacokinetics in HIV/HCV-coinfected patients with or without cirrhosis.
Back, DJ; Cargnel, A; Cordier, L; Cusato, M; Dickinson, L; Duca, P; Khoo, SH; Meraviglia, P; Micheli, V; Orlando, G; Regazzi, M; Rizzardini, G; Viganò, P; Villani, P, 2008
)
1.79
" It is coformulated with low doses of ritonavir in order to enhance its pharmacokinetic profile."( Simultaneous population pharmacokinetic model for lopinavir and ritonavir in HIV-infected adults.
Barbanoj, MJ; Blanco, A; Clotet, B; Costa, J; Domingo, P; Miranda, C; Moltó, J; Negredo, E; Santos, JR; Valle, M, 2008
)
0.6
"To develop and validate a population pharmacokinetic model for lopinavir and ritonavir administered simultaneously in a population of HIV-infected adults."( Simultaneous population pharmacokinetic model for lopinavir and ritonavir in HIV-infected adults.
Barbanoj, MJ; Blanco, A; Clotet, B; Costa, J; Domingo, P; Miranda, C; Moltó, J; Negredo, E; Santos, JR; Valle, M, 2008
)
0.84
" First, a population pharmacokinetic model was developed for lopinavir and for ritonavir separately."( Simultaneous population pharmacokinetic model for lopinavir and ritonavir in HIV-infected adults.
Barbanoj, MJ; Blanco, A; Clotet, B; Costa, J; Domingo, P; Miranda, C; Moltó, J; Negredo, E; Santos, JR; Valle, M, 2008
)
0.84
" 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
)
0.59
"This was an open-label, three-session, pharmacokinetic trial."( Pharmacokinetics of atazanavir/ritonavir once daily and lopinavir/ritonavir twice and once daily over 72 h following drug cessation.
Back, D; Boffito, M; Else, L; Gazzard, B; Khoo, S; Moyle, G; Pozniak, A; Sousa, M; Taylor, J, 2008
)
0.59
"This study investigated the pharmacokinetic forgiveness of two boosted protease inhibitors."( Pharmacokinetics of atazanavir/ritonavir once daily and lopinavir/ritonavir twice and once daily over 72 h following drug cessation.
Back, D; Boffito, M; Else, L; Gazzard, B; Khoo, S; Moyle, G; Pozniak, A; Sousa, M; Taylor, J, 2008
)
0.59
" The aims of this study were to develop a population pharmacokinetic (PK) model of LPV in children and to estimate the probability of achieving a PIQ of >15."( Population pharmacokinetics of lopinavir predict suboptimal therapeutic concentrations in treatment-experienced human immunodeficiency virus-infected children.
Baghdassarian, A; Neely, MN; Rakhmanina, N; Soldin, S; van den Anker, J; Williams, K, 2009
)
0.64
" Statistical analyses were performed on pharmacokinetic parameters: the area under the concentration-time curve from 0 to 4 h (AUC(0-4)), the maximum concentration of the drug (C(max)), and the residual concentration of the drug at the end of the dosing interval (C(trough)) for plasma and the AUC(0-4) and C(trough) for intracellular data."( Pilot pharmacokinetic study of human immunodeficiency virus-infected patients receiving tenofovir disoproxil fumarate (TDF): investigation of systemic and intracellular interactions between TDF and abacavir, lamivudine, or lopinavir-ritonavir.
Ayen, R; Clotet, B; Grassi, J; Levi, M; Negredo, E; Pruvost, A; Puig, J; Théodoro, F, 2009
)
0.54
" For artemether, trends toward Cmax and AUC decreases (Cmax 14."( Lopinavir/ritonavir affects pharmacokinetic exposure of artemether/lumefantrine in HIV-uninfected healthy volunteers.
Aweeka, FT; Charlebois, E; Dorsey, G; German, P; Hanpithakpong, W; Havlir, D; Lawrence, J; Lindegardh, N; Parikh, S; Rosenthal, PJ, 2009
)
1.8
" Full pharmacokinetic profiles were analysed for lopinavir and ritonavir with a validated HPLC tandem mass spectrometry assay."( Pharmacokinetics and tolerability of once- versus twice-daily lopinavir/ritonavir treatment in HIV-1-infected children.
la Porte, C; Mitchell, CD; Parker, J; Rongkavilit, C; van Heeswijk, R; Zhang, G, 2009
)
0.85
" A 12 h pharmacokinetic study was done at 4-6 weeks after starting treatment."( Pharmacokinetics and 48 week efficacy of low-dose lopinavir/ritonavir in HIV-infected children.
Ananworanich, J; Boonrak, P; Bunupuradah, T; Burger, D; Gorowara, M; Jupimai, T; Pancharoen, C; Phasomsap, C; Puthanakit, T; Ruxrungtham, K; van der Lugt, J, 2009
)
0.61
"Low-dose lopinavir displayed adequate pharmacokinetic parameters and good efficacy as compared with standard-dose lopinavir in Thai children."( Pharmacokinetics and 48 week efficacy of low-dose lopinavir/ritonavir in HIV-infected children.
Ananworanich, J; Boonrak, P; Bunupuradah, T; Burger, D; Gorowara, M; Jupimai, T; Pancharoen, C; Phasomsap, C; Puthanakit, T; Ruxrungtham, K; van der Lugt, J, 2009
)
1.02
" Noncompartmental and population pharmacokinetic analyses (2-compartment open model) were performed."( Pharmacokinetic evaluation of rifabutin in combination with lopinavir-ritonavir in patients with HIV infection and active tuberculosis.
Ashkin, D; Boulanger, C; Espinoza, LA; Farrell, K; Graham, JJ; Hollender, E; Maasen, D; Peloquin, CA; Rivero, RO; Stambaugh, JJ; Symes, S, 2009
)
0.6
" For the five pharmacokinetic trials of lopinavir/ritonavir, a meta-analysis was used to estimate the effects of lopinavir dose versus ritonavir dose on lopinavir pharmacokinetics."( How much ritonavir is needed to boost protease inhibitors? Systematic review of 17 dose-ranging pharmacokinetic trials.
Boffito, M; Hill, A; Sawyer, W; van der Lugt, J, 2009
)
0.62
"A population pharmacokinetic model for lopinavir was developed using data from 424 HIV type-1-infected patients, and the final model was used to estimate the probability to achieve target C(troughs) via Monte Carlo simulations."( A population analysis of weight-related differences in lopinavir pharmacokinetics and possible consequences for protease inhibitor-naive and -experienced patients.
Bouillon-Pichault, M; Chhun, S; Dupin, N; Jullien, V; Krivine, A; Launay, O; Lortholary, O; Morini, JP; Piketty, C; Pons, G; Salmon, D; Treluyer, JM; Viard, JP; Weiss, L, 2009
)
0.87
"To determine the pharmacokinetic profiles of lopinavir and ritonavir in two newly developed generic co-formulations for HIV-infected children (Lopimune paediatric tablets and granules, 100/25 mg of lopinavir/ritonavir, Cipla Pharmaceuticals), and to compare these with the branded product (Kaletra)."( Pharmacokinetics of two generic co-formulations of lopinavir/ritonavir for HIV-infected children: a pilot study of paediatric Lopimune versus the branded product in healthy adult volunteers.
Burger, DM; Colbers, EP; de Kanter, CT; Fillekes, Q; Hoitsma, A, 2010
)
0.87
" A 32 h pharmacokinetic curve was recorded."( Pharmacokinetics of two generic co-formulations of lopinavir/ritonavir for HIV-infected children: a pilot study of paediatric Lopimune versus the branded product in healthy adult volunteers.
Burger, DM; Colbers, EP; de Kanter, CT; Fillekes, Q; Hoitsma, A, 2010
)
0.61
"Large differences in pharmacokinetic parameters can be excluded for Lopimune paediatric tablets when compared with the branded product and taken on an empty stomach, and also for Lopimune granules when these are taken with food."( Pharmacokinetics of two generic co-formulations of lopinavir/ritonavir for HIV-infected children: a pilot study of paediatric Lopimune versus the branded product in healthy adult volunteers.
Burger, DM; Colbers, EP; de Kanter, CT; Fillekes, Q; Hoitsma, A, 2010
)
0.61
"We aimed to investigate the extent of pharmacokinetic drug interactions between bosentan and a fixed combination of lopinavir/ritonavir."( Mutual pharmacokinetic interactions between bosentan and lopinavir/ritonavir in healthy participants.
Dingemanse, J; Nilsson, PN; Patat, A; van Giersbergen, PL, 2010
)
0.82
" 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
)
0.68
" LPV/r pharmacokinetic parameters were calculated using noncompartmental analysis."( Pharmacokinetics and virologic response of zidovudine/lopinavir/ritonavir initiated during the third trimester of pregnancy.
Chirayus, S; Cressey, TR; Jourdain, G; Kongpanichkul, R; Lallemant, M; Ngo-Giang-Huong, N; Pattarakulwanich, S; Rawangban, B; Sabsanong, P; Varadisai, S; Voramongkol, N; Yuthavisuthi, P, 2010
)
0.61
" Geometric mean (90% confidence interval) LPV AUC, Cmax and Cmin were 64."( Pharmacokinetics and virologic response of zidovudine/lopinavir/ritonavir initiated during the third trimester of pregnancy.
Chirayus, S; Cressey, TR; Jourdain, G; Kongpanichkul, R; Lallemant, M; Ngo-Giang-Huong, N; Pattarakulwanich, S; Rawangban, B; Sabsanong, P; Varadisai, S; Voramongkol, N; Yuthavisuthi, P, 2010
)
0.61
"International Maternal Pediatric Adolescent AIDS Clinical Trials 1026s is a prospective nonblinded pharmacokinetic study in HIV-infected pregnant women, including a cohort receiving 2 lopinavir/ritonavir tablets (400 mg/100 mg) twice daily during the second trimester, 3 tablets (600 mg/150 mg) twice daily during the third trimester, and 2 tablets (400 mg/100 mg) twice daily post delivery through 2 weeks postpartum."( Lopinavir tablet pharmacokinetics with an increased dose during pregnancy.
Best, BM; Burchett, SK; Capparelli, EV; Hu, C; Li, H; Mirochnick, M; Read, JS; Rossi, SS; Smith, E; Stek, AM, 2010
)
1.99
"Steady-state 12-hour pharmacokinetic profiles were performed during pregnancy and at 2 weeks postpartum."( Lopinavir tablet pharmacokinetics with an increased dose during pregnancy.
Best, BM; Burchett, SK; Capparelli, EV; Hu, C; Li, H; Mirochnick, M; Read, JS; Rossi, SS; Smith, E; Stek, AM, 2010
)
1.8
"This study was conducted to examine the pharmacokinetic interactions between buprenorphine/naloxone (BUP/NLX) and lopinavir/ritonavir (LPV/r) in HIV-seronegative subjects chronically maintained on BUP/NLX."( Pharmacokinetic interactions between buprenorphine/naloxone and once-daily lopinavir/ritonavir.
Altice, FL; Andrews, L; Bruce, RD; Fang, WB; Friedland, GH; Lin, SN; Ma, Q; Moody, DE; Morse, GD, 2010
)
0.8
"This study was an open labeled pharmacokinetic study in twelve HIV-seronegative subjects stabilized on at least 3 weeks of BUP/NLX therapy."( Pharmacokinetic interactions between buprenorphine/naloxone and once-daily lopinavir/ritonavir.
Altice, FL; Andrews, L; Bruce, RD; Fang, WB; Friedland, GH; Lin, SN; Ma, Q; Moody, DE; Morse, GD, 2010
)
0.59
"2 ng*hr/mL) and Cmax (6."( Pharmacokinetic interactions between buprenorphine/naloxone and once-daily lopinavir/ritonavir.
Altice, FL; Andrews, L; Bruce, RD; Fang, WB; Friedland, GH; Lin, SN; Ma, Q; Moody, DE; Morse, GD, 2010
)
0.59
" Pharmacodynamic responses indicate that the altered norbuprenorphine clearance did not lead to opioid withdrawal."( Pharmacokinetic interactions between buprenorphine/naloxone and once-daily lopinavir/ritonavir.
Altice, FL; Andrews, L; Bruce, RD; Fang, WB; Friedland, GH; Lin, SN; Ma, Q; Moody, DE; Morse, GD, 2010
)
0.59
" Pharmacokinetic parameters were compared using the 400/100 mg twice daily dose as reference, by determining geometric mean ratios (GMRs) and 90% confidence intervals."( Pharmacokinetics of plasma lopinavir/ritonavir following the administration of 400/100 mg, 200/150 mg and 200/50 mg twice daily in HIV-negative volunteers.
Amin, J; Back, D; Boffito, M; Else, L; Emery, S; Gazzard, B; Hill, A; Jackson, A; Khoo, S; Lin, E; Morley, R; Puls, R, 2011
)
0.67
"These pharmacokinetic data show that therapeutic plasma concentrations of lopinavir can be achieved with 200/150 mg of lopinavir/ritonavir twice daily (one Meltrex tablet and one 100 mg ritonavir capsule twice daily)."( Pharmacokinetics of plasma lopinavir/ritonavir following the administration of 400/100 mg, 200/150 mg and 200/50 mg twice daily in HIV-negative volunteers.
Amin, J; Back, D; Boffito, M; Else, L; Emery, S; Gazzard, B; Hill, A; Jackson, A; Khoo, S; Lin, E; Morley, R; Puls, R, 2011
)
0.9
" This 2-step, multicenter, pharmacokinetic study enrolled human immunodeficiency virus (HIV)-infected adults on lopinavir/ritonavir (LPV/r) capsules (400/100 mg bid) plus 1 or more nucleoside reverse transcriptase inhibitors."( Sex differences in lopinavir and ritonavir pharmacokinetics among HIV-infected women and men.
Cramer, Y; Currier, JS; Fletcher, CV; Hermes, AE; Park, JG; Umeh, OC, 2011
)
0.91
" Data were modeled first separately and then together by using individually predicted ritonavir pharmacokinetic parameters in the final lopinavir model."( Sequential population pharmacokinetic modeling of lopinavir and ritonavir in healthy volunteers and assessment of different dosing strategies.
Aarons, L; Back, D; Boffito, M; Davies, G; Dickinson, L; Else, L; Khoo, S; Moyle, G; Pozniak, A; von Hentig, N, 2011
)
0.83
" There were no significant differences in the LPV area under the plasma concentration-time curve from 0 to 12 h (AUC(0-12)), C(0), C(12), maximum concentration of drug in serum (C(max)), or half-life (t(1/2)) between the baseline and double-dose LPV/r time points."( Pharmacokinetics of lopinavir in HIV-infected adults receiving rifampin with adjusted doses of lopinavir-ritonavir tablets.
Decloedt, EH; Maartens, G; McIlleron, H; Merry, C; Orrell, C; Smith, P, 2011
)
0.69
" 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
)
1.17
" Each subject had 2 separate (within 30 days) steady-state 12-hour pharmacokinetic (PK) studies with crushed and whole 200/50 mg lopinavir/ritonavir tablets."( Pharmacokinetics of lopinavir/ritonavir crushed versus whole tablets in children.
Best, BM; Capparelli, EV; Diep, H; Farrell, MJ; Lee, G; Rakhmanina, N; Rossi, SS; van den Anker, JN; Williams, E, 2011
)
0.9
" This study determined the pharmacokinetic (PK) parameters of a low-dose LPV/r tablet (70% of standard dose) in HIV-infected Thai adolescents."( Low dose lopinavir/ritonavir tablet achieves adequate pharmacokinetic parameters in HIV-infected Thai adolescents.
Ananworanich, J; Burger, D; Gorowara, M; Kerr, S; Klinklom, A; Pancharoen, C; Phasomsap, C; Puthanakit, T; Ruxrungtham, K; Sriheara, C, 2012
)
0.8
" A mechanistic evaluation was undertaken using various in vitro and ex vivo studies to support the in vivo pharmacokinetic data."( Effect of grapefruit juice and ritonavir on pharmacokinetics of lopinavir in Wistar rats.
Aditya, N; Ravi, PR; Srivani, S; Thakur, R; Vats, R, 2012
)
0.62
" A phase I pharmacokinetic study was conducted to assess the impact of long-term use of ritonavir-boosted lopinavir (LPV/r) on quinine pharmacokinetics in healthy volunteers."( Effects of ritonavir-boosted lopinavir on the pharmacokinetics of quinine.
El-Gasim, M; Hendrix, CW; Lu, Y; Nyunt, MM; Parsons, TL; Petty, BG, 2012
)
0.88
" Intensive pharmacokinetic sampling was performed 7 days apart after LPV/r dosing under moderate fat, high fat, and fasted meal conditions."( Steady-state pharmacokinetics of lopinavir plus ritonavir when administered under different meal conditions in HIV-infected Ugandan adults.
Back, D; Boffito, M; Byakika-Kibwika, P; Khoo, S; Lamorde, M; Mayito, J; Merry, C; Nabukeera, L; Ogwal-Okeng, J; Ryan, M; Tjia, J, 2012
)
0.66
" The primary objective was to investigate pharmacokinetic (PK) effects of lopinavir/ritonavir 400 mg/100 mg twice daily on pitavastatin 4 mg when coadministered."( Effects of steady-state lopinavir/ritonavir on the pharmacokinetics of pitavastatin in healthy adult volunteers.
Campbell, SE; Medlock, MM; Morgan, RE; Sponseller, CA; Suehira, K; Yu, CY, 2012
)
0.92
"To evaluate the pharmacokinetic profile of ritonavir-boosted lopinavir in HIV-infected patients during rifabutin-based anti-mycobacterial therapy."( Lopinavir pharmacokinetic profiles in HIV-infected patients during rifabutin-based anti-mycobacterial therapy.
Apostoli, A; Bigoni, S; Calabresi, A; Carvalho, AC; Cusato, M; Dal Zoppo, S; El-Hamad, I; Marcantoni, C; Matteelli, A; Regazzi, M; Villani, P, 2012
)
2.06
"A longitudinal, cross-over pharmacokinetic evaluation of lopinavir with and without rifabutin in HIV-infected subjects with mycobacterial disease was done."( Lopinavir pharmacokinetic profiles in HIV-infected patients during rifabutin-based anti-mycobacterial therapy.
Apostoli, A; Bigoni, S; Calabresi, A; Carvalho, AC; Cusato, M; Dal Zoppo, S; El-Hamad, I; Marcantoni, C; Matteelli, A; Regazzi, M; Villani, P, 2012
)
2.07
"In 10 patients with complete lopinavir curves at T1, T2 and T3 pharmacokinetic values were, respectively: AUC(0-12), 187."( Lopinavir pharmacokinetic profiles in HIV-infected patients during rifabutin-based anti-mycobacterial therapy.
Apostoli, A; Bigoni, S; Calabresi, A; Carvalho, AC; Cusato, M; Dal Zoppo, S; El-Hamad, I; Marcantoni, C; Matteelli, A; Regazzi, M; Villani, P, 2012
)
2.11
"Once-daily LPV/r monotherapy in HIV-HCV coinfected individuals offers a safe and effective approach to the management of the HIV infection, with a predictable pharmacokinetic profile."( A pilot, prospective, open-label simplification study to evaluate the safety, efficacy, and pharmacokinetics of once-daily lopinavir-ritonavir monotherapy in HIV-HCV coinfected patients: the MONOCO study.
Ackad, N; Conway, B; Cooper, C; la Porte, C; Sampalis, J; Tossonian, H,
)
0.34
"Boceprevir represents a new treatment option for hepatitis C (HCV)-infected patients, including those with HCV/human immunodeficiency virus coinfection; however, little is known about pharmacokinetic interactions between boceprevir and antiretroviral drugs."( Pharmacokinetic interactions between the hepatitis C virus protease inhibitor boceprevir and ritonavir-boosted HIV-1 protease inhibitors atazanavir, darunavir, and lopinavir.
Butterton, JR; Feng, HP; Hughes, EA; Hulskotte, EG; O'Mara, E; Treitel, MA; van Zutven, MG; Wagner, JA; Xuan, F; Youngberg, SP, 2013
)
0.59
"A randomized, open-label study to assess the pharmacokinetic interactions between boceprevir and ritonavir-boosted protease inhibitors (PI/r) was conducted in 39 healthy adults."( Pharmacokinetic interactions between the hepatitis C virus protease inhibitor boceprevir and ritonavir-boosted HIV-1 protease inhibitors atazanavir, darunavir, and lopinavir.
Butterton, JR; Feng, HP; Hughes, EA; Hulskotte, EG; O'Mara, E; Treitel, MA; van Zutven, MG; Wagner, JA; Xuan, F; Youngberg, SP, 2013
)
0.59
" The objective of this study was to develop a population pharmacokinetic model describing the pharmacokinetic differences of lopinavir and ritonavir, with and without rifampicin, between children and adults."( Model-based evaluation of the pharmacokinetic differences between adults and children for lopinavir and ritonavir in combination with rifampicin.
Decloedt, EH; Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Zhang, C, 2013
)
0.82
"An integrated population pharmacokinetic model developed in nonmem 7 was used to describe the pharmacokinetics of lopinavir and ritonavir in 21 HIV infected adults, 39 HIV infected children and 35 HIV infected children with tuberculosis, who were established on lopinavir/ritonavir-based antiretroviral therapy with and without rifampicin-containing antituberculosis therapy."( Model-based evaluation of the pharmacokinetic differences between adults and children for lopinavir and ritonavir in combination with rifampicin.
Decloedt, EH; Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Zhang, C, 2013
)
0.82
" In children, the absorption half-life of lopinavir and the mean transit time of ritonavir were lengthened, compared with those in adults."( Model-based evaluation of the pharmacokinetic differences between adults and children for lopinavir and ritonavir in combination with rifampicin.
Decloedt, EH; Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Zhang, C, 2013
)
0.88
" The current study evaluated the pharmacokinetic interaction between etravirine and the lopinavir/ritonavir melt extrusion formulation."( Steady-state pharmacokinetics of etravirine and lopinavir/ritonavir melt extrusion formulation, alone and in combination, in healthy HIV-negative volunteers.
Akuma, SH; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Schöller-Gyüre, M; Spittaels, K; Vyncke, V; Witek, J, 2013
)
0.87
" Steady-state pharmacokinetics were assessed for all antiretrovirals alone and coadministered; pharmacokinetic parameters were obtained by noncompartmental analysis."( Steady-state pharmacokinetics of etravirine and lopinavir/ritonavir melt extrusion formulation, alone and in combination, in healthy HIV-negative volunteers.
Akuma, SH; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Schöller-Gyüre, M; Spittaels, K; Vyncke, V; Witek, J, 2013
)
0.65
"The evidence to date does not support major pharmacokinetic changes in adults between ∼ 20 and 60 years of age."( Clinical pharmacokinetics of antiretroviral drugs in older persons.
Anderson, PL; Erlandson, KM; Schoen, JC, 2013
)
0.39
"The mean Cmax and AUC0-24 of rifabutin in patients on rifabutin 150 mg every other day were 36% and 26% lower than on 300 mg/day rifabutin, while the mean Cmax and AUC0-24 of 25-O-desacetyl rifabutin were 186% and 152% higher, respectively."( Pharmacokinetics of rifabutin in Japanese HIV-infected patients with or without antiretroviral therapy.
Aoki, T; Gatanaga, H; Honda, H; Kikuchi, Y; Oka, S; Sano, K; Tanuma, J; Teruya, K; Tsukada, K; Watanabe, K; Yazaki, H, 2013
)
0.39
" They are characterized by highly cooperative dose-response curves that are not explained by current pharmacodynamic theory."( Multi-step inhibition explains HIV-1 protease inhibitor pharmacodynamics and resistance.
Bailey, JR; Chioma, S; Durand, CM; Laird, GM; Laskey, S; Moore, RD; Rabi, SA; Shan, L; Siliciano, RF, 2013
)
0.39
" Reference lopinavir concentrations were Cmin 1-8 μg/mL."( Pharmacokinetics of lopinavir determined with an ELISA test in youths with perinatally acquired HIV.
De Hoffer, L; Di Biagio, A; Furfaro, E; Giacomet, V; Ginocchio, F; Miletich, F; Nulvesu, L; Prinapori, R; Rosso, R; Schiavetti, I; Signori, A; Sormani, MP; Taramasso, L; Viscoli, C, 2014
)
1.12
" Lopinavir Cmin was <1 μg/mL in only one sample (2."( Pharmacokinetics of lopinavir determined with an ELISA test in youths with perinatally acquired HIV.
De Hoffer, L; Di Biagio, A; Furfaro, E; Giacomet, V; Ginocchio, F; Miletich, F; Nulvesu, L; Prinapori, R; Rosso, R; Schiavetti, I; Signori, A; Sormani, MP; Taramasso, L; Viscoli, C, 2014
)
1.64
" We aimed to develop a biologically relevant pharmacokinetic model of lopinavir with a description of a CYP3A4-mediated first pass metabolism and enterohepatic circulation (EHC)."( Compartmental pharmacokinetic modeling of lopinavir in humans.
Duangchaemkarn, K; Lohitnavy, M, 2013
)
0.89
"A theoretical model of lopinavir was developed using the classical pharmacokinetic modeling concept."( Compartmental pharmacokinetic modeling of lopinavir in humans.
Duangchaemkarn, K; Lohitnavy, M, 2013
)
0.96
"Modified one compartment with first-order absorption from gastrointestinal (GI) depot and first-order clearance into recycling depot describes a pharmacokinetic of oral single dose of lopinavir 400 mg."( Compartmental pharmacokinetic modeling of lopinavir in humans.
Duangchaemkarn, K; Lohitnavy, M, 2013
)
0.85
" The primary objective was to develop an integrated LPV population pharmacokinetic model to investigate the influence of α-1-acid glycoprotein and link total and free LPV exposure to pharmacodynamic changes in HIV-1 RNA and assess viral dynamic and drug efficacy parameters."( Integrated population pharmacokinetic/viral dynamic modelling of lopinavir/ritonavir in HIV-1 treatment-naïve patients.
Acosta, EP; D'Argenio, DZ; Delille, C; Kerstner-Wood, C; Lennox, JL; Ofotokun, I; Sheth, AN; Wang, K, 2014
)
0.64
"For the total group, LPV geometric mean AUC0-12, Cmax and C12 were 106."( Pharmacokinetics of pediatric lopinavir/ritonavir tablets in children when administered twice daily according to FDA weight bands.
Bastiaans, DE; Burger, DM; Chalermpantmetagul, S; Colbers, AP; Compagnucci, A; Cressey, TR; Forcat, S; Giaquinto, C; Hansudewechakul, R; Harper, LM; Inshaw, JR; Kanjanavanit, S; Königs, C; Lyall, H; Noguera-Julian, A; Saïdi, Y, 2014
)
0.69
"Sixteen and seventeen patients were respectively randomized to the two arms, and pharmacokinetic analysis carried out in 12 and 13 respectively."( Randomised pharmacokinetic trial of rifabutin with lopinavir/ritonavir-antiretroviral therapy in patients with HIV-associated tuberculosis in Vietnam.
Barrail-Tran, A; Borand, L; Connolly, C; Duc, NH; Dung, NH; Harries, AD; Lagarde, D; Lan, NN; Lan, NT; Laureillard, D; Lien, TT; Lienhardt, C; Pym, A; Quillet, C; Taburet, AM; Thu, NT, 2014
)
0.65
"Steady-state 12-hour pharmacokinetic profiles of lopinavir/ritonavir were assessed in patients with (group 1, n = 20) or without (group 2, n = 36) hepatitis coinfection, taking lopinavir/ritonavir 400/100 mg twice a day plus nucleoside reverse transcriptase inhibitors, measured by means of high-performance liquid chromatography-tandem mass spectrometry."( Lopinavir/ritonavir pharmacokinetics, efficacy, and safety in HIV and hepatitis B or C coinfected adults without symptoms of hepatic impairment.
Bickel, M; Brodt, R; Haberl, A; Khaykin, P; Kotzerke, P; Kurowski, M; Nisius, G; Stephan, C; Stürmer, M; von Hentig, N, 2014
)
2.1
" Comparative oral pharmacokinetic studies and tissue distribution studies of optimized SLNs and LPV/RTV coformulation were done in Wistar rats."( A hybrid design to optimize preparation of lopinavir loaded solid lipid nanoparticles and comparative pharmacokinetic evaluation with marketed lopinavir/ritonavir coformulation.
Dalal, V; Murthy, AN; Ravi, PR; Vats, R, 2014
)
0.67
" 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
)
0.87
" Twelve-hour intensive pharmacokinetic sampling after observed LPV/r intake (plus 2 nucleoside reverse transcriptase inhibitors) following World Health Organization 2010 dosing with food was performed 4 weeks after enrollment."( The pharmacokinetics and acceptability of lopinavir/ritonavir minitab sprinkles, tablets, and syrups in african HIV-infected children.
Burger, D; Fillekes, Q; Gibb, DM; Keishanyu, R; Kekitiinwa, A; Kendall, L; Lallemant, M; Musiime, V; Namuddu, R; Opilo, W; Walker, AS; Young, N, 2014
)
0.67
" Among 132 evaluable pharmacokinetic profiles, there were 13/21/25 within-child comparisons in cohort A/B/C."( The pharmacokinetics and acceptability of lopinavir/ritonavir minitab sprinkles, tablets, and syrups in african HIV-infected children.
Burger, D; Fillekes, Q; Gibb, DM; Keishanyu, R; Kekitiinwa, A; Kendall, L; Lallemant, M; Musiime, V; Namuddu, R; Opilo, W; Walker, AS; Young, N, 2014
)
0.67
" Further, extensive pharmacokinetic and tissue distribution studies were performed in Wistar rats."( Modified pullulan nanoparticles for oral delivery of lopinavir: formulation and pharmacokinetic evaluation.
Adapa, SP; Aditya, N; Balija, J; Ravi, PR; Vats, R, 2014
)
0.65
" We investigated the association of CYP3A4*22 with the pharmacokinetics of lopinavir through a population pharmacokinetic approach."( CYP3A4*22 (c.522-191 C>T; rs35599367) is associated with lopinavir pharmacokinetics in HIV-positive adults.
Back, D; Egan, D; Khoo, S; Olagunju, A; Owen, A; Schipani, A; Siccardi, M, 2014
)
0.88
" 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
)
0.61
"Single-sequence, open-label, single-center pharmacokinetic investigation."( Influence of Panax ginseng on the steady state pharmacokinetic profile of lopinavir-ritonavir in healthy volunteers.
Alfaro, RM; Calderón, MM; Chairez, CL; Gordon, LA; Kovacs, JA; Penzak, SR, 2014
)
0.63
" Lopinavir and ritonavir pharmacokinetic parameter values were determined using noncompartmental methods, and preadministration and postadministration ginseng values were compared using a Student t test, where p<0."( Influence of Panax ginseng on the steady state pharmacokinetic profile of lopinavir-ritonavir in healthy volunteers.
Alfaro, RM; Calderón, MM; Chairez, CL; Gordon, LA; Kovacs, JA; Penzak, SR, 2014
)
1.54
" Intensive steady-state pharmacokinetic sampling was conducted after six doses."( Pharmacokinetics and safety of rifabutin in young HIV-infected children receiving rifabutin and lopinavir/ritonavir.
Gous, H; Kellermann, T; Kindra, G; McIlleron, H; Moultrie, H; Sawry, S; Van Rie, A; Wiesner, L, 2015
)
0.64
"Rifabutin dosed at 5 mg/kg three times per week resulted in lower AUC0-48, AUC0-24 and Cmax values for rifabutin and 25-O-desacetyl rifabutin compared with adults receiving 150 mg of rifabutin daily, the current recommended dose."( Pharmacokinetics and safety of rifabutin in young HIV-infected children receiving rifabutin and lopinavir/ritonavir.
Gous, H; Kellermann, T; Kindra, G; McIlleron, H; Moultrie, H; Sawry, S; Van Rie, A; Wiesner, L, 2015
)
0.64
"5 h for 20 mg group; the mean Cmax of last dose was 498 ± 54 ng/mL for 10 mg group and 897 ± 136 ng/mL for 20 mg group."( Pharmacokinetics of sifuvirtide in treatment-naive and treatment-experienced HIV-infected patients.
Che, J; Chen, X; Cheng, Y; Dong, T; Meng, Q; Qian, X; Tong, B, 2014
)
0.4
" But there are limited pharmacokinetic data evaluating the higher dose of rifabutin in combination with LPV/r."( Randomized pharmacokinetic evaluation of different rifabutin doses in African HIV- infected tuberculosis patients on lopinavir/ritonavir-based antiretroviral therapy.
Connolly, C; Harries, A; Kellerman, T; Lienhardt, C; McIlleron, H; Naiker, S; Pym, A; Reddy, T; Wiesner, L, 2014
)
0.61
" The median AUC0-48 and Cmax of rifabutin in patients taking 150 mg rifabutin tiw was significantly reduced compared to the other treatment arms."( Randomized pharmacokinetic evaluation of different rifabutin doses in African HIV- infected tuberculosis patients on lopinavir/ritonavir-based antiretroviral therapy.
Connolly, C; Harries, A; Kellerman, T; Lienhardt, C; McIlleron, H; Naiker, S; Pym, A; Reddy, T; Wiesner, L, 2014
)
0.61
" A compartmental pharmacokinetic (PK) model of LPV/r was developed, including a mechanistic description of competitive inhibition."( A pharmacokinetic model of lopinavir in combination with ritonavir in human.
Duangchaemkarn, K; Lohitnavy, M; Reisfeld, B, 2014
)
0.7
"To evaluate the pharmacokinetic profiles of lopinavir (LPV) in Chinese HIV-infected patients."( [Pharmacokinetic profiles of lopinavir (LPV) in Chinese HIV-infected patients].
Du, X; Fu, Q; Li, T; Liu, Z; Zhang, X, 2015
)
0.97
"A total of 16 patients were enrolled in the LPV pharmacokinetic study."( [Pharmacokinetic profiles of lopinavir (LPV) in Chinese HIV-infected patients].
Du, X; Fu, Q; Li, T; Liu, Z; Zhang, X, 2015
)
0.71
"The non-compartment model pharmacokinetic (PK) parameters were as follows: the peak time of LPV (T(max)) (3."( [Pharmacokinetic profiles of lopinavir (LPV) in Chinese HIV-infected patients].
Du, X; Fu, Q; Li, T; Liu, Z; Zhang, X, 2015
)
0.71
"The pharmacokinetic profiles of LPV in Chinese HIV-1 infected patients demonstrate lower C(min) than those of reported studies, while other parameters are similar."( [Pharmacokinetic profiles of lopinavir (LPV) in Chinese HIV-infected patients].
Du, X; Fu, Q; Li, T; Liu, Z; Zhang, X, 2015
)
0.71
"This study aimed to investigate the pharmacokinetic interactions between quinine and lopinavir boosted with ritonavir (LPV/r) in healthy Thai adults (8 males and 12 females)."( Pharmacokinetic Interactions Between Quinine and Lopinavir/Ritonavir in Healthy Thai Adults.
Cressey, TR; Kongjam, P; Na-Bangchang, K; Rattanapunya, S; Rueangweerayut, R; Tawon, Y, 2015
)
0.9
" The aim of the study was to investigate the pharmacokinetic interaction between the anti-malarial drugs, artesunate-mefloquine and the antiretroviral drug, lopinavir boosted with ritonavir (LPV/r)."( Pharmacokinetic interactions between artesunate-mefloquine and ritonavir-boosted lopinavir in healthy Thai adults.
Cressey, TR; Kongjam, P; Na-Bangchang, K; Rattanapunya, S; Rueangweerayut, R; Tawon, Y, 2015
)
0.84
"The study was an open-label, three-way, sequential, cross-over, pharmacokinetic study in healthy Thai adults."( Pharmacokinetic interactions between artesunate-mefloquine and ritonavir-boosted lopinavir in healthy Thai adults.
Cressey, TR; Kongjam, P; Na-Bangchang, K; Rattanapunya, S; Rueangweerayut, R; Tawon, Y, 2015
)
0.64
" We studied the effect of INH on LPV concentrations by administering INH for 7 days and performing intensive pharmacokinetic sampling in 16 human immunodeficiency virus infected patients established on LPV/r-based ART."( The pharmacokinetics of lopinavir/ritonavir when given with isoniazid in South African HIV-infected individuals.
Decloedt, EH; Maartens, G; McIlleron, H; van der Walt, JS; Wiesner, L, 2015
)
0.72
" We have compared non-compartmental analysis (NCA) and model-based predictions of DDIs for long half-life drugs by conducting simulation studies and reviewing published trials, using antituberculosis drug bedaquiline (BDQ) as a model compound."( Pharmacokinetic Interactions for Drugs with a Long Half-Life—Evidence for the Need of Model-Based Analysis.
Acharya, C; Clauson, B; Dooley, KE; Karlsson, MO; Svensson, EM, 2016
)
0.43
" We conducted a population pharmacokinetic analysis of lopinavir and ritonavir concentrations collected from 84 pregnant and 595 nonpregnant treatment-naive and -experienced HIV-1-infected subjects enrolled in six clinical studies."( No Need for Lopinavir Dose Adjustment during Pregnancy: a Population Pharmacokinetic and Exposure-Response Analysis in Pregnant and Nonpregnant HIV-Infected Subjects.
Jones, AK; Klein, CE; Nilius, AM; Patterson, KB; Salem, AH; Santini-Oliveira, M; Taylor, GP, 2016
)
1.06
"Open-label, single-sequence pharmacokinetic study."( Lack of an Effect of Ritonavir Alone and Lopinavir-Ritonavir on the Pharmacokinetics of Fenofibric Acid in Healthy Volunteers.
Alfaro, RM; Calderón, MM; Gordon, LA; Hadigan, C; Kovacs, JA; Malati, CY; McLaughlin, M; Penzak, SR, 2016
)
0.7
" Fenofibric acid pharmacokinetic parameter values were compared before and after concomitant ritonavir or lopinavir-ritonavir administration."( Lack of an Effect of Ritonavir Alone and Lopinavir-Ritonavir on the Pharmacokinetics of Fenofibric Acid in Healthy Volunteers.
Alfaro, RM; Calderón, MM; Gordon, LA; Hadigan, C; Kovacs, JA; Malati, CY; McLaughlin, M; Penzak, SR, 2016
)
0.91
"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
)
0.64
"Linear regression equations describing the relationships of lopinavir peak and trough concentrations to lopinavir AUC values were established using pharmacokinetic data from published studies of patients or healthy subjects receiving lopinavir and ritonavir at standard dosages."( Prediction of area under the concentration-time curve for lopinavir from peak or trough lopinavir concentrations in patients receiving lopinavir-ritonavir therapy.
Srinivas, NR, 2016
)
0.92
" Here we present a population pharmacokinetic model to describe the longitudinal change of unbound lopinavir/ritonavir (LPV/RTV) PK parameters with gestational age, and to predict unbound LPV concentrations under different dosing regimens."( Model-Based Analysis of Unbound Lopinavir Pharmacokinetics in HIV-Infected Pregnant Women Supports Standard Dosing in the Third Trimester.
Chen, J; Dumond, JB; Malone, S; Patterson, KB; Prince, HM, 2016
)
0.93
" Here we aimed to quantify nevirapine and LPV/r drug-drug interaction effects on bedaquiline and M2 in patients co-infected with HIV and multidrug-resistant tuberculosis (MDR-TB) using population pharmacokinetic (PK) analysis and compare these with model-based predictions from single-dose studies in subjects without TB."( Confirming model-predicted pharmacokinetic interactions between bedaquiline and lopinavir/ritonavir or nevirapine in patients with HIV and drug-resistant tuberculosis.
Brill, MJ; Karlsson, MO; Maartens, G; Pandie, M; Svensson, EM, 2017
)
0.68
" The overall objective of this project was to develop separate physiologically based pharmacokinetic (PBPK) substrate models for the protease inhibitors darunavir and lopinavir."( Physiologically Based Pharmacokinetic Modeling for Predicting the Effect of Intrinsic and Extrinsic Factors on Darunavir or Lopinavir Exposure Coadministered With Ritonavir.
Arya, V; Au, S; Mullick, C; Struble, K; Wagner, C; Zhao, P, 2017
)
0.86
"To develop a population pharmacokinetic model and identify sources of variability, genetic and nongenetic factors, of tenofovir."( Pharmacogenetics-based population pharmacokinetic analysis of tenofovir in Thai HIV-infected patients.
Avihingsanon, A; Burger, DM; Mitruk, S; Punyawudho, B; Rungtivasuwan, K; Ruxrungtham, K; Sukasem, C; Thammajaruk, N, 2017
)
0.46
" A nonlinear mixed effects model was used to develop the population pharmacokinetic model and investigate the influence of these polymorphisms and other patient specific covariates on the pharmacokinetics of tenofovir."( Pharmacogenetics-based population pharmacokinetic analysis of tenofovir in Thai HIV-infected patients.
Avihingsanon, A; Burger, DM; Mitruk, S; Punyawudho, B; Rungtivasuwan, K; Ruxrungtham, K; Sukasem, C; Thammajaruk, N, 2017
)
0.46
" A combined population pharmacokinetic model was developed to jointly describe the pharmacokinetics of lopinavir and ritonavir in 32 HIV-infected children (16 with MDR-TB receiving treatment with combinations of high-dose isoniazid, pyrazinamide, ethambutol, ethionamide, terizidone, a fluoroquinolone, and amikacin and 16 without TB) who were established on a lopinavir-ritonavir-containing antiretroviral regimen."( Pharmacokinetics and Drug-Drug Interactions of Lopinavir-Ritonavir Administered with First- and Second-Line Antituberculosis Drugs in HIV-Infected Children Treated for Multidrug-Resistant Tuberculosis.
de Kock, M; Denti, P; Garcia-Prats, AJ; Hesseling, AC; McIlleron, H; Norman, J; Schaaf, HS; Tikiso, T; van der Laan, LE; Wiesner, L; Winckler, J, 2018
)
0.95
" Covariates were screened to assess their influence on the pharmacokinetics of LPV, and the relationship between pharmacokinetic variability and treatment outcomes were assessed."( Population Pharmacokinetics of Lopinavir in Severely Malnourished HIV-infected Children and the Effect on Treatment Outcomes.
Archary, M; Bobat, R; Hennig, S; La Russa, P; Mcllleron, H; Sibaya, T; Wiesner, L, 2018
)
0.77
" Pharmacokinetic exposure did not correlate with virologic outcomes or death at 12 or 48 weeks."( Population Pharmacokinetics of Lopinavir in Severely Malnourished HIV-infected Children and the Effect on Treatment Outcomes.
Archary, M; Bobat, R; Hennig, S; La Russa, P; Mcllleron, H; Sibaya, T; Wiesner, L, 2018
)
0.77
" To provide insights into the complex mechanisms of absorption and disposition of TLC-ART101, we constructed novel mechanism-based pharmacokinetic (MBPK) models."( Mechanism-based pharmacokinetic (MBPK) models describe the complex plasma kinetics of three antiretrovirals delivered by a long-acting anti-HIV drug combination nanoparticle formulation.
Collier, AC; Collins, C; Ho, RJY; Kinman, L; Koehn, J; Kraft, JC; McConnachie, LA; Shen, DD; Sun, J, 2018
)
0.48
"To evaluate the proportion of children with lopinavir Cmin ≥1 mg/L when receiving a novel 8-hourly lopinavir/ritonavir dosing strategy during rifampicin co-treatment."( Pharmacokinetics of adjusted-dose 8-hourly lopinavir/ritonavir in HIV-infected children co-treated with rifampicin.
McIlleron, H; Rabie, H; Rawizza, H; Van Rie, A; Wiesner, L; Winckler, J; Zar, H; Zuidewind, P, 2019
)
1.04
"HIV-infected children on lopinavir/ritonavir and rifampicin were enrolled in a prospective pharmacokinetic study."( Pharmacokinetics of adjusted-dose 8-hourly lopinavir/ritonavir in HIV-infected children co-treated with rifampicin.
McIlleron, H; Rabie, H; Rawizza, H; Van Rie, A; Wiesner, L; Winckler, J; Zar, H; Zuidewind, P, 2019
)
1.08
"A population pharmacokinetic (PopPK) model for pretomanid was developed using data from 14 studies in the pretomanid development program: six phase 1 studies, six phase 2 studies, and two phase 3 studies."( Population Pharmacokinetics of the Antituberculosis Agent Pretomanid.
Everitt, D; Nedelman, JR; Salinger, DH; Subramoney, V, 2019
)
0.51
" The objective of the study was to apply physiologically-based pharmacokinetic (PBPK) modeling to predict optimal dosage regimens of quinine when coadministered with lopinavir/ritonavir in malaria and HIV coinfected patients with different conditions."( Physiologically-Based Pharmacokinetic Modeling for Optimal Dosage Prediction of Quinine Coadministered With Ritonavir-Boosted Lopinavir.
Karbwang, J; Na-Bangchang, K; Rajoli, RKR; Saeheng, T; Siccardi, M, 2020
)
0.96
"To evaluate the safety and pharmacokinetic profile of adjusted doses of darunavir/ritonavir with rifampicin."( Pharmacokinetic profile and safety of adjusted doses of darunavir/ritonavir with rifampicin in people living with HIV.
Ebrahim, I; Maartens, G; McIlleron, H; Orrell, C; Smythe, W; Wiesner, L, 2020
)
0.56
" Therefore, an intravenous study of TLC-ART 101 in nonhuman primates was conducted to elucidate the degree of association of drugs in vivo, estimate subcutaneous bioavailability, and refine a mechanism-based pharmacokinetic (MBPK2) model."( Integration of Computational and Experimental Approaches to Elucidate Mechanisms of First-Pass Lymphatic Drug Sequestration and Long-Acting Pharmacokinetics of the Injectable Triple-HIV Drug Combination TLC-ART 101.
Collier, AC; Ho, RJY; Kinman, L; Koehn, J; Lane, S; Lee, W; McConnachie, LA; Perazzolo, S; Shen, DD; Shireman, LM, 2020
)
0.56
" A population pharmacokinetic meta-analysis was conducted using individual participant data from 10 studies with 6,100 lumefantrine concentrations from 793 nonpregnant adult participants (41% HIV-malaria-coinfected, 36% malaria-infected, 20% HIV-infected, and 3% healthy volunteers)."( An Individual Participant Data Population Pharmacokinetic Meta-analysis of Drug-Drug Interactions between Lumefantrine and Commonly Used Antiretroviral Treatment.
Aweeka, FT; Barnes, KI; Byakika-Kibwika, P; Bygbjerg, IC; Chijioke-Nwauche, I; Denti, P; Francis, J; Hoglund, RM; Khoo, SH; Kredo, T; Lamorde, M; Lemnge, MM; Merry, C; Nyagonde, N; Parikh, S; Scarsi, KK; Sutherland, CJ; Tarning, J; Vestergaard, LS; Walimbwa, SI; Workman, L, 2020
)
0.56
"This study aimed to assess the pharmacokinetic profile of 150 mg rifabutin (RBT) taken every other day (every 48 h) versus 300 mg RBT taken every other day (E."( Pharmacokinetic study of two different rifabutin doses co-administered with lopinavir/ritonavir in African HIV and tuberculosis co-infected adult patients.
Cisse, K; Compaoré, TR; Diagbouga, S; Kouanda, S; Matteelli, A; Ouedraogo, HG; Regazzi, M; Roggi, A; Sangare, L; Simporé, J; Sulis, G; Tarnagda, G; Villani, P, 2020
)
0.79
" Lopinavir and ritonavir pharmacokinetic parameters were determined after an intensive pharmacokinetic analysis."( Pharmacokinetics of lopinavir/ritonavir oral solution to treat COVID-19 in mechanically ventilated ICU patients.
Bouadma, L; de Montmollin, E; Descamps, D; Jaquet, P; Kauv, J; Laouénan, C; Le Hingrat, Q; Lê, MP; Patrier, J; Peytavin, G; Sonneville, R; Timsit, JF; Veyrier, M; Visseaux, B; Wicky, PH, 2020
)
1.79
" After the dose reduction to 400/100 mg q24h, lopinavir/ritonavir pharmacokinetic parameters were assessed in nine patients."( Pharmacokinetics of lopinavir/ritonavir oral solution to treat COVID-19 in mechanically ventilated ICU patients.
Bouadma, L; de Montmollin, E; Descamps, D; Jaquet, P; Kauv, J; Laouénan, C; Le Hingrat, Q; Lê, MP; Patrier, J; Peytavin, G; Sonneville, R; Timsit, JF; Veyrier, M; Visseaux, B; Wicky, PH, 2020
)
1.14
" However, it remains difficult to safely recommend its dose reduction without compromising the benefit of the antiviral strategy, and careful pharmacokinetic and toxicity monitoring are needed."( Pharmacokinetics of lopinavir/ritonavir oral solution to treat COVID-19 in mechanically ventilated ICU patients.
Bouadma, L; de Montmollin, E; Descamps, D; Jaquet, P; Kauv, J; Laouénan, C; Le Hingrat, Q; Lê, MP; Patrier, J; Peytavin, G; Sonneville, R; Timsit, JF; Veyrier, M; Visseaux, B; Wicky, PH, 2020
)
0.88
" This study evaluated S-warfarin limited sampling strategy with a population pharmacokinetic (PK) approach to estimate CYP2C9 activity in healthy adults."( S-warfarin limited sampling strategy with a population pharmacokinetic approach to estimate exposure and cytochrome P450 (CYP) 2C9 activity in healthy adults.
Bertino, JS; Capparelli, EV; Kashuba, ADM; Ma, JD; Nafziger, AN; Nikanjam, M; Tran, L; Turpault, S, 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
)
0.82
" Pooled LPV AUC12 (157 203 hours × ng/mL) and Ctrough (9876 ng/mL) were similar to historical controls; RBT AUC24 (7374 hours × ng/mL) and Ctrough (208 ng/mL) were higher, although 3 participants in arm C had RBT Cmax <250 ng/mL."( Safety and Pharmacokinetics of Double-Dose Lopinavir/Ritonavir + Rifampin Versus Lopinavir/Ritonavir + Daily Rifabutin for Treatment of Human Immunodeficiency Virus-Tuberculosis Coinfection.
Benson, CA; Cardoso, SW; Fletcher, CV; Ive, P; Kendall, MA; Lalloo, U; Podany, AT; Wu, X, 2021
)
0.88
" Faster RBT clearance and low Cmax in 3 participants on RBT+RAL requires further study."( Safety and Pharmacokinetics of Double-Dose Lopinavir/Ritonavir + Rifampin Versus Lopinavir/Ritonavir + Daily Rifabutin for Treatment of Human Immunodeficiency Virus-Tuberculosis Coinfection.
Benson, CA; Cardoso, SW; Fletcher, CV; Ive, P; Kendall, MA; Lalloo, U; Podany, AT; Wu, X, 2021
)
0.88
" We used physiologically-based pharmacokinetic (PBPK) modeling to simulate the effect of inflammation on the pharmacokinetics of CYP3A metabolized drugs."( Physiologically Based Pharmacokinetic Modelling to Investigate the Impact of the Cytokine Storm on CYP3A Drug Pharmacokinetics in COVID-19 Patients.
Battegay, M; Marzolini, C; Sendi, P; Stader, F, 2022
)
0.72
"We previously developed a mechanism-based pharmacokinetic (MBPK) model to characterize the PK of a lymphocyte-targeted, long-acting 3 HIV drug-combination nanoparticle (DcNP) formulation of lopinavir, ritonavir, and tenofovir."( Physiologically Based Pharmacokinetic Modeling of 3 HIV Drugs in Combination and the Role of Lymphatic System after Subcutaneous Dosing. Part 2: Model for the Drug-combination Nanoparticles.
Ho, RJY; Perazzolo, S; Shen, DD, 2022
)
0.91
" In stage 1, term neonates exposed to HIV on standard antiretroviral prophylaxis (nevirapine ± zidovudine) received single dose(s) of the 4-in-1 formulation, followed by intensive pharmacokinetic sampling and safety assessments."( Pharmacokinetics and Safety of the Abacavir/Lamivudine/Lopinavir/Ritonavir Fixed-Dose Granule Formulation (4-in-1) in Neonates: PETITE Study.
Andrieux-Meyer, I; Bekker, A; Capparelli, E; Cotton, MF; Cressey, R; Cressey, TR; du Toit, S; Groenewald, M; Kumar, M; Lallemant, M; Nielsen, J; Rabie, H; Salvadori, N; Than-In-At, K, 2022
)
0.97
"Sixteen neonates, with a median (range) birth weight of 3130 g (2790-3590 g), completed 24 pharmacokinetic visits."( Pharmacokinetics and Safety of the Abacavir/Lamivudine/Lopinavir/Ritonavir Fixed-Dose Granule Formulation (4-in-1) in Neonates: PETITE Study.
Andrieux-Meyer, I; Bekker, A; Capparelli, E; Cotton, MF; Cressey, R; Cressey, TR; du Toit, S; Groenewald, M; Kumar, M; Lallemant, M; Nielsen, J; Rabie, H; Salvadori, N; Than-In-At, K, 2022
)
0.97
"Physiologically based pharmacokinetic (PBPK) models have gained in popularity in the last decade in both drug development and regulatory science."( A Comparative Analysis of Physiologically Based Pharmacokinetic Models for Human Immunodeficiency Virus and Tuberculosis Infections.
Jacobs, BA; Mtshali, S, 2022
)
0.72
"Therapy failure caused by complex population-drug-drug (PDDI) interactions including CYP3A4 can be predicted using mechanistic physiologically-based pharmacokinetic (PBPK) modeling."( The investigation of the complex population-drug-drug interaction between ritonavir-boosted lopinavir and chloroquine or ivermectin using physiologically-based pharmacokinetic modeling.
Alsmadi, MM, 2023
)
1.13
" This study aimed to develop a population pharmacokinetic model of LPV/r and provide dosage optimization in Thai PLWH."( Dose optimization with population pharmacokinetics of ritonavir-boosted lopinavir for Thai people living with HIV with and without active tuberculosis.
Avihingsanon, A; Chaivichacharn, P; Gatechompol, S; Punyawudho, B; Ubolyam, S, 2022
)
0.95
"The population pharmacokinetic model was developed by integrating the interaction between LPV and RTV."( Dose optimization with population pharmacokinetics of ritonavir-boosted lopinavir for Thai people living with HIV with and without active tuberculosis.
Avihingsanon, A; Chaivichacharn, P; Gatechompol, S; Punyawudho, B; Ubolyam, S, 2022
)
0.95
" This study compared the bioequivalence and safety of 2 lopinavir/ritonavir (200/50 mg) formulations under fasted and fed conditions in healthy Chinese volunteers and compared the pharmacokinetic parameters of lopinavir and ritonavir."( Pharmacokinetics, Safety, and Bioequivalence of 2 Lopinavir/Ritonavir (200/50 mg) Tablets in Healthy Chinese Volunteers: Effect of Food on Absorption.
Bao, D; Fu, W; Hu, W; Lin, L; Liu, Y; Zhang, Q; Zhang, W; Zheng, L, 2023
)
1.41
" At steady state, 8-9 blood samples were taken to construct pharmacokinetic curves."( First Pharmacokinetic Data of Tenofovir Alafenamide Fumarate and Tenofovir With Dolutegravir or Boosted Protease Inhibitors in African Children: A Substudy of the CHAPAS-4 Trial.
Bamford, A; Burger, DM; Bwakura-Dangarembizi, M; Chabala, C; Colbers, A; Denti, P; Doerholt, K; Gibb, DM; Griffiths, AL; Makumbi, S; McIlleron, HM; Monkiewicz, LN; Mulenga, V; Mumbiro, V; Musiime, V; Nangiya, J; Szubert, AJ; Waalewijn, H; Wasmann, RE; Wiesner, L, 2023
)
0.91
" For each combination, tenofovir GM (CV%) AUCtau and Cmax remained below reference values in adults taking 25 mg TAF with a boosted protease inhibitors."( First Pharmacokinetic Data of Tenofovir Alafenamide Fumarate and Tenofovir With Dolutegravir or Boosted Protease Inhibitors in African Children: A Substudy of the CHAPAS-4 Trial.
Bamford, A; Burger, DM; Bwakura-Dangarembizi, M; Chabala, C; Colbers, A; Denti, P; Doerholt, K; Gibb, DM; Griffiths, AL; Makumbi, S; McIlleron, HM; Monkiewicz, LN; Mulenga, V; Mumbiro, V; Musiime, V; Nangiya, J; Szubert, AJ; Waalewijn, H; Wasmann, RE; Wiesner, L, 2023
)
0.91
" The present analysis aims to evaluate LPV levels in individuals exposed to SARS-CoV-2 versus people living with HIV (PLWH) by developing a population pharmacokinetic (popPK) model, while characterizing external and patient-related factors that might affect LPV exposure along with dose-response association."( Population pharmacokinetic analysis of lopinavir in HIV negative individuals exposed to SARS-CoV-2: a COPEP (COronavirus Post-Exposure Prophylaxis) sub-study.
Andre, P; Buclin, T; Calmy, A; Decosterd, LA; Delfraysse, M; Fedeli, C; Guidi, M; Thoueille, P; Ustero, P, 2023
)
1.18

Compound-Compound Interactions

The KLEAN study extension assessed the long-term efficacy and safety of fosamprenavir-ritonavir (FPV/r) and lopinavirs (LPV) Both are administered with abacavir/lamivudine (ABC/3TC) fix.

ExcerptReferenceRelevance
"0 microM) were marginal and are not likely to produce clinically significant drug-drug interactions."( Potent inhibition of the cytochrome P-450 3A-mediated human liver microsomal metabolism of a novel HIV protease inhibitor by ritonavir: A positive drug-drug interaction.
Dykstra, J; Granneman, GR; Hickman, D; Jayanti, VK; Kumar, GN; Roberts, EM; Surber, B; Thomas, S; Uchic, J; Yao, Y, 1999
)
0.3
"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
)
0.81
"We describe a drug-drug interaction between coformulated lopinavir/ritonavir and itraconazole in a patient infected with human immunodeficiency virus type 1 who had disseminated histoplasmosis."( Drug-drug interaction between itraconazole and the antiretroviral drug lopinavir/ritonavir in an HIV-1-infected patient with disseminated histoplasmosis.
Beijnen, JH; Crommentuyn, KM; Huitema, AD; Mulder, JW; Schellens, JH; Sparidans, RW, 2004
)
0.8
" In the present study, two adjusted-dose regimens of lopinavir-ritonavir were tested in combination with rifampin."( Pharmacokinetics of adjusted-dose lopinavir-ritonavir combined with rifampin in healthy volunteers.
Bertz, R; Boeree, MJ; Burger, DM; Colbers, EP; Hekster, YA; Koopmans, PP; la Porte, CJ; Voncken, DS; Wikstrom, K, 2004
)
0.85
" The tissue distribution of radioactivity was examined in rats dosed with [14C]lopinavir in combination with ritonavir."( Metabolism and disposition of the HIV-1 protease inhibitor lopinavir (ABT-378) given in combination with ritonavir in rats, dogs, and humans.
Denissen, JF; Grabowski, BA; Jayanti, VK; Johnson, MK; Kempf, DJ; Kumar, GN; Lee, RD; Marsh, KC; Roberts, SA; Sham, HL; Sun, E; Thomas, S; Uchic, J, 2004
)
0.79
"To develop a population pharmacokinetic model for lopinavir in combination with ritonavir, in which the interaction between both drugs was characterized, and in which relationships between patient characteristics and pharmacokinetics were identified."( Population pharmacokinetics of lopinavir in combination with ritonavir in HIV-1-infected patients.
Beijnen, JH; Crommentuyn, KM; Huitema, AD; Kappelhoff, BS; Mairuhu, AT; Meenhorst, PL; Mulder, JW; van Gorp, EC, 2005
)
0.87
" Fosamprenavir-ritonavir has shown similar efficacy and safety to lopinavir-ritonavir when each is combined with two nucleoside reverse transcriptase inhibitors."( The KLEAN study of fosamprenavir-ritonavir versus lopinavir-ritonavir, each in combination with abacavir-lamivudine, for initial treatment of HIV infection over 48 weeks: a randomised non-inferiority trial.
DeJesus, E; Eron, J; Estrada, V; Gathe, J; Katlama, C; Lackey, P; Patel, L; Shaefer, M; Staszewski, S; Sutherland-Phillips, D; Vavro, C; Wannamaker, P; Yau, L; Yeni, P; Yeo, J; Young, B, 2006
)
0.82
"Fosamprenavir-ritonavir twice daily in treatment-naive patients provides similar antiviral efficacy, safety, tolerability, and emergence of resistance as lopinavir-ritonavir, each in combination with abacavir-lamivudine."( The KLEAN study of fosamprenavir-ritonavir versus lopinavir-ritonavir, each in combination with abacavir-lamivudine, for initial treatment of HIV infection over 48 weeks: a randomised non-inferiority trial.
DeJesus, E; Eron, J; Estrada, V; Gathe, J; Katlama, C; Lackey, P; Patel, L; Shaefer, M; Staszewski, S; Sutherland-Phillips, D; Vavro, C; Wannamaker, P; Yau, L; Yeni, P; Yeo, J; Young, B, 2006
)
0.78
" Together, these in vitro results indicate that combination with other antiretrovirals does not significantly increase the toxic potential of TFV in RPTECs."( In vitro cytotoxicity and mitochondrial toxicity of tenofovir alone and in combination with other antiretrovirals in human renal proximal tubule cells.
Alvarez, ML; Cihlar, T; Cordobilla, B; Domingo, JC; Domingo, P; Giralt, M; Guallar, J; López-Dupla, M; Sánchez de la Rosa, R; Saumoy, M; Torres, F; Vidal, F; Villarroya, F, 2006
)
0.33
" When brecanavir was tested in combination with nucleoside reverse transcriptase inhibitors, the antiviral activity of brecanavir was synergistic with the effects of stavudine and additive to the effects of zidovudine, tenofovir, dideoxycytidine, didanosine, adefovir, abacavir, lamivudine, and emtricitabine."( In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV.
Boone, L; Craig, C; Ferris, R; Furfine, E; Griffin, P; Hale, M; Hanlon, M; Harvey, R; Hazen, R; Kaldor, I; Miller, J; Ray, J; Samano, V; Spaltenstein, A; St Clair, M; Tung, R; Yates, P, 2007
)
0.34
"Our objective was to identify possible differences in protease inhibitor plasma concentrations between and within three protease inhibitor regimens (indinavir, saquinavir and lopinavir all in combination with low-dose ritonavir) and to relate these differences to safety and efficacy."( Pharmacokinetics of two randomized trials evaluating the safety and efficacy of indinavir, saquinavir and lopinavir in combination with low-dose ritonavir: the MaxCmin1 and 2 trials.
Cahn, P; Castagna, A; Clumeck, N; Dragsted, UB; Fox, Z; Gerstoft, J; Justesen, US; Losso, M; Lundgren, JD; Obel, N; Pedersen, C; Peters, B, 2007
)
0.75
"7-fold in combination with lopinavir/ritonavir."( Drug/Drug interaction between lopinavir/ritonavir and rosuvastatin in healthy volunteers.
Flynn, DM; Gerber, JG; Hoody, DW; Kiser, JJ; Predhomme, JA; Wolfe, P, 2008
)
0.93
"HIV-1-infected men enrolled in the Monark randomized trial were eligible for the present study after 48 weeks of a first-line lopinavir/ritonavir alone or in combination with zidovudine and lamivudine."( Absence of HIV-1 shedding in male genital tract after 1 year of first-line lopinavir/ritonavir alone or in combination with zidovudine/lamivudine.
Bresson, JL; Chaix, ML; Cohen-Codar, I; Delfraissy, JF; Galimand, J; Ghosn, J; Girard, PM; Peytavin, G; Raffi, F; Rouzioux, C, 2008
)
0.78
" Patients with HIV may also have simultaneous chronic medical conditions, resulting in the possibility of complex drug-drug interactions."( Possible antiretroviral therapy-warfarin drug interaction.
Fulco, PP; Higginson, RT; Zingone, MM, 2008
)
0.35
"In this open-label, international non-inferiority study, 883 antiretroviral-naive, HIV-1-infected patients were randomly assigned to receive atazanavir/ritonavir 300/100 mg once daily (n=440) or lopinavir/ritonavir 400/100 mg twice daily (n=443), in combination with fixed-dose tenofovir/emtricitabine 300/200 mg once daily."( Once-daily atazanavir/ritonavir versus twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 48 week efficacy and safety results of the CASTLE study.
Andrade-Villanueva, J; Chetchotisakd, P; Corral, J; David, N; Echevarria, J; Mancini, M; McGrath, D; Molina, JM; Moyle, G; Percival, L; Thiry, A; Yang, R, 2008
)
0.79
" 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
"A total of 191 patients were randomized 2:2:2:1 to one of three APL dosing regimens or to lamivudine (3TC)/zidovudine (ZDV) twice daily (bid), each in combination with lopinavir/ritonavir (LPV/r) 400 mg/100 mg bid."( Antiviral activity and safety of aplaviroc, a CCR5 antagonist, in combination with lopinavir/ritonavir in HIV-infected, therapy-naïve patients: results of the EPIC study (CCR100136).
Adkison, KK; Berger, D; Bonny, T; Cimoch, P; Lamarca, A; Lazzarin, A; Madison, SJ; McCarty, D; Millard, J; Nichols, WG; Salvato, P; Smaill, FM; Teofilo, E; Yeni, P, 2009
)
0.77
"The KLEAN study extension assessed the long-term efficacy and safety of fosamprenavir-ritonavir (FPV/r) and lopinavir-ritonavir (LPV/r), both administered with abacavir/lamivudine (ABC/3TC) fixed dose combination, over 144 weeks."( Long-term efficacy and safety of fosamprenavir plus ritonavir versus lopinavir/ritonavir in combination with abacavir/lamivudine over 144 weeks.
Baril, JG; Duiculescu, D; Estrada, V; Lim, ML; Logue, K; Pharo, C; Plettenberg, A; Pulido, F; Schewe, K; Vavro, C; Yau, L,
)
0.58
"The findings of the KLEAN study extension (48 to 144 weeks) support durable viral suppression with both FPV/r and LPV/r treatment regimens when used in combination with ABC/3TC irrespective of viral load at baseline."( Long-term efficacy and safety of fosamprenavir plus ritonavir versus lopinavir/ritonavir in combination with abacavir/lamivudine over 144 weeks.
Baril, JG; Duiculescu, D; Estrada, V; Lim, ML; Logue, K; Pharo, C; Plettenberg, A; Pulido, F; Schewe, K; Vavro, C; Yau, L,
)
0.37
"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
)
0.84
"International, multicenter, open-label, 96-week noninferiority randomized trial of atazanavir/ritonavir 300/100 mg once daily vs lopinavir/ritonavir 400/100 mg twice daily, each in combination with fixed-dose tenofovir/emtricitabine 300/200 mg once daily, in antiretroviral-naive, HIV-1-infected patients."( Once-daily atazanavir/ritonavir compared with twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 96-week efficacy and safety results of the CASTLE study.
Absalon, J; Andrade-Villanueva, J; Chetchotisakd, P; Corral, J; David, N; Echevarria, J; Lataillade, M; Mancini, M; McGrath, D; Molina, JM; Moyle, G; Percival, L; Wirtz, V; Yang, R, 2010
)
0.81
"Increasing the ritonavir dose to achieve a lopinavir/ritonavir ratio of 1:1 when given in combination with rifampicin-based TB treatment did not completely compensate for the enhancement of lopinavir CL/F caused by rifampicin."( Population pharmacokinetics of lopinavir in combination with rifampicin-based antitubercular treatment in HIV-infected South African children.
Elsherbiny, D; Maartens, G; McIlleron, H; Ren, Y; Simonsson, US, 2010
)
0.91
" 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
)
1.17
" The aim of this study was to develop an integrated population pharmacokinetic model accounting for the drug-drug interactions between lopinavir, ritonavir and rifampicin, and to evaluate optimal doses of lopinavir/ritonavir when co-administered with rifampicin."( Model-based approach to dose optimization of lopinavir/ritonavir when co-administered with rifampicin.
Decloedt, E; Denti, P; Karlsson, MO; Maartens, G; McIlleron, H; Simonsson, US; Zhang, C, 2012
)
0.84
"The model describes the drug-drug interactions between lopinavir, ritonavir and rifampicin in adults."( Model-based approach to dose optimization of lopinavir/ritonavir when co-administered with rifampicin.
Decloedt, E; Denti, P; Karlsson, MO; Maartens, G; McIlleron, H; Simonsson, US; Zhang, C, 2012
)
0.89
" Mean plasma concentration-time profiles for atazanavir, tenofovir disoproxil fumarate/emtricitabine (TDF/FTC), darunavir (DRV, administered with ritonavir [RTV]), and drospirenone/ethinylestradiol were similar following co-administration of GSK2248761."( Drug interaction profile for GSK2248761, a next generation non-nucleoside reverse transcriptase inhibitor.
de Serres, M; Gould, E; Johnson, M; Kim, J; Lou, Y; Mayers, D; Pietropaolo, K; Piscitelli, S; White, S; Zhou, XJ, 2012
)
0.38
"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
)
0.8
" As adult studies cannot reliably predict their magnitude in children, drug-drug interactions should be evaluated in paediatric patient populations."( Model-based evaluation of the pharmacokinetic differences between adults and children for lopinavir and ritonavir in combination with rifampicin.
Decloedt, EH; Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Zhang, C, 2013
)
0.61
" The objective of this study was to compare changes in body composition between ritonavir-boosted atazanavir (ATV/r) and ritonavir-boosted lopinavir (LPV/r) over 96 weeks using data from a substudy of CASTLE, which compared once-daily ATV/r with twice-daily LPV/r, both in combination with tenofovir disoproxil fumarate/emtricitabine in treatment-naïve patients with HIV-1 infection."( Comparison of body composition changes between atazanavir/ritonavir and lopinavir/ritonavir each in combination with tenofovir/emtricitabine in antiretroviral-naïve patients with HIV-1 infection.
DeGrosky, M; Farajallah, A; Hardy, H; McGrath, D; Moyle, GJ, 2014
)
0.84
"We conducted an open-label, steady-state pharmacokinetic (PK) study of drug-drug interactions between depot medroxyprogesterone acetate (DMPA) and twice-daily lopinavir (LPV) plus low-dose ritonavir (RTV) (LPV/r) among 24 HIV-infected women and compared the results to those for HIV-infected women receiving DMPA while on no antiretroviral therapy or on nucleosides only (n = 14 subjects from the control arm of AIDS Clinical Trials Group [ACTG] study 5093)."( Depot medroxyprogesterone acetate in combination with a twice-daily lopinavir-ritonavir-based regimen in HIV-infected women showed effective contraception and a lack of clinically significant interactions, with good safety and tolerability: results of the
Aweeka, F; Cohn, SE; Cramer, Y; Klingman, KL; Livingston, E; Luque, AE; Park, JG; Watts, DH; Weinberg, A, 2015
)
0.85
" Single-dose drug-drug interaction studies found no significant interactions with nevirapine or lopinavir/ritonavir, but these findings could be misleading, especially because of bedaquiline's long terminal t1/2."( Drug-drug interactions between bedaquiline and the antiretrovirals lopinavir/ritonavir and nevirapine in HIV-infected patients with drug-resistant TB.
Conradie, F; Hughes, J; Maartens, G; McIlleron, H; Pandie, M; Siwendu, S; Variava, E; Wiesner, L, 2016
)
0.89
" We describe the pharmacokinetics of and potential drug-drug interactions between lopinavir-ritonavir and drugs routinely used for MDR-TB treatment in HIV-infected children."( Pharmacokinetics and Drug-Drug Interactions of Lopinavir-Ritonavir Administered with First- and Second-Line Antituberculosis Drugs in HIV-Infected Children Treated for Multidrug-Resistant Tuberculosis.
de Kock, M; Denti, P; Garcia-Prats, AJ; Hesseling, AC; McIlleron, H; Norman, J; Schaaf, HS; Tikiso, T; van der Laan, LE; Wiesner, L; Winckler, J, 2018
)
0.96
"To assess the potential of second-generation proteasome inhibition by carfilzomib and its combination with the human immunodeficiency virus (HIV) protease inhibitors (HIV-PIs) lopinavir and nelfinavir in vitro for improved treatment of clear cell renal cell cancer (ccRCC)."( Improving the efficacy of proteasome inhibitors in the treatment of renal cell carcinoma by combination with the human immunodeficiency virus (HIV)-protease inhibitors lopinavir or nelfinavir.
Abt, D; Bader, J; Besse, A; Besse, L; Driessen, C; Engeler, DS; Kraus, M; Schmid, HP; Sedlarikova, L; Silzle, T; Slaby, O; Vodinska, M, 2018
)
0.87
" A single subcutaneous (SC) injection of this first-generation formulation of drug combination nanoparticles (DcNPs), named TLC-ART101, provided persistent ARV levels in macaque lymph node mononuclear cells (LNMCs) for at least 1 week, and in peripheral blood mononuclear cells (PBMCs) and plasma for at least 2 weeks, demonstrating long-acting pharmacokinetics for all three drugs."( Mechanism-based pharmacokinetic (MBPK) models describe the complex plasma kinetics of three antiretrovirals delivered by a long-acting anti-HIV drug combination nanoparticle formulation.
Collier, AC; Collins, C; Ho, RJY; Kinman, L; Koehn, J; Kraft, JC; McConnachie, LA; Shen, DD; Sun, J, 2018
)
0.48
"The coformulated lopinavir/ritonavir significantly reduces quinine concentration in healthy volunteers due to potential drug-drug interactions (DDIs)."( Physiologically-Based Pharmacokinetic Modeling for Optimal Dosage Prediction of Quinine Coadministered With Ritonavir-Boosted Lopinavir.
Karbwang, J; Na-Bangchang, K; Rajoli, RKR; Saeheng, T; Siccardi, M, 2020
)
1.1
"TLC-ART101 is a long-acting triple-HIV drug combination of lopinavir-ritonavir-tenofovir in one nanosuspension intended for subcutaneous injection."( Integration of Computational and Experimental Approaches to Elucidate Mechanisms of First-Pass Lymphatic Drug Sequestration and Long-Acting Pharmacokinetics of the Injectable Triple-HIV Drug Combination TLC-ART 101.
Collier, AC; Ho, RJY; Kinman, L; Koehn, J; Lane, S; Lee, W; McConnachie, LA; Perazzolo, S; Shen, DD; Shireman, LM, 2020
)
0.8
"Treating malaria in HIV-coinfected individuals should consider potential drug-drug interactions."( An Individual Participant Data Population Pharmacokinetic Meta-analysis of Drug-Drug Interactions between Lumefantrine and Commonly Used Antiretroviral Treatment.
Aweeka, FT; Barnes, KI; Byakika-Kibwika, P; Bygbjerg, IC; Chijioke-Nwauche, I; Denti, P; Francis, J; Hoglund, RM; Khoo, SH; Kredo, T; Lamorde, M; Lemnge, MM; Merry, C; Nyagonde, N; Parikh, S; Scarsi, KK; Sutherland, CJ; Tarning, J; Vestergaard, LS; Walimbwa, SI; Workman, L, 2020
)
0.56
"D), both in combination with lopinavir/ritonavir (LPV/r), in adult patients with human immunodeficiency virus (HIV) and tuberculosis (TB) co-infection."( Pharmacokinetic study of two different rifabutin doses co-administered with lopinavir/ritonavir in African HIV and tuberculosis co-infected adult patients.
Cisse, K; Compaoré, TR; Diagbouga, S; Kouanda, S; Matteelli, A; Ouedraogo, HG; Regazzi, M; Roggi, A; Sangare, L; Simporé, J; Sulis, G; Tarnagda, G; Villani, P, 2020
)
1.08
"This study confirmed that the 150 mg dose of rifabutin ingested EOD in combination with LPV/r is inadequate and could lead to selection of rifamycin-resistant mycobacteria."( Pharmacokinetic study of two different rifabutin doses co-administered with lopinavir/ritonavir in African HIV and tuberculosis co-infected adult patients.
Cisse, K; Compaoré, TR; Diagbouga, S; Kouanda, S; Matteelli, A; Ouedraogo, HG; Regazzi, M; Roggi, A; Sangare, L; Simporé, J; Sulis, G; Tarnagda, G; Villani, P, 2020
)
0.79
" We confirmed that ATV inhibits SARS-CoV-2 replication, alone or in combination with ritonavir (RTV) in Vero cells and a human pulmonary epithelial cell line."( Atazanavir, Alone or in Combination with Ritonavir, Inhibits SARS-CoV-2 Replication and Proinflammatory Cytokine Production.
Alves, CR; Bozza, FA; Bozza, PT; Cardoso Soares, V; Carels, N; da Silva Gomes Dias, S; de Freitas, CS; Ferreira, AC; Fintelman-Rodrigues, N; Matos, AR; Mattos, M; Miranda, MD; Ribeiro Lima, C; Sacramento, CQ; Siqueira, MM; Souza da Silva, F; Souza, TML; Temerozo, JR, 2020
)
0.56
" This potent, time-dependent interference of major hepatic drug-metabolizing enzymes by ritonavir leads to several clinically important drug-drug interactions."( Lopinavir-Ritonavir in SARS-CoV-2 Infection and Drug-Drug Interactions with Cardioactive Medications.
Agarwal, S; Agarwal, SK, 2021
)
2.06
"Patients hospitalised with severe acute respiratory syndrome coronavirus 2 [SARS-CoV-2; coronavirus 2019 disease (COVID-19)] infection are frequently older with co-morbidities and receiving polypharmacy, all of which are known risk factors for drug-drug interactions (DDIs)."( Drug-Drug Interactions and Prescription Appropriateness in Patients with COVID-19: A Retrospective Analysis from a Reference Hospital in Northern Italy.
Antinori, S; Bradanini, L; Cattaneo, D; Covizzi, A; Gervasoni, C; Giacomelli, A; Maggioni, AP; Oreni, L; Pasina, L; Ridolfo, A; Schiuma, M, 2020
)
0.56
"The impact of drug-drug interactions (DDI) between ritonavir-boosted lopinavir (LPV-r) to treat patients with coronavirus disease 2019 (COVID-19) and commonly used drugs in clinical practice is not well-known."( High rate of major drug-drug interactions of lopinavir-ritonavir for COVID-19 treatment.
Contreras-Macias, E; Corma, A; Fernández-Fuertes, M; González-Serna, A; Gutierrez-Pizarraya, A; Lao-Dominguez, FA; Macías, J; Morillo-Verdugo, R; Pineda, JA; Pinilla, A; Real, LM; Trigo, M, 2020
)
1.05
" The objective of this study was to analyse the potential drug-drug interactions (pDDIs) derived from the medication used in COVID-19 patients in the first pandemic wave and to evaluate the real consequences of such interactions in clinical practice."( Real-world prevalence and consequences of potential drug-drug interactions in the first-wave COVID-19 treatments.
Álvarez-Payero, M; Casanova-Martínez, C; Castro-Núñez, I; García-Beloso, N; González-Costas, S; Inaraja-Bobo, MT; Leboreiro-Enríquez, B; López-López, A; Lorenzo-Lorenzo, K; Martínez-López-de-Castro, N; Martínez-Reglero, C; Otero-Millán, L; Paradela-Carreiro, A; Pérez-Landeiro, A; Piñeiro-Corrales, G; Regueira-Arcay, AM; Robles-Torres, D; Samartín-Ucha, M; Vázquez-López, C; Yaiza Romero-Ventosa, E, 2021
)
0.62
" To fight against COVID-19 in a more efficient way, drug-drug or drug-herb combinations are frequently used in clinical settings."( Inhibition of drug-metabolizing enzymes by Qingfei Paidu decoction: Implication of herb-drug interactions in COVID-19 pharmacotherapy.
Chen, HZ; Ge, GB; Huang, J; Liang, XM; Liu, W; Liu, YF; Tu, DZ; Wang, CR; Yang, L; Zhang, F; Zhang, WD, 2021
)
0.62
"This study aimed to evaluate the antiviral efficacy of lopinavir-ritonavir alone or combined with arbidol in the treatment of hospitalized patients with common coronavirus disease-19 (COVID-19)."( Lopinavir-ritonavir alone or combined with arbidol in the treatment of 73 hospitalized patients with COVID-19: A pilot retrospective study.
Lan, X; Shao, C; Wu, Z; Xu, Y; Zeng, X, 2021
)
2.31
"No benefit was observed in the antiviral effect of lopinavir-ritonavir combined with arbidol compared with lopinavir-ritonavir alone in the hospitalized patients with COVID-19."( Lopinavir-ritonavir alone or combined with arbidol in the treatment of 73 hospitalized patients with COVID-19: A pilot retrospective study.
Lan, X; Shao, C; Wu, Z; Xu, Y; Zeng, X, 2021
)
2.32
" However, management of acute seizures in patients with COVID-19 as well as management of PWE and COVID-19 needs to consider potential drug-drug interactions between antiseizure drugs and candidate drugs currently assessed as therapeutic options for COVID-19."( Management of COVID-19 in patients with seizures: Mechanisms of action of potential COVID-19 drug treatments and consideration for potential drug-drug interactions with anti-seizure medications.
Chandra, PP; Jain, S; Potschka, H; Tripathi, M; Vohora, D, 2021
)
0.62
"Primary aim was to assess prevalence and severity of potential and real drug-drug interactions (DDIs) among therapies for COVID-19 and concomitant medications in hospitalized patients with confirmed SARS-CoV-2 infection."( Drug-drug interactions between treatment specific pharmacotherapy and concomitant medication in patients with COVID-19 in the first wave in Spain.
Cantudo-Cuenca, MD; Contreras-Macías, E; Fernández-Fuertes, M; Gutiérrez-Pizarraya, A; Lao-Domínguez, FA; Macías, J; Morillo-Verdugo, R; Pineda, JA; Pinilla-Fernández, A; Rincón, P, 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 review the drug-drug interactions between tacrolimus and lopinavir/ritonavir in 23 patients who received solid organ transplant during the first wave of COVID-19 and to determine the efficacy as well as safety of prednisone monotherapy."( Drug-drug interactions of ritonavir-boosted SARS-CoV-2 protease inhibitors in solid organ transplant recipients: experience from the initial use of lopinavir-ritonavir.
Ambrosioni, J; Arranz, N; Bodro, M; Brunet, M; Castel, MÁ; Cofan, F; Crespo, G; Diekmann, F; Farrero, M; Forner, A; Gonzalez-García, R; LLigoña, A; Marcos, MÁ; Miró, JM; Moreno, A; Rodríguez-García, M; Roma, JR; Ruiz, P; Soy, D; Tuset, M, 2023
)
1.35
"Previous use of a mechanistic static model to accurately quantify the increased rosuvastatin exposure due to drug-drug interaction (DDI) with coadministered atazanavir underpredicted the magnitude of area under the plasma concentration-time curve ratio (AUCR) based on inhibition of breast cancer resistance protein (BCRP) and organic anion transporting polypeptide (OATP) 1B1."( Mechanistic in vitro studies indicate that the clinical drug-drug interactions between protease inhibitors and rosuvastatin are driven by inhibition of intestinal BCRP and hepatic OATP1B1 with minimal contribution from OATP1B3, NTCP and OAT3.
Atkinson, H; Coghlan, H; Edgerton, J; Elsby, R; Hodgson, D; Outteridge, S, 2023
)
0.91

Bioavailability

Lopinavir (LPV), a newer HIV protease inhibitor, has poor bioavailability being a substrate of both cytochrome P450 3A enzyme system (CYP3A) and permeability-glycoprotein (P-gp) In HIV+ children on lopinavIR/ritonavir, bioavailability was reduced by 32% [median (IQR) steady-state Cmax = 0.0].

ExcerptReferenceRelevance
" The model parameters volume of distribution and absorption rate constant were 61."( Population pharmacokinetics of lopinavir in combination with ritonavir in HIV-1-infected patients.
Beijnen, JH; Crommentuyn, KM; Huitema, AD; Kappelhoff, BS; Mairuhu, AT; Meenhorst, PL; Mulder, JW; van Gorp, EC, 2005
)
0.61
"9 L), absorption rate constant (0."( No significant influence of saquinavir hard-gel capsule administration on pharmacokinetics of lopinavir in combination with ritonavir: a population approach.
Allavena, C; Dailly, E; Gagnieu, MC; Jolliet, P; Raffi, F, 2005
)
0.55
" The fexofenadine AUC(infinity) was increased by lopinavir/ritonavir, likely due to increased bioavailability secondary to P-glycoprotein inhibition."( Time-dependent interaction between lopinavir/ritonavir and fexofenadine.
Bourbeau, M; Cameron, DW; Campbell, P; Chauhan, BM; Foster, BC; Seguin, I; van Heeswijk, RP, 2006
)
0.87
"Lopinavir, an HIV protease inhibitor, is coformulated with ritonavir to enhance the bioavailability and pharmacokinetics of lopinavir."( The tablet formulation of lopinavir/ritonavir provides similar bioavailability to the soft-gelatin capsule formulation with less pharmacokinetic variability and diminished food effect.
Awni, W; Breitenbach, J; Brun, SC; Chiu, YL; Doan, T; Hanna, GJ; Heuser, RS; Klein, CE; Morris, JB; Zhu, T, 2007
)
2.08
" In conclusion, this study presents direct evidence that LVR is effluxed by both P-gp and MRP2 which may contribute to its poor oral bioavailability and limited penetration into the CNS."( Both P-gp and MRP2 mediate transport of Lopinavir, a protease inhibitor.
Agarwal, S; Mitra, AK; Pal, D, 2007
)
0.61
"This investigation was carried out to evaluate the bioavailability of a new single fixed-dose combination formulation of lopinavir and ritonavir, relative to reference product, Kaletra (133."( A bioequivalence study comparing two formulations of lopinavir/ritonavir capsules.
Gurule, S; Khuroo, AH; Lao, VK; Mishra, S; Monif, T; Raghuvanshi, R; Thudi, NR; Tippabhotla, SK, 2008
)
0.8
" The results indicated that lopinavir bioavailability was not affected by the coadministration of omeprazole or ranitidine."( Effects of acid-reducing agents on the pharmacokinetics of lopinavir/ritonavir and ritonavir-boosted atazanavir.
Beck, K; Cai, Y; Causemaker, SJ; Chiu, YL; Doan, T; Esslinger, HU; Hanna, GJ; King, KR; Klein, CE; Podsadecki, TJ, 2008
)
0.88
"In this study, we explored the bioavailability in dogs and chemical potency of generic ritonavir and lopinavir/ritonavir tablet products manufactured by various pharmaceutical companies."( Bioavailability of generic ritonavir and lopinavir/ritonavir tablet products in a dog model.
Garren, KW; Marsh, K; Morris, JB; Rahim, S, 2010
)
0.84
" Modification of the core regiochemistry and stereochemistry significantly affected the potency, metabolic stability, and oral bioavailability of the inhibitors, as did the variation of a pendent arylmethyl P3 group."( 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
Chen, HJ; Colletti, L; Degoey, DA; Dekhtyar, T; Flentge, CA; Flosi, WJ; Grampovnik, DJ; Kati, WM; Kempf, DJ; Klein, LL; Mamo, M; Marsh, KC; Mo, H; Molla, A; Morfitt, DC; Nguyen, B; Randolph, JT; Schmidt, JM; Stoll, V; Swanson, SJ; Yeung, CM, 2009
)
0.35
" The ritonavir dose-dependence of boosting effects did not correlate with their bioavailability or their effects on ritonavir plasma levels."( How much ritonavir is needed to boost protease inhibitors? Systematic review of 17 dose-ranging pharmacokinetic trials.
Boffito, M; Hill, A; Sawyer, W; van der Lugt, J, 2009
)
0.35
" Meltrex) have proven to be a promising formulation tool for poorly water-soluble and poorly bioavailable drugs."( In situ formation of nanoparticles upon dispersion of melt extrudate formulations in aqueous medium assessed by asymmetrical flow field-flow fractionation.
Brandl, M; Fricker, G; Hölig, P; Hupfeld, S; Kanzer, J; Mägerlein, M; Tho, I; Vasskog, T, 2010
)
0.36
" We also evaluated whether ritonavir increases lopinavir oral bioavailability by inhibition of CYP3A, ABCB1 and/or ABCC2."( Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir.
Beijnen, JH; Huitema, AD; Rooswinkel, RW; Schinkel, AH; ter Heine, R; van der Kruijssen, CM; van Waterschoot, RA; Wagenaar, E, 2010
)
0.82
" Both intestinal and hepatic CYP3A activity contributed importantly to low oral bioavailability of lopinavir."( Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir.
Beijnen, JH; Huitema, AD; Rooswinkel, RW; Schinkel, AH; ter Heine, R; van der Kruijssen, CM; van Waterschoot, RA; Wagenaar, E, 2010
)
0.78
" The percentage bioavailability was significantly enhanced."( Lopinavir loaded solid lipid nanoparticles (SLN) for intestinal lymphatic targeting.
Aji Alex, MR; Chacko, AJ; Jose, S; Souto, EB, 2011
)
1.81
"0%), and the apparent volume of distribution and absorption rate constant were 55."( Sequential population pharmacokinetic modeling of lopinavir and ritonavir in healthy volunteers and assessment of different dosing strategies.
Aarons, L; Back, D; Boffito, M; Davies, G; Dickinson, L; Else, L; Khoo, S; Moyle, G; Pozniak, A; von Hentig, N, 2011
)
0.62
" Overall, compound 13 demonstrated the best balance of potency against drug resistant strains of HIV and oral bioavailability in pharmacokinetic studies."( P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.
Chen, HJ; Degoey, DA; Dekhtyar, T; Flosi, WJ; Grampovnik, DJ; Kempf, DJ; Klein, LL; Mamo, M; Molla, A; Stoll, V, 2011
)
0.37
" LPV alone suffers the poor bioavailability due to its rapid and extensive metabolism."( CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
Li, F; Lu, J; Ma, X, 2012
)
0.72
" Although lopinavir (tablet) exposures were reduced during the third trimester, the higher total and unbound concentrations achieved in women receiving the tablet than in women receiving the SGC suggest that the tablet's improved oral bioavailability may partly compensate for the reduction in lopinavir exposure during the later stages of pregnancy."( Improved oral bioavailability of lopinavir in melt-extruded tablet formulation reduces impact of third trimester on lopinavir plasma concentrations.
Back, DJ; Dickinson, L; Douglas, M; Else, LJ; Khoo, SH; Taylor, GP, 2012
)
1.06
" Rifampicin reduced the oral bioavailability of lopinavir and ritonavir by 20% and 45% respectively, and it increased their clearance by 71% and 36% respectively."( Model-based approach to dose optimization of lopinavir/ritonavir when co-administered with rifampicin.
Decloedt, E; Denti, P; Karlsson, MO; Maartens, G; McIlleron, H; Simonsson, US; Zhang, C, 2012
)
0.89
" The higher trough concentrations observed in the morning were explained by both higher bioavailability with the evening meal and lower clearance overnight."( Model-based approach to dose optimization of lopinavir/ritonavir when co-administered with rifampicin.
Decloedt, E; Denti, P; Karlsson, MO; Maartens, G; McIlleron, H; Simonsson, US; Zhang, C, 2012
)
0.64
" Antitubercular treatment reduced the oral bioavailability of lopinavir by 77% in children receiving twice usual lopinavir/ritonavir doses and increased ritonavir clearance by 50%."( Population pharmacokinetics of lopinavir and ritonavir in combination with rifampicin-based antitubercular treatment in HIV-infected children.
Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Simonsson, US; van der Walt, JS; Zhang, C, 2012
)
0.91
"Lopinavir (LPV), a newer HIV protease inhibitor, has poor bioavailability being a substrate of both cytochrome P450 3A enzyme system (CYP3A) and permeability-glycoprotein (P-gp)."( Effect of grapefruit juice and ritonavir on pharmacokinetics of lopinavir in Wistar rats.
Aditya, N; Ravi, PR; Srivani, S; Thakur, R; Vats, R, 2012
)
2.06
"Eltrombopag is an orally bioavailable thrombopoietin receptor agonist that is approved for the treatment of chronic idiopathic thrombocytopenic purpura."( Assessment of the pharmacokinetic interaction between eltrombopag and lopinavir-ritonavir in healthy adult subjects.
McLean, HB; Park, JW; Pendry, C; Peng, B; Theodore, D; Wire, MB, 2012
)
0.61
"75 min, respectively, with a significant increase in bioavailability in a rat model compared with a free-drug suspension."( Enhanced delivery of lopinavir to the CNS using Compritol-based solid lipid nanoparticles.
Alex, A; Chacko, AJ; Paul, W; Sharma, CP, 2011
)
0.69
" Clinical utility via transdermal route was acknowledged using in vivo bioavailability study in male Wistar rats."( Formulation of niosomal gel for enhanced transdermal lopinavir delivery and its comparative evaluation with ethosomal gel.
Kumar, P; Patel, KK; Thakkar, HP, 2012
)
0.63
"Solid lipid nanoparticles (SLNs) of poor orally bioavailable drug lopinavir were prepared using hot self nano-emulsification (SNE) technique."( Development of solid lipid nanoparticles (SLNs) of lopinavir using hot self nano-emulsification (SNE) technique.
Chattopadhyay, P; Negi, JS; Ram, V; Sharma, AK, 2013
)
0.88
"The aim of the present study was to prepare surface-stabilized nanoparticles (NPs) for oral bioavailability enhancement of lopinavir (LPN), a Biopharmaceutics Classification System class II antiretroviral drug that possesses low oral bioavailability due to its poor aqueous solubility and extensive metabolism by liver microsomal enzymes."( Surface-stabilized lopinavir nanoparticles enhance oral bioavailability without coadministration of ritonavir.
Jain, AK; Jain, S; Mahajan, RR; Sharma, JM, 2013
)
0.93
"11-fold enhancement in bioavailability in comparison to free LPN with ritonavir (conventional formulation)."( Surface-stabilized lopinavir nanoparticles enhance oral bioavailability without coadministration of ritonavir.
Jain, AK; Jain, S; Mahajan, RR; Sharma, JM, 2013
)
0.72
"The bioavailability of lopinavir was reduced by 25% in adults whereas children on antituberculosis treatment experienced a 59% reduction, an effect that was moderated by the dose of ritonavir."( Model-based evaluation of the pharmacokinetic differences between adults and children for lopinavir and ritonavir in combination with rifampicin.
Decloedt, EH; Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Zhang, C, 2013
)
0.92
" The drug has a very low bioavailability due to a rapid metabolism by cytochrome P450 3A (CYP3A) isoenzyme."( Compartmental pharmacokinetic modeling of lopinavir in humans.
Duangchaemkarn, K; Lohitnavy, M, 2013
)
0.65
" Pharmacokinetic study results in male Wistar rats indicated an increase in oral bioavailability of LPV by 4-folds after incorporation into PCL NPs."( Design, optimization and evaluation of poly-ε-caprolactone (PCL) based polymeric nanoparticles for oral delivery of lopinavir.
Dalal, V; Gadekar, N; N, A; Ravi, PR; Vats, R, 2015
)
0.63
" The principal aim of this study was to compare bioavailability of two doses of rifabutin (150 mg three times per week and 150 mg daily) in patients with HIV-associated tuberculosis who initiated lopinavir/ritonavir-based antiretroviral therapy in Vietnam."( Randomised pharmacokinetic trial of rifabutin with lopinavir/ritonavir-antiretroviral therapy in patients with HIV-associated tuberculosis in Vietnam.
Barrail-Tran, A; Borand, L; Connolly, C; Duc, NH; Dung, NH; Harries, AD; Lagarde, D; Lan, NN; Lan, NT; Laureillard, D; Lien, TT; Lienhardt, C; Pym, A; Quillet, C; Taburet, AM; Thu, NT, 2014
)
0.84
" Significant increase in oral bioavailability of LPV from LPV SLNs (5 folds) and LPV/RTV coformulation (3."( A hybrid design to optimize preparation of lopinavir loaded solid lipid nanoparticles and comparative pharmacokinetic evaluation with marketed lopinavir/ritonavir coformulation.
Dalal, V; Murthy, AN; Ravi, PR; Vats, R, 2014
)
0.67
"SLNs enhanced oral bioavailability and improved distribution profile of LPV to HIV reservoirs and hence could be better alternative to LPV/RTV coformulation."( A hybrid design to optimize preparation of lopinavir loaded solid lipid nanoparticles and comparative pharmacokinetic evaluation with marketed lopinavir/ritonavir coformulation.
Dalal, V; Murthy, AN; Ravi, PR; Vats, R, 2014
)
0.67
"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
)
0.67
"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
)
0.67
"An open-label comparative bioavailability (randomized crossover) study compared a novel twice-daily minitab sprinkle formulation (40 mg/10 mg, Cipla Pharmaceuticals) versus innovator syrup in HIV-infected Ugandan infants aged 3 to <12 months (cohort A) and children aged 1-4 years (cohort B) and versus Cipla tablets (100/25 mg) in children aged 4 to <13 years (cohort C)."( The pharmacokinetics and acceptability of lopinavir/ritonavir minitab sprinkles, tablets, and syrups in african HIV-infected children.
Burger, D; Fillekes, Q; Gibb, DM; Keishanyu, R; Kekitiinwa, A; Kendall, L; Lallemant, M; Musiime, V; Namuddu, R; Opilo, W; Walker, AS; Young, N, 2014
)
0.67
" From the pharmacokinetic study data, we found that the relative bioavailability of Lopinavir from nanoparticles was ∼2 folds higher than the free drug."( Modified pullulan nanoparticles for oral delivery of lopinavir: formulation and pharmacokinetic evaluation.
Adapa, SP; Aditya, N; Balija, J; Ravi, PR; Vats, R, 2014
)
0.88
" Concentrations of Arga-L® at 12 h after intake were considerably lower than those of Kaletra®, revealing very low oral bioavailability of generic lopinavir and ritonavir (<10%) compared to the brand-name drug."( [Lack of bioavailability of generic lopinavir/ritonavir not prequalified by WHO marketed in Africa (Congo Brazzaville)].
Camara, S; Goudjo, A; Guillard, E; Peytavin, G; Vasse, M; Zucman, D, 2015
)
0.89
" 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
)
0.65
" LPV bioavailability is increased by co-formulated ritonavir (r), which may enhance the interaction of INH on LPV."( The pharmacokinetics of lopinavir/ritonavir when given with isoniazid in South African HIV-infected individuals.
Decloedt, EH; Maartens, G; McIlleron, H; van der Walt, JS; Wiesner, L, 2015
)
0.72
"56-fold increase in bioavailability and significantly increased LPV concentrations in tested tissues, especially in HIV sanctuary sites, as compared to the commercial LPV/RTV tablet (Kaletra®) in rats."( Development and in vivo evaluation of child-friendly lopinavir/ritonavir pediatric granules utilizing novel in situ self-assembly nanoparticles.
Dong, X; Guo, S; Li, D; Penzak, S; Pham, K, 2016
)
0.68
"Lopinavir (LPV), an antiretroviral protease inhibitor shows poor bioavailability because of poor aqueous solubility and extensive hepatic first-pass metabolism."( Statistical modeling, optimization and characterization of solid self-nanoemulsifying drug delivery system of lopinavir using design of experiment.
Lalwani, A; Patel, G; Shelat, P, 2016
)
2.09
" In vivo bioavailability of S-SNEDDS, marketed Lopinavir + Ritonavir (LPV/RTV) formulation and pure LPV was studied in Wistar rats."( Statistical modeling, optimization and characterization of solid self-nanoemulsifying drug delivery system of lopinavir using design of experiment.
Lalwani, A; Patel, G; Shelat, P, 2016
)
0.9
"The significant increase in drug dissolution and bioavailability by prepared SNEDDS suggest that the developed S-SNEDDS is a useful solid platform for improving oral bioavailability of poorly soluble LPV."( Statistical modeling, optimization and characterization of solid self-nanoemulsifying drug delivery system of lopinavir using design of experiment.
Lalwani, A; Patel, G; Shelat, P, 2016
)
0.65
" 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
)
0.64
"Lopinavir is a BCS Class IV drug exhibiting poor bioavailability due to P-gp efflux and limited permeation."( Improvement of Oral Bioavailability of Lopinavir Without Co-administration of Ritonavir Using Microspheres of Thiolated Xyloglucan.
Bhalekar, MR; Kadam, AA; Madgulkar, AR, 2018
)
2.19
" MDR-TB treatment did not have a significant effect on the bioavailability, clearance, or absorption rate constants of lopinavir or ritonavir."( Pharmacokinetics and Drug-Drug Interactions of Lopinavir-Ritonavir Administered with First- and Second-Line Antituberculosis Drugs in HIV-Infected Children Treated for Multidrug-Resistant Tuberculosis.
de Kock, M; Denti, P; Garcia-Prats, AJ; Hesseling, AC; McIlleron, H; Norman, J; Schaaf, HS; Tikiso, T; van der Laan, LE; Wiesner, L; Winckler, J, 2018
)
0.95
" LPV pharmacokinetics was found to be highly variable and bioavailability greatly reduced, resulting in a high CL estimate in this population."( Population Pharmacokinetics of Lopinavir in Severely Malnourished HIV-infected Children and the Effect on Treatment Outcomes.
Archary, M; Bobat, R; Hennig, S; La Russa, P; Mcllleron, H; Sibaya, T; Wiesner, L, 2018
)
0.77
"Amorphous solid dispersions (ASDs) are a promising formulation strategy to increase both the apparent aqueous solubility and bioavailability of poorly water-soluble drugs."( Mechanistic understanding of the phase behavior of supersaturated solutions of poorly water-soluble drugs.
Hall, SD; Mohutsky, MA; Posada, MM; Taylor, LS; Tres, F, 2018
)
0.48
"Lopinavir is a specific reversible inhibitor of the enzyme HIV protease with mean oral bioavailability of less than 20 % due to extensive hepatic metabolism by cytochrome P450 3A4."( Formulation and in-vivo Evaluation of Novel Topical Gel of Lopinavir for Targeting HIV.
Ansari, H; Singh, P, 2018
)
2.17
"The objective was to develop solid lipid nanoparticles (SLN) of lopinavir and formulate a topical gel for improved systemic bioavailability of lopinavir."( Formulation and in-vivo Evaluation of Novel Topical Gel of Lopinavir for Targeting HIV.
Ansari, H; Singh, P, 2018
)
0.96
" To explore the potential of topical route, invivo bioavailability study was conducted in male Wistar rats."( Formulation and in-vivo Evaluation of Novel Topical Gel of Lopinavir for Targeting HIV.
Ansari, H; Singh, P, 2018
)
0.72
" Also, the AUC was higher in the case of SLN based gel indicating good bioavailability as compared to oral suspension and plain gel of drug."( Formulation and in-vivo Evaluation of Novel Topical Gel of Lopinavir for Targeting HIV.
Ansari, H; Singh, P, 2018
)
0.72
"Lymphatic transport of oral drugs allows extraordinary gains in bioavailability and efficacy through avoidance of first-pass hepatic metabolism and preservation of drugs at lymphatic tissues against lymph-mediated diseases."( Chylomicron-pretended nano-bio self-assembling vehicle to promote lymphatic transport and GALTs target of oral drugs.
Di, D; Feng, S; Li, S; Liu, Y; Mao, Y; Wang, S; Zhao, Q, 2019
)
0.51
" In the study, we developed novel solid dispersions (SD) of LPV to improve its bioavailability and to describe their overall behaviors."( Solubility and bioavailability enhancement study of lopinavir solid dispersion matrixed with a polymeric surfactant - Soluplus.
Bao, Y; Gao, J; Ju, C; Lu, J; Su, Z; Sun, J; Zhang, C; Zi, P, 2019
)
0.76
" Pretomanid pharmacokinetic behavior was described by a one-compartment model that at a given dose was linear in its absorption and clearance processes but where the rate of absorption and extent of bioavailability changed with dose."( Population Pharmacokinetics of the Antituberculosis Agent Pretomanid.
Everitt, D; Nedelman, JR; Salinger, DH; Subramoney, V, 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
" However, their effectiveness is limited due to lack of bioavailability and they need to be coadministered with another drug."( Lopinavir Loaded Spray Dried Liposomes with Penetration Enhancers for Cytotoxic Activity.
Chandak, A; Kokare, C; Maniyar, M, 2020
)
2
" The fluorescence microscopy, histopathological study, and in-vivo bioavailability studies were performed to measure the penetration and inertness of cream in animals."( Lopinavir Loaded Spray Dried Liposomes with Penetration Enhancers for Cytotoxic Activity.
Chandak, A; Kokare, C; Maniyar, M, 2020
)
2
" The histopathological study demonstrates the inertness of cream while in-vivo bioavailability studies showed the many-fold increase in bioavailability of LPV."( Lopinavir Loaded Spray Dried Liposomes with Penetration Enhancers for Cytotoxic Activity.
Chandak, A; Kokare, C; Maniyar, M, 2020
)
2
" For all 3 drugs, we found a high association with the nanoparticles in plasma (>87% lopinavir-ritonavir, 97% tenofovir), and an incomplete subcutaneous bioavailability (<29% lopinavir-ritonavir, 85% tenofovir)."( Integration of Computational and Experimental Approaches to Elucidate Mechanisms of First-Pass Lymphatic Drug Sequestration and Long-Acting Pharmacokinetics of the Injectable Triple-HIV Drug Combination TLC-ART 101.
Collier, AC; Ho, RJY; Kinman, L; Koehn, J; Lane, S; Lee, W; McConnachie, LA; Perazzolo, S; Shen, DD; Shireman, LM, 2020
)
0.78
" Lopinavir is an HIV-1 protease inhibitor with low aqueous solubility leading to poor oral bioavailability and thus frequent dosing."( Central composite design-based optimization of lopinavir vitamin E-TPGS micelle: In vitro characterization and in vivo pharmacokinetic study.
Mahajan, HS; Patil, PH, 2020
)
1.73
"Lopinavir (LPV), a well-known drug administered in human immunodeficiency virus (HIV) infection, has shown limitation for pediatric treatment owing to poor aqueous solubility that gives rise to limited oral bioavailability and short plasma half-life (5-6 h)."( Polyethylene glycol (5,000) succinate conjugate of lopinavir and its associated toxicity using Danio rerio as a model organism.
Aremu, OS; Botha, TL; Katata-Seru, L; Mkhize, Z; Wepener, V, 2020
)
2.25
" Extensive use of atazanavir (ATV) as antiretroviral and previous evidence suggesting its bioavailability within the respiratory tract prompted us to study this molecule against SARS-CoV-2."( Atazanavir, Alone or in Combination with Ritonavir, Inhibits SARS-CoV-2 Replication and Proinflammatory Cytokine Production.
Alves, CR; Bozza, FA; Bozza, PT; Cardoso Soares, V; Carels, N; da Silva Gomes Dias, S; de Freitas, CS; Ferreira, AC; Fintelman-Rodrigues, N; Matos, AR; Mattos, M; Miranda, MD; Ribeiro Lima, C; Sacramento, CQ; Siqueira, MM; Souza da Silva, F; Souza, TML; Temerozo, JR, 2020
)
0.56
" The present research aims to develop a nanoparticle-based orodispersible pediatric drug delivery platform to improve oral bioavailability and taste of poorly water-soluble and unpalatable therapeutics."( Development of nanoparticle-based orodispersible palatable pediatric formulations.
Deng, Y; Shen, J; Shen, L; Yang, Y, 2021
)
0.62
" LPV/r-A tablets contain key excipients critical to ensuring acceptable bioavailability of lopinavir and ritonavir in humans."( Comparative Bioavailability of Two Formulations of Biopharmaceutical Classification System (BCS) Class IV Drugs: A Case Study of Lopinavir/Ritonavir.
Jarvis, MF; Morris, JB; Mostafa, NM; Munasinghe, WP; Saeed, AM; Schmidt, JM; Vallabh, BK, 2021
)
1.05
"Analytical characterizations of LPV/r-B tablets were performed and a clinical study was conducted to assess the relative bioavailability of Kalidavir® (LPV/r-B) 400/100 mg tablets relative to Kaletra® (LPV/r-A) 400/100 mg tablets under fasting conditions."( Comparative Bioavailability of Two Formulations of Biopharmaceutical Classification System (BCS) Class IV Drugs: A Case Study of Lopinavir/Ritonavir.
Jarvis, MF; Morris, JB; Mostafa, NM; Munasinghe, WP; Saeed, AM; Schmidt, JM; Vallabh, BK, 2021
)
0.83
" In HIV+ children on lopinavir/ritonavir, bioavailability was reduced by 32% [median (IQR) steady-state Cmax = 0."( Population pharmacokinetics of ethambutol in African children: a pooled analysis.
Abdelwahab, MT; Andrieux-Meyer, I; Bekker, A; Chabala, C; Cotton, MF; Davies, G; Denti, P; Hesseling, A; Lee, J; McIlleron, H; Rabie, H; Tikiso, T; Wiesner, L; Zar, HJ, 2022
)
1.04
" It indicates the potential use of SNEDDS to enhance the solubility of LPV, which eventually could help improve the oral bioavailability of LPV."( Lopinavir-Loaded Self-Nanoemulsifying Drug Delivery System for Enhanced Solubility: Development, Characterisation and Caco-2 Cell Uptake.
Akhtar, S; Alelwani, W; Atiya, A; Bannunah, AM; Khan, AA; Mahmood, S; Yadav, Y, 2023
)
2.35
"Formulations containing nanosized drug particles such as nanocrystals and nanosized amorphous drug aggregates recently came into light as promising strategies to improve the bioavailability of poorly soluble drugs."( Mechanisms and Extent of Enhanced Passive Permeation by Colloidal Drug Particles.
Li, N; Narula, A; Sabra, R, 2022
)
0.72
"Lopinavir is effective in treatment of HIV infection but experiences low oral bioavailability due to poor solubility, pre-systemic metabolism, and P-gp intestinal efflux."( Menthol augmented niosomes for enhanced intestinal absorption of lopinavir.
El Maghraby, GM; Essa, EA; Fayed, ND, 2022
)
2.4
" The antiviral activity of lopinavir/ritonavir in vivo is mainly derived from lopinavir, while ritonavir improves the bioavailability of lopinavir."( Pharmacokinetics, Safety, and Bioequivalence of 2 Lopinavir/Ritonavir (200/50 mg) Tablets in Healthy Chinese Volunteers: Effect of Food on Absorption.
Bao, D; Fu, W; Hu, W; Lin, L; Liu, Y; Zhang, Q; Zhang, W; Zheng, L, 2023
)
1.46
" 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

Dosage Studied

Lopinavir-ritonavir (LPV/r) recently became the preferred protease inhibitor (PI) for use in Nigeria since it is dosed once daily, which may improve treatment adherence. Further efficacy studies are necessary before routinely recommending this dosing strategy.

ExcerptRelevanceReference
" 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: protease inhibitors.
,
)
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
"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
)
0.81
" The pharmacokinetics of lopinavir did not appear to be dependent on age when dosing was based on body surface area but were decreased on coadministration with nevirapine."( Forty-eight-week evaluation of lopinavir/ritonavir, a new protease inhibitor, in human immunodeficiency virus-infected children.
Allen, U; Arpadi, S; Bernstein, B; Bertz, RJ; Cahn, P; Castrejón, MM; Chadwick, E; Deetz, CO; Gomez, P; Handelsman, E; Heuser, RS; Hsu, AF; Kempf, DJ; Pelton, S; Ramilo, O; Renz, CL; Rode, RA; Sáez-Llorens, X; Sun, E; Violari, A, 2003
)
0.91
" Column chromatography methodology was developed to separate lopinavir from ritonavir starting from the commercially available lopinavir-ritonavir combination dosage form."( Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir.
Greenblatt, DJ; Harmatz, JS; Hesse, LM; Richert, C; von Moltke, LL; Weemhoff, JL, 2003
)
0.8
"This study examines the pharmacokinetic/pharmacodynamic interactions between (1) lopinavir-ritonavir (L/R), a fixed combination of protease inhibitors used for the treatment of HIV disease, and (2) ritonavir alone at the same dosage as that in the L/R formulation, with methadone, an opiate frequently used in substance abuse pharmacotherapy for opioid (heroin)-dependent injection drug users, many of whom are infected with HIV."( The protease inhibitor lopinavir-ritonavir may produce opiate withdrawal in methadone-maintained patients.
Friedland, G; Jatlow, P; McCance-Katz, EF; Rainey, PM, 2003
)
0.86
" Great caution is required in the management of tacrolimus dosage when Kaletra is introduced or withdrawn in HIV-positive patients after liver transplantation, particularly in the presence of hepatic dysfunction."( Effect of coadministered lopinavir and ritonavir (Kaletra) on tacrolimus blood concentration in liver transplantation patients.
Eghtesad, B; Fung, JJ; Jain, AB; Marcos, A; Rafail, AB; Ragni, M; Shapiro, R; Venkataramanan, R, 2003
)
0.62
" The aim of the study was to measure unbound plasma concentrations of lopinavir (LPV) and to relate them to the total plasma concentrations to establish the unbound percentage in vivo during a full dosage interval."( Lopinavir protein binding in vivo through the 12-hour dosing interval.
Back, DJ; Boffito, M; Bonora, S; Di Perri, G; Hoggard, PG; Khoo, SH; Lindup, WE; Sinicco, A, 2004
)
2
" A retrospective study carried out of 72 probable SARS patients has shown that cases who received pulse methylprendisolone did not differ in cumulative steroid dosage or adverse reactions, although the former patients had less oxygen requirement, better radiographic outcome, and less likelihood of requiring rescue pulse steroid therapy than their counterparts."( SARS: pharmacotherapy.
Tsang, K; Zhong, NS, 2003
)
0.32
" After 48 weeks, LPV/r was dosed open-label at 400/100 mg every 12 hours with stavudine and lamivudine."( Long-term safety and durable antiretroviral activity of lopinavir/ritonavir in treatment-naive patients: 4 year follow-up study.
Benson, C; Brun, SC; Eron, JJ; Gulick, RM; Hicks, C; Kessler, HA; King, KR; King, MS; Murphy, RL; White, AC, 2004
)
0.57
" The dosage of itraconazole was reduced when it was used in combination with lopinavir/ritonavir."( Drug-drug interaction between itraconazole and the antiretroviral drug lopinavir/ritonavir in an HIV-1-infected patient with disseminated histoplasmosis.
Beijnen, JH; Crommentuyn, KM; Huitema, AD; Mulder, JW; Schellens, JH; Sparidans, RW, 2004
)
0.79
" After studying 12-hour pharmacokinetic profiles in 3 HIV-positive patients after liver transplantation, we describe how dosing of cyclosporine A can be adjusted to maintain effective immunosuppressive drug levels on a daily dosing schedule when ritonavir-boosted indinavir or lopinavir-based antiretroviral therapy is given."( Management of drug-to-drug interactions between cyclosporine A and the protease-inhibitor lopinavir/ritonavir in liver-transplanted HIV-infected patients.
Michaelis, HC; Rockstroh, JK; Sauerbruch, T; Spengler, U; Sudhop, T; Türler, A; Vogel, M; Voigt, E; Wolff, M, 2004
)
0.72
" Management should be individualized to each patient; dosage or medication adjustments may be necessary."( Coadministration of lopinavir/ritonavir and phenytoin results in two-way drug interaction through cytochrome P-450 induction.
Bertz, RJ; Eron, JJ; Gaedigk, A; Kashuba, AD; Lim, ML; Min, SS; Robinson, M, 2004
)
0.65
" The tissue distribution of radioactivity was examined in rats dosed with [14C]lopinavir in combination with ritonavir."( Metabolism and disposition of the HIV-1 protease inhibitor lopinavir (ABT-378) given in combination with ritonavir in rats, dogs, and humans.
Denissen, JF; Grabowski, BA; Jayanti, VK; Johnson, MK; Kempf, DJ; Kumar, GN; Lee, RD; Marsh, KC; Roberts, SA; Sham, HL; Sun, E; Thomas, S; Uchic, J, 2004
)
0.79
" On oral dosing to rats, ritonavir was found to increase the exposure of lopinavir-derived radioactivity 13-fold."( Metabolism and disposition of the HIV-1 protease inhibitor lopinavir (ABT-378) given in combination with ritonavir in rats, dogs, and humans.
Denissen, JF; Grabowski, BA; Jayanti, VK; Johnson, MK; Kempf, DJ; Kumar, GN; Lee, RD; Marsh, KC; Roberts, SA; Sham, HL; Sun, E; Thomas, S; Uchic, J, 2004
)
0.8
" 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
)
0.81
" Therefore, we studied the plasma and intracellular (cell-associated) steady-state pharmacokinetics of this PI combination in a dosage of 400/100 mg twice daily in a non-randomized cohort of HIV-1-infected individuals."( The plasma and intracellular steady-state pharmacokinetics of lopinavir/ritonavir in HIV-1-infected patients.
Beijnen, JH; Crommentuyn, KM; Huitema, AD; Mairuhu, AT; Meenhorst, PL; Mulder, JW; van Gorp, EC, 2004
)
0.56
"In antiretroviral-experienced subjects with sustained viral suppression, dual therapy with NVP plus LPV/rtv at standard dosage was as potent and safe as standard-of-care HAART at 48 weeks of follow-up."( Lopinavir/ritonavir plus nevirapine as a nucleoside-sparing approach in antiretroviral-experienced patients (NEKA study).
Burger, D; Clotet, B; Côté, H; López, S; Martínez, E; Miró, O; Moltó, J; Montaner, J; Negredo, E; Puig, J; Rey-Joly, C; Ribalta, J; Ruiz, L; Salazar, J, 2005
)
1.77
"Pharmacokinetic studies rely on blood sampling at times relative to predefined dosing intervals."( Successful projection of the time course of drug concentration in plasma during a 1-year period from electronically compiled dosing-time data used as input to individually parameterized pharmacokinetic models.
Bertz, R; Mayer, S; Rode, R; Tousset, E; Urquhart, J; Vrijens, B, 2005
)
0.33
" The median (interquartile range) LPV AUC(0,24 h), maximum plasma concentration (C(max)) and concentration at the end of the dosing interval (C(24 h)) after am and pm dosing was, respectively, 143 (116-214) mg l(-1) h, 12."( Absence of circadian variation in the pharmacokinetics of lopinavir/ritonavir given as a once daily dosing regimen in HIV-1-infected patients.
Bourbeau, M; Cameron, DW; Garber, GE; Giguere, P; Seguin, I; van Heeswijk, RP, 2005
)
0.57
"No differences were observed in the pharmacokinetics of LPV/r after am or pm dosing with food, which suggests that this once daily combination, can be taken in the morning or evening."( Absence of circadian variation in the pharmacokinetics of lopinavir/ritonavir given as a once daily dosing regimen in HIV-1-infected patients.
Bourbeau, M; Cameron, DW; Garber, GE; Giguere, P; Seguin, I; van Heeswijk, RP, 2005
)
0.57
" However, many of the available agents in this class suffer shortcomings, including poor tolerability, difficult dosing regimens, and variable drug concentrations which may lead to generation of viral resistance."( Safety and antiviral activity of lopinavir/ritonavir-based therapy in human immunodeficiency virus type 1 (HIV-1) infection.
Hicks, CB; Kaplan, SS, 2005
)
0.61
" However, many available agents suffer shortcomings that limit their clinical value, including adverse effects, difficult dosing requirements and rapid development of resistance."( Lopinavir/ritonavir in the treatment of human immunodeficiency virus infection.
Hicks, CB; Kaplan, SS, 2005
)
1.77
" The dosage was 50 mg/kg twice daily (bid) for saquinavir and 230/57."( Pharmacokinetics and 24-week efficacy/safety of dual boosted saquinavir/lopinavir/ritonavir in nucleoside-pretreated children.
Ananworanich, J; Bergshoeff, A; Burger, D; Engchanil, C; Hill, A; Kosalaraksa, P; Pancharoen, C; Ruxrungtham, K; Siangphoe, U, 2005
)
0.56
"Ritonavir dosed at 100 mg bid significantly increased the concentration of total cholesterol, LDL cholesterol, total/HDL cholesterol ratio and triglycerides and reduced HDL cholesterol concentration."( The effect of low-dose ritonavir monotherapy on fasting serum lipid concentrations.
Mashinter, LD; Roberts, SE; Shafran, SD, 2005
)
0.33
" No significant relationship was established between the presence or the daily dosage of saquinavir in the treatment and lopinavir population pharmacokinetic parameters."( No significant influence of saquinavir hard-gel capsule administration on pharmacokinetics of lopinavir in combination with ritonavir: a population approach.
Allavena, C; Dailly, E; Gagnieu, MC; Jolliet, P; Raffi, F, 2005
)
0.76
" The Ccell/Ctot and Cu/Ctot ratio was unaffected by the addition of the second PI and remained stable throughout dosing interval."( Ritonavir-boosted atazanavir-lopinavir combination: a pharmacokinetic interaction study of total, unbound plasma and cellular exposures.
Biollaz, J; Buclin, T; Cavassini, M; Colombo, S; Decosterd, LA; Franc, C; Guignard, N; Khonkarly, M; Rochat, B; Tarr, PE; Telenti, A, 2006
)
0.63
" The clinical significance of this decrease is unknown and warrants further investigation to determine the need for tailoring LPV dosage in selected cases."( Ritonavir-boosted atazanavir-lopinavir combination: a pharmacokinetic interaction study of total, unbound plasma and cellular exposures.
Biollaz, J; Buclin, T; Cavassini, M; Colombo, S; Decosterd, LA; Franc, C; Guignard, N; Khonkarly, M; Rochat, B; Tarr, PE; Telenti, A, 2006
)
0.63
"Lopinavir/ritonavir is approved for treatment of HIV-infected children at a dosage regimen of 230/57."( Lopinavir/ritonavir exposure in treatment-naive HIV-infected children following twice or once daily administration.
Bassetti, M; Dentone, C; Di Biagio, A; Gatti, G; Gattinara, GC; Giaquinto, C; Martino, AM; Merlo, M; Rampon, O; Rosso, R; Viganò, A; Viscoli, C, 2006
)
3.22
" In both instances, the carbamazepine dosage was decreased by 33%, which resulted in resolution of symptoms."( Carbamazepine toxicity induced by lopinavir/ritonavir and nelfinavir.
Bates, DE; Herman, RJ, 2006
)
0.61
" Carbamazepine toxicity may be prevented by reducing the carbamazepine dosage by 25-50% when protease inhibitors are introduced."( Carbamazepine toxicity induced by lopinavir/ritonavir and nelfinavir.
Bates, DE; Herman, RJ, 2006
)
0.61
"The purpose of this study was to determine the pharmacokinetics and tolerability of three different indinavir and lopinavir/ritonavir dosing regimens."( Association of total bilirubin with indinavir and lopinavir plasma concentrations in HIV-infected patients receiving three different double-boosted dosing regimens.
Dicenzo, R; Larppanichpoonphol, P; Luque, A; Reichman, R, 2006
)
0.8
"HIV-infected adults receiving lopinavir/ritonavir 400/100 mg twice daily with food had nine plasma samples taken over a 12 h dosing interval at baseline (BL), after adding indinavir 600 mg twice daily for 10 days (R1), indinavir 800 mg twice daily for 5 days (R2) and lopinavir/ritonavir 533/133 mg plus indinavir 600 mg twice daily for 10 days (R3)."( Association of total bilirubin with indinavir and lopinavir plasma concentrations in HIV-infected patients receiving three different double-boosted dosing regimens.
Dicenzo, R; Larppanichpoonphol, P; Luque, A; Reichman, R, 2006
)
0.88
" Once-daily dosing may offer an advantage to adherence."( Pharmacokinetics of a once-daily regimen of lopinavir/ritonavir in HIV-1-infected children.
Burger, D; de Groot, R; van der Lee, M; Verweel, G, 2006
)
0.59
" Further research, especially in young children, is necessary to determine whether a higher dosage of lopinavir/ritonavir once daily must be given to reach the target level for Cmin."( Pharmacokinetics of a once-daily regimen of lopinavir/ritonavir in HIV-1-infected children.
Burger, D; de Groot, R; van der Lee, M; Verweel, G, 2006
)
0.81
" 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
)
0.54
" Additional investigations are warranted to determine the optimal dosing of FPV with LPV/RTV."( Dose separation does not overcome the pharmacokinetic interaction between fosamprenavir and lopinavir/ritonavir.
Corbett, AH; Eron, JJ; Kalvass, LA; Kashuba, AD; Lim, ML; Ngo, LT; Patterson, KB; Tien, HC, 2006
)
0.55
" The consequences of these pharmacokinetic discrepancies and the necessity to modify the currently recommended dosage regimen should be further investigated."( Population analysis of weight-, age-, and sex-related differences in the pharmacokinetics of lopinavir in children from birth to 18 years.
Blanche, S; Chaix, ML; Delaugerre, C; Firtion, G; Hirt, D; Jullien, V; Macassa, E; Pons, G; Rey, E; Rouzioux, C; Teglas, JP; Tréluyer, JM; Urien, S; Vaz, P, 2006
)
0.55
" The pharmacokinetics, safety, and effectiveness of increased LPV/r dosing during the third trimester of pregnancy should be investigated."( Reduced lopinavir exposure during pregnancy.
Best, BM; Burchett, SK; Capparelli, E; Cotter, A; Elgie, C; Holland, DT; Hu, C; Mirochnick, M; Read, JS; Smith, E; Stek, AM; Tuomala, R, 2006
)
0.77
" After a regular oral dose of Kaletra (400 mg lopinavir, 100 mg ritonavir) analyte concentrations were detectable over a full dosing interval in plasma, ultrafiltrate, and PBMCs."( Monitoring of lopinavir and ritonavir in peripheral blood mononuclear cells, plasma, and ultrafiltrate using a selective and highly sensitive LC/MS/MS assay.
Burhenne, J; Ehrhardt, M; Haefeli, WE; Mikus, G; Möck, M, 2007
)
0.96
" Melt extrusion technology was used to produce a tablet formulation reducing the number of dosage units administered per day and simplifying storage requirements."( The tablet formulation of lopinavir/ritonavir provides similar bioavailability to the soft-gelatin capsule formulation with less pharmacokinetic variability and diminished food effect.
Awni, W; Breitenbach, J; Brun, SC; Chiu, YL; Doan, T; Hanna, GJ; Heuser, RS; Klein, CE; Morris, JB; Zhu, T, 2007
)
0.64
"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 ATV area under the concentration-time curve from dosing to 24 hours after the dose (AUC0-24; GM: 36."( Beneficial pharmacokinetic interaction between atazanavir and lopinavir/ritonavir.
Agarwala, S; Barditch-Crovo, P; Carson, K; Flexner, C; Fuchs, E; Parsons, T; Pham, PA; Vasist, L, 2007
)
0.58
" This coformulation was designed to overcome the problems of earlier agents of this class of drugs concerning unfavorable pharmacokinetics with a higher frequency of dosing and therapy failure."( Lopinavir/ritonavir: appraisal of its use in HIV therapy.
von Hentig, N, 2007
)
1.78
" The timing and dosage regimens of steroid in the treatment of SARS are controversial."( Pharmacologic treatment of SARS: current knowledge and recommendations.
Tai, DY, 2007
)
0.34
" Individuals established on ATV (300 mg and 100 mg ritonavir daily) or LPV (400 mg and 100 mg ritonavir twice daily)-containing regimens completed two clinical visits (trough and directly observed therapy) during which dosing characteristics, concomitant medication, and substance use were recorded."( Assessing the impact of substance use and hepatitis coinfection on atazanavir and lopinavir trough concentrations in HIV-infected patients during therapeutic drug monitoring.
Boston, NS; Brazeau, D; Catanzaro, L; DiFrancesco, R; Fischl, MA; Forrest, A; Gripshover, B; Ma, Q; Morse, GD; Reichman, RC; Slish, J; Zingman, BS, 2007
)
0.57
" 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
" These data indicate that chronic HIV treatment may be assisted with plasma concentration monitoring to identify those patients who may require dosage modification and/or regimen adjustment in order to optimize antiretroviral effects."( Factors associated with altered pharmacokinetics in substance users and non-substance users receiving lopinavir and atazanavir.
Boston, N; Brazeau, D; Catanzaro, LM; DiFrancesco, R; Fischl, MA; Forrest, A; Gripshover, B; Higgins, N; Lliguicota, F; Ma, Q; Morse, GD; Reichman, RC; Slish, J; Tooley, K; Zingman, BS,
)
0.35
"We assessed the safety and efficacy and evaluated the adherence to lopinavir/ritonavir (LPV/r) dosed QD or BID in antiretroviral-naive, HIV-1-infected subjects through 96 weeks of treatment."( A lopinavir/ritonavir-based once-daily regimen results in better compliance and is non-inferior to a twice-daily regimen through 96 weeks.
Domingo, P; Hairrell, JM; Hanna, GJ; Johnson, MA; King, MS; Molina, JM; Myers, R; Podsadecki, TJ; Rode, RA; Wilkin, A, 2007
)
1.3
" Rosuvastatin and lopinavir/ritonavir should be used with caution until the safety, efficacy, and appropriate dosing of this combination have been demonstrated in larger populations."( Drug/Drug interaction between lopinavir/ritonavir and rosuvastatin in healthy volunteers.
Flynn, DM; Gerber, JG; Hoody, DW; Kiser, JJ; Predhomme, JA; Wolfe, P, 2008
)
0.97
" From days 6-15, volunteers were randomized to receive lopinavir/ritonavir tablets dosed as either 600/150 or 800/200 mg twice daily, both in addition to 600 mg rifampicin once daily."( High incidence of adverse events in healthy volunteers receiving rifampicin and adjusted doses of lopinavir/ritonavir tablets.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Koopmans, PP; L'homme, RF; Nijland, HM; Rongen, GA; van Crevel, R; van Uden, P, 2008
)
0.81
"Fifty children at 2 sites in Thailand were treated with standard dosing of SQV and LPV/r."( Double boosted protease inhibitors, saquinavir, and lopinavir/ritonavir, in nucleoside pretreated children at 48 weeks.
Ananworanich, J; Boonrak, P; Bunupuradah, T; Burger, D; Engchanil, C; Intasan, J; Kosalaraksa, P; Lumbiganon, P; Ruxrungtham, K; Schutz, M, 2008
)
0.6
"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
)
0.59
" Further exploration of regimens and dosing of antiretrovirals for children in these settings is needed."( Two-year outcomes of children on non-nucleoside reverse transcriptase inhibitor and protease inhibitor regimens in a South African pediatric antiretroviral program.
Berrisford, AE; Boulle, AM; Jaspan, HB, 2008
)
0.35
"Use of standard adult lopinavir/ritonavir (LPV/RTV) dosing (400/100 mg) during the third trimester of pregnancy results in reduced LPV exposure."( Lopinavir exposure with an increased dose during pregnancy.
Best, BM; Burchett, SK; Capparelli, E; Gaddipati, S; Holland, DT; Hu, C; Mirochnick, M; Read, JS; Smith, E; Stek, AM, 2008
)
2.1
" These data suggest that the higher LPV/RTV dose should be used in third trimester pregnant women; that it should be considered in second trimester pregnant women, especially those who are protease inhibitor experienced; and that postpartum LPV/RTV dosing can be reduced to standard dosing by 2 weeks after delivery."( Lopinavir exposure with an increased dose during pregnancy.
Best, BM; Burchett, SK; Capparelli, E; Gaddipati, S; Holland, DT; Hu, C; Mirochnick, M; Read, JS; Smith, E; Stek, AM, 2008
)
1.79
" Three different dosing regimens of elvucitabine were administered with lopinavir-ritonavir to 24 subjects with moderate levels of HIV."( Multiple-dose pharmacokinetic behavior of elvucitabine, a nucleoside reverse transcriptase inhibitor, administered over 21 days with lopinavir-ritonavir in human immunodeficiency virus type 1-infected subjects.
Colucci, P; Ducharme, MP; Hoepelman, IM; Pottage, JC; Robison, H; Schürmann, D; Turgeon, J, 2009
)
0.79
" These values were lower compared with the half-life over the respective dosing intervals (7."( Pharmacokinetics of atazanavir/ritonavir once daily and lopinavir/ritonavir twice and once daily over 72 h following drug cessation.
Back, D; Boffito, M; Else, L; Gazzard, B; Khoo, S; Moyle, G; Pozniak, A; Sousa, M; Taylor, J, 2008
)
0.59
" 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
" No evidence is available to guide dosing of lopinavir/ritonavir in tablet formulation in this setting."( Lopinavir/ritonavir pharmacokinetics in a substitution of high-dose soft-gelatin capsule to tablet formulation.
Guillemi, S; Harrigan, PR; Harris, M; Hull, MW; Lima, V; Montaner, JS, 2009
)
2.06
"The tablet formulation could probably result in improved lopinavir dosing and increases the feasibility of once-daily lopinavir/ritonavir-based regimens in children."( Pharmacokinetics of lopinavir in HIV type-1-infected children taking the new tablet formulation once daily.
Burger, DM; Driessen, GJ; Hartwig, NG; van der Flier, M; van der Knaap, LC; van der Lee, M; van Jaarsveld, P; Verweel, G, 2008
)
0.91
" We have some theoretical and clinical data available that enables us to consider the possibility of administering DRV/r once a day in some patients with a few mutations in the protease and in those where this dosing regime is considered important."( [Darunavir as first-line therapy. The TITAN study].
Curran, A; Ribera Pascuet, E, 2008
)
0.35
"A total of 191 patients were randomized 2:2:2:1 to one of three APL dosing regimens or to lamivudine (3TC)/zidovudine (ZDV) twice daily (bid), each in combination with lopinavir/ritonavir (LPV/r) 400 mg/100 mg bid."( Antiviral activity and safety of aplaviroc, a CCR5 antagonist, in combination with lopinavir/ritonavir in HIV-infected, therapy-naïve patients: results of the EPIC study (CCR100136).
Adkison, KK; Berger, D; Bonny, T; Cimoch, P; Lamarca, A; Lazzarin, A; Madison, SJ; McCarty, D; Millard, J; Nichols, WG; Salvato, P; Smaill, FM; Teofilo, E; Yeni, P, 2009
)
0.77
" Study M05-730 compared LPV/r tablets dosed once daily vs."( A once-daily lopinavir/ritonavir-based regimen is noninferior to twice-daily dosing and results in similar safety and tolerability in antiretroviral-naive subjects through 48 weeks.
Bernstein, B; Cohen, DE; da Silva, BA; Fredrick, L; Gathe, J; Gibbs, S; Loutfy, MR; Marsh, T; Naylor, C; Podzamczer, D; Rubio, R, 2009
)
0.72
" Safety and tolerability of once-daily and twice-daily dosing was also comparable."( A once-daily lopinavir/ritonavir-based regimen is noninferior to twice-daily dosing and results in similar safety and tolerability in antiretroviral-naive subjects through 48 weeks.
Bernstein, B; Cohen, DE; da Silva, BA; Fredrick, L; Gathe, J; Gibbs, S; Loutfy, MR; Marsh, T; Naylor, C; Podzamczer, D; Rubio, R, 2009
)
0.72
" We report the pharmacokinetics of standard LPV-ritonavir dosing (400/100 mg twice daily) in the immediate and early postpartum period when initiated during labor."( Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
Achalapong, J; Chotivanich, N; Cressey, TR; Jourdain, G; Maupin, R; Mirochnick, M; Prommas, S; Puthanakit, T; Roongpisuthipong, A; Shapiro, DE; Smith, E; Van Dyke, R; Yuthavisuthi, P, 2009
)
0.63
" Statistical analyses were performed on pharmacokinetic parameters: the area under the concentration-time curve from 0 to 4 h (AUC(0-4)), the maximum concentration of the drug (C(max)), and the residual concentration of the drug at the end of the dosing interval (C(trough)) for plasma and the AUC(0-4) and C(trough) for intracellular data."( Pilot pharmacokinetic study of human immunodeficiency virus-infected patients receiving tenofovir disoproxil fumarate (TDF): investigation of systemic and intracellular interactions between TDF and abacavir, lamivudine, or lopinavir-ritonavir.
Ayen, R; Clotet, B; Grassi, J; Levi, M; Negredo, E; Pruvost, A; Puig, J; Théodoro, F, 2009
)
0.54
" However, oxymethylphosphate (OMP) and oxyethylphosphate (OEP) prodrugs provided improved rates of cleavage, high levels of aqueous solubility, and high plasma levels of the parent drugs when dosed orally in rats and dogs."( Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir.
DeGoey, DA; Flosi, WJ; Grampovnik, DJ; Kati, WM; Kempf, DJ; Klein, LL; Liu, Y; Long, MA; Marsh, KC; McDaniel, KF; Molla, A; Wang, XC, 2009
)
0.58
"In total, 50 children from two sites in Thailand were treated with standard dosing of SQV and LPV/r."( Safety and efficacy of a double-boosted protease inhibitor combination, saquinavir and lopinavir/ritonavir, in pretreated children at 96 weeks.
Ananworanich, J; Boonrak, P; Bunupuradah, T; Burger, D; Engchanil, C; Kosalaraksa, P; Lumbiganon, P; Mahanontharit, A; Mengthaisong, T; Puthanakit, T; Ruxrungtham, K; Tompkins, E; van der Lugt, J, 2009
)
0.58
"This study suggests that the pharmacokinetics of lopinavir after twice-daily and once-daily dosing are similar, with no observable difference in tolerability, in this group of patients between 5 and 15 years old."( Pharmacokinetics and tolerability of once- versus twice-daily lopinavir/ritonavir treatment in HIV-1-infected children.
la Porte, C; Mitchell, CD; Parker, J; Rongkavilit, C; van Heeswijk, R; Zhang, G, 2009
)
0.85
"A total of 136 antiretroviral-naïve patients, with a CD4 cell count above 100 cells/microL and a plasma HIV RNA below 100,000 HIV-1 RNA copies/mL, were randomized and dosed with either lopinavir/ritonavir monotherapy (n = 83) or lopinavir/ritonavir + zidovudine/lamivudine (n = 53)."( Long-term (96-week) follow-up of antiretroviral-naïve HIV-infected patients treated with first-line lopinavir/ritonavir monotherapy in the MONARK trial.
Chaix, ML; Cohen-Codar, I; Delfraissy, JF; Dellamonica, P; Flandre, P; Ghosn, J; Girard, PM; Ngovan, P; Norton, M; Raffi, F, 2010
)
0.77
"Virologically controlled patients treated with lopinavir/ritonavir were included in a 48 week pilot trial during which lopinavir/ritonavir dosage was reduced if lopinavir concentration was >5000 ng/mL at inclusion."( Impact of reduced dosing of lopinavir/ritonavir in virologically controlled HIV-infected patients: the Kaledose trial.
Girard, PM; Lacombe, K; Meynard, JL; Morand-Joubert, L; Poirier, JM; Slama, L; Valantin, MA, 2010
)
0.91
"This pilot study evaluating the biochemical and virological impact of a reduced dosing of lopinavir/ritonavir suggests that lower exposure to lopinavir/ritonavir could be associated with a significant decrease in triglycerides during treatment, without occurrence of resistance mutations that might impact the virological response to treatment."( Impact of reduced dosing of lopinavir/ritonavir in virologically controlled HIV-infected patients: the Kaledose trial.
Girard, PM; Lacombe, K; Meynard, JL; Morand-Joubert, L; Poirier, JM; Slama, L; Valantin, MA, 2010
)
0.88
" Each subject had 8 plasma lopinavir concentrations determined over a 12-hour dosing interval and 1 CSF lopinavir C(trough) value determined at the end of the study."( Lopinavir cerebrospinal fluid steady-state trough concentrations in HIV-infected adults.
Cruttenden, K; DiCenzo, R; DiFrancesco, R; Donnelly, J; Schifitto, G, 2009
)
2.09
"In this case, dosing recommendations of itraconazole 200 mg daily with lopinavir/ritonavir were appropriate."( Drug-drug interaction between itraconazole and the protease inhibitor lopinavir/ritonavir.
Hills-Nieminen, C; Houston, S; Hughes, CA; Shafran, SD, 2009
)
0.82
"The dose of itraconazole was reduced to 200 mg daily as recommended by current guidelines, and therapeutic drug monitoring of both itraconazole and lopinavir concentrations confirmed that no further dosage adjustments were necessary."( Drug-drug interaction between itraconazole and the protease inhibitor lopinavir/ritonavir.
Hills-Nieminen, C; Houston, S; Hughes, CA; Shafran, SD, 2009
)
0.79
"LPV/r dosed QD resulted in increased treatment adherence and was as efficacious as BID LPV/r while providing similar safety, tolerability, and limited resistance evolution."( Similar safety and efficacy of once- and twice-daily lopinavir/ritonavir tablets in treatment-experienced HIV-1-infected subjects at 48 weeks.
Andrade-Villanueva, J; Badal-Faesen, S; Bernstein, BM; Fredrick, LM; Gathe, J; Gaultier, IA; Mingrone, H; Podsadecki, TJ; Woodward, WC; Zajdenverg, R, 2010
)
0.61
" To compare efficacy of once-daily (QD) versus twice-daily (BID) antiretroviral therapy, we randomized human immunodeficiency virus (HIV)-positive, treatment-naive patients to lopinavir-ritonavir (LPV/r) administered at a dosage of 400 mg of lopinavir and 100 mg of ritonavir BID (n = 160) or 800 mg of lopinavir and 200 mg of ritonavir QD (n = 161), plus either emtricitabine 200 mg QD and extended-release stavudine at a dosage of 100 mg QD or tenofovir at a dosage of 300 mg QD."( Comparison of once-daily versus twice-daily combination antiretroviral therapy in treatment-naive patients: results of AIDS clinical trials group (ACTG) A5073, a 48-week randomized controlled trial.
Aberg, J; Andrade, A; Dehlinger, M; Eshleman, SH; Ferguson, E; Flexner, C; Gross, R; Kashuba, A; Kmack, A; Lalama, C; Mildvan, D; Parsons, T; Rosenkranz, SL; Sanne, I; Tierney, C, 2010
)
0.55
" A total of 82% of subjects completed the study, and 71% continued to receive the initially assigned dosage schedule."( Comparison of once-daily versus twice-daily combination antiretroviral therapy in treatment-naive patients: results of AIDS clinical trials group (ACTG) A5073, a 48-week randomized controlled trial.
Aberg, J; Andrade, A; Dehlinger, M; Eshleman, SH; Ferguson, E; Flexner, C; Gross, R; Kashuba, A; Kmack, A; Lalama, C; Mildvan, D; Parsons, T; Rosenkranz, SL; Sanne, I; Tierney, C, 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
)
0.96
" No dosage adjustment for S/GSK1349572 is required when used with lopinavir/ritonavir or darunavir/ritonavir."( The effect of lopinavir/ritonavir and darunavir/ritonavir on the HIV integrase inhibitor S/GSK1349572 in healthy participants.
Borland, J; Chen, S; Ishibashi, T; Lou, Y; Min, SS; Patel, P; Piscitelli, SC; Song, I, 2011
)
0.97
" Lopinavir CL/F increased linearly during the dosing interval."( Population pharmacokinetics of lopinavir in combination with rifampicin-based antitubercular treatment in HIV-infected South African children.
Elsherbiny, D; Maartens, G; McIlleron, H; Ren, Y; Simonsson, US, 2010
)
1.56
" The time-dependent lopinavir CL/F might be due to a time-dependent recovery from ritonavir inhibition of lopinavir metabolism during the dosing interval."( Population pharmacokinetics of lopinavir in combination with rifampicin-based antitubercular treatment in HIV-infected South African children.
Elsherbiny, D; Maartens, G; McIlleron, H; Ren, Y; Simonsson, US, 2010
)
0.97
" Postpartum dosing can be reduced to standard dosing before 2 weeks postpartum."( Lopinavir tablet pharmacokinetics with an increased dose during pregnancy.
Best, BM; Burchett, SK; Capparelli, EV; Hu, C; Li, H; Mirochnick, M; Read, JS; Rossi, SS; Smith, E; Stek, AM, 2010
)
1.8
" Buprenorphine/naloxone and LPV/r can be safely coadministered without need for dosage modification."( Pharmacokinetic interactions between buprenorphine/naloxone and once-daily lopinavir/ritonavir.
Altice, FL; Andrews, L; Bruce, RD; Fang, WB; Friedland, GH; Lin, SN; Ma, Q; Moody, DE; Morse, GD, 2010
)
0.59
" Emergence of postbaseline resistance mutations occurred at similar low rates in each dosing group."( Short communication: Comparable safety and efficacy with once-daily versus twice-daily dosing of lopinavir/ritonavir tablets with emtricitabine + tenofovir DF in antiretroviral-naïve, HIV type 1-infected subjects: 96 week final results of the randomized t
Bernstein, B; Cohen, D; da Silva, B; Fredrick, L; González-García, J; Johnson, M; Naylor, C; Sloan, L, 2010
)
0.58
" Coadministration with LPV/r resulted in a 51% decrease in steady-state area under plasma concentration-time curve from 0 to 12 hours (AUC(0-12,ss)) and steady-state maximum measured plasma concentration over a dosing interval (C(max,ss)) and a 50% decrease in steady-state plasma concentration 12 hours post last dosing (C(12,ss)) for BILR 355."( Coadministration with lopinavir and ritonavir decreases exposure to BILR 355, a nonnucleoside reverse transcriptase inhibitor, in healthy volunteers.
Berger, F; Castles, MA; Huang, DB; Huang, F; MacGregor, TR; Robinson, P; Scholl, P; Vinisko, R, 2011
)
0.68
" Conclusions The above target concentrations achieved in the majority of women and similarities in the fu% suggest standard dosing of the LPV/r tablet is appropriate during pregnancy."( Therapeutic drug monitoring of lopinavir/ritonavir in pregnancy.
Back, DJ; Boyle, N; Breiden, J; Brennan, M; Connor, EO; Coulter-Smith, S; Dickinson, L; Else, LJ; Fleming, C; Gibbons, S; Jackson, V; Khoo, SH; Lambert, JS, 2011
)
0.66
" Healthy volunteer studies have demonstrated a decrease in glucose disposal associated with dosing with specific antiretrovirals."( Effect of boosted fosamprenavir or lopinavir-based combinations on whole-body insulin sensitivity and lipids in treatment-naive HIV-type-1-positive men.
Back, DJ; Boffito, M; Jackson, AG; Mandalia, S; Moyle, GJ; Randell, PA; Taylor, J; Tjia, JF, 2010
)
0.64
" Initial TDM results prompted dosage change in 10% and assessment of adherence and/or pharmacist review in 11%."( Utility of therapeutic drug monitoring in the management of HIV-infected pregnant women in receipt of lopinavir.
Caswell, RJ; Chaponda, M; Ghanem, M; Gibbons, S; Jackson, V; Khoo, SH; Lambert, JS; Phillips, D; Poulton, M; Taylor, GP; Welch, J, 2011
)
0.58
"Nonlinear mixed-effects modeling was applied to explore the relationship between lopinavir and ritonavir concentrations over 72 h following drug cessation and also to assess other lopinavir and ritonavir dosing strategies compared to the standard 400-mg-100-mg twice-daily dose."( Sequential population pharmacokinetic modeling of lopinavir and ritonavir in healthy volunteers and assessment of different dosing strategies.
Aarons, L; Back, D; Boffito, M; Davies, G; Dickinson, L; Else, L; Khoo, S; Moyle, G; Pozniak, A; von Hentig, N, 2011
)
0.85
" We aimed at determining the optimal dosing regimen in neonates and infants weighing 1 to 10."( Lopinavir/ritonavir population pharmacokinetics in neonates and infants.
Anderson, ST; Blanche, S; Faye, A; Firtion, G; Giraud, C; Hirt, D; Khoo, S; Leprevost, M; Lyall, H; Peytavin, G; Solas, C; Thuret, I; Tréluyer, JM; Urien, S, 2011
)
1.81
" Based upon trough concentration limitations, suggested LPV/r dosing regimens were 40 mg 12 h(-1), 80 mg 12 h(-1) and 120 mg 12 h(-1) in the 1-2 kg, 2-6 kg and 6-10 kg group, respectively."( Lopinavir/ritonavir population pharmacokinetics in neonates and infants.
Anderson, ST; Blanche, S; Faye, A; Firtion, G; Giraud, C; Hirt, D; Khoo, S; Leprevost, M; Lyall, H; Peytavin, G; Solas, C; Thuret, I; Tréluyer, JM; Urien, S, 2011
)
1.81
"To describe laboratory abnormalities among HIV-infected women and their infants with standard and increased lopinavir/ritonavir (LPV/r) dosing during the third trimester of pregnancy."( Lopinavir/ritonavir dosing during pregnancy in Brazil and maternal/infant laboratory abnormalities.
Ceriotto, M; João, EC; Kreitchmann, R; Melo, VH; Mussi-Pinhata, MM; Peixoto, MF; Pilotto, JH; Read, J; Souza, Rda S; Stoszek, SK,
)
1.79
"164 women received LPV/r standard dosing [(798/198 or 800/200 mg/day) (Group 1)] and 70 increased dosing [(> 800/200 mg/day) (Group 2)]."( Lopinavir/ritonavir dosing during pregnancy in Brazil and maternal/infant laboratory abnormalities.
Ceriotto, M; João, EC; Kreitchmann, R; Melo, VH; Mussi-Pinhata, MM; Peixoto, MF; Pilotto, JH; Read, J; Souza, Rda S; Stoszek, SK,
)
1.57
" Increased LPV/r dosing during the third trimester of pregnancy appears to be safe for HIV-infected women and their infants."( Lopinavir/ritonavir dosing during pregnancy in Brazil and maternal/infant laboratory abnormalities.
Ceriotto, M; João, EC; Kreitchmann, R; Melo, VH; Mussi-Pinhata, MM; Peixoto, MF; Pilotto, JH; Read, J; Souza, Rda S; Stoszek, SK,
)
1.57
" 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
)
1.28
"Lopinavir exposure was reduced during the third trimester in pregnant women receiving standard dosing of the soft-gel capsule (SGC; 400/100 mg twice daily [b."( Improved oral bioavailability of lopinavir in melt-extruded tablet formulation reduces impact of third trimester on lopinavir plasma concentrations.
Back, DJ; Dickinson, L; Douglas, M; Else, LJ; Khoo, SH; Taylor, GP, 2012
)
2.1
"Atazanavir geometric mean (CV%) C(max), C(min) and AUC over the dosing interval were 2897 (46) ng/mL, 526 (57) ng/mL and 28 605 (46) ng · h/mL, respectively, and for lopinavir they were 10 655 (51) ng/mL, 5944 (68) ng/mL and 90 946 (59) ng · h/mL, respectively."( Pharmacokinetics and inhibitory quotient of atazanavir/ritonavir versus lopinavir/ritonavir in HIV-infected, treatment-naive patients who participated in the CASTLE Study.
Bertz, R; Child, M; Eley, T; Farajallah, A; Krystal, M; Liao, S; McGrath, D; Molina, JM; Persson, A; Sevinsky, H; Xu, X; Zhang, J; Zhu, L, 2012
)
0.81
" A population PK analysis was performed using NONMEM to characterize changes in lopinavir (LPV) PK relating to maturational changes in infants, and to assess dosing requirements in this population."( Assessment of lopinavir pharmacokinetics with respect to developmental changes in infants and the impact on weight band-based dosing.
Alvero, C; Capparelli, EV; Chadwick, EG; Hazra, R; Heckman, BE; Hughes, ML; Nikanjam, M; Palumbo, P; Pinto, J; Robbins, B; Yogev, R, 2012
)
0.97
"In this study, a slight but not significant decrease in the plasma lopinavir C(trough) was found during the third trimester of pregnancy, suggesting that standard dosing of the tablet formulation is also appropriate during the later stages of pregnancy."( Lopinavir/ritonavir trough concentrations with the tablet formulation in HIV-1-infected women during the third trimester of pregnancy.
Borderi, M; Calza, L; Colangeli, V; Grossi, G; Manfredi, R; Motta, R; Salvadori, C; Trapani, F; Viale, P, 2012
)
2.06
" Simulations of the lopinavir concentration profile were performed with different dosing regimens considering the different alleles."( Estimation of the effect of SLCO1B1 polymorphisms on lopinavir plasma concentration in HIV-infected adults.
Back, DJ; Boffito, M; Davies, G; Dickinson, L; Egan, D; Khoo, SH; Owen, A; Schipani, A; Youle, M, 2012
)
0.95
" Intensive pharmacokinetic sampling was performed 7 days apart after LPV/r dosing under moderate fat, high fat, and fasted meal conditions."( Steady-state pharmacokinetics of lopinavir plus ritonavir when administered under different meal conditions in HIV-infected Ugandan adults.
Back, D; Boffito, M; Byakika-Kibwika, P; Khoo, S; Lamorde, M; Mayito, J; Merry, C; Nabukeera, L; Ogwal-Okeng, J; Ryan, M; Tjia, J, 2012
)
0.66
" Prospective pharmacokinetic studies to devise a rational dosing strategy for vinblastine in patients receiving ritonavir/lopinavir are warranted."( Incidence, predictors and significance of severe toxicity in patients with human immunodeficiency virus-associated Hodgkin lymphoma.
Boro, J; Cheung, MC; Ezzat, HM; Harris, M; Hicks, LK; Leitch, HA; Lima, VD; Montaner, JS, 2012
)
0.59
" Factors that may have contributed to the suboptimal results with nevirapine include elevated viral load at baseline, selection for nevirapine resistance, background regimen of nucleoside reverse-transcriptase inhibitors, and the standard ramp-up dosing strategy."( Nevirapine versus ritonavir-boosted lopinavir for HIV-infected children.
Abrams, EJ; Barlow-Mosha, L; Bobat, R; Chi, BH; Cotton, MF; Eshleman, SH; Hughes, MD; Jean-Philippe, P; Kamthunzi, P; Khadse, S; Lindsey, JC; Millar, L; Mofenson, LM; Moultrie, H; Mujuru, HA; Palumbo, P; Petzold, E; Purdue, L; Schimana, W; Violari, A, 2012
)
0.65
" 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
" However, there are challenges to initiate ART in early life, including the possibility of drug resistance in the context of prevention of mother-to-child transmission (PMTCT) programs, a paucity of drug choices , uncertain dosing for some medications and long-term toxicities."( Effectiveness of antiretroviral therapy in HIV-infected children under 2 years of age.
Cotton, M; Gibb, D; Penazzato, M; Prendergast, A; Tierney, J, 2012
)
0.38
" We described the free and total pharmacokinetics of lopinavir in HIV-infected pregnant and non-pregnant women, and evaluated whether significant alterations in its disposition and protein binding warrant systematic dosage adjustment."( Free and total plasma levels of lopinavir during pregnancy, at delivery and postpartum: implications for dosage adjustments in pregnant women.
Biollaz, J; Buclin, T; Cavassini, M; Cruchon, S; Decosterd, LA; Eap, CB; Fayet-Mello, A; Grawe, C; Gremlich, E; Guignard, N; Martinez de Tejada, B; Popp, KA; Schmid, F; Telenti, A, 2013
)
0.92
" No dosage adjustment is therefore needed during pregnancy as it is unlikely to further enhance treatment efficacy but could potentially increase the risk of maternal and fetal toxicity."( Free and total plasma levels of lopinavir during pregnancy, at delivery and postpartum: implications for dosage adjustments in pregnant women.
Biollaz, J; Buclin, T; Cavassini, M; Cruchon, S; Decosterd, LA; Eap, CB; Fayet-Mello, A; Grawe, C; Gremlich, E; Guignard, N; Martinez de Tejada, B; Popp, KA; Schmid, F; Telenti, A, 2013
)
0.67
" Lopinavir AUC(0-24) following twice-daily and once-daily dosing was 169."( Once- versus twice-daily lopinavir/ritonavir tablets in virologically suppressed, HIV-infected, treatment-experienced children: comparative pharmacokinetics and virological outcome after switching to once-daily lopinavir/ritonavir.
Chokephaibulkit, K; Cressey, TR; Lapphra, K; Nuntarukchaikul, M; Phongsamart, W; Vanprapar, N; Wittawatmongkol, O, 2012
)
1.59
" Further efficacy studies of lopinavir/ritonavir once daily in children are necessary before routinely recommending this dosing strategy."( Once- versus twice-daily lopinavir/ritonavir tablets in virologically suppressed, HIV-infected, treatment-experienced children: comparative pharmacokinetics and virological outcome after switching to once-daily lopinavir/ritonavir.
Chokephaibulkit, K; Cressey, TR; Lapphra, K; Nuntarukchaikul, M; Phongsamart, W; Vanprapar, N; Wittawatmongkol, O, 2012
)
0.97
"In HIV-infected patients receiving rifampicin-based treatment for tuberculosis (TB), the dosage of lopinavir/ritonavir (LPV/r) is adjusted to prevent sub-therapeutic lopinavir concentrations."( Coadministration of lopinavir/ritonavir and rifampicin in HIV and tuberculosis co-infected adults in South Africa.
Gandhi, RT; Kuritzkes, DR; Marconi, VC; Murphy, RA; Sunpath, H, 2012
)
0.92
" The durability of coadministered treatment was significantly shorter in patients who received super-boosted lopinavir/ritonavir with TB treatment compared to patients who received standard lopinavir/ritonavir dosing (log rank, P = 0."( Coadministration of lopinavir/ritonavir and rifampicin in HIV and tuberculosis co-infected adults in South Africa.
Gandhi, RT; Kuritzkes, DR; Marconi, VC; Murphy, RA; Sunpath, H, 2012
)
0.91
"Uncertainty surrounds the correct dosing of lopinavir/r (LPV/r) in HIV-infected children not receiving non-nucleoside reverse transcriptase inhibitors."( Lopinavir dosing in HIV-infected children in the United Kingdom and Ireland.
Butler, K; Doerholt, K; Donegan, K; Gibb, DM; Judd, A; Lyall, H; Menson, E; Riordan, A; Shingadia, D; Tookey, P; Tudor-Williams, G; Walker, AS, 2013
)
2.09
" Results highlight the importance of optimizing dosing in HIV-infected children of all ages."( Lopinavir dosing in HIV-infected children in the United Kingdom and Ireland.
Butler, K; Doerholt, K; Donegan, K; Gibb, DM; Judd, A; Lyall, H; Menson, E; Riordan, A; Shingadia, D; Tookey, P; Tudor-Williams, G; Walker, AS, 2013
)
1.83
" Coadministration with boceprevir decreased RTV AUC during a dosing interval τ (AUC(τ)) by 22%-36%."( Pharmacokinetic interactions between the hepatitis C virus protease inhibitor boceprevir and ritonavir-boosted HIV-1 protease inhibitors atazanavir, darunavir, and lopinavir.
Butterton, JR; Feng, HP; Hughes, EA; Hulskotte, EG; O'Mara, E; Treitel, MA; van Zutven, MG; Wagner, JA; Xuan, F; Youngberg, SP, 2013
)
0.59
"Standard LPV dosing achieved therapeutic levels in pregnancy and no appreciable concentrations in breast milk."( Therapeutic levels of lopinavir in late pregnancy and abacavir passage into breast milk in the Mma Bana Study, Botswana.
Capparelli, E; Essex, M; Leidner, J; Lockman, S; Makhema, J; Moffat, C; Moss, M; Moyo, S; Ogwu, A; Rossi, S; Shapiro, RL, 2013
)
0.7
" Until then, guidelines for drug-drug interactions and dosing in renal and hepatic impairment should be followed in older HIV-infected individuals."( Clinical pharmacokinetics of antiretroviral drugs in older persons.
Anderson, PL; Erlandson, KM; Schoen, JC, 2013
)
0.39
" Lopinavir plasma exposure as estimated by the area under the concentration-time curve over the 12-h dosing interval (AUC(0-12h), AUCτ) was determined on day 14 and again on day 21."( Co-administration of a commonly used Zimbabwean herbal treatment (African potato) does not alter the pharmacokinetics of lopinavir/ritonavir.
Aweeka, F; Greenblatt, R; Guglielmo, BJ; Gwaza, L; Huang, L; Lizak, P, 2013
)
1.51
" Our results demonstrate that the HIV PI lopinavir inhibits liver stage parasites at clinically relevant concentrations, that is, at drug levels achieved in HIV-infected patients on standard dosing regimens."( The effect of antiretrovirals on Plasmodium falciparum liver stages.
Borkowsky, W; De La Vega, P; Duffy, PE; Hobbs, CV; Krzych, U; Penzak, SR; Sinnis, P; Van Vliet, J, 2013
)
0.66
" They are characterized by highly cooperative dose-response curves that are not explained by current pharmacodynamic theory."( Multi-step inhibition explains HIV-1 protease inhibitor pharmacodynamics and resistance.
Bailey, JR; Chioma, S; Durand, CM; Laird, GM; Laskey, S; Moore, RD; Rabi, SA; Shan, L; Siliciano, RF, 2013
)
0.39
" The model can also simulate a concentration-time course with a difference dosing and variable which can be used for further describing the pharmacology of the drug interaction when combine with the other drugs."( Compartmental pharmacokinetic modeling of lopinavir in humans.
Duangchaemkarn, K; Lohitnavy, M, 2013
)
0.65
" Pharmacokinetic studies suggest increasing the dosage of lopinavir/ritonavir (LPV/r) in pregnancy."( A randomized controlled trial to assess safety, tolerability, and antepartum viral load with increased lopinavir/ritonavir dosage in pregnancy.
Bonafe, SM; Castelo, A; Costa, DA; Machado, RH; Pott-Junior, H; Senise, JF; Vaz, MJ, 2013
)
0.85
"No major changes were identified in the group treated with the lowest dosing compared with the control."( Effects of combined zidovudine/lopinavir/ritonavir therapy during rat pregnancy: morphological aspects.
de Carvalho, LP; Kulay, L; Nakamura, MU; Oliveira-Filho, RM; Simões, RS; Tavella, JS; Wagner, A, 2013
)
0.68
" This comprehensive modelling and simulation approach could be used as a surrogate assessment of antiretroviral (ARV) activity where adequate early-phase dose-ranging studies are lacking in order to define target trough concentrations and possibly refine dosing recommendations."( Integrated population pharmacokinetic/viral dynamic modelling of lopinavir/ritonavir in HIV-1 treatment-naïve patients.
Acosta, EP; D'Argenio, DZ; Delille, C; Kerstner-Wood, C; Lennox, JL; Ofotokun, I; Sheth, AN; Wang, K, 2014
)
0.64
" Dosing is based on body weight bands or body surface area under FDA approval and only body surface area by the EMA."( Pharmacokinetics of pediatric lopinavir/ritonavir tablets in children when administered twice daily according to FDA weight bands.
Bastiaans, DE; Burger, DM; Chalermpantmetagul, S; Colbers, AP; Compagnucci, A; Cressey, TR; Forcat, S; Giaquinto, C; Hansudewechakul, R; Harper, LM; Inshaw, JR; Kanjanavanit, S; Königs, C; Lyall, H; Noguera-Julian, A; Saïdi, Y, 2014
)
0.69
"FDA weight band-based dosing recommendations provide adequate exposure to LPV when using LPV/r pediatric tablets."( Pharmacokinetics of pediatric lopinavir/ritonavir tablets in children when administered twice daily according to FDA weight bands.
Bastiaans, DE; Burger, DM; Chalermpantmetagul, S; Colbers, AP; Compagnucci, A; Cressey, TR; Forcat, S; Giaquinto, C; Hansudewechakul, R; Harper, LM; Inshaw, JR; Kanjanavanit, S; Königs, C; Lyall, H; Noguera-Julian, A; Saïdi, Y, 2014
)
0.69
" With both dosing regimens, 2 - 5 fold increases of the 25-O-desacetyl- rifabutin metabolite were observed when rifabutin was given with lopinavir/ritonavir compared with rifabutin alone."( Randomised pharmacokinetic trial of rifabutin with lopinavir/ritonavir-antiretroviral therapy in patients with HIV-associated tuberculosis in Vietnam.
Barrail-Tran, A; Borand, L; Connolly, C; Duc, NH; Dung, NH; Harries, AD; Lagarde, D; Lan, NN; Lan, NT; Laureillard, D; Lien, TT; Lienhardt, C; Pym, A; Quillet, C; Taburet, AM; Thu, NT, 2014
)
0.86
" LPV concentrations were also monitored on a routine basis, after 2 weeks of treatment initiation, between 1 and 24 hours after dosing in all children."( Concentration-response model of lopinavir/ritonavir in HIV-1-infected pediatric patients.
Benaboud, S; Blanche, S; Bouazza, N; Foissac, F; Frange, P; Hirt, D; Tréluyer, JM; Urien, S, 2014
)
0.69
"The CLPV90 derived from this model supports current dosing guidelines."( Concentration-response model of lopinavir/ritonavir in HIV-1-infected pediatric patients.
Benaboud, S; Blanche, S; Bouazza, N; Foissac, F; Frange, P; Hirt, D; Tréluyer, JM; Urien, S, 2014
)
0.69
" Twelve-hour intensive pharmacokinetic sampling after observed LPV/r intake (plus 2 nucleoside reverse transcriptase inhibitors) following World Health Organization 2010 dosing with food was performed 4 weeks after enrollment."( The pharmacokinetics and acceptability of lopinavir/ritonavir minitab sprinkles, tablets, and syrups in african HIV-infected children.
Burger, D; Fillekes, Q; Gibb, DM; Keishanyu, R; Kekitiinwa, A; Kendall, L; Lallemant, M; Musiime, V; Namuddu, R; Opilo, W; Walker, AS; Young, N, 2014
)
0.67
" However, there are challenges to initiation of ART in early life, including the possibility of drug resistance in the context of prevention of mother-to-child transmission (PMTCT) programs, a paucity of drug choices , uncertain dosing for some medications and long-term toxicities."( Optimisation of antiretroviral therapy in HIV-infected children under 3 years of age.
Abrams, E; Muhe, LM; Penazzato, M; Prendergast, AJ; Tindyebwa, D, 2014
)
0.4
" In South Africa, clinicians are advised to use 'double-dose' LPV/r dosed at 800 mg/200 mg twice daily during anti-tuberculosis treatment."( Double-dose lopinavir-ritonavir in combination with rifampicin-based anti-tuberculosis treatment in South Africa.
Chelin, N; Cohen, S; Gandhi, RT; Murphy, RA; Sunpath, H; Tennant, I; Winternheimer, P, 2014
)
0.78
" 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
)
0.61
" Efficacious, safe bedaquiline dosing for MDR-TB patients receiving antiretrovirals is important."( Impact of lopinavir-ritonavir or nevirapine on bedaquiline exposures and potential implications for patients with tuberculosis-HIV coinfection.
Dooley, KE; Karlsson, MO; Svensson, EM, 2014
)
0.8
"Standard dosing provides adequate lopinavir trough concentrations for the majority of pregnant women but increased doses may be preferable for women weighing >100 kg and with a history of lopinavir/ritonavir use and/or adherence issues."( Impact of body weight and missed doses on lopinavir concentrations with standard and increased lopinavir/ritonavir doses during late pregnancy.
Best, BM; Buranabanjasatean, S; Capparelli, EV; Cressey, TR; Jourdain, G; Lallemant, M; Limtrakul, A; Mirochnick, M; Rawangban, B; Sabsanong, P; Stek, A; Treluyer, JM; Urien, S, 2015
)
0.96
" This work aimed to develop appropriate drug ratios and dosing for each FDC."( Lopinavir/ritonavir plus lamivudine and abacavir or zidovudine dose ratios for paediatric fixed-dose combinations.
Bouazza, N; Burger, D; Capparelli, EV; Fauchet, F; Foissac, F; Kiechel, JR; Lallemant, M; Treluyer, JM; Urien, S, 2015
)
1.86
" Monte-Carlo simulations of WHO and FDA dosing recommendations were performed to assess their ability to provide optimal exposure in children weighing 4 to 25 kg based on consensus plasma targets."( Lopinavir/ritonavir plus lamivudine and abacavir or zidovudine dose ratios for paediatric fixed-dose combinations.
Bouazza, N; Burger, D; Capparelli, EV; Fauchet, F; Foissac, F; Kiechel, JR; Lallemant, M; Treluyer, JM; Urien, S, 2015
)
1.86
" Given the recommended drug ratios, the dosage for the 4-5."( Lopinavir/ritonavir plus lamivudine and abacavir or zidovudine dose ratios for paediatric fixed-dose combinations.
Bouazza, N; Burger, D; Capparelli, EV; Fauchet, F; Foissac, F; Kiechel, JR; Lallemant, M; Treluyer, JM; Urien, S, 2015
)
1.86
"We conducted an open-label study of rifabutin dosed at 5 mg/kg three times a week in HIV-infected children≤5 years of age receiving lopinavir/ritonavir."( Pharmacokinetics and safety of rifabutin in young HIV-infected children receiving rifabutin and lopinavir/ritonavir.
Gous, H; Kellermann, T; Kindra, G; McIlleron, H; Moultrie, H; Sawry, S; Van Rie, A; Wiesner, L, 2015
)
0.84
"Rifabutin dosed at 5 mg/kg three times per week resulted in lower AUC0-48, AUC0-24 and Cmax values for rifabutin and 25-O-desacetyl rifabutin compared with adults receiving 150 mg of rifabutin daily, the current recommended dose."( Pharmacokinetics and safety of rifabutin in young HIV-infected children receiving rifabutin and lopinavir/ritonavir.
Gous, H; Kellermann, T; Kindra, G; McIlleron, H; Moultrie, H; Sawry, S; Van Rie, A; Wiesner, L, 2015
)
0.64
" These high concentrations continued after delivery in spite of a dosage reduction."( CYP3A4 polymorphism and lopinavir toxicity in an HIV-infected pregnant woman.
Cabrera Figueroa, SE; Domínguez-Gil Hurlé, A; Iglesias Gómez, A; López Aspiroz, E; Valverde Merino, MP, 2015
)
0.72
"We document our experience with therapeutic drug monitoring (TDM) of antiretroviral agents (1807 determinations) carried out as day-by-day clinical practice for the optimization of drug dosing in HIV-infected patients."( Is it time to revise antiretrovirals dosing? a pharmacokinetic viewpoint.
Baldelli, S; Castoldi, S; Cattaneo, D; Charbe, N; Clementi, E; Cozzi, V; Fucile, S, 2014
)
0.4
" As these anti-HIV lipid nanoparticles also prolonged plasma drug exposure, they hold promise as a long-acting dosage form for HIV patients in addressing residual virus in cells and tissue."( Anti-HIV drug-combination nanoparticles enhance plasma drug exposure duration as well as triple-drug combination levels in cells within lymph nodes and blood in primates.
Freeling, JP; Ho, RJ; Koehn, J; Shu, C; Sun, J, 2015
)
0.42
" Sub-optimal dosing can lead to acquired rifamycin resistance (ARR)."( Randomized pharmacokinetic evaluation of different rifabutin doses in African HIV- infected tuberculosis patients on lopinavir/ritonavir-based antiretroviral therapy.
Connolly, C; Harries, A; Kellerman, T; Lienhardt, C; McIlleron, H; Naiker, S; Pym, A; Reddy, T; Wiesner, L, 2014
)
0.61
" Plasma d-RBT concentrations increased 5-fold with tiw rifabutin dosing and 15-fold with daily doses of rifabutin."( Randomized pharmacokinetic evaluation of different rifabutin doses in African HIV- infected tuberculosis patients on lopinavir/ritonavir-based antiretroviral therapy.
Connolly, C; Harries, A; Kellerman, T; Lienhardt, C; McIlleron, H; Naiker, S; Pym, A; Reddy, T; Wiesner, L, 2014
)
0.61
" The development of new antiretroviral drugs with simpler dosing regimens and lower toxicity has led to evaluation of innovative strategies such as dual therapy for initial ART in treatment-naive, with the aim of preventing long-term toxicity and increasing treatment adherence."( [Lopinavir/ritonavir in new initial antiretroviral treatment strategies].
Cahn, P; Figueroa, MI; Rolón, MJ; Sued, O, 2014
)
1.31
" In patients with renal failure, LPV/r does not require dosage adjustment because it is metabolized in the liver."( [Lopinavir/ritonavir in patients with human immunodeficiency virus infection in special situations].
Aldeguer, JL; Tasias, M, 2014
)
1.31
" Although combinations of ritonavir and lopinavir have shown higher plasma concentration level of LPV in clinical settings, dosage adjustment is still required to maintain an adequate therapeutic efficacy and reduce side effects."( A pharmacokinetic model of lopinavir in combination with ritonavir in human.
Duangchaemkarn, K; Lohitnavy, M; Reisfeld, B, 2014
)
0.97
" Plasma progesterone concentrations were measured every 2 weeks after DMPA dosing through week 12."( Depot medroxyprogesterone acetate in combination with a twice-daily lopinavir-ritonavir-based regimen in HIV-infected women showed effective contraception and a lack of clinically significant interactions, with good safety and tolerability: results of the
Aweeka, F; Cohn, SE; Cramer, Y; Klingman, KL; Livingston, E; Luque, AE; Park, JG; Watts, DH; Weinberg, A, 2015
)
0.65
"Atazanavir/ritonavir (ATV/r) recently became the preferred protease inhibitor (PI) for use in Nigeria since it is dosed once daily, which may improve treatment adherence and has fewer side effects than lopinavir/ritonavir (LPV/r)--the most widely available PI in resource-limited settings."( Immunological and Virological Outcomes of Patients Switched from LPV/r to ATV/r-Containing Second- Line Regimens.
Adeyemo, T; Akanmu, AS; Awolola, A; Bello, FO; Kanki, PJ; Lesi, F; Ogunsola, FT; Okonkwo, P; Okwuegbuna, K; Oloko, K, 2015
)
0.61
"The aims of this study were to describe the unbound and total lopinavir (LPV) pharmacokinetics in pregnant women in order to evaluate if a dosing adjustment is necessary during pregnancy."( Population approach to analyze the pharmacokinetics of free and total lopinavir in HIV-infected pregnant women and consequences for dose adjustment.
Blanche, S; Delmas, S; Fauchet, F; Hirt, D; Illamola, SM; Lechedanec, J; Lui, G; Mandelbrot, L; Pressiat, C; Treluyer, JM; Tubiana, R; Urien, S; Valade, E; Warszawski, J, 2015
)
0.89
"Major protease inhibitor resistance mutations were common in this study of HIV-1-infected children, with the timing of tuberculosis treatment and subsequent protease inhibitor dosing strategy proving to be important associated factors."( Factors Associated with the Development of Drug Resistance Mutations in HIV-1 Infected Children Failing Protease Inhibitor-Based Antiretroviral Therapy in South Africa.
Avenant, T; du Plessis, NM; Feucht, UD; Melikian, G; Rossouw, TM; Thomas, W; van Dyk, G, 2015
)
0.42
" In addition, linear mixed-effect analysis was used to compare the area under the concentration-time curve from 0 to 12 h (AUC0-12) and concentration prior to dosing (Cpredose) in pregnant women and nonpregnant subjects."( No Need for Lopinavir Dose Adjustment during Pregnancy: a Population Pharmacokinetic and Exposure-Response Analysis in Pregnant and Nonpregnant HIV-Infected Subjects.
Jones, AK; Klein, CE; Nilius, AM; Patterson, KB; Salem, AH; Santini-Oliveira, M; Taylor, GP, 2016
)
0.81
") dosing in children."( Once vs. twice-daily lopinavir/ritonavir in HIV-1-infected children.
, 2015
)
0.74
" dosing remains an option in selected, adherent children, with close viral load monitoring."( Once vs. twice-daily lopinavir/ritonavir in HIV-1-infected children.
, 2015
)
0.74
"The aim of this study was to develop a nanotechnology to formulate a fixed-dose combination of poorly water-soluble drugs in a children-friendly, flexible solid dosage form."( Development and in vivo evaluation of child-friendly lopinavir/ritonavir pediatric granules utilizing novel in situ self-assembly nanoparticles.
Dong, X; Guo, S; Li, D; Penzak, S; Pham, K, 2016
)
0.68
"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
)
0.64
"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
)
0.94
"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
)
0.64
"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
)
0.64
" This study sheds light on the complex dissolution and solution phase behavior of multicomponent amorphous dosage forms, in particular those containing poorly water soluble drugs, which may undergo supersaturation in vivo."( Compromised in vitro dissolution and membrane transport of multidrug amorphous formulations.
Alhalaweh, A; Bergström, CAS; Taylor, LS, 2016
)
0.43
" Here we present a population pharmacokinetic model to describe the longitudinal change of unbound lopinavir/ritonavir (LPV/RTV) PK parameters with gestational age, and to predict unbound LPV concentrations under different dosing regimens."( Model-Based Analysis of Unbound Lopinavir Pharmacokinetics in HIV-Infected Pregnant Women Supports Standard Dosing in the Third Trimester.
Chen, J; Dumond, JB; Malone, S; Patterson, KB; Prince, HM, 2016
)
0.93
" One hundred patients with pulmonary tuberculosis (65% coinfected with HIV-1) were intensively sampled to determine rifampin, isoniazid, and pyrazinamide plasma concentrations after 7 to 8 weeks of a daily quadruple-therapy regimen dosed according to World Health Organization (WHO) weight bands."( HIV-1 Coinfection Does Not Reduce Exposure to Rifampin, Isoniazid, and Pyrazinamide in South African Tuberculosis Outpatients.
Chirehwa, M; Denti, P; McIlleron, H; Meintjes, G; Rockwood, N; Wiesner, L; Wilkinson, RJ, 2016
)
0.43
" A hyperinsulinaemic euglycaemic clamp was performed prior to and following each 2-week dosing phase."( An open-label, randomized study of the impact on insulin sensitivity, lipid profile and vascular inflammation by treatment with lopinavir/ritonavir or raltegravir in HIV-negative male volunteers.
Boffito, M; Jackson, A; Milinkovic, A; Moyle, G; Randell, P, 2017
)
0.66
" For treatment, the WHO dosing guidelines should be suitable to maintain values above the therapeutic pharmacokinetic targets in most infants."( Are Prophylactic and Therapeutic Target Concentrations Different?: the Case of Lopinavir-Ritonavir or Lamivudine Administered to Infants for Prevention of Mother-to-Child HIV-1 Transmission during Breastfeeding.
Blanche, S; Blume, J; Bouazza, N; Foissac, F; Harper, K; Hirt, D; Illamola, SM; Kankasa, C; Meda, N; Nagot, N; Singata-Madliki, M; Tréluyer, JM; Tumwine, JK; Tylleskär, T; Van de Perre, P, 2017
)
0.68
" To normalise bedaquiline exposure in patients with concomitant LPV/r therapy, an adjusted bedaquiline dosing regimen is proposed for further study."( Confirming model-predicted pharmacokinetic interactions between bedaquiline and lopinavir/ritonavir or nevirapine in patients with HIV and drug-resistant tuberculosis.
Brill, MJ; Karlsson, MO; Maartens, G; Pandie, M; Svensson, EM, 2017
)
0.68
" Also, the exposure to LPV on the initial once-daily dosing regimen was determined."( Sustained Viral Suppression in HIV-infected Children on Once-daily Lopinavir/Ritonavir in Clinical Practice.
Bastiaans, DET; Burger, DM; de Groot, R; Driessen, GJA; Fraaij, PLA; Gondrie, IPE; Hartwig, NG; van der Knaap, LC; van Jaarsveld, P; van Rossum, AMC; Visser, EG, 2017
)
0.69
" Geometric mean LPV area under the plasma concentration-time curve (linear up-log down method) over a dosing interval from time 0 to 24 hours after dosing was 169."( Sustained Viral Suppression in HIV-infected Children on Once-daily Lopinavir/Ritonavir in Clinical Practice.
Bastiaans, DET; Burger, DM; de Groot, R; Driessen, GJA; Fraaij, PLA; Gondrie, IPE; Hartwig, NG; van der Knaap, LC; van Jaarsveld, P; van Rossum, AMC; Visser, EG, 2017
)
0.69
"Current presentations of the anti-HIV drugs lopinavir and ritonavir make appropriate dosing for children difficult."( Developing a Flexible Pediatric Dosage Form for Antiretroviral Therapy: A Fast-Dissolving Tablet.
Estrada, M; Lai, M; Lal, M; Zhu, C, 2017
)
0.72
" These factors should be taken into consideration to guide the individual tenofovir disoproxil fumarate dosage regimen in Thai HIV-infected patients."( Pharmacogenetics-based population pharmacokinetic analysis of tenofovir in Thai HIV-infected patients.
Avihingsanon, A; Burger, DM; Mitruk, S; Punyawudho, B; Rungtivasuwan, K; Ruxrungtham, K; Sukasem, C; Thammajaruk, N, 2017
)
0.46
"The World Health Organization (WHO) recommends weight band dosing of antiretrovirals for children."( A Phase II/III Trial of Lopinavir/Ritonavir Dosed According to the WHO Pediatric Weight Band Dosing Guidelines.
Capparelli, EV; Cressey, TR; Mirochnick, M; Pinto, JA; Qin, M; Siberry, GK; Smith, B; Spector, SA; Warshaw, M; Zimmer, B, 2018
)
0.79
"International Maternal Pediatric Adolescent AIDS Clinical Trials (IMPAACT) P1083 was a phase II/III trial assessing the pharmacokinetics (PK) and short-term safety, tolerance and efficacy of lopinavir/ritonavir in human immunodeficiency virus-infected children 3-25 kg dosed according to WHO weight bands, with liquid solution or meltrex extrusion tablets."( A Phase II/III Trial of Lopinavir/Ritonavir Dosed According to the WHO Pediatric Weight Band Dosing Guidelines.
Capparelli, EV; Cressey, TR; Mirochnick, M; Pinto, JA; Qin, M; Siberry, GK; Smith, B; Spector, SA; Warshaw, M; Zimmer, B, 2018
)
0.98
" The median (Q1, Q3) difference between individual observed PK parameters and those expected if Food and Drug Administration dosing guidelines were followed was 30."( A Phase II/III Trial of Lopinavir/Ritonavir Dosed According to the WHO Pediatric Weight Band Dosing Guidelines.
Capparelli, EV; Cressey, TR; Mirochnick, M; Pinto, JA; Qin, M; Siberry, GK; Smith, B; Spector, SA; Warshaw, M; Zimmer, B, 2018
)
0.79
"WHO weight band dosing guidelines in children achieved adequate LPV plasma exposure but was higher than that expected with Food and Drug Administration dosing guidelines."( A Phase II/III Trial of Lopinavir/Ritonavir Dosed According to the WHO Pediatric Weight Band Dosing Guidelines.
Capparelli, EV; Cressey, TR; Mirochnick, M; Pinto, JA; Qin, M; Siberry, GK; Smith, B; Spector, SA; Warshaw, M; Zimmer, B, 2018
)
0.79
"HIV-infected children admitted with severe acute malnutrition were randomized to early or delayed initiation of lopinavir (LPV)/ritonavir, abacavir and lamivudine using World Health Organization weight band dosage charts."( Population Pharmacokinetics of Lopinavir in Severely Malnourished HIV-infected Children and the Effect on Treatment Outcomes.
Archary, M; Bobat, R; Hennig, S; La Russa, P; Mcllleron, H; Sibaya, T; Wiesner, L, 2018
)
0.98
" In 4 macaques dosed subcutaneously, drug levels over 5 weeks in plasma, lymph node mononuclear cells (LNMCs), and peripheral blood mononuclear cells (PBMCs) were analyzed by liquid chromatography-tandem mass spectrometry."( Long-Acting Profile of 4 Drugs in 1 Anti-HIV Nanosuspension in Nonhuman Primates for 5 Weeks After a Single Subcutaneous Injection.
Collier, AC; Ho, RJY; Kinman, LM; Koehn, J; Kraft, JC; Lane, S; Lee, W; McConnachie, LA, 2018
)
0.48
"To evaluate the proportion of children with lopinavir Cmin ≥1 mg/L when receiving a novel 8-hourly lopinavir/ritonavir dosing strategy during rifampicin co-treatment."( Pharmacokinetics of adjusted-dose 8-hourly lopinavir/ritonavir in HIV-infected children co-treated with rifampicin.
McIlleron, H; Rabie, H; Rawizza, H; Van Rie, A; Wiesner, L; Winckler, J; Zar, H; Zuidewind, P, 2019
)
1.04
" Rifampicin was dosed at 10-20 mg/kg/day."( Pharmacokinetics of adjusted-dose 8-hourly lopinavir/ritonavir in HIV-infected children co-treated with rifampicin.
McIlleron, H; Rabie, H; Rawizza, H; Van Rie, A; Wiesner, L; Winckler, J; Zar, H; Zuidewind, P, 2019
)
0.78
" The final analysis data set contained 17,725 observations from 1,054 subjects, including healthy subjects and subjects with drug-sensitive, multidrug-resistant, or extensively drug-resistant pulmonary tuberculosis dosed pretomanid in monotherapy or combination therapy for up to 6 months."( Population Pharmacokinetics of the Antituberculosis Agent Pretomanid.
Everitt, D; Nedelman, JR; Salinger, DH; Subramoney, V, 2019
)
0.51
" The objective of the study was to apply physiologically-based pharmacokinetic (PBPK) modeling to predict optimal dosage regimens of quinine when coadministered with lopinavir/ritonavir in malaria and HIV coinfected patients with different conditions."( Physiologically-Based Pharmacokinetic Modeling for Optimal Dosage Prediction of Quinine Coadministered With Ritonavir-Boosted Lopinavir.
Karbwang, J; Na-Bangchang, K; Rajoli, RKR; Saeheng, T; Siccardi, M, 2020
)
0.96
" 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
)
1.47
"HIV is a global public health threat and requires life-long, daily oral dosing to effectively treat."( Tuning HIV drug release from a nanogel-based in situ forming implant by changing nanogel size.
Corker, A; Dawson, K; Elbaz, NM; Garcia-Tuñón, E; McDonald, TO; Niezabitowska, E; Taylor, J; Town, AR, 2019
)
0.51
" After LPV loading, the antiviral profile of pHPβCD was reversed to the sigmoidal dose-response profile of LPV, while pMβCD maintained its dose-independent profile followed by a LPV mediated increase in viral inhibition."( Pyromellitic dianhydride crosslinked soluble cyclodextrin polymers: Synthesis, lopinavir release from sub-micron sized particles and anti-HIV-1 activity.
Adeoye, O; Bártolo, I; Cabral-Marques, H; Conceição, J; da Silva, AB; Duarte, N; Francisco, AP; Taveira, N, 2020
)
0.79
"Diverging physicochemical properties of HIV drug combinations are challenging to formulate as a single dosage form."( Controlled Solvent Removal from Antiviral Drugs and Excipients in Solution Enables the Formation of Novel Combination Multi-Drug-Motifs in Pharmaceutical Powders Composed of Lopinavir, Ritonavir and Tenofovir.
Ho, RJY; Lane, S; McConnachie, L; Yu, D; Yu, J, 2020
)
0.75
" Surges in volume of patients requiring mechanical ventilation coupled with prolonged ventilator days and the high sedative dosing requirements observed quickly led to the depletion of "just-in-time" inventories typically maintained by institutions."( It Takes a Village…: Contending With Drug Shortages During Disasters.
Barletta, JF; Burry, LD; Christian, MD; Dichter, J; Erstad, BL; Geiling, J; Kanji, S; Maves, RC; Williamson, D, 2020
)
0.56
" (2) The patients were divided into normal dose group (500 mg, twice a day, n = 19) and reduced dose group (250 mg, twice a day, n = 5) according to the dosage of kaletra."( [Clinical characteristics of liver damage in 30 patients with severe coronavirus disease 2019 in Sichuan area].
Chen, H; Deng, C; Du, Q; Guo, Y; Huang, X; Li, T; Lu, S; Yue, R, 2020
)
0.56
" Chloroquine (CQ) had a 100% discharge rate compared to 50% with lopinavir-ritonavir at day 14, however a trial has recommended against a high dosage due to cardiotoxic events."( Repurposing of drugs for COVID-19: a systematic review and meta-analysis.
Amparore, D; Checcucci, E; Dasgupta, P; Elhage, O; Fiori, C; Kotecha, P; Light, A; Porpiglia, F, 2022
)
0.96
" Therefore, in the absence of adverse drug reaction, lopinavir dosage should not be reduced."( Plasma Concentrations and Safety of Lopinavir/Ritonavir in COVID-19 Patients.
Azoulay, C; Batista, R; Benaboud, S; Boujaafar, S; Canouï, E; Carlier, N; Chouchana, L; Gana, I; Kernéis, S; Legendre, P; Preta, LH; Regard, L; Terrier, B; Treluyer, JM; Zerbit, J; Zheng, Y, 2021
)
1.15
"7%)) and incorrect dosing (n=6 (10."( Prescribing practices of lopinavir/ritonavir, hydroxychloroquine and azithromycin during the COVID-19 epidemic crisis and pharmaceutical interventions in a French teaching hospital.
Belmas, AS; Danion, F; Fourtage, M; Gourieux, B; Michel, B; Nai, T; Nivoix, Y; Reisz, F; Reiter-Schatz, A; Ruch, Y; Walther, J, 2021
)
0.92
" This review summarizes the current data for the most commonly used drugs for coronavirus disease 2019 and will cover the unique factors that may affect the dosing of these medications in patients with CKD."( Treatment Options for Coronavirus Disease 2019 in Patients With Reduced or Absent Kidney Function.
Govil, A; Luckett, K; Miller-Handley, H, 2020
)
0.56
" Lower white blood cell count and lactate dehydrogenase at the time of drug administration as well as shorter time from supplemental oxygen initiation to dosing were significantly associated with clinical improvement in the univariate analysis."( Early clinical outcomes with tocilizumab for severe COVID-19: a two-centre retrospective study.
Daniel, NM; Hilden, P; Raja, K; Smoke, SM, 2021
)
0.62
"PK and safety findings for ZDV, 3TC, and LPV/r support current WHO weight band dosing of syrup formulations in children with SAM."( Pharmacokinetics and Safety of Zidovudine, Lamivudine, and Lopinavir/Ritonavir in HIV-infected Children With Severe Acute Malnutrition in Sub-Saharan Africa: IMPAACT Protocol P1092.
Aweeka, F; Bradford, S; Browning, R; Coletti, A; Costello, D; Graham, B; Hughes, E; Kamthunzi, P; Kawalazira, R; Mmbaga, BT; Moye, J; Musoke, P; Nathoo, K; Norman, J; Owor, M; Purdue, L; Reding, C; Tierney, C; Whalen, ME; Wiesner, L; Ziemba, L, 2021
)
0.86
"Despite a collaborative effort towards developing suitable oral drug products for pediatrics over the past decade, appropriate pediatric dosage forms have remained lacking due to special considerations in dose flexibility, swallowability, palatability, and safety of excipients for pediatrics."( Development of nanoparticle-based orodispersible palatable pediatric formulations.
Deng, Y; Shen, J; Shen, L; Yang, Y, 2021
)
0.62
" However, should some hospitalized patients have dosage escalation to intermediate dose? Should some be considered for full-dose anticoagulation without a measurable thromboembolic event and how should that anticoagulation be monitored? Should patients receive postdischarge anticoagulation and with what medication and for how long? What thrombotic issues are related to the various medications being used to treat this coagulopathy? Is antiphospholipid antibody part of this syndrome? What is the significance of isolated ischemic stroke and limb ischemia in this disorder and how does this interface with the rest of the clinical and laboratory features of this disorder? The aims of this article are to explore these questions and interpret the available data based on the current evidence."( COVID-19 and Its Implications for Thrombosis and Anticoagulation.
Berkman, SA; Tapson, VF, 2021
)
0.62
" Trough plasma concentrations of lopinavir and ritonavir were higher than those expected, while those of hydroxychloroquine were those expected with the dosing regimen."( An open-label randomized controlled trial of the effect of lopinavir/ritonavir, lopinavir/ritonavir plus IFN-β-1a and hydroxychloroquine in hospitalized patients with COVID-19.
Ader, F; Alfaiate, T; Andrejak, C; Belhadi, D; Botelho-Nevers, E; Bouadma, L; Bouiller, K; Bouscambert-Duchamp, M; Burdet, C; Cabié, A; Clere-Jehl, R; Costagliola, D; Courjon, J; Danion, F; Dechanet, A; Delmas, C; Diallo, A; Dubost, C; Dupont, A; Epaulard, O; Faure, E; Gaci, R; Gagneux-Brunon, A; Gallien, S; Goehringer, F; Hites, M; Jaureguiberry, S; Kimmoun, A; Lacombe, K; Lanoix, JP; Launay, O; Lê, MP; Leroy, S; Lescure, FX; Lina, B; Makinson, A; Martin-Blondel, G; Mentré, F; Mercier, N; Mootien, J; Mourvillier, B; Navellou, JC; Noret, M; Nseir, S; Peiffer-Smadja, N; Peytavin, G; Piroth, L; Poissy, J; Pourcher, V; Raffi, F; Reignier, J; Reuter, J; Richard, JC; Saillard, J; Staub, T; Tolsma, V; Wallet, F; Yazdanpanah, Y, 2021
)
1.15
"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
"We conclude that despite availability of clinical evidence, double dosing LPV/r in patients receiving rifampicin-based TB treatment is low in Uganda's public HIV clinics but this does not seem to affect patient survival and viral suppression."( Adoption of evidence-informed guidelines in prescribing protease inhibitors for HIV-Tuberculosis co-infected patients on rifampicin and effects on HIV treatment outcomes in Uganda.
Castelnuovo, B; Haguma, P; Kalibbala, D; Kirenga, B; Muddu, M; Mulindwa, F; Semitala, FC, 2021
)
0.62
" He was treated with azithromycin, isoprinosine, lopinavir, and fondaparinux with thromboprophylaxis dosage since admission."( The Challenging Anticoagulant Therapy in COVID19 Patient with Associated Coagulopathy.
Airlangga, MP; Fatimah, FN; Miftahussurur, M; Pradana, AD; Rianda, RA; Rianda, RV; Subkhan, M, 2021
)
0.88
" We describe the population pharmacokinetics of ethambutol in children with TB to guide dosing in this population."( Population pharmacokinetics of ethambutol in African children: a pooled analysis.
Abdelwahab, MT; Andrieux-Meyer, I; Bekker, A; Chabala, C; Cotton, MF; Davies, G; Denti, P; Hesseling, A; Lee, J; McIlleron, H; Rabie, H; Tikiso, T; Wiesner, L; Zar, HJ, 2022
)
0.72
" However, local safety profile should also be evaluated depending on the new indication, administration route and dosage form."( Antivirals and the Potential Benefits of Orally Inhaled Drug Administration in COVID-19 Treatment.
Akbal-Dagistan, O; Basarir, NS; Culha, M; Erturk, A; Sahin, G; Sancar, S; Yildiz-Pekoz, A, 2022
)
0.72
" The established correlation equations can be useful in therapeutic drug monitoring (TDM) and dosing regimen optimization."( The investigation of the complex population-drug-drug interaction between ritonavir-boosted lopinavir and chloroquine or ivermectin using physiologically-based pharmacokinetic modeling.
Alsmadi, MM, 2023
)
1.13
", a hyperimmune anti-COVID-19 intravenous immunoglobulin), methylprednisolone, interferon-beta/standard-of-care (SOC), interferon-beta-1b, convalescent plasma, remdesivir, lopinavir/ritonavir, immunoglobulin gamma, high dosage sarilumab (HS), auxora, and imatinib were effective when compared with placebo or SOC group."( Comparative efficacy and safety of pharmacological interventions for severe COVID-19 patients: An updated network meta-analysis of 48 randomized controlled trials.
Chen, J; Cheng, Q; Fang, Z; Jia, Q; Zhao, G, 2022
)
0.92
" This study aimed to develop a population pharmacokinetic model of LPV/r and provide dosage optimization in Thai PLWH."( Dose optimization with population pharmacokinetics of ritonavir-boosted lopinavir for Thai people living with HIV with and without active tuberculosis.
Avihingsanon, A; Chaivichacharn, P; Gatechompol, S; Punyawudho, B; Ubolyam, S, 2022
)
0.95
" The reduced LPV/r dosage offers sufficient LPV exposure for Thai PLWH."( Dose optimization with population pharmacokinetics of ritonavir-boosted lopinavir for Thai people living with HIV with and without active tuberculosis.
Avihingsanon, A; Chaivichacharn, P; Gatechompol, S; Punyawudho, B; Ubolyam, S, 2022
)
0.95
"6% probability of improving 6-month survival across varying hydrocortisone dosing strategies."( Long-term (180-Day) Outcomes in Critically Ill Patients With COVID-19 in the REMAP-CAP Randomized Clinical Trial.
Al-Beidh, F; Angus, DC; Annane, D; Arabi, YM; Beane, A; Berry, LR; Berry, S; Bhimani, Z; Bonten, MJM; Bradbury, CA; Brunkhorst, FM; Burrell, A; Buxton, M; Buzgau, A; Charles, WN; Cove, M; Derde, LPG; Detry, MA; Estcourt, LJ; Fagbodun, EO; Fitzgerald, M; Girard, TD; Goligher, EC; Goossens, H; Gordon, AC; Green, C; Haniffa, R; Higgins, AM; Hills, T; Horvat, CM; Huang, DT; Ichihara, N; Lamontagne, F; Lawler, PR; Lewis, RJ; Lorenzi, E; Marshall, JC; McArthur, CJ; McAuley, DF; McGlothlin, A; McGuinness, SP; McQuilten, Z; McVerry, BJ; Mouncey, PR; Murthy, S; Neal, MD; Nichol, AD; Parke, RL; Parker, JC; Parry-Billings, K; Peters, SEC; Reyes, LF; Rowan, KM; Saito, H; Santos, MS; Saunders, CT; Serpa-Neto, A; Seymour, CW; Shankar-Hari, M; Stronach, LM; Turgeon, AF; Turner, AM; van Bentum-Puijk, W; van de Veerdonk, FL; Webb, SA; Zarychanski, R, 2023
)
0.91
"Although super-boosted lopinavir/ritonavir (LPV/r; ratio 4:4 instead of 4:1) is recommended for infants living with HIV and receiving concomitant rifampicin, in clinical practice, many different LPV/r dosing strategies are applied due to poor availability of pediatric separate ritonavir formulations needed to superboost."( Brief Report: Suboptimal Lopinavir Exposure in Infants on Rifampicin Treatment Receiving Double-dosed or Semisuperboosted Lopinavir/Ritonavir: Time for a Change.
Ballesteros, A; Buck, WC; Burger, DM; Chabala, C; Chitsamatanga, M; Colbers, A; Domínguez-Rodríguez, S; Jacobs, TG; Madrid, L; Moraleda, C; Mujuru, HA; Mumbiro, V; Namuziya, N; Nathoo, KJ; Nduna, B; Passanduca, A; Rojo, P; Tagarro, A, 2023
)
1.52
" Daily emtricitabine/TAF was dosed according to World Health Organization (WHO)-recommended weight bands: 120/15 mg in children weighing 14 to <25 kg and 200/25 mg in those weighing ≥25 kg."( First Pharmacokinetic Data of Tenofovir Alafenamide Fumarate and Tenofovir With Dolutegravir or Boosted Protease Inhibitors in African Children: A Substudy of the CHAPAS-4 Trial.
Bamford, A; Burger, DM; Bwakura-Dangarembizi, M; Chabala, C; Colbers, A; Denti, P; Doerholt, K; Gibb, DM; Griffiths, AL; Makumbi, S; McIlleron, HM; Monkiewicz, LN; Mulenga, V; Mumbiro, V; Musiime, V; Nangiya, J; Szubert, AJ; Waalewijn, H; Wasmann, RE; Wiesner, L, 2023
)
0.91
"In children, TAF combined with boosted PIs or dolutegravir and dosed according to WHO-recommended weight bands provides TAF and tenofovir concentrations previously demonstrated to be well tolerated and effective in adults."( First Pharmacokinetic Data of Tenofovir Alafenamide Fumarate and Tenofovir With Dolutegravir or Boosted Protease Inhibitors in African Children: A Substudy of the CHAPAS-4 Trial.
Bamford, A; Burger, DM; Bwakura-Dangarembizi, M; Chabala, C; Colbers, A; Denti, P; Doerholt, K; Gibb, DM; Griffiths, AL; Makumbi, S; McIlleron, HM; Monkiewicz, LN; Mulenga, V; Mumbiro, V; Musiime, V; Nangiya, J; Szubert, AJ; Waalewijn, H; Wasmann, RE; Wiesner, L, 2023
)
0.91
" We evaluated whether increased daily dosing with modified 8-hourly lopinavir/ritonavir 4:1 would maintain therapeutic plasma concentrations of lopinavir in children living with HIV receiving rifampicin-based antituberculosis treatment."( Inadequate Lopinavir Concentrations With Modified 8-Hourly Lopinavir/Ritonavir 4:1 Dosing During Rifampicin-based Tuberculosis Treatment in Children Living With HIV.
Chabala, C; Choo, L; Chungu, C; Crook, A; Gibb, D; Kapasa, M; LeBeau, K; Lungu, J; McIlleron, H; Mulenga, V; Tembo, CH; Turkova, A; Weisner, L; Zimba, K; Zyambo, K, 2023
)
1.54
"9 kg, on rifampicin-based antituberculosis treatment were commenced or switched to 8-hourly liquid lopinavir/ritonavir 4:1 with increased daily dosing using weight-band dosing approach."( Inadequate Lopinavir Concentrations With Modified 8-Hourly Lopinavir/Ritonavir 4:1 Dosing During Rifampicin-based Tuberculosis Treatment in Children Living With HIV.
Chabala, C; Choo, L; Chungu, C; Crook, A; Gibb, D; Kapasa, M; LeBeau, K; Lungu, J; McIlleron, H; Mulenga, V; Tembo, CH; Turkova, A; Weisner, L; Zimba, K; Zyambo, K, 2023
)
1.52
"7 mg/L]) were lower than on standard dosing without rifampicin (n = 12; area under the curve 24 121."( Inadequate Lopinavir Concentrations With Modified 8-Hourly Lopinavir/Ritonavir 4:1 Dosing During Rifampicin-based Tuberculosis Treatment in Children Living With HIV.
Chabala, C; Choo, L; Chungu, C; Crook, A; Gibb, D; Kapasa, M; LeBeau, K; Lungu, J; McIlleron, H; Mulenga, V; Tembo, CH; Turkova, A; Weisner, L; Zimba, K; Zyambo, K, 2023
)
1.3
"Modified 8-hourly dosing of lopinavir/ritonavir failed to achieve adequate lopinavir concentrations with concurrent antituberculosis treatment."( Inadequate Lopinavir Concentrations With Modified 8-Hourly Lopinavir/Ritonavir 4:1 Dosing During Rifampicin-based Tuberculosis Treatment in Children Living With HIV.
Chabala, C; Choo, L; Chungu, C; Crook, A; Gibb, D; Kapasa, M; LeBeau, K; Lungu, J; McIlleron, H; Mulenga, V; Tembo, CH; Turkova, A; Weisner, L; Zimba, K; Zyambo, K, 2023
)
1.59
" These drugs are typically available in liquid formulations to aid in dosing for children who cannot swallow tablets."( Anti-HIV drugs lopinavir/ritonavir activate bitter taste receptors.
Chen, S; Cui, M; Lu, Y; Wen, J; Xu, K; Zhou, X, 2023
)
1.26
" The present analysis aims to evaluate LPV levels in individuals exposed to SARS-CoV-2 versus people living with HIV (PLWH) by developing a population pharmacokinetic (popPK) model, while characterizing external and patient-related factors that might affect LPV exposure along with dose-response association."( Population pharmacokinetic analysis of lopinavir in HIV negative individuals exposed to SARS-CoV-2: a COPEP (COronavirus Post-Exposure Prophylaxis) sub-study.
Andre, P; Buclin, T; Calmy, A; Decosterd, LA; Delfraysse, M; Fedeli, C; Guidi, M; Thoueille, P; Ustero, P, 2023
)
1.18
"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
)
1.16
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antiviral drugA substance used in the prophylaxis or therapy of virus diseases.
HIV protease inhibitorAn inhibitor of HIV protease, an enzyme required for production of proteins needed for viral assembly.
anticoronaviral agentAny antiviral agent which inhibits the activity of coronaviruses.
[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 (2)

ClassDescription
amphetaminesAmines that constitute a class of central nervous system stimulants based on the structure of the parent amphetamine 1-phenylpropan-2-amine.
dicarboxylic acid diamide
[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 (99)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency29.84930.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency23.91450.173734.304761.8120AID1346859
Fumarate hydrataseHomo sapiens (human)Potency37.22120.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency44.66840.031637.5844354.8130AID504865
SMAD family member 3Homo sapiens (human)Potency23.91450.173734.304761.8120AID1346859
TDP1 proteinHomo sapiens (human)Potency13.96500.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency29.84930.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency25.85440.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743036; AID743042; AID743054; AID743063
Smad3Homo sapiens (human)Potency12.58930.00527.809829.0929AID588855
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency24.22580.000657.913322,387.1992AID1259377; AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency33.49150.001022.650876.6163AID1224838; AID1224893
progesterone receptorHomo sapiens (human)Potency33.49150.000417.946075.1148AID1346784; AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.46400.01237.983543.2770AID1346984; AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency26.99690.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency20.42230.000214.376460.0339AID720691; AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency3.78270.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency21.45520.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency20.50620.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency29.84700.375827.485161.6524AID743217; AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency16.91520.005428.02631,258.9301AID1346982; AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency27.47590.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743075; AID743078; AID743079
GVesicular stomatitis virusPotency17.37680.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency13.80290.00108.379861.1304AID1645840
polyproteinZika virusPotency37.22120.00308.794948.0869AID1347053
67.9K proteinVaccinia virusPotency7.94330.00018.4406100.0000AID720580
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency8.41200.001024.504861.6448AID743212
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency13.41840.001019.414170.9645AID743094; AID743140; AID743191
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency33.49150.001723.839378.1014AID743083
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency11.22020.10009.191631.6228AID1346983
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency22.38720.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency29.01450.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency23.81280.000627.21521,122.0200AID743202; AID743219
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency12.58930.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency35.54200.004611.374133.4983AID624296; AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency20.31480.005612.367736.1254AID624032
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency33.49150.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency17.37680.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency17.37680.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency0.29850.002319.595674.0614AID651631
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency33.49150.001551.739315,848.9004AID1259244
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency17.37680.01238.964839.8107AID1645842
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency23.71010.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency23.71010.011912.222168.7989AID651632
cytochrome P450 2C9, partialHomo sapiens (human)Potency17.37680.01238.964839.8107AID1645842
[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, proteaseHuman immunodeficiency virus 1Ki0.00000.00000.00000.0000AID977610
Chain B, proteaseHuman immunodeficiency virus 1Ki0.00000.00000.00000.0000AID977610
Chain A, ProteaseHuman immunodeficiency virus 1Ki0.00000.00000.00000.0000AID977610
Chain B, ProteaseHuman immunodeficiency virus 1Ki0.00000.00000.00000.0000AID977610
Chain A, ProteaseHuman immunodeficiency virus 1Ki0.00000.00000.00000.0000AID977610
Chain B, ProteaseHuman immunodeficiency virus 1Ki0.00000.00000.00000.0000AID977610
Chain A, ProteaseHuman immunodeficiency virus 1Ki0.00000.00000.00000.0000AID977610
Chain B, ProteaseHuman immunodeficiency virus 1Ki0.00000.00000.00000.0000AID977610
Chain A, PROTEASE RETROPEPSINHuman immunodeficiency virus 1Ki0.00110.00110.00110.0011AID977610
Chain B, PROTEASE RETROPEPSINHuman immunodeficiency virus 1Ki0.00110.00110.00110.0011AID977610
Chain A, Protease RetropepsinHuman immunodeficiency virus 1Ki0.00450.00080.00450.0082AID977610
Chain B, Protease RetropepsinHuman immunodeficiency virus 1Ki0.00450.00080.00450.0082AID977610
Chain A, Protease RetropepsinHuman immunodeficiency virus 1Ki0.00450.00080.00450.0082AID977610
Chain B, Protease RetropepsinHuman immunodeficiency virus 1Ki0.00450.00080.00450.0082AID977610
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)21.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)47.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)17.30000.11007.190310.0000AID1443980; AID1473738
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (BRU ISOLATE)Ki0.00170.00000.08283.3000AID1797110
Gag-Pol polyproteinHIV-1 M:B_ARV2/SF2Ki0.00180.00000.01090.0895AID1796953
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (RF/HAT ISOLATE)Ki0.00170.00000.05051.6160AID1797110
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)6.00000.00022.318510.0000AID416864; AID679931
Cytochrome P450 3A4Homo sapiens (human)Ki0.70500.00011.41629.9000AID589156
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusKi15.00000.00753.00839.1100AID1805801
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC50 (µMol)14.91500.00022.45859.9600AID1804171; AID1845236
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Ki15.00000.00001.63079.0000AID1805801
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (NEW YORK-5 ISOLATE)IC50 (µMol)0.03500.00020.10421.7000AID1796876
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)10.30000.00021.874210.0000AID416864
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)10.30000.00021.270410.0000AID416864
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (STRAIN UGANDAN / ISOLATE U455)Ki0.00170.00000.05051.6160AID1797110
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)10.30000.00001.819410.0000AID416864
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)8.51140.00091.901410.0000AID576612
Protease Human immunodeficiency virus 1IC50 (µMol)0.02500.00010.22487.3200AID618426
Protease Human immunodeficiency virus 1Ki0.00070.00000.04433.1000AID160461; AID163477; AID1669454; AID238682; AID274379; AID274380; AID274381; AID274382; AID343015; AID343016; AID343017; AID343018; AID343019; AID343020; AID343021
CAAX prenyl protease 1 homologMus musculus (house mouse)IC50 (µMol)18.40001.20001.20001.2000AID328893
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)7.60000.00401.966610.0000AID1873200
Protease Human immunodeficiency virus 1IC50 (µMol)0.01750.00000.81769.8500AID1057016; AID590915; AID664437
Protease Human immunodeficiency virus 1Ki0.00020.00000.02841.1000AID1669455; AID1669456; AID321660; AID343014; AID374591; AID443165; AID537765; AID698062
[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)
Chain A, proteaseHuman immunodeficiency virus 1Kd0.00000.00000.00390.0150AID977611
Chain B, proteaseHuman immunodeficiency virus 1Kd0.00000.00000.00390.0150AID977611
Chain A, proteaseHuman immunodeficiency virus 1Kd0.00000.00000.00390.0150AID977611
Chain B, proteaseHuman immunodeficiency virus 1Kd0.00000.00000.00390.0150AID977611
Chain A, proteaseHuman immunodeficiency virus 1Kd0.00000.00000.00390.0150AID977611
Chain B, proteaseHuman immunodeficiency virus 1Kd0.00000.00000.00390.0150AID977611
Chain A, proteaseHuman immunodeficiency virus 1Kd0.00000.00000.00390.0150AID977611
Chain B, proteaseHuman immunodeficiency virus 1Kd0.00000.00000.00390.0150AID977611
Chain A, proteaseHuman immunodeficiency virus 1Kd0.00000.00000.00390.0150AID977611
Chain B, proteaseHuman immunodeficiency virus 1Kd0.00000.00000.00390.0150AID977611
Spike glycoproteinBetacoronavirus England 1EC50 (µMol)12.82000.00304.57559.8200AID1804127
Replicase polyprotein 1abBetacoronavirus England 1EC50 (µMol)12.82000.00304.57559.8200AID1804127
Transmembrane protease serine 2Homo sapiens (human)EC50 (µMol)12.82000.00304.51689.8200AID1804127
Procathepsin LHomo sapiens (human)EC50 (µMol)12.82000.00304.48749.8200AID1804127
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC50 (µMol)12.82000.00304.61369.8200AID1804127
Replicase polyprotein 1abHuman coronavirus 229EEC50 (µMol)12.82000.00304.61369.8200AID1804127
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC50 (µMol)12.82000.00304.45549.8200AID1804127
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC50 (µMol)12.82000.00304.11059.8200AID1804127
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC50 (µMol)12.82000.00304.57559.8200AID1804127
Protease Human immunodeficiency virus 1Kd0.00010.00010.04120.5770AID238043
Angiotensin-converting enzyme 2 Homo sapiens (human)EC50 (µMol)12.82000.00304.57559.8200AID1804127
Protease Human immunodeficiency virus 1EC50 (µMol)1.16000.00070.69422.7300AID1350502
Protease Human immunodeficiency virus 1Kd0.00060.00000.61178.1500AID1307690; AID1307691
[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)
AlbuminHomo sapiens (human)KD26.00006.00006.00006.0000AID239810
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (331)

Processvia Protein(s)Taxonomy
viral translationTransmembrane protease serine 2Homo sapiens (human)
proteolysisTransmembrane protease serine 2Homo sapiens (human)
protein autoprocessingTransmembrane protease serine 2Homo sapiens (human)
positive regulation of viral entry into host cellTransmembrane protease serine 2Homo sapiens (human)
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)
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)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
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)
adaptive immune responseProcathepsin LHomo sapiens (human)
proteolysisProcathepsin LHomo sapiens (human)
protein autoprocessingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host plasma membraneProcathepsin LHomo sapiens (human)
receptor-mediated endocytosis of virus by host cellProcathepsin LHomo sapiens (human)
antigen processing and presentationProcathepsin LHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IIProcathepsin LHomo sapiens (human)
collagen catabolic processProcathepsin LHomo sapiens (human)
zymogen activationProcathepsin LHomo sapiens (human)
enkephalin processingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host endosome membraneProcathepsin LHomo sapiens (human)
CD4-positive, alpha-beta T cell lineage commitmentProcathepsin LHomo sapiens (human)
symbiont entry into host cellProcathepsin LHomo sapiens (human)
antigen processing and presentation of peptide antigenProcathepsin LHomo sapiens (human)
proteolysis involved in protein catabolic processProcathepsin LHomo sapiens (human)
elastin catabolic processProcathepsin LHomo sapiens (human)
macrophage apoptotic processProcathepsin LHomo sapiens (human)
cellular response to thyroid hormone stimulusProcathepsin LHomo sapiens (human)
positive regulation of apoptotic signaling pathwayProcathepsin LHomo sapiens (human)
positive regulation of peptidase activityProcathepsin LHomo sapiens (human)
immune responseProcathepsin LHomo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
symbiont-mediated perturbation of host ubiquitin-like protein modificationReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
symbiont-mediated perturbation of host ubiquitin-like protein modificationReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo 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)
negative regulation of signaling receptor activityAngiotensin-converting enzyme 2 Homo sapiens (human)
symbiont entry into host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cytokine productionAngiotensin-converting enzyme 2 Homo sapiens (human)
angiotensin maturationAngiotensin-converting enzyme 2 Homo sapiens (human)
angiotensin-mediated drinking behaviorAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinAngiotensin-converting enzyme 2 Homo sapiens (human)
tryptophan transportAngiotensin-converting enzyme 2 Homo sapiens (human)
viral life cycleAngiotensin-converting enzyme 2 Homo sapiens (human)
receptor-mediated endocytosis of virus by host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of vasoconstrictionAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of transmembrane transporter activityAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cell population proliferationAngiotensin-converting enzyme 2 Homo sapiens (human)
symbiont entry into host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
receptor-mediated virion attachment to host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
negative regulation of smooth muscle cell proliferationAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of inflammatory responseAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of amino acid transportAngiotensin-converting enzyme 2 Homo sapiens (human)
maternal process involved in female pregnancyAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of cardiac muscle contractionAngiotensin-converting enzyme 2 Homo sapiens (human)
membrane fusionAngiotensin-converting enzyme 2 Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeAngiotensin-converting enzyme 2 Homo sapiens (human)
blood vessel diameter maintenanceAngiotensin-converting enzyme 2 Homo sapiens (human)
entry receptor-mediated virion attachment to host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of gap junction assemblyAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cardiac conductionAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of L-proline import across plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processAngiotensin-converting enzyme 2 Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (147)

Processvia Protein(s)Taxonomy
serine-type endopeptidase activityTransmembrane protease serine 2Homo sapiens (human)
protein bindingTransmembrane protease serine 2Homo sapiens (human)
serine-type peptidase activityTransmembrane protease serine 2Homo sapiens (human)
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)
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)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
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)
fibronectin bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activityProcathepsin LHomo sapiens (human)
protein bindingProcathepsin LHomo sapiens (human)
collagen bindingProcathepsin LHomo sapiens (human)
cysteine-type peptidase activityProcathepsin LHomo sapiens (human)
histone bindingProcathepsin LHomo sapiens (human)
proteoglycan bindingProcathepsin LHomo sapiens (human)
serpin family protein bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processProcathepsin LHomo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
RNA-dependent RNA polymerase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
cysteine-type endopeptidase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
K63-linked deubiquitinase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
K48-linked deubiquitinase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K63-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K48-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoestersReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
protein guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo 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)
virus receptor activityAngiotensin-converting enzyme 2 Homo sapiens (human)
endopeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
carboxypeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
metallocarboxypeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
protein bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
metallopeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
peptidyl-dipeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
zinc ion bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
identical protein bindingAngiotensin-converting enzyme 2 Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (71)

Processvia Protein(s)Taxonomy
extracellular regionTransmembrane protease serine 2Homo sapiens (human)
nucleoplasmTransmembrane protease serine 2Homo sapiens (human)
plasma membraneTransmembrane protease serine 2Homo sapiens (human)
extracellular exosomeTransmembrane protease serine 2Homo sapiens (human)
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)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo 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)
extracellular regionProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
nucleusProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
multivesicular bodyProcathepsin LHomo sapiens (human)
Golgi apparatusProcathepsin LHomo sapiens (human)
plasma membraneProcathepsin LHomo sapiens (human)
apical plasma membraneProcathepsin LHomo sapiens (human)
endolysosome lumenProcathepsin LHomo sapiens (human)
chromaffin granuleProcathepsin LHomo sapiens (human)
lysosomal lumenProcathepsin LHomo sapiens (human)
intracellular membrane-bounded organelleProcathepsin LHomo sapiens (human)
collagen-containing extracellular matrixProcathepsin LHomo sapiens (human)
extracellular exosomeProcathepsin LHomo sapiens (human)
endocytic vesicle lumenProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
double membrane vesicle viral factory outer membraneReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo 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)
plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular regionAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme 2 Homo sapiens (human)
endoplasmic reticulum lumenAngiotensin-converting enzyme 2 Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
ciliumAngiotensin-converting enzyme 2 Homo sapiens (human)
cell surfaceAngiotensin-converting enzyme 2 Homo sapiens (human)
membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
apical plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
endocytic vesicle membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
brush border membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
membrane raftAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular exosomeAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme 2 Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (803)

Assay IDTitleYearJournalArticle
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2008Journal of virology, Jun, Volume: 82, Issue:12
Ninety-nine is not enough: molecular characterization of inhibitor-resistant human immunodeficiency virus type 1 protease mutants with insertions in the flap region.
AID1797110Protease Inhibition Assay from Article 10.1021/bi051886s: \\Analysis of HIV-1 CRF_01 A/E protease inhibitor resistance: structural determinants for maintaining sensitivity and developing resistance to atazanavir.\\2006Biochemistry, May-02, Volume: 45, Issue:17
Analysis of HIV-1 CRF_01 A/E protease inhibitor resistance: structural determinants for maintaining sensitivity and developing resistance to atazanavir.
AID1796953Enzyme Inhibition Assay from Article 10.1021/jm060666p: \\Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.\\2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.
AID1799570Inhibition Assay from Article 10.1111/j.1747-0285.2007.00514.x: \\Design of mutation-resistant HIV protease inhibitors with the substrate envelope hypothesis.\\2007Chemical biology & drug design, May, Volume: 69, Issue:5
Design of mutation-resistant HIV protease inhibitors with the substrate envelope hypothesis.
AID1796876Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2005.03.008: \\Oximinoarylsulfonamides as potent HIV protease inhibitors.\\2005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Oximinoarylsulfonamides as potent HIV protease inhibitors.
AID328893Inhibition of mouse ZMPSTE24 expressed n delta ste24 delta rce1 yeast2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID369953Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID374591Inhibition of HIV1 protease2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID557231Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir measured before administering last dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID328891Inhibition of human ICMT expressed in yeast assessed as methylation of N-acetyl-farnesylcysteine2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID557282Ratio of EC50 for HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M in protease encoding region to EC50 for HIV1 ERS104pre2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID369954Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID519783Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-60K/N-65E protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID668809Antiviral activity against Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant infected in human MT4 cells2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID297669Inhibition of HIV1 Protease M2 variant by FRET based assay2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres.
AID564038Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID558383Drug level in HIV-infected pregnant woman amniotic fluid at 400 mg, po BID by HPLC/UV analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women.
AID238682Inhibition constant for human immunodeficiency virus type 1 protease2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
AID1482906Antiviral activity against tipranavir-resistant HIV1 NL4-3 harboring protease L10I/L33I/M36I/M46I/I54V/K55R/I62V/L63P/A71V/G73S/V82T/L90M/I93L mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemilumi2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID415245Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
AID374626Resistance index, ratio of EC50 for HIV1 with protease 33F/46I/53L/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
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]
AID369941Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID372182Resistance index, ratio of EC50 for HIV1 with protease 33I/46I/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID1482921Antiviral activity against atazanavir-resistant HIV1 NL4-3 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme 2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID321695Ratio of EC50 for HIV1 mutant strain 3 to EC50 for wild type HIV12008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID558397Ratio of drug level in HIV-infected pregnant woman amniotic fluid to maternal blood plasma at 400 mg, po BID by HPLC/UV analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women.
AID622660Antiviral activity against HIV1 harboring protease L10I, I13V, G16A, Q18H, L33F, N37D, M46I, I54V, G57R, Q61H,I62V, L63P, A71L, I72T, L76V, V77I, V82A, N88G, L90M, I93L mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death 2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.
AID519552Antiviral activity against HIV1 isolate 9 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I15I/V, K20R, L33F, E35D, M36I, N37D, R41K, K43I, M46I, I54V, I62V, L63P, A71T, I72T, V82A, I84V, L90M, I93L 2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID564031Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID1219738Maximum plasma concentration in healthy human at 400 mg co-administered with 50 mg ritonavir2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID328878Toxicity in mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 48 hrs by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID278976Antiviral activity against HIV1 C9 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID374593Cytotoxicity against human MT4 cells after 6 days by MTT assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID519545Antiviral activity against HIV1 isolate 2 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I15V, G16E, K20R, E35D, M36I, R41K, I54A, R57K, Q61D, A71V, I72R, V82A, L89I, L90M, Q92K mutation derived fro2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID519789Antiviral activity against HIV 2 subtype A clinical isolate expressing 10V/I-40D-43I-56V-70K-82F-84V-89V-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T2 during compound treatment measured after 3 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID557273Antiviral activity against HIV1 A harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID519780Antiviral activity against HIV 2 subtype H expressing 10I-34E-40P-41Y-60H-63N-70T-73G-82F-89L-92E protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID396260Antiviral activity against HIV1 NL4-32007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV.
AID622658Antiviral activity against HIV1 B26 harboring protease L33F, K45I, M46I, I50V, A71V and V82F mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay relative to wild type HIV1 pNL4-32011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.
AID105346Tested for cytopathic effect of HIVIIIB in MT-4 cells in presence of 50% human serum2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Novel lopinavir analogues incorporating heterocyclic replacements of six-member cyclic urea--synthesis and structure-activity relationships.
AID372186Resistance index, ratio of EC50 for HIV1 with protease 54V/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID1350503Ratio of EC50 for inhibition of protease L10F/V32I/M46I/I47V/Q58E/I84V mutant in HIV1 A17 infected in human MT4 cells to EC50 for wild-type HIV-1 pNL4-3 infected in human MT4 cells2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine.
AID13678Cmax value in the period of 8 hr after dosing. 2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
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.
AID279336Antiviral activity against wild type HIV2 in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID322122Antiviral activity against HIV1 97ZA003 R5 subtype C in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID343025Ratio of Ki for HIV1 recombinant protease V32I/I47A mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID1669456Inhibition of HIV1 NL4-3 protease I50V/A71V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 62020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.
AID532460Antiviral activity against Human immunodeficiency virus 1 isolate 20 harboring Gag-capsid I138L, V215L, V218P, H219Q, M228I, E230D, G248T, T280A, E312D, A340G and G357S mutant gene and protease L10F, A22V, D30N, S37N, K45R, I54L, I62V, L63P, A71V, V77I, I2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1717746Selectivity index, ratio of CC50 for African green monkey Vero E6 cells to EC50 for SARS-CoV isolate Frankfurt-1 infected in African green monkey Vero E6 cells2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).
AID375204Ratio of EC50 for multidrug-resistant HIV1 isolate TM to EC50 for wild type HIV1 isolate ERS104pre2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.
AID519577Antiviral activity against HIV1 clone2 infected in HEK293 cells harboring A-790742-selected protease V82L mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pNL4-32008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1482925Ratio of IC50 for nelfinavir-resistant HIV1 NL4-3 harboring protease L10F/K20T/D30N/K45I/A71V/V77I mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID519554Antiviral activity against HIV1 isolate 11 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I15V, K20R, E21Q, E35D, M36I, N37D, R41K, M46L, I54V, I62V, L63P, A71V, T74D, P79A, V82T, I84V, I85V, L90M, 2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID446195Antiviral activity against multidrug-resistant HIV1 isolate C infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID278958Antiviral activity against HIV1 A6 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID547020Selectivity ratio of EC50 for HIV1 subtype C harboring protease L10R, M46I, I54V, V82S mutant gene and polymorphism at M36 position to EC50 for wild type HIV1 subtype C2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes.
AID279344Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M and L99F mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID1219734Drug metabolism in human liver microsomes assessed as CYP2D6-mediated lopinavir-GSH adduct formation at 2 uM after after 50 mins by UPLC-TOFMS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID416859Increase in P-glycoprotein-mediated tenofovir disoproxil fumarate permeation from apical to basolateral side of human Caco-2 cells at 20 uM2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
AID374623Resistance index, ratio of EC50 for HIV1 with protease 32I/46L/47V/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID353726Aqueous solubility in water by shake flask method2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir.
AID557290Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID374628Resistance index, ratio of EC50 for HIV1 with protease 33F/46L/53L/54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID1474091Ratio of drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs to IC50 for human MRP3 overexpressed in Sf9 insect cells2013Toxicological 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.
AID21894The partition coefficient was reported2002Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir).
AID519580Antiviral activity against HIV1 clone5 infected in HEK293 cells harboring A-790742-selected protease L63P, A71V, and V82G mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 RF2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID572579Cmax in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen.
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.
AID248098Inhibitory concentration against resistant (A17) human immunodeficiency virus2005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Oximinoarylsulfonamides as potent HIV protease inhibitors.
AID278969Antiviral activity against HIV1 C2 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID374613Resistance index, ratio of EC50 for non-B type HIV1 with protease 32I/47A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID162683Inhibition of HIV protease at 0.5 nM2002Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir).
AID297668Inhibition of HIV1 Protease M1 variant by FRET based assay2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres.
AID558390Ratio of drug level in HIV-infected pregnant woman cord blood plasma to maternal blood plasma at 400 mg, po BID by HPLC/UV analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID369958Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 1 passage2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID532473Antiviral activity against Human immunodeficiency virus 1 isolate 34 harboring Gag-capsid I138L, I147L, V159I, V215L, T280V, A309C, S310T, E312D and G357S mutant gene and protease L10I, I13V, E35D, S37N, I62V, L63P and I64M mutant gene infected in human M2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID369956Ratio of EC50 for HIV2 ROD with protease V47A mutation to EC50 for wild type HIV2 ROD2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID242933Dissociation rate constant for the interaction between the compound and serum albumin2005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID572577Apparent oral clearance in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir with NRTI2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen.
AID374592Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID369957Ratio of EC50 for HIV2 ROD with protease G17N/V47A mutation to EC50 for wild type HIV2 ROD2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID353765AUC in Sprague-Dawley rat plasma at 5 mg/kg, po coadministered with RTV2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir.
AID668815Cytotoxicity against human MT4 cells2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID1669457Antiviral activity against wild-type HIV1 NL4-3 infected in human TZM-bl cells infected with supernatants from virus-infected human 293T cells treated with compound for 18 hrs assessed as reduction in viral replication by luciferase assay2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.
AID582282Plasma concentration in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI measured 12 hrs after last dose2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors.
AID521547Antiviral activity against Human immunodeficiency virus type 2 (ISOLATE ROD) after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID519550Antiviral activity against HIV1 isolate 7 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, M46M/L, G48V, I54V, L63P, A71V, I72M, V77I, V82A, L90M, I93L mutation derived from viral passages with Lopina2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID679931TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells2003AIDS (London, England), May-02, Volume: 17, Issue:7
Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein.
AID446202Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate G to IC50 for wild type HIV1 isolate ERS104pre2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID532453Antiviral activity against Human immunodeficiency virus 1 isolate 32 harboring Gag-capsid, I138L, A146P, I147L, V159I, V215L, I223A, N252S/N, T280V and S310T and protease R41K/R, I62V, L63P, V77I and I93L mutant gene infected in human MT-2 cells by XTT-as2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID564048Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID1219720Drug metabolism in human liver microsomes assessed as GSH-conjugated monohydroxylated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID321698Ratio of EC50 for HIV1 mutant strain 6 to EC50 for wild type HIV12008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID242868Association rate constant for the interaction between the compound and serum albumin2005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID557286Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
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.
AID557297Ratio of EC50 for HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
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.
AID278975Antiviral activity against HIV1 C8 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID321660Inhibition of HIV1 protease2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID417048Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells at 20 uM2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
AID446205Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate JSL to IC50 for wild type HIV1 isolate ERS104pre2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID572581Half life in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen.
AID369946Ratio of EC50 for HIV2 CDC310319 infected in human PBMC to EC50 for HIV1 NL4-3 infected in human MT4 cells2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID658567Resistance factor, ratio of EC50 for multidrug-resistant HIV1 106-PR 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.
AID557232Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir measured 2 hrs post last dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID322105Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID278974Antiviral activity against HIV1 C7 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID537771Antiviral activity against multidrug resistant Human immunodeficiency virus 1 harboring protease M46I, I54V, V82A and L90M mutant2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
AID1482914Antiviral activity against darunavir-resistant HIV1 derived from 51 passages harboring protease L10I/I15V/K20R/L24I/V32I/L33F/M36I/M46L/I54M/L63P/K70Q/V82I/I84V/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production af2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID519793Antiviral activity against HIV 2 subtype B clinical isolate expressing 12T-14Y-19P-40N-41D-61N-62I-96S-99L protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID278956Antiviral activity against HIV1 A4 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID374622Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/73S/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID278966Antiviral activity against HIV1 A14 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
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.
AID572582Apparent oral clearance in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen.
AID369951Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID374627Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/82T/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID557277Ratio of EC50 for HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L in protease encoding region to EC50 for HIV1 ERS104pre2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID1482926Ratio of IC50 for atazanavir-resistant HIV1 NL4-3 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
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.
AID519546Antiviral activity against HIV1 isolate 3 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, E35D, N37D, M461, I54V, L63P, A71V, T74P, I84V, L90M, I93L mutation derived from viral passages with Lopinavi2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
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.
AID519575Antiviral activity against HIV1 P13 infected in human MT4 cells derived from viral passages with A-790742 harboring protease M46I, L63P, A71V, and V82G mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days p2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
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.
AID525488Antigametocyte activity against Plasmodium falciparum harboring GFP-tagged Pfs16 protein assessed as reduction in number of gametocytes after 40 hrs by [3H]hypoxanthine incorporation assay2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
AID557278Ratio of EC50 for HIV1 MM harboring L10I/K43T/M46L/I54V/L63P/A71V/V82A/L90M/Q92K in protease encoding region infected to EC50 for HIV1 ERS104pre2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID1725421Antiviral activity against DRV resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities.
AID374630Resistance index, ratio of EC50 for HIV1 with protease 46L/54V/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID575063Antiviral activity against Human immunodeficiency virus 1 harboring M46I mutation in viral protease assessed as fold change in drug susceptibility relative to wild type2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease.
AID321681Metabolic stability in dog liver microsomes assessed as compound remaining at 5 uM in presence of 2.5 uM ritonavir by RP-HPLC2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID1295706Aqueous solubility of the compound by shake flask method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.
AID278973Antiviral activity against HIV1 C6 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID519786Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-17D-40D-43I-45K/R-46V-54M-64I/V-69K/R-71V/I-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID566850Antiviral activity against HIV-1 MDR/TM infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID343028Ratio of Ki for HIV1 recombinant protease L10F/L19I/K20R/L33F/E35D/M36I/R41K/F53L/I54V/L63P/H69K/A71V/T74P/I84V/L89M/L90M/I93L mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID537768Antiviral activity against Human immunodeficiency virus 1 clade A isolated from HIV-AIDS patient2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
AID1725420Antiviral activity against ATV-resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities.
AID532469Antiviral activity against Human immunodeficiency virus 1 isolate 6 harboring Gag-capsid I138L and V215L mutant gene and protease L10I, S37N, M46L, G48V, R57K, L63P, I66F, A71V, V82T and I84V mutant gene infected in human MT-2 cells by XTT-assay relative 2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID557295Ratio of EC50 for HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID1380930Resistance index, ratio of EC50 for antiviral activity against APV resistant HIV1 harboring protease L10F/M46I/I50V/I85V mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
AID586625Antiviral activity against HIV1 harboring mutant protease with matrix K76R mutant infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID586618Ratio of EC50 for HIV1 harboring mutant protease with matrix Y79F mutant to EC50 for wild type HIV12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID558369Drug level in HIV-infected pregnant woman maternal blood plasma at 400 mg, po BID by HPLC/UV analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women.
AID532463Antiviral activity against Human immunodeficiency virus 1 isolate 9 harboring Gag-capsid I138L, A146S, I147L, V215L, N252H, T280A, A340G and E345D mutant gene and protease L10I, I13V, K20M, L33V, M36I, S37N, I54V, R57K, I62V, L63P, I66L, A71V, G73S, P79A,2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID726411Selectivity ratio of EC50 for Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant to EC50 for wild type Human immunodeficiency virus 1 3B2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID343026Ratio of Ki for HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID322112Antiviral activity against wild type HIV1 ERS104prc X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID105589Cytotoxicity against MT-4 cells2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships.
AID519553Antiviral activity against HIV1 isolate 10 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I13V, K20R, L33F, E35D, M36I, N37D, I54L, Q58E, I62V, L63P, A71V, V82A, I84V, L90M mutation derived from vir2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID532466Antiviral activity against Human immunodeficiency virus 1 isolate 27 harboring Gag-capsid I138L, S173T/S, V215L, L268M, R275K/R, T280V, S310T, E319D and G357S and protease L10I, I15V, L19V, V32I, L33F, M46I, I54V, K55R, R57K, L63P, C67F, H69Q, A71V, G73C/2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID589156Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone hydroxylation2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID321662Antiviral activity against HIV1 3B in presence of 50% human serum2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID1057015Inhibition of HIV-1 multidrug-resistant protease 769 preincubated for 20 mins by FRET analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID162704Compound was tested for its inhibitory potency against HIV protease at 0.5 nM2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships.
AID278982Resistance to HIV1 with protease 46I, 54I and I84A mutation in HEK 293 cells relative to similar background2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID279341Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID297670Inhibition of HIV1 Protease M3 variant by FRET based assay2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres.
AID1482913Antiviral activity against darunavir-resistant HIV1 derived from 30 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/K70R/V82A/I84V/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID278961Antiviral activity against HIV1 A9 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID1057014Ratio of IC50 for HIV-1 multidrug-resistant protease 769 to IC50 for HIV-1 NL4-3 wild type protease2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID446198Antiviral activity against multidrug-resistant HIV1 isolate MM infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID415251Metabolic stability in human liver microsomes assessed as inhibition of metabolism at 2 uM by LC/MS/MS analysis in presence of ritonavir2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
AID446201Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate C to IC50 for wild type HIV1 isolate ERS104pre2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID369962Ratio of EC50 for HIV2 MS infected in human MT4 cells after 18 passages to EC50 for HIV2 MS infected in human MT4 cells2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID546990Antiviral activity against HIV1 subtype B harboring protease polymorphism at M36 position and L10F, V82A mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes.
AID278984Resistance to HIV1 with protease 46I, 54V and I84V mutation in HEK 293 cells relative to similar background2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID525477Antigametocyte activity against ring stage Plasmodium falciparum D10 assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
AID1482923Ratio of IC50 for lopinavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/M46I/I47A/A71V/I84V mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID622656Antiviral activity against wild type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay in presence of 50% human serum2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.
AID537774Resistance index, ratio of EC50 for multidrug resistant Human immunodeficiency virus 1 MDRC4 to EC50 for wild type Human immunodeficiency virus 12010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
AID446200Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate B to IC50 for wild type HIV1 isolate ERS104pre2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID321696Ratio of EC50 for HIV1 mutant strain 4 to EC50 for wild type HIV12008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID443166Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells.
AID532478Antiviral activity against Human immunodeficiency virus 1 isolate 12 harboring Gag-capsid I138L E207D, V215L, V218P, H219Q, M228I, G248T, T280S, E312D, A340G, G357S and V362I mutant gene and protease S37N, I62V/I, L63P, I64L and V82I mutant gene infected 2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
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.
AID724346Inhibition of C-south african HIV-1 protease assessed as hydrolysis of the chromogenic peptide substrate Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH22013European journal of medicinal chemistry, Feb, Volume: 60Linear and cyclic glycopeptide as HIV protease inhibitors.
AID1482918Ratio of IC50 for darunavir-resistant HIV1 derived from 51 passages harboring protease L10I/I15V/K20R/L24I/V32I/L33F/M36I/M46L/I54M/L63P/K70Q/V82I/I84V/L89M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID1422658Inhibition of ZMPSTE24 in human KP4 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration.
AID1725423Antiviral activity against HIV1 DRVR P51 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities.
AID369952Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID446196Antiviral activity against multidrug-resistant HIV1 isolate G infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
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]
AID1409312Antiviral activity against darunavir-resistant HIV1 at passage 30 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.
AID442713Antiviral activity against indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket.
AID279347Antiviral activity against HIV1 isolate 5512 with D30N, M461 and V771 mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID328892Inhibition of mouse RCE1 expressed in delta ste24 delta rce1 yeast2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID547007Antiviral activity against HIV1 subtype CRF02_AG harboring protease M46, I47A, I84V mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes.
AID246194Protease inhibitory activity against HIV-1 r13034 mutant strain was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
AID532655Antiviral activity against Human immunodeficiency virus 1 isolate 39 harboring Gag-capsid A146P, I147L, V215L, M228I, G248A, R286K, A326S, G357S and V362I mutant gene and protease K14R, E35D, M36I, S37N, R41K, K45R, D60E, I62V and I64V mutant gene infecte2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID417028Effect on tenofovir disoproxil fumarate metabolism in HIV infected patient assessed as change in plasma Cmax of tenofovir at 400 mg, po, BID co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
AID586617Ratio of EC50 for HIV1 harboring mutant protease with matrix A81T mutant to EC50 for wild type HIV12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID416864Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
AID432028Antimalarial activity against Plasmodium falciparum W2 by [3H]hypoxanthine uptake2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2.
AID322102Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID322100Selectivity index, ratio of CC50 for MT2 cells to EC50 for HIV1 LAI2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID519782Antiviral activity against HIV 2 subtype A clinical isolate expressing 5L/F-14Y/H-17G/D-43T-54I/M-62V/A-70R/K-71I protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID1845236Inhibition of SARS-CoV-2 MPro2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Protease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors.
AID525279Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
AID1422656Inhibition of ZMPSTE24 in human U2OS cells assessed as increase in intracellular accumulation of prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration.
AID564063Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID564032Cytotoxicity against human MT2 cells after 7 days by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID442704Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket.
AID279346Antiviral activity against HIV1 isolate 5512 with V321 and M46L mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID521549Antiviral activity against HIV 2 subtype H expressing 10I-40P-41Y-60H-63N-70T-73G-89L-92E protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID446204Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate MM to IC50 for wild type HIV1 isolate ERS104pre2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID162693Inhibitory activity (0.5 nM) against Protease2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Novel lopinavir analogues incorporating heterocyclic replacements of six-member cyclic urea--synthesis and structure-activity relationships.
AID322101Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
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.
AID343017Inhibition of HIV1 recombinant protease A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID519784Antiviral activity against HIV 2 subtype A clinical isolate expressing 54M-65E-71I-74N-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID575060Antiviral activity against Human immunodeficiency virus 1 harboring protease inhibitor resistance-associated mutations and protease L76V mutation in viral protease assessed as fold change in drug susceptibility relative to wild type2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease.
AID532457Antiviral activity against Human immunodeficiency virus 1 isolate 26 harboring Gag-capsid I138L, A146S, I147L, E312D, A326S, L337M, and A340G mutant gene and protease T4S, L10F, V11L, I13V, I15V, K20A, V32I, L33F, M36I, S37D, K43T, M46I, I54L, I62V, L63P,2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID557239Ratio of drug level in 2 hrs to 30 days post last dose of HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
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.
AID374603Resistance index, ratio of EC50 for HIV1 with protease 54V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID1323585Binding affinity to mouse anti-dsDNA monoclonal antibody R4A assessed as inhibition of RA4 binding to DWEYS peptide at 5 to 50 uM preincubated for 1 hr followed by DWEYS peptide addition measured after 1 hr by ELISA2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Amending HIV Drugs: A Novel Small-Molecule Approach To Target Lupus Anti-DNA Antibodies.
AID278959Antiviral activity against HIV1 A7 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID163477Binding affinity against ritonavir-resistant strains.2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID564042Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID1057016Inhibition of HIV-1 NL4-3 wild type protease expressed in Escherichia coli preincubated for 20 mins by FRET analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease.
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.
AID328888Effect on HDJ2 farnesylation in mouse fibroblast cells at 20 uM after 24 hrs by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID1219735Drug metabolism in human liver microsomes assessed as CYP1A2-mediated GSH-conjugated hydroxylated DMP adduct formation adduct formation at 2 uM after after 30 mins by UPLC-TOFMS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID546996Antiviral activity against HIV1 subtype C harboring protease L10R, M46I, I54V, V82S mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes.
AID683726Antimalarial activity against liver stages of Plasmodium yoelii 17XNL infected in Swiss Webster mouse assessed as reduction in liver parasite load at 100 mg/kg, po co-administered with 50 mg/kg ritonavir incubated for 6 hrs prior to sporozoite inoculation2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Targeting the liver stage of malaria parasites: a yet unmet goal.
AID519792Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-19P-61N-64V-71I-90M-95I protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T2 during compound treatment measured after 3 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID532455Antiviral activity against Human immunodeficiency virus 1 isolate 8 harboring Gag-capsid V215T mutant gene and protease L10I, L24I, L33F, S37N, R41K, I54V, D60E, I62V, L63P, A71V, V77I, V82A and I84V mutant gene infected in human MT-2 cells by XTT-assay r2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID374639Resistance index, ratio of EC50 for HIV1 with protease 46L/50L/54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID547004Antiviral activity against HIV1 subtype CRF02_AG harboring protease L76V, M46I, I84V mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporte2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes.
AID557221Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured 4 hrs post last dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID274380Inhibition of HIV1 protease L10I/G48V/I54V/L63P/V82A mutant2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.
AID343018Inhibition of HIV1 recombinant protease V32I/I47A mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID105401Antiviral activity against the cytopathic effects of HIV IIIB in MT-4 cells was assayed in the presence of 50% human serum2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships.
AID247984Inhibitory concentration against wild type human immunodeficiency virus2005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Oximinoarylsulfonamides as potent HIV protease inhibitors.
AID532471Antiviral activity against Human immunodeficiency virus 1 isolate 31 harboring Gag-capsid I138L, S173T, V215L, I223N, M228L, G248Q, N252H, T280V and E312D mutant gene and protease I13V, K14R/K, M36I, S37N, I64V, H69K and I72V mutant gene infected in human2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID566851Antiviral activity against HIV-1 MDR/MM infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation.
AID586622Ratio of EC50 for HIV1 harboring HIV1 harboring wild type 8.9NSX with gag RF79F and T81A mutant to EC50 for wild type HIV12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID547018Selectivity ratio of EC50 for HIV1 subtype B harboring protease polymorphism at M36 position and L10F, V82A mutant gene to EC50 for wild type HIV1 subtype B2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes.
AID557279Ratio of EC50 for HIV1 JSL harboring L10I/L24I/L33F/E35D/M36I/N37S/M46L/I54V/R57K/I62V/L63P/A71V/G73S/82A in protease encoding region to EC50 for HIV1 ERS104pre2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID1482905Antiviral activity against amprenavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/L33F/M46L/I54M/A71V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID274379Inhibition of wild type HIV1 protease Q7K mutant2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.
AID582276Clearance in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors.
AID278985Resistance to HIV1 with protease 46I, 54M/V and I84A mutation in HEK 293 relative to similar background2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID417038Effect on tenofovir disoproxil fumarate metabolism in HIV infected patient assessed as change in plasma Cmin of tenofovir at 400 mg, po, BID co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
AID279345Antiviral activity against wild type HIV1 in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID532462Antiviral activity against Human immunodeficiency virus 1 isolate 37 harboring Gag-capsid V135I, I138P, V143I, Q182H, V215L/V, V218P/A, H219Q, I223V, E230D, N252S, T280A, R286K, K302R and G357S mutant gene and protease S37D, R41K, L63P and I93L mutant gen2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID369959Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 11 passages2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID274381Inhibition of HIV1 protease D30N/L63P/N88D mutant2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.
AID532467Antiviral activity against Human immunodeficiency virus 1 isolate 1 harboring Gag-capsid I138L, V159I, E203D, V215L, I223V, T280V, E312D and V323I mutant gene and protease L10I, K20R, M36I, S37N, G48V, I54M, I62V, L63P, A71V, I72V, V82A, I84V, L90M and I92010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID698059Selectivity index, ratio of Ki for HIV protease V82A mutant to Ki for HIV1 wild type protease2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Rational approaches to improving selectivity in drug design.
AID352084Antimalarial activity after 24 hrs against chloroquine-resistant Plasmodium falciparum W2 by [3H]hypoxanthine uptake2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antimalarial activity of hydroxyethylpiperazine derivatives.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1380926Antiviral activity against LPV resistant HIV1 harboring protease L10F/M46/I54V/V82A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
AID321679Metabolic stability in dog liver microsomes assessed as compound remaining at 5 uM by RP-HPLC2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID322117Antiviral activity against HIV1 MDR/C X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID321677Metabolic stability in rat liver microsomes assessed as compound remaining at 5 uM in presence of 0.5 uM ritonavir by RP-HPLC2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID279340Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 150V mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID668816Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 3B2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
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.
AID1717754Antiviral activity against SARS-CoV isolate Frankfurt-1 infected in African green monkey Vero E6 cells incubated for 3 days2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1409308Antiviral activity against Atazanavir-resistant HIV1 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.
AID446193Antiviral activity against wild type HIV1 isolate ERS104pre infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID1193134Antimalarial activity against Plasmodium knowlesi infected Chinese rhesus macaques assessed as parasitemia level in blood smears at 40 mg/kg, intragastric treated 5 days before infection measured between day 0 to 7 by Giemsa-staining in presence of ritona2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Ritonavir-boosted indinavir but not lopinavir inhibits erythrocytic stage Plasmodium knowlesi malaria in rhesus macaques.
AID532657Antiviral activity against Human immunodeficiency virus 1 isolate 4 harboring Gag-capsid A146P, V159I, K162R, Q182S, T186I, V215L, I223G/V, N252G, P255A, E260D, E312D and G357S mutant gene and protease L10R, S37N, M46L, I62V, L63P, A71V, T74S, V82T, L90M 2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID372181Resistance index, ratio of EC50 for HIV1 with protease 46I/50L/54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID572574Cmax in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen.
AID557244Toxicity in HIV-infected Thai pregnant women assessed as adverse effect at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID374625Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID519544Antiviral activity against HIV1 isolate 1 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10V, I15V, G16E, K20R, E35D, M36I, R41K, M46I, I54V, R57K, Q61N, I64L, A71V, I72R, V82A, L89I, L90M, Q92K mutation2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID374638Resistance index, ratio of EC50 for HIV1 with protease 46L/48V/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID532458Antiviral activity against Human immunodeficiency virus 1 isolate 28 harboring Gag-capsid I138M mutant gene and protease L10I, I13V, L23I, L33F, S37N, M46I, I54V, K55R, R57K, Q58E, D60E, I62V, L63P, A71I, I72V, L76V, V77I, V82A, I84V, I85V, L89M, L90M and2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID683725Antimalarial activity against liver stages of Plasmodium yoelii 17XNL infected in Swiss Webster mouse assessed as reduction in liver parasite load at 25 mg/kg, po co-administered with 12.5 mg/kg ritonavir incubated for 6 hrs prior to sporozoite inoculatio2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Targeting the liver stage of malaria parasites: a yet unmet goal.
AID322110Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID321680Metabolic stability in dog liver microsomes assessed as compound remaining at 5 uM in presence of 0.5 uM ritonavir by RP-HPLC2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID322111Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID537766Inhibition of multidrug resistant HIV1 protease L101I, L36P, A71V, G73S, I84V, L90M mutant by FRET2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
AID668810Antiviral activity against Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant infected in human MT4 cells2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID328894Effect on change in ZMPSTE24 mRNA expression level in mouse fibroblasts at 20 uM after 10 days by PCR2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID369943Antiviral activity against HIV2 CDC310319 isolate infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID321694Ratio of EC50 for HIV1 mutant strain 2 to EC50 for wild type HIV12008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID239810Equilibrium dissociation constant for the interaction between the compound and serum albumin2005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID375205Ratio of EC50 for multidrug-resistant HIV1 isolate MM to EC50 for wild type HIV1 isolate ERS104pre2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.
AID553577Antiviral activity against HIV1 MM harboring L10I/K43T/M46L/I54V/L63P/A71V/V82A/L90M/Q92K in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID519785Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-17D-40D-43I-46V-66V/A-70R/K protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID374609Resistance index, ratio of EC50 for HIV1 with protease 84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID557299Ratio of EC50 for HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID322097Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID372184Resistance index, ratio of EC50 for HIV1 with protease 37T/41K/70E mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID519579Antiviral activity against HIV1 clone4 infected in HEK293 cells harboring A-790742-selected protease L33F, A71V, G73S, V77I, V82L, and I84V mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pN2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID374601Resistance index, ratio of EC50 for HIV1 with protease 24I/33F/54V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID279338Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 182F mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID278967Antiviral activity against HIV1 A15 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID321685Antiviral activity against wild type HIV12008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID668808Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID1380929Resistance index, ratio of EC50 for antiviral activity against LPV resistant HIV1 harboring protease L10F/M46/I54V/V82A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
AID297671Antiviral activity against HIV1 infected MT4 cells by MTT method2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres.
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.
AID375199Antiviral activity against wild type HIV1 isolate ERS104pre infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.
AID532465Antiviral activity against Human immunodeficiency virus 1 isolate 25 harboring Gag-capsid I138M, S173A, V215L, N252S, I256T, S310T/S, A340G and E345D mutant gene and protease L10F, V11I, I13V, K20I, V32I, L33F, E34Q, E35D, M36I, S37N, K43T, M46I, F53Y, I52010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID586628Ratio of EC50 for HIV1 harboring 8gpNS with K76R, F79Y, and A81T mutant to EC50 for wild type HIV12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID343027Ratio of Ki for HIV1 recombinant protease L10I/L24I/L33F/M46L/154V/L63P/A71V/V82A/I84V mutant to Ki for wild-type HIV1 BH10 protease expressed in Escherichia coli2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID369960Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 18 passages2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID369947Antiviral activity against HIV2 MS infected in human MT4 cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID553576Antiviral activity against HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID553571Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID321690Antiviral activity against HIV1 mutant strain 52008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID519573Antiviral activity against HIV1 P15 infected in human MT4 cells derived from viral passages with A-790742 harboring protease L33L/F, K45I, V82L, and I84V mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID668817Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells in presence of 50% human serum2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID519538Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID343022Ratio of Ki for HIV1 recombinant protease D30N/N88D mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID374612Resistance index, ratio of EC50 for HIV1 with protease 30N/88D/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID532475Antiviral activity against Human immunodeficiency virus 1 isolate 38 harboring Gag-capsid I138L, I147L, V215L, H219Q/H, I223V, N252H, P292S, A336S/A and A340G mutant gene and protease E35D, S37A and L63P mutant gene infected in human MT-2 cells by XTT-ass2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID564040Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID557298Ratio of EC50 for HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID1482915Antiviral activity against nelfinavir-resistant HIV1 NL4-3 harboring protease L10F/K20T/D30N/K45I/A71V/V77I mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID369944Ratio of EC50 for HIV2 MS to EC50 for HIV1 NL4-3 infected in human MT4 cells2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID588986Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1A22010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID374604Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/73S/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID257271Antiviral activity against HIV1 in the presence of 50% human serum2005Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
AID586624Antiviral activity against HIV1 harboring wild type 8.9NSX with mutant amino acid 116 insertion infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID1219721Drug metabolism in human liver microsomes assessed as GSH-conjugated dihydroxylated/dehydrogenated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID1219719Drug metabolism in human liver microsomes assessed as compound-GSH adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID557276Antiviral activity against HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID322098Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID582278Tmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors.
AID1725418Antiviral activity against HIV1 NL4-3 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities.
AID622659Antiviral activity against HIV1 isolate 1 harboring protease L10I, E35D, N37D, M46I, I54V, G57R, L63P, A71V, T74P, I84V, L90M, I93L mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay relative to2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.
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.
AID328886Toxicity in HEK293 cells transfected with GFP-prelamin A construct assessed as accumulation of uncleaved protein at 20 uM by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID374610Resistance index, ratio of EC50 for HIV1 with protease 33F/50V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID322115Antiviral activity against HIV1 MDR/JSL R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID557287Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID1482919Antiviral activity against saquinavir-resistant HIV1 NL4-3 harboring protease L10I/N37D/G48V/I54V/L63P/G73C/I84V/L90M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassa2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID557293Ratio of EC50 for HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID532454Antiviral activity against Human immunodeficiency virus 1 isolate 7 harboring Gag-capsid I138L, I147L, S173A, V215L, I223V, T242N, G248A, N252A, I126T, T280V and E312D mutant gene and protease K20R, M36I, R41K, M46I, L63Q, I64V, P79S, V82F and L90M mutant2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID521548Antiviral activity against Human immunodeficiency virus type 1 (BRU ISOLATE) after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID564037Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID321697Ratio of EC50 for HIV1 mutant strain 5 to EC50 for wild type HIV12008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID664437Inhibition of South African HIV1 subtype C protease expressed in Escherichia coli BL21S4 (DE3)pLysS cells using Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 as substrate by spectrophotometry2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and molecular modelling studies of novel carbapeptide analogs for inhibition of HIV-1 protease.
AID519787Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-40D-70K-72R/K-91T/S protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID566847Antiviral activity against HIV-1 MDR/B infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation.
AID278971Antiviral activity against HIV1 C4 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID248600Inhibitory concentration against wild type Human immuno deficiency virus (D545701) was determined in an MT-4 cell line2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles.
AID328883Toxicity in mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 10 days by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID525281Antimicrobial activity against Plasmodium falciparum harboring HFP-tagged Pfs16 protein after 48 hrs2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
AID726413Selectivity ratio of EC50 for Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant to EC50 for wild type Human immunodeficiency virus 1 3B2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID519572Antiviral activity against HIV1 P9 infected in human MT4 cells derived from viral passages with A-790742 harboring protease V82V/L and I84V mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infectio2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID343019Inhibition of HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID525484Antigametocyte activity against drug-resistant Plasmodium falciparum Dd2 trophozoites assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID278964Antiviral activity against HIV1 A12 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID343015Inhibition of HIV1 recombinant protease D30N/N88D mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID238043Binding affinity for human immunodeficiency virus type 1 protease2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
AID369942Antiviral activity against HIV2 CBL-23 infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID1409313Antiviral activity against darunavir-resistant HIV1 at passage 51 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.
AID353764Cmax in Sprague-Dawley rat plasma at 5 mg/kg, po coadministered with RTV2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir.
AID374620Resistance index, ratio of EC50 for HIV1 with protease 32I/46I/47V/50L mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID519790Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-61N-99L protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID519556Antiviral activity against HIV1 isolate 13 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, K14R, L33F, E34Q, R41K, K45R, M46I, I50V, K55R, L63P, A71V, G73T, V77I, V82A, L90M, I93L mutation derived fr2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID374629Resistance index, ratio of EC50 for HIV1 with protease 46L/54M/82L/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID525166Antimicrobial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocytes assessed as potentiation of choloroquine-mediated antimalarial activity by light microscopy2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID547237Selectivity ratio of EC50 for HIV1 subtype CRF02_AG harboring protease L76V, M46I, I84V mutant gene and polymorphism at M36 position to EC50 for wild type HIV1 subtype CRF02_AG2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes.
AID353740AUC in po dosed Beagle dog at dose molar equivalent to 5 mg/kg LPV, po coadministered with RTV dosed as 5% dextrose containing solution2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir.
AID537773Resistance index, ratio of EC50 for multidrug resistant Human immunodeficiency virus 1 harboring protease M46I, I54V, V82A and L90M mutant to EC50 for wild type Human immunodeficiency virus 12010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
AID572578Cmin in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen.
AID415249Metabolic stability in human liver microsomes assessed as compound disappearance at 2 uM by LC/MS/MS analysis2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
AID557280Ratio of EC50 for HIV1 A harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region to EC50 for HIV1 ERS104pre2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID698061Selectivity index, ratio of Ki for HIV protease L10I mutant to Ki for HIV1 wild type protease2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Rational approaches to improving selectivity in drug design.
AID557294Ratio of EC50 for HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID532464Antiviral activity against Human immunodeficiency virus 1 isolate 30 harboring Gag-capsid I138L, V215L, R286K and Q311A mutant gene and protease I13V, E35D, S37N and L63P mutant gene infected in human MT-2 cells by XTT-assay relative to wild-type2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
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.
AID1219737Maximum plasma concentration in healthy human at 400 mg2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID519548Antiviral activity against HIV1 isolate 5 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10F, I15V, M46I, L63P, A71V, I72L, V82T, I84V, I85V, L90M mutation derived from viral passages with Lopinavir asse2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1482927Ratio of IC50 for tipranavir-resistant HIV1 NL4-3 harboring protease L10I/L33I/M36I/M46I/I54V/K55R/I62V/L63P/A71V/G73S/V82T/L90M/I93L mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID374611Resistance index, ratio of EC50 for HIV1 with protease 48V/54V/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
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]
AID519794Antiviral activity against HIV 2 subtype B clinical isolate expressing 12Q-14R-17G/D-19P-61N-62I-92A protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID588982Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1B32010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID564029Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID343016Inhibition of HIV1 recombinant protease M46I/A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID374624Resistance index, ratio of EC50 for HIV1 with protease 33F/54L/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID1350495Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days in absence of human serum by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine.
AID328877Toxicity in human AG07095 cells assessed as accumulation of prelamin A at 20 uM after 10 days by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID375202Antiviral activity against multidrug-resistant HIV1 isolate C infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.
AID242866Dissociation rate constant for human immunodeficiency virus type 1 protease2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID322116Antiviral activity against HIV1 MDR/B X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID343020Inhibition of HIV1 recombinant protease L10I/L24I/L33F/M46L/154V/L63P/A71V/V82A/I84V mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID1409310Antiviral activity against amprenavir-resistant HIV1 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.
AID586626Antiviral activity against HIV1 harboring mutant protease with matrix Y79F mutant infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID279343Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M and 184V mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID322096Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID321693Ratio of EC50 for HIV1 mutant strain 1 to EC50 for wild type HIV12008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID564061Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID321699Ratio of EC50 for HIV1 mutant strain 7 to EC50 for wild type HIV12008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID582283Tmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors.
AID321676Metabolic stability in rat liver microsomes assessed as compound remaining at 5 uM by RP-HPLC2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID519542Antiviral activity against HIV1 B26 infected in human MT4 cells harboring protease L33F, K45I, M46I, I50V, I54V, A71V, and V82F mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infectio2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID278965Antiviral activity against HIV1 A13 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID257270Antiviral activity against HIV1 in the absence of human serum2005Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
AID104835Effective concentration against ritonavir -resistant strains in MT-4 cells.2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID557218AUC (0 to 12 hrs) in HIV-infected Thai pregnant women at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured within 72 hrs postpartum2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID322103Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID532461Antiviral activity against Human immunodeficiency virus 1 isolate 5 harboring Gag-capsid I138M, V159I, T280V and S310T mutant gene and protease I13V, D30N, L33I, E35D, M36I, S37N, M46I/L, I54V, I62V, L63P, I66M/I, A71N/T, I72T/I, V82L/V, N88D, L90M and I92010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID519781Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-17D-43T-68N/D protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID726416Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID248546Inhibitory concentration against wild type Human immuno deficiency virus (HXB2) was determined in an MT-4 cell line2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles.
AID1307691Binding affinity to HIV1 protease I47A mutant2016Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9
OpenGrowth: An Automated and Rational Algorithm for Finding New Protein Ligands.
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.
AID1323586Binding affinity to mouse anti-dsDNA monoclonal antibody R4A assessed as inhibition of RA4 binding to DWEYS peptide preincubated for 1 hr followed by DWEYS peptide addition measured after 1 hr by ELISA2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Amending HIV Drugs: A Novel Small-Molecule Approach To Target Lupus Anti-DNA Antibodies.
AID279342Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M and L90M mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID1482909Antiviral activity against lopinavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/M46I/I47A/A71V/I84V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID1725419Antiviral activity against LPV-resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities.
AID343014Inhibition of wild-type HIV1 BH10 protease expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID372190Resistance index, ratio of EC50 for HIV1 with protease 46I/50V/54V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID374607Resistance index, ratio of EC50 for HIV1 with protease 46I/82T/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
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.
AID415248Fold resistance, ratio of EC50 for HIV1 bearing protease gene with A17 mutation to EC50 for wild-type HIV1 pNL4-32009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
AID1422660Inhibition of ZMPSTE24 in human HCT116 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration.
AID1593661Prodrug conversion in cannulated Sprague-Dawley rat plasma assessed as atazanavir formation at 3 mg/kg equiv of atazanavir administered orally by UPLC/MS/MS analysis2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir.
AID374634Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID1350502Inhibition of protease L10F/V32I/M46I/I47V/Q58E/I84V mutant in HIV1 A17 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine.
AID1219724Drug metabolism in human liver microsomes assessed as GSH-conjugated hydroxylated DMP adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
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.
AID586619Ratio of EC50 for HIV1 harboring mutant protease with matrix K76R mutant to EC50 for wild type HIV12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID519791Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-19P-33I-61N-71I-75M-84V-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID375200Antiviral activity against multidrug-resistant HIV1 isolate TM infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.
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.
AID28092Cmax value in the period of 8 hr after dosing, when administered with ritonavir.2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID519541Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID278953Antiviral activity against HIV1 A1 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID372188Resistance index, ratio of EC50 for HIV1 with protease 46L mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID372185Resistance index, ratio of EC50 for HIV1 with protease 46I/53L/82T/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID575062Antiviral activity against Human immunodeficiency virus 1 harboring M46I, M46L, I54V, V82A and L76V mutations in viral protease assessed as fold change in drug susceptibility relative to wild type2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease.
AID537769Antiviral activity against Human immunodeficiency virus 1 clade B isolated from HIV-AIDS patient2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
AID572575AUC in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen.
AID374605Resistance index, ratio of EC50 for HIV1 with protease 33F/46L/54V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID375207Ratio of EC50 for multidrug-resistant HIV1 isolate G to EC50 for wild type HIV1 isolate ERS104pre2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.
AID279348Antiviral activity against HIV1 isolate 5512 with M36I/M and V82T mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID416860Increase in P-glycoprotein-mediated forward permeation of tenofovir disoproxil fumarate in human Caco-2 cells at 2 uM2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
AID415250Metabolic stability in human liver microsomes assessed as compound disappearance at 2 uM by LC/MS/MS analysis in presence of ritonavir2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
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.
AID257273Antiviral activity against Lopinavir resistant HIV A17 mutant strain2005Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
AID278980Resistance to HIV1 with protease 46M, 54I and I84C mutation in HEK 293 cells relative to similar background2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID374615Resistance index, ratio of EC50 for HIV1 with protease 46I/47A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID328889Effect on Rap1A isoprenylation in mouse fibroblast cells at 20 uM after 24 hrs by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID321682Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM by RP-HPLC2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID557292Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID1717745Antiviral activity against HCoV-229E harboring GFP infected in human Huh-7 cells treated 1 hr prior to viral infection by fluorometric analysis2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).
AID557284Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID566849Antiviral activity against HIV-1 MDR/G infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation.
AID328880Toxicity in ICMT deficient mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 24 hrs by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID278963Antiviral activity against HIV1 A11 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID446197Antiviral activity against multidrug-resistant HIV1 isolate TM infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID322114Antiviral activity against HIV1 MDR/MM R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID321691Antiviral activity against HIV1 mutant strain 62008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID658565Antiviral activity against multidrug-resistant HIV1 106-PR 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.
AID372183Resistance index, ratio of EC50 for HIV1 with protease 37S/41K/70E mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID1669454Inhibition of HIV1 NL4-3 protease expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET as2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.
AID726415Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant infected in human MT4 cells assessed as inhibition of viral replication2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID1219736Drug metabolism in human liver microsomes assessed as CYP2D6-mediated GSH-conjugated hydroxylated DMP adduct formation adduct formation at 2 uM after after 30 mins by UPLC-TOFMS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID374600Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID372191Resistance index, ratio of EC50 for HIV1 with protease 46I/50V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID525290Antigametocyte activity against Plasmodium falciparum D10 schizonts assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
AID668814Selectivity index, ratio of EC50 for Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant to EC50 for Human immunodeficiency virus 1 3B expressing wild-type protease2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID586623Antiviral activity against 8gpNS with amino acid 116 insertion removed HIV1 infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID369950Antiviral activity against HIV1 NL4-3 infected in human PBMC cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID553574Antiviral activity against HIV1 ERS104pre infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID278972Antiviral activity against HIV1 C5 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID557274Antiviral activity against HIV1 B harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID519576Antiviral activity against HIV1 clone1 infected in HEK293 cells harboring A-790742-selected protease I84V mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pNL4-32008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID415246Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay in presence of 50% human serum2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
AID106958Compound was tested for antiviral activity against HIV-IIIB in MT-4 cells in presence of 50% human serum2002Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir).
AID564043Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID322118Antiviral activity against HIV1 MDR/G X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID564046Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID564039Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID1409309Antiviral activity against lopinavir-resistant HIV1 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.
AID374633Resistance index, ratio of EC50 for HIV1 with protease 46I/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID668811Antiviral activity against Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant infected in human MT4 cells2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID321686Antiviral activity against HIV1 mutant strain 12008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID1474092Ratio of drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells2013Toxicological 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.
AID396259Antiviral activity against HIV1 drug resistant mutant isolates from protease inhibitor treated HIV patient2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV.
AID537767Antiviral activity against wild type Human immunodeficiency virus 12010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
AID1678482Antiviral activity against SARS-CoV-2 infected in Vero E6 cells preincubated for 1 hr followed by viral infection at MOI of 0.02 and measured after 48 hrs by qRT-PCR method2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2.
AID374619Resistance index, ratio of EC50 for HIV1 with protease 30N/33F/46L/54L/84V/88D mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID257272Antiviral activity against indinavir resistant HIV IND-R mutant strain2005Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
AID278970Antiviral activity against HIV1 C3 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID519555Antiviral activity against HIV1 isolate 12 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I13V, K20I, E35D, M36I, M46I, I50V, I54V, R57K, I62V, L63P, A71V, V82A, L89V, L90M, Q92K mutation derived fr2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID278979Resistance to HIV1 with protease 46M, 54I and I84V mutation in HEK 293 cells relative to similar background2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID443165Inhibition of HIV1 protease expressed in Escherichia coli by fluorometric assay2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells.
AID566848Antiviral activity against HIV-1 MDR/C infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation.
AID575059Antiviral activity against Human immunodeficiency virus 1 harboring protease inhibitor resistance-associated mutations assessed as fold change in drug susceptibility relative to wild type2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease.
AID278977Antiviral activity against HIV1 C10 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID625397Antimalarial activity against chloroquine resistant, mefloquine sensitive Plasmodium falciparum W2 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and antimalarial activity of thioetherhydroxyethylsulfonamides, potential aspartyl protease inhibitors, Part 3.
AID1065160Inhibition of Plasmodium falciparum DC6 plasmepsin-5 using DABCYL-GNKRTLAQKQG-EDANS as substrate measured every 15 mins of 75 mins by fluorescence assay2014ACS medicinal chemistry letters, Jan-09, Volume: 5, Issue:1
Evaluation of aminohydantoins as a novel class of antimalarial agents.
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.
AID582280Cmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors.
AID415282Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
AID557283Ratio of EC50 for HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M in protease encoding region to EC50 for HIV1 ERS104pre2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID1380927Antiviral activity against APV resistant HIV1 harboring protease L10F/M46I/I50V/I85V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
AID532452Antiviral activity against Human immunodeficiency virus 1 isolate 22 harboring Gag-capsid V215L, H219Q, I223V, N252S, P255A, L268M and A340G mutant gene and Protease L19I, E35D, M36I, S37N, L63P, V77I and I93L mutant gene infected in human MT-2 cells by X2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID160461Inhibitory activity against HIV protease2001Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
AID442705Antiviral activity against HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket.
AID278960Antiviral activity against HIV1 A8 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID557237Ratio of drug level before intrapartum initiation to 30 days pre-last dose of HIV-infected Thai pregnant women serum at 400 mg, po bid in combination with 100 mg, po bid ritonavir2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID246193Protease inhibitory activity against HIV-1 r13025 mutant strain was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
AID1717747Cytotoxicity against African green monkey Vero E6 cells incubated for 3 days by the MTS assay2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).
AID557241Ratio of drug level in 4 hrs to 30 days post last dose of HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID698060Selectivity index, ratio of Ki for HIV protease G48V mutant to Ki for HIV1 wild type protease2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Rational approaches to improving selectivity in drug design.
AID278968Antiviral activity against HIV1 C1 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID726412Selectivity ratio of EC50 for Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant to EC50 for wild type Human immunodeficiency virus 1 3B2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID532474Antiviral activity against Human immunodeficiency virus 1 isolate 35 harboring Gag-capsid V159I, I223T, N252S, A326S/A, A340G and G357S mutant gene and protease I15V, G16E, E35D, S37N, L63H and I72V mutant gene infected in human MT-2 cells by XTT-assay re2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1669455Inhibition of HIV1 NL4-3 protease I84V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 min2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.
AID415247Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
AID564033Selectivity ratio of CC50 for human MT2 cells to EC50 for HIV1 LAI infected human MT2 cells2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID396261Ratio of EC50 for HIV1 drug resistant mutant isolates from protease inhibitor treated HIV patient to EC50 for drug sensitive HIV1 NL4-32007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV.
AID1482922Ratio of IC50 for amprenavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/L33F/M46L/I54M/A71V mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID532470Antiviral activity against Human immunodeficiency virus 1 isolate 10 harboring Gag-capsid I138L, I147L, V159I, V215L, G248A, I256V, T280V, R286K and N315H mutant gene and protease L10I, K20R, E35D, M36I, S37N, R41K, K45R, F53L, I54V, L63P, I64V, A71T, V822010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID374618Resistance index, ratio of EC50 for HIV1 with protease 33F/46I/84V/88D/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID572573Cmin in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen.
AID353733Cmax in po dosed Beagle dog at dose molar equivalent to 5 mg/kg LPV, po coadministered with RTV dosed as 5% dextrose containing solution2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir.
AID575064Antiviral activity against Human immunodeficiency virus 1 harboring M46I and L76V mutations in viral protease assessed as fold change in drug susceptibility relative to wild type2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease.
AID1422659Inhibition of ZMPSTE24 in human SW1990 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration.
AID525289Antigametocyte activity against Plasmodium falciparum D10 trophozoites assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
AID519551Antiviral activity against HIV1 isolate 8 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I13V, L33F, E34Q, R41K, M46I, I54V, K55R, R57K, Q58E, I62V, L63P, A71V, I72I/T, G73S, V82A, I84V, L90M mutati2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
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
AID1725422Antiviral activity against HIV1 DRVR P30 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities.
AID557229Drug level in HIV-infected Thai pregnant women serum before intrapartum initiation of 400 mg, po bid in combination with 100 mg, po bid ritonavir2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID249499Toxicity value against wild type HIV-1 IIIB was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
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.
AID1482917Ratio of IC50 for darunavir-resistant HIV1 derived from 30 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/K70R/V82A/I84V/L89M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID590915Inhibition of HIV1 subtype C protease expressed in Escherichia coli BL21 assessed as hydrolysis of substrate using chromogenic substrate Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 by spectrophotometric analysis2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease.
AID525167Antimicrobial activity against chloroquine-resistant Plasmodium falciparum 3D7 infected in human erythrocytes assessed as potentiation of choloroquine-mediated antimalarial activity by light microscopy2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo.
AID525171Antimicrobial activity against chloroquine-resistant Plasmodium chabaudi ASCQ infected in NIH mice (Mus musculus) assessed as potentiation of 2.5 mg/kg chloroquine-mediated antimalarial activity at 100 mg/kg, perorally administered after 72 hrs post inocu2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo.
AID374635Resistance index, ratio of EC50 for HIV1 with protease 46L/48V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID586627Antiviral activity against HIV1 harboring mutant protease with matrix A81T mutant infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID321687Antiviral activity against HIV1 mutant strain 22008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID519574Antiviral activity against HIV1 P21 infected in human MT4 cells derived from viral passages with A-790742 harboring protease L23I, L33F, K45I, A71A/V, V77I, V82L, and I84V mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infecti2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID322099Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID372189Resistance index, ratio of EC50 for HIV1 with protease 46I mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID564030Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID519537Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID557220Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured 2 hrs post last dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
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]
AID322121Antiviral activity against HIV1 BaL R5 subtype B in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID321689Antiviral activity against HIV1 mutant strain 42008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID242869Association rate constant for the interaction between the compound and serum albumin2005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID532459Antiviral activity against Human immunodeficiency virus 1 isolate 36 harboring Gag-capsid I138L, A146P, S165N/S, E207D, V215L and E312D mutant gene and protease K14R/K, I15V, E35D, S37D, R57K/R and L63P mutant gene infected in human MT-2 cells by XTT-assa2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID618427Cytotoxicity against human MT4 cells after 5 days by XTT assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: a hybrid 2D NMR and docking/QM/MM/MD approach.
AID374602Resistance index, ratio of EC50 for HIV1 with protease 24I/33F/46I/54L/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID1474090Ratio of drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological 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.
AID446203Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate TM to IC50 for wild type HIV1 isolate ERS104pre2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID374616Resistance index, ratio of EC50 for HIV1 with protease 46I/88S mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID705597Time dependent inhibition of CYP3A4-mediated testosterone-6-beta hydroxylation in human liver microsome2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.
AID1482912Antiviral activity against darunavir-resistant HIV1 derived from 20 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/V82A/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemil2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID278981Resistance to HIV1 with protease 46I, 54I and I84V mutation in HEK 293 cells relative to similar background2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID1422662Antimigratory activity against human KP4 cells at 10 uM after 10 days by crystal violet staining-based assay2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration.
AID547234Selectivity ratio of EC50 for HIV1 subtype C harboring protease L32I, M46I/M, L76V mutant gene and polymorphism at I36 position to EC50 for wild type HIV1 subtype C2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes.
AID683727Antimalarial activity against liver stages of Plasmodium berghei 17XNL infected in human Hepa1-6 cells assessed as reduction in liver parasite load at 10 uM/L incubated for 1 hr prior to sporozoite inoculation measured after 46 to 48 hrs by fluorescence m2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Targeting the liver stage of malaria parasites: a yet unmet goal.
AID726417Cytotoxicity against human MT4 cells2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID622657Antiviral activity against HIV1 A17 harboring protease L10F, V32I, M46I, I47V, Q58E and I84V mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay relative to wild type HIV1 pNL4-32011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.
AID321692Antiviral activity against HIV1 mutant strain 72008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
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.
AID572576Half life in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen.
AID519795Antiviral activity against HIV 2 subtype B clinical isolate expressing 41D protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID343024Ratio of Ki for HIV1 recombinant protease A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
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.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1482920Antiviral activity against indinavir-resistant HIV1 NL4-3 harboring protease L10F/L24I/M46I/I54V/L63P/A71V/G73S/V82T mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID1219722Drug metabolism in human liver microsomes assessed as GSH-conjugated dihydroxylated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID375206Ratio of EC50 for multidrug-resistant HIV1 isolate C to EC50 for wild type HIV1 isolate ERS104pre2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.
AID369838Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID582279AUC in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors.
AID557291Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID519788Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-40D-43I-70K-82F-84V-85L-89V-90M-91T/L-98N/K protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
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.
AID532476Antiviral activity against Human immunodeficiency virus 1 isolate 23 harboring Gag-capsid I138L, V215L, E319D, A340G, G357S and V362I mutant gene and protease L10V, V11L, V32I, L33F, E34Q, E35D, M36L, S37T, M46I, I47V, G48V, I54M, I62V, L63P, I64V, I72V, 2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID321688Antiviral activity against HIV1 mutant strain 32008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID618426Inhibition of HIV1 subtype C protease Q7K mutant expressed in Escherichia coli BL21 (DE3) pLysS using Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 as substrate by spectrophotometry2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: a hybrid 2D NMR and docking/QM/MM/MD approach.
AID1474089Drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs2013Toxicological 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.
AID1219723Drug metabolism in human liver microsomes assessed as GSH-conjugated trihydroxylated/dehydrogenated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID374621Resistance index, ratio of EC50 for HIV1 with protease 33F/54L/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID557285Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID519539Antiviral activity against wild-type HIV1 RF infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1380928Resistance index, ratio of EC50 for antiviral activity against ATV resistant HIV1 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 NL4-3 infected 2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
AID532656Antiviral activity against Human immunodeficiency virus 1 isolate 2 harboring Gag-capsid A146P, S173A, V215L, H219P, E230D, N252S, R264K, L268M and A340G mutant gene and protease L10I, I15V, K20R, M36I, S37N, M46I, L63P, T80A, V82A, N83H, I84V, I85T and L2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID248545Inhibitory concentration against wild type Human immuno deficiency virus (EP13) was determined in an MT-4 cell line2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles.
AID553578Antiviral activity against HIV1 JSL harboring L10I/L24I/L33F/E35D/M36I/N37S/M46L/I54V/R57K/I62V/L63P/A71V/G73S/82A in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID263208Antiviral activity against HIV1 EP13 in MT4 cells2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
AID537772Antiviral activity against multidrug resistant Human immunodeficiency virus 1 MDRC42010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
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.
AID372187Resistance index, ratio of EC50 for HIV1 with protease 54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID278955Antiviral activity against HIV1 A3 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID726414Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID557300Ratio of EC50 for HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID564041Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
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.
AID106953Antiviral activity against HIV in presence of 50% human serum in MT-4 cell was determined2001Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
AID564060Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID1409307Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.
AID322106Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID566852Antiviral activity against HIV-1 MDR/JSL infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation.
AID1717811Toxicity in human infected with SARS-CoV2 assessed as adverse events at at 400 mg, po administered twice daily cotreated with 100 mg ritonavir and measured after 14 days2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).
AID321684Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM in presence of 2.5 uM ritonavir by RP-HPLC2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID278962Antiviral activity against HIV1 A10 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID446194Antiviral activity against multidrug-resistant HIV1 isolate B infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID415283Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
AID1717742Antiviral actvity against SARS-CoV2 infected in human assessed as improvement rate of chest at 400 mg, po administered twice daily cotreated with 100 mg ritonavir and measured after 14 days by computed tomography2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).
AID1717743Selectivity index, ratio of CC50 for human Huh-7 cells to EC50 for HCoV-229E harboring GFP infected in human Huh-7 cells2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).
AID575061Antiviral activity against Human immunodeficiency virus 1 harboring M46I, M46L, I54V, and V82A mutations in viral protease assessed as fold change in drug susceptibility relative to wild type2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease.
AID572580AUC in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen.
AID328890Inhibition of farnesyl transferase2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID328885Toxicity in human HeLa cells transfected with GFP-prelamin A construct assessed as accumulation of uncleaved protein at 20 uM by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID557288Antiviral activity against HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of nelfinavir by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
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.
AID566846Antiviral activity against wild type HIV-1 ERS104 pre infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation.
AID705596Inhibition of CYP3A4-mediated testosterone 6 beta hydroxylation in human liver microsome by Dixon plot analysis2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.
AID374636Resistance index, ratio of EC50 for HIV1 with protease 48V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID374608Resistance index, ratio of EC50 for HIV1 with protease 33I/46I/84V/88D/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID375201Antiviral activity against multidrug-resistant HIV1 isolate MM infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.
AID446199Antiviral activity against multidrug-resistant HIV1 isolate JSL infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
AID582281Clearance in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors.
AID321678Metabolic stability in rat liver microsomes assessed as compound remaining at 5 uM in presence of 2.5 uM ritonavir by RP-HPLC2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID279339Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with V62A and L99F mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID537765Inhibition of wild type HIV1 protease by FRET2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
AID564044Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID1380924Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
AID582275Cmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors.
AID322123Antiviral activity against HIV1 92TH019 R5 subtype E in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID668812Selectivity index, ratio of EC50 for Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant to EC50 for Human immunodeficiency virus 1 3B expressing wild-type protease2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID622578Antiviral activity against wild type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.
AID1593667Prodrug conversion assessed as calf intestinal alkaline phosphatase-mediated compound dephosphorylation by measuring half life by UPLC-MS/MS analysis2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID519540Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID257269Inhibitory activity against HIV1 protease at 0.5 uM2005Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
AID239809Equilibrium dissociation constant for the interaction between the compound and serum albumin2005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID1482916Ratio of IC50 for darunavir-resistant HIV1 derived from 20 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/V82A/L89M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID369955Ratio of EC50 for HIV2 ROD with protease G17N mutation to EC50 for wild type HIV2 ROD2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID558376Drug level in HIV-infected pregnant woman cord blood plasma at 400 mg, po BID by HPLC/UV analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women.
AID343023Ratio of Ki for HIV1 recombinant protease M46I/A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID532468Antiviral activity against Human immunodeficiency virus 1 isolate 3 harboring Gag-capsid I138L, A146P, I147L, V159I, S176A, V215L, H219Q/H, T242N, G248A, T280V, A340G and G357S mutant gene and protease L10I, T31S/T, V32I, M36I/M, S37C, R41K, M46I, F53L, I2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID537770Antiviral activity against Human immunodeficiency virus 1 clade C isolated from HIV-AIDS patient2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
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.
AID525485Antigametocyte activity against drug-resistant Plasmodium falciparum Dd2 schizonts assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
AID519547Antiviral activity against HIV1 isolate 4 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease N37T, M46I, Q58E, I64V, T74K, V77I, V82F, L90M mutation derived from viral passages with Lopinavir assessed as redu2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1380925Antiviral activity against ATV resistant HIV1 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
AID374606Resistance index, ratio of EC50 for HIV1 with protease 46I/82T/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID322104Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID532472Antiviral activity against Human immunodeficiency virus 1 isolate 33 harboring Gag-capsid I138L, V215L, V218P, H219Q, I223V, M228I, G248T, N252S, N253T, I256M, E312D and A326S mutant gene and protease T12S/T, I13V/I, I15V, L19I, S37T, L63V/A/P/L and I72V/2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID557233Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir measured 4 hrs post last dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID557281Ratio of EC50 for HIV1 B harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region to EC50 for HIV1 ERS104pre2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID278957Antiviral activity against HIV1 A5 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID369961Ratio of EC50 for HIV2 MS infected in human MT4 cells after 1 passage to EC50 for HIV2 MS infected in human MT4 cells2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID328879Toxicity in RCE1 deficient mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 24 hrs by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID369945Ratio of EC50 for HIV2 CBL-23 infected in human PBMC to EC50 for HIV1 NL4-3 infected in human MT4 cells2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID417047Inhibition of esterase mediated-hydrolysis of tenofovir disoproxil fumarate in human intestinal sub cellular fraction S9 at 2 uM after 30 mins2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
AID274382Inhibition of HIV1 protease L10I/L63P/A71V/G73S/I84V/L90M mutant2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.
AID321683Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM in presence of 0.5 uM ritonavir by RP-HPLC2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
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.
AID557296Ratio of EC50 for HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID374632Resistance index, ratio of EC50 for HIV1 with protease 46L/54V/73C/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID278983Resistance to HIV1 with protease 46I/L, 54I and I84C mutation in HEK 293 cells relative to similar background2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID322113Antiviral activity against HIV1 MDR/TM X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID442714Fold resistance, ratio of EC50 for indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells to EC50 for HIV1 pNL4-3 infected in human MT4 cells2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket.
AID1482924Ratio of IC50 for indinavir-resistant HIV1 NL4-3 harboring protease L10F/L24I/M46I/I54V/L63P/A71V/G73S/V82T mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID375203Antiviral activity against multidrug-resistant HIV1 isolate G infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.
AID557222Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured 12 hrs post last dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID698062Binding affinity to wild type HIV1 protease2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Rational approaches to improving selectivity in drug design.
AID322107Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID374614Resistance index, ratio of EC50 for non-B type HIV1 with protease 46I/47V/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID532477Antiviral activity against Human immunodeficiency virus 1 isolate 24 harboring Gag-capsid I138L, V159I, V215L, I223A, T239S, N252S, T280V, R286K, S310T and V362I mutant gene and protease L10V, I13V, I15V, K20R, D30N, V32I, L33F, E35D, M36I, S37N, K43T, M42010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID263207Antiviral activity against HIV1 HXB2 in MT4 cells2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
AID1409311Antiviral activity against darunavir-resistant HIV1 at passage 21 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.
AID374594Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-32007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID557217Cmax in HIV-infected Thai pregnant women at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured within 72 hrs postpartum2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID726419Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID242932Dissociation rate constant for the interaction between the compound and serum albumin2005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions.
AID369948Antiviral activity against HIV2 MS infected in human PBMC cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
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.
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.
AID328895Effect on change in ZMPSTE24 protein level in mouse fibroblasts at 20 uM after 10 days by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID1219725Drug metabolism in human liver microsomes assessed as lopinavir semicarbazide adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.
AID582274AUC in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors.
AID519644Antiviral activity against HIV1 isolate 6 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, L24I, M46I, I54V, K55R, Q58E, L63P, I64V, A71V, V82A, T91A mutation derived from viral passages with Lopinavi2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID278978Antiviral activity against HIV1 C11 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID1482911Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID246965Effective dose of compound required to inhibit replication of human immunodeficiency virus type 1 in MT-4 cells2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
AID553570Cytotoxicity against human MT2 cells by MTT assay2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
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.
AID321661Antiviral activity against HIV1 3B2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
AID1307690Binding affinity to HIV1 protease2016Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9
OpenGrowth: An Automated and Rational Algorithm for Finding New Protein Ligands.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID279337Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 182L mutation in CBMCs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
AID322120Antiviral activity against HIV1 92UG037 subtype A R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID322109Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID557289Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID369949Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID263209Antiviral activity against HIV D545701 in MT4 cells2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
AID564036Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID582277Plasma concentration in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir measured 12 hrs after last dose2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors.
AID1482907Ratio of IC50 for saquinavir-resistant HIV1 NL4-3 harboring protease L10I/N37D/G48V/I54V/L63P/G73C/I84V/L90M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
AID374617Resistance index, ratio of EC50 for HIV1 with protease 33F/54L/88S/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID374637Resistance index, ratio of EC50 for HIV1 with protease 46L/48V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID246225Protease inhibitory activity against HIV-1 GSS004421 mutant strain was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
AID525486Antigametocyte activity against drug-resistant ring stage Plasmodium falciparum Dd2 assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
AID726418Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication in presence of 50% human plasma2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID372192Resistance index, ratio of EC50 for HIV1 with protease 46I/50V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID278954Antiviral activity against HIV1 A2 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
AID343021Inhibition of HIV1 recombinant protease L10F/L19I/K20R/L33F/E35D/M36I/R41K/F53L/I54V/L63P/H69K/A71V/T74P/I84V/L89M/L90M/I93L mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID239819Association rate constant for human immunodeficiency virus type 1 protease2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
AID519543Antiviral activity against HIV1 P25 infected in human MT4 cells harboring protease L10F, G16E, V32I, M46I, I47A, H69Y, I84V, and T91S mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post in2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID416867Effect on tenofovir disoproxil fumarate metabolism in ritonavir booster drug treated HIV infected patient assessed as change in plasma AUC of tenofovir at 400 mg, po, BID co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
AID532456Antiviral activity against Human immunodeficiency virus 1 isolate 21 harboring Gag-capsid I138L, A146P, I147L/I, V159I/V, E211D, V215L, N252H/N, R286K/R and K331R/K mutant gene and protease E35D, M36I, S37N, I62V and L63C mutant gene infected in human MT-2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID532658Antiviral activity against Human immunodeficiency virus 1 isolate 29 harboring Gag-capsid I138M, A146P, R286K, T303V and A326S mutant gene and protease L10F, I13V, V32I, M36L, S37N, L38W, P39Q, M46I, I47V, I50V, I62V, L63P, A71I, I72V and V82A mutant gene2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
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.
AID564045Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID557219Tmax in HIV-infected Thai pregnant women at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured within 72 hrs postpartum2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women.
AID588981Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1B12010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID322108Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
AID246195Protease inhibitory activity against HIV-1 r13363 mutant strain was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
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]
AID1474088AUC in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs2013Toxicological 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.
AID553575Antiviral activity against HIV1 MOKW infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID668813Selectivity index, ratio of EC50 for Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant to EC50 for Human immunodeficiency virus 1 3B expressing wild-type protease2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID553568Selectivity index, ratio of CC50 for human MT2 cells to EC50 for HIV1 LAI2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
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.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID564062Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID1350504Cytotoxicity against human MT4 cells after 5 days by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine.
AID525280Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum D10 after 48 hrs2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
AID1717744Cytotoxicity against human Huh-7 cells incubated for 1 hr by MTS assay2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).
AID374631Resistance index, ratio of EC50 for HIV1 with protease 46I/54V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
AID246160Protease inhibitory activity against wild type HIV-1 IIIB was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
AID1422657Inhibition of ZMPSTE24 in human HPAF2 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration.
AID547240Selectivity ratio of EC50 for HIV1 subtype CRF02_AG harboring protease M46, I47A, I84V mutant gene and polymorphism at I36 position to EC50 for wild type HIV1 subtype CRF02_AG2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes.
AID519578Antiviral activity against HIV1 clone3 infected in HEK293 cells harboring A-790742-selected protease L33F, K45I, V82L, and I84V mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pNL4-32008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID546999Antiviral activity against HIV1 subtype C harboring protease L32I, M46I/M, L76V mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gen2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes.
AID416857Decrease in P-glycoprotein-mediated tenofovir disoproxil fumarate efflux in MDCK2 expressing human MDR1 cells at 20 uM2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
AID557275Antiviral activity against HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
AID328876Toxicity in human AG08470 cells assessed as accumulation of prelamin A at 20 uM after 10 days by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID564047Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
AID322119Antiviral activity against HIV1 92UG029 X4 subtype A in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory 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.
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.
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.
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.
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.
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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2013Biochemical and biophysical research communications, Jul-26, Volume: 437, Issue:2
Crystallographic study of multi-drug resistant HIV-1 protease lopinavir complex: mechanism of drug recognition and resistance.
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.
AID1804127No assay is provided from Article 10.1002/med.21724: \\The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.\\2021Medicinal research reviews, 01, Volume: 41, Issue:1
The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.
AID1804171DRC analysis by immunofluorescence from Article 10.1128/AAC.00819-20: \\Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.\\2020Antimicrobial agents and chemotherapy, 06-23, Volume: 64, Issue:7
Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.
AID1805801Various Assay from Article 10.1021/acs.jmedchem.1c00409: \\Perspectives on SARS-CoV-2 Main Protease Inhibitors.\\2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Perspectives on SARS-CoV-2 Main Protease Inhibitors.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2002Bioorganic & medicinal chemistry, Aug, Volume: 10, Issue:8
X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease.
AID1811Experimentally measured binding affinity data derived from PDB2002Bioorganic & medicinal chemistry, Aug, Volume: 10, Issue:8
X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease.
AID1811Experimentally measured binding affinity data derived from PDB2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2007Journal of virology, May, Volume: 81, Issue:10
Unique thermodynamic response of tipranavir to human immunodeficiency virus type 1 protease drug resistance mutations.
AID1811Experimentally measured binding affinity data derived from PDB2007Journal of virology, May, Volume: 81, Issue:10
Unique thermodynamic response of tipranavir to human immunodeficiency virus type 1 protease drug resistance mutations.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2008Protein science : a publication of the Protein Society, Sep, Volume: 17, Issue:9
Enzymatic and structural analysis of the I47A mutation contributing to the reduced susceptibility to HIV protease inhibitor lopinavir.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,262)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's19 (0.84)18.2507
2000's771 (34.08)29.6817
2010's840 (37.14)24.3611
2020's632 (27.94)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 59.80

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 Index59.80 (24.57)
Research Supply Index7.97 (2.92)
Research Growth Index6.04 (4.65)
Search Engine Demand Index101.74 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (59.80)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials499 (20.94%)5.53%
Reviews213 (8.94%)6.00%
Case Studies198 (8.31%)4.05%
Observational62 (2.60%)0.25%
Other1,411 (59.21%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (281)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Pharmacokinetics of Pediatric Aluvia® (Lopinavir /Ritonavir 100/25 mg) and Generic Lopinavir/Ritonavir Tablet Formulation (200/50 mg) in Clinically and Virologically Stable HIV-1 Infected Thai Adults [NCT01159275]Phase 1/Phase 220 participants (Actual)Interventional2009-07-31Completed
Pharmacokinetic Interactions Between an Herbal Medicine (African Potato) and Antiretroviral Agents (Lopinavir/Ritonavir) [NCT01227590]Phase 118 participants (Actual)Interventional2010-02-28Completed
Phase II, Parallel, Randomized, Clinical Trials Comparing the Responses to Initiation of NNRTI-Based Versus PI-Based Antiretroviral Therapy in HIV Infected Infants Who Have and Have Not Previously Received Single Dose Nevirapine for Prevention of Mother-t [NCT00307151]Phase 2452 participants (Actual)Interventional2005-12-31Completed
Maternal Tenofovir-containing Combination Drug Regimen During the Second and Third Trimesters of Pregnancy for Prevention of Mother-to-child Transmission of HIV and HBV in HIV-HBV Co-infected Mothers [NCT01125696]Phase 245 participants (Actual)Interventional2012-05-31Completed
The Influence of Ritonavir, Alone and in Combination With Lopinavir, on Fenofibric Acid Pharmacokinetics in Healthy Volunteers [NCT01148004]Phase 125 participants (Actual)Interventional2010-05-13Completed
Phase 2 Comparison of Low-Dose Naltrexone vs ARV Effectiveness in HIV+ Progression [NCT01174914]Phase 2171 participants (Actual)Interventional2008-03-31Completed
Optimal Combination Therapy After Nevirapine Exposure [NCT00089505]Phase 3745 participants (Actual)Interventional2006-11-30Completed
A Multicenter Phase III Trial of Second-line Antiretroviral Treatment Strategies in African Adults (Tanzania Ans South Africa) Using Atazanavir or Lopinavir/Ritonavir [NCT01255371]Phase 30 participants (Actual)Interventional2012-03-31Withdrawn(stopped due to drug procurement issues)
A Randomized Controlled Study Compares the 48 Weeks Results of HIV-1 RNA Between Ritonavir-boosted Lopinavir Monotherapy and Ritonavir-boosted Lopinavir + Optimized Background Regimens in HIV-1 Infected Patients Who Have HIV-1 RNA <50 Copies/ml More Than [NCT01189695]Phase 463 participants (Actual)Interventional2010-12-31Completed
Comparative LUSZ Therapeutic Study of Antiviral, Antiretroviral, and Immunosuppressive Treatments in Hospitalized COVID-19 Patients With High-Risk Factors, Biomarkers, and Disease Progression. [NCT05925140]Phase 11,000 participants (Anticipated)Interventional2020-03-28Recruiting
Randomised Evaluation of COVID-19 Therapy [NCT04381936]Phase 2/Phase 350,000 participants (Anticipated)Interventional2020-03-19Recruiting
The Effect of Kaletra on CD4 Immune Reconstitution in HIV-infected Patients With Long-term Virologic Suppression on a Non-Kaletra Containing ART Regimen, But With a Blunted Immune Response [NCT00344487]3 participants (Actual)Interventional2005-12-31Terminated(stopped due to Inability to enroll subjects.)
Randomized Trial of a Switch to a Kaletra + Current Dual Nucleoside Reverse Transcriptase Inhibitor (NRTI) Backbone Versus Continuation of the Current Regimen in Patients With Poor Immune Responses to Highly Active Antiretroviral Therapy (HAART) in Patien [NCT00145795]Phase 420 participants (Actual)Interventional2004-04-30Completed
"Safeguard the Household - A Study of HIV Antiretroviral Therapy Treatment Strategies Appropriate for a Resource Poor Country" [NCT00255840]812 participants (Actual)Interventional2006-07-31Completed
Metabolic Effects of Switching Kaletra to Boosted Reyataz [NCT00413153]15 participants (Actual)Interventional2006-05-31Completed
Maintaining Options for Mothers Study (MOMS): A Phase II Randomized Comparison of Three Antiretroviral Strategies Administered for 7 or 21 Days to Reduce the Emergence of Nevirapine Resistant HIV-1 Following a Single Intrapartum Dose of Nevirapine [NCT00099632]Phase 2484 participants (Actual)Interventional2006-03-31Completed
Use of an Aluvia Based Highly Active Antiretroviral Therapy (HAART) Regimen in the Prevention of Mother to Child HIV Transmission (PMTCT) Antepartum, Intrapartum and Postpartum in Africa [NCT01088516]Phase 4280 participants (Actual)Interventional2008-12-31Completed
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.)
Changes in Insulin Resistance in Healthy Volunteers on STRIBILD® Medication - A Controlled, Mono Center, Three-arm, Randomized Phase I Study. [NCT02203461]Phase 130 participants (Actual)Interventional2014-07-31Completed
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
Multicenter Study of Options for Second-Line Effective Combination Therapy (SELECT) [NCT01352715]Phase 3515 participants (Actual)Interventional2012-03-13Completed
Combination Therapies to Reduce the Nasopharyngeal Carriage of SARS-CoV-2 and Improve the Outcome of COVID-19 Infection in Ivory Coast (INTENSE-COV): a Phase IIb Randomized Clinical Trial [NCT04466241]Phase 2/Phase 3294 participants (Anticipated)Interventional2020-11-27Recruiting
Phase II Study of the Pharmacokinetics of Nevirapine and the Incidence of Nevirapine Resistance Mutations in HIV-Infected Women Receiving a Single Intrapartum Dose of Nevirapine With the Concomitant Administration of Zidovudine/Didanosine or Zidovudine/Di [NCT00109590]Phase 2175 participants (Actual)Interventional2006-06-30Completed
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
Efficacy and Safety of Darunavir/Cobicistat vs. Lopinavir/Ritonavir in the Management of Patients With COVID-19 Pneumonia in Qatar [NCT04425382]400 participants (Actual)Observational2020-03-01Completed
Multi-centre, Adaptive, Randomized Trial of the Safety and Efficacy of Treatments of COVID-19 in Hospitalized Adults [NCT04315948]Phase 31,552 participants (Actual)Interventional2020-03-22Completed
HIV Infection and Gut Mucosal Immune Function: Longitudinal Analyses of Intestinal CD4+ and Th17 T Cells in HIV-infected Individuals on Short-term Antiretroviral Therapy [NCT02097381]10 participants (Actual)Interventional2010-04-30Active, not recruiting
Implementation and Evaluation of an HIV-2 Viral Load and ARV Resistance Informed Algorithm for 2nd-line ART in HIV-2 Infected Patients in the Initiative Sénégalaise d'Accès Aux Antirétroviraux (ISAARV) Program [NCT03394196]152 participants (Actual)Interventional2018-07-04Terminated(stopped due to COVID-19 and Funding)
A Phase 3, Randomized, Open Label, Controlled Study of Lopinavir/Ritonavir and Lamivudine Versus Standard Therapy in Naïve HIV-1 Infected Subjects. [NCT01237444]Phase 3417 participants (Actual)Interventional2010-12-31Completed
The SETPOINT Study - A Randomized Study of the Effect of Immediate Treatment With Potent Antiretroviral Therapy Versus Observation With Treatment as Indicated in Newly Infected HIV-1 Infected Subjects: Does Early Therapy After the Virologic Setpoint? [NCT00090779]Phase 2130 participants (Actual)Interventional2005-01-31Terminated(stopped due to The DSMB concluded that the findings regarding the primary analysis would persist and that no additional study goals would be achieved by continuing the study.)
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289]1,578 participants (Actual)Observational2003-06-09Completed
Exploratory, Cross-sectional Study to Compare the Virologic Efficacy in Cerebrospinal Fluid (CSF) and Neurocognitive State in Patients Infected by HIV-1 Long-term Treatment (> 3 Years) With Lopinavir / Ritonavir Monotherapy [NCT01116817]Phase 435 participants (Actual)Interventional2010-08-31Completed
Pharmacokinetics of Low- Dose Lopinavir/Ritonavir Tablet Formulation HIV-1 Infected Children [NCT01139905]Phase 224 participants (Actual)Interventional2010-04-30Completed
A Phase IIa Randomized, Controlled Study of Combination Therapies to Treat COVID-19 Infection [NCT04459702]Phase 20 participants (Actual)Interventional2020-07-31Withdrawn(stopped due to Was never started)
COVID-19 Ring-based Prevention Trial With Lopinavir/Ritonavir [NCT04321174]Phase 3123 participants (Actual)Interventional2020-04-17Active, not recruiting
A Randomized Prospective Open Label Study of Switching to Raltegravir Based ART Compared to Maintaining Ritonavir Boosted PI-based ART on Liver Fibrosis Progression in HIV-HCV Coinfected Patients [NCT01231685]Phase 29 participants (Actual)Interventional2011-12-31Completed
A Double-Blind, Randomized, Placebo-Controlled Phase II Study of Lopinavir/Ritonavir Versus Placebo in COVID-19 Positive Patients With Cancer and Immune Suppression in the Last Year [NCT04455958]Phase 20 participants (Actual)Interventional2021-05-01Withdrawn(stopped due to limited resources)
Ensayo clínico, Abierto, Aleatorizado Para Comparar la Calidad de Vida de Los Pacientes VIH+ Que Inician Monoterapia Con Comprimidos de LPV/r vs Triple Terapia Que Contenga un IP Potenciado [NCT01166477]Phase 4228 participants (Actual)Interventional2010-01-31Completed
the Investigation Into Beneficial Effects of High-dose Interferon Beta 1-a, Compared to Low-dose Interferon Beta 1-a in Moderate to Severe Covid-19 [NCT04521400]Phase 2100 participants (Anticipated)Interventional2020-08-20Not yet recruiting
Phase II Trial of Ritonavir/Lopinavir in Patients With Progressive of Recurrent High-Grade Gliomas [NCT01095094]Phase 219 participants (Actual)Interventional2009-01-31Terminated(stopped due to Study did not meet its primary objective)
Multicenter Clinical Study on the Efficacy and Safety of Xiyanping Injection in the Treatment of New Coronavirus Infection Pneumonia (General and Severe) [NCT04295551]80 participants (Anticipated)Interventional2020-03-14Not yet recruiting
Protease Inhibitors to Reduce Malaria Morbidity in HIV-Infected Pregnant Women [NCT00993031]Phase 3389 participants (Actual)Interventional2009-12-15Completed
Atazanavir (BMS-232632) for HIV Infected Individuals Completing Atazanavir Clinical Trials: An Extended Access Study [NCT01003990]Phase 3710 participants (Actual)Interventional2002-10-31Completed
A Randomised Controlled Trial Comparing the Efficacy of Infant Peri-exposure Prophylaxis With Lopinavir/Ritonavir (LPV/r) Versus Lamivudine to Prevent HIV-1 Transmission by Breastfeeding [NCT00640263]Phase 31,500 participants (Anticipated)Interventional2009-12-31Completed
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
A Randomised, Open Label Switch Study Comparing Darunavir/Ritonavir 400mg/100mg Daily With Lopinavir/Ritonavir 800mg/200mg Daily, in HIV-positive Participants [NCT02671383]Phase 3300 participants (Actual)Interventional2016-06-30Completed
Phase IV, Non Randomized Study in ARV Experienced Patients Under Switch Therapy With Kaletra [NCT00648999]Phase 4207 participants (Actual)Interventional2003-11-30Completed
A Pilot Study Of the Effects of Highly Active Antiretroviral Therapy on Kaposi's Sarcoma in Zimbabwe [NCT00834457]Phase 2/Phase 349 participants (Actual)Interventional2007-06-30Completed
A Randomized, Open-label Trial to Compare the Efficacy and Safety of Early Initiation of cART With or Without Autologous HIV-1 Specific Cytotoxic T Lymphocyte (CTL) Infusion in Treatment-Naïve Acute HIV-1 Infected Adults [NCT02231281]Phase 365 participants (Anticipated)Interventional2014-08-31Active, not recruiting
A Randomized, Non-comparative, Phase IIb, Unblinded Trial, Evaluating the Efficacy and Safety of Tenofovir-emtricitabine or Lamivudine Plus Zidovudine, Lopinavir/Ritonavir, or Raltegravir, Among ARV-naïve HIV-2 Infected Adult Patients, in West Africa [NCT02150993]Phase 2/Phase 3210 participants (Actual)Interventional2016-01-26Completed
Trial of Early Therapies During Non-hospitalized Outpatient Window (TREAT NOW) for COVID-19 [NCT04372628]Phase 2452 participants (Actual)Interventional2020-06-01Completed
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
Lopinavir/Ritonavir as an Immunomodulator to Enhance Vaccine Responsiveness [NCT01165645]0 participants (Actual)Interventional2010-11-30Withdrawn(stopped due to no patients enrolled)
An Adaptive, Multicenter, Randomized, Open-label, Comparative Clinical Study to Assess Efficacy and Safety of Favipiravir in Hospitalized Patients With COVID-19 [NCT04434248]Phase 2/Phase 3330 participants (Actual)Interventional2020-04-23Active, not recruiting
A 48-week, Randomized, Open-label, 2-arm Study to Compare the Efficacy of Saquinavir/Ritonavir Twice Daily (BID) Plus Emtricitabine/Tenofovir Once Daily (QD) Versus Lopinavir/Ritonavir BID Plus Emtricitabine/Tenofovir QD in Treatment-naïve Human Immunodef [NCT00105079]Phase 3337 participants (Actual)Interventional2005-04-30Completed
ProSpective, MultI-Center, Observational PrograM to Assess the Effectiveness of Dual TheraPy (Lopinavir/Ritonavir + LamivudinE) in Treatment-Experienced HIV Infected Patients in the Routine Clinical Settings of the Russian Federation (SIMPLE) [NCT02581202]216 participants (Actual)Observational2015-12-21Completed
Prophylaxis for HIV-1: Tenofovir/Emtricitabine (Truvada ®) + Lopinavir/Ritonavir (Kaletra ®) vs Tenofovir/Emtricitabine/Cobicistat/Elvitegravir (Stribild ®). Prospective, Randomized, Open. [NCT02198443]Phase 4160 participants (Actual)Interventional2015-06-06Completed
A Pilot Study to Assess the Safety, Efficacy, and PK Profile of a Switch in Antiretroviral Therapy to a RTI Sparing Combination of LPV/r and RAL in Virologically Suppressed HIV-infected Patients [NCT00700115]Phase 460 participants (Actual)Interventional2008-06-30Completed
Pilot Assessment of Lopinavir/Ritonavir and Maraviroc in Experienced Patients [NCT00981318]Phase 43 participants (Actual)Interventional2009-12-31Terminated(stopped due to unable to enroll expected number of subjects)
IMPAACT P1058A: Intensive Pharmacokinetic Studies of New Classes of Antiretroviral Drug Combinations in Children, Adolescents and Young Adults [NCT00977756]168 participants (Actual)Observational2002-08-31Completed
A Phase I, Open-label, Randomized Cross-over, 2-period, 2-way Interaction Trial to Investigate the Pharmacokinetic Interaction Between Lopinavir/Ritonavir and TMC125 Both at Steady-state in Healthy Subjects. [NCT00767117]Phase 116 participants (Actual)Interventional2008-09-30Completed
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
A Multicenter, Double-Blind, Randomized, Active-Controlled Study to Evaluate the Safety and Antiretroviral Activity of MK0518 Versus KALETRA in HIV-Infected Patients Switched From a Stable KALETRA-Based Regimen - Study A [NCT00443703]Phase 3352 participants (Actual)Interventional2007-05-31Terminated(stopped due to primary efficacy analysis at Week 24 did not demonstrate non-inferiority of raltegravir versus lopinavir (+) ritonavir)
Randomised and Prospective Clinical Study to Evaluate the Efficacy and Safety of Lopinavir/Ritonavir Monotherapy Versus Darunavir/Ritonavir Monotherapies as Simplification Switching Strategies of PI/NNRTI-Triple Therapy Based-Regimens [NCT00994344]Phase 473 participants (Actual)Interventional2009-10-31Completed
Randomized, Embedded, Multifactorial Adaptive Platform Trial for Community- Acquired Pneumonia [NCT02735707]Phase 310,000 participants (Anticipated)Interventional2016-04-11Recruiting
Phase III Open Label Atazanavir (BMS-232632) in Combination With Ritonavir or Saquinavir, and Lopinavir/Ritonavir, Each With Tenofovir and a Nucleoside in Subjects With HIV [NCT00035932]Phase 3571 participants (Actual)Interventional2001-11-30Completed
A Multicenter, Double-Blind, Randomized, Active-Controlled Study to Evaluate the Safety and Antiretroviral Activity of MK0518 Versus KALETRA in HIV-Infected Patients Switched From a Stable KALETRA-Based Regimen - Study B [NCT00443729]Phase 3355 participants (Actual)Interventional2007-05-31Terminated(stopped due to Primary efficacy analysis at Week 24 did not demonstrate non-inferiority of raltegravir versus lopinavir (+) ritonavir)
International Trial of Modified Directly Observed Therapy Versus Self-Administered Therapy for Participants With First Virologic Failure on a Non-Nucleoside Reverse Transcriptase Inhibitor-Containing Antiretroviral Regimen [NCT00608569]529 participants (Actual)Interventional2009-03-31Completed
A Randomized, Open-label, Multi-centre Clinical Trial Evaluating and Comparing the Safety and Efficiency of ASC09/Ritonavir and Lopinavir/Ritonavir for Confirmed Cases of Pneumonia Caused by Novel Coronavirus Infection [NCT04261907]6 participants (Actual)Interventional2020-02-11Terminated(stopped due to There were no more subjects enrolled.)
A Randomised Open-label Study Comparing the Safety and Efficacy of Ritonavir Boosted Lopinavir and 2-3N(t)RTI Backbone Versus Ritonavir Boosted Lopinavir and Raltegravir in Participants Virologically Failing First-line NNRTI/2N(t)RTI Therapy [NCT00931463]Phase 4558 participants (Actual)Interventional2009-09-30Completed
Multicentric, Non-inferiority, Randomized, Non-blinded Phase 3 Trial Comparing Virological Response at 48 Weeks of 3 Antiretroviral Treatment Regimens in HIV-1-infected Patients With Treatment Failure After 1st Line Antiretroviral Therapy (Cameroon, Burki [NCT00928187]Phase 3454 participants (Actual)Interventional2009-11-30Completed
An International Randomized Trial of Additional Treatments for COVID-19 in Hospitalized Patients Who Are All Receiving the Local Standard of Care Philippines [NCT05024006]1,314 participants (Actual)Interventional2020-04-23Completed
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
Lumefantrine Pharmacokinetics When Administered as a Fixed Dose Combination With Artemether in HIV Positive Patients on Lopinavir/Ritonavir [NCT00619944]Phase 432 participants (Anticipated)Interventional2008-02-29Completed
Pharmacokinetics of Rifabutin Combined With Antiretroviral Therapy in the Treatment of Tuberculosis Patient With HIV Infection in Vietnam : A Phase II Trial [NCT00651066]Phase 247 participants (Actual)Interventional2010-06-30Completed
A Randomised Controlled Trial to Evaluate Options for Second-line Therapy in Patients Failing a First-line 2NRTI + NNRTI Regimen in Africa [NCT00988039]Phase 31,277 participants (Actual)Interventional2010-03-31Completed
P1060 Substudy Comparing Differences in Malaria Parasitemia by Real Time Quantitative PCR in HIV-Infected Infants and Children on PI-Based HAART Versus NNRTI-Based HAART [NCT00719602]Early Phase 1105 participants (Actual)Interventional2009-08-31Completed
A Multicenter, Randomized, Open Label, Pilot Study to Assess the Possibility of Concomitant Treatment of HCV/HIV co Infection With Peg-interferon + Ribavirin, and Lopinavir/r as a Single Antiretroviral Agent. [NCT00866021]Phase 468 participants (Actual)Interventional2008-02-29Completed
A Phase IV-III Comparative, Randomized, Open-label Study to Evaluate the Efficacy for the Recovery of Peripheral Fat (or of the Extremities) of Lopinavir/Ritonavir in Monotherapy Versus Abacavir/Lamivudine and Lopinavir/Ritonavir [NCT00865007]Phase 488 participants (Actual)Interventional2008-12-31Completed
Effects of Traditional Chinese Medicines (TCMs) on Patients With COVID-19 Infection: A Perspective, Open-labeled, Randomized, Controlled Trial [NCT04251871]150 participants (Anticipated)Interventional2020-01-22Recruiting
Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs [NCT04278404]5,000 participants (Anticipated)Observational2020-03-05Recruiting
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
A Phase 3, Randomized, Open-Label Study of Lopinavir/Ritonavir (LPV/r) Tablets 800/200 Milligram (mg) Once-Daily (QD) Versus 400/100 mg Twice-Daily (BID) When Coadministered With Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs) in Antiretrov [NCT00358917]Phase 3599 participants (Actual)Interventional2006-08-31Completed
A Comparison of the Bioavailability of Rifabutin With and Without Lopinavir/Ritonavir in Healthy Adult Subjects [NCT00743470]Phase 115 participants (Actual)Interventional2008-08-31Terminated
Pharmacokinetics and Pharmacodynamics of Lopinavir an Anti-HIV Drug in Israeli Ethiopian and Non-Ethiopian Populations [NCT00347750]0 participants (Actual)Observational2006-09-30Withdrawn(stopped due to lack of participants)
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
Pilot Study Of Novel Combination Of Maraviroc + Atazanavir/Ritonavir vs. Atazanavir/Ritonavir + Emtricitabine/Tenofovir For The Treatment Of Naïve HIV-Infected Patients With R5 HIV-1 [NCT00827112]Phase 2129 participants (Actual)Interventional2009-03-31Completed
Prospective, Open Label and Randomized Clinical Trial About Hepatic Security of Antiretroviral Treatment Based on Kaletra Versus Nevirapine in Co-infected HIV/HCV Patients [NCT00661349]Phase 49 participants (Actual)Interventional2008-02-29Terminated(stopped due to It has been impossible to achieve the number of patients defined by protocol)
The Pharmacokinetics of Two Generic Co-formulations of Lopinavir/Ritonavir for HIV Infected Children: a Pilot Study of Lopimune vs. the Branded Product (SURF Study). [NCT00665951]Phase 112 participants (Actual)Interventional2008-09-30Completed
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
Pharmacokinetics of Lopinavir Crushed Versus Whole Tablets in Pediatric Patients [NCT00810108]Phase 412 participants (Actual)Interventional2006-06-30Completed
A Phase I Study to Evaluate the Effect of Darunavir/Ritonavir and Lopinavir/Ritonavir on GSK2248761 Pharmacokinetics and to Assess the Effect of GSK2248761 on CYP450 Probe Drugs in Healthy Adult Subjects [NCT00920088]Phase 124 participants (Actual)Interventional2009-06-30Completed
A Randomized, Open-label Study of Lopinavir/Ritonavir 400/100 mg Tablet Twice Daily + Co-formulated Emtricitabine/Tenofovir Disoproxil Fumarate 200/300 mg Once Daily Versus Lopinavir/Ritonavir 400/100 mg Tablet Twice Daily + Raltegravir 400 mg Twice Daily [NCT00711009]Phase 3206 participants (Actual)Interventional2008-07-31Completed
Safety and Efficacy of Lopinavir/Ritonavir in Combination With Raltegravir in HIV-infected Patients [NCT00752037]Phase 430 participants (Actual)Interventional2008-09-30Completed
Adjusting Antiretroviral Therapy Dosage Using Therapeutic Drug Monitoring [NCT00836212]Phase 412 participants (Anticipated)Interventional2008-03-31Recruiting
CID 0708 - Sex, Aging and Antiretroviral Pharmacokinetics [NCT00666055]11 participants (Actual)Observational2008-03-31Completed
Randomized Controlled Clinical Trials of Lopinavir/Ritonavir or Hydroxychloroquine in Patients With Mild Coronavirus Disease (COVID-19) [NCT04307693]Phase 265 participants (Actual)Interventional2020-03-11Terminated(stopped due to Terminated early because no patients were further enrolled since mid-Apr 2020.)
An Open, Prospective/Retrospective, Randomized Controlled Cohort Study to Compare the Efficacy of Three Antiviral Drugs(Abidol Hydrochloride, Oseltamivir and Lopinavir/Ritonavir) in the Treatment of 2019-nCoV Pneumonia. [NCT04255017]Phase 4400 participants (Anticipated)Interventional2020-02-01Recruiting
Kaletra and Maraviroc in Antiretroviral Therapy-Naïve Patients - KALMAR Study -Version 1.0 Amendment 2 [NCT01068873]Phase 41 participants (Actual)Interventional2010-04-30Terminated(stopped due to Poor enrollment)
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
The Effect of Pregnancy on the Pharmacokinetics of the Kaletra Tablet: A Longitudinal Investigation in the Second and Third Trimesters Including Empiric Dosage Adjustment [NCT00766818]Phase 112 participants (Actual)Interventional2007-01-31Completed
A Phase I, Open Label, Randomized, Three Period, One-way, Two Cohort, Adaptive Crossover Study to Evaluate the Effect of Darunavir/Ritonavir Plus Etravirine and Lopinavir/Ritonavir Plus Etravirine on GSK1349572 Pharmacokinetics in Healthy Adult Subjects ( [NCT00867152]Phase 117 participants (Actual)Interventional2009-04-30Completed
An Evaluation of the Pharmacological Interaction of Lopinavir 800mg - Ritonavir 200mg Combination and Rifampin in Subjects Presenting Tuberculosis, With Contraindication for Antiretroviral Regimens Including Efavirenz [NCT00771498]Phase 430 participants (Actual)Interventional2008-11-30Completed
Pharmacokinetics and Efficacy of Low- or Standard-dose of Lopinavir/Ritonavir (Kaletra®) in PI-naïve HIV-1 Infected Children [NCT00887120]Phase 224 participants (Actual)Interventional2007-04-30Completed
Low Doses of Lung Radiation Therapy in Cases of COVID-19 Pneumonia: Prospective Multicentric Study in Radiation Oncology Centers [NCT04394182]15 participants (Anticipated)Interventional2020-04-21Suspended(stopped due to lack of recruitment)
A Phase I Study of Intra-anally Administered Lopinavir/Ritonavir in People Living With HIV (PLWH) With High-Grade Anal Intraepithelial Neoplasia (AIN 2/3) [NCT05334004]Phase 121 participants (Anticipated)Interventional2024-01-31Recruiting
Treatment Outcomes and Plasma Level of Ritonavir-boosted Lopinavir Monotherapy Among HIV-infected Patients Who Had Non-nucleoside Reverse Transcriptase Inhibitor (NRTI) and NNRTI Failure: A Pilot Study [NCT01002898]Phase 340 participants (Actual)Interventional2007-04-30Completed
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.)
Multicenter, International, Prospective, Phase III, Randomized, Superiority Trial Comparing Two Maintenance Strategies With Mono or Bi-therapy of Protease Inhibitors With or Without Lamivudine in Virologically Suppressed HIV Patients on Second Line Antire [NCT01905059]Phase 3265 participants (Actual)Interventional2014-02-28Completed
A Phase II Exploratory Study Examining Immunologic and Virologic Indices in Two Age-Differentiated Cohorts of HIV-Infected Subjects to Explore the Basis of Accelerated HIV-Disease Progression Associated With Aging [NCT00006144]Phase 290 participants Interventional2000-10-31Completed
An Open-Label Study of a Once Daily Dose of Emtricitabine in Combination With Other Antiretroviral Agents in HIV-Infected Pediatric Patients [NCT00017992]Phase 2100 participants InterventionalRecruiting
A Phase III, Randomized, Controlled, Open-Label, Multicentre, Three Arm Study to Compare the Efficacy and Safety of a Dual-Boosted HIV-1 Protease Inhibitor Regimen of Fosamprenavir/Lopinavir/Ritonavir 1400mg/533mg/133mg Twice Daily and an Increased Dosage [NCT00144833]Phase 3150 participants (Anticipated)Interventional2005-03-31Terminated(stopped due to Incomplete data)
Pilot Simplification Study to Lopinavir/Ritonavir 800/200 mg Monotherapy Regimen Once Daily [NCT01581853]Phase 421 participants (Actual)Interventional2012-05-31Completed
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
A Phase 3, Randomized, Open-label, Study of Lopinavir/Ritonavir Tablets Versus Soft Gel Capsules and Once Daily Versus Twice Daily Administration, When Coadministered With NRTIs in Antiretroviral Naive HIV-1 Infected Subjects [NCT00262522]Phase 3664 participants (Actual)Interventional2005-11-30Completed
A Pilot Study of Lopinavir/Ritonavir in Participants Experiencing Virologic Relapse on NNRTI-Containing Regimens [NCT00357552]123 participants (Actual)Interventional2008-01-31Completed
Optimizing Antiretroviral Therapy in HIV-Infected Children and Adolescents [NCT00207948]4 participants (Actual)Observational2004-11-30Terminated(stopped due to no measurable response was detected at the 50% increase threshold.)
Lopinavir/r Plus Saquinavir Salvage Therapy in HIV-infected Children With NRTI and/or NNRTI Failure: PK and Two-year Treatment Follow up [NCT00476359]Phase 450 participants (Actual)Interventional2003-10-31Completed
An Open-Label, Sequential, 3-Period Study to Evaluate Pharmacokinetics of Coadministered Raltegravir (Isentress) and Lopinavir-Ritonavir (Kaletra) in Healthy Adults [NCT00564772]Phase 415 participants (Actual)Interventional2007-11-30Completed
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
Evaluation of Clinical Response and Safety in HIV Positive Subjects Co-infected With Hepatitis C Treated With a Kaletra Containing HAART Regimen [NCT00234975]Phase 486 participants (Actual)Interventional2002-10-31Completed
A Phase II/III Trial of Lopinavir/Ritonavir Dosed According to the WHO Pediatric Weight Band Dosing Guidelines [NCT01172535]Phase 2/Phase 397 participants (Actual)Interventional2010-11-30Completed
Randomized, Double-blinded, Controlled Trial of Intensive HAART Including Raltegravir, and Maraviroc, on HIV-1 Pro-viral DNA and Reservoir Decay in HIV-1-infected Individuals During the Acute/Early Infection [NCT01154673]Phase 2/Phase 332 participants (Actual)Interventional2011-11-30Completed
Long-term Effectiveness and Safety in Hepatitis-co-infected Patients [NCT01153269]33 participants (Actual)Observational2001-05-31Completed
Treatment Options for Protease Inhibitor-exposed Children [NCT01146873]Phase 3300 participants (Actual)Interventional2010-07-31Completed
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
Evaluation of Kaletra Therapy Over the Long-term [NCT01083810]284 participants (Actual)Observational2001-06-30Completed
A Multi-centre, Double-blinded, Randomized, Placebo-controlled Trial on the Efficacy and Safety of Lopinavir / Ritonavir Plus Ribavirin in the Treatment of Severe Acute Respiratory Syndrome [NCT00578825]340 participants (Anticipated)InterventionalNot yet recruiting
Study on the Impact of Triptolide Woldifiion on HIV-1 Reservoir of Chinese HIV/AIDS Patients In Acute HIV-1 Infection [NCT02219672]Phase 318 participants (Anticipated)Interventional2014-07-31Recruiting
Clinical, Virological and Safety Outcomes of a Lopinavir/Ritonavir-Based Regimen in HIV-1 Infected Patients in Routine Clinical Use in China: A Multicenter Post-Marketing Observational Study [NCT01074931]98 participants (Actual)Observational2008-04-30Completed
Effect of HIV-1 Protease Inhibitors on Endothelial Function and Glucose Metabolism in Normal, HIV-Uninfected Subjects: Atazanavir or Lopinavir/Ritonavir or Placebo [NCT00720590]30 participants (Actual)Interventional2003-11-30Completed
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)
Therapeutic Drug Monitoring of the Generic Lopinavir/Ritonavir Tablets 200/50 mg in the Thai HIV-infected Patient [NCT00802334]Phase 270 participants (Actual)Interventional2008-01-31Completed
A Phase I, Open-label, Single Sequence, Crossover Study Evaluating the Safety and the Pharmacokinetics of Lopinavir/Ritonavir and Eltrombopag Given Alone and When Co-administered in Healthy Adult Subjects. [NCT00833378]Phase 140 participants (Actual)Interventional2009-01-19Completed
Pharmacokinetics of the Tablet Formulation of Lopinavir/r as Standard and Increased Dosage During Pregnancy in HIV-infected Women [NCT00605098]Phase 460 participants (Actual)Interventional2008-02-29Completed
The Pharmacokinetics and Safety of Generic Lopinavir/Ritonavir (200/50 mg Tablets) 400/100 mg q12h in Thai HIV-infected Pregnant Women [NCT00621166]Phase 220 participants (Actual)Interventional2008-06-30Completed
Special Investigation of Kaletra in Pregnant Women [NCT01076985]24 participants (Actual)Observational2000-12-31Completed
MERS-CoV Infection tReated With A Combination of Lopinavir /Ritonavir and Interferon Beta-1b: a Multicenter, Placebo-controlled, Double-blind Randomized Trial [NCT02845843]Phase 2/Phase 395 participants (Actual)Interventional2016-07-31Completed
Breastfeeding Version of the PROMISE Study (Promoting Maternal and Infant Survival Everywhere) [NCT01061151]Phase 33,747 participants (Actual)Interventional2011-03-01Completed
A Phase IV Study of Antiretroviral Therapy for HIV Infected Adults Presenting With Acute Opportunistic Infections: Immediate Versus Deferred Initiation of Antiretroviral Therapy [NCT00055120]Phase 4283 participants (Actual)Interventional2003-03-31Completed
A 3 Arm, Prospective Study to Compare the Effect of 6 Weeks Exposure to the Combination of Lopinavir (LPVr)/Combivir® (AZT/3TC) Versus Lopinavir Alone or Combivir® Alone in HIV-negative Healthy Subjects on the Development of Abnormalities of Lipid and Glu [NCT00192621]Phase 450 participants (Actual)Interventional2004-11-30Completed
A Phase I/II Safety, Tolerability, and Pharmacokinetic Study of High Dose Lopinavir/Ritonavir With or Without Saquinavir in HIV-Infected Pediatric Subjects Previously Treated With Protease Inhibitors [NCT00084058]Phase 1/Phase 226 participants (Actual)InterventionalCompleted
A Phase III Randomized Trial of the Safety and Antiretroviral Effects of Zidovudine/Lamivudine/Abacavir Versus Zidovudine/Lamivudine/Lopinavir/Ritonavir in the Prevention of Perinatal Transmission of HIV [NCT00086359]Phase 319 participants (Actual)Interventional2004-07-31Completed
Evaluation of the Use of Antiretroviral Regimens Containing Raltegravir for Prophylaxis of Mother-to-child-transmission of HIV Infection in Pregnant Women Presenting With Detectable Viral Load After 32 Weeks of Gestation: a Pilot Study [NCT01854762]Phase 2/Phase 340 participants (Anticipated)Interventional2015-03-31Recruiting
Drug-Drug Interaction Study to Assess the Effects of Steady-State Lopinavir/Ritonavir on Pitavastatin in Healthy Adult Volunteers [NCT01057433]Phase 424 participants (Actual)Interventional2010-01-31Completed
A 24-week, Randomized, Open-label, 2-arm Study to Compare the Safety, Efficacy and Tolerability of Invirase® Tablets With Ritonavir Versus Kaletra® Tablets in HIV 1 Infected Adults on a Kaletra® Based Regimen With 2 Nucleosides/Nucleotides [NCT00438152]Phase 453 participants (Actual)Interventional2006-09-30Completed
[NCT00525239]60 participants (Anticipated)Interventional2004-03-31Recruiting
HIV- Monotherapy in Switzerland (MOST- ch) [NCT00531986]Phase 460 participants (Actual)Interventional2007-01-31Terminated(stopped due to Unexpectedely high rates of treatment-failure)
Baricitinib Combined With Antiviral Therapy in Symptomatic Patients Infected by COVID-19: an Open-label, Pilot Study [NCT04320277]Phase 2/Phase 3200 participants (Anticipated)Interventional2020-05-16Not yet recruiting
Monotherapy in Africa: Evaluation of New Therapy [NCT02155101]Phase 3120 participants (Actual)Interventional2014-05-31Completed
Comprehensive in Vitro Proarrhythmia Assay (CiPA) Clinical Phase 1 ECG Biomarker Validation Study (CiPA Phase 1 ECG Biomarker Study) [NCT03070470]Phase 160 participants (Actual)Interventional2017-03-14Completed
Phase I/II Study of ABT-378/Ritonavir in Combination With Reverse Transcriptase Inhibitors in Antiretroviral Naive HIV-Infected Patients [NCT00004578]Phase 1/Phase 2100 participants (Actual)Interventional1997-11-30Completed
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
A Phase III, Open Label, Randomized, Comparative Study of the Antiviral Efficacy of ARV Therapy With Lopinavir/Ritonavir (LPV/r-Kaletra) in Combination With Tenofovir (TDF) Versus Standard of Care (Kaletra in Combination With 2 Nucleoside RTIs) in naïve-H [NCT00234910]Phase 3152 participants (Actual)Interventional2005-01-31Completed
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
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, 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
MEDICLAS Study (Metabolic Effects of Different Classes of AntiretroviralS) [NCT00122226]Phase 450 participants Interventional2003-01-31Active, not recruiting
A Pharmacokinetic Study of Super-boosted Lopinavir/Ritonavir in Combination With Rifampin in HIV-1-infected Patients With Tuberculosis. [NCT01700790]Phase 49 participants (Actual)Interventional2016-02-29Terminated(stopped due to No Further Funding)
Very Early Intensive Treatment of HIV-Infected Infants to Achieve HIV Remission: A Phase I/II Proof of Concept Study [NCT02140255]Phase 1/Phase 2905 participants (Anticipated)Interventional2015-01-23Recruiting
The Pharmacokinetics of Lopinavir/Ritonavir in Combination With Atazanavir in HIV-Infected Subjects [NCT00420355]Phase 419 participants (Actual)Interventional2007-04-30Terminated(stopped due to Unexpected adverse event)
Randomised, Prospective Multicentre Clinical Study on the Effect of the Combination of Lopinavir/Rtv + Nevirapine as Maintenance Bitherapy (Without Nucleoside Analogues) in Comparison With a Triple Therapy Including Lopinavir/Rtv + Nucleoside Analogues in [NCT00335686]Phase 467 participants (Actual)Interventional2003-10-31Completed
A Randomized Clinical Trial Assessing Continuous HAART Versus Interrupted HAART in a Resource Poor Clinic [NCT00100646]30 participants (Actual)Interventional2007-03-31Completed
A Phase II, Randomized, Open-Label Study to Evaluate the Safety and Effectiveness of Two Antiretroviral Therapeutic Strategies: A Dual PI-Based HAART Regimen Versus a Multi-NRTI ART Regimen, in ART-Experienced Children and Youth Who Have Experienced Virol [NCT00102206]Phase 26 participants (Actual)InterventionalCompleted
Sex Differences in Lopinavir/Ritonavir Pharmacokinetics Among HIV-1-Infected Men and Women [NCT00102986]116 participants (Actual)Interventional2005-10-31Completed
Phase III-IV, Comparative, Randomized, Open-Label, Study to Evaluate Safety and Efficacy of Suspending Nucleosides From a Triple-Drug Therapy Based on Lopinavir/Ritonavir Versus Continuing Triple-Drug Therapy in HIV-Infected Subjects With Undetectable Pla [NCT00114933]Phase 4200 participants Interventional2005-01-31Completed
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 48-Weeks National Multicenter Randomized Open Clinical Trial Evaluating Tolerance and Efficacy of a Treatment Simplification by Lopinavir/Ritonavir Versus Continuation of Current Treatment in HIV-Infected Patients With a Viral Load Inferior to 50 Copies [NCT00140751]Phase 3186 participants (Actual)Interventional2005-10-31Completed
Evaluation of Efficacy of Pharmacotherapy Treatment of COVID- 19 Infection Using Oral Levamisole and Formoterol+Budesonide Inhaler and Comparison of This Treatment Protocol With Standard National Treatment of the Disease [NCT04331470]Phase 2/Phase 330 participants (Anticipated)Interventional2020-04-04Recruiting
Effect of HIV Protease Inhibitor Drugs on Glucose and Insulin Metabolism [NCT00135434]Phase 125 participants Interventional2004-09-30Completed
Randomized, Single Oral Dose,Two Treatment,Four-period,Full-replicated,Cross-over Trial to Assess the BE of Orvical 200 mg/50 mg FT in Comparison With Kaletra 200 mg/50 mg FT in Healthy Male Subjects Under Fasting Conditions [NCT04386876]Phase 130 participants (Actual)Interventional2020-04-30Completed
The Regimen of Favipiravir Plus Hydroxychloroquine Can Accelerate Recovery of the COVID-19 Patients With Moderate Severity in Comparison to Lopinavir/Ritonavir Plus Hydroxychloroquine Regimen: an Open-label, Non-randomized Clinical Trial Study [NCT04376814]40 participants (Actual)Interventional2020-03-29Completed
A Randomized Trial of Efficacy and Safety of an Early OUTpatient Treatment of COVID-19 in Patients With Risk Factor for Poor Outcome: a Strategy to Prevent Hospitalization [NCT04365582]Phase 30 participants (Actual)Interventional2020-05-07Withdrawn(stopped due to The PI decided.)
Efficacy of Pragmatic Same-day Ring COVID-19 Prophylaxis for Adult Individuals Exposed to SARS-CoV-2 in Switzerland: an Open-label Cluster Randomized Trial [NCT04364022]Phase 3326 participants (Actual)Interventional2020-04-23Completed
Efficacy and Safety of Umifenovir as an Adjuvant Therapy Compared to the Control Therapeutic Regiment of Interferon Beta 1a, Lopinavir / Ritonavir and a Single Dose of Hydroxychloroquine in Moderate to Severe COVID-19: A Randomized, Double-Blind, Placebo- [NCT04350684]Phase 440 participants (Anticipated)Interventional2020-04-15Enrolling by invitation
A Multi-Center Comparison of Raltegravir to Lopinavir/Ritonavir, Both in Combination With Truvada, in HIV-Infected Individuals Naive to Antiretroviral Therapy [NCT00632970]Phase 46 participants (Actual)Interventional2008-02-29Terminated(stopped due to no patients completed)
A Proof of Concept Study for GSK2248761 (An Extension of NV-05A-002: A Phase I/IIa Double-Blind Study to Evaluate the Safety and Tolerability, Antiretroviral Activity, Pharmacokinetics and Pharmacodynamics of IDX12899 in Antiretroviral Treatment-Naive HIV [NCT00945282]Phase 28 participants (Actual)Interventional2009-10-20Completed
Bone and Body Comp: A Sub Study of the SECOND-LINE Study [NCT01513122]Phase 4210 participants (Actual)Interventional2010-02-28Completed
HIV Infection and Breastfeeding: Interventions for Maternal and Infant Health [NCT00164736]Phase 32,369 participants (Actual)Interventional2004-03-31Completed
"Study ACA-ARGE-04-001 A Pilot, Open-Label Study Assessing Safety, Tolerability, Efficacy of a Simplified Lopinavir/Ritonavir Induction/Maintenance Therapy in HIV-Infected Subjects on Their First Protease Inhibitor-Based Regimen." [NCT00159224]Phase 4100 participants (Actual)Interventional2005-04-30Completed
The Efficacy and Safety of Carrimycin Treatment in Patients With Novel Coronavirus Infectious Disease (COVID-19) : A Multicenter, Randomized, Open-controlled Study [NCT04286503]Phase 4520 participants (Anticipated)Interventional2020-02-23Not yet recruiting
A Randomized, Open-label, Controlled Study of the Efficacy of Lopinavir Plus Ritonavir and Arbidol for Treating With Patients With Novel Coronavirus Infection [NCT04252885]Phase 486 participants (Actual)Interventional2020-01-28Completed
An Open Label Study of the Impact on Insulin Sensitivity, Lipid Profile and Vascular Inflammation by Treatment With Lopinavir / Ritonavir (400 / 100 mg Twice Daily) or Raltegravir 400 mg Twice Daily in HIV Negative Male Volunteers. [NCT00531999]Phase 118 participants (Actual)Interventional2007-10-31Completed
Open Randomized Study Comparing Two Alternatives of Antiretroviral Therapy as Post-exposure Prophylaxis to HIV-1: TENOFOVIR+EMTRICITABINA + LOPINAVIR/RITONAVIR VS TENOFOVIR+EMTRICITABINA + MARAVIROC [NCT01533272]Phase 4240 participants (Actual)Interventional2012-02-29Completed
Pharmacokinetics of and Rate of HIV-1 RNA Decline in ARV-naive HIV-1 Infected Patients Treated With Low- or Standard-dose Saquinavir HGC (Invirase®) and Lopinavir/Ritonavir (Kaletra® [NCT00400738]Phase 248 participants (Actual)Interventional2004-03-31Completed
A Phase IIb, 96 Week, Randomized, Open-label Multicenter, Parallel Group, Repeat Dose Study to Evaluate the Safety, Tolerability, PK and Antiviral Effect of Different Doses and Regimens of GW873140 in Combination With Kaletra (Lopinavir and Ritonavir) in [NCT00102778]Phase 2175 participants Interventional2004-12-31Terminated
Prospective Trial to Evaluate How Therapeutic Drug Monitoring of Protease Inhibitors Increases Virologic Success and Tolerance of HAART (ANRS 111 COPHAR2) [NCT00122590]115 participants Interventional2002-07-31Terminated
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 Randomized, Comparative Study of Lopinavir/Ritonavir Versus GW433908 and Ritonavir Versus Lopinavir/Ritonavir and GW433908 (In Combination With Tenofovir Disoproxil Fumarate and One or Two Nucleoside Reverse Transcriptase Inhibitors) in HIV-1-Infected S [NCT00028366]56 participants InterventionalCompleted
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
A Randomized, Open-Label Study of 800 Mg Lopinavir/200 Mg Ritonavir QD in Combination With Tenofovir and Emtricitabine Vs. 400 Mg Lopinavir /100 Mg Ritonavir BID in Combination With Tenofovir and Emtricitabine in HIV-Infected Antiretroviral Naïve Subjects [NCT00043966]Phase 3200 participants Interventional2002-07-31Completed
A Phase II, Randomized, Open-Label Study Comparing Fixed-Dose Versus Concentration-Adjusted Lopinavir/Ritonavir Therapy in HIV-Infected Subjects on Salvage Therapy [NCT00046033]Phase 2118 participants InterventionalCompleted
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
A Pilot Study of a Nucleoside Analogue Reverse Transcriptase Inhibitor Sparing Regimen in Antiretroviral-Naïve, HIV-infected Patients [NCT00143689]Phase 413 participants (Actual)Interventional2002-04-30Completed
A Phase II Study of the Predictive Value of Pharmacokinetic-Adjusted Phenotypic Susceptibility (C12h/IC50) on Antiretroviral Response to Ritonavir-Enhanced Protease Inhibitors in Subjects With Failure of Previous Protease Inhibitor-Based Regimens [NCT00027339]Phase 253 participants (Actual)InterventionalCompleted
A Restrictively Randomized, Open-Label, Controlled, Pilot Study of the Effect of a Thymidine Analogue Substitution or Change to a Nucleoside-Sparing Regimen on Peripheral Fat Wasting [NCT00028314]150 participants Interventional2002-03-31Completed
Immunologic Consequences of Antiretroviral Therapy Intensification in Subjects With Moderately Advanced HIV-1 Disease: A Follow-Up Study to ACTG 315/375 [NCT00034086]22 participants InterventionalCompleted
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
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
A Phase III, Randomized, Multicenter, Parallel Group, Open-Label, Three Arm Study to Compare the Efficacy and Safety of Two Dosing Regimens of GW433908/Ritonavir (700mg/100mg Twice Daily or 1400mg/200mg Once Daily) Versus Lopinavir/Ritonavir (400mg/100mg [NCT00025727]Phase 3330 participants Interventional2001-05-31Active, not recruiting
A Randomized, Phase II, Open Label Study to Compare Twice Daily and Once Daily Potent Antiretroviral Therapy and to Compare Self-Administered Therapy and Therapy Administered Under Direct Observation [NCT00036452]Phase 2402 participants (Actual)InterventionalCompleted
A Randomized, Open-Label, Phase III Study of ABT-378/Ritonavir in Combination With Nevirapine and Two Nucleoside Reverse Transcriptase Inhibitors (NRTIs) vs. Investigator Selected Protease Inhibitor(s) in Combination With Nevirapine and Two NRTIs in Antir [NCT00004581]Phase 3300 participants InterventionalCompleted
A Phase I/II Study of Lopinavir/Ritonavir in HIV-1 Infected Infants Less Than 6 Months of Age [NCT00038480]Phase 131 participants (Actual)InterventionalCompleted
A Study of Two Different Doses of ABT-378/Ritonavir in HIV-Infected Patients Who Have Taken Protease Inhibitors and Non-Nucleoside Reverse Transcriptase Inhibitors [NCT00038636]Phase 336 participants Interventional2000-09-30Completed
A Phase II Pharmacokinetic Study of the Transdermal Contraceptive System and Oral Contraceptive in HIV-1 Infected Women on Lopinavir/Ritonavir [NCT00125983]Phase 232 participants (Actual)InterventionalCompleted
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
A Phase II Study of Lopinavir/Ritonavir in Combination With Saquinavir Mesylate or Lamivudine/Zidovudine to Explore Metabolic Toxicities in Antiretroviral HIV-Infected Subjects [NCT00043953]Phase 230 participants (Actual)Interventional2002-08-31Completed
Study on the Feasibility of Antiretroviral Therapy With a Single Agent - Lopinavir/r - in Patients Treated With HAART and With Viral Load Below 80 Copies/Ml [NCT00160849]Phase 460 participants Interventional2004-08-31Completed
Boosted PI VS. NNRTI Based Therapy as Initial Treatment for HIV-1 Infected Patients With Advanced Disease [NCT00162643]Phase 4300 participants Interventional2004-12-31Recruiting
Maternal and Infant Peripartum Nevirapine, Versus Infant Only Peripartum Nevirapine, or Maternal Lopinavir/Ritonavir in Addition to Standard Zidovudine Prophylaxis for the Prevention of Perinatal HIV in Thailand. [NCT00409591]Phase 3435 participants (Actual)Interventional2008-07-31Terminated(stopped due to Change in National PMTCT guidelines in Thailand)
Latency and Early Neonatal Provision of Antiretroviral Drugs Clinical Trial [NCT02431975]Phase 473 participants (Actual)Interventional2015-08-31Completed
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
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.)
Pharmacokinetic Interactions Between Buprenorphine and Kaletra (Lopinavir/Ritonavir) [NCT00571961]12 participants (Actual)Interventional2007-01-31Completed
An Open-label Randomized Controlled Trial on Lopinavir/ Ritonavir, Ribavirin and Interferon Beta 1b Combination Versus Lopinavir/ Ritonavir Alone, as Treatment for 2019 Novel Coronavirus Infection [NCT04276688]Phase 2127 participants (Actual)Interventional2020-02-10Completed
Pharmacokinetic Properties of Antiretroviral and Anti-Tuberculosis Drugs During Pregnancy and Postpartum [NCT04518228]325 participants (Anticipated)Observational2021-06-08Recruiting
Pharmacokinetic Interactions Between Antiretroviral Agents, Lopinavir/Ritonavir and Efavirenz and Antimalarial Drug Combination, Artemether/Lumefantrine [NCT00266058]Phase 133 participants (Actual)Interventional2005-12-31Completed
A Pilot, Open-Label, Randomized, Comparative Study of the Antiviral Efficacy of Lopinavir/Ritonavir Single-Drug Regimen Versus Lopinavir/Ritonavir in Combination With Lamivudine/Zidovudine in Antiretroviral Naïve Patients [NCT00234923]Phase 3138 participants (Actual)Interventional2003-08-31Completed
Factors Associated With Adherence in a Cohort of HIV Positive Subjects on a First Time PI Containing HAART Regimen: Observational Study of the Impact of Adherence on Viral Load for a HAART Regimen Containing Kaletra vs Other Selected PI Containing HAART. [NCT00234962]Phase 4200 participants Interventional2002-08-31Terminated
Prevention of HIV1 Mother to Child Transmission Without Nucleoside Analogue Reverse Transcriptase Inhibitors in the Pre-partum Phase. A Multicenter Randomised Phase II/III Open Label Study With a Group of 100 Pregnant Women Receiving Lopinavir/Ritonavir a [NCT00424814]Phase 2/Phase 3105 participants (Actual)Interventional2007-03-31Completed
A Phase IV, Randomized, Open-label Study of the Tolerability of Once Daily Lopinavir/Ritonavir (LPV/r) Liquid Versus Capsules [NCT00281606]Phase 465 participants (Actual)Interventional2006-02-14Completed
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
Low Dose Anti-inflammatory Radiotherapy for the Treatment of Pneumonia by COVID-19: Multi-central Prospective Study [NCT04380818]106 participants (Anticipated)Interventional2020-06-05Recruiting
Maraviroc Switch Central Nervous System (CNS) Substudy: a Substudy of MARCH, a Randomised, Open-label Study to Evaluate the Efficacy and Safety of Maraviroc (MVC) as a Switch for Either Nucleoside or Nucleotide Analogue Reverse Transcriptase Inhibitors (N [NCT01637233]28 participants (Actual)Observational2012-06-30Completed
Maraviroc Switch Collaborative Study Renal Substudy [NCT01637259]Phase 476 participants (Actual)Interventional2012-06-30Completed
Optimal Dosing of 1st Line Antituberculosis and Antiretroviral Drugs in Children (a Pharmacokinetic Study) [NCT01637558]Phase 4200 participants (Actual)Interventional2012-11-30Completed
A Phase 1, Open-Label, Parallel Study to Evaluate the Effect of Multiple Doses of Isavuconazole on the Pharmacokinetics of Multiple Doses of Lopinavir/Ritonavir and the Effects of Lopinavir/Ritonavir on the Pharmacokinetics of Multiple Doses of Isavuconaz [NCT01660477]Phase 168 participants (Actual)Interventional2012-06-30Completed
Nevirapine vs Ritonavir-boosted Lopinavir in ART HIV-infected Adults in a Resource-limited Setting; a Randomized, Multicenter, Parallel Group Study [NCT01772940]Phase 4425 participants (Actual)Interventional2008-12-31Completed
A Multicenter, Randomized, Active Controlled, Open Label, Platform Trial on the Efficacy and Safety of Experimental Therapeutics for Patients With COVID-19 (Caused by Infection With Severe Acute Respiratory Syndrome Coronavirus-2) [NCT04351724]Phase 2/Phase 3500 participants (Anticipated)Interventional2020-04-16Recruiting
An Investigation Into Beneficial Effects of Interferon Beta 1a, Compared to The Base Therapeutic Regiment in Moderate to Severe COVID-19: A Randomized, Double-Blind, Placebo-Controlled, Clinical Trial [NCT04350671]Phase 440 participants (Anticipated)Interventional2020-04-15Enrolling by invitation
A Pilot Study of the Pharmacokinetics and Safety of Rifabutin 150 mg Once Daily Versus Rifabutin 300 mg Thrice Weekly With Lopinavir/Ritonavir Based HAART in HIV/TB Co-infected Patients [NCT02415985]Phase 240 participants (Actual)Interventional2015-06-30Completed
A Study on ART Naïve Patients On Different Regimens to Treat Hiv (a Phase 4 Study) [NCT01445223]Phase 4242 participants (Actual)Interventional2004-04-30Completed
Pharmacokinetics of Plasma Lopinavir/Ritonavir Over a 12 Hour Dosing Interval Following Administration of 400/100, 200/150, and 200/50 mg Twice Daily to HIV-negative Healthy Volunteers [NCT00985543]Phase 122 participants (Actual)Interventional2009-10-31Completed
Real-Life Effectiveness of the Kaletra Adherence Support Assistance (KASA) Program: A Prospective Observational Cohort Study (KASA PMOS) [NCT01662336]173 participants (Actual)Observational2012-06-30Completed
A Phase II Study of ABT-378/Ritonavir and Efavirenz in Multiple Protease Inhibitor-Experienced Subjects [NCT00004582]Phase 20 participants InterventionalCompleted
Comparative Therapeutic Efficacy and Safety of Remdesivir Plus Lopinavir/ Ritonavir and Tocilizumab Versus Hydroxychloroquine Plus Ivermectin and Tocilizumab in COVID-19 Patients. [NCT04779047]Phase 4150 participants (Anticipated)Interventional2020-10-01Recruiting
Efficacy of Novel Agents for Treatment of SARS-CoV-2 Infection Among High-Risk Outpatient Adults: An Adaptive Randomized Platform Trial [NCT04354428]Phase 2/Phase 3289 participants (Actual)Interventional2020-04-16Terminated(stopped due to Low number of events contributing to primary outcome)
A Randomized Phase II Study of the Safety, Immunologic, and Virologic Effects of Cyclosporine A in Conjunction With Trizivir(R) and Kaletra(R) Versus Trizivir(R) and Kaletra(R) Alone During Primary HIV-1 Infection [NCT00084149]Phase 254 participants (Actual)Interventional2004-02-29Completed
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
Open Randomized Study Comparing Two Alternatives of Antiretroviral Therapy as Post-exposure Prophylaxis to HIV-1: Tenofovir + Emtricitabine + Lopinavir/Ritonavir Versus Tenofovir + Emtricitabine + Raltegravir [NCT01576731]Phase 4240 participants (Actual)Interventional2012-07-31Completed
Randomized Controlled Pilot Study of Highly Active Anti-Retroviral Therapy for Patients With Primary Biliary Cirrhosis [NCT01614405]13 participants (Actual)Interventional2012-06-30Completed
Safety and Efficacy of Intravenous Infusion of Wharton's Jelly Derived Mesenchymal Stem Cell Plus Standard Therapy for the Treatment of Patients With Acute Respiratory Distress Syndrome Diagnosis Due to COVID 19: A Randomized Controlled Trial [NCT04390152]Phase 1/Phase 240 participants (Anticipated)Interventional2020-01-13Recruiting
An Open Label, Randomized, Parallel-group Pharmacokinetics Trial of Tipranavir / Ritonavir (TPV/RTV), Alone or in Combination With RTV-boosted Saquinavir (SQV), Amprenavir (APV), or Lopinavir (LPV), Plus an Optimized Background Regimen, in Multiple Antire [NCT00056641]Phase 2328 participants Interventional2003-02-18Completed
Phase I/II Study of ABT-378/Ritonavir in Protease Inhibitor Experienced HIV-Infected Patients [NCT00004580]Phase 10 participants InterventionalCompleted
A Randomized, Open-Label, Pilot Treatment Trial Evaluating Cellular Dynamics and Immune Restoration in Treatment-Naive HIV-Infected Subjects Receiving Either the Protease Inhibitor LPV/r or the Nucleoside Analogue Reverse Transcriptase Inhibitors d4T/3TC/ [NCT00004855]55 participants InterventionalCompleted
Chemoprophylaxis of SARS-CoV-2 Infection (COVID-19) in Exposed Healthcare Workers : A Randomized Double-blind Placebo-controlled Clinical Trial [NCT04328285]Phase 3118 participants (Actual)Interventional2020-04-14Terminated(stopped due to French authority's decision)
An Investigation Into Beneficial Effects of Interferon Beta 1a, Compared to Interferon Beta 1b And The Base Therapeutic Regiment in Moderate to Severe COVID-19: A Randomized Clinical Trial [NCT04343768]Phase 260 participants (Actual)Interventional2020-04-09Completed
Comparative Therapeutic Efficacy and Safety of Remdesivir Versus Lopinavir/ Ritonavir and Remdesivir Combination in COVID-19 Patients [NCT04738045]Phase 490 participants (Anticipated)Interventional2020-11-01Recruiting
A Phase 1 Clinical Study to Assess the Effect of Darunavir/Ritonavir or Lopinavir/Ritonavir on the Pharmacokinetics of Daclatasvir in Healthy Subjects [NCT02159352]Phase 149 participants (Actual)Interventional2014-06-30Completed
Evaluation of Additional Treatments for COVID-19: a Randomized Trial in Niger [NCT04409483]Phase 30 participants (Actual)Interventional2020-06-01Withdrawn(stopped due to Epidemic dynamics)
The Influence of Lopinavir/Ritonavir on Gemfibrozil Pharmacokinetics in Healthy Volunteers [NCT00474201]15 participants (Actual)Interventional2007-05-31Completed
Neuropsychiatric Adverse Effects of Efavirenz in Children Living With HIV in Kilimanjaro, Tanzania [NCT03227653]144 participants (Actual)Observational2017-06-19Completed
Switching From Regimens Consisting of a RTV-Boosted Protease Inhibitor Plus TDF/FTC to a Combination of Raltegravir Plus Nevirapine and Lamivudine in HIV Patients With Suppressed Viremia and Impaired Renal Function (RANIA Study) (Pilot Study) Protocol MK- [NCT02116660]Phase 211 participants (Actual)Interventional2014-09-03Terminated(stopped due to This study was terminated early due to poor recruitment.)
Pharmacokinetics Study of Tenofovir in HIV-infected Thai Children Using Tenofovir-based Regimen [NCT02404259]32 participants (Actual)Interventional2010-06-30Completed
A Pharmacokinetics Study Comparing Lopinavir Plasma Exposure When Given as Lopinavir/Ritonavir (1:1) in the Presence of Rifampicin and Lopinavir/Ritonavir (4:1) Without Rifampicin in HIV and TB Co-infected Children in South Africa. [NCT02348177]Phase 496 participants (Actual)Interventional2013-01-31Completed
Efficacy and Safety of Albuvirtide for Injection Combined With LPV/r for Treatment of HIV-1-Infected Patients Failed First-line Antiretroviral Therapy [NCT02369965]Phase 3418 participants (Actual)Interventional2014-02-19Completed
HIV Postexposure Prophylaxis With Darunavir/r (PEPDar) [NCT01516970]Phase 3312 participants (Actual)Interventional2011-11-25Completed
A Pilot Study to Assess Virologic Suppression and Immune Recovery With Raltegravir and Lopinavir/Ritonavir and Raltegravir and Emtricitabine/Tenofovir in HIV-1 Infected Treatment-naïve Subjects [NCT00654147]Phase 244 participants (Actual)Interventional2008-04-30Completed
Lopinavir/Ritonavir/Combivir vs. Abacavir/Zidovudine/Lamivudine for Virologic Efficacy and the Prevention of Mother-to-Child HIV Transmission Among Breastfeeding Women With CD4 Counts Greater Than or Equal to 200 Cells/mm3 in Botswana [NCT00270296]Phase 2730 participants (Actual)Interventional2006-06-30Completed
Drug Use Investigation of Kaletra [NCT01076972]1,184 participants (Actual)Observational2000-12-31Completed
Retrospective Cohort to Evaluate the Effectiveness and Safety of Xiyanping Injection Combined With Conventional Treatment for New Coronavirus Infection Pneumonia (Common Type) [NCT04275388]426 participants (Anticipated)Observational2020-05-15Not yet recruiting
Immune Reconstitution as a Determinant of Adverse Effects to New Antiretroviral Therapy in Persons With Advanced HIV Infection [NCT00885664]Phase 460 participants (Actual)Interventional2005-10-31Completed
Baricitinib Therapy in COVID-19: A Pilot Study on Safety and Clinical Impact [NCT04358614]Phase 2/Phase 312 participants (Actual)Interventional2020-03-16Completed
A Pilot Project to Operationalize the Prevention Strategy of Post Exposure Prophylaxis Following Sexual Exposure to HIV in Combination With Educational Programming and Behavioral Risk Reduction Strategies in Los Angeles County [NCT00949234]Phase 2267 participants (Actual)Interventional2010-03-31Completed
"Hydroxychloroquine and Lopinavir/ Ritonavir for Hospitalization and Mortality Reduction in Patients With COVID-19 and Mild Disease Symptoms: The Hope Coalition" [NCT04403100]Phase 31,968 participants (Anticipated)Interventional2020-06-03Recruiting
A Randomized, Double-Blind, Phase III Study of ABT-378/Ritonavir Plus Stavudine and Lamivudine vs Nelfinavir Plus Stavudine and Lamivudine in Antiretroviral Naive HIV-Infected Subjects [NCT00004583]Phase 3660 participants Interventional1999-03-31Completed
An Open-Label Randomized Clinical Trial to Evaluate the Efficacy and Safety of Short Course Antiretroviral Therapy for Acute or Recent HIV-1 Infection in Zimbabwe and the United States [NCT00414518]16 participants (Actual)Interventional2007-01-31Completed
Comparison of Liquid Kaletra and Low Dose Kaletra Tablets in HIV-Positive Children [NCT00762320]8 participants (Actual)Interventional2008-10-31Completed
Antiretroviral Regime for Viral Eradication in Newborns After Intervention Failure of Mother-to-child Transmission of HIV [NCT02712801]Phase 4600 participants (Actual)Interventional2016-04-30Completed
IMPAACT 1092: Phase IV Evaluation Of The Steady State Pharmacokinetics Of Zidovudine, Lamivudine, and Lopinavir/Ritonavir in Severely Malnourished HIV-1-Infected Children [NCT01818258]Phase 452 participants (Actual)Interventional2015-10-26Completed
A Randomized, Phase 2b Study of a Double-Dose Lopinavir/Ritonavir-Based Antiretroviral Regimen With Rifampin-Based Tuberculosis Treatment Versus a Standard-Dose Lopinavir/Ritonavir-Based Antiretroviral Regimen With Rifabutin-Based Tuberculosis Treatment W [NCT01601626]Phase 271 participants (Actual)Interventional2013-07-13Terminated(stopped due to The study was stopped early due to feasibility concerns.)
A Phase IIIb, Open -Label, Randomized Multi-center Study Comparing the Antiviral Efficacy, Safety, and Effect on Serum Lipids of Atazanavir/Ritonavir Versus Lopinavir/Ritonavir, in Combination With Two Nucleoside or Nucleotide Reverse Transcriptase Inhibi [NCT00135395]Phase 3200 participants (Anticipated)Interventional2004-05-31Completed
A Randomized Open-label Study of the Antiviral Efficacy and Safety of Atazanavir Versus Lopinavir/Ritonavir(LPV/RTV), Each in Combination With Two Nucleosides in Subjects Who Have Experienced Virologic Failure With Prior Protease Inhibitor-Containing HAAR [NCT00028301]Phase 30 participants Interventional2001-02-28Completed
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
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
HIV Reservoir Dynamics After Switching to Dolutegravir in Patients With Two NRTI and a Protease Inhibitor Based Regimen. A Phase IV Open Randomized Trial [NCT02513147]Phase 444 participants (Actual)Interventional2015-06-30Completed
Favipiravir, Lopinavir/Ritonavir or Combination Therapy: a Randomised, Double Blind, 2x2 Factorial Placebo-controlled Trial of Early Antiviral Therapy in COVID-19 [NCT04499677]Phase 2240 participants (Actual)Interventional2020-09-24Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00035932 (38) [back to overview]Fridericia-corrected QT (QTcF) Interval and Change From Baseline by Analysis Time Point
NCT00035932 (38) [back to overview]Mean Score of European Quality of Life-5 Dimensions (EQ-5D) Health Index Score at Baseline, Mid-Study (Week 24), and Final (Week 48)
NCT00035932 (38) [back to overview]Mean ATV, RTV and SQV Minimum Concentration (Cmin) Values
NCT00035932 (38) [back to overview]Lipid Mean Percent Change From Baseline at Week 96, Observed Values
NCT00035932 (38) [back to overview]Lipid Mean Percent Change From Baseline at Week 48
NCT00035932 (38) [back to overview]Lipid Mean Percent Change From Baseline at Week 24
NCT00035932 (38) [back to overview]HIV RNA Level - Treated Subjects With Evaluable Cmins at Week 24
NCT00035932 (38) [back to overview]Grade 3/4 Laboratory Abnormalities Through Week 48
NCT00035932 (38) [back to overview]Participants Achieving Virologic Half Log Suppression (LOQ = 400 c/mL) at Week 96
NCT00035932 (38) [back to overview]Deaths, Serious Adverse Events (SAEs), and Adverse Events (AEs) Through Week 48
NCT00035932 (38) [back to overview]Correlation of ATV Minimum Plasma Concentration (Cmin), Inhibitory Quotient (IQ), and Number of Protease Inhibitor (PI) Mutations at Baseline With HIV RNA Change From Baseline at Week 24
NCT00035932 (38) [back to overview]Correlation of ATV Minimum Plasma Concentration (Cmin) Inhibitory Quotient (IQ), and Number of PI Mutations at Baseline and CD4 Cell Count Change From Baseline at Week 24
NCT00035932 (38) [back to overview]Adherence to Regimen Though Week 48 Based on MACS the Multicenter AIDS Cohort Study (MACS) Adherence Questionnaire
NCT00035932 (38) [back to overview]Participants Achieving Virologic Half Log Suppression (LOQ = 50 c/mL) at Week 96
NCT00035932 (38) [back to overview]Participants Achieving Virologic Half Log Suppression (LOQ = 50 c/mL) at Week 48
NCT00035932 (38) [back to overview]Participants Achieving Virologic Half Log Suppression (LOQ = 50 c/mL) at Week 24
NCT00035932 (38) [back to overview]Mean Change From Baseline in HIV Ribonucleic Acid (RNA) at Week 24
NCT00035932 (38) [back to overview]Participants Achieving Treatment Response (LOQ = 50 c/mL) Without Prior Failure at Week 96
NCT00035932 (38) [back to overview]Participants Achieving Treatment Response (LOQ = 50 c/mL) Without Prior Failure at Week 48
NCT00035932 (38) [back to overview]Participants Achieving Treatment Response (LOQ = 50 c/mL) Without Prior Failure at Week 24
NCT00035932 (38) [back to overview]Participants Achieving Treatment Response (LOQ = 400 c/mL) Without Prior Failure at Week 96
NCT00035932 (38) [back to overview]HIV IC50 at Week 24
NCT00035932 (38) [back to overview]Fasting Glucose Mean Change From Baseline at Week 48
NCT00035932 (38) [back to overview]Fasting Glucose Mean Change From Baseline at Week 24
NCT00035932 (38) [back to overview]Change From Baseline in CD4 Cell Count at Week 96
NCT00035932 (38) [back to overview]Participants Achieving Treatment Response (LOQ = 400 c/mL) Without Prior Failure at Week 48
NCT00035932 (38) [back to overview]Change From Baseline in CD4 Cell Count at Week 24
NCT00035932 (38) [back to overview]Inhibitory Quotient at Week 24
NCT00035932 (38) [back to overview]Participants Achieving Virologic Half Log Suppression (LOQ = 400 c/mL) at Week 48, (Overall and by PI Sensitivity)
NCT00035932 (38) [back to overview]Participants Achieving Virologic Half Log Suppression (Limit of Quantification [LOQ] = 400 c/mL) at Week 24 (Overall and by Protease Inhibitor [PI] Sensitivity)
NCT00035932 (38) [back to overview]Most Common AEs and AEs of Interest Through Week 48
NCT00035932 (38) [back to overview]PR Interval and Change From Baseline by Analysis Time Point
NCT00035932 (38) [back to overview]Mean Score of European Quality of Life-5 Dimensions (EQ-5D) Visual Analog Scale (VAS) at Baseline, Mid-Study (Week 24), and Final (Week 48)
NCT00035932 (38) [back to overview]Change From Baseline in CD4 Cell Count at Week 48
NCT00035932 (38) [back to overview]Participants Achieving Treatment Response (LOQ = 400 c/mL) Without Prior Failure at Week 24
NCT00035932 (38) [back to overview]Mean Change From Baseline in HIV RNA at Week 96
NCT00035932 (38) [back to overview]Mean Change From Baseline in HIV RNA at Week 48
NCT00035932 (38) [back to overview]Mean Change From Baseline in HIV RNA at Week 2
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]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of 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 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]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
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 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
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: 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: 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]PK Parameter: Trough Concentration (C24) With Median (Range) for 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]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) 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
NCT00084149 (7) [back to overview]Levels of Proviral DNA in Peripheral Blood Mononuclear Cells (PBMC) (log10)
NCT00084149 (7) [back to overview]HIV-1 Viral Load Levels
NCT00084149 (7) [back to overview]Adverse Events Related to Study Medication
NCT00084149 (7) [back to overview]CD4 T Cell Levels
NCT00084149 (7) [back to overview]Proviral DNA Levels (log10)
NCT00084149 (7) [back to overview]Proviral DNA (log10)
NCT00084149 (7) [back to overview]Number of Patients With Viral Load Less Than 50 Copies/ml
NCT00089505 (9) [back to overview]Number of Participants Who Experienced HIV-related Disease Progression or Death
NCT00089505 (9) [back to overview]Time From Randomization to Virologic Failure or Death for Participants Without SD NVP Exposure Prior to Study Entry
NCT00089505 (9) [back to overview]Number of Participants Who Experienced Treatment-related Toxicity That Led to Discontinuation of Randomized Regimen.
NCT00089505 (9) [back to overview]Number of Participants Who Experienced Virologic Failure or Died.
NCT00089505 (9) [back to overview]Number of Participants Who Received NVP-containing Regimens at Randomization and Experienced NVP-associated Rash or Grade 2+ Liver Lab Abnormality
NCT00089505 (9) [back to overview]CD4 Count Change From Randomization
NCT00089505 (9) [back to overview]Percent of Participants Who Experienced Virologic Failure or Died
NCT00089505 (9) [back to overview]Percent of Participants Who Reported to Never Missed Any of the Study Drug Regimen in the Past Month
NCT00089505 (9) [back to overview]Time From Randomization to Virologic Failure or Death for Participants Who Had SD NVP Exposure Prior to Study Entry
NCT00090779 (9) [back to overview]Ranked log10 HIV-1 RNA Viral Load (log10 Copies/mL) Averaged at Weeks 72 and 76 for the IT Arm and Ranked log10 HIV-1 RNA Viral Load (log10 Copies/mL) Averaged at Weeks 36 and 40 for the DT Arm
NCT00090779 (9) [back to overview]Change in CD4 Counts Cells/mm^3 From Week 36 for IT Arm and From Week 0 for DT Arm
NCT00090779 (9) [back to overview]Time to Meeting the Clinical, Virologic, or Immunologic Criteria for Treatment Initiation or Re-initiation
NCT00090779 (9) [back to overview]Time to Treatment Initiation or Death
NCT00090779 (9) [back to overview]Number of Participants Experiencing Either a CDC Category B or C Diagnosis, CD4<200 Cells/mm^3 or CD4 Percent <14%.
NCT00090779 (9) [back to overview]Number of Participants in IT Arm Off Treatment Before 36 Weeks
NCT00090779 (9) [back to overview]Time From Study Entry in DT Arm Participants or From Week 36 in IT Arm Participants to Meeting the Clinical, Virologic, or Immunologic Criteria for Treatment Initiation or Re-initiation
NCT00090779 (9) [back to overview]Number of Participants Meeting Clinical, Virologic, or Immunologic Criteria for Treatment Initiation or Re-initiation
NCT00090779 (9) [back to overview]Ranked Log10 HIV-1 RNA Viral Load (log10 Copies/mL) Averaged at 72 and 76 Weeks for the IT Arm and DT Arm
NCT00099632 (5) [back to overview]Number of Participants Who Discontinued Study Treatment Prematurely
NCT00099632 (5) [back to overview]Severe (Grade 3) and Higher Adverse Events and Any Grade Adverse Event That Leads to a Treatment Change From First Day of Study Treatment to Week 12
NCT00099632 (5) [back to overview]Number of Participants With New PI-resistant Variants as Detected by Standard Composite (Bulk) Genotyping.
NCT00099632 (5) [back to overview]Number of Participants With New Circulating NRTI-resistant Variants Detected by Standard Composite (Bulk) Genotyping.
NCT00099632 (5) [back to overview]Number of Participants With New Circulating Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI)-Resistant Variants as Detected by Standard Composite (Bulk) Genotyping
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]Number of Participants Who Experienced Regimen-limiting ART Drug Toxicity
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]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]Duration of Hospitalisation
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]Time From Randomization to Starting or Needing to Start Continuous Therapy
NCT00102960 (13) [back to overview]Time to Failure of First Line Therapy or Death
NCT00102960 (13) [back to overview]Time to First Hospitalization
NCT00102960 (13) [back to overview]Total Occurrence of Grade 3 or 4 Clinical Events
NCT00102960 (13) [back to overview]Total Occurrence of Grade 3 or 4 Laboratory Events
NCT00105079 (6) [back to overview]Number of Patients Who Discontinued Treatment Due to Abnormal Laboratory Parameters
NCT00105079 (6) [back to overview]Change From Baseline in Cluster Differentiation Antigen 4 Positive (CD4+) Lymphocyte Count
NCT00105079 (6) [back to overview]Change From Baseline in HIV-1 RNA Viral Load
NCT00105079 (6) [back to overview]Number of Patients With HIV-1 RNA Viral Load <50 and <400 Copies/mL
NCT00105079 (6) [back to overview]Number of Patients With Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Viral Load <50 Copies/mL
NCT00105079 (6) [back to overview]Number of Participants Assessed for Adverse Events (AEs)
NCT00109590 (12) [back to overview]The Proportion of Women Who Develop One or More New NVP Resistance Mutations as Identified by Consensus Sequencing or Oligonucleotide Ligation Assay in Plasma (Sampling Was Done at Days 10,21,30, and Weeks 5,6, and 8 Postpartum).
NCT00109590 (12) [back to overview]Area Under the Curve Pharmacokinetic Outcome for LPV/r. (AUC ug*hr/mL)
NCT00109590 (12) [back to overview]Four (4) Hour Concentration Pharmacokinetic Outcome for LPV/r (C4hour ug/mL).
NCT00109590 (12) [back to overview]Maximum Concentration Pharmacokinetic Outcome for LPV/r (Cmax ug/mL) .
NCT00109590 (12) [back to overview]Median HIV-1 Viral Load at 24 Weeks Postpartum in Women
NCT00109590 (12) [back to overview]Pre-dose Concentration Pharmacokinetic Outcome for LPV/r (Cpredose ug/mL).
NCT00109590 (12) [back to overview]Resistance Mutations in HIV Infected Infants
NCT00109590 (12) [back to overview]The Proportion of Women in Each Randomized Arm Who Have One or More New NVP Resistance Mutations as Identified by Consensus Sequencing or Oligonucleotide Ligation Assay (OLA) in Plasma
NCT00109590 (12) [back to overview]The Proportion of Women in Each Randomized Arm Who Have One or More New NVP Resistance Mutations for the Subgroup of Women With Plasma HIV RNA >= 500 Copies/ml At Entry
NCT00109590 (12) [back to overview]Proportion of Women With New NVP Resistance Mutation Within 8 Weeks Postpartum Who Had a NVP Resistance Mutation Detected at 72 Weeks Postpartum.
NCT00109590 (12) [back to overview]The Proportion of Women With Any New ZDV, ddI, or LPV/r Resistance Mutations.
NCT00109590 (12) [back to overview]Number of Women With Grade >=3 Events After Start of Study Treatment
NCT00145795 (10) [back to overview]Rates of ex Vivo T Cell Apoptosis: CD4+ Memory Cell Population [6 Months]
NCT00145795 (10) [back to overview]Rates of ex Vivo T Cell Apoptosis: CD4+ Memory Cell Population [3 Months]
NCT00145795 (10) [back to overview]Immune Reconstitution [6 Months]
NCT00145795 (10) [back to overview]Immune Reconstitution [3 Months]
NCT00145795 (10) [back to overview]Clinical HIV-related Events
NCT00145795 (10) [back to overview]Rates of ex Vivo T Cell Apoptosis: CD4+ naïve Cell Population [3 Months]
NCT00145795 (10) [back to overview]Rates of Virologic Failure
NCT00145795 (10) [back to overview]Rates of ex Vivo T Cell Apoptosis: CD8+ Cell Population [6 Months]
NCT00145795 (10) [back to overview]Rates of ex Vivo T Cell Apoptosis: CD8+ Cell Population [3 Months]
NCT00145795 (10) [back to overview]Rates of ex Vivo T Cell Apoptosis: CD4+ naïve Cell Population [6 Months]
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).
NCT00262522 (4) [back to overview]Percentage of Subjects With Plasma Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Levels < 50 Copies/mL at Week 96
NCT00262522 (4) [back to overview]Mean Change From Baseline to Week 96 in CD4+ T Cell Counts
NCT00262522 (4) [back to overview]Percentage of Subjects With Plasma Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Levels < 50 Copies/mL at Week 48
NCT00262522 (4) [back to overview]Percentage of Subjects With Adverse Events of Diarrhea During the First 8 Weeks
NCT00270296 (2) [back to overview]Number of Participants With Virologic Suppression
NCT00270296 (2) [back to overview]Number of HIV+ Infants
NCT00307151 (9) [back to overview]Percent of Participants Experiencing Virologic Failure
NCT00307151 (9) [back to overview]Percent of Participants With Treatment Failure, Defined as a Confirmed Virologic Failure or Permanent Discontinuation of the Randomized NNRTI or PI Component of Study Treatment
NCT00307151 (9) [back to overview]Time From Randomization to Death
NCT00307151 (9) [back to overview]Time From Randomization to HIV-related Disease Progression or Death
NCT00307151 (9) [back to overview]Time From Randomization to Treatment Failure, Defined as Virologic Failure or Permanent Discontinuation of the Randomized NNRTI or PI Component of Study Treatment
NCT00307151 (9) [back to overview]Time From Randomization to Virologic Failure
NCT00307151 (9) [back to overview]Time From Start of Study Treatment to First New Grade >=3 Lab Abnormality, Sign or Symptom Occurring on Study Treatment
NCT00307151 (9) [back to overview]Number of Participants Developing New NRTI, NNRTI or PI-resistant Virus
NCT00307151 (9) [back to overview]Change in CD4 Percent From Entry to Week 48
NCT00342355 (2) [back to overview]Progression to AIDS or Death in tx naïve Pts With Adv HIV dx in the Four Randomly Assigned Regimens.
NCT00342355 (2) [back to overview]Serious Adverse Events
NCT00357552 (11) [back to overview]Probability of Grade 3 or 4 Sign or Symptom, or Laboratory Toxicity Over 24 Weeks on Study.
NCT00357552 (11) [back to overview]Percentage of Subjects Reporting Not Skipping Medications in the Last Month.
NCT00357552 (11) [back to overview]Proportion of Participants With Plasma HIV-1 RNA Levels < 400 Copies/mL From Baseline to Week 104
NCT00357552 (11) [back to overview]Number of Screened Subjects With at Least One NNRTI, or NRTI-associated Resistance Mutation at A5230 Screening.
NCT00357552 (11) [back to overview]Level of HIV-1 RNA as Ascertained From Paired DBS and Plasma
NCT00357552 (11) [back to overview]Time to Treatment Failure, Defined as the First Occurrence of Death, Disease Progression, or Virologic Failure.
NCT00357552 (11) [back to overview]Time to First New Grade 3 or 4 Sign or Symptom or Laboratory Toxicity Following LPV/r Intensification
NCT00357552 (11) [back to overview]Percentage of Enrolled Participants With Virologic Success at Week 24 on LPV/r Monotherapy
NCT00357552 (11) [back to overview]Number of Subjects With at Least One New PI-associated Resistance Mutation at Time of Virologic Failure.
NCT00357552 (11) [back to overview]Number of Participants With Study-targeted Diagnoses and Clinical Events
NCT00357552 (11) [back to overview]Change in CD4+ Cell Counts From Study Entry to Week 104
NCT00358917 (5) [back to overview]Percentage of Participants With New Primary Protease Mutations at Week 48
NCT00358917 (5) [back to overview]Percentage of Participants With Plasma Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Levels < 50 Copies/Milliliter (mL) at Week 48
NCT00358917 (5) [back to overview]Virologic Response (HIV-1 RNA <50 Copies/mL) at Week 48 for Participants With 0-2 Protease Inhibitor Substitutions at Baseline Associated With Reduced Response to Lopinavir/Ritonavir
NCT00358917 (5) [back to overview]Percentage of Participants Responding at Week 48 Based on the Food and Drug Administration (FDA) Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00358917 (5) [back to overview]Mean Change From Baseline to Week 48 in Cluster of Differentiation 4 Single-Positive Thymocyte (CD4+ T) Cell Counts
NCT00413153 (9) [back to overview]Fasting Glucose
NCT00413153 (9) [back to overview]Immune Parameters -- CD4 Count
NCT00413153 (9) [back to overview]Insulin Sensitivity
NCT00413153 (9) [back to overview]Lipid Metabolism - Serum Triglyceride
NCT00413153 (9) [back to overview]Liver Enzymes -- Alanine Aminotransferase (ALT)
NCT00413153 (9) [back to overview]Liver Enzymes -- Aspartate Aminotransferase (AST)
NCT00413153 (9) [back to overview]Total Bilirubin
NCT00413153 (9) [back to overview]Body Composition - Visceral Adipose Tissue
NCT00413153 (9) [back to overview]Glucose Trafficking
NCT00414518 (3) [back to overview]Viral Set Point
NCT00414518 (3) [back to overview]Plasma HIV-1 Viral Load (Copies/ml) at Week 24 as Compared Between the Two Arms
NCT00414518 (3) [back to overview]Number of Participants Experiencing Either an AIDS-defining Event, a Grade 3 or 4 Adverse Event, or Acute Retroviral Syndrome
NCT00427297 (4) [back to overview]Incidence of Severe Adverse Events (Excluding Mortality)
NCT00427297 (4) [back to overview]Immunologic Failure
NCT00427297 (4) [back to overview]Incidence of Mortality
NCT00427297 (4) [back to overview]Viral Failure
NCT00443703 (23) [back to overview]Number of Patients With Serious LAEs Through 24 Weeks
NCT00443703 (23) [back to overview]Number of Patients With Clinical Adverse Experiences (CAEs) Through 24 Weeks
NCT00443703 (23) [back to overview]Mean Percent Change From Baseline in Fasting Serum Cholesterol at Week 12
NCT00443703 (23) [back to overview]Mean Percent Change From Baseline in Fasting Serum Cholesterol at Week 24
NCT00443703 (23) [back to overview]Mean Percent Change From Baseline in Fasting Serum High-Density Lipoprotein Cholesterol (HDL-C) at Week 12
NCT00443703 (23) [back to overview]Mean Percent Change From Baseline in Fasting Serum High-Density Lipoprotein Cholesterol (HDL-C) at Week 24
NCT00443703 (23) [back to overview]Mean Percent Change From Baseline in Fasting Serum Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT00443703 (23) [back to overview]Mean Percent Change From Baseline in Fasting Serum Low-Density Lipoprotein Cholesterol (LDL-C) at Week 24
NCT00443703 (23) [back to overview]Mean Percent Change From Baseline in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C) at Week 12
NCT00443703 (23) [back to overview]Mean Percent Change From Baseline in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24
NCT00443703 (23) [back to overview]Median Percent Change From Baseline in Serum Triglyceride at Week 12
NCT00443703 (23) [back to overview]Median Percent Change From Baseline in Serum Triglyceride at Week 24
NCT00443703 (23) [back to overview]Number of Patients With Plasma Human Immunodeficiency Virus (HIV) RiboNucleic Acid (RNA) <50 Copies/mL at Week 24
NCT00443703 (23) [back to overview]Number of Patients That Died by 24 Week Last Patient Last Visit
NCT00443703 (23) [back to overview]Number of Patients That Discontinued Due to CAEs Through 24 Weeks
NCT00443703 (23) [back to overview]Number of Patients That Discontinued Due to Drug Related CAEs Through 24 Weeks
NCT00443703 (23) [back to overview]Number of Patients That Discontinued Due to LAEs Through 24 Weeks
NCT00443703 (23) [back to overview]Number of Patients That Discontinued With Drug Related LAEs Through 24 Weeks
NCT00443703 (23) [back to overview]Number of Patients With Drug-related CAEs Through 24 Weeks
NCT00443703 (23) [back to overview]Number of Patients With Drug-related Laboratory Adverse Experiences (LAEs) Through 24 Weeks
NCT00443703 (23) [back to overview]Number of Patients With Laboratory Adverse Experiences (LAEs) Through 24 Weeks
NCT00443703 (23) [back to overview]Number of Patients With Serious CAEs Through 24 Weeks
NCT00443703 (23) [back to overview]Number of Patients With Serious Drug-related CAEs Through 24 Weeks
NCT00443729 (21) [back to overview]Mean Percent Change From Baseline in Fasting Serum Cholesterol at Week 12
NCT00443729 (21) [back to overview]Mean Percent Change From Baseline in Fasting Serum Cholesterol at Week 24
NCT00443729 (21) [back to overview]Number of Patients With Serious Drug-related CAEs Through 24 Weeks
NCT00443729 (21) [back to overview]Number of Patients With Serious CAEs Through 24 Weeks
NCT00443729 (21) [back to overview]Number of Patients With Laboratory Adverse Experiences (LAEs) Through 24 Weeks
NCT00443729 (21) [back to overview]Number of Patients With Drug-related LAEs Through 24 Weeks
NCT00443729 (21) [back to overview]Number of Patients With Drug-related CAEs Through 24 Weeks
NCT00443729 (21) [back to overview]Number of Patients With Clinical Adverse Experiences (CAEs) Through 24 Weeks
NCT00443729 (21) [back to overview]Number of Patients That Discontinued Due to LAEs Through 24 Weeks
NCT00443729 (21) [back to overview]Number of Patients That Discontinued Due to CAEs Through 24 Weeks
NCT00443729 (21) [back to overview]Number of Patients That Died by 24 Week Last Patient Last Visit
NCT00443729 (21) [back to overview]Number of Patients With Plasma Human Immunodeficiency Virus (HIV) RiboNucleic Acid (RNA) <50 Copies/mL at Week 24
NCT00443729 (21) [back to overview]Median Percent Change From Baseline in Serum Triglyceride at Week 24
NCT00443729 (21) [back to overview]Number of Patients With Serious LAEs Through 24 Weeks
NCT00443729 (21) [back to overview]Median Percent Change From Baseline in Serum Triglyceride at Week 12
NCT00443729 (21) [back to overview]Mean Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at Week 24
NCT00443729 (21) [back to overview]Mean Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at Week 12
NCT00443729 (21) [back to overview]Mean Percent Change From Baseline in Fasting Serum Low-density Lipoprotein Cholesterol (LDL-C) at Week 24
NCT00443729 (21) [back to overview]Mean Percent Change From Baseline in Fasting Serum Low-density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT00443729 (21) [back to overview]Mean Percent Change From Baseline in Fasting Serum High-density Lipoprotein Cholesterol (HDL-C) at Week 24
NCT00443729 (21) [back to overview]Mean Percent Change From Baseline in Fasting Serum High-density Lipoprotein Cholesterol (HDL-C) at Week 12
NCT00474201 (1) [back to overview]Gemfibrozil Area Under the Concentration vs. Time Curve (AUC)
NCT00571961 (1) [back to overview]Buprenorphine Area Under the Curve With LPV/r (ng/mL*hr)
NCT00608569 (8) [back to overview]CD4 Count at Follow-up Visits
NCT00608569 (8) [back to overview]Time to First Grade 3 or 4 Lab or Sign/Symptom Event
NCT00608569 (8) [back to overview]Adherence to Second Line HAART Regimen
NCT00608569 (8) [back to overview]Time to First Grade 3 or 4 Lab Event
NCT00608569 (8) [back to overview]Confirmed Virologic Failure at or Prior to Week 48
NCT00608569 (8) [back to overview]Confirmed Virologic Failure at or Prior to Week 24
NCT00608569 (8) [back to overview]CD8 Count at Follow-up Visits
NCT00608569 (8) [back to overview]Time to First Grade 3 or 4 Sign or Symptom
NCT00632970 (1) [back to overview]Absolute Change in CD4 Cell Counts
NCT00654147 (6) [back to overview]Study Medication Toxicity-related Discontinuation .
NCT00654147 (6) [back to overview]Time to Confirmed Virologic Failure
NCT00654147 (6) [back to overview]Time to Virologic Failure
NCT00654147 (6) [back to overview]Study Medication Tolerability
NCT00654147 (6) [back to overview]Change From Baseline CD4+ and CD8+ Cell Counts
NCT00654147 (6) [back to overview]Weeks to HIV-1 RNA <200 Copies/ml
NCT00700115 (2) [back to overview]To Compare Plasma Triglyceride Levels at 48 Weeks Between LPV/r + RAL and Standard HAART Treated Subjects
NCT00700115 (2) [back to overview]Plasma Viral Loads (HIV-1 RNA PCR)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Alkaline Phosphatase (Units/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Aspartate Aminotransferase (Units/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Basophils (x 10^9/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Bicarbonate (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Blood Urea Nitrogen (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Calcium (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Calculated Creatinine Clearance (Milliliters/Second)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Chest Measurement (cm)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Chloride (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Cholesterol (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Creatine Phosphokinase (Units/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Creatinine (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in DEXA Scan of Lower Extremity Lean Mass (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Bone Mineral Content (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Bone Mineral Density (Grams/cm^2)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Lower Extremity Fat (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Lower Extremity Total Mass (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Total Body Fat (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Total Body Lean Mass (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Total Body Mass (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Trunk Fat (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Trunk Lean Mass (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Trunk Mass (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Upper Extremity Fat (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Upper Extremity Lean Mass (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Upper Extremity Total Mass (Grams)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Eosinophils (x 10^9/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Fasting Glucose (Millimoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Hematocrit (Fraction)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Hemoglobin (Grams/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in High Density Lipoprotein Cholesterol (HDL) (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Hips Measurement (cm)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Inorganic Phosphate (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Insulin (Picomoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Interleukin-6 (Nanograms/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Lactate (Millimoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Lactate Dehydrogenase (Units/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Leptin (Nanograms/Milliliter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Lipase (Units/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Low Density Lipoprotein (LDL) (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Low Density Lipoprotein (LDL): High Density Lipoprotein (HDL) Ratio (Ratio)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Lymphocytes (x 10^9/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Magnesium (Millimoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Mid-Arm Measurement (cm)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Mid-Thigh Measurement (cm)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Monocytes (x 10^9/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Neutrophils (x 10^9/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Platelet Count (x 10^9/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Potassium (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Red Blood Cell Count (x 10^12/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Sitting Diastolic Blood Pressure (mm Hg)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Sitting Heart Rate (Beats Per Minute)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Sitting Systolic Blood Pressure (mm Hg)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Sodium (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Soluble Tumor Necrosis Factor Receptor-1 (Picograms/Milliliter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Soluble Tumor Necrosis Factor Receptor-2 (Picograms/Milliliter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Temperature (°F)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Total Bilirubin (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Total Protein (Grams/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Triglycerides (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Uric Acid (Micromoles/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Urine pH
NCT00711009 (82) [back to overview]Mean Change From Baseline in Urine Specific Gravity
NCT00711009 (82) [back to overview]Mean Change From Baseline in Waist Measurement (cm)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Weight (kg)
NCT00711009 (82) [back to overview]Mean Change From Baseline in White Blood Cell Count (x 10^9/Liter)
NCT00711009 (82) [back to overview]Number of Participants Who Developed Resistance, Defined Conservatively, to Lopinavir
NCT00711009 (82) [back to overview]Percentage of Participants Responding (Plasma HIV-1 Ribonucleic Acid [RNA] Levels Less Than 40 Copies/Milliliter [mL]) at Week 48 Based on the Food and Drug Administration (FDA) Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00711009 (82) [back to overview]Score on Effectiveness Scale of Treatment Satisfaction Questionnaire for Medication (TSQM)
NCT00711009 (82) [back to overview]Score on Global Satisfaction Scale of Treatment Satisfaction Questionnaire for Medication
NCT00711009 (82) [back to overview]Score on Side Effects Scale of Treatment Satisfaction Questionnaire for Medication
NCT00711009 (82) [back to overview]Time to Loss of Virologic Response - Percentage of Participants Still Categorized as Responders at Day 672
NCT00711009 (82) [back to overview]Mean Change in CD4+ T-Cell Counts From Baseline to Each Visit
NCT00711009 (82) [back to overview]Number of Participants Who Developed Resistance to Each Drug in the Study Regimen, as Defined by the International AIDS Society-USA (IAS-USA) Panel.
NCT00711009 (82) [back to overview]Percentage of Participants Responding (Plasma HIV-1 RNA Levels Below 40 Copies/Milliliter [mL]) at Each Visit Based on the FDA Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00711009 (82) [back to overview]Percentage of Participants With Moderate or Severe Treatment-emergent, Drug-related Adverse Events
NCT00711009 (82) [back to overview]Primary Outcome: Percentage of Participants With Potentially Clinically Significant Laboratory Values
NCT00711009 (82) [back to overview]Change From Baseline on Mental Component of Medical Outcomes Study HIV Health Survey
NCT00711009 (82) [back to overview]Change From Baseline on Physical Component Score of the Medical Outcomes Study HIV Health Survey
NCT00711009 (82) [back to overview]Mean Change From Baseline in Adiponectin (Micrograms/Milliliter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Alanine Aminotransferase (Units/Liter)
NCT00711009 (82) [back to overview]Mean Change From Baseline in Albumin (Grams/Liter)
NCT00752856 (4) [back to overview]Viral Suppression Efficacy at 48 Weeks
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]To Compare the Phase 1 Viral Decay Rates Between LPV/r + RAL vs. EFV/TDF/FTC Treatment Combinations.
NCT00762320 (10) [back to overview]Lopinavir (Lpv) and Ritonavir (Rtv) Cmax at 4 Weeks
NCT00762320 (10) [back to overview]Absolute CD4 and CD4 %
NCT00762320 (10) [back to overview]Symptoms Across All Patients
NCT00762320 (10) [back to overview]Lopinavir and Ritonavir AUC on Low Dose Tablet
NCT00762320 (10) [back to overview]Lopinavir and Ritonavir Area Under the Curve (AUC) Liquid Kaletra
NCT00762320 (10) [back to overview]Lopinavir (Lpv) and Ritonavir (Rtv) Maximumu Plasma Concentration (CMax) Liquid
NCT00762320 (10) [back to overview]Viral Load (VL)
NCT00762320 (10) [back to overview]Patient Satisfaction
NCT00762320 (10) [back to overview]Parent Satisfaction
NCT00762320 (10) [back to overview]Lopinavir AUC Ratio of Baseline:Week 4
NCT00775606 (6) [back to overview]Naive, Central Memory, Effector Memory, and T Reg CD4+ T-cell Frequency
NCT00775606 (6) [back to overview]Naive, Central Memory, Effector Memory, and T Reg CD4+ T-cell Frequency
NCT00775606 (6) [back to overview]CD4+ (Cluster of Differentiation 4) T-cell Apoptosis
NCT00775606 (6) [back to overview]CD4+ T-cell Change
NCT00775606 (6) [back to overview]Activated and Regulatory CD4+ and CD8+ T-cell Frequencies
NCT00775606 (6) [back to overview]Activation and Proliferation of CD4+ and CD8+ T-cell Frequencies
NCT00810108 (1) [back to overview]Lopinavir Area Under the Curve (AUC)
NCT00827112 (16) [back to overview]Percentage of Participants With Less Than 50 Copies/mL of HIV-1 RNA
NCT00827112 (16) [back to overview]Percentage of Participants With Less Than 400 Copies/mL of HIV-1 RNA
NCT00827112 (16) [back to overview]Number of Participants With HIV-1 RNA Tropism Status Using Trofile Assay
NCT00827112 (16) [back to overview]HIV-1 RNA Levels at Baseline
NCT00827112 (16) [back to overview]Change From Baseline in HIV-1 RNA Levels of First 15 Participants at Days 4, 7, 10 and 14
NCT00827112 (16) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Maraviroc
NCT00827112 (16) [back to overview]Change From Baseline in Cluster of Differentiation 8+T Lymphocyte (CD8) Cell Count at Weeks 16, 24, 48 and 96
NCT00827112 (16) [back to overview]Change From Baseline in Cluster of Differentiation 4+T Lymphocyte (CD4) Cell Counts at Weeks 16, 24, 48 and 96
NCT00827112 (16) [back to overview]Time to Loss of Virological Response (TLOVR)
NCT00827112 (16) [back to overview]Percentage of Participants With Plasma Human Immuno Deficiency Virus-1 Ribonucleic Acid (HIV-1 RNA) Levels Less Than 50 Copies/Milliliter (mL)
NCT00827112 (16) [back to overview]Number of Participants With Phenotypic Resistance
NCT00827112 (16) [back to overview]Number of Participants With Genotypic Resistance
NCT00827112 (16) [back to overview]Average Observed Plasma Concentration (Cavg) of Maraviroc
NCT00827112 (16) [back to overview]Minimum Observed Plasma Concentration (Cmin) of Maraviroc
NCT00827112 (16) [back to overview]Change From Baseline in Plasma log10 Viral Load at Weeks 16, 24, 48 and 96
NCT00827112 (16) [back to overview]Time-Averaged Difference (TAD) in log10 Viral Load
NCT00884793 (4) [back to overview]Number of Subjects Who Experienced an Increase in CD4% 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 Had a Decrease in HIV RNA Per Million CD4+ T Cells in the Ileum
NCT00884793 (4) [back to overview]"Average Change in Activated (CD38+HLADR+) CD8+ T Cells in the Ileum"
NCT00885664 (11) [back to overview]IL-4
NCT00885664 (11) [back to overview]TNF Alpha
NCT00885664 (11) [back to overview]Symptom Score
NCT00885664 (11) [back to overview]SF-12 Mental Capacity Score
NCT00885664 (11) [back to overview]INF Gamma
NCT00885664 (11) [back to overview]IL-7
NCT00885664 (11) [back to overview]IL-8
NCT00885664 (11) [back to overview]SF-12 Physical Capacity Score
NCT00885664 (11) [back to overview]IL-1 Beta
NCT00885664 (11) [back to overview]IL-6
NCT00885664 (11) [back to overview]IL-10
NCT00928187 (13) [back to overview]Development of Metabolic Syndrome
NCT00928187 (13) [back to overview]Gain in CD4 Cells Between Baseline and W48
NCT00928187 (13) [back to overview]Number of Patients Discontinuing Study Treatment
NCT00928187 (13) [back to overview]Number of Patients With HIV Plasma Viral Load < 200 Copies/ml
NCT00928187 (13) [back to overview]Number of Patients With HIV Plasma Viral Load < 50 Copies/ml
NCT00928187 (13) [back to overview]Number of Patients With Resistance Mutations
NCT00928187 (13) [back to overview]Number of Patients With WHO Stage 3 and 4 HIV Related Events
NCT00928187 (13) [back to overview]Patients With Plasma HIV RNA < 200 Copies/ml
NCT00928187 (13) [back to overview]Tolerance: Equal or Superior to a 25% Reduction in eGFR (Glomerular Filtration Rate)
NCT00928187 (13) [back to overview]Tolerance: Gastrointestinal Complains
NCT00928187 (13) [back to overview]Tolerance: Neuropathies (Grade 1 to 4)
NCT00928187 (13) [back to overview]Adherence
NCT00928187 (13) [back to overview]Number of Patients With Plasma HIV RNA < 50 Copies/mL
NCT00931463 (5) [back to overview]Participants With Plasma HIV RNA < 200 Copies/mL 48 Weeks After Randomization
NCT00931463 (5) [back to overview]Participants With Plasma HIV RNA < 200 Copies/mL 48 Weeks After Randomization, Per-protocol Population
NCT00931463 (5) [back to overview]Participants With Plasma HIV RNA < 200 Copies/mL 48 Weeks After Randomization, Per-protocol Population, Baseline VL >100,000 Copies Per mL
NCT00931463 (5) [back to overview]Participants With Plasma HIV RNA < 200 Copies/mL 48 Weeks After Randomization, Per-protocol Population, Non-completer Classed as Failure
NCT00931463 (5) [back to overview]Participants With Plasma HIV RNA < 200 Copies/mL 48 Weeks After Randomization, Per-protocol Population, VL Less Than or Equal to 100,000 Copies Per mL
NCT00945282 (38) [back to overview]Change From Baseline in Clinical Chemistry Paramaters- Albumin and Total Protein
NCT00945282 (38) [back to overview]Change From Baseline in CD4+ and CD8+ T-lymphocyte Cell Count at Day1 and Day 8.
NCT00945282 (38) [back to overview]Assessment of the Achievement of Pre-dose GSK2248761 Steady State Concentration Following Repeat Dose Administration on Day 2 Through 7
NCT00945282 (38) [back to overview]Accumulation Ratio for AUC , Cmax, Cτ, and Time Invariance Ratio Following Repeat Administration
NCT00945282 (38) [back to overview]HIV-1 Rate of Decline by Treatment
NCT00945282 (38) [back to overview]GSK2248761 PK Parameters Following Dose Administration on Day 7: Tmax
NCT00945282 (38) [back to overview]GSK2248761 PK Parameters Following Dose Administration on Day 7: t1/2
NCT00945282 (38) [back to overview]GSK2248761 PK Parameters Following Dose Administration on Day 7: AUC(0-τ)
NCT00945282 (38) [back to overview]GSK2248761 PK Parameters Following Dose Administration on Day 1: Apparent Clearance (CL/F)
NCT00945282 (38) [back to overview]Change From Baseline to Nadir in Plasma HIV-1 RNA
NCT00945282 (38) [back to overview]Change From Baseline Through Day 8 in Plasma HIV-1 RNA
NCT00945282 (38) [back to overview]Change From Baseline in Clinical Chemistry Paramaters-sodium, Potassium and Carbondioxide or Bicarbonate
NCT00945282 (38) [back to overview]PK Data of Day 1 AUC(0-inf) and Day 7 AUC(0-tau) at Different Doses for the Assessment of Dose Proportionality
NCT00945282 (38) [back to overview]PK Data of Cmax and Ctau at Different Doses for the Assessment of Dose Proportionality
NCT00945282 (38) [back to overview]Percent Change From Baseline in CD4+ and CD8+ T-lymphocyte Cell Count at Day 1 and Day 8
NCT00945282 (38) [back to overview]Number of Participants With Serious Adverse Events (SAEs) and Adverse Events (AEs)
NCT00945282 (38) [back to overview]Number of Participants With Abnormal Electrocardiogram (ECG) Findings
NCT00945282 (38) [back to overview]GSK2248761 PK Parameters Following Dose Administration on Day 7: Predose Concentration (C0), Concentration at End of Dosing Interval (Cτ), Minimum Observed Concentration During One Dosing Interval (Cmin) and Cmax
NCT00945282 (38) [back to overview]GSK2248761 PK Parameters Following Dose Administration on Day 1: Time to Maximum Observed Concentration (Tmax), Terminal Half-life (t1/2), Absorption Lag Time (Tlag)
NCT00945282 (38) [back to overview]GSK2248761 PK Parameters Following Dose Administration on Day 1: Maximum Observed Concentration (Cmax) and Concentration at 24 Hours Post Dose (C24)
NCT00945282 (38) [back to overview]GSK2248761 Pharmacokinetic (PK) Parameters Following Dose Administration on Day 1: Area Under the Plasma Concentration Time Curve 0 to Infinite (AUC[0-∞]) and Area Under the Plasma Concentration Time Curve (AUC [0-24])
NCT00945282 (38) [back to overview]Change From Baseline in Vital Signs-systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT00945282 (38) [back to overview]Change From Baseline in HR
NCT00945282 (38) [back to overview]Change From Baseline in Hematology Parameters- Total Neutrophil
NCT00945282 (38) [back to overview]Change From Baseline in Hematology Paramaters-Mean Corpuscle Hemoglobin Concentration
NCT00945282 (38) [back to overview]Change From Baseline in Hematology Paramaters- Red Blood Cell Count
NCT00945282 (38) [back to overview]Change From Baseline in Hematology Paramaters- Platelet Count
NCT00945282 (38) [back to overview]Change From Baseline in Hematology Paramaters- Mean Corpuscle Volume (MCV)
NCT00945282 (38) [back to overview]Change From Baseline in Hematology Paramaters- Mean Corpuscle Hemoglobin (MCH)
NCT00945282 (38) [back to overview]Change From Baseline in Hematology Paramaters- Hemoglobin
NCT00945282 (38) [back to overview]Change From Baseline in Hematology Paramaters- Hematocrit
NCT00945282 (38) [back to overview]Change From Baseline in Hematology Paramaters- Basophils, Eosinophils, Lymphocytes, Monocytes, White Blood Cell Count
NCT00945282 (38) [back to overview]Change From Baseline in Clinical Chemistry Parameters- Blood Urea Nitrogen, Triglycerides, Glucose, Creatinine, Calcium, Cholesterol, Total Bilirubin, and Direct Bilirubin.
NCT00945282 (38) [back to overview]Change From Baseline in Clinical Chemistry Paramaters- Uric Acid
NCT00945282 (38) [back to overview]Change From Baseline in Clinical Chemistry Paramaters- Thyroxine, Free
NCT00945282 (38) [back to overview]Change From Baseline in Clinical Chemistry Paramaters- Thyroxine Total, Thyroxine Binding Globulin, Total T3.
NCT00945282 (38) [back to overview]Change From Baseline in Clinical Chemistry Paramaters- Phosphorus
NCT00945282 (38) [back to overview]Change From Baseline in Clinical Chemistry Paramaters- Alkaline Phosphatase, Alanine Amino Transferase, Aspartate Amino Transferase
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]Incidence-density of Malaria Defined as the Number of Incident Episodes of Complicated Malaria Per Time at Risk.
NCT00978068 (6) [back to overview]Estimates of the 6-month Risk of a First Episode of Malaria
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]Incidence-density of Malaria Defined as the Number of Incident Episodes of Malaria Per Time at Risk.
NCT00985543 (2) [back to overview]Adverse Events
NCT00985543 (2) [back to overview]Plasma Lopinavir/Ritonavir Concentrations as Measured by the Area Under the Curve (AUC 0-12h).
NCT00993031 (14) [back to overview]Number of Participants With Maternal HIV RNA Suppression of <400 Copies/mL
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]Number of Participants With Grade 3 or 4 Toxicity in the Two Treatment Groups in Women
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]Number of Participants With Maternal to Child Transmission of HIV, Measured by Infant HIV DNA PCR
NCT00993031 (14) [back to overview]ART Levels in Hair Samples at Delivery
NCT00993031 (14) [back to overview]Change in Maternal CD4 Cell Counts
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]Placental Malaria Defined as Positive Placental RDT
NCT00993031 (14) [back to overview]Placental Malaria Defined Placental Histopathologic Analysis
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]Prevalence of Malaria Defined as Positive Placental Blood PCR
NCT00993031 (14) [back to overview]Prevalence of Malaria Defined as Positive Placental Blood Smear
NCT00993031 (14) [back to overview]Maternal Malaria Defined as the Number of Treatments for New Episodes of Malaria Per Time at Risk After Pregnancy
NCT01003990 (1) [back to overview]Number of Participants With Serious Adverse Events (SAEs), Treatment Related SAEs, Treatment Related Adverse Events (AEs), AEs Leading to Discontinuation of Study Therapy, Grade 3 to Grade 4 AEs, Grade 3 to Grade 4 AEs, CDC Class C AIDS Events, or Death
NCT01057433 (1) [back to overview]Area Under the Curve From Time 0 to Tau (AUC 0-τ)
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Obstetrical Complications
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Obstetrical Complications
NCT01061151 (28) [back to overview]Antepartum Component: Probability of Overall and HIV-free Infant Survival Until 104 Weeks of Age, by Antepartum Arm (in Conjunction With Infants in the Postpartum Component)
NCT01061151 (28) [back to overview]Antepartum Component: Probability of Overall and HIV-free Infant Survival Until 104 Weeks of Age, by Antepartum Arm (in Conjunction With Infants in the Postpartum Component)
NCT01061151 (28) [back to overview]Postpartum Component: Proportion of Infants Alive Through 12 and 24 Months Post-delivery
NCT01061151 (28) [back to overview]Antepartum Component: Maternal HIV RNA Less Than 400 Copies/mL at Delivery
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence Rate of Cardiovascular or Other Metabolic Events
NCT01061151 (28) [back to overview]Postpartum Component: Adherence to the Maternal and/or Infant ARV Regimens, as Measured by Maternal Report and Hair Measures
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Grade 3 or Higher Toxicities and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Adverse Pregnancy Outcomes (e.g.,Stillbirth, Preterm Delivery (< 37 Weeks), Low Birth Weight (< 2,500 Grams), and Congenital Anomalies)
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Adverse Pregnancy Outcomes (e.g.,Stillbirth, Preterm Delivery (< 37 Weeks), Low Birth Weight (< 2,500 Grams), and Congenital Anomalies)
NCT01061151 (28) [back to overview]Postpartum Component: Proportion of Mother-Infant Pairs With no Death or HIV Diagnosis Through 24 Months Post-delivery
NCT01061151 (28) [back to overview]Postpartum Component: Incidence of Grade 3 or Higher Adverse Events and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events
NCT01061151 (28) [back to overview]Postpartum Component: Incidence of Confirmed Infant HIV Infection
NCT01061151 (28) [back to overview]Maternal Health Component: Toxicity: Incidence of Grade 3 or Greater Laboratory Results or Signs and Symptoms and Selected Grade 2 Hematologic, Renal, and Hepatic Laboratory Results
NCT01061151 (28) [back to overview]Maternal Health Component: Other Targeted Medical Conditions
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence Rate of Progression to AIDS-defining Illness, Death, or a Serious Non-AIDS Cardiovascular, Hepatic, or Renal Event
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence Rate of Death or Any Condition of Particular Concern
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of Tuberculosis
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of Progression to AIDS-defining Illness or Death
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of HIV/AIDS-related Events
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of HIV/AIDS-related Event or Death
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of Death
NCT01061151 (28) [back to overview]Antepartum Component: Number of Confirmed Infant HIV Infections
NCT01061151 (28) [back to overview]Antepartum Component: Number of Infant HIV Infections
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of AIDS-defining Illness
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of HIV/AIDS-related Event or World Health Organization (WHO) Clinical Stage 2 or 3 Events
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Grade 3 or Higher Toxicities and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events
NCT01068873 (1) [back to overview]Number of Participants With HIV RNA < 50 and <400 Copies/ml.
NCT01074931 (6) [back to overview]Number of Participants Who Missed Doses, Interrupt or Discontinue Regimen, and Experience Changes in Dosage or of Combination Regimen
NCT01074931 (6) [back to overview]Adverse Events Observed and Development of Lipodystrophy Lesion and Their Locations
NCT01074931 (6) [back to overview]Evolution of CD4 Count
NCT01074931 (6) [back to overview]Evolution of the HIV Viral Response
NCT01074931 (6) [back to overview]Evolution of the Tolerance Issues
NCT01074931 (6) [back to overview]The Duration on Treatment Until Development of an Adverse Event Leading to Treatment Discontinuation or Until Escape From Treatment
NCT01076972 (4) [back to overview]Number of Patients Included in Each Center for Disease Control and Prevention (CDC) Classification Category for HIV-infected Adults and Adolescents
NCT01076972 (4) [back to overview]Cluster of Differentiation 4 Lymphocyte Count (CD4)
NCT01076972 (4) [back to overview]Mean Number of Human Immunodeficiency Virus (HIV) Ribonucleic Acid (RNA) Copies Per Milliliter (mL) Using a Logarithmic (Base 10) Transformation at Each Visit
NCT01076972 (4) [back to overview]Total Number of Patients With Adverse Drug Reactions
NCT01076985 (1) [back to overview]Number of Patients With Adverse Drug Reactions (ADRs)
NCT01083810 (6) [back to overview]Percentage of Patients With HIV-1 RNA 50 to <200 Copies/ml
NCT01083810 (6) [back to overview]Change in Absolute CD4 Cell Count [CD4+ Cells/µL]
NCT01083810 (6) [back to overview]Number of Patients With Virus That Develop Mutations Conferring Resistance to Lopinavir/Ritonavir, NRTIs or NNRTIs
NCT01083810 (6) [back to overview]Percentage of Patients With HIV-1 RNA <50 Copies/ml
NCT01083810 (6) [back to overview]Percentage of Patients With HIV-1 RNA >500 Copies/ml
NCT01083810 (6) [back to overview]Percentage of Patients With HIV-1 RNA 200 to <500 Copies/ml
NCT01095094 (2) [back to overview]Progression-free Survival
NCT01095094 (2) [back to overview]Grade 3-5 Toxicity as Assessed by NCI CTC v3.0
NCT01146873 (5) [back to overview]CD4 Cell Percentage at 48 Weeks After Randomization
NCT01146873 (5) [back to overview]Highest Grade ALT After Randomization
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]Viral Failure
NCT01146873 (5) [back to overview]Viral Rebound
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]Viral Load
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]CD4 Cell Count
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01153269 (42) [back to overview]Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters
NCT01154673 (1) [back to overview]Change in Proviral HIV-1 DNA in Total CD4+ T-cells From Baseline to Week 48 in Participants Randomized to the Intensified Arm Versus the Control Arm Who Received Placebo in Addition to Standard HAART.
NCT01172535 (10) [back to overview]Clearance of Lopinavir/Ritonavir (CL/F)
NCT01172535 (10) [back to overview]Adherence
NCT01172535 (10) [back to overview]Treatment Efficacy (CD4%)
NCT01172535 (10) [back to overview]Lopinovir/Ritonavir Area Under the Concentration-time Curve (AUC0-24)
NCT01172535 (10) [back to overview]Maximum Concentration of Lopinavir/Ritonavir (Cmax)
NCT01172535 (10) [back to overview]Number of Participants Experiencing Adverse Events of Grade 3 or 4
NCT01172535 (10) [back to overview]Proportion of Participants Tolerating LPV/r
NCT01172535 (10) [back to overview]Proportion of Participants With an AUC of Less Than 10% of Adults
NCT01172535 (10) [back to overview]Treatment Efficacy (HIV Viral Load)
NCT01172535 (10) [back to overview]Minimum Concentration of Lopinavir/Ritonavir (Cmin)
NCT01352715 (9) [back to overview]Number of Participants With Grade 3 or Higher Adverse Event (AE) at Least One Grade Higher Than Baseline
NCT01352715 (9) [back to overview]Percentage of Time Spent in Hospital
NCT01352715 (9) [back to overview]Changes in Fasting Total Cholesterol, High-density Lipoprotein (HDL) Cholesterol, Low-density Lipoprotein (LDL) Cholesterol, Triglycerides, and Glucose From Baseline
NCT01352715 (9) [back to overview]Number of Participants With HIV-1 Drug Resistance Mutations in Protease, Reverse Transcriptase, and Integrase in Participants With Virologic Failure at Baseline and at Time of Virologic Failure
NCT01352715 (9) [back to overview]Change in CD4+ Cell Count From Baseline to Week 48
NCT01352715 (9) [back to overview]Cumulative Probability of Virologic Failure by Week 48
NCT01352715 (9) [back to overview]Number of Participants Discontinuing Randomized Treatment for Toxicity
NCT01352715 (9) [back to overview]Number of Participants With a New AIDS-defining Events or Death
NCT01352715 (9) [back to overview]Number of Participants With a Targeted Serious Non-AIDS-defining Event or Death
NCT01513122 (6) [back to overview]Mean Total Body Fat Changes From Baseline to 48 Weeks as Measured by DXA Scan
NCT01513122 (6) [back to overview]Mean Total Cholesterol Changes From Baseline to 48 Weeks
NCT01513122 (6) [back to overview]Mean Triglycerides Changes From Baseline to 48 Weeks
NCT01513122 (6) [back to overview]Mean Bone Mineral Density Changes From Baseline to 48 Weeks as Measured by DXA Scan
NCT01513122 (6) [back to overview]Mean Limbs Fat Changes From Baseline to 48 Weeks as Measured by DXA Scan
NCT01513122 (6) [back to overview]Mean Glucose Changes From Baseline to 48 Weeks
NCT01516970 (4) [back to overview]Worst Sheehan Disability Scale (SDS) Score for the Safety Population
NCT01516970 (4) [back to overview]Percentage of Participants Who Developed Detectable HIV Antibodies
NCT01516970 (4) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT01516970 (4) [back to overview]Number of Participants With Early Discontinuation From Randomized Human Immunodeficiency Virus Postexposure Prophylaxis (HIV PEP)
NCT01601626 (26) [back to overview]Number of Participants Reporting a Grade 3 or 4 Laboratory Abnormality
NCT01601626 (26) [back to overview]LPV AUC in Participants Enrolled in Arms A, B, and C
NCT01601626 (26) [back to overview]Cumulative Probability of HIV Virologic Failure at Week 72
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 8
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 72
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 48
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 24
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Relapse/Recurrence
NCT01601626 (26) [back to overview]RAL AUC in Participants Enrolled in Arm C
NCT01601626 (26) [back to overview]Percent of Participants Whose HIV Viral Load Was Less Than 50 Copies/mL at Week 48
NCT01601626 (26) [back to overview]Percent of Participants Whose HIV Viral Load Was Less Than 400 Copies/mL at Week 48.
NCT01601626 (26) [back to overview]Percent of Participants Who Interrupted or Discontinued at Least One TB Drug Due to Toxicity
NCT01601626 (26) [back to overview]Percent of Participants Who Interrupted or Discontinued at Least One HIV Drug Due to Toxicity
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Treatment Failure
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Relapse/Recurrence and Who Had TB Drug Resistance
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced Sputum Conversion at Week 8.
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced HIV Virologic Failure
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced a New AIDS-defining Illness or Died
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced a New AIDS-defining Illness
NCT01601626 (26) [back to overview]Number of Participants Who Experienced MTB IRIS
NCT01601626 (26) [back to overview]Number of Participants Reporting a Grade 3 or 4 Sign or Symptom
NCT01601626 (26) [back to overview]Percent of Participants Who Died
NCT01601626 (26) [back to overview]RBT Cmax and Cmin in Participants Enrolled in Arms A and C
NCT01601626 (26) [back to overview]RAL Cmax and Cmin in Participants Enrolled in Arm C
NCT01601626 (26) [back to overview]LPV Cmax and Cmin in Participants Enrolled in Arms A, B, and C
NCT01601626 (26) [back to overview]RBT AUC in Participants Enrolled in Arms A and C
NCT01632891 (7) [back to overview]Change in log10(Pf Gametocyte Density) From Entry to Day 30
NCT01632891 (7) [back to overview]Time to First Pf SCP Clearance
NCT01632891 (7) [back to overview]Number of Participants With Uncomplicated Clinical Malaria
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 Detectable Pf Gametocyte Density
NCT01632891 (7) [back to overview]Proportion of Participants With Plasmodium Falciparum (Pf) Subclinical Parasitemia (SCP) Clearance
NCT01632891 (7) [back to overview]Log10(Pf Parasite Density)
NCT01662336 (20) [back to overview]Percentage of Participants Adherent to Treatment at Month 12
NCT01662336 (20) [back to overview]Percentage of Participants Adherent to Treatment at Month 6
NCT01662336 (20) [back to overview]Change From Baseline in Adherence Integration Subscale Score at Months 6 and 12
NCT01662336 (20) [back to overview]Change From Baseline in Adherence Perseverance Subscale Score at Months 6 and 12
NCT01662336 (20) [back to overview]Change From Baseline in Adherence Summative Score at Months 6 and 12
NCT01662336 (20) [back to overview]Change From Baseline in Coping Self-Efficacy
NCT01662336 (20) [back to overview]Change From Baseline in Health-related Quality of Life Cognitive Functioning Domain Score
NCT01662336 (20) [back to overview]Change From Baseline in Health-related Quality of Life Energy/ Fatigue Domain Score
NCT01662336 (20) [back to overview]Change From Baseline in Health-related Quality of Life General Health Perception Domain Score
NCT01662336 (20) [back to overview]Change From Baseline in Health-related Quality of Life Mental Health Domain Score
NCT01662336 (20) [back to overview]Change From Baseline in Health-related Quality of Life Pain Domain Score
NCT01662336 (20) [back to overview]Change From Baseline in Health-related Quality of Life Physical Functioning Domain Score
NCT01662336 (20) [back to overview]Health Resource Utilization
NCT01662336 (20) [back to overview]Viral Load at Each Visit
NCT01662336 (20) [back to overview]Healthcare Provider Satisfaction
NCT01662336 (20) [back to overview]Change From Baseline in Health-related Quality of Life Role Functioning Domain Score
NCT01662336 (20) [back to overview]Cluster of Differentiation 4 (CD4) Positive Cell Counts at Each Visit
NCT01662336 (20) [back to overview]Change From Baseline in Psychological Well-being
NCT01662336 (20) [back to overview]Change From Baseline in Patient Perception of Stress
NCT01662336 (20) [back to overview]Change From Baseline in Health-related Quality of Life Social Functioning Domain Score
NCT01818258 (17) [back to overview]Free Fraction of LPV at Hour 2 Post Dose
NCT01818258 (17) [back to overview]HIV Viral Load <400 Copies/mL
NCT01818258 (17) [back to overview]Minimum Trough Concentration (Ctrough) of Lopinavir
NCT01818258 (17) [back to overview]Plasma Clearance of Lamivudine
NCT01818258 (17) [back to overview]Plasma Clearance of Lopinavir
NCT01818258 (17) [back to overview]Plasma Clearance of Ritonavir
NCT01818258 (17) [back to overview]Plasma Clearance of Zidovudine
NCT01818258 (17) [back to overview]Steady-state Lopinavir Area Under the Curve
NCT01818258 (17) [back to overview]Steady-state Ritonavir Area Under the Curve
NCT01818258 (17) [back to overview]Steady-state Zidovudine Area Under the Curve
NCT01818258 (17) [back to overview]Grade 3 or Higher Adverse Events Related to Study Drugs Through Week 24
NCT01818258 (17) [back to overview]Steady-state Lamivudine Area Under the Curve
NCT01818258 (17) [back to overview]Grade 3 or Higher Adverse Events Through 24 Weeks
NCT01818258 (17) [back to overview]Change in CD4 Percent
NCT01818258 (17) [back to overview]Change in HIV Viral Load From Baseline
NCT01818258 (17) [back to overview]Change in Mid-upper Arm Circumference
NCT01818258 (17) [back to overview]Change in WHO Weight-for-height Z-score
NCT02116660 (1) [back to overview]Change From Baseline in Estimated Glomerular Filtration Rate (eGFR)
NCT02155101 (3) [back to overview]HIV-1 RNA Viral Load
NCT02155101 (3) [back to overview]HIV-1 RNA Viral Load
NCT02155101 (3) [back to overview]HIV-1 RNA Viral Load
NCT02159352 (11) [back to overview]Number of Participants With Marked Abnormalities in Hematology Laboratory Test Results
NCT02159352 (11) [back to overview]Dose-normalized Area Under the Concentration-Time Curve in 1 Dosing Interval (AUC[TAU]/D) of Daclatasvir
NCT02159352 (11) [back to overview]Maximum Observed Plasma Concentration (Cmax) for Daclatasvir
NCT02159352 (11) [back to overview]Number of Participants With Abnormalities in Vital Sign Measurements
NCT02159352 (11) [back to overview]Plasma Concentration Observed at 24 Hours Postdose (C24) of Daclatasvir
NCT02159352 (11) [back to overview]Time of Maximum Observed Plasma Concentration (Tmax) of Daclatasvir
NCT02159352 (11) [back to overview]Number of Participants With Serious Adverse Events (SAEs) and Discontinuations Due to Adverse Events (AEs) and Who Died
NCT02159352 (11) [back to overview]Dose-normalized Maximum Observed Plasma Concentration (Cmax/D) and Dose-normalized Plasma Concentration Observed at 24 Hours Postdose (C24/D) of Daclatasvir
NCT02159352 (11) [back to overview]Number of Participants With Abnormalities in Electrocardiogram (ECG) Findings
NCT02159352 (11) [back to overview]Number of Participants With Abnormalities in Urinalysis and Other Chemistry Testing Results
NCT02159352 (11) [back to overview]Area Under the Concentration-Time Curve in 1 Dosing Interval (AUC[TAU]) for Daclatasvir
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in CD4+ T-cell Counts (Cells/mm^3) at Week 24
NCT02581202 (36) [back to overview]Number of Participants With Adverse Events
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: HDL
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: LDL
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Aspartate Aminotransferase (µmol/L)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Aspartate Aminotransferase (U/L)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Alanine Aminotransferase (µmol/L)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Alanine Aminotransferase (U/L)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in HIV-1- RNA Viral Load at Week 48 (Untransformed Data)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in HIV-1- RNA Viral Load at Week 48 (Base-10 Logarithm Transformed Data)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in CD4+ T-cell Counts (Cells/mm^3) at Week 48
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in CD4+ T-cell Counts (%) at Week 48
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in CD4+ T-cell Counts (%) at Week 24
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Anthropometric Measurements At Week 48
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Anthropometric Measurements At Week 24
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline (BL) in HIV-1- RNA Viral Load at Week 24 (Untransformed Data)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Serum Creatinine
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline (BL) in HIV-1- RNA Viral Load at Week 24 (Base-10 Logarithm Transformed Data)
NCT02581202 (36) [back to overview]Percentage of Participants on Dual Therapy (LPV/r + 3TC) With Undetectable HIV-1 RNA Level at Week 48
NCT02581202 (36) [back to overview]Percentage of Participants on Dual Therapy (LPV/r + 3TC) With Undetectable HIV-1 RNA Level at Week 24
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Total Cholesterol
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Triglycerides
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Alanine Aminotransferase (U/L)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Alanine Aminotransferase (µmol/L)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Aspartate Aminotransferase (U/L)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Aspartate Aminotransferase (µmol/L)
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Glucose
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: HDL
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Insulin
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Glucose
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Insulin
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: LDL
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Serum Creatinine
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Total Cholesterol
NCT02581202 (36) [back to overview]Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Triglycerides
NCT02581202 (36) [back to overview]Number of Participants Who Developed Resistance to Nucleoside Reverse Transcriptase Inhibitors (NRTIs), Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs), and Protease Inhibitors (PIs)
NCT03070470 (3) [back to overview]"Change From Baseline J-Tpeakc With Balanced Ion Channel Drugs (Ranolazine, Verapamil, Lopinavir / Ritonavir)"
NCT03070470 (3) [back to overview]QTc Shortening From Calcium Block (Diltiazem) in the Presence of hERG Block (Dofetilide)
NCT03070470 (3) [back to overview]"Change From Baseline QTc With Predominant hERG Blocking Drug (Chloroquine)"
NCT04354428 (6) [back to overview]Time to Resolution of COVID-19 Symptom Resolution in Days
NCT04354428 (6) [back to overview]Time to Clearance of Nasal SARS-CoV-2
NCT04354428 (6) [back to overview]Number of Persons With Lower Respiratory Tract Infection (LRTI), Defined as Resting Blood Oxygen Saturation (SpO2<93%) Level Sustained for 2 Readings 2 Hours Apart and Presence of Subjective Dyspnea or Cough
NCT04354428 (6) [back to overview]Number of Participants With Serious Adverse Events and Adverse Events Resulting in Treatment Discontinuation
NCT04354428 (6) [back to overview]Number of Participants With Hospitalization or Mortality
NCT04354428 (6) [back to overview]COVID-19-related Hospitalization Days
NCT04372628 (8) [back to overview]Fever-free Days: Day 1 to Day 29 (Group 2 and Placebo Control Group)
NCT04372628 (8) [back to overview]Hospital-free Days: Day 1 to Day 29 (Group 2 and Placebo Control Group)
NCT04372628 (8) [back to overview]ICU-free Days: Day 1 to Day 29 (Group 2 and Placebo Control Group)
NCT04372628 (8) [back to overview]Time to Hospitalization Day 1 to Day 29 (Group 2 and Placebo Control Group)
NCT04372628 (8) [back to overview]Time to Symptom Resolution: Day 1 to Day 29 (Group 2 and Placebo Control Group)
NCT04372628 (8) [back to overview]Vasopressor-free Days Through Study Day 29 (Group 2 and Placebo Control Group)
NCT04372628 (8) [back to overview]Ventilator-free Days: Day 1 to Day 29 (Group 2 and Placebo Control Group)
NCT04372628 (8) [back to overview]Oxygen-free Days: Day 1 to Day 29 (Group 2 and Placebo Control Group)

Fridericia-corrected QT (QTcF) Interval and Change From Baseline by Analysis Time Point

The QT interval is a measure of the time between the start of the Q wave and the end of the T wave in the heart's electrical cycle. The QT interval was corrected for heart rate using Fridericia's (QTcF) formula. (NCT00035932)
Timeframe: Baseline, Week 4 predose, 2-3 hours postdose, 6-12 hours postdose, Week 12, Week 24, Week 48

,,
Interventionmsec (Mean)
Baseline Mean (n=119, 110, 118)Mean Change at Week 4 predose (n=117, 104, 110)Mean Change Wk 4 2-3 hrs postdose (n=113,102,106)Mean Change Wk 4 6-12 hrs postdose (n=112,101,105)Mean Change at Week 12 (n=110, 97, 107)Mean Change at Week 24 (n=108, 92, 109)Mean Change at Week 48 (n=89, 75, 97)
ATV 300 mg / RTV390-3-2-421-1
ATV 400 mg / SQV3871-3-133-1
LPV / RTV390-2-7-8220

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Mean Score of European Quality of Life-5 Dimensions (EQ-5D) Health Index Score at Baseline, Mid-Study (Week 24), and Final (Week 48)

The EQ-5D is a 5-item questionnaire to assess health-related quality of life in 5 health dimensions (mobility, self-care, usual activity, pain/discomfort, anxiety/depression) are scored on a 3-level scale: no problems (1), some problems (2), extreme problems (3). Using a standard algorithm, responses are summarized into a single score, the EQ-5D Health Index Score (HIS), which ranges between 1 (representing perfect health) and 0 (representing the worst imaginable health state or death). The smallest coefficient of change is 0.03. (NCT00035932)
Timeframe: Baseline, Week 24, Week 48

,,
Interventionunits on a scale (Mean)
Baseline (n=99, 86, 100)Mid-Study (n=103, 83, 95)Final (n=93, 84, 96)
ATV 300 mg / RTV0.830.870.84
ATV 400 mg / SQV0.850.860.85
LPV / RTV0.860.890.88

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Mean ATV, RTV and SQV Minimum Concentration (Cmin) Values

"The minimum or trough concentration (Cmin) of a drug observed after its administration and just prior to the administration of a subsequent dose." (NCT00035932)
Timeframe: collected at the pre-dose time point after receiving atazanavir for at least four weeks

,
Interventionng/mL (Mean)
ATV (n=40,23)RTV (n=40,0)SQV (n=0,19)
ATV 300 mg / RTV719.53154.83NA
ATV 400 mg / SQV312.01NA52.15

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Lipid Mean Percent Change From Baseline at Week 96, Observed Values

Mean percent change in total cholesterol, high density lipoprotein (HDL) cholesterol, fasting low density lipoprotein (LDL) cholesterol, and fasting triglycerides. (NCT00035932)
Timeframe: Week 96

,,
Interventionpercent change in lipid values (Number)
Total Cholesterol (n=60, 46, 54)HDL Cholesterol (n=60, 46, 54)Fasting LDL Cholesterol (n=52, 39, 43)Fasting Triglycerides (n=52, 40, 43)
ATV 300 mg / RTV-7-5-11-2
ATV 400 mg / SQV-13-74
LPV / RTV97130

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Lipid Mean Percent Change From Baseline at Week 48

Mean percent change in total cholesterol, high density lipoprotein (HDL) cholesterol, fasting low density lipoprotein (LDL) cholesterol, and fasting triglycerides. (NCT00035932)
Timeframe: Week 48

,,
Interventionpercent change in lipid values (Number)
Total CholesterolHDL CholesterolFasting LDL CholesterolFasting Triglycerides
ATV 300 mg / RTV-8-7-10-4
ATV 400 mg / SQV-44-3-14
LPV / RTV62130

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Lipid Mean Percent Change From Baseline at Week 24

Mean percent change in total cholesterol, high density lipoprotein (HDL) cholesterol, fasting low density lipoprotein (LDL) cholesterol, and fasting triglycerides. (NCT00035932)
Timeframe: Baseline, Week 24

,,
Interventionpercent change (Number)
Total CholesterolHigh Density Lipoprotein (HDL) CholesterolFasting Low Density Lipoprotein (LDL) CholesterolFasting Triglycerides
ATV 300 mg / RTV-8-7-10-2
ATV 400 mg / SQV-9-1-11-14
LPV / RTV30-431

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HIV RNA Level - Treated Subjects With Evaluable Cmins at Week 24

Week 24 HIV RNA level and change from baseline were summarized for treated subjects with evaluable Cmins. (NCT00035932)
Timeframe: Baseline, Week 24

,
Interventionlog10 c/mL (Mean)
Baseline ValuesWeek 24 ValuesChange from Baseline at Week 24
ATV 300 mg / RTV4.532.62-1.91
ATV 400 mg / SQV4.412.83-1.57

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Grade 3/4 Laboratory Abnormalities Through Week 48

Common Terminology Criteria for Adverse Events v3.0 (CTCAE) Grades:1=Mild, 2=Moderate, 3=Severe, 4=Life-threatening/disabling, 5=Death. Abnormal values: absolute neutrophil count: ≥500 to <750/mm3 (grade 3), <500/mm3 (grade 4); platelets: 20,000-49,999/mm3 (grade 3), <20,000/mm3 or diffuse petechiae (grade 4); alanine transaminase (ALT): 5.1-10 x upper limit of normal (ULN; grade 3), >10 x ULN (grade 4); aspartate transaminase (AST): 5.1-10 x ULN (grade 3), >10 x ULN (grade 4); bilirubin: 2.6-5 x ULN (grade 3), >5 x ULN (grade 4). (NCT00035932)
Timeframe: From Enrollment to Week 48

,,
Interventionparticipants (Number)
Neutrophil ReductionPlatelet ReductionALT ElevationAST ElevationTotal Bilirubin Elevation
ATV 300 mg / RTV825458
ATV 400 mg / SQV844222
LPV / RTV103441

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Participants Achieving Virologic Half Log Suppression (LOQ = 400 c/mL) at Week 96

Number of participants with a >=0.5 log10 decrease in HIV RNA from baseline or HIV RNA < 400 c/mL at Week 96. (NCT00035932)
Timeframe: Baseline, Week 96

Interventionparticipants (Number)
ATV 300 mg / RTV61
LPV / RTV58

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Deaths, Serious Adverse Events (SAEs), and Adverse Events (AEs) Through Week 48

AE=any new untoward medical occurrence/worsening of a pre-existing medical condition regardless of causal relationship. SAE=any untoward medical occurrence at any dose that: results in death; is life-threatening; requires/prolongs inpatient hospitalization; results in persistent/significant disability; is cancer; is congenital anomaly/birth defect; results in drug dependency/abuse; is an important medical event. (NCT00035932)
Timeframe: From Enrollment through Week 48

,,
Interventionparticipants (Number)
Deaths (n = 120, 115, 123)AEs leading to discontinuation (n = 119, 110, 118)SAEs (n = 120, 115, 123)AEs, grades 1-4 (n = 119, 110, 118)AEs, grades 3-4 (n = 119, 110, 118)
ATV 300 mg / RTV06129711
ATV 400 mg / SQV18149318
LPV / RTV151110312

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Correlation of ATV Minimum Plasma Concentration (Cmin), Inhibitory Quotient (IQ), and Number of Protease Inhibitor (PI) Mutations at Baseline With HIV RNA Change From Baseline at Week 24

Pearson correlations of the Cmin (trough plasma concentration), IQ (the ratio of Cmin of ATV to HIV IC50), and Number of baseline PI Mutations with HIV RNA change from baseline at Week 24 were explored. (NCT00035932)
Timeframe: Baseline, Week 24

,
InterventionPearson Correlation Coefficient (Number)
ATV CminIQ (<10; >=10)# of PI Mutations at baseline (<4; >=4)
ATV 300 mg / RTV-0.056-0.3910.306
ATV 400 mg / SQV0.254-0.0810.437

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Correlation of ATV Minimum Plasma Concentration (Cmin) Inhibitory Quotient (IQ), and Number of PI Mutations at Baseline and CD4 Cell Count Change From Baseline at Week 24

Pearson correlations of the Cmin (trough plasma concentration), IQ (the ratio of Cmin of ATV to HIV IC50), and Number of baseline PI Mutations with CD4 cell count change from baseline at Week 24 were explored. (NCT00035932)
Timeframe: Baseline, Week 24

,
InterventionPearson Correlation Coefficient (Number)
ATV CminIQ (<10; >=10)# of PI Mutations at baseline (<4; >=4)
ATV 300 mg / RTV0.370.376-0.395
ATV 400 mg / SQV-0.210.105-0.227

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Adherence to Regimen Though Week 48 Based on MACS the Multicenter AIDS Cohort Study (MACS) Adherence Questionnaire

The MACS adherence questionnaire asks patients how many medication doses they missed during the previous day, 2 days, 3 days and 4 days. Drug-specific questions included adherence with dose and frequency. Adherence was defined as taking all doses and numbers of pills as prescribed for each medication. This strict adherence cut-off was based on the guidelines stating that anything less than excellent adherence may result in a virus breakthrough and development of resistance. (NCT00035932)
Timeframe: Baseline, Week 24, Week 48

,,
Interventionparticipants (Number)
Adherent at Baseline (n=27, 25, 33)Adherent at Week 24 (n=18, 11, 25)Adherent at Week 48 (n=11, 4, 20)
ATV 300 mg / RTV12108
ATV 400 mg / SQV1052
LPV / RTV182313

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Participants Achieving Virologic Half Log Suppression (LOQ = 50 c/mL) at Week 96

(NCT00035932)
Timeframe: Week 96

InterventionParticipants (Number)
ATV 300 mg / RTV61
LPV / RTV57

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Participants Achieving Virologic Half Log Suppression (LOQ = 50 c/mL) at Week 48

(NCT00035932)
Timeframe: Week 48

InterventionParticipants (Number)
ATV 300 mg / RTV76
ATV 400 mg / SQV60
LPV / RTV84

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Participants Achieving Virologic Half Log Suppression (LOQ = 50 c/mL) at Week 24

(NCT00035932)
Timeframe: Week 24

Interventionparticipants (Number)
ATV 300 mg / RTV95
ATV 400 mg / SQV74
LPV / RTV93

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Mean Change From Baseline in HIV Ribonucleic Acid (RNA) at Week 24

(NCT00035932)
Timeframe: Baseline, Week 24

Interventionlog10 c/mL (Mean)
ATV 300 mg / RTV-1.86
ATV 400 mg / SQV-1.52
LPV / RTV-1.89

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Participants Achieving Treatment Response (LOQ = 50 c/mL) Without Prior Failure at Week 96

Treatment Response = confirmed suppression to LOQ (50 c/mL). The Algorithm for Treatment Response Without Prior Failure (TRPWF) = participants staying in response at the analysis timepoint without having an intervening, confirmed rebound. (NCT00035932)
Timeframe: Week 96

Interventionparticipants (Number)
ATV 300 mg / RTV38
LPV / RTV41

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Participants Achieving Treatment Response (LOQ = 50 c/mL) Without Prior Failure at Week 48

Treatment Response = confirmed suppression to LOQ (50 c/mL). The Algorithm for Treatment Response Without Prior Failure (TRPWF) = participants staying in response at the analysis timepoint without having an intervening, confirmed rebound. (NCT00035932)
Timeframe: Week 48

Interventionparticipants (Number)
ATV 300 mg / RTV43
ATV 400 mg / SQV28
LPV / RTV52

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Participants Achieving Treatment Response (LOQ = 50 c/mL) Without Prior Failure at Week 24

Treatment Response = confirmed suppression to LOQ (50 c/mL). The Algorithm for Treatment Response Without Prior Failure (TRPWF) = participants staying in response at the analysis timepoint without having an intervening, confirmed rebound. (NCT00035932)
Timeframe: Week 24

Interventionparticipants (Number)
ATV 300 mg / RTV46
ATV 400 mg / SQV25
LPV / RTV50

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Participants Achieving Treatment Response (LOQ = 400 c/mL) Without Prior Failure at Week 96

Treatment Response = confirmed suppression to LOQ (400 c/mL). The Algorithm for Treatment Response Without Prior Failure (TRPWF) = participants staying in response at the analysis timepoint without having an intervening, confirmed rebound. (NCT00035932)
Timeframe: Week 96

Interventionparticipants (Number)
ATV 300 mg / RTV52
LPV / RTV53

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HIV IC50 at Week 24

IC50: inhibitory concentration of drug required to reduce viral replication by 50%. (NCT00035932)
Timeframe: Week 24

Interventionng/mL (Mean)
ATV 300 mg / RTV17.83
ATV 400 mg / SQV22.84

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Fasting Glucose Mean Change From Baseline at Week 48

(NCT00035932)
Timeframe: Week 48

Interventionmg/dL (Mean)
ATV 300 mg / RTV4
ATV 400 mg / SQV-1
LPV / RTV1

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Fasting Glucose Mean Change From Baseline at Week 24

(NCT00035932)
Timeframe: Baseline, Week 24

Interventionmg/dL (Mean)
ATV 300 mg / RTV0
ATV 400 mg / SQV-3
LPV / RTV0

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Change From Baseline in CD4 Cell Count at Week 96

(NCT00035932)
Timeframe: Baseline, Week 96

Interventioncells/mm3 (Mean)
ATV 300 mg / RTV122
LPV / RTV154

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Participants Achieving Treatment Response (LOQ = 400 c/mL) Without Prior Failure at Week 48

Treatment Response = confirmed suppression to LOQ (400 c/mL). The Algorithm for Treatment Response Without Prior Failure (TRPWF) = participants staying in response at the analysis timepoint without having an intervening, confirmed rebound. (NCT00035932)
Timeframe: Week 48

Interventionparticipants (Number)
ATV 300 mg / RTV64
ATV 400 mg / SQV42
LPV / RTV67

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Change From Baseline in CD4 Cell Count at Week 24

(NCT00035932)
Timeframe: Baseline, Week 24

Interventioncells/mm3 (Mean)
ATV 300 mg / RTV83
ATV 400 mg / SQV59
LPV / RTV90

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Inhibitory Quotient at Week 24

Inhibitory quotient is a measure of drug exposure and susceptibility in an individual. The IQ is typically calculated as the ratio of Cmin to HIV IC50. (NCT00035932)
Timeframe: Baseline, Week 24

Interventionratio (Mean)
ATV 300 mg / RTV136.94
ATV 400 mg / SQV25.04

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Participants Achieving Virologic Half Log Suppression (LOQ = 400 c/mL) at Week 48, (Overall and by PI Sensitivity)

Number of participants with a >=0.5 log10 decrease in HIV RNA from baseline or HIV RNA < 400 c/mL at Week 48, by their baseline phenotypic sensitivity to their randomized PI. (NCT00035932)
Timeframe: Baseline, Week 48

,,
Interventionparticipants (Number)
Overall (n=120, 115, 123)PI Sensitive (n=88, 84, 88)PI Resistant (n=32, 30, 33)
ATV 300 mg / RTV776512
ATV 400 mg / SQV60527
LPV / RTV846716

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Participants Achieving Virologic Half Log Suppression (Limit of Quantification [LOQ] = 400 c/mL) at Week 24 (Overall and by Protease Inhibitor [PI] Sensitivity)

Number of participants with a >=0.5 log10 decrease in HIV RNA from baseline or HIV RNA < 400 c/mL at Week 24, by their baseline phenotypic sensitivity to their randomized PI. (NCT00035932)
Timeframe: Baseline, Week 24

,,
Interventionparticipants (Number)
Overall (n=120, 115, 123)PI Sensitive (n=88, 83, 88)PI Resistant (n=32, 30, 33)
ATV 300 mg / RTV957916
ATV 400 mg / SQV745815
LPV / RTV937219

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Most Common AEs and AEs of Interest Through Week 48

Prespecified AEs of interest included jaundice, ocular icterus, and hyperbilirubinemia. (NCT00035932)
Timeframe: From Enrollment to Week 48

,,
Interventionparticipants (Number)
Diarrhea (Most Common)Headache (Most Common)Nausea (Most Common)Jaundice (AE of Interest)Ocular Icterus (AE of Interest)Hyperbilirubinemia (AE of Interest)
ATV 300 mg / RTV252119191324
ATV 400 mg / SQV292424638
LPV / RTV541815001

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PR Interval and Change From Baseline by Analysis Time Point

The PR interval is measured from the beginning of the P wave to the beginning of the QRS complex, and reflects the time the electrical impulse takes to travel from the sinus node through the atrioventricular (AV) node and entering the ventricles. The PR interval is therefore a good estimate of AV node function. (NCT00035932)
Timeframe: Baseline, Week 4 predose, 2-3 hours postdose, 6-12 hours postdose, Week 12, Week 24, Week 48

,,
Interventionmsec (Mean)
Baseline Mean (n=119, 110, 118)Mean Change at Week 4 predose (n=117, 104, 110)Mean Change Wk 4 2-3 hrs postdose (n=113,102,106)Mean Change Wk 4 6-12 hrs postdose (n=112,101,105)Mean Change at Week 12 (n=110, 97, 107)Mean Change at Week 24 (n=108, 92, 109)Mean Change at Week 48 (n=89, 75, 97)
ATV 300 mg / RTV153412520
ATV 400 mg / SQV155966772
LPV / RTV154312854

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Mean Score of European Quality of Life-5 Dimensions (EQ-5D) Visual Analog Scale (VAS) at Baseline, Mid-Study (Week 24), and Final (Week 48)

The EQ-5D has a Visual Analog Scale (VAS), which is a feeling thermometer-like scale with a range between 0 and 100. Patients are required to draw a line from a box on the VAS scale to an actual mark on the thermometer-like scale that corresponds with a number that reflects their self-assessed health status at the time they are completing the questionnaire. Higher VAS scores indicate better overall health. There is no minimum clinically important difference reported in the literature for VAS. (NCT00035932)
Timeframe: Baseline, Week 24, Week 48

,,
Interventionunits on a scale (Mean)
Baseline (n=98, 85, 101)Mid-Study (n=102, 83, 97)Final (n=95, 81, 96)
ATV 300 mg / RTV81.3384.8982.77
ATV 400 mg / SQV81.7283.3485.80
LPV / RTV81.5285.0986.16

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Change From Baseline in CD4 Cell Count at Week 48

(NCT00035932)
Timeframe: Baseline, Week 48

Interventioncells/mm3 (Mean)
ATV 300 mg / RTV110
ATV 400 mg / SQV72
LPV / RTV121

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Participants Achieving Treatment Response (LOQ = 400 c/mL) Without Prior Failure at Week 24

Treatment Response = confirmed suppression to LOQ (400 c/mL). The Algorithm for Treatment Response Without Prior Failure (TRPWF) = participants staying in response at the analysis timepoint without having an intervening, confirmed rebound. (NCT00035932)
Timeframe: Week 24

Interventionparticipants (Number)
ATV 300 mg / RTV76
ATV 400 mg / SQV50
LPV / RTV74

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Mean Change From Baseline in HIV RNA at Week 96

(NCT00035932)
Timeframe: Baseline, Week 96

Interventionlog10 c/mL (Mean)
ATV 300 mg / RTV-2.29
LPV / RTV-2.08

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Mean Change From Baseline in HIV RNA at Week 48

(NCT00035932)
Timeframe: Baseline, Week 48

Interventionlog10 c/mL (Mean)
ATV 300 mg / RTV-1.93
ATV 400 mg / SQV-1.55
LPV / RTV-1.87

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Mean Change From Baseline in HIV RNA at Week 2

(NCT00035932)
Timeframe: Baseline, Week 2

Interventionlog10 c/mL (Mean)
ATV 300 mg / RTV-1.18
ATV 400 mg / SQV-1.14
LPV / RTV-1.30

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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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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: 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 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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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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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 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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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: 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: 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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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: 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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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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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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Levels of Proviral DNA in Peripheral Blood Mononuclear Cells (PBMC) (log10)

(NCT00084149)
Timeframe: At 48 weeks after the start of treatment

Interventionlog10(copies/mL) (Median)
Cyclosporine1.88
No Cyclosporine1.92

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HIV-1 Viral Load Levels

(NCT00084149)
Timeframe: At Week 48

Interventionlog10(copies/mL) (Mean)
Cyclosporine1.70
No Cyclosporine1.70

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CD4 T Cell Levels

(NCT00084149)
Timeframe: At Week 48

Interventioncells/mm^3 (Median)
Cyclosporine301
No Cyclosporine287

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Proviral DNA Levels (log10)

(NCT00084149)
Timeframe: At Week 24

Interventionlog10(copies/mL) (Median)
Cyclosporine2.12
No Cyclosporine1.96

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Proviral DNA (log10)

(NCT00084149)
Timeframe: At Week 12

Interventionlog10(copies/mL) (Median)
Cyclosporine2.22
No Cyclosporine2.13

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Number of Patients With Viral Load Less Than 50 Copies/ml

(NCT00084149)
Timeframe: Week 48

InterventionParticipants (Count of Participants)
Cyclosporine27
No Cyclosporine13

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Time From Randomization to Virologic Failure or Death for Participants Without SD NVP Exposure Prior to Study Entry

5th and 10th Percentiles in weeks from randomization to virologic failure (VF) or death. VF is defined as a plasma HIV-1 RNA level that is 1 log10 below baseline 12 weeks after treatment is initiated or as a plasma HIV-1 RNA level that is >=400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized treatment was being taken at the time of VF. (NCT00089505)
Timeframe: Throughout study with median follow-up 72 weeks and range from 0 to 180 weeks.

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
NoNVP/LPV_r1236132
NoNVP/NVP2436NA

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Number of Participants Who Experienced Virologic Failure or Died.

Virologic failure (VF) is defined as a plasma HIV-1 RNA level that is 1 log10 below baseline 12 weeks after treatment is initiated or as a plasma HIV-1 RNA level that is >=400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized treatment was being taken at the time of VF. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) for NVP/NVP and NVP/LPV_r. Throughout study for NoNVP/NVP and NoNVP/LPV_r.

Interventionparticipants (Number)
NVP/NVP32
NVP/LPV_r10
NoNVP/NVP42
NoNVP/LPV_r50

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Number of Participants Who Received NVP-containing Regimens at Randomization and Experienced NVP-associated Rash or Grade 2+ Liver Lab Abnormality

Any grade of rash or grade 2+ liver lab abnormality events that were claimed to be NVP associated (definitely, probably, or possibly) by site investigators were evaluated. Grade 2+ liver lab abnormality is defined as aspartate aminotransferase (AST)>=2.6 x ULN or alanine aminotransferase (ALT)>=2.6 x ULN. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) for NVP/NVP arm. Throughout study for NoNVP/NVP arm.

Interventionparticipants (Number)
NVP/NVP20
NoNVP/NVP51

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CD4 Count Change From Randomization

Change was calculated as the CD4 count at Week 48 (or at Week 96) minus the baseline CD4 count (last CD4 before/on treatment start date). For NVP/NVP and NVP/LPV_r arms, data through DSMB review cutoff (October 6, 2008) were used to report the outcome. For NoNVP/NVP and NoNVP/LPV_r arms, since the follow-up continued as planned, data through overall study were used. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) for NVP/NVP and NVP/LPV_r. Throughout study for NoNVP/NVP and NoNVP/LPV_r. Week 48 and 96.

,,,
Interventioncells/mm^3 (Median)
Week 48 CD4 count change from randomizationWeek 96 CD4 count change from randomization
NoNVP/LPV_r172256
NoNVP/NVP172223
NVP/LPV_r201278
NVP/NVP191291

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Percent of Participants Who Experienced Virologic Failure or Died

Results report cumulative percent of participants reaching virologic failure (VF) or death by week 48 and week 96 calculated using the Kaplan-Meier method. VF is defined as a plasma HIV-1 RNA level that is 1 log10 below baseline 12 weeks after treatment is initiated or as a plasma HIV-1 RNA level that is >=400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized treatment was being taken at the time of VF. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) for NVP/NVP and NVP/LPV_r arms. Throughout study for NoNVP/NVP and NoNVP/LPV_r arms.

,,,
InterventionPercent of participants (Number)
week 48 percent of virologic failure or deathweek 96 percent of virologic failure or death
NoNVP/LPV_r1420
NoNVP/NVP1417
NVP/LPV_r412
NVP/NVP2331

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Percent of Participants Who Reported to Never Missed Any of the Study Drug Regimen in the Past Month

Self-reported adherence at week 48 and 96 while participants remained on randomized regimen. Adherence interviews for each antiretroviral drug drug the participant is taking was performed by site personnel every 24 weeks. For NVP/NVP and NVP/LPV_r arms, data through DSMB review cutoff (October 6, 2008) were used to report the outcome. For NoNVP/NVP and NoNVP/LPV_r arms, since the follow-up continued as planned, data through overall study were used. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) for NVP/NVP and NVP/LPV_r arms. Throughout study for NoNVP/NVP and NoNVP/LPV_r arms.

,,,
Interventionpercent of participants (Number)
week 48 percent of full adherence in past monthweek 96 percent of full adherence in past month
NoNVP/LPV_r8687
NoNVP/NVP9093
NVP/LPV_r8895
NVP/NVP8994

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Time From Randomization to Virologic Failure or Death for Participants Who Had SD NVP Exposure Prior to Study Entry

5th and 10th Percentiles in weeks from randomization to virologic failure (VF) or death. VF is defined as a plasma HIV-1 RNA level that is 1 log10 below baseline 12 weeks after treatment is initiated or as a plasma HIV-1 RNA level that is >=400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized treatment was being taken at the time of VF. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) with median follow-up 72 weeks and range from 0 to 144 weeks.

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
NVP/LPV_r6084NA
NVP/NVP121260

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Ranked log10 HIV-1 RNA Viral Load (log10 Copies/mL) Averaged at Weeks 72 and 76 for the IT Arm and Ranked log10 HIV-1 RNA Viral Load (log10 Copies/mL) Averaged at Weeks 36 and 40 for the DT Arm

"The primary endpoint is (i) average wk 36 and 40 VL for those who continued to wk 36 off ARV for the DT arm, (ii) average wk 72 and 76 VL for those who continued to wk 36 off ARV for the IT arm and (iii) an assigned VL rank for the failures who needed ARVs or met criteria for entry into Step 2 prior to these study visits. The assigned rank for the failures was either the last observed rank carried forward or the worst rank relative to the other possible outcomes. This approach was designed to, if anything, bias against finding a treatment effect. To illustrate, consider five participants who enter the study (A, B, C, D, and E), 4 of whom (A, B, C, D) make it to 72 wks off therapy with RNA levels that increase from A to D. Participant E enters Step 2 at wk 12, at which time his RNA is in the 50th percentile. This rank would be carried forward, so the rank order of the log10 HIV-1 RNA endpoints would be A B E C D." (NCT00090779)
Timeframe: IT arm (weeks 72 and 76) and DT arm ( weeks 36 and 40)

Interventionrank (Median)
IT Arm26.0
DT Arm48.5

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Change in CD4 Counts Cells/mm^3 From Week 36 for IT Arm and From Week 0 for DT Arm

(NCT00090779)
Timeframe: IT arm (weeks 36, 60, 72, 84 and 96) and DT arm (weeks 0, 24, 36, 48 and 60)

,
InterventionChange in Log10 transformed CD4 Counts (Mean)
IT arm (wk 60- wk 36) vs. DT arm (wk 24- wk 0)IT arm (wk 72- wk 36) vs. DT arm (wk 36- wk 0)IT arm (wk 84- wk 36) vs. DT arm (wk 48- wk 0)IT arm (wk 96- wk 36) vs. DT arm (wk 60- wk 0)
DT Arm-0.02-0.03-0.06-0.02
IT Arm-0.11-0.10-0.10-0.12

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Time to Meeting the Clinical, Virologic, or Immunologic Criteria for Treatment Initiation or Re-initiation

5th, 10th, 25th, 50th, 75th and 90th percentiles in weeks from randomization to meeting the criteria for treatment initiation or re-initiation which include CD4 count below 350 cells/mm^3 on two consecutive measurements at least 4 weeks apart, at least 12 weeks into the study or 12 weeks post-treatment discontinuation, confirmed CD4 count below 200 cells/mm^3 or CD4 percent below 14% at any time on study, confirmed HIV-1 RNA level above 750,000 copies/mL 4 weeks into the study or above 200,000 copies/mL 12 weeks or more into the study, or CDC Category B or C diagnosis. (NCT00090779)
Timeframe: 96 weeks since randomization

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile50th percentile75th percentile90th percentile
DT Arm6.912.326.360.096.096.0
IT Arm6.313.036.472.0NANA

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Time to Treatment Initiation or Death

5th, 10th, 25th, 50th and 75th percentiles in weeks from randomization to treatment initiation or death (NCT00090779)
Timeframe: 5 years since randomization

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile50th percentile75th percentile
DT Arm13.920.943.797.3157.7
IT Arm3636.967.196.4163.3

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Number of Participants Experiencing Either a CDC Category B or C Diagnosis, CD4<200 Cells/mm^3 or CD4 Percent <14%.

(NCT00090779)
Timeframe: 96 weeks since randomization

Interventionparticipants (Number)
IT Arm2
DT Arm8

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Number of Participants in IT Arm Off Treatment Before 36 Weeks

The study provided fixed-dose combination emtricitabine/tenofovir DF 200/300 mg orally once daily and lopinavir/ritonavir 200/50 mg administered either as two tablets twice daily or four tablets once daily, for the first 36 weeks for individuals in the IT arm. (NCT00090779)
Timeframe: At Week 36

Interventionparticipants (Number)
IT Arm8

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Time From Study Entry in DT Arm Participants or From Week 36 in IT Arm Participants to Meeting the Clinical, Virologic, or Immunologic Criteria for Treatment Initiation or Re-initiation

5th, 10th, 25th, 50th, 75th and 90th percentiles in weeks from randomization for DT arm or from week 36 for IT arm to meeting the criteria for treatment initiation or re-initiation which include two consecutive CD4 count below 350 cells/mm^3 at least 4 weeks apart, at least 12 weeks into the study or 12 weeks post-treatment discontinuation, confirmed CD4 count below 200 cells/mm^3 or CD4 percent below 14% at any time on study, confirmed HIV-1 RNA level above 750,000 copies/mL 4 weeks into the study or above 200,000 copies/mL 12 weeks or more into the study, or CDC Category B or C diagnosis. (NCT00090779)
Timeframe: 96 weeks since randomization

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile50th percentile75th percentile90th percentile
DT Arm6.912.326.360.096.096.0
IT Arm5.110.422.758.1NANA

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Number of Participants Meeting Clinical, Virologic, or Immunologic Criteria for Treatment Initiation or Re-initiation

The clinical, virologic, or immunologic criteria for treatment initiation or re-initiation include CD4 count below 350 cells/mm^3 on two consecutive determinations at least 4 weeks apart, at least 12 weeks into the study or 12 weeks post-treatment discontinuation, (2) confirmed CD4 count below 200 cells/mm^3 or CD4 percent below 14% at any time on study, (3) confirmed HIV-1 RNA level above 750,000 copies/mL 4 weeks into the study or above 200,000 copies/mL 12 weeks or more into the study, or (4) CDC Category B or C diagnosis. (NCT00090779)
Timeframe: 96 weeks since randomization

InterventionParticipants (Number)
IT Arm7
DT Arm23

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Ranked Log10 HIV-1 RNA Viral Load (log10 Copies/mL) Averaged at 72 and 76 Weeks for the IT Arm and DT Arm

"The primary endpoint is (i) the average of log10 viral loads (VL) at wks 72 and 76 for participants who continued to wk 72 off ARV for the DT arm, (ii) average wk 72 and 76 VL for those who continued to wk 36 off ARV for the IT arm and (iii) an assigned VL rank for the failures who needed ARVs or met criteria for entry into Step 2 prior to these study visits. The assigned rank for the failures was either the last observed rank carried forward or the worst rank relative to the other possible outcomes. This approach was designed to, if anything, bias against finding a treatment effect. To illustrate, consider five participants who enter the study (A, B, C, D, and E), 4 of whom (A, B, C, D) make it to 72 wks off therapy with RNA levels that increase from A to D. Participant E enters Step 2 at wk 12, at which time his RNA is in the 50th percentile. This rank would be carried forward, so the rank order of the log10 HIV-1 RNA endpoints would be A B E C D." (NCT00090779)
Timeframe: At Weeks 72 and 76

Interventionrank (Median)
IT Arm26.0
DT Arm49.3

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Number of Participants Who Discontinued Study Treatment Prematurely

participants assigned to 7-day treatment arm and 21-day treatment arm were supposed to stay in study treatment for 7 days and 21 days respectively. (NCT00099632)
Timeframe: From first day of study treatment to last day of study treatment (up to 21 days)

Interventionparticipants (Number)
7-day Lamivudine/Zidovudine (3TC/ZDV)0
21-day Lamivudine/Zidovudine (3TC/ZDV)2
7-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
21-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
7-day Lopinavir/Ritonavir (LPV/r)0
21-day Lopinavir/Ritonavir (LPV/r)5

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Severe (Grade 3) and Higher Adverse Events and Any Grade Adverse Event That Leads to a Treatment Change From First Day of Study Treatment to Week 12

"Grade 3 or higher signs and symptoms, laboratory abnormalities, events that are reported through the EAE system, and any grade event that leads to a treatment change from first day of study treatment to week 12.~Grade 3 = Severe Grade 4 = Life threatening Grade 5 = Death" (NCT00099632)
Timeframe: From first day of study treatment to week 12

Interventionparticipants (Number)
7-day Lamivudine/Zidovudine (3TC/ZDV)5
21-day Lamivudine/Zidovudine (3TC/ZDV)1
7-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)1
21-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
7-day Lopinavir/Ritonavir (LPV/r)2
21-day Lopinavir/Ritonavir (LPV/r)2

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Number of Participants With New PI-resistant Variants as Detected by Standard Composite (Bulk) Genotyping.

For the 7-day treatment duration group, only the genotype results from weeks 3 and 7 contributed; For the 21-day treatment duration groups, only the genotype results from weeks 5 and 9 contributed. (NCT00099632)
Timeframe: 2 and 6 weeks after completion of treatment

Interventionparticipants (Number)
7-day Lamivudine/Zidovudine (3TC/ZDV)0
21-day Lamivudine/Zidovudine (3TC/ZDV)0
7-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
21-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
7-day Lopinavir/Ritonavir (LPV/r)0
21-day Lopinavir/Ritonavir (LPV/r)0

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Number of Participants With New Circulating NRTI-resistant Variants Detected by Standard Composite (Bulk) Genotyping.

For the 7-day treatment duration group, only the genotype results from weeks 3 and 7 contributed; For the 21-day treatment duration groups, only the genotype results from weeks 5 and 9 contributed. (NCT00099632)
Timeframe: 2 and 6 weeks after completion of treatment

Interventionparticipants (Number)
7-day Lamivudine/Zidovudine (3TC/ZDV)0
21-day Lamivudine/Zidovudine (3TC/ZDV)1
7-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)1
21-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)1
7-day Lopinavir/Ritonavir (LPV/r)1
21-day Lopinavir/Ritonavir (LPV/r)0

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Number of Participants With New Circulating Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI)-Resistant Variants as Detected by Standard Composite (Bulk) Genotyping

"For the 7-day treatment duration group, only the genotype results from weeks 3 and 7 contributed to the primary endpoint; For the 21-day treatment duration groups, only the genotype results from weeks 5 and 9 contributed to primary endpoint.~10 participants who did not have resistance samples available were excluded from the primary endpoint analysis." (NCT00099632)
Timeframe: 2 and 6 weeks after completion of treatment

Interventionparticipants (Number)
7-day Lamivudine/Zidovudine (3TC/ZDV)1
21-day Lamivudine/Zidovudine (3TC/ZDV)0
7-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
21-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
7-day Lopinavir/Ritonavir (LPV/r)3
21-day Lopinavir/Ritonavir (LPV/r)1

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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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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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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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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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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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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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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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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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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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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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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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Number of Patients Who Discontinued Treatment Due to Abnormal Laboratory Parameters

Routine clinical testing, including hematology and standard chemistry panel was performed at all study visits. Laboratory tests for a fasting lipid profile and fasting insulin determination were obtained at baseline, weeks 24 and 48, and the 4-week follow-up visit. The number of participants who discontinued treatment due to an abnormal laboratory result at any visit is reported. (NCT00105079)
Timeframe: baseline and all study visits (Up to Week 52)

Interventionparticipants (Number)
Saquinavir/Ritonavir0
Lopinavir/Ritonavir0

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Change From Baseline in Cluster Differentiation Antigen 4 Positive (CD4+) Lymphocyte Count

Summary statistics for change from baseline in CD4+ lymphocyte count were presented by treatment arm. Change from baseline in CD4+ lymphocyte count was derived as follows: Change from baseline = (CD4+ count at week x) - (CD4+ count at baseline). (NCT00105079)
Timeframe: Baseline to Week 48

,
Interventioncells/mm^3 (Median)
Baseline (n=166,169)Week 48 (n=122,131)Change from Baseline to Week 48 (n=121,130)
Lopinavir/Ritonavir142.0348.0204.0
Saquinavir/Ritonavir141.5319.0178.0

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Change From Baseline in HIV-1 RNA Viral Load

Descriptive statistics for change from baseline in log10 transformed plasma HIV-1 RNA load (copies/mL) were presented by treatment arm. Logarithmic transformation (base 10) was applied to HIV-1 RNA viral load at baseline and at each study visit. Change from baseline in plasma HIV-1 RNA was derived as follows: Change from baseline = Log10 (HIV-1 RNA at week x) - Log10 (HIV-1 RNA at baseline) (NCT00105079)
Timeframe: Baseline to Week 48

,
Interventioncopies/mL (Mean)
BaselineWeek 48 (n=126,133)Change from Baseline to Week 48 (n=126,133)
Lopinavir/Ritonavir5.171.83-3.36
Saquinavir/Ritonavir5.201.80-3.39

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Number of Patients With HIV-1 RNA Viral Load <50 and <400 Copies/mL

"The secondary objectives of the study were to evaluate the safety, adherence, and tolerability of saquinavir/ritonavir BID plus emtricitabine/tenofovir QD versus lopinavir/ritonavir BID plus emtricitabine/tenofovir QD in treatment-naïve HIV-1 infected adults.~Blood samples for HIV-1 RNA viral load measurement were collected at the Week 48 clinic visit. The number of participants with HIV-1 RNA results <50 copies/mL and the number of participants with HIV-1 RNA results <400 copies/mL are reported." (NCT00105079)
Timeframe: Week 48

,
Interventionparticipants (Number)
Patients with <50 Copies/mLPatients with <400 Copies/mL
Lopinavir/Ritonavir108127
Saquinavir/Ritonavir108121

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Number of Patients With Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Viral Load <50 Copies/mL

"The primary objective of this study was to evaluate the efficacy of saquinavir/ritonavir BID plus emtricitabine/tenofovir QD versus lopinavir/ritonavir BID plus emtricitabine/tenofovir QD in treatment-naïve HIV-1 infected adults.~Blood samples for HIV-1 RNA viral load measurement were collected at the Week 48 clinic visit. The number of participants with HIV-1 RNA results <50 copies/mL is reported." (NCT00105079)
Timeframe: Week 48

,
Interventionparticipants (Number)
Pts. with HIV-1 RNA Viral Load <50 copies/mL - YESPts. with HIV-1 RNA Viral Load <50 copies/mL - NO
Lopinavir/Ritonavir10862
Saquinavir/Ritonavir10859

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Number of Participants Assessed for Adverse Events (AEs)

Detailed information for Adverse Events and Serious Adverse Events will be represented in the SAE/AE section of PRS. (NCT00105079)
Timeframe: reported up to 28 days after the last dose of study treatment. (Up to 52 weeks)

Interventionparticipants (Number)
Saquinavir/Ritonavir163
Lopinavir/Ritonavir168

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The Proportion of Women Who Develop One or More New NVP Resistance Mutations as Identified by Consensus Sequencing or Oligonucleotide Ligation Assay in Plasma (Sampling Was Done at Days 10,21,30, and Weeks 5,6, and 8 Postpartum).

The incidence of new NVP resistance mutation in plasma HIV within 8 weeks postpartum in each randomized arm was estimated using an exact binomial confidence interval. If a resistance mutation was detected at any of the timepoints then an endpoint was met. Samples with VL <500 copies/mL were considered free of mutations. If a resistance result was missing for reasons other than VL <500 copies/ml (e.g.missed visit), it was conservatively imputed as resistant in the primary analysis. (NCT00109590)
Timeframe: within 8 weeks postpartum.

Interventionpercent of participants (Number)
Arm A : LPV/r x 7d7.1
Arm B : no LPV/r12.5
Arm C: LPV/r x 30d5.3

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Area Under the Curve Pharmacokinetic Outcome for LPV/r. (AUC ug*hr/mL)

Data was analyzed with WinNonLin (Version 5.2, Pharsight, USA) using non-compartmental methods. The pharmacokinetic parameters were calculated using the linear-trapezoidal rule. Cpredose and C4hour at the two measurement times were compared within-subject using the Wilcoxon signed-rank test. (NCT00109590)
Timeframe: Within 72 hours postpartum and during the first 30 days postpartum

Interventionug*hr/mL (Median)
Within 72 Hrs Ppm99.7
At Day 30 PpmNA

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Four (4) Hour Concentration Pharmacokinetic Outcome for LPV/r (C4hour ug/mL).

Data was analyzed with WinNonLin (Version 5.2, Pharsight, USA) using non-compartmental methods. The pharmacokinetic parameters were calculated using the linear-trapezoidal rule. Cpredose and C4hour at the two measurement times were compared within-subject using the Wilcoxon signed-rank test. (NCT00109590)
Timeframe: Within 72 hours postpartum and during the first 30 days postpartum

Interventionug/mL (Median)
Within 72 Hrs Ppm10.78
At Day 30 Ppm12.96

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Maximum Concentration Pharmacokinetic Outcome for LPV/r (Cmax ug/mL) .

Data was analyzed with WinNonLin (Version 5.2, Pharsight, USA) using non-compartmental methods. The pharmacokinetic parameters were calculated using the linear-trapezoidal rule. Cpredose and C4hour at the two measurement times were compared within-subject using the Wilcoxon signed-rank test. (NCT00109590)
Timeframe: Within 72 hours postpartum and during the first 30 days postpartum

Interventionug/mL (Median)
Within 72 Hrs Ppm11.2
At Day 30 PpmNA

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Median HIV-1 Viral Load at 24 Weeks Postpartum in Women

(NCT00109590)
Timeframe: at 24 weeks postpartum

Interventionlog10 copies/mL (Median)
Arm A : LPV/r x 7d4.3
Arm B : no LPV/r3.9
Arm C: LPV/r x 30d4.0

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Pre-dose Concentration Pharmacokinetic Outcome for LPV/r (Cpredose ug/mL).

Data was analyzed with WinNonLin (Version 5.2, Pharsight, USA) using non-compartmental methods. The pharmacokinetic parameters were calculated using the linear-trapezoidal rule. Cpredose and C4hour at the two measurement times were compared within-subject using the Wilcoxon signed-rank test. (NCT00109590)
Timeframe: Within 72 hours postpartum and during the first 30 days postpartum

Interventionug/mL (Median)
Within 72 Hrs Ppm6.08
At Day 30 Ppm9.17

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Resistance Mutations in HIV Infected Infants

Resistance mutations as identified by consensus sequencing or OLA (NCT00109590)
Timeframe: 24 weeks postpartum

Interventionparticipants (Number)
Arm B : no LPV/r0
Arm C: LPV/r x 30d0

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The Proportion of Women in Each Randomized Arm Who Have One or More New NVP Resistance Mutations as Identified by Consensus Sequencing or Oligonucleotide Ligation Assay (OLA) in Plasma

The incidence of new NVP resistance mutations at day 10 or week 6 postpartum in each randomized arm. Samples with viral load <500 copies/mL were considered free of mutations. If a resistance result was missing for reasons other than VL <500 copies/ml it was conservatively imputed as resistant in the primary analysis. (NCT00109590)
Timeframe: at Day 10 or Week 6 postpartum.

Interventionpercent of participants (Number)
Arm A : LPV/r x 7d3.6
Arm B : no LPV/r7.1
Arm C : LPV/r x 30d5.3

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The Proportion of Women in Each Randomized Arm Who Have One or More New NVP Resistance Mutations for the Subgroup of Women With Plasma HIV RNA >= 500 Copies/ml At Entry

The incidence of new NVP resistance mutations at day 10 or week 6 postpartum in each randomized arm. Samples with viral load <500 copies/mL were considered free of mutations. If a resistance result was missing for reasons other than VL <500 copies/ml it was conservatively imputed as resistant in the primary analysis. (NCT00109590)
Timeframe: at Day 10 or Week 6 postpartum.

Interventionpercent of participants (Number)
Arm A: LPV/r x 7d4.9
Arm B: no LPV/r9.5
Arm C : LPV/r x 30d7.0

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Proportion of Women With New NVP Resistance Mutation Within 8 Weeks Postpartum Who Had a NVP Resistance Mutation Detected at 72 Weeks Postpartum.

Resistance mutations as identified by OLA in plasma samples or PBMC at 72 weeks postpartum amongst women who had new NVP resistance mutations within 8 weeks postpatrum. These results were based on the 13 women who developed a new NVP resistance mutation in the first 8 weeks postpartum. For the primary outcome measure 1, one particpant in arm A was unavailable for follow-up after week 5 and was conservatively imputed to have developed resistance mutation. (NCT00109590)
Timeframe: within 72 weeks postpartum

,,
Interventionparticipants (Number)
OLA in plasma samplesOLA in PBMC
Arm A : LPV/r x 7d00
Arm B : no LPV/r00
Arm C: LPV/r x 30d01

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The Proportion of Women With Any New ZDV, ddI, or LPV/r Resistance Mutations.

(NCT00109590)
Timeframe: At Week 5 postpartum (ZDV) and at the first timepoint with viral load >=500 copies/ml after treatment discontinuation (ddI and LPV/r).

,,
Interventionpercent of participants (Number)
The proportion of women with new ZDV resistanceThe proportion of women with new ddI resistanceThe proportion of women with new LPV/r resistance
Arm A : LPV/r x 7d000
Arm B : no LPV/r1.7800
Arm C: LPV/r x 30d000

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Number of Women With Grade >=3 Events After Start of Study Treatment

Adverse events were graded using the Division of AIDS (DAIDS) Table for Grading > the Severity of Adult and Pediatric Adverse Events (December 2004). All grade 3 and higher signs, symptoms, and laboratory toxicities (and events of any grade that led to a change in study treatment) were included. (NCT00109590)
Timeframe: After start of study Treatment (postpartum)

Interventionparticipants (Number)
Arm A : LPV/r x 7d2
Arm B : no LPV/r0
Arm C: LPV/r x 30d2

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Rates of ex Vivo T Cell Apoptosis: CD4+ Memory Cell Population [6 Months]

(NCT00145795)
Timeframe: 6 months

Interventionpercent apoptosis (Mean)
Kaletra + Current Dual NRTI Backbone14.10
Current Regimen17.94

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Rates of ex Vivo T Cell Apoptosis: CD4+ Memory Cell Population [3 Months]

Ex vivo T cell apoptosis can be assessed many different ways. The use of propidium iodide staining to determine the proportion of isolated cells that have undergone apoptosis after ex vivo incubation is a standard method that has been used by many investigators. Apoptotic cells intercalate less PI into their DNA, and on flow cytometry, this cell population is identified by a decrease in mean fluorescence (shift to the left). We have experience with this assay, and we have published on the use of method for determining rates of ex vivo apoptosis for different immune effector cells. (NCT00145795)
Timeframe: 3 months

Interventionpercent apoptosis (Mean)
Kaletra + Current Dual NRTI Backbone15.27
Current Regimen24.53

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Immune Reconstitution [6 Months]

Immune reconstitution is defined as the absolute CD4+ lymphocyte count after 6 months of therapy. Absolute CD4+ T cell count, our measure of immune recovery, was assessed in the clinical laboratory using fluorescent labeled monoclonal antibodies to the CD4 on lymphocytes. This is the main target cell for HIV infection. The absolute CD4+ T cell count is also the only clinically validated surrogate marker of immune dysfunction in HIV. CD4+ count is also our best predictor of morbidity and mortality outcomes. (NCT00145795)
Timeframe: 6 months

Interventioncells per cubic millimeter (Mean)
Kaletra + Current Dual NRTI Backbone116
Current Regimen32

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Immune Reconstitution [3 Months]

Immune reconstitution is defined as the absolute CD4+ lymphocyte count after 3 months of therapy. Absolute CD4+ T cell count, our measure of immune recovery, was assessed in the clinical laboratory using fluorescent labeled monoclonal antibodies to the CD4 on lymphocytes. This is the main target cell for HIV infection. The absolute CD4+ T cell count is also the only clinically validated surrogate marker of immune dysfunction in HIV. CD4+ count is also our best predictor of morbidity and mortality outcomes. (NCT00145795)
Timeframe: 3 months

Interventioncells per cubic millimeter (Mean)
Kaletra + Current Dual NRTI Backbone41.56
Current Regimen49.40

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Rates of ex Vivo T Cell Apoptosis: CD4+ naïve Cell Population [3 Months]

Ex vivo T cell apoptosis can be assessed many different ways. The use of propidium iodide staining to determine the proportion of isolated cells that have undergone apoptosis after ex vivo incubation is a standard method that has been used by many investigators. Apoptotic cells intercalate less PI into their DNA, and on flow cytometry, this cell population is identified by a decrease in mean fluorescence (shift to the left). We have experience with this assay, and we have published on the use of method for determining rates of ex vivo apoptosis for different immune effector cells. (NCT00145795)
Timeframe: 3 months

Interventionpercent apoptosis (Mean)
Kaletra + Current Dual NRTI Backbone16.60
Current Regimen22.53

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Rates of Virologic Failure

Virologic failure defined as HIV RNA > 2,000 copies/mL (NCT00145795)
Timeframe: 6 months

Interventionpercentage of randomized subjects (Number)
Kaletra + Current Dual NRTI Backbone0
Current Regimen0

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Rates of ex Vivo T Cell Apoptosis: CD8+ Cell Population [6 Months]

(NCT00145795)
Timeframe: 6 months

Interventionpercent apoptosis (Mean)
Kaletra + Current Dual NRTI Backbone17.07
Current Regimen19.01

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Rates of ex Vivo T Cell Apoptosis: CD8+ Cell Population [3 Months]

(NCT00145795)
Timeframe: 3 months

Interventionpercent apoptosis (Mean)
Kaletra + Current Dual NRTI Backbone20.92
Current Regimen16.74

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Rates of ex Vivo T Cell Apoptosis: CD4+ naïve Cell Population [6 Months]

(NCT00145795)
Timeframe: 6 months

Interventionpercent apoptosis (Mean)
Kaletra + Current Dual NRTI Backbone10.03
Current Regimen18.92

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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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Percentage of Subjects With Plasma Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Levels < 50 Copies/mL at Week 96

(NCT00262522)
Timeframe: Week 96 (End of Study)

InterventionPercentage of Subjects (Number)
LPV/r 800/200 mg QD Tablet64.9
LPV/r 400/100 mg BID Tablet69.2

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Mean Change From Baseline to Week 96 in CD4+ T Cell Counts

(NCT00262522)
Timeframe: Week 96 (End of Study)

Interventioncells/microliter (Mean)
LPV/r 800/200 mg QD Tablet238.4
LPV/r 400/100 mg BID Tablet254.0

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Percentage of Subjects With Plasma Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Levels < 50 Copies/mL at Week 48

(NCT00262522)
Timeframe: Week 48

InterventionPercentage of Subjects (Number)
LPV/r 800/200 mg QD Tablet77.2
LPV/r 400/100 mg BID Tablet75.8

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Percentage of Subjects With Adverse Events of Diarrhea During the First 8 Weeks

(NCT00262522)
Timeframe: Week 8

InterventionPercentage of Subjects (Number)
LPV/r 800/200 mg QD Tablet49.1
LPV/r 800/200 mg QD SGC (Through Week 8)54.8
LPV/r 400/100 mg BID Tablet44.6
LPV/r 400/100 mg BID SGC (Through Week 8)49.7

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Number of Participants With Virologic Suppression

Suppression of the plasma HIV-1 RNA level to less than 400 copies per milliliter (NCT00270296)
Timeframe: Throughout study, including breastfeeding, assessed up to 24 months

InterventionParticipants (Count of Participants)
TZV Arm274
Kaletra Arm256
NVP Arm160

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Number of HIV+ Infants

Number of infants with HIV-positive status (NCT00270296)
Timeframe: Throughout study, including breastfeeding, assessed up to 24 months

InterventionInfants (Number)
TZV Arm6
Kaletra Arm1
NVP Arm1

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Percent of Participants Experiencing Virologic Failure

Virologic failure is defined as a confirmed plasma HIV-1 RNA level that is <1 log10 copies/mL below the study entry value at 12 to 24 weeks after treatment is initiated OR a confirmed plasma HIV-1 RNA level >400 copies/mL at 24 weeks OR death on or before 24 weeks. Results report percent of participants reaching a virologic failure endpoint by week 24 calculated using the Kaplan-Meier method. (NCT00307151)
Timeframe: Earlier of 24 weeks or date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009; Coh II: October 27, 2010)

InterventionPercent of participants (Number)
Coh I: NVP27.4
Coh I: LPV/r10.4
Coh II: NVP28.6
Coh II: LPV/r12.9

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Percent of Participants With Treatment Failure, Defined as a Confirmed Virologic Failure or Permanent Discontinuation of the Randomized NNRTI or PI Component of Study Treatment

Treatment failure is defined as a confirmed plasma HIV-1 RNA level that is <1 log10 copies/mL below the study entry value at 12 to 24 weeks after treatment is initiated OR a confirmed plasma HIV-1 RNA level >400 copies/mL at 24 weeks OR permanent discontinuation of the randomized NNRTI or PI component of study treatment at or prior to 24 weeks of treatment for any reason including death. Results report percent of participants reaching a treatment failure endpoint by week 24 calculated using the Kaplan-Meier method. (NCT00307151)
Timeframe: Earlier of 24 weeks or date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009; Coh II: October 27, 2010)

InterventionPercent of participants (Number)
Coh I: NVP39.6
Coh I: LPV/r21.7
Coh II: NVP40.8
Coh II: LPV/r19.3

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Time From Randomization to Death

Results report 2nd percentile of time from randomization to death (NCT00307151)
Timeframe: Until date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009 - median follow-up 48 weeks and range 0 - 125 weeks; Coh II: October 27, 2010 - median follow-up 72 weeks and range from 0 to 204 weeks)

InterventionWeeks (Number)
Coh I: NVP11
Coh I: LPV/r3
Coh II: NVP2
Coh II: LPV/r83

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Time From Randomization to Treatment Failure, Defined as Virologic Failure or Permanent Discontinuation of the Randomized NNRTI or PI Component of Study Treatment

Treatment failure is defined as a confirmed plasma HIV-1 RNA level that is <1 log10 copies/mL below the study entry value at 12 to 24 weeks after treatment is initiated OR a confirmed plasma HIV-1 RNA level >400 copies/mL at 24 weeks OR a confirmed viral rebound >4000 copies/mL after week 24 OR permanent discontinuation of the randomized NNRTI or PI component of study treatment for any reason including death. (NCT00307151)
Timeframe: Until date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009 - median follow-up 48 weeks and range 0 - 125 weeks; Coh II: October 27, 2010 - median follow-up 72 weeks and range from 0 to 204 weeks)

,,,
InterventionWeeks (Number)
10th percentile25th percentile
Coh I: LPV/r436
Coh I: NVP1216
Coh II: LPV/r1436
Coh II: NVP416

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Time From Randomization to Virologic Failure

Virologic failure is defined as the earlier of a confirmed plasma HIV-1 RNA level that is <1 log10 copies/mL below the study entry value at 12 to 24 weeks after treatment is initiated OR a confirmed plasma HIV-1 RNA level >400 copies/mL at 24 weeks OR a confirmed viral rebound >4000 copies/mL after week 24 OR death. (NCT00307151)
Timeframe: Until date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009 - median follow-up 48 weeks and range 0 - 125 weeks; Coh II: October 27, 2010 - median follow-up 72 weeks and range from 0 to 204 weeks)

,,,
InterventionWeeks (Number)
5th percentile10th percentile
Coh I: LPV/r1624
Coh I: NVP1212
Coh II: LPV/r1624
Coh II: NVP1216

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Time From Start of Study Treatment to First New Grade >=3 Lab Abnormality, Sign or Symptom Occurring on Study Treatment

Safety events include lab abnormalities, signs or symptoms of grade 3 or higher. Events were graded according to the Division of AIDS Table for Grading Severity of Adult and Pediatric Adverse Events, Version 1.0. Events defined as new if first occurrence was after initiation of study treatment or if severity increased from entry and while on the NNRTI or PI component of study treatment. (NCT00307151)
Timeframe: On randomized NNRTI or PI component of study treatment and until date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009; Coh II: October 27, 2010)

,,,
InterventionWeeks (Number)
10th percentile25th percentile
Coh I: LPV/r836
Coh I: NVP424
Coh II: LPV/r412
Coh II: NVP34

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Number of Participants Developing New NRTI, NNRTI or PI-resistant Virus

Numbers of participants developing new NRTI, NNRTI or PI-resistant virus after reaching a virologic failure endpoint (NCT00307151)
Timeframe: Until date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009 - median follow-up 48 weeks and range 0 - 125 weeks; Coh II: October 27, 2010 - median follow-up 72 weeks and range from 0 to 204 weeks)

Interventionparticipants (Number)
Coh I: NVP16
Coh I: LPV/r1
Coh II: NVP10
Coh II: LPV/r4

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Change in CD4 Percent From Entry to Week 48

Change was calculated as CD4 percent at week 48 minus entry CD4 percent (last CD4 percent before randomization date). Only subjects who reached 48 weeks of follow-up before DSMB decisions to unblind each Cohort were included in summary. (NCT00307151)
Timeframe: 48 weeks if before date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009; Coh II: October 27, 2010)

InterventionPercent of CD4 (Mean)
Coh I: NVP13.9
Coh I: LPV/r12.0
Coh II: NVP15.2
Coh II: LPV/r14.3

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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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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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Probability of Grade 3 or 4 Sign or Symptom, or Laboratory Toxicity Over 24 Weeks on Study.

Probability of Grade 3 or 4 sign or symptom, or laboratory toxicity over 24 weeks on study using Kaplan-Meier estimates of the cumulative probability of Grade 3 or 4 sign or symptom, or laboratory toxicity at week 24. Grading of adverse events (signs and symptoms and laboratory toxicities) was according to Division of AIDS Table for Grading the Severity of Adult and Pediatric Adverse Events, Version 1.0, December 2004. (NCT00357552)
Timeframe: From study entry to week 24

Interventioncumulative probability of grade 3 or 4 (Number)
LPV/r Monotherapy0.23

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Percentage of Subjects Reporting Not Skipping Medications in the Last Month.

The percentage of subjects reporting never missing medications in the last month. (NCT00357552)
Timeframe: Study entry and weeks 2, 4, 8, 12, 16, 20, and 24

Interventionpercentage of subjects with data (Number)
week 2 (N=120)week 4 (N=121)week 8 (N=123)week 12 (N=123)week 16 (N=122)week 20 (N=120)week 24 (N=122)
LPV/r Monotherapy9086.887.886.286.190.989.4

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Proportion of Participants With Plasma HIV-1 RNA Levels < 400 Copies/mL From Baseline to Week 104

(NCT00357552)
Timeframe: At Weeks 0, 12, 16, 20, 24, 32, 40, 48, 56, 68, 80, 92, 104

Interventionproportion of participants (Number)
week 0 (N=123)week 12 (N=122)week 16 (N=121)week 20 (N=115)week 24 (N=122)week 32 (N=121)week 40 (N=118)week 48 (N=118)week 56 (N=120)week 68 (N=116)week 80 (N=117)week 92 (N=116)week 104 (N=117)
LPV/r Monotherapy0.020.750.870.840.840.830.840.870.860.910.850.870.89

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Number of Screened Subjects With at Least One NNRTI, or NRTI-associated Resistance Mutation at A5230 Screening.

Number of screened subjects with at least one NNRTI, or NRTI-associated resistance mutation. Resistance interpretations used the November 30, 2011 Stanford algorithm. (NCT00357552)
Timeframe: Screening

Interventionnumber of screened subjects (Number)
At least one NNRTI-associated mutationAt least one NRTI-associated mutation
All Screened Subjects With Available Sequences201197

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Level of HIV-1 RNA as Ascertained From Paired DBS and Plasma

Proportion of DBS samples with HIV-1 RNA level <= 400 copies/mL, proportion of plasma samples with HIV-1 RNA level <= 400 copies/mL and proportion of paired DBS and plasma samples that are concordant (both <= 400 copies/mL or both > 400 copies/mL). Results are pooled over 4 different storage temperature conditions (-80C, -20C, 4C and room temperature). (NCT00357552)
Timeframe: At study entry and weeks 24 and 48

Interventionproportion of samples (Number)
study entry DBS <= 400 cp/mLstudy entry plasma <= 400 cp/mLstudy entry DBS & plasma concordanceweek 24 DBS <= 400 cp/mLweek 24 plasma <= 400 cp/mLweek 24 DBS & plasma concordanceweek 48 DBS <= 400 cp/mLweek 48 plasma <= 400 cp/mLweek 48 DBS & plasma concordance
LPV/r Monotherapy0.170.000.830.820.800.800.940.910.97

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Time to Treatment Failure, Defined as the First Occurrence of Death, Disease Progression, or Virologic Failure.

25th percentile in weeks from study entry to treatment failure, defined as the first occurrence of death, disease progression, or virologic failure. Virologic failure was defined as HIV-1 >= 400 copies/mL after week 24 or 2 consecutive HIV-1 RNA >= 400 copies/mL after week 16 following suppression on LPV/r monotherapy. (NCT00357552)
Timeframe: Study entry to Week 104

Interventionweeks (Number)
LPV/r Monotherapy48.0

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Time to First New Grade 3 or 4 Sign or Symptom or Laboratory Toxicity Following LPV/r Intensification

25th percentile in weeks from study entry to first new grade 3 or 4 sign or symptom or laboratory toxicity following LPV/r intensification. Grading of adverse events (signs and symptoms and laboratory toxicities) was according to Division of AIDS Table for Grading the Severity of Adult and Pediatric Adverse Events, Version 1.0, December 2004. (NCT00357552)
Timeframe: From LPV/r intensification to week 104

Interventionweeks (Number)
LPV/r Monotherapy26.0

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Percentage of Enrolled Participants With Virologic Success at Week 24 on LPV/r Monotherapy

Virologic success at week 24 on LPV/r monotherapy was defined as remaining on LPV/r monotherapy at week 24 without prior virologic failure. Virologic failure was met with either of these two conditions: (i) failure to suppress HIV-1 RNA to < 400 copies/mL by week 24 or (ii) confirmed HIV-1 RNA >= 400 copies/mL after confirmed HIV-1 RNA < 400 copies/mL. (NCT00357552)
Timeframe: From study entry to week 24

Interventionpercentage of enrolled subjects (Number)
LPV/r Monotherapy87

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Number of Subjects With at Least One New PI-associated Resistance Mutation at Time of Virologic Failure.

Number of subjects with at least one new PI-associated resistance mutation at time of virologic failure. Resistance interpretations used the May 6, 2009 Stanford algorithm. (NCT00357552)
Timeframe: At time of virologic failure

Interventionparticipants (Number)
Virologic Failures by Week 24.2

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Number of Participants With Study-targeted Diagnoses and Clinical Events

Cardiac disorders, Infections and infestations, Metabolism and nutrition disorders, Neoplasms benign, malignant and unspecified (including cysts and polyps), Pregnancy, puerperium and perinatal conditions, Vascular disorders, were specified a priori as study-targeted events by the study chair. (NCT00357552)
Timeframe: Study entry to week 104

Interventionparticipants (Number)
LPV/r Monotherapy39

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Change in CD4+ Cell Counts From Study Entry to Week 104

(NCT00357552)
Timeframe: Study entry and week 104

Interventioncells/mm^3 (Median)
LPV/r Monotherapy213

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Percentage of Participants With New Primary Protease Mutations at Week 48

Emergence of new primary protease inhibitor mutations (i.e., mutations at codons 30, 32, 48, 50, 82, 84, and 90 that were not present at baseline). (NCT00358917)
Timeframe: Week 48 (End of Study)

InterventionPercentage of Participants (Number)
LPV/r 800/200 mg QD Tablet8.0
LPV/r 400/100 mg BID Tablet15.6

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Percentage of Participants With Plasma Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Levels < 50 Copies/Milliliter (mL) at Week 48

(NCT00358917)
Timeframe: Week 48 (End of Study)

InterventionPercentage of Participants (Number)
LPV/r 800/200 mg QD Tablet76.0
LPV/r 400/100 mg BID Tablet72.2

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Virologic Response (HIV-1 RNA <50 Copies/mL) at Week 48 for Participants With 0-2 Protease Inhibitor Substitutions at Baseline Associated With Reduced Response to Lopinavir/Ritonavir

Substitutions considered in the analysis were L10F/I/R/V, K20M/N/R, L24I, L33F, M36I, I47V, G48V, I54L/T/V, V82A/C/F/S/T, and I84V as defined in the proposed United States Package Insert. (NCT00358917)
Timeframe: Week 48 (End of Study)

InterventionPercentage of Participants (Number)
LPV/r 800/200 mg QD Tablet65.5
LPV/r 400/100 mg BID Tablet61.6

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Percentage of Participants Responding at Week 48 Based on the Food and Drug Administration (FDA) Time to Loss of Virologic Response (TLOVR) Algorithm

A participant was classified as a responder at the first of 2 consecutive human immunodeficiency virus type 1 (HIV-1) ribonucleic acid (RNA) levels <50 copies/mL. The participant continued to be a responder until 2 consecutive values >=50 copies/mL were reached, until the final value if that value was >=50 copies/mL, or until discontinuation or death. (NCT00358917)
Timeframe: Week 48 (End of Study)

InterventionPercentage of Participants (Number)
LPV/r 800/200 mg QD Tablet55.3
LPV/r 400/100 mg BID Tablet51.8

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Mean Change From Baseline to Week 48 in Cluster of Differentiation 4 Single-Positive Thymocyte (CD4+ T) Cell Counts

(NCT00358917)
Timeframe: Week 48 (End of Study)

Interventioncells/microliter (Mean)
LPV/r 800/200 mg QD Tablet135.3
LPV/r 400/100 mg BID Tablet121.5

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Fasting Glucose

6 month mean and standard deviation for fasting glucose. (NCT00413153)
Timeframe: 6 months

Interventionmg/dL (Mean)
Boosted Reyataz (ATV/r)84
Continue Kaletra (LPV/r)90

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Immune Parameters -- CD4 Count

6 month mean and standard deviation for CD4+ count. (NCT00413153)
Timeframe: 6 months

Interventioncells/microL (Mean)
Boosted Reyataz (ATV/r)432
Continue Kaletra (LPV/r)688

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Insulin Sensitivity

6 month mean and standard deviation for insulin-stimulated glucose uptake (M) per unit insulin at 120 minutes as measured by euglycemic hyperinsulinemic clamp. (NCT00413153)
Timeframe: 6 months

Interventionumol/kg/min per uU/mL insulin (Mean)
Boosted Reyataz (ATV/r)39.0
Continue Kaletra (LPV/r)49.2

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Lipid Metabolism - Serum Triglyceride

6 month mean and standard deviation for serum triglyceride. (NCT00413153)
Timeframe: 6 months

Interventionmg/dL (Mean)
Boosted Reyataz (ATV/r)147
Continue Kaletra (LPV/r)209

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Liver Enzymes -- Alanine Aminotransferase (ALT)

6 month mean and standard deviation for ALT. (NCT00413153)
Timeframe: 6 months

InterventionU/L (Mean)
Boosted Reyataz (ATV/r)61
Continue Kaletra (LPV/r)65

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Liver Enzymes -- Aspartate Aminotransferase (AST)

6 month mean and standard deviation for AST. (NCT00413153)
Timeframe: 6 months

InterventionU/L (Mean)
Boosted Reyataz (ATV/r)39
Continue Kaletra (LPV/r)42

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Total Bilirubin

6 month mean and standard deviation for total bilirubin. (NCT00413153)
Timeframe: 6 months

Interventionmg/dL (Mean)
Boosted Reyataz (ATV/r)2.8
Continue Kaletra (LPV/r)0.6

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Body Composition - Visceral Adipose Tissue

6 month mean and standard deviation for visceral adipose tissue (VAT) as measured by single slice computed tomography (CT) scan at the L4 pedicle (pedicle of 4th lumbar vertebra). (NCT00413153)
Timeframe: 6 months

Interventionsquare centimeters (Mean)
Boosted Reyataz (ATV/r)91
Continue Kaletra (LPV/r)167

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Glucose Trafficking

"6 month mean and standard deviation for glucose uptake into anterior thigh muscle as measured by FDG/PET scanning during euglycemic hyperinsulinemic clamp. During the hyperinsulinemic conditions of the clamp, glucose and 18-FDG [labeled glucose] are taken up by muscle. The quantity of 18-FDG taken up is measured by the PET scan. Although there are no well-accepted norms for this measurement, a higher value indicates that more glucose is being taken up by (or trafficked to) muscle. Increased uptake of glucose indicates increased muscle insulin sensitivity." (NCT00413153)
Timeframe: 6 months

Interventionumol/kg/min (Mean)
Boosted Reyataz (ATV/r)26.7
Continue Kaletra (LPV/r)24.4

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Viral Set Point

set point is reached after the immune system has developed HIV antibodies and begins to attempt to fight the virus (NCT00414518)
Timeframe: Throughout study

InterventionLog 10 copies virus/ml (Mean)
12 Week Treatment Folllowed by Treatment Interruption4.8627
CD4 T Cell Guided Therapy4.2434

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Plasma HIV-1 Viral Load (Copies/ml) at Week 24 as Compared Between the Two Arms

(NCT00414518)
Timeframe: At Week 24

InterventionLog 10 copies of virus/ml (Mean)
12 Week Treatment Arm Followed by Treatment Interruption4.8627
CD4 T Cell Guided Therapyh4.2620

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Number of Participants Experiencing Either an AIDS-defining Event, a Grade 3 or 4 Adverse Event, or Acute Retroviral Syndrome

(NCT00414518)
Timeframe: At Week 24

Interventionparticipants (Number)
Arm A1
Arm B1

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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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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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Incidence of Mortality

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

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

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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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Number of Patients With Serious LAEs Through 24 Weeks

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 (NCT00443703)
Timeframe: 24 Week last patient last visit

,
Interventionparticipants (Number)
With LAEsWithout LAEs
KALETRA™ 400/100 mg b.i.d.0174
MK0518 400 mg b.i.d.0174

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Number of Patients With Clinical Adverse Experiences (CAEs) Through 24 Weeks

An adverse experience 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 (Merck & Co., Inc.) product, whether or not considered related to the use of the product (NCT00443703)
Timeframe: 24 Week last patient last visit

,
InterventionParticipants (Number)
With CAEsWithout CAEs
KALETRA™ 400/100 mg b.i.d.10668
MK0518 400 mg b.i.d.10965

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Mean Percent Change From Baseline in Fasting Serum Cholesterol at Week 12

(NCT00443703)
Timeframe: Baseline and Week 12

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-12.83
KALETRA™ 400/100 mg b.i.d.0.70

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Mean Percent Change From Baseline in Fasting Serum Cholesterol at Week 24

(NCT00443703)
Timeframe: Baseline and Week 24

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-13.81
KALETRA™ 400/100 mg b.i.d.2.70

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Mean Percent Change From Baseline in Fasting Serum High-Density Lipoprotein Cholesterol (HDL-C) at Week 12

(NCT00443703)
Timeframe: Baseline and Week 12

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-0.86
KALETRA™ 400/100 mg b.i.d.0.78

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Mean Percent Change From Baseline in Fasting Serum High-Density Lipoprotein Cholesterol (HDL-C) at Week 24

(NCT00443703)
Timeframe: Baseline and Week 24

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-4.42
KALETRA™ 400/100 mg b.i.d.-1.70

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Mean Percent Change From Baseline in Fasting Serum Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12

(NCT00443703)
Timeframe: Baseline and Week 12

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-2.43
KALETRA™ 400/100 mg b.i.d.2.05

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Mean Percent Change From Baseline in Fasting Serum Low-Density Lipoprotein Cholesterol (LDL-C) at Week 24

(NCT00443703)
Timeframe: Baseline and Week 24

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-1.12
KALETRA™ 400/100 mg b.i.d.8.54

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Mean Percent Change From Baseline in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C) at Week 12

(NCT00443703)
Timeframe: Baseline and Week 12

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-15.17
KALETRA™ 400/100 mg b.i.d.2.31

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Mean Percent Change From Baseline in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24

(NCT00443703)
Timeframe: Baseline and Week 24

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-15.03
KALETRA™ 400/100 mg b.i.d.5.53

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Median Percent Change From Baseline in Serum Triglyceride at Week 12

Standard Deviation (Robust): calculated as interquartile range (IQR)/1.075, where IQR=3rd quartile-1st quartile. (NCT00443703)
Timeframe: Baseline and Week 12

InterventionPercent Change (Median)
MK0518 400 mg b.i.d.-41.50
KALETRA™ 400/100 mg b.i.d.3.56

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Median Percent Change From Baseline in Serum Triglyceride at Week 24

Standard Deviation (Robust): calculated as interquartile range (IQR)/1.075, where IQR=3rd quartile-1st quartile. (NCT00443703)
Timeframe: Baseline and Week 24

InterventionPercent Change (Median)
MK0518 400 mg b.i.d.-44.53
KALETRA™ 400/100 mg b.i.d.6.14

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Number of Patients With Plasma Human Immunodeficiency Virus (HIV) RiboNucleic Acid (RNA) <50 Copies/mL at Week 24

(NCT00443703)
Timeframe: Week 24

InterventionParticipants (Number)
MK0518 400 mg b.i.d.139
KALETRA™ 400/100 mg b.i.d.152

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Number of Patients That Died by 24 Week Last Patient Last Visit

(NCT00443703)
Timeframe: 24 Week last patient last visit

,
Interventionparticipants (Number)
DiedDid Not Die
KALETRA™ 400/100 mg b.i.d.0174
MK0518 400 mg b.i.d.0174

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Number of Patients That Discontinued Due to CAEs Through 24 Weeks

(NCT00443703)
Timeframe: 24 Week last patient last visit

,
Interventionparticipants (Number)
Discontinued with CAEsDid not Discontinue with CAEs
KALETRA™ 400/100 mg b.i.d.4170
MK0518 400 mg b.i.d.4170

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Number of Patients That Discontinued Due to LAEs Through 24 Weeks

(NCT00443703)
Timeframe: 24 Week last patient last visit

,
Interventionparticipants (Number)
Discontinued with LAEsDid Not Discontinue with LAEs
KALETRA™ 400/100 mg b.i.d.1173
MK0518 400 mg b.i.d.2172

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Number of Patients With Laboratory Adverse Experiences (LAEs) Through 24 Weeks

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 (Merck & Co., Inc.) product, whether or not considered related to the use of the product (NCT00443703)
Timeframe: 24 Week last patient last visit

,
Interventionparticipants (Number)
With LAEsWithout LAEs
KALETRA™ 400/100 mg b.i.d.7167
MK0518 400 mg b.i.d.11163

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Number of Patients With Serious CAEs Through 24 Weeks

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 (NCT00443703)
Timeframe: 24 Week last patient last visit

,
Interventionparticipants (Number)
With Serious CAEsWithout Serious CAEs
KALETRA™ 400/100 mg b.i.d.10164
MK0518 400 mg b.i.d.15159

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Mean Percent Change From Baseline in Fasting Serum Cholesterol at Week 12

(NCT00443729)
Timeframe: Baseline and Week 12

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-12.41
KALETRA™ 400/100 mg b.i.d.1.29

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Mean Percent Change From Baseline in Fasting Serum Cholesterol at Week 24

(NCT00443729)
Timeframe: Baseline and Week 24

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-13.64
KALETRA™ 400/100 mg b.i.d.3.55

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Number of Patients With Serious CAEs Through 24 Weeks

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 (NCT00443729)
Timeframe: 24 Week last patient last visit

,
InterventionParticipants (Number)
With Serious CAEsWithout Serious CAEs
KALETRA™ 400/100 mg b.i.d.8170
MK0518 400 mg b.i.d.4172

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Number of Patients With Laboratory Adverse Experiences (LAEs) Through 24 Weeks

(NCT00443729)
Timeframe: 24 Week last patient last visit

,
InterventionParticipants (Number)
With LAEsWithout LAEs
KALETRA™ 400/100 mg b.i.d.6172
MK0518 400 mg b.i.d.8168

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Number of Patients With Clinical Adverse Experiences (CAEs) Through 24 Weeks

(NCT00443729)
Timeframe: 24 Week last patient last visit

,
InterventionParticipants (Number)
With CAEsWithout CAEs
KALETRA™ 400/100 mg b.i.d.11266
MK0518 400 mg b.i.d.12353

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Number of Patients That Discontinued Due to LAEs Through 24 Weeks

(NCT00443729)
Timeframe: 24 Week last patient last visit

,
InterventionParticipants (Number)
Discontinued with LAEsDid Not Discontinue with LAEs
KALETRA™ 400/100 mg b.i.d.0178
MK0518 400 mg b.i.d.0176

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Number of Patients That Discontinued Due to CAEs Through 24 Weeks

(NCT00443729)
Timeframe: 24 Week last patient last visit

,
InterventionParticipants (Number)
Discontinued with CAEsDid Not Discontinue with CAEs
KALETRA™ 400/100 mg b.i.d.0178
MK0518 400 mg b.i.d.0176

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Number of Patients That Died by 24 Week Last Patient Last Visit

(NCT00443729)
Timeframe: 24 Week last patient last visit

,
InterventionParticipants (Number)
DiedDid Not Die
KALETRA™ 400/100 mg b.i.d.0178
MK0518 400 mg b.i.d.0176

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Number of Patients With Plasma Human Immunodeficiency Virus (HIV) RiboNucleic Acid (RNA) <50 Copies/mL at Week 24

(NCT00443729)
Timeframe: 24 Weeks

InterventionParticipants (Number)
MK0518 400 mg b.i.d.154
KALETRA™ 400/100 mg b.i.d.167

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Median Percent Change From Baseline in Serum Triglyceride at Week 24

Standard Deviation (Robust): calculated as interquartile range (IQR)/1.075, where IQR=3rd quartile-1st quartile. (NCT00443729)
Timeframe: Baseline and Week 24

InterventionPercent Change (Median)
MK0518 400 mg b.i.d.-44.50
KALETRA™ 400/100 mg b.i.d.7.06

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Number of Patients With Serious LAEs Through 24 Weeks

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 (NCT00443729)
Timeframe: 24 Week last patient last visit

,
InterventionParticipants (Number)
With LAEsWithout LAEs
KALETRA™ 400/100 mg b.i.d.0178
MK0518 400 mg b.i.d.0176

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Median Percent Change From Baseline in Serum Triglyceride at Week 12

Standard Deviation (Robust): calculated as interquartile range (IQR)/1.075, where IQR=3rd quartile-1st quartile. (NCT00443729)
Timeframe: Baseline and Week 12

InterventionPercent Change (Median)
MK0518 400 mg b.i.d.-42.82
KALETRA™ 400/100 mg b.i.d.8.20

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Mean Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at Week 24

(NCT00443729)
Timeframe: Baseline and Week 24

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-15.83
KALETRA™ 400/100 mg b.i.d.5.26

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Mean Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at Week 12

(NCT00443729)
Timeframe: Baseline and Week 12

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-14.77
KALETRA™ 400/100 mg b.i.d.2.91

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Mean Percent Change From Baseline in Fasting Serum Low-density Lipoprotein Cholesterol (LDL-C) at Week 24

(NCT00443729)
Timeframe: Baseline and Week 24

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.5.12
KALETRA™ 400/100 mg b.i.d.6.06

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Mean Percent Change From Baseline in Fasting Serum Low-density Lipoprotein Cholesterol (LDL-C) at Week 12

(NCT00443729)
Timeframe: Baseline and Week 12

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.3.99
KALETRA™ 400/100 mg b.i.d.0.55

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Mean Percent Change From Baseline in Fasting Serum High-density Lipoprotein Cholesterol (HDL-C) at Week 24

(NCT00443729)
Timeframe: Baseline and Week 24

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-1.77
KALETRA™ 400/100 mg b.i.d.-0.15

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Mean Percent Change From Baseline in Fasting Serum High-density Lipoprotein Cholesterol (HDL-C) at Week 12

(NCT00443729)
Timeframe: Baseline and Week 12

InterventionPercent Change (Mean)
MK0518 400 mg b.i.d.-0.64
KALETRA™ 400/100 mg b.i.d.-2.50

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Gemfibrozil Area Under the Concentration vs. Time Curve (AUC)

AUC (ng*hr/mL) of gemfibrozil when given as a 600 mg dose by itself compared to gemfibrozil AUC after 14.5 days of lopinavir-ritonavir (400mg/100mg) twice daily. (NCT00474201)
Timeframe: 22 days per subject (approximately 1 year for entire study completion)

Interventionng*hr/mL (Geometric Mean)
Gemfibrozil Alone (Control Group)104
Gemfibrozil + Lopinavir-ritonavir62

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Buprenorphine Area Under the Curve With LPV/r (ng/mL*hr)

Pharmacokinetic parameters were determined by use of non compartmental methods. The area under the plasma concentration versus time curve was determined by use of the trapezoidal rule and measured over a 24-hr time period. (NCT00571961)
Timeframe: 15 days

Intervention(ng/mL)*hr (Mean)
Lopinavir Coformulated With Ritonavir (LPV/r), 800mg/200mg46.2

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CD4 Count at Follow-up Visits

CD4 cell count (median, inter-quartile range) (NCT00608569)
Timeframe: At Weeks 4, 12, 24, 36, and 48

,
Interventioncells/mm3 (Median)
Week 4Week 12Week 24Week 36Week 48
mDOT Arm212225268281301
Non-mDOT Arm219235266294347

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Time to First Grade 3 or 4 Lab or Sign/Symptom Event

5th and 10th percentiles in weeks from randomization to first grade 3 or 4 lab or sign/ symptom event (NCT00608569)
Timeframe: 52 weeks since randomization

,
Interventionweeks (Number)
5th percentile10th percentile
mDOT Arm6.424
Non-mDOT Arm2432.6

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Adherence to Second Line HAART Regimen

Number of participants with self-reported 100% adherence over the week prior to study visit (NCT00608569)
Timeframe: At weeks 4, 8, 12, 24, 36, 48 and 52

,
Interventionparticipants (Number)
Week 4Week 8Week 12Week 24Week 48Week 52
mDOT Arm105108114107103104
Non-mDOT Arm117115116116109109

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Time to First Grade 3 or 4 Lab Event

5th and 10th percentiles in weeks from randomization to first grade 3 or 4 lab event (NCT00608569)
Timeframe: 52 weeks since randomization

,
Interventionweeks (Number)
5th percentile10th percentile
mDOT Arm24NA
Non-mDOT ArmNANA

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Confirmed Virologic Failure at or Prior to Week 48

Confirmed virologic failure was defined as two successive HIV-1 RNA measurements at least 24 hours apart that were either:1) <1 log10 copies/mL below the baseline level and >400 copies/mL at the week 12 HIV-1 RNA evaluation (obtained at least 11 weeks after the date of the randomization) 2) >400 copies/mL at or after the week 24 HIV-1 RNA evaluation (obtained at least 23 weeks after the date of randomization). 3) subjects who discontinued the study follow-up for any reason other than study completion, including death, and who did so ≤50 weeks after randomization was considered to be a virologic failure. Number of participants experiencing or not experiencing virologic failure at or prior to week 48 was reported. (NCT00608569)
Timeframe: At or prior to Week 48

,
Interventionparticipants (Number)
No FailureExperienced Failure
mDOT Arm9534
Non-mDOT Arm10523

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Confirmed Virologic Failure at or Prior to Week 24

Confirmed virologic failure was defined as two successive HIV-1 RNA measurements at least 24 hours apart that were either:1) <1 log10 copies/mL below the baseline level and >400 copies/mL at the week 12 HIV-1 RNA evaluation (obtained at least 11 weeks after the date of the randomization) 2) >400 copies/mL at or after the week 24 HIV-1 RNA evaluation (obtained at least 23 weeks after the date of randomization). 3) subjects who discontinued the study follow-up for any reason other than study completion, including death, and who did so ≤30 weeks after randomization was considered to be a virologic failure. Number of participants experiencing or not experiencing virologic failure at or prior to week 24 was reported. (NCT00608569)
Timeframe: At or prior to Week 24

,
Interventionparticipants (Number)
No FailureExperienced Failure
mDOT Arm10524
Non-mDOT Arm11117

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CD8 Count at Follow-up Visits

CD8 cell count (median, inter-quartile range) (NCT00608569)
Timeframe: At week 4, 12, 24, 36, and 48

,
Interventioncells/mm3 (Median)
Week 4Week 12Week 24Week 36Week 48
mDOT Arm776895816787815
Non-mDOT Arm859916818833823

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Time to First Grade 3 or 4 Sign or Symptom

5th and 10th percentiles in weeks from randomization to first grade 3 or 4 sign or symptom (NCT00608569)
Timeframe: 52 weeks since randomization

,
Interventionweeks (Number)
5th percentile10th percentile
mDOT Arm13.7NA
Non-mDOT Arm26.748.9

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Absolute Change in CD4 Cell Counts

(NCT00632970)
Timeframe: 24 and 48 weeks

Interventioncells/mm^3 (Mean)
Raltegravir50
Lopinavir/Ritonavir50

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Time to Confirmed Virologic Failure

time to confirmed viologic failure at 24 weeks (up to 48 weeks) (NCT00654147)
Timeframe: weeks

Interventionweeks (Median)
Raltegravir & Lopinavir/Ritonavir28
Raltegravir & Emtricitabine/Tenofovir29

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Time to Virologic Failure

time to virologic failure at week 24 (up to 48 weeks) (NCT00654147)
Timeframe: week 24 (up to 48 weeks)

Interventionweeks (Median)
Raltegravir & Lopinavir/Ritonavir3.2296
Raltegravir & Emtricitabine/Tenofovir2.9952

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Study Medication Tolerability

study treatment tolerability as measured by number of subjects receiving study treatment who either discontinued or changed any component of study treatment (NCT00654147)
Timeframe: date started study treatment to first week documented change study treatment up to week 48

Interventionparticipants (Number)
Raltegravir & Lopinavir/Ritonavir1
Raltegravir & Emtricitabine/Tenofovir0

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Change From Baseline CD4+ and CD8+ Cell Counts

mean change in CD4+ and CD8+ T-lymphocytes counts from baseline (defined as the average of pre-entry and entry values) at weeks 16 and 24 in the two treatment arms (NCT00654147)
Timeframe: Baseline, Weeks 16 and 24

,
Interventioncells/mm3 (Mean)
week 16 CD4 cellsweek 24 CD4 cells
Raltegravir & Emtricitabine/Tenofovir452.11482.36
Raltegravir & Lopinavir/Ritonavir516.34521.31

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Weeks to HIV-1 RNA <200 Copies/ml

time to viral suppression noted as week on study treatment to attain HIV-1 RNA < 200 copies/ml (NCT00654147)
Timeframe: from date of treatment start to first week documented viral suppression

,
Interventionweek to viral supresssion (Median)
week to <200 Copies/mlweek to <50 Copies/ml
Raltegravir & Emtricitabine/Tenofovir2856
Raltegravir & Lopinavir/Ritonavir2856

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To Compare Plasma Triglyceride Levels at 48 Weeks Between LPV/r + RAL and Standard HAART Treated Subjects

(NCT00700115)
Timeframe: 48 weeks

Interventionmg/dL (Mean)
Kaletra + Isentress238.1
Standard HAART133.3

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Plasma Viral Loads (HIV-1 RNA PCR)

Percentage subjects with undetectable Plasma viral loads (NCT00700115)
Timeframe: baseline to week 48

Interventionpercentage of subjects (Number)
Kaletra + Isentress92.7
Standard HAART88

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Mean Change From Baseline in Alkaline Phosphatase (Units/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionunits/liter (Mean)
LPV/r + FTC/TDF14.5
LPV/r + RAL1.7

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Mean Change From Baseline in Aspartate Aminotransferase (Units/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionunits/liter (Mean)
LPV/r + FTC/TDF-0.8
LPV/r + RAL-9.6

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Mean Change From Baseline in Basophils (x 10^9/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionnumber of cells x 10^9/liter (Mean)
LPV/r + FTC/TDF0.005
LPV/r + RAL0.003

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Mean Change From Baseline in Bicarbonate (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF-0.5
LPV/r + RAL-0.8

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Mean Change From Baseline in Blood Urea Nitrogen (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF0.00
LPV/r + RAL0.37

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Mean Change From Baseline in Calcium (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF-0.040
LPV/r + RAL-0.016

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Mean Change From Baseline in Calculated Creatinine Clearance (Milliliters/Second)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmilliliters/second (Mean)
LPV/r + FTC/TDF-0.122
LPV/r + RAL-0.024

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Mean Change From Baseline in Chest Measurement (cm)

Chest circumference is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. Participant's chest circumference was measured at 5 cm above the xiphoid process using non-stretchable measuring tape with half centimeter marks. (NCT00711009)
Timeframe: Baseline to Week 96

Interventioncm (Mean)
LPV/r + FTC/TDF1.13
LPV/r + RAL4.06

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Mean Change From Baseline in Chloride (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF-0.4
LPV/r + RAL0.2

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Mean Change From Baseline in Cholesterol (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF0.808
LPV/r + RAL1.113

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Mean Change From Baseline in Creatine Phosphokinase (Units/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionunits/liter (Mean)
LPV/r + FTC/TDF398.9
LPV/r + RAL157.2

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Mean Change From Baseline in Creatinine (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF5.7
LPV/r + RAL1.6

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Mean Change From Baseline in DEXA Scan of Lower Extremity Lean Mass (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF1.97
LPV/r + RAL2.27

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Bone Mineral Content (Grams)

The dual energy X-ray absorptiometry (DEXA) scan of bone mineral content was used to evaluate potential bone effects of treatment. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF-3.69
LPV/r + RAL0.52

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Bone Mineral Density (Grams/cm^2)

The dual energy X-ray absorptiometry (DEXA) scan of bone mineral content was used to evaluate potential bone effects of treatment. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams/cm^2 (Mean)
LPV/r + FTC/TDF-2.48
LPV/r + RAL0.68

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Lower Extremity Fat (Grams)

The dual energy X-ray absorptiometry (DEXA) is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF15.32
LPV/r + RAL28.82

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Lower Extremity Total Mass (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF4.32
LPV/r + RAL6.96

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Total Body Fat (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF12.71
LPV/r + RAL25.31

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Total Body Lean Mass (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF1.08
LPV/r + RAL1.56

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Total Body Mass (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF2.9
LPV/r + RAL5.4

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Trunk Fat (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF13.75
LPV/r + RAL27.01

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Trunk Lean Mass (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF1.67
LPV/r + RAL2.56

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Trunk Mass (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF3.48
LPV/r + RAL6.34

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Upper Extremity Fat (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF7.28
LPV/r + RAL21.53

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Upper Extremity Lean Mass (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF-1.49
LPV/r + RAL-1.25

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Mean Change From Baseline in Dual Energy X-ray Absorptiometry (DEXA) Scan of Upper Extremity Total Mass (Grams)

The dual energy X-ray absorptiometry (DEXA) scan is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. (NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams (Mean)
LPV/r + FTC/TDF-0.33
LPV/r + RAL1.52

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Mean Change From Baseline in Eosinophils (x 10^9/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionnumber of cells x 10^9/liter (Mean)
LPV/r + FTC/TDF-0.012
LPV/r + RAL0.015

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Mean Change From Baseline in Fasting Glucose (Millimoles/Liter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionmillimoles/liter (Mean)
LPV/r + FTC/TDF-0.011
LPV/r + RAL0.109

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Mean Change From Baseline in Hematocrit (Fraction)

Hematocrit fraction is the percentage (%) by volume of packed red blood cells (RBCs) in the participant's blood. It was measured using standard clinical laboratory analysis of participants' blood samples. (NCT00711009)
Timeframe: Baseline to Week 96

Intervention% by volume of packed RBCs in blood (Mean)
LPV/r + FTC/TDF0.038
LPV/r + RAL0.036

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Mean Change From Baseline in Hemoglobin (Grams/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams/liter (Mean)
LPV/r + FTC/TDF5.4
LPV/r + RAL5.1

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Mean Change From Baseline in High Density Lipoprotein Cholesterol (HDL) (Micromoles/Liter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF0.257
LPV/r + RAL0.346

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Mean Change From Baseline in Hips Measurement (cm)

Hip circumference is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. Participant was measured at widest width of the hip using non-stretchable measuring tape with half centimeter marks. (NCT00711009)
Timeframe: Baseline to Week 96

Interventioncm (Mean)
LPV/r + FTC/TDF2.45
LPV/r + RAL4.70

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Mean Change From Baseline in Inorganic Phosphate (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF-0.046
LPV/r + RAL-0.028

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Mean Change From Baseline in Insulin (Picomoles/Liter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionpicomoles/liter (Mean)
LPV/r + FTC/TDF-6.724
LPV/r + RAL4.441

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Mean Change From Baseline in Interleukin-6 (Nanograms/Liter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionnanograms/liter (Mean)
LPV/r + FTC/TDF-1.584
LPV/r + RAL-53.286

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Mean Change From Baseline in Lactate (Millimoles/Liter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionmillimoles/liter (Mean)
LPV/r + FTC/TDF0.281
LPV/r + RAL0.444

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Mean Change From Baseline in Lactate Dehydrogenase (Units/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionunits/liter (Mean)
LPV/r + FTC/TDF-21.157
LPV/r + RAL-28.926

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Mean Change From Baseline in Leptin (Nanograms/Milliliter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionnanograms/milliliter (Mean)
LPV/r + FTC/TDF3.623
LPV/r + RAL2.927

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Mean Change From Baseline in Lipase (Units/Liter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionunits/liter (Mean)
LPV/r + FTC/TDF4.674
LPV/r + RAL-1.898

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Mean Change From Baseline in Low Density Lipoprotein (LDL) (Micromoles/Liter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF0.535
LPV/r + RAL0.715

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Mean Change From Baseline in Low Density Lipoprotein (LDL): High Density Lipoprotein (HDL) Ratio (Ratio)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionratio (Mean)
LPV/r + FTC/TDF-0.056
LPV/r + RAL-0.040

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Mean Change From Baseline in Lymphocytes (x 10^9/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionnumber of cells x 10^9/liter (Mean)
LPV/r + FTC/TDF0.332
LPV/r + RAL0.368

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Mean Change From Baseline in Magnesium (Millimoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmillimoles/liter (Mean)
LPV/r + FTC/TDF0.019
LPV/r + RAL-0.009

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Mean Change From Baseline in Mid-Arm Measurement (cm)

Arm circumference is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. Particpant's arm circumference was measured halfway between the acromial process on the shoulder and the tip of the elbow (olecranon process) using non-stretchable measuring tape with half centimeter marks. (NCT00711009)
Timeframe: Baseline to Week 96

Interventioncm (Mean)
LPV/r + FTC/TDF1.76
LPV/r + RAL4.71

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Mean Change From Baseline in Mid-Thigh Measurement (cm)

Mid-thigh circumference is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. Particpant's thigh circumference was measured halfway between the inguinal crease and the midpoint of the upper border of the patella using non-stretchable measuring tape with half centimeter marks. (NCT00711009)
Timeframe: Baseline to Week 96

Interventioncm (Mean)
LPV/r + FTC/TDF2.09
LPV/r + RAL5.13

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Mean Change From Baseline in Monocytes (x 10^9/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionnumber of cells x 10^9/liter (Mean)
LPV/r + FTC/TDF0.065
LPV/r + RAL0.112

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Mean Change From Baseline in Neutrophils (x 10^9/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionnumber of cells x 10^9/liter (Mean)
LPV/r + FTC/TDF0.509
LPV/r + RAL0.705

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Mean Change From Baseline in Platelet Count (x 10^9/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionnumber of cells x 10^9/liter (Mean)
LPV/r + FTC/TDF46.8
LPV/r + RAL34.2

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Mean Change From Baseline in Potassium (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF0.13
LPV/r + RAL0.03

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Mean Change From Baseline in Red Blood Cell Count (x 10^12/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionnumber of cells x 10^12/liter (Mean)
LPV/r + FTC/TDF0.12
LPV/r + RAL0.16

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Mean Change From Baseline in Sitting Diastolic Blood Pressure (mm Hg)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmm Hg (Mean)
LPV/r + FTC/TDF-2.4
LPV/r + RAL-1.8

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Mean Change From Baseline in Sitting Heart Rate (Beats Per Minute)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionbeats per minute (Mean)
LPV/r + FTC/TDF-4.6
LPV/r + RAL-6.3

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Mean Change From Baseline in Sitting Systolic Blood Pressure (mm Hg)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmm Hg (Mean)
LPV/r + FTC/TDF-0.7
LPV/r + RAL-2.4

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Mean Change From Baseline in Sodium (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF0.1
LPV/r + RAL0.7

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Mean Change From Baseline in Soluble Tumor Necrosis Factor Receptor-1 (Picograms/Milliliter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionpicograms/milliliter (Mean)
LPV/r + FTC/TDF-138.602
LPV/r + RAL-166.403

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Mean Change From Baseline in Soluble Tumor Necrosis Factor Receptor-2 (Picograms/Milliliter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionpicograms/milliliter (Mean)
LPV/r + FTC/TDF-1257.9
LPV/r + RAL-1594.7

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Mean Change From Baseline in Temperature (°F)

(NCT00711009)
Timeframe: Baseline to Week 96

Intervention°F (Mean)
LPV/r + FTC/TDF-0.152
LPV/r + RAL-0.183

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Mean Change From Baseline in Total Bilirubin (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF0.9
LPV/r + RAL1.9

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Mean Change From Baseline in Total Protein (Grams/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams/liter (Mean)
LPV/r + FTC/TDF-6.3
LPV/r + RAL-7.2

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Mean Change From Baseline in Triglycerides (Micromoles/Liter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF0.846
LPV/r + RAL1.103

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Mean Change From Baseline in Uric Acid (Micromoles/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicromoles/liter (Mean)
LPV/r + FTC/TDF-29.0
LPV/r + RAL-6.1

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Mean Change From Baseline in Urine pH

(NCT00711009)
Timeframe: Baseline to Week 96

InterventionpH (Mean)
LPV/r + FTC/TDF0.00
LPV/r + RAL0.03

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Mean Change From Baseline in Urine Specific Gravity

Urine specific gravity is a laboratory test that measures the concentration of all chemical particles in the urine. The measurement produces a ratio of the urine density to water density. (NCT00711009)
Timeframe: Baseline to Week 96

Interventionratio of urine density to water density (Mean)
LPV/r + FTC/TDF0.0042
LPV/r + RAL0.0052

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Mean Change From Baseline in Waist Measurement (cm)

Waist circumference is included in the measures of somatic toxicity, which is characterized by loss of fat in the face, arms, and legs, and increase in fat in the base of the back of the neck and in the abdomen. Circumference of participant's waist was measured at the level of the navel using non-stretchable measuring tape with half centimeter marks. (NCT00711009)
Timeframe: Baseline to Week 96

Interventioncm (Mean)
LPV/r + FTC/TDF1.88
LPV/r + RAL4.93

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Mean Change From Baseline in Weight (kg)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionkg (Mean)
LPV/r + FTC/TDF1.83
LPV/r + RAL3.77

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Mean Change From Baseline in White Blood Cell Count (x 10^9/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionnumber of cells x 10^9/liter (Mean)
LPV/r + FTC/TDF0.90
LPV/r + RAL1.20

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Number of Participants Who Developed Resistance, Defined Conservatively, to Lopinavir

Beginning at Week 8, if participant's plasma HIV-1 RNA was greater than/equal to 40 copies/milliliter (mL) and was below 40 copies/mL at the previous visit, additional procedures were undertaken to determine if resistance occurred. Evidence of lopinavir resistance was more conservatively defined as the presence of 1 or more of these mutations: protease I47V or A, G48V, I50V, V82A or F or T or S, I84V, L90M; or presence of at least 3 or more of these mutations: protease L10F or I or R or V, K20M or R, L24I, V32I, L33F, M36I, M46I or L, F53L, any change to I54, A71V or T, and G73S. (NCT00711009)
Timeframe: Baseline to Week 96

InterventionParticipants (Number)
LPV/r + FTC/TDF0
LPV/r + RAL1

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Percentage of Participants Responding (Plasma HIV-1 Ribonucleic Acid [RNA] Levels Less Than 40 Copies/Milliliter [mL]) at Week 48 Based on the Food and Drug Administration (FDA) Time to Loss of Virologic Response (TLOVR) Algorithm

A participant was classified as a responder at the first of 2 consecutive visits with plasma HIV-1 RNA levels below 40 copies/mL. The participant continued to be a responder until one of the following: the participant had 2 consecutive values greater than or equal to 40 copies/mL; the final measurement, if the final measurement was the first one documenting an increase in plasma HIV-1 RNA level to greater than or equal to 40 copies/mL; the participant discontinued participation in the study or died. (NCT00711009)
Timeframe: Baseline to Week 48

InterventionPercentage of Participants (Number)
LPV/r + FTC/TDF84.8
LPV/r + RAL83.2

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Score on Effectiveness Scale of Treatment Satisfaction Questionnaire for Medication (TSQM)

The Effectiveness Scale of the TSQM evaluates the participant's satisfaction or dissatisfaction (1=extremely dissatisfied to 7=extremely satisfied) with the ability of the medication to prevent or treat the condition, the way the medication relieves symptoms, the amount of time it takes for the medication to start working, and other questions. Scores are converted to a range of 0 to 100. A higher score indicates greater satisfaction. (NCT00711009)
Timeframe: Week 96

InterventionScores on a scale (Mean)
LPV/r + FTC/TDF75.5
LPV/r + RAL76.0

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Score on Global Satisfaction Scale of Treatment Satisfaction Questionnaire for Medication

The Global Satisfaction scale of the TSQM evaluates the participants rating of whether the good things about the medication outweigh the bad things (1=not at all certain to 5=extremely certain) and how satisfied or dissatisfied the participant is with the medication (1=extremely dissatisfied to 7=extremely satisfied). Scores are converted to a range of 0 to 100. Higher scores indicate greater satisfaction. (NCT00711009)
Timeframe: Week 96

InterventionScores on a scale (Mean)
LPV/r + FTC/TDF82.5
LPV/r + RAL85.5

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Score on Side Effects Scale of Treatment Satisfaction Questionnaire for Medication

The Side Effects scale of the TSQM asks if the participant experiences side effects (yes/no), and if so, how bothersome the side effects are, to what extent they interfere with physical health and ability to function (for example, strength and energy levels), to what extent they interfere with mental function (for example, ability to think clearly, stay awake, etc.), and to what extent the side effects affect the participants overall satisfaction with the medication. Scores are converted to a range of 0 to 100. Higher scores indicate less interference and/or less dissatisfaction. (NCT00711009)
Timeframe: Week 96

InterventionScores on a scale (Mean)
LPV/r + FTC/TDF84.6
LPV/r + RAL86.2

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Time to Loss of Virologic Response - Percentage of Participants Still Categorized as Responders at Day 672

Time of loss of virologic response was defined as the first of the following: first of 2 consecutive visits with plasma HIV-1 RNA greater than or equal to 40 copies/milliliter (mL), if the participant previously demonstrated 2 consecutive plasma HIV-1 RNA levels below 40 copies/mL; Study Day 1, if the subject never achieved 2 consecutive plasma HIV-1 RNA levels below 40 copies/mL; the day of the final measurement, if the final measurement was the first one documenting an increase in plasma HIV-1 RNA level to greater than or equal to 40 copies/mL. (NCT00711009)
Timeframe: Baseline to Week 96

InterventionPercentage of Participants (Number)
LPV/r + FTC/TDF79.1
LPV/r + RAL77.8

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Mean Change in CD4+ T-Cell Counts From Baseline to Each Visit

(NCT00711009)
Timeframe: Baseline to Week 96

,
Interventioncells/microliter (Mean)
Week 4Week 8Week 16Week 24Week 32Week 40Week 48Week 60Week 72Week 84Week 96
LPV/r + FTC/TDF97.2107.9158.7154.9180.0204.6245.0243.4277.4309.6296.4
LPV/r + RAL113.4124.5141.6174.5188.2223.0241.9250.6269.9280.2281.0

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Number of Participants Who Developed Resistance to Each Drug in the Study Regimen, as Defined by the International AIDS Society-USA (IAS-USA) Panel.

Resistance to study drugs was defined as described by the International AIDS Society-USA (IAS-USA) Panel. All participants had an HIV-1 drug resistance genotype (lopinavir/ritonavir, tenofovir, or emtricitabine) obtained at the Screening Visit. Beginning at Week 8, if participant's plasma HIV-1 RNA was greater than or equal to 40 copies/milliliter (mL) and was below 40 copies/mL at the previous visit, additional procedures were undertaken to determine if resistance to study drug occurred. (NCT00711009)
Timeframe: Baseline to Week 96

,
InterventionParticipants (Number)
Lopinavir resistanceEmtricitabine resistanceTenofovir resistanceRaltegravir resistance
LPV/r + FTC/TDF010NA
LPV/r + RAL0003

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Percentage of Participants Responding (Plasma HIV-1 RNA Levels Below 40 Copies/Milliliter [mL]) at Each Visit Based on the FDA Time to Loss of Virologic Response (TLOVR) Algorithm

A participant was classified as a responder at the first of 2 consecutive visits with plasma HIV-1 RNA levels below 40 copies/mL. The participant continued to be a responder until one of the following: 1) the participant had 2 consecutive values greater than or equal to 40 copies/mL; the final measurement, if the final measurement was the first one documenting an increase in plasma HIV-1 RNA level to greater than or equal to 40 copies/mL; the participant discontinued participation in the study or died. (NCT00711009)
Timeframe: Baseline to Week 96

,
InterventionPercentage of Participants (Number)
Week 2Week 4Week 8Week 16Week 24Week 32Week 40Week 48Week 60Week 72Week 84Week 96
LPV/r + FTC/TDF7.617.136.267.680.085.784.884.882.978.174.368.6
LPV/r + RAL33.763.475.281.283.285.187.183.275.271.370.366.3

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Primary Outcome: Percentage of Participants With Potentially Clinically Significant Laboratory Values

Potentially clinically significant laboratory values that occurred in at least 2% of participants in either treatment arm are presented. (NCT00711009)
Timeframe: Baseline to Week 96

,
InterventionPercentage of participants (Number)
Alananine aminotransferase >5x upper limit normalAspartate aminotransferase >5x upper limit normalCreatinine phosphokinase >4x upper limit of normalCalcium <1.75 millimoles/literCholesterol >7.77 millimoles/literTriglycerides >8.475 millimoles/literCalc. creatinine clearance <50 milliliters/minuteLipase >2x upper limit of normalNeutrophils < 0.75 x 10^9/literMagnesium < 0.5 millimoles/liter
LPV/r + FTC/TDF2.92.98.7013.54.83.87.73.80
LPV/r + RAL5.05.019.82.016.89.91.04.002.0

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Change From Baseline on Mental Component of Medical Outcomes Study HIV Health Survey

The Survey is a brief, comprehensive health status measure used in studies of people with HIV/AIDS. Participants rate their health and mental/emotional condition, how much their health limits physical activities (eating, dressing, bathing, climbing stairs, walking one block, etc.) and social activities (visiting with friends or relatives, etc.), and other questions that measure quality of life. The mental component summarizes answers to questions about emotional and mental wellbeing. Possible scores range from 0 to 100. Higher scores indicates better health, and increases indicate improvement. (NCT00711009)
Timeframe: Baseline to Week 96

InterventionScores on a scale (Mean)
LPV/r + FTC/TDF1.3
LPV/r + RAL1.3

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Change From Baseline on Physical Component Score of the Medical Outcomes Study HIV Health Survey

The Survey is a brief, comprehensive health status measure used in studies of people with HIV/AIDS. Participants rate their health and mental/emotional condition, how much their health limits physical activities (eating, dressing, bathing, climbing stairs, walking one block, etc.) and social activities (for example, visiting with friends or relatives), and other questions that measure quality of life. The physical component summarizes answers to questions about physical status. Possible scores range from 0 to 100. A higher score indicates better health, and increases indicate improvement. (NCT00711009)
Timeframe: Baseline to Week 96

InterventionScores on a scale (Mean)
LPV/r + FTC/TDF-1.0
LPV/r + RAL-1.1

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Mean Change From Baseline in Adiponectin (Micrograms/Milliliter)

Included in measures of metabolic toxicity (NCT00711009)
Timeframe: Baseline to Week 96

Interventionmicrograms/milliliter (Mean)
LPV/r + FTC/TDF2.112
LPV/r + RAL2.064

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Mean Change From Baseline in Alanine Aminotransferase (Units/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventionunits/liter (Mean)
LPV/r + FTC/TDF-6.1
LPV/r + RAL-13.4

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Mean Change From Baseline in Albumin (Grams/Liter)

(NCT00711009)
Timeframe: Baseline to Week 96

Interventiongrams/liter (Mean)
LPV/r + FTC/TDF1.4
LPV/r + RAL1.3

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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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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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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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Lopinavir (Lpv) and Ritonavir (Rtv) Cmax at 4 Weeks

Lpv and rtv Cmax at 4 weeks when participants are receiving study intervention, low dose Kaletra. Time points for data collection: 0, 2hrs, 4hrs, 6hrs, 8hrs (NCT00762320)
Timeframe: 4 weeks

Interventionng/ml (Median)
Lpv Cmax at 4 weeksRtv Cmax at 4 weeks
Low Dose Kaletra11143912.1

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Absolute CD4 and CD4 %

Number of participants who had no clinically significant deterioration in absolute CD4 and % CD4 count for the duration of the study. Absolute CD4 and Percent CD4 counts were determined by single or dual platform analysis performed on blood samples by Phoenix Children's Hospital Laboratory, Sonora Quest Laboratory or Labcorp Laboratory. Clinically significant change was determine to be a deterioration in both Absolute CD4 to less than 500 and %CD4 to less than 25%. (NCT00762320)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

Interventionparticipants (Number)
Low Dose Kaletra8

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Symptoms Across All Patients

Cumulative tally of symptoms for each patients across all visits. Targetted symptoms were asked for at each visit and patients and parents were encouraged to report additional symptoms that were experienced. Each patient got a score for the total number of symptoms at each visit. Scores were totalled, but it the same symptoms occurred continuously it was counted as 1 symptom. (NCT00762320)
Timeframe: Baseline, 1 month, 3 months, 6 months

Interventionnumer of symptoms (Mean)
Symptoms for all subjects at BaselineSymptoms for all subjects at 4 WeeksSymptoms for all subjects at 12 WeeksSymptoms for all subjects at 24 weeks
Low Dose Kaletra20.2021.8026.4026.60

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Lopinavir and Ritonavir AUC on Low Dose Tablet

Lopinavir and Ritonavir AUC at 4 weeks when participants are receiving the study intervention, low dose tablet formulation of Kaletra. Data collection points for AUC were 0, 2, 4, 6, and 8 hours post dose. (NCT00762320)
Timeframe: 4 weeks

Interventionhr*ng/ml (Median)
Lpv AUC at 4 weeksRtv AUC at 4 weeks
Low Dose Kaletra856704876.1

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Lopinavir and Ritonavir Area Under the Curve (AUC) Liquid Kaletra

Area under the curve values for lopinavir at baseline when participants are taking liquid Kaletra as part of their baseline treatment. Time points for data collection: 0, 2 hrs post, 4 hrs post, 6 hrs post, 8 hrs post. (NCT00762320)
Timeframe: Baseline

Interventionhr*ng/ml (Median)
Lpv AUC at baselineRtv AUC at baseline
Low Dose Kaletra906513701.2

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Lopinavir (Lpv) and Ritonavir (Rtv) Maximumu Plasma Concentration (CMax) Liquid

Cmax values at baseline (participants are taking liquid Kaletra as part of baseline treatment). Time points for data collection: 0, 2hrs post dose, 4 hrs post dose, 8 hrs post dose. (NCT00762320)
Timeframe: Baseline

Interventionng/ml (Median)
Cmax LpvCmax Rtv
Low Dose Kaletra9742637.0

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Viral Load (VL)

Number of participants who maintained their Viral load undetectable (< 20 copies/ml) for the duration of the study (NCT00762320)
Timeframe: Baseline, Week 4, Week 12 and Week 24

Interventionparticipants (Number)
Low Dose Kaletra8

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Patient Satisfaction

Patient Satisfaction Survey. Eight item Likert scale of patient satisfaction with their HIV treatment regimen for patients 7 years of age and older. Items scores are summed to compute a total score. Total scores are reported with a minimum of 0 and a maximum of 32, with higher scores indicating higher satisfaction. (NCT00762320)
Timeframe: Baseline, 1 month

Interventionunits on a scale (Mean)
Low Dose Kaletra Baseline Visit20.2
Low Dose Kaletra Week 4 Visit21.8

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Parent Satisfaction

Parent Satisfaction Survey. Eight item Likert scale of parent/guardian satisfaction with the child's HIV treatment regimen. Item scores are summed to compute a total score. Total scores are reported with a minimum of 0 and a maximum of 32, with higher scores indicating higher satisfaction. (NCT00762320)
Timeframe: Baseline, 4 week, 12 weeks and 24 weeks

InterventionScore on a survey (Mean)
Low Dose Kaletra Baseline26.75
Low Dose Kaletra Week 428.38

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Lopinavir AUC Ratio of Baseline:Week 4

Ratio of AUC at baseline (liquid)to week 4 (reduced dose tablet). AUC data were collected at 0, 2, 4, 6, and 8 hours post dose. (NCT00762320)
Timeframe: Baseline, week 4

Interventionratio (Mean)
Low Dose Kaletra1.01

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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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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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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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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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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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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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Lopinavir Area Under the Curve (AUC)

Lopinavir Area Under the Plasma Concentration versus Time Curve (AUC) (NCT00810108)
Timeframe: pre-dose, 1,2,4,6,8, and 12 hours post-dose

Interventionmg*hr/L (Median)
All Subjects Taking Whole Tablets144
All Subjects Taking Crushed Tablets92

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Percentage of Participants With Less Than 50 Copies/mL of HIV-1 RNA

(NCT00827112)
Timeframe: 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, Week 96

,
InterventionPercentage of participants (Number)
Week 2 (n= 55, 60)Week 4 (n= 57, 60)Week 8 (n= 57, 59)Week 12 (n= 55, 59)Week 16 (n= 54, 58)Week 20 (n= 56, 57)Week 24 (n= 56, 58)Week 32 (n= 55, 57)Week 40 (n= 54, 55)Week 48 (n= 53, 54)Week 60 (n= 52, 53)Week 72 (n= 52, 53)Week 84 (n= 50, 52)Week 96 (n= 49, 51)
Atazanavir / Ritonavir + Emtricitabine / Tenofovir6.6021.3042.6062.3073.8083.6188.5288.5288.5283.6185.2581.9783.6181.97
Maraviroc+ Atazanavir / Ritonavir08.5047.5061.0072.9071.2081.3679.6681.3674.5867.8074.5876.2767.80

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Percentage of Participants With Less Than 400 Copies/mL of HIV-1 RNA

(NCT00827112)
Timeframe: 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, Week 96

,
InterventionPercentage of participants (Number)
Week 2 (n= 55, 60)Week 4 (n= 57, 60)Week 8 (n= 57, 59)Week 12 (n= 55, 59)Week 16 (n= 54, 58)Week 20 (n= 56, 57)Week 24 (n= 56, 58)Week 32 (n= 55, 57)Week 40 (n= 54, 55)Week 48 (n= 53, 54)Week 60 (n= 52, 53)Week 72 (n= 52, 53)Week 84 (n= 50, 52)Week 96 (n= 49, 51)
Atazanavir / Ritonavir + Emtricitabine / Tenofovir34.4352.4677.0588.5291.8093.4493.4493.4490.1686.8986.8985.2585.2583.61
Maraviroc+ Atazanavir / Ritonavir27.1250.8579.6689.8388.1489.8391.5389.8391.5389.8386.4486.4481.3677.97

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Number of Participants With HIV-1 RNA Tropism Status Using Trofile Assay

Viral tropism was determined using the trofile assay with enhanced sensitivity for participants with HIV-1 RNA greater than equal to 1000 copies/mL. The enhanced trofile assay had the sensitivity to detect 100 percent of spiked samples when C-X-C chemokine receptor type 4 {CXCR4} [X4]-using HIV-1 RNA represented 0.3 percent of the total viral population. (NCT00827112)
Timeframe: Baseline to Week 96 or Time of treatment Failure

,
InterventionParticipants (Number)
BaselineWeek 96 or Time of treatment Failure
Atazanavir / Ritonavir + Emtricitabine / Tenofovir610
Maraviroc+ Atazanavir / Ritonavir600

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HIV-1 RNA Levels at Baseline

(NCT00827112)
Timeframe: Baseline

Interventioncopies/mL (Mean)
Maraviroc+ Atazanavir / Ritonavir84982
Atazanavir / Ritonavir + Emtricitabine / Tenofovir114827

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Change From Baseline in HIV-1 RNA Levels of First 15 Participants at Days 4, 7, 10 and 14

Plasma HIV-1 RNA levels were evaluated for first 15 participants enrolled at United States (U.S) sites only. (NCT00827112)
Timeframe: Baseline , Days 4, 7, 10 and 14

,
Interventioncopies/mL (Mean)
Change at Day 4Change at Day 7Change at Day 10Change at Day 14
Atazanavir / Ritonavir + Emtricitabine / Tenofovir-46479.40-52137.10-54925.90-55449.90
Maraviroc+ Atazanavir / Ritonavir1800.00-36947.90-58595.80-47271.60

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Maximum Observed Plasma Concentration (Cmax) of Maraviroc

(NCT00827112)
Timeframe: Day 14 (0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 24 hours post dose)

Interventionnanogram (ng)/mL (Median)
Maraviroc+ Atazanavir / Ritonavir650

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Change From Baseline in Cluster of Differentiation 8+T Lymphocyte (CD8) Cell Count at Weeks 16, 24, 48 and 96

(NCT00827112)
Timeframe: Baseline, Week 16, Week 24, Week 48, Week 96

,
Interventioncells/mcL (Mean)
Baseline (n= 59, 61)Change at Week 16 (n= 54, 58)Change at Week 24 (n= 54, 57)Change at Week 48 (n= 52, 53)Change at Week 96 (n= 50, 51)
Atazanavir / Ritonavir + Emtricitabine / Tenofovir1125.60-153.80-178.00-267.60-231.40
Maraviroc+ Atazanavir / Ritonavir931.1063.706.20-76.80-63.00

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Change From Baseline in Cluster of Differentiation 4+T Lymphocyte (CD4) Cell Counts at Weeks 16, 24, 48 and 96

(NCT00827112)
Timeframe: Baseline, Week 16, Week 24, Week 48, Week 96

,
Interventioncells/microliter (cells/mcL) (Mean)
Baseline (n= 59, 61)Change at Week 16 (n= 54, 58)Change at Week 24 (n= 54, 57)Change at Week 48 (n= 52, 53)Change at Week 96 (n= 50, 51)
Atazanavir / Ritonavir + Emtricitabine / Tenofovir390.00139.80173.30226.60298.50
Maraviroc+ Atazanavir / Ritonavir357.70169.60188.90215.70287.50

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Time to Loss of Virological Response (TLOVR)

TLOVR (virological failure) was defined as the time from first dose of study treatment (Day 1) until the time of virologic failure using the time to loss of virologic response algorithm. (NCT00827112)
Timeframe: Baseline through Week 96

InterventionDays (Mean)
Maraviroc+ Atazanavir / Ritonavir436.2
Atazanavir / Ritonavir + Emtricitabine / Tenofovir463.8

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Percentage of Participants With Plasma Human Immuno Deficiency Virus-1 Ribonucleic Acid (HIV-1 RNA) Levels Less Than 50 Copies/Milliliter (mL)

(NCT00827112)
Timeframe: Week 48

InterventionPercentage of participants (Number)
Maraviroc+ Atazanavir / Ritonavir74.60
Atazanavir / Ritonavir + Emtricitabine / Tenofovir83.60

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Number of Participants With Phenotypic Resistance

Phenotypic resistance was assessed for all participants at screening and was evaluated for PIs, NRTIs, and NNRTIs using Monogram GenoSeq and/or PhenoSenseGT assays. This was then repeated for all participants with HIV-1 viral load more than 500 copies/mL either at treatment failure or at early termination, up to Week 96. (NCT00827112)
Timeframe: Week 96 or Time of treatment failure

InterventionParticipants (Number)
Maraviroc+ Atazanavir / Ritonavir0
Atazanavir / Ritonavir + Emtricitabine / Tenofovir0

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Number of Participants With Genotypic Resistance

Genotypic resistance was assessed for all participants at screening and was evaluated for protease inhibitors (PIs), Nucleotide reverse transcriptase inhibitors (NRTIs), and non-NRTIs (NNRTIs) using Monogram GenoSeq and/or PhenoSenseGT assays. This was then repeated for all participants with HIV-1 viral load more than 500 copies/mL either at treatment failure or at early termination, up to Week 96. (NCT00827112)
Timeframe: Week 96 or Time of treatment failure

InterventionParticipants (Number)
Maraviroc+ Atazanavir / Ritonavir0
Atazanavir / Ritonavir + Emtricitabine / Tenofovir0

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Average Observed Plasma Concentration (Cavg) of Maraviroc

Cavg was described as area under the plasma concentration-time profile from time zero to time 24 hours (AUC24) divided by the dosing interval (AUC24/ 24). (NCT00827112)
Timeframe: Day 14 (0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 24 hours post dose)

Interventionng/mL (Mean)
Maraviroc+ Atazanavir / Ritonavir185.10

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Minimum Observed Plasma Concentration (Cmin) of Maraviroc

(NCT00827112)
Timeframe: Day 14 (0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 24 hours post dose)

Interventionng/mL (Median)
Maraviroc+ Atazanavir / Ritonavir37.0

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Change From Baseline in Plasma log10 Viral Load at Weeks 16, 24, 48 and 96

(NCT00827112)
Timeframe: Baseline, Week 16, Week 24, Week 48, Week 96

,
Interventionlog10 copies/ml (Mean)
Baseline (n= 59, 61)Change at Week 16 (n= 54, 58)Change at Week 24 (n= 56, 58)Change at Week 48 (n= 53, 54)Change at Week 96 (n= 49, 51)
Atazanavir / Ritonavir + Emtricitabine / Tenofovir114827-107684.6-110498.1-115582.9-99662.6
Maraviroc+ Atazanavir / Ritonavir84982-89859.1-87241.2-82343.4-80117.7

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Time-Averaged Difference (TAD) in log10 Viral Load

TAD was calculated as area under the curve of HIV divided by time period minus baseline HIV where HIV was denoted as HIV-1 RNA (log10 copies/mL). (NCT00827112)
Timeframe: Week 16, Week 24, Week 48, Week 96

,
Interventionlog10 copies/mL (Mean)
Week 16Week 24Week 48Week 96
Atazanavir / Ritonavir + Emtricitabine / Tenofovir-2.402-2.626-2.868-3.001
Maraviroc+ Atazanavir / Ritonavir-2.459-2.663-2.897-2.998

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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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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 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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"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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IL-4

Interleukin-4 measured by Luminex multiplex assay in picograms/mL, dynamic range 0.13-2000 pg/mL (NCT00885664)
Timeframe: 4 weeks

Interventionpg/mL (Median)
CD4<1000.07
CD4>/=1000.07

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TNF Alpha

Tumor Necrosis Factor Alpha - measured by Luminex multiplex assay in picograms/mL, dynamic range 0.13-2000 pg/mL (NCT00885664)
Timeframe: 4 weeks

Interventionpg/mL (Median)
CD4<10013.07
CD4>/=1009.07

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Symptom Score

AIDS Clinical Trials Group Symptom Summary Score (20 item scale with severity from 0-4); Severity scale, 0=absent, 1=is least severe and 4 is most severe. Minimum score = 0 units on scale. Maximum score = 80 units on scale. (NCT00885664)
Timeframe: Week 4

Interventionunits on a scale (Median)
CD4<10010
CD4>/=1008

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SF-12 Mental Capacity Score

Measure of mental functioning where lower is better out of a scale of 100. (NCT00885664)
Timeframe: 4 weeks

Interventionscore on a scale (Median)
CD4<10046
CD4>/=10050

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INF Gamma

Interferon gamma measured by Luminex multiplex assay in picograms/mL, dynamic range 0.13-2000 pg/mL (NCT00885664)
Timeframe: 4 weeks

Interventionpg/mL (Median)
CD4<1002.24
CD4>/=1001.06

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IL-7

Interleukin 7 measured by Luminex multiplex assay in picograms/mL, dynamic range 0.13-2000 pg/mL (NCT00885664)
Timeframe: 4 weeks

Interventionpg/mL (Median)
CD4<10017.50
CD4>/=10010.53

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IL-8

Interleukin 8 measured by Luminex multiplex assay in picograms/mL, dynamic range 0.13-2000 pg/mL (NCT00885664)
Timeframe: 4 weeks

Interventionpg/mL (Median)
CD4<1007.58
CD4>/=1005.18

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SF-12 Physical Capacity Score

Measure of physical function out of 100. Lower score means less physical capacity. (NCT00885664)
Timeframe: 4 weeks

Interventionunits on a scale (Median)
CD4<10043
CD4>/=10054

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IL-1 Beta

Cytokine IL-1 beta measurement by Luminex multiplex assay in picograms/mL, dynamic range 0.13-2000 pg/mL (NCT00885664)
Timeframe: 4 weeks

Interventionpg/mL (Median)
CD4<1000.03
CD4>/=1000.03

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IL-6

Interleukin 6 measured by Luminex multiplex assay in picograms/mL, dynamic range 0.13-2000 pg/mL (NCT00885664)
Timeframe: 4 weeks

Interventionpg/mL (Median)
CD4<1004.41
CD4>/=1004.01

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IL-10

Interleukin 10 measured by Luminex multiplex assay in picograms/mL, dynamic range 0.13-2000 pg/mL (NCT00885664)
Timeframe: 4 weeks

Interventionpg/mL (Median)
CD4<10021.32
CD4>/=10010.30

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Development of Metabolic Syndrome

number of patients developing metabolic syndrome over a period of 48 weeks (NCT00928187)
Timeframe: from baseline to week 48

InterventionParticipants (Count of Participants)
Arm A12
Arm B21
Arm C9

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Gain in CD4 Cells Between Baseline and W48

median gain in circulating CD4 cells between baseline and W48 (NCT00928187)
Timeframe: between baseline and 48 weeks

Interventioncell/mm3 (Median)
Arm A133
Arm B136
Arm C115

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Number of Patients Discontinuing Study Treatment

number of patients discounting treatment because of adverse events (NCT00928187)
Timeframe: between baseline and W48

Interventionparticipants (Number)
Arm A0
Arm B4
Arm C1

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Number of Patients With HIV Plasma Viral Load < 200 Copies/ml

number of patients having a plasma viral load below 200 copies/ml at week 24 (NCT00928187)
Timeframe: Week 24

InterventionParticipants (Count of Participants)
Arm A127
Arm B117
Arm C129

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Number of Patients With HIV Plasma Viral Load < 50 Copies/ml

Snapshot of patients with HIV viral load less then 50 copies/ml at week 24 (NCT00928187)
Timeframe: Week 24

InterventionParticipants (Count of Participants)
Arm A90
Arm B81
Arm C97

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Number of Patients With Resistance Mutations

number of patients with resistance mutations after second line treatment failure (HIV RNA> 1000 copies/ml) (NCT00928187)
Timeframe: between W12 and W48

Interventionparticipants (Number)
Arm A0
Arm B0
Arm C0

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Patients With Plasma HIV RNA < 200 Copies/ml

number of patients with plasma HIV RNA below 200 copies/ml (NCT00928187)
Timeframe: 48 weeks

Interventionparticipants (Number)
Arm A130
Arm B118
Arm C127

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Tolerance: Equal or Superior to a 25% Reduction in eGFR (Glomerular Filtration Rate)

evaluation of estimated glomerular filtration rate and number of participant with a decrease equal or superior to 25% of the baseline value (NCT00928187)
Timeframe: between baseline and W48

Interventionparticipants (Number)
Arm A28
Arm B14
Arm C19

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Tolerance: Gastrointestinal Complains

Gastrointestinal complaints (grade 1 to 4) between baseline and W48. (NCT00928187)
Timeframe: between baseline and 48 weeks

Interventionparticipants (Number)
Arm A50
Arm B48
Arm C26

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Tolerance: Neuropathies (Grade 1 to 4)

any symptom of peripheral neuropathy (NCT00928187)
Timeframe: between baseline and W48

Interventionparticipants (Number)
Arm A5
Arm B11
Arm C8

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Adherence

number of patients in different categories of adherence as measured by questionnaire (NCT00928187)
Timeframe: between baseline and W48

,,
Interventionparticipants (Number)
Always above 95%At least once 80-95%At least once < 80%
Arm A508911
Arm B547214
Arm C67784

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Number of Patients With Plasma HIV RNA < 50 Copies/mL

(NCT00928187)
Timeframe: 48 weeks

Interventionparticipants (Number)
Arm A105
Arm B92
Arm C97

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Participants With Plasma HIV RNA < 200 Copies/mL 48 Weeks After Randomization

(NCT00931463)
Timeframe: 48 weeks following randomization

Interventionparticipants (Number)
Ritonavir-boosted Lopinavir and 2N(t)RTI219
Ritonavir-boosted Lopinavir and Raltegravir223

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Participants With Plasma HIV RNA < 200 Copies/mL 48 Weeks After Randomization, Per-protocol Population

The per- protocol population includes those participants who fulfil the protocol in the terms of the eligibility, interventions, and outcome assessment (NCT00931463)
Timeframe: 48 weeks

Interventionparticipants (Number)
Ritonavir-boosted Lopinavir and 2N(t)RTI211
Ritonavir-boosted Lopinavir and Raltegravir211

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Participants With Plasma HIV RNA < 200 Copies/mL 48 Weeks After Randomization, Per-protocol Population, Baseline VL >100,000 Copies Per mL

The difference between treatment arms in proportion of participants with plasma HIV RNA < 200 copies/mL 48 weeks after randomization, per-protocol population: stratified analysis by baseline plasma viral load (less than or equal to 100,000 copies per mL or >100,000 copies per mL) on those participants who fulfil the protocol in the terms of the eligibility, interventions, and outcome assessment (NCT00931463)
Timeframe: 48 weeks

Interventionparticipants (Number)
Ritonavir-boosted Lopinavir and 2N(t)RTI31
Ritonavir-boosted Lopinavir and Raltegravir39

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Participants With Plasma HIV RNA < 200 Copies/mL 48 Weeks After Randomization, Per-protocol Population, Non-completer Classed as Failure

"The non-completer classed as failure analysis will include all randomised participants; participants who meet the following criteria will be defined as failures:~i. week 48 HIV RNA being above each threshold ii. has missing HIV-1 RNA data for any reason iii. stops randomly assigned therapy" (NCT00931463)
Timeframe: 48 weeks

Interventionparticipants (Number)
Ritonavir-boosted Lopinavir and 2N(t)RTI208
Ritonavir-boosted Lopinavir and Raltegravir210

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Participants With Plasma HIV RNA < 200 Copies/mL 48 Weeks After Randomization, Per-protocol Population, VL Less Than or Equal to 100,000 Copies Per mL

The per- protocol population includes those participants who fulfil the protocol in the terms of the eligibility, interventions, and outcome assessment (NCT00931463)
Timeframe: 48 weeks

Interventionparticipants (Number)
Ritonavir-boosted Lopinavir and 2N(t)RTI188
Ritonavir-boosted Lopinavir and Raltegravir184

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Change From Baseline in Clinical Chemistry Paramaters- Albumin and Total Protein

The data for clinical chemistry parameters Albumin and total protein, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventiongram per deciliter (Mean)
Albumin, Day 2Albumin, Day 4Albumin, Day 7Albumin, Day 8Albumin, Follow-upTotal protein, Day 2Total protein, Day 4Total protein, Day 7Total protein, Day 8Total protein, Follow-up
GSK2248761 30 mg-0.17-0.08-0.10-0.05-0.07-0.45-0.100.100.00-0.30
Placebo-0.200.00-0.05-0.100.05-0.55-0.100.05-0.25-0.20

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Change From Baseline in CD4+ and CD8+ T-lymphocyte Cell Count at Day1 and Day 8.

Whole venous blood samples were obtained from each participant for the analysis of lymphocyte subsets by flow cytometry (total lymphocyte counts, percentage, CD4+ cell counts, and CD8+ cell counts) at Screening, Day 1 and Day 8. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values (Day 1 and Day 8). Baseline was defined as Screening. (NCT00945282)
Timeframe: Baseline (Screening), Day 1 and Day 8

,
Interventionper cubic millimeter (Mean)
CD4+ cells, Day 1CD4+ cells, Day 8CD8+ cells, Day 1CD8+ cells, Day 8
GSK2248761 30 mg1.287.5123.5313.3
Placebo76.0102.0526.0531.5

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Assessment of the Achievement of Pre-dose GSK2248761 Steady State Concentration Following Repeat Dose Administration on Day 2 Through 7

The pre-dose GSK2248761 steady state concentration, following repeated dose administration from Day 2 through Day 7 was assessed. Serial dose sampling was done on each day of Day 2, 3, 4, 5 and Day 6 and for Day 7 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose), before the administration of the study drug daily. (NCT00945282)
Timeframe: Day 7 (Pre - dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose) and Days 2, 3, 4. 5 and 6: pre-dose only

Interventionng/mL (Mean)
Days 4, 5, 6 and 7Days 5, 6 and 7Days 6 and 7
GSK2248761 30 mg0.052-0.019-0.056

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Accumulation Ratio for AUC , Cmax, Cτ, and Time Invariance Ratio Following Repeat Administration

The accumulation ratio is based on the parameters, Cmax, AUC(0-tau), AUC(0-24), C(tau), C24, AND AUC(0-inf). The accumulation ratio Ro was the ratio of AUC(0-tau) on Day 7 to that of AUC(0-24) on Day 1; the accumulation ratio R (Cmax) was the ratio of Cmax on Day 7 to that of Cmax on Day 1; the accumulation ratio R(Ctau) was the ratio of Ctau on Day 7 to the ratio of C24 on Day 1 and the Time Invariance Ratio Rs was defined as the ratio of AUC(0-tau) on Day 7 to that of AUC(0-inf) on Day 1. The ratio has been reported as number. (NCT00945282)
Timeframe: (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose ) on Day 1 and Day 7

Interventionratio (Number)
Accumulation Ratio RoAccumulation Ratio R [Cmax]Accumulation Ratio R[Ctau]Time Invariance Ratio Rs
GSK2248761 30 mg1.5761.2121.7501.309

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HIV-1 Rate of Decline by Treatment

The rate of decrease in the viral load of HIV-1 virus in response to individual treatment was measured. The viral load data was assumed to have a log normal prior distribution and followed linear decline with non-informative conjugate prior densities. The rate of decline (slope of the day) for each treatment was measured using a PCR from Day 1 to Day 8. The slope has been reported as mean. (NCT00945282)
Timeframe: Day 1 to Day 8

Interventionlog10 copies/mL (Mean)
GSK2248761 30 mg-0.1243
Placebo0.0189

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GSK2248761 PK Parameters Following Dose Administration on Day 7: Tmax

Tmax is defined as the, time of maximum measured GSK2248761 concentration in the plasma, on Day 7. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 7 and used for analysis (NCT00945282)
Timeframe: Day 7 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post dose)

Interventionhours (Median)
GSK2248761 30 mg4.01

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GSK2248761 PK Parameters Following Dose Administration on Day 7: t1/2

The t1/2 was defined as the time measured for plasma concentration to decrease by one half. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 7 and used for analysis (NCT00945282)
Timeframe: Day 7 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post dose)

Interventionhour (Geometric Mean)
GSK2248761 30 mg9.69

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GSK2248761 PK Parameters Following Dose Administration on Day 7: AUC(0-τ)

AUC(0-τ) is the AUC to the end of dosing period. For Day 7, it is the AUC measured at the end of the dosing period at Day 7. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 7 and used for analysis. (NCT00945282)
Timeframe: Day 7 (Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose)

Interventionhour*ng/mL (Geometric Mean)
GSK2248761 30 mg9679.71

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GSK2248761 PK Parameters Following Dose Administration on Day 1: Apparent Clearance (CL/F)

The Clearance factor was defined as the volume of plasma cleared of the drug GSK2248761, per unit time. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 1 and used for analysis. (NCT00945282)
Timeframe: Day 1 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose)

Interventionliter per hour (Geometric Mean)
GSK2248761 30 mg13.53

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Change From Baseline to Nadir in Plasma HIV-1 RNA

The quantification of plasma HIV-1 RNA, was conducted for the change from baseline to on treatment nadir (maximum change) before starting HAART or Kaletra monotherapy on Day 8. The quantification was done using a PCR. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose Day 1) to Day 8

Interventionlog10 copies/mL (Mean)
GSK2248761 30 mg-1.019
Placebo-0.580

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Change From Baseline Through Day 8 in Plasma HIV-1 RNA

The quantitative analysis of plasma was done to evaluate the amount of HIV-1 RNA at Day 1,2,3,4,5,6,7, 8 and End of treatment visit. The quantification was done using a Polymerase chain reactor (PCR). The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose Day 1) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose Day 1) to Day 8

Interventionlog 10 copies per milliliter (mL) (Mean)
GSK2248761 30 mg-0.967
Placebo-0.036

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Change From Baseline in Clinical Chemistry Paramaters-sodium, Potassium and Carbondioxide or Bicarbonate

The data for clinical chemistry parameters- sodium, potassium and carbon dioxide or bicarbonate, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventionmilliequivalents per liter (Mean)
Sodium, Day 2Sodium, Day 4Sodium, Day 7Sodium, Day 8Sodium, Follow-upPotassium, Day 2Potassium, Day 4Potassium, Day 7Potassium, Day 8Potassium, Follow-upCarbondioxide, Day 2Carbondioxide, Day 4Carbondioxide, Day 7Carbondioxide, Day 8Carbondioxide, Follow-up
GSK2248761 30 mg-1.2-0.8-1.5-1.72.3-0.020.10-0.17-0.18-0.08-0.803.172.930.872.03
Placebo-0.51.00.0-0.51.0-0.250.10-0.10-0.00-0.30-1.352.703.601.65-0.30

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PK Data of Day 1 AUC(0-inf) and Day 7 AUC(0-tau) at Different Doses for the Assessment of Dose Proportionality

Data for IDX899 100 mg, IDX899 200 mg, IDX899 400 mg and IDX899 800 mg for Day 1 and Day 2 were taken from the Idenix NV-05A-002 study which were combined with GSK2248761 30 mg once daily data from this study, to assess the dose proportionality. The dose proportionality occurred when increase in the administered doses were accompanied by proportional increases in measure of exposure of the drug in the plasma PK parameters like AUC, Cmax, Ctau and other factors. The dose proportionality effects of IDX899 100 mg, IDX899 200 mg, IDX899 400 mg and IDX899 800 mg, following repeat dose administration on Day 7 for the PK parameter AUC(0-tau) has been reported. (NCT00945282)
Timeframe: (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose ) From Day 1 to Up to Day 7

,,,,
Interventionhour*ng/mL (Geometric Mean)
AUC(0-inf), Day 1AUC(0-tau), Day 7
GSK2248761 30 mg2217.732903.91
IDX899 100 mg990811650
IDX899 200 mg2381727209
IDX899 400 mg3382049649
IDX899 800 mg3781253683

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PK Data of Cmax and Ctau at Different Doses for the Assessment of Dose Proportionality

Data for IDX899 100 mg, IDX899 200 mg, IDX899 400 mg and IDX899 800 mg for Day 1 and Day 2 were taken from the Idenix NV-05A-002 study which were combined with GSK2248761 30 mg once daily data from this study, to assess the dose proportionality. The dose proportionality occurred when increase in the administered doses were accompanied by proportional increases in measure of exposure of the drug in the plasma PK parameters like AUC, Cmax, Ctau and other factors. Data for Ctau on Day 1 is presented for concentration at 24 hours post-dose on Day 1. (NCT00945282)
Timeframe: (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose ) From Day 1 to Up to Day 7

,,,,
Interventionng/mL (Geometric Mean)
Cmax, Day 1Cmax, Day 7Ctau, Day 1Ctau, Day 7
GSK2248761 30 mg175.63212.9331.0254.27
IDX899 100 mg797.8960.1128.9204.7
IDX899 200 mg1686.22158.9325.6469.2
IDX899 400 mg2625.94140.7422.9864.5
IDX899 800 mg3406.45394.5364.5540.3

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Percent Change From Baseline in CD4+ and CD8+ T-lymphocyte Cell Count at Day 1 and Day 8

Data for CD4+ and CD8+ cells was collected at Screening, Day 1 and Day 8. The percent change from baseline was reported at Day 1 and Day 8. Baseline was defined as Screening. The percent change from baseline was calculated as post-randomization value minus the baseline value. (NCT00945282)
Timeframe: Baseline (Screening), Day 1 and Day 8

,
InterventionPercent change (Mean)
CD4+, Day 1CD4+, Day 8CD8+, Day 1CD8+, Day 8
GSK2248761 30 mg-3.2-2.4-2.8-0.4
Placebo-2.9-1.72.80.4

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Number of Participants With Serious Adverse Events (SAEs) and Adverse Events (AEs)

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 AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An 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, or is an important medical events that jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed in the above definition, or a drug-induced liver injury. (NCT00945282)
Timeframe: Up to 38 days

,
InterventionParticipants (Count of Participants)
Any AEAny SAE
GSK2248761 30 mg40
Placebo10

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Number of Participants With Abnormal Electrocardiogram (ECG) Findings

Triplicate 12-lead ECGs were collected at different timepoints, after participants were supine for 5 minutes, during the study using an ECG machine that automatically calculated the heart rate (HR) and measures PR, QRS, QT, and QTc intervals. The three consecutive determinations were collected 5 plus or minus 2 minutes apart and all three tracings were recorded. The participants with abnormal values categorized as abnormal clinically significant (CS) and not clinically significant (NCS) were reported. (NCT00945282)
Timeframe: Day 1, Day 4, Day 7, Day 8 and follow-up

,
InterventionParticipants (Count of Participants)
Day 1, Pre-dose, NCSDay 1, 4 hour, NCSDay 1, 8 hour, NCSDay 4, Pre-dose, NCSDay 4, 4 hour, NCSDay 4, 8 hour, NCSDay 7, Pre-dose, NCSDay 7, 4 hour, NCSDay 7, 8 hour, NCSDay 8, Pre-dose, NCSFollow-up, NCS
GSK2248761 30 mg32222333233
Placebo00000000000

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GSK2248761 PK Parameters Following Dose Administration on Day 7: Predose Concentration (C0), Concentration at End of Dosing Interval (Cτ), Minimum Observed Concentration During One Dosing Interval (Cmin) and Cmax

The C0 was defined as the concentration of drug in plasma, before dose administration on Day 7. Cτ, was defined as the concentration of drug in the plasma at the end of dosing interval. The Cmin was defined as the minimum concentration of the drug in plasma during one dosing interval on Day 7. Cmax represents the maximum concentration of GSK2248761 in the plasma on Day 7. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 7 and used for analysis. (NCT00945282)
Timeframe: Day 7 (Pre -dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose)

Interventionng/mL (Geometric Mean)
C0, Day 7Cτ, Day 7Cmin, Day 7Cmax, Day 7
GSK2248761 30 mg57.4754.2746.37212.93

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GSK2248761 PK Parameters Following Dose Administration on Day 1: Time to Maximum Observed Concentration (Tmax), Terminal Half-life (t1/2), Absorption Lag Time (Tlag)

Tmax is defined as the, time of maximum measured GSK2248761 concentration in the plasma, on Day 1. The t1/2 was defined as the time measured for plasma concentration to decrease by one half. The tlag was defined as the time taken for the drug GSK2248761, to appear in the systemic circulation following administration. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 1 and used for analysis. (NCT00945282)
Timeframe: Day 1 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose)

Interventionhour (Median)
tmaxt1/2tlag
GSK2248761 30 mg4.007.990.49

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GSK2248761 PK Parameters Following Dose Administration on Day 1: Maximum Observed Concentration (Cmax) and Concentration at 24 Hours Post Dose (C24)

Cmax represents the maximum concentration of GSK2248761 in the plasma. C24 is defined as the measure of plasma drug concentration of GSK2248761, 24 hours post dose, determined on Day 1. Serial blood samples were collected on Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 1 and used for analysis.Data for dose normalized Cmax and C24 was reported. (NCT00945282)
Timeframe: Day 1 (Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours)

Interventionng/mL (Geometric Mean)
CmaxC24
GSK2248761 30 mg585.43103.40

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GSK2248761 Pharmacokinetic (PK) Parameters Following Dose Administration on Day 1: Area Under the Plasma Concentration Time Curve 0 to Infinite (AUC[0-∞]) and Area Under the Plasma Concentration Time Curve (AUC [0-24])

AUC (0-24), measured the plasma concentration of GSK2248761 against time, from time zero (pre-dose) to 24 hrs post-dose AUC (0-24) and from time zero to extrapolated infinite time AUC (0-∞). Serial blood samples were collected on Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours postdose on Day 1 and used for analysis. (NCT00945282)
Timeframe: Day 1 (Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose)

Interventionhours*nanograms (ng)/mL (Geometric Mean)
AUC(0-inf)AUC(0-24)
GSK2248761 30 mg2217.731842.19

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Change From Baseline in Vital Signs-systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)

Vital sign measurements for SBP and DBP after sitting for 5 minutes were measured. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 1, 4, 7 , Day 8 and Follow-up (Day 14)

,
Interventionmillimeters of mercury (Mean)
SBP, Day 1, 4 hourSBP, Day 4, Pre-doseSBP, Day 4, 4 hourSBP, Day 7, Pre-doseSBP, Day 7, 4 hourSBP, Day 8SBP, Follow-upDBP, Day 1, 4 hourDBP, Day 4, Pre-doseDBP, Day 4, 4 hourDBP, Day 7, Pre-doseDBP, Day 7, 4 hourDBP, Day 8DBP, Follow-up
GSK2248761 30 mg4.3-0.73.06.29.88.55.88.25.89.78.26.05.24.5
Placebo-4.50.512.56.514.513.514.51.01.03.07.08.015.08.0

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Change From Baseline in HR

Vital sign measurements for HR after sitting for 5 minutes were measured. The average mean values were measured. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 1 (4-hour), Day 4 (Pre-dose and 4 hour), Day 7 (pre-dose and 4-hour), Day 8 and follow up (Day 14)

,
InterventionBeats per minute (Mean)
HR , Day 1, 4 hourHR, Day 4, Pre-doseHR, Day 4, 4 hourHR, Day 7, Pre-doseHR, Day 7, 4 hourHR, Day 8HR, Follow-up
GSK2248761 30 mg-2.5-2.7-2.23.0-0.33.7-0.3
Placebo-3.0-6.0-6.0-1.0-2.50.05.0

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Change From Baseline in Hematology Parameters- Total Neutrophil

The data for hematology parameter total neutrophil count, for the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventiongiga cells per liter (Mean)
Day 2Day 4Day 7Day 8Follow-up
GSK2248761 30 mg243.3508.3-30.0296.776.7
Placebo980.0-375.0-745.0-705.0105.0

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Change From Baseline in Hematology Paramaters-Mean Corpuscle Hemoglobin Concentration

The data for hematology parameter Mean Corpuscle Hemoglobin concentration, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventionpercentage of red blood cells (Mean)
Day 2Day 4Day 7Day 8Follow-up
GSK2248761 30 mg0.020.050.070.02-0.03
Placebo0.550.150.400.150.45

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Change From Baseline in Hematology Paramaters- Red Blood Cell Count

The data for hematology parameter red blood cell count, for the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventionmillion cells per microliter (Mean)
Day 2Day 4Day 7Day 8Follow-up
GSK2248761 30 mg-0.153-0.112-0.083-0.170-0.343
Placebo-0.2400.200-0.190-0.170-0.375

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Change From Baseline in Hematology Paramaters- Platelet Count

The data for hematology parameter platelet count, for the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventionper cubic millimeter (Mean)
Day 2Day 4Day 7Day 8Follow-up
GSK2248761 30 mg-5.75.018.529.323.3
Placebo3.0-23.52.52.0-1.0

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Change From Baseline in Hematology Paramaters- Mean Corpuscle Volume (MCV)

The change from baseline data for hematology parameter MCV, was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventionfemtoliters (Mean)
Day 2Day 4Day 7Day 8Follow-up
GSK2248761 30 mg0.270.15-0.100.130.47
Placebo-0.10-0.20-0.40-0.15-0.50

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Change From Baseline in Hematology Paramaters- Mean Corpuscle Hemoglobin (MCH)

The data for hematology parameter MCH, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventionpicogram (Mean)
Day 2Day 4Day 7Day 8Follow-up
GSK2248761 30 mg0.070.080.030.070.13
Placebo0.450.050.200.100.25

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Change From Baseline in Hematology Paramaters- Hemoglobin

The data for hematology parameter hemoglobin from the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventiongram per decilitre (Mean)
Day 2Day 4Day 7Day 8Follow-up
GSK2248761 30 mg-0.40-0.28-0.25-0.48-0.93
Placebo-0.500.60-0.45-0.45-1.00

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Change From Baseline in Hematology Paramaters- Hematocrit

The data for hematology parameter Hematocrit, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventionpercentage of red blood cells (Mean)
Day 2Day 4Day 7Day 8Follow-up
GSK2248761 30 mg-1.22-0.92-0.80-1.45-2.78
Placebo-2.151.70-1.85-1.55-3.55

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Change From Baseline in Hematology Paramaters- Basophils, Eosinophils, Lymphocytes, Monocytes, White Blood Cell Count

The data for hematology parameters for Basophils, eosinophils, lymphocytes, monocytes, and white blood cell count from the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventionthousand cells per microliter (Mean)
Basophils, Day 2Basophils, Day 4Basophils, Day 7Basophils, Day 8Basophils, Follow-UpEosinophils, Day 2Eosinophils, Day 4Eosinophils, Day 7Eosinophils, Day 8Eosinophils, Follow-UpLymphocytes, Day 2Lymphocytes, Day 4Lymphocytes, Day 7Lymphocytes, Day 8Lymphocytes, Follow-UpMonocytes, Day 2Monocytes, Day 4Monocytes, Day 7Monocytes, Day 8Monocytes, Follow-UpWhite blood cell, Day 2White blood cell, Day 4White blood cell, Day 7White blood cell, Day 8White blood cell, Follow-Up
GSK2248761 30 mg-1.78.31.73.3-3.3-1.7-60.0-38.3-96.7-63.3-120.0268.3126.7273.3-110.028.333.3-15.023.310.0148.3758.345.0500.0-90.0
Placebo-5.05.0-10.0-10.0-15.0-120.0-20.0-50.0-80.0-135.0315.0260.0180.0480.050.0125.0120.025.075.0-115.01295.0-10.0-600.0-240.0-110.0

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Change From Baseline in Clinical Chemistry Parameters- Blood Urea Nitrogen, Triglycerides, Glucose, Creatinine, Calcium, Cholesterol, Total Bilirubin, and Direct Bilirubin.

The data for clinical chemistry parameters- Blood urea nitrogen, triglycerides, glucose, creatinine, calcium, cholesterol, total bilirubin, and direct bilirubin. The change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventionmilligram per deciliter (Mean)
Blood urea nitrogen, Day 2Blood urea nitrogen, Day 4Blood urea nitrogen, Day 7Blood urea nitrogen, Day 8Blood urea nitrogen, Follow-upTriglycerides, Day 2Triglycerides, Day 4Triglycerides, Day 7Triglycerides, Day 8Triglycerides, Follow-upGlucose, Day 2Glucose, Day 4Glucose, Day 7Glucose, Day 8Glucose, Follow-upCreatinine, Day 2Creatinine, Day 4Creatinine, Day 7Creatinine, Day 8Creatinine, Follow-upCalcium, Day 2Calcium, Day 4Calcium, Day 7Calcium, Day 8Calcium, Follow-upCholesterol, Day 2Cholesterol, Day 4Cholesterol, Day 7Cholesterol, Day 8Cholesterol, Follow-upTotal bilirubin, Day 2Total bilirubin, Day 4Total bilirubin, Day 7Total bilirubin, Day 8Total bilirubin, Follow-upDirect bilirubin, Day 2Direct bilirubin, Day 4Direct bilirubin, Day 7Direct bilirubin, Day 8Direct bilirubin, Follow-up
GSK2248761 30 mg1.54.31.02.7-2.2-17.8-19.85.220.8-3.01.30.0-1.8-5.23.0-0.0480.025-0.003-0.060-0.003-0.25-0.13-0.40-0.470.08-11.8-15.3-12.0-8.3-5.5-0.12-0.08-0.03-0.080.08-0.08-0.08-0.05-0.050.02
Placebo-1.04.03.55.51.05.05.520.534.0114.06.0-0.5-1.0-5.010.00.0000.0250.035-0.0400.060-0.250.05-0.20-0.450.05-12.0-17.5-20.5-13.5-0.5-0.10-0.15-0.05-0.100.000.000.000.050.000.10

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Change From Baseline in Clinical Chemistry Paramaters- Uric Acid

The data for clinical chemistry parameters Uric acid, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
InterventionMicromole per liter (Mean)
Uric acid, Day 2Uric acid, Day 4Uric acid, Day 7Uric acid, Day 8Uric acid, Follow-up
GSK2248761 30 mg0.270.17-0.15-0.60-0.53
Placebo-0.55-0.70-0.80-1.05-0.80

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Change From Baseline in Clinical Chemistry Paramaters- Thyroxine, Free

The data for clinical chemistry parameters Thyroxine, free the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
InterventionPicomole per liter (Mean)
Thyroxine free, Day 2Thyroxine free, Day 4Thyroxine free, Day 7Thyroxine free, Day 8Thyroxine free, Follow- up
GSK2248761 30 mg-0.0180.1080.0650.1170.072
Placebo0.0150.1900.1200.1300.135

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Change From Baseline in Clinical Chemistry Paramaters- Thyroxine Total, Thyroxine Binding Globulin, Total T3.

The data for clinical chemistry parameters Thyroxine total, thyroxine binding globulin, Total T3 the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
InterventionNanomoles per liter (Mean)
Thyroxine total, Day 2Thyroxine total, Day 4Thyroxine total, Day 7Thyroxine total, Day 8Thyroxine total, Follow-upThyroxine binding globulin, Day 2Thyroxine binding globulin, Day 4Thyroxine binding globulin, Day 7Thyroxine binding globulin, Day 8Thyroxine binding globulin, Follow-upTotal T3, Day 2Total T3, Day 4Total T3, Day 7Total T3, Day 8Total T3, Follow-up
GSK2248761 30 mg-0.60-0.08-0.280.00-0.37-0.33-5.00-0.670.17-1.83-0.0130.068-0.055-0.035-0.005
Placebo-0.400.500.100.000.052.00-6.50-3.00-1.00-1.000.1700.3100.2250.1900.375

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Change From Baseline in Clinical Chemistry Paramaters- Phosphorus

The data for clinical chemistry paramaters- phosphorous, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
Interventionmillimole per liter (Mean)
Phosphorus, Day 2Phosphorus, Day 4Phosphorus, Day 7Phosphorus, Day 8Phosphorus, Follow-up
GSK2248761 30 mg-0.050.07-0.17-0.27-0.58
Placebo-0.800.25-0.00-0.35-0.95

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Change From Baseline in Clinical Chemistry Paramaters- Alkaline Phosphatase, Alanine Amino Transferase, Aspartate Amino Transferase

The data for clinical chemistry paramaters- alkaline phosphatase, alanine amino transferase, aspartate amino transferase, the change from baseline was reported. The change from baseline was calculated by subtracting the baseline values from the individual post-randomization values. Baseline (pre-dose [Screening, Day -1 or Day 1]) was defined as last available scheduled assessment prior to time of the first dose unless it is specified otherwise. (NCT00945282)
Timeframe: Baseline (pre-dose at Day -1 or Day 1) and Day 2, 4 , 7 , Day 8 and Follow-up (Day 14)

,
InterventionInternational units (IU) per liter (Mean)
Alkaline phosphatase, Day 2Alkaline phosphatase, Day 4Alkaline phosphatase, Day 7Alkaline phosphatase, Day 8Alkaline phosphatase, Follow-upAlanine amino transferase, Day 2Alanine amino transferase, Day 4Alanine amino transferase, Day 7Alanine amino transferase, Day 8Alanine amino transferase, Follow-upAspartate amino transferase, Day 2Aspartate amino transferase, Day 4Aspartate amino transferase, Day 7Aspartate amino transferase, Day 8Aspartate amino transferase, Follow-up
GSK2248761 30 mg-5.8-1.51.83.34.2-3.0-2.01.73.7-7.20.8-0.2-0.31.7-0.2
Placebo-16.0-16.0-7.5-14.5-9.50.5-3.5-3.50.0-1.51.0-4.5-3.00.02.5

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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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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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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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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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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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Adverse Events

Number of reported adverse events, severity of adverse events and relationship to study drug was assessed by questions, physical examination and laboratory parameters. Adverse event data was used to assess the safety and tolerability of low lopinavir/ritonavir doses. (NCT00985543)
Timeframe: Up to 11 weeks from screening to final study visit

Interventionnumber of adverse events (Number)
LPV/r 400/100 mg27
LPV/r 200/150 mg2
LPV/r 200/50 mg4

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Plasma Lopinavir/Ritonavir Concentrations as Measured by the Area Under the Curve (AUC 0-12h).

Pharmacokinetics of plasma lopinavir/ritonavir over a 12-hour dosing interval following administration of lopinavir/ritonavir 400/100mg, 200/150mg and 200/50mg twice daily. (NCT00985543)
Timeframe: at the end of each 7-day dosing phase

Interventionng.h/mL (Geometric Mean)
LPV/r 400/100 mg99599
LPV/r 200/150 mg73603
LPV/r 200/50 mg45146

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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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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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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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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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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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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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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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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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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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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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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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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 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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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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Area Under the Curve From Time 0 to Tau (AUC 0-τ)

Area under the curve from start to elimination. (NCT01057433)
Timeframe: 0, 1, 2, 3, 4, 5, 6, 8, and 12 hours after dosing on days 19 and 24

Interventionng•h/mL (Mean)
All Subjects113.92

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Antepartum Component: Number of Mothers With Obstetrical Complications

"Complications included deaths, diagnoses, signs/symptoms, chemistry lab tests, or hematological lab tests, with grades of 3 (Severe) or worse. Obstetrical complications were those classified by the MedDra coding system as Pregnancy, puerperium and perinatal conditions, except if the condition was the death of the fetus: Abortions not specified as induced or spontaneous, Abortions spontaneous, or Stillbirth and foetal death." (NCT01061151)
Timeframe: Measured through the Week 1 postpartum study visit

InterventionParticipants (Count of Participants)
Period 2
Antepartum Arm C23

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Antepartum Component: Number of Mothers With Obstetrical Complications

"Complications included deaths, diagnoses, signs/symptoms, chemistry lab tests, or hematological lab tests, with grades of 3 (Severe) or worse. Obstetrical complications were those classified by the MedDra coding system as Pregnancy, puerperium and perinatal conditions, except if the condition was the death of the fetus: Abortions not specified as induced or spontaneous, Abortions spontaneous, or Stillbirth and foetal death." (NCT01061151)
Timeframe: Measured through the Week 1 postpartum study visit

,
InterventionParticipants (Count of Participants)
Periods 1 and 2Period 2
Antepartum Arm A8920
Antepartum Arm B7512

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Antepartum Component: Probability of Overall and HIV-free Infant Survival Until 104 Weeks of Age, by Antepartum Arm (in Conjunction With Infants in the Postpartum Component)

For overall survival, failure was defined to be death. For HIV-free survival, failure was defined to be either death or developing HIV. The probability of living, or living without HIV infection, at 104 weeks was calculated by Kaplan-Meier estimation of the survival function. (NCT01061151)
Timeframe: Measured from birth through 104 weeks of age

InterventionProportional probability (Number)
Overall survival, period 2 groupHIV-free survival, period 2 group
Antepartum Arm C0.9420.921

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Antepartum Component: Probability of Overall and HIV-free Infant Survival Until 104 Weeks of Age, by Antepartum Arm (in Conjunction With Infants in the Postpartum Component)

For overall survival, failure was defined to be death. For HIV-free survival, failure was defined to be either death or developing HIV. The probability of living, or living without HIV infection, at 104 weeks was calculated by Kaplan-Meier estimation of the survival function. (NCT01061151)
Timeframe: Measured from birth through 104 weeks of age

,
InterventionProportional probability (Number)
Overall survival, Periods 1 & 2 group (arms A & B only)Overall survival, period 2 groupHIV-free survival, Periods 1&2 group (arms A&B only)HIV-free survival, period 2 group
Antepartum Arm A0.9590.9510.9370.936
Antepartum Arm B0.9670.9820.9470.940

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Postpartum Component: Proportion of Infants Alive Through 12 and 24 Months Post-delivery

Analyses (Kaplan-Meier probabilities) conducted for all individual infants (rather than M-I pair) (NCT01061151)
Timeframe: Measured at 12 and 24 months post-delivery

,
InterventionProbability (Number)
12 months post delivery24 months post delivery
Postpartum Arm A (Maternal Prophylaxis)0.9880.978
Postpartum Arm B (Infant Prophylaxis)0.9890.987

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Antepartum Component: Maternal HIV RNA Less Than 400 Copies/mL at Delivery

Analysis used the principle of intent to treat. (NCT01061151)
Timeframe: Measured at the time of delivery

InterventionParticipants (Count of Participants)Participants (Count of Participants)
Periods 1 and 272329519Periods 1 and 272329520Period 272329520Period 272329519Period 272329521
HIV RNA < 400 copies/mLHIV RNA >= 400 copies/mL
Antepartum Arm A415
Antepartum Arm B1092
Antepartum Arm A929
Antepartum Arm B275
Antepartum Arm A102
Antepartum Arm B259
Antepartum Arm C225
Antepartum Arm A210
Antepartum Arm B62
Antepartum Arm C79

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Maternal Health Component: Incidence Rate of Cardiovascular or Other Metabolic Events

"Cardiovascular or metabolic events of particular concern were included in this analysis. A Poisson model with time to first event as an offset and an over-dispersion parameter was used to estimate incidence rates.~Metabolic events considered were diabetes mellitus, lipodystrophy, or dyslipidemia. Cardiovascular events considered were hypertension, congestive heart failure, stroke, Transient Ischemia Event (TIA), pulmonary embolism, myocardial infarction (whether acute symptomatic or silent), coronary artery disease, deep vein thrombosis, peripheral vascular disease, or symptomatic HIV-associated cardiomyopathy." (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

Interventionevents per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)2.9
Maternal Health Arm B (Discontinue Triple ARVs)5.7

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Postpartum Component: Adherence to the Maternal and/or Infant ARV Regimens, as Measured by Maternal Report and Hair Measures

"Adherence is by maternal report; adherence through hair analysis is not included here.~The protocol did not distinguish between outcomes essential to the primary publication and outcomes for subsequent publications of lesser priority. This outcome measure was listed as secondary in the protocol but the intention was as an exploratory outcome since adherence was not a focus of the study." (NCT01061151)
Timeframe: Week 6 visit (14 days - 9 weeks postpartum); Week 14 visit (10-19 weeks postpartum); Week 26 visit (20 to 31 weeks postpartum); Week 50 visit (44 to 55 weeks postpartum); and Week 74 visit (68 to 80 weeks postpartum).

InterventionParticipants (Count of Participants)
Week 6 visit72329524Week 6 visit72329525Week 14 visit72329524Week 14 visit72329525Week 26 visit72329524Week 26 visit72329525Week 50 visit72329524Week 50 visit72329525Week 74 visit72329524Week 74 visit72329525
Missed dose over 1 month agoNever missed a doseMissed dose 2-4 weeks agoMissed dose within last 2 weeks
Postpartum Arm A (Maternal Prophylaxis)1003
Postpartum Arm B (Infant Prophylaxis)1104
Postpartum Arm A (Maternal Prophylaxis)12
Postpartum Arm A (Maternal Prophylaxis)17
Postpartum Arm B (Infant Prophylaxis)4
Postpartum Arm A (Maternal Prophylaxis)140
Postpartum Arm B (Infant Prophylaxis)74
Postpartum Arm A (Maternal Prophylaxis)956
Postpartum Arm B (Infant Prophylaxis)1081
Postpartum Arm A (Maternal Prophylaxis)20
Postpartum Arm B (Infant Prophylaxis)0
Postpartum Arm A (Maternal Prophylaxis)35
Postpartum Arm A (Maternal Prophylaxis)112
Postpartum Arm B (Infant Prophylaxis)50
Postpartum Arm A (Maternal Prophylaxis)888
Postpartum Arm B (Infant Prophylaxis)1035
Postpartum Arm A (Maternal Prophylaxis)48
Postpartum Arm A (Maternal Prophylaxis)31
Postpartum Arm B (Infant Prophylaxis)8
Postpartum Arm A (Maternal Prophylaxis)103
Postpartum Arm B (Infant Prophylaxis)47
Postpartum Arm A (Maternal Prophylaxis)716
Postpartum Arm B (Infant Prophylaxis)841
Postpartum Arm A (Maternal Prophylaxis)37
Postpartum Arm A (Maternal Prophylaxis)34
Postpartum Arm B (Infant Prophylaxis)7
Postpartum Arm A (Maternal Prophylaxis)64
Postpartum Arm B (Infant Prophylaxis)30
Postpartum Arm A (Maternal Prophylaxis)311
Postpartum Arm B (Infant Prophylaxis)377
Postpartum Arm A (Maternal Prophylaxis)15
Postpartum Arm B (Infant Prophylaxis)2
Postpartum Arm B (Infant Prophylaxis)1
Postpartum Arm B (Infant Prophylaxis)9

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Antepartum Component: Number of Mothers With Grade 3 or Higher Toxicities and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events

These events were graded using the Division of AIDS (DAIDS) AE Grading Table, Version 1.0, December 2004, Clarification August 2009, which is available on the RSC website (http://rsc.tech-res.com). (NCT01061151)
Timeframe: Measured through the Week 1 postpartum study visit

InterventionParticipants (Count of Participants)
Period 2
Antepartum Arm C60

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Antepartum Component: Number of Mothers With Adverse Pregnancy Outcomes (e.g.,Stillbirth, Preterm Delivery (< 37 Weeks), Low Birth Weight (< 2,500 Grams), and Congenital Anomalies)

Composite outcome (NCT01061151)
Timeframe: Measured at birth

,
InterventionParticipants (Count of Participants)
Periods 1 and 2Period 2
Antepartum Arm A38991
Antepartum Arm B563123

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Antepartum Component: Number of Mothers With Adverse Pregnancy Outcomes (e.g.,Stillbirth, Preterm Delivery (< 37 Weeks), Low Birth Weight (< 2,500 Grams), and Congenital Anomalies)

Composite outcome (NCT01061151)
Timeframe: Measured at birth

InterventionParticipants (Count of Participants)
Period 2
Antepartum Arm C111

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Postpartum Component: Proportion of Mother-Infant Pairs With no Death or HIV Diagnosis Through 24 Months Post-delivery

Defined as infant HIV NAT positivity of a specimen drawn at any post-randomization visit, confirmed by HIV NAT positivity of a second specimen drawn at a different time point, or infant death. Analyses (Kaplan-Meier probabilities) were conducted at the Mother-Infant (M-I) pair level, hence the worst outcome for multiple births was counted as a single event. (NCT01061151)
Timeframe: Measured through 24 months post-delivery

InterventionProbability (Number)
Postpartum Arm A (Maternal Prophylaxis)0.971
Postpartum Arm B (Infant Prophylaxis)0.977

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Postpartum Component: Incidence of Grade 3 or Higher Adverse Events and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events

These events were graded using the Division of AIDS (DAIDS) AE Grading Table, Version 1.0, December 2004, Clarification August 2009, which is available on the RSC website (http://rsc.tech-res.com). (NCT01061151)
Timeframe: Measured through site recommended duration of breastfeeding, complete cessation of breastfeeding or 18 months of age, whichever comes first

InterventionNew cases per 100 person-years (Number)
Postpartum Arm A (Maternal Prophylaxis)14.4
Postpartum Arm B (Infant Prophylaxis)14.1

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Postpartum Component: Incidence of Confirmed Infant HIV Infection

Defined as infant HIV NAT positivity of a specimen drawn at any post-randomization visit (i.e., any visit after the Week 1 [Day 6-14] visit), confirmed by HIV NAT positivity of a second specimen drawn at a different time point. Analyses were conducted at the Mother-Infant (M-I) pair level, hence the worst outcome for multiple births was counted as a single event. (NCT01061151)
Timeframe: Measured through site recommended duration of breastfeeding, complete cessation of breastfeeding or 18 months of age, whichever comes first

InterventionNew cases per 100 person-years (Number)
Postpartum Arm A (Maternal Prophylaxis)0.56
Postpartum Arm B (Infant Prophylaxis)0.55

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Maternal Health Component: Toxicity: Incidence of Grade 3 or Greater Laboratory Results or Signs and Symptoms and Selected Grade 2 Hematologic, Renal, and Hepatic Laboratory Results

The maternal safety endpoints summarized include grade 2, 3 or 4 hematologies (hemoglobin (Hb), White Blood Cells (WBC), Absolute Neutrophil Count (ANC), platelet count), chemistries (Alanine Aminotransferase (ALT or SGPT), serum creatinine), and grade 3 or 4 signs and symptoms that occurred post-randomization. These events were graded using the Division of AIDS (DAIDS) AE Grading Table, Version 1.0, December 2004, Clarification August 2009, which is available on the RSC website (http://rsc.tech-res.com). (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

InterventionNew cases per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)15.3
Maternal Health Arm B (Discontinue Triple ARVs)13.9

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Maternal Health Component: Other Targeted Medical Conditions

Other (non-cardiologic) medical conditions of particular concern were included in this outcome. A Poisson model with time to first event as an offset and an over-dispersion parameter was used to estimate incidence rates. Events included were metabolic events, hepatic events, renal events, infections such as pulmonary tuberculosis, malaria, or other serious bacterial infections, and others. (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

Interventionevents per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)4.0
Maternal Health Arm B (Discontinue Triple ARVs)4.6

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Maternal Health Component: Incidence Rate of Progression to AIDS-defining Illness, Death, or a Serious Non-AIDS Cardiovascular, Hepatic, or Renal Event

"This outcome included AIDS-defining illnesses or cardiovascular, hepatic, or renal adverse events of particular concern which were evaluated as serious. Serious outcomes were both those defined as serious according to the International Conference on Harmonization (ICH) definition, or outcomes with grades equal to or worse than 3 (Severe). A Poisson model with time to first event as an offset and an over-dispersion parameter was used to estimate incidence rates. Cardiovascular events considered were hypertension, congestive heart failure, stroke, Transient Ischemia Event (TIA), pulmonary embolism, myocardial infarction (whether acute symptomatic or silent), coronary artery disease, deep vein thrombosis, peripheral vascular disease, or symptomatic HIV-associated cardiomyopathy. Hepatic events considered were cirrhosis and idiopathic sclerosing cholangitis. Renal events considered were renal insufficiency, acute or chronic." (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

Interventionevents per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)0.5
Maternal Health Arm B (Discontinue Triple ARVs)0.9

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Maternal Health Component: Incidence Rate of Death or Any Condition of Particular Concern

Particular events were targeted as those of particular concern. This outcome considered all such events: death, events defining WHO stages II, III, or IV, targeted cardiovascular adverse events, other targeted adverse events, or cancers which were not AIDS-defining. A complete list can be found in Appendix IV of the Protocol. A Poisson model with time to first event as an offset and an over-dispersion parameter was used to estimate incidence rates. (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

Interventionevents per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)9.0
Maternal Health Arm B (Discontinue Triple ARVs)14.0

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Maternal Health Component: Incidence of Tuberculosis

Incidence of tuberculosis. (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

InterventionNew cases per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)0.40
Maternal Health Arm B (Discontinue Triple ARVs)0.31

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Maternal Health Component: Incidence of Progression to AIDS-defining Illness or Death

AIDS-defining illness refers to the WHO Clinical Stage 4 illnesses in Appendix IV of the protocol. These events were reviewed and confirmed by an Endpoint review group. (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

InterventionNew cases per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)0.24
Maternal Health Arm B (Discontinue Triple ARVs)0.49

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Maternal Health Component: Incidence of Death

Number of women who died during the maternal health component; that is, who had been randomized to either continue or discontinue ART after risk of HIV vertical transmission through breastfeeding was over. (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

InterventionNew cases per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)0.24
Maternal Health Arm B (Discontinue Triple ARVs)0.43

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Antepartum Component: Number of Confirmed Infant HIV Infections

Defined as HIV nucleic acid test (NAT) positivity of the specimen drawn at either the birth (Day 0-5) or Week 1 (Day 6-14) visit, confirmed by HIV NAT positivity of a second specimen collected at a different time point (NCT01061151)
Timeframe: Measured at birth or Week 1 study visit

InterventionParticipants (Count of Participants)
Antepartum Arm A25
Antepartum Arm B7
Antepartum Arm C2

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Antepartum Component: Number of Infant HIV Infections

Detected by HIV NAT positivity (NCT01061151)
Timeframe: Measured at the birth (<= 3 days postpartum) visit

InterventionParticipants (Count of Participants)
Antepartum Arm A22
Antepartum Arm B4
Antepartum Arm C2

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Maternal Health Component: Incidence of AIDS-defining Illness

"AIDS-defining illness refers to the WHO Clinical Stage 4 illnesses listed in Appendix IV. Stage 4 illnesses were reviewed and confirmed by an Endpoint review group." (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

InterventionNew cases per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)0.08
Maternal Health Arm B (Discontinue Triple ARVs)0.25

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Antepartum Component: Number of Mothers With Grade 3 or Higher Toxicities and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events

These events were graded using the Division of AIDS (DAIDS) AE Grading Table, Version 1.0, December 2004, Clarification August 2009, which is available on the RSC website (http://rsc.tech-res.com). (NCT01061151)
Timeframe: Measured through the Week 1 postpartum study visit

,
InterventionParticipants (Count of Participants)
Periods 1 and 2Period 2
Antepartum Arm A26159
Antepartum Arm B31861

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Number of Participants With HIV RNA < 50 and <400 Copies/ml.

(NCT01068873)
Timeframe: week 24

InterventionParticipants (Count of Participants)
Open Label Single Arm1

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Number of Participants Who Missed Doses, Interrupt or Discontinue Regimen, and Experience Changes in Dosage or of Combination Regimen

Visits were to occur at approximately 3, 6, 12, and 18 months after starting treatment. The frequency with which each participant forgot to take their medication since the last visit and discontinuations of treatment and the reasons were documented at each visit and are summarized. The number of participants changing from lopinavir/ritonavir soft gel capsule to tablet are also presented. The exact dates of each visit depended on the physician's judgment, so data are reported for Visits 1 through 4 rather than by month. Note: participants may have had multiple missed doses or therapy changes. (NCT01074931)
Timeframe: Month 3, 6, 12, 18

InterventionParticipants (Number)
Total Missed Dosesa) Missed doses reported at Visit 1b) Missed doses reported at Visit 2c) Missed doses reported at Visit 3d) Missed doses reported at Visit 4Discontinued lopinavir/ritonavir therapya) Discontinued due to serious adverse eventb) Discontinued due to economic reasonsInterrupted lopinavir/ritonavir therapya) Interrupted due to adverse eventb) Required treatment with prohibited medicationc) Away because of workTherapy change: Switch from capsule to tableta) Switch from capsule to tablet at Visit 1b) Switch from capsule to tablet at Visit 2c) Switch from capsule to tablet at Visit 3d) Switch from capsule to tablet at Visit 4
Lopinavir/Ritonavir Group499131710651421151351240

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Adverse Events Observed and Development of Lipodystrophy Lesion and Their Locations

The types of adverse events reported are summarized. The presence of lipodystrophy (abnormal body fat distribution) and its location was to be recorded. However, due to an oversight, there was not a place to record the location of lipodystrophy on the case report form. Doctors used clinical judgment to rate lipodystrophy in treatment-experienced participants. Study visits were to occur at approximately 3, 6, 12, and 18 months after starting treatment. The exact dates of each visit depended on the physician's judgment, so data are reported for Visits 1 through 4 rather than by month. (NCT01074931)
Timeframe: Month 3, 6, 12, 18

InterventionParticipants (Number)
Non-serious adverse eventsSerious adverse eventsLipodystrophy: Visit 1 evaluationLipodystrophy: Visit 2 evaluationc) WorsenedLipodystrophy: Visit 3 evaluationb) UnchangedLipodystrophy: Visit 4 evaluationa) Improved
Lopinavir/Ritonavir Group189024651888782878790849750

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Evolution of CD4 Count

The evolution of participants' CD4-positive (CD4+) T-lymphocyte counts after starting the lopinavir/ritonavir-containing regimen was to be assessed by measuring the number of CD4+ cells at baseline and each subsequent study visit. CD4+ count results are reported as the number of CD4+ cells per cubic millimeter (cmm). Study visits were to occur at approximately 3, 6, 12, and 18 months after starting treatment. The exact dates of each visit depended on the physician's judgment, so data are reported for Visits 1 through 4 rather than by month. (NCT01074931)
Timeframe: Month 3, 6, 12, 18

,
Interventioncells per cmm (Mean)
CD4+ count at BaselineCD4+ count at Visit 1CD4+ count at Visit 2CD4+ count at Visit 3CD4+ count at Visit 4
Lopinavir/Ritonavir: Treatment-experienced249.03285.96317.10378.56413.77
Lopinavir/Ritonavir: Treatment-naive101.00136.67200.57200.00239.00

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Evolution of the HIV Viral Response

The protocol recommended that HIV viral load tests be performed at baseline and each study visit. Test results indicate the number of HIV-1 ribonucleic acid (RNA) copies per milliliter (mL). The number of participants who underwent testing and had detectable levels (greater than 50 copies/mL) or undetectable levels (less than 50 copies/mL) are presented by subgroup. Study visits were to occur at approximately 3, 6, 12, and 18 months after starting treatment. The exact dates of each visit depended on the physician's judgment, so data are reported for Visits 1 through 4 rather than by month. (NCT01074931)
Timeframe: Month 3, 6, 12, 18

,
Interventionparticipant (Number)
Viral load detectable at BaselineViral load detectable at Visit 1Viral load detectable at Visit 2Viral load detectable at Visit 3Viral load detectable at Visit 4Viral load undetectable at BaselineViral load undetectable at Visit 1Viral load undetectable at Visit 2Viral load undetectable at Visit 3Viral load undetectable at Visit 4
Lopinavir/Ritonavir: Treatment-experienced51312551522394725
Lopinavir/Ritonavir: Treatment-naive0000010010

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Evolution of the Tolerance Issues

At each study visit, treating physicians evaluated participants and used their clinical judgment to determine if they were tolerating the lopinavir/ritonavir-containing regimen. Study visits were to occur at approximately 3, 6, 12, and 18 months after starting treatment. The exact dates of each visit depended on the physician's judgment, so data are reported for Visits 1 through 4 rather than by month. (NCT01074931)
Timeframe: Month 3, 6, 12, 18

InterventionParticipants (Number)
Lopinavir/ritonavir not tolerated at Visit 1Lopinavir/ritonavir not tolerated at Visit 2Lopinavir/ritonavir not tolerated at Visit 3Lopinavir/ritonavir not tolerated at Visit 4
Lopinavir/Ritonavir Group2000

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The Duration on Treatment Until Development of an Adverse Event Leading to Treatment Discontinuation or Until Escape From Treatment

As so few participants withdrew from lopinavir/ritonavir treatment, durations of lopinavir/ritonavir therapy required for 25 percent, 50 percent and 75 percent of participants could not be established. The numbers of participants in each subgroup who discontinued from treatment due to an adverse event are presented. (NCT01074931)
Timeframe: Month 3, 6, 12, 18

InterventionParticipants (Number)
Lopinavir/Ritonavir Group: Treatment-naive1
Lopinavir/Ritonavir Group: Treatment-experienced5

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Number of Patients Included in Each Center for Disease Control and Prevention (CDC) Classification Category for HIV-infected Adults and Adolescents

Number of patients in each CDC category at Baseline (last assessment within 30 days prior to first dose of Kaletra) and after treatment. CDC categories defined as: Category A (asymptomatic acute HIV infection), Category B (symptomatic HIV infection; not Categories A and C), Category C (acquired immunodeficiency syndrome [AIDS] indicator status), Class P-0 (children not confirmed for HIV infection), Class P-1 (children with asymptomatic HIV infection), or Class P-2 (children with symptomatic HIV infection). (NCT01076972)
Timeframe: Baseline (Month 0) and following last treatment dose during the course of the survey period

,,,,
Interventionparticipants (Number)
Category A after lopinavir/ritonavir treatmentCategory B after lopinavir/ritonavir treatmentCategory C after lopinavir/ritonavir treatmentCategory P-0 after lopinavir/ritonavir treatmentCategory P-1 after lopinavir/ritonavir treatmentCategory P-2 after lopinavir/ritonavir treatmentCategory unknown after treatment
Lopinavir/Ritonavir: Baseline Category A20626000164
Lopinavir/Ritonavir: Baseline Category B032200037
Lopinavir/Ritonavir: Baseline Category C00191000132
Lopinavir/Ritonavir: Baseline Category P-20000001
Lopinavir/Ritonavir: Baseline Category Unknown1032286010199

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Cluster of Differentiation 4 Lymphocyte Count (CD4)

The evolution of patients' CD4-positive (CD4+) T-lymphocyte counts after starting treatment with Kaletra was assessed by measuring the number of CD4+ cells at baseline and each subsequent study visit. CD4+ counts are reported as the number of CD4+ cells per cubic millimeter (cmm) and presented by the mean at each visit. Only observed cases were included in analyses; no data were imputed. n = xx, xx is the number of patients naive to previous antiretroviral treatment and those that were not who had CD4+ T-cell counts available for analysis at each study visit. (NCT01076972)
Timeframe: Baseline (Month 0), every 3 months thereafter up to Month 12 and every year thereafter up to Year 8 (Month 96) during the course of the survey period

,
Interventioncells per cubic millimeter (Mean)
Baseline (Month 0 [n = 416, 420])Month 3 (n = 315, 283)Month 6 (n = 288, 252)Month 9 (n = 223, 238)Month 12 (Year 1 [n = 201, 233])Year 2 (n = 146, 190)Year 3 (n = 106, 150)Year 4 (n = 69, 99)Year 5 (n = 40, 73)Year 6 (n = 25, 42)Year 7 (n = 3, 17)Year 8 (n = 0, 3)
Lopinavir/Ritonavir: Treatment-Experienced290.6342.9366.4385.0410.4437.4481.5526.6496.2569.7597.7493.7
Lopinavir/Ritonavir: Treatment-Naive125.0257.2275.9311.1329.9419.4455.6475.2535.1577.1602.0NA

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Mean Number of Human Immunodeficiency Virus (HIV) Ribonucleic Acid (RNA) Copies Per Milliliter (mL) Using a Logarithmic (Base 10) Transformation at Each Visit

Number of HIV RNA copies per mL is presented by the mean per visit for patients that were naive to previous antiretroviral treatment and those that were not. HIV-RNA data reported as < 400 copies/mL were considered 399 copies/mL in calculations. The mean and standard deviation of HIV-RNA levels were thus calculated after logarithmic (base 10) transformation (log10 399 is 2.6). Only observed cases were included in analyses; no data were imputed. n = xx, xx is the number of treatment-naive, treatment-experienced participants who had CD4+ T-cell counts available for analysis at each study visit. (NCT01076972)
Timeframe: Baseline (Month 0), every 3 months thereafter up to Month 12 and every year thereafter up to Year 8 (Month 96) during the course of the survey period

,
Interventioncopies/mL (Mean)
Baseline (Month 0 [n = 416, 418])Month 3 (n = 315, 280)Month 6 (n = 288, 253)Month 9 (n = 224, 238)Month 12 (Year 1 [n = 203, 230])Year 2 (n = 145, 190)Year 3 (n = 107, 147)Year 4 (n = 70, 99)Year 5 (n = 39, 72)Year 6 (n = 25, 41)Year 7 (n = 3, 17)Year 8 (n = 0, 3)
Lopinavir/Ritonavir: Treatment-experienced3.52.82.82.82.82.72.72.72.82.62.82.6
Lopinavir/Ritonavir: Treatment-Naive4.92.72.72.62.72.72.62.62.72.72.6NA

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Total Number of Patients With Adverse Drug Reactions

"Number of patients with adverse drug reactions, defined as adverse events for which the causal relationship with Kaletra was something other than not related by the investigator (i.e., probable, possible, or unclear), that occurred in ≥ 5% of patients. Adverse drug reactions are reported by preferred term and inclusive of all those reported at each visit. Although a patient may experience a particular preferred term more than once, each patient was counted only once for each preferred term." (NCT01076972)
Timeframe: During the course of the survey period up to Year 8

Interventionparticipants (Number)
Any adverse drug reactionHypertriglyceridaemiaHyperlipidaemiaDiarrhoeaNauseaBlood triglycerides increased
Lopinavir/Ritonavir Group649672111307299

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Number of Patients With Adverse Drug Reactions (ADRs)

"The number of patients (mothers and infants) with adverse drug reactions, defined as adverse events for which the causal relationship with Kaletra was something other than not related by the investigator (i.e., probable, possible, or unclear). ADRs are reported by preferred term and inclusive of all those reported at any visit. Although a patient may experience a particular preferred term more than once, each patient was counted only once for each preferred term." (NCT01076985)
Timeframe: During pregnancy and for one year after birth

,
Interventionparticipants (Number)
AnemiaHypercholesterolemiaHyperlipidemiaDiarrheaNauseaRashAbortion missedPremature laborThreatened laborNeutropeniaHypoglycemiaCardio-respiratory arrestApneaNeonatal respiratory distress syndromeTransient tachypnea of the newbornSmall for dates babyPyrexia
Infants50000100011111111
Lopinavir/Ritonavir21112111100000000

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Percentage of Patients With HIV-1 RNA 50 to <200 Copies/ml

All 3 protocols recommended that HIV viral load tests be performed at Baseline and each study visit. Study visits were to occur at approximately Weeks 4, 12, and 24, followed by 12-week intervals up to Week 144 in therapy-naive participants and up to Week 240 in the pre-treated and non-B subtype groups. The percentage of participants with HIV-1 RNA levels of 50 to less than 200 copies/mL at each time point is presented by subgroup. (NCT01083810)
Timeframe: Baseline, Week 4, 12, 24, followed by 12-week intervals up to 144/240 weeks

,,
InterventionPercentage of participants (Number)
BaselineWeek 4Week 12Week 24Week 36Week 48Week 60Week 72Week 84Week 96Week 108Week 120Week 132Week 144Week 156Week 168Week 180Week 192Week 204Week 216Week 228Week 240
Non-B0142518105636104400008000250
Pre-treated5151520912101713983130005561000
Therapy-naive117322218101359614530NANANANANANANANA

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Change in Absolute CD4 Cell Count [CD4+ Cells/µL]

The evolution of participants' CD4-positive (CD4+) T-lymphocyte counts after starting the lopinavir/ritonavir-containing regimen was to be assessed by measuring the number of CD4+ cells at baseline and each subsequent study visit. Study visits were to occur at approximately Weeks 4, 12, 24, followed by 12-week intervals up to Week 144 in therapy-naive participants and up to Week 240 in the pre-treated and non-B subtype groups. CD4+ cell count results are reported as the change from Baseline in the absolute number of CD4+ cells per microliter. (NCT01083810)
Timeframe: Baseline, Week 4, 12, 24, followed by 12-week intervals up to 144/240 weeks

,,
InterventionCD4+ cells/µL (Mean)
BaselineWeek 4Week 12Week 24Week 36Week 48Week 60Week 72Week 84Week 96Week 108Week 120Week 132Week 144Week 156Week 168Week 180Week 192Week 204Week 216Week 228Week 240
Non-B013192128148204222259226239255275325320404426422474420395399542
Pre-treated06898106144114144179181192223217213251220190174192131210208179
Therapy-naive0140146193211240266248295296329316313292NANANANANANANANA

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Number of Patients With Virus That Develop Mutations Conferring Resistance to Lopinavir/Ritonavir, NRTIs or NNRTIs

Standard genotypic resistance assays were developed for HIV-1 viral load levels greater than 500 to 1000 copies per milliliter (mL). All 3 protocols recommended this testing be done at Baseline prior to lopinavir/ritonavir therapy and (if possible) in cases of virologic failure. The exact timing varied and depended on whether there was an adequate viral load and physician clinical judgment. Participants with resistance to lopinavir/ritonavir, nucleoside reverse transcriptase inhibitors (NRTI) or non-nucleoside reverse transcriptase inhibitors (NNRTI) at Baseline and follow-up are reported. (NCT01083810)
Timeframe: Baseline and at any timepoint where testing is possible

,,
InterventionParticipants (Number)
Genotypic resistance testing performed at BaselineComplete resistance testing results at Baseline>Resistance to lopinavir/ritonavir at Baseline>Partial resistance to NRTI at Baseline>Partial resistance to NNRTI at BaselineUnderwent resistance testing at follow-up>Resistance to lopinavir/ritonavir*>>Resistance to NRTIs>>Resistance to NNRTIs*No baseline results avail for this participant
Non-B55550002000NA
Pre-treated686820021101
Therapy-naive1371220502000NA

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Percentage of Patients With HIV-1 RNA <50 Copies/ml

All 3 protocols recommended that HIV viral load tests be performed at Baseline and each study visit. Study visits were to occur at approximately Weeks 4, 12, and 24, followed by 12-week intervals up to Week 144 in therapy-naive participants and up to Week 240 in the pre-treated and non-B subtype groups. The percentage of participants with HIV-1 ribonucleic acid (RNA) less than 50 copies/mL at each time point is presented by subgroup. (NCT01083810)
Timeframe: Baseline, Week 4, 12, 24, followed by 12-week intervals up to 144/240 weeks

,,
InterventionPercentage of participants (Number)
BaselineWeek 4Week 12Week 24Week 36Week 48Week 60Week 72Week 84Week 96Week 108Week 120Week 132Week 144Week 156Week 168Week 180Week 192Week 204Week 216Week 228Week 240
Non-B054274768079838877878895100100918310010010075100
Pre-treated3263858606765626658666352654852534541504438
Therapy-naive07446975837889879081858788NANANANANANANANA

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Percentage of Patients With HIV-1 RNA >500 Copies/ml

All 3 protocols recommended that HIV viral load tests be performed at Baseline and each study visit. Study visits were to occur at approximately Weeks 4, 12, and 24, followed by 12-week intervals up to Week 144 in therapy-naive participants and up to Week 240 in the pre-treated and non-B subtype groups. The percentage of participants with more than 500 HIV-1 RNA copies/mL at each time point is presented by subgroup. (NCT01083810)
Timeframe: Baseline, Week 4, 12, 24, followed by 12-week intervals up to 144/240 weeks

,,
InterventionPercentage of participants (Number)
BaselineWeek 4Week 12Week 24Week 36Week 48Week 60Week 72Week 84Week 96Week 108Week 120Week 132Week 144Week 156Week 168Week 180Week 192Week 204Week 216Week 228Week 240
Non-B10063154836637985009000000
Pre-treated89463217232118151626262636264338424053405056
Therapy-naive995913666752457813NANANANANANANANA

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Percentage of Patients With HIV-1 RNA 200 to <500 Copies/ml

All 3 protocols recommended that HIV viral load tests be performed at Baseline and each study visit. Study visits were to occur at approximately Weeks 4, 12, and 24, followed by 12-week intervals up to Week 144 in therapy-naive participants and up to Week 240 in the pre-treated and non-B subtype groups. The percentage of participants with HIV-1 RNA levels of 200 to less than 500 copies/mL at each time point is presented by subgroup. (NCT01083810)
Timeframe: Baseline, Week 4, 12, 24, followed by 12-week intervals up to 144/240 weeks

,,
InterventionPercentage of participants (Number)
BaselineWeek 4Week 12Week 24Week 36Week 48Week 60Week 72Week 84Week 96Week 108Week 120Week 132Week 144Week 156Week 168Week 180Week 192Week 204Week 216Week 228Week 240
Non-B0191746139837000000800000
Pre-treated3121569066570901010100100066
Therapy-naive0181231120200230NANANANANANANANA

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Progression-free Survival

Number of patients that remained disease free at 6 months from start of treatment. (NCT01095094)
Timeframe: At 6 months

Interventionparticipants (Number)
Arm I4

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Grade 3-5 Toxicity as Assessed by NCI CTC v3.0

Number of participants with adverse events grades 3-5. For a detailed list of adverse events see the adverse event module. (NCT01095094)
Timeframe: at 6 months from start of treatment

Interventionparticipants (Number)
Arm I7

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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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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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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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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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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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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 4 are presented. (NCT01153269)
Timeframe: Week 4

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST85
HIV-infected Participants With Hepatitis Co-infection: ALT85

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 96 are presented. (NCT01153269)
Timeframe: Week 96

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.6

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 84 are presented. (NCT01153269)
Timeframe: Week 84

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.5

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 72 are presented. (NCT01153269)
Timeframe: Week 72

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.6

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 48 are presented. (NCT01153269)
Timeframe: Week 48

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST60
HIV-infected Participants With Hepatitis Co-infection: ALT79

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 48 are presented. (NCT01153269)
Timeframe: Week 48

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.7

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 4 are presented. (NCT01153269)
Timeframe: Week 4

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection2.5

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 36 are presented. (NCT01153269)
Timeframe: Week 36

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.6

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 24 are presented. (NCT01153269)
Timeframe: Week 24

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.7

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 144 are presented. (NCT01153269)
Timeframe: Week 144

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.5

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 36 are presented. (NCT01153269)
Timeframe: Week 36

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST54
HIV-infected Participants With Hepatitis Co-infection: ALT75

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 24 are presented. (NCT01153269)
Timeframe: Week 24

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST78
HIV-infected Participants With Hepatitis Co-infection: ALT97

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 144 are presented. (NCT01153269)
Timeframe: Week 144

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST52
HIV-infected Participants With Hepatitis Co-infection: ALT53

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 132 are presented. (NCT01153269)
Timeframe: Week 132

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.6

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 120 are presented. (NCT01153269)
Timeframe: Week 120

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.6

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 132 are presented. (NCT01153269)
Timeframe: Week 132

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST49
HIV-infected Participants With Hepatitis Co-infection: ALT51

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 120 are presented. (NCT01153269)
Timeframe: Week 120

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST56
HIV-infected Participants With Hepatitis Co-infection: ALT65

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 12 are presented. (NCT01153269)
Timeframe: Week 12

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST69
HIV-infected Participants With Hepatitis Co-infection: ALT85

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 108 are presented. (NCT01153269)
Timeframe: Week 108

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST47
HIV-infected Participants With Hepatitis Co-infection: ALT43

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Baseline are presented. (NCT01153269)
Timeframe: Baseline

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST64
HIV-infected Participants With Hepatitis Co-infection: ALT69

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 60 are presented. (NCT01153269)
Timeframe: Week 60

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST55
HIV-infected Participants With Hepatitis Co-infection: ALT59

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 108 are presented. (NCT01153269)
Timeframe: Week 108

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.6

[back to top]

Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 12 are presented. (NCT01153269)
Timeframe: Week 12

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection2.0

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 60 are presented. (NCT01153269)
Timeframe: Week 60

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection424

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Baseline are presented. (NCT01153269)
Timeframe: Baseline

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection3.9

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 96 are presented. (NCT01153269)
Timeframe: Week 96

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection503

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 84 are presented. (NCT01153269)
Timeframe: Week 84

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection405

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 72 are presented. (NCT01153269)
Timeframe: Week 72

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection431

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 48 are presented. (NCT01153269)
Timeframe: Week 48

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection402

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 4 are presented. (NCT01153269)
Timeframe: Week 4

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection350

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Viral Load

The decision to perform HIV-1 ribonucleic acid (RNA) tests to monitor participants' viral load was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 60 are presented. (NCT01153269)
Timeframe: Week 60

Interventionlog10 copies/mL (Mean)
HIV-infected Participants With Hepatitis Co-infection1.7

[back to top]

CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 36 are presented. (NCT01153269)
Timeframe: Week 36

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection408

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 24 are presented. (NCT01153269)
Timeframe: Week 24

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection383

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Baseline are presented. (NCT01153269)
Timeframe: Baseline

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection288

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 144 are presented. (NCT01153269)
Timeframe: Week 144

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection525

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 132 are presented. (NCT01153269)
Timeframe: Week 132

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection502

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 120 are presented. (NCT01153269)
Timeframe: Week 120

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection565

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 12 are presented. (NCT01153269)
Timeframe: Week 12

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection378

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CD4 Cell Count

The decision to perform laboratory tests to determine participants' CD4-positive (CD4+) T-lymphocyte counts was left to the treating physician's clinical judgment. The mean and standard deviation for those tested at Week 108 are presented. (NCT01153269)
Timeframe: Week 108

InterventionCD4+ cells/μL (Mean)
HIV-infected Participants With Hepatitis Co-infection581

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Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 96 are presented. (NCT01153269)
Timeframe: Week 96

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST63
HIV-infected Participants With Hepatitis Co-infection: ALT63

[back to top]

Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 84 are presented. (NCT01153269)
Timeframe: Week 84

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST55
HIV-infected Participants With Hepatitis Co-infection: ALT49

[back to top]

Aspartate Aminotransferase (AST) / Alanine Aminotransferase (ALT) Parameters

The decision to perform aspartate aminotransferase (AST) and alanine aminotransferase (ALT) laboratory tests to monitor participants' liver function was left to the treating physician's clinical judgment. The mean values and standard deviations for those tested at Week 72 are presented. (NCT01153269)
Timeframe: Week 72

InterventionU/liter (Mean)
HIV-infected Participants With Hepatitis Co-infection: AST51
HIV-infected Participants With Hepatitis Co-infection: ALT50

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Change in Proviral HIV-1 DNA in Total CD4+ T-cells From Baseline to Week 48 in Participants Randomized to the Intensified Arm Versus the Control Arm Who Received Placebo in Addition to Standard HAART.

The level of HIV Provirus in CD4 T cells obtained from peripheral blood at 48 weeks compared to baseline. A quantitative HIV PCR assay was done. The mean/median values from the standard HAART group is compared to the intensive HAART treatment regimen. (NCT01154673)
Timeframe: Baseline to Week 48

InterventionHIV DNA copies/ million CD4 cells (Median)
Intensive HAART279
Placebo Arm244

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Clearance of Lopinavir/Ritonavir (CL/F)

Clearance of lopinavir/ritonavir, as determined by analysis of 12-hour pharmacokinetic sampling (NCT01172535)
Timeframe: Measured at 4 weeks of treatment prior to the observed dose and at 2, 4, 6, 8, and 12 hours post-dose

InterventionL/h/kg (Geometric Mean)
Lopinavir/Ritonavir0.15

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Adherence

Adherence, defined as proportion of doses taken (note: proportion could be greater than 1.0 for reasons such as tablets having to be taken twice due to first one being spit out or imprecise measurement of liquid doses) (NCT01172535)
Timeframe: Measured at week 4, week 12, and study completion (week 24)

InterventionProportion of expected doses taken (Median)
Week 41.00
Week 120.99
Week 241.00

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Treatment Efficacy (CD4%)

Having CD4%≥25 at the week 24 visit. (NCT01172535)
Timeframe: Measured at entry and study completion (week 24)

Interventionproportion of participants (Number)
Lopinavir/Ritonavir0.71

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Lopinovir/Ritonavir Area Under the Concentration-time Curve (AUC0-24)

Area under the curve over 24 hours (AUC0-24), as determined by a non-compartmental analysis of 12-hour pharmacokinetic sampling for lopinavir/ritonavir (NCT01172535)
Timeframe: Measured at 4 weeks of treatment prior to the observed dose and at 2, 4, 6, 8, and 12 hours post-dose

Interventionmcg*hr/mL (Geometric Mean)
Lopinavir/Ritonavir196

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Maximum Concentration of Lopinavir/Ritonavir (Cmax)

Maximum concentration of lopinavir/ritonavir, as determined by analysis of 12-hour pharmacokinetic sampling (NCT01172535)
Timeframe: Measured at 4 weeks of treatment prior to the observed dose and at 2, 4, 6, 8, and 12 hours post-dose

Interventionmcg/mL (Geometric Mean)
Lopinavir/Ritonavir11.25

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Number of Participants Experiencing Adverse Events of Grade 3 or 4

Adverse events were graded by the Division of AIDS Table for Grading the Severity of Adult and Pediatric Adverse Events, Version 1.0, dated December, 2004, Clarification August 2009, which is available on the RSC web site (http://rsc.tech-res.com/safetyandpharmacovigilance/). Grade 1 = mild, Grade 2 = moderate, Grade 3 = severe, Grade 4 = potentially life-threatening, Grade 5 = death (NCT01172535)
Timeframe: Measured at study visits through end of study (weeks 2, 4, 12, 24)

Interventionparticipants (Number)
Lopinavir/Ritonavir32

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Proportion of Participants Tolerating LPV/r

Participants were considered to have tolerated medication if they did not stop treatment before the 24 week PK visit for any reason other than completing treatment or death not related to treatment. (NCT01172535)
Timeframe: Measured at study completion (week 24)

Interventionproportion of participants (Number)
Lopinavir/Ritonavir0.93

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Proportion of Participants With an AUC of Less Than 10% of Adults

Proportion of participants with an AUC less that 10% of adults (AUC0-24 <104 mcg*hr/mL) (NCT01172535)
Timeframe: Measured at 4 weeks of treatment prior to the observed dose and at 2, 4, 6, 8, and 12 hours post-dose

Interventionproportion of participants (Number)
Lopinavir/Ritonavir0.15

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Treatment Efficacy (HIV Viral Load)

Having HIV viral load <400 copies/mL at the week 24 visit (NCT01172535)
Timeframe: Measured at entry and study completion (week 24)

Interventionproportion of participants (Number)
Lopinavir/Ritonavir0.72

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Minimum Concentration of Lopinavir/Ritonavir (Cmin)

Minimum concentration of lopinavir/ritonavir, as determined by analysis of 12-hour pharmacokinetic sampling (NCT01172535)
Timeframe: Measured at 4 weeks of treatment prior to the observed dose and at 2, 4, 6, 8, and 12 hours post-dose

Interventionmcg/mL (Geometric Mean)
Lopinavir/Ritonavir2.47

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Number of Participants With Grade 3 or Higher Adverse Event (AE) at Least One Grade Higher Than Baseline

The DAIDS Adverse Event (AE) Grading Table, Version 1.0, December 2004 (Clarification, August 2009) was used for grading of AEs. (NCT01352715)
Timeframe: From start of randomized treatment to off randomized treatment (up to 96 weeks)

Interventionparticipants (Number)
Arm A: LPV/r Plus RAL62
Arm B: LPV/r Plus Best Available NRTIs81

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Percentage of Time Spent in Hospital

The percentage of total study time that participants were in hospital. (NCT01352715)
Timeframe: From study entry throughout follow-up (up to 96 weeks)

Interventionpercentage of time spent in hospital (Number)
Arm A: LPV/r Plus RAL0.08
Arm B: LPV/r Plus Best Available NRTIs0.12

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Changes in Fasting Total Cholesterol, High-density Lipoprotein (HDL) Cholesterol, Low-density Lipoprotein (LDL) Cholesterol, Triglycerides, and Glucose From Baseline

Fasting was for 8 hours and the metabolic panel was drawn locally. (NCT01352715)
Timeframe: Study entry and week 48

,
Interventionmg/dL (Mean)
total cholesterol changehigh-density lipoprotein (HDL) cholesterol changelow-density lipoprotein (LDL) cholesterol changetriglycerides changeglucose change
Arm A: LPV/r Plus RAL31417802
Arm B: LPV/r Plus Best Available NRTIs15210313

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Number of Participants With HIV-1 Drug Resistance Mutations in Protease, Reverse Transcriptase, and Integrase in Participants With Virologic Failure at Baseline and at Time of Virologic Failure

Mutations were defined as major IAS mutations in the IAS-USA July 2014 list. New mutations were those detected at virologic failure but not at baseline. (NCT01352715)
Timeframe: From study entry through to week 96

,
Interventionparticipants (Number)
No new IAS mutations1-2 new IAS mutations3 new IAS mutations
Arm A: LPV/r Plus RAL2991
Arm B: LPV/r Plus Best Available NRTIs32130

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Change in CD4+ Cell Count From Baseline to Week 48

Change in CD4+ cell count was calculated as CD4+ cell count at week 48 minus CD4+ cell count at study entry. (NCT01352715)
Timeframe: Study entry and week 48

Interventioncells/mm^3 (Mean)
Arm A: LPV/r Plus RAL199
Arm B: LPV/r Plus Best Available NRTIs190

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Cumulative Probability of Virologic Failure by Week 48

The primary endpoint was time to virologic failure. Virologic failure was defined as confirmed viral load >400 copies/mL at or after week 24. The Kaplan-Meier estimate of the cumulative probability of virologic failure by week 48 was used. (NCT01352715)
Timeframe: From study entry to week 48

Interventioncumulative probability per 100 persons (Number)
Arm A: LPV/r Plus RAL10.3
Arm B: LPV/r Plus Best Available NRTIs12.4

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Number of Participants Discontinuing Randomized Treatment for Toxicity

Discontinuation of randomized treatment for toxicity included participant decision to discontinue for low grade toxicity. Within class NRTI changes were not considered discontinuations. (NCT01352715)
Timeframe: From Start of Randomized Treatment to Off Randomized Treatment (up to 96 weeks)

Interventionparticipants (Number)
Arm A: LPV/r Plus RAL3
Arm B: LPV/r Plus Best Available NRTIs3

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Number of Participants With a New AIDS-defining Events or Death

AIDS-defining events were those recognized by the Centers for Disease Control (CDC) and World Health Organization (WHO) (NCT01352715)
Timeframe: From study entry throughout follow-up (up to 96 weeks)

Interventionparticipants (Number)
Arm A: LPV/r Plus RAL15
Arm B: LPV/r Plus Best Available NRTIs17

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Number of Participants With a Targeted Serious Non-AIDS-defining Event or Death

Serious non-AIDS diagnoses were based on ACTG Appendix 60 Diagnosis Codes (NCT01352715)
Timeframe: From study entry throughout follow-up (up to 96 weeks)

Interventionparticipants (Number)
Arm A: LPV/r Plus RAL7
Arm B: LPV/r Plus Best Available NRTIs7

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Mean Total Body Fat Changes From Baseline to 48 Weeks as Measured by DXA Scan

(NCT01513122)
Timeframe: 48 weeks

Interventionkg (Mean)
Arm 1. Lopinavir / Ritonavir + 2-3N(t)RTI1.4
Arm 2. Lopinavir /Ritonavir + Raltegravir2.1

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Mean Total Cholesterol Changes From Baseline to 48 Weeks

(NCT01513122)
Timeframe: 48 weeks

Interventionmmol/L (Mean)
Arm 1. Lopinavir / Ritonavir + 2-3N(t)RTI0.4
Arm 2. Lopinavir /Ritonavir + Raltegravir0.6

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Mean Triglycerides Changes From Baseline to 48 Weeks

(NCT01513122)
Timeframe: 48 weeks

Interventionmmol/L (Mean)
Arm 1. Lopinavir / Ritonavir + 2-3N(t)RTI0.6
Arm 2. Lopinavir /Ritonavir + Raltegravir0.8

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Mean Bone Mineral Density Changes From Baseline to 48 Weeks as Measured by DXA Scan

(NCT01513122)
Timeframe: 48 weeks

Interventionpercentage change (Mean)
Arm 1. Lopinavir / Ritonavir + 2-3N(t)RTI-5.2
Arm 2. Lopinavir /Ritonavir + Raltegravir-2.9

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Mean Limbs Fat Changes From Baseline to 48 Weeks as Measured by DXA Scan

(NCT01513122)
Timeframe: 48 weeks

Interventionpercentage change (Mean)
Arm 1. Lopinavir / Ritonavir + 2-3N(t)RTI15.7
Arm 2. Lopinavir /Ritonavir + Raltegravir21.1

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Mean Glucose Changes From Baseline to 48 Weeks

(NCT01513122)
Timeframe: 48 weeks

Interventionmmol/L (Mean)
Arm 1. Lopinavir / Ritonavir + 2-3N(t)RTI-0.04
Arm 2. Lopinavir /Ritonavir + Raltegravir-0.1

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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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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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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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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 Reporting a Grade 3 or 4 Laboratory Abnormality

The number of participants reporting a grade 3 (severe) or grade 4 (life-threatening) laboratory abnormality were summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT6
B: Double-dose LPV/r w/RIF3
C: Standard-Dose LPV/r + RAL w/RBT5

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LPV AUC in Participants Enrolled in Arms A, B, and C

Describe LPV plasma PK characteristics (area under the curve [AUC] between 0 and 12 hours) in participants enrolled in Arms A, B, and C, determined by non-compartmental analysis of 12-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous LPV dose and was used as the 12-hour LPV concentration. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, and 6 hours post-dose

Interventionhours*ng/mL (Median)
A: Standard-dose LPV/r w/RBT159796
B: Double-dose LPV/r w/RIF161772
C: Standard-Dose LPV/r + RAL w/RBT149247

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Cumulative Probability of HIV Virologic Failure at Week 72

Virologic failure was defined as the occurrence of two consecutive plasma HIV-1 RNA levels ≥1000 copies/mL at or after 16 weeks and within 24 weeks of treatment initiation or ≥400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized ART was being taken at the time of virologic failure. The percent of participants with HIV virologic failure at week 72 was calculated using a Kaplan-Meier estimator with an associated standard error. The confidence interval was calculated using a log-log transformation. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At weeks 16, 24, 48, and 72

Interventioncumulative events per 100 participants (Number)
A: Standard-dose LPV/r w/RBT29.2
B: Double-dose LPV/r w/RIF50.0
C: Standard-Dose LPV/r + RAL w/RBT30.4

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CD4 Count Change From Baseline to Week 8

The difference in CD4 count from baseline to week 8 was calculated as the CD4 count at week 8 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 8 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT7
B: Double-dose LPV/r w/RIF26
C: Standard-Dose LPV/r + RAL w/RBT37

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CD4 Count Change From Baseline to Week 72

The difference in CD4 count from baseline to week 72 was calculated as the CD4 count at week 72 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 72 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT126
B: Double-dose LPV/r w/RIF212
C: Standard-Dose LPV/r + RAL w/RBT54

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CD4 Count Change From Baseline to Week 48

The difference in CD4 count from baseline to week 48 was calculated as the CD4 count at week 48 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 48 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT99
B: Double-dose LPV/r w/RIF119
C: Standard-Dose LPV/r + RAL w/RBT74

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CD4 Count Change From Baseline to Week 24

The difference in CD4 count from baseline to week 24 was calculated as the CD4 count at week 24 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 24 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT20
B: Double-dose LPV/r w/RIF56
C: Standard-Dose LPV/r + RAL w/RBT13

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Percent of Participants Who Experienced TB Relapse/Recurrence

TB relapse/recurrence was defined as having had 2 consecutive MTB-negative cultures and subsequently had clinical or radiographic deterioration consistent with active TB at or after week 24 and before week 72. The percent of participants who experienced TB relapse/recurrence was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At or after 24 weeks and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF4.2
C: Standard-Dose LPV/r + RAL w/RBT4.3

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RAL AUC in Participants Enrolled in Arm C

Describe RAL plasma PK characteristics (area under the curve [AUC] between 0 and 24 hours) in participants enrolled in Arm C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous RAL dose and was used as the 12-hour RAL concentration. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionhours*ng/mL (Median)
C: Standard-Dose LPV/r + RAL w/RBT11338

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Percent of Participants Whose HIV Viral Load Was Less Than 50 Copies/mL at Week 48

The percent of participants whose HIV viral load was less than 50 copies/mL at week 48 was calculated with an associated standard error. Participants who were lost-to-follow-up or dead by week 48 or had missing RNA at week 48 were coded as having HIV viral load greater than 50 copies/mL. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 48 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT45.8
B: Double-dose LPV/r w/RIF54.2
C: Standard-Dose LPV/r + RAL w/RBT56.5

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Percent of Participants Whose HIV Viral Load Was Less Than 400 Copies/mL at Week 48.

The percent of participants whose HIV viral load was less than 400 copies/mL at week 48 was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. Participants who were lost-to-follow-up or dead by week 48 or had missing results at week 48 were coded as having HIV viral load greater than 400 copies/mL. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 48 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT58.3
B: Double-dose LPV/r w/RIF66.7
C: Standard-Dose LPV/r + RAL w/RBT60.9

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Percent of Participants Who Interrupted or Discontinued at Least One TB Drug Due to Toxicity

The percent of participants who interrupted or discontinued at least one TB drug due to toxicity was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through to the discontinuation of the last TB drug

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT20.8
B: Double-dose LPV/r w/RIF8.3
C: Standard-Dose LPV/r + RAL w/RBT13.0

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Percent of Participants Who Interrupted or Discontinued at Least One HIV Drug Due to Toxicity

The percent of participants who interrupted or discontinued at least one HIV drug due to toxicity was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT20.8
B: Double-dose LPV/r w/RIF16.7
C: Standard-Dose LPV/r + RAL w/RBT21.7

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Percent of Participants Who Experienced TB Treatment Failure

TB treatment failure was defined as having a MTB-positive culture after 16 weeks of TB treatment for a participant who was documented to be taking TB medications. The percent of participants who experienced TB treatment failure was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After 16 weeks and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF0.0
C: Standard-Dose LPV/r + RAL w/RBT0.0

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Percent of Participants Who Experienced TB Relapse/Recurrence and Who Had TB Drug Resistance

TB relapse/recurrence was defined as having had 2 consecutive MTB-negative cultures and subsequently had clinical or radiographic deterioration consistent with active TB at or after week 24 and before week 72. The drug resistance was determined based on phenotypic methods. The percent of participants who experienced TB relapse/recurrence and who had TB drug resistance was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At or after 24 weeks and through week 72

Interventionparticipants (Number)
B: Double-dose LPV/r w/RIF0
C: Standard-Dose LPV/r + RAL w/RBT0

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Percent of Participants Who Experienced Sputum Conversion at Week 8.

Sputum conversion was defined as culture MTB-negative at week 8 or AFB smear negative at week 8 (and culture contaminated or missing at week 8); there were no Xpert MTB/RIF results at week 8. The percent of participants experienced sputum conversion at week 8 was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 8 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT87.5
B: Double-dose LPV/r w/RIF81.8
C: Standard-Dose LPV/r + RAL w/RBT70.0

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Percent of Participants Who Experienced HIV Virologic Failure

Virologic failure was defined as the occurrence of two consecutive plasma HIV-1 RNA levels ≥1000 copies/mL at or after 16 weeks and within 24 weeks of treatment initiation or ≥400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized ART was being taken at the time of virologic failure. Participants who were missing data due to being lost-to-follow-up or dead were coded as virologic failures. The percent of participants who experienced HIV virologic failure was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At weeks 16, 24, 48, and 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT29.2
B: Double-dose LPV/r w/RIF50.0
C: Standard-Dose LPV/r + RAL w/RBT30.4

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Percent of Participants Who Experienced a New AIDS-defining Illness or Died

New post-randomization diagnoses were considered AIDS-defining based on the CDC classification system. The percent of participants who experienced a new AIDS-defining illness or died was calculated with an associated standard error. Confidence intervals were calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT4.2
B: Double-dose LPV/r w/RIF8.3
C: Standard-Dose LPV/r + RAL w/RBT4.3

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Percent of Participants Who Experienced a New AIDS-defining Illness

New post-randomization diagnoses were considered AIDS-defining based on the CDC classification system. The percent of participants who experienced a new AIDS-defining illness was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF4.2
C: Standard-Dose LPV/r + RAL w/RBT0.0

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Number of Participants Who Experienced MTB IRIS

The number of participants who experienced MTB immune reconstitution inflammatory syndrome (IRIS) was summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT1
B: Double-dose LPV/r w/RIF2
C: Standard-Dose LPV/r + RAL w/RBT3

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Number of Participants Reporting a Grade 3 or 4 Sign or Symptom

The number of participants reporting a grade 3 (severe) or grade 4 (life-threatening) sign or symptom were summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT7
B: Double-dose LPV/r w/RIF5
C: Standard-Dose LPV/r + RAL w/RBT5

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Percent of Participants Who Died

The percent of participants who died was calculated with an associated standard error. Confidence intervals were calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT4.2
B: Double-dose LPV/r w/RIF4.7
C: Standard-Dose LPV/r + RAL w/RBT4.3

[back to top]

RBT Cmax and Cmin in Participants Enrolled in Arms A and C

Describe RBT plasma PK characteristics (Cmax and Cmin) in participants enrolled in Arms A and C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 24 hours after the previous RBT dose. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

,
Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
A: Standard-dose LPV/r w/RBT461161
C: Standard-Dose LPV/r + RAL w/RBT349115

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RAL Cmax and Cmin in Participants Enrolled in Arm C

Describe RAL plasma PK characteristics (Cmax and Cmin) in participants enrolled in Arm C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous RAL dose and was used as the 12-hour RAL concentration. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
C: Standard-Dose LPV/r + RAL w/RBT2830166

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LPV Cmax and Cmin in Participants Enrolled in Arms A, B, and C

Describe LPV plasma pharmacokinetic (PK) characteristics (maximum concentration [Cmax] and minimum concentration [Cmin]) in participants enrolled in Arms A, B, and C, determined by non-compartmental analysis of 12-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous LPV dose and was used as the 12-hour LPV concentration. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, and 6 hours post-dose

,,
Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
A: Standard-dose LPV/r w/RBT185319920
B: Double-dose LPV/r w/RIF181388033
C: Standard-Dose LPV/r + RAL w/RBT168028548

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RBT AUC in Participants Enrolled in Arms A and C

Describe RBT plasma PK characteristics (area under the curve [AUC] between 0 and 24 hours) in participants enrolled in Arms A and C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 24 hours after the previous RBT dose. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionhours*ng/mL (Median)
A: Standard-dose LPV/r w/RBT7374
C: Standard-Dose LPV/r + RAL w/RBT5516

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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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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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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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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 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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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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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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Percentage of Participants Adherent to Treatment at Month 12

Adherence was assessed by the Adherence Self-Efficacy Scale (ASES). The ASES is a 12 item tool that measures the patient's confidence to undertake treatment related activities and behaviors including medication regimen, diet and exercise. Each question was answered on a scale from 0 (cannot do at all) to 10 (certain can do). A summative score ranging from 0 to 120 was calculated, with higher scores indicating higher treatment self-efficacy. A participant was considered to have maintained adherence if the change in the ASES summative score at month 12 was greater than or equal to zero. Participants who discontinued from the study or were lost to follow-up were considered non-adherent. (NCT01662336)
Timeframe: Baseline and 12 months

Interventionpercentage of participants (Number)
Lopinavir/Ritonavir + KASA30.2

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Percentage of Participants Adherent to Treatment at Month 6

Adherence was assessed by the Adherence Self-Efficacy Scale (ASES). The ASES is a 12 item tool that measures the patient's confidence to undertake treatment related activities and behaviors including medication regimen, diet and exercise. Each question is answered on a scale from 0 (cannot do at all) to 10 (certain can do). A summative score ranging from 0 to 120 was calculated, with higher scores indicating higher treatment self-efficacy. A participant was considered to have maintained adherence if the change in the ASES summative score at month 6 relative to Baseline was greater than or equal to zero. Participants who discontinued from the study or were lost to follow-up were considered non-adherent. (NCT01662336)
Timeframe: Baseline and 6 months

Interventionpercentage of participants (Number)
Lopinavir/Ritonavir + KASA43.3

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Change From Baseline in Adherence Integration Subscale Score at Months 6 and 12

"Adherence was assessed by the Adherence Self-Efficacy Scale (ASES). The ASES is a 12-item tool that measures the patient's confidence to undertake treatment-related activities and behaviors including medication regimen, diet and exercise. Each question was answered on a scale from 0 (cannot do at all) to 10 (certain can do).~The 12 items converge to two subscales measuring adherence integration and adherence perseverance. The adherence integration subscale score ranges from 0 to 90, with higher scores indicating higher treatment self-efficacy." (NCT01662336)
Timeframe: Baseline, Month 6 and Month 12

Interventionunits on a scale (Mean)
Change from Baseline to Month 6Change from Baseline to Month 12
Lopinavir/Ritonavir + KASA-0.7-3.6

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Change From Baseline in Adherence Perseverance Subscale Score at Months 6 and 12

Adherence was assessed by the Adherence Self-Efficacy Scale (ASES). The ASES is a 12-item tool that measures the patient's confidence to undertake treatment-related activities and behaviors including medication regimen, diet and exercise. Each question was answered on a scale from 0 (cannot do at all) to 10 (certain can do). The 12 items converge to two subscales measuring adherence integration and adherence perseverance. The adherence perseverance subscale score ranges from 0 to 30, with higher scores indicating higher treatment self-efficacy. (NCT01662336)
Timeframe: Baseline, Month 6 and Month 12

Interventionunits on a scale (Mean)
Change from Baseline to Month 6Change from Baseline to Month 12
Lopinavir/Ritonavir + KASA-0.1-1.0

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Change From Baseline in Adherence Summative Score at Months 6 and 12

Adherence was assessed by the Adherence Self-Efficacy Scale (ASES). The ASES is a 12-item tool that measures the participant's confidence to undertake treatment-related activities and behaviors including medication regimen, diet and exercise. Each question was answered on a scale from 0 (cannot do at all) to 10 (certain can do). A summative score ranging from 0 to 120 was calculated, with higher scores indicating higher treatment self-efficacy. (NCT01662336)
Timeframe: Baseline, Month 6 and Month 12

Interventionunits on a scale (Mean)
Change from Baseline to Month 6Change from Baseline to Month 12
Lopinavir/Ritonavir + KASA-1.2-5.1

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Change From Baseline in Coping Self-Efficacy

Change in coping self-efficacy was measured by the Coping Self-Efficacy Scale (CSE), a 26-item questionnaire that measures perceived self-efficacy in coping with daily psychological challenges. A summative score ranging from 0 to 260 was calculated, with higher scores indicating higher coping self-efficacy. (NCT01662336)
Timeframe: Baseline, Month 6 and Month 12

Interventionunits on a scale (Mean)
Change from Baseline to Month 6Change from Baseline to Month 12
Lopinavir/Ritonavir + KASA2.48.1

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Health Resource Utilization

Health resource utilization (HRU) was measured by a self-administered questionnaire that contained a series of questions aimed at measuring the patient's utilization of healthcare resources and economic impact of the disease. (NCT01662336)
Timeframe: Baseline, Month 6 and Month 12

,,
Interventionpercentage of participants (Number)
Emergency RoomAdmitted to HospitalAdmitted to a Long-Term Care FacilityVisit to a Doctor's Office/ ClinicAmbulance ServicePhysiotherapist/ RehabilitationPsychiatrist/ Psychologist/ CounselorNursing ServicesSpecialist
Baseline8.13.50.055.52.93.59.212.716.2
Month 125.53.70.950.51.88.312.811.014.7
Month 68.52.80.750.71.47.712.014.812.7

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Viral Load at Each Visit

(NCT01662336)
Timeframe: Baseline, Month 6 and Month 12

Interventioncopies/mL (Mean)
BaselineMonth 6Month 12
Lopinavir/Ritonavir + KASA111.355.747.2

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Healthcare Provider Satisfaction

For each participant, healthcare provider (HCP) satisfaction with the KASA program was measured by three questions assessing 1) the overall satisfaction with the KASA program, 2) subjective assessment on whether the KASA program was beneficial in maintaining adherence with HIV treatments, and 3) the likelihood of recommending KASA in the future. The scores for each question ranged from 0 to 100, with higher scores indicating higher satisfaction. (NCT01662336)
Timeframe: Month 6 and Month 12

,
Interventionunits on a scale (Mean)
Overall Satisfaction with KASA ProgramBenefits in Maintaining Treatment AdherenceLikelihood to Recommend KASA Program in Future
Month 1273.362.770.0
Month 674.165.674.7

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Cluster of Differentiation 4 (CD4) Positive Cell Counts at Each Visit

(NCT01662336)
Timeframe: Baseline, Month 6 and Month 12

Interventioncells/mm³ (Mean)
BaselineMonth 6Month 12
Lopinavir/Ritonavir + KASA547.0620.8620.2

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Change From Baseline in Psychological Well-being

Change in psychological well-being was measured by the Center for Epidemiologic Studies Depression scale (CES-D), a 20-item questionnaire assessing the presence of depressive state during the previous week. The possible range of scores is 0 to 60, with higher scores indicating the presence of more symptomatology. (NCT01662336)
Timeframe: Baseline, Month 6 and Month 12

Interventionunits on a scale (Mean)
Change from Baseline to Month 6Change from Baseline to Month 12
Lopinavir/Ritonavir + KASA1.71.0

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Change From Baseline in Patient Perception of Stress

Change in perception of stress was measured by the Perceived Stress Scale (PSS), a 10-item questionnaire that assesses the degree to which the participant considered situations as stressful. The PSS score ranges from 0 to 40, with higher scores indicating higher levels of perceived stress. (NCT01662336)
Timeframe: Baseline, Month 6 and Month 12

Interventionunits on a scale (Mean)
Change from Baseline to Month 6Change from Baseline to Month 12
Lopinavir/Ritonavir + KASA-0.3-0.8

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Free Fraction of LPV at Hour 2 Post Dose

Free fraction of steady-state lopinavir at 2 hours post dose (NCT01818258)
Timeframe: Weeks 1, 12 and 24

,
InterventionPercent of Unbound LPV (Mean)
Week 1Week 12Week 24
Normal Nutrition/Mild Malnutrition Cohort3.26.02.1
Severe Malnutrition Cohort0.82.23.1

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HIV Viral Load <400 Copies/mL

Count (%) of participants with plasma HIV RNA viral load <400 copies/mL (NCT01818258)
Timeframe: Baseline and weeks 12, 24, and 48

,
InterventionParticipants (Count of Participants)
BaselineWeek 12Week 24Week 48
Normal Nutrition/Mild Malnutrition Cohort2141818
Severe Malnutrition Cohort281111

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Minimum Trough Concentration (Ctrough) of Lopinavir

Count (%) of participants with minimum trough concentration (Ctrough) of steady-state Lopinavir >= 1 ug/mL (NCT01818258)
Timeframe: Measured 0, 1, 2, 4, 8, and 12 hours post-dose on 1, 4, 8, 12, 16, 24, 36 and 48 weeks following study entry

,
InterventionParticipants (Count of Participants)
Week 1Week 4Week 8Week 12Week 16Week 24Week 36Week 48
Normal Nutrition/Mild Malnutrition Cohort2118181815191918
Severe Malnutrition Cohort1214131711141616

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Plasma Clearance of Lamivudine

Steady-state plasma clearance (CL/F) of Lamivudine (3TC) (NCT01818258)
Timeframe: 0, 1, 2, 4, 8, and 12 hours post-dose on 1, 12, and 24 weeks following study entry

,
InterventionL/hours (Geometric Mean)
3TC CL/F at Week 13TC CL/F at Week 123TC CL/F at Week 24
Normal Nutrition/Mild Malnutrition Cohort8.46.88.8
Severe Malnutrition Cohort8.79.57.5

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Plasma Clearance of Lopinavir

Steady-state plasma clearance (CL/F) of LPV (NCT01818258)
Timeframe: 0, 1, 2, 4, 8, and 12 hours post-dose on 1, 12, and 24 weeks following study entry

,
InterventionL/hours (Geometric Mean)
LPV CL/F at Week 1LPV CL/F at Week 12LPV CL/F at Week 24
Normal Nutrition/Mild Malnutrition Cohort2.01.61.7
Severe Malnutrition Cohort2.22.32.1

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Plasma Clearance of Ritonavir

Steady-state plasma clearance (CL/F) of RTV (NCT01818258)
Timeframe: 0, 1, 2, 4, 8, and 12 hours post-dose on 1, 12, and 24 weeks following study entry

,
InterventionL/hours (Geometric Mean)
RTV CL/F at Week 1RTV CL/F at Week 12RTV CL/F at Week 24
Normal Nutrition/Mild Malnutrition Cohort15.811.211.5
Severe Malnutrition Cohort16.917.314.8

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Plasma Clearance of Zidovudine

Steady-state plasma clearance (CL/F) of Zidovudine (ZDV) (NCT01818258)
Timeframe: 0, 1, 2, 4, 8, and 12 hours post-dose on 1, 12, and 24 weeks following study entry

,
InterventionL/hours (Geometric Mean)
ZDV CL/F at Week 1ZDV CL/F at Week 12ZDV CL/F at Week 24
Normal Nutrition/Mild Malnutrition Cohort58.381.864.0
Severe Malnutrition Cohort34.848.840.8

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Steady-state Lopinavir Area Under the Curve

Steady-state area under the curve (AUC) for Lopinavir (LPV) (NCT01818258)
Timeframe: 0, 1, 2, 4, 8, and 12 hours post-dose on 1, 12, and 24 weeks following study entry

,
Interventionug*hours/mL (Geometric Mean)
Week 1Week 12Week 24
Normal Nutrition/Mild Malnutrition Cohort64.883.479.4
Severe Malnutrition Cohort49.853.064.6

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Steady-state Ritonavir Area Under the Curve

Steady-state area under the curve (AUC) for Ritonavir (RTV) (NCT01818258)
Timeframe: 0, 1, 2, 4, 8, and 12 hours post-dose on 1, 12, and 24 weeks following study entry

,
Interventionug*hours/mL (Geometric Mean)
RTV AUC Week 1RTV AUC Week 12RTV AUC Week 24
Normal Nutrition/Mild Malnutrition Cohort2.13.03.0
Severe Malnutrition Cohort1.61.82.3

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Steady-state Zidovudine Area Under the Curve

Steady-state area under the curve (AUC) of zidovudine (ZDV) (NCT01818258)
Timeframe: 0, 1, 2, 4, 8, and 12 hours post-dose on 1, 12, and 24 weeks following study entry

,
Interventionng*hours/mL (Geometric Mean)
ZDV AUC at Week 1ZDV AUC at Week 12ZDV AUC at Week 24
Normal Nutrition/Mild Malnutrition Cohort1,774.01,335.71,609.3
Severe Malnutrition Cohort2,261.01,826.02,449.7

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Steady-state Lamivudine Area Under the Curve

Steady-state area under the curve (AUC) of Lamivudine (3TC) (NCT01818258)
Timeframe: 0, 1, 2, 4, 8, and 12 hours post-dose on 1, 12, and 24 weeks following study entry

,
Interventionng*hours/mL (Geometric Mean)
3TC AUC at Week 13TC AUC at Week 123TC AUC at Week 24
Normal Nutrition/Mild Malnutrition Cohort5,520.27,233.05,849.2
Severe Malnutrition Cohort4,245.04,365.56,359.0

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Grade 3 or Higher Adverse Events Through 24 Weeks

Number (percent) of participants with at least one grade 3 or higher adverse event (AE) regardless of the relationship to study drugs. (NCT01818258)
Timeframe: From week 0 to week 24

InterventionParticipants (Count of Participants)
Severe Malnutrition Cohort13
Normal Nutrition/Mild Malnutrition Cohort10

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Change in CD4 Percent

Change in CD4 percent from baseline (NCT01818258)
Timeframe: Weeks 0, 12, 24, 36 and 48

,
Interventionpercent (Mean)
Change in CD4 Percent at Week 12Change in CD4 Percent at Week 24Change in CD4 Percent at Week 36Change in CD4 Percent at Week 48
Normal Nutrition/Mild Malnutrition Cohort3.06.87.16.7
Severe Malnutrition Cohort3.39.310.312.7

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Change in HIV Viral Load From Baseline

Change from baseline in plasma HIV RNA viral load (NCT01818258)
Timeframe: Weeks 0, 12, 24, 36 and 48

,
Interventionlog10 copies/mL (Mean)
Change in Log10 Viral Load between Baseline and Week 12Change in Log10 Viral Load between Baseline and Week 24Change in Log10 Viral Load between Baseline and Week 36Change in Log10 Viral Load between Baseline and Week 48
Normal Nutrition/Mild Malnutrition Cohort-2.1-2.5-2.5-2.6
Severe Malnutrition Cohort-1.4-1.7-1.8-1.8

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Change in Mid-upper Arm Circumference

Change in mid-upper arm circumference (MUAC) from entry (NCT01818258)
Timeframe: Weeks 0, 24, and 48

,
Interventioncentimeters (Mean)
Week 24Week 48
Normal Nutrition/Mild Malnutrition Cohort1.21.6
Severe Malnutrition Cohort2.63.5

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Change in WHO Weight-for-height Z-score

Change in WHO weight-for-height Z-score from entry. A Z-score indicates the number of standard deviations the measurement is away from the mean. A Z-score of 0 is equal to the mean of the reference population. Negative numbers indicate values lower than the reference population and positive numbers indicate values higher than the reference population. The reference population was determined by the World Health Organization for children from 0 up to 5 years. (NCT01818258)
Timeframe: Weeks 0, 24, and 48

,
InterventionZ-Score (Mean)
Week 24Week 48
Normal Nutrition/Mild Malnutrition Cohort0.10.4
Severe Malnutrition Cohort2.32.7

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Change From Baseline in Estimated Glomerular Filtration Rate (eGFR)

Glomerular Filtration Rate (eGFR) was estimated from the Modification of Diet in Renal Disease (MDRD)-6 equation. The MDRD-6 equation = 198 × [serum creatinine(mg/dL)]^-0.858 × [age]-0.167 × [0.822 if patient is female] × [1.178 if patient is black] × [serum urea nitrogen concentration (mg/dL)]^-0.293 × [urine urea nitrogen excretion (g/d)]^0.249. (NCT02116660)
Timeframe: Baseline and Week 48

InterventionmL/min (Mean)
Raltegravir Plus Nevirapine Plus Lamivudine-1.1
Protease Inhibitor/Ritonavir Plus Tenofovir/Emtricitabine-5.5

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HIV-1 RNA Viral Load

"Percentage of subjects who have plasma HIV-1 RNA levels <50 cps/ml after 12 weeks of follow-up following a switch to DRV/r monotherapy versus continuing triple therapy containing 2 NRTIs + LPV/r (or ATV/r), using the FDA Time to Loss of Virologic Response method. The FDA 'Snapshot' algorithm evaluates HIV RNA response using only the results at the week 12 time-point which also means that rebound at earlier time-points are not classified as treatment failure, unless it lead to discontinuation prior to the week 48." (NCT02155101)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
ART With 2 NRTIs Plus LPV/r (or ATV/r)35
Darunavir73

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HIV-1 RNA Viral Load

"Percentage of subjects who have plasma HIV-1 RNA levels <50 cps/ml after 24 weeks of follow-up following a switch to DRV/r monotherapy versus continuing triple therapy containing 2 NRTIs + LPV/r (or ATV/r), using the FDA Time to Loss of Virologic Response method. The FDA 'Snapshot' algorithm evaluates HIV RNA response using only the results at the week 24 time-point which also means that rebound at earlier time-points are not classified as treatment failure, unless it lead to discontinuation prior to the week 48." (NCT02155101)
Timeframe: 24 weeks

InterventionParticipants (Count of Participants)
ART With 2 NRTIs Plus LPV/r (or ATV/r)36
Darunavir62

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HIV-1 RNA Viral Load

Percentage of subjects who have plasma HIV-1 RNA levels <400 cps/ml after 24 weeks of follow-up following a switch to DRV/r monotherapy versus continuing triple therapy containing 2 NRTIs + LPV/r (or ATV/r) (FDA Snapshot method). The FDA 'Snapshot' algorithm evaluates HIV RNA response using only the results at the week 24 time-point which also means that rebound at earlier time-points are not classified as treatment failure, unless it lead to discontinuation prior to the week 48. (NCT02155101)
Timeframe: 24 weeks

InterventionParticipants (Count of Participants)
ART With 2 NRTIs Plus LPV/r (or ATV/r)37
Darunavir72

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Number of Participants With Marked Abnormalities in Hematology Laboratory Test Results

Criteria for marked abnormalities in test results: Platelet count >1.5*upper limits of normal (ULN) value, >1.5*ULN if pretreatment (PreRx) value is missing, <0.85*lower limit of normal (LLN) if PreRx ≥LLN, <0.85*LLN if PreRx is missing, <0.85*PreRx if PreRx 1.2*ULN if LLN ≤PreRx ≤ULN, >1.2*ULN if PreRx is missing, >1.5*PreRx if PreRx >ULN, >ULN if PreRx ULN. Lymphocytes >7.5*10^3 c/uL and <0.75*10^3 c/uL. Neutrophils <0.85*PreRx if PreRx <1.5*ULN, <1.5*ULN if PreRx ≥1.5*ULN and <1.5*ULN if PreRx is missing. (NCT02159352)
Timeframe: From start of study treatment (Day 1) to study discharge (up to 15 days)

,,,
Interventionparticipants (Number)
Platelet CountLeukocytesNeutrophils (absolute)Lymphocytes (absolute)
Group 1: Daclatasvir (30 mg) + Darunavir/Ritonavir0121
Group 1: Daclatasvir (60 mg)1000
Group 2: Daclatasvir (30 mg) + Lopinavir/Ritonavir0100
Group 2: Daclatasvir (60 mg)0110

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Dose-normalized Area Under the Concentration-Time Curve in 1 Dosing Interval (AUC[TAU]/D) of Daclatasvir

AUC(TAU)/D was obtained from concentration-time plot of daclatasvir by using noncompartmental method by a validated pharmacokinetic analysis program. (NCT02159352)
Timeframe: Predose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

Intervention(ng*h/mL)/mg (Geometric Mean)
Group 1: Daclatasvir (60 mg)211
Group 1: Daclatasvir (30 mg) + Darunavir/Ritonavir276
Group 2: Daclatasvir (60 mg)230
Group 2: Daclatasvir (30 mg) + Lopinavir/Ritonavir262

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Maximum Observed Plasma Concentration (Cmax) for Daclatasvir

Cmax was obtained from concentration-time plot using a noncompartmental method and a validated pharmacokinetic analysis program. (NCT02159352)
Timeframe: Predose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

Interventionng/mL (Geometric Mean)
Group 1: Daclatasvir (60 mg)1335
Group 1: Daclatasvir (30 mg) + Darunavir/Ritonavir493
Group 2: Daclatasvir (60 mg)1412
Group 2: Daclatasvir (30 mg) + Lopinavir/Ritonavir476

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Number of Participants With Abnormalities in Vital Sign Measurements

Criteria for abnormalities in vital sign measurements: Diastolic blood pressure: Value >90 and change from baseline > 0 or value < 55 and change from baseline <-10. Systolic blood pressure: Value >140 and change from baseline >20 or value <90 and change from baseline <-20. Heart rate: Value >100 and change from baseline >30 or value <55 and change from baseline <-15. Respiration: Value >16 or change from baseline >10. Temperature: Value >38.3°C or change from baseline >1.6°C. (NCT02159352)
Timeframe: From start of study treatment (Day 1) to study discharge (up to 15 days)

Interventionparticipants (Number)
Group 1: Daclatasvir + Darunavir/Ritonavir3
Group 2: Daclatasvir + Lopinavir/Ritonavir2

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Plasma Concentration Observed at 24 Hours Postdose (C24) of Daclatasvir

C24 was obtained from concentration time plot of daclatasvir by using noncompartmental method by a validated pharmacokinetic analysis program. (NCT02159352)
Timeframe: Predose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

Interventionng/mL (Geometric Mean)
Group 1: Daclatasvir (60 mg)225
Group 1: Daclatasvir (30 mg) + Darunavir/Ritonavir250
Group 2: Daclatasvir (60 mg)225
Group 2: Daclatasvir (30 mg) + Lopinavir/Ritonavir280

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Time of Maximum Observed Plasma Concentration (Tmax) of Daclatasvir

Tmax was obtained from concentration-time plot of daclatasvir by using non-compartmental method by a validated pharmacokinetic analysis program. (NCT02159352)
Timeframe: Predose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

Interventionhours (Median)
Group 1: Daclatasvir (60 mg)2.00
Group 1: Daclatasvir (30 mg) + Darunavir/Ritonavir3.00
Group 2: Daclatasvir (60 mg)2.00
Group 2: Daclatasvir (30 mg) + Lopinavir/Ritonavir2.00

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Number of Participants With Serious Adverse Events (SAEs) and Discontinuations Due to Adverse Events (AEs) and Who Died

AE was defined as any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that does not necessarily have a causal relationship with treatment. SAE was defined as a medical event that at any dose resulted in death, persistent or significant disability/incapacity, or drug dependency/abuse; was life threatening, an important medical event, or a congenital anomaly/birth defect; or required or prolonged hospitalization. (NCT02159352)
Timeframe: From start of study treatment (Day 1) to study discharge for AEs (up to 15 days); Day 1 to 30 days after last dose of study treatment for SAEs (up to 44 days)

,,,
Interventionparticipants (Number)
SAEDiscontinued due to AEsDeath
Group 1: Daclatasvir (30 mg) + Darunavir/Ritonavir030
Group 1: Daclatasvir (60 mg)000
Group 2: Daclatasvir (30 mg) + Lopinavir/Ritonavir010
Group 2: Daclatasvir (60 mg)000

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Dose-normalized Maximum Observed Plasma Concentration (Cmax/D) and Dose-normalized Plasma Concentration Observed at 24 Hours Postdose (C24/D) of Daclatasvir

Cmax/D and C24/D are obtained from concentration-time plot of daclatasvir by using noncompartmental method by a validated pharmacokinetic analysis program. (NCT02159352)
Timeframe: Predose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

,,,
Interventionng/mL/mg (Geometric Mean)
Cmax/DC24/D
Group 1: Daclatasvir (30 mg) + Darunavir/Ritonavir16.48.34
Group 1: Daclatasvir (60 mg)22.23.75
Group 2: Daclatasvir (30 mg) + Lopinavir/Ritonavir15.99.33
Group 2: Daclatasvir (60 mg)23.53.76

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Number of Participants With Abnormalities in Electrocardiogram (ECG) Findings

Abnormalities in ECG findings included: PR ≥210 msec, QRS ≥120 msec, QT ≥500 msec, QTcF ≥450 msec, and second- or third-degree heart block. (NCT02159352)
Timeframe: From start of study treatment (Day 1) to study discharge (up to 15 days)

,,,
Interventionparticipants (Number)
PR >210QRS >120QT >500QTcF >450
Group 1: Daclatasvir (30 mg) + Darunavir/Ritonavir4001
Group 1: Daclatasvir (60 mg)2000
Group 2: Daclatasvir (30 mg) + Lopinavir/Ritonavir1000
Group 2: Daclatasvir (60 mg)0000

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Number of Participants With Abnormalities in Urinalysis and Other Chemistry Testing Results

Criteria for marked abnormalities on laboratory test results: urinary dipstick blood: ≥2 if pretreatment (PreRx) <1, ≥2 if PreRx is missing or ≥2*PreRx if PreRx ≥1. Urinary microscopic red blood cell (RBC): ≥2 if PreRx <2, ≥2 if PreRx is missing or ≥4 if PreRx ≥2. Urinary microscopic white blood cell (WBC): ≥2 if PreRx <2, ≥2 if PreRx is missing or ≥4 if PreRx ≥2. Lactate dehydrogenase >1.25*upper limit of normal (ULN) if PreRx ≤ULN, >1.25*ULN if PreRx is missing and >1.5*PreRx if PreRx >ULN. (NCT02159352)
Timeframe: From start of study treatment (Day 1) to study discharge (up to 15 days)

,,,
Interventionparticipants (Number)
Blood, urineRBC, urineWBC, urineLactate dehydrogenase
Group 1: Daclatasvir (30 mg) + Darunavir/Ritonavir1132
Group 1: Daclatasvir (60 mg)2112
Group 2: Daclatasvir (30 mg) + Lopinavir/Ritonavir0001
Group 2: Daclatasvir (60 mg)1001

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Area Under the Concentration-Time Curve in 1 Dosing Interval (AUC[TAU]) for Daclatasvir

AUC(TAU) was the area under the curve from time zero to end of dosing interval. AUC(TAU) was obtained from concentration-time plot of daclatasvir using noncompartmental method and a validated pharmacokinetic analysis program. (NCT02159352)
Timeframe: Predose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

Interventionng*h/mL (Geometric Mean)
Daclatasvir (60 mg) Days 1-412677
Daclatasvir (30 mg) + Darunavir/Ritonavir Days 5-148295
Daclatasvir (60 mg) Days 5-1413799
Daclatasvir (30 mg) + Lopinavir/Ritonavir Days 5-147855

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Absolute Values and Change From Baseline in CD4+ T-cell Counts (Cells/mm^3) at Week 24

(NCT02581202)
Timeframe: Baseline, Week 24

Interventioncells/mm^3 (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants703.4364.70

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Number of Participants With Adverse Events

Adverse events were not recorded in a solicited manner as in an interventional trial, but were recorded by spontaneous reporting in line with the requirements described in European Medicines Agency (EMA) Guideline on Good Pharmacovigilance Practices (GVP) module VI and local pharmacovigilance practice of the Russian Federation. (NCT02581202)
Timeframe: up to Week 48

InterventionParticipants (Count of Participants)
HIV-1 Infected Participants3

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: HDL

(NCT02581202)
Timeframe: Baseline, Week 24

Interventionmmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants1.530.07

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: LDL

(NCT02581202)
Timeframe: Baseline, Week 24

Interventionmmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants2.66-0.07

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Aspartate Aminotransferase (µmol/L)

(NCT02581202)
Timeframe: Baseline, Week 24

Interventionµmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants46.5625.00

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Aspartate Aminotransferase (U/L)

(NCT02581202)
Timeframe: Baseline, Week 24

InterventionU/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants26.90-0.38

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Alanine Aminotransferase (µmol/L)

(NCT02581202)
Timeframe: Baseline, Week 24

Interventionµmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants39.8119.06

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Alanine Aminotransferase (U/L)

(NCT02581202)
Timeframe: Baseline, Week 24

InterventionU/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants29.37-1.31

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Absolute Values and Change From Baseline in HIV-1- RNA Viral Load at Week 48 (Untransformed Data)

Statistics for absolute HIV-1 RNA viral load, where all participants with undetectable HIV-1-RNA viral load data were included into calculations with half of the lower indication limit (50/2 copies/mL, or 25.00 copies/mL). (NCT02581202)
Timeframe: Baseline, Week 48

Interventioncopies/mL (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants25.000.00

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Absolute Values and Change From Baseline in HIV-1- RNA Viral Load at Week 48 (Base-10 Logarithm Transformed Data)

(NCT02581202)
Timeframe: Baseline, Week 48

Interventionlog10 copies/mL (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants3.220.000

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Absolute Values and Change From Baseline in CD4+ T-cell Counts (Cells/mm^3) at Week 48

(NCT02581202)
Timeframe: Baseline, Week 48

Interventioncells/mm^3 (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants752.44111.75

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Absolute Values and Change From Baseline in CD4+ T-cell Counts (%) at Week 48

(NCT02581202)
Timeframe: Baseline, Week 48

Interventionpercentage of lymphocytes that are CD4+ (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants33.111.43

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Absolute Values and Change From Baseline in CD4+ T-cell Counts (%) at Week 24

(NCT02581202)
Timeframe: Baseline, Week 24

Interventionpercentage of lymphocytes that are CD4+ (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants32.500.96

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Absolute Values and Change From Baseline in Anthropometric Measurements At Week 48

(NCT02581202)
Timeframe: Baseline, Week 48

Interventioncm (Mean)
Absolute values: arm circumferenceChange from BL: arm circumferenceAbsolute values: hip circumferenceChange from BL: hip circumferenceAbsolute values: waist circumferenceChange from BL: waist circumference
HIV-1 Infected Participants30.05-0.2055.251.1483.640.63

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Absolute Values and Change From Baseline in Anthropometric Measurements At Week 24

(NCT02581202)
Timeframe: Baseline, Week 24

Interventioncm (Mean)
Absolute values: arm circumferenceChange from BL: arm circumferenceAbsolute values: hip circumferenceChange from BL: hip circumferenceAbsolute values: waist circumferenceChange from BL: waist circumference
HIV-1 Infected Participants29.82-0.3854.620.5783.290.31

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Absolute Values and Change From Baseline (BL) in HIV-1- RNA Viral Load at Week 24 (Untransformed Data)

(NCT02581202)
Timeframe: Baseline, Week 24

Interventioncopies/mL (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants25.220.22

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Serum Creatinine

(NCT02581202)
Timeframe: Baseline, Week 24

Interventionµmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants81.502.36

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Absolute Values and Change From Baseline (BL) in HIV-1- RNA Viral Load at Week 24 (Base-10 Logarithm Transformed Data)

(NCT02581202)
Timeframe: Baseline, Week 24

Interventionlog10 copies/mL (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants3.220.01

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Percentage of Participants on Dual Therapy (LPV/r + 3TC) With Undetectable HIV-1 RNA Level at Week 48

(NCT02581202)
Timeframe: Week 48

Interventionpercentage of participants (Number)
HIV-1 Infected Participants100

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Percentage of Participants on Dual Therapy (LPV/r + 3TC) With Undetectable HIV-1 RNA Level at Week 24

(NCT02581202)
Timeframe: Week 24

Interventionpercentage of participants (Number)
HIV-1 Infected Participants99.5

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Total Cholesterol

(NCT02581202)
Timeframe: Baseline, Week 24

Interventionmmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants5.110.07

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Triglycerides

(NCT02581202)
Timeframe: Baseline, Week 24

Interventionmmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants1.72-0.70

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Alanine Aminotransferase (U/L)

(NCT02581202)
Timeframe: Baseline, Week 48

InterventionU/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants28.35-2.14

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Alanine Aminotransferase (µmol/L)

(NCT02581202)
Timeframe: Baseline, Week 48

Interventionµmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants27.566.81

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Aspartate Aminotransferase (U/L)

(NCT02581202)
Timeframe: Baseline, Week 48

InterventionU/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants26.92-0.49

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Aspartate Aminotransferase (µmol/L)

(NCT02581202)
Timeframe: Baseline, Week 48

Interventionµmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants27.195.63

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Glucose

(NCT02581202)
Timeframe: Baseline, Week 48

Interventionmmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants4.83-0.16

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: HDL

(NCT02581202)
Timeframe: Baseline, Week 48

Interventionmmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants1.43-0.00

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Insulin

(NCT02581202)
Timeframe: Baseline, Week 48

InterventionµEq/mL (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants10.000.69

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Glucose

(NCT02581202)
Timeframe: Baseline, Week 24

Interventionmmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants4.88-0.10

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 24: Insulin

(NCT02581202)
Timeframe: Baseline, Week 24

InterventionµEq/mL (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants10.000.68

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: LDL

(NCT02581202)
Timeframe: Baseline, Week 48

Interventionmmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants2.920.14

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Serum Creatinine

(NCT02581202)
Timeframe: Baseline, Week 48

Interventionµmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants82.132.75

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Total Cholesterol

(NCT02581202)
Timeframe: Baseline, Week 48

Interventionmmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants5.120.11

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Absolute Values and Change From Baseline in Metabolic Parameters at Week 48: Triglycerides

(NCT02581202)
Timeframe: Baseline, Week 48

Interventionmmol/L (Mean)
Absolute valuesChange from BL
HIV-1 Infected Participants1.61-0.06

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Number of Participants Who Developed Resistance to Nucleoside Reverse Transcriptase Inhibitors (NRTIs), Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs), and Protease Inhibitors (PIs)

(NCT02581202)
Timeframe: Week 48

InterventionParticipants (Count of Participants)
NRTINNRTIPI
HIV-1 Infected Participants110

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"Change From Baseline J-Tpeakc With Balanced Ion Channel Drugs (Ranolazine, Verapamil, Lopinavir / Ritonavir)"

"The primary outcome measure for the balanced ion channel drugs (ranolazine, verapamil, lopinavir / ritonavir) is for the upper bound of the 2-sided 90% confidence interval (CI) to be <10 msec for the projected placebo-corrected change from baseline J-Tpeakc effect at the peak plasma level on Day 3 using a linear mixed-effects exposure response model. Placebo drug concentration was set to 0 (see SAP)." (NCT03070470)
Timeframe: 3 days

Interventionms (Median)
Ranolazine-8.3
Verapamil-7.8
Lopinavir / Ritonavir-11.5
Placebo-10.9

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QTc Shortening From Calcium Block (Diltiazem) in the Presence of hERG Block (Dofetilide)

"It will be assessed whether the projected QTc effect of dofetilide alone is significantly greater (i.e., p<0.05) than the projected QTc effect of the combination of dofetilide + diltiazem. This will be assessed at the dofetilide peak plasma level on Day 3 (computed from the combination of dofetilide + diltiazem) on the pooled dofetilide alone, diltiazem alone, and dofetilide + diltiazem data using a linear mixed effects model.~Subsequently, and if the test is significant for QTc, the same test will be performed to assess calcium block (diltiazem) effects on J-Tpeakc." (NCT03070470)
Timeframe: 3 days

Interventionms (Median)
Dofetilide2.2
Diltiazem+Dofetilide-1.7

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"Change From Baseline QTc With Predominant hERG Blocking Drug (Chloroquine)"

"The primary outcome measure for the predominant hERG drug (chloroquine) is for the upper bound of the 2-sided 90% CI to be ≥10 msec for the projected placebo-corrected change from baseline QTc effect at the peak plasma level on Day 1 using a linear mixed-effects exposure response model" (NCT03070470)
Timeframe: 3 days

Interventionms (Median)
Chloroquine17.7
Placebo-9.3

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Time to Resolution of COVID-19 Symptom Resolution in Days

"COVID-19 symptoms are based on the following criteria:~At least TWO of the following symptoms: Fever (≥ 38ºC), chills, rigors, myalgia, headache, sore throat, new olfactory and taste disorder(s), OR~At least ONE of the following symptoms: cough, shortness of breath or difficulty breathing, OR~Severe respiratory illness with at least 1 of the following:~Clinical or radiological evidence of pneumonia, OR~Acute respiratory distress syndrome (ARDS), OR~LRTI, defined by resting SpO2<93% sustained for 2 readings 2 hours apart AND presence of subjective dyspnea or cough Death or COVID-19-related hospitalizations will count as a failure to resolve symptoms." (NCT04354428)
Timeframe: Day 1 through Day 14 after enrolment

InterventionDays (Median)
Ascorbic Acid and Folic Acid11.5
Hydroxychloroquine and Folic Acid10.5
Hydroxychloroquine and AzithromycinNA
Lopinavir-ritonavirNA
Ascorbic AcidNA

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Time to Clearance of Nasal SARS-CoV-2

Time to clearance of nasal SARS-CoV-2, defined as 2 consecutive negative swabs (NCT04354428)
Timeframe: Day 1 through Day 14 after enrolment

InterventionDays (Median)
Ascorbic Acid and Folic Acid7
Hydroxychloroquine and Folic Acid5
Hydroxychloroquine and Azithromycin6
Lopinavir-ritonavir4
Ascorbic Acid5

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Number of Persons With Lower Respiratory Tract Infection (LRTI), Defined as Resting Blood Oxygen Saturation (SpO2<93%) Level Sustained for 2 Readings 2 Hours Apart and Presence of Subjective Dyspnea or Cough

Resting blood oxygen saturation (SpO2<93%) level sustained for 2 readings 2 hours apart and presence of subjective dyspnea or cough (NCT04354428)
Timeframe: 28 days from enrolment

InterventionParticipants (Count of Participants)
Ascorbic Acid and Folic Acid2
Hydroxychloroquine and Folic Acid0
Hydroxychloroquine and Azithromycin4
Lopinavir-ritonavir2
Ascorbic Acid1

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Number of Participants With Serious Adverse Events and Adverse Events Resulting in Treatment Discontinuation

Serious adverse events (including death and hospitalization) and adverse events resulting in treatment discontinuation (NCT04354428)
Timeframe: 28 days from enrolment

InterventionParticipants (Count of Participants)
Ascorbic Acid and Folic Acid6
Hydroxychloroquine and Folic Acid6
Hydroxychloroquine and Azithromycin8
Lopinavir-ritonavir9
Ascorbic Acid1

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Number of Participants With Hospitalization or Mortality

Number of participants with hospitalization or mortality (NCT04354428)
Timeframe: Day 28 after enrolment

InterventionParticipants (Count of Participants)
Ascorbic Acid and Folic Acid4
Hydroxychloroquine and Folic Acid2
Hydroxychloroquine and Azithromycin3
Lopinavir-ritonavir0
Ascorbic Acid1

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Fever-free Days: Day 1 to Day 29 (Group 2 and Placebo Control Group)

Number of days without fever from Day 1 to Day 29 (Group 2 and Placebo Control Group) (NCT04372628)
Timeframe: Day 1 to Day 29

Interventiondays (Median)
Group 2 - Lopinavir/Ritonavir16
Placebo Control Group17

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Hospital-free Days: Day 1 to Day 29 (Group 2 and Placebo Control Group)

Number of days outside the hospital from Day 1 to Day 29 (Group 2 and Placebo Control Group) (NCT04372628)
Timeframe: Day 1 to Day 29

Interventiondays (Median)
Group 2 - Lopinavir/Ritonavir17
Placebo Control Group17

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ICU-free Days: Day 1 to Day 29 (Group 2 and Placebo Control Group)

Number of days outside the ICU from Day 1 to Day 29 (Group 2 and Placebo Control Group) (NCT04372628)
Timeframe: Day 1 to Day 29

Interventiondays (Median)
Group 2 - Lopinavir/Ritonavir17
Placebo Control Group17

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Time to Hospitalization Day 1 to Day 29 (Group 2 and Placebo Control Group)

Number of days from enrollment to hospitalization (Group 2 and Placebo Control Group) (NCT04372628)
Timeframe: Day 1 to Day 29

Interventiondays (Median)
Group 2 - Lopinavir/Ritonavir6
Placebo Control Group7

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Time to Symptom Resolution: Day 1 to Day 29 (Group 2 and Placebo Control Group)

Number of days from enrollment to resolution of COVID-19 symptoms (Group 2 and Placebo Control Group) (NCT04372628)
Timeframe: Day 1 to Day 29

Interventiondays (Median)
Group 2 - Lopinavir/Ritonavir11
Placebo Control Group11

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Vasopressor-free Days Through Study Day 29 (Group 2 and Placebo Control Group)

Number of vasopressor-free days through Study Day 29 (Group 2 and Placebo Control Group) (NCT04372628)
Timeframe: Day 1 to Day 29

Interventiondays (Median)
Group 2 - Lopinavir/Ritonavir17
Placebo Control Group17

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Ventilator-free Days: Day 1 to Day 29 (Group 2 and Placebo Control Group)

Number of days without ventilator use from Day 1 to Day 29 (Group 2 and Placebo Control Group) (NCT04372628)
Timeframe: Day 1 to Day 29

Interventiondays (Median)
Group 2 - Lopinavir/Ritonavir17
Placebo Control Group17

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Oxygen-free Days: Day 1 to Day 29 (Group 2 and Placebo Control Group)

Number of Days without oxygen Day 1 to Day 29 (Group 2 and Placebo Control Group) (NCT04372628)
Timeframe: Day 1 to Day 29

Interventiondays (Median)
Group 2 - Lopinavir/Ritonavir17
Placebo Control Group17

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