rilpivirine profile

ID Source	ID
PubMed CID	6451164
CHEMBL ID	175691
CHEBI ID	68606
SCHEMBL ID	385113
SCHEMBL ID	384696
MeSH ID	M0482137

Synonym
HY-10574
rilpivirine ,
r278474 ,
4-{4-[4-((e)-2-cyano-vinyl)-2,6-dimethyl-phenylamino]-pyrimidin-2-ylamino}-benzonitrile
edurant(tm)
tmc278
4-[[4-[4-[(e)-2-cyanovinyl]-2,6-dimethyl-anilino]pyrimidin-2-yl]amino]benzonitrile
T27 ,
4-{[4-({4-[(e)-2-cyanoethenyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
r-278474
CHEMBL175691
r 278474
chebi:68606 ,
fi96a8x663 ,
hsdb 8153
rilpivirine [usan:inn]
unii-fi96a8x663
tmc 278
benzonitrile, 4-((4-((4-((1e)-2-cyanoethenyl)-2,6-dimethylphenyl)amino)-2-pyrimidinyl)amino)-
4-((4-((4-((1e)-2-cyanoethenyl)-2,6-dimethylphenyl)amino)-2-pyrimidinyl)amino)benzonitrile
rilpivirine (jan/usan/inn)
D09720
A827939
500287-72-9
4-[[4-[4-[(e)-2-cyanoethenyl]-2,6-dimethylanilino]-2-pyrimidinyl]amino]benzonitrile
4-[[4-[[4-[(e)-2-cyanoethenyl]-2,6-dimethyl-phenyl]amino]pyrimidin-2-yl]amino]benzenecarbonitrile
BCP9000016
BCP0726000192
CS-0440
4-{[4-({4-[(e)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
AKOS015901680
S7303
STL484047
rilpivirine [mi]
rilpivirine [who-dd]
rilpivirine [orange book]
rilpivirine [mart.]
rilpivirine [vandf]
rilpivirine [jan]
4-{[4-({4-[(1e)-2-cyanoethenyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
rilpivirine [inn]
benzonitrile, 4-((4-((4-((1e)-2-cyanoethenyl)-2,6-dimethylphenyl)amino)-2- pyrimidinyl)amino)-
cabenuva component rilpivirine
rilpivirine [usan]
rilpivirine component of cabenuva
DB08864 ,
KE-0036
YIBOMRUWOWDFLG-ONEGZZNKSA-N
SCHEMBL385113
SCHEMBL384696
W-202888
(e)-4-((4-((4-(2-cyanovinyl)-2,6-dimethylphenyl)amino)pyrimidin-2-yl)amino)benzonitrile
AC-30619
(e)-4-(4-(4-(2-cyanovinyl)-2,6-dimethylphenylamino)pyrimidin-2-ylamino)benzonitrile
4-[[4-[[4-[(e)-2-cyanoethenyl]-2,6-dimethyl-phenyl]amino]pyrimidin-2-yl]amino]benzonitrile
DTXSID10198189 ,
EX-A245
mfcd11046372
bdbm222178
SW220232-1
rilpivirine(r 278474, tmc 278)
r278474;tmc278
BCP03563
Q421547
500287-72-9 (free base)
rilpivirine free base
(e)-3-{4-[2-(p-cyanophenylamino)-4-pyrimidinylamino]-3,5-xylyl}acrylonitrile; 4-[[4-[[4-[(1e)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
CCG-268241
NCGC00319175-03
rilpivirine z-isomer hcl
NCGC00319175-08
gtpl11387
rilpivirina
EN300-21682062
4-{[4-({4-[(1e)-2-cyanoeth-1-en-1-yl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
4-[[4-[[4-[(1e)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
rilpivirine (mart.)
rilpivirinum
dtxcid90120680
4-((4-((4-((e)-2-cyanoethenyl)-2,6-dimethylphenyl)amino)pyrimidin-2-yl)amino)benzonitrile
4-((4-((4-((e)-2-cyanovinyl)-2,6-dimethylphenyl)amino)pyrimidin-2-yl)amino)benzonitrile
4-((4-((4-((1e)-2-cyanoethenyl)-2,6-dimethylphenyl)amino)pyrimidin-2-yl)amino)benzonitrile
j05ag05

Excerpt	Reference	Relevance
" The incidences of the most commonly reported grade 2-4 adverse events at least possibly related to study medication, including nausea, dizziness, abnormal dreams/nightmare, dyspepsia, asthenia, rash, somnolence and vertigo, were low and lower with TMC278 than with efavirenz."	( Efficacy and safety of TMC278 in antiretroviral-naive HIV-1 patients: week 96 results of a phase IIb randomized trial. Boven, K; Grinsztejn, B; Katabira, E; Lupo, SH; Morales-Ramirez, J; Pozniak, AL; Rimsky, LT; Ruxrungtham, K; Santoscoy, M; Steyn, D; Vanveggel, S, 2010)	0.36
" TMC278 was well tolerated with lower incidences of neurological and psychiatric adverse events, rash and lower lipid elevations than those with efavirenz."	( Efficacy and safety of TMC278 in antiretroviral-naive HIV-1 patients: week 96 results of a phase IIb randomized trial. Boven, K; Grinsztejn, B; Katabira, E; Lupo, SH; Morales-Ramirez, J; Pozniak, AL; Rimsky, LT; Ruxrungtham, K; Santoscoy, M; Steyn, D; Vanveggel, S, 2010)	0.36
" In the week 192 analysis, RPV compared with EFV was associated with a lower overall incidence of grade 2-4 adverse events (AEs) at least possibly related to treatment, including rash (p<0."	( Long-term efficacy, safety, and tolerability of rilpivirine (RPV, TMC278) in HIV type 1-infected antiretroviral-naive patients: week 192 results from a phase IIb randomized trial. Boven, K; Grinsztejn, B; Lupo, SH; Morales-Ramirez, J; Pozniak, AL; Rimsky, LT; Ruxrungtham, K; Santoscoy, M; Vanveggel, S; Wilkin, A, 2012)	0.38
" Rilpivirine compared with efavirenz gave smaller incidences of adverse events leading to discontinuation (3% vs."	( Efficacy and safety of rilpivirine (TMC278) versus efavirenz at 48 weeks in treatment-naive HIV-1-infected patients: pooled results from the phase 3 double-blind randomized ECHO and THRIVE Trials. Boven, K; Cahn, P; Clotet, B; Cohen, CJ; Crauwels, H; Fourie, J; Grinsztejn, B; Johnson, MA; Lefebvre, E; Molina, JM; Rimsky, LT; Saag, M; Supparatpinyo, K; Vanveggel, S; Williams, P; Wu, H, 2012)	0.38
" Beyond week 48, the incidence of virologic failure was comparable (3 versus 2%) between treatment groups, rilpivirine resistance-associated mutations were consistent with those observed in year 1, there were few adverse events in both groups and no new safety concerns."	( Week 96 efficacy and safety of rilpivirine in treatment-naive, HIV-1 patients in two Phase III randomized trials. Boven, K; Cassetti, I; Chetchotisakd, P; Cohen, CJ; Crauwels, H; Lazzarin, A; Li, T; Molina, JM; Orkin, C; Rhame, F; Rimsky, L; Stellbrink, HJ; Vanveggel, S; Williams, P, 2013)	0.39
" However, data on the long-term exposure to these therapeutic options are needed, and a handful of case reports are emerging, reporting rare but potentially life-threatening adverse hepatic events in patients with hepatitis co-infection or taking other hepatotoxic drugs."	( Hepatoxicity of new antiretrovirals: a systematic review. Lacombe, K; Surgers, L, 2013)	0.39
" The pathogenic mechanisms involved are related to hypersensitivity, as described with nevirapine, impaired metabolism and therefore increased drug levels, and direct toxic effects with production of toxic metabolites."	( Liver toxicity in HIV-infected patients receiving novel second-generation nonnucleoside reverse transcriptase inhibitors etravirine and rilpivirine. Casado, JL, )	0.13
"Due to ongoing neuropsychiatric adverse events in some efavirenz (EFV)-treated patients, a switch to an alternative non-nucleoside reverse transcriptase inhibitor may be considered."	( Efficacy and safety 48 weeks after switching from efavirenz to rilpivirine using emtricitabine/tenofovir disoproxil fumarate-based single-tablet regimens. Brinson, C; Cheng, AK; Chuck, SK; Cohen, C; Dejesus, E; Mills, AM; Ramanathan, S; Wang, MH; White, K; Williams, S; Yale, KL, )	0.13
" No subjects discontinued the study due to an adverse event."	( Efficacy and safety 48 weeks after switching from efavirenz to rilpivirine using emtricitabine/tenofovir disoproxil fumarate-based single-tablet regimens. Brinson, C; Cheng, AK; Chuck, SK; Cohen, C; Dejesus, E; Mills, AM; Ramanathan, S; Wang, MH; White, K; Williams, S; Yale, KL, )	0.13
" All studies have found a lower incidence and severity of neuropsychiatric adverse effects, a better lipid profile, and a lower number of patients with subclinical transaminase elevation in patients treated with rilpivirine."	( [Safety profile of rilpivirine: general and neuropsychiatric tolerability, safety in patients with hepatitis B or C viruses, and lipid profile]. López Cortés, LF; Martínez, E; von Wichmann, MÁ, 2013)	0.39
"Growing evidence associates the non-nucleoside reverse transcriptase inhibitor efavirenz with several adverse events."	( Lack of mitochondrial toxicity of darunavir, raltegravir and rilpivirine in neurons and hepatocytes: a comparison with efavirenz. Alegre, F; Apostolova, N; Blas-García, A; Esplugues, JV; Funes, HA; Martínez, E; Polo, M, 2014)	0.4
"Darunavir, rilpivirine and raltegravir do not induce toxic effects on Hep3B cells and primary rat neurons, which suggests a safer hepatic and neurological profile than that of efavirenz."	( Lack of mitochondrial toxicity of darunavir, raltegravir and rilpivirine in neurons and hepatocytes: a comparison with efavirenz. Alegre, F; Apostolova, N; Blas-García, A; Esplugues, JV; Funes, HA; Martínez, E; Polo, M, 2014)	0.4
" 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
" There were no grade 3 or 4 adverse events and no clinically significant trends in laboratory abnormalities, electrocardiograms, or vital signs."	( Pharmacokinetics, safety, and tolerability with repeat doses of GSK1265744 and rilpivirine (TMC278) long-acting nanosuspensions in healthy adults. Crauwels, H; Ford, SL; Gould, E; Lou, Y; Margolis, D; Piscitelli, S; Spreen, W; Stevens, M; Williams, P, 2014)	0.4
" The incidences of the most commonly reported adverse events related to study medication, including rash, and neurological events, were lower with rilpivirine than with efavirenz (RR = 0."	( Effectiveness and safety of rilpivirine, a non-nucleoside reverse transcriptase inhibitor, in treatment-naive adults infected with HIV-1: a meta-analysis. Li, SL; Lu, ZJ; Sun, GX; Xu, P; Zhang, L, )	0.13
"Grade 1/2 RPV-related adverse events in the 300, 600 and 1200/600/600 mg groups were: rash (zero, one and one subject, respectively, the last of whom discontinued participation in the study); musculoskeletal stiffness (three, zero and zero subjects, respectively); injection site reactions (one, two and two subjects, respectively)."	( Safety, tolerability and pharmacokinetics of rilpivirine following administration of a long-acting formulation in healthy volunteers. Crauwels, H; Deleu, S; Meyvisch, P; Niemeijer, N; Verloes, R; Williams, P, 2015)	0.42
" The study limitations include its retrospective design, the relatively short follow-up, and the absence of data concerning the severity of clinical adverse events; however, it does provide new information concerning the laboratory changes that occur in patients switching from PI-based or PI-sparing regimens to RTE STR."	( Efficacy and safety in clinical practice of a rilpivirine, tenofovir and emtricitabine single-tablet regimen in virologically suppressed HIV-positive patients on stable antiretroviral therapy. Bossolasco, S; Castagna, A; Cernuschi, M; Cinque, P; Galli, L; Gianotti, N; Lazzarin, A; Maillard, M; Nozza, S; Poli, A; Spagnuolo, V; Tambussi, G, 2015)	0.42
" RPV-based regimens were overall well tolerated and only 23 (8%) patients discontinued ART because of adverse events, mostly neuropsychiatric adverse events."	( Efficacy and safety of a switch to rilpivirine-based regimens in treatment-experienced HIV-1-infected patients: a cohort study. Delaugerre, C; Denis, B; Desseaux, K; Fonsart, J; Gatey, C; Gazaignes, S; Guionie, M; Molina, JM; Resche-Rigon, M; Rozenbaum, W; Yang, C, 2016)	0.43
" Additional assessments included CD4 cell counts, genotypic/phenotypic resistance, adverse events, patient-reported outcomes, and quality of life questionnaires."	( Rilpivirine vs. efavirenz-based single-tablet regimens in treatment-naive adults: week 96 efficacy and safety from a randomized phase 3b study. Antinori, A; Arribas, JR; Bloch, M; Bosse, M; Chuck, SK; Cohen, CJ; De-Oertel, S; Garner, W; Piontkowsky, D; Porter, D; Rachlis, A; Rieger, A; Segal-Maurer, S; van Lunzen, J; Wohl, DA, 2016)	0.43
" Compared with EFV/FTC/TDF, RPV/FTC/TDF was associated with fewer adverse event-related discontinuations (3."	( Rilpivirine vs. efavirenz-based single-tablet regimens in treatment-naive adults: week 96 efficacy and safety from a randomized phase 3b study. Antinori, A; Arribas, JR; Bloch, M; Bosse, M; Chuck, SK; Cohen, CJ; De-Oertel, S; Garner, W; Piontkowsky, D; Porter, D; Rachlis, A; Rieger, A; Segal-Maurer, S; van Lunzen, J; Wohl, DA, 2016)	0.43
" Two patients were lost to follow-up and five ceased the new regimen (4 due to adverse effects and 1 virologic failure)."	( Efficacy and safety of switching to abacavir/lamivudine (ABC/3TC) plus rilpivirine (RPV) in virologically suppressed HIV-infected patients on HAART. González-Domenech, CM; Hernández-Quero, J; Martínez, MA; Mayorga, ML; Olalla, J; Omar, M; Palacios, R; Pérez-Camacho, I; Pérez-Hernández, IA; Romero, A; Romero, JM; Santos, J, 2016)	0.43
" At week 48, adverse events considered possibly related to treatment occurred in 13 (36%) patients, mostly (excluding investigations) somnolence (n = 5, 14%) and nausea (n = 2, 6%)."	( Rilpivirine as a Treatment for HIV-infected Antiretroviral-naïve Adolescents: Week 48 Safety, Efficacy, Virology and Pharmacokinetics. Bunupuradah, T; Crauwels, H; Flynn, PM; Hoogstoel, A; Lombaard, J; Ramapuram, J; Ssali, F; Stevens, M; Van Eygen, V, 2016)	0.43
" The secondary objectives analyzed were adverse effects changes in renal, hepatic or lipid profiles, changes in CD4+ cell count and treatment discontinuations."	( Abacavir/Lamivudine plus Rilpivirine Is an Effective and Safe Strategy for HIV-1 Suppressed Patients: 48 Week Results of the SIMRIKI Retrospective Study. Barrufet, P; Berenguer, J; Boix, V; Carrero, A; Castaño, M; Esteban, H; Galindo, MJ; González-García, J; Hontañón, V; Imaz, A; Knobel, H; Moreno, S; Podzamczer, D; Raffo, M; Ribera, E; Ryan, P; Solís, J; Suárez-Lozano, I; Terrón, JA; Troya, J; Yllescas, M, 2016)	0.43
" Thirty-eight adverse events (AE) were detected in 32 patients."	( Abacavir/Lamivudine plus Rilpivirine Is an Effective and Safe Strategy for HIV-1 Suppressed Patients: 48 Week Results of the SIMRIKI Retrospective Study. Barrufet, P; Berenguer, J; Boix, V; Carrero, A; Castaño, M; Esteban, H; Galindo, MJ; González-García, J; Hontañón, V; Imaz, A; Knobel, H; Moreno, S; Podzamczer, D; Raffo, M; Ribera, E; Ryan, P; Solís, J; Suárez-Lozano, I; Terrón, JA; Troya, J; Yllescas, M, 2016)	0.43
" The safety of RPV/FTC/TDF (incidence of adverse events leading to discontinuation and laboratory abnormalities) and adherence to this regimen were evaluated, and the cost of switching was analysed."	( Switching to a rilpivirine/emtricitabine/tenofovir single-tablet regimen in RNA-suppressed patients infected with human immunodeficiency virus 1: Effectiveness, safety and costs at 96 weeks. Arrabal-Durán, P; Chamorro-de-Vega, E; Gijón-Vidaurreta, P; Herranz-Alonso, A; Rodríguez-González, CG; Sanjurjo-Sáez, M, 2017)	0.46
" However, the relatively high rates of virological failure and treatment discontinuation because of adverse events make this combination a less favourable choice over other regimens currently available."	( Switching to a rilpivirine/emtricitabine/tenofovir single-tablet regimen in RNA-suppressed patients infected with human immunodeficiency virus 1: Effectiveness, safety and costs at 96 weeks. Arrabal-Durán, P; Chamorro-de-Vega, E; Gijón-Vidaurreta, P; Herranz-Alonso, A; Rodríguez-González, CG; Sanjurjo-Sáez, M, 2017)	0.46
" Safety (incidence of adverse events leading to discontinuation and laboratory abnormalities), adherence, and costs were analyzed."	( Effectiveness, Safety, and Costs of a Treatment Switch to Dolutegravir Plus Rilpivirine Dual Therapy in Treatment-Experienced HIV Patients. Alonso, R; Chamorro-de-Vega, E; Herranz-Alonso, A; Revuelta-Herrero, JL; Rodríguez-González, CG; Sanjurjo-Sáez, M, 2018)	0.48
"Switching to DTG plus RPV seems to be an effective and safe strategy."	( Effectiveness, Safety, and Costs of a Treatment Switch to Dolutegravir Plus Rilpivirine Dual Therapy in Treatment-Experienced HIV Patients. Alonso, R; Chamorro-de-Vega, E; Herranz-Alonso, A; Revuelta-Herrero, JL; Rodríguez-González, CG; Sanjurjo-Sáez, M, 2018)	0.48
" Investigators monitored adverse events to assess safety."	( Efficacy, safety, and tolerability of dolutegravir-rilpivirine for the maintenance of virological suppression in adults with HIV-1: phase 3, randomised, non-inferiority SWORD-1 and SWORD-2 studies. Aboud, M; Angelis, K; Blair, EA; Brinson, C; Castelli, F; Gartland, M; Girard, PM; Hung, CC; Kahl, LP; Llibre, JM; Smith, K; Underwood, M; Vandermeulen, K; Wynne, B, 2018)	0.48
" 395 (77%) of 513 participants in the dolutegravir-rilpivirine group and 364 (71%) of 511 participants in the CAR group reported adverse events."	( Efficacy, safety, and tolerability of dolutegravir-rilpivirine for the maintenance of virological suppression in adults with HIV-1: phase 3, randomised, non-inferiority SWORD-1 and SWORD-2 studies. Aboud, M; Angelis, K; Blair, EA; Brinson, C; Castelli, F; Gartland, M; Girard, PM; Hung, CC; Kahl, LP; Llibre, JM; Smith, K; Underwood, M; Vandermeulen, K; Wynne, B, 2018)	0.48
" Efficacy (HIV RNA <50 copies/mL), adverse events, and metabolic changes at 24 weeks were analyzed."	( Safety and Efficacy of Dolutegravir Plus Rilpivirine in Treatment-Experienced HIV-Infected Patients: The DORIVIR Study. Castaño, M; de la Torre, J; Gálvez, C; González-Domenech, CM; Hidalgo-Tenorio, C; Lozano, A; Mayorga, M; Muñoz-Medina, L; Omar, M; Palacios, R; Santos, J, )	0.13
" No patient discontinued due to adverse events."	( Safety and Efficacy of Dolutegravir Plus Rilpivirine in Treatment-Experienced HIV-Infected Patients: The DORIVIR Study. Castaño, M; de la Torre, J; Gálvez, C; González-Domenech, CM; Hidalgo-Tenorio, C; Lozano, A; Mayorga, M; Muñoz-Medina, L; Omar, M; Palacios, R; Santos, J, )	0.13
"Dolutegravir/RPV is effective and safe in long-term HIV-infected patients under any prior ART."	( Safety and Efficacy of Dolutegravir Plus Rilpivirine in Treatment-Experienced HIV-Infected Patients: The DORIVIR Study. Castaño, M; de la Torre, J; Gálvez, C; González-Domenech, CM; Hidalgo-Tenorio, C; Lozano, A; Mayorga, M; Muñoz-Medina, L; Omar, M; Palacios, R; Santos, J, )	0.13
"Dual therapy with RPV + DRVb proved to be effective and safe in patients with advanced HIV infection, long exposure to ART, low CD4 nadir, previous virologic failure, and/or history of ineffective ART."	( Effectiveness and safety of dual therapy with rilpivirine and boosted darunavir in treatment-experienced patients with advanced HIV infection: a preliminary 24 week analysis (RIDAR study). Arazo, P; Carmena, J; Crusells, MJ; de Jesus, SE; de la Torre, J; Galindo, MJ; Hidalgo-Tenorio, C; Lozano, F; Palacios, Z; Pasquau, J; Ríos, MJ; Samperiz, G; Santos, J; Tornero, C; Verdejo, G, 2019)	0.51
" Drug-related adverse events occurred in 103 (20%) participants in the early-switch group and 58 (12%) in the late-switch group."	( Efficacy and safety of dolutegravir-rilpivirine for maintenance of virological suppression in adults with HIV-1: 100-week data from the randomised, open-label, phase 3 SWORD-1 and SWORD-2 studies. Aboud, M; Adkison, K; Angelis, K; Baker, D; Blair, EA; Bogner, JR; Gartland, M; Kahl, LP; Khuong-Josses, MA; Matthews, JE; Orkin, C; Parks, D; Podzamczer, D; Smith, K; Underwood, M; Vandermeulen, K; Wynne, B, 2019)	0.51
" Secondary outcomes included CD4-count change, treatment discontinuation and treatment-related adverse events."	( Efficacy and safety of abacavir/lamivudine plus rilpivirine as a first-line regimen in treatment-naïve HIV-1 infected adults. Ho, S; Lee, CC; Leo, YS; Lye, DCB; Ng, OT; Wong, CS; Wong, JG, 2020)	0.56
" Of these, 23 discontinuations were due to drug adverse effects, and only 1 attributed to RPV (p < 0."	( Efficacy and safety of abacavir/lamivudine plus rilpivirine as a first-line regimen in treatment-naïve HIV-1 infected adults. Ho, S; Lee, CC; Leo, YS; Lye, DCB; Ng, OT; Wong, CS; Wong, JG, 2020)	0.56
"RPV is effective, safe and considerably more tolerable than compared to NNRTI or boosted PI in ABC/3TC-containing regimens for treatment-naïve patients."	( Efficacy and safety of abacavir/lamivudine plus rilpivirine as a first-line regimen in treatment-naïve HIV-1 infected adults. Ho, S; Lee, CC; Leo, YS; Lye, DCB; Ng, OT; Wong, CS; Wong, JG, 2020)	0.56
" Outcomes were incidence rate and rate ratios for discontinuation due to all causes (DAC), to adverse events (DAE) and to virological failure (VF) after 4 years of follow-up."	( Comparison of the efficacy, safety and durability of a switch to co-formulated RPV/TDF-TAF/FTC or DTG/ABC/3TC in virologically-suppressed HIV-1-infected patients in a single Italian centre: a cohort data analysis. Bartoloni, A; Borchi, B; Botta, A; Cavallo, A; Kiros, ST; Lagi, F; Meli, M; Pozzi, M; Sterrantino, G, 2022)	0.72
" A total of 49 adverse events were observed in 31 out of 222 individuals (14."	( Safety and effectiveness of switching to Abacavir/Lamivudine plus rilpivirine for maintenance therapy in virologically suppressed HIV-1 individuals in Singapore (SEALS). Ang, JH; Ang, LW; Hoo, GS; Law, HL; Lee, CC; Leo, YS; Lim, ZC; Ng, OT; Teng, CB; Wong, CS, 2021)	0.62
"ABC/3TC + RPV is a safe and effective switch option for maintenance therapy in virologically suppressed HIV-1 individuals with in Singapore."	( Safety and effectiveness of switching to Abacavir/Lamivudine plus rilpivirine for maintenance therapy in virologically suppressed HIV-1 individuals in Singapore (SEALS). Ang, JH; Ang, LW; Hoo, GS; Law, HL; Lee, CC; Leo, YS; Lim, ZC; Ng, OT; Teng, CB; Wong, CS, 2021)	0.62
" Rilpivirine (RPV) is better tolerated, and switching from EFV to RPV in virologically suppressed adults has been safe and efficacious, but data in adolescents are limited."	( Switching efavirenz to rilpivirine in virologically suppressed adolescents with HIV: a multi-centre 48-week efficacy and safety study in Thailand. Anugulruengkitt, S; Chantaratin, S; Chokephaibulkit, K; Jantarabenjakul, W; Kosalaraksa, P; Maleesatharn, A; Phongsamart, W; Sirikutt, P; Suntarattiwong, P, 2022)	0.72
" HIV RNA viral load, CD4 cell count, fasting total cholesterol (TC), triglyceride, glucose, neuropsychiatric adverse events, depression and QOL were assessed over 48 weeks."	( Switching efavirenz to rilpivirine in virologically suppressed adolescents with HIV: a multi-centre 48-week efficacy and safety study in Thailand. Anugulruengkitt, S; Chantaratin, S; Chokephaibulkit, K; Jantarabenjakul, W; Kosalaraksa, P; Maleesatharn, A; Phongsamart, W; Sirikutt, P; Suntarattiwong, P, 2022)	0.72
" Treatment efficacy and safety assessments at Week 48 included virologic suppression and lack of virologic suppression (proportion of participants with plasma HIV-1 RNA < 50 copies/mL or ≥ 50 copies/mL, respectively; both as per FDA snapshot algorithm), CD4-cell count change from baseline, no virologic data, discontinuations due to adverse events (AEs), and overall AEs, serious AEs and Grade 3-5 AEs excluding injection-site reactions."	( Indirect comparison of 48-week efficacy and safety of long-acting cabotegravir and rilpivirine maintenance every 8 weeks with daily oral standard of care antiretroviral therapy in participants with virologically suppressed HIV-1-infection. Chounta, V; Snedecor, SJ; Van de Velde, N; Wu, S, 2022)	0.72
" Efficacy, adverse events and metabolic changes at 48 weeks were analysed."	( Efficacy and safety of dolutegravir/rilpivirine in real-world clinical practice. GeSIDA study 1119. Casado, JL; Castaño, M; de la Torre, J; Fanjul, F; Fariñas, C; Galindo, MJ; Gómez-Ayerbe, C; Hidalgo, C; Montero, M; Montes, ML; Ocampo, A; Palacios, R; Payeras, T; Rial, D; Ribera, E; Santos, J; Tejerina, F, 2023)	0.91
" The switch to DTG/RPV was safe with few discontinuations due to adverse effects."	( Efficacy and safety of dolutegravir/rilpivirine in real-world clinical practice. GeSIDA study 1119. Casado, JL; Castaño, M; de la Torre, J; Fanjul, F; Fariñas, C; Galindo, MJ; Gómez-Ayerbe, C; Hidalgo, C; Montero, M; Montes, ML; Ocampo, A; Palacios, R; Payeras, T; Rial, D; Ribera, E; Santos, J; Tejerina, F, 2023)	0.91
" Adverse drug reactions were uncommon."	( Efficacy and Safety of Two-Drug Regimens with Dolutegravir plus Rilpivirine or Lamivudine in HIV-1 Virologically Suppressed People Living with HIV. Buzón, L; De la Fuente, S; De Los Santos, I; Dueñas-Gutiérrez, C; Ferreira, E; Gómez, J; Iribarren, JA; Moran, MA; Moreno, E; Pedrero-Tomé, R; Pousada, G; Troya, J, 2023)	0.91
"We conclude that DTG-based 2DRs (combined with 3TC or RPV) in clinical practice were effective and safe as a switching strategy, with a low VF and high viral suppression rates."	( Efficacy and Safety of Two-Drug Regimens with Dolutegravir plus Rilpivirine or Lamivudine in HIV-1 Virologically Suppressed People Living with HIV. Buzón, L; De la Fuente, S; De Los Santos, I; Dueñas-Gutiérrez, C; Ferreira, E; Gómez, J; Iribarren, JA; Moran, MA; Moreno, E; Pedrero-Tomé, R; Pousada, G; Troya, J, 2023)	0.91

Excerpt	Reference	Relevance
" Pharmacokinetic parameters were determined by non-compartmental methods and analyzed using a linear mixed-effects model."	( Impact of food and different meal types on the pharmacokinetics of rilpivirine. Boven, K; Buelens, A; Crauwels, HM; Hoetelmans, RM; Stevens, M; van Heeswijk, RP, 2013)	0.39
" Steady-state pharmacokinetic (PK) parameters were estimated using noncompartmental analysis of data collected on the last day of each period."	( Lack of pharmacokinetic interaction between rilpivirine and integrase inhibitors dolutegravir and GSK1265744. Chen, S; Crauwels, H; Ford, SL; Gould, E; Margolis, D; Piscitelli, S; Spreen, W, 2013)	0.39
"Rilpivirine coadministration had no effect on (least square mean ratio, 90% confidence interval) ethinylestradiol Cmin (1."	( Lack of an effect of rilpivirine on the pharmacokinetics of ethinylestradiol and norethindrone in healthy volunteers. Buelens, A; Crauwels, HM; Hoetelmans, RM; Stevens, M; van Heeswijk, RP, 2014)	0.4
" Rilpivirine decreased methadone minimum and maximum plasma concentrations (Cmin ; Cmax ) and area under the plasma concentration-time curve versus methadone alone (least-square mean ratio; 90% confidence interval) by 22% (0."	( The effect of rilpivirine on the pharmacokinetics of methadone in HIV-negative volunteers. Buelens, A; Crauwels, HM; Hoetelmans, RM; Stevens, M; van Heeswijk, RP; Vandevoorde, A, 2014)	0.4
" Substituting nevirapine for rilpivirine resulted in ongoing virological suppression and did not have clinically relevant pharmacokinetic effects by cytochrome P450 interactions."	( The efficacy, pharmacokinetics, and safety of a nevirapine to rilpivirine switch in virologically suppressed HIV-1-infected patients. Blonk, M; Burger, D; Rijnders, BJ; Rokx, C; Verbon, A, 2015)	0.42
"This was an open-label, three-period, longitudinal pharmacokinetic study with patients serving as their own controls."	( Steady-state pharmacokinetics of rilpivirine under different meal conditions in HIV-1-infected Ugandan adults. Back, DJ; Byakika-Kibwika, P; Else, L; Katwere, M; Khoo, SH; Lamorde, M; Merry, C; Mukisa, L; Sempa, JB; Walimbwa, S, 2015)	0.42
" Pharmacokinetic parameters were unchanged during administration with a low-fat meal, except for C24, which was significantly increased by 15% (1."	( Steady-state pharmacokinetics of rilpivirine under different meal conditions in HIV-1-infected Ugandan adults. Back, DJ; Byakika-Kibwika, P; Else, L; Katwere, M; Khoo, SH; Lamorde, M; Merry, C; Mukisa, L; Sempa, JB; Walimbwa, S, 2015)	0.42
"A food effect was observed for steady-state pharmacokinetic parameters of rilpivirine (AUC0-24 and C24) when TDF/FTC/RPV was administered in the fasted state compared with the moderate-fat meal."	( Steady-state pharmacokinetics of rilpivirine under different meal conditions in HIV-1-infected Ugandan adults. Back, DJ; Byakika-Kibwika, P; Else, L; Katwere, M; Khoo, SH; Lamorde, M; Merry, C; Mukisa, L; Sempa, JB; Walimbwa, S, 2015)	0.42
" Pharmacokinetic assessments were conducted for each drug at steady-state when given alone and when coadministered; statistical analyses were least-square means with 90% confidence intervals."	( Pharmacokinetic interaction between etravirine or rilpivirine and telaprevir in healthy volunteers: A randomized, two-way crossover trial. Bertelsen, KM; Crauwels, HM; Hoetelmans, RM; Kakuda, TN; Leopold, L; Nijs, S; Stevens, M; Tomaka, F; van Delft, Y; Vandevoorde, A; Witek, J, 2014)	0.4
" Preclinical testing was undertaken to define RPV pharmacokinetic (PK) and pharmacodynamic (PD) activities in ectocervical and colonic tissue treated in vitro Tenfold dilutions of RPV were added to the basolateral medium of polarized ectocervical and colonic explant tissues."	( Distinct Pharmacodynamic Activity of Rilpivirine in Ectocervical and Colonic Explant Tissue. Back, DJ; Dezzutti, CS; Else, LJ; McGowan, I; Russo, J; Shetler, C; Yandura, SE, 2016)	0.43
" Intensive pharmacokinetic sampling was performed at steady state during the second trimester, the third trimester, and postpartum."	( Pharmacokinetics of Rilpivirine in HIV-Infected Pregnant Women. Best, BM; Burchett, SK; Capparelli, EV; Chakhtoura, N; Cressey, TR; George, K; Kreitchmann, R; Mirochnick, M; Rungruengthanakit, K; Shapiro, DE; Smith, E; Stek, A; Tran, AH; Wang, J, 2016)	0.43
" High variability in pharmacokinetic parameters was observed between subjects."	( Pharmacokinetics of Rilpivirine in HIV-Infected Pregnant Women. Best, BM; Burchett, SK; Capparelli, EV; Chakhtoura, N; Cressey, TR; George, K; Kreitchmann, R; Mirochnick, M; Rungruengthanakit, K; Shapiro, DE; Smith, E; Stek, A; Tran, AH; Wang, J, 2016)	0.43
"Rilpivirine safety, virologic and pharmacokinetic profiles were similar in treatment-naïve HIV-1-infected adolescents and adults, supporting use of rilpivirine 25 mg qd, plus other antiretrovirals, in treatment-naïve adolescents with VL ≤100,000 copies/mL at treatment initiation."	( Rilpivirine as a Treatment for HIV-infected Antiretroviral-naïve Adolescents: Week 48 Safety, Efficacy, Virology and Pharmacokinetics. Bunupuradah, T; Crauwels, H; Flynn, PM; Hoogstoel, A; Lombaard, J; Ramapuram, J; Ssali, F; Stevens, M; Van Eygen, V, 2016)	0.43
" A precise method is required to quantify the drug concentration in biological matrices to study pharmacokinetic behavior and tissue distribution profile in animals and/or humans."	( Simultaneous quantification of tenofovir, emtricitabine, rilpivirine, elvitegravir and dolutegravir in mouse biological matrices by LC-MS/MS and its application to a pharmacokinetic study. Destache, CJ; Mandal, S; Prathipati, PK, 2016)	0.43
" The MWRI-01 study was done to characterise the safety, acceptability, and pharmacokinetic and pharmacodynamic profile of long-acting rilpivirine."	( Long-acting rilpivirine as potential pre-exposure prophylaxis for HIV-1 prevention (the MWRI-01 study): an open-label, phase 1, compartmental, pharmacokinetic and pharmacodynamic assessment. Abebe, K; Achilles, S; Adler, A; Back, D; Brand, RM; Chen, B; Cranston, RD; Dezzutti, CS; Duffill, K; Egan, D; Egan, JE; Else, L; Engstrom, J; Khoo, S; McGowan, I; Nikiforov, A; Rehman, KK; Richardson-Harman, N; Shetler, C; Siegel, A; Stall, R; Williams, PE, 2016)	0.43
" The aim of this observational study was to characterize the RPV pharmacokinetic profile, to quantify interpatient variability, and to identify potential factors that could influence drug exposure."	( Population Pharmacokinetics and Pharmacogenetics Analysis of Rilpivirine in HIV-1-Infected Individuals. Aouri, M; Barcelo, C; Buclin, T; Cavassini, M; Csajka, C; Decosterd, LA; Guidi, M; Hizrel, C; Rotger, M, 2017)	0.46
" The aim of this study was to simulate and predict drug-drug interactions (DDIs) between these LA antiretroviral agents and rifampicin using physiologically based pharmacokinetic (PBPK) modeling."	( Predicting Drug-Drug Interactions Between Rifampicin and Long-Acting Cabotegravir and Rilpivirine Using Physiologically Based Pharmacokinetic Modeling. Back, D; Chiong, J; Curley, P; Flexner, C; Owen, A; Rajoli, RKR; Siccardi, M, 2019)	0.51
" Qualified PBPK models were utilized for pharmacokinetic prediction of DDIs."	( Predicting Drug-Drug Interactions Between Rifampicin and Long-Acting Cabotegravir and Rilpivirine Using Physiologically Based Pharmacokinetic Modeling. Back, D; Chiong, J; Curley, P; Flexner, C; Owen, A; Rajoli, RKR; Siccardi, M, 2019)	0.51
" The estimated apparent elimination half-life of rilpivirine LA was 200 days."	( Population pharmacokinetics of the rilpivirine long-acting formulation after intramuscular dosing in healthy subjects and people living with HIV. Crauwels, HM; Neyens, M; Perez-Ruixo, JJ; Rossenu, S, 2021)	0.62
"The population pharmacokinetic model suitably describes the time course and associated variability of rilpivirine plasma concentrations after rilpivirine LA intramuscular administration."	( Population pharmacokinetics of the rilpivirine long-acting formulation after intramuscular dosing in healthy subjects and people living with HIV. Crauwels, HM; Neyens, M; Perez-Ruixo, JJ; Rossenu, S, 2021)	0.62
"Two separate, parallel, three-group, non-randomized, pharmacokinetic studies evaluated either etonogestrel or levonorgestrel in women receiving rilpivirine- or darunavir-based ART compared with women without HIV (control group)."	( Pharmacokinetics of levonorgestrel and etonogestrel contraceptive implants over 48 weeks with rilpivirine- or darunavir-based antiretroviral therapy. Byakika-Kibwika, P; Chappell, CA; Fletcher, CV; Jeppson, J; Kaboggoza, J; Kyohairwe, I; Lamorde, M; Mbabazi, L; Musaazi, J; Nakalema, S; Nakijoba, R; Nassiwa, S; Pham, M; Scarsi, KK; Siccardi, M; Walimbwa, SI; Winchester, L, 2022)	0.72
" Outcomes in pregnant participants exposed to CAB + RPV, and pharmacokinetic washout data in those exposed to CAB + RPV long-acting (LA) with live births, are presented."	( Pregnancy outcomes and pharmacokinetics in pregnant women living with HIV exposed to long-acting cabotegravir and rilpivirine in clinical trials. Baker, M; Baugh, B; Birmingham, E; Crauwels, H; D'Amico, R; Ford, SL; Garside, L; Meyer, C; Patel, P; Polli, JW; Seal, C; Spreen, WR; Thiagarajah, S; Van Solingen-Ristea, R; van Wyk, J; Vannappagari, V; Yagüe Muñoz, I, 2023)	0.91
" Upon pregnancy in the trial programme, CAB + RPV was discontinued, an alternative antiretroviral regimen was initiated, and quarterly pharmacokinetic sampling for 52 weeks post-last injection was obtained."	( Pregnancy outcomes and pharmacokinetics in pregnant women living with HIV exposed to long-acting cabotegravir and rilpivirine in clinical trials. Baker, M; Baugh, B; Birmingham, E; Crauwels, H; D'Amico, R; Ford, SL; Garside, L; Meyer, C; Patel, P; Polli, JW; Seal, C; Spreen, WR; Thiagarajah, S; Van Solingen-Ristea, R; van Wyk, J; Vannappagari, V; Yagüe Muñoz, I, 2023)	0.91
"As of 31 March 2021, 25 pregnancies following CAB + RPV exposure at conception were reported (five oral, 20 LA), including four who conceived during pharmacokinetic washout following treatment discontinuation."	( Pregnancy outcomes and pharmacokinetics in pregnant women living with HIV exposed to long-acting cabotegravir and rilpivirine in clinical trials. Baker, M; Baugh, B; Birmingham, E; Crauwels, H; D'Amico, R; Ford, SL; Garside, L; Meyer, C; Patel, P; Polli, JW; Seal, C; Spreen, WR; Thiagarajah, S; Van Solingen-Ristea, R; van Wyk, J; Vannappagari, V; Yagüe Muñoz, I, 2023)	0.91

Excerpt	Reference	Relevance
" 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
"Rilpivirine (TMC278) is a non-nucleoside reverse transcriptase inhibitor approved in combination with other antiretrovirals for the treatment of HIV-1 infection in treatment-naive adults (Edurant(®) 25 mg once daily; Complera(®) [USA]/Eviplera(®) [EU] once daily single-tablet regimen)."	( Clinical perspective on drug-drug interactions with the non-nucleoside reverse transcriptase inhibitor rilpivirine. Boven, K; Buelens, A; Crauwels, H; Hoetelmans, R; Stevens, M; van Heeswijk, RP; Vanveggel, S, )	0.13
" The 3D regimen of 150/100 mg daily paritaprevir/ritonavir, 25 mg daily ombitasvir, and 400 mg twice-daily dasabuvir was administered alone or in combination with 200 mg daily of emtricitabine and 300 mg daily of tenofovir disoproxil fumarate (tenofovir DF), 25 mg daily of rilpivirine, or 400 mg of raltegravir twice daily."	( Evaluation of Drug-Drug Interactions between Direct-Acting Anti-Hepatitis C Virus Combination Regimens and the HIV-1 Antiretroviral Agents Raltegravir, Tenofovir, Emtricitabine, Efavirenz, and Rilpivirine. Awni, W; Dunbar, M; Dutta, S; Khatri, A; Menon, R; Podsadecki, T; Trinh, R, 2016)	0.43
"To evaluate the plasma trough concentrations ( C trough ) of dolutegravir and rilpivirine used in combination with simeprevir and sofosbuvir in HIV/hepatitis C virus (HCV)-coinfected patients with liver cirrhosis."	( Pharmacokinetics of dolutegravir and rilpivirine in combination with simeprevir and sofosbuvir in HIV/hepatitis C virus-coinfected patients with liver cirrhosis. Ariaudo, A; Bonora, S; Castagna, A; D'Avolio, A; Galli, L; Hasson, H; Lazzarin, A; Marinaro, L; Merli, M; Messina, E; Uberti-Foppa, C, 2017)	0.46
"Dolutegravir plasma trough concentrations were measured in 78 HIV-infected patients given the drug in combination with a protease inhibitor, a non-nucleoside reverse transcriptase inhibitor or abacavir/lamivudine."	( Dolutegravir plasma concentrations according to companion antiretroviral drug: unwanted drug interaction or desirable boosting effect? Cattaneo, D; Clementi, E; Cozzi, V; Galli, M; Gervasoni, C; Meraviglia, P; Minisci, D; Riva, A, 2017)	0.46
" The aim of this study was to simulate and predict drug-drug interactions (DDIs) between these LA antiretroviral agents and rifampicin using physiologically based pharmacokinetic (PBPK) modeling."	( Predicting Drug-Drug Interactions Between Rifampicin and Long-Acting Cabotegravir and Rilpivirine Using Physiologically Based Pharmacokinetic Modeling. Back, D; Chiong, J; Curley, P; Flexner, C; Owen, A; Rajoli, RKR; Siccardi, M, 2019)	0.51
"Combined antiretroviral treatments have significantly improved the morbidity and mortality related to HIV infection, thus transforming HIV infection into a chronic disease; however, the efficacy of antiretroviral treatments is highly dependent on the ability of infected individuals to adhere to life-long drug combination therapies."	( Pharmacokinetics and Drug-Drug Interactions of Long-Acting Intramuscular Cabotegravir and Rilpivirine. Back, DJ; Gibbons, S; Hodge, D; Khoo, SH; Marzolini, C, 2021)	0.62
"To evaluate the effect of methadone maintenance treatment (MMT) combined with rilpivirine (RPV)-based regimens on drug use of HIV individuals."	( Outcomes of Methadone Maintenance Therapy Combined with Rilpivirine/Efavirenz in Treatment-Naive HIV-Infected Patients. Dong, X; Hong, L; Huang, S; Lei, S; Li, H; Li, X; Xie, R; Xin, J; Yang, C; Yang, X; Zhang, B; Zhang, R, 2021)	0.62
"This study was a prospective, open-label, controlled, drug-drug interaction trial at a single center for 24 weeks."	( Outcomes of Methadone Maintenance Therapy Combined with Rilpivirine/Efavirenz in Treatment-Naive HIV-Infected Patients. Dong, X; Hong, L; Huang, S; Lei, S; Li, H; Li, X; Xie, R; Xin, J; Yang, C; Yang, X; Zhang, B; Zhang, R, 2021)	0.62
"We assessed virological failure (VF) and resistance-associated mutations (RAMs) on dolutegravir maintenance regimens in combination with rilpivirine or with lamivudine or emtricitabine (xTC) and analysed the factors associated with VF."	( Dolutegravir-based dual maintenance regimens combined with lamivudine/emtricitabine or rilpivirine: risk of virological failure in a real-life setting. Allavena, C; Bani-Sadr, F; Cabie, A; Cuzin, L; Deschanvres, C; Duvivier, C; Hocqueloux, L; Joly, V; Lamaury, I; Palich, R; Raffi, F; Rey, D; Reynes, J; Robineau, O, 2021)	0.62
"To evaluate the long-term safety and efficacy of rilpivirine (RPV), a non-nucleoside reverse transcriptase inhibitor (NNRTI), in combination with nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) in human immunodeficiency virus (HIV)-infected patients."	( Long-term safety and efficacy of rilpivirine in combination with nucleoside/nucleotide reverse transcriptase inhibitors in HIV-1 infected patients: 336-week rollover study of phase 2b and 3 clinical studies. Cahn, P; Ene, L; Fätkenheuer, G; Lombaard, J; Molina, JM; Van Eygen, V; Van Solingen-Ristea, R; Van Wijngaerden, E; Vanveggel, S; Zakharova, N, 2021)	0.62
"RPV 25 mg QD in combination with an investigator-selected background regimen of two NRTIs demonstrated sustained long-term virologic suppression."	( Long-term safety and efficacy of rilpivirine in combination with nucleoside/nucleotide reverse transcriptase inhibitors in HIV-1 infected patients: 336-week rollover study of phase 2b and 3 clinical studies. Cahn, P; Ene, L; Fätkenheuer, G; Lombaard, J; Molina, JM; Van Eygen, V; Van Solingen-Ristea, R; Van Wijngaerden, E; Vanveggel, S; Zakharova, N, 2021)	0.62
"Long-acting (LA) intramuscular cabotegravir and rilpivirine are prone to drug-drug interactions (DDI)."	( Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study. Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023)	0.91
" Cabotegravir and rilpivirine were given alone and in combination with rifampicin or rifabutin."	( Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study. Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023)	0.91
" Here we provide a detailed review of the clinical pharmacology, administration and available formulations of the novel HIV integrase inhibitor cabotegravir with in-depth analysis of the clinical trial data, safety, satisfaction and viral resistance development when combined with rilpivirine as the first long-acting injectable program for the treatment of HIV infection."	( Cabotegravir: a novel HIV integrase inhibitor combined with rilpivirine as the first long-acting injectable program for the treatment of HIV infection. Otto, A; Rivera, CG; Smith, BL; Temesgen, Z; Zeuli, JD, 2022)	0.72

Excerpt	Reference	Relevance
"Ideally, an anti-HIV drug should (1) be highly active against wild-type and mutant HIV without allowing breakthrough; (2) have high oral bioavailability and long elimination half-life, allowing once-daily oral treatment at low doses; (3) have minimal adverse effects; and (4) be easy to synthesize and formulate."	( In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). Andries, K; Arnold, E; Bohets, H; Clark, AD; Daeyaert, F; Das, K; de Béthune, MP; De Clerck, F; de Jonge, M; De Knaep, F; Frenkel, YV; Guillemont, J; Heeres, J; Hughes, SH; Janssen, PA; Koymans, L; Kukla, M; Lampo, A; Lewi, PJ; Ludovici, D; Medaer, B; Pasquier, E; Pauwels, R; Stoffels, P; Vinkers, M; Williams, P, 2005)	0.33
" Compared to the tablet, the relative bioavailability obtained with the powders ranged between 69% and 89% for TMC278/PVP-VA 64 1:9 (w/w) and between 85% and 157% for TMC278/PVP-VA 64/Cremophor EL 1:8."	( Powder for reconstitution of the anti-HIV-1 drug TMC278 - Formulation development, stability and animal studies. Adams, E; Baert, L; Bouche, MP; De Man, H; Hoogmartens, J; Pendela, M; Rosier, J; Schueller, L; Van 't Klooster, G; Van den Mooter, G; Van Gyseghem, E; Van Remoortere, P; Wigerinck, P, 2008)	0.35
"The non-nucleoside reverse transcriptase inhibitor (NNRTI) TMC278/rilpivirine is an anti-AIDS therapeutic agent with high oral bioavailability despite its high hydrophobicity."	( Molecular dynamics study of non-nucleoside reverse transcriptase inhibitor 4-[[4-[[4-[(E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile (TMC278/rilpivirine) aggregates: correlation between amphiphilic properties of the drug an Arnold, E; Das, K; Frenkel, YV; Gallicchio, E; Levy, RM, 2009)	0.35
" The absolute bioavailability approached 100%, indicating a complete release from the depot, in spite of rilpivirine concentrations still being high at the injection site(s) 3 months after administration in dogs."	( Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation. Baert, L; Borghys, H; Bouche, MP; Hoeben, E; Looszova, A; van 't Klooster, G; van Velsen, F, 2010)	0.36
" Administration of rilpivirine under fasting conditions or with only a protein-rich nutritional drink substantially lowered the oral bioavailability when compared to administration with a normal-fat breakfast."	( Impact of food and different meal types on the pharmacokinetics of rilpivirine. Boven, K; Buelens, A; Crauwels, HM; Hoetelmans, RM; Stevens, M; van Heeswijk, RP, 2013)	0.39
" RPV can be given once daily, is well absorbed and should be administered with food."	( Rilpivirine: drug profile of a second-generation non-nucleoside reverse transcriptase HIV-inhibitor. Bombana, E; Ripamonti, D; Rizzi, M, 2014)	0.4
"To synthesize β cyclodextrin nanosponges using a novel and efficient microwave mediated method for enhancing bioavailability of Rilpivirine HCl (RLP)."	( Enhancement of oral bioavailability of anti-HIV drug rilpivirine HCl through nanosponge formulation Momin, M; Sangshetti, JN; Zaheer, Z; Zainuddin, R, 2017)	0.46
"0166 mg/ml) and dissolution rate leading to low bioavailability (32%)."	( Investigation of Cyclodextrin-Based Nanosponges for Solubility and Bioavailability Enhancement of Rilpivirine. Caldera, F; Chaudhari, J; Rao, MRP; Trotta, F, 2018)	0.48
"Many lead compounds fail to reach clinical trials despite being potent because of low bioavailability attributed to their insufficient solubility making solubility a primary and crucial factor in early phase drug discovery."	( Structural modification aimed for improving solubility of lead compounds in early phase drug discovery. Baidya, ATK; Das, B; Kumar, R; Mathew, AT; Yadav, AK, 2022)	0.72

Excerpt	Relevance	Reference
" Their flexible dosing ability makes them suitable for patients looking for a different approach for antiretroviral (ARV) therapy."	( Powder for reconstitution of the anti-HIV-1 drug TMC278 - Formulation development, stability and animal studies. Adams, E; Baert, L; Bouche, MP; De Man, H; Hoogmartens, J; Pendela, M; Rosier, J; Schueller, L; Van 't Klooster, G; Van den Mooter, G; Van Gyseghem, E; Van Remoortere, P; Wigerinck, P, 2008)	0.35
"No TMC278 dose-response relationship for efficacy and safety was observed."	( Efficacy and safety of TMC278 in antiretroviral-naive HIV-1 patients: week 96 results of a phase IIb randomized trial. Boven, K; Grinsztejn, B; Katabira, E; Lupo, SH; Morales-Ramirez, J; Pozniak, AL; Rimsky, LT; Ruxrungtham, K; Santoscoy, M; Steyn, D; Vanveggel, S, 2010)	0.36
" No significant RPV dose-response relationships with respect to the primary endpoint (composite ITT-TLOVR algorithm) were observed at week 48 or 96."	( Long-term efficacy, safety, and tolerability of rilpivirine (RPV, TMC278) in HIV type 1-infected antiretroviral-naive patients: week 192 results from a phase IIb randomized trial. Boven, K; Grinsztejn, B; Lupo, SH; Morales-Ramirez, J; Pozniak, AL; Rimsky, LT; Ruxrungtham, K; Santoscoy, M; Vanveggel, S; Wilkin, A, 2012)	0.38
"The pharmacology, pharmacokinetics, drug interactions, clinical efficacy, adverse effects, dosage and administration, and place in therapy of rilpivirine are reviewed."	( Rilpivirine: a second-generation nonnucleoside reverse transcriptase inhibitor. James, C; Preininger, L; Sweet, M, 2012)	0.38
" RPV is dosed once daily with food and has been coformulated into a single tablet containing tenofovir and emtricitabine."	( Rilpivirine, a novel non-nucleoside reverse transcriptase inhibitor for the management of HIV-1 infection: a systematic review. Schafer, JJ; Short, WR, 2012)	0.38
" Once-daily dosing options are essential to treatment simplification strategies, which have been shown to enhance regimen compliance and durabiltiy."	( New therapeutic landscape of NNRTIs for treatment of HIV: a look at recent data. Dilanchian, P; Jayaweera, D, 2012)	0.38
"72) under fasting conditions compared to dosing with a normal-fat breakfast."	( Impact of food and different meal types on the pharmacokinetics of rilpivirine. Boven, K; Buelens, A; Crauwels, HM; Hoetelmans, RM; Stevens, M; van Heeswijk, RP, 2013)	0.39
" As a fixed-dose combination tablet given once daily, EFV/FTC/TDF was the first available STR combining efficacy, tolerability and convenience, with the simplest dosing schedule and smallest numbers of pills of any ART combination therapy."	( Single-tablet regimens in HIV: does it really make a difference? Aldir, I; Horta, A; Serrado, M, 2014)	0.4
"The need for combination ART and physicochemical and dosing limitations of current ARV drugs impede attempts to redevelop them as long-acting injectable formulations."	( Long-acting injectable antiretrovirals for HIV treatment and prevention. Margolis, DA; Pottage, JC; Spreen, WR, 2013)	0.39
" Phase I studies of the pharmacokinetics and safety of each long-acting formulation alone and in combination indicate that a monthly dosing regimen is possible for HIV treatment."	( Long-acting injectable antiretrovirals for HIV treatment and prevention. Margolis, DA; Pottage, JC; Spreen, WR, 2013)	0.39
" The 90% confidence interval (CI) of the geometric mean ratio for rilpivirine, emtricitabine, tenofovir exposure was estimated for fed versus fasted dosing and light versus standard meal, with equivalence boundaries of 80 - 125%."	( Effect of food on rilpivirine/emtricitabine/tenofovir disoproxil fumarate, an antiretroviral single-tablet regimen for the treatment of HIV infection. Cheng, A; Custodio, JM; Hepner, M; Kearney, BP; Ling, KH; Ramanathan, S; Yin, X, 2014)	0.4
"At weeks 12 and 24, all 49 dosed subjects remained suppressed on RPV/FTC/TDF."	( Efficacy and safety 48 weeks after switching from efavirenz to rilpivirine using emtricitabine/tenofovir disoproxil fumarate-based single-tablet regimens. Brinson, C; Cheng, AK; Chuck, SK; Cohen, C; Dejesus, E; Mills, AM; Ramanathan, S; Wang, MH; White, K; Williams, S; Yale, KL, )	0.13
"Co-administration of rilpivirine, at the therapeutic dosing regimen, with ethinylestradiol/norethindrone does not affect hormone pharmacokinetics, and is, therefore, unlikely to affect the efficacy or safety of this oral hormonal contraceptive."	( Lack of an effect of rilpivirine on the pharmacokinetics of ethinylestradiol and norethindrone in healthy volunteers. Buelens, A; Crauwels, HM; Hoetelmans, RM; Stevens, M; van Heeswijk, RP, 2014)	0.4
"Despite improvements in access to antiretroviral therapy and the use of simplified dosing regimens, HIV infection is still an important global public health problem."	( An overview of antiretroviral pre-exposure prophylaxis of HIV infection. McGowan, I, 2014)	0.4
"In the present investigation, a simple and isocratic HPLC-UV method was developed and validated for determination of rilpivirine (RPV) from dosage forms (tablets and nanoparticles) and biological matrices like HeLa cell lysates."	( Development and validation of a simple and isocratic reversed-phase HPLC method for the determination of rilpivirine from tablets, nanoparticles and HeLa cell lysates. Bruck, P; Date, AA; Destache, CJ; Shibata, A, 2015)	0.42
" New treatment options show high efficacy and safety and include single-tablet coformulations for once-daily dosing to improve convenience."	( HIV: new drugs, new guidelines. Geretti, AM; Tsakiroglou, M, 2014)	0.4
"Pharmacokinetics, safety, and tolerability of GSK1265744 (744) and rilpivirine (RPV) (TMC278) were assessed after repeat dosing of long-acting (LA) injectable formulations in healthy subjects."	( Pharmacokinetics, safety, and tolerability with repeat doses of GSK1265744 and rilpivirine (TMC278) long-acting nanosuspensions in healthy adults. Crauwels, H; Ford, SL; Gould, E; Lou, Y; Margolis, D; Piscitelli, S; Spreen, W; Stevens, M; Williams, P, 2014)	0.4
" All dose cohorts achieved therapeutically relevant plasma concentrations of each drug within 3 days with prolonged exposure over the dosing interval."	( Pharmacokinetics, safety, and tolerability with repeat doses of GSK1265744 and rilpivirine (TMC278) long-acting nanosuspensions in healthy adults. Crauwels, H; Ford, SL; Gould, E; Lou, Y; Margolis, D; Piscitelli, S; Spreen, W; Stevens, M; Williams, P, 2014)	0.4
" Enrolled patients underwent 24 h blood sampling with TDF/FTC/RPV dosing in the fasted state (day 42), with a low-fat meal (11 g of fat/353 kcal, day 49) and with a moderate-fat meal (19 g of fat/589 kcal, day 56; reference)."	( Steady-state pharmacokinetics of rilpivirine under different meal conditions in HIV-1-infected Ugandan adults. Back, DJ; Byakika-Kibwika, P; Else, L; Katwere, M; Khoo, SH; Lamorde, M; Merry, C; Mukisa, L; Sempa, JB; Walimbwa, S, 2015)	0.42
" In conclusion, this genotypic resistance analysis strongly suggests that the latest NNRTI, rilpivirine, may retain activity in a large proportion of HIV-1 patients in whom resistance failed while they were on an efavirenz- or nevirapine-containing regimen, and may present an attractive option for second-line treatment given its good safety profile and dosing convenience."	( Predicted residual activity of rilpivirine in HIV-1 infected patients failing therapy including NNRTIs efavirenz or nevirapine. Camacho, RJ; Gomes, P; Rhee, SY; Theys, K; Vandamme, AM, 2015)	0.42
" The mean (standard deviation) RPV plasma concentration across the 28-day dosing interval after the last injection in the 1200/600/600 mg group was 79 (19) ng/mL."	( Safety, tolerability and pharmacokinetics of rilpivirine following administration of a long-acting formulation in healthy volunteers. Crauwels, H; Deleu, S; Meyvisch, P; Niemeijer, N; Verloes, R; Williams, P, 2015)	0.42
" The high potency and low daily dosing requirements of oral cabotegravir and rilpivirine facilitate long-acting formulation development."	( Long-acting antiviral agents for HIV treatment. Boffito, M; Margolis, DA, 2015)	0.42
" It is not yet certain whether oral dosing will remain a prerequisite in future trials or post licensure."	( Long-acting rilpivirine for HIV prevention. Jackson, A; McGowan, I, 2015)	0.42
" Adherence to required dosing regimens for protection may pose challenges."	( The promise and pitfalls of long-acting injectable agents for HIV prevention. Kofron, R; Landovitz, RJ; McCauley, M, 2016)	0.43
"RPV PK in this adolescent population was similar to adults when dosed without DRV/r."	( Rilpivirine Pharmacokinetics Without and With Darunavir/Ritonavir Once Daily in Adolescents and Young Adults. Acosta, EP; Britto, P; Carey, VJ; Cressey, TR; Foca, M; Graham, B; Hazra, R; Jean-Philippe, P; King, J; Wiznia, A; Yogev, R, 2016)	0.43
" The CCR5-antagonist maraviroc (MVC), the non-nucleoside reverse transcriptase inhibitors (NNRTIs) etravirine (ETV) and rilpivirine (RPV), as well as the integrase strand transfer inhibitor (INSTI) raltegravir (RAL), have all been evaluated using both oral and non-oral dosing regimens, demonstrating a need for dynamic and sensitive bioanalytical tools for drug quantification in plasma and tissue."	( Development and validation of a liquid chromatographic-tandem mass spectrometric method for the multiplexed quantification of etravirine, maraviroc, raltegravir, and rilpivirine in human plasma and tissue. Marzinke, MA; Parsons, TL, 2016)	0.43
"Rilpivirine (RPV), the latest nonnucleoside reverse transcriptase inhibitor active against HIV-1, is prescribed in a standard dosage of 25 mg once a day in combination with emtricitabine (FTC) and tenofovir disoproxil fumarate (TDF)."	( Population Pharmacokinetics and Pharmacogenetics Analysis of Rilpivirine in HIV-1-Infected Individuals. Aouri, M; Barcelo, C; Buclin, T; Cavassini, M; Csajka, C; Decosterd, LA; Guidi, M; Hizrel, C; Rotger, M, 2017)	0.46
" This boosting effect of atazanavir could be used to optimize dolutegravir dosing in particular clinical settings."	( Dolutegravir plasma concentrations according to companion antiretroviral drug: unwanted drug interaction or desirable boosting effect? Cattaneo, D; Clementi, E; Cozzi, V; Galli, M; Gervasoni, C; Meraviglia, P; Minisci, D; Riva, A, 2017)	0.46
" The objective of this study was to simulate potential dosing strategies for existing long-acting injectable depot formulations of cabotegravir and rilpivirine in children and adolescents (aged 3-18 years) using physiologically-based pharmacokinetic modelling."	( In Silico Dose Prediction for Long-Acting Rilpivirine and Cabotegravir Administration to Children and Adolescents. Back, DJ; Flexner, C; Meyers, CF; Owen, A; Rajoli, RKR; Rannard, S; Siccardi, M, 2018)	0.48
"The reported findings represent a rational platform for the identification of suitable dosing strategies and can inform prospective clinical investigation of long-acting injectable formulations in children and adolescents."	( In Silico Dose Prediction for Long-Acting Rilpivirine and Cabotegravir Administration to Children and Adolescents. Back, DJ; Flexner, C; Meyers, CF; Owen, A; Rajoli, RKR; Rannard, S; Siccardi, M, 2018)	0.48
" The objective of this study was to select an intramuscular dosing regimen based on a comparison of the antiviral activity, tolerability, and safety of the two intramuscular dosing regimens relative to oral cabotegravir plus abacavir-lamivudine."	( Long-acting intramuscular cabotegravir and rilpivirine in adults with HIV-1 infection (LATTE-2): 96-week results of a randomised, open-label, phase 2b, non-inferiority trial. Angel, JB; Clair, MS; Clotet, B; Crauwels, H; Dorey, D; Eron, JJ; Ford, SL; Gonzalez-Garcia, J; Griffith, SK; Gutierrez, F; Lutz, T; Margolis, DA; Mrus, J; Murray, M; Patel, P; Podzamczer, D; Richmond, GJ; Sloan, L; Smith, KY; Spreen, WR; Stellbrink, HJ; Sutton, KC; Williams, PE; Yazdanpanah, Y, 2017)	0.46
" However, a fatty meal enhances its absorption hence the therapy indicates that the dosage form be consumed with a meal."	( Enhancement of oral bioavailability of anti-HIV drug rilpivirine HCl through nanosponge formulation Momin, M; Sangshetti, JN; Zaheer, Z; Zainuddin, R, 2017)	0.46
"The approach offers a comfortable dosing zone for AIDs patients, negating the requirement of consuming the formulation in a fed state due to enhancement in drugs' oral bioavailability."	( Enhancement of oral bioavailability of anti-HIV drug rilpivirine HCl through nanosponge formulation Momin, M; Sangshetti, JN; Zaheer, Z; Zainuddin, R, 2017)	0.46
" The good efficacy, safety profi le, and convenient dosing of RPV account for the unique durability of RPV-based regimens."	( Rilpivirine: The Key for Long-term Success. Viciana, P, )	0.13
" Here we describe an oral dosage form composed of distinct drug-polymer matrices which achieved week-long systemic drug levels of the antiretrovirals dolutegravir, rilpivirine and cabotegravir in a pig."	( Development of an oral once-weekly drug delivery system for HIV antiretroviral therapy. Abouzid, O; Bellinger, AM; Bensel, T; Bershteyn, A; Booth, L; Cleveland, C; Craig, M; Eckhoff, PA; Grant, T; Hayward, A; Hill, AL; Javid, F; Kirtane, AR; Langer, R; Lee, YL; Mazdiyasni, H; Minahan, D; Mo, SS; Nikolic, B; Nowak, MA; Rogner, J; Selinger, C; Traverso, G; Wood, L; Wu, SJ, 2018)	0.48
"Regimen switching in virally suppressed HIV-1-infected patients may be considered to reduce pill burden or dosing frequency, decrease short- or long-term toxicity, prevent or manage drug-drug interactions, and/or decrease cost."	( Dolutegravir Dual Therapy as Maintenance Treatment in HIV-Infected Patients: A Review. Boswell, R; Foisy, MM; Hughes, CA, 2018)	0.48
" Additionally, we observe additive inhibitory activity against pseudotyped viruses when B#24 is dosed in competition with the clinically used non-nucleoside reverse transcriptase inhibitor (NNRTI) efavirenz."	( Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline. Banerjee, S; Blakemore, PR; Brack-Werner, R; Herrmann, A; Loesgen, S; Milicevic Sephton, S; Neuhaus, GF; Overacker, RD; Strother, JA, 2019)	0.51
"Antiretroviral therapy requires lifelong daily dosing to attain viral suppression, restore immune function, and improve quality of life."	( Creation of a long-acting rilpivirine prodrug nanoformulation. Alnouti, Y; Bade, AN; Dash, PK; Dyavar Shetty, BL; Edagwa, BJ; Fox, HS; Gautam, N; Gendelman, HE; Herskovitz, J; Hilaire, JR; Lamberty, BG; McMillan, JM; Sillman, B; Sravanam, S; Szlachetka, A; Wojtkiewicz, MS, 2019)	0.51
" nanoformulation dose and release rates) and inform dosing strategies to maintain plasma concentrations above target trough concentrations for the designated dosing interval."	( Modelling the intradermal delivery of microneedle array patches for long-acting antiretrovirals using PBPK. Chiong, J; Donnelly, RF; Flexner, C; Larrañeta, E; Owen, A; Rajoli, RKR; Siccardi, M, 2019)	0.51
" Recently approved or investigational antiretroviral drugs present considerable advantages, allowing once daily oral dosage along with activity against resistant variants (eg, bictegravir and doravirine) and also parenteral intramuscular administration that facilitates treatment adherence (eg, long-acting injectable formulations such as cabotegravir and rilpivirine)."	( Development and validation of a multiplex UHPLC-MS/MS assay with stable isotopic internal standards for the monitoring of the plasma concentrations of the antiretroviral drugs bictegravir, cabotegravir, doravirine, and rilpivirine in people living with HI Alves Saldanha, S; André, P; Buclin, T; Cavassini, M; Choong, E; Courlet, P; Csajka, C; Decosterd, LA; Desfontaine, V; Günthard, HF; Marzolini, C, 2020)	0.56
"\ Conclusions: The patients were generally satisfied with the change in medication and well nformed about the dosage and advantages of TAF over TDF, but less well informed about the possible adverse effects of TAF."	( Satisfaction and knowledge among patients with HIV after switching from tenofovir to tenofovir alafenamide in regimens containing emtricitabine and rilpivirine Bermejo-Vicedo, T; Gramage-Caro, T; Montero-Llorente, B; Rodríguez-Sagrado, MÁ; Vélez-Díaz-Pallarés, M, 2020)	0.56
" We previously characterized RPV metabolism after oral dosing and identified seven metabolites: four metabolites resulting from mono- or dioxygenation of the 2,6-dimethylphenyl ring itself or either of the two methyl groups located on that ring, one N-linked RPV glucuronide conjugate, and two O-linked RPV glucuronides produced via glucuronidation of mono- and dihydroxymethyl metabolites."	( Metabolism of Long-Acting Rilpivirine After Intramuscular Injection: HIV Prevention Trials Network Study 076 (HPTN 076). Bekker, LG; Bumpus, NN; Farrior, J; Hendrix, CW; Justman, J; Lade, JM; Li, S; Mgodi, N; Pathak, S; Richardson, P; Seneviratne, HK; Sista, N; Swaminathan, S; Tillotson, J, 2021)	0.62
"Phase 3 clinical studies showed non-inferiority of long-acting intramuscular cabotegravir and rilpivirine dosed every 4 weeks to oral antiretroviral therapy."	( Long-acting cabotegravir and rilpivirine dosed every 2 months in adults with HIV-1 infection (ATLAS-2M), 48-week results: a randomised, multicentre, open-label, phase 3b, non-inferiority study. Andrade-Villanueva, JF; Benn, P; Bredeek, F; Chounta, V; Crauwels, H; Cutrell, A; Ford, S; García Deltoro, M; Hudson, KJ; Jaeger, H; Khuong-Josses, MA; Margolis, DA; Nagimova, F; Orrell, C; Overton, ET; Patel, P; Richmond, G; Rizzardini, G; Shaefer, M; Smith, KY; Spreen, W; Swindells, S; Talarico, C; van Eygen, V; Van Solingen-Ristea, R; Vanveggel, S; Wang, Y; Wong, A, 2021)	0.62
" Cabotegravir plus rilpivirine long-acting every 8 weeks was non-inferior to dosing every 4 weeks (HIV-1 RNA ≥50 copies per mL; 2% vs 1%) with an adjusted treatment difference of 0·8 (95% CI -0·6-2·2)."	( Long-acting cabotegravir and rilpivirine dosed every 2 months in adults with HIV-1 infection (ATLAS-2M), 48-week results: a randomised, multicentre, open-label, phase 3b, non-inferiority study. Andrade-Villanueva, JF; Benn, P; Bredeek, F; Chounta, V; Crauwels, H; Cutrell, A; Ford, S; García Deltoro, M; Hudson, KJ; Jaeger, H; Khuong-Josses, MA; Margolis, DA; Nagimova, F; Orrell, C; Overton, ET; Patel, P; Richmond, G; Rizzardini, G; Shaefer, M; Smith, KY; Spreen, W; Swindells, S; Talarico, C; van Eygen, V; Van Solingen-Ristea, R; Vanveggel, S; Wang, Y; Wong, A, 2021)	0.62
"The efficacy and safety profiles of dosing every 8 weeks and dosing every 4 weeks were similar."	( Long-acting cabotegravir and rilpivirine dosed every 2 months in adults with HIV-1 infection (ATLAS-2M), 48-week results: a randomised, multicentre, open-label, phase 3b, non-inferiority study. Andrade-Villanueva, JF; Benn, P; Bredeek, F; Chounta, V; Crauwels, H; Cutrell, A; Ford, S; García Deltoro, M; Hudson, KJ; Jaeger, H; Khuong-Josses, MA; Margolis, DA; Nagimova, F; Orrell, C; Overton, ET; Patel, P; Richmond, G; Rizzardini, G; Shaefer, M; Smith, KY; Spreen, W; Swindells, S; Talarico, C; van Eygen, V; Van Solingen-Ristea, R; Vanveggel, S; Wang, Y; Wong, A, 2021)	0.62
" Also, agents with novel mechanisms of action, such as Lenacapavir, have been tested in early-phase studies and are currently being tested in phase 2-3 clinical trials; if successful, this may allow six-monthly dosing schedules."	( Long-acting injectable HIV therapies: the next frontier. Orkin, C; Thornhill, J, 2021)	0.62
" Treatment with long-acting (LA), injection-based ART administered by healthcare professionals (directly observed therapy (DOT)) eliminates the need for adherence to daily dosing and may improve clinical outcomes."	( Cost-effectiveness of the long-acting regimen cabotegravir plus rilpivirine for the treatment of HIV-1 and its potential impact on adherence and viral transmission: A modelling study. Anderson, SJ; Arthurs, E; Becker, D; Chounta, V; Hayward, O; Jacob, I; Parker, B; Van de Velde, N; Ward, T, 2021)	0.62
" Also, agents with novel mechanisms of action, such as Lenacapavir, have been tested in early-phase studies and are currently being tested in phase 2-3 clinical trials; if successful, this may allow six-monthly dosing schedules."	( Long-acting injectable HIV therapies: the next frontier: Republication. Orkin, C; Thornhill, J, 2021)	0.62
"Efficacy and safety of long-acting cabotegravir (CAB) and rilpivirine (RPV) dosed intramuscularly every 4 or 8 weeks has been demonstrated in three Phase 3 trials."	( Exploring predictors of HIV-1 virologic failure to long-acting cabotegravir and rilpivirine: a multivariable analysis. Aboud, M; Baker, M; Clair, MS; Crauwels, H; Cutrell, AG; Dorey, D; Ford, SL; Jeffrey, J; Kuritzkes, DR; Margolis, DA; Patel, P; Perno, CF; Polli, JW; Quercia, R; Schapiro, JM; Spreen, WR; Talarico, CL; Van Eygen, V; van Lunzen, J; Vandermeulen, K; Vanveggel, S; Wang, Y; White, CT; Wu, S, 2021)	0.62
"Data from 1039 adults naive to long-acting CAB+RPV were pooled in a multivariable analysis to examine the influence of baseline viral and participant factors, dosing regimen and drug concentrations on confirmed virologic failure (CVF) occurrence using a logistic regression model."	( Exploring predictors of HIV-1 virologic failure to long-acting cabotegravir and rilpivirine: a multivariable analysis. Aboud, M; Baker, M; Clair, MS; Crauwels, H; Cutrell, AG; Dorey, D; Ford, SL; Jeffrey, J; Kuritzkes, DR; Margolis, DA; Patel, P; Perno, CF; Polli, JW; Quercia, R; Schapiro, JM; Spreen, WR; Talarico, CL; Van Eygen, V; van Lunzen, J; Vandermeulen, K; Vanveggel, S; Wang, Y; White, CT; Wu, S, 2021)	0.62
" The phase 3 ATLAS and FLAIR studies showed non-inferiority of long-acting cabotegravir and rilpivirine dosed every 4 weeks compared with standard oral therapy for the maintenance of virological suppression in adults with HIV-1 over 48 weeks."	( Long-acting cabotegravir plus rilpivirine for treatment in adults with HIV-1 infection: 96-week results of the randomised, open-label, phase 3 FLAIR study. Bassa, A; Brinson, C; Chounta, V; Crauwels, H; Cutrell, A; D'Amico, R; Degen, O; Dorey, D; Ford, SL; García, JG; Griffith, S; Gusev, D; Margolis, DA; Morell, EB; Oka, S; Orkin, C; Patel, P; Philibert, P; Smith, KY; Spreen, WR; St Clair, M; Tan, DHS; Thiagarajah, S; Van Eygen, V; Van Solingen-Ristea, R; Vandermeulen, K; Vanveggel, S, 2021)	0.62
" Patient-reported outcomes (PROs) collected in an HIV-1 clinical trial (ATLAS-2M; NCT03299049) comparing participants' experience with two dosing regimens (every 4 weeks [Q4W] vs."	( Patient-Reported Outcomes Through 1 Year of an HIV-1 Clinical Trial Evaluating Long-Acting Cabotegravir and Rilpivirine Administered Every 4 or 8 Weeks (ATLAS-2M). Benn, PD; Chounta, V; Hudson, KJ; Margolis, DA; Mills, A; Overton, ET; Shaefer, MS; Smith, KY; Spreen, WR; Swindells, S; van Solingen-Ristea, R; Vanveggel, S; Wang, Y, 2021)	0.62
" For participants without prior CAB + RPV exposure, large increases from baseline were reported in treatment satisfaction in both long-acting arms (HIVTSQ status version), with Q8W dosing statistically significantly favored at Weeks 24 (p = 0."	( Patient-Reported Outcomes Through 1 Year of an HIV-1 Clinical Trial Evaluating Long-Acting Cabotegravir and Rilpivirine Administered Every 4 or 8 Weeks (ATLAS-2M). Benn, PD; Chounta, V; Hudson, KJ; Margolis, DA; Mills, A; Overton, ET; Shaefer, MS; Smith, KY; Spreen, WR; Swindells, S; van Solingen-Ristea, R; Vanveggel, S; Wang, Y, 2021)	0.62
"Both long-acting regimens provided high treatment satisfaction and acceptance, irrespective of prior CAB + RPV exposure, with most participants preferring Q8W dosing over both the Q4W regimen and their previous daily oral regimen."	( Patient-Reported Outcomes Through 1 Year of an HIV-1 Clinical Trial Evaluating Long-Acting Cabotegravir and Rilpivirine Administered Every 4 or 8 Weeks (ATLAS-2M). Benn, PD; Chounta, V; Hudson, KJ; Margolis, DA; Mills, A; Overton, ET; Shaefer, MS; Smith, KY; Spreen, WR; Swindells, S; van Solingen-Ristea, R; Vanveggel, S; Wang, Y, 2021)	0.62
"ATLAS (NCT02951052), a phase 3, multicenter, open-label study, demonstrated that switching to injectable cabotegravir (CAB) with rilpivirine (RPV) long-acting dosed every 4 weeks was noninferior at week (W) 48 to continuing three-drug daily oral current antiretroviral therapy (CAR)."	( Week 96 extension results of a Phase 3 study evaluating long-acting cabotegravir with rilpivirine for HIV-1 treatment. Benn, P; Chounta, V; Crauwels, H; Ford, SL; Harrington, CM; Hove, K; Huang, JO; Lutz, T; Margolis, DA; Mitha, E; Porteiro, N; Shon, A; Smith, KY; Spreen, WR; Stoll, M; Swindells, S; Talarico, CL; Van Solingen-Ristea, R; Van Zyl, L; Vandermeulen, K; Vanveggel, S, 2022)	0.72
" In addition, islatravir, a first-in-class nucleoside reverse transcriptase translocation inhibitor, is intended to be formulated as an implant with a dosing interval of 1 year or more."	( Long-acting antiretrovirals: a new era for the management and prevention of HIV infection. Buclin, T; Cavassini, M; Choong, E; Decosterd, LA; Thoueille, P, 2022)	0.72
" Virologically suppressed adults with HIV-1, either already receiving intramuscular long-acting cabotegravir and rilpivirine every 4 weeks (ie, ATLAS study rollover participants) or oral standard of care, were randomly assigned (1:1), in an unblinded fashion, to receive either intramuscular long-acting cabotegravir (600 mg) and rilpivirine (900 mg) every 8 weeks (ie, the every 8-week dosing group) or intramuscular long-acting cabotegravir (400 mg) and rilpivirine (600 mg) every 4 weeks (ie, the every 4-week dosing group)."	( Long-acting cabotegravir and rilpivirine dosed every 2 months in adults with HIV-1 infection (ATLAS-2M), 96-week results: a randomised, multicentre, open-label, phase 3b, non-inferiority study. Ajana, F; Andrade-Villanueva, JF; Belonosova, E; Benn, PD; Crauwels, H; Español, CM; Ford, SL; Hermida, AO; Hudson, KJ; Jaeger, H; Margolis, DA; Mngqibisa, R; Overton, ET; Richmond, G; Rizzardini, G; Smith, KY; Spreen, WR; Talarico, CL; Thalme, A; van Eygen, V; Van Solingen-Ristea, R; Vanveggel, S; Wang, Y, 2021)	0.62
"Between Oct 27, 2017, and May 31, 2018, a total of 1149 participants were screened; of whom, 1049 (91%) were randomly assigned and 1045 (91%) initiated treatment (522 in the every 8-week dosing group and 523 in the every 4-week dosing group)."	( Long-acting cabotegravir and rilpivirine dosed every 2 months in adults with HIV-1 infection (ATLAS-2M), 96-week results: a randomised, multicentre, open-label, phase 3b, non-inferiority study. Ajana, F; Andrade-Villanueva, JF; Belonosova, E; Benn, PD; Crauwels, H; Español, CM; Ford, SL; Hermida, AO; Hudson, KJ; Jaeger, H; Margolis, DA; Mngqibisa, R; Overton, ET; Richmond, G; Rizzardini, G; Smith, KY; Spreen, WR; Talarico, CL; Thalme, A; van Eygen, V; Van Solingen-Ristea, R; Vanveggel, S; Wang, Y, 2021)	0.62
"Long-acting cabotegravir and rilpivirine dosed every 8 weeks had non-inferior efficacy compared with that of every 4 weeks through the 96-week analysis, with both regimens maintaining high levels of virological suppression."	( Long-acting cabotegravir and rilpivirine dosed every 2 months in adults with HIV-1 infection (ATLAS-2M), 96-week results: a randomised, multicentre, open-label, phase 3b, non-inferiority study. Ajana, F; Andrade-Villanueva, JF; Belonosova, E; Benn, PD; Crauwels, H; Español, CM; Ford, SL; Hermida, AO; Hudson, KJ; Jaeger, H; Margolis, DA; Mngqibisa, R; Overton, ET; Richmond, G; Rizzardini, G; Smith, KY; Spreen, WR; Talarico, CL; Thalme, A; van Eygen, V; Van Solingen-Ristea, R; Vanveggel, S; Wang, Y, 2021)	0.62
" This has necessitated the development of long-acting antiretroviral formulations administrable via an infrequent dosing regimen."	( Use of long-acting injectable antiretroviral agents for human immunodeficiency Virus: A review. Ariyo, OE; Jones, CE, 2022)	0.72
" Prescribed dosage and drug concentrations in plasma are based on patient data collected in clinical trials, but actual patients are expected to exhibit more variability in drug concentrations, which is important to quantify."	( Miniature mass spectrometer-based point-of-care assay for cabotegravir and rilpivirine in whole blood. Anderson, PL; Bushman, LR; Castillo-Mancilla, J; Cooks, RG; Hu, Y; Pandey, S, 2022)	0.72
" By extending the dosing interval, increasing convenience and being discreet these regimens may reduce HIV treatment challenges."	( Implementation of long-acting antiretroviral therapy in low-income and middle-income countries. Cresswell, FV; Lamorde, M, 2022)	0.72
"Long-acting (LA) anti-HIV regimens show promise for increasing dosing intervals and consequently, improving the patients' quality of life."	( Drug Interactions in Lenacapavir-Based Long-Acting Antiviral Combinations. Cilento, ME; Ong, YT; Sarafianos, SG; Tedbury, PR, 2022)	0.72
" The COVID-19 pandemic presents a potential challenge to patients' ability to attend scheduled clinic visits for dosing administration."	( Brief Report: Impact of COVID-19 on Cabotegravir Plus Rilpivirine Long-Acting Dosing Across 6 Ongoing Global Phase IIb and III Clinical Trials. Benn, P; Czarnogorski, M; D'Amico, R; Español, CM; Fricker, J; Goodchild, J; Griffith, S; Harrington, C; McCoig, C; Nwafor, T; Patel, P; Saggu, P; Sutton, K; Williams, W; Yague, I, 2022)	0.72
"COVID-19-impacted visits were defined as modified dosing visits for which oral therapy was provided to participants unable to attend the clinic or injection visits that were rescheduled."	( Brief Report: Impact of COVID-19 on Cabotegravir Plus Rilpivirine Long-Acting Dosing Across 6 Ongoing Global Phase IIb and III Clinical Trials. Benn, P; Czarnogorski, M; D'Amico, R; Español, CM; Fricker, J; Goodchild, J; Griffith, S; Harrington, C; McCoig, C; Nwafor, T; Patel, P; Saggu, P; Sutton, K; Williams, W; Yague, I, 2022)	0.72
"Of 2127 participants in cabotegravir + rilpivirine LA trials, 1997 (94%) had LA dosing visits proceed as planned during the COVID-19 pandemic."	( Brief Report: Impact of COVID-19 on Cabotegravir Plus Rilpivirine Long-Acting Dosing Across 6 Ongoing Global Phase IIb and III Clinical Trials. Benn, P; Czarnogorski, M; D'Amico, R; Español, CM; Fricker, J; Goodchild, J; Griffith, S; Harrington, C; McCoig, C; Nwafor, T; Patel, P; Saggu, P; Sutton, K; Williams, W; Yague, I, 2022)	0.72
"During the COVID-19 pandemic, most trial participants maintained their LA dosing schedules."	( Brief Report: Impact of COVID-19 on Cabotegravir Plus Rilpivirine Long-Acting Dosing Across 6 Ongoing Global Phase IIb and III Clinical Trials. Benn, P; Czarnogorski, M; D'Amico, R; Español, CM; Fricker, J; Goodchild, J; Griffith, S; Harrington, C; McCoig, C; Nwafor, T; Patel, P; Saggu, P; Sutton, K; Williams, W; Yague, I, 2022)	0.72
" The approval of intramuscular cabotegravir (CAB) and rilpivirine (RPV) offers a new therapeutic modality with the opportunity of a longer dosing frequency."	( An evaluation of long-acting cabotegravir + rilpivirine for the treatment of virologically suppressed adults living with HIV. Cory, TJ; Parganas, C; Qazzaz, H, 2022)	0.72
" However, given the long dosing interval, the conduct of clinical DDIs studies with LA antiretrovirals is challenging."	( Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study. Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023)	0.91
" An increase in the dosing frequency did not overcome the DDI with rifampicin."	( Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study. Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023)	0.91
"LA cabotegravir/rilpivirine should be avoided with strong inducers but coadministration with moderate inducers is possible by adding oral rilpivirine daily dosing to the monthly injection."	( Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study. Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023)	0.91
"Cabotegravir (CAB) + rilpivirine (RPV) dosed intramuscularly monthly or every 2 months is a complete, long-acting (LA) regimen for the maintenance of HIV-1 virologic suppression."	( Long-Acting Cabotegravir and Rilpivirine Dosed Every 2 Months in Adults With Human Immunodeficiency Virus 1 Type 1 Infection: 152-Week Results From ATLAS-2M, a Randomized, Open-Label, Phase 3b, Noninferiority Study. Acuipil, C; Aksar, A; Crauwels, H; D'Amico, R; Español, CM; Ford, SL; Girard, PM; Harrington, C; Latham, CL; Noe, S; Overton, ET; Porteiro, N; Reynes, J; Richmond, G; Rizzardini, G; Smith, KY; Spreen, WR; Swindells, S; Thalme, A; Thiagarajah, S; van Eygen, V; Van Solingen-Ristea, R; Vandermeulen, K; Wang, Y; Wong, A, 2023)	0.91
" Long-acting cabotegravir with rilpivirine ART has reduced required dosing frequency from once daily to once every month or every 2 months injections."	( Long-acting antiretrovirals and HIV treatment adherence. Archary, M; Decloedt, E; Gandhi, M; Geng, EH; Mellors, JW; Mofenson, LM; Nachega, JB; Nachman, S; Rawat, A; Scarsi, KK; Scott, RK; Wilson, L, 2023)	0.91
"Pooled data from 1651 participants were used to explore dosing regimen (every 4 or every 8 weeks), demographic, viral, and pharmacokinetic covariates as potential predictors of CVF."	( Expanded Multivariable Models to Assist Patient Selection for Long-Acting Cabotegravir + Rilpivirine Treatment: Clinical Utility of a Combination of Patient, Drug Concentration, and Viral Factors Associated With Virologic Failure. Crauwels, H; Cutrell, AG; D'Amico, R; DeMoor, R; Dorey, D; Ford, SL; Garges, HP; Han, K; Kuritzkes, DR; Latham, CL; Orkin, C; Patel, P; Perno, CF; Polli, JW; Schapiro, JM; Spreen, WR; St Clair, M; Van Eygen, V; van Wyk, J; Vandermeulen, K; Vanveggel, S; Wang, Y; Zolopa, A, 2023)	0.91
" However, each remains limited by existing dosing intervals, ease of administration, or difficulties in finding drug partners."	( Advances in long-acting slow effective release antiretroviral therapies for treatment and prevention of HIV infection. Das, S; Deodhar, S; Edagwa, B; Gendelman, HE; Hasan, M; Sillman, B; Soriano, V; Sultana, A; Thai Hoang Le, N; Ullah Nayan, M, 2023)	0.91
" Due to their long dosing interval, clinical studies with IM CAB/RPV are challenging."	( Intramuscular cabotegravir and rilpivirine concentrations after switching from efavirenz-containing regimen. Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023)	0.91
"Cabotegravir plus rilpivirine is the only approved complete long-acting regimen for the maintenance of HIV-1 virological suppression dosed every 2 months."	( Efficacy, safety, and tolerability of switching to long-acting cabotegravir plus rilpivirine versus continuing fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed adults with HIV, 12-month results (SOLAR): a random Berni, A; Castagna, A; Cazanave, C; Chounta, V; D'Amico, R; Di Perri, G; Diaz-Brito, V; Dretler, R; Garges, HP; Latham, CL; Oka, S; Osiyemi, O; Pascual Bernáldez, M; Patel, P; Ramgopal, MN; Sims, J; Smith, K; Spreen, WR; Sutherland-Phillips, D; Sutton, K; Van Eygen, V; Van Solingen-Ristea, R; van Wyk, J; Walmsley, S; Zhang, F, 2023)	0.91
" Participants with HIV-1 RNA less than 50 copies per mL were randomly assigned (2:1), stratified by sex at birth and BMI, to either long-acting cabotegravir (600 mg) plus rilpivirine (900 mg) dosed intramuscularly every 2 months or to continue daily oral bictegravir (50 mg), emtricitabine (200 mg), and tenofovir alafenamide (25 mg)."	( Efficacy, safety, and tolerability of switching to long-acting cabotegravir plus rilpivirine versus continuing fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed adults with HIV, 12-month results (SOLAR): a random Berni, A; Castagna, A; Cazanave, C; Chounta, V; D'Amico, R; Di Perri, G; Diaz-Brito, V; Dretler, R; Garges, HP; Latham, CL; Oka, S; Osiyemi, O; Pascual Bernáldez, M; Patel, P; Ramgopal, MN; Sims, J; Smith, K; Spreen, WR; Sutherland-Phillips, D; Sutton, K; Van Eygen, V; Van Solingen-Ristea, R; van Wyk, J; Walmsley, S; Zhang, F, 2023)	0.91
"These data support the use of long-acting cabotegravir plus rilpivirine dosed every 2 months as a complete antiretroviral regimen that has similar efficacy to a commonly used integrase strand transfer inhibitor-based first-line regimen, while addressing unmet psychosocial issues associated with daily oral treatment."	( Efficacy, safety, and tolerability of switching to long-acting cabotegravir plus rilpivirine versus continuing fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed adults with HIV, 12-month results (SOLAR): a random Berni, A; Castagna, A; Cazanave, C; Chounta, V; D'Amico, R; Di Perri, G; Diaz-Brito, V; Dretler, R; Garges, HP; Latham, CL; Oka, S; Osiyemi, O; Pascual Bernáldez, M; Patel, P; Ramgopal, MN; Sims, J; Smith, K; Spreen, WR; Sutherland-Phillips, D; Sutton, K; Van Eygen, V; Van Solingen-Ristea, R; van Wyk, J; Walmsley, S; Zhang, F, 2023)	0.91
" Body mass index, late injection, and monthly versus every two-month dosing were not associated with detectable viremia after switch."	( Predictors of Post-switch Viremia in People With HIV on Injectable Cabotegravir/Rilpivirine. Abulhosn, K; Bamford, L; Hill, L; Karim, A; Kenney, S; Patel, N; Yin, J, 2024)	1.44

Role	Description
HIV-1 reverse transcriptase inhibitor	An entity which inhibits the activity of HIV-1 reverse transcriptase.
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor	A DNA polymerase inhibitor that interferes with the activity of reverse transcriptase, EC 2.7.7.49, a viral DNA polymerase enzyme that retroviruses need in order to reproduce.
[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]

Class	Description
nitrile	A compound having the structure RC#N; thus a C-substituted derivative of hydrocyanic acid, HC#N. In systematic nomenclature, the suffix nitrile denotes the triply bound #N atom, not the carbon atom attached to it.
aminopyrimidine	A member of the class of pyrimidines that is pyrimidine substituted by at least one amino group and its derivatives.
[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	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	22.3872	0.0096	10.5250	35.4813	AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Gag-Pol polyprotein	HIV-1 M:B_HXB2R	IC50 (µMol)	0.0680	0.0006	0.9141	8.3200	AID1802585
Cytochrome P450 1A2	Homo sapiens (human)	IC50 (µMol)	6.1612	0.0001	1.7740	10.0000	AID1561725; AID1583018; AID1773465; AID1811055; AID1862573; AID1884496
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	1.7406	0.0001	1.7536	10.0000	AID1561730; AID1773469; AID1811059; AID1862577; AID1884499
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	2.3635	0.0000	2.0151	10.0000	AID1561728; AID1583018; AID1773468; AID1811058; AID1862576; AID1884498
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	0.2818	0.0000	2.8005	10.0000	AID1561726; AID1773466; AID1811056; AID1862574; AID1884495
Cytochrome P450 2C19	Homo sapiens (human)	IC50 (µMol)	0.3363	0.0000	2.3983	10.0000	AID1773467; AID1811057; AID1862575; AID1884497
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	0.5000	0.0009	1.9014	10.0000	AID1561756; AID1583018; AID1773473; AID1880375; AID1884536
Reverse transcriptase/RNaseH	Human immunodeficiency virus 1	IC50 (µMol)	0.5721	0.0001	1.0768	10.0000	AID1264545; AID1264546; AID1552565; AID1552566; AID1561723; AID1561724; AID1561725; AID1561726; AID1561727; AID1561728; AID1561729; AID1561730; AID1572530; AID1591871; AID1685253; AID1773463; AID1773843; AID1822283; AID508800
Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)	IC50 (µMol)	1.5000	0.0040	1.9666	10.0000	AID1873190
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Reverse transcriptase/RNaseH	Human immunodeficiency virus 1	EC50 (µMol)	0.0016	0.0004	0.6153	9.7000	AID1466753; AID1882483; AID757627
Reverse transcriptase	Human immunodeficiency virus 1	EC50 (µMol)	0.0010	0.0002	1.1683	9.0740	AID1882484; AID1882485; AID1882486; AID1882487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
viral life cycle	Gag-Pol polyprotein	HIV-1 M:B_HXB2R
establishment of integrated proviral latency	Gag-Pol polyprotein	HIV-1 M:B_HXB2R
steroid catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
porphyrin-containing compound metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
toxin biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
post-embryonic development	Cytochrome P450 1A2	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
regulation of gene expression	Cytochrome P450 1A2	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
dibenzo-p-dioxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lung development	Cytochrome P450 1A2	Homo sapiens (human)
methylation	Cytochrome P450 1A2	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
cellular respiration	Cytochrome P450 1A2	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
hydrogen peroxide biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 1A2	Homo sapiens (human)
cellular response to cadmium ion	Cytochrome P450 1A2	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C19	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C19	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C19	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
lipid transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
organic anion transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
biotin transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
sphingolipid biosynthetic process	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
riboflavin transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate metabolic process	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
transmembrane transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
transepithelial transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
renal urate salt excretion	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
export across plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
transport across blood-brain barrier	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
cellular detoxification	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
peptidase activity	Gag-Pol polyprotein	HIV-1 M:B_HXB2R
integrase activity	Gag-Pol polyprotein	HIV-1 M:B_HXB2R
monooxygenase activity	Cytochrome P450 1A2	Homo sapiens (human)
iron ion binding	Cytochrome P450 1A2	Homo sapiens (human)
protein binding	Cytochrome P450 1A2	Homo sapiens (human)
electron transfer activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 1A2	Homo sapiens (human)
enzyme binding	Cytochrome P450 1A2	Homo sapiens (human)
heme binding	Cytochrome P450 1A2	Homo sapiens (human)
demethylase activity	Cytochrome P450 1A2	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 1A2	Homo sapiens (human)
aromatase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activity	Cytochrome P450 1A2	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C19	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C19	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxygen binding	Cytochrome P450 2C19	Homo sapiens (human)
enzyme binding	Cytochrome P450 2C19	Homo sapiens (human)
heme binding	Cytochrome P450 2C19	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C19	Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activity	Cytochrome P450 2C19	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C19	Homo sapiens (human)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATP binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
organic anion transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
biotin transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
efflux transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATP hydrolysis activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
riboflavin transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
identical protein binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
protein homodimerization activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
sphingolipid transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
endoplasmic reticulum membrane	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C19	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C19	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C19	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C19	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C19	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
nucleoplasm	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
apical plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
brush border membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
mitochondrial membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
membrane raft	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
external side of apical plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (771)

Assay ID	Title	Year	Journal	Article
AID1750714	Antiviral activity against HIV-1 infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1357807	Cytotoxicity against human TZM-bl cells by CytoTox-Glo reagent-based assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID585331	Drug level in Beagle dog lymph node popliteal at 5 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561739	Solubility of the compound in pH 2.0 buffer by HPLC analysis
AID701093	Antiviral activity against HIV1 infected in human assessed as log reduction in viral load at 25 to 150 mg administered QD for 7 days measured on day 8 relative to placebo-control	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
AID1773459	Resistance factor, ratio of EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID585293	Ratio of drug level in spleen to plasma in male Beagle dog at 200 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID635194	Antiviral activity against Human immunodeficiency virus expressing RT K103N mutant infected in human MT4 cells by p24 antigen assay in the presence of 50% normal human serum	2011	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24	Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID508659	Antiviral activity against Human immunodeficiency virus 1 group M subtype C assessed as days to viral replication breakthrough at 200 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1693799	Antiviral activity against HIV-3B infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 01-15, Volume: 30	Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID585065	Cmax in male Sprague-Dawley rat at 200 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1302310	Antiviral activity against HIV1 NL4-3 assessed as inhibition of viral infection in human TZM-bl cells measured after 1 day by luciferase reporter gene assay	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID584855	Tmax in Sprague-Dawley rat at 20 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1819215	Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID252955	Ratio of CC50 and EC50 against wild type human immunodeficiency virus type 1 LAI strain	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID508822	Antiviral activity against Human immunodeficiency virus 1 group M subtype AG assessed as days f for viral replication at 200 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508810	Antiviral activity against Human immunodeficiency virus 1 group M subtype A1 assessed as days to viral replication breakthrough at 40 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID757622	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B	2013	European journal of medicinal chemistry, Jul, Volume: 65	Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID585091	AUC (0 to last) in Beagle dog at 5 mg/kg, sc after 184 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID757624	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2013	European journal of medicinal chemistry, Jul, Volume: 65	Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1072806	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells	2014	Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6	Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
AID1773451	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells
AID1811059	Inhibition of human CYP3A4 using testosterone as substrate in presence of NADPH incubated for 15 to 45 mins	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID767499	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID585072	Tmax in female Sprague-Dawley rat at 200 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1466754	Inhibition of rilpivirine-resistant HIV1 NL4-3 reverse transcriptase E138K/M1841 double mutant infected in human TZM-b1 cells after 2 days by bright Glo-luciferase reporter gene assay	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID1264540	Antiviral activity against HIV-1 X4 expressing reverse transcriptase K103N mutant infected in human CD4+ T cells for 3 days by FACS analysis	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID508752	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773455	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring E138K mutant infected in human MT4 cells
AID585303	Ratio of drug level in spleen to plasma in male Beagle dog at 200 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID709859	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C/V179F double mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1184481	Aqueous solubility of the compound at pH 7.4 by HPLC analysis	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID585542	Ratio of drug level in spleen to plasma in female Beagle dog at 400 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585546	Ratio of drug level in thymus to plasma in female Beagle dog at 400 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585318	Drug level in Beagle dog liver at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585101	Drug level in Sprague-Dawley rat muscle at injected site at 20 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585507	Drug level in Beagle dog spleen at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585070	AUC (0 to last) in male Sprague-Dawley rat at 400 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585267	Drug level in Beagle dog skin at non-injected site at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508651	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585076	AUC (0 to last) in female Sprague-Dawley rat at 400 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID237173	Half life in dog was determined by intravenous administration	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID585044	Cmax in male Sprague-Dawley rat at 400 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585038	Cmax in female Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585535	Drug level in female Beagle dog spleen at 200 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID293566	Metabolic stability in rat liver microsomes after 15 mins	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID585501	Drug level in Beagle dog lymph node mandibular at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID653699	Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for Human immunodeficiency virus 1 NL4-3	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID508780	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138S mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1882483	Inhibition of wild type HIV-1 reverse transcriptase assessed as reduction in luciferase reporter activity by single-round assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1819233	Aqueous solubility of the compound at pH 7.0 by HPLC analysis
AID585290	Drug level in female Beagle dog thymus at 400 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID293571	Half life in Wistar rat at 10 mg/kg, po after 6 hrs	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID508785	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138A mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508776	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179T mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585312	Plasma concentration in Beagle dog at 5 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585510	Ratio of drug level in spleen to plasma in Beagle dog at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585552	Ratio of drug level in spleen to plasma in female Beagle dog at 400 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585539	Drug level in female Beagle dog thymus at 200 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1884496	Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate incubated for 15 to 40 mins in presence of NADPH	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID585037	AUC (0 to last) in female Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773845	Intrinsic clearance in human liver microsomes at 1 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID585302	Ratio of drug level in spleen to plasma in male Beagle dog at 400 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1552565	Inhibition of HIV1 Reverse transcriptase polymerase assessed as decrease in digoxigenin and biotin-dUTP incorporation into DNA using poly(A)/oligo(dT)15 as template/primer by ELISA	2019	Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16	Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID585046	AUC (0 to last) in male Sprague-Dawley rat at 400 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585034	AUC (0 to last) in male Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584853	Tmax in Sprague-Dawley rat at 5 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID293559	Antiviral activity against HIV1 LAI with RT Y188L mutation in MT4 cells by EGFP based replication assay	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID449195	Antimalarial activity against Plasmodium falciparum W2mef at 10 uM after 48 hrs by hoechst 33342-thiazole orange stain based flow cytometry assay	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID585548	Ratio of drug level in thymus to plasma in female Beagle dog at 400 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584861	Absolute bioavailability in Sprague-Dawley rat at 5 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508772	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y188L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585039	Tmax in female Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585063	Tmax in female Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773460	Resistance factor, ratio of EC50 for HIV1 harboring Y188L mutant mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID585276	Drug level in male Beagle dog spleen at 400 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508779	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1289687	Antiviral activity against HIV1 NL4.3 expressing reverse transcriptase K103N mutant infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hrs by luciferase assay	2016	Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5	2,6-Di(arylamino)-3-fluoropyridine Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors.
AID1819217	Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1636149	Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase K103N/V179F/Y181C mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells	2016	Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15	Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID508634	Antiviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1552566	Inhibition of HIV1 reverse transcriptase RNase H using 18-nucleotide 3'-fluorescein-labeled RNA/5'-dabcyl-labeled DNA hybrid as substrate measured after 1 hr by FRET based assay	2019	Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16	Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID585557	Toxicity in Beagle dog assessed as untoward effects at 20 mg/kg, sc	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1466756	Fold resistance, ratio of EC50 for rilpivirine-resistant HIV1 NL4-3 reverse transcriptase E138K/M184I double mutant to EC50 for wild type HIV1 NL4-3 reverse transcriptase	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID1633403	Antiviral activity against wild-type HIV1 NL4-3 infected infected in human MT2 cells assessed as reduction in HIV1 intracellular genomic RNA level at 1 uM and measured after 30 hrs post infection by TaqMan probe based RT-PCR analysis	2019	ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4	Synthesis and Evaluation of Bifunctional Aminothiazoles as Antiretrovirals Targeting the HIV-1 Nucleocapsid Protein.
AID1811048	Aqueous solubility of compound in PBS at pH 7 by HPLC-UV analysis	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID585082	Cmax in Beagle dog at 5 mg/kg, sc after 176 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585337	Ratio of drug level in lymph node popliteal to plasma in Beagle dog at 5 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508791	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101Q mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585288	Drug level in female Beagle dog spleen at 400 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773465	Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate in presence of NADPH incubated for 10 mins by LC-MS/MS analysis
AID1264545	Inhibition of wild-type HIV-1 reverse transcriptase by fluorescence assay	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID585052	AUC (0 to last) in female Sprague-Dawley rat at 400 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585339	Ratio of drug level in lymph node popliteal to plasma in Beagle dog at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508625	Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 93TH073 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1811055	Inhibition of human CYP1A2 using phenacetin as substrate in presence of NADPH incubated for 15 to 45 mins	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID585309	Plasma concentration in Beagle dog at 5 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508763	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585272	Plasma concentration in male Beagle dog at 400 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773464	Solubility in phosphate buffer at pH7
AID246348	Effective concentration against human immunodeficiency virus type 1 mutated at 100I	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1750715	Cytotoxicity against in human MT-4 cells after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1884495	Inhibition of CYP2C9 in human liver microsomes using sulfaphenazole as substrate incubated for 15 to 40 mins in presence of NADPH	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID508819	Antiviral activity against Human immunodeficiency virus 1 group M subtype H assessed as days to viral replication breakthrough at 40 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID653697	Antiviral activity against Human immunodeficiency virus 1 NL4-3 infected in human TZM-bl cells assessed as inhibition of viral replication	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID585298	Ratio of drug level in thymus to plasma in male Beagle dog at 400 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1880375	Inhibition of human ERG potassium channel	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Structure-Based Discovery of Novel NH
AID653701	Aqueous solubility of the compound at pH 2 by HPLC/UV analysis	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1773444	Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV1 RES056 infected in MT4 cells
AID246265	Effective concentration against human immunodeficiency virus type 1 G190S mutant strain	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1636928	Cytotoxicity against human MT2 cells assessed as growth inhibition by MTT method	2016	Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20	Computer-aided discovery of anti-HIV agents.
AID698953	Aqueous solubility of the compound at pH 2.0 after 4 hrs	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID585549	Ratio of drug level in spleen to plasma in female Beagle dog at 200 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID698951	n-octane-water partition coefficient, log P of the compound at pH 7.4	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID585048	Tmax in female Sprague-Dawley rat at 200 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508646	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, Y188L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585300	Ratio of drug level in thymus to plasma in male Beagle dog at 400 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1302312	Resistance index, ratio of EC50 for rilpivirine resistant HIV1 harboring reverse transcriptase E138K mutant infected in human TZM-bl cells to EC50 for HIV1 NL4-3 infected in human TZM-bl cells	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID1773826	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID653702	Antiviral activity against multi-reverse transcriptase-resistant Human immunodeficiency virus 1	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID585284	Plasma concentration in female Beagle dog at 400 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1302315	Resistance index, ratio of EC50 for multi-NRTI resistant HIV1 A17 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells to EC50 for HIV1 3B infected in human MT2 cells	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID1873190	Inhibition of human ABCG2 expressed in dog MDCK-II-BCRP cells mediated pheophorbide A efflux by flow cytometry	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
AID508789	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103S mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1264544	Ratio of EC50 for HIV-1 expressing reverse transcriptase K101P mutant to EC50 for HIV-1 X4 expressing wild-type reverse transcriptase	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1572521	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells
AID585054	Tmax in male Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508753	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508635	Antiviral activity against Human immunodeficiency virus 1 subtype (H) infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585074	Cmax in female Sprague-Dawley rat at 400 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585531	Plasma concentration in female Beagle dog at 200 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID726436	Cytotoxicity in human MT2 cells assessed as inhibition of cell growth	2013	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4	Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID508788	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106A mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585274	Drug level in male Beagle dog spleen at 400 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773440	Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID508770	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190S mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1866020	Thermodynamic aqueous solubility of the compound	2022	Bioorganic & medicinal chemistry, 02-15, Volume: 56	Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
AID1184479	Fold resistance, ratio of EC50 for HIV1 A17 expressing K103N/Y181C mutant infected in human MT2 cells to EC50 for wild-type HIV1 3B infected in human MT2 cells	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1302309	Antiviral activity against rilpivirine resistant HIV1 harboring reverse transcriptase E138K mutant assessed as inhibition of viral infection in human TZM-bl cells measured after 1 day by luciferase reporter gene assay	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID585516	Ratio of drug level in thymus to plasma in Beagle dog at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID698948	Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human TZM-bl cells assessed as inhibition of viral replication after 2 days by luciferase reporter gene based luminescence assay	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID1072807	Antiviral activity against HIV1 harboring reverse transcriptase K101N mutant infected in human MT4 cells	2014	Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6	Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
AID673432	Cytotoxicity against human MT4 assessed as cell viability after 2 days	2012	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16	Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants.
AID1561708	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID585105	Drug level in Beagle dog muscle at injected site at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508761	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, F227L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508832	Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93IN101 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508833	Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93MW959 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585047	Cmax in female Sprague-Dawley rat at 200 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773456	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells
AID1184477	Selectivity index, ratio of CC50 for human MT2 cells to EC50 for wild type HIV1 3B	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1693800	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 01-15, Volume: 30	Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID585088	AUC (0 to last) in Beagle dog at 5 mg/kg administered intramuscularly after 184 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585506	Drug level in Beagle dog spleen at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508652	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P, K103N, V108I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585514	Drug level in Beagle dog thymus at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID236452	Area under the concentration time curve value in rat (intravenous dosage of 4 mg/kg) was determined	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID585051	Tmax in female Sprague-Dawley rat at 400 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584860	AUC (0 to last) in Sprague-Dawley rat at 5 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508826	Antiviral activity against Human immunodeficiency virus 1 subtype B isolate 93BR021 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID293556	Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1561756	Inhibition of human ERG expressed in HEK293 cells by whole cell electrophysiology assay
AID1811045	Cytotoxicity against mock infected human MT4 cells by MTT assay	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1773446	Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1811050	Oral bioavailability in rat	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID508804	Antiviral activity against Human immunodeficiency virus 1 group M subtype BG assessed as days to viral replication breakthrough at 10 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508751	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID246268	Effective concentration against human immunodeficiency virus type 1 Y181C mutant strain	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1561729	Inhibition of HIV1 RT V106A/F227L mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID585497	Ratio of drug level in lymph node axillar to plasma in Beagle dog at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561727	Inhibition of HIV1 RT Y188L mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID508778	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1583018	Inhibition of human ERG	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID508793	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773827	Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1811047	Aqueous solubility of compound in PBS at pH 2 by HPLC-UV analysis	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1773447	Antiviral activity against wild type HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID508818	Antiviral activity against Human immunodeficiency virus 1 group M subtype G assessed as days to viral replication breakthrough at 40 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID698949	Antiviral activity against multidrug-resistant HIV-1 RTMDR infected in human TZM-bl cells assessed as inhibition of viral replication after 2 days by luciferase reporter gene based luminescence assay	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID585261	Drug level in Beagle dog skin at injected site at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584858	Cmax in Sprague-Dawley rat at 5 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584863	Tmax in Sprague-Dawley rat at 20 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508623	Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG035 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1822283	Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID508628	Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR020 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585328	Ratio of drug level in lymph node iliac to plasma in Beagle dog at 5 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585326	Drug level in Beagle dog lymph node iliac at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585505	Drug level in Beagle dog spleen at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1264538	Antiviral activity against HIV-1 X4 expressing wild-type reverse transcriptase infected in human CD4+ T cells for 3 days by FACS analysis	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID585286	Drug level in female Beagle dog spleen at 400 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID726438	Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method	2013	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4	Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID1773469	Inhibition of CYP3A4M in human liver microsomes using midazolam as substrate in presence of NADPH incubated for 10 mins by LC-MS/MS analysis
AID653705	Half life in human liver microsomes at 1 uM	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID585042	Tmax in male Sprague-Dawley rat at 200 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585106	Drug level in Beagle dog muscle at non-injected site at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID635196	Antiviral activity against Human immunodeficiency virus expressing RT K103N/Y181C double mutant infected in human MT4 cells by p24 antigen assay in the presence of 50% normal human serum	2011	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24	Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID508816	Antiviral activity against Human immunodeficiency virus 1 group M subtype D assessed as days to viral replication breakthrough at 40 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID726439	Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method	2013	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4	Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID585317	Drug level in Beagle dog liver at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508799	Antiviral activity against Human immunodeficiency virus 1 group M subtype A1 assessed as days to viral replication breakthrough at 10 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585333	Drug level in Beagle dog lymph node popliteal at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID237161	Half life in rat was determined after oral administration	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID508760	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V108I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508823	Antiviral activity against Human immunodeficiency virus 1 group M subtype B assessed as days viral replication at 200 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585311	Plasma concentration in Beagle dog at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508641	Antiviral activity against Human immunodeficiency virus 1 subtype AG infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1561707	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID1302321	Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM incubated for 30 mins in presence of NADPH by LC-MS analysis	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID1561725	Inhibition of HIV1 RT K103N mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID757627	Inhibition of HIV RT K103N/Y181C mutant by cell based assay	2013	European journal of medicinal chemistry, Jul, Volume: 65	Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID585285	Drug level in female Beagle dog spleen at 200 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID293560	Antiviral activity against HIV1 LAI with RT K103N mutation in MT4 cells by EGFP based replication assay	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1561716	Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in absence of test compound assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1775792	Antiviral activity against NNRTI-resistant HIV-1 RES056 harboring RT K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1561724	Inhibition of HIV1 RT L100I mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID585543	Ratio of drug level in spleen to plasma in female Beagle dog at 200 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID246266	Effective concentration against human immunodeficiency virus type 1 K103N mutant strain	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID584856	AUC (0 to last) in Sprague-Dawley rat at 20 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID236451	Area under the concentration time curve in rabbit (intravenous dosage of 1.25 mg/kg) was determined	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1773829	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID508774	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585036	Tmax in female Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585081	Absolute bioavailability in Beagle dog rat at 5 mg/kg administered intramuscularly after 176 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773449	Antiviral activity against wild type HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID584865	Absolute bioavailability in Sprague-Dawley rat at 20 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID757626	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2013	European journal of medicinal chemistry, Jul, Volume: 65	Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1636929	Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against viral infection by MTT method	2016	Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20	Computer-aided discovery of anti-HIV agents.
AID508754	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585061	AUC (0 to last) in female Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508621	Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID767497	Cytotoxicity against human MT2 cells assessed as growth inhibition	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID585099	Plasma concentration in Beagle dog at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585278	Drug level in male Beagle dog thymus at 400 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1591875	Cytotoxicity against human MT2 cells infected with wild-type HIV1 NL4-3 measured 48 hrs by MTT assay	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16	Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase.
AID1862573	Inhibition of CYP1A2 (unknown origin)
AID293568	Metabolic stability in human liver microsomes after 15 mins	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1302320	n-octanol-water partition coefficient, logP of compound at pH 7.4 stirred for 24 hrs followed by overnight incubation by HPLC analysis	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID698950	Antiviral activity against HIV-1 harboring reverse transcriptase K101E mutant infected in human TZM-bl cells assessed as inhibition of viral replication after 2 days by luciferase reporter gene based luminescence assay	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID293574	Half life in Beagle dog at 10 mg/kg, po after 23 hrs	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID237195	In vivo half life in dog was determined after oral administration	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1171416	Aqueous solubility of the compound at pH 7	2014	ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11	Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1302319	Aqueous solubility in 0.01 M Hcl at pH 2 at 10 mg/ml after 4 hrs by by UV-HPLC method	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID585053	Cmax in male Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508766	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230V mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1561719	Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against v
AID632804	Cytotoxicity against human MT2 cells infected with HIV1 NL4.3 by MTT assay	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID585504	Ratio of drug level in lymph node mandibular to plasma in Beagle dog at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585524	Drug level in male Beagle dog spleen at 400 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID293569	Cmax in Wistar rat at 10 mg/kg, po	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID767501	Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1561693	Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1591873	Antiviral activity against wild-type HIV1 NL4-3 infected in human MT2 cells measured 48 hrs post-infection by MTT assay	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16	Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase.
AID585057	Tmax in male Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561706	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID585083	Tmax in Beagle dog at 5 mg/kg, sc after 176 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID246349	Effective concentration against human immunodeficiency virus type 1 mutated at 103N	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID585069	Tmax in male Sprague-Dawley rat at 400 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1289686	Antiviral activity against efavirenz resistant R5-tropic HIV1 subtype C VI829 expressing reverse transcriptase L100I-K103N mutant infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hr	2016	Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5	2,6-Di(arylamino)-3-fluoropyridine Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors.
AID585314	Plasma concentration in Beagle dog at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585513	Drug level in Beagle dog thymus at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1636930	Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against viral infection by MTT method	2016	Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20	Computer-aided discovery of anti-HIV agents.
AID1862575	Inhibition of CYP2C19 (unknown origin)
AID508653	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585320	Ratio of drug level in liver to plasma in Beagle dog at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585308	Ratio of drug level in thymus to plasma in male Beagle dog at 400 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508759	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585526	Drug level in male Beagle dog thymus at 400 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585313	Plasma concentration in Beagle dog at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1819213	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 IIIB harboring K103N/Y181C double mutant infected in human MT4 cells
AID1561703	Antiviral activity against HIV1 expressing RT F227L + V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID508803	Antiviral activity against Human immunodeficiency virus 1 group M subtype B assessed as days to viral replication breakthrough at 10 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID653708	Clearance in rat liver microsomes at 1 uM	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1069122	Antiviral activity against HIV harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID1561700	Antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID508830	Antiviral activity against Human immunodeficiency virus 1 subtype B isolate WEJO infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1594860	Half life in human serum at 25 mg, qd	2019	Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10	The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.
AID1775801	Antiviral activity against HIV-1 harboring RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID585110	Drug level in Sprague-Dawley rat skin at injected site at 5 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585301	Ratio of drug level in spleen to plasma in male Beagle dog at 200 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID766431	Cytotoxicity against human MT2 cells by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.
AID508648	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, T386A mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID449198	Antimalarial activity against Plasmodium falciparum W2mef ring form by hoechst 33342-thiazole orange stain based flow cytometry assay	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID585289	Drug level in female Beagle dog thymus at 200 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1819218	Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1302317	Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for HIV1 3B infected in human MT2 cells	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID632799	Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID293561	Antiviral activity against HIV1 LAI with RT Y181C mutation in MT4 cells by EGFP based replication assay	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID508636	Antiviral activity against Human immunodeficiency virus 1 subtype G infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508622	Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG024 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585341	Drug level in Beagle dog lymph node axillar at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID726437	Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase K103N and Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method	2013	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4	Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID757625	Antiviral activity against HIV1 RES056 expressing RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2013	European journal of medicinal chemistry, Jul, Volume: 65	Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID585533	Drug level in female Beagle dog spleen at 200 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585508	Drug level in Beagle dog spleen at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1775798	Antiviral activity against HIV-1 harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID585560	Toxicity in Beagle dog assessed as inflammatory signs at 20 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585305	Ratio of drug level in thymus to plasma in male Beagle dog at 200 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1171411	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay	2014	ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11	Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID585520	Plasma concentration in male Beagle dog at 400 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508765	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M236L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508802	Antiviral activity against Human immunodeficiency virus 1 group M subtype AG assessed as days to viral replication breakthrough at 10 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773462	Resistance factor, ratio of EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID1264542	Aqueous solubility of compound	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1561713	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID709836	Ratio of EC50 for HIV1 expressing wild type reverse transcriptase in presence of human serum albumin and human alpha-1 acid glycoprotein to EC50 for HIV1 expressing wild type reverse transcriptase	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1773453	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells
AID1561696	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID1572554	Solubility in water at pH 7
AID236595	pKa value was determined	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability.
AID508797	Ratio of EC50 for HIV1 in presence of 45 mg/ml HSA to EC50 for HIV1 in absence of serum proteins by GFP assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID236443	Area under the concentration time curve in dog (intravenous dosage of 1.25 mg/kg) was determined	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID449194	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID585068	Cmax in male Sprague-Dawley rat at 400 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561737	Solubility of the compound in pH 7.4 buffer by HPLC analysis
AID508661	Antiviral activity against Human immunodeficiency virus 1 group M subtype F1 assessed as days to viral replication breakthrough at 200 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508626	Antiviral activity against Human immunodeficiency virus 1 subtype E isolate CMU08 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508657	Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF02 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1535520	Solubility of the compound at pH 7.0	2019	Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3	Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
AID653707	Half life in rat liver microsomes at 1 uM	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1171414	Cytotoxicity against human MT2 cells assessed as reduction in cell viability by MTT assay	2014	ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11	Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1773466	Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate in presence of NADPH incubated for 10 mins by LC-MS/MS analysis
AID585277	Drug level in male Beagle dog thymus at 200 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508755	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID584866	Cmax in male Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585551	Ratio of drug level in spleen to plasma in female Beagle dog at 200 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508629	Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR029 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585040	AUC (0 to last) in female Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561697	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 RES056 infected in human MT4 cells
AID632797	Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT2 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID1561720	Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenes
AID673431	Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaV370 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI	2012	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16	Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants.
AID1775800	Antiviral activity against HIV-1 harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID508649	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, V179L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID709858	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181I/V179F double mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID585060	Tmax in female Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585104	Drug level in Beagle dog muscle at injected site at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID236456	Area under the concentration time curve in monkey (intravenous dosage of 1.25 mg/ kg) was determined	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID632800	Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID1069126	Antiviral activity against wild-type HIV infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID236424	Area under the concentration time curve in rat after 40 mg/kg oral dosage	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability.
AID701094	Half life in HIV-infected patient plasma	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
AID585547	Ratio of drug level in thymus to plasma in female Beagle dog at 200 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1862577	Inhibition of CYP3A4T (unknown origin)
AID585094	Plasma concentration in Sprague-Dawley rat at 5 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561717	Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenesulfonamide assessed as protection ag
AID293572	Cmax in Beagle dog at 10 mg/kg, po	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID653706	Clearance in human liver microsomes at 1 uM	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID632795	Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT2 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID585304	Ratio of drug level in spleen to plasma in male Beagle dog at 400 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1775795	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells reduction in cell viability for 5 days by MTT assay to EC50 for antiviral activity against wild type HIV-1 strain IIIB infected in human MT4 cells assessed as reduction in virus-ind	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID508817	Antiviral activity against Human immunodeficiency virus 1 group M subtype F1 assessed as days to viral replication breakthrough at 40 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585528	Drug level in male Beagle dog thymus at 400 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID698958	Half life in human liver microsomes at 1 uM	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID767494	Aqueous solubility of the compound at pH 7	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID585260	Drug level in Sprague-Dawley rat skin at injected site at 20 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1302318	Aqueous solubility in pH 7.4 phosphate buffer at 10 mg/ml after 4 hrs by by UV-HPLC method	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID1069124	Antiviral activity against HIV harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID1775802	Antiviral activity against HIV-1 harboring RT F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID508662	Antiviral activity against Human immunodeficiency virus 1 group M subtype G assessed as days to viral replication breakthrough at 200 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1591871	Inhibition of recombinant HIV1 reverse transcriptase p66/p51 Y181C mutant expressed in Escherichia coli BL21 (DE3) pLysS cells preincubated followed by primer/template addition and measured after 30 mins by picogreen dye-based fluorescence assay	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16	Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase.
AID246352	Effective concentration against human immunodeficiency virus type 1 mutated at 227C	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1552568	Inhibition of Murine leukemia virus reverse transcriptase RNase H using 18-nucleotide 3'-fluorescein-labeled RNA/5'-dabcyl-labeled DNA hybrid as substrate measured after 1 hr by FRET based assay	2019	Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16	Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID508828	Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92RW020 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1466757	Aqueous solubility of the compound in phosphate buffer at pH 7.4 after 4 hrs by HPLC-UV analysis	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID253332	Cytotoxic concentration against wild type human immunodeficiency virus type 1 LA1 strain	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1302316	Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 1 day by CytoTox-Glo assay	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID1289685	Antiviral activity against nevirapine resistant R5-tropic HIV1 subtype C VI829 expressing reverse transcriptase Y181C mutant infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hrs by	2016	Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5	2,6-Di(arylamino)-3-fluoropyridine Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors.
AID508642	Antiviral activity against Human immunodeficiency virus 1 subtype AE infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1685255	Cytotoxicity against human MT2 cells assessed as cell growth inhibition after 5 days by MTT assay	2021	ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2	Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.
AID1561734	Inhibition of CYP2D6 in human liver microsomes using dextromethorphan substrate incubated for 10 mins in presence of NADPH
AID585553	Ratio of drug level in thymus to plasma in female Beagle dog at 200 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585335	Drug level in Beagle dog lymph node popliteal at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID766432	Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.
AID585545	Ratio of drug level in thymus to plasma in female Beagle dog at 200 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585565	Toxicity in Beagle dog assessed as abscess formation at 20 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585556	Ratio of drug level in thymus to plasma in female Beagle dog at 400 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1264550	Selectivity ratio for antiviral activity against HIV-1 expressing reverse transcriptase K101P mutant to HIV-1 expressing wild-type reverse transcriptase	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1773461	Resistance factor, ratio of EC50 for HIV1 harboring E138K mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID585319	Ratio of drug level in liver to plasma in Beagle dog at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585266	Drug level in Beagle dog skin at non-injected site at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585109	Drug level in Beagle dog muscle at non-injected site at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585338	Ratio of drug level in lymph node popliteal to plasma in Beagle dog at 5 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508820	Antiviral activity against Human immunodeficiency virus 1 group M subtype A1 assessed as days to viral replication breakthrough at 200 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1302313	Antiviral activity against HIV1 3B infected in human MT2 cells measured on day 4 post infection by p24 ELISA method	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID508771	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190A mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585268	Drug level in Beagle dog skin at non-injected site at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561721	Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide to EC
AID1819216	Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1548582	Inhibition of purified recombinant HIV1 reverse transcriptase assessed as remaining enzyme activity at 0.73 nM using template/primer hybrid, digoxigenin-labeled nucleotides and biotin-labeled nucleotides incubated for 1 hr by calorimetric assay relative t	2020	Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9	Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.
AID585059	Cmax in female Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561709	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID698945	Ratio of EC50 for multidrug-resistant HIV-1 RTMDR to EC50 for wild type HIV-1 NL4-3	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID508633	Cytotoxicity against human MT4 cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1466759	Octanol-water partition coefficient, log P of the compound at pH 7.4 after 24 hrs by HPLC method	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID632801	Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID698947	Ratio of EC50 for HIV-1 harboring reverse transcriptase K101E mutant to EC50 for wild type HIV-1 NL4-3	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID1775791	Antiviral activity against HIV-1 strain IIIB infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID585079	Tmax in Beagle dog at 5 mg/kg administered intramuscularly after 176 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585071	Cmax in female Sprague-Dawley rat at 200 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585519	Plasma concentration in male Beagle dog at 200 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508809	Antiviral activity against Human immunodeficiency virus 1 group M subtype H assessed as days to viral replication breakthrough at 10 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585269	Plasma concentration in male Beagle dog at 200 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585530	Plasma concentration in female Beagle dog at 400 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585073	AUC (0 to last) in female Sprague-Dawley rat at 200 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585498	Ratio of drug level in lymph node axillar to plasma in Beagle dog at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1884536	Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by automated patch clamp method	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1552567	Inhibition of Escherichia coli reverse transcriptase RNase H using 18-nucleotide 3'-fluorescein-labeled RNA/5'-dabcyl-labeled DNA hybrid as substrate measured after 1 hr by FRET based assay	2019	Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16	Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID508786	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V108I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID584864	AUC (0 to last) in Sprague-Dawley rat at 20 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508812	Antiviral activity against Human immunodeficiency virus 1 group M subtype AG assessed as days to viral replication breakthrough at 40 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID449196	Antimalarial activity against Plasmodium falciparum W2mef assessed as DNA positive erythrocytes by hoechst 33342-thiazole orange stain based flow cytometry assay	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID1302311	Resistance index, ratio of EC50 for rilpivirine resistant HIV1 harboring reverse transcriptase K101E mutant infected in human TZM-bl cells to EC50 for HIV1 NL4-3 infected in human TZM-bl cells	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID1466755	Fold resistance, ratio of EC50 for rilpivirine-resistant HIV1 NL4-3 reverse transcriptase E138K mutant to EC50 for wild type HIV1 NL4-3 reverse transcriptase	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID1552575	Binding affinity to recombinant wild-type full length HIV1 reverse transcriptase p66/p51 expressed in Escherichia coli by biolayer interferometry	2019	Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16	Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID1289684	Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for R5-tropic HIV1 subtype B BaL infected in human TZM-bl cells	2016	Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5	2,6-Di(arylamino)-3-fluoropyridine Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors.
AID585100	Drug level in Sprague-Dawley rat muscle at injected site at 5 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561702	Antiviral activity against HIV1 expressing RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1171413	Antiviral activity against wild type HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay	2014	ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11	Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1466760	Half life in human liver microsomes at 1 uM pretreated up to 45 mins followed by NADPH addition by LC/MS/MS analysis	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID585322	Drug level in Beagle dog lymph node iliac at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584859	Tmax in Sprague-Dawley rat at 5 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585540	Drug level in female Beagle dog thymus at 400 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508663	Antiviral activity against Human immunodeficiency virus 1 group M subtype H assessed as days to viral replication breakthrough at 200 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1685254	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2	Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.
AID508764	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K101E mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585324	Drug level in Beagle dog lymph node iliac at 5 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585523	Drug level in male Beagle dog spleen at 200 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773450	Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID585330	Ratio of drug level in lymph node iliac to plasma in Beagle dog at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1819214	Antiviral activity against HIV1 L1001 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID585280	Drug level in male Beagle dog thymus at 400 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585544	Ratio of drug level in spleen to plasma in female Beagle dog at 400 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585558	Toxicity in Beagle dog assessed as white deposits at 20 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585325	Drug level in Beagle dog lymph node iliac at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1302314	Antiviral activity against multi-NRTI resistant HIV1 A17 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells measured on day 4 post infection by p24 ELISA method	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID508639	Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585090	Tmax in Beagle dog at 5 mg/kg, sc after 184 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508632	Antiviral activity against Human immunodeficiency virus 1 subtype G isolate RU132 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585264	Drug level in Beagle dog skin at injected site at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585512	Drug level in Beagle dog thymus at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584849	Cmax in Sprague-Dawley rat at 20 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1184480	Aqueous solubility of the compound at pH 2 by HPLC analysis	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID246346	Effective concentration against human immunodeficiency virus type 1 K103N and Y181C mutant strains	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1773844	Half life in human liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1819232	Aqueous solubility of the compound at pH 7.4 by HPLC analysis
AID585334	Drug level in Beagle dog lymph node popliteal at 5 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508660	Antiviral activity against Human immunodeficiency virus 1 group M subtype D assessed as days to viral replication breakthrough at 200 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585033	Tmax in male Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1572530	Inhibition of HIV1 reverse transcriptase p66/p51 using poly(rA)/oligo(dT)16 as template/primer measured after 40 mins by pico-green based spectrofluorometric analysis
AID1775796	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells reduction in cell viability for 5 days by MTT assay to EC50 for antiviral activity against NNRTI-resistant HIV-1 RES056 harboring RT K103N/Y181C mutant infected in human MT4 cells a	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1561694	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID585270	Plasma concentration in male Beagle dog at 400 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585283	Plasma concentration in female Beagle dog at 200 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1882470	Antiviral activity against HIV-1 harboring K103N/Y181C mutant infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID585340	Ratio of drug level in lymph node popliteal to plasma in Beagle dog at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585499	Drug level in Beagle dog lymph node mandibular at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773442	Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
AID585085	Absolute bioavailability in Beagle dog at 5 mg/kg, sc after 176 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1302322	Half life in human liver microsomes at 1 uM by LC-MS analysis	2016	Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8	Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
AID632796	Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID585564	Toxicity in Beagle dog assessed as abscess formation at 20 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID635136	Antiviral activity against Human immunodeficiency virus expressing wild type RT infected in human MT4 cells by p24 antigen assay in the presence of 50% normal human serum	2011	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24	Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID293573	AUC in Beagle dog at 10 mg/kg, po	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1561712	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID585056	Cmax in male Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585521	Drug level in male Beagle dog spleen at 200 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1552569	Inhibition of Avian myeloblastosis virus reverse transcriptase RNase H using 18-nucleotide 3'-fluorescein-labeled RNA/5'-dabcyl-labeled DNA hybrid as substrate measured after 1 hr by FRET based assay	2019	Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16	Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.
AID1773457	Resistance factor, ratio of EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID508758	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585511	Drug level in Beagle dog thymus at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1819234	Aqueous solubility of the compound at pH 2.0 by HPLC analysis
AID1289683	Antiviral activity against R5-tropic HIV1 subtype B BaL infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hrs by luciferase assay	2016	Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5	2,6-Di(arylamino)-3-fluoropyridine Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors.
AID709865	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C/F227C double mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID585107	Drug level in Beagle dog muscle at non-injected site at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561695	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
AID584868	AUC (0 to last) in male Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585273	Drug level in male Beagle dog spleen at 200 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585077	AUC (0 to infinity) in Beagle dog at 1.25 mg/kg, iv after 2 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585102	Drug level in Beagle dog muscle at injected site at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585287	Drug level in female Beagle dog spleen at 200 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585332	Drug level in Beagle dog lymph node popliteal at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584862	Cmax in Sprague-Dawley rat at 20 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561718	Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against virus-indu
AID1775797	Antiviral activity against HIV-1 harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1693808	Antiviral activity against HIV-3B harboring reverse transcriptase Y181C mutant infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 01-15, Volume: 30	Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID1561715	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT F227L + V106A mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID585321	Drug level in Beagle dog lymph node iliac at 5 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508783	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585262	Drug level in Beagle dog skin at injected site at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584851	AUC (0 to infinity) in Sprague-Dawley rat at 1.25 mg/kg, iv after 2 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1572520	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
AID585329	Ratio of drug level in lymph node iliac to plasma in Beagle dog at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508825	Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG029 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508631	Antiviral activity against Human immunodeficiency virus 1 subtype G isolate JV1083 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1636150	Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase L100I/K103N/H221Y mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells	2016	Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15	Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID1561735	Inhibition of CYP3A4 in human liver microsomes using midazolam substrate incubated for 10 mins in presence of NADPH
AID237189	Half life in rat was determined after intravenous administration	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID585538	Drug level in female Beagle dog thymus at 400 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508815	Antiviral activity against Human immunodeficiency virus 1 group M subtype C assessed as days to viral replication breakthrough at 40 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585534	Drug level in female Beagle dog spleen at 400 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1811056	Inhibition of human CYP2C9 using tolbutamide as substrate in presence of NADPH incubated for 15 to 45 mins	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID585263	Drug level in Beagle dog skin at injected site at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1636147	Antiviral activity against NNRTI resistant HIV1 harboring reverse transcriptase V106I/Y181C/G190A/H221Y mutant assessed as inhibition of viral infection in human TZM-bl cells after 48 hrs by luciferase reporter gene assay	2016	Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15	Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID585323	Drug level in Beagle dog lymph node iliac at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585096	Plasma concentration in Beagle dog at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585529	Plasma concentration in female Beagle dog at 200 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585067	AUC (0 to last) in male Sprague-Dawley rat at 200 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID449193	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID585296	Ratio of drug level in spleen to plasma in male Beagle dog at 400 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID767498	Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1561711	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID1882488	Cytotoxicity against human HOS cells assessed as reduction in cell viability measured after 48 hrs	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID673429	Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA	2012	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16	Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants.
AID1561705	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID1773467	Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate in presence of NADPH incubated for 10 mins by LC-MS/MS analysis
AID1811049	Aqueous solubility of compound in PBS at pH 7.4 by HPLC-UV analysis	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID585279	Drug level in male Beagle dog thymus at 200 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585509	Ratio of drug level in spleen to plasma in Beagle dog at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585532	Plasma concentration in female Beagle dog at 400 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1882484	Inhibition of HIV-1 reverse transcriptase K103N mutant assessed as reduction in luciferase reporter activity by single-round assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID585041	Cmax in male Sprague-Dawley rat at 200 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508824	Antiviral activity against Human immunodeficiency virus 1 group M subtype BG assessed as days to viral replication breakthrough at 200 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585064	AUC (0 to last) in female Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID698955	Cytotoxicity against human TZM-bl cells after 4 days by XTT assay	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID1773830	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 infected in human MT4 cells	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID508640	Antiviral activity against Human immunodeficiency virus 1 subtype BG infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773445	Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1775799	Antiviral activity against HIV-1 harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1884498	Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate incubated for 15 to 40 mins in presence of NADPH	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1882468	Antiviral activity against wild type HIV-1 IIIB infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1773439	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1289688	Antiviral activity against HIV1 NL4.3 expressing reverse transcriptase K103N-Y181C mutant infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hrs by luciferase assay	2016	Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5	2,6-Di(arylamino)-3-fluoropyridine Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors.
AID673428	Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA	2012	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16	Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants.
AID585562	Toxicity in Beagle dog assessed as irritation at 20 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585502	Drug level in Beagle dog lymph node mandibular at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508757	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K, M230L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585049	AUC (0 to last) in female Sprague-Dawley rat at 200 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561710	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID585336	Drug level in Beagle dog lymph node popliteal at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508775	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1264539	Antiviral activity against HIV-1 X4 expressing reverse transcriptase K101P mutant infected in human CD4+ T cells for 3 days by FACS analysis	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1561732	Inhibition of CYP2C9 in human liver microsomes using diclofenac substrate incubated for 10 mins in presence of NADPH
AID1633406	Antiviral activity against wild-type HIV1 NL4-3 infected infected in human MT2 cells assessed as reduction in HIV1 extracellular genomic RNA level at 1 uM and measured after 30 hrs post infection by TaqMan probe based RT-PCR analysis	2019	ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4	Synthesis and Evaluation of Bifunctional Aminothiazoles as Antiretrovirals Targeting the HIV-1 Nucleocapsid Protein.
AID508814	Antiviral activity against Human immunodeficiency virus 1 group M subtype BG assessed as days to viral replication breakthrough at 40 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585055	AUC (0 to last) in male Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508831	Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 92BR025 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1750716	Selectivity index, ratio of CC50 for human MT-4 cells to EC50 for HIV-1 infected in MT-4 cells	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID585343	Drug level in Beagle dog lymph node axillar at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585500	Drug level in Beagle dog lymph node mandibular at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585062	Cmax in female Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508806	Antiviral activity against Human immunodeficiency virus 1 group M subtype D assessed as days to viral replication breakthrough at 10 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508796	Ratio of EC50 for HIV1 in presence of 1 mg/ml alpha-1 acid-glycoprotein to EC50 for HIV1 in absence of serum proteins by GFP assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1184475	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as inhibition of viral replication	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1773458	Resistance factor, ratio of EC50 for HIV1 harboring K103N mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID1171412	Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay	2014	ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11	Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1357806	Antiviral activity against wild-type HIV-1 NL4-3 infected in human TZM-bl cells assessed as inhibition of viral replication after 2 days by bright Glo-luciferase reporter gene assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID585103	Drug level in Beagle dog muscle at injected site at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID673430	Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaT371 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI	2012	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16	Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants.
AID709864	Selectivity ratio of EC50 for NNRTI-resistant HIV1 harboring reverse transcriptase Y181I mutant to EC50 for HIV1 expressing wild type reverse transcriptase	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID508637	Antiviral activity against Human immunodeficiency virus 1 subtype D infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508794	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508624	Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 92TH006 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585075	Tmax in female Sprague-Dawley rat at 400 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1636146	Antiviral activity against wild type HIV1 NL4-3	2016	Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15	Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID585032	Cmax in male Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585342	Drug level in Beagle dog lymph node axillar at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID293562	Antiviral activity against HIV1 LAI with RT F227C mutation in MT4 cells by EGFP based replication assay	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID585291	Drug level in female Beagle dog thymus at 200 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID698954	Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for HIV-1NL4-3	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID585306	Ratio of drug level in thymus to plasma in male Beagle dog at 400 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584867	Tmax in male Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID757623	Cytotoxicity against human MT4 cells after 5 days by MTT assay	2013	European journal of medicinal chemistry, Jul, Volume: 65	Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1466761	Half life in human liver S9 fractions at 1 uM measured pretreated up to 45 mins followed by NADPH addition by LC/MS/MS analysis	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID1884497	Inhibition of CYP2C19 in human liver microsomes using s-mephenytoin as substrate incubated for 15 to 40 mins in presence of NADPH	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID766429	Aqueous solubility of the compound at pH 7	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.
AID508829	Antiviral activity against Human immunodeficiency virus 1 subtype B isolate JR-CSF infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1685253	Covalent inhibition of recombinant wild type HIV-1 reverse transcriptase using poly(rA)350/oligo(dT)16 as template/primer preincubated followed by substrate addition measured after 1 hr by pico-green reagent based fluorescence analysis	2021	ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2	Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.
AID585537	Drug level in female Beagle dog thymus at 200 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID293557	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 LAI	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1572518	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID1636148	Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase A98G/K101E/Y181C/G190A mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells	2016	Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15	Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID508790	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585087	Tmax in Beagle dog at 5 mg/kg administered intramuscularly after 184 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585275	Drug level in male Beagle dog spleen at 200 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585097	Plasma concentration in Beagle dog at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585299	Ratio of drug level in thymus to plasma in male Beagle dog at 200 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID635197	Plasma protein binding in human	2011	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24	Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID246482	Effective concentration for the inhibition of wild type human immunodeficiency virus type 1 LAI strain	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1264547	Selectivity index, ratio of IC50 for HIV-1 reverse transcriptase K101P mutant to IC50 for wild-type HIV-1 reverse transcriptase	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID585527	Drug level in male Beagle dog thymus at 200 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1882485	Inhibition of HIV-1 reverse transcriptase E138K mutant assessed as reduction in luciferase reporter activity by single-round assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID508811	Antiviral activity against Human immunodeficiency virus 1 group M subtype AE assessed as days to viral replication breakthrough at 40 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773448	Antiviral activity against wild type HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1561723	Inhibition of HIV1 RT in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID585503	Ratio of drug level in lymph node mandibular to plasma in Beagle dog at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508645	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, G190S mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773454	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y188L mutant infected in human MT4 cells
AID246267	Effective concentration against human immunodeficiency virus type 1 L100I mutant strain	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID508647	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, E138G mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585518	Plasma concentration in male Beagle dog at 400 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1069125	Inhibition of HIV wild-type reverse transcriptase by electrochemiluminescence assay	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID293564	Antiviral activity against HIV1 LAI with RT K103N and Y181C mutation in MT4 cells by EGFP based replication assay	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1773468	Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate in presence of NADPH incubated for 10 mins by LC-MS/MS analysis
AID1561738	Solubility of the compound in pH 7.0 buffer by HPLC analysis
AID585095	Plasma concentration in Sprague-Dawley rat at 20 mg/kg, sc after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID635195	Antiviral activity against Human immunodeficiency virus expressing RT Y181C mutant infected in human MT4 cells by p24 antigen assay in the presence of 50% normal human serum	2011	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24	Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID508773	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181V mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1561733	Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin substrate incubated for 10 mins in presence of NADPH
AID508643	Antiviral activity against Human immunodeficiency virus 1 subtype A1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID293567	Metabolic stability in dog liver microsomes after 15 mins	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID585086	Cmax in Beagle dog at 5 mg/kg administered intramuscularly after 184 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585307	Ratio of drug level in thymus to plasma in male Beagle dog at 200 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1866034	Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured by MTT assay	2022	Bioorganic & medicinal chemistry, 02-15, Volume: 56	Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
AID701092	Antiviral activity against HIV1 infected in human assessed as viral copies at 25 to 150 mg	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
AID1072808	Antiviral activity against HIV1 harboring wild type reverse transcriptase infected in human MT4 cells	2014	Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6	Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
AID508656	Antiviral activity against Human immunodeficiency virus 1 subtype O misolate BCF01 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1561698	Antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID585098	Plasma concentration in Beagle dog at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID698956	Antiviral activity against HIV-1 NL4-3 infected in human TZM-bl cells assessed as inhibition of viral replication after 2 days by luciferase reporter gene based luminescence assay	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID508827	Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG037 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1184482	Lipophilicity, log P of the compound by HPLC analysis	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID585108	Drug level in Beagle dog muscle at non-injected site at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID632798	Cytotoxicity against human MT4 cells infected with HIV1 NL4.3 by MTT assay	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID584857	Absolute bioavailability in Sprague-Dawley rat at 20 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1884499	Inhibition of CYP3A4T in human liver microsomes using testosterone as substrate incubated for 15 to 40 mins in presence of NADPH	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1466762	Half life in human plasma at 10 ug/ml by LC/MS/MS analysis	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID508769	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase H221Y mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585078	Cmax in Beagle dog at 5 mg/kg administered intramuscularly after 176 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1819211	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
AID1882487	Inhibition of HIV-1 reverse transcriptase Y188L mutant assessed as reduction in luciferase reporter activity by single-round assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID508638	Antiviral activity against Human immunodeficiency virus 1 subtype F1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585327	Ratio of drug level in lymph node iliac to plasma in Beagle dog at 5 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508787	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106M mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID698957	Intrinsic clearance in human liver microsomes at 1 uM	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID585092	Plasma concentration in Sprague-Dawley rat at 5 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508650	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID709868	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1775793	Antiviral activity against HIV-1 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID508782	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138Q mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1775794	Cytotoxicity in mock-infected human MT4 assessed as reduction in cell viability incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID508821	Antiviral activity against Human immunodeficiency virus 1 group M subtype AE assessed as days to viral replication breakthrough at 200 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1862576	Inhibition of CYP2D6 (unknown origin)
AID508630	Antiviral activity against Human immunodeficiency virus 1 subtype G isolate G3 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID635128	Cytotoxicity against human MT4 cells	2011	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24	Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID1184476	Cytotoxicity against human MT2 cells assessed as cell viability	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID508658	Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF03 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1811058	Inhibition of human CYP2D6 using dextromethorphan as substrate in presence of NADPH incubated for 15 to 45 mins	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1561699	Antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID449274	Antimalarial activity against Plasmodium falciparum W2mef schizont form by hoechst 33342-thiazole orange stain based flow cytometry assay	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID508768	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1811057	Inhibition of human CYP2C19 using S-mephenytoin as substrate in presence of NADPH incubated for 15 to 45 mins	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID584850	Absolute bioavailability in Sprague-Dawley rat at 5 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID246394	Effective concentration against human immunodeficiency virus type 1 mutated at 227L+106A	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID653704	Antiviral activity against Human immunodeficiency virus 1 harboring reverse transcriptase E138K mutant	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID508644	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1811044	Antiviral activity against HIV1 IIIB infected human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1466753	Inhibition of rilpivirine-resistant HIV1 NL4-3 reverse transcriptase E138K mutant infected in human TZM-b1 cells after 2 days by bright Glo-luciferase reporter gene assay	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID1466752	Inhibition of wild type HIV1 NL4-3 reverse transcriptase infected in human TZM-b1 cells after 2 days by bright Glo-luciferase reporter gene assay	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID1819219	Antiviral activity against HIV-1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1069123	Antiviral activity against HIV harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID449273	Antimalarial activity against Plasmodium falciparum W2mef trophozoite form by hoechst 33342-thiazole orange stain based flow cytometry assay	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID709870	Antiviral activity against HIV1 expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID508654	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508795	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V090I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508807	Antiviral activity against Human immunodeficiency virus 1 group M subtype F1 assessed as days to viral replication breakthrough at 10 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508808	Antiviral activity against Human immunodeficiency virus 1 group M subtype G assessed as days to viral replication breakthrough at 10 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508813	Antiviral activity against Human immunodeficiency virus 1 group M subtype B assessed as days to viral replication breakthrough at 40 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585541	Ratio of drug level in spleen to plasma in female Beagle dog at 200 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585315	Drug level in Beagle dog liver at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585265	Drug level in Beagle dog skin at non-injected site at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID709860	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C/K103N double mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID585344	Drug level in Beagle dog lymph node axillar at 5 mg/kg, sc after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508777	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773843	Inhibition of wild type HIV1 p66/p51 reverse transcriptase using poly(rA) as template, oligo(dT)16 as primer and RNA/DNA as substrate measured after 40 mins by PICOGreen-dye based spectrofluorimetry analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID246393	Effective concentration against human immunodeficiency virus type 1 mutated at 103N+181C	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID585517	Plasma concentration in male Beagle dog at 200 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1184478	Antiviral activity against wild type HIV1 A17 expressing K103N/Y181C mutant infected in human MT2 cells assessed as inhibition of viral replication	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1773473	Inhibition of human ERG expressed in CHO cells by manual patch clamp technique
AID1591874	Antiviral activity against HIV1 NL4-3 harboring Y181C mutant infected in human MT2 cells measured 48 hrs post-infection by MTT assay	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16	Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase.
AID508792	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1819212	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 IIIB infected in human MT4 cells
AID508801	Antiviral activity against Human immunodeficiency virus 1 group M subtype AE assessed as days to viral replication breakthrough at 10 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1561730	Inhibition of HIV1 RT K103N/Y181C mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID1561701	Antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID585093	Plasma concentration in Sprague-Dawley rat at 20 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1882486	Inhibition of HIV-1 reverse transcriptase Y181C mutant assessed as reduction in luciferase reporter activity by single-round assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID585295	Ratio of drug level in spleen to plasma in male Beagle dog at 200 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585316	Drug level in Beagle dog liver at 5 mg/kg administered intramuscularly after 6 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID653700	Aqueous solubility of the compound at pH 7.4 by HPLC/UV analysis	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID246269	Effective concentration against human immunodeficiency virus type 1 Y188L mutant strain	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID585310	Plasma concentration in Beagle dog at 5 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1862574	Inhibition of CYP2C9 (unknown origin)
AID1773463	Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into protein incubated for 1 hrs by ELISA
AID1882469	Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID293555	Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID508798	Ratio of EC50 for HIV1 in presence of 50% human serum to EC50 for HIV1 in absence of serum proteins by GFP assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585282	Plasma concentration in female Beagle dog at 400 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID698952	Aqueous solubility of the compound at pH 7.4 after 4 hrs	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID653703	Antiviral activity against Human immunodeficiency virus 1 harboring reverse transcriptase K101E mutant	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID508784	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138G mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508767	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID392513	Antiviral activity against HIV1	2009	Bioorganic & 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.
AID1636927	Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against viral infection by MTT method	2016	Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20	Computer-aided discovery of anti-HIV agents.
AID1882471	Cytotoxicity against human MT2 cells assessed as cell viability by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1561722	Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonam
AID1072805	Antiviral activity against HIV1 harboring reverse transcriptase K101N/Y181C double mutant infected in human MT4 cells	2014	Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6	Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
AID585281	Plasma concentration in female Beagle dog at 200 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID584852	Cmax in Sprague-Dawley rat at 5 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1264543	Cytotoxicity against human CD4-positive T cells	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID585058	AUC (0 to last) in male Sprague-Dawley rat at 400 mg/kg administered intramuscularly after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561726	Inhibition of HIV1 RT Y181C mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID293558	Antiviral activity against HIV1 LAI with RT L100I mutation in MT4 cells by EGFP based replication assay	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID584854	AUC (0 to last) in Sprague-Dawley rat at 5 mg/kg administered intramuscularly after 56 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID293563	Antiviral activity against HIV1 LAI with RT L100I and K103N mutation in MT4 cells by EGFP based replication assay	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID585294	Ratio of drug level in spleen to plasma in male Beagle dog at 400 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID246307	Effective concentration against rhuman immunodeficiency virus type 1 wild type mutant strain	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID585559	Toxicity in Beagle dog assessed as white deposits at 20 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585561	Toxicity in Beagle dog assessed as inflammatory signs at 20 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585550	Ratio of drug level in spleen to plasma in female Beagle dog at 400 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585066	Tmax in male Sprague-Dawley rat at 200 mg/kg, sc after 85 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID653698	Cytotoxicity against human TZM-bl cells	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID293570	AUC in Wistar rat at 10 mg/kg, po	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1264541	Antiviral activity against HIV-1 X4 expressing reverse transcriptase Y181C mutant infected in human CD4+ T cells for 3 days by FACS analysis	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID1466763	Cytotoxicity against human TZM-bl cells infected with HIV1 NL4-3	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID1561714	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT F227L + V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID585089	Cmax in Beagle dog at 5 mg/kg, sc after 184 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585035	Cmax in female Sprague-Dawley rat at 200 mg/kg administered intramuscularly after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1357808	Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for wild-type HIV-1 NL4-3 infected in human TZM-bl cells	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID508800	Inhibition of HIV1 Reverse transcriptase by primer extension-based scintillation assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585522	Drug level in male Beagle dog spleen at 400 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773452	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring K103N mutant infected in human MT4 cells
AID508762	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E, K103N mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID246392	Effective concentration against human immunodeficiency virus type 1 mutated at 100I+103N	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1773443	Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV-1 3B infected in MT4 cells
AID246351	Effective concentration against human immunodeficiency virus type 1 mutated at 188L	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID698946	Ratio of EC50 for HIV-1 harboring reverse transcriptase E138K mutant to EC50 for wild type HIV-1 NL4-3	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID1466758	Aqueous solubility of the compound in 0.01 M HCl at pH 2 after 4 hrs by HPLC-UV analysis	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID585050	Cmax in female Sprague-Dawley rat at 400 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID246350	Effective concentration against human immunodeficiency virus type 1 mutated at 181C	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID508756	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID585563	Toxicity in Beagle dog assessed as irritation at 20 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585536	Drug level in female Beagle dog spleen at 400 mg/kg administered intramuscularly after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID293565	Antiviral activity against HIV1 LAI with RT F227C and V106A mutation in MT4 cells by EGFP based replication assay	2007	European journal of medicinal chemistry, May, Volume: 42, Issue:5	Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID585292	Drug level in female Beagle dog thymus at 400 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585084	AUC (0 to last) in Beagle dog at 5 mg/kg, sc after 176 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561728	Inhibition of HIV1 RT E138K mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID585080	AUC (0 to last) in Beagle dog at 5 mg/kg administered intramuscularly after 176 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID709867	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID585554	Ratio of drug level in thymus to plasma in female Beagle dog at 400 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1264546	Inhibition of HIV-1 reverse transcriptase K101P mutant by fluorescence assay	2015	ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10	Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
AID585297	Ratio of drug level in thymus to plasma in male Beagle dog at 200 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1773828	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1561731	Inhibition of CYP1A2 in human liver microsomes using phenacetin substrate incubated for 10 mins in presence of NADPH
AID508627	Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR019 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508781	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138R mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1819210	Antiviral activity against HIV-1 IIIB harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay
AID585043	AUC (0 to last) in male Sprague-Dawley rat at 200 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID508805	Antiviral activity against Human immunodeficiency virus 1 group M subtype C assessed as days to viral replication breakthrough at 10 nM by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1819209	Antiviral activity against HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay
AID585555	Ratio of drug level in thymus to plasma in female Beagle dog at 200 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1535521	Solubility of the compound at pH 7.4	2019	Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3	Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
AID709869	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID585515	Ratio of drug level in thymus to plasma in Beagle dog at 5 mg/kg, sc after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID585045	Tmax in male Sprague-Dawley rat at 400 mg/kg, sc after 29 days	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1811046	Selectivity index, ratio of CC50 for mock infected human MT4 cells to IC50 for HIV1 IIIB infected human MT4 cells	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID585271	Plasma concentration in male Beagle dog at 200 mg/kg administered intramuscularly after 3 months	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1561704	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID585525	Drug level in male Beagle dog thymus at 200 mg/kg, sc after 1 month	2010	Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5	Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
AID1802585	RT Assay from Article 10.1016/j.bioorg.2017.01.006: \\Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.\\	2017	Bioorganic chemistry, 02, Volume: 70	Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1745854	NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS	2023	Disease models & mechanisms, 03-01, Volume: 16, Issue:3	In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745855	NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay	2023	Disease models & mechanisms, 03-01, Volume: 16, Issue:3	In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	28 (5.04)	29.6817
2010's	320 (57.55)	24.3611
2020's	208 (37.41)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	93 (16.03%)	5.53%
Reviews	92 (15.86%)	6.00%
Case Studies	21 (3.62%)	4.05%
Observational	25 (4.31%)	0.25%
Other	349 (60.17%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (91)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Rilpivirine Long Acting Single Patient Requests [NCT03847376]		0 participants	Expanded Access		Approved for marketing
An Open-label, Roll-over Study With Rilpivirine in Combination With a Background Regimen Containing Other Antiretrovirals (ARVs) in Human Immunodeficiency Virus Type 1 (HIV-1) Infected Subjects Who Participated in Rilpivirine Pediatric Studies [NCT02494986]	Phase 2	48 participants (Actual)	Interventional	2015-07-31	Active, not recruiting
Phase I/II Study of the Safety, Acceptability, Tolerability, and Pharmacokinetics of Oral and Long-Acting Injectable Cabotegravir and Long-Acting Injectable Rilpivirine in Virologically Suppressed HIV-Infected Children and Adolescents [NCT03497676]	Phase 1/Phase 2	155 participants (Anticipated)	Interventional	2019-03-19	Recruiting
Neurocognitive Function Improvement After Switching From Efavirenz to Rilpivirine in HIV-infected Adults: A Randomized Control Trial [NCT03567304]	Phase 4	28 participants (Anticipated)	Interventional	2018-07-06	Enrolling by invitation
A Phase I, Open-label, Randomized, Crossover Trial in Healthy Subjects to Investigate the Pharmacokinetic Interaction Between TMC278 25 mg q.d. and Raltegravir 400 mg b.i.d. [NCT01288755]	Phase 1	24 participants (Actual)	Interventional	2011-02-28	Completed
A Phase I, 2-panel, Open-label, Randomized, Cross-over Trial in Healthy Subjects to Investigate the Pharmacokinetic Interaction Between TMC435 and Antiretroviral Agents, TMC278 and Tenofovir Disoproxil Fumarate (TDF), at Steady State [NCT01205139]	Phase 1	48 participants (Actual)	Interventional	2010-11-30	Completed
Efficacy of Rilpivirine-based Regimens as Switch Therapy From Nevirapine-based Regimens in HIV-infected Patients With Complete Virological Suppression: A Randomized Controlled Trial [NCT03664440]		106 participants (Actual)	Interventional	2016-12-01	Completed
A Phase I, Open Label, Randomized, 2-Panel, 2-Way Crossover Trial to Investigate the Pharmacokinetic Interaction Between Etravirine or TMC278 and Telaprevir at Steady-State in Healthy Subjects. [NCT01336829]	Phase 1	33 participants (Actual)	Interventional	2011-03-31	Completed
"Switch From Nevirapine-based Regimen to Once a Day Rilpivirine/Emtricitabine/Tenofovir in Virologically-suppressed HIV-infected Rwandans (Near-Rwanda)" [NCT02104700]	Phase 2/Phase 3	150 participants (Actual)	Interventional	2014-04-30	Completed
A Phase IIIb, Randomized, Multicenter, Parallel-group, Non-inferiority, Open-label Study Evaluating the Efficacy, Safety, and Tolerability of Long-acting Cabotegravir Plus Long-acting Rilpivirine Administered Every 8 Weeks or Every 4 Weeks in HIV-1-infect [NCT03299049]	Phase 3	1,049 participants (Actual)	Interventional	2017-10-27	Active, not recruiting
Switching Tenofovir/Emtricitabine/Efavirenz to Tenofovir/Emtricitabine/Rilpivirine Versus Continuing Tenofovir/Emtricitabine/Efavirenz in HIV1-infected Patients With Complete Virological Suppression [NCT03251690]		246 participants (Actual)	Interventional	2016-10-27	Completed
Sub-study to the A2M Study to Evaluate the Pharmacokinetics, Tolerability and Efficacy of Cabotegravir and Rilpivirine Long-Acting Injections Following Intramuscular Administration in the Vastus Lateralis Muscle (Thigh) in HIV-infected Adult Participants [NCT05896761]	Phase 3	118 participants (Actual)	Interventional	2021-10-28	Completed
Effect of SwitChing AtriPla to Eviplera on Neurocognitive and Emotional Functioning, ESCAPE Study [NCT02308332]	Phase 4	58 participants (Actual)	Interventional	2015-02-28	Completed
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289]		1,578 participants (Actual)	Observational	2003-06-09	Completed
A Phase 1, Open-Label Study to Evaluate the Pharmacokinetics and Tolerability of Cabotegravir and Rilpivirine Long-Acting Injections Following Intramuscular Administration in the Vastus Lateralis Muscle of Healthy Adult Participants [NCT04371380]	Phase 1	15 participants (Actual)	Interventional	2020-09-16	Completed
A Phase 3b Randomised, Multicentre, Open-label Study Evaluating the Effectiveness of Switching to Two-monthly Long-acting Injectable Cabotegravir and Rilpivirine From First-line Oral Antiretroviral Therapy in HIV-1 Positive Virologically Suppressed Adults [NCT05546242]	Phase 3	540 participants (Anticipated)	Interventional	2022-12-08	Recruiting
'COMBINE-2': Real-world Evidence for Effectiveness of Two Drug Regimen, Antiretroviral Therapy With Integrase Inhibitors Plus a Reverse Transcriptase Inhibitor [NCT04019873]		1 participants (Actual)	Observational	2019-11-18	Completed
A Phase I, Open-label Trial to Explore the Pharmacokinetics, Safety and Tolerability of TMC278 25 mg Once Daily Following a 2-week Period Receiving Efavirenz, in Healthy Male and Female Subjects [NCT01268839]	Phase 1	20 participants (Actual)	Interventional	2010-01-31	Completed
Clinical Effectiveness-Implementation Hybrid Type 2 Study on Home-Delivered Cabenuva for People Living With HIV Who Are Not Retained in Care [NCT06062979]		180 participants (Anticipated)	Observational [Patient Registry]	2023-11-01	Not yet recruiting
A Phase IV, Open-label, Multi Centre Pilot Study to Assess Changes in Cerebral Function Parameters in Patients Without Perceived Central Nervous System (CNS) Symptoms When Switched From a Fixed Dose Combination of Tenofovir/Emtricitabine/Efavirenz (Atripl [NCT02529059]	Phase 4	40 participants (Anticipated)	Interventional	2015-11-30	Completed
Phase I, Double Blind, Randomized, Placebo-controlled Trial to Examine the Safety, Tolerability and Plasma Pharmacokinetics of Multiple (Monthly) Intramuscular and Subcutaneous Doses of TMC278LA. [NCT00741741]	Phase 1	20 participants (Actual)	Interventional	2008-07-31	Terminated(stopped due to Strategic decision)
Cabotegravir-Rilpivirine Long Acting (CAB-RPV LA) Implementation Strategies Among High-Risk Populations [NCT04973254]		25 participants (Actual)	Interventional	2022-02-23	Completed
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 3	100 participants (Actual)	Interventional	2014-07-31	Completed
A Phase IV 48 Week, Open Label, Pilot Study of Darunavir Boosted by Cobicistat in Combination With Rilpivirine to Treat HIV+ Naïve Subjects (PREZENT) [NCT02404233]	Phase 4	30 participants (Anticipated)	Interventional	2015-03-31	Not yet recruiting
A Phase III Study to Evaluate Long-Acting Antiretroviral Therapy in Non-Adherent HIV-Infected Individuals [NCT03635788]	Phase 3	350 participants (Anticipated)	Interventional	2019-03-28	Recruiting
A Phase IIb Randomized, Partially Blinded, Dose-Finding Trial of TMC278 in Antiretroviral-Naive HIV-1 Infected Subjects [NCT00110305]	Phase 2	368 participants (Actual)	Interventional	2005-06-30	Completed
A Phase I, Double-blind, Double-dummy, Randomized, Placebo Controlled and Active Controlled Trial to Evaluate the Effect of TMC278 25 mg Daily at Steady-state and the Effect of Efavirenz (EFV) 600 mg Daily at Steady-state on the QT/QTc Interval, in 2 Rand [NCT00744809]	Phase 1	120 participants (Actual)	Interventional	2008-08-31	Completed
PrEP TMC278LA: Safety, Tolerability and Pharmacokinetics of TMC278LA in HIV Negative Volunteers [NCT01049932]	Phase 1/Phase 2	0 participants (Actual)	Interventional	2010-03-31	Terminated(stopped due to Trial closed due to additional safety information.)
Study in Healthy Volunteers to Examine the Safety, Tolerability and Plasma Pharmacokinetics of One Intramuscular (IM) Injection of a Novel TMC278 LA Formulation at 2 Different Doses (Open Label), Followed by a Placebo-controlled Part of Multiple IM Inject [NCT01031589]	Phase 1	19 participants (Actual)	Interventional	2010-01-31	Completed
An Open-Label Study to Evaluate the Pharmacokinetics of Rilpivirine/Tenofovir/Emtricitabine After a Single-Oral Administration of a Rilpivirine/Tenofovir Disoproxil Fumarate/Emtricitabine Fixed-Dose Combination Tablet in Healthy Japanese Adult Male Subjec [NCT02530060]	Phase 4	8 participants (Actual)	Interventional	2015-08-31	Completed
An Open Label, Comparative, Randomized , Phase IV Pilot Study to Evaluate the Efficacy and Safety of a Rilpivarine-based Antiretroviral Tratment Regimen in HIV- Infected Patients With Liver Metabolic Disease Who Maintain Udetectable HIV Viral Load [NCT05898841]	Phase 4	75 participants (Anticipated)	Interventional	2023-05-26	Recruiting
An Amendment to the FLAIR Study to Evaluate the Pharmacokinetics, Safety, Tolerability, Maintenance of Virological Suppression and Patient Reported Outcomes for Participants Receiving Cabotegravir (CAB 200 mg/mL) and Rilpivirine (300 mg/mL) Long-Acting In [NCT05896748]	Phase 3	93 participants (Actual)	Interventional	2022-11-08	Completed
A Phase III, Randomized, Double-blind Trial of TMC278 25mg q.d. Versus Efavirenz 600mg q.d. in Combination With a Background Regimen Containing 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors in Antiretroviral-naive HIV-1 Infected Subjects. [NCT00543725]	Phase 3	680 participants (Actual)	Interventional	2008-06-30	Completed
A Phase III, Randomized, Double-blind Trial of TMC278 25 mg q.d. Versus Efavirenz 600mg q.d. in Combination With a Fixed Background Regimen Consisting of Tenofovir Disoproxil Fumarate and Emtricitabine in Antiretroviral-naive HIV-1 Infected Subjects. [NCT00540449]	Phase 3	694 participants (Actual)	Interventional	2008-05-31	Completed
Pharmacokinetics, Safety and Tolerability of TMC278 in Subjects With Mildly or Moderately Impaired Hepatic Function [NCT00736905]	Phase 1	32 participants (Actual)	Interventional	2008-06-30	Completed
A Single Arm, Open Label Study to Assess the Pharmacokinetics of Darunavir and Ritonavir, Darunavir and Cobicistat, Etravirine, and Rilpivirine in HIV-1 Infected Pregnant Women [NCT00855335]	Phase 3	77 participants (Actual)	Interventional	2009-04-09	Completed
A Phase I, Open-label Drug-drug Interaction Trial to Investigate the Effect of TMC278 25 mg q.d. on the Steady State Pharmacokinetics of Ethinylestradiol and Norethindrone, in Healthy Women [NCT00739622]	Phase 1	18 participants (Actual)	Interventional	2008-07-31	Completed
A Phase IIIb, Multi-center, Non-randomized, Parallel-group, Open-label, Hybrid Type I Study Evaluating the Efficacy, Safety, Implementation Effectiveness, and Patient-reported Outcomes of Oral Dolutegravir/Lamivudine Once-daily as a First-line Regimen Fol [NCT05917509]	Phase 3	180 participants (Anticipated)	Interventional	2023-07-06	Recruiting
A Phase I, Open Label, Randomized, 4-way Crossover Trial to Evaluate the Pharmacokinetics of TMC278 25mg and 50mg in the Presence of Omeprazole 20mg q.d., in Healthy Subjects [NCT01001247]	Phase 1	18 participants (Actual)	Interventional	2010-01-31	Completed
A Phase I, Open-label, Single-sequence Drug-drug Interaction Trial in Subjects on Stable Methadone Maintenance Therapy, to Investigate the Potential Interaction Between TMC278 25 mg q.d. and Methadone, at Steady-state. [NCT00744770]	Phase 1	13 participants (Actual)	Interventional	2008-10-31	Completed
A Phase 1, Open-label, Randomized, 2-panel, 4-way Crossover Study in Healthy Adult Subjects to Assess the Rilpivirine Relative Bioavailability Compared to the 25-mg Oral Tablet and the Food Effect Following Single Dose Administration of Oral Pediatric For [NCT02561936]	Phase 1	32 participants (Actual)	Interventional	2015-10-31	Completed
A Phase I, Open-label, Randomized, Crossover Trial in Healthy Adults to Compare the Oral Bioavailability of TMC278 From Three Concept Pediatric Formulations (Solution, Suspension, Granules) With That From the Adult Phase III Tablet Formulation. [NCT00812292]	Phase 1	36 participants (Actual)	Interventional	2009-01-31	Completed
A Phase 1 Open-Label, Randomized, Parallel-Group Study in Healthy Subjects to Investigate the Effect of Different Storage Conditions of a Long-Acting Nanosuspension of Rilpivirine on the Single-Dose Plasma Pharmacokinetics of Rilpivirine After Intramuscul [NCT02547870]	Phase 1	61 participants (Actual)	Interventional	2015-08-14	Completed
An Open-Label, Multi-Centre, Randomised, Switch Study to Evaluate the Virological Efficacy Over 96 Weeks Of 2-Drug Therapy With DTG/RPV FDC in Antiretroviral Treatment-Experienced HIV-1 Infected Subjects Virologically Suppressed With NNRTIs Resistance Mut [NCT05349838]	Phase 3	140 participants (Actual)	Interventional	2018-11-05	Completed
Co-benefits of Co-delivery of Long-acting Antiretrovirals and Contraceptives [NCT05044962]		700 participants (Anticipated)	Interventional	2021-11-26	Recruiting
A Phase I/II, Open-Label Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Antiviral Activity of Rilpivirine in Antiretroviral Naive HIV-1 Infected Children, < 12 Years of Age [NCT01975012]	Phase 1/Phase 2	0 participants (Actual)	Interventional	2014-09-30	Withdrawn
Implementation of Out-of-HOspital Administration of the Long-Acting Combination Cabotegravir+Rilpivirine as an Optional Therapy in HIV-Infected Patients From Spain: Acceptability, Appropriateness, Feasibility and Satisfaction: The HOLA Study [NCT06185452]	Phase 4	110 participants (Anticipated)	Interventional	2023-09-26	Recruiting
Prospective Evaluation of Neurologic and Psychiatric Adverse Events of Rilpivirine, Elvitegravir, or Dolutegravir in a Real Life Setting [NCT02882230]		1 participants (Actual)	Observational	2018-11-19	Terminated(stopped due to Unfavourable opinion of ethical comittee for Amendment Nr 3)
Multicenter, National, Prospective, Open Label, Randomized, Pilot, Proof-of-concept Study on the Use of Rilpivirine Plus Darunavir/Cobicistat as Substitutive Agents in Virologic Suppressed Patients [NCT04064632]	Phase 4	1,609 participants (Actual)	Interventional	2017-02-01	Active, not recruiting
Long-Acting Treatment in Adolescents (LATA): A Randomised Open-label 2-arm 96 Week Trial in Virologically Suppressed HIV-1-positive Adolescents Aged 12-19 Years of Age in Sub-Saharan Africa [NCT05154747]	Phase 3	460 participants (Anticipated)	Interventional	2023-06-22	Recruiting
A Phase II, Open Label, Single Arm Trial to Evaluate the Pharmacokinetics,Safety, Tolerability, and Antiviral Activity of Rilpivirine (TMC278) in Antiretroviral Naive HIV-1 Infected Adolescents and Children Aged >= 6 to <18 Years [NCT00799864]	Phase 2	54 participants (Actual)	Interventional	2011-01-07	Completed
Phase 1/2 Study of Switching to Fixed Dose Combination Dolutegravir/Rilpivirine Among Virologically Suppressed Children, 6 to Less Than 12 Years of Age, Living With HIV-1 [NCT05674656]	Phase 1/Phase 2	20 participants (Anticipated)	Interventional	2023-06-01	Not yet recruiting
Characterization of Acute and Recent HIV-1 Infections in Zurich: a Long-term Observational Study [NCT00537966]		2,017 participants (Anticipated)	Interventional	2002-01-31	Recruiting
Contribution of the Integrase Inhibitor Dolutegravir to Obesity and Cardiovascular Disease in Persons Living With HIV [NCT04340388]	Phase 4	10 participants (Actual)	Interventional	2020-09-17	Completed
A Phase I Pharmacokinetic Study to Assess the Cerebrospinal-fluid (CSF) Exposure of Rilpivirine in HIV-infected Subjects Switching From TDF/FTC/Nevirapine to TDF/FTC/Rilpivirine [NCT01562886]	Phase 1	14 participants (Actual)	Interventional	2012-03-31	Completed
An Open-label Trial With TMC278 25 mg q.d. in Combination With a Background Regimen Containing 2 N(t)RTI's in HIV-1 Infected Subjects Who Participated in TMC278 Clinical Trials and Were Still Benefitting From Treatment With TMC278 [NCT01266902]	Phase 3	482 participants (Actual)	Interventional	2011-02-28	Completed
A Phase I, Open Label, Randomized, Crossover Trial in Healthy Subjects to Investigate the Effect of Steady-state TMC278 on the Pharmacokinetics of a Single Dose of Digoxin [NCT01519128]	Phase 1	22 participants (Actual)	Interventional	2012-01-31	Completed
A Pharmacokinetic Evaluation of Etonogestrel Implant in HIV-infected Women on Darunavir Versus Ripilvirine-based Antiretroviral Therapy [NCT03589040]	Phase 2	60 participants (Anticipated)	Interventional	2018-09-25	Recruiting
A Pharmacokinetic Evaluation of the Exposure and Distribution of TMC278LA for Use as Pre-exposure Prophylaxis, in Plasma and Genital Tract / Rectal Compartments, Following a Single Intramuscular Dose at Different Doses in HIV-negative Healthy Volunteers. [NCT01275443]	Phase 1	66 participants (Actual)	Interventional	2011-01-31	Completed
A Phase III, Randomized, Multicenter, Parallel-group, Open-Label Study Evaluating the Efficacy, Safety, and Tolerability of Long-Acting Intramuscular Cabotegravir and Rilpivirine for Maintenance of Virologic Suppression Following Switch From an Integrase [NCT02938520]	Phase 3	631 participants (Actual)	Interventional	2016-10-27	Active, not recruiting
Phase 1 Open Label Safety, Acceptability, Pharmacokinetic and ex Vivo Pharmacodynamic Study of TMC278 Long Acting (LA) Administered Intramuscularly to HIV-1 Seronegative Individuals [NCT01656018]	Phase 1	4 participants (Actual)	Interventional	2012-11-30	Completed
What is the Impact of Current HIV Medication Regimens on Endothelial Dysfunction? [NCT03782142]		22 participants (Actual)	Observational	2018-11-01	Completed
Open-Label Study With Rilpivirine in Treatment-naïve Indian Subjects With HIV-1 Infection to Determine Safety and Efficacy [NCT03563742]	Phase 3	58 participants (Actual)	Interventional	2018-09-24	Terminated(stopped due to High SF rate (less treatment-naïve subjects & subjects with viral load <100000). Reevaluation in scientific position in India after internal discussion.)
A Pilot Study to Assess the Feasibility of Switching, Individuals Receiving Atripla With Continuing Central Nervous System (CNS) Toxicity, to a Fixed Dose Combination of Tenofovir/Emtricitabine/Rilpivirine [NCT01701882]	Phase 3	40 participants (Actual)	Interventional	2012-09-30	Completed
Safety, Tolerability, and Adherence to Co-formulated Emtricitabine-rilpivirine-tenofovir Used as HIV Nonoccupational Post Exposure Prophylaxis in Men Who Have Sex With Men (EPEP) [NCT01715636]	Phase 4	100 participants (Actual)	Interventional	2012-12-31	Completed
A Phase I, Open-Label Study in Healthy Subjects to Explore the Potential for a Pharmacokinetic Interaction Between Steady-State Rilpivirine and a Single Dose Of Metformin [NCT01719614]	Phase 1	20 participants (Actual)	Interventional	2012-10-31	Completed
A Phase IV, Open-label Single-arm Study Investigating the Pharmacokinetics and Pharmacodynamics of the Antiretroviral Combination of Rilpivirine and Ritonavirboosted Darunavir in Therapy-naive HIV-1 Infected Patients. [NCT01736761]	Phase 4	36 participants (Actual)	Interventional	2012-12-31	Completed
Strategic Study of Dual-therapy With Darunavir/Ritonavir and Rilpivirine QD Versus Triple-therapy in Patients With Suppressed Viral Load: Virological Efficacy and Evaluation of Non-HIV Related Morbidity. [NCT01792570]	Phase 3	37 participants (Actual)	Interventional	2014-09-30	Completed
An Open-label, Single-dose Study to Investigate the Pharmacokinetics and Safety of TMC278 After Oral Administration of TMC278 25 mg Tablet Under Fed Condition in Healthy Japanese Adult Male Subjects [NCT01804244]	Phase 4	8 participants (Actual)	Interventional	2013-03-31	Completed
A Randomized Controlled Trial Comparing Efavirenz With Rilpivirine on Changes in Endothelial Function, Inflammatory Markers, and Oxidative Stress in HIV-uninfected Healthy Volunteers [NCT01585038]	Phase 4	40 participants (Actual)	Interventional	2012-07-31	Completed
A Phase I, Open-label, Single-dose Study to Investigate the Pharmacokinetics, Safety and Tolerability of Dolutegravir + Rilpivirine (JULUCA™) 50 mg/25 mg Tablets in Healthy Participants of Japanese Descent [NCT03984838]	Phase 1	16 participants (Actual)	Interventional	2019-06-17	Completed
Evaluation of Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide (ECF/TAF) Switch Followed by Ledipasvir-Sofosbuvir HCV Therapy in HIV-HCV Co-Infection: A CIHR Canadian HIV Trials Network-Gilead Pilot Trial Proposal [NCT02660905]	Phase 3	25 participants (Actual)	Interventional	2016-04-30	Completed
A Phase IIb Study Evaluating a Long-Acting Intramuscular Regimen of GSK1265744 Plus TMC278 For The Maintenance of Virologic Suppression Following an Induction of Virologic Suppression on an Oral Regimen of GSK1265744 Plus Abacavir/Lamivudine in HIV-1 Infe [NCT02120352]	Phase 2	309 participants (Actual)	Interventional	2014-04-28	Completed
A Randomized, Open Label Study to Investigate the Safety, Tolerability and Pharmacokinetics of Repeat Dose Administration of Long-Acting GSK1265744 and Long-Acting TMC278 Intramuscular and Subcutaneous Injections in Healthy Adult Subjects [NCT01593046]	Phase 1	43 participants (Actual)	Interventional	2012-05-31	Completed
A Phase I, Open-Label Study in Healthy Subjects, to Explore the Pharmacokinetics of Different Dosing Regimens of Rilpivirine in Combination With Rifabutin, at Steady-State [NCT01615614]	Phase 1	20 participants (Actual)	Interventional	2012-04-30	Completed
A Phase III, Randomized, Multicenter, Parallel-group, Non-inferiority, Open-label Study Evaluating the Efficacy, Safety, and Tolerability of Switching to Long-acting Cabotegravir Plus Long-acting Rilpivirine From Current INI- NNRTI-, or PI-based Antiretro [NCT02951052]	Phase 3	618 participants (Actual)	Interventional	2016-10-28	Active, not recruiting
HPTN 076 - Phase II Safety and Acceptability of an Investigational Injectable Product, TMC278 LA, for Pre-Exposure Prophylaxis (PrEP) [NCT02165202]	Phase 2	136 participants (Actual)	Interventional	2014-10-31	Completed
Population Pharmacokinetics of Antiretroviral in Children [NCT03194165]		65 participants (Actual)	Observational	2017-06-16	Completed
Integrating Long-Acting Injectable Treatment to Improve Medication Adherence Among Persons Living With HIV and Opioid Use Disorder [NCT05991622]	Early Phase 1	40 participants (Anticipated)	Interventional	2022-04-01	Recruiting
Treatment Switch From Efavirenz to Rilpivirine in Virologically-suppressed HIV-infected Thai Adolescents [NCT03033368]	Phase 2/Phase 3	100 participants (Actual)	Interventional	2015-07-31	Enrolling by invitation
A Phase 3b, Randomized, Open-label Clinical Study to Demonstrate Non-inferiority in Virologic Response Rates of HIV-1 RNA Suppression <400 Copies/mL of TDF/FTC/RPV Versus TDF/FTC/EFV in First-line Antiretroviral NNRTI-based Suppressed Patients. Switching [NCT01709084]	Phase 3	426 participants (Actual)	Interventional	2013-10-02	Completed
Cohort Study of HIV-positive People, Treated With Long Acting Antiretroviral Therapy (SCohoLART) [NCT05663580]		1,500 participants (Anticipated)	Observational	2022-07-17	Recruiting
A Phase IIIb, Randomized, Multicenter, Active-controlled, Parallel-group, Non-inferiority, Open-label Study Evaluating the Efficacy, Safety, and Tolerability of Switching to Long-acting Cabotegravir Plus Long-acting Rilpivirine Administered Every Two Mont [NCT04542070]	Phase 3	687 participants (Actual)	Interventional	2020-11-09	Completed
Cost-effectiveness of Different Antiretroviral Treatment in Patients HIV Naive. Randomized Clinical, Not Masked, Trial Comparing DRVr3TC, ABC3TC (Kivexa) RPV, or EVG COBI FTC TDF (Stribild) for 48 Weeks [NCT02470650]	Phase 4	150 participants (Anticipated)	Interventional	2015-06-30	Recruiting
A Prospective, Single-Arm, Open-Label Study to Evaluate the Effect of Fixed-Dose Emtricitabine/Rilpivirine/Tenofovir Disoproxil Fumarate on T-Cell Activation, Absolute CD4+ T-Cell Count, Inflammatory Biomarkers and Viral Reservoir in Treatment-Naïve HIV-1 [NCT01777997]	Phase 4	38 participants (Actual)	Interventional	2013-04-25	Completed
A Phase 2, Open-label, Single-arm, Multicenter Study to Evaluate the Pharmacokinetics, Safety, Tolerability, and Efficacy of Switching to RPV Plus Other ARVs in HIV-1-infected Children (Aged 2 to <12 Years) Who Are Virologically Suppressed [NCT04012931]	Phase 2	26 participants (Actual)	Interventional	2019-07-18	Completed
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 3	224 participants (Actual)	Interventional	2014-12-31	Completed
A Phase 1, Open-label, Randomized, Parallel-group Study in Healthy Subjects to Investigate the Effect of Different Particle Sizes on the Single-dose Pharmacokinetics of Rilpivirine After Intramuscular Injection of a Long-acting Nanosuspension [NCT03127189]	Phase 1	110 participants (Actual)	Interventional	2017-04-20	Completed
A Pharmacokinetic Evaluation of Levonorgestrel Implant in HIV-Infected Women on Darunavir Versus Rilpivirine-based Antiretroviral Therapy [NCT03589027]	Phase 2	60 participants (Anticipated)	Interventional	2018-08-07	Recruiting
Decrease of Neuropsychiatric and Neurocognitive Side Effects Prevalence [NCT02447016]	Phase 4	25 participants (Actual)	Interventional	2015-05-31	Terminated(stopped due to no more participants taking atripla)
A Phase IIb, Dose Ranging Study of Oral GSK1265744 in Combination With Nucleoside Reverse Transcriptase Inhibitors for Induction of Human Immunodeficiency Virus -1 (HIV-1) Virologic Suppression Followed by an Evaluation of Maintenance of Virologic Suppres [NCT01641809]	Phase 2	244 participants (Actual)	Interventional	2012-08-06	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
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: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: 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]	Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	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]	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 (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	Plasma Concentration for Contraceptives
NCT00042289 (26) [back to overview]	Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]	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]	PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs
NCT00110305 (14) [back to overview]	Change From Baseline in CD4+ Cell Count (Absolute) at Week 96
NCT00110305 (14) [back to overview]	Area Under the Plasma Concentration Time Curve From Time 0 to 24 Hours (AUC24h) for TMC278
NCT00110305 (14) [back to overview]	Change From Baseline in CD4+ Cell Count (Absolute) at Week 240
NCT00110305 (14) [back to overview]	Change From Baseline in CD4+ Cell Count (Relative) at Week 240
NCT00110305 (14) [back to overview]	Change From Baseline in CD4+ Cell Count (Relative) at Week 96
NCT00110305 (14) [back to overview]	Number of Participants With Virologic Response (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm, by Area Under the Plasma Concentration Time Curve From Time 0 to 24 Hours (AUC24h) Quartiles
NCT00110305 (14) [back to overview]	Number of Participants With Virologic Response at Week 240 (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00110305 (14) [back to overview]	Number of Participants With Virologic Response at Week 240 (Viral Load Less Than 50 Copies Per mL) - Snapshot Analysis
NCT00110305 (14) [back to overview]	Number of Participants With Virologic Response at Week 48 (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00110305 (14) [back to overview]	Number of Participants With Virologic Response at Week 240 (Viral Load Less Than 400 Copies/mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00110305 (14) [back to overview]	Number of Participants With Virologic Response at Week 96 (Viral Load Less Than 50 Copies Per mL) - as Defined by the Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00110305 (14) [back to overview]	Number of Participants With Virologic Response at Week 96 (Viral Load Less Than 50 Copies Per mL) - Snapshot Analysis
NCT00110305 (14) [back to overview]	Trough Plasma Concentration (Ctrough) for TMC278
NCT00110305 (14) [back to overview]	Number of Participants With Virologic Failure for the Resistance Determinations by Developing Mutations: First Available On-Treatment Genotypic Data After Failure
NCT00540449 (9) [back to overview]	Mean Change From Baseline to Week 48 and Week 96 in Absolute and Relative CD4+ Cell Counts (Using Imputed Data)
NCT00540449 (9) [back to overview]	Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies/ml) at Week 96
NCT00540449 (9) [back to overview]	Number of Participants With Virological Response (Observed, <50 Copies/ml) at Last On-Treatment Visit (Post-Week 96).
NCT00540449 (9) [back to overview]	Number of Participants With Virologic Failure for the Resistance Determination by Emerging Resistance Associated Mutations: First Available On-Treatment Genotypic Data After Failure
NCT00540449 (9) [back to overview]	Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies/ml) at Week 96
NCT00540449 (9) [back to overview]	The Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies/ml) at Week 48
NCT00540449 (9) [back to overview]	The Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies/ml) at Week 96
NCT00540449 (9) [back to overview]	Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies/ml) at Week 48
NCT00540449 (9) [back to overview]	Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies/ml) at Week 48
NCT00543725 (9) [back to overview]	Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies Per mL) at Week 96
NCT00543725 (9) [back to overview]	Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies Per mL) at Week 48
NCT00543725 (9) [back to overview]	Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <50 Copies Per mL) at Week 96
NCT00543725 (9) [back to overview]	Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies Per mL) at Week 96
NCT00543725 (9) [back to overview]	Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies Per mL) at Week 48
NCT00543725 (9) [back to overview]	Number of Participants With Virological Response (Observed, <50 Copies/mL) at Last On-Treatment Visit (Post-Week 96).
NCT00543725 (9) [back to overview]	Mean Change From Baseline to Week 48 and Week 96 in Absolute and Relative CD4+ Cell Counts (Using Imputed Data)
NCT00543725 (9) [back to overview]	Number of Participants With Virologic Failure for the Resistance Determinations by Developing Mutations: First Available On-Treatment Genotypic Data After Failure
NCT00543725 (9) [back to overview]	Number of Participants With Virological Response (Intent-to-Treat - Snapshot, <50 Copies Per mL) at Week 48
NCT00855335 (15) [back to overview]	Mean Change From Baseline in Log10 Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) Viral Load Value
NCT00855335 (15) [back to overview]	Mean Change From Baseline in Log10 Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) Viral Load Value
NCT00855335 (15) [back to overview]	Minimum Plasma Concentration (Cmin)
NCT00855335 (15) [back to overview]	Number of Infants With Human Immunodeficiency Virus (HIV) Positive Test Result
NCT00855335 (15) [back to overview]	Time to Reach the Maximum Plasma Concentration (Tmax)
NCT00855335 (15) [back to overview]	Predose (Trough) Plasma Concentration (C0h)
NCT00855335 (15) [back to overview]	Plasma Concentration of Drug in the Cord Plasma and Maternal Plasma Samples Collected at the Time of Delivery
NCT00855335 (15) [back to overview]	Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00855335 (15) [back to overview]	Number of Participants With Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) Plasma Viral Load (<) 50 Copies/Milliliter (mL)
NCT00855335 (15) [back to overview]	Number of Participants With Resistance at Virological Failure
NCT00855335 (15) [back to overview]	Area Under the Plasma Concentration-Time Curve From Time of Administration to 12 Hours Post-dose (AUC0-12h)
NCT00855335 (15) [back to overview]	Area Under the Plasma Concentration-Time Curve From Time of Administration to 24 Hours Post-dose (AUC0-24h)
NCT00855335 (15) [back to overview]	Maximum Plasma Concentration (Cmax)
NCT00855335 (15) [back to overview]	Mean Change From Baseline in CD4+ Cell Count
NCT00855335 (15) [back to overview]	Mean Change From Baseline in CD4+ Cell Count
NCT01266902 (8) [back to overview]	Time to Virologic Rebound
NCT01266902 (8) [back to overview]	Change From Baseline in Cluster of Differentiation 4 (CD4+) Cell Count for Observed Case Approach Until Week 336
NCT01266902 (8) [back to overview]	Change From Baseline in CD4+ Cell Count for Non-Completer Equals Failure (NC=F) Approach Until Week 336
NCT01266902 (8) [back to overview]	Number of Participants With Serious Adverse Events (SAEs)
NCT01266902 (8) [back to overview]	Number of Participants With Grade 3/4 Events of Rash Irrespective of Causality
NCT01266902 (8) [back to overview]	Number of Participants With AEs Related to Rilpivirine (RPV)
NCT01266902 (8) [back to overview]	Number of Participants With Adverse Events (AEs)
NCT01266902 (8) [back to overview]	Time To Treatment Failure
NCT01562886 (2) [back to overview]	Number of Subjects With HIV Viral Load Above 50 Copies Per mL
NCT01562886 (2) [back to overview]	CSF:Plasma Ratio of Rilpivirine Levels
NCT01585038 (4) [back to overview]	Oxidative Stress Markers
NCT01585038 (4) [back to overview]	Inflammatory Markers
NCT01585038 (4) [back to overview]	Endothelial Activation Markers
NCT01585038 (4) [back to overview]	Change in Flow-mediated Dilation of the Brachial Artery
NCT01641809 (57) [back to overview]	Number of Participants With Adherence to Study Treatment
NCT01641809 (57) [back to overview]	Change From Baseline in Total Neutrophils, Platelet Count and WBC Count Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Total Neutrophils, Platelet Count and WBC Count Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Plasma log10 HIV-1 RNA Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Plasma log10 HIV-1 RNA Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Hemoglobin Level Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Hemoglobin Level Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Estimated Creatinine Clearance Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Estimated Creatinine Clearance Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Estimated Creatinine Clearance Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Estimated Creatinine Clearance Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Creatinine and Total Bilirubin Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in Creatinine and Total Bilirubin Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in CD4+ Cell Count Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in CD4+ Cell Count Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in ALT, AST and CK Over Time by Visit
NCT01641809 (57) [back to overview]	Change From Baseline in ALT, AST and CK Over Time by Visit
NCT01641809 (57) [back to overview]	Absolute Values for Platelet Count, Total Neutrophils and WBC Count During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]	Absolute Values for Plasma Logarithm to the Base 10 (log10) HIV-1 RNA Over Time by Visit
NCT01641809 (57) [back to overview]	Absolute Values for Plasma Logarithm to the Base 10 (log10) HIV-1 RNA Over Time by Visit
NCT01641809 (57) [back to overview]	Absolute Values for Hemoglobin During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]	Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]	Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]	Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]	Absolute Values for Estimated Creatinine Clearance During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]	Absolute Values for Creatinine and Total Bilirubin During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]	Absolute Values for Cluster of Differentiation 4+ (CD4+) Cell Count During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]	Absolute Values for ALT, AST, CK During Double-blind Randomized Treatment Until Week 96
NCT01641809 (57) [back to overview]	Percentage of Participants With HIV-1 Ribonucleic Acid (RNA) <50 Copies/Milliliter (mL) at Week 48 Using the Missing, Switch, Discontinuation Equals Failure (MSDF) Algorithm
NCT01641809 (57) [back to overview]	Percentage of Participants Who Discontinued Treatment Due to Adverse Events-Maintenance Phase
NCT01641809 (57) [back to overview]	Percentage of Participants Who Discontinued Treatment Due to Adverse Events-Induction Phase
NCT01641809 (57) [back to overview]	Percentage of Participants Who Discontinued Investigational Product Due to Adverse Events
NCT01641809 (57) [back to overview]	Number of Participants With Clinically Significant Electrocardiogram (ECG) Findings
NCT01641809 (57) [back to overview]	Maximum Observed Concentration (Cmax) for GSK1265744 at Week 2
NCT01641809 (57) [back to overview]	Concentration at the End of a Dosing Interval (Ctau) for GSK1265744 at Week 2
NCT01641809 (57) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <400 Copies/mL Until Week 96 Using the Observed Case Analysis
NCT01641809 (57) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <50 Copies/mL Over Time by Visit Using Observed Case Analysis
NCT01641809 (57) [back to overview]	Area Under the Concentration Time Curve Over the Dosing Interval (AUC[0-tau]) for GSK1265744 at Week 2
NCT01641809 (57) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <50 Copies/mL Over Time by Visit Using Observed Case Analysis
NCT01641809 (57) [back to overview]	Number of Participants With Adherence to Study Treatment
NCT01641809 (57) [back to overview]	Number of Participants With Adherence to Study Treatment
NCT01641809 (57) [back to overview]	Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)-Maintenance Phase
NCT01641809 (57) [back to overview]	Number of Participants With AEs and SAEs Over Time
NCT01641809 (57) [back to overview]	Number of Participants With AEs and SAEs-Induction Phase
NCT01641809 (57) [back to overview]	Number of Participants With Maximum Treatment-emergent Clinical Chemistry Toxicities Over Time
NCT01641809 (57) [back to overview]	Number of Participants With Maximum Treatment-emergent Clinical Chemistry Toxicities-Maintenance Phase
NCT01641809 (57) [back to overview]	Number of Participants With Maximum Treatment-emergent Clinical Chemistry Toxicity-Induction Phase
NCT01641809 (57) [back to overview]	Number of Participants With Maximum Treatment-emergent Hematology Toxicities Over Time
NCT01641809 (57) [back to overview]	Number of Participants With Maximum Treatment-emergent Hematology Toxicities-Induction Phase
NCT01641809 (57) [back to overview]	Number of Participants With Maximum Treatment-emergent Hematology Toxicities-Maintenance Phase
NCT01641809 (57) [back to overview]	Number of Participants With Post-Baseline HIV-1 Associated Conditions Progression of Disease
NCT01641809 (57) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <50 Copies/mL Over Time by Visit Using the MSDF Algorithm
NCT01641809 (57) [back to overview]	Number of Participants With Treatment Emergent Genotypic Mutations Associated With Development of Resistance
NCT01641809 (57) [back to overview]	Number of Participants With Treatment Emergent Phenotypic Resistance
NCT01641809 (57) [back to overview]	Percentage of Participants With HIV-1 RNA <50 Copies/mL at Week 16 and Week 24 Using MSDF Algorithm-Induction Phase
NCT01641809 (57) [back to overview]	Percentage of Participants With HIV-1 RNA <50 Copies/mL From Week 24 Through Week 96 by Visit Using MSDF Algorithm-Maintenance Phase
NCT01641809 (57) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <400 Copies/mL Until Week 96 Using the MSDF Algorithm
NCT01709084 (6) [back to overview]	Percentage of Participants With Plasma Human Immunodeficiency Virus - Type 1 Ribonucleic Acid (HIV-1 RNA) Levels Less Than (<) 400 Copies Per Milliliter (Copies/mL) at Week 48
NCT01709084 (6) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA Levels More Than or Equal to (>=) 400 Copies/mL at Week 48 Based on Time to Loss of Virologic Response (TLOVR) [Non-virologic Failure Censored] Imputation Method.
NCT01709084 (6) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA Levels >= 50 Copies Per Milliliter (Copies/mL) at Week 48 Based on Time to Loss of Virologic Response (TLOVR) [Non-virologic Failure Censored] Imputation Method.
NCT01709084 (6) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA Levels < 50 Copies/mL at Week 48
NCT01709084 (6) [back to overview]	Percentage of Participant With Treatment Adherence Based on Tablet Count
NCT01709084 (6) [back to overview]	Number of Participants With Treatment-Emergent Nucleoside Reverse Transcriptase Inhibitor (N[t]RTI) or Nucleoside/Nucleotide Reverse Transcriptase Inhibitor (NNRTI) Mutations
NCT01777997 (9) [back to overview]	Plasma HIV-1 RNA Level Measured by Single Copy Assay Using Primer in Integrase (iSCA) as the Proportion of Participants Below the Limit of the Assay
NCT01777997 (9) [back to overview]	Change in Quality of Life (QoL) Index
NCT01777997 (9) [back to overview]	Change in Levels of Interleukin (IL)-6
NCT01777997 (9) [back to overview]	Change in Levels of D-dimer
NCT01777997 (9) [back to overview]	Change in Levels of CD8+ T-cell Activation
NCT01777997 (9) [back to overview]	Change in Levels of CD4+ T-cell Activation (Defined as the Percentage HLA-DR+/CD38+)
NCT01777997 (9) [back to overview]	Change in CD4+ T-cell Count
NCT01777997 (9) [back to overview]	Number of Subjects Who Experience Grade 3 or 4 Signs and Symptoms or Laboratory Abnormalities, Diagnoses (Any Grade), or Other Serious Adverse Events (SAEs)
NCT01777997 (9) [back to overview]	Change in Levels of CD8+ T-cell Activation (Defined as the Percentage HLA-DR+/CD38+) From Baseline to Weeks 24 and 48 on ART
NCT02120352 (67) [back to overview]	Number of Participants With AEs by Their Severity Grades, for Oral Dose of CAB 30 mg Plus ABC/3TC (Induction Period)
NCT02120352 (67) [back to overview]	Virologic Failure (From MSDF Algorithm) in Relation With PK Parameter (Cmax) of CAB LA and RPV LA at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Virologic Failure (From MSDF Algorithm) in Relation With PK Parameter (Average C0) of CAB LA and RPV LA at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Virologic Failure (From MSDF Algorithm) in Relation With PK Parameter (AUC[0-tau]) of CAB LA and RPV LA at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Trough Concentration (Ctrough) of CAB LA (Q8W IM Dosing) Used for Assessment of Steady State (Maintenance Period)
NCT02120352 (67) [back to overview]	Pharmacodynamic Response (HIV-1 RNA<50 c/mL) in Relation With PK Parameter (Cmax) of CAB LA and RPV LA at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Pharmacodynamic Response (HIV-1 RNA<50 c/mL) in Relation With PK Parameter (Average C0) of CAB LA and RPV LA at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Pharmacodynamic Response (HIV-1 RNA<50 c/mL) in Relation With PK Parameter (AUC[0-tau]) of CAB LA and RPV LA at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Number of Participants With AEs by Their Severity Grades Over Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Ctrough of RPV LA (Q8W IM Dosing) Used for Assessment of Steady State (Maintenance Period)
NCT02120352 (67) [back to overview]	Ctrough of CAB LA (Q4W IM Dosing) Used for Assessment of Steady State (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Plasma HIV-1 RNA, for Oral Dose of CAB 30 mg Plus ABC/3TC (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Hematology Parameters: Basophil, Eosinophils, Lymphocytes, Total Neutrophils, Monocytes, Platelets Count and White Blood Cells (WBC) Count (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Hematology Parameters: Basophil, Eosinophils, Lymphocytes, Total Neutrophils, Monocytes, Platelet Count and WBC Count at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Hematology Parameter: Red Blood Cell Count (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Hematology Parameter: Mean Corpuscle Volume (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Hematology Parameter: Hemoglobin (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Hematology Parameter: Hematocrit (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Clinical Chemistry Parameters: Total CO2, Chloride, Cholesterol, Glucose, Potassium, Sodium, Triglyceride and Urea at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Clinical Chemistry Parameters: Total Bilirubin and Creatinine at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Clinical Chemistry Parameters: Total Bilirubin and Creatinine (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Clinical Chemistry Parameters: CO2, Chloride, Cholesterol, Glucose, Potassium, Sodium, Triglyceride and Urea (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Clinical Chemistry Parameters: ALT, ALP, AST and CK at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Clinical Chemistry Parameters: ALT, ALP, AST and CK (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Clinical Chemistry Parameter: Lipase (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Clinical Chemistry Parameter: Albumin (Induction Period)
NCT02120352 (67) [back to overview]	Change From Baseline in CD4+, for Oral Dose of CAB 30 mg Plus ABC/3TC (Induction Period)
NCT02120352 (67) [back to overview]	Average Initial Concentration (C0) and Maximum Plasma Concentration (Cmax) of CAB LA (Q4W IM and Q8W IM Dosing) (Maintenance Period)
NCT02120352 (67) [back to overview]	Average Initial Concentration (C0) and Cmax of RPV LA (Q4W IM and Q8W IM Dosing) (Maintenance Period)
NCT02120352 (67) [back to overview]	Absolute Values of Plasma HIV-1 RNA, for Oral Dose of CAB 30 mg Plus ABC/3TC (Induction Period)
NCT02120352 (67) [back to overview]	Absolute Values of Cluster of Differentiation 4+ (CD4+), for Oral Dose of CAB 30 mg Plus ABC/3TC (Induction Period)
NCT02120352 (67) [back to overview]	Percentage of Participants With Plasma Human Immunodeficiency Virus-1 (HIV-1) Ribonucleic Acid (RNA) Level Below 50 Copies/Milliliter (c/mL) at Week 32
NCT02120352 (67) [back to overview]	Number of Participants With Protocol Defined Virologic Failure at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Number of Participants With Protocol Defined Virologic Failure (PDVF) Until Week 32
NCT02120352 (67) [back to overview]	HIV Treatment Satisfaction Questionnaire - Status Version (HIVTSQ[s]) Total Score at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	HIV Treatment Satisfaction Questionnaire - Change Version (HIVTSQ[c]) Total Score at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Plasma HIV-1 RNA at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Hematology Parameter: Red Blood Cell Count at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Hematology Parameter: Mean Corpuscle Volume at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Hematology Parameter: Hemoglobin at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Hematology Parameter: Hematocrit at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Ctrough of RPV LA (Q4W IM Dosing) Used for Assessment of Steady State (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Clinical Chemistry Parameter: Lipase at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in Clinical Chemistry Parameter: Albumin at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Change From Baseline in CD4+ at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Absolute Value of Plasma HIV-1 RNA at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA Level <50 c/mL and <200 c/mL Over Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Absolute Value of CD4+ at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Number of Participants With HIV-1 Disease Progression Over Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Number of Participants With Maximum Post-Baseline Emergent Toxicities for Clinical Chemistry Parameters, for Oral Dose of CAB 30 mg Plus ABC/3TC (Induction Period)
NCT02120352 (67) [back to overview]	Number of Participants With Maximum Post-Baseline Emergent Toxicities for Hematology Parameters
NCT02120352 (67) [back to overview]	Number of Participants With Maximum Post-Baseline Emergent Toxicities for Hematology Parameters, for Oral Dose of CAB 30 mg Plus ABC/3TC (Induction Period)
NCT02120352 (67) [back to overview]	Number of Participants With Post-Baseline Adverse Events by Maximum Toxicity Grade
NCT02120352 (67) [back to overview]	Number of Participants With Post-Baseline Urinalysis Dipstick Results
NCT02120352 (67) [back to overview]	Number of Participants With Treatment-emergent Genotypic Resistance
NCT02120352 (67) [back to overview]	Number of Participants With Treatment-emergent Phenotypic Resistance
NCT02120352 (67) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <200 c/mL and <50 c/mL, for Oral Dose of CAB 30 mg Plus ABC/3TC (Induction Period)
NCT02120352 (67) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA Level <50 c/mL Over Week 32 by Subgroups (Maintenance Period)
NCT02120352 (67) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA Level <50 c/mL Over Week 32 by Subgroups (Maintenance Period)
NCT02120352 (67) [back to overview]	Number of Participants With Maximum Post-Baseline Emergent Toxicities for Clinical Chemistry Parameters
NCT02120352 (67) [back to overview]	Number of Participants With HIV Medication Questionnaire (HIVMQ) Item E and F Scores at Week 32 (Maintenance Period)
NCT02120352 (67) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA Level <50 c/mL Over Week 32 by Subgroups (Maintenance Period)
NCT02120352 (67) [back to overview]	Percentage of Participants With Protocol Defined Virologic Failure (PDVF) at Week 32 by Subgroups(Maintenance Period)
NCT02120352 (67) [back to overview]	Percentage of Participants With Protocol Defined Virologic Failure (PDVF) at Week 32 by Subgroups(Maintenance Period)
NCT02120352 (67) [back to overview]	Percentage of Participants With Protocol Defined Virologic Failure (PDVF) at Week 32 by Subgroups(Maintenance Period)
NCT02120352 (67) [back to overview]	Number of Participants With Any Serious Adverse Event (SAE) and Any Non-serious Adverse Event (Non-SAE) (Maintenance Period)
NCT02120352 (67) [back to overview]	Number of Participants With Any Serious Adverse Event (SAE) and Any Non-serious Adverse Event (Non-SAE) (Induction Period)
NCT02165202 (1) [back to overview]	Number of Participants Experiencing Any Grade 2 or Higher AEs During Injection Phase
NCT02938520 (66) [back to overview]	Change From Baseline Values in Urine Retinol Binding Protein Over Time Including Week 48
NCT02938520 (66) [back to overview]	Change in Treatment Satisfaction Over Time Using HIVTSQc at Week 48
NCT02938520 (66) [back to overview]	Cmax in Plasma for RPV LA Evaluable at Week 41
NCT02938520 (66) [back to overview]	Maximum Concentration (Cmax) in Plasma for CAB LA Evaluable at Week 41
NCT02938520 (66) [back to overview]	Number of Participants Who Discontinued or Withdrawn Due to AEs Over Time Including Week 48
NCT02938520 (66) [back to overview]	Number of Participants With Confirmed Virologic Failure (CVF) During the Maintenance Phase
NCT02938520 (66) [back to overview]	Number of Participants With Disease Progression
NCT02938520 (66) [back to overview]	Number of Participants With HIV-1 RNA <200 Copies/mL Using Snapshot Algorithm at Week 48
NCT02938520 (66) [back to overview]	Percentage of Participants With HIV-1 RNA <50 Copies/mL Using Snapshot Algorithm at Week 48
NCT02938520 (66) [back to overview]	Percentage of Participants With Virologic Failure (HIV-1 Ribonucleic Acid [RNA] >=50 Copies Per Millilter [mL]) Using Snapshot Algorithm at Week 48
NCT02938520 (66) [back to overview]	"Change From Baseline in Treatment Acceptance at Weeks 8, 24 and 48 Using General Acceptance Dimension of the Chronic Treatment Acceptance (ACCEPT) Questionnaire"
NCT02938520 (66) [back to overview]	Absolute Values for Clinical Chemistry Parameter Over Time Including Week 48: Albumin
NCT02938520 (66) [back to overview]	Absolute Values for Clinical Chemistry Parameter Over Time Including Week 48: Creatinine Clearance.
NCT02938520 (66) [back to overview]	Absolute Values for Clinical Chemistry Parameter Over Time Including Week 48: Lipase
NCT02938520 (66) [back to overview]	Absolute Values for Clinical Chemistry Parameters Over Time Including Week 48: Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST) and Creatinine Kinase (CK)
NCT02938520 (66) [back to overview]	Absolute Values for Clinical Chemistry Parameters Over Time Including Week 48: Bilirubin, Direct Bilirubin and Creatinine
NCT02938520 (66) [back to overview]	Absolute Values for Clinical Chemistry Parameters: Total Carbon-dioxide (CO2), Chloride, Glucose, Phosphate, Potassium, Sodium and Urea Over Time Including Week 48
NCT02938520 (66) [back to overview]	Absolute Values for Fasting Lipid Panel Overtime Including Week 48
NCT02938520 (66) [back to overview]	Absolute Values for Hematology Parameters Over Time Including Week 48: Basophils, Eosinophils, Leukocytes, Lymphocytes, Neutrophils, Monocytes, and Platelets
NCT02938520 (66) [back to overview]	Absolute Values for Hematology Parameters Over Time Including Week 48: Erythrocyte Mean Corpuscular Volume
NCT02938520 (66) [back to overview]	Absolute Values for Hematology Parameters Over Time Including Week 48: Erythrocytes
NCT02938520 (66) [back to overview]	Absolute Values for Hematology Parameters Over Time Including Week 48: Hematocrit
NCT02938520 (66) [back to overview]	Absolute Values for Hematology Parameters Over Time Including Week 48: Hemoglobin
NCT02938520 (66) [back to overview]	Change From 4b in Tolerability of Injection at Weeks 5, 40 and 41 Using Numeric Rating Scale (NRS) Within CAB LA+RPV LA Arm
NCT02938520 (66) [back to overview]	Change From Baseline for Hematology Parameters: Basophil, Eosinophils, Leukocytes, Lymphocytes, Neutrophils, Monocytes, and Platelets
NCT02938520 (66) [back to overview]	Change From Baseline for Hematology Parameters: Erythrocyte Mean Corpuscular Volume
NCT02938520 (66) [back to overview]	Change From Baseline for Hematology Parameters: Erythrocytes
NCT02938520 (66) [back to overview]	Change From Baseline for Hematology Parameters: Hematocrit
NCT02938520 (66) [back to overview]	Change From Baseline for Hematology Parameters: Hemoglobin
NCT02938520 (66) [back to overview]	Change From Baseline in Clinical Chemistry Parameters Over Time Including Week 48: ALT, ALP, AST and CK
NCT02938520 (66) [back to overview]	Change From Baseline in DISWO Using HATQoL
NCT02938520 (66) [back to overview]	Change From Baseline in Health Status Using 12-item Short Form Survey (SF-12)
NCT02938520 (66) [back to overview]	Change From Baseline in HIV Medication, MEDWO Using HATQoL
NCT02938520 (66) [back to overview]	Change From Baseline in Individual Item Scores of HIVTSQs at Weeks 4b, 24 and 44
NCT02938520 (66) [back to overview]	Change From Baseline in Life Satisfaction (LISAT) Using HIV/AIDs-targeted Quality of Life (HATQoL) Questionnaire
NCT02938520 (66) [back to overview]	Change From Baseline in Total Treatment Satisfaction Using HIV Treatment Satisfaction Questionnaire (HIVTSQs) at Weeks 4b, 24 and 44
NCT02938520 (66) [back to overview]	Change From Baseline in Total Treatment Satisfaction Using HIV Treatment Satisfaction Questionnaire (HIVTSQs) at Weeks 4b, 24 and 44
NCT02938520 (66) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameter Over Time Including Week 48: Creatinine Clearance
NCT02938520 (66) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameter Over Time Including Week 48: Lipase
NCT02938520 (66) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameters Over Time Including Week 48
NCT02938520 (66) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameters Over Time Including Week 48: Bilirubin, Direct Bilirubin and Creatinine
NCT02938520 (66) [back to overview]	Change From Baseline Values for Fasting Lipid Panel and Glucose Overtime Including Week 48
NCT02938520 (66) [back to overview]	Change From Baseline Values in Urine Albumin/Creatinine Ratio and Urine Protein/Creatinine Ratio Over Time Including Week 48
NCT02938520 (66) [back to overview]	Change From Baseline Values in Urine Creatinine Over Time Including Week 48
NCT02938520 (66) [back to overview]	Change From Baseline Values in Urine pH Over Time Including Week 48
NCT02938520 (66) [back to overview]	Change From Baseline Values in Urine Phosphate Over Time Including Week 48
NCT02938520 (66) [back to overview]	Change From Baseline Values in Urine Specific Gravity Over Time Including Week 48
NCT02938520 (66) [back to overview]	Change From Week 5 in Dimension Scores Using Perception of Injection Questionnaire (PIN)-Last Observation Carried Forward (LOCF)
NCT02938520 (66) [back to overview]	Ctrough for RPV LA Evaluable
NCT02938520 (66) [back to overview]	Number of Participants With Phenotypic Resistance Through Week 48
NCT02938520 (66) [back to overview]	Number of Participants With Abnormal Urinalysis Parameter Over Time Including Week 48
NCT02938520 (66) [back to overview]	Number of Participants With Severity of Adverse Events
NCT02938520 (66) [back to overview]	Number of Participants With Urine Potential of Hydrogen (pH) Over Time Including Week 48
NCT02938520 (66) [back to overview]	Percentage Change From Baseline in Fasting Lipids Overtime Including Week 48
NCT02938520 (66) [back to overview]	Percentage of Participants With Extremely or Very Acceptable Pain and Local Reaction: Acceptability Score on PIN Questionnaire
NCT02938520 (66) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameter Over Time Including Week 48: Albumin
NCT02938520 (66) [back to overview]	Plasma Trough Concentration (Ctrough) for CAB LA Evaluable
NCT02938520 (66) [back to overview]	Change From Baseline in Individual Item Scores of HIVTSQs at Weeks 4b, 24 and 44
NCT02938520 (66) [back to overview]	Number of Participants With Genotypic Resistance Through Week 48
NCT02938520 (66) [back to overview]	Absolute Values for CD4+ Lymphocyte Count at Week 48
NCT02938520 (66) [back to overview]	Absolute Values for Plasma HIV-1 RNA at Week 48
NCT02938520 (66) [back to overview]	Area Under the Curve (AUC) for CAB LA
NCT02938520 (66) [back to overview]	AUC for RPV LA
NCT02938520 (66) [back to overview]	Change From Baseline Values for CD4+ Lymphocyte Count at Week 48
NCT02938520 (66) [back to overview]	Change From Baseline Values for Plasma HIV-1 RNA at Week 48
NCT02938520 (66) [back to overview]	Number of Participants With Non-serious Adverse Events (Non-SAEs) and Serious Adverse Events (SAEs)
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameters Over Time Including Week 48: Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST) and Creatinine Kinase (CK)
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameters Over Time Including Week 48: Bilirubin, Direct Bilirubin and Creatinine
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48: Albumin
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48: ALT, ALP, AST and CK
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48: Bilirubin, Direct Bilirubin and Creatinine
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48: Creatinine Clearance
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48: Lipase
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameters: Total Carbon-dioxide (CO2), Chloride, Glucose, Phosphate, Potassium, Sodium and Urea Over Time Including Week 48
NCT02951052 (86) [back to overview]	Absolute Values for Fasting Lipid Panel Using Baseline Third Agent Treatment Class Overtime Including Week 48
NCT02951052 (86) [back to overview]	Absolute Values for Hematology Parameters Over Time Including Week 48: Basophil, Eosinophils, Leukocytes, Lymphocytes, Neutrophils, Monocytes, and Platelets
NCT02951052 (86) [back to overview]	Absolute Values for Hematology Parameters: Erythrocyte Mean Corpuscular Volume
NCT02951052 (86) [back to overview]	Absolute Values for Hematology Parameters: Erythrocytes
NCT02951052 (86) [back to overview]	Absolute Values for Hematology Parameters: Hematocrit
NCT02951052 (86) [back to overview]	Absolute Values for Hematology Parameters: Hemoglobin
NCT02951052 (86) [back to overview]	Change From 4b in Tolerability of Injection at Week 5, 40 and 41 Using Numeric Rating Scale (NRS) Within CAB LA+RPV LA Arm
NCT02951052 (86) [back to overview]	Change From Baseline for Hematology Parameters: Basophil, Eosinophils, Leukocytes, Lymphocytes, Neutrophils, Monocytes, and Platelets
NCT02951052 (86) [back to overview]	Change From Baseline for Hematology Parameters: Erythrocyte Mean Corpuscular Volume
NCT02951052 (86) [back to overview]	Change From Baseline for Hematology Parameters: Erythrocytes
NCT02951052 (86) [back to overview]	Change From Baseline for Hematology Parameters: Hematocrit
NCT02951052 (86) [back to overview]	Change From Baseline for Hematology Parameters: Hemoglobin
NCT02951052 (86) [back to overview]	Change From Baseline in Clinical Chemistry Parameters Over Time Including Week 48: ALT, ALP, AST and CK
NCT02951052 (86) [back to overview]	Change From Baseline in DISWO Using HATQoL
NCT02951052 (86) [back to overview]	Change From Baseline in Health Status Using 12-item Short Form Survey (SF-12)
NCT02951052 (86) [back to overview]	Change From Baseline in HIV Medication, MEDWO Using HATQoL
NCT02951052 (86) [back to overview]	Change From Baseline in Individual Item Scores of HIVTSQc at Weeks 4b, 24 and 44
NCT02951052 (86) [back to overview]	Change From Baseline in Individual Item Scores of HIVTSQc at Weeks 4b, 24 and 44
NCT02951052 (86) [back to overview]	Change From Baseline in Life Satisfaction (LISAT) Using HIV/AIDs-targeted Quality of Life (HATQoL) Questionnaire
NCT02951052 (86) [back to overview]	Change From Baseline in Total Treatment Satisfaction Using HIV Treatment Satisfaction Questionnaire (HIVTSQs) at Weeks 4b, 24 and 44
NCT02951052 (86) [back to overview]	Change From Baseline in Total Treatment Satisfaction Using HIV Treatment Satisfaction Questionnaire (HIVTSQs) at Weeks 4b, 24 and 44
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameter Over Time Including Week 48: Albumin
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameter Over Time Including Week 48: Creatinine Clearance.
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameter Over Time Including Week 48: Lipase
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameters Over Time Including Week 48
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameters Over Time Including Week 48: Bilirubin, Direct Bilirubin and Creatinine
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48: ALT, ALP, AST and CK
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48: Bilirubin, Direct Bilirubin and Creatinine
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48: Creatinine Clearance
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48: Lipase
NCT02951052 (86) [back to overview]	Change From Baseline Values for Fasting Lipid Panel Over Time Including Week 48
NCT02951052 (86) [back to overview]	Change From Baseline Values for Fasting Lipid Panel Using Baseline Third Agent Treatment Class Overtime Including Week 48
NCT02951052 (86) [back to overview]	Change From Baseline Values in Urine Albumin/Creatinine Ratio and Urine Protein/Creatinine Ratio Over Time Including Week 48
NCT02951052 (86) [back to overview]	Change From Baseline Values in Urine Creatinine Over Time Including Week 48
NCT02951052 (86) [back to overview]	Change From Baseline Values in Urine pH Over Time Including Week 48
NCT02951052 (86) [back to overview]	Change From Baseline Values in Urine Phosphate Over Time Including Week 48
NCT02951052 (86) [back to overview]	Change From Baseline Values in Urine Specific Gravity Over Time Including Week 48
NCT02951052 (86) [back to overview]	Change From Week 5 in Dimension Scores Using Percerption of Injection Questionnaire (PIN)-Last Observation Carried Forward (LOCF) in Q4W Arm
NCT02951052 (86) [back to overview]	Ctrough for RPV LA Evaluable
NCT02951052 (86) [back to overview]	Number of Participants Discontinued or Withdrawn Due to AEs When Baseline Third Agent Treatment Class Was Used Over Time Including Week 48
NCT02951052 (86) [back to overview]	Number of Participants With Abnormal Urinalysis Parameters Over Time Including Week 48
NCT02951052 (86) [back to overview]	Number of Participants With AEs by Using Baseline Third Agent Treatment Class Overtime Including Week 48
NCT02951052 (86) [back to overview]	Number of Participants With Confirmed Virologic Failure (CVF)
NCT02951052 (86) [back to overview]	Number of Participants With Genotypic Resistance Through Week 48
NCT02951052 (86) [back to overview]	Number of Participants With Genotypic Resistance Using Baseline Third Agent Through Week 48
NCT02951052 (86) [back to overview]	Number of Participants With Non-serious Adverse Events (Non-SAEs) and Serious Adverse Events (SAEs)
NCT02951052 (86) [back to overview]	Number of Participants With Phenotypic Resistance Through Week 48
NCT02951052 (86) [back to overview]	Number of Participants With Phenotypic Resistance Using Baseline Third Agent Through Week 48
NCT02951052 (86) [back to overview]	Number of Participants With Severity of Adverse Events
NCT02951052 (86) [back to overview]	Number of Participants With Severity of Adverse Events by Baseline Third Agents
NCT02951052 (86) [back to overview]	Number of Participants With Urine Potential of Hydrogen (pH) Over Time Including Week 48
NCT02951052 (86) [back to overview]	Percentage Change From Baseline in Fasting Lipids Overtime Including Week 48
NCT02951052 (86) [back to overview]	Percentage of Participants With a Virologic Failure Using Snapshot Algorithm by Baseline Third Agent
NCT02951052 (86) [back to overview]	Percentage of Participants With Extremely or Very Acceptable Pain and Local Reaction: Acceptability Score on PIN Questionnaire in Q4W Arm
NCT02951052 (86) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <50copies/mL Using Snapshot Algorithm by Baseline Third Agent
NCT02951052 (86) [back to overview]	Plasma Trough Concentration (Ctrough) for CAB LA Evaluable
NCT02951052 (86) [back to overview]	Change From Baseline Values for Clinical Chemistry Parameters Using Baseline Third Agent Treatment Class Overtime Including Week 48: Albumin
NCT02951052 (86) [back to overview]	Absolute Values for CD4+ Lymphocyte Count at Week 48
NCT02951052 (86) [back to overview]	Absolute Values for Plasma HIV-1 RNA at Week 48
NCT02951052 (86) [back to overview]	Area Under the Curve (AUC) for CAB LA
NCT02951052 (86) [back to overview]	AUC for RPV LA
NCT02951052 (86) [back to overview]	Change From Baseline Values for CD4+ Lymphocyte Count at Week 48
NCT02951052 (86) [back to overview]	Change From Baseline Values for Plasma HIV-1 RNA
NCT02951052 (86) [back to overview]	Change From Baseline Values in Urine Retinol Binding Protein Over Time Including Week 48
NCT02951052 (86) [back to overview]	Change in Treatment Satisfaction Over Time Using HIVTSQ Change (HIVTSQc) at Week 48 in Q4W Arm
NCT02951052 (86) [back to overview]	Cmax in Plasma for RPV LA Evaluable at Week 41
NCT02951052 (86) [back to overview]	Maximum Concentration (Cmax) in Plasma for CAB LA Evaluable at Week 41
NCT02951052 (86) [back to overview]	Number of Participants Who Discontinued or Withdrawn Due to AEs Over Time Including Week 48
NCT02951052 (86) [back to overview]	Number of Participants With Disease Progression
NCT02951052 (86) [back to overview]	Number of Participants With HIV-1 RNA <200 Copies/mL Using Snapshot Algorithm at Week 48
NCT02951052 (86) [back to overview]	Number of Participants With HIV-1 RNA <50 Copies/mL Using Snapshot Algorithm at Week 48
NCT02951052 (86) [back to overview]	Number of Participants With Virologic Failure (HIV-1 Ribonucleic Acid [RNA] >=50 Copies Per Millilter [mL]) Using Snapshot Algorithm at Week 48
NCT02951052 (86) [back to overview]	"Change From Baseline in Treatment Acceptance at Weeks 8, 24 and 48 Using General Acceptance Dimension of the Chronic Treatment Acceptance (ACCEPT) Questionnaire"
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameter Over Time Including Week 48: Albumin
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameter Over Time Including Week 48: Creatinine Clearance
NCT02951052 (86) [back to overview]	Absolute Values for Clinical Chemistry Parameter Over Time Including Week 48: Lipase
NCT03299049 (46) [back to overview]	"Change From Baseline in Treatment Acceptance a Using General Acceptance Dimension of the Chronic Treatment Acceptance (ACCEPT) Questionnaire in Participants With or Without Prior Exposure to CAB+RPV"
NCT03299049 (46) [back to overview]	Change From Baseline in Clinical Chemistry Parameter: Albumin Over Time
NCT03299049 (46) [back to overview]	Change From Baseline in Clinical Chemistry Parameter: GFR From Creatinine Adjusted Using Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) Over Time
NCT03299049 (46) [back to overview]	Change From Baseline in Clinical Chemistry Parameter: Lipase Over Time
NCT03299049 (46) [back to overview]	Change From Baseline in Clinical Chemistry Parameters: ALT, ALP, AST and Creatinine Kinase Over Time
NCT03299049 (46) [back to overview]	Change From Baseline in Clinical Chemistry Parameters: Bilirubin and Creatinine Over Time
NCT03299049 (46) [back to overview]	Change From Baseline in Clinical Chemistry Parameters: Cholesterol, Glucose, Direct High Density Lipoprotein (HDL) Cholesterol, LDL Cholesterol Calculation and Triglycerides at Week 48
NCT03299049 (46) [back to overview]	Change From Baseline in Clinical Chemistry Parameters: CO2, Chloride, Phosphate, Potassium, Sodium and Urea Over Time
NCT03299049 (46) [back to overview]	Change From Baseline in DISWO Using HATQoL Questionnaire in Participants With or Without Prior Exposure to CAB+RPV
NCT03299049 (46) [back to overview]	Change From Baseline in Hematology Parameter: Erythrocyte Mean Corpuscular Volume (MCV) Over Time
NCT03299049 (46) [back to overview]	Change From Baseline in Hematology Parameter: Erythrocytes Over Time
NCT03299049 (46) [back to overview]	Change From Baseline in Hematology Parameter: Hematocrit Over Time
NCT03299049 (46) [back to overview]	Plasma Ctrough for RPV LA Evaluable
NCT03299049 (46) [back to overview]	Plasma Trough Concentration (Ctrough) for CAB LA Evaluable
NCT03299049 (46) [back to overview]	Total Treatment Satisfaction Change Score Using HIV Treatment Satisfaction Change Questionnaire (HIVTSQc) at Week 48
NCT03299049 (46) [back to overview]	Absolute Values for Cluster of Differentiation 4 Plus (CD4+) at Week 48
NCT03299049 (46) [back to overview]	Change From Baseline in Hematology Parameter: Hemoglobin Over Time
NCT03299049 (46) [back to overview]	Percentage of Participants With Protocol Defined Confirmed Virologic Failure (CVF) Through Weeks 24 and 48
NCT03299049 (46) [back to overview]	Change From Baseline in Hematology Parameters: Basophils, Eosinophils, Leukocytes, Lymphocytes, Monocytes, Neutrophils and Platelets Over Time
NCT03299049 (46) [back to overview]	Change From Baseline in HIV Medication, MEDWO Using HATQoL Questionnaire in Participants With or Without Prior Exposure to CAB+RPV
NCT03299049 (46) [back to overview]	Change From Baseline in Individual Item Scores Using HIVTSQs at Weeks 24 and 48
NCT03299049 (46) [back to overview]	Absolute Values for HIV-1 RNA at Week 48
NCT03299049 (46) [back to overview]	Change From Baseline in Life Satisfaction (LISAT) Using HIV/AIDs-targeted Quality of Life (HATQoL) Questionnaire in Participants With or Without Prior Exposure to CAB+RPV
NCT03299049 (46) [back to overview]	Change From Baseline in Total Treatment Satisfaction Score Using HIV Treatment Satisfaction Status Questionnaire (HIVTSQs) at Weeks 24 and 48
NCT03299049 (46) [back to overview]	Change From Week 8 in Dimension Scores Using Perception of Injection (PIN) Questionnaire.
NCT03299049 (46) [back to overview]	Change From Week 8 in Individual Item Scores (Anxiety Before, Pain, Satisfaction, Anxiety After and Willingness) Using Perception of Injection (PIN) Questionnaire.
NCT03299049 (46) [back to overview]	Number of Participants With Genotypic Resistance-Maintenance Phase
NCT03299049 (46) [back to overview]	Number of Participants With Maximum Post-Baseline Chemistry Toxicities-Maintenance Phase
NCT03299049 (46) [back to overview]	Number of Participants With Maximum Post-Baseline Hematology Toxicities-Maintenance Phase
NCT03299049 (46) [back to overview]	Number of Participants With Non-serious Adverse Events (Non-SAEs >=5% Incidence) and Serious Adverse Events (SAEs)-Maintenance Phase
NCT03299049 (46) [back to overview]	Number of Participants With Phenotypic Resistance- Maintenance Phase
NCT03299049 (46) [back to overview]	Number of Participants With Severity of Adverse Events-Maintenance Phase
NCT03299049 (46) [back to overview]	Number of Participants With Their Treatment Preference as Assessed Using Preference Questionnaire at Week 48 With >=1 Weeks of Prior Exposure to CAB+RPV-CAB 600 mg LA +RPV 900 mg LA Q8W Arm Only
NCT03299049 (46) [back to overview]	Number of Participants With Their Treatment Preference as Assessed Using Preference Questionnaire at Week 48 Without (w/o) Prior Exposure to CAB+RPV-CAB 600 mg LA +RPV 900 mg LA Q8W Arm Only
NCT03299049 (46) [back to overview]	Area Under the Curve (AUC) for CAB LA
NCT03299049 (46) [back to overview]	AUC for RPV LA
NCT03299049 (46) [back to overview]	Change From Baseline Values for CD4+ at Week 48
NCT03299049 (46) [back to overview]	Change From Baseline Values for HIV-1 RNA at Week 48
NCT03299049 (46) [back to overview]	Cmax in Plasma for RPV LA Evaluable
NCT03299049 (46) [back to overview]	Maximum Concentration (Cmax) in Plasma for CAB LA Evaluable
NCT03299049 (46) [back to overview]	Percentage of Participants Who Discontinued Treatment Due to Adverse Events-Maintenance Phase
NCT03299049 (46) [back to overview]	Percentage of Participants With HIV-RNA >=50 c/mL as Per FDA Snapshot Algorithm at Week 24
NCT03299049 (46) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <50 c/mL Using FDA Snapshot Algorithm at Week 24
NCT03299049 (46) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <50 c/mL Using FDA Snapshot Algorithm at Week 48
NCT03299049 (46) [back to overview]	Number of Participants With Their Treatment Preference as Assessed Using Preference Questionnaire at Week 48-CAB 400 mg LA +RPV 600 mg LA Q4W Arm Only
NCT03299049 (46) [back to overview]	Percentage of Participants With Plasma Human Immunodeficiency Virus-ribonucleic Acid (HIV-RNA) >=50 Copies Per Milliliter (c/mL) as Per Food and Drug Administration (FDA) Snapshot Algorithm at Week 48
NCT03984838 (57) [back to overview]	T1/2 of RPV
NCT03984838 (57) [back to overview]	Percentage of AUC(0-infinity) That Was Extrapolated (%AUCex) of DTG
NCT03984838 (57) [back to overview]	Percentage AUCex of RPV
NCT03984838 (57) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of DTG
NCT03984838 (57) [back to overview]	Last Quantifiable Concentration (Ct) of DTG
NCT03984838 (57) [back to overview]	Lambda z of RPV
NCT03984838 (57) [back to overview]	Elimination Half-life (t1/2) of DTG
NCT03984838 (57) [back to overview]	Ct of RPV
NCT03984838 (57) [back to overview]	Concentration at 24-hour Post-dose (C24) of DTG
NCT03984838 (57) [back to overview]	Cmax of RPV
NCT03984838 (57) [back to overview]	CL/F of RPV
NCT03984838 (57) [back to overview]	Change From Baseline in Reticulocytes
NCT03984838 (57) [back to overview]	Change From Baseline in Pulse Rate
NCT03984838 (57) [back to overview]	Change From Baseline in Mean Corpuscular Volume (MCV)
NCT03984838 (57) [back to overview]	Change From Baseline in Mean Corpuscular Hemoglobin (MCH)
NCT03984838 (57) [back to overview]	Change From Baseline in Hemoglobin Level
NCT03984838 (57) [back to overview]	Change From Baseline in Hematocrit Level
NCT03984838 (57) [back to overview]	Change From Baseline in Erythrocytes
NCT03984838 (57) [back to overview]	Change From Baseline in Body Temperature
NCT03984838 (57) [back to overview]	C24 of RPV
NCT03984838 (57) [back to overview]	AUC (0-t) of RPV
NCT03984838 (57) [back to overview]	AUC (0-72) of RPV
NCT03984838 (57) [back to overview]	AUC (0-24) of RPV
NCT03984838 (57) [back to overview]	Area Under the Plasma Concentration Time Curve From Time Zero to 72 Hours (AUC[0-72]) of DTG
NCT03984838 (57) [back to overview]	Area Under the Plasma Concentration Time Curve From Time Zero to 24 Hours (AUC[0-24]) of DTG
NCT03984838 (57) [back to overview]	Area Under the Concentration Time Curve From Time Zero to Last Time of Quantifiable Concentration (AUC [0-t]) of DTG
NCT03984838 (57) [back to overview]	Area Under the Concentration (AUC) Time Curve From Time Zero Extrapolated to Infinite Time (AUC [0-infinity]) of DTG
NCT03984838 (57) [back to overview]	Apparent Oral Volume of Distribution (Vz/F) of DTG
NCT03984838 (57) [back to overview]	Apparent Oral Clearance (CL/F) of DTG
NCT03984838 (57) [back to overview]	Apparent Elimination Rate Constant (Lambda z) of DTG
NCT03984838 (57) [back to overview]	Time to Reach Maximum Observed Concentration (Tmax) of DTG
NCT03984838 (57) [back to overview]	Absorption Lag Time (Tlag) of DTG
NCT03984838 (57) [back to overview]	Time of Last Quantifiable Concentration (Tlast) of DTG
NCT03984838 (57) [back to overview]	Absolute Values of Hematocrit Level
NCT03984838 (57) [back to overview]	Absolute Values of Hemoglobin Level
NCT03984838 (57) [back to overview]	Absolute Values of MCH
NCT03984838 (57) [back to overview]	Absolute Values of MCV
NCT03984838 (57) [back to overview]	Absolute Values of Neutrophil, Lymphocyte, Leukocyte, Monocyte, Eosinophil, Basophil and Platelet Count
NCT03984838 (57) [back to overview]	AUC (0-infinity) of RPV
NCT03984838 (57) [back to overview]	Absolute Values of Pulse Rate
NCT03984838 (57) [back to overview]	Absolute Values of Reticulocytes
NCT03984838 (57) [back to overview]	Absolute Values of SBP and DBP
NCT03984838 (57) [back to overview]	Absolute Values of Total and Direct Bilirubin, Creatinine and Protein Levels
NCT03984838 (57) [back to overview]	Change From Baseline in Aspartate Aminotransferase (AST), Alanine Aminotransferase (ALT) and Alkaline Phosphatase (ALP) Levels
NCT03984838 (57) [back to overview]	Change From Baseline in Blood Urea Nitrogen (BUN), Glucose, Calcium, Sodium, and Potassium Levels
NCT03984838 (57) [back to overview]	Change From Baseline in Neutrophil, Lymphocyte, Leukocyte, Monocyte, Eosinophil, Basophil and Platelet Count
NCT03984838 (57) [back to overview]	Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT03984838 (57) [back to overview]	Change From Baseline in Total and Direct Bilirubin, Creatinine and Protein Levels
NCT03984838 (57) [back to overview]	Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)
NCT03984838 (57) [back to overview]	Absolute Values of Erythrocytes
NCT03984838 (57) [back to overview]	Absolute Values of BUN, Glucose, Calcium, Sodium, and Potassium Levels
NCT03984838 (57) [back to overview]	Absolute Values of Body Temperature
NCT03984838 (57) [back to overview]	Absolute Values of AST, ALT and ALP Levels
NCT03984838 (57) [back to overview]	Vz/F of RPV
NCT03984838 (57) [back to overview]	Tmax of RPV
NCT03984838 (57) [back to overview]	Tlast of RPV
NCT03984838 (57) [back to overview]	Tlag of RPV
NCT04542070 (33) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA Greater Than or Equal to (>=) 50 c/mL at Month 6/5
NCT04542070 (33) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <50 c/mL at Month 12/11 -mITT-E Population
NCT04542070 (33) [back to overview]	HIV Treatment Satisfaction Change Questionnaire (HIVTSQc) Total Score at Month 12/11
NCT04542070 (33) [back to overview]	Change From Baseline in Bone Biomarkers: Serum 25-hydroxyvitamin D (Nanomoles Per Liter (Nmol/L))
NCT04542070 (33) [back to overview]	Absolute Values of HIV Viral Load
NCT04542070 (33) [back to overview]	Absolute Values of Cluster of Differentiation 4 Plus (CD4+) Cell Count
NCT04542070 (33) [back to overview]	Percentage of Participants With Plasma Human Immunodeficiency Viruses (HIV)-1 Ribonucleic Acid (RNA) Greater Than or Equal to (>=) 50 Copies Per Milliliter (c/mL) at Month 12/11 - ITT-E Population
NCT04542070 (33) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA Less Than (<)50 c/mL at Month 12/11 - ITT-E Population
NCT04542070 (33) [back to overview]	Number of Participants With Treatment-emergent Genotypic Resistance Through Month 12/11
NCT04542070 (33) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA Greater >=50 Copies Per Milliliter (c/mL) at Month 12/11 - mITT-E Population
NCT04542070 (33) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <50 c/mL at Month 6/5 - mITT-E Population
NCT04542070 (33) [back to overview]	Percentage of Participants With Plasma HIV-1 RNA <50 c/mL at Month 6/5 - ITT-E Population
NCT04542070 (33) [back to overview]	Change From Baseline in Individual Item Scores Using HIVTSQs
NCT04542070 (33) [back to overview]	Change From Baseline in Percentage of Participants With Metabolic Syndrome at Month 12/11
NCT04542070 (33) [back to overview]	Change From Baseline in Percentage of Participants With Metabolic Syndrome at Month 6/5
NCT04542070 (33) [back to overview]	Change From Baseline in Renal Biomarker: Urine Beta-2 Microglobulin/ Creatinine (Grams Per Mole (g/Mol))
NCT04542070 (33) [back to overview]	Change From Baseline in Renal Biomarker: Urine Retinol Binding Protein 4 (Microgram Per Liter (ug/L))
NCT04542070 (33) [back to overview]	Change From Baseline in Renal Biomarker: Urine Retinol Binding Protein/Creatinine (Milligram Per Mole (mg/Mol))
NCT04542070 (33) [back to overview]	Change From Baseline in Renal Biomarkers: Specific Serum Beta-2 Microglobulin, Cystatin c, Retinol Binding Protein, Urine Beta-2 Microglobulin (Milligrams Per Liter [mg/L])
NCT04542070 (33) [back to overview]	Change From Baseline in Renal Biomarkers: Urine Phosphate (Millimoles Per Liter (mmol/L))
NCT04542070 (33) [back to overview]	Change From Baseline in Total Treatment Satisfaction Score Using HIV Treatment Satisfaction Status Questionnaire (HIVTSQs)
NCT04542070 (33) [back to overview]	Change From Month 2/1 in Dimension Scores Using Perception of Injection (PIN) Questionnaire - Q2M
NCT04542070 (33) [back to overview]	Change From Month 2/1 in Individual Item Scores Using PIN Questionnaire- Q2M
NCT04542070 (33) [back to overview]	Individual Item Scores of HIVTSQc at Month 12/11
NCT04542070 (33) [back to overview]	Number of Participants With Protocol-defined Confirmed Virologic Failure (CVF) Through Month 6/5 and 12/11
NCT04542070 (33) [back to overview]	Number of Participants With Treatment-emergent Genotypic Resistance Through Month 6/5
NCT04542070 (33) [back to overview]	Change From Baseline in Homeostasis Model of Assessment-insulin Resistance (HOMA-IR)
NCT04542070 (33) [back to overview]	Number of Participants With Treatment-emergent Phenotypic Resistance Through Month 6/5
NCT04542070 (33) [back to overview]	Percentage of Participants With Treatment Preference as Assessed Using Preference Questionnaire at Month 12/11 - Q2M
NCT04542070 (33) [back to overview]	Change From Baseline in HIV Viral Load
NCT04542070 (33) [back to overview]	Change From Baseline in CD4+ Cell Count
NCT04542070 (33) [back to overview]	Change From Baseline in Bone Biomarkers: Specific Alkaline Phosphatase, Procollagen Type 1 N-Terminal Propeptide, Type 1 Collagen Cross-linked C-telopeptide, Osteocalcin (Micrograms Per Liter (ug/L))
NCT04542070 (33) [back to overview]	Number of Participants With Treatment-emergent Phenotypic Resistance Through Month 12/11
NCT05896761 (32) [back to overview]	Number of Participants Who Discontinue Treatment Due to ISRs and AESIs-Thigh Injection Phase
NCT05896761 (32) [back to overview]	Number of Participants With Injection Site Reactions (ISRs) by Maximum Severity Grade - Thigh Injection Phase
NCT05896761 (32) [back to overview]	Number of Participants With Post-injection Pain Using Numerical Rating Scale (NRS) for CAB LA + RPV LA Q4W Arm on Week 12- Thigh Injection Phase
NCT05896761 (32) [back to overview]	Number of Participants With Post-injection Pain Using Numerical Rating Scale (NRS) for CAB LA + RPV LA Q8W Arm on Week 8- Thigh Injection Phase
NCT05896761 (32) [back to overview]	Number of Participants With Post-injection Pain Using Numerical Rating Scale (NRS) on Day 1-Thigh Injection Phase
NCT05896761 (32) [back to overview]	Number of Participants With Post-injection Pain Using Numerical Rating Scale (NRS)- Return to Gluteal Injection Phase
NCT05896761 (32) [back to overview]	Number of Participants With Their Treatment Preference as Assessed Using Preference Questionnaire for CAB LA + RPV LA Q4W Arm
NCT05896761 (32) [back to overview]	Number of Participants With Their Treatment Preference as Assessed Using Preference Questionnaire for CAB LA + RPV LA Q8W Arm
NCT05896761 (32) [back to overview]	Percentage of Participants With Plasma HIV RNA Greater Than or Equal to (>=)50 Copies/mL Over Time as Per the FDA Snapshot Algorithm- Thigh Injection Phase
NCT05896761 (32) [back to overview]	Percentage of Participants With Plasma HIV-1 Ribonucleic Acid (RNA) Less Than (<)50 Copies Per Milliliter (Copies/mL) Using the Food and Drug (FDA) Snapshot Algorithm-Thigh Injection Phase
NCT05896761 (32) [back to overview]	Number of Participants With Adverse Events of Special Interest (AESI) Based on Maximum Severity Grade- Thigh Injection Phase
NCT05896761 (32) [back to overview]	Concentration at End of Dosing Interval (Ctau) of CAB LA Following Administration of CAB LA + RPV LA Q8W
NCT05896761 (32) [back to overview]	Area Under the Concentration Curve From 0 Hours to the Time of Next Dosing (AUC [0-tau]) of CAB LA Following Administration of CAB LA + RPV LA Q4W
NCT05896761 (32) [back to overview]	Area Under the Concentration Curve From 0 Hours to the Time of Next Dosing (AUC [0-tau]) of CAB LA Following Administration of CAB LA + RPV LA Q8W
NCT05896761 (32) [back to overview]	Area Under the Concentration Curve From 0 Hours to the Time of Next Dosing (AUC [0-tau]) of RPV LA Following Administration of CAB LA + RPV LA Q4W
NCT05896761 (32) [back to overview]	Area Under the Concentration Curve From 0 Hours to the Time of Next Dosing (AUC [0-tau]) of RPV LA Following Administration of CAB LA + RPV LA Q8W
NCT05896761 (32) [back to overview]	Concentration at End of Dosing Interval (Ctau) of CAB LA Following Administration of CAB LA + RPV LA Q4W
NCT05896761 (32) [back to overview]	Concentration at End of Dosing Interval (Ctau) of RPV LA Following Administration of CAB LA + RPV LA Q4W
NCT05896761 (32) [back to overview]	HIV Treatment Satisfaction Questionnaire - Change Version (HIVTSQc) Total Score at Indicated Time Points- Thigh Injection Phase
NCT05896761 (32) [back to overview]	HIV Treatment Satisfaction Questionnaire - Status Version (HIVTSQs) Total Score at Indicated Time Points for CAB LA + RPV LA Q4W Arm -Return to Gluteal Injection Phase
NCT05896761 (32) [back to overview]	HIV Treatment Satisfaction Questionnaire - Status Version (HIVTSQs) Total Score at Indicated Time Points for CAB LA + RPV LA Q8W Arm -Return to Gluteal Injection Phase
NCT05896761 (32) [back to overview]	Maximum Plasma Concentration (Cmax) of CAB LA Following Administration of CAB LA + RPV LA Q4W
NCT05896761 (32) [back to overview]	Maximum Plasma Concentration (Cmax) of CAB LA Following Administration of CAB LA + RPV LA Q8W
NCT05896761 (32) [back to overview]	HIV Treatment Satisfaction Questionnaire - Status Version (HIVTSQs) Total Score at Indicated Time Points-Thigh Injection Phase
NCT05896761 (32) [back to overview]	Maximum Plasma Concentration (Cmax) of RPV LA Following Administration of CAB LA + RPV LA Q4W
NCT05896761 (32) [back to overview]	Maximum Plasma Concentration (Cmax) of RPV LA Following Administration of CAB LA + RPV LA Q8W
NCT05896761 (32) [back to overview]	Percentage of Participants With Protocol-defined Confirmed Virologic Failure (CVF)- Thigh Injection Phase
NCT05896761 (32) [back to overview]	Change From Baseline in HIV Treatment Satisfaction Questionnaire - Status Version (HIVTSQs) Individual Item Score at Indicated Time Points- Thigh Injection Phase
NCT05896761 (32) [back to overview]	Change From Study Week 16 to Study Week 20 in HIV Treatment Satisfaction Questionnaire - Status Version (HIVTSQs) Individual Item Score at Indicated Time Points for CAB LA + RPV LA Q4W Arm- Return to Gluteal Injection Phase
NCT05896761 (32) [back to overview]	Change From Study Week 16 to Study Week 24 in HIV Treatment Satisfaction Questionnaire - Status Version (HIVTSQs) Individual Item Score at Indicated Time Points for CAB LA + RPV LA Q8W Arm- Return to Gluteal Injection
NCT05896761 (32) [back to overview]	HIV Treatment Satisfaction Questionnaire - Change Version (HIVTSQc) Individual Item Score at Indicated Time Points- Thigh Injection Phase
NCT05896761 (32) [back to overview]	Concentration at End of Dosing Interval (Ctau) of RPV LA Following Administration of CAB LA + RPV LA Q8W

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.

Intervention	ng/mL (Median)
	3rd Trimester	Postpartum
MVC 150 or 300mg b.i.d.	448	647

Intervention	ng*hour/mL (Geometric Mean)
	2nd Trimester	3rd Trimester	Postpartum
MVC 150 or 300mg b.i.d.	NA	2717	3645

Intervention	mcg/mL (Median)
	2-10 hours after birth	18-28 hours after birth	36-72 hours after birth	5-9 days after birth
DRV/COBI 800/150 mg q.d.	0.35	1.43	1.87	1.72
DTG 50mg q.d.	1.73	1.53	1.00	0.06
EFV 600 mg q.d. (Outside THA)	1.1	1.0	0.9	0.4
EVG/COBI 150/150mg q.d.	0.132	0.032	0.005	0.005

Intervention	hour (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

Intervention	unitless (Median)
TAF 10mg q.d. w/COBI	0.97
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

Intervention	pg/mL (Median)
ATV/RTV/TFV 300/100/300mg q.d. With ENG	604
LPV/RTV 400/100 b.i.d. With ENG	428
EFV 600mg q.d. With ENG	125

Intervention	mcg*hr/mL (Median)
	Before contraceptive initiation	After contraceptive initiation
LPV/RTV 400/100 b.i.d. With ENG	115.97	100.20

Intervention	unitless (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

Intervention	Cells per microliter (Mean)
TMC278 25mg	145.9
TMC278 75 mg	172.0
TMC278 150 mg	158.9
All TMC278	159.0
Efavirenz	159.8

Intervention	Participants (Number)
AUC24h Quartile 1	48
AUC24h Quartile 2	50
AUC24h Quartile 3	55
AUC24h Quartile 4	51

Intervention	Participants (Number)
TMC278 25 mg	74
TMC278 75 mg	76
TMC278 150 mg	70
All TMC278	220
Efavirenz	72

Intervention	Participants (Number)
	Treatment-emergent NNRTI RAM	E138K	K101E	K103N	Treatment-emergent N(t)RTI RAM	M184V
All TMC278	17	7	6	1	13	10
Efavirenz	4	0	0	3	0	0

Intervention	cells per microliter (Mean)
	Absolute cell count, Week 48	Absolute cell count, Week 96	Relative cell count, Week 48	Relative cell count, Week 96
Efavirenz	181.6	226.7	8.7	10.2
TMC278	195.5	220.7	8.6	10.1

Intervention	Participants (Number)
	Any RAM from Extended NNRTI RAMs list	NNRTI RAM: E138K	NNRTI RAM: K101E	NNRTI RAM: Y181C	NNRTI RAM: V90I	NNRTI RAM: V189I	NNRTI RAM: H221Y	NNRTI RAM: E138Q	NNRTI RAM: K103N	Any RAM from IAS-USA N(t)RTI RAMs list	N(t)RTI RAM: M184I	N(t)RTI RAM: M184V	N(t)RTI RAM: K065R	N(t)RTI RAM: K219E	N(t)RTI RAM: Y115F
Efavirenz	9	0	0	0	0	0	0	0	8	5	3	3	0	0	0
TMC278	29	18	5	5	4	4	4	3	1	31	24	7	3	3	2

Intervention	Participants (Number)
	Responder	Virologic failure	Death	Discontinued due to AE	Discontinued due to other reason than AE
Efavirenz	271	16	3	29	25
TMC278	263	45	0	10	28

Intervention	Participants (Number)
	Virologic Response HIV RNA <50 copies/mL at Wk 48	Virologic Failure	No Viral Load Data in 48 week window
Efavirenz	281	24	39
TMC278	285	47	14

Intervention	Participants (Number)
	Virologic Response, <50 copies/ml	Virologic failure	No viral load data in the 96 week window
Efavirenz	268	27	49
TMC278	265	54	27

Intervention	Participants (Number)
	Responder	Virologic failure	Discontinued due to Adverse Event (AE)	Discontinued due to other reason than AE
Efavirenz	285	15	25	19
TMC278	287	38	6	15

Intervention	Participants (Number)
	Virologic response (<50 copies/mL)	Virologic failure	No plasma viral load data in 96-Week window
Efavirenz	254	38	46
TMC278	259	53	28

Intervention	Participants (Number)
	Treatment-emergent NNRTI RAM	E138K	H221Y	K101E	K103N	V90I	V106M	V189I	Y188C	Treatment-emergent N(t)RTI RAM	K65R	K219E	M184I	M184V
Efavirenz	11	1	0	2	6	1	2	0	2	6	2	0	1	3
TMC278	17	13	3	3	0	2	0	2	0	17	0	2	8	10

Intervention	Participants (Number)
	Virologic Response (<50 copies/mL)	Virologic failure	No plasma viral load data in 48-week window
Efavirenz	265	38	35
TMC278	281	41	18

rilpivirine

Cross-References

Synonyms (83)

Research Excerpts

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (2)

Drug Classes (2)

Protein Targets (12)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (80)

Molecular Functions (58)

Ceullar Components (17)

Bioassays (771)

Research

Studies (556)

Study Types

Clinical Trials (91)

Trial Overview

Trial Outcomes

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Plasma Concentration for Contraceptives

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Trough Plasma Concentration (Ctrough) for TMC278

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

Mean Change From Baseline to Week 48 and Week 96 in Absolute and Relative CD4+ Cell Counts (Using Imputed Data)

Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies/ml) at Week 96

Number of Participants With Virological Response (Observed, <50 Copies/ml) at Last On-Treatment Visit (Post-Week 96).

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

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

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

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

Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies/ml) at Week 48

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

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

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

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

Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies Per mL) at Week 96

Number of Participants With Virological Response (Intent-to-Treat - Time to Loss of Virologic Response [TLOVR], <400 Copies Per mL) at Week 48

Number of Participants With Virological Response (Observed, <50 Copies/mL) at Last On-Treatment Visit (Post-Week 96).

Intervention	Log 10 copies per milliliter (copies/mL) (Mean)
	Baseline	2nd trimester	3rd trimester	Postpartum (2-5 weeks)	Postpartum (6-12 weeks)
Darunavir 800 mg/Cobicistat 150 mg Once Daily	1.77	0.1	0.21	0.18	0.23

Intervention	Log 10 copies per milliliter (copies/mL) (Mean)
	Baseline	4 Weeks after Baseline	2nd trimester	3rd trimester	Postpartum (2-5 weeks)	Postpartum (6-12 weeks)
Darunavir 600 mg /Ritonavir 100 Twice Daily	2.12	-0.26	-0.19	-0.31	-0.18	0.09
Darunavir 800 mg /Ritonavir 100 mg Once Daily	1.88	-0.27	-0.16	-0.23	-0.04	0.11
Etravirine 200 mg Twice Daily	2.06	0.18	0.16	0.17	0.13	0.05
Rilpivirine 25 mg Once Daily	1.84	0.20	0.16	0.25	0.20	0.08

Intervention	nanogram per milliliter (ng/mL) (Mean)
	Postpartum (6-12 W)	2nd Trimester	3rd Trimester
Cobicistat 150 mg (Darunavir 800/Cobicistat 150 mg) Once Daily	41.4	NA	NA
Darunavir 600 mg (Darunavir 600/Ritonavir 100 mg) Twice Daily	2851	1922	2661
Darunavir 800 mg (Darunavir 800/Cobicistat 150 mg) Once Daily	1538	168	184
Darunavir 800 mg (Darunavir 800/Ritonavir 100 mg) Once Daily	1473	1248	1075
Etravirine 200 mg Twice Daily	269	383	349
Rilpivirine 25 mg Once Daily	84.0	54.3	52.9
Ritonavir 100 mg (Darunavir 600/Ritonavir 100 mg) Twice Daily	264.7	141.1	148.1
Ritonavir 100 mg (Darunavir 800/Ritonavir 100 mg) Once Daily	40.5	32.2	28.0

Intervention	nanogram per milliliter (ng/mL) (Mean)
	Cord Plasma	Maternal Plasma
Cobicistat 150 mg (Darunavir 800/Cobicistat 150 mg) Once Daily	NA	74.5
Darunavir 600 mg (Darunavir 600/Ritonavir 100 mg) Twice Daily	348.4	2149
Darunavir 800 mg (Darunavir 800/Cobicistat 150 mg) Once Daily	125	857
Darunavir 800 mg (Darunavir 800/Ritonavir 100 mg) Once Daily	228	1663
Etravirine 200 mg Twice Daily	147	421
Rilpivirine 25 mg Once Daily	32.8	59.0
Ritonavir 100 mg (Darunavir 600/Ritonavir 100 mg) Twice Daily	17.07	316.7
Ritonavir 100 mg (Darunavir 800/Ritonavir 100 mg) Once Daily	NA	154

Intervention	Participants (Number)
	Any AE	Any SAE
Darunavir 600 mg /Ritonavir 100 Twice Daily	14	6
Darunavir 800 mg /Ritonavir 100 mg Once Daily	17	6
Darunavir 800 mg/Cobicistat 150 mg Once Daily	5	1
Etravirine 200 mg Twice Daily	12	4
Rilpivirine 25 mg Once Daily	9	4

Intervention	Participants (Number)
	2nd trimester Less than(<)50 copies/milliLiter(mL)	3rd trimester: <50 copies/mL	Postpartum (2-5 weeks): <50 copies/mL	Postpartum (6-12 weeks): <50 copies/mL
Darunavir 600 mg /Ritonavir 100 Twice Daily	6	5	5	6
Darunavir 800 mg /Ritonavir 100 mg Once Daily	9	8	8	7
Darunavir 800 mg/Cobicistat 150 mg Once Daily	6	5	5	5
Etravirine 200 mg Twice Daily	12	10	9	8
Rilpivirine 25 mg Once Daily	13	13	9	10

Intervention	days (Mean)
	>= 50 copies/mL	>= 200 copies/mL
Rilpivirine (RPV) (TMC278-C204 [C204])	1670.6	1901.3
RPV (TMC278-TiDP6-C209 [C209] and TMC278-TiDP6-C215 [C215])	1939.3	1877.3

Intervention	cells/microliter (cells/mcL) (Mean)
	Week 96	Week 192	Week 288	Week 336
Rilpivirine (RPV) (TMC278-C204 [C204])	72.63	148.76	122.29	161.73
RPV (TMC278-TiDP6-C209 [C209] and TMC278-TiDP6-C215 [C215])	55.91	132.73	101.50	76.49

Intervention	Participants (Count of Participants)
	Baseline; n=57, 55, 56, 52	Week 4; n=54, 52, 53, 50	Week 8; n=53, 50, 56, 48	Week 12; n=55, 48, 53, 48	Week 16; n=53, 51, 53, 44	Week 20; n=51, 49, 55, 44	Week 24; n=51, 46, 51, 43	Week 28; n=49, 48, 53, 41	Week 32; n=47, 48, 55, 41	Week 36; n=46, 48, 50, 41	Week 40; n=38, 35, 45, 39	Week 48; n=33, 37, 45, 35	Week 60; n=38, 38, 40, 37	Week 72; n=35, 37, 44, 32	Week 84; n=36, 39, 42, 33
Efavirenz 600 mg	48	44	47	43	42	41	39	35	37	36	34	33	35	27	29

Intervention	Giga cells per liter (Mean)
	T. neutrophils; Week 2; n=57, 56, 59, 59	T. neutrophils; Week 4; n=57, 57, 59, 57	T. neutrophils; Week 8; n=58, 56, 56, 55	T. neutrophils; Week 12; n=58, 53, 57, 51	T. neutrophils; Week 16; n=57, 54, 57, 52	T. neutrophils; Week 20; n=56, 54, 55, 49	T. neutrophils; Week 24; n=56, 53, 56, 47	T. neutrophils; Week 26; n=48, 50, 53, 45	T. neutrophils; Week 28; n=50, 52, 52, 45	T. neutrophils; Week 32; n=51, 53, 55, 45	T. neutrophils; Week 36; n=52, 53, 55, 44	T. neutrophils; Week 40; n=51, 53, 55, 45	T. neutrophils; Week 48; n=51, 53, 54, 44	T. neutrophils; Week 60; n=48, 47, 52, 44	T. neutrophils; Week 72; n=47, 48, 52, 42	T. neutrophils; Week 84; n=46, 48, 51, 42	T. neutrophils; Week 96; n=46, 46, 52, 41	Platelet count; Week 2; n=57, 56, 59, 59	Platelet count; Week 4; n=57, 57, 59, 57	Platelet count; Week 8; n=58, 56, 56, 55	Platelet count; Week 12; n=58, 53, 57, 51	Platelet count; Week 16; n=57, 54, 57, 52	Platelet count; Week 20; n=56, 54, 55, 49	Platelet count; Week 24; n=56, 53, 56, 47	Platelet count; Week 26; n=48, 50, 53, 45	Platelet count; Week 28; n=50, 52, 52, 45	Platelet count; Week 32; n=51, 52, 55, 45	Platelet count; Week 36; n=52, 53, 55, 44	Platelet count; Week 40; n=51, 53, 54, 45	Platelet count; Week 48; n=51, 52, 53, 44	Platelet count; Week 60; n=48, 47, 51, 44	Platelet count; Week 72; n=47, 48, 52, 42	Platelet count; Week 84; n=46, 48, 51, 42	Platelet count; Week 96; n=46, 45, 51, 41	WBC count; Week 2; n=57, 56, 59, 59	WBC count; Week 4; n=57, 57, 59, 57	WBC count; Week 8; n=58, 56, 56, 55	WBC; Week 12; n=58, 53, 57, 51	WBC count; Week 16; n=57, 54, 57, 52	WBC count; Week 20; n=56, 54, 55, 49	WBC count; Week 24; n=56, 53, 56, 47	WBC count; Week 26; n=48, 50, 53, 45	WBC count; Week 28; n=50, 52, 52, 45	WBC count; Week 32; n=51, 53, 55, 45	WBC count; Week 36; n=52, 53, 55, 44	WBC count; Week 40; n=51, 53, 55, 45	WBC count; Week 48; n=51, 53, 54, 44	WBC count; Week 60; n=48, 47, 52, 44	WBC count; Week 72; n=47, 48, 52, 42	WBC count; Week 84; n=46, 48, 51, 42	WBC count; Week 96; n=46, 46, 52, 41
Efavirenz 600 mg	0.716	0.375	0.273	0.525	0.367	0.740	0.637	0.449	0.446	0.717	0.414	0.730	0.665	0.800	0.892	0.790	0.831	17.1	15.6	10.3	11.2	9.3	17.1	23.9	17.5	17.2	13.8	12.3	18.9	20.6	30.8	28.3	18.9	17.5	0.69	0.29	0.27	0.54	0.36	0.78	0.55	0.35	0.39	0.71	0.36	0.75	0.73	0.95	1.02	0.95	0.92