dapivirine profile

Dapivirine: effectively prevented human immunodeficiency virus (HIV) infection in cocultures of monocyte-derived dendritic cells and T cells, representing primary targets in sexual transmission [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	214347
CHEMBL ID	70663
SCHEMBL ID	383370
MeSH ID	M0461044

Synonym
benzonitrile, 4-[[4-[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]amino]-
tmc120
tmc 120
4-({4-[(2,4,6-trimethylphenyl)amino]pyrimidin-2-yl}amino)benzenecarbonitrile
dapivirinum
tmc120-r147681
gel-002
dapivirine
r 147681
r147681 ,
tmc-120/r-147681
4-[[4-(2,4,6-trimethylanilino)pyrimidin-2-yl]amino]benzonitrile
4-[4-(2,4,6-trimethyl-phenylamino)-pyrimidin-2-ylamino]-benzonitrile
tmc-120
r-147681
DB08639
gel-02
aids-105293
CHEMBL70663
244767-67-7
FT-0665472
ring-004
dapivirine [usan:inn]
tcn4mg2vxs ,
unii-tcn4mg2vxs
4-((4-((2,4,6-trimethylphenyl)amino)pyrimidin-2-yl)amino)benzonitrile
dapivirine intravaginal ring
4-({4-[(2,4,6-trimethylphenyl)amino]pyrimidin-2-yl}amino)benzonitrile
dapivirine [who-dd]
dapivirine [usan]
dapivirine [inn]
S2914
HY-14266
AKOS016513117
ILAYIAGXTHKHNT-UHFFFAOYSA-N
4-[[4-[(2,4,6trimethylphenyl)amino]-2-pyrimidinyl]amino]benzonitrile
4-[[4-[(2,4,6-trimethylphenyl)-amino]-2-pyrimidinyl]amino]benzonitrile
4-[[4-[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]amino]benzonitrile
4-[[4[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]amino]benzonitrile
SCHEMBL383370
4-(4-(mesitylamino)pyrimidin-2-ylamino)benzonitrile
4-((4-(mesitylamino)pyrimidin-2-yl)amino)benzonitrile
AC-30627
dapivirine (tmc120)
DTXSID40179244
J-690269
EX-A115
HMS3651J10
mfcd09833899
NCGC00371120-06
dapivirine,tmc-120
SW220193-1
dapivirine,4-[[4-(2,4,6-trimethylphenyl)amino]pyrimidin-2-yl]amino]benzonitrile
dapivirine(tmc120)
BCP06491
DT-0051
Q27097831
dapivirine (usan/inn)
D11246
SB16698
CCG-267802
tmc120;r147681
bdbm50467334

Excerpt	Reference	Relevance
"The dapivirine vaginal ring is a novel topical PrEP delivery method."	( Correlates of Adherence to the Dapivirine Vaginal Ring for HIV-1 Prevention. Baeten, JM; Brown, ER; Dadabhai, SS; Gaffoor, Z; Husnik, MJ; Jeenarain, N; Kiweewa, FM; Livant, E; Mansoor, LE; Mirembe, BG; Palanee-Phillips, T; Singh, D; Siva, S; Soto-Torres, L; van der Straten, A, 2021)	1.39
"Dapivirine (DPV) is a nonnucleoside reverse transcriptase inhibitor with a favorable safety profile following vaginal application. "	( A randomized male tolerance study of dapivirine gel following multiple topical penile exposures (MTN 012/IPM 010). Carballo-Diéguez, A; Cranston, RD; Hall, W; Hendrix, CW; Hoesley, C; Husnik, M; Levy, L; Nel, AM; Soto-Torres, L, 2014)	2.12
"Dapivirine is a non-nucleoside reverse transcriptase inhibitor designed to prevent HIV-1 viral replication and subsequent propagation. "	( The development and validation of an UHPLC-MS/MS method for the rapid quantification of the antiretroviral agent dapivirine in human plasma. Emory, JF; Hendrix, CW; Marzinke, MA; Seserko, LA, 2013)	2.04
"Dapivirine is a nonnucleoside reverse transcriptase inhibitor being developed as a topical microbicide for the prevention of human immunodeficiency virus infection. "	( Concentrations of dapivirine in the rhesus macaque and rabbit following once daily intravaginal administration of a gel formulation of [14C]dapivirine for 7 days. Ferkany, JW; Lewis, MG; Mitchnick, MA; Nuttall, JP; Romano, JW; Thake, DC, 2008)	2.12

Excerpt	Reference	Relevance
"The dapivirine vaginal ring has a safety and pharmacokinetic profile that supports its use as a sustained-release topical microbicide for HIV-1 prevention in women."	( A safety and pharmacokinetic trial assessing delivery of dapivirine from a vaginal ring in healthy women. Haazen, W; Nel, A; Nuttall, J; Romano, J; Rosenberg, Z; van Niekerk, N, 2014)	1.21
"The dapivirine vaginal ring has a favourable safety and acceptability profile. "	( Safety, Acceptability and Adherence of Dapivirine Vaginal Ring in a Microbicide Clinical Trial Conducted in Multiple Countries in Sub-Saharan Africa. Bekker, LG; Bukusi, E; Hellstrӧm, E; Kotze, P; Louw, C; Martinson, F; Masenga, G; Montgomery, E; Ndaba, N; Nel, A; van der Straten, A; van Niekerk, N; Woodsong, C, 2016)	1.26
"The dapivirine vaginal ring has been well-tolerated and shown to prevent HIV in clinical trials. "	( Men's Sexual Experiences with the Dapivirine Vaginal Ring in Malawi, South Africa, Uganda and Zimbabwe. Chitukuta, M; Duby, Z; Garcia, M; Guma, V; Katz, AWK; Leslie, J; Mansoor, LE; Montgomery, ET; Morar, NS; Naidoo, K; Naidoo, S; Tenza, S; Tsidya, M, 2021)	1.46
"The dapivirine vaginal ring has a safety and pharmacokinetic profile that supports its use as a sustained-release topical microbicide for HIV-1 prevention in women."	( A safety and pharmacokinetic trial assessing delivery of dapivirine from a vaginal ring in healthy women. Haazen, W; Nel, A; Nuttall, J; Romano, J; Rosenberg, Z; van Niekerk, N, 2014)	1.21
"The dapivirine vaginal ring has a favourable safety and acceptability profile. "	( Safety, Acceptability and Adherence of Dapivirine Vaginal Ring in a Microbicide Clinical Trial Conducted in Multiple Countries in Sub-Saharan Africa. Bekker, LG; Bukusi, E; Hellstrӧm, E; Kotze, P; Louw, C; Martinson, F; Masenga, G; Montgomery, E; Ndaba, N; Nel, A; van der Straten, A; van Niekerk, N; Woodsong, C, 2016)	1.26

Excerpt	Reference	Relevance
" The IVR was generally safe and well tolerated with similar adverse events observed in the placebo and dapivirine groups."	( Safety and availability of dapivirine (TMC120) delivered from an intravaginal ring. Coplan, P; Douville, K; Mitchnick, M; Romano, J; Rosenberg, Z; Temmerman, M; Van Bortel, L; Van Roey, J; Variano, B; Verstraelen, H; Weyers, S, 2009)	0.86
" The primary endpoints were colposcopic findings, adverse events, Division of AIDS grade 3 or grade 4 laboratory values, and plasma levels of dapivirine."	( Safety, tolerability, and systemic absorption of dapivirine vaginal microbicide gel in healthy, HIV-negative women. Coplan, P; Geubbels, E; Kapiga, SH; Kiwelu, I; Masenga, G; Moyes, J; Nel, AM; Rees, HV; Smythe, SC; van de Wijgert, JH; von Mollendorf, C; Vyankandondera, J, 2009)	0.81
" None of the adverse events with incidence more than 5% occurred with greater frequency in the dapivirine than placebo groups."	( Safety, tolerability, and systemic absorption of dapivirine vaginal microbicide gel in healthy, HIV-negative women. Coplan, P; Geubbels, E; Kapiga, SH; Kiwelu, I; Masenga, G; Moyes, J; Nel, AM; Rees, HV; Smythe, SC; van de Wijgert, JH; von Mollendorf, C; Vyankandondera, J, 2009)	0.83
"Twice daily administration of dapivirine vaginal gel for 42 days was safe and well tolerated with low systemic absorption in healthy, HIV-negative women suggesting that continued development is warranted."	( Safety, tolerability, and systemic absorption of dapivirine vaginal microbicide gel in healthy, HIV-negative women. Coplan, P; Geubbels, E; Kapiga, SH; Kiwelu, I; Masenga, G; Moyes, J; Nel, AM; Rees, HV; Smythe, SC; van de Wijgert, JH; von Mollendorf, C; Vyankandondera, J, 2009)	0.9
" Safety was assessed by pelvic/colposcopic examinations, clinical laboratory tests, and adverse events."	( Safety and pharmacokinetics of dapivirine delivery from matrix and reservoir intravaginal rings to HIV-negative women. Malcolm, K; McCoy, C; Nel, A; Romano, J; Rosenberg, Z; Smythe, S; Young, K, 2009)	0.64
" Safety was evaluated by pelvic examination, colposcopy, adverse events, and clinical laboratory assessments."	( Pharmacokinetics of 2 dapivirine vaginal microbicide gels and their safety vs. Hydroxyethyl cellulose-based universal placebo gel. Habibi, S; Kaptur, PE; Nel, AM; Romano, JW; Smythe, SC, 2010)	0.68
"The dapivirine vaginal ring was safe and well tolerated with no differences in safety endpoints between the active and placebo ring."	( A safety and pharmacokinetic trial assessing delivery of dapivirine from a vaginal ring in healthy women. Haazen, W; Nel, A; Nuttall, J; Romano, J; Rosenberg, Z; van Niekerk, N, 2014)	1.21
" Safety was assessed by adverse events."	( Phase 1 Safety, Pharmacokinetics, and Pharmacodynamics of Dapivirine and Maraviroc Vaginal Rings: A Double-Blind Randomized Trial. Chen, BA; Dezzutti, CS; Hendrix, CW; Hoesley, CJ; Husnik, MJ; Johnson, S; Marzinke, MA; Nel, A; Panther, L; Rabe, LK; Richardson-Harman, N; Soto-Torres, L; van der Straten, A, 2015)	0.66
"There was no difference in related genitourinary adverse events between treatment arms compared with placebo."	( Phase 1 Safety, Pharmacokinetics, and Pharmacodynamics of Dapivirine and Maraviroc Vaginal Rings: A Double-Blind Randomized Trial. Chen, BA; Dezzutti, CS; Hendrix, CW; Hoesley, CJ; Husnik, MJ; Johnson, S; Marzinke, MA; Nel, A; Panther, L; Rabe, LK; Richardson-Harman, N; Soto-Torres, L; van der Straten, A, 2015)	0.66
"In this first study of a combination microbicide vaginal ring, all 4 rings were safe and well tolerated."	( Phase 1 Safety, Pharmacokinetics, and Pharmacodynamics of Dapivirine and Maraviroc Vaginal Rings: A Double-Blind Randomized Trial. Chen, BA; Dezzutti, CS; Hendrix, CW; Hoesley, CJ; Husnik, MJ; Johnson, S; Marzinke, MA; Nel, A; Panther, L; Rabe, LK; Richardson-Harman, N; Soto-Torres, L; van der Straten, A, 2015)	0.66
" The proportion of participants experiencing grade 2 and higher adverse events related to study product were compared."	( A Phase 1 Trial to Assess the Safety, Acceptability, Pharmacokinetics, and Pharmacodynamics of a Novel Dapivirine Vaginal Film. Bunge, KE; Devlin, B; Dezzutti, CS; Hendrix, CW; Hillier, SL; Marzinke, MA; Meyn, LA; Moncla, BJ; Richardson-Harman, N; Rohan, LC; Spiegel, HM, 2016)	0.65
"Two grade 2 related adverse events occurred in the placebo film group."	( A Phase 1 Trial to Assess the Safety, Acceptability, Pharmacokinetics, and Pharmacodynamics of a Novel Dapivirine Vaginal Film. Bunge, KE; Devlin, B; Dezzutti, CS; Hendrix, CW; Hillier, SL; Marzinke, MA; Meyn, LA; Moncla, BJ; Richardson-Harman, N; Rohan, LC; Spiegel, HM, 2016)	0.65
" Safety was evaluated by pelvic examination, colposcopy, clinical laboratory assessments, and adverse events."	( Safety, Acceptability and Adherence of Dapivirine Vaginal Ring in a Microbicide Clinical Trial Conducted in Multiple Countries in Sub-Saharan Africa. Bekker, LG; Bukusi, E; Hellstrӧm, E; Kotze, P; Louw, C; Martinson, F; Masenga, G; Montgomery, E; Ndaba, N; Nel, A; van der Straten, A; van Niekerk, N; Woodsong, C, 2016)	0.7
" If proven safe and effective in large-scale trials, it will be an important component of combination HIV prevention approaches for women."	( Safety, Acceptability and Adherence of Dapivirine Vaginal Ring in a Microbicide Clinical Trial Conducted in Multiple Countries in Sub-Saharan Africa. Bekker, LG; Bukusi, E; Hellstrӧm, E; Kotze, P; Louw, C; Martinson, F; Masenga, G; Montgomery, E; Ndaba, N; Nel, A; van der Straten, A; van Niekerk, N; Woodsong, C, 2016)	0.7
" Serious adverse events occurred more often in the dapivirine group (in 38 participants [2."	( Safety and Efficacy of a Dapivirine Vaginal Ring for HIV Prevention in Women. Bekker, LG; Borremans, M; Carstens, H; Devlin, B; Gama, C; Gill, K; Isaacs, M; Kamali, A; Kapiga, S; Kotze, P; Kusemererwa, S; Louw, C; Mabude, Z; Malherbe, M; Mans, W; Miti, N; Nel, A; Ntshele, S; Nuttall, J; Parys, W; Resseler, S; Rosenberg, Z; Russell, M; Smit, M; Solai, L; Spence, P; Steytler, J; Tempelman, H; Van Baelen, B; van Niekerk, N; Van Roey, J; Vangeneugden, T; Windle, K, 2016)	0.99
" We assessed safety by adverse events (AEs)."	( Phase 2a Safety, Pharmacokinetics, and Acceptability of Dapivirine Vaginal Rings in US Postmenopausal Women. Chen, BA; Dezzutti, CS; Gundacker, HM; Hall, WB; Hendrix, CW; Hoesley, CJ; Jacobson, CE; Johnson, S; Marzinke, MA; McGowan, I; Nel, AM; Salata, RA; Soto-Torres, L; van der Straten, A; Zhang, J, 2019)	0.76
" Primary safety end points included grade 2 product related adverse events and any grade 3 and higher adverse events."	( Brief Report: Phase IIa Safety Study of a Vaginal Ring Containing Dapivirine in Adolescent Young Women. Bunge, KE; Futterman, D; Gaur, AH; Gorbach, PM; Hendrix, CW; Hillier, SL; Hoesley, C; Kapogiannis, B; Levy, L; Marzinke, MA; Mayer, KH; Nel, A; Reirden, D; Soto-Torres, L; Squires, KE; Szydlo, DW; Wilson, CM; Zhang, J, 2020)	0.8
" Former participants from The Ring Study, who remained HIV-negative and who did not discontinue the study due to an adverse event or safety concern that was considered to be related to the investigational product, were eligible."	( Safety, adherence, and HIV-1 seroconversion among women using the dapivirine vaginal ring (DREAM): an open-label, extension study. Bekker, LG; Carter, A; Craig, C; Devlin, B; Gill, K; Gwetu, T; Kotze, P; Kusemererwa, S; Louw, C; Mabude, Z; Malherbe, M; Mans, W; Moraba, R; Nel, A; Rosenberg, Z; Steytler, J; Tempelman, H; Van Baelen, B; van der Ryst, E; van Niekerk, N, 2021)	0.86
" 616 (65·5%) of 941 participants reported treatment-emergent adverse events."	( Safety, adherence, and HIV-1 seroconversion among women using the dapivirine vaginal ring (DREAM): an open-label, extension study. Bekker, LG; Carter, A; Craig, C; Devlin, B; Gill, K; Gwetu, T; Kotze, P; Kusemererwa, S; Louw, C; Mabude, Z; Malherbe, M; Mans, W; Moraba, R; Nel, A; Rosenberg, Z; Steytler, J; Tempelman, H; Van Baelen, B; van der Ryst, E; van Niekerk, N, 2021)	0.86
" No serious adverse events or grade 3 or higher adverse events observed were assessed as related to the DVR."	( Safety, uptake, and use of a dapivirine vaginal ring for HIV-1 prevention in African women (HOPE): an open-label, extension study. Baeten, JM; Balán, IC; Brown, ER; Bunge, K; Chinula, L; Chirenje, ZM; Garcia, M; Gati Mirembe, B; Govender, V; Hendrix, CW; Hillier, SL; Hunidzarira, P; Jacobson, C; Jiao, Y; Jones, J; Livant, E; Makanani, B; Mansoor, LE; Mayo, AJ; Mellors, JW; Mgodi, NM; Mhlanga, F; Naidoo, L; Nair, G; Nakabiito, C; Nel, A; Ngure, K; Palanee-Phillips, T; Parikh, UM; Patterson, K; Peda, M; Ramjee, G; Rosenberg, Z; Scheckter, R; Singh, D; Singh, N; Siva, S; Soto-Torres, LE; Szydlo, DW; Taha, TE; Torjesen, K; van der Straten, A, 2021)	0.91
" Safety was assessed by recording adverse events (AEs)."	( Phase 1 pharmacokinetics and safety study of extended duration dapivirine vaginal rings in the United States. Beamer, M; Bunge, K; Devlin, B; Dominguez Islas, C; Gundacker, H; Harrell, T; Hendrix, CW; Hoesley, C; Jacobson, CE; Liu, AY; Marzinke, MA; McClure, T; Neradilek, B; Nuttall, J; Piper, JM; Spence, P; Steytler, J; van der Straten, A, 2021)	0.86
" The primary safety endpoint was grade 2 or higher adverse events during each randomised period of 24 weeks of ring and oral PrEP."	( Adherence, safety, and choice of the monthly dapivirine vaginal ring or oral emtricitabine plus tenofovir disoproxil fumarate for HIV pre-exposure prophylaxis among African adolescent girls and young women: a randomised, open-label, crossover trial. Akello, CA; Anderson, P; Baeten, JM; Bekker, LG; Brown, ER; Bunge, K; Celum, C; Garcia, M; Hendrix, C; Hillier, SL; Hosek, S; Jacobson, C; Johnson, S; Levy, L; Livant, E; Macdonald, P; McClure, T; Milan, G; Muhlanga, F; Nair, G; Nakabiito, C; Nakalega, R; Ngure, K; Palanee-Phillips, T; Parikh, U; Reddy, K; Rooney, JF; Siziba, B; Soto-Torres, L; Steytler, J; Szydlo, D; Tahuringana, E; van der Straten, A, 2023)	1.17
" 54 grade 2 or higher product-related adverse events were reported during oral PrEP and five during dapivirine ring use, with no product-related serious adverse events."	( Adherence, safety, and choice of the monthly dapivirine vaginal ring or oral emtricitabine plus tenofovir disoproxil fumarate for HIV pre-exposure prophylaxis among African adolescent girls and young women: a randomised, open-label, crossover trial. Akello, CA; Anderson, P; Baeten, JM; Bekker, LG; Brown, ER; Bunge, K; Celum, C; Garcia, M; Hendrix, C; Hillier, SL; Hosek, S; Jacobson, C; Johnson, S; Levy, L; Livant, E; Macdonald, P; McClure, T; Milan, G; Muhlanga, F; Nair, G; Nakabiito, C; Nakalega, R; Ngure, K; Palanee-Phillips, T; Parikh, U; Reddy, K; Rooney, JF; Siziba, B; Soto-Torres, L; Steytler, J; Szydlo, D; Tahuringana, E; van der Straten, A, 2023)	1.39
"In this first study of a long-acting HIV prevention agent in pregnancy, adverse pregnancy outcomes and complications were uncommon when DVR and TDF/FTC were used in the third trimester of pregnancy, suggesting a favorable safety profile for both prevention products."	( DELIVER: A Safety Study of a Dapivirine Vaginal Ring and Oral PrEP for the Prevention of HIV During Pregnancy. Balkus, JE; Bunge, K; Chakhtoura, N; Chappell, CA; Fairlie, L; Gadama, L; Hillier, SL; Matrimbira, M; Mayo, AJ; Mgodi, N; Nakabiito, C; Piper, J; Richardson, B; Szydlo, DW, 2024)	1.73

Excerpt	Reference	Relevance
" Blood and vaginal fluid samples were collected sequentially over 24 days for pharmacokinetic analysis."	( Pharmacokinetics of 2 dapivirine vaginal microbicide gels and their safety vs. Hydroxyethyl cellulose-based universal placebo gel. Habibi, S; Kaptur, PE; Nel, AM; Romano, JW; Smythe, SC, 2010)	0.68
" Participants were followed during and for 28 days after ring use for safety and pharmacokinetic evaluations."	( A safety and pharmacokinetic trial assessing delivery of dapivirine from a vaginal ring in healthy women. Haazen, W; Nel, A; Nuttall, J; Romano, J; Rosenberg, Z; van Niekerk, N, 2014)	0.65
" Dapivirine vaginal fluid concentrations were highest near the ring, followed by the cervix and introïtus (mean Cmax of 80, 67 and 31 μg/g, respectively)."	( A safety and pharmacokinetic trial assessing delivery of dapivirine from a vaginal ring in healthy women. Haazen, W; Nel, A; Nuttall, J; Romano, J; Rosenberg, Z; van Niekerk, N, 2014)	1.56
"The dapivirine vaginal ring has a safety and pharmacokinetic profile that supports its use as a sustained-release topical microbicide for HIV-1 prevention in women."	( A safety and pharmacokinetic trial assessing delivery of dapivirine from a vaginal ring in healthy women. Haazen, W; Nel, A; Nuttall, J; Romano, J; Rosenberg, Z; van Niekerk, N, 2014)	1.21
" We performed a 3-month general toxicology study, a preliminary pharmacokinetic study using drug-loaded vaginal gel, and a detailed assessment of the kinetics of dapivirine delivery to plasma, vaginal, and rectal fluid and rectal, vaginal, and cervical tissue over 28 days of exposure and 3 and 7 days after removal of the ring."	( The sheep as a model of preclinical safety and pharmacokinetic evaluations of candidate microbicides. Cameron, D; Dias, N; Dreier, P; Holding, J; Holt, JD; Muntendam, A; Nuttall, J; Oostebring, F; Rohan, L, 2015)	0.61
" Fresh and cryopreserved tissues were evaluated for human immunodeficiency virus (HIV) infection and pharmacokinetic (PK)/pharmacodynamic (PD) relationships."	( Pharmacodynamic correlations using fresh and cryopreserved tissue following use of vaginal rings containing dapivirine and/or maraviroc in a randomized, placebo controlled trial. Chen, BA; Dezzutti, CS; Hoesley, CJ; Johnson, S; Marzinke, MA; Nel, A; Nuttall, JP; Panther, L; Richardson-Harman, N; Rohan, LC, 2016)	0.65
" Clinical, pharmacokinetic, and antiviral pharmacodynamic assessments (ex vivo HIV-BaL challenge of tissue explants) were performed over 168 h postdose."	( Comparison of Dapivirine Vaginal Gel and Film Formulation Pharmacokinetics and Pharmacodynamics (FAME 02B). Aung, W; Bakshi, RP; Coleman, JS; Fuchs, EJ; Hendrix, CW; Marzinke, MA; Radebaugh, CL; Robinson, JA; Rohan, LC; Spiegel, HM, 2017)	0.82
"A physiologically-based pharmacokinetic (PBPK) model of the vaginal space was developed with the aim of predicting concentrations in the vaginal and cervical space."	( Physiologically-based pharmacokinetic model of vaginally administered dapivirine ring and film formulations. Bies, R; Kay, K; Rohan, L; Shah, DK, 2018)	0.71
" These results suggest that ring placement and fit is an important species-specific study parameter that should be optimised prior to pharmacokinetic testing."	( Impact of ring size and drug loading on the pharmacokinetics of a combination dapivirine-darunavir vaginal ring in cynomolgus macaques. Boyd, P; Caldwell, A; Dereuddre-Bosquet, N; Desjardins, D; Kelly, C; Le Grand, R; Malcolm, RK; Murphy, DJ; Stimmer, L; van Roey, J, 2018)	0.71
" Given the reassuring safety and pharmacokinetic data, the DPV VR is promising for preexposure prophylaxis in postmenopausal women."	( Phase 2a Safety, Pharmacokinetics, and Acceptability of Dapivirine Vaginal Rings in US Postmenopausal Women. Chen, BA; Dezzutti, CS; Gundacker, HM; Hall, WB; Hendrix, CW; Hoesley, CJ; Jacobson, CE; Johnson, S; Marzinke, MA; McGowan, I; Nel, AM; Salata, RA; Soto-Torres, L; van der Straten, A; Zhang, J, 2019)	0.76
" Also, we report the pharmacokinetic testing of this combination ring formulation in sheep, where vaginal concentrations of both drugs are maintained over 28 days at levels potentially useful for preventing HIV infection in women."	( Development and pharmacokinetics of a combination vaginal ring for sustained release of dapivirine and the protein microbicide 5P12-RANTES. Boyd, P; Cameron, D; Devlin, B; Dias, N; Hartley, O; Kett, VL; Malcolm, RK; McBride, JW; Offord, RE, 2019)	0.74

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
" Lactobacillus crispatus actively transported tenofovir leading to a loss in drug bioavailability and culture supernatants from Gardnerella vaginalis, but not Atopobium vaginae, blocked tenofovir endocytosis."	( Vaginal microbiome modulates topical antiretroviral drug pharmacokinetics. Cameron, SA; Cheshenko, N; Frank, B; Fredricks, D; Herold, BC; Keller, MJ; Mesquita, PM; Reagle, K; Sinclair, S; Srinivasan, S; Taneva, E; Weinrick, B, 2018)	0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" IVRs provide a long-term dosing alternative to hydrogel use, and might provide improved user adherence."	( Compartmental transport model of microbicide delivery by an intravaginal ring. Geonnotti, AR; Katz, DF, 2010)	0.36
"The Microbicide Trials Network 003 study, a large phase IIb trial, was unable to show that daily dosing with 1% tenofovir vaginal gel was effective for HIV prevention."	( Current status of topical antiretroviral chemoprophylaxis. Szpir, M; Van Damme, L, 2012)	0.38
" Phase II and III trials continue to explore different dosing strategies for topical products that contain one or more ARV agents."	( Current status of topical antiretroviral chemoprophylaxis. Szpir, M; Van Damme, L, 2012)	0.38
" This paper reviews dapivirine ring's pipeline development process, including efforts to determine safe and effective dosing levels as well as identify delivery platforms with the greatest likelihood of success for correct and consistent use."	( Development of dapivirine vaginal ring for HIV prevention. Devlin, B; Nuttall, J; Rosenberg, Z; Wilder, S; Woodsong, C, 2013)	1.07
"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
" A dosage form containing DPV must be able to deliver the drug to the tissue site of action."	( Increased Dapivirine tissue accumulation through vaginal film codelivery of dapivirine and Tenofovir. Akil, A; Cost, M; Devlin, B; Rohan, LC, 2014)	0.8
"Polymeric films can be used as a stable dosage form for the delivery of antiretroviral combinations as microbicides."	( Formulation and characterization of polymeric films containing combinations of antiretrovirals (ARVs) for HIV prevention. Agashe, H; Akil, A; Devlin, B; Dezzutti, CS; Hillier, SL; Moncla, BJ; Rohan, LC; Shi, Y; Uranker, K, 2015)	0.42
" Dapivirine, a non-nucleoside reverse transcriptase inhibitor, is one of the leading drug candidates in the field, currently being tested in various dosage forms, namely vaginal rings, gels, and films."	( Will dapivirine redeem the promises of anti-HIV microbicides? Overview of product design and clinical testing. das Neves, J; Martins, JP; Sarmento, B, 2016)	1.86
"Multipurpose prevention technologies (MPTs) are preferably single dosage forms designed to simultaneously address multiple sexual and reproductive health needs, such as unintended pregnancy, HIV infection and other sexually transmitted infections (STIs)."	( Development of a multi-layered vaginal tablet containing dapivirine, levonorgestrel and acyclovir for use as a multipurpose prevention technology. Brimer, A; Devlin, B; Major, I; McConville, C, 2016)	0.68
" Data were log-transformed and analyzed by linear least squared regression, nonlinear Emax dose-response model and Satterthwaite t test."	( Pharmacodynamic correlations using fresh and cryopreserved tissue following use of vaginal rings containing dapivirine and/or maraviroc in a randomized, placebo controlled trial. Chen, BA; Dezzutti, CS; Hoesley, CJ; Johnson, S; Marzinke, MA; Nel, A; Nuttall, JP; Panther, L; Richardson-Harman, N; Rohan, LC, 2016)	0.65
"Although a number of drugs have been developed for the treatment and prevention of human immunodeficiency virus (HIV) infection, it has proven difficult to optimize the drug and dosage parameters."	( Pharmacokinetic modeling of a gel-delivered dapivirine microbicide in humans. Frieboes, HB; Halwes, ME; Steinbach-Rankins, JM, 2016)	0.7
" No infants were exposed to the drug, but infant dosage was estimated according to FDA guidance."	( Pharmacokinetics of Dapivirine Transfer into Blood Plasma, Breast Milk, and Cervicovaginal Fluid of Lactating Women Using the Dapivirine Vaginal Ring. Beigi, RH; Bogen, DL; Bunge, K; Dezzutti, CS; Hendrix, CW; Hillier, SL; Hoesley, C; Kelly, C; Marzinke, MA; Nel, A; Noguchi, LM; Piper, JM; Scheckter, R, 2019)	0.84
" This work presents a new opportunity to increase the release of poorly water-soluble compounds or to achieve desired dosing levels using lower drug loadings than those required using conventional thermoplastic processing techniques."	( Dapivirine-releasing vaginal rings produced by plastic freeforming additive manufacturing. Boyd, P; Devlin, B; Malcolm, RK; Welsh, NR, 2019)	1.96

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	0.8487	0.0123	7.9835	43.2770	AID1645841
G	Vesicular stomatitis virus	Potency	3.7908	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	10.6840	0.0010	8.3798	61.1304	AID1645840
Interferon beta	Homo sapiens (human)	Potency	3.7908	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	3.7908	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	3.7908	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	3.7908	0.0123	8.9648	39.8107	AID1645842
[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)
Kappa-type opioid receptor	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	0.3220	0.0003	0.7123	7.0700	AID573468
Reverse transcriptase/RNaseH	Human immunodeficiency virus 1	IC50 (µMol)	0.9303	0.0001	1.0768	10.0000	AID1421303; AID1421304; AID1421305; AID1421306; AID1421307; AID1421308; AID1421309; AID518734; AID518735; AID518737; AID518738; AID573464; AID573465; AID573466; AID573468; AID573469; AID573470; AID620437
[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)
Acetylcholinesterase	Rattus norvegicus (Norway rat)	ID50	1.0000	0.0800	0.0800	0.0800	AID650690
Reverse transcriptase/RNaseH	Human immunodeficiency virus 1	ID50	0.3108	0.0060	2.1898	9.0000	AID1574384; AID1574385; AID1574386; AID1574387; AID650688; AID650689; AID650690; AID650691; AID650692; AID663305; AID663306; AID663307; AID663308; AID663310
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (313)

Assay ID	Title	Year	Journal	Article
AID518737	Inhibition of DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by gel-based primer extension assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID650691	Inhibition of wild type HIV1 NL4-3 reverse transcriptase assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID581811	Antiviral activity against X4 tropic HIV1 3B infected in human TZM-b1 cells after 2 hrs by luciferase assay	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID246300	Effective concentration of the compound to inhibit HIV-1 mutant Y181C replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID663296	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1157581	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1574376	Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1157584	Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID83550	Potency evaluated against NNRTI-Resistant HIV-1 strain Lys103Asn	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID449191	Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for HIV1 NL4-3	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID620430	Cytotoxicity against human TZM-b1 cells infected with wild type HIV1 BaL after 48 hrs using formazan dye by WST1 assay	2011	Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20	Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID571981	Antiviral activity against HIV-1 subtype B V022813 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1157586	Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID717417	Ratio of EC50 for HIV1 harboring reverse transcriptase VI829/Y181C mutant to EC50 for HIV1 harboring reverse transcriptase V106A mutant	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
AID717422	Selectivity index, ratio of CC50 for human TZM-b1 cells to EC50 for HIV1	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
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.
AID571976	Antiviral activity against HIV-1 subtype B V022807 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID518738	Inhibition of DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by gel-based primer extension assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1157601	Antiviral activity against HIV1 CRF02 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1157608	Antiviral activity against HIV1 infected in human MT4 cells assessed as lowest compound concentration required to irreversibly knock out vial multiplication treated 4 hrs after infection measured after 40 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1157597	Antiviral activity against HIV1 MP582 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID620429	Antiviral activity against wild type HIV1 BaL in human TZM-b1 cells after 48 hrs by luciferase assay	2011	Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20	Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID571978	Antiviral activity against HIV-1 subtype B V022810 harboring NNRTI A98S andK101R mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID246256	Effective concentration against human immunodeficiency virus type 1Y181C 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).
AID518742	Selectivity ratio of EC50 for antiviral activity against HIV 1 subtype B harboring reverse transcriptase M230L mutant to EC50 for antiviral activity against HIV 1 subtype B harboring wild type reverse transcriptase	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID83551	Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr181Cys	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID581819	Antiviral activity against HIV1 A17 harboring reverse transcriptase K103N, Y181C mutant infected in human TZM-b1 cells after 2 hrs by luciferase assays	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
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.
AID1157582	Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID246299	Effective concentration of the compound to inhibit HIV-1 mutant L100I replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID572197	Antiviral activity against HIV-1 Bal infected in 2 hrs 100 nM compound pretreated human ectocervical explant tissue assessed as prolonged inhibition of viral infection post compound removal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID246362	Effective concentration against rhuman 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).
AID572181	Antiviral activity against HIV-1 SM007 harboring NNTRI 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1157595	Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID663315	Resistance ratio of ID50 for HIV1 reverse transcriptase Y188L mutant to ID50 HIV1 wild type reverse transcriptase	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID246344	Effective concentration of the compound to inhibit HIV-1 mutant L100I+K103N replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1421306	Inhibition of recombinant HIV1 reverse transcriptase Y181C mutant	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID246343	Effective concentration of the compound to inhibit HIV-1 mutant K103N+Y181C replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1163233	Antiviral activity against HIV1 infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hrs by	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID417447	Inhibition of HIV1 reverse transcriptase Y181C mutant	2009	European journal of medicinal chemistry, Feb, Volume: 44, Issue:2	QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
AID571983	Antiviral activity against HIV-1 subtype B V022815 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1059727	Cytotoxicity against human MT2 cells after 5 days by MTT assay	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Design, Synthesis, and Antiviral Evaluation of Chimeric Inhibitors of HIV Reverse Transcriptase.
AID573471	Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID571967	Antiviral activity against HIV-1 subtype CRF02_AG V022808 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1574387	Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 L100I mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID417446	Inhibition of HIV1 reverse transcriptase L100I mutant	2009	European journal of medicinal chemistry, Feb, Volume: 44, Issue:2	QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
AID106053	Inhibitory activity against 100I strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID572178	Antiviral activity against HIV-1 subtype H V029523 harboring NNRTI K101Q and V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID417449	Hydrophobic index, Log P of the compound	2009	European journal of medicinal chemistry, Feb, Volume: 44, Issue:2	QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
AID1157587	Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID573474	Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5269 by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID766430	Aqueous solubility of the compound at pH 6.5 by shake-flask method	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.
AID572173	Antiviral activity against HIV-1 subtype CRF05_DF V022824 harboring NNRTI V106I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1157604	Antiviral activity against HIV1 MP1033 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID571952	Antiviral activity against HIV-1 Bal infected in human PM1 cells after 7 days by RT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID246283	Effective concentration of the compound to inhibit HIV-1 mutant LAI replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID581820	Antiviral activity against R5 tropic HIV1 YU.2 infected in human PBMC assessed as inhibition of p24 antigen production after 2 hrs by ELISA	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID663299	Cytotoxicity against human MT4 cells after 5 days by MTT assay	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1157580	Cytotoxicity against human MT4 cells after 96 hrs by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1290401	Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 2 days by WST-1 assay	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family.
AID620433	Antiviral activity against HIV1 BaL expressing reverse transcriptase V106A mutant infected in human TZM-bl cells after 48 hrs by luciferase assay	2011	Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20	Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID1163255	Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID572195	Antiviral activity against HIV-1 Bal infected in human PM1 cells assessed as inhibition of transmission of virus to premissive T cells at 100 uM	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1574381	Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV-1 NL4-3	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID663309	Inhibition of HIV1 recombinant reverse transcriptase V106A mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID572202	Antiviral activity against HIV-1 Bal infected in 24 hrs 100 to 1000 nM compound pretreated human ectocervical explant tissue assessed as prolonged inhibition of viral infection post compound removal measured after 2 days post compound removal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1157585	Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID620436	Ratio of EC50 for HIV1 VI829 expressing reverse transcriptase Y181C mutant infected in human TZM-b1 cells to EC50 for wild type HIV1 VI829 in human TZM-b1 cells	2011	Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20	Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID572177	Antiviral activity against HIV-1 subtype H V022828 harboring NNRTI K101Q and V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1421305	Inhibition of recombinant HIV1 reverse transcriptase K103N mutant	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID571980	Antiviral activity against HIV-1 subtype B V022812 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
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.
AID449189	Antiviral activity against HIV1 RTMDR1 infected in human TZM-bl 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.
AID571970	Antiviral activity against HIV-1 subtype CRF02_AG V022830 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
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).
AID663300	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 NL4-3	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID571941	Antiviral activity against HIV-1 Bal infected in 1 hr compound pretreated human ectocervical explant tissue assessed as inhibition of viral replication at 0.1 nM by RT-PCR	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571968	Antiviral activity against HIV-1 subtype CRF02_AG V022825 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571984	Antiviral activity against HIV-1 subtype C V022816 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID573465	Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID571954	Antiviral activity against HIV-1 3B infected in human TZM-bl cells after 7 days by RT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID650688	Inhibition of HIV 1 reverse transcriptase L100I mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID572191	Antiviral activity against HIV-1 Bal infected in 1 hr compound pretreated human ectocervical explant tissue assessed as inhibition of provirus formation at 1 nM by RT-PCR	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID581814	Antiviral activity against X4 tropic HIV1 NL4.3 infected in human TZM-b1 cells after 2 hrs by luciferase assay	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID1574372	Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID572198	Antiviral activity against HIV-1 Bal infected in 2 hrs 1000 nM compound pretreated human ectocervical explant tissue assessed as prolonged inhibition of viral infection post compound removal measured after 2 days post compound removal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID663298	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID572203	Antiviral activity against HIV-1 Bal infected in 24 hrs 100 to 1000 nM compound pretreated human ectocervical explant tissue assessed as prolonged inhibition of viral infection post compound removal measured after 4 days post compound removal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571943	Cytotoxicity against human TZM-bl cells after 24 hrs by MTT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID573475	Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5331 by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID449188	Antiviral activity against HIV1 NL4-3 infected in human TZM-bl 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.
AID717418	Antiviral activity against HIV1 harboring reverse transcriptase VI829/Y181C mutant	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
AID650696	Ratio of ID50 for HIV 1 reverse transcriptase K103N mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID571966	Antiviral activity against HIV-1 Bal infected in human TZM-bl cells after 24 hrs by luciferase reporter gene assay in presence of 12.5% cervical mucus	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID572199	Antiviral activity against HIV-1 Bal infected in 2 hrs 10000 nM compound pretreated human ectocervical explant tissue assessed as prolonged inhibition of viral infection post compound removal measured after 4 days post compound removal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID246290	Effective concentration against human immunodeficiency virus type 1 in 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).
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.
AID1574371	Therapeutic index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 NL4-3 infected in human MT4 cells	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1421307	Inhibition of recombinant HIV1 reverse transcriptase Y188L mutant	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID573466	Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID650549	Resistance ratio of EC50 for HIV 1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1574386	Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1163230	Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei brucei Squib427 assessed as reduction in parasite growth after 72 hrs	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID417450	Inhibition of HIV1 wild type reverse transcriptase	2009	European journal of medicinal chemistry, Feb, Volume: 44, Issue:2	QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
AID572200	Antiviral activity against HIV-1 Bal infected in 2 hrs 10000 nM compound pretreated human ectocervical explant tissue assessed as prolonged inhibition of viral infection post compound removal measured after 6 days post compound removal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID106057	Inhibitory activity against 103N strain and 181C strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1163234	Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID106049	Inhibitory activity against 100I strain and 103N strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1574380	Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV-1 NL4-3	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1421309	Inhibition of recombinant HIV1 reverse transcriptase K103N/Y181C double mutant	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID620437	Inhibition of wild type HIV1 reverse transcriptase	2011	Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20	Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID663306	Inhibition of HIV1 recombinant reverse transcriptase K103N mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID650542	Antiviral activity against multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant infected in human MT4 cells assessed as virus-induced cytopathic effect after 5 days by MTT assay	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
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.
AID572187	Antiviral activity against HIV-1 SM051 harboring NNTRI 100I and 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID573464	Inhibition of RNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID571960	Selectivity index, ratio of CC50 for human monocyte derived macrophages to IC50 for HIV-1 Bal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571962	Selectivity index, ratio of CC50 for human MT-4 cells to IC50 for HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1574379	Resistance index, ratio of EC50 for HIV-1 IRLL98 harboring reverse transcriptase M41L, D67N, Y181C, M184V, R211K, and T215Y mutants to EC50 for wild type HIV-1 NL4-3	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1574377	Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID581812	Antiviral activity against R5 tropic HIV1 BaL infected in human TZM-b1 cells after 2 hrs by luciferase assay	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID650548	Resistance ratio of EC50 for HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID572170	Antiviral activity against HIV-1 subtype D V022818 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID83549	Potency evaluated against NNRTI-Resistant HIV-1 strain Leu100Ile	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID581821	Antiviral activity against X4 tropic HIV1 NL4.3 infected in human PBMC assessed as inhibition of p24 antigen production after 2 hrs by ELISA	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID246245	Effective concentration against human immunodeficiency virus type 1 wild type 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).
AID106074	Inhibitory activity against LAI strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID383498	Partition coefficient, log P of the compound	2008	European journal of medicinal chemistry, Mar, Volume: 43, Issue:3	SAR and QSAR studies: modelling of new DAPY derivatives.
AID581816	Antiviral activity against X4 tropic HIV1 RF infected in human PBMC assessed as inhibition of p24 antigen production after 2 hrs by ELISA	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID571958	Selectivity index, ratio of CC50 for human TZM-bl cells to IC50 for HIV-1 Bal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID572205	Antiviral activity against HIV-1 SF162 infected in hu-SCID mouse assessed as protection from viral infection at 225 uM	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1574384	Inhibition of recombinant wild type HIV-1 His-tagged reverse transcriptase p66/p51 expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysis	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1157583	Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID767490	Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced effect	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID663305	Inhibition of HIV1 wild type recombinant reverse transcriptase assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID571964	Antiviral activity against HIV-1 Bal infected in human TZM-bl cells after 24 hrs by luciferase reporter gene assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID83553	Potency evaluated against NNRTI-Resistant HIV-1 strain Val106Ala	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID572196	Antiviral activity against HIV-1 Bal infected in human PM1 cells assessed as inhibition of transmission of virus to premissive T cells at 10 uM	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1574385	Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID572204	Antiviral activity against HIV-1 Bal infected in 24 hrs 100 to 1000 nM compound pretreated human ectocervical explant tissue assessed as prolonged inhibition of viral infection post compound removal measured after 6 days post compound removal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID106069	Inhibitory activity against 188L strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID573468	Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase DNA-dependent DNA polymerase activity by gel-based primer extension assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID571969	Antiviral activity against HIV-1 subtype CRF02_AG V022826 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571947	Cytotoxicity against human monocyte derived macrophages after 24 hrs by MTT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID572179	Antiviral activity against HIV-1 subtype O V029524 harboring NNRTI A98G, V179E and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571965	Antiviral activity against HIV-1 Bal infected in human TZM-bl cells after 24 hrs by luciferase reporter gene assay in presence of 12.5% whole semen	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID572206	Antiviral activity against HIV-1 SF162 infected in hu-SCID mouse assessed as protection from viral infection at 22.5 uM	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1574383	Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase K103N/Y181C double mutant to EC50 for wild type HIV-1 NL4-3	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
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.
AID581810	Antiviral activity against X4 tropic HIV1 RF infected in human TZM-b1 cells after 2 hrs by luciferase assay	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID663310	Inhibition of HIV1 recombinant reverse transcriptase Y188L mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1157603	Antiviral activity against HIV1 MP411 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID572172	Antiviral activity against HIV-1 subtype CRF05_DF V022823 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID573478	Antiviral activity of Human immunodeficiency virus 1 isolate 8117 harboring A98S, G190A mutation in reverse transcriptase by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID518739	Selectivity ratio of IC50 for DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant to IC50 for DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID571950	Antiviral activity against HIV-1 Bal infected in human TZM-bl cells after 7 days by RT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571985	Antiviral activity against HIV-1 subtype C V022817 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID767500	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced effect	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID573470	Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID83547	Potency evaluated against NNRTI-Resistant HIV-1 strain Gly190Ala	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID1574375	Antiviral activity against HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1574382	Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV-1 NL4-3	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID572175	Antiviral activity against HIV-1 subtype F V029522 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
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).
AID1163253	Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID650540	Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID573469	Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID573481	Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8117 harboring A98S, G190A mutation in reverse transcriptase to wild-type	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID620435	Antiviral activity against HIV1 VI829 expressing reverse transcriptase Y181C mutant infected in human TZM-bl cells after 48 hrs by luciferase assay	2011	Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20	Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID650694	Ratio of ID50 for HIV 1 reverse transcriptase Y181I mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID572193	Antiviral activity against HIV-1 Bal infected in human cervical tissue explants assessed as inhibition of dissemination of virus via migratory cells after 2 hrs in presence of 12.5% whole semen	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571944	Cytotoxicity against human MT4 cells after 24 hrs by MTT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID620432	Antiviral activity against wild type HIV1 VI829 infected in human TZM-b1 cells after 48 hrs by luciferase assay	2011	Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20	Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID1421304	Inhibition of recombinant HIV1 reverse transcriptase L100I mutant	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1157609	Antiviral activity against HIV1 infected in human MT4 cells assessed as lowest compound concentration required to irreversibly knock out vial multiplication treated 4 hrs before infection measured after 40 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID663311	Resistance ratio of ID50 for HIV1 reverse transcriptase K103N mutant to ID50 HIV1 wild type reverse transcriptase	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID571951	Antiviral activity against HIV-1 Bal infected in human MT4 cells after 7 days by RT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID449190	Cytotoxicity against human TZM-bl cells	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
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.
AID1157602	Antiviral activity against HIV1 MP634 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID572184	Antiviral activity against HIV-1 SM026 harboring NNTRI 103N and 181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID573482	Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase to wild-type	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID717414	Antiviral activity against HIV1 Ba-L harboring reverse transcriptase V106A mutant	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
AID572171	Antiviral activity against HIV-1 subtype D V022819 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID106065	Inhibitory activity against 181C strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID572190	Antiviral activity against HIV-1 Bal infected in 1 hr compound pretreated human ectocervical explant tissue assessed as inhibition of viral replication by RT-PCR	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1163231	Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei rhodesiense STIB-900 assessed as reduction in parasite growth after 72 hrs	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID518736	Selectivity ratio of IC50 for RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant to IC50 for RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
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.
AID83552	Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr188Leu	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID571986	Antiviral activity against HIV-1 subtype C V022829 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID663301	Resistance ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-3	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID573476	Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5512 by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1157600	Antiviral activity against HIV1 CRF01 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID717424	Antiviral activity against HIV1 infected in human TZM-b1 cells	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
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.
AID83554	Potency evaluated against wild type HIV-1 strain IIIB	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
AID650690	Inhibition of HIV 1 reverse transcriptase Y181I mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID572169	Antiviral activity against HIV-1 subtype D V022832 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID106061	Inhibitory activity against 103N strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID383497	Inhibition of HIV reverse transcriptase	2008	European journal of medicinal chemistry, Mar, Volume: 43, Issue:3	SAR and QSAR studies: modelling of new DAPY derivatives.
AID1574390	Resistance index, ratio of ID50 for recombinant HIV-1 His-tagged reverse transcriptase p66/p51 L100I mutant to ID50 for recombinant wild type HIV-1 reverse transcriptase His-tagged p66/p51	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID571977	Antiviral activity against HIV-1 subtype B V022809 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID572182	Antiviral activity against HIV-1 SM012 harboring NNTRI 108I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571953	Antiviral activity against HIV-1 Bal infected in human monocyte derived macrophages after 7 days by RT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571959	Selectivity index, ratio of CC50 for human PM1 cells to IC50 for HIV-1 Bal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1290408	Inhibition of recombinant HIV1 His-tagged p66/p51 reverse transcriptase expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)-oligo(dT) (12 to 18 bp) as template/primer incubated for 20 mins by scintillation counting	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family.
AID1157592	Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-in	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID717420	Antiviral activity against HIV1 harboring reverse transcriptase VI829 mutant	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
AID1157594	Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID571940	Antiviral activity against HIV-1 Bal infected in human cervical tissue explants assessed as inhibition of dissemination of virus via migratory cells after 2 hrs	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571945	Cytotoxicity against human PM1 cells after 24 hrs by MTT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
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).
AID571975	Antiviral activity against HIV-1 subtype CRF01_AE V029525 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID717419	Ratio of EC50 for HIV1 Ba-L harboring reverse transcriptase V106A mutant to EC50 for wild type HIV1 Ba-L	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
AID572174	Antiviral activity against HIV-1 subtype CRF05_DF V022833 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571961	Selectivity index, ratio of CC50 for human TZM-bl cells to IC50 for HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1290399	Antiviral activity against HIV1 NL4.3 infected in human TZM-bl cells incubated for 30 mins prior to infection measured after 48 hrs by luciferase assay	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family.
AID663308	Inhibition of HIV1 recombinant reverse transcriptase Y181I mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID581815	Antiviral activity against R5 tropic HIV1 R8.BaL infected in human TZM-b1 cells after 2 hrs by luciferase assay	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
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.
AID246298	Effective concentration of the compound to inhibit HIV-1 mutant K103N replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID663302	Resistance ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-3	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID573479	Antiviral activity of Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID518734	Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by filter-based filtration assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID717421	Antiviral activity against wild type HIV1 Ba-L	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
AID572192	Antiviral activity against HIV-1 Bal infected in human PM1 cells assessed as inhibition of transmission of virus to premissive T cells	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID620431	Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for wild type HIV1 BaL	2011	Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20	Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID571973	Antiviral activity against HIV-1 subtype CRF01_AE V022822 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID650544	Antiviral activity against HIV 1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID663297	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID572189	Antiviral activity against HIV-1 SM058 harboring NNTRI 227L and 106A mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1574378	Antiviral activity against HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1574388	Resistance index, ratio of ID50 for recombinant HIV-1 His-tagged reverse transcriptase p66/p51 K103N mutant to ID50 for recombinant wild type HIV-1 reverse transcriptase His-tagged p66/p51	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID572188	Antiviral activity against HIV-1 SM052 harboring NNTRI 101E and 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1163232	Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID572183	Antiviral activity against HIV-1 SM024 harboring NNTRI 190A mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID650693	Ratio of ID50 for HIV 1 reverse transcriptase Y188L mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID650687	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV 1 NL4-3	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID572194	Antiviral activity against HIV-1 Bal infected in human cervical tissue explants assessed as inhibition of dissemination of virus via migratory cells after 2 hrs in presence of 12.5% cervical mucus	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID581824	Antiviral activity against HIV1 isolate 71361-1 harboring reverse transcriptase K65R mutant infected in human TZM-b1 cells after 2 hrs by luciferase assays	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID518735	Inhibition of RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by filter-based filtration assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID663295	Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID717415	Ratio of EC50 for HIV1 harboring reverse transcriptase VI829 L100I, K103N mutant to EC50 for HIV1 harboring reverse transcriptase V106A mutant	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
AID571982	Antiviral activity against HIV-1 subtype B V022814 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID571942	Toxicity against human Ectocervical tissue explants at 0.0001 to 100 uM after 24 hrs by MTT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID717413	Antiviral activity against HIV1 assessed as inhibition of viral p24 antigen production treated every 1 hr for 12 hrs by ELISA based time-of-drug addition assay	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
AID236429	Area under the concentration time curve in human after 100 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.
AID571963	Selectivity index, ratio of CC50 for human PM1 cells to IC50 for HIV-1 RF	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID573480	Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase to wild-type	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID581817	Cytotoxicity against human TZM-bl cells by MTT assay	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID663303	Resistance ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-3	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID650545	Antiviral activity against HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID650692	Inhibition of HIV 1 reverse transcriptase Y188L mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID572201	Antiviral activity against HIV-1 Bal infected in 24 hrs 10 nM compound pretreated human ectocervical explant tissue assessed as prolonged inhibition of viral infection post compound removal	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1163254	Antileishmanial activity against Leishmania infantum MHOM/MA (BE)/67 infected in primary peritoneal mouse macrophages assessed as reduction in parasite burdun	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID650543	Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID573477	Antiviral activity of Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID571972	Antiviral activity against HIV-1 subtype CRF01_AE V022821 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID717416	Antiviral activity against HIV1 harboring reverse transcriptase VI829 L100I, K103N mutant	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
AID571971	Antiviral activity against HIV-1 subtype CRF01_AE V022820 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID581813	Antiviral activity against R5 tropic HIV1 YU.2 infected in human TZM-b1 cells after 2 hrs by luciferase assay	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID571946	Toxicity against human cervical tissue explants at 1 mM after 24 hrs by MTT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID581822	Antiviral activity against R5 tropic HIV1 R8.BaL infected in human PBMC assessed as inhibition of p24 antigen production after 2 hrs by ELISA	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID571974	Antiviral activity against HIV-1 subtype CRF01_AE V029521 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID572185	Antiviral activity against HIV-1 SM030 harboring NNTRI 100I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
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.
AID581823	Cytotoxicity against human PBMC by MTT assay	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID571987	Antiviral activity against HIV-1 subtype C V022831 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1157598	Antiviral activity against HIV1 MP1308 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID449192	Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for HIV1 RTMDR1	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1574374	Antiviral activity against HIV-1 IRLL98 harboring reverse transcriptase M41L, D67N, Y181C, M184V, R211K, and T215Y mutants infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1157606	Cytotoxicity against human MT4 cells after 40 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID650547	Resistance ratio of EC50 for HIV 1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID650546	Antiviral activity against HIV 1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID572180	Antiviral activity against HIV-1 SM002 harboring NNTRI 181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID518741	Antiviral activity against HIV 1 subtype B harboring reverse transcriptase M230L mutant infected in human TZM-bl cells assessed as inhibition of viral growth by luciferase reporter gene assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID663307	Inhibition of HIV1 recombinant reverse transcriptase L100I mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID518740	Antiviral activity against HIV 1 subtype B harboring wild type reverse transcriptase infected in human TZM-bl cells assessed as inhibition of viral growth by luciferase reporter gene assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID767489	Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced effect	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID650541	Resistance ratio of EC50 for multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1157593	Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID620434	Ratio of EC50 for HIV1 BaL expressing reverse transcriptase V106A mutant infected in human TZM-bl cells to EC50 for wild type HIV1 BaL in human TZM-bl cells	2011	Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20	Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
AID571955	Antiviral activity against HIV-1 3B infected in human MT4 cells after 7 days by RT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID767495	Aqueous solubility of the compound in Britton-Robinson buffer at pH 6.5 after 48 hrs by shake-flask method	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID663312	Resistance ratio of ID50 for HIV1 reverse transcriptase L100I mutant to ID50 HIV1 wild type reverse transcriptase	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID572186	Antiviral activity against HIV-1 SM034 harboring NNTRI 188L mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1636931	Aqueous solubility of compound in pH 6.5 solution by shake flask method	2016	Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20	Computer-aided discovery of anti-HIV agents.
AID571979	Antiviral activity against HIV-1 subtype B V022811 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID246301	Effective concentration of the compound to inhibit HIV-1 mutant Y188L replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1421308	Inhibition of recombinant HIV1 reverse transcriptase L100I/K103N double mutant	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID417448	Inhibition of HIV1 reverse transcriptase Y188L mutant	2009	European journal of medicinal chemistry, Feb, Volume: 44, Issue:2	QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
AID571957	Antiviral activity against HIV-1 3B infected in human monocyte derived macrophages after 7 days by RT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID573467	Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID717423	Cytotoxicity against human TZM-b1 cells	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.
AID571956	Antiviral activity against HIV-1 RF infected in human PM1 cells after 7 days by RT assay	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
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.
AID581818	Ratio of IC50 for wild type HIV1 to IC50 for HIV1 A17 harboring reverse transcriptase K103N, Y181C mutant	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Reverse transcriptase inhibitors as potential colorectal microbicides.
AID1157607	Antiviral activity against HIV1 infected in human MT4 cells assessed as lowest compound concentration required to irreversibly knock out vial multiplication treated by chronic treatment measured after 40 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1421303	Inhibition of wild-type HIV1 3B reverse transcriptase	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1574373	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1157596	Antiviral activity against HIV1 W5269 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID650695	Ratio of ID50 for HIV 1 reverse transcriptase L100I mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1157599	Antiviral activity against NRTI-resistant HIV1 MP1315 infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID572176	Antiviral activity against HIV-1 subtype H V022827 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B	2009	Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2	Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID650689	Inhibition of HIV 1 reverse transcriptase K103N mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)	2011	Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8	Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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	26 (13.47)	29.6817
2010's	107 (55.44)	24.3611
2020's	60 (31.09)	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	64 (32.65%)	5.53%
Reviews	15 (7.65%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	2 (1.02%)	0.25%
Other	115 (58.67%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (42)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Double-Blind, Randomised, Placebo-Controlled Pharmacokinetic and Safety Trial in Healthy HIV-Negative Women to Assess the Delivery of Dapivirine From a Matrix Vaginal Ring and to Evaluate the Safety of a Matrix Vaginal Ring Containing 25 MG of Dapivirin [NCT01144676]	Phase 1	45 participants (Actual)	Interventional	2010-04-30	Completed
Phase 3B, Randomized, Open-Label, Safety, and Drug Detection Study of Dapivirine Vaginal Ring and Oral TRUVADA® in Breastfeeding Mother-Infant Pairs [NCT04140266]	Phase 3	394 participants (Actual)	Interventional	2020-09-24	Completed
A Multi-Centre, Randomised, Double-Blind, Placebo-Controlled Phase III Safety and Efficacy Trial of a Vaginal Matrix Ring With Dapivirine for the Prevention of HIV-1 Infection in Women [NCT01337583]	Phase 3	0 participants (Actual)	Interventional	2011-07-31	Withdrawn
A Phase 1, Randomized Pharmacokinetics and Safety Study of Extended Duration Dapivirine Vaginal Rings [NCT03234400]	Phase 1	49 participants (Actual)	Interventional	2017-12-04	Completed
A Randomized, Double Blind, Placebo-Controlled, Phase 1 Safety and Pharmacokinetic Study of Dapivirine Gel (0.05%) Administered Rectally to HIV-1 Seronegative Adults [NCT03239483]	Phase 1	28 participants (Actual)	Interventional	2017-10-26	Completed
Phase 1 Safety and Pharmacokinetics of Dapivirine/Maraviroc Vaginal Ring [NCT01363037]	Phase 1	48 participants (Actual)	Interventional	2011-11-30	Completed
A Phase I, Open-Label, Randomized, Crossover Trial to Investigate the Relative Bioavailability of the 25 mg Dapivirine Vaginal Ring-004 Inserted Every 30 Days and 100 mg DPV Ring-008 Inserted for 90 Days in Healthy Female Participants [NCT05416021]	Phase 1	110 participants (Anticipated)	Interventional	2022-08-01	Recruiting
A DOUBLE-BLIND, RANDOMIZED, PLACEBO-CONTROLLED PHASE I/II TRIAL TO EVALUATE THE SAFETY OF DAPIVIRINE GEL 4759, 0.05% 2.5g AND DAPIVIRINE GEL 4789, 0.05% 2.5g FORMULATIONS AS COMPARED TO THE VAGINAL HEC-BASED UNIVERSAL PLACEBO GEL, 2.5g IN HEALTHY HIV-NEGA [NCT00799058]	Phase 1/Phase 2	128 participants (Actual)	Interventional	2009-07-06	Completed
A Follow-On, Open-Label Trial To Assess Continued Safety Of And Adherence To The Dapivirine (25 Mg) Vaginal Ring-004 In Healthy, HIV-Negative Women [NCT02862171]	Phase 3	941 participants (Actual)	Interventional	2016-07-12	Completed
A Phase 3B Open-Label Follow-on Trial to Assess the Continued Safety of and Adherence to a Vaginal Ring Containing Dapivirine in Women [NCT02858037]	Phase 3	1,456 participants (Actual)	Interventional	2016-07-18	Completed
A Multi-Centre, Randomised, Double-Blind, Placebo-Controlled Phase III Safety and Efficacy Trial of a Vaginal Matrix Ring With Dapivirine for the Prevention of HIV-1 Infection in Women [NCT01337570]	Phase 3	0 participants (Actual)	Interventional	2011-07-31	Withdrawn
A Two-Cohort, Open-Label, Randomised, Three-Period Crossover Trial In Healthy HIV-Negative Women To Assess The Effect Of Menses And Tampon Use On The Pharmacokinetics Of Dapivirine, Delivered By Dapivirine Vaginal Ring-004, Containing 25 Mg Of Dapivirine [NCT02858024]	Phase 1	16 participants (Actual)	Interventional	2015-01-12	Completed
A Phase 2a Crossover Trial Evaluating the Safety of and Adherence to a Vaginal Matrix Ring Containing Dapivirine and Oral Emtricitabine/Tenofovir Disoproxil Fumarate in an Adolescent and Young Adult Female Population [NCT03074786]	Phase 2	0 participants (Actual)	Interventional	2017-11-30	Withdrawn(stopped due to Study was transferred to partner who will conduct under its own IND)
A Multi-Center, Randomized, Double-Blind, Placebo-Controlled Phase 3 Safety and Effectiveness Trial of a Vaginal Matrix Ring Containing Dapivirine for the Prevention of HIV-1 Infection in Women [NCT01617096]	Phase 3	2,629 participants (Actual)	Interventional	2012-07-24	Completed
Phase I Study of a Vaginal Ring for Delivery of TMC120 (Dapivirine) as a Vaginal Microbicide [NCT00700284]	Phase 1	12 participants (Actual)	Interventional	2004-10-31	Completed
A Double-blind, Randomized, Placebo-Controlled Phase I/II Study to Evaluate the Safety and Acceptability of Dapivirine Gel 4789, 0.05%, 2.5g, a Vaginal Microbicide, Conducted Using Daily Monitored Adherence in Healthy, HIV-Negative Women. [NCT00917904]	Phase 1/Phase 2	100 participants (Actual)	Interventional	2009-07-31	Completed
AN OPEN-LABEL, RANDOMISED TRIAL, WITH A THREE-PERIOD CROSSOVER PART IN HEALTHY HIV-NEGATIVE WOMEN TO ASSESS THE DRUG-DRUG INTERACTION POTENTIAL BETWEEN DAPIVIRINE VAGINAL RING-004, CONTAINING 25 MG OF DAPIVIRINE, AND CLOTRIMAZOLE 10 mg/g (1%) ADMINISTERED [NCT02847286]	Phase 1	36 participants (Actual)	Interventional	2015-09-01	Completed
A Double-blind, Randomized, Placebo-Controlled Phase I/II Study to Evaluate the Safety and Acceptability of Dapivirine Gel 4759, 0.05%, 2.5g, a Vaginal Microbicide, Conducted Using Daily Monitored Adherence in Healthy, HIV-Negative Women. [NCT00917891]	Phase 1/Phase 2	280 participants (Actual)	Interventional	2009-11-30	Completed
A Double-Blind, Randomized, Placebo-Controlled Phase I/II Study to Evaluate the Safety of an Intravaginal Matrix Ring With Dapivirine in Healthy, HIV-Negative Women. [NCT01071174]	Phase 1/Phase 2	280 participants (Actual)	Interventional	2010-04-30	Completed
An Open-label, Parallel-group Pharmacokinetic Trial in Healthy HIV-negative Women to Characterize the Release Profile of Dapivirine Delivered by a Silicone Matrix Ring (Ring 004), Containing 25 mg of Dapivirine, Over Various Ring Use Periods [NCT01952561]	Phase 1	40 participants (Actual)	Interventional	2013-11-30	Completed
A Phase I/II Double-Blind, Randomized Study of the Safety, Tolerability and Systemic Absorption of TMC120 Vaginal Microbicide Gel and Matching Placebo in Healthy HIV-Negative Women. [NCT00303576]	Phase 1/Phase 2	112 participants	Interventional	2005-10-31	Completed
A Double-Blind, Randomized, Placebo-Controlled Phase I Study to Compare the Pharmacokinetics of Intravaginal Dapivirine Gel 4750, 0.05%, 2.5g and Dapivirine Gel 4789, 0.05%, 2.5g Formulations and to Assess the Safety as Compared to the Intravaginal HEC-Ba [NCT00613249]	Phase 1	36 participants (Actual)	Interventional	2007-11-30	Completed
A Phase 1, Randomized, Double-Blind Pharmacokinetic and Safety Study of Dapivirine/Levonorgestrel Vaginal Rings [NCT02855346]	Phase 1	24 participants (Actual)	Interventional	2017-05-03	Completed
Phase 1 Pharmacokinetic Study of the Dapivirine Vaginal Ring in Lactating Women [NCT02808949]	Phase 1	16 participants (Anticipated)	Interventional	2015-02-28	Completed
A Double-Blind, Randomised, Placebo-Controlled Phase I Trial to Compare the Pharmacokinetics of Maraviroc and Dapivirine Following Application of Maraviroc Vaginal Vaginal Gel, 0.1% 2.5g, Dapivirine Vaginal Gel, 0.05%, 2.5g and Maraviroc 0.1% + Dapivirine [NCT01242579]	Phase 1	0 participants (Actual)	Interventional	2011-01-31	Withdrawn(stopped due to In order to focus efforts on the combination ring formulation, IPM decided not to move forward with this trial.)
A Double-Blind, Randomised, Placebo-Controlled Safety and Pharmacokinetic Trial in Healthy HIV-Negative Women to Assess Delivery of Dapivirine From the Matrix Vaginal Ring Containing 25 MG of Dapivirine [NCT02920827]	Phase 1	16 participants (Actual)	Interventional	2009-08-31	Completed
Male Tolerance Study of Dapivirine Gel Following Multiple Topical Penile Exposures [NCT01277640]	Phase 1	48 participants (Actual)	Interventional	2011-03-31	Completed
A Multi-Centre, Randomised, Double-Blind, Placebo-Controlled Safety and Efficacy Trial of a Dapivirine Vaginal Matrix Ring in Healthy HIV-Negative Women [NCT01539226]		1,959 participants (Actual)	Interventional	2012-03-27	Completed
A Study to Assess the Pharmacokinetics of Dapivirine (TMC120) Vaginal Microbicide Gel in Healthy HIV-Negative Women. [NCT00304642]	Phase 1	18 participants	Interventional	2005-11-30	Completed
A Phase I/II Single-Centre Double-Blinded Randomized Study of the Safety and Tolerability of TMC120 Vaginal Microbicide Gel vs. HEC-Based Universal Placebo Gel in Healthy HIV-Negative Women. [NCT00309205]	Phase 1/Phase 2	36 participants	Interventional	2005-12-31	Completed
Double-blind, Randomized, Placebo Controlled Trial to Study Safety, Local and Systemic Availability of TMC120 From a Vaginal Ring. [NCT00332995]	Phase 1	13 participants	Interventional	2005-07-31	Completed
A Double-blind, Randomized, Placebo-controlled Safety and Pharmacokinetic Study in Healthy HIV-negative Women to Assess the Delivery of Dapivirine From Matrix and Reservoir Intravaginal Rings Each Containing 25 mg of Dapivirine [NCT00469768]	Phase 1	24 participants (Actual)	Interventional	2007-05-31	Completed
[NCT01548560]	Phase 1	60 participants (Actual)	Interventional	2012-08-31	Completed
A Phase I/II Single-Centre Double-Blinded Randomized Study of the Safety and Tolerability of TMC120 Vaginal Microbicide Gel (TMC120 Gel-002) vs. HEC-Based Universal Placebo Gel in Healthy HIV-Negative Women. [NCT00304668]	Phase 1/Phase 2	0 participants (Actual)	Interventional		Withdrawn
An Open-label, Randomized, Three-period Crossover Trial in Healthy HIV-negative Women to Assess the Drug-drug Interaction Between Dapivirine Vaginal Ring-004 and Miconazole Nitrate [NCT01731574]	Phase 1	36 participants (Actual)	Interventional	2012-12-31	Completed
Comparison of the Pharmacokinetics and Pharmacodynamics of Single Dose Dapivirine Vaginal Gel and Film Formulation [NCT01924091]	Phase 1	60 participants (Actual)	Interventional	2013-09-30	Completed
Phase 3b, Randomized, Open Label Safety Trial of Dapivirine Vaginal Ring and Oral TRUVADA® Use in Pregnancy [NCT03965923]	Phase 3	859 participants (Actual)	Interventional	2020-01-09	Active, not recruiting
A Randomized, Double Blind, Placebo-Controlled, Phase 1 Safety and Pharmacokinetic Study of Dapivirine Gel (0.05%) Administered Rectally to HIV-1 Seronegative Adults [NCT03044379]	Phase 1	0 participants (Actual)	Interventional	2015-09-29	Withdrawn(stopped due to Current program is on hold, not for safety reason)
A Phase 2a Crossover Trial Evaluating the Safety of and Adherence to a Vaginal Matrix Ring Containing Dapivirine and Oral Emtricitabine/Tenofovir Disoproxil Fumarate in an Adolescent and Young Adult Female Population [NCT03593655]	Phase 2	247 participants (Actual)	Interventional	2019-01-14	Completed
An Open Label Randomized Phase 1 Pharmacokinetic Study of Dapivirine Gel Administered Rectally to HIV-1 Seronegative Adults [NCT03393468]	Phase 1	16 participants (Actual)	Interventional	2018-05-10	Completed
Phase 2a Safety Study of a Vaginal Matrix Ring Containing Dapivirine in a Postmenopausal Female Population [NCT02010593]	Phase 2	96 participants (Actual)	Interventional	2013-12-31	Completed
Phase 2a Safety Study of a Vaginal Ring Containing Dapivirine in Adolescent Females [NCT02028338]	Phase 2	96 participants (Actual)	Interventional	2014-06-27	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00799058 (8) [back to overview]	The Distribution of Dapivirine Levels Observed in Vaginal Tissue at Each Specified Time Point.
NCT00799058 (8) [back to overview]	The Distribution of Dapivirine Levels Observed in Vaginal Fluid at Each Specified Time Point.
NCT00799058 (8) [back to overview]	Acceptability of Once Daily Application of a Vaginal Microbicide Gel Over a 12-week Period in Healthy, Sexually Active, HIV-negative Women
NCT00799058 (8) [back to overview]	The Adherence to Once Daily Application of a Vaginal Microbicide Gel Over a 12-week Period in Healthy, Sexually Active, HIV-negative Women
NCT00799058 (8) [back to overview]	The Percentage of Women With the Composite Endpoint of Abnormal Safety Findings.
NCT00799058 (8) [back to overview]	Changes in the Vaginal Flora
NCT00799058 (8) [back to overview]	Changes in the Vaginal pH
NCT00799058 (8) [back to overview]	The Distribution of Dapivirine Levels Observed in Plasma Samples at Each Specified Time Point
NCT01539226 (8) [back to overview]	The Percentage of Women Who Report the Use of the Vaginal Ring as Acceptable;
NCT01539226 (8) [back to overview]	The Percentage of Women Who Report Adherence to the Use of the Vaginal Ring Inserted Once Every 4 Weeks Over the Trial Period;
NCT01539226 (8) [back to overview]	The Percentage of Participants With HIV-1 Drug Resistance Mutations Among Participants Who Acquire HIV-1.
NCT01539226 (8) [back to overview]	The Incidence Rate of HIV-2 Seroconversion.
NCT01539226 (8) [back to overview]	The Incidence of Curable STIs
NCT01539226 (8) [back to overview]	Percentage of Participants With Pregnancy in Each Trial Arm Over the IP Use Period;
NCT01539226 (8) [back to overview]	HIV-1 Seroconversion According to Comprehensive HIV Testing Algorithm.
NCT01539226 (8) [back to overview]	All Adverse Events
NCT01617096 (5) [back to overview]	Adherence to the Dapivirine Vaginal Ring.
NCT01617096 (5) [back to overview]	The Number of Participants That Experienced Grade 2, 3, 4 and Serious Adverse Events Over the Investigational Product Used Period (25 mg Dapivirine Administered in a Silicone Elastomer Vaginal Matrix Ring (DVR), Inserted Once Every 4 Weeks).
NCT01617096 (5) [back to overview]	Human Immunodeficiency Virus Type 1 Drug Resistance Mutations Among Participants Who Acquired HIV-1 Infection.
NCT01617096 (5) [back to overview]	Efficacy as Determined by the Proportion of Women in Each Arm With HIV-1 Seroconversion After 120 Endpoints Are Observed in the Trial.
NCT01617096 (5) [back to overview]	Acceptability of the DVR and Placebo Vaginal Ring
NCT02010593 (5) [back to overview]	The Percentage of Participants Who Find the Study Vaginal Ring to be as Acceptable
NCT02010593 (5) [back to overview]	Safety of Dapivirine (25 mg) Administered in a Silicone Elastomer Vaginal Matrix Ring in HIV-uninfected Postmenopausal Women, When Inserted Once Every 4 Weeks During 12 Weeks of Study Product Use
NCT02010593 (5) [back to overview]	Pharmacokinetics - The Intent is to Determine if the Vaginal Fluid Dapivirine Concentrations Are Different in Postmenopausal Women Than in Pre-menopausal Adult Women After Placement of Dapivirine Vaginal Rings.
NCT02010593 (5) [back to overview]	Pharmacokinetics - The Intent is to Determine if the Plasma Dapivirine Concentrations Are Different in Postmenopausal Women Than in Pre-menopausal Adult Women After Placement of Dapivirine Vaginal Rings.
NCT02010593 (5) [back to overview]	Percentage of Women Who Were Adherent to Daily Study Product Use Based on Self-report Over the 12-week Study Product Use Period
NCT02028338 (5) [back to overview]	The Acceptability of the Study VR (Dapivirine or Placebo) in HIV Uninfected Adolescent Females, When Inserted Once Every 4 Weeks for a 24 Week Period
NCT02028338 (5) [back to overview]	The Systemic Dapivirine Exposure
NCT02028338 (5) [back to overview]	The Safety of Dapivirine (25 mg) Administered Via a Silicone Vaginal Ring in HIV-uninfected Adolescent Females, When Inserted Once Every 4 Weeks During 24 Weeks of Study Product Use
NCT02028338 (5) [back to overview]	Local Dapivirine Exposure
NCT02028338 (5) [back to overview]	Adherence to the Study VR (Dapivirine or Placebo) in HIV Uninfected Adolescent Females, When Inserted Once Every 4 Weeks for a 24 Week Period
NCT02858037 (4) [back to overview]	Incidence of HIV-1 Infection
NCT02858037 (4) [back to overview]	Number of Participant Who Acquired HIV-1 With HIV-1 Drug Resistance Associated Mutations.
NCT02858037 (4) [back to overview]	The Safety Profile Associated With the Open-label Use of the Dapivirine Vaginal Matrix Ring (25 mg) in Women
NCT02858037 (4) [back to overview]	Adherence to the Open Label Use of the Dapivirine Vaginal Matrix Ring (25 mg) in Women
NCT02862171 (4) [back to overview]	Incidence of HIV-1 Seroconversion
NCT02862171 (4) [back to overview]	Number of Participants Who Acquired HIV-1 With HIV-1 Drug Resistance-associated Mutations. Infection
NCT02862171 (4) [back to overview]	Adherence to the Use of the 25 mg Dapivirine Vaginal Ring-004 Inserted at Monthly Intervals, in an Open-label Trial
NCT02862171 (4) [back to overview]	The Safety Profile of the 25 mg Dapivirine Vaginal Ring-004, When Inserted at Monthly Intervals. Participants Attended RC at Monthly Visits (up to Max of Three Monthly Visits) Followed by 3-monthly Follow-up Visits.
NCT03239483 (7) [back to overview]	Measurement of Dapivirine Concentrations in Rectal Fluid
NCT03239483 (7) [back to overview]	Terminal Half-life of Dapivirine Concentrations in Plasma
NCT03239483 (7) [back to overview]	Measurement of Dapivirine Concentrations in Plasma
NCT03239483 (7) [back to overview]	Frequency of Grade 2 or Higher Adverse Events (AEs)
NCT03239483 (7) [back to overview]	Acceptability: Ease of Use
NCT03239483 (7) [back to overview]	Acceptability: Comfort
NCT03239483 (7) [back to overview]	Measurement of Dapivirine Concentrations in Rectal Mucosal Tissue Homogenates
NCT03593655 (4) [back to overview]	Number of Participant-Visits Reporting Acceptability of Study Product
NCT03593655 (4) [back to overview]	Number of Participant-Visits With No Product Use
NCT03593655 (4) [back to overview]	Number of Participants With Grade 2 or Higher Adverse Events (AEs)
NCT03593655 (4) [back to overview]	Percentage of Participants Reporting Preference for Dapivirine VR as Compared to FTC/TDF Oral Tablets
NCT04140266 (26) [back to overview]	Participant Willingness to Use Their Assigned Study Products During Breastfeeding in the Future (Y/N)
NCT04140266 (26) [back to overview]	Proportion of Participants Who Find Their Study Product to be at Least as Acceptable as Other HIV Prevention Methods
NCT04140266 (26) [back to overview]	Geometric Mean of Infant DPV Concentrations From Plasma by Visit
NCT04140266 (26) [back to overview]	The Number of Mothers Non-adherent to Study Product for Each Month of Product Use by Study Product
NCT04140266 (26) [back to overview]	Residual Drug Levels in Returned VRs
NCT04140266 (26) [back to overview]	Number and Proportion of Mothers With Detectable Tenofovir Diphosphate (TFV-DP) Concentrations
NCT04140266 (26) [back to overview]	Number and Proportion of Mothers With Detectable Plasma Dapivirine (DPV) Concentrations
NCT04140266 (26) [back to overview]	Number and Proportion of Mothers With Detectable Emtricitabine Triphosphate (FTC-TP) Concentrations
NCT04140266 (26) [back to overview]	Number and Proportion of Mothers With Detectable Breastmilk TFV Concentrations
NCT04140266 (26) [back to overview]	Number and Proportion of Mothers With Detectable Breastmilk FTC Concentrations
NCT04140266 (26) [back to overview]	Number and Proportion of Mothers With Detectable Breastmilk DPV Concentrations
NCT04140266 (26) [back to overview]	Number and Proportion of Infants With Detectable TFV-DP Concentrations
NCT04140266 (26) [back to overview]	Number of Infant Participants With Grade 3 or Higher AEs in Both Study Arms
NCT04140266 (26) [back to overview]	Number of Infant Participants With SAEs Including Infant Deaths in Both Study Arms
NCT04140266 (26) [back to overview]	Number of Mother Participants With Grade 3 or Higher Adverse Events (AEs) in Both Study Arms
NCT04140266 (26) [back to overview]	Number of Mother Participants With Serious Adverse Events (SAEs) Including Maternal Deaths in Both Study Arms
NCT04140266 (26) [back to overview]	Geometric Mean of Maternal DPV Concentrations From Breastmilk by Visit
NCT04140266 (26) [back to overview]	Number and Proportion of Infants With Detectable Plasma DPV Concentrations
NCT04140266 (26) [back to overview]	Number and Proportion of Infants With Detectable FTC-TP Concentrations
NCT04140266 (26) [back to overview]	Geometric Mean of Maternal TFV-DP Concentrations by Visit
NCT04140266 (26) [back to overview]	Geometric Mean of Maternal TFV Concentrations From Breastmilk by Visit
NCT04140266 (26) [back to overview]	Geometric Mean of Maternal FTC-TP Concentrations by Visit
NCT04140266 (26) [back to overview]	Geometric Mean of Maternal FTC Concentrations From Breastmilk by Visit
NCT04140266 (26) [back to overview]	Geometric Mean of Maternal DPV Concentrations From Plasma by Visit
NCT04140266 (26) [back to overview]	Geometric Mean of Infant TFV-DP Concentrations by Visit
NCT04140266 (26) [back to overview]	Geometric Mean of Infant FTC-TP Concentration by Visit

The Distribution of Dapivirine Levels Observed in Vaginal Tissue at Each Specified Time Point.

The distribution of dapivirine levels observed in vaginal tissue sample will be summarized using simple descriptive statistics. (NCT00799058)
Timeframe: 12 weeks. Measured at 2, 4, and 8 weeks post-enrolment and at one of these at week 12; 24, 48, or 72 hours after gel discontinuation. (Participants were randomized to have vaginal fluid samples collected at one of these visits (5a, 5b, or 5c).

Intervention	nanogram/gram (Mean)
	Visit 5a (24 hours after gel discontinuation)	Visit 5b (48 hours after gel discontinuation)	Visit 5c (72 hours after gel discontinuation)
Dapivirine Gel 4759	3518	841.0	4781
Dapivirine Gel 4789	9343	1150	1142

Intervention	nanogram/milliliter (Mean)
	Visit 2 (2 weeks post-enrollment)	Visit 3 (4 weeks post-enrolment)	Visit 4 (8 weeks post-enrolment)	Visit 5a (24 hours after gel discontinuation)	Visit 5b (48 hours after gel discontinuation)	Visit 5c (72 hours after gel discontinuation)
Dapivirine Gel 4759	467.1	347.8	526.9	192.0	98.63	177.0
Dapivirine Gel 4789	880.7	462.6	298.1	680.0	164.0	245.6

Intervention	Participants (Count of Participants)
Dapivirine Gel 4789	24
Dapivirine Gel 4759	25
HEC-based Placebo Gel, 2.5g Containing no Dapivirine	29

Intervention	percentage of participants with data (Number)
	Week 0 : Normal Flora (0-3)	Week 0 : Altered Flora (4-6)	Week 0 : Abnormal Flora (7 or more)	Week 4 : Normal Flora (0-3)	Week 4 : Altered Flora (4-6)	Week 4 : Abnormal Flora (7 or more)	Week 12: Normal Flora (0-3)	Week 12: Altered Flora (4-6)	Week 12: Abnormal Flora (7 or more)	Week 16 (Follow-up after IP discontinuation): Normal Flora (0-3)	Week 16 (Follow-up after IP discontinuation): Altered Flora (4-6)	Week 16 (Follow-up after IP discontinuation): Abnormal Flora (7 or more)
Dapivirine Gel 4759	66.7	14.3	19.0	67.6	8.1	24.3	61.8	23.5	14.7	70.6	2.9	26.5
Dapivirine Gel 4789	60.5	11.6	27.9	55.0	12.5	32.5	65.7	20.0	14.3	66.7	18.2	15.2
HEC-based Placebo Gel, 2.5g Containing no Dapivirine	54.8	23.8	21.4	65.9	19.5	14.6	59.5	24.3	16.2	64.9	18.9	16.2

Intervention	Vaginal pH (Mean)
	Screening (Week 0)	Visit 1 (Enrollment)	Visit 5 (Week 12)
Dapivirine Gel 4759	4.46	4.45	4.4
Dapivirine Gel 4789	4.55	4.48	4.44
HEC-based Placebo Gel, 2.5g Containing no Dapivirine	4.55	4.3	4.38

Intervention	picograms/mililiter (Mean)
	Week 2	Week 4	Week 8	Week 12
Dapivirine Gel 4759	536.8	599.5	572.6	519.1
Dapivirine Gel 4789	475.8	446.1	432.6	366.1

Intervention	percentage of participants with data (Number)
	Week 4	Week 24
Dapivirine Vaginal Ring	97.4	98.7
Placebo Vaginal Ring	98.7	98.6

Intervention	participants with data (Number)
	Month 1	Month 2	Month 3	Month 4	Month 5	Month 6	Month 7	Month 8	Month 9	Month 10	Month 11	Month 12	Month 13	Month 14	Month 15	Month 16	Month 17	Month 18	Month 19	Month 20	Month 21	Month 22	Month 23	Month 24	Month 25	Month 26	Month 27	Month 28	Month 29	Month 30	Month 31	Month 32	Month 33	Month 34
Dapivirine Vaginal Ring	443	460	953	537	573	963	687	699	943	830	916	922	872	858	793	704	701	675	600	598	576	499	485	471	391	384	367	263	258	251	133	130	120	4

Intervention	Participants (Count of Participants)
	DAIDS Grade 2 or higher	DAIDS grade 3
Dapivirine Vaginal Ring	6	4
Placebo	3	0

Intervention	Participants (Count of Participants)
	Week 0 - 4	Week 4 - 8	Week 8 - 12
Dapivirine Vaginal Ring	58	67	65
Placebo	22	22	21

Intervention	Participants (Count of Participants)
	Discreetness71977697		Discreetness71977698	Likes and dislikes concerning the ring71977697	Likes and dislikes concerning the ring71977698	Attitude toward product characteristics71977697	Attitude toward product characteristics71977698	Comfort and ease of use71977697	Comfort and ease of use71977698	Partner reaction71977697	Partner reaction71977698	Effect on sex71977697	Effect on sex71977698
	At least one negative report	All responses positive
Dapivirine Ring	39
Placebo Ring	1
Dapivirine Ring	18
Placebo Ring	7
Dapivirine Ring	37
Placebo Ring	12
Dapivirine Ring	14
Placebo Ring	4
Dapivirine Ring	34
Placebo Ring	11
Dapivirine Ring	27
Placebo Ring	10
Dapivirine Ring	36
Dapivirine Ring	12
Placebo Ring	3
Dapivirine Ring	16
Placebo Ring	5
Dapivirine Ring	9
Placebo Ring	6

Intervention	Participants (Count of Participants)
	Grade 2 Adverse Events related to IP	Grade 3 or higher events
Dapivirine Ring	8	3
Placebo Ring	2	0

Intervention	Participants (Count of Participants)
	At least one Grade 3 or higher AE	At least one serious AE	At least one grade 2 or higher related AE
HIV Open-label Prevention	52	19	2

Intervention	mg (Mean)
	Enrollment. The month the ring was used is defined as the month the ring was dispensed.	Trial Month 1. The month the ring was used is defined as the month the ring was dispensed.	Trial Month 2.The month the ring was used is defined as the month the ring was dispensed.	Trial Month 3. The month the ring was used is defined as the month the ring was dispensed.	Trial Month 4. The month the ring was used is defined as the month the ring was dispensed	Trial Month 5. The month the ring was used is defined as the month the ring was dispensed	Trial Month 6. The month the ring was used is defined as the month the ring was dispensed.	Trial Month 7. The month the ring was used is defined as the month the ring was dispensed	Trial Month 8. The month the ring was used is defined as the month the ring was dispensed.	Trial Month 9.The month the ring was used is defined as the month the ring was dispensed.	Trial Month 10. The month the ring was used is defined as the month the ring was dispensed.	Trial Month 11. The month the ring was used is defined as the month the ring was dispensed.	Trial Month 12. The month the ring was used is defined as the month the ring was dispensed	Trial Month 13. The month the ring was used is defined as the month the ring was dispensed	Trial Month 14. The month the ring was used is defined as the month the ring was dispensed.	Trial Month 15. The month the ring was used is defined as the month the ring was dispensed.	Trial Month 16. The month the ring was used is defined as the month the ring was dispensed.
Dapivirine Vaginal Ring-004	20.77	20.57	20.59	20.83	20.61	20.70	20.77	20.44	20.59	20.72	20.47	20.82	20.84	20.49	20.81	20.92	20.20

Intervention	Participants (Count of Participants)
	At least one treatment emergent adverse event (TEAE)	At least one serious TEAE	At least one serious non-TEAE	At least one DAIDS Grade 3 or 4 TEAE	At least one product-related TEAE	TEAEs leading to death	TEAEs leading to temporary IP discontinuation	Urogenital TEAEs	Social harms reported as TEAEs	Non-TEAEs
Dapivirine Vaginal Ring-004	616	20	3	37	6	1	2	410	8	31

Intervention	ng/mg (Median)
	30 to 60 minutes after first application	120 minutes after single dose	24 hours after single dose	48 hours after single dose	72 hours after single dose	24 hours after first daily dose	30 to 60 minutes after last daily dose	120 minutes after last daily dose	24 hours after last daily dose	48 hours after last daily dose	72 hours after last daily dose
Dapivirine Gel	30.1	12.765	0	0.009	0	0.180	89.7	26.65	0.007	0	0

Intervention	pg/mL (Median)
	30 to 60 minutes after single dose	120 minutes after single dose	24 hours after single dose	48 hours after single dose	72 hours after single dose	24 hours after first daily dose	Before last daily dose	30 to 60 minutes after last daily dose	120 minutes after last daily dose	24 hours after last daily dose	48 hours after last daily dose	72 hours after last daily dose
Dapivirine Gel	31.5	326	20.1	0	0	67.9	167	290.5	403	119.0	113	80.3

Intervention	Visits (Count of Units)
	Week 1271925903		Week 1271925904	Week 2471925903	Week 2471925904	Week 3671925903	Week 3671925904	Week 4871925904	Week 4871925903
	Neither like nor dislike, dislike, or dislike very	Like, or like very much
FTC/TDF	72
Dapivirine Vaginal Ring	5
FTC/TDF	35
Dapivirine Vaginal Ring	105
FTC/TDF	73
Dapivirine Vaginal Ring	6
FTC/TDF	32
Dapivirine Vaginal Ring	91
FTC/TDF	93
Dapivirine Vaginal Ring	14
FTC/TDF	18
Dapivirine Vaginal Ring	90
FTC/TDF	68
Dapivirine Vaginal Ring	21
FTC/TDF	47

Intervention	Visits (Count of Units)
	Study Period 171925903		Study Period 171925904	Study Period 271925904	Study Period 271925903
	No use	At least some use
Dapivirine Vaginal Ring	19
FTC/TDF	11
Dapivirine Vaginal Ring	705
FTC/TDF	660
Dapivirine Vaginal Ring	41
FTC/TDF	10
Dapivirine Vaginal Ring	642
FTC/TDF	635

Intervention	Participants (Count of Participants)
	Study Period 1 (Weeks 1-24)71925903		Study Period 1 (Weeks 1-24)71925904	Study Period 2 (Weeks 25-48)71925903	Study Period 2 (Weeks 25-48)71925904
	No grade 2+ AE	At least one grade 2+ AE
Dapivirine Vaginal Ring	36
FTC/TDF	36
Dapivirine Vaginal Ring	88
FTC/TDF	87
Dapivirine Vaginal Ring	22
FTC/TDF	28
Dapivirine Vaginal Ring	95
FTC/TDF	94

Intervention	Participants (Count of Participants)
	Enrollment71925906					Enrollment71925905	Month 1271925905	Month 1271925906	Month 1871925905	Month 1871925906
	Neither product	Skipped question	Preferred ring	Preferred tablets	Either product equally
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	51
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	43
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	43
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	57
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	29
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	18
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	0
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	1
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	74
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	76
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	37
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	30
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	5
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	2
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	1
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	67
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	66
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	35
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	33
Sequence A: Dapivirine Vaginal Ring + FTC/TDF	13
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	5
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	4
Sequence B: FTC/TDF + Dapivirine Vaginal Ring	0

dapivirine

Description

Cross-References

Synonyms (63)

Research Excerpts

Overview

Effects

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Protein Targets (10)

Potency Measurements

Inhibition Measurements

Other Measurements

Biological Processes (45)

Molecular Functions (18)

Ceullar Components (22)

Bioassays (313)

Research

Studies (193)

Market Indicators

Research Demand Index: 47.73

Study Types

Clinical Trials (42)

Trial Overview

Trial Outcomes

The Distribution of Dapivirine Levels Observed in Vaginal Tissue at Each Specified Time Point.

The Distribution of Dapivirine Levels Observed in Vaginal Fluid at Each Specified Time Point.

Acceptability of Once Daily Application of a Vaginal Microbicide Gel Over a 12-week Period in Healthy, Sexually Active, HIV-negative Women

The Adherence to Once Daily Application of a Vaginal Microbicide Gel Over a 12-week Period in Healthy, Sexually Active, HIV-negative Women

The Percentage of Women With the Composite Endpoint of Abnormal Safety Findings.

Changes in the Vaginal Flora

Changes in the Vaginal pH

The Distribution of Dapivirine Levels Observed in Plasma Samples at Each Specified Time Point

The Percentage of Women Who Report the Use of the Vaginal Ring as Acceptable;

The Percentage of Women Who Report Adherence to the Use of the Vaginal Ring Inserted Once Every 4 Weeks Over the Trial Period;

The Percentage of Participants With HIV-1 Drug Resistance Mutations Among Participants Who Acquire HIV-1.

The Incidence Rate of HIV-2 Seroconversion.

The Incidence of Curable STIs

Percentage of Participants With Pregnancy in Each Trial Arm Over the IP Use Period;

HIV-1 Seroconversion According to Comprehensive HIV Testing Algorithm.

All Adverse Events

Adherence to the Dapivirine Vaginal Ring.

The Number of Participants That Experienced Grade 2, 3, 4 and Serious Adverse Events Over the Investigational Product Used Period (25 mg Dapivirine Administered in a Silicone Elastomer Vaginal Matrix Ring (DVR), Inserted Once Every 4 Weeks).

Human Immunodeficiency Virus Type 1 Drug Resistance Mutations Among Participants Who Acquired HIV-1 Infection.

Efficacy as Determined by the Proportion of Women in Each Arm With HIV-1 Seroconversion After 120 Endpoints Are Observed in the Trial.

Acceptability of the DVR and Placebo Vaginal Ring

The Percentage of Participants Who Find the Study Vaginal Ring to be as Acceptable

Safety of Dapivirine (25 mg) Administered in a Silicone Elastomer Vaginal Matrix Ring in HIV-uninfected Postmenopausal Women, When Inserted Once Every 4 Weeks During 12 Weeks of Study Product Use

Pharmacokinetics - The Intent is to Determine if the Vaginal Fluid Dapivirine Concentrations Are Different in Postmenopausal Women Than in Pre-menopausal Adult Women After Placement of Dapivirine Vaginal Rings.

Pharmacokinetics - The Intent is to Determine if the Plasma Dapivirine Concentrations Are Different in Postmenopausal Women Than in Pre-menopausal Adult Women After Placement of Dapivirine Vaginal Rings.

Percentage of Women Who Were Adherent to Daily Study Product Use Based on Self-report Over the 12-week Study Product Use Period

The Acceptability of the Study VR (Dapivirine or Placebo) in HIV Uninfected Adolescent Females, When Inserted Once Every 4 Weeks for a 24 Week Period

The Systemic Dapivirine Exposure

The Safety of Dapivirine (25 mg) Administered Via a Silicone Vaginal Ring in HIV-uninfected Adolescent Females, When Inserted Once Every 4 Weeks During 24 Weeks of Study Product Use

Local Dapivirine Exposure

Adherence to the Study VR (Dapivirine or Placebo) in HIV Uninfected Adolescent Females, When Inserted Once Every 4 Weeks for a 24 Week Period

Incidence of HIV-1 Infection

Number of Participant Who Acquired HIV-1 With HIV-1 Drug Resistance Associated Mutations.

The Safety Profile Associated With the Open-label Use of the Dapivirine Vaginal Matrix Ring (25 mg) in Women

Adherence to the Open Label Use of the Dapivirine Vaginal Matrix Ring (25 mg) in Women

Incidence of HIV-1 Seroconversion

Number of Participants Who Acquired HIV-1 With HIV-1 Drug Resistance-associated Mutations. Infection

Adherence to the Use of the 25 mg Dapivirine Vaginal Ring-004 Inserted at Monthly Intervals, in an Open-label Trial

The Safety Profile of the 25 mg Dapivirine Vaginal Ring-004, When Inserted at Monthly Intervals. Participants Attended RC at Monthly Visits (up to Max of Three Monthly Visits) Followed by 3-monthly Follow-up Visits.

Measurement of Dapivirine Concentrations in Rectal Fluid

Terminal Half-life of Dapivirine Concentrations in Plasma

Measurement of Dapivirine Concentrations in Plasma

Frequency of Grade 2 or Higher Adverse Events (AEs)

Acceptability: Ease of Use

Acceptability: Comfort

Measurement of Dapivirine Concentrations in Rectal Mucosal Tissue Homogenates

Number of Participant-Visits Reporting Acceptability of Study Product

Number of Participant-Visits With No Product Use

Number of Participants With Grade 2 or Higher Adverse Events (AEs)

Percentage of Participants Reporting Preference for Dapivirine VR as Compared to FTC/TDF Oral Tablets

Participant Willingness to Use Their Assigned Study Products During Breastfeeding in the Future (Y/N)

Proportion of Participants Who Find Their Study Product to be at Least as Acceptable as Other HIV Prevention Methods

Geometric Mean of Infant DPV Concentrations From Plasma by Visit

Intervention	Participants (Count of Participants)
Mothers - Group A: Dapivirine (DPV) Vaginal Ring (VR)-004	142
Mothers - Group B: Truvada Tablet	48

Intervention	Participants (Count of Participants)
	Week 1	Week 2	Month 1	Month 2	Product Use End Visit	Study End Visit
Mothers - Group B: Truvada Tablet	47	48	45	44	47	45

Intervention	Participants (Count of Participants)
Infants - Group A: DPV VR	10
Infants - Group B: Truvada Tablet	1

Intervention	Participants (Count of Participants)
Group A: Dapivirine (DPV) Vaginal Ring (VR)-004	3
Group B: Truvada Tablet	2

Condition	Indicated	Relationship Strength	Studies	Trials
HIV Coinfection [description not available]	0	18.26	131	63
HIV Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.	0	13.81	6	4
HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).	1	22.99	262	126
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.83	3	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
AIDS Seroconversion [description not available]	0	10.38	15	11
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	0	9.59	10	10
Bacterial Vaginitides [description not available]	0	3.6	2	0
Vaginosis, Bacterial Polymicrobial, nonspecific vaginitis associated with positive cultures of Gardnerella vaginalis and other anaerobic organisms and a decrease in lactobacilli. It remains unclear whether the initial pathogenic event is caused by the growth of anaerobes or a primary decrease in lactobacilli.	0	3.6	2	0
Innate Inflammatory Response [description not available]	0	2.55	2	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	2.55	2	0
Sexually Transmitted Diseases Diseases due to or propagated by sexual contact.	0	3.23	1	0
Genital Tract Infections [description not available]	0	2.15	1	0
Experimental Neoplasms [description not available]	0	3.56	1	1
Adverse Drug Event [description not available]	0	6.17	3	2
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	0	6.17	3	2
Disease Exacerbation [description not available]	0	7.63	4	4
Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.	0	3.59	1	1
Sexually Transmitted Disease, Viral [description not available]	0	3.85	2	1
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	2.47	2	0
Bilateral Headache [description not available]	0	3.44	1	1
Bleeding [description not available]	0	3.44	1	1
Headache The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.	0	3.44	1	1
Hemorrhage Bleeding or escape of blood from a vessel.	0	3.44	1	1
Vaginal Diseases Pathological processes of the VAGINA.	0	3.44	1	1
Petechiae Pinhead size (3 mm) skin discolorization due to hemorrhage.	0	3.42	1	1
Erythema Redness of the skin produced by congestion of the capillaries. This condition may result from a variety of disease processes.	0	3.42	1	1
Purpura Purplish or brownish red discoloration, easily visible through the epidermis, caused by hemorrhage into the tissues. When the size of the discolorization is	0	3.42	1	1