etravirine has been researched along with rilpivirine in 71 studies
Studies (etravirine) | Trials (etravirine) | Recent Studies (post-2010) (etravirine) | Studies (rilpivirine) | Trials (rilpivirine) | Recent Studies (post-2010) (rilpivirine) |
---|---|---|---|---|---|
572 | 90 | 321 | 580 | 93 | 513 |
Protein | Taxonomy | etravirine (IC50) | rilpivirine (IC50) |
---|---|---|---|
Gag-Pol polyprotein | HIV-1 M:B_HXB2R | 0.068 | |
Cytochrome P450 1A2 | Homo sapiens (human) | 6.1612 | |
Cytochrome P450 3A4 | Homo sapiens (human) | 1.7406 | |
Cytochrome P450 2D6 | Homo sapiens (human) | 2.3635 | |
Cytochrome P450 2C9 | Homo sapiens (human) | 0.2818 | |
Cytochrome P450 2C19 | Homo sapiens (human) | 0.3363 | |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | 0.5 | |
Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | 0.0759 | |
Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | 1.5 |
Timeframe | Studies, this research(%) | All Research% |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 5 (7.04) | 29.6817 |
2010's | 52 (73.24) | 24.3611 |
2020's | 14 (19.72) | 2.80 |
Authors | Studies |
---|---|
Arnold, E; Clark, AD; Das, K; Frenkel, YV; Janssen, PA; Lewi, PJ; Wang, YH | 1 |
Chen, CH; Jiang, S; Lai, W; Lee, KH; Lu, H; Qin, B; Tian, X; Xie, L | 1 |
Grimberg, BT; Hough, LB; Jaworska, MM; Phillips, JG; Zimmerman, PA | 1 |
Azijn, H; Boven, K; de Béthune, MP; Jochmans, D; Kraus, G; Picchio, G; Rimsky, LT; Tirry, I; Van Craenenbroeck, E; Vingerhoets, J | 1 |
Anderson, KS; Bollini, M; Domaoal, RA; Gallardo-Macias, R; Jorgensen, WL; Spasov, KA; Thakur, VV | 1 |
De Clercq, E; Li, D; Liu, X; Zhan, P | 1 |
Chen, CH; Huang, L; Lee, KH; Qian, K; Qin, B; Sun, LQ; Xie, L; Zhu, L | 1 |
Chong, P; Edelstein, M; Ferris, RG; Garrido, D; Mathis, A; Nolte, RT; Peat, A; Sebahar, P; Stewart, EL; Wang, L; Weaver, K; Youngman, M; Zhang, H | 1 |
Anderson, KS; Bollini, M; Gallardo-Macias, R; Jorgensen, WL; Spasov, KA; Tirado-Rives, J | 1 |
Chen, FE; Daelemans, D; De Clercq, E; Liu, Y; Ma, XD; Pannecouque, C; Yang, S | 1 |
Anderson, KS; Bollini, M; Cisneros, JA; Jorgensen, WL; Spasov, KA | 1 |
Asante-Appiah, E; Bayly, C; Bédard, L; Blouin, M; Burch, JD; Campeau, LC; Cauchon, E; Chan, M; Chefson, A; Côté, B; Coulombe, N; Cromlish, W; Debnath, S; Deschênes, D; Ducharme, Y; Dupont-Gaudet, K; Falgueyret, JP; Forget, R; Gagné, S; Gauvreau, D; Girardin, M; Guiral, S; Langlois, E; Li, CS; Nguyen, N; Ouellet, S; Papp, R; Plamondon, S; Roy, A; Roy, S; Seliniotakis, R; St-Onge, M; Tawa, P; Truchon, JF; Vacca, J; Wrona, M; Yan, Y | 1 |
Balzarini, J; Chen, W; De Clercq, E; Liu, H; Liu, X; Pannecouque, C; Rai, D; Zhan, P; Zhou, Z | 1 |
Anderson, KS; Bollini, M; Frey, KM; Gallardo-Macias, R; Jorgensen, WL; Lee, WG; Spasov, KA | 1 |
Elgaher, WA; Hartmann, RW; Haupenthal, J; Mély, Y; Pires, M; Real, E; Saladini, F; Sharma, KK | 1 |
Jorgensen, WL | 1 |
Chen, CH; Huang, L; Lee, KH; Morris-Natschke, SL; Wang, HL; Wei, L; Xie, L | 1 |
Chen, CH; Daelemans, D; De Clercq, E; Huang, B; Kang, D; Lee, KH; Liu, J; Liu, X; Liu, Z; Pannecouque, C; Tian, Y; Zhan, P; Zhang, H | 1 |
Byrareddy, SN; Kongsted, J; Kramer, VG; Kurup, S; Liu, X; Namasivayam, V; Vanangamudi, M; Zhan, P | 1 |
Daelemans, D; De Clercq, E; Kang, D; Liu, X; Pannecouque, C; Tian, Y; Wang, Z; Yu, Z; Zhan, P; Zhang, J | 1 |
Anderson, KS; Frey, KM; Gannam, ZTK; Jorgensen, WL; Kudalkar, SN; Lee, WG; Sasaki, T; Spasov, KA | 1 |
Arnold, E; De Clercq, E; Fang, Z; Feng, D; Kang, D; Liu, X; Pannecouque, C; Pilch, A; Ruiz, FX; Sun, Y; Wang, Z; Wei, F; Zhan, P; Zhao, T | 1 |
De Clercq, E; Frutos-Beltrán, E; Gao, P; Kang, D; Li, W; Liu, X; Menéndez-Arias, L; Pannecouque, C; Song, S; Sun, B; Zhan, P; Zhang, J; Zou, J | 1 |
Arnold, E; De Clercq, E; Feng, D; Gao, S; Jing, L; Kang, D; Liu, X; Pannecouque, C; Ruiz, FX; Sun, L; Sun, Y; Wang, Z; Zhan, P; Zhang, T | 1 |
Chen, FE; De Clercq, E; Ding, L; Pannecouque, C; Zhuang, C | 3 |
Daelemans, D; De Clercq, E; Gao, P; Ginex, T; Huang, B; Jiang, X; Kang, D; Liu, X; Luque, FJ; Pannecouque, C; Zhan, P; Zhang, J | 1 |
Baidya, ATK; Das, B; Kumar, R; Mathew, AT; Yadav, AK | 1 |
Cherukupalli, S; De Clercq, E; Jia, R; Jiang, X; Kang, D; Liu, X; Pannecouque, C; Wang, W; Wang, Z; Xie, M; Zhan, P | 1 |
Chen, FE; De Clercq, E; Huang, WJ; Jin, X; Pannecouque, C; Wang, S; Zhang, YX; Zhao, LM | 1 |
Chen, FE; Clercq, E; Hao, QQ; Ling, X; Pannecouque, C | 1 |
Dranchak, PK; Huang, R; Inglese, J; Lamy, L; Oliphant, E; Queme, B; Tao, D; Wang, Y; Xia, M | 1 |
Boone, LR | 1 |
Fulco, PP; McNicholl, IR | 1 |
Crauwels, HM; Kakuda, TN | 1 |
Back, D; Else, L; Hughes, A; Khoo, S; Siccardi, M; Tjia, J; Watson, V | 1 |
Birkus, G; Brendza, KM; Hung, M; Jin, D; Kutty, N; Lansdon, EB; Liu, X; Mukund, S; Wang, R | 1 |
Coluccia, A; La Regina, G; Silvestri, R | 1 |
Tian, XT; Xie, L | 1 |
Ananworanich, J; Bhakeecheep, S; Bowonwattanuwong, C; Bunupuradah, T; Chetchotisakd, P; Hirschel, B; Jirajariyavej, S; Kantipong, P; Klinbuayaem, V; Munsakul, W; Petoumenos, K; Prasithsirikul, W; Ruxrungtham, K; Sirivichayakul, S; Sungkanuparph, S | 1 |
Giaquinto, C; Penazzato, M | 1 |
Balamane, M; Fessel, WJ; Katzenstein, DA; Melikian, GL; Shafer, RW; Varghese, V | 1 |
Calvez, V; Flandre, P; Fofana, DB; Fourati, S; Katlama, C; Lambert, S; Malet, I; Marcelin, AG; Sayon, S; Simon, A; Soulie, C; Wirden, M | 1 |
Dilanchian, P; Jayaweera, D | 1 |
Asahchop, EL; Brenner, BG; Ibanescu, IR; Moisi, D; Oliveira, M; Tremblay, C; Wainberg, MA; Xu, H | 1 |
Lacombe, K; Surgers, L | 1 |
Chang, TK; Lau, AJ; Sharma, D; Sherman, MA | 2 |
Asahchop, EL; Colby-Germinario, SP; Han, Y; McCallum, M; Oliveira, M; Quan, Y; Sarafianos, SG; Schader, SM; Wainberg, MA; Xu, HT | 1 |
Calvez, V; Fofana, DB; Fourati, S; Lambert-Niclot, S; Maiga, AI; Malet, I; Marcelin, AG; Soulie, C; Tounkara, A; Traore, HA; Wirden, M | 1 |
Colby-Germinario, SP; Han, Y; Huang, W; Oliveira, M; Petropoulos, CJ; Quan, Y; Wainberg, MA; Xu, HT | 1 |
Colby-Germinario, SP; Han, Y; Oliveira, M; Quan, Y; Wainberg, MA; Xu, HT; Zanichelli, V | 1 |
Haddad, M; Napolitano, LA; Picchio, GR; Rimsky, LT; Van Eygen, V; Vingerhoets, J | 1 |
Crawford, KW | 1 |
Aboulker, JP; Charreau, I; de Castro, N; Delaugerre, C; Gallien, S; Mahjoub, N; Molina, JM; Nere, ML; Simon, F | 1 |
Feng, M; Grobler, JA; Hazuda, DJ; Lai, MT; Miller, MD; Wang, D | 1 |
Álvarez, M; Andrés, C; Betancor, G; Marcelli, B; Martínez, MA; Menéndez-Arias, L | 1 |
Bertelsen, KM; Crauwels, HM; Hoetelmans, RM; Kakuda, TN; Leopold, L; Nijs, S; Stevens, M; Tomaka, F; van Delft, Y; Vandevoorde, A; Witek, J | 1 |
Hannongbua, S; Ishii, K; Kato, K; Thammaporn, R; Uchiyama, S; Yagi-Utsumi, M | 1 |
Avihingsanon, A; Mekprasan, S; Ohata, PJ; Putcharoen, O; Ruxrungtham, K; Sirivichayakul, S; Teeranaipong, P | 1 |
Marzinke, MA; Parsons, TL | 1 |
Gomathi, S; Kantor, R; Kausalya, B; Mothi, SN; Pachamuthu, B; Pradeep, A; Saravanan, S; Selvamuthu, P; Sivamalar, S; Smith, DM; Sunil, S | 1 |
Diphoko, T; Essex, M; Gaseitsiwe, S; Kasvosve, I; Makhema, J; Marlink, R; Moyo, S; Musonda, R; Novitsky, V; Okatch, H; Wainberg, M | 1 |
Agher, R; Calvez, V; Katlama, C; Marcelin, AG; Nguyen, T; Nouchi, A; Sayon, S; Simon, A; Soulie, C; Valantin, MA | 1 |
Abraham, OC; Demosthenes, JP; Ghale, BC; Kannangai, R; Ramalingam, VV; Rupali, P; Varghese, GM | 1 |
Andreoni, M; Antinori, A; Bagnarelli, P; Borghi, V; Bruzzone, B; Callegaro, AP; De Gennaro, M; Gianotti, N; Maffongelli, G; Maggiolo, F; Saladini, F; Sterrantino, G; Vergori, A; Zaccarelli, M; Zazzi, M | 1 |
Dunn, KJ; Kagan, RM; Kaufman, HW; Nettles, RE; Snell, GP | 1 |
Baszczyňski, O; Brumshtein, B; Dračínský, M; Janeba, Z; Jansa, P; Kaiser, MM; Lansdon, EB; Lee, YJ; Prener, L; Stepan, G; Yu, H | 1 |
Castagna, A; Celesia, BM; Cenderello, G; Corbelli, GM; Ferrara, M; Giammarino, F; Gianotti, N; Maggiolo, F; Martellotta, F; Rusconi, S; Saladini, F; Santoro, MM; Spagnuolo, V; Zazzi, M | 1 |
9 review(s) available for etravirine and rilpivirine
Article | Year |
---|---|
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
Topics: Acetamides; Anti-HIV Agents; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Prodrugs; Pyridones; Reverse Transcriptase Inhibitors; Triazoles | 2019 |
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Topics: Drug Discovery; Hydrogen Bonding; Molecular Structure; Prodrugs; Solubility | 2022 |
Next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Animals; Anti-HIV Agents; Azepines; Clinical Trials as Topic; Drug Design; Drug Evaluation, Preclinical; Drug Resistance, Viral; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Mutation; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2006 |
Etravirine and rilpivirine: nonnucleoside reverse transcriptase inhibitors with activity against human immunodeficiency virus type 1 strains resistant to previous nonnucleoside agents.
Topics: Anti-HIV Agents; Drug Resistance, Viral; HIV Infections; HIV-1; Humans; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2009 |
Looking for an active conformation of the future HIV type-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Binding Sites; Cell Line; Drug Design; Drug Resistance, Viral; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Indoles; Models, Molecular; Molecular Conformation; Nitriles; Phosphinic Acids; Pyrazoles; Pyridazines; Pyridines; Pyrimidines; Quinoxalines; Reverse Transcriptase Inhibitors; Rilpivirine | 2010 |
[Discovery and development of diarylpyrimidines (DAPYs) as next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs)].
Topics: Anti-HIV Agents; Drug Resistance, Viral; HIV Infections; HIV-1; Humans; Molecular Structure; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2010 |
Role of non-nucleoside reverse transcriptase inhibitors in treating HIV-infected children.
Topics: Adolescent; Alkynes; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Benzoxazines; Child; Child, Preschool; Cyclopropanes; HIV Infections; Humans; Infant; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2011 |
New therapeutic landscape of NNRTIs for treatment of HIV: a look at recent data.
Topics: Antiretroviral Therapy, Highly Active; Clinical Trials as Topic; Drug Resistance, Viral; HIV; HIV Infections; Humans; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2012 |
Hepatoxicity of new antiretrovirals: a systematic review.
Topics: Anti-Retroviral Agents; Chemical and Drug Induced Liver Injury; Clinical Trials as Topic; Cyclohexanes; Darunavir; Heterocyclic Compounds, 3-Ring; Humans; Maraviroc; Nitriles; Oxazines; Piperazines; Pyridazines; Pyridones; Pyrimidines; Pyrrolidinones; Quinolones; Raltegravir Potassium; Rilpivirine; Sulfonamides; Triazoles | 2013 |
3 trial(s) available for etravirine and rilpivirine
Article | Year |
---|---|
Etravirine and rilpivirine resistance in HIV-1 subtype CRF01_AE-infected adults failing non-nucleoside reverse transcriptase inhibitor-based regimens.
Topics: Adult; Alkynes; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; Female; Genotype; HIV Infections; HIV-1; Humans; Lamivudine; Male; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; RNA, Viral; Stavudine | 2011 |
Archived HIV-1 DNA resistance mutations to rilpivirine and etravirine in successfully treated HIV-1-infected individuals pre-exposed to efavirenz or nevirapine.
Topics: Adult; Aged; Alkynes; Antiretroviral Therapy, Highly Active; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; Female; Genotype; HIV Infections; HIV-1; Humans; Male; Microbial Sensitivity Tests; Middle Aged; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Retreatment; Reverse Transcriptase Inhibitors; Rilpivirine; Young Adult | 2015 |
Pharmacokinetic interaction between etravirine or rilpivirine and telaprevir in healthy volunteers: A randomized, two-way crossover trial.
Topics: Adolescent; Adult; Anti-HIV Agents; Cross-Over Studies; Drug Interactions; Female; Healthy Volunteers; Humans; Male; Middle Aged; Nitriles; Oligopeptides; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Young Adult | 2014 |
59 other study(ies) available for etravirine and rilpivirine
Article | Year |
---|---|
Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability.
Topics: Absorption; Administration, Oral; Animals; Biological Availability; Chemical Phenomena; Chemistry, Physical; Gastrointestinal Tract; Half-Life; Humans; Hydrogen-Ion Concentration; Hydrophobic and Hydrophilic Interactions; Light; Microscopy, Electron, Transmission; Models, Biological; Pyrimidines; Rats; Reverse Transcriptase Inhibitors; Scattering, Radiation; Solutions; Triazines | 2005 |
Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
Topics: Anti-HIV Agents; Drug Resistance, Viral; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Pyridines; Structure-Activity Relationship | 2009 |
Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
Topics: Animals; Antimalarials; DNA, Protozoan; Drug Discovery; Drug Resistance; Erythrocytes; Flow Cytometry; Malaria, Falciparum; Parasitic Sensitivity Tests; Plasmodium falciparum; RNA, Protozoan; Structure-Activity Relationship | 2009 |
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cell Line; Cells, Cultured; Cyclopropanes; Drug Resistance, Viral; HIV Infections; HIV-1; Humans; Molecular Structure; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Rilpivirine | 2010 |
Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
Topics: Anti-HIV Agents; Catechols; Computer Simulation; Ethers; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Molecular Structure; Protein Binding; Quantitative Structure-Activity Relationship; Reverse Transcriptase Inhibitors; Stereoisomerism; T-Lymphocytes | 2011 |
Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
Topics: Anti-HIV Agents; Benzodiazepines; Binding Sites; Crystallography, X-Ray; Drug Design; HIV Reverse Transcriptase; HIV-1; Hydrogen Bonding; Imidazoles; Indoles; Nitriles; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2012 |
Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
Topics: Aniline Compounds; Anti-HIV Agents; Cell Line; Drug Design; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; In Vitro Techniques; Microsomes, Liver; Mutation; Reverse Transcriptase Inhibitors; Solubility; Stereoisomerism; Structure-Activity Relationship; Virus Replication | 2012 |
Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Topics: Crystallography, X-Ray; Drug Design; HIV Reverse Transcriptase; HIV-1; Microbial Sensitivity Tests; Models, Molecular; Reverse Transcriptase Inhibitors | 2012 |
Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
Topics: Anti-HIV Agents; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2013 |
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
Topics: Anti-HIV Agents; Benzophenones; Cell Line, Tumor; Dose-Response Relationship, Drug; Drug Design; HIV Reverse Transcriptase; HIV-1; HIV-2; Humans; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2013 |
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
Topics: Anti-HIV Agents; Cell Line, Transformed; Cell Proliferation; Dose-Response Relationship, Drug; HIV-1; Humans; Hydrazines; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Solubility; Structure-Activity Relationship | 2013 |
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
Topics: Animals; Anti-HIV Agents; Cells, Cultured; Crystallography, X-Ray; Dogs; Drug Discovery; Drug Resistance, Viral; HIV-1; Humans; Inhibitory Concentration 50; Molecular Structure; Mutation; Pyridones; Rats; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Triazoles | 2014 |
Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
Topics: Anti-HIV Agents; Crystallization; Dose-Response Relationship, Drug; Drug Discovery; HIV Reverse Transcriptase; HIV-1; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Pyridones; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2014 |
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
Topics: | 2014 |
Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
Topics: Anti-Bacterial Agents; Anti-HIV Agents; Carboxylic Acids; DNA-Directed RNA Polymerases; Dose-Response Relationship, Drug; Drug Discovery; Enzyme Inhibitors; Escherichia coli; HEK293 Cells; HeLa Cells; HIV; Humans; Microbial Sensitivity Tests; Molecular Structure; RNA-Directed DNA Polymerase; Structure-Activity Relationship; Thiophenes | 2016 |
Computer-aided discovery of anti-HIV agents.
Topics: Anti-HIV Agents; Computer-Aided Design; Dose-Response Relationship, Drug; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; T-Lymphocytes | 2016 |
Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
Topics: Aniline Compounds; Anti-HIV Agents; Dose-Response Relationship, Drug; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Microbial Sensitivity Tests; Molecular Structure; Mutation; Reverse Transcriptase Inhibitors; Rilpivirine; Structure-Activity Relationship; Virus Replication | 2017 |
Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
Topics: Anti-HIV Agents; Drug Design; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Niacinamide; Point Mutation; Structure-Activity Relationship; Triazoles | 2018 |
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.
Topics: Animals; Anti-HIV Agents; Clinical Trials as Topic; Drug Discovery; HIV Infections; HIV-1; Humans; Reverse Transcriptase Inhibitors | 2019 |
Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase.
Topics: Anti-HIV Agents; Catechols; Drug Design; HIV Reverse Transcriptase; Molecular Structure; Reverse Transcriptase Inhibitors | 2019 |
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
Topics: Animals; Anti-HIV Agents; Cell Line; Crystallography, X-Ray; Drug Discovery; ERG1 Potassium Channel; Female; Fluorine; HIV Reverse Transcriptase; HIV-1; Humans; Male; Mice; Microsomes, Liver; Molecular Structure; Protein Binding; Pyrimidines; Rats, Wistar; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Thiophenes | 2020 |
Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
Topics: Anti-HIV Agents; Dose-Response Relationship, Drug; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Indoles; Molecular Structure; Mutation; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Sulfones | 2021 |
2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
Topics: Animals; Anti-HIV Agents; Crystallography, X-Ray; Drug Design; HEK293 Cells; HIV Reverse Transcriptase; HIV-1; Humans; Mice; Microbial Sensitivity Tests; Molecular Structure; Mutation; Protein Binding; Pyrimidines; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
Topics: Alkylation; Animals; Binding Sites; Biphenyl Compounds; Cell Line; Cell Survival; Drug Design; Drug Stability; Female; Half-Life; HIV Reverse Transcriptase; Humans; Hydrophobic and Hydrophilic Interactions; Mice; Microsomes, Liver; Molecular Docking Simulation; Mutation; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
Topics: Animals; Anti-HIV Agents; Dose-Response Relationship, Drug; Female; HIV Reverse Transcriptase; HIV-1; Humans; Male; Mice; Microbial Sensitivity Tests; Microsomes, Liver; Models, Molecular; Molecular Structure; Pyrimidines; Rats; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
Topics: Anti-HIV Agents; Cell Line; Drug Design; Heterocyclic Compounds, 2-Ring; HIV Reverse Transcriptase; HIV-1; Humans; Microsomes, Liver; Molecular Dynamics Simulation; Molecular Structure; Mutation; Protein Binding; Pyridines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
Topics: Animals; Anti-HIV Agents; Binding Sites; Cell Survival; Cytochrome P-450 Enzyme System; Drug Design; Drug Resistance, Viral; Drug Stability; Female; Half-Life; HIV Reverse Transcriptase; HIV-1; Humans; Mice; Molecular Docking Simulation; Mutation; Pyridines; Pyrimidines; Solubility; Structure-Activity Relationship | 2022 |
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
Topics: Anti-HIV Agents; Chemistry, Pharmaceutical; Heterocyclic Compounds, 1-Ring; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Reverse Transcriptase Inhibitors | 2022 |
Structure-Based Discovery of Novel NH
Topics: Anti-HIV Agents; Biphenyl Compounds; Drug Design; Heterocyclic Compounds, 1-Ring; HIV Reverse Transcriptase; HIV-1; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2022 |
Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
Topics: Animals; Anti-HIV Agents; HIV Reverse Transcriptase; HIV-1; Mice; Molecular Docking Simulation; Rats; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2022 |
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
Topics: Animals; Caenorhabditis elegans; Drug Discovery; High-Throughput Screening Assays; Humans; Proteomics; Small Molecule Libraries | 2023 |
Drug interactions with new and investigational antiretrovirals.
Topics: Anti-HIV Agents; Dose-Response Relationship, Drug; Drug Interactions; Humans; Nitriles; Pyridazines; Pyrimidines; Rilpivirine | 2010 |
Validation of a rapid and sensitive high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) assay for the simultaneous determination of existing and new antiretroviral compounds.
Topics: Analysis of Variance; Anti-HIV Agents; Chromatography, High Pressure Liquid; Cyclohexanes; Drug Stability; Maraviroc; Nitriles; Pyridazines; Pyrimidines; Reproducibility of Results; Rilpivirine; Sensitivity and Specificity; Tandem Mass Spectrometry; Triazoles | 2010 |
Crystal structures of HIV-1 reverse transcriptase with etravirine (TMC125) and rilpivirine (TMC278): implications for drug design.
Topics: Binding Sites; Crystallography, X-Ray; Drug Design; HIV Reverse Transcriptase; HIV-1; Models, Molecular; Mutation; Nitriles; Protein Binding; Protein Conformation; Pyridazines; Pyrimidines; Rilpivirine | 2010 |
Panel of prototypical recombinant infectious molecular clones resistant to nevirapine, efavirenz, etravirine, and rilpivirine.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cloning, Molecular; Cyclopropanes; Drug Resistance, Multiple, Viral; Drug Resistance, Viral; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2012 |
E138K and M184I mutations in HIV-1 reverse transcriptase coemerge as a result of APOBEC3 editing in the absence of drug exposure.
Topics: Adenine; Anti-HIV Agents; APOBEC Deaminases; Cytidine Deaminase; Cytosine Deaminase; DNA Mutational Analysis; Drug Resistance, Viral; Female; Glutamic Acid; HIV Reverse Transcriptase; HIV-1; Humans; Isoleucine; Lysine; Male; Methionine; Mutation; Nitriles; Organophosphonates; Pyridazines; Pyrimidines; Rilpivirine; Tenofovir; Treatment Failure; Virus Replication | 2012 |
[HIV therapy of the next generation. Modern active drugs for long-term treatment].
Topics: Anti-HIV Agents; Clinical Trials as Topic; Darunavir; Drug Administration Schedule; Drug Therapy, Combination; Drugs, Investigational; HIV Infections; Humans; Long-Term Care; Nitriles; Pyridazines; Pyrimidines; Rilpivirine; Sulfonamides | 2012 |
Distinct resistance patterns to etravirine and rilpivirine in viruses containing nonnucleoside reverse transcriptase inhibitor mutations at baseline.
Topics: Anti-HIV Agents; DNA Mutational Analysis; Drug Resistance, Viral; Genotype; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Mutagenesis, Site-Directed; Mutation, Missense; Nitriles; Pyridazines; Pyrimidines; Rilpivirine; Selection, Genetic; Serial Passage; Virus Replication | 2013 |
Agonism of human pregnane X receptor by rilpivirine and etravirine: comparison with first generation non-nucleoside reverse transcriptase inhibitors.
Topics: Cell Line, Tumor; Dose-Response Relationship, Drug; Fluorescence Resonance Energy Transfer; Genes, Reporter; Humans; Hydroxylation; Nitriles; Pregnane X Receptor; Pyridazines; Pyrimidines; Real-Time Polymerase Chain Reaction; Receptors, Steroid; Reverse Transcriptase Inhibitors; Reverse Transcriptase Polymerase Chain Reaction; Rilpivirine; Steroid Hydroxylases; Two-Hybrid System Techniques | 2013 |
Effect of mutations at position E138 in HIV-1 reverse transcriptase and their interactions with the M184I mutation on defining patterns of resistance to nonnucleoside reverse transcriptase inhibitors rilpivirine and etravirine.
Topics: Anti-HIV Agents; Cells, Cultured; Drug Resistance, Viral; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Mutation; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Virus Replication | 2013 |
Genetic barrier to the development of resistance to rilpivirine and etravirine between HIV-1 subtypes CRF02_AG and B.
Topics: Anti-HIV Agents; Conserved Sequence; Drug Resistance, Viral; Genotype; HIV-1; Humans; Mutation, Missense; Nitriles; Pyridazines; Pyrimidines; Rilpivirine | 2013 |
Role of the K101E substitution in HIV-1 reverse transcriptase in resistance to rilpivirine and other nonnucleoside reverse transcriptase inhibitors.
Topics: Alkynes; Amino Acid Substitution; Benzoxazines; Cyclopropanes; Delavirdine; Deoxycytidine; Drug Resistance, Viral; Emtricitabine; HEK293 Cells; HIV Reverse Transcriptase; HIV-1; Humans; Leukocytes, Mononuclear; Microbial Sensitivity Tests; Mutagenesis, Site-Directed; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Virus Replication | 2013 |
The connection domain mutation N348I in HIV-1 reverse transcriptase enhances resistance to etravirine and rilpivirine but restricts the emergence of the E138K resistance mutation by diminishing viral replication capacity.
Topics: Amino Acid Motifs; Drug Resistance, Viral; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Mutation, Missense; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Virus Replication | 2014 |
Prevalence in the USA of rilpivirine resistance-associated mutations in clinical samples and effects on phenotypic susceptibility to rilpivirine and etravirine.
Topics: Anti-HIV Agents; Drug Resistance, Viral; Genotype; HIV Infections; HIV-1; Humans; Microbial Sensitivity Tests; Mutation; Nitriles; Prevalence; Pyridazines; Pyrimidines; Rilpivirine; United States | 2014 |
Etravirine and rilpivirine-specific mutations selected by efavirenz and nevirapine exposure in patients infected with HIV-1 non-B subtypes.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; Genotype; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Mutation, Missense; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Rilpivirine; Treatment Outcome; Viral Load | 2014 |
Differential activation of human constitutive androstane receptor and its SV23 and SV24 splice variants by rilpivirine and etravirine.
Topics: Adolescent; Adult; Aged; Alternative Splicing; Constitutive Androstane Receptor; Cytochrome P-450 CYP2B6; Dose-Response Relationship, Drug; Female; Hep G2 Cells; Hepatocytes; Humans; Male; Molecular Structure; Nitriles; Pyridazines; Pyrimidines; Receptors, Cytoplasmic and Nuclear; Reverse Transcriptase Inhibitors; Rilpivirine; Structure-Activity Relationship; Tumor Cells, Cultured; Young Adult | 2015 |
In vitro resistance selection with doravirine (MK-1439), a novel nonnucleoside reverse transcriptase inhibitor with distinct mutation development pathways.
Topics: Anti-HIV Agents; Drug Resistance, Viral; HEK293 Cells; HIV-1; Humans; Mutation; Nitriles; Pyridazines; Pyridones; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Selection, Genetic; Triazoles | 2015 |
Effects of HIV-1 reverse transcriptase connection subdomain mutations on polypurine tract removal and initiation of (+)-strand DNA synthesis.
Topics: Anti-HIV Agents; DNA; Drug Resistance, Viral; HIV Reverse Transcriptase; Mutation; Nitriles; Protein Structure, Tertiary; Purines; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Ribonuclease H; Rilpivirine; RNA; Templates, Genetic | 2015 |
Mass Spectrometric Characterization of HIV-1 Reverse Transcriptase Interactions with Non-nucleoside Reverse Transcriptase Inhibitors.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cyclopropanes; HIV Reverse Transcriptase; Mass Spectrometry; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2016 |
Role of Rilpivirine and Etravirine in Efavirenz and Nevirapine-Based Regimens Failure in a Resource-Limited Country: A Cross- Sectional Study.
Topics: Adult; Alkynes; Anti-HIV Agents; Benzoxazines; Cross-Sectional Studies; Cyclopropanes; Drug Resistance, Viral; Female; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Male; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Thailand; Viral Load; Young Adult | 2016 |
Development and validation of a liquid chromatographic-tandem mass spectrometric method for the multiplexed quantification of etravirine, maraviroc, raltegravir, and rilpivirine in human plasma and tissue.
Topics: Chromatography, Liquid; Cyclohexanes; Humans; Maraviroc; Nitriles; Pyridazines; Pyrimidines; Raltegravir Potassium; Reproducibility of Results; Rilpivirine; Tandem Mass Spectrometry; Triazoles | 2016 |
Etravirine and Rilpivirine Drug Resistance Among HIV-1 Subtype C Infected Children Failing Non-Nucleoside Reverse Transcriptase Inhibitor-Based Regimens in South India.
Topics: Adolescent; Anti-HIV Agents; Child; Child, Preschool; Drug Resistance, Viral; Female; Genotype; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; India; Male; Mutation, Missense; Nitriles; Pyridazines; Pyrimidines; Retrospective Studies; Rilpivirine; Sequence Analysis, DNA; Treatment Failure | 2017 |
Prevalence of Rilpivirine and Etravirine Resistance Mutations in HIV-1 Subtype C-Infected Patients Failing Nevirapine or Efavirenz-Based Combination Antiretroviral Therapy in Botswana.
Topics: Adult; Alkynes; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Benzoxazines; Botswana; Cyclopropanes; Drug Resistance, Viral; Female; Genotype; Genotyping Techniques; HIV Infections; HIV-1; Humans; Male; Microbial Sensitivity Tests; Mutation; Nevirapine; Nitriles; pol Gene Products, Human Immunodeficiency Virus; Prevalence; Pyridazines; Pyrimidines; Rilpivirine; Treatment Failure; Young Adult | 2018 |
Dynamics of drug resistance-associated mutations in HIV-1 DNA reverse transcriptase sequence during effective ART.
Topics: Anti-HIV Agents; DNA, Viral; Drug Resistance, Viral; Emtricitabine; Evolution, Molecular; Female; HIV Reverse Transcriptase; HIV-1; Humans; Lamivudine; Male; Middle Aged; Mutation; Nitriles; Pyridazines; Pyrimidines; Rilpivirine; RNA, Viral | 2018 |
Frequency of cross-resistance to rilpivirine and etravirine among HIV-1 subtype C infected individuals failing nevirapine/efavirenz based ART regimen.
Topics: Alkynes; Benzoxazines; Cyclopropanes; HIV Infections; HIV-1; Humans; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Rilpivirine; Sweden | 2019 |
Prevalence of predicted resistance to doravirine in HIV-1-positive patients after exposure to non-nucleoside reverse transcriptase inhibitors.
Topics: Adult; Alkynes; Anti-HIV Agents; Benzoxazines; Cross-Sectional Studies; Cyclopropanes; Delavirdine; Drug Resistance, Viral; Female; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Male; Nevirapine; Nitriles; Pyridazines; Pyridones; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Treatment Outcome; Triazoles | 2019 |
Trends in HIV-1 Drug Resistance Mutations from a U.S. Reference Laboratory from 2006 to 2017.
Topics: Anti-HIV Agents; Darunavir; Dideoxynucleosides; Drug Resistance, Viral; Genotype; Heterocyclic Compounds, 3-Ring; HIV Infections; HIV Integrase Inhibitors; HIV Protease Inhibitors; HIV-1; Humans; Mutation; Nitriles; Oxazines; Piperazines; Pyridazines; Pyridones; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2019 |
Design and Synthesis of Novel HIV-1 NNRTIs with Bicyclic Cores and with Improved Physicochemical Properties.
Topics: Anti-HIV Agents; Drug Design; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Reverse Transcriptase Inhibitors; Rilpivirine | 2023 |
Residual phenotypic susceptibility to doravirine in multidrug-resistant HIV-1 from subjects enrolled in the PRESTIGIO Registry.
Topics: Anti-HIV Agents; Drug Resistance, Viral; Female; HIV Infections; HIV-1; Humans; Male; Middle Aged; Mutation; Reverse Transcriptase Inhibitors; Rilpivirine | 2023 |