Page last updated: 2024-09-05

dapivirine and etravirine

dapivirine has been researched along with etravirine in 19 studies

Compound Research Comparison

Studies
(dapivirine)
Trials
(dapivirine)
Recent Studies (post-2010)
(dapivirine)
Studies
(etravirine)
Trials
(etravirine)
Recent Studies (post-2010) (etravirine)
1966416057290321

Protein Interaction Comparison

ProteinTaxonomydapivirine (IC50)etravirine (IC50)
Chain A, Reverse transcriptase/ribonuclease HHIV-1 M:B_HXB2R0.0021
Chain B, p51 RTHIV-1 M:B_HXB2R0.0021
Chain A, Reverse transcriptase/ribonuclease HHIV-1 M:B_HXB2R0.0021
Chain B, p51 RTHIV-1 M:B_HXB2R0.0021
ATP-binding cassette sub-family C member 3Homo sapiens (human)5.1
Cytochrome P450 1A2Homo sapiens (human)0.025
ATP-dependent translocase ABCB1Homo sapiens (human)7.6
Cytochrome P450 3A4Homo sapiens (human)0.019
Cytochrome P450 2D6Homo sapiens (human)0.032
Cytochrome P450 2C9 Homo sapiens (human)0.017
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (NEW YORK-5 ISOLATE)0.37
CruzipainTrypanosoma cruzi4
Multidrug resistance-associated protein 1 Homo sapiens (human)8.5
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)0.01
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)0.097
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)0.01
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)0.01
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)0.01
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)0.01
Reverse transcriptase/RNaseH Human immunodeficiency virus 10.2711
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)0.01
Canalicular multispecific organic anion transporter 1Homo sapiens (human)7.8
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)0.01
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)6
Reverse transcriptase Human immunodeficiency virus 10.0186

Research

Studies (19)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's10 (52.63)29.6817
2010's8 (42.11)24.3611
2020's1 (5.26)2.80

Authors

AuthorsStudies
Andries, K; Arnold, E; Azijn, H; Daeyaert, FF; Das, K; de Béthune, MP; De Corte, BL; de Jonge, MR; Heeres, J; Ho, CY; Janssen, PA; Kavash, RW; Koymans, LM; Kukla, MJ; Lewi, PJ; Lichtenstein, MA; Ludovici, DW; Pauwels, R; Van Aken, KJ; Ye, H1
Andries, K; Arnold, E; Boyer, PL; Clark, AD; Clark, P; Daeyaert, F; Das, K; De Béthune, MP; De Corte, B; De Jonge, MR; Heeres, J; Ho, CY; Hughes, SH; Janssen, PA; Kavash, RW; Koymans, LM; Kukla, MJ; Lewi, PJ; Lichtenstein, MA; Ludovici, DW; Pauwels, R; Vinkers, HM; Ye, H1
De Corte, BL1
Arnold, E; Clark, AD; Das, K; Frenkel, YV; Janssen, PA; Lewi, PJ; Wang, YH1
Bharadwaj, A; Thakur, A; Thakur, M; Thakur, S1
Chen, FE; Liang, YH1
Chen, CH; Jiang, S; Lai, W; Lee, KH; Lu, H; Qin, B; Tian, X; Xie, L1
Bar-Magen, T; Brenner, BG; Oliveira, M; Quan, Y; Schader, SM; Wainberg, MA; Xu, H1
Bar-Magen, T; Oliveira, M; Quan, Y; Schader, SM; Wainberg, MA; Xu, HT1
Anderson, KS; Bollini, M; Cisneros, JA; Jorgensen, WL; Spasov, KA1
Collu, G; Giliberti, G; La Colla, P; Loddo, R; Loksha, YM; Pedersen, EB; Sanna, G1
Ariën, KK; Augustyns, K; Cos, P; Dirié, B; Heeres, J; Joossens, J; Lewi, PJ; Lyssens, S; Maes, L; Michiels, J; Van der Veken, P; Vanham, G; Venkatraj, M1
Jorgensen, WL1
Gu, SX; Ju, XL; Liu, GY; Lu, HH; Zhu, YY1
Armijos Rivera, JI; Badia, R; Cirilli, R; Crespan, E; Esté, JA; Forgione, M; Hailu, GS; Kirillov, IA; Lucidi, A; Maga, G; Mai, A; Nawrozkij, MB; Panella, C; Patsilinakos, A; Ragno, R; Riveira-Muñoz, E; Rotili, D; Tomaselli, D; Yablokov, AS1
Dranchak, PK; Huang, R; Inglese, J; Lamy, L; Oliphant, E; Queme, B; Tao, D; Wang, Y; Xia, M1
Tarby, CM1
Fransen, K; Garcia, S; Janssen, CG; Janssen, PA; Kestens, L; Lewi, PJ; Njai, HF; Vanham, G1
Colby-Germinario, SP; Han, Y; Huang, W; Oliveira, M; Petropoulos, CJ; Quan, Y; Wainberg, MA; Xu, HT1

Reviews

3 review(s) available for dapivirine and etravirine

ArticleYear
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.
    Journal of medicinal chemistry, 2005, Mar-24, Volume: 48, Issue:6

    Topics: Anti-HIV Agents; Benzodiazepines; Drug Design; Drug Resistance, Viral; HIV Reverse Transcriptase; Imidazoles; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors

2005
Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
    European journal of medicinal chemistry, 2018, Oct-05, Volume: 158

    Topics: Anti-HIV Agents; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship

2018
Recent advances in the development of next generation non-nucleoside reverse transcriptase inhibitors.
    Current topics in medicinal chemistry, 2004, Volume: 4, Issue:10

    Topics: Anti-HIV Agents; Clinical Trials as Topic; Coumarins; HIV Reverse Transcriptase; Humans; Imidazoles; Molecular Structure; Nitriles; Patents as Topic; Pyranocoumarins; Pyridazines; Pyrimidines; Quinazolines; Reverse Transcriptase Inhibitors; Sulfur Compounds

2004

Other Studies

16 other study(ies) available for dapivirine and etravirine

ArticleYear
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
    Bioorganic & medicinal chemistry letters, 2001, Sep-03, Volume: 11, Issue:17

    Topics: Anti-HIV Agents; Drug Evaluation, Preclinical; HIV Reverse Transcriptase; HIV-1; Inhibitory Concentration 50; Mutation; Nitriles; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship

2001
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
    Journal of medicinal chemistry, 2004, May-06, Volume: 47, Issue:10

    Topics: Anti-HIV Agents; Crystallography, X-Ray; Drug Resistance, Viral; HIV Reverse Transcriptase; Models, Molecular; Mutation; Nitriles; Protein Conformation; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors

2004
Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability.
    Journal of medicinal chemistry, 2005, Mar-24, Volume: 48, Issue:6

    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
SAR and QSAR studies: modelling of new DAPY derivatives.
    European journal of medicinal chemistry, 2008, Volume: 43, Issue:3

    Topics: Models, Molecular; Pyrimidines; Quantitative Structure-Activity Relationship; Reverse Transcriptase Inhibitors; Structure-Activity Relationship

2008
QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
    European journal of medicinal chemistry, 2009, Volume: 44, Issue:2

    Topics: HIV-1; Hydrophobic and Hydrophilic Interactions; Models, Molecular; Mutation, Missense; Pyrimidines; Quantitative Structure-Activity Relationship

2009
Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
    Bioorganic & medicinal chemistry letters, 2009, Sep-15, Volume: 19, Issue:18

    Topics: Anti-HIV Agents; Drug Resistance, Viral; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Pyridines; Structure-Activity Relationship

2009
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
    Antimicrobial agents and chemotherapy, 2009, Volume: 53, Issue:11

    Topics: Anti-HIV Agents; Drug Resistance, Viral; HIV Reverse Transcriptase; Microbial Sensitivity Tests; Mutation; Nitriles; Pyridazines; Pyrimidines; Recombinant Proteins; Reverse Transcriptase Inhibitors

2009
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:6

    Topics: Anti-HIV Agents; Base Sequence; Cell Line; DNA, Viral; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Mutation; Recombinant Proteins; Reverse Transcriptase Inhibitors; Virus Replication

2010
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
    Bioorganic & medicinal chemistry letters, 2013, Sep-15, Volume: 23, Issue:18

    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
Synthesis of novel fluoro analogues of MKC442 as microbicides.
    Journal of medicinal chemistry, 2014, Jun-26, Volume: 57, Issue:12

    Topics: Anti-HIV Agents; Cell Line; Drug Resistance, Viral; HIV Protease Inhibitors; HIV Reverse Transcriptase; HIV-1; Humans; Mutation; Pyrimidinones; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Uracil

2014
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
    Bioorganic & medicinal chemistry, 2014, Oct-01, Volume: 22, Issue:19

    Topics: Anti-HIV Agents; Cell Line; Cell Survival; Dose-Response Relationship, Drug; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Structure; Parasitic Sensitivity Tests; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Trypanocidal Agents; Trypanosoma brucei brucei; Trypanosoma brucei rhodesiense

2014
Computer-aided discovery of anti-HIV agents.
    Bioorganic & medicinal chemistry, 2016, 10-15, Volume: 24, Issue:20

    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
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
    Journal of medicinal chemistry, 2019, 01-24, Volume: 62, Issue:2

    Topics: Anti-HIV Agents; Binding Sites; Cell Line; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Mutation; Protein Structure, Tertiary; Pyrimidinones; Stereoisomerism; Structure-Activity Relationship

2019
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
    Disease models & mechanisms, 2023, 03-01, Volume: 16, Issue:3

    Topics: Animals; Caenorhabditis elegans; Drug Discovery; High-Throughput Screening Assays; Humans; Proteomics; Small Molecule Libraries

2023
Pre-incubation of cell-free HIV-1 group M isolates with non-nucleoside reverse transcriptase inhibitors blocks subsequent viral replication in co-cultures of dendritic cells and T cells.
    Antiviral therapy, 2005, Volume: 10, Issue:2

    Topics: CD4-Positive T-Lymphocytes; Coculture Techniques; Dendritic Cells; Dose-Response Relationship, Drug; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Leukocytes, Mononuclear; Nitriles; Pyridazines; Pyrimidines; Virus Replication

2005
Role of the K101E substitution in HIV-1 reverse transcriptase in resistance to rilpivirine and other nonnucleoside reverse transcriptase inhibitors.
    Antimicrobial agents and chemotherapy, 2013, Volume: 57, Issue:11

    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