Compounds > epoxyfarnesyl diazoacetate
Page last updated: 2024-12-11

epoxyfarnesyl diazoacetate

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Description

2'-deoxy-4'-C-ethynyl-2-fluoroadenosine: has anti-HIV activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6483431
CHEMBL ID517231
SCHEMBL ID2528556
MeSH IDM0121227

Synonyms (39)

Synonym
(2r,3s,5r)-5-(6-amino-2-fluoro-purin-9-yl)-2-ethynyl-2-(hydroxymethyl)tetrahydrofuran-3-ol
4'-e-d2-fa
2f-eda
e2-fda
4'-ethynyl-2-fluoro-2'-deoxyadenosine
9h-purin-6-amine, 9-(2-deoxy-4-c-ethynyl-.beta.-d-erythro-pentofuranosyl)-2-fluoro-
efda
mk-8591
islatravir
islatravir anhydrous
CHEMBL517231
(2r,3s,5r)-5-(6-amino-2-fluoropurin-9-yl)-2-ethynyl-2-(hydroxymethyl)oxolan-3-ol
2'-deoxy-4'-c-ethynyl-2-fluoroadenosine
IKKXOSBHLYMWAE-QRPMWFLTSA-N
SCHEMBL2528556
islatravir [usan]
islatravir [inn]
islatravir [who-dd]
865363-93-5
QPQ082R25D ,
adenosine, 2'-deoxy-4'-c-ethynyl-2-fluoro-
2'-deoxy-4'-ethynyl-2-fluoroadenosine
mk8591
unii-qpq082r25d
AKOS028113263
HY-104012
CS-0023675
(2r,3s,5r)-5-(6-amino-2-fluoro-9h-purin-9-yl)-2-ethynyl-2-(hydroxymethyl)tetrahydrofuran-3-ol
Q24977417
D11432
islatravir (usan)
A51131
MS-24188
nsc-787789
nsc787789
A848914
2'-deoxy-4'-c-ethynyl-2-fluoroadenosine;mk-8591
mk-8591 (islatravir)
DTXSID601046407

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" 27 (90%) participants had 60 adverse events after receipt of drug, of which 21 (35%) were deemed to be drug related."( Safety, pharmacokinetics, and antiretroviral activity of islatravir (ISL, MK-8591), a novel nucleoside reverse transcriptase translocation inhibitor, following single-dose administration to treatment-naive adults infected with HIV-1: an open-label, phase
De Lepeleire, I; Friedman, E; Grobler, JA; Hofmann, J; Hüser, A; Iwamoto, M; Keicher, C; Matthews, RP; Robberechts, M; Rudd, DJ; Schürmann, D; Stoch, SA; Zhang, S, 2020)		0.56
" Islatravir was generally well-tolerated, with no serious adverse events or discontinuations due to adverse events."( Safety, tolerability, and pharmacokinetics of single- and multiple-dose administration of islatravir (MK-8591) in adults without HIV.
Ankrom, W; De Lepeleire, I; Friedman, E; Grobler, JA; Iwamoto, M; Jackson Rudd, D; Liu, Y; Matthews, RP; Mogg, R; Panebianco, D; Petkova, M; Stoch, SA, 2021)		0.62
" The most frequently reported adverse events were mild-to-moderate implant-site reactions (induration, hematoma, pain)."( Safety and pharmacokinetics of islatravir subdermal implant for HIV-1 pre-exposure prophylaxis: a randomized, placebo-controlled phase 1 trial.
Barrett, SE; Goodey, A; Grobler, JA; Haspeslagh, L; Iwamoto, M; Matthews, RP; Patel, M; Reynders, T; Rottey, S; Stoch, SA; Vargo, RC; Zhang, S, 2021)		0.62
" Safety was assessed by adverse event (AE) reporting."( Brief Report: Efficacy and Safety of Oral Islatravir Once Daily in Combination With Doravirine Through 96 Weeks for Treatment-Naive Adults With HIV-1 Infection Receiving Initial Treatment With Islatravir, Doravirine, and Lamivudine.
Afani Saud, A; Bettacchi, C; Chahin Anania, C; Correll, T; Eves, K; Grandhi, A; Hanna, GJ; Hepler, D; Hwang, C; Klopfer, SO; Molina, JM; Robertson, MN; Yazdanpanah, Y, 2022)		0.72

Pharmacokinetics

ExcerptReferenceRelevance
" In preclinical studies, intracellular islatravir-triphosphate exhibits a long half-life and prolonged virological effects."( Safety, pharmacokinetics, and antiretroviral activity of islatravir (ISL, MK-8591), a novel nucleoside reverse transcriptase translocation inhibitor, following single-dose administration to treatment-naive adults infected with HIV-1: an open-label, phase
De Lepeleire, I; Friedman, E; Grobler, JA; Hofmann, J; Hüser, A; Iwamoto, M; Keicher, C; Matthews, RP; Robberechts, M; Rudd, DJ; Schürmann, D; Stoch, SA; Zhang, S, 2020)		0.56
"Islatravir (MK-8591) is a highly potent type 1 human immunodeficiency virus (HIV-1) nucleoside reverse transcriptase translocation inhibitor with a long intracellular half-life that is in development for the prevention and treatment of HIV-1."( Safety and pharmacokinetics of islatravir subdermal implant for HIV-1 pre-exposure prophylaxis: a randomized, placebo-controlled phase 1 trial.
Barrett, SE; Goodey, A; Grobler, JA; Haspeslagh, L; Iwamoto, M; Matthews, RP; Patel, M; Reynders, T; Rottey, S; Stoch, SA; Vargo, RC; Zhang, S, 2021)		0.62
" Blood samples were taken at prespecified time points for pharmacokinetic analysis of islatravir (plasma) and islatravir-triphosphate (ISL-TP; peripheral blood mononuclear cells [PBMCs])."( Safety and Pharmacokinetics of Once-Daily Multiple-Dose Administration of Islatravir in Adults Without HIV.
Fillgrove, KL; Grobler, JA; Iwamoto, M; Jackson Rudd, D; Matthews, RP; Sterling, LM; Stoch, SA; Vargo, RC; Zhang, S, 2021)		0.62
" The apparent terminal half-life of ISL-TP was 177-209 hours."( Safety and Pharmacokinetics of Once-Daily Multiple-Dose Administration of Islatravir in Adults Without HIV.
Fillgrove, KL; Grobler, JA; Iwamoto, M; Jackson Rudd, D; Matthews, RP; Sterling, LM; Stoch, SA; Vargo, RC; Zhang, S, 2021)		0.62

Compound-Compound Interactions

ExcerptReferenceRelevance
" Doravirine in combination with islatravir has the potential to be a potent two-drug regimen that warrants further clinical development."( Islatravir in combination with doravirine for treatment-naive adults with HIV-1 infection receiving initial treatment with islatravir, doravirine, and lamivudine: a phase 2b, randomised, double-blind, dose-ranging trial.
Afani Saud, A; Bettacchi, C; Chahin Anania, C; Correll, T; DeJesus, E; Eves, K; Grandhi, A; Hanna, GJ; Hwang, C; Molina, JM; Olsen Klopfer, S; Robertson, MN; Sklar, P; Yazdanpanah, Y, 2021)		0.62
" The potential for islatravir to interact with commonly co-prescribed medications was studied in vitro."( Islatravir Is Not Expected to Be a Victim or Perpetrator of Drug-Drug Interactions via Major Drug-Metabolizing Enzymes or Transporters.
Bleasby, K; Fillgrove, KL; Guo, J; Hafey, M; Houle, R; Lin, M; Lu, B; Sanchez, RI, 2021)		0.62
" Because islatravir may be coadministered with other antiretroviral agents, assessment of potential drug-drug interactions are warranted."( Lack of a Clinically Meaningful Drug Interaction Between the HIV-1 Antiretroviral Agents Islatravir, Dolutegravir, and Tenofovir Disoproxil Fumarate.
Armas, D; Fillgrove, KL; Fox-Bosetti, S; Friedman, E; Iwamoto, M; Matthews, RP; Rudd, DJ; Stoch, SA; Zhang, S, 2021)		0.62
"Hormonal contraceptives are among the most effective forms of reversible contraception, but many other compounds, including some antiretrovirals, have clinically meaningful drug-drug interactions (DDIs) with hormonal contraceptives."( A phase 1, open-label study to evaluate the drug interaction between islatravir (MK-8591) and the oral contraceptive levonorgestrel/ethinyl estradiol in healthy adult females.
Ankrom, W; Brimhall, D; Fillgrove, KL; Gravesande, KN; Iwamoto, MN; Jackson Rudd, D; Matthews, RP; Stoch, SA; Zhang, S, 2021)		0.62
"The results of this trial support the use of LNG/EE contraceptives in combination with islatravir without dose adjustment."( A phase 1, open-label study to evaluate the drug interaction between islatravir (MK-8591) and the oral contraceptive levonorgestrel/ethinyl estradiol in healthy adult females.
Ankrom, W; Brimhall, D; Fillgrove, KL; Gravesande, KN; Iwamoto, MN; Jackson Rudd, D; Matthews, RP; Stoch, SA; Zhang, S, 2021)		0.62

Dosage Studied

ExcerptRelevanceReference
" Investigational antiretroviral drugs include the nucleoside analogue reverse transcriptase translocation inhibitor (NRTTI) MK-8591, a long-acting compound that could be dosed once weekly."( Investigational Antiretroviral Drugs: What is Coming Down the Pipeline.
Gulick, RM, 2018)		0.48
" As a result of the prolonged intracellular half-life of its active moiety, it is amenable to flexibility in dosing of at least daily to weekly and perhaps longer."( 4'-Ethynyl-2-fluoro-2'-deoxyadenosine, MK-8591: a novel HIV-1 reverse transcriptase translocation inhibitor.
Markowitz, M; Sarafianos, SG, 2018)		0.48
" Long-acting drug formulations requiring less-frequent dosing offer an opportunity to improve adherence and allow for more forgiving options with regard to missed doses."( Extended-Duration MK-8591-Eluting Implant as a Candidate for HIV Treatment and Prevention.
Barrett, SE; Doto, GJ; Fillgrove, KL; Forster, SP; Gindy, ME; Grobler, JA; Lebron, J; Li, L; Liu, Z; Lu, B; Mackey, MA; Niu, T; Sanchez, RI; Skomski, D; Sun, L; Teller, RS; Wood, SL; Yang, Z, 2018)		0.48
"Islatravir (4'-ethynyl-2-fluoro-2'-deoxyadenosine, MK-8591) is a long-acting first-in-class nucleoside reverse transcriptase translocation inhibitor with the potential for versatile dosing routes and dosing intervals."( Islatravir for the treatment and prevention of infection with the human immunodeficiency virus type 1.
Grobler, JA; Markowitz, M, 2020)		0.56
" Participants were enrolled in one of five consecutive dosing panels, receiving a single oral dose of islatravir (0·5-30 mg)."( Safety, pharmacokinetics, and antiretroviral activity of islatravir (ISL, MK-8591), a novel nucleoside reverse transcriptase translocation inhibitor, following single-dose administration to treatment-naive adults infected with HIV-1: an open-label, phase
De Lepeleire, I; Friedman, E; Grobler, JA; Hofmann, J; Hüser, A; Iwamoto, M; Keicher, C; Matthews, RP; Robberechts, M; Rudd, DJ; Schürmann, D; Stoch, SA; Zhang, S, 2020)		0.56
"Capsid inhibitors (CAI) demonstrate high potency and potential for extended-duration dosing in pre-clinical trials."( Novel Antiretroviral Agents.
Cambou, MC; Landovitz, RJ, 2020)		0.56
" In Study 1, 24 participants, assigned to 1 of 3 panels, received alternating single doses of islatravir in a fasted state from 5 mg to 400 mg, or placebo, over 3 dosing periods; a 30 mg dose was additionally assessed following a high-fat meal."( Safety, tolerability, and pharmacokinetics of single- and multiple-dose administration of islatravir (MK-8591) in adults without HIV.
Ankrom, W; De Lepeleire, I; Friedman, E; Grobler, JA; Iwamoto, M; Jackson Rudd, D; Liu, Y; Matthews, RP; Mogg, R; Panebianco, D; Petkova, M; Stoch, SA, 2021)		0.62
" Multiple once-daily dosing of islatravir in adults without HIV was generally well tolerated up to doses of 5 mg administered for up to 6 weeks."( Safety and Pharmacokinetics of Once-Daily Multiple-Dose Administration of Islatravir in Adults Without HIV.
Fillgrove, KL; Grobler, JA; Iwamoto, M; Jackson Rudd, D; Matthews, RP; Sterling, LM; Stoch, SA; Vargo, RC; Zhang, S, 2021)		0.62
"Islatravir is an investigational antiretroviral agent with unique pharmacologic properties that facilitate flexible dosing regimens."( Role of islatravir in HIV treatment and prevention: an update.
Cottrell, M; Derbalah, A; Karpick, HC; Maize, H; Rao, GG; Skersick, P, 2022)		0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (51)

Assay IDTitleYearJournalArticle
AID341354Metabolic stability of the compound in human CEM cells assessed as 3'-azido-2',3'-dideoxythymidine triphosphate intracellular levels at 200 nM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID582477Toxicity in HIV1 JR-FL infected human PBMC transplanted NOD/SCID/Janus kinase 3 knockout mouse assessed as adverse effect at 0.5 mg/kg, ip bid for 15 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID1656989Antiviral activity against HIV-1 3B infected in human MT4 cells incubated for 5 days by MTT assay2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Acetylene Group, Friend or Foe in Medicinal Chemistry.
AID1656991Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV-1 3B2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Acetylene Group, Friend or Foe in Medicinal Chemistry.
AID341190Metabolic stability of the compound in human CD4+ CEM cells assessed as 4'-ethynyl-2-fluoro-2'-deoxyadenosine triphosphate intracellular levels at 200 nM after 8 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID582475Toxicity in BALB/c mouse assessed as ruffled fur at 50 mg/kg, ip bid for 14 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID582478Antiviral activity against HIV1 JR-FL infected in human PBMC transplanted NOD/SCID/Janus kinase 3 knockout mouse assessed as decrease of p24 expressing human CD4+ cells in peritoneal cavity cells at 0.5 mg/kg, ip bid for 15 days by flow cytometry2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID341365Drug level in human CD4+CEM cells per 10'9 cells at 0.1 uM2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID582476Antiviral activity against HIV1 JR-FL infected in human PBMC transplanted NOD/SCID/Janus kinase 3 knockout mouse assessed as increase of CD4/CD8 ratio in PBMC at 0.5 mg/kg, ip bid for 15 days by flow cytometry2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID582468Drug level in BALB/c mouse blood at 20 mg/kg, ip2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID582480Antiviral activity against HIV1 JR-FL infected in human PBMC transplanted NOD/SCID/Janus kinase 3 knockout mouse assessed as decrease of p24 expressing human CD3+ cells in spleen cells at 0.5 mg/kg, ip bid for 15 days by flow cytometry2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID341184Cytotoxicity against human MT4 cells by MTT assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID341185Cytotoxicity against human PHA-PBMC cells by MTT assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID341353Metabolic stability of the compound in human CEM cells assessed as 3'-azido-2',3'-dideoxythymidine diphosphate intracellular levels at 200 nM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID341355Drug uptake in human CD4+CEM cells assessed as 4'-ethynyl-2-fluoro-2'-deoxyadenosine monophosphate half life at 200 nM2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID1387654AUC (0 to infinity) in Sprague-Dawley rat at 5 mg/kg, po2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4'-Ethynyl-2-fluoro-2'-deoxyadenosine).
AID1387650Antiviral activity against HIV1 infected in human PBMC incubated for 24 hrs in presence of 10% NHS by GFP based single cycle HIV replication assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4'-Ethynyl-2-fluoro-2'-deoxyadenosine).
AID1387657Half life in Sprague-Dawley rat at 1 mg/kg, iv2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4'-Ethynyl-2-fluoro-2'-deoxyadenosine).
AID582469Toxicity in BALB/c mouse assessed as change in body weight at 5 mg/kg, ip bid for 14 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID341186Drug level in human CD4+CEM cells assessed as increase in 4'-ethynyl-2-fluoro-2'-deoxyadenosine triphosphate level at 0.1 uM after 6 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID582470Toxicity in BALB/c mouse assessed as change in body weight at 50 mg/kg, ip bid for 14 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID341181Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID341372Antiviral activity against R5-HIV1MDR/G assessed as inhibition of p24 Gag protein in human PHA-PBMC by ELISA relative to X4-HIV1NL4-32007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID341371Ratio of EC50 for X4-HIV1MDR/C in human PHA-PBMC to EC50 for X4-HIV1NL4-3 in human MT4 cells2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID582467Tmax in BALB/c mouse at 20 mg/kg, ip2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID582481Antiviral activity against HIV1 JR-FL infected in human PBMC transplanted NOD/SCID/Janus kinase 3 knockout mouse assessed as increase of CD4/CD8 ratio in spleen at 0.5 mg/kg, ip bid for 15 days by flow cytometry2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID341182Antiviral activity against R5-HIV1MDR/C assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID582482Antiviral activity against HIV1 JR-FL infected in human PBMC transplanted NOD/SCID/Janus kinase 3 knockout mouse assessed as increase of CD4/CD8 ratio in peritoneal cavity at 0.5 mg/kg, ip bid for 15 days by flow cytometry2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID341352Metabolic stability of the compound in human CEM cells assessed as 3'-azido-2',3'-dideoxythymidine monophosphate intracellular levels at 200 nM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID1387653AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, iv2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4'-Ethynyl-2-fluoro-2'-deoxyadenosine).
AID341366Antiviral activity against HIV1 NL4-3 replication in human MT4 cells at 0.01 uM pretreated 24 hrs before infection assessed as protection at 0.01 uM by MTT assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID582473Toxicity in BALB/c mouse assessed as subacute whole-body effect at 5 mg/kg, ip bid for 14 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID341356Drug uptake in human CD4+CEM cells assessed as 4'-ethynyl-2-fluoro-2'-deoxyadenosine diphosphate half life at 200 nM2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID582483Antiviral activity against HIV1 JR-FL infected in human PBMC transplanted NOD/SCID/Janus kinase 3 knockout mouse assessed as decrease of viral p24 antigen level in plasma at 0.5 mg/kg, ip bid for 15 days by ELISA2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID582471Toxicity in BALB/c mouse assessed as acute whole-body effect at 5 mg/kg, ip bid for 14 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID341357Drug uptake in human CD4+CEM cells assessed as 4'-ethynyl-2-fluoro-2'-deoxyadenosine triphosphate half life at 200 nM2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID582472Toxicity in BALB/c mouse assessed as acute whole-body effect at 50 mg/kg, ip bid for 14 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID341188Metabolic stability of the compound in human CD4+ CEM cells assessed as 4'-ethynyl-2-fluoro-2'-deoxyadenosine monophosphate intracellular levels at 200 nM after 8 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID341189Metabolic stability of the compound in human CD4+ CEM cells assessed as 4'-ethynyl-2-fluoro-2'-deoxyadenosine diphosphate intracellular levels at 200 nM after 8 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID341367Antiviral activity against HIV1 NL4-3 replication in human MT4 cells at 0.01 uM pretreated 48 hrs before infection assessed as protection at 0.01 uM by MTT assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID341183Antiviral activity against R5-HIV1MDR/G assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID582479Antiviral activity against HIV1 JR-FL infected in human PBMC transplanted NOD/SCID/Janus kinase 3 knockout mouse assessed as decrease of p24 expressing human CD4+ cells in PBMC at 0.5 mg/kg, ip bid for 15 days by flow cytometry2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID582474Toxicity in BALB/c mouse assessed as subacute whole-body effect at 50 mg/kg, ip bid for 14 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID582484Antiviral activity against HIV1 JR-FL infected in human PBMC transplanted NOD/SCID/Janus kinase 3 knockout mouse assessed as decrease of viremia in plasma at 0.5 mg/kg, ip bid for 15 days by ELISA2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase 3 kno
AID1656990Cytotoxicity against human MT4 cells2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Acetylene Group, Friend or Foe in Medicinal Chemistry.
AID341370Ratio of EC50 for R5-HIV1MDR/MM in human PHA-PBMC to EC50 for R5-HIV1Ba-L in human PHA-PBMC2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID1387651Cytotoxicity in human MT4 cells expressing GFP assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4'-Ethynyl-2-fluoro-2'-deoxyadenosine).
AID341179Antiviral activity against R5-HIV1Ba-L assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID341180Antiviral activity against R5-HIV1MDR/MM assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.
AID1387656Clearance in Sprague-Dawley rat at 1 mg/kg, iv2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4'-Ethynyl-2-fluoro-2'-deoxyadenosine).
AID1387658Oral bioavailability in Sprague-Dawley rat at 5 mg/kg2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4'-Ethynyl-2-fluoro-2'-deoxyadenosine).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (67)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (8.96)29.6817
2010's32 (47.76)24.3611
2020's29 (43.28)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.15

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.15 (24.57)
Research Supply Index4.34 (2.92)
Research Growth Index5.49 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.15)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (13.43%)5.53%
Reviews7 (10.45%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other51 (76.12%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
adenine
[no description available]		4.47606-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
glyceraldehyde
Glyceraldehyde: An aldotriose containing the propionaldehyde structure with hydroxy groups at the 2- and 3-positions. It is involved in the formation of ADVANCED GLYCOSYLATION END PRODUCTS.. glyceraldehyde : An aldotriose comprising propanal having hydroxy groups at the 2- and 3-positions. It plays role in the formation of advanced glycation end-products (AGEs), a deleterious accompaniment to ageing.. aldose : Aldehydic parent sugars (polyhydroxy aldehydes H[CH(OH)]nC(=O)H, n >= 2) and their intramolecular hemiacetals.		2.0710aldotriosefundamental metabolite
triphosphoric acid
triphosphoric acid: used as water softener, peptizing agent, emulsifier & dispersing agent; ingredient of cleansers; meat preservative; RN given refers to parent cpd; structure		3.9911acyclic phosphorus acid anhydride;
phosphorus oxoacid
thymidine
[no description available]		2.110pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
metabolite;
mouse metabolite
bromouracil
Bromouracil: 5-Bromo-2,4(1H,3H)-pyrimidinedione. Brominated derivative of uracil that acts as an antimetabolite, substituting for thymine in DNA. It is used mainly as an experimental mutagen, but its deoxyriboside (BROMODEOXYURIDINE) is used to treat neoplasms.. 5-bromouracil : A pyrimidine having keto groups at the 2- and 4-positions and a bromo group at the 5-position. Used mainly as an experimental mutagen.		2.2510nucleobase analogue;
pyrimidines		mutagen
trifluoromethyluracil
[no description available]		2.2510
alanine
Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.		3.6920alanine zwitterion;
alanine;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid		EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor;
fundamental metabolite
ethinyl estradiol
Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.		3.71117-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
levonorgestrel
Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis.		3.71117beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound		contraceptive drug;
female contraceptive drug;
progestin;
synthetic oral contraceptive
deoxycytidine
[no description available]		2.4920pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
stavudine
Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase		2.2510dihydrofuran;
nucleoside analogue;
organic molecular entity		antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
selegiline
Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.		2.2510selegiline;
terminal acetylenic compound		geroprotector
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		2.4620azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
eniluracil
eniluracil: structure in first source; inactivates dihydropyrimidine dehydrogenase		2.2510pyrimidone
mifepristone
Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.		2.25103-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound		abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive
zileuton
[no description available]		2.25101-benzothiophenes;
ureas		anti-asthmatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor;
leukotriene antagonist;
non-steroidal anti-inflammatory drug
lamivudine
[no description available]		7.8862monothioacetal;
nucleoside analogue;
oxacycle;
primary alcohol		allergen;
anti-HBV agent;
antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor;
prodrug
emtricitabine
Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection.		4.3250monothioacetal;
nucleoside analogue;
organofluorine compound;
pyrimidone		antiviral drug;
HIV-1 reverse transcriptase inhibitor
amprenavir
[no description available]		2.0310carbamate ester;
sulfonamide;
tetrahydrofuryl ester		antiviral drug;
HIV protease inhibitor
2',3'-dideoxyadenosine triphosphate
[no description available]		2.0310purine deoxyribonucleoside triphosphate
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		7.66421,2,3-triazole
a-76745
fenleuton: LoFrin is tradename		2.2510
5-diazouracil
5-diazouracil: RN given refers to parent cpd; structure		2.2510
5-cyanouracil
[no description available]		2.2510
gefitinib
[no description available]		2.2510aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
erlotinib
[no description available]		2.2510aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
organophosphonates
hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.		2.7830divalent inorganic anion;
phosphite ion
tv3326
[no description available]		2.2510indanes
saquinavir
Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease.		2.0310L-asparagine derivative;
quinolines		antiviral drug;
HIV protease inhibitor
lamivudine triphosphate
[no description available]		2.1710
tenofovir
tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.		7.81102nucleoside analogue;
phosphonic acids		antiviral drug;
drug metabolite;
HIV-1 reverse transcriptase inhibitor
glycosides
[no description available]		2.1510
5-(2-bromovinyl)uracil
5-(2-bromovinyl)uracil: RN given refers to (E)-isomer		2.2510
2',3'-didehydro-3'-deoxy-4'-ethynylthymidine
2',3'-didehydro-3'-deoxy-4'-ethynylthymidine: a highly active anti-HIV agent; structure in first source		2.5520
bw b70c
BW B70C: arachidonic acid antagonist. BW B70C : A hydroxamic acid that is urea in which both the hydrogens attached to one of the nitrogens are replaced by a hydroxy and a (1E)-1-[3-(4-fluorophenoxy)phenyl]but-1-en-3-yl group. A selective inhibitor of arachidonate 5-lipoxygenase, it can be used for the treatment of asthma.		2.2510aromatic ether;
hydroxamic acid;
organofluorine compound;
ureas		EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor
deoxyribose
[no description available]		2.2510deoxypentosehuman metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
enviradene
[no description available]		2.2510
rilpivirine
[no description available]		4.6320aminopyrimidine;
nitrile		EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor
gs-7340
tenofovir alafenamide: component of Biktarvy. tenofovir alafenamide : An L-alanine derivative that is isopropyl L-alaninate in which one of the amino hydrogens is replaced by an (S)-({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)(phenoxy)phosphoryl group. A prodrug for tenofovir, it is used (as the fumarate salt) in combination therapy for the treatment of HIV-1 infection.		3.69206-aminopurines;
ether;
isopropyl ester;
L-alanine derivative;
phosphoramidate ester		antiviral drug;
HIV-1 reverse transcriptase inhibitor;
prodrug
pf9601n
[no description available]		2.2510
bms-663068
fostemsavir: an HIV-1 attachment inhibitor; structure in first source		3.3510
lucifer yellow
lucifer yellow: RN given refers to di-Li salt		2.110organic lithium saltfluorochrome
gsk1265744
[no description available]		4.3310difluorobenzene;
monocarboxylic acid amide;
organic heterotricyclic compound;
secondary carboxamide		HIV-1 integrase inhibitor
dolutegravir
[no description available]		4.0421difluorobenzene;
monocarboxylic acid amide;
organic heterotricyclic compound;
secondary carboxamide		HIV-1 integrase inhibitor
doravirine
[no description available]		7.6642
bictegravir
bictegravir: HIV Integrase Inhibitors. bictegravir : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxylic acid with the amino group of 2,4,6-trifluorobenzylamine. It is a second-generation integrase strand transfer inhibitor (INSTI) and used (as its sodium salt) for the treatment of HIV-1.		2.1710monocarboxylic acid amide;
organic heterotetracyclic compound;
secondary carboxamide;
trifluorobenzene		HIV-1 integrase inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
HIV Coinfection
[description not available]		012.93399
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).		117.557818
Vaccine Preventable Diseases
[description not available]		02.2110
AIDS, Simian
[description not available]		03.7730
Acute Kidney Failure
[description not available]		02.3110
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		02.3110
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.8430
Genital Tract Infections
[description not available]		02.1310
Recrudescence
[description not available]		02.0710
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.		02.0710