Compounds > idx 899
Page last updated: 2024-11-13

idx 899

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

IDX 899: a reverse transcriptase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44232529
CHEMBL ID2104968
SCHEMBL ID1035677
MeSH IDM0528267

Synonyms (21)

Synonym
gsk2248761
idx-899
idx899
gsk-2248761
idx-12899
fosdevirine
D09906
fosdevirine (usan/inn)
1018450-26-4
gsk-2248761a
CHEMBL2104968
SCHEMBL1035677
1097733-15-7
gsk 2248761
idx 899
5dv ,
EN300-37081906
(r)-(methyl (2-carbamoyl-5-chloro-1h-indol-3-yl)[3-(2-cyanoeth-1-en-1-yl)-5-methylphenyl]phosphinate)
DTXSID501031227
HY-14891
CS-0003617

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" IDX899 was well tolerated; and no serious adverse events, dose-dependent adverse events, or laboratory abnormalities were detected."( Single-dose escalation and multiple-dose safety, tolerability, and pharmacokinetics of IDX899, a candidate human immunodeficiency virus type 1 nonnucleoside reverse transcriptase inhibitor, in healthy subjects.
Belanger, B; Chen, J; Damphousse, D; Mayers, D; Pietropaolo, K; Sullivan-Bólyai, J; Zhou, XJ, 2009)		0.35
" Adverse events, viral load (VL), PK, and reverse transcriptase mutations were assessed and combined for analysis."( Safety and efficacy of GSK2248761, a next-generation nonnucleoside reverse transcriptase inhibitor, in treatment-naive HIV-1-infected subjects.
Dudas, K; Dumont, E; Kim, J; Lou, Y; Mayers, D; Pietropaolo, K; Piscitelli, S; St Clair, M; White, S; Zala, C; Zhou, XJ, 2012)		0.38

Pharmacokinetics

ExcerptReferenceRelevance
" These data show for the first time that IDX899 and IDX989 possess favorable pharmacokinetic properties in humans, including high mean absolute bioavailability and long half-life."( Microdose pharmacokinetics of IDX899 and IDX989, candidate HIV-1 non-nucleoside reverse transcriptase inhibitors, following oral and intravenous administration in healthy male subjects.
Garner, RC; Kissling, CJ; Mayers, D; Nicholson, S; Zhou, XJ, 2009)		0.35

Compound-Compound Interactions

ExcerptReferenceRelevance
" Mean plasma concentration-time profiles for atazanavir, tenofovir disoproxil fumarate/emtricitabine (TDF/FTC), darunavir (DRV, administered with ritonavir [RTV]), and drospirenone/ethinylestradiol were similar following co-administration of GSK2248761."( Drug interaction profile for GSK2248761, a next generation non-nucleoside reverse transcriptase inhibitor.
de Serres, M; Gould, E; Johnson, M; Kim, J; Lou, Y; Mayers, D; Pietropaolo, K; Piscitelli, S; White, S; Zhou, XJ, 2012)		0.38

Bioavailability

ExcerptReferenceRelevance
" For the parent drug, mean absolute bioavailability is 61% and 65% for IDX899 and IDX989, respectively."( Microdose pharmacokinetics of IDX899 and IDX989, candidate HIV-1 non-nucleoside reverse transcriptase inhibitors, following oral and intravenous administration in healthy male subjects.
Garner, RC; Kissling, CJ; Mayers, D; Nicholson, S; Zhou, XJ, 2009)		0.35

Dosage Studied

ExcerptRelevanceReference
" The levels of plasma exposure were similar between the single dosing and the repeat dosing with 800 mg QD and was approximately twofold higher with 400 mg BID."( Single-dose escalation and multiple-dose safety, tolerability, and pharmacokinetics of IDX899, a candidate human immunodeficiency virus type 1 nonnucleoside reverse transcriptase inhibitor, in healthy subjects.
Belanger, B; Chen, J; Damphousse, D; Mayers, D; Pietropaolo, K; Sullivan-Bólyai, J; Zhou, XJ, 2009)		0.35
" Because a dose-response relationship was not identified, a second study examined a lower, 30-mg QD dose in 8 subjects (6 active and 2 placebo)."( Safety and efficacy of GSK2248761, a next-generation nonnucleoside reverse transcriptase inhibitor, in treatment-naive HIV-1-infected subjects.
Dudas, K; Dumont, E; Kim, J; Lou, Y; Mayers, D; Pietropaolo, K; Piscitelli, S; St Clair, M; White, S; Zala, C; Zhou, XJ, 2012)		0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (33)

Assay IDTitleYearJournalArticle
AID1286671Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286690Half life in fed beagle dog at 5 mg/kg, po by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286696Oral bioavailability in fasted Sprague-Dawley rat at 10 mg/kg after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286702Half life in human hepatocytes2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286701Half life in monkey hepatocytes2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286699Half life in rat hepatocytes2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286679Cmax in fasted Sprague-Dawley rat at 10 mg/kg, po after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286697Oral bioavailability in fed beagle dog at 5 mg/kg after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286691Half life in fed cynomolgus monkey at 1 mg/kg, iv by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286672Antiviral activity against HIV1 harboring reverse transcriptase Y181C/K103N double mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286670Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286683Cmax in fed cynomolgus monkey at 5 mg/kg, po after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286685Tmax in fed beagle dog at 5 mg/kg, po by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286693Clearance in fasted Sprague-Dawley rat at 2 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286703Potency index, ratio of EFV EC50 to compound EC50 for HIV1 harboring reverse transcriptase K103N mutant2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286681Cmax in fed beagle dog at 5 mg/kg, po after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286698Oral bioavailability in fed cynomolgus monkey at 5 mg/kg after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286694Clearance in fed beagle dog at 1 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286689Half life in fed beagle dog at 1 mg/kg, iv by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286684Tmax in fasted Sprague-Dawley rat at 10 mg/kg, po by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID701088Antiviral activity against HIV1 infected in human assessed as log reduction in viral load at 800 mg administered QD for 7 days measured on day 8 relative to placebo-control2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
AID1286682Cmax in fed cynomolgus monkey at 1 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286695Clearance in fed cynomolgus monkey at 1 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286687Half life in fasted Sprague-Dawley rat at 2 mg/kg, iv by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286678Cmax in fasted Sprague-Dawley rat at 2 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286680Cmax in fed beagle dog at 1 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286686Tmax in fed cynomolgus monkey at 5 mg/kg, po by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286669Antiviral activity against HIV1 BH10 harboring wild type reverse transcriptase infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286700Half life in dog hepatocytes2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286704Potency index, ratio of EFV EC50 to compound EC50 for HIV1 harboring reverse transcriptase Y181C/K103N double mutant2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286677Aqueous solubility of the compound at pH 72016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286692Half life in fed cynomolgus monkey at 5 mg/kg, po by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
AID1286688Half life in fasted Sprague-Dawley rat at 10 mg/kg, po by LC-MS/MS method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (33.33)29.6817
2010's8 (66.67)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.80

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.80 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.80)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (41.67%)5.53%
Reviews3 (25.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (33.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
adenine
[no description available]		7.5446-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
loviride
loviride: structure given in first source; inhibits virion and recombinant HIV-1 reverse transcriptase		2.0710
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.		7.54417-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
quinoxalines
quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.		3.1510mancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		7.544pyrrole;
secondary amine
fluorobenzenes
Fluorobenzenes: Derivatives of BENZENE that contain FLUORINE.. monofluorobenzene : The simplest member of the class of monofluorobenzenes that is benzene carrying a single fluoro substituent.. fluorobenzenes : Any fluoroarene that is a benzene or a substituted benzene carrying at least one fluoro group.		7.544monofluorobenzenesNMR chemical shift reference compound
deoxycytidine
[no description available]		7.544pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
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.		2.0710azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
simvastatin
Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.		7.544delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)		EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug
atorvastatin
[no description available]		7.544aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)		environmental contaminant;
xenobiotic
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.		7.544monothioacetal;
nucleoside analogue;
organofluorine compound;
pyrimidone		antiviral drug;
HIV-1 reverse transcriptase inhibitor
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		4.821acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
lopinavir
[no description available]		7.544amphetamines;
dicarboxylic acid diamide		anticoronaviral agent;
antiviral drug;
HIV protease inhibitor
drospirenone and ethinyl estradiol combination
drospirenone and ethinyl estradiol combination: female oral combined contraceptive containing 30 mcg (0.030 mg) Ethinyl Estradiol and 3 mg drospirenone (Androstenes)		7.544
atazanavir sulfate
Atazanavir Sulfate: An azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS.		7.544organic sulfate salt
organophosphonates
hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.		7.544divalent inorganic anion;
phosphite ion
etravirine
[no description available]		3.5720aminopyrimidine;
aromatic ether;
dinitrile;
organobromine compound		antiviral agent;
HIV-1 reverse transcriptase inhibitor
darunavir
Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors.		7.544carbamate ester;
furofuran;
sulfonamide		antiviral drug;
HIV protease inhibitor
ritonavir
Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		7.5441,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
l 737126
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: structure given in first source; an inhibitor of HIV-1 reverse transcriptase		2.0710
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.		7.544nucleoside analogue;
phosphonic acids		antiviral drug;
drug metabolite;
HIV-1 reverse transcriptase inhibitor
r 82150
R 82150: structure given in first source; inhibits HIV-1 replication		2.0710
hby 097
HBY 097: a quinoxaline derivative		3.1510
rilpivirine
[no description available]		4.3630aminopyrimidine;
nitrile		EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor
uk 453,061
UK 453,061: a reverse transcriptase inhibitor/anti-HIV agent; structure in first source		3.5720aromatic ether
raltegravir potassium
Raltegravir Potassium: A pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION.		7.544
ConditionIndicatedRelationship StrengthStudiesTrials
Absence Seizure
[description not available]		03.4811
HIV Coinfection
[description not available]		07.4152
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		03.4811
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).		07.4152
Adverse Drug Event
[description not available]		04.3711
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		04.3711