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 Source | ID |
---|---|
PubMed CID | 44232529 |
CHEMBL ID | 2104968 |
SCHEMBL ID | 1035677 |
MeSH ID | M0528267 |
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
Excerpt | Reference | Relevance |
---|---|---|
" 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
Excerpt | Reference | Relevance |
---|---|---|
" 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
Excerpt | Reference | Relevance |
---|---|---|
" 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
Excerpt | Reference | Relevance |
---|---|---|
" 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
Excerpt | Relevance | Reference |
---|---|---|
" 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 ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1286671 | Antiviral 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 assay | 2016 | Journal 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. |
AID1286690 | Half life in fed beagle dog at 5 mg/kg, po by LC-MS/MS method | 2016 | Journal 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. |
AID1286696 | Oral bioavailability in fasted Sprague-Dawley rat at 10 mg/kg after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286702 | Half life in human hepatocytes | 2016 | Journal 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. |
AID1286701 | Half life in monkey hepatocytes | 2016 | Journal 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. |
AID1286699 | Half life in rat hepatocytes | 2016 | Journal 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. |
AID1286679 | Cmax in fasted Sprague-Dawley rat at 10 mg/kg, po after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286697 | Oral bioavailability in fed beagle dog at 5 mg/kg after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286691 | Half life in fed cynomolgus monkey at 1 mg/kg, iv by LC-MS/MS method | 2016 | Journal 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. |
AID1286672 | Antiviral 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 assay | 2016 | Journal 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. |
AID1286670 | Antiviral 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 assay | 2016 | Journal 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. |
AID1286683 | Cmax in fed cynomolgus monkey at 5 mg/kg, po after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286685 | Tmax in fed beagle dog at 5 mg/kg, po by LC-MS/MS method | 2016 | Journal 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. |
AID1286693 | Clearance in fasted Sprague-Dawley rat at 2 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286703 | Potency index, ratio of EFV EC50 to compound EC50 for HIV1 harboring reverse transcriptase K103N mutant | 2016 | Journal 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. |
AID1286681 | Cmax in fed beagle dog at 5 mg/kg, po after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286698 | Oral bioavailability in fed cynomolgus monkey at 5 mg/kg after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286694 | Clearance in fed beagle dog at 1 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286689 | Half life in fed beagle dog at 1 mg/kg, iv by LC-MS/MS method | 2016 | Journal 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. |
AID1286684 | Tmax in fasted Sprague-Dawley rat at 10 mg/kg, po by LC-MS/MS method | 2016 | Journal 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. |
AID701088 | Antiviral 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-control | 2012 | Journal 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. |
AID1286682 | Cmax in fed cynomolgus monkey at 1 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286695 | Clearance in fed cynomolgus monkey at 1 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286687 | Half life in fasted Sprague-Dawley rat at 2 mg/kg, iv by LC-MS/MS method | 2016 | Journal 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. |
AID1286678 | Cmax in fasted Sprague-Dawley rat at 2 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286680 | Cmax in fed beagle dog at 1 mg/kg, iv after 0.083 to 24 hrs by LC-MS/MS method | 2016 | Journal 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. |
AID1286686 | Tmax in fed cynomolgus monkey at 5 mg/kg, po by LC-MS/MS method | 2016 | Journal 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. |
AID1286669 | Antiviral 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 assay | 2016 | Journal 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. |
AID1286700 | Half life in dog hepatocytes | 2016 | Journal 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. |
AID1286704 | Potency index, ratio of EFV EC50 to compound EC50 for HIV1 harboring reverse transcriptase Y181C/K103N double mutant | 2016 | Journal 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. |
AID1286677 | Aqueous solubility of the compound at pH 7 | 2016 | Journal 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. |
AID1286692 | Half life in fed cynomolgus monkey at 5 mg/kg, po by LC-MS/MS method | 2016 | Journal 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. |
AID1286688 | Half life in fasted Sprague-Dawley rat at 10 mg/kg, po by LC-MS/MS method | 2016 | Journal 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)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 4 (33.33) | 29.6817 |
2010's | 8 (66.67) | 24.3611 |
2020's | 0 (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.
| This Compound (16.80) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 5 (41.67%) | 5.53% |
Reviews | 3 (25.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 4 (33.33%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |