Page last updated: 2024-11-08

racivir

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

Cross-References

ID SourceID
PubMed CID9837769
CHEMBL ID161381
SCHEMBL ID122131
MeSH IDM0204281

Synonyms (34)

Synonym
AC-392
LS-13423
racivir
FT-0667848
FT-0667849
CHEMBL161381
ftc, dl-
emtricitabine, (+/-)-
A808077
4-amino-5-fluoro-1-[(2r,5s)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-1,2-dihydropyrimidin-2-one
AKOS015964253
FT-0601789
SCHEMBL122131
4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-2 (1h)-pyrimidinone
4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-2(1h)-pyrimidinone
XQSPYNMVSIKCOC-UHFFFAOYSA-N ,
4-amino-5-fluoro-1-(2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1h)-one
144371-00-6
F2173-0571
mfcd00870151
4-amino-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2(1h)-one
4-amino-5-fluoro-1-((2r,5s)-rel-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1h)-one
HMS3655G21
5-epi emtricitabine
4-amino-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-1,2-dihydropyrimidin-2-one
BCP02951
SB18984
SY109006
4-amino-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one
SB58547
SB46757
DTXSID60861371
2-epi-(-)-emtricitabine
EN300-296204

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic parameters were generated by area/moment analysis."( Pharmacokinetics of 2',3'-dideoxy-5-fluoro-3'-thiacytidine in rats.
Abobo, CV; Boudinot, FD; Liotta, DC; Ni, L; Schinazi, RF, 1994
)
0.29
" Plasma concentrations from a group of 54 rats, 12 pregnant rabbits and 60 dogs enrolled in large toxicity studies using a wide variety of oral doses, were compared using non-compartment pharmacokinetic modelling versus dose, treatment duration, species and gender."( Comparative pharmacokinetics of Racivir, (+/-)-beta-2',3'-dideoxy-5-fluoro-3'-thiacytidine in rats, rabbits, dogs, monkeys and HIV-infected humans.
Hurwitz, SJ; Otto, MJ; Schinazi, RF, 2005
)
0.33
" Pharmacokinetic parameters were dose proportional, and the maximum concentration of drug in serum at all doses exceeded the 90% effective concentration for wild-type HIV-1."( Safety, pharmacokinetics, and efficacy of (+/-)-beta-2',3'-dideoxy-5-fluoro-3'-thiacytidine with efavirenz and stavudine in antiretroviral-naïve human immunodeficiency virus-infected patients.
Arastèh, K; Beard, A; Cartee, L; Drauz, D; Herzmann, C; Kreckel, P; Murphy, RL; Otto, MJ; Schinazi, RF; Schulbin, H, 2005
)
0.33

Bioavailability

ExcerptReferenceRelevance
" Absorption of FTC after oral administration was rapid, with bioavailability averaging 73 +/- 6%."( Pharmacokinetics and metabolism of racemic 2',3'-dideoxy-5-fluoro-3'-thiacytidine in rhesus monkeys.
Boudinot, FD; Ibrahim, SS; Liotta, DC; Manning, C; McClure, HM; Schinazi, RF, 1992
)
0.28
" The pharmacokinetics and bioavailability of 524W91 after oral dosing were studied in mice dosed with 10, 100, and 600 mg of 524W91 per kg of body weight by the oral and intravenous routes."( Pharmacokinetics, oral bioavailability, and metabolism in mice and cynomolgus monkeys of (2'R,5'S-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl] cytosine, an agent active against human immunodeficiency virus and human hepatitis B virus.
Frick, LW; Lambe, CU; Nelson, DJ; St John, L; Taylor, LC, 1994
)
0.29
"1 liters/h/kg, and the oral bioavailability was 90% +/- 8%."( Pharmacokinetics, oral bioavailability, and metabolic disposition in rats of (-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl] cytosine, a nucleoside analog active against human immunodeficiency virus and hepatitis B virus.
Frick, LW; Furfine, ES; Furman, PA; Liotta, DC; Nelson, DJ; Painter, GR; St John, L; Taylor, LC, 1993
)
0.29

Dosage Studied

ExcerptRelevanceReference
"15 cells showed reductions in levels of HBV in serum and in intracellular levels of HBV when the mice were orally dosed with (-) cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine (FTC)."( Evaluation of the potent anti-hepatitis B virus agent (-) cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine in a novel in vivo model.
Condreay, LD; Daluge, SM; Ellis, MN; Furman, PA; Jansen, RW; Johnson, LC; Paff, MT; Painter, GR; Powdrill, TF; Selleseth, DW, 1994
)
0.29
" The pharmacokinetics and bioavailability of 524W91 after oral dosing were studied in mice dosed with 10, 100, and 600 mg of 524W91 per kg of body weight by the oral and intravenous routes."( Pharmacokinetics, oral bioavailability, and metabolism in mice and cynomolgus monkeys of (2'R,5'S-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl] cytosine, an agent active against human immunodeficiency virus and human hepatitis B virus.
Frick, LW; Lambe, CU; Nelson, DJ; St John, L; Taylor, LC, 1994
)
0.29
" This study highlights the importance of selecting animal species that demonstrate similar cytidine deaminase activity to humans when performing preclinical dosing studies on Racivir and other antiviral agents that are substrates for mammalian cytidine deaminases."( Comparative pharmacokinetics of Racivir, (+/-)-beta-2',3'-dideoxy-5-fluoro-3'-thiacytidine in rats, rabbits, dogs, monkeys and HIV-infected humans.
Hurwitz, SJ; Otto, MJ; Schinazi, RF, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's22 (70.97)18.2507
2000's7 (22.58)29.6817
2010's2 (6.45)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (12.90%)5.53%
Reviews2 (6.45%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other25 (80.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Randomized, Double-Blind, Placebo-Controlled, Multicenter Study Exploring the Safety, Tolerability, and Antiviral Effect of Substituting 600 mg Racivir for 3TC in HIV-Infected Subjects Who Have the M184V Mutation and Are Currently Failing on a HAART Regim [NCT00121979]Phase 260 participants Interventional2004-09-30Completed
[NCT00040300]Phase 118 participants Interventional2002-06-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]