Pharmacokinetics of 2’,3’-Dideoxy-5-fluoro-3’-thiacytidine in Rats

Effect of Oral Administration of Emtricitabine on Woodchuck Hepatitis Virus Replication in Chronically Infected Woodchucks

“…In a previously published report, (Ϫ)FTC was shown to be moderately effective against WHV replication in chronically infected woodchucks when delivered by intraperitoneal injection (3). The pharmacokinetic profile of (Ϫ)FTC given orally is favorable to antiviral therapy and is similar to, or in some aspects superior to, that observed for lamivudine [(Ϫ)3TC] both in vitro and in vivo (1,13,16). The pharmacokinetic profile of lamivudine delivered orally in woodchucks is similar to that observed in humans, and lamivudine is an effective antiviral agent against chronic WHV infection (9,12,15).…”

Simultaneous quantification of emtricitabine and tenofovir in human plasma using high-performance liquid chromatography after solid phase extraction

“…1). FTC is classified as a dideoxycytidine nucleoside analogue reverse transcriptase inhibitor, and is potent and selective against HIV types I and II and hepatitis B virus [1,2]. FTC is phosphorylated by cellular enzymes to form emtricitabine 5 -triphosphate, which competes with deoxycytidine 5 -triphosphate and terminates the amino acid chain of newly forming viral DNA.…”

Safety, Pharmacokinetics, and Efficacy of (+/−)-β-2′,3′-Dideoxy-5-Fluoro-3′-Thiacytidine with Efavirenz and Stavudine in Antiretroviral-Naïve Human Immunodeficiency Virus-Infected Patients

“…A major advantage of using RCV would be that the virus would be challenged with two different compounds, which should increase the difficulty of developing resistance to both enantiomers (10). Both enantiomers are well absorbed orally and have demonstrated low toxicity in preclinical safety studies (1,2,3,4,8).…”