Dexelvucitabine (Reverset; d-d4FC), a Cytidine analog, is an orally active nucleoside reverse transcriptase inhibitor. Dexelvucitabine is a powerful drug against HIV-1-resistant viruses containing a thymidine analog and/or M184V mutation in the viral polymerase. Dexelvucitabine is a 2′-Deoxycytidine antiretroviral agent[1].
Dexelvucitabine (Reverset; d-d4FC; 33.3 mg/kg by i.v. or p.o.) has distribution and elimination half-lives (t1/2α and t1/2β, respectively) of 0.7 and 3.6 h in monkeys, respectively. The Cmax ranges from 21.1 to 47.5 μM[2]. Dexelvucitabine has a favorable pharmacokinetic profile with a long half-life (4.71 and 10.75 h after administration by the intravenous [i.v.] and oral [p.o.] routes, respectively) in woodchucks[2].
[1]. Brenda I Hernandez-Santiago, et al. Antiviral and cellular metabolism interactions between Dexelvucitabine and lamivudine. Antimicrob Agents Chemother. 2007 Jun;51(6):2130-5. [2]. L Ma, et al. Pharmacokinetics of the antiviral agent beta-D-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine in rhesus monkeys. Antimicrob Agents Chemother. 1999 Feb;43(2):381-4.