Description
AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1 -infected human PBM cells and HIV-1 -infected human macrophages, the EC 50 values of AzddMeC are 9 nM and 6 nM, respectivelyIn VitroAzddMeC (CS-92) is also effective against HIV-2 in lymphocytes. The replication of Friend murine virus is only weakly inhibited, and no effect is observed against HSV type 1 and type 2 and coxsackievirus B4. The interaction of the 5'-triphosphate of AzddMeC with HIV-1 reverse transcriptase indicated competitive inhibition (the inhibition constant, Kis, is 9.3 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoThe pharmacokinetics of AzddMeC are characterized following intravenous and oral administration of 60 mg/kg of the compound to male rhesus monkeys. 3'-azido-3'-deoxythymidine (AZT) is a major metabolite of AzddMeC in monkeys. AzddMeC concentrations in serum declined rapidly in a biexponential fashion with the terminal half-life ranging from 0.5 to 1.3 hr. Renal excretion of unchanged nucleoside and metabolic deamination yielding AZT are the primary routes of AzddMeC clearance. The oral bioavailability is 26%. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:HIV-1 9 nM (EC 50, Human PBM cells) HIV-1 6 nM (EC 50, Human macrophages)