Zalcitabine

A pyrimidine analog reverse transcriptase inhibitor (NRTI) for the treatment of HIV/AIDS; also incorporates into the viral DNA, hence terminating the chain elongation due to the missing hydroxyl group; highly oral activity.HIV Infection Approved (In Vitro) :Zalcitabine is a dideoxynucleoside antiretroviral agent that is phosphorylated to the active metabolite 2',3'-dideoxycytidine 5'-triphosphate (ddCTP) within both uninfected and HIV-infected cells. At therapeutic concentrations, ddCTP inhibits HIV replication by inhibiting the enzyme reverse transcriptase and terminating elongation of the proviral DNA chain. Zalcitabine exhibits the inhibition effect on the cellular uptake of [3H]-PAH in CHO/hOAT1 cells with an IC50 value of 1.23 mM. Furthermore, the cellular uptake of zalcitabine increased threefold with the enhancement of hOATI activity in CHO/hOAT1 cells.