A pyrimidine analog reverse transcriptase inhibitor (NRTI) for the treatment of HIV/AIDS.
Description :
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
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[1]. 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[2].