Current study on the prodrugs of tenofovir / 国际药学研究杂志

ABSTRACT

Tenofovir, the 9-[2-(R)-(phosphonomethoxy) propyl] adenine (PMPA), is an acyclic nucleoside phosphonate that has potent antiviral activity against both HIV and HBV. Despite its demonstrated antiviral potency, PMPA has limited oral bioavailability, poor cell penetration and moderate-to-severe renal toxicity, presumably resulting from the presence of two negative charges on the phosphonyl group. In order to improve the oral bioavailability and reduce the cytotoxicity, prodrug design is used to mask the high charge of the parent drug. In this paper, we review the advances on the prodrug of tenofovir from three aspects; esterification, ester amidation and dimerization. © 2006 Editorial office of Foreign Medical Sciences.