ABSTRACT

Amdoxovir (also known as DAPD, AMDX, or (–)-beta-d-2,6-diamino-purine dioxolane) was a nucleoside analog reverse transcriptase (NRTI) inhibitor that was developed to treat HIV-1 infections. Amdoxovir is a prodrug of the purine nucleoside analog (–)-beta-d-dioxolane guanosine (DXG). Amdoxovir is rapidly deaminated in vivo by adenosine deaminase to its active metabolite, DXG (Furman et al., 2001) and then phosphorylated to DXG triphosphate, the inhibitor of HIV reverse transcriptase. In vitro, DXG has potent antiviral activity against wild-type HIV-1, and, more significant, against clinical isolates of HIV-that are resistant to nucleoside and nucleotide analogs.