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Chemical Compound Review:

Amdoxovir [(2R,4R)-4-(2,6-diaminopurin- 9-yl)-1,3...

Synonyms: DAPD, CHEMBL458876, SureCN141228, DAPD cpd, AC1L3XUG, ...

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of Amdoxovir

BACKGROUND: Amdoxovir (2,6-diaminopurine dioxolane; DAPD) is a nucleoside reverse transcriptase inhibitor (NRTI) of human immunodeficiency virus-1 (HIV-1) with activity against wild-type and NRTI-resistant viruses [1].
DXG ([2R-cis]-2-amino-1,9-dihydro-9-[2-[hydroxymethyl]-1,3-dioxolan-4-yl]-6H-purin-6-one) and its prodrug DAPD ([2R-cis]-4-[2,6-diamino-9H-purin-9-yl]-1,3-dioxolane-2-methanol; amdoxovir) are novel 2',3'-dideoxynucleosides (ddNs) displaying activity against human immunodeficiency virus type 1 (HIV-1) [2].

High impact information on Amdoxovir

This mechanistic study provided detailed information on the amdoxovir-related drug resistance at a molecular level [3].
These studies suggest a potential role for the use of IMPDH inhibitors in combination therapy with amdoxovir in the treatment of HIV [4].
Anabolism of amdoxovir: phosphorylation of dioxolane guanosine and its 5'-phosphates by mammalian phosphotransferases [5].

Analytical, diagnostic and therapeutic context of Amdoxovir

Overall, the enzymatic data correlated well with the antiviral data obtained from cell culture experiments and further supported the use of amdoxovir for the treatment of nucleoside reverse transcriptase inhibitor-experienced patients [3].

References

Amdoxovir versus placebo with enfuvirtide plus optimized background therapy for HIV-1-infected subjects failing current therapy (AACTG A5118). Gripshover, B.M., Ribaudo, H., Santana, J., Gerber, J.G., Campbell, T.B., Hogg, E., Jarocki, B., Hammer, S.M., Kuritzkes, D.R. Antivir. Ther. (Lond.) (2006) [Pubmed]
Enzymatic assay for measurement of intracellular DXG triphosphate concentrations in peripheral blood mononuclear cells from human immunodeficiency virus type 1-infected patients. Kewn, S., Wang, L.H., Hoggard, P.G., Rousseau, F., Hart, R., MacNeela, J.P., Khoo, S.H., Back, D.J. Antimicrob. Agents Chemother. (2003) [Pubmed]
Dioxolane guanosine 5'-triphosphate, an alternative substrate inhibitor of wild-type and mutant HIV-1 reverse transcriptase. Steady state and pre-steady state kinetic analyses. Jeffrey, J.L., Feng, J.Y., Qi, C.C., Anderson, K.S., Furman, P.A. J. Biol. Chem. (2003) [Pubmed]
In vitro combination of amdoxovir and the inosine monophosphate dehydrogenase inhibitors mycophenolic acid and ribavirin demonstrates potent activity against wild-type and drug-resistant variants of human immunodeficiency virus type 1. Borroto-Esoda, K., Myrick, F., Feng, J., Jeffrey, J., Furman, P. Antimicrob. Agents Chemother. (2004) [Pubmed]
Anabolism of amdoxovir: phosphorylation of dioxolane guanosine and its 5'-phosphates by mammalian phosphotransferases. Feng, J.Y., Parker, W.B., Krajewski, M.L., Deville-Bonne, D., Veron, M., Krishnan, P., Cheng, Y.C., Borroto-Esoda, K. Biochem. Pharmacol. (2004) [Pubmed]

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