Chemical Property of AMDOXOVIR
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Chemical Property:
- Purity/Quality:
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95-99% *data from raw suppliers
Safty Information:
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Useful:
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Description
Amdoxovir (also known as DAPD, AMDX, or ()-b-D-2,6-diaminopurine dioxolane) is a new drug in the class of nucleoside analog reverse transcriptase (NRTI) inhibitors used for the treatment of human immunodeficiency virus (HIV) type 1 infections. Amdoxovir is a prodrug of the purine nucleoside analog ()-b-D-dioxolane guanosine (DXG). Amdoxovir is rapidly deaminated in vivo by adenosine deaminase to its active metabolite, DXG. DXG is phosphorylated to DXG triphosphate, which is the inhibitor of (HIV) reverse transcriptase (RT). Both amdoxovir and DXG are dioxolane derivatives of the nucleoside guanine, which contain an oxygen atom at the 3u position of the sugar moiety.
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Uses
Amdoxovir is used in the treatment of HIV-1 and hepatitis B infections (reverse transcriptase inhibitor).
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Clinical Use
In early studies, dioxolane nucleoside derivatives showed potent anti-HIV activity in vitro. DXG has poor solubility and low oral bioavailability; amdoxovir, a more bioavailable prodrug, was developed initially at Triangle Pharmaceuticals and development is now continuing at RFS Pharma LLC. In vitro, DXG has potent antiviral activity against wild-type HIV-1, and, more significantly, against clinical isolates of HIV-1 which are resistant to current NRTIs. DXG also has in vitro activity against HIV2 and hepatitis B viruses, but the drug is not being developed for these indications. Amdoxovir has undergone three phase I and four phase I/ II trials for treatment of HIV-1. Amdoxovir is formulated as 300- or 500-mg capsules for oral administration.
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Drug interactions
Amdoxovir has been administered to humans in combination with
mycophenolate mofetil, enfuvirtide (T-20, fusion inhibitor), and
zidovudine. Pharmacokinetic studies have been performed only with
zidovudine. No drug interactions were identified for either zidovudine
or amdoxovir in relationship to the plasma concentrations of ZDV or
DXG . This was not unexpected given the
different phosphorylating pathways of these two drugs. No drug
interaction studies were reported for the mycophenolate mofetil study.
No clinical data on the other guanosine analog, abacavir, are available. However, nucleotide
competition studies conducted in tissue-cultured cells indicate no
competitive inhibition of carbovir triphosphate, the active metabolite
of abacavir. Additionally, abacavir did not interfere with the
phosphorylation of DXG. Since abacavir uses a different phosphorylation pathway to produce carbovir triphosphate, amdoxovir and
abacavir could be administered together.
