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Adefovir dipivoxil is a nucleotide analog used to treat chronic hepatitis B. It is ineffective against HIV-1.
- Mechanism
- Curator reviewed
Adefovir dipivoxil is a prodrug of adefovir. Adefovir is an acyclic nucleotide analog of adenosine monophosphate which is phosphorylated to the active metabolite adefovir diphosphate by cellular kinases. Adefovir diphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate deoxyadenosine triphosphate and by causing DNA chain termination after its incorporation into viral DNA. The inhibition constant (Ki) for adefovir diphosphate for HBV DNA polymerase was 0.1 μM. Adefovir diphosphate is a weak inhibitor of human DNA polymerases α and γ with Ki values of 1.18 μM and 0.97μM, respectively.
- Primary indication
- Indicated for the treatment of chronic hepatitis B in adult patients with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease; this is...Curator reviewed · 1 structured indication
- Formula / weight
- C20H32N5O8P · 501.4705 g/mol (avg)
- First approval
- Canada, 2009 · United States, 2002
- Also known as
- Adefovir pivoxil · bis-POM PMEA
- Code names
- GS-0840
- Brand names
- Hepsera
Resolves to
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Which drugs share a target with Adefovir dipivoxil, and which of those have an active Phase 3 trial?