arrow

From NeuroLex

Jump to: navigation, search



Adefovir Dipivoxil

Name: Adefovir Dipivoxil
Description: Adefovir dipivoxil, previously called bis-POM PMEA, with trade names Preveon and Hepsera, is an orally-administered nucleotide analog reverse transcriptase inhibitor (ntRTI) used for treatment of hepatitis B. It is a failed treatment for HIV. (Wikipedia) Pharmacology: Adefovir dipivoxil a diester prodrug of adefovir. Adefovir is an acyclic nucleotide analog with activity against human hepatitis B virus (HBV). The concentration of adefovir that inhibited 50% of viral DNA synthesis (IC50) in vitro ranged from 0.2 to 2.5 M in HBV transfected human hepatoma cell lines. The combination of adefovir with lamivudine showed additive anti-HBV activity. Mechanism of action: 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 M. Adefovir diphosphate is a weak inhibitor of human DNA polymerases and with Ki values of 1.18 M and 0.97M, respectively. Drug type: Approved. Investigational. Small Molecule. Drug category: Antiviral Agents. Reverse Transcriptase Inhibitors
Synonym(s): ADV, Adefovir, Adefovir pivoxil, Adefovirdipivoxl, GS-840, PMEA, adefovir dipivoxil, bis-POM PMEA, Hepsera, Preveon
Related to: P protein (Includes: DNA-directed DNA polymerase
Has role: Drug
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB00718
Id: DB00718
Link to OWL / RDF: Download this content as OWL/RDF


Contributors

Ccdbuser, Nifbot2



bookmark
Facts about Adefovir DipivoxilRDF feed
Commenttaken from DrugBank
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB00718  +
DefinitionAdefovir dipivoxil, previously called bis- Adefovir dipivoxil, previously called bis-POM PMEA, with trade names Preveon and Hepsera, is an orally-administered nucleotide analog reverse transcriptase inhibitor (ntRTI) used for treatment of hepatitis B. It is a failed treatment for HIV. (Wikipedia) Pharmacology: Adefovir dipivoxil a diester prodrug of adefovir. Adefovir is an acyclic nucleotide analog with activity against human hepatitis B virus (HBV). The concentration of adefovir that inhibited 50% of viral DNA synthesis (IC50) in vitro ranged from 0.2 to 2.5 M in HBV transfected human hepatoma cell lines. The combination of adefovir with lamivudine showed additive anti-HBV activity. Mechanism of action: 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 M. Adefovir diphosphate is a weak inhibitor of human DNA polymerases and with Ki values of 1.18 M and 0.97M, respectively. Drug type: Approved. Investigational. Small Molecule. Drug category: Antiviral Agents. Reverse Transcriptase Inhibitors l Agents. Reverse Transcriptase Inhibitors
Has roleDrug  +
IdDB00718  +
LabelAdefovir Dipivoxil  +
ModifiedDate14 April 2014  +
RelatedToP protein (Includes: DNA-directed DNA polymerase  +
SuperCategoryMolecular entity  +
SynonymADV  +, Adefovir  +, Adefovir pivoxil  +, Adefovirdipivoxl  +, GS-840  +, PMEA  +, adefovir dipivoxil  +, bis-POM PMEA  +, Hepsera  +, and Preveon  +