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Abacavir ADME
Stable Identifier
R-HSA-2161522
DOI
10.3180/REACT_121189.1
Type
Pathway
Species
Homo sapiens
Synonyms
Abacavir transport and metabolism
ReviewStatus
5/5
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Drug ADME (Homo sapiens)
Abacavir ADME (Homo sapiens)
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Abacavir is a nucleoside analogue reverse transcriptase inhibitor with antiretroviral activity, widely used in combination with other drugs to treat HIV-1 infection (Yuen et al. 2008). Its uptake across the plasma membrane is mediated by organic cation transporters SLC22A1, 2, and 3; the transport proteins ABCB1 and ABCG2 mediate its efflux. Abacavir itself is a prodrug. Activation requires phosphorylation by a cytosolic adenosine phosphotransferase and deamination by ADAL deaminase to yield carbovir monophosphate. Cytosolic nucleotide kinases convert carbovir monophosphate to carbovir triphosphate, the active HIV reverse transcriptase inhibitor. Abacavir can be glucuronidated or oxidized to a 5'-carboxylate; these are the major forms in which it is excreted from the body.
Literature References
PubMed ID
Title
Journal
Year
18479171
A review of the pharmacokinetics of abacavir
Pakes, GE
,
Weller, S
,
Yuen, GJ
Clin Pharmacokinet
2008
Participants
Events
Abacavir transmembrane transport
(Homo sapiens)
Abacavir metabolism
(Homo sapiens)
Participates
as an event of
Drug ADME (Homo sapiens)
Orthologous Events
Abacavir ADME (Bos taurus)
Abacavir ADME (Caenorhabditis elegans)
Abacavir ADME (Canis familiaris)
Abacavir ADME (Danio rerio)
Abacavir ADME (Dictyostelium discoideum)
Abacavir ADME (Drosophila melanogaster)
Abacavir ADME (Gallus gallus)
Abacavir ADME (Mus musculus)
Abacavir ADME (Rattus norvegicus)
Abacavir ADME (Saccharomyces cerevisiae)
Abacavir ADME (Schizosaccharomyces pombe)
Abacavir ADME (Sus scrofa)
Abacavir ADME (Xenopus tropicalis)
Authored
D'Eustachio, P (2012-03-14)
Reviewed
Jassal, B (2012-03-16)
Created
D'Eustachio, P (2012-03-14)
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