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Detoxication versus Bioactivation Pathways of Lapatinib In Vitro: UGT1A1 Catalyzes the Hepatic Glucuronidation of Debenzylated Lapatinib

O-Dealkylation of the tyrosine kinase inhibitor lapatinib by cytochrome P450 3A enzymes is implicated in the development of lapatinib-induced hepatotoxicity. Conjugative metabolism of debenzylated lapatinib (M1) via glucuronidation and sulfation is thought to be a major detoxication pathway for lapa...

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Bibliografiske detaljer
Udgivet i:Drug Metab Dispos
Main Authors: Nardone-White, Dasean T., Bissada, Jennifer E., Abouda, Arsany A., Jackson, Klarissa D.
Format: Artigo
Sprog:Inglês
Udgivet: The American Society for Pharmacology and Experimental Therapeutics 2021
Fag:
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7883098/
https://ncbi.nlm.nih.gov/pubmed/33376146
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/dmd.120.000236
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