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Evaluation of Icotinib as a Potent and Selective Inhibitor of Aldehyde Oxidase for Reaction Phenotyping in Human Hepatocytes.

Drug metabolism and disposition: the biological fate of chemicals - 16 May 2024

Tang Lloyd Wei Tat, DaSilva Ethan, Lapham Kimberly, Obach R Scott

Abstract excerpt

Aldehyde oxidase (AO) is a molybdenum cofactor-containing cytosolic enzyme that has gained prominence due to its involvement in the developmental failure of several drug candidates in first-in-human trials. Unlike cytochrome P450s (P450) and glucuronosyltransferase, AO substrates have been plagued by poor in vitro to in vivo extrapolation, leading to low systemic exposures and underprediction of human dose....

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Identifiers

PMID: 38565303
DOI: 10.1124/dmd.124.001693

Genes

UGT1A1

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