ArticleDrug metabolism and disposition: the biological fate of chemicals2025
Interindividual variability in imatinib metabolism in human liver microsomes and primary human hepatocytes: Impact of CYP2C8 and CYP3A phenotypes.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Imatinib is a kinase inhibitor used in the treatment of chronic myeloid leukemia and other cancers. Although its pharmacokinetics is generally predictable, substantial interindividual variability in clearance and exposure remains. In this study, we investigated the impact of cytochrome P450 (P450) enzymes CYP2C8, CYP3A4, and CYP3A5 phenotypes and genotypes on imatinib metabolism using both human liver microsomes (HLMs) and primary human hepatocytes (PHHs). Imatinib clearance and N-desmethyl imatinib formation were quantified by liquid chromatography-tandem mass spectrometry and correlated with enzyme activity, protein concentration, and compared by genotype groups. In single-donor HLMs (n = 21), imatinib clearance varied 45-fold between donors and was strongly associated with CYP2C8 (r = 0.91) and CYP3A (r = 0.90) protein concentrations and CYP2C8 (r = 0.66) and CYP3A (r = 0.86) enzyme activities. A multiple linear regression model identified CYP3A activity and biological sex as significant predictors of imatinib clearance (adjusted R
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