ArticleEuropean journal of drug metabolism and pharmacokinetics2026
Evaluation of the Effects of Nicardipine on Entrectinib Metabolism in vitro and in Rats.
Article in European journal of drug metabolism and pharmacokinetics, 2026. 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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Funding
Abstract
backgroundEntrectinib, a multi-target tyrosine kinase inhibitor (TKI) against TRK, ROS1, and ALK, is clinically approved for genetically-defined solid tumors. The prevalence of drug-drug interactions (DDIs) with increased use indicates the need for further research.
objectiveThis present study aimed to screen 32 cardiovascular drugs for inhibitory effects on entrectinib metabolism and to elucidate the pharmacokinetic interaction with nicardipine.
methodsWe utilized rat liver microsomes to screen cardiovascular drugs and identify potent inhibitors. The inhibition kinetics of nicardipine were determined in vitro, and molecular docking to the primary entrectinib-metabolizing cytochrome P450 isoform was performed to investigate a potential mechanism for the observed interaction. Furthermore, in vivo pharmacokinetic studies were conducted in rats to evaluate the impact of nicardipine on entrectinib exposure.
resultsIn rat liver microsomes, nicardipine was identified as a moderately potent inhibitor with a half-maximal inhibitory concentration (IC
conclusionsThese findings in rat models and in silico docking indicate that nicardipine increases entrectinib exposure. While these results underscore the risk of significant DDIs, further clinical studies in humans are required to confirm this interaction and determine if entrectinib dose adjustments are necessary to mitigate adverse events.
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