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Cytochrome P450 (CYP) inhibition studies are routinely conducted in human liver microsomes (HLM). However, microsomal systems may overexpose CYP enzymes to test articles, especially high-molecular-weight drug candidates, due to limited membrane permeability, potentially increasing the risk of overestimating CYP inhibition. Therefore, an in vitro assay using human hepatocytes was established to provide more physiologically relevant conditions for CYP inhibition assessment.

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