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Functional characterization of 27 CYP3A4 variants on macitentan metabolism in vitro

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Macitentan is a new choice for pulmonary hypertension treatment which is converted to active metabolite ACT132577 by human cytochrome P450 3A4. Human cytochrome P450 3A4 often occurred gene mutations. Gene… Click to show full abstract

Macitentan is a new choice for pulmonary hypertension treatment which is converted to active metabolite ACT132577 by human cytochrome P450 3A4. Human cytochrome P450 3A4 often occurred gene mutations. Gene polymorphism might cause a variety of changes of protein expression and thus give rise to metabolic difference. The aim of this study was to investigate the catalytic characteristics of 27 CYP3A4 protein variants on the metabolism of macitentan in vitro.

Keywords: variants macitentan; metabolism; macitentan metabolism; functional characterization; characterization cyp3a4; cyp3a4 variants

Journal Title: Journal of Pharmacy and Pharmacology
Year Published: 2019

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