In vitro assessment of cytochrome P450 inhibition and induction potential of azacitidine

Authors :: Gondi Kumar
Eric Laille
Yong Chen
Sekhar Surapaneni
Lisa Liu
Source :: Cancer Chemotherapy and Pharmacology
Publication Year :: 2010
Publisher :: Springer Science and Business Media LLC, 2010.
Abstract: Purpose To assess the potential inhibitory and inductive effects of azacitidine on cytochrome P450 isozymes in vitro. Methods The inhibitory effects of azacitidine on various CYP isozymes were determined in human liver microsomes. In addition, the ability of azacitidine to induce CYP enzymes in cultured human hepatocytes was evaluated. Results Azacitidine did not inhibit CYP2B6-, CYP2C8-, CYP2C9-, CYP2C19-, CYP2D6-, and CYP3A4-mediated activities in human liver microsomes up to a concentration of 100 μM, while weak inhibition (

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