CYP-Mediated Sulfoximine Deimination of AZD6738

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CYP-Mediated Sulfoximine Deimination of AZD6738.

In hepatic S9 and human liver microsomes (HLMs) the sulfoximine moiety of the ATR inhibitor AZD6738 is metabolized to its corresponding sulfoxide (AZ8982) and sulfone (AZ0002). The initial deimination to AZ8982 is nominally a reductive reaction, but in HLMs it required both NADPH and oxygen and also was inhibited by 1-aminobenzotriazole at a concentration of 1 mM. Studies conducted in a panel o...

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ژورنال

عنوان ژورنال: Drug Metabolism and Disposition

سال: 2017

ISSN: 0090-9556,1521-009X

DOI: 10.1124/dmd.117.077776