Xuyi Zhan, Shaoyin Bao, Xumei Li, Shaojun Zhou, Maha Raja Dahar, Nengming Lin, Xiugui Chen, Chengshan Niu, Kaige Ji, Yusheng Wu, Kui Zeng, Zhihua Tang, Lushan Yu
Osimertinib is a highly selective third-generation irreversible inhibitor of epidermal growth factor receptor mutant, which can be utilized to treat non-small cell lung cancer. As the substrate of cytochrome P450 enzyme, it is mainly metabolized by the CYP3A enzyme in humans. Among the metabolites produced by osimertinib, AZ5104, and AZ7550, which are demethylated that is most vital. Nowadays, deuteration is a new design approach for several drugs. This popular strategy is deemed to improve the pharmacokinetic characteristics of the original drugs...
January 17, 2023: Biopharmaceutics & Drug Disposition