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Effect of N-methyl deuteration on pharmacokinetics and pharmacodynamics of enzalutamide.

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机构： [1]Chengdu Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chengdu, China [2]University of Chinese Academy of Sciences, Beijing, China [3]Lab of YWChen, Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center, Chengdu, China [4]Hinova Pharmaceuticals Inc, Chengdu, China

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关键词： CRPC deuterated drug enzalutamide LNCaP/AR xenograft PK/PD

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Enzalutamide, a second-generation antiandrogen, has been developed for the treatment of castration-resistance prostate cancer. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger antitumor potency in preclinical settings. Compound 6 is being developed clinically for the potential to be differentiated from enzalutamide through reduced dosages and a higher safety margin. Copyright © 2017 John Wiley & Sons, Ltd.

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出版当年[2017]版：

大类 | 4 区医学

小类 | 4 区生化研究方法 4 区分析化学 4 区药物化学

最新[2023]版：

大类 | 4 区医学

小类 | 4 区生化研究方法 4 区分析化学 4 区药物化学

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第一作者机构： [1]Chengdu Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chengdu, China [2]University of Chinese Academy of Sciences, Beijing, China

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通讯机构： [1]Chengdu Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chengdu, China [2]University of Chinese Academy of Sciences, Beijing, China [3]Lab of YWChen, Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center, Chengdu, China [4]Hinova Pharmaceuticals Inc, Chengdu, China [*1]State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.

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