期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 5, 页码 2077-2087出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm501239f
关键词
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资金
- NIH [R01 CA 129379]
- NCI [R01 CA027440, R21 CA117991]
- Tokai Pharmaceuticals Inc.
In our effort to discover potent and specific inhibitors of 17a-hydroxylase/17,20-lyase (CYP17), the key enzyme which catalyzes the biosynthesis of androgens from progestins, 3 beta-(hydroxy)-17-(1H-benzimidazole-1-yl)androsta-5,16-diene (Galeterone or TOK-001, formerly called VN/124-1) was identified as a selective development candidate which modulates multiple targets in the androgen receptor (AR) signaling pathway. This drug annotation summarizes the mechanisms of action, scientific rationale, medicinal chemistry, pharmacokinetic properties, and human efficacy data for galeterone, which has successfully completed phase II clinical development in men with castration resistant (advanced) prostate cancer (CRPC). Phase III clinical studies in CRPC patients are scheduled to begin in early 2015.
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