期刊
MOLECULES
卷 25, 期 10, 页码 -出版社
MDPI
DOI: 10.3390/molecules25102448
关键词
androgen receptor; prostate cancer; enzalutamide; apalutamide; darolutamide
资金
- National Institutes of Health (National Institute of General Medical Sciences) [SC2GM121185]
- Fresno State NIH Bridges to Doctorate Program
- National Institutes of Health [R25GM131956, R25GM115293]
- Fresno State NIH RISE Program
- Henry Madden Library at California State University Fresno
Enzalutamide is the first second-generation nonsteroidal androgen receptor (AR) antagonist with a strong binding affinity to AR. Most significantly, enzalutamide can prolong not only overall survival time and metastatic free survival time for patients with lethal castration-resistant prostate cancer (CRPC), but also castration-resistant free survival time for patients with castration-sensitive prostate cancer (CSPC). Enzalutamide has thus been approved by the US Food and Drug Administration (FDA) for the treatment of both metastatic (in 2012) and non-metastatic (in 2018) CRPC, as well as CSPC (2019). This is an inspiring drug discovery story created by an amazing interdisciplinary collaboration. Equally important, the successful clinical use of enzalutamide proves the notion that the second-generation AR antagonists can serve as hormonal therapeutics for three forms of advanced prostate cancer. This has been further verified by the recent FDA approval of the other two second-generation AR antagonists, apalutamide and darolutamide, for the treatment of prostate cancer. This review focuses on the rational design and discovery of these three second-generation AR antagonists, and then highlights their syntheses, clinical studies, and use. Strategies to overcome the resistance to the second-generation AR antagonists are also reviewed.
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