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Open AccessReview

Second-Generation Androgen Receptor Antagonists as Hormonal Therapeutics for Three Forms of Prostate Cancer

Department of Chemistry, California State University, Fresno, CA 93740, USA
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Authors to whom correspondence should be addressed.
Academic Editor: Laura Cerchia
Molecules 2020, 25(10), 2448; https://doi.org/10.3390/molecules25102448
Received: 1 May 2020 / Revised: 20 May 2020 / Accepted: 21 May 2020 / Published: 24 May 2020
(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation)
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. View Full-Text
Keywords: androgen receptor; prostate cancer; enzalutamide; apalutamide; darolutamide androgen receptor; prostate cancer; enzalutamide; apalutamide; darolutamide
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MDPI and ACS Style

Rajaram, P.; Rivera, A.; Muthima, K.; Olveda, N.; Muchalski, H.; Chen, Q.-H. Second-Generation Androgen Receptor Antagonists as Hormonal Therapeutics for Three Forms of Prostate Cancer. Molecules 2020, 25, 2448. https://doi.org/10.3390/molecules25102448

AMA Style

Rajaram P, Rivera A, Muthima K, Olveda N, Muchalski H, Chen Q-H. Second-Generation Androgen Receptor Antagonists as Hormonal Therapeutics for Three Forms of Prostate Cancer. Molecules. 2020; 25(10):2448. https://doi.org/10.3390/molecules25102448

Chicago/Turabian Style

Rajaram, Pravien; Rivera, Alyssa; Muthima, Kevin; Olveda, Nicholas; Muchalski, Hubert; Chen, Qiao-Hong. 2020. "Second-Generation Androgen Receptor Antagonists as Hormonal Therapeutics for Three Forms of Prostate Cancer" Molecules 25, no. 10: 2448. https://doi.org/10.3390/molecules25102448

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