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ACS Med Chem Lett. 2015 Jun 19;6(8):908-12. doi: 10.1021/acsmedchemlett.5b00173. eCollection 2015 Aug 13.

Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.

Author information

1
Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States.
2
Albany Molecular Research Inc. , 21 Corporate Circle, Albany, New York 12203, United States.

Abstract

BMS-641988 (23) is a novel, nonsteroidal androgen receptor antagonist designed for the treatment of prostate cancer. The compound has high binding affinity for the AR and acts as a functional antagonist in vitro. BMS-641988 is efficacious in multiple human prostate cancer xenograft models, including CWR22-BMSLD1 where it displays superior efficacy relative to bicalutamide. Based on its promising preclinical profile, BMS-641988 was selected for clinical development.

KEYWORDS:

BMS-641988; CRPC; Prostate cancer; androgen receptor

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