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

Aaron Balog; Richard Rampulla; Gregory S Martin; Stanley R Krystek; Ricardo Attar; Janet Dell-John; John D DiMarco; David Fairfax; Jack Gougoutas; Christian L Holst; Andrew Nation; Cheryl Rizzo; Lana M Rossiter; Liang Schweizer; Weifang Shan; Steven Spergel; Thomas Spires; Georgia Cornelius; Marco Gottardis; George Trainor; Gregory D Vite; Mark E Salvati

doi:10.1021/acsmedchemlett.5b00173

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

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

Authors

Aaron Balog¹, Richard Rampulla¹, Gregory S Martin², Stanley R Krystek¹, Ricardo Attar¹, Janet Dell-John¹, John D DiMarco¹, David Fairfax², Jack Gougoutas¹, Christian L Holst², Andrew Nation¹, Cheryl Rizzo¹, Lana M Rossiter², Liang Schweizer¹, Weifang Shan¹, Steven Spergel¹, Thomas Spires¹, Georgia Cornelius¹, Marco Gottardis¹, George Trainor¹, Gregory D Vite¹, Mark E Salvati¹

Affiliations

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.