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.
Aaron Balog  1 ,  Richard Rampulla  1 ,  Gregory S Martin  2 ,  Stanley R Krystek  1 ,  Ricardo Attar  1 ,  Janet Dell-John  1 ,  John D DiMarco  1 ,  David Fairfax  2 ,  Jack Gougoutas  1 ,  Christian L Holst  2 ,  Andrew Nation  1 ,  Cheryl Rizzo  1 ,  Lana M Rossiter  2 ,  Liang Schweizer  1 ,  Weifang Shan  1 ,  Steven Spergel  1 ,  Thomas Spires  1 ,  Georgia Cornelius  1 ,  Marco Gottardis  1 ,  George Trainor  1 ,  Gregory D Vite  1 ,  Mark E Salvati  1
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.
PMID: 26288692 DOI: 10.1021/acsmedchemlett.5b00173
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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