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

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

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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