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Updated: Apr 5, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
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A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer

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

Aaron Balog1, Richard Rampulla1, Gregory S Martin2

  • 1Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States.

ACS Medicinal Chemistry Letters
|August 20, 2015
PubMed

Insights

BMS-641988 is a new nonsteroidal androgen receptor antagonist showing promise for prostate cancer treatment. It demonstrated superior efficacy in preclinical models compared to bicalutamide, leading to its clinical development.

Area of Science:

  • Oncology
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Prostate cancer treatment often involves targeting the androgen receptor (AR).
  • Novel antagonists are needed to overcome resistance and improve efficacy.

Purpose of the Study:

  • To evaluate the preclinical profile of BMS-641988, a novel nonsteroidal AR antagonist.
  • To assess its efficacy in prostate cancer models.

Main Methods:

  • In vitro binding affinity and functional antagonism assays for AR.
  • In vivo efficacy studies using human prostate cancer xenograft models (e.g., CWR22-BMSLD1).

Main Results:

  • BMS-641988 exhibits high binding affinity for the AR.
  • It functions as a potent in vitro antagonist.
  • Demonstrated superior efficacy compared to bicalutamide in the CWR22-BMSLD1 xenograft model.

Conclusions:

  • BMS-641988 possesses a promising preclinical profile for prostate cancer therapy.
  • Its demonstrated efficacy supports its advancement into clinical development.
Keywords:
BMS-641988CRPCProstate cancerandrogen receptor

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