Discovery of BMS-986365, a First-in-Class Dual Androgen Receptor Ligand-Directed Degrader and Antagonist, for the Treatment of Advanced Prostate Cancer
The preclinical observations, coupled with clinical data, strongly support the potential for BMS-986365 to overcome ARPI-resistant disease regardless of AR mutational status. These findings establish BMS-986365 as a first-in-class dual AR degrader and competitive antagonist, likely to emerge as an important tool in the armamentarium to treat prostate cancer. See related commentary by Nyquist and Nelson, p. 13.
Authors
- Dana E. Rathkopf (ORCID: https://orcid.org/0000-0002-4503-7582)
- Marwa Khater (ORCID: https://orcid.org/0009-0002-5482-8711)
- Neil Bence (ORCID: https://orcid.org/0000-0002-6723-2880)
- John D. Norris (ORCID: https://orcid.org/0000-0001-6553-8053)
- Lawrence G. Hamann (ORCID: https://orcid.org/0000-0002-8997-7912)
- Raju Kandimalla (ORCID: https://orcid.org/0000-0002-0342-5229)
- Andy Christoforou (ORCID: https://orcid.org/0000-0002-3933-1793)
- Samantha Reiss (ORCID: https://orcid.org/0000-0001-5273-0898)
- Rama Krishna Narla (ORCID: https://orcid.org/0000-0001-5181-3376)
- Brandon H. Toyama (ORCID: https://orcid.org/0000-0002-8355-9138)
- Minerva Tran
- Suzanne E. Wardell (ORCID: https://orcid.org/0000-0002-5792-1447)
- Brian E. Cathers (ORCID: https://orcid.org/0000-0003-2793-7533)
- Veronique Plantevin-Krenitsky
- Joseph D. Meiring
- Mark Rolfe (ORCID: https://orcid.org/0009-0001-7585-2684)
- Donald P. McDonnell (ORCID: https://orcid.org/0000-0002-7331-4700)
- Joshua D. Hansen (ORCID: https://orcid.org/0000-0002-4881-5247)
- Celia Fontanillo (ORCID: https://orcid.org/0000-0002-3631-7881)
- Vivek Arora (ORCID: https://orcid.org/0000-0003-1694-9109)
- Joseph R. Piccotti (ORCID: https://orcid.org/0000-0003-4082-1850)
- Massimo Ammirante
- Emily Rychak (ORCID: https://orcid.org/0000-0002-6363-5922)
- Joshua M. Baughman (ORCID: https://orcid.org/0000-0002-3975-1528)
- Daniel W. Pierce (ORCID: https://orcid.org/0000-0002-4954-3781)
- Deborah S. Mortensen (ORCID: https://orcid.org/0000-0002-9144-0962)
- Ken Liu
- Shuichan Xu (ORCID: https://orcid.org/0009-0001-9105-4199)
- Toshiya Tsuji (ORCID: https://orcid.org/0009-0005-6948-671X)
- Debbie Liao
- Shankar K. Nayak (ORCID: https://orcid.org/0009-0005-7327-3944)
Institutions
- Memorial Sloan Kettering Cancer Center (US)
- Bristol-Myers Squibb (Germany) (DE)
- Duke University (US)
- Washington University in St. Louis (US)
- Piedmont International University (US)
- Kettering University (US)
- Bristol-Myers Squibb (United States) (US)
Publication Details
- Journal
- Clinical Cancer Research
- Published
- 2025-08-11
- DOI
- https://doi.org/10.1158/1078-0432.ccr-25-0471
- Citations
- 6
- Primary Topic
- Prostate Cancer Treatment and Research
- Type
- article
- Field-Weighted Citation Impact
- 9.11