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BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader, capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. (Blue: HY-W247437; Black: linker (HY-W126831); Pink: HY-168697)[1][2][3][4][5]. | [References]
[1] Xu S, et al. Abstract ND02: Discovery of BMS-986365, a ligand-directed androgen receptor degrader (AR LDD) with a dual mechanism-of-action and best-in-class potential, for the treatment of advanced prostate cancer[J]. Cancer Research, 2024, 84(7_Supplement): ND02-ND02.
[2] Rathkopf DE, et al. Safety and clinical activity of BMS-986365 (CC-94676), a dual androgen receptor ligand-directed degrader and antagonist, in heavily pretreated patients with metastatic castration-resistant prostate cancer. Ann Oncol. 2024 Sep 16:S0923-7534(24)04001-8. DOI:10.1016/j.annonc.2024.09.005
[3] Poh A. A Dual AR Degrader–Inhibitor for Prostate Cancer[J]. 2024.
[4] Rathkopf D E, et al. First-in-human phase 1 study of CC-94676, a first-in-class androgen receptor (AR) ligand-directed degrader (LDD), in patients (pts) with metastatic castration-resistant prostate cancer (mCRPC)[J]. 2024.
[5] Scott JS, et al. Property-based optimisation of PROTACs. RSC Med Chem. 2024 Nov 7. DOI:10.1039/d4md00769g |
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