Chemistry:Gridegalutamide
Gridegalutamide is an investigational oral androgen receptor (AR) degrader being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It belongs to a class of drugs called proteolysis targeting chimeras (PROTACs), which are designed to selectively degrade specific proteins by hijacking the ubiquitin-proteasome system.[1][2] CC-94676 employs a unique dual mechanism of action, combining AR degradation with AR antagonism, potentially offering advantages over traditional AR inhibitors in overcoming resistance mechanisms.[3] Initially developed by Celgene and now under Bristol Myers Squibb, CC-94676 has demonstrated AR protein degradation and suppression of tumor growth in CRPC mouse models.[2] As of 2024, CC-94676 is being evaluated in phase I clinical trials for patients with mCRPC who have progressed on androgen deprivation therapy and at least one prior secondary hormonal therapy.[1][2]
References
- ↑ 1.0 1.1 "Targeted Protein Degradation: Clinical Advances in the Field of Oncology". International Journal of Molecular Sciences 23 (23). December 2022. doi:10.3390/ijms232315440. PMID 36499765.
- ↑ 2.0 2.1 2.2 "The clinical advances of proteolysis targeting chimeras in oncology". Exploration of Targeted Anti-Tumor Therapy 2 (6): 511–521. 2021. doi:10.37349/etat.2021.00061. PMID 36046114.
- ↑ "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". Annals of Oncology 36 (1): 76–88. September 2024. doi:10.1016/j.annonc.2024.09.005. PMID 39293515.
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