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CPI-1205 + enzalutamide
- Development stage
- Unknown
- Lead developer
- Constellation Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**CPI-1205 + enzalutamide** is a combination therapy under clinical investigation for the treatment of metastatic castration-resistant prostate cancer (mCRPC). CPI-1205 is a potent, selective, cofactor-competitive small molecule inhibitor of the histone methyltransferase EZH2, targeting both wild-type and mutant forms, and is believed to exert anti-proliferative effects through epigenetic reprogramming. Enzalutamide is a second-generation androgen receptor inhibitor that blocks androgen receptor signaling, a key pathway in prostate cancer progression. The rationale for their combination stems from preclinical data indicating that inhibition of EZH2 may restore androgen receptor sensitivity and overcome resistance to antiandrogen therapy. The combined regimen is formulated as two orally administered drugs.[1][2][4][5][7][9]
- Other names
- CPI-1205 + enzalutamide
02
Targets
EZH1AR (Adrenergic receptors)EZH2 (Histone-lysine N-methyltransferase EZH2)
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