Drug intelligence / Profile preview

CPI-1205 + abiraterone + prednisone

Development stage
Unknown
Lead developer
Constellation Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

CPI-1205 + abiraterone + prednisone is a **combination therapy** under clinical investigation for the treatment of metastatic castration-resistant prostate cancer (mCRPC). CPI-1205 is an oral, potent, selective, and cofactor-competitive small molecule inhibitor of EZH2 (Enhancer of Zeste Homolog 2), an epigenetic regulator frequently mutated or overexpressed in advanced prostate cancer. Abiraterone is a CYP17 inhibitor that suppresses androgen synthesis, and prednisone (a corticosteroid) is co-administered to counteract side effects and provide anti-inflammatory benefit. The combination is designed to leverage synergistic effects: EZH2 inhibition restores androgen receptor expression and sensitivity to antiandrogen therapy, potentially overcoming resistance to abiraterone and enhancing anti-tumor activity.

Other names
abirateroneprednisone
02

Targets

GR (Glucocorticoid receptor)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)EZH2 (Histone-lysine N-methyltransferase EZH2)

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