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CPI-1205 + cobicistat
- Development stage
- Discontinued
- Lead developer
- Constellation Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
CPI-1205 + cobicistat is an investigational combination therapy consisting of the EZH2 inhibitor CPI-1205 (lulonostat) and the pharmacokinetic enhancer cobicistat (Tybost). Developed by Constellation Pharmaceuticals (later acquired by MorphoSys), this combination was specifically evaluated for the treatment of metastatic castration-resistant prostate cancer (mCRPC). CPI-1205 is a potent and selective small-molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2), a histone methyltransferase that plays a critical role in epigenetic regulation and is frequently overexpressed in advanced prostate cancer. Cobicistat, a potent inhibitor of the cytochrome P450 3A (CYP3A) enzyme, is co-administered to increase the systemic exposure and half-life of CPI-1205. The combination was studied in the Phase 1b/2 ProSTAR clinical trial, where it was administered in conjunction with androgen receptor pathway inhibitors such as enzalutamide or abiraterone. Development of the CPI-1205 program was discontinued following MorphoSys's strategic decision to prioritize other pipeline assets.
- Brand names
- Tybost
- Other names
- lulonostat + cobicistat
02
Targets
EZH2 (Histone-lysine N-methyltransferase EZH2)CYP3A4 (Cytochrome P450 3A4)
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