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onalespib + abiraterone acetate
- Development stage
- Unknown
- Lead developer
- Astex Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Onalesip + abiraterone acetate is an investigational combination therapy studied in men with castration-resistant prostate cancer (CRPC) who had progressed on prior abiraterone acetate and prednisone or prednisolone therapy. Onalespib is a second-generation HSP90 inhibitor that impairs chaperoning of several oncogenic proteins, including androgen receptor (AR), while abiraterone acetate is a CYP17A1 inhibitor that blocks androgen biosynthesis, a key driver of prostate cancer. Both drugs were administered together to evaluate potential synergy in AR depletion and tumor control. Clinical trials showed the combination had limited biological activity (transient AR depletion, HSP72 upregulation) but no substantial clinical benefit, with diarrhea and fatigue as notable toxicities.
- Other names
- abiraterone acetate
02
Targets
AR (Adrenergic receptors)HSP90 (Heat shock protein 90 chaperone complex)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)
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