Drug intelligence / Profile preview

cabozantinib + abiraterone

Development stage
Unknown
Lead developer
Exelixis
Modality
Small Molecules
Administration
Oral
01

Overview

**Cabozantinib + abiraterone** is a combination of two oral small molecule drugs, evaluated mainly for the treatment of advanced prostate cancer (particularly castration-resistant and hormone-sensitive subtypes). Cabozantinib is a multi-kinase inhibitor targeting VEGFR, MET, AXL, RET, and other receptor tyrosine kinases, disrupting tumor angiogenesis, invasiveness, and metastatic potential. Abiraterone inhibits CYP17A1, a key enzyme in androgen biosynthesis, thereby reducing androgen production and signaling that drive prostate cancer growth. The combination shows preclinical and early clinical evidence of enhanced anti-prostate cancer activity: cabozantinib may counteract mechanisms of resistance to abiraterone by inhibiting compensatory pathways such as IGF-1 receptor (IGF1R) signaling. Clinical and preclinical studies suggest the combination may be superior to abiraterone alone in overcoming resistance and improving antitumor efficacy in metastatic prostate cancer[2][5]. The combination is still under clinical investigation and is not an approved fixed-dose product.

02

Targets

AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)AR (Adrenergic receptors)VEGFR2 (Vascular endothelial growth factor receptor 2)RET (Rearranged during transfection receptor tyrosine kinase)

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