Drug intelligence / Profile preview

abiraterone

Development stage
Approved
Lead developer
Janssen Biotech
Modality
Small Molecules
Administration
Oral
01

Overview

Abiraterone is an orally administered small molecule antiandrogen used in combination with prednisone to treat metastatic castration-resistant prostate cancer (mCRPC) and metastatic high-risk castration-sensitive prostate cancer (CSPC). It acts as a potent, irreversible, and selective inhibitor of the enzyme 17α-hydroxylase/C17,20-lyase (CYP17), which is crucial for androgen biosynthesis in testicular, adrenal, and prostatic tumor tissues. By inhibiting CYP17, abiraterone reduces androgen production—male hormones that can promote tumor growth in the prostate gland. Abiraterone acetate is a prodrug developed to improve oral bioavailability and stability. The drug was first approved by regulatory agencies such as the FDA and EMA in 2011 for use in advanced prostate cancer settings. Developed and manufactured by Janssen.

Brand names
ZytigaYonsa
Other names
abiraterone acetate
02

Targets

CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)CYP2C8 (Cytochrome P450 2C8)

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