Abiraterone acetate is a steroidal CYP17 inhibitor used as androgen-directed therapy in advanced prostate cancer. Its clinical development established androgen biosynthesis inhibition as an effective treatment strategy in metastatic prostate cancer.
Pharmacology
Abiraterone inhibits CYP17, reducing androgen synthesis from adrenal and other non-gonadal precursors. This contributes to suppression of androgen-receptor signaling.
Pharmacokinetics
Abiraterone exposure is affected by food, which explains the fasting requirement. Abiraterone is metabolized through several pathways, and CYP3A4 participates in its metabolism. Strong CYP3A4 inducers can substantially reduce exposure.
Protein binding and distribution
Abiraterone is highly protein bound in plasma. Its pharmacokinetic behavior supports once-daily administration in the approved treatment regimens.
Clinical development
The COU-AA-301 trial established a survival benefit in men with metastatic castration-resistant prostate cancer previously treated with docetaxel. Final analysis reported median overall survival of 15.8 months with abiraterone acetate plus prednisone versus 11.2 months with placebo plus prednisone.
The COU-AA-302 study evaluated abiraterone plus prednisone in chemotherapy-naive men with metastatic castration-resistant disease and demonstrated improvement in radiographic progression-free survival and other clinical outcomes.
The LATITUDE program evaluated abiraterone plus prednisone in newly diagnosed high-risk metastatic castration-sensitive prostate cancer.
Evidence limitations
Clinical-trial results describe populations studied under defined protocols. They do not predict the response or safety outcome of an individual patient.