Drug intelligence / Profile preview

abiraterone acetate + prednisone + bicalutamide

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

Overview

Abiraterone acetate + prednisone + bicalutamide is a multi-drug regimen used primarily in the treatment of metastatic prostate cancer. - **Abiraterone acetate** is a prodrug converted in vivo to abiraterone, a potent and selective inhibitor of the enzyme steroid 17α-hydroxylase/17,20-lyase (CYP17A1), which blocks androgen biosynthesis from both testicular, adrenal, and tumor sources. - **Prednisone** is a glucocorticoid administered at low doses in this combination to compensate for abiraterone-induced cortisol suppression, thereby preventing an increase in adrenocorticotropic hormone and managing mineralocorticoid excess-related adverse events such as hypertension, hypokalemia, and fluid retention[1]. - **Bicalutamide** is a non-steroidal antiandrogen that competes with androgens for binding to the androgen receptor, hindering androgen-stimulated growth of prostate cancer cells[2][3]. This combination targets androgen signaling via both androgen biosynthesis inhibition and receptor blockade, and glucocorticoid support. The regimen is used for patients with high-risk, hormone-sensitive or castration-resistant metastatic prostate cancer, aiming to improve progression-free and overall survival compared to androgen blockade therapies alone[2][3][4].

Brand names
Zytiga
Other names
abiraterone acetate + prednisone + bicalutamide
02

Targets

GR (Glucocorticoid receptor)AR (Adrenergic receptors)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)

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