Drug intelligence / Profile preview

abiraterone acetate + glucocorticoid

Development stage
Unknown
Lead developer
Janssen Biotech
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Abiraterone acetate + glucocorticoid is a **combination therapy** used primarily for metastatic castration-resistant prostate cancer. Abiraterone acetate is a prodrug of **abiraterone**, a selective and irreversible inhibitor of the enzyme CYP17A1 (cytochrome P450 17α-hydroxylase/17,20-lyase), which blocks **androgen biosynthesis** required for prostate cancer growth[2][3]. However, CYP17A1 inhibition also reduces cortisol synthesis, resulting in compensatory increase in adrenocorticotropic hormone (ACTH), and accumulation of mineralocorticoid precursors that can cause hypertension, hypokalemia, and fluid retention[2][3][1]. A **glucocorticoid** (commonly prednisone or dexamethasone) is co-administered as replacement therapy, suppressing ACTH and reducing these mineralocorticoid-related toxicities; it may also modestly improve symptoms/efficacy[1][2][3]. The FDA-approved regimen is abiraterone acetate 1000 mg daily plus prednisone 5 mg twice daily[5].

Other names
abiraterone acetate + prednisoneabiraterone acetate + dexamethasone
02

Targets

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

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