Drug intelligence / Profile preview

abiraterone + leuprolide + prednisone

Development stage
Unknown
Lead developer
Janssen Biotech
Modality
Small Molecules
Administration
Oral (abiraterone, Prednisone), Intramuscular (leuprolide), Subcutaneous (leuprolide; Less Commonly)
01

Overview

This is a **combination regimen** used primarily in the treatment of prostate cancer. **Abiraterone** (administered as abiraterone acetate) is a selective inhibitor of **CYP17A1**, a critical enzyme in androgen biosynthesis; by blocking this pathway, it reduces androgen (testosterone) production from adrenal glands, testes, and tumor tissue[2][4]. **Leuprolide** is a **luteinizing hormone-releasing hormone (LHRH) agonist** (also referred to as a gonadotropin-releasing hormone (GnRH) agonist) that suppresses testicular androgen production via downregulation of the pituitary-gonadal axis[1][4]. **Prednisone** serves as a glucocorticoid replacement, mitigating the mineralocorticoid excess and adverse effects induced by abiraterone's suppression of cortisol[2]. This combination intensifies androgen suppression, offering improved clinical outcomes—including prolonged progression-free survival and overall survival—in high-risk or metastatic castration-sensitive and castration-resistant prostate cancer patients[3][4]. The regimen may be administered with or without radiation therapy in localized cases[1].

Other names
abiraterone acetate + leuprolide acetate + prednisone
02

Targets

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

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