Drug intelligence / Profile preview

rezvilutamide + abiraterone

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Rezvilutamide + abiraterone is an investigational combination therapy for prostate cancer, specifically being studied in metastatic hormone-sensitive prostate cancer (mHSPC). Rezvilutamide is a novel, orally bioavailable androgen receptor antagonist developed by Jiangsu Hengrui Medicine. It inhibits androgen receptor signaling with lower blood–brain barrier penetration than other agents in its class, potentially reducing central nervous system side effects. Abiraterone is a CYP17 inhibitor that blocks androgen biosynthesis and is commonly used with prednisone to manage side effects. The combination aims to provide dual blockade of the androgen axis—by inhibiting both the production of androgens (abiraterone) and their action at the receptor level (rezvilutamide)—to improve disease control in advanced prostate cancer[1][2][4][5].

02

Targets

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

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