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gonadotropin releasing hormone analog + abiraterone + apalutamide + rezvilutamide

Development stage
Preclinical
Lead developer
- Gonadotropin releasing hormone analogs: AbbVie
Modality
Peptides, Small Molecules
Administration
Oral, Intramuscular, Subcutaneous
01

Overview

This is a combination therapy consisting of a gonadotropin releasing hormone (GnRH) analog, abiraterone, apalutamide, and rezvilutamide. GnRH analogs are synthetic peptides that act as agonists at the GnRH receptor, leading to downregulation of pituitary secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), resulting in suppression of sex steroid production (testosterone in men)[1][2][5]. Abiraterone is an androgen biosynthesis inhibitor that blocks CYP17A1 enzyme activity, reducing androgen production. Apalutamide is a nonsteroidal antiandrogen that inhibits the androgen receptor[6][8]. Rezvilutamide is also a nonsteroidal antiandrogen with similar action to apalutamide. This combination targets multiple points in the androgen axis and is primarily investigated or used for advanced prostate cancer.

02

Targets

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

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