Drug intelligence / Profile preview

apalutamide + relugolix

Development stage
Unknown
Lead developer
Myovant Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

Apalutamide + relugolix is a combination therapy of two oral small molecule agents, used primarily for the treatment of prostate cancer. Apalutamide is an androgen receptor inhibitor, while relugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist. When used together, apalutamide blocks androgen receptor signaling and relugolix suppresses testicular testosterone production, thereby achieving and maintaining castrate testosterone levels and inhibiting prostate cancer progression. The combination is primarily studied in settings such as high-risk localized or advanced prostate cancer post-radical prostatectomy, aiming to reduce the risk of biochemical recurrence and provide androgen deprivation therapy.

Other names
apalutamide + relugolix
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)AR (Adrenergic receptors)

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