Drug intelligence / Profile preview

darolutamide + relugolix

Development stage
Phase 2
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

Darolutamide + relugolix is an investigational oral combination therapy for prostate cancer, specifically hormone-sensitive and high-risk localized or locally advanced prostate cancer. Darolutamide is a nonsteroidal androgen receptor antagonist that blocks the action of androgens (male hormones) by binding to the androgen receptor, thereby inhibiting tumor growth driven by these hormones. Relugolix is an oral gonadotropin-releasing hormone (GnRH) receptor antagonist that rapidly suppresses testosterone production by blocking GnRH receptors in the pituitary gland, leading to medical castration without the initial testosterone surge seen with GnRH agonists. The combination aims to provide potent androgen deprivation therapy (ADT) with rapid onset and recovery of testosterone suppression, potentially improving outcomes while minimizing long-term side effects associated with traditional ADT regimens[1][2][3][4][5].

02

Targets

AR (Adrenergic receptors)GnRHR (Gonadotropin-releasing hormone receptor)

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