Drug intelligence / Profile preview

relugolix + androgen receptor pathway inhibitor (Myovant Sciences)

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

Overview

Relugolix + androgen receptor pathway inhibitor (ARPI) is a combination therapeutic regimen being investigated for the treatment of metastatic hormone-sensitive prostate cancer (mHSPC). Relugolix (Orgovyx) is an oral, small-molecule gonadotropin-releasing hormone (GnRH) receptor antagonist that rapidly reduces serum testosterone levels by competitively blocking GnRH receptors in the pituitary gland. ARPIs, such as enzalutamide or apalutamide, are small molecules that further inhibit the androgen signaling axis by antagonizing the androgen receptor or inhibiting androgen synthesis. This combination is the focus of the Phase II OPTIMAS trial (NCT05467176), an investigator-initiated study at the University of Utah and Huntsman Cancer Institute. The trial evaluates whether an intermittent dosing strategy—where treatment is paused in patients achieving an optimal prostate-specific antigen (PSA) response—can maintain clinical efficacy while improving quality of life by allowing for rapid testosterone recovery during treatment breaks.

Brand names
Orgovyx
Other names
relugolix or androgen deprivation therapy + androgen receptor pathway inhibitor-University of Utah-metastatic hormone-sensitive prostate cancerrelugolix + ARPIOPTIMAS regimenintermittent relugolix + ARPI
02

Targets

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

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