Relugolix

Orgovyx · Relumina

GnRH Agonist Oral FDA/EMA Label

Half-life

2.6 days

Time to Peak

3 hr

Steady State

~13 days

Bioavailability

12%

Dose Range

120–360 mg

Frequency

Daily

Overview

First oral GnRH antagonist approved for advanced prostate cancer (Orgovyx). Also available in combination with estradiol and norethindrone for endometriosis (Myfembree). Oral dosing eliminates the need for injections. Loading dose of 360 mg on day 1, then 120 mg daily. Rapid onset of testosterone suppression without flare. Testosterone recovery is faster after discontinuation compared to depot GnRH agonists.

Mechanism of Action

Non-peptide oral GnRH receptor antagonist. Directly blocks pituitary GnRH receptors, suppressing LH, FSH, and gonadal sex hormones without flare effect.

Dosing Information

Route	Dose Range	Half-life	Tmax	Frequency
Oral	120–360 mg	2.6 days	3 hr	Daily

Used in Regimens

Relugolix is not currently part of any catalog regimen.

Data Sources

FDA Label Orgovyx (relugolix) FDA Prescribing Information

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