Relugolix (Orgovyx) is a novel gonadotropin-releasing hormone (GnRH) receptor antagonist that was approved in the United States in 2020 for the treatment of prostate cancer.

What are the Indications of Relugolix (Orgovyx)?

Indications and Clinical Applications

Relugolix is specifically indicated for the treatment of adult patients with advanced prostate cancer.

Its mechanism of action involves competitive binding to pituitary GnRH receptors, inhibiting the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby rapidly reducing testosterone levels.

Clinical studies have shown that 56% of patients achieved castrate-level testosterone (<50 ng/dL) on Day 4 after the first dose, and this proportion increased to 99% by Day 15, with sustained efficacy for more than 48 weeks.

Notably, the drug typically requires continuous administration in both metastatic and non-metastatic castration-resistant prostate cancer settings.

Dosage Form, Specification, and Characteristics of Relugolix (Orgovyx)

Dosage Form and Specification

Relugolix is available as film-coated oral tablets, each containing 120 mg of relugolix.

The tablets are light red, almond-shaped, engraved with the letter "R" on one side and marked "120" on the other, facilitating identification and dosage management.

Composition

In addition to the active ingredient relugolix, excipients include mannitol, hydroxypropyl cellulose, sodium starch glycolate, etc., which ensure drug stability and bioavailability.

Relugolix itself is a white to pale yellow solid, with a molecular structure specifically designed to achieve high-efficiency receptor antagonism.

Administration Characteristics

Tablets must be swallowed whole; do not chew or crush.

Drug absorption is not affected by food, and it can be taken with or without meals.

Initial treatment requires a loading dose of 360 mg (i.e., 3 tablets) on the first day, followed by a daily oral dose of 120 mg (1 tablet) at a fixed time.

If a dose is missed by more than 12 hours, skip the missed dose and take the next scheduled dose directly.

If treatment is interrupted for more than 7 days, restart the course with a loading dose of 360 mg.

Storage Conditions for Relugolix (Orgovyx)

Temperature Control

The drug should be stored at room temperature, with a maximum storage temperature not exceeding 30℃ (86℉). Avoid freezing or exposure to high temperatures.

Packaging Management

Bottle packaging: Each bottle contains 30 tablets with a built-in desiccant. Tightly close the bottle cap after the first opening.

Blister packaging: Each blister pack contains 9 tablets, covered with moisture-proof aluminum foil.

The original packaging must be maintained; do not transfer the drug to other containers to ensure moisture-proof and airtight conditions.

Safety Precautions

Store the drug in an area inaccessible to children to avoid the risk of accidental ingestion.

Unused drugs should be disposed of through recycling channels. If no such channels are available, dispose of them as household waste in accordance with FDA guidelines. Do not flush directly down the toilet.