Relugolix (Orgovyx)

General information

Class/mechanism: Gonadotropin-releasing hormone (GnRH) receptor antagonist. Reversibly binds to pituitary GnRH receptors, reducing the release of luteinizing hormone (LH) and follicle stimulation hormone (FSH), resulting in rapid androgen deprivation/decreased testosterone levels. There is no initial testosterone surge/flare with relugolix, in contrast to GnRH agonists.
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is used

• Prostate cancer

Patient drug information

• Relugolix (Orgovyx) package insert
• Relugolix (Orgovyx) patient drug information (UpToDate)

History of changes in FDA indication

• 2020-12-18: Approved for adult patients with advanced prostate cancer. (Based on HERO)

History of changes in EMA indication

• 2022-04-29: Initial authorization as Orgovyx. Orgovyx is indicated for the treatment of adult patients with advanced hormone-sensitive prostate cancer. (Based on HERO)

History of changes in PMDA indication

• 2019-01-08: Initial approval for the alleviation of menorrhagia, lower abdominal pain, backache, and anemia that are associated with uterine fibroids.

Also known as

• Code name: TAK-385
• Brand names: Orgovyx, Relumina