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.
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
- HERO: Shore ND, Saad F, Cookson MS, George DJ, Saltzstein DR, Tutrone R, Akaza H, Bossi A, van Veenhuyzen DF, Selby B, Fan X, Kang V, Walling J, Tombal B; HERO Study Investigators. Oral Relugolix for Androgen-Deprivation Therapy in Advanced Prostate Cancer. N Engl J Med. 2020 Jun 4;382(23):2187-2196. link to original article contains verified protocol PubMed NCT03085095
- Dearnaley DP, Saltzstein DR, Sylvester JE, Karsh L, Mehlhaff BA, Pieczonka C, Bailen JL, Shi H, Ye Z, Faessel HM, Lin H, Zhu Y, Saad F, MacLean DB, Shore ND. The Oral Gonadotropin-releasing Hormone Receptor Antagonist Relugolix as Neoadjuvant/Adjuvant Androgen Deprivation Therapy to External Beam Radiotherapy in Patients with Localised Intermediate-risk Prostate Cancer: A Randomised, Open-label, Parallel-group Phase 2 Trial. Eur Urol. 2020 Apr 6:S0302-2838(20)30142-1. link to original article contains verified protocol PubMed
History of changes in FDA indication
- 12/18/2020: Approved for adult patients with advanced prostate cancer.
Also known as
- Code name: TAK-385
- Brand names: Orgovyx, Relumina