Relugolix: First Global Approval
The orally active nonpeptide gonadotropin-releasing hormone (GnRH)-receptor antagonist relugolix (Relumina) is being developed by Takeda and ASKA Pharmaceutical as a treatment for various sex hormone related disorders. Relugolix was recently approved for marketing in Japan as a treatment for symptoms associated with uterine fibroids, and studies evaluating the efficacy of the drug as treatment for endometriosis-associated pain and prostate cancer are currently underway. This article summarizes the milestones in the development of relugolix leading to this first approval for the treatment of symptoms associated with uterine fibroids.
Compliance with Ethical Standards
The preparation of this review was not supported by any external funding.
Conflict of interest
During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the author on the basis of scientific completeness and accuracy. A. Markham, a contracted employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.
- 2.Takeda. Uterine fibroids treatment agent (GnRH antagonists) “Rerumina for manufacturing and marketing approval in Japan of Tablets 40 mg” [media release]. 8 Jan 2019. https://www.takeda.com/jp/newsroom/newsreleases/2019/20190108-8038/.
- 3.Myovant Sciences. Relugolix Japanese prescribing information; 2019. http://www.pmda.go.jp/PmdaSearch/iyakuDetail/ResultDataSetPDF/400256_2499013F1027_1_02 Accessed 7 March 2019.
- 4.Takeda, Roivant Sciences. Roivant Sciences and Takeda launch Myovant Sciences to develop innovative therapeutics for women’s health and prostate cancer [media release]. 6 June 2016. http://www.takeda.com.
- 5.Takeda, Aska Pharmaceutical. ASKA and Takeda enter into licensing agreement for Relugolix in women’s health indications [media release]. 31 May 2018. http://www.takeda.com.
- 6.Nakata D, Masaki T, Tanaka A, et al. Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice. Eur J Pharmacol. 2014;723:167–74.CrossRefGoogle Scholar
- 7.Lukes A, Johnson B, Jones L, et al. Pharmacokinetics, pharmacodynamics, and safety of relugolix, a potent oral once-daily gonadotropin-releasing hormone (GnRH) receptor antagonist, as monotherapy and in combination with estradiol/norethindrone acetate add-back therapy [abstract no. P-287]. Hum Reprod. 2017;32(Suppl 1):i267–8.Google Scholar
- 10.Shore ND, Bailen JL, Pieczonka C, et al. Testosterone lowering, PSA response and quality of life in patients with advanced hormone sensitive prostate cancer receiving TAK-385, an oral GNRH antagonist: phase 2 interim analysis [abstract no. PD28-01]. J Urol. 2016;195(4 Suppl):e654.Google Scholar
- 11.Saad F, Bailen JL, Pieczonka CM, et al. Second interim analysis (IA2) results from a phase II trial of TAK-385, an oral GnRH antagonist, in prostate cancer patients (pts) [abstract no. 200]. J Clin Oncol. 2016;34(2 Suppl).Google Scholar
- 12.Dearnaley D, Saltzstein DR, Sylvester JE, et al. Neo/adjuvant ADT to EBRT: randomized phase 2 trial of the oral GnRH antagonist, TAK-385 (relugolix, RGX) and degarelix (DGX) in patients (pts) with prostate cancer (PC) [abstract no. 734P]. Ann Oncol. 2016;27(Suppl 6).Google Scholar