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.