Relugolix is an oral, once-daily, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist and has been evaluated in over 1,300 study participants in Phase 1 and multiple large controlled Phase 2 clinical trials. In these trials, relugolix was generally well tolerated and suppressed estrogen and progesterone levels in women and testosterone levels in men. Common side effects of relugolix are consistent with its mechanism of action in lowering these sex hormones.
Myovant Sciences has an exclusive, worldwide license (excluding Japan and certain other Asian countries) to develop and commercialize relugolix. Myovant is developing relugolix as an oral, once-daily, GnRH receptor antagonist for heavy menstrual bleeding associated with uterine fibroids, endometriosis-associated pain, and advanced prostate cancer.
About Endometriosis
Endometriosis is a disease in which tissue that normally lines the uterus is found outside the uterine cavity, commonly in...
Phase 2 Study Results
Relugolix demonstrated statistical significance over placebo in the primary endpoint of the proportion of subjects who had reduction in menstrual blood loss from a score of at least 120 required at study entry to less than 10 from Week 6 through Week 12 on the Pictorial Blood Loss Assessment Chart (PBAC). Relugolix decreased menstrual blood loss in a dose-dependent manner with the highest proportion of responses [84%, 95% confidence interval (74% to 93%) vs. placebo] in the relugolix 40-mg group.
In the relugolix 40-mg group, 73% of women achieved amenorrhea (i.e. a PBAC score of 0, representing no menstrual blood loss) from Week 6 through Week 12. No women in the placebo group achieved amenorrhea. At Week 12, the 40-mg group demonstrated an absolute reduction in myoma and uterine volumes of approximately 50% from baseline compared to placebo. By Week 12, there was an increase in hemoglobin levels in the relugolix 20- and 40-mg groups compared to...
