Relugolix successfully
reduced heavy menstrual blood loss among Japanese women in a Multicenter,
Randomized, Double-Blind, Parallel-Group, Phase 3 Study to Evaluate the
Efficacy and Safety of Oral relugolix 40 mg as compared with injectable leuprolide in the
Treatment of Uterine Fibroids.
Relugolix is
an oral, once-daily, small molecule GnRH receptor antagonist that has been
evaluated in almost 1,600 study participants in Phase 1, Phase 2 and Phase 3
clinical trials. In these trials, it has shown to suppress estrogen and
progesterone levels in women and testosterone levels in men. (It is also being evaluated
in advanced prostate cancer via ongoing phase-3 HERO study).
The drug is
being developed by Switzerland’s Myovant
Sciences along with Japan’s Takeda.
They said that these results will support the other ongoing global trials evaluating
the drug in endometriosis and uterine fibroid patients.
"The
positive results of decreased menstrual bleeding from Takeda's Phase 3 study of
relugolix in Japanese women with uterine fibroids provides strong support for
Myovant's ongoing Phase 3 studies with relugolix in North America, Europeand
other regions," stated Lynn Seely, M.D., President and Chief
Executive Officer of Myovant Sciences in a press release.
"Uterine
fibroids result in debilitating heavy menstrual bleeding and anemia in millions
of women throughout the world, oftentimes requiring a hysterectomy to control
the bleeding. Myovant is working to develop relugolix, an oral,
once-daily medication that can potentially provide women with an alternative
option to major surgery for the treatment of uterine fibroids."
The study
recruited 288 women with heavy menstrual bleeding associated with uterine
fibroids. They were randomized to receive either relugolix 40 mg,
administered orally once daily, or leuprolide acetate, an injectable GnRH
agonist, administered by subcutaneous injection every four weeks, at a dose of
1.88 mg or 3.75 mg, for 24 weeks.
The amount
of blood loss was assessed by Pictorial Blood Loss Assessment Chart, or PBAC self-reported
by patient themselves. At entry into study all patient had PBAC ≥ 120.
In the study,
relugolix successfully demonstrated that it was as good as leuprolide acetate
with 82.2% of patients achieving a score of less than 10 on the PBAC, compared
with 83.1% of patients treated with leuprolide acetate (p = 0.0013).
The
incidence of adverse effects was nearly similar and varied according to the
drug. Another phase 3 trial with relugolix is currently ongoing in Japan with
70 patients who also complained of pain because of fibroids.
Two more
trials (LIBERTY 1 and LIBERTY 2) are ongoing and were initiated by Myovant in
January 2017. These trials are looking
at reducing heavy menstrual blood loss by relugolix alone followed by leuprolide as monotherapy, relugolix combined with low dose leuprolide or placebo
for 24 weeks.
Myovant is
solely responsible for obtaining Food and Drug Administration (FDA) approval
for relugolix in the United States and the results of Takeda study will
definitely reinforce its application.
