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Takeda Announces Positive Results from its Phase 3 Confirmatory Clinical Trial in Japan Evaluating the Efficacy and Safety of GnRH Receptor Antagonist Relugolix in Uterine Fibroids

October 3, 2017

-82.2% of women treated with relugolix responded with a decrease in menstrual blood loss


Osaka, Japan, October 3, 2017 — Takeda Pharmaceutical Company Limited [TSE: 4502] (“Takeda”) today announced that a Phase 3 confirmatory clinical trial (“TAK-385/CCT-002 Study”) evaluating the efficacy and safety of relugolix (generic name, development code: TAK-385), a gonadotropin-releasing hormone (GnRH) receptor antagonist, met the primary endpoint of non-inferiority to the active control group in the treatment of uterine fibroids. This randomized, double-blind, parallel-group, multicenter study was designed to evaluate the efficacy and safety of treatment with oral relugolix versus leuprorelin acetate for 24 weeks in Japanese women with symptomatic uterine fibroids.

Relugolix inhibits the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) by blocking GnRH receptors in the pituitary gland, which in turn suppresses sex hormones such as estrogen and progesterone. Through this hormonal effect, relugolix has the potential to improve the symptoms of uterine fibroids or endometriosis.

Approximately 280 patients in the TAK-385/CCT-002 Study were randomized 1:1 to receive either 40 mg of relugolix, administered orally once daily, or leuprorelin acetate (1.88 or 3.75 mg based on body weight and symptoms), administered by injection once every four weeks. This study demonstrated that relugolix was statistically non-inferior to leuprorelin acetate based on the proportion of patients with a total Pictorial Blood-loss Assessment Chart (a patient-reported outcome measure to assess menstrual blood loss) score of < 10 from week 6 to week 12, which was the primary endpoint in the study (relugolix group: 82.2%, control group: 83.1%; p-value for non-inferiority test=
0.0013). All participants had a PBAC ≥ 120 upon entry into the study. The most commonly observed adverse events in patients treated with relugolix were metrorrhagia, hot flush, menorrhagia and headache, which are consistent with the mechanism of action and those observed 
in previous studies. The most commonly observed adverse events in patients treated with leuprorelin acetate were metrorrhagia, hot flush, menorrhagia and hyperhidrosis.

“Once-daily oral administration of relugolix has the potential to be a valuable treatment option for patients with uterine fibroids,” said Toshiro Heya, head of Takeda Development Center Japan. “We are very proud of these results which we plan to submit to regulatory authorities in Japan for marketing authorization of relugolix for the treatment of uterine fibroids.”  


Media Contacts:
Takeda Pharmaceutical Company Limited
Tatsuhiro Kanoo
Corporate Communications
Tel: +81-3-3278-3634
E-mail: [email protected]