Takeda Announces Positive Results from its Phase 3 Clinical Trial in Japan Evaluating the Efficacy and Safety of Relugolix in the Treatment of Pain Symptoms Associated with Uterine Fibroids

-       57.6% of women treated once daily with relugolix had a reduction in their maximum pain score compared with 3.1% of women who received placebo

Osaka, Japan, November 9, 2017 — Takeda Pharmaceutical Company Limited [TSE: 4502] (“Takeda”) today announced that a Phase 3 clinical trial (“TAK-385-3008 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 statistical significance in improvement of pain symptoms associated with uterine fibroids compared to the control group. This randomized, double-blind, parallel-group, multicenter study was designed to evaluate the efficacy and safety of treatment with oral relugolix versus placebo for 12 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.

In the TAK-385-3008 study, sixty-five patients with pain due to uterine fibroids were randomized 1:1 to receive either 40 mg of relugolix or placebo administered orally once daily. The results demonstrated that relugolix was associated with a statistically significant and clinically meaningful improvement relative to placebo (relugolix group: 57.6%, placebo group: 3.1%; p < 0.0001) in pain symptoms associated with uterine fibroids as determined by the proportion of patients with a maximum Numerical Rating Scale (NRS) score of 1 or less during the 28 days before the final dose, which was the primary endpoint in the study. All participants had a maximum NRS ≥ 4 upon entry into the study. The adverse events such as hot flush, metrorrhagia, hyperhidrosis and menorrhagia were commonly observed in patients treated with relugolix, which are consistent with the mechanism of action of relugolix and those observed in previous studies.

In another Phase 3 study (TAK-385/CCT-002) evaluating the efficacy and safety of relugolix compared to leuprorelin acetate for the treatment of uterine fibroids which was announced in October 2017, relugolix successfully demonstrated non-inferiority to leuprorelin acetate with 82.2% of patients treated with relugolix meeting the study’s primary endpoint, the proportion of patients achieving a pre-defined reduction in menstrual bleeding, compared with 83.1% of patients treated with leuprorelin acetate (p = 0.0013). The incidence of adverse events in this study was generally similar between treatment groups and consistent with the mechanism of action of the study medications.

“Based on the results of two phase 3 studies, once-daily oral administration of relugolix may be a potential treatment option for patients suffering from symptoms associated with uterine fibroids such as pain or heavy menstrual bleeding,” 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.” 

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