Relugolix
Combination
Therapy

Relugolix combination therapy consists of relugolix 40 mg in combination with estradiol (1.0 mg) and a progestin (0.5 mg norethindrone acetate). Relugolix combination therapy is an oral investigational drug candidate for the treatment of uterine fibroids and endometriosis.

Relugolix Combination Therapy
is not approved by the FDA.

How it works

As a GnRH receptor antagonist, relugolix binds to and blocks the GnRH receptor in the anterior pituitary gland.

Blocking GnRH receptors decreases the release of gonadotropins – luteinizing hormone (LH) and follicle-stimulating hormone (FSH) – thereby decreasing the downstream production of estrogen and progesterone by the ovaries in women.

We are investigating whether relugolix combination therapy can maintain estrogen in the low normal range to balance the potential benefits of relugolix, while also maintaining bone health and mitigating the side effects that can result from a low-estrogen state.

Clinical trial results

Relugolix combination therapy is not approved by the FDA.

Uterine fibroids

Our Phase 3 clinical program for uterine fibroids consisted of two multinational, replicate pivotal clinical studies (LIBERTY 1 and LIBERTY 2) of relugolix combination therapy (relugolix 40 mg plus estradiol 1.0 mg and norethindrone acetate 0.5 mg) in women with heavy menstrual bleeding associated with uterine fibroids for 24 weeks. Eligible women who completed the LIBERTY 1 or LIBERTY 2 studies were offered the opportunity to enroll in an active treatment extension study in which all women received relugolix combination therapy for an additional 28-week period for a total treatment period of 52 weeks, designed to evaluate the safety and sustained efficacy of longer-term treatment. Upon completion of this 52-week total treatment period, eligible women could elect to participate in a second 52-week randomized withdrawal study designed to provide two-year safety and efficacy data on relugolix combination therapy and to evaluate the need for maintenance therapy. Across studies, a response was defined as a menstrual blood loss volume of less than 80 mL and a 50% or greater reduction from baseline in menstrual blood loss volume during the last 35 days of treatment measured using the alkaline hematin method.

LIBERTY 1 and 2 met the primary endpoint (p < 0.0001) with 73.4% and 71.2% of women receiving relugolix combination therapy achieving the responder criteria compared with 18.9% and 14.7% of women receiving placebo at 24 weeks, respectively. On average, women receiving relugolix combination therapy in both studies experienced an 84.3% reduction in menstrual blood loss from baseline (p < 0.0001). Bone mineral density was comparable between the relugolix combination therapy and placebo groups in LIBERTY 1 and 2. The distribution of the change in bone mineral density, including outliers, was similar for the relugolix combination therapy and placebo groups at 24 weeks, as assessed by dual energy x-ray absorptiometry (DXA). The overall incidence of adverse events in the relugolix combination and placebo groups was comparable in both studies. The open-label extension study also met the primary endpoint with relugolix combination therapy demonstrating an 87.7% response rate at one year, showing the durability of the response observed in LIBERTY 1 and 2. In addition, women experienced, on average, an 89.9% reduction in menstrual blood loss from baseline. Changes in bone mineral density through one year, as assessed by DXA every three months, were consistent with LIBERTY 1 and 2. The overall incidence of adverse events in the relugolix combination and placebo groups was comparable in both studies.

Endometriosis

Our Phase 3 clinical program for endometriosis consisted of two multinational, replicate pivotal clinical studies (SPIRIT 1 and SPIRIT 2) of relugolix combination therapy (relugolix 40 mg plus estradiol 1.0 mg and norethindrone acetate 0.5 mg) in women with pain associated with endometriosis. Eligible women who completed the SPIRIT 1 or SPIRIT 2 studies were offered the opportunity to enroll in an active treatment extension study in which all women receive relugolix combination therapy for an additional 80-week period, resulting in a total treatment period of up to 104 weeks, designed to evaluate the safety and sustained efficacy of longer-term treatment.

SPIRIT 1 and 2 met their co-primary endpoints (p < 0.0001) with 74.5% and 75.2% of women receiving relugolix combination therapy achieving clinically-meaningful reductions in dysmenorrhea (menstrual pain) compared with 26.9% and 30.4% of women receiving placebo at 24 weeks, respectively. 58.5% and 66.0% of women receiving relugolix combination therapy also achieved clinically-meaningful reductions in non-menstrual pelvic pain compared to 39.6% and 42.6% of women receiving placebo at 24 weeks, respectively. On average, women receiving relugolix combination therapy in SPIRIT 1 and 2 experienced a 73.3% and 75.1% reduction, respectively, on the Numerical Rating Scale from severe to mild pain. Relugolix combination therapy was generally well-tolerated with minimal bone mineral density loss over 24 weeks in SPIRIT 1 and 2. The overall incidence of adverse events in the relugolix combination and placebo groups was comparable in both studies.

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