How effective is Ryeqo in treating uterine fibroids?

Ryeqo is a gonadotropin-releasing hormone (GnRH) receptor antagonist that reduces the levels of estrogen produced by the ovaries and relieves a range of symptoms of uterine fibroids.

In the LIBERTY 1 and LIBERTY 2 placebo-controlled trials, once-daily Ryeqo combination therapy reduced menstrual blood loss and pain, was well tolerated, and preserved bone mineral density (BMD) for 24 weeks in women with heavy menstrual bleeding associated with uterine leiomyomas.

Women with uterine leiomyoma-related heavy menstrual bleeding who completed any treatment arm in the LIBERTY 1 or LIBERTY 2 trials were eligible to participate in the 28-week long-term extension study. In the extension study, all participants received once-daily Ryeqo combination therapy (Ryeqo 40 mg, estradiol 1 mg, norethindrone acetate 0.5 mg).

Results: A total of 477 women were enrolled, 476 received treatment, and 363 (76.1%) completed 52 weeks of treatment. Among patients who received combination therapy for 52 weeks (n=163), 87.7% of patients (responders) experienced sustained improvement in heavy menstrual bleeding. The least squares mean menstrual blood loss was reduced by 89.9%, with 70.6% of patients experiencing amenorrhea.

At Week 52, 59.0% of anemic patients at baseline had an improvement in hemoglobin concentration of more than 2 g/dL. Distress from uterine leiomyoma-related symptoms, as measured by the BPD (Bleeding and Pelvic Discomfort) scale score, was reduced by 51.3 points. A sustained reduction in uterine and uterine leiomyoma volume was observed. Bone density was maintained until week 52.

Conclusions: Improvements in heavy menstrual bleeding and anemia and reductions in uterine leiomyoma-related symptom burden were sustained after 52 weeks in women with uterine leiomyoma treated with Ryeqo combination. No new safety issues were identified and BMD was maintained.

Ryeqo shows selective antagonism to human pituitary GnRH receptors and blocks the effects of GnRH. Ryeqo inhibits the secretion of gonadotropins (LH and FSH) in the pituitary gland, thereby inhibiting the secretion of sex hormones such as E2 (estradiol) and progesterone in the ovaries.

Ryeqo: Take one tablet orally once a day, before or after meals, at approximately the same time each day. Take the medication as soon as possible after the start of menstruation, but no later than 7 days after the start of menstruation. It is recommended that patients take medication under the guidance of a doctor and receive symptomatic treatment.

Recommended related articles:

References

Al-Hendy A, Lukes AS, Poindexter AN 3rd, Venturella R, Villarroel C, Critchley HOD, Li Y, McKain L, Arjona Ferreira JC, Langenberg AGM, Wagman RB, Stewart EA. Treatment of Uterine Fibroid Symptoms with Relugolix Combination Therapy. N Engl J Med. 2021 Feb 18;384(7):630-642. doi: 10.1056/NEJMoa2008283. PMID: 33596357; PMCID: PMC8262231.