relugolix + estradiol + norethindrone

Relugolix + estradiol + norethindrone is an oral fixed-dose combination tablet (40 mg relugolix, 1 mg estradiol, 0.5 mg norethindrone acetate) approved for managing heavy menstrual bleeding associated with uterine fibroids and moderate to severe pain associated with endometriosis in premenopausal women. Relugolix, a gonadotropin-releasing hormone (GnRH) receptor antagonist, rapidly suppresses pituitary LH and FSH release, reducing ovarian estradiol and progesterone production to induce a hypoestrogenic state that alleviates symptoms. Low-dose estradiol and norethindrone acetate provide hormonal add-back therapy to mitigate hypoestrogenic side effects such as bone mineral density loss, vasomotor symptoms, and endometrial hyperplasia, enabling sustained treatment up to 24 months with once-daily dosing.[1][2][3][6]

Brand names

MyfembreeRyeqo

Other names

relugolix/estradiol/norethisterone acetaterelugolix combination therapy