Myfembree (Relugolix, Estradiol, and Norethindrone Acetate) for Endometriosis

Overview
Myfembree is approved by the U.S. Food and Drug Administration (FDA) for managing moderate to severe pain associated with endometriosis in premenopausal women, according to the drug’s prescribing information. Myfembree is also known by its drug name, relugolix, estradiol, and norethindrone acetate.

This combination treatment includes: 

• Relugolix, a gonadotropin-releasing hormone (GnRH) receptor antagonist that suppresses hormones involved in the menstrual cycle
• Estradiol, an estrogen that helps maintain bone health
• Norethindrone acetate, a progestin that reduces the risk of excessive estrogen exposure. 

These components work together to reduce symptoms associated with endometriosis, such as pain and abnormal bleeding.

How do I take it?
Prescribing information states that Myfembree is taken as one tablet orally, once daily. It should be taken at the same time each day. Before starting Myfembree, pregnancy should be ruled out, and any hormonal contraceptives should be discontinued. The medication should always be taken exactly as prescribed by a health care provider.

Side effects
Common side effects of Myfembree when treating endometriosis include headache, vasomotor symptoms (hot flashes and night sweats), mood changes (such as depression or anxiety), abnormal uterine bleeding, nausea, back pain, toothache, decreased sexual desire or arousal, arthralgia (joint pain), fatigue, and dizziness.

Rare but serious side effects may include thromboembolic events (blood clots), osteoporosis (bone loss), liver injury, uncontrolled high blood pressure, changes in menstrual bleeding patterns, risk of early pregnancy loss, hypersensitivity reactions (allergic reactions such as rash, itching, swelling, or difficulty breathing), uterine fibroid prolapse or expulsion (the partial or complete passage of fibroids through the vagina, potentially causing severe bleeding or pain), and suicidal thoughts or mood disorders. Myfembree should not be taken by individuals with a history of thrombotic disorders, hormone-sensitive cancers, known osteoporosis, severe liver impairment, or undiagnosed abnormal uterine bleeding.

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Label: Myfembree — Relugolix, Estradiol Hemihydrate, and Norethindrone Acetate Tablet, Film Coated — DailyMed