What Is Estradiol/Norethindrone/Relugolix? Uses, Dosage, and What You Need to Know in 2026

What Is Estradiol/Norethindrone/Relugolix?

Estradiol/Norethindrone/Relugolix is a once-daily oral combination medication used to treat heavy menstrual bleeding from uterine fibroids and moderate to severe pain from endometriosis in premenopausal women.

Sold under the brand name Myfembree, this medication combines three active ingredients into a single tablet: Relugolix (a GnRH receptor antagonist that suppresses hormone production), Estradiol (a form of estrogen), and Norethindrone Acetate (a progestin). The Estradiol and Norethindrone components serve as "add-back therapy" — they replace just enough hormone to prevent the worst menopause-like side effects and protect your bones while the Relugolix does its job.

Myfembree is manufactured by Myovant Sciences, a Sumitovant Biopharma company (subsidiary of Sumitomo Pharma).

Brand Name, Generic Status, and FDA Approval

• Brand name: Myfembree
• Generic available: No. As of March 2026, no generic version of Myfembree has been approved. Patent exclusivities began expiring in late 2025/early 2026, and generic entry may be possible in 2026, but nothing is on the market yet.
• Drug class: GnRH receptor antagonist combination with estrogen/progestin add-back therapy
• Controlled substance: No — Myfembree is not a controlled substance and has no DEA schedule.
• FDA approval: May 2021 for uterine fibroids (heavy menstrual bleeding); August 2023 for endometriosis (moderate to severe pain)

What Is Estradiol/Norethindrone/Relugolix Used For?

Myfembree is FDA-approved for two conditions:

1. Heavy Menstrual Bleeding from Uterine Fibroids

Uterine fibroids are noncancerous growths in the uterus that affect up to 80% of women by age 50. When fibroids cause heavy periods — the kind that soak through a pad or tampon every hour, cause large clots, or last more than 7 days — Estradiol/Norethindrone/Relugolix can significantly reduce that bleeding. In clinical trials, the majority of women experienced a meaningful reduction in menstrual blood loss.

2. Moderate to Severe Endometriosis Pain

Endometriosis occurs when tissue similar to the uterine lining grows outside the uterus, causing chronic pain, painful periods, and pain during intercourse. Myfembree was approved in August 2023 for managing moderate to severe pain associated with endometriosis in premenopausal women.

Off-Label Uses

Some providers may prescribe Estradiol/Norethindrone/Relugolix off-label for adenomyosis symptom management or as a preoperative treatment to reduce fibroid size before surgery (myomectomy or hysterectomy).

How Is Estradiol/Norethindrone/Relugolix Taken?

Myfembree is taken as one tablet by mouth, once daily, at approximately the same time each day. Here are the details:

• Dose: Each tablet contains Relugolix 40 mg, Estradiol 1 mg, and Norethindrone Acetate 0.5 mg
• With or without food: Either is fine — take it however works best for your routine
• When to start: Treatment should begin within the first 5 days of your menstrual period
• Missed dose: If you miss a dose, take it as soon as possible on the same day, then go back to your regular schedule the next day
• Treatment duration: Up to 24 months for both fibroids and endometriosis
• Contraception: Use non-hormonal contraception (like condoms or a copper IUD) during treatment. Combined hormonal contraceptives (birth control pills, patches, rings) are contraindicated with Myfembree.

For information on how this medication works in your body, see our article on how Estradiol/Norethindrone/Relugolix works.

Who Should Not Take Estradiol/Norethindrone/Relugolix?

Myfembree is not appropriate for everyone. It is contraindicated (should not be used) in the following situations:

• Pregnancy — Known or suspected. A pregnancy test is required before starting treatment.
• History of blood clots — Including deep vein thrombosis (DVT), pulmonary embolism (PE), stroke, or heart attack.
• High risk for blood clots — Including women over 35 who smoke.
• Known osteoporosis — Because the medication can cause additional bone density loss.
• Hormone-sensitive cancers — Current or history of breast cancer or other hormone-sensitive malignancies.
• Liver disease — Any hepatic impairment or liver disease.
• Uncontrolled high blood pressure
• Allergy to any component — Hypersensitivity to Relugolix, Estradiol, Norethindrone Acetate, or any inactive ingredient.
• Use of combined hormonal contraceptives — Cannot be taken at the same time as birth control pills, patches, or rings that contain estrogen and progestin.

Myfembree also carries a boxed warning about thromboembolic disorders and vascular events. Learn more about what to watch for in our side effects guide.

How Much Does Estradiol/Norethindrone/Relugolix Cost?

Cost is a significant factor for this medication:

• Cash price (without insurance): $1,300 to $1,700 per month for a 28-tablet supply
• With commercial insurance: Most plans cover Myfembree but typically require prior authorization and may classify it as a specialty tier drug with higher copays
• Manufacturer copay assistance: The Myfembree Copay Assistance Program can reduce your cost to as little as $5 per fill (28-day supply) or $15 for a 90-day supply, with an annual maximum savings of $5,000. This is available to commercially insured patients only — not those on Medicare, Medicaid, or other government insurance.
• Patient assistance: Myovant Sciences offers a patient assistance program for eligible uninsured or underinsured patients. Additional resources are available through NeedyMeds and RxAssist.
• Generic: No generic is currently available.

For a complete breakdown of savings options, see our guide on how to save money on Estradiol/Norethindrone/Relugolix.

Final Thoughts

Estradiol/Norethindrone/Relugolix (Myfembree) represents a meaningful advance in treating uterine fibroids and endometriosis. It's the first once-daily oral combination that includes both a GnRH antagonist and hormonal add-back therapy in a single tablet, making it more convenient than older treatments that required multiple pills or injections.

If you think Myfembree might be right for you, talk to your OB/GYN or find a prescriber using our guide on how to find a doctor who prescribes Estradiol/Norethindrone/Relugolix. And when you're ready to fill your prescription, Medfinder can help you find a pharmacy with it in stock.

Find Estradiol/Norethindrone/Relugolix in stock near you with Medfinder →