Relugolix, Estradiol, and Norethindrone
Relugolix, estradiol, and norethindrone is a three-ingredient combination used in premenopausal women to manage heavy menstrual bleeding from uterine fibroids and moderate to severe pain from endometriosis.
🧬 Where this information comes from Click to expand
The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 1 clinical label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →
⚠️ FDA Boxed Warning — the FDA’s strongest safety alert ▾
Myfembree carries a serious warning about blood clots and related vascular events. The estrogen and progestin in Myfembree increase the risk of dangerous blood clots, including deep vein thrombosis (clots in the legs), pulmonary embolism (clots in the lungs), stroke, and heart attack. This risk is highest in women who are over 35 and smoke, or who have uncontrolled high blood pressure. Myfembree must not be used by women who already have these conditions or who have had them in the past. Watch for warning signs such as chest pain, sudden shortness of breath, severe headache, leg swelling, or sudden vision changes, and seek emergency care immediately if any occur.
📖 Relugolix, Estradiol, and Norethindrone: Patient Information Guide
A plain-language walkthrough of Relugolix, Estradiol, and Norethindrone — what it treats, how it works, how it’s taken, side effects, warnings and interactions. Tap any section to expand it.
🎯What it's used for▾
Myfembree (relugolix, estradiol, and norethindrone) is approved for use in premenopausal women for two conditions:
- Myfembree is indicated for the management of heavy menstrual bleeding caused by uterine leiomyomas (fibroids)
- Myfembree is indicated for the management of moderate to severe pain associated with endometriosis
- Total treatment duration with Myfembree should not exceed 24 months, due to the risk of bone loss that may not be fully reversible
⚙️How it works▾
Myfembree works through three ingredients acting together. Relugolix is a GnRH receptor antagonist — it blocks signals in the pituitary gland that normally tell the ovaries to produce estrogen and progesterone. By lowering these hormones, relugolix reduces the bleeding caused by fibroids and the pain caused by endometriosis. Because low estrogen can lead to bone loss, a low dose of estradiol is added to help offset that effect. Norethindrone, a progestin, is included to protect the uterine lining from estrogen exposure without a progestin to balance it.
💊How it's taken▾
Myfembree is taken as one tablet by mouth once a day, at roughly the same time each day. It can be taken with or without food. Treatment should begin as early as possible after the start of your period, but no later than 7 days in. The total duration of use should not go beyond 24 months.
- If you miss a dose, take it as soon as you can on the same day, then continue your regular schedule the next day
- If you need to take an oral P-gp inhibitor drug at the same time, take Myfembree first and wait at least 6 hours before taking the other drug
- Stop hormonal contraceptives and confirm you are not pregnant before starting Myfembree
🤒Side effects — in detail▾
The most commonly reported side effects with Myfembree include:
- Vasomotor symptoms — hot flashes, sweating, and night sweats
- Abnormal uterine bleeding
- Hair loss or thinning (alopecia)
- Decreased sex drive or sexual desire
- Headache
- Nausea
- Mood changes, depression, anxiety, or irritability
- Fatigue, dizziness, and back pain (reported in endometriosis trials)
More serious reactions — including blood clots, liver problems, worsening depression or suicidal thoughts, and severe allergic reactions — require prompt medical attention. Do not ignore sudden chest pain, vision changes, severe mood shifts, or signs of a rash or swelling.
⚠️Warnings & precautions▾
- Blood clots and vascular events: Myfembree increases the risk of DVT, pulmonary embolism, stroke, and heart attack. Risk is highest in women over 35 who smoke or have uncontrolled high blood pressure. Stop the medication and get emergency help if you have chest pain, leg swelling, sudden shortness of breath, or vision changes.
- Bone loss: Myfembree can reduce bone mineral density, and that loss may not be fully reversible. A bone density scan is recommended before starting and periodically during treatment. Treatment must not exceed 24 months.
- Mood changes and suicidal ideation: Depression, anxiety, and — rarely — suicidal thoughts have been reported. Women with a history of mood disorders should be monitored closely. Seek immediate care for any suicidal thoughts.
- Liver injury: Myfembree is contraindicated in anyone with liver disease. Report yellowing of the skin or eyes, or upper right abdominal pain, right away.
- Elevated blood pressure: Myfembree can raise blood pressure. It must not be used in women with uncontrolled hypertension, and blood pressure should be monitored in women with well-controlled hypertension.
- Effects on pregnancy recognition: Myfembree can reduce menstrual bleeding, which makes it harder to notice if you become pregnant. Use non-hormonal contraception throughout treatment and for one week after stopping.
- Hair loss: Hair thinning or loss has been reported and may not resolve after stopping treatment.
- Cholesterol and blood sugar: Myfembree can raise total cholesterol, LDL cholesterol, and blood glucose levels. Monitoring may be needed, especially in women with diabetes or high triglycerides.
🔀What it interacts with▾
Myfembree can interact with certain medications in ways that make it less effective or more likely to cause side effects:
- Oral P-gp inhibitors (drugs that block the P-glycoprotein transporter) — raise relugolix levels in the blood, increasing side effect risk. Avoid using them together. If you must, take Myfembree first and wait at least 6 hours.
- Combined P-gp and strong CYP3A inducers (such as rifampin or certain anti-seizure medications) — lower the levels of all three Myfembree ingredients, reducing how well the medication works. Avoid this combination.
- Hormonal contraceptives — can raise estrogen to unsafe levels and reduce Myfembree's effectiveness. Use non-hormonal contraception instead while on Myfembree.
This is not a complete list of interactions. Always talk with your doctor or pharmacist before starting, stopping, or changing any medication.
📋Before taking it▾
- Do not take Myfembree if you have a current or past history of blood clots (DVT or PE), stroke, or heart attack
- Do not take Myfembree if you are over 35 and smoke, or have uncontrolled high blood pressure
- Myfembree is contraindicated in pregnancy — confirm you are not pregnant before starting, and use effective non-hormonal contraception throughout treatment and for at least 1 week after stopping
- Do not take Myfembree if you have known osteoporosis — it can cause further bone loss
- Do not take Myfembree if you have or have had breast cancer or another hormone-sensitive cancer
- Do not take Myfembree if you have liver disease or known liver impairment
- Do not take Myfembree for undiagnosed abnormal uterine bleeding
- Tell your doctor if you have a history of depression, anxiety, or suicidal thoughts before starting
- Tell your doctor if you take thyroid hormone or cortisol replacement therapy — Myfembree can affect the lab tests used to monitor those conditions
- Myfembree has been detected in breast milk; discuss the risks with your doctor if you are breastfeeding
- Safety and effectiveness have not been established in pediatric patients
🚑If you take too much▾
Taking too much of an estrogen-progestin combination (such as in Myfembree) may cause nausea, vomiting, breast tenderness, stomach pain, drowsiness, fatigue, and withdrawal bleeding. If an overdose occurs, supportive care is recommended. It is not known whether hemodialysis removes relugolix, estradiol, or norethindrone from the body.
📡Pharmacodynamics — effects in the body▾
By blocking pituitary GnRH receptors, relugolix reduces circulating estrogen and progesterone, which lessens fibroid-related bleeding and endometriosis pain. The estradiol and norethindrone components of Myfembree can also affect the body's protein levels — including proteins that bind thyroid hormones, cortisol, and sex hormones — which may alter lab test results without necessarily changing how those hormones actually function. Myfembree can also affect blood clotting factors, lipid levels (raising HDL and triglycerides while reducing LDL), and may reduce glucose tolerance.
🔬Pharmacokinetics — how your body processes it▾
After a single dose of Myfembree, relugolix reaches peak blood levels in about 2 hours, while estradiol peaks around 7 hours and norethindrone around 1 hour. Relugolix reaches steady-state levels in the blood within about 12 days of daily dosing; estradiol and norethindrone reach steady state within 2 weeks. Relugolix is broken down mainly by CYP3A liver enzymes and is excreted primarily in feces; estradiol is processed by the liver and excreted in urine; norethindrone is mainly excreted in urine as well. Eating a high-fat meal reduces relugolix absorption somewhat, but this is not considered clinically meaningful, and food has no significant effect on estradiol or norethindrone levels.
📦How to store it▾
Store at 15ºC to 30ºC (59ºF to 86ºF).
📄 Written from Relugolix, Estradiol, and Norethindrone’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Every point is grounded in that labeling — nothing is invented. How we use AI →
Supplements & herbs that interact with Relugolix, Estradiol, and Norethindrone
219 supplements and herbal products have documented interactions with Relugolix, Estradiol, and Norethindrone in the licensed clinical database we use. Most are manageable — but your pharmacist should know about everything you take, including vitamins and herbals.
- Major · 8
- Moderate · 174
- Minor · 37
Educational information from a licensed clinical database (Natural Medicines) — see our data sources & update cadence. Not medical advice: an interaction being documented does not mean it will happen to you; do not start or stop medications or supplements without professional guidance.
Nutrient depletion considerations
Relugolix, Estradiol, and Norethindrone has been associated with lower levels of 5 nutrients in the clinical literature. This does not mean a deficiency will occur — it means these may be worth discussing with your pharmacist or healthcare provider, especially with long-term use.
- Higher significance · 3
- Moderate · 2
Educational information from a licensed clinical database (Natural Medicines) — not medical advice. Do not start or stop medications or supplements without professional guidance.
🩺 Pharmacist Counseling Corner
Quick, plain-English answers to the questions patients ask most about Relugolix, Estradiol, and Norethindrone — the kind of thing our pharmacy team would talk through with you at the counter.
What is Myfembree actually doing in my body, and why does it have three ingredients? ▾
How do I take it, and does it matter if I take it with food? ▾
What side effects should I expect, and which ones mean I need to call my doctor? ▾
Can I use my hormonal birth control while I'm on Myfembree? ▾
Will Myfembree affect my bones, and is that permanent? ▾
What should I know about Myfembree if I'm planning to get pregnant or think I might be pregnant? ▾
Is Relugolix, Estradiol, and Norethindrone available over the counter? ▾
When was Relugolix, Estradiol, and Norethindrone first available? ▾
Who makes Relugolix, Estradiol, and Norethindrone? ▾
💬 Answers drafted from Relugolix, Estradiol, and Norethindrone’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Grounded in that labeling — nothing is made up. How we use AI →
🧰 Keep exploring
💊 How Relugolix, Estradiol, and Norethindrone comes
Relugolix, Estradiol, and Norethindrone is available in 1 form. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.
Tablet
How this form is used
- Myfembree is used to manage heavy menstrual bleeding associated with uterine fibroids in premenopausal women
- Myfembree is used to manage moderate to severe pain associated with endometriosis in premenopausal women
- Myfembree use is limited to a maximum of 24 months due to the risk of bone loss
- Myfembree: take one tablet by mouth once daily at approximately the same time each day, with or without food
- Myfembree: start as early as possible after your period begins, but no later than 7 days after it starts
- Myfembree: if you miss a dose, take it as soon as possible on the same day, then resume your normal schedule the next day — never double up
- Myfembree: if you must take an oral P-gp inhibitor drug, take Myfembree first and wait at least 6 hours before taking the other drug
📊 Relugolix, Estradiol, and Norethindrone across the U.S. market
How Relugolix, Estradiol, and Norethindrone appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.
Share of FDA-listed product records by manufacturer — FDA National Drug Code Directory. Record counts are not sales or prescription volume.
📈 How widely Relugolix, Estradiol, and Norethindrone is used
A general measure of how commonly Relugolix, Estradiol, and Norethindrone is prescribed, based on Medicaid — one of the largest public drug programs. The figure below is prescriptions filled in Q2 2025 – Q1 2026, summed across every form and brand of the drug.
Think of this as a proxy for how widely Relugolix, Estradiol, and Norethindrone is used, drawn from freely available public data. Medicaid is just one program — these numbers don’t include Medicare, other government coverage, or commercial and cash-pay prescriptions, so real-world use is higher than what’s shown here.
How commonly is Relugolix, Estradiol, and Norethindrone prescribed? Of the 1,597 medications we measure, Relugolix, Estradiol, and Norethindrone ranks #803 by Medicaid prescriptions — more than 50% of them.
Source: Medicaid State Drug Utilization Data (CMS), aggregated by generic ingredient — summed across every NDC (all brands, strengths, salt forms and dosage forms) of Relugolix, Estradiol, and Norethindrone, and across all states and both fee-for-service and managed-care claims. A general popularity signal; it excludes Medicare, commercial insurance and cash prescriptions, so it is not total U.S. use. Based on the 1 of 3 listed Relugolix, Estradiol, and Norethindrone NDCs with Medicaid activity.
🔍 Compare Relugolix, Estradiol, and Norethindrone products
A representative set of FDA-listed product records for Relugolix, Estradiol, and Norethindrone — across manufacturers, strengths, and dosage forms, grouped by form with each product’s manufacturer and how the FDA approved it. The same medicine may be made and packaged by different companies, so a single drug can have many directory entries. (It’s also why a refill can look different — a new shape, color, or box — even though it contains the same medication.)
| Strength | Route | Manufacturer / Labeler | Category ⓘ | Details |
|---|---|---|---|---|
| 💊Tablet | ||||
| 1; 0.5; 40 mg/1; mg/1; mg | Oral | Myovant Sciences, Inc. | NDA | View NDC → |
| RELUGOLIX 40 mg/1; ESTRADIOL HEMIHYDRATE 1 mg/1; NORETHINDRONE ACETATE 0.5 mg | — | Patheon, Inc. | DRUG FOR FURTHER PROCESSING | View NDC → |
| RELUGOLIX 40 mg/1; ESTRADIOL HEMIHYDRATE 1 mg/1; NORETHINDRONE ACETATE 0.5 mg | Oral | Sumitomo Pharma America, Inc | NDA | View NDC → |
| 1; 0.5; 40 mg/1; mg/1; mg | Oral | Sumitomo Pharma America, Inc | NDA | View NDC → |
Showing 4 of 4 products — FDA National Drug Code Directory. See every product, package size and price: browse all 4 Relugolix, Estradiol, and Norethindrone NDCs →
📈 What people report — real-world data (FDA FAERS)
After a medicine reaches the market, patients, doctors and drugmakers can send the FDA reports of problems they think may be linked to it. Here’s what’s been reported for Relugolix, Estradiol, and Norethindrone — a signal of what to watch for, not proof the drug caused it.
Source: openFDA, from the FDA Adverse Event Reporting System (FAERS). These are voluntary reports — they don’t prove the drug caused the effect, and counts reflect how often something was reported, not how often it actually happens. Reports also often name the very problem the medicine is taken for — a common reason to file one is that the drug didn’t help — so for a pain reliever you may see “pain” high on the list; that points to why the report was filed, not to the drug causing the symptom. This counts every report that lists Relugolix, Estradiol, and Norethindrone in any role, so the total runs higher than the FDA’s official dashboard, which counts only cases where the drug is the suspect. For the authoritative figures, see the FDA FAERS Public Dashboard. Always talk to your pharmacist or doctor.
🏛️ The road to your pharmacy
How Relugolix, Estradiol, and Norethindrone went from FDA review to the pharmacy shelf — the key milestones in its regulatory journey.
Source: Drugs@FDA.
🚨 Recall history
A recall is when a specific batch of a medicine is pulled from the market — usually a manufacturing issue, not a problem with the drug itself. Class I is most serious, Class III least.
Source: openFDA drug enforcement (recall) reports.
📦 Supply & shortage status
Whether Relugolix, Estradiol, and Norethindrone is in short supply in the U.S. right now, plus any shortage history the FDA has on record. A shortage usually reflects a manufacturing or demand issue — not a safety problem with the drug.
Source: openFDA, from the FDA Drug Shortages database.
🏷️ Sold under these brand names
🏭 Manufacturers & labelers
🔬 Where this comes from
Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.
How we combine label and product data
HelloPharmacist combines public FDA and NLM records; we don’t author the underlying clinical facts. We identified 1 FDA-filed SPL label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. The representative label is the starting point for the displayed reference monograph; the 12 largest stored in-scope SPL records, which may include that representative, are compared section by section, and the longest available version of each section is retained. Forms, routes, brands, labelers, product-listed strengths, and product-record counts are aggregated separately from ingredient-matched FDA NDC Directory records; package records listed above are associated with the linked SPL; and the normalized concept hierarchy comes from NLM RxNorm.
For canonical ingredient pages, bounded product-attributed indication and administration excerpts may be added to the AI evidence, and the generator is instructed to preserve available product, brand, route, and form qualifiers instead of treating one label as universal. Where a section is identified as AI-written, its plain-language text is generated from bounded label evidence. New draft drug pages remain in the admin review queue before first publication. Myovant Sciences, Inc. is the representative DailyMed label linked for verification and dates; it is not the sole source used for the page.
This is general education, not medical advice — always consult your doctor or pharmacist about your medications and any medical condition. For the exact wording of the linked representative label, view that label on DailyMed; some displayed composite sections may come from other in-scope SPL labels. Learn how we use AI and our data sources & update cadence.