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Relugolix, estradiol, and norethindrone: Drug information

Relugolix, estradiol, and norethindrone: Drug information
2025© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Relugolix, estradiol, and norethindrone: Patient drug information"

For abbreviations, symbols, and age group definitions show table
ALERT: US Boxed Warning
Thromboembolic disorders and vascular events

Estrogen and progestin combination products, including relugolix/estradiol/norethindrone, increase the risk of thrombotic or thromboembolic disorders including pulmonary embolism, deep vein thrombosis, stroke and myocardial infarction, especially in women at increased risk for these events. Relugolix/estradiol/norethindrone is contraindicated in women with current or a history of thrombotic or thromboembolic disorders and in women at increased risk for these events, including women >35 years of age who smoke or women with uncontrolled hypertension.

Brand Names: US
  • Myfembree
Brand Names: Canada
  • Myfembree
Pharmacologic Category
  • Estrogen Derivative;
  • Gonadotropin Releasing Hormone Antagonist;
  • Progestin
Dosing: Adult
Endometriosis, moderate to severe pain

Endometriosis, moderate to severe pain: Oral: One tablet once daily. Maximum duration of therapy: 24 months. Treatment should be started as soon as possible after the onset of menses, but no later than 7 days after menses has started.

Heavy menstrual bleeding

Heavy menstrual bleeding: Oral: One tablet once daily. Maximum duration of therapy: 24 months. Treatment should be started as soon as possible after the onset of menses, but no later than 7 days after menses has started.

Missed doses: If a dose is missed, the dose should be administered as soon as remembered the same day, then resume the regular dosing the next day.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling. Also refer to individual monographs.

Dosing: Liver Impairment: Adult

Use is contraindicated in patients with hepatic impairment. Also refer to individual monographs.

Dosing: Older Adult

Not approved for use in postmenopausal patients.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults. Also see individual agents.

>10%:

Cardiovascular: Vasomotor symptoms (11% to 13%; including flushing, hot flash, hyperhidrosis, night sweats)

Endocrine & metabolic: Hypercholesterolemia (200 to <240 mg/dL: 14%; ≥240 mg/dL: 2%)

Nervous system: Headache (33%)

1% to 10%:

Cardiovascular: Hypertension (≤7%; including exacerbation of hypertension), peripheral edema (2%)

Dermatologic: Alopecia (4%)

Endocrine & metabolic: Decreased libido (3% to 4%), increased LDL cholesterol (130 to <160 mg/dL: 9%; ≥160 mg/dL: ≤2%)

Gastrointestinal: Diarrhea (2%), dyspepsia (2% to 3%), nausea (6%), toothache (6%)

Genitourinary: Abnormal uterine bleeding (6% to 7%), breast cyst (2% to 3%), vaginal dryness (2%)

Nervous system: Dizziness (3%), fatigue (3%), mood disorder (≤9%; including anxiety, depressed mood, depression, emotional lability, irritability, suicidal ideation)

Neuromuscular & skeletal: Arthralgia (4%), back pain (5%)

<1%:

Cardiovascular: Deep vein thrombosis, pulmonary embolism

Gastrointestinal: Cholecystitis, cholelithiasis

Genitourinary: Pelvic pain, uterine fibroids (degeneration, expulsion, prolapse)

Hepatic: Increased serum alanine aminotransferase

Neuromuscular & skeletal: Bone fracture

Frequency not defined:

Cardiovascular: Acute myocardial infarction, thromboembolism

Nervous system: Cerebrovascular accident

Neuromuscular & skeletal: Decreased bone mineral density

Postmarketing:

Dermatologic: Fixed drug eruption, urticaria

Hypersensitivity: Angioedema, nonimmune anaphylaxis

Contraindications

Hypersensitivity (eg, anaphylactic reaction, angioedema) to relugolix, estradiol, norethindrone, or any component of the formulation; pregnancy; osteoporosis; current or history of breast cancer or other hormone-sensitive malignancies, and with increased risk for hormone-sensitive malignancies; known hepatic impairment or disease; with undiagnosed abnormal uterine bleeding.

Use is also contraindicated in patients at high risk of arterial, venous thrombotic, or thromboembolic disorders, including patients >35 years of age who smoke; patients known to have current or history of deep vein thrombosis or pulmonary embolism, vascular disease (eg, cerebrovascular disease, coronary artery disease, peripheral vascular disease); thrombogenic valvular or thrombogenic rhythm diseases of the heart (eg, subacute bacterial endocarditis with valvular disease, atrial fibrillation); inherited or acquired hypercoagulopathies; uncontrolled hypertension; headaches with focal neurological symptoms or migraine headaches with aura if >35 years of age.

Canadian labeling: Additional contraindications (not in US labeling): Current or history of liver tumors (benign or malignant); partial or complete loss of vision associated with ophthalmic vascular disease; endometrial hyperplasia; concomitant use of hormonal contraceptives; breastfeeding.

Warnings/Precautions

Concerns related to adverse effects:

• Alopecia: May cause alopecia. Reversibility is unknown. Consider discontinuation if alopecia becomes a concern.

• Bleeding irregularities: Menstrual bleeding patterns may change, causing a decrease in the amount, intensity, or duration of bleeding. Changes in bleeding patterns may alter the ability to detect pregnancy. Pregnancy testing should be conducted if pregnancy is suspected; discontinue use if pregnancy is confirmed.

• Bone mineral density loss: Associated with bone mineral density (BMD) loss; risk is increased with duration of use and may not be completely reversible following discontinuation. Consider supplementation with calcium and vitamin D. Limit duration of treatment to 24 months to reduce the extent of BMD loss. Use caution in patients with risk factors for osteoporosis, including medications that may decrease BMD.

• Breast cancer: May increase the risk for breast cancer and other hormone-sensitive malignancies. Hormone therapy may be associated with increased breast density and an increase in abnormal mammogram findings requiring further evaluation. Discontinue if a hormone-sensitive malignancy is diagnosed.

• Depression: May increase the risk of suicidal ideation and mood disorders (including depression). Evaluate new or worsening psychiatric symptoms and refer to a mental health care professional if appropriate. Patients should seek immediate medical attention for suicidal ideation and behavior. Consider risks and benefits of therapy if mood disturbances occur.

• Hepatic impairment: Discontinue if jaundice develops during therapy or if liver function becomes abnormal.

• Hypertension: Discontinue if BP rises significantly with use.

• Hypersensitivity: Hypersensitivity reactions (eg, anaphylactic reaction, angioedema, urticaria) have been reported with use; discontinue treatment if hypersensitivity occurs.

• Lipid effects: May adversely affect lipid levels, including serum triglycerides leading to pancreatitis, especially in patients with preexisting hypertriglyceridemia.

• Retinal thrombosis: Discontinue if unexplained loss of vision, proptosis, diplopia, papilledema, or retinal vascular lesions occur and immediately evaluate for retinal thrombosis.

• Thromboembolic disorders: The estradiol/norethindrone component increases the risk of thrombotic or thromboembolic disorders particularly in patients otherwise at high risk. Discontinue use if an arterial or venous thromboembolic event occurs. Age >35 years, hypertension, obesity, and tobacco use increase the risk of thromboembolic events.

Disease-related concerns:

• Diabetes: May impair glucose tolerance; closely monitor patients with diabetes or prediabetes.

• Gallbladder disease: May increase risk of gallbladder disease, especially in patients with a history of cholestatic jaundice associated with past estrogen use or with pregnancy. Discontinue if jaundice occurs.

• Uterine fibroids: Uterine fibroid prolapse or expulsion may occur in patients with submucosal uterine fibroids.

Special populations:

• Surgical patients: Whenever possible, should be discontinued at least 4 to 6 weeks prior to surgery associated with an increased risk of thromboembolism or during periods of prolonged immobilization.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Myfembree: Relugolix 40 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg

Generic Equivalent Available: US

No

Pricing: US

Tablets (Myfembree Oral)

40-1-0.5 mg (per each): $53.57

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Myfembree: Relugolix 40 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg

Administration: Adult

Oral: Administer by mouth at the same time each day, with or without food.

Hazardous Drugs Handling Considerations

Hazardous agent (NIOSH 2024 [table 1]).

Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2023; NIOSH 2024; USP-NF 2020).

Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.

Use: Labeled Indications

Endometriosis, moderate to severe pain: Management of moderate to severe pain associated with endometriosis in premenopausal patients.

Heavy menstrual bleeding: Management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal patients.

Limitations of use: Use should be limited to 24 months due to the risk of continued bone loss, which may not be reversible.

Medication Safety Issues
High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs (contraindicated in pregnancy) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Community/Ambulatory Care Settings).

Metabolism/Transport Effects

Substrate of CYP1A2 (Minor), CYP2C8 (Minor), CYP3A4 (Minor), P-glycoprotein (Major with inhibitors), P-glycoprotein (Minor with inducers); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP1A2 (Weak);

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Ajmaline: Estrogen Derivatives may increase adverse/toxic effects of Ajmaline. Specifically, the risk for cholestasis may be increased. Risk C: Monitor

Anastrozole: Estrogen Derivatives may decrease therapeutic effects of Anastrozole. Risk X: Avoid

Anthrax Immune Globulin (Human): Estrogen Derivatives may increase thrombogenic effects of Anthrax Immune Globulin (Human). Risk C: Monitor

Antidiabetic Agents: Hyperglycemia-Associated Agents may decrease therapeutic effects of Antidiabetic Agents. Risk C: Monitor

Asciminib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor

C1 Inhibitors: Estrogen Derivatives may increase thrombogenic effects of C1 Inhibitors. Risk C: Monitor

Chenodiol: Estrogen Derivatives may decrease therapeutic effects of Chenodiol. Risk C: Monitor

Chlorprothixene: Estrogen Derivatives may increase adverse/toxic effects of Chlorprothixene. Estrogen Derivatives may increase therapeutic effects of Chlorprothixene. Risk C: Monitor

Chlorprothixene: Progestins may increase therapeutic effects of Chlorprothixene. Progestins may increase adverse/toxic effects of Chlorprothixene. Risk C: Monitor

CloZAPine: CYP1A2 Inhibitors (Weak) may increase serum concentration of CloZAPine. Risk C: Monitor

Corticosteroids (Systemic): Estrogen Derivatives may increase serum concentration of Corticosteroids (Systemic). Risk C: Monitor

Cosyntropin: Coadministration of Estrogen Derivatives and Cosyntropin may alter diagnostic results. Management: Discontinue estrogen containing drugs 4 to 6 weeks prior to cosyntropin (ACTH) testing. Risk D: Consider Therapy Modification

Dantrolene: Estrogen Derivatives may increase hepatotoxic effects of Dantrolene. Risk C: Monitor

Elacestrant: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor

Erdafitinib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Management: If coadministration with these narrow therapeutic index/sensitive P-gp substrates is unavoidable, separate erdafitinib administration by at least 6 hours before or after administration of these P-gp substrates. Risk D: Consider Therapy Modification

Exemestane: Estrogen Derivatives may decrease therapeutic effects of Exemestane. Risk X: Avoid

Fezolinetant: CYP1A2 Inhibitors (Weak) may increase serum concentration of Fezolinetant. Risk X: Avoid

Futibatinib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor

Gilteritinib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor

Growth Hormone Analogs: Estrogen Derivatives may decrease therapeutic effects of Growth Hormone Analogs. Management: Initiate somapacitan at 2 mg once weekly in patients receiving oral estrogens. Monitor for reduced efficacy of growth hormone analogs; increased doses may be required. Risk D: Consider Therapy Modification

Hemin: Estrogen Derivatives may decrease therapeutic effects of Hemin. Risk X: Avoid

Hyaluronidase: Estrogen Derivatives may decrease therapeutic effects of Hyaluronidase. Risk C: Monitor

Hydrocortisone (Systemic): Estrogen Derivatives may increase serum concentration of Hydrocortisone (Systemic). Estrogen Derivatives may decrease serum concentration of Hydrocortisone (Systemic). Risk C: Monitor

Immune Globulin: Estrogen Derivatives may increase thrombogenic effects of Immune Globulin. Management: Use the lowest dose of immune globulin and minimum infusion rate practicable during coadministration with estrogen derivatives. Risk D: Consider Therapy Modification

Indium 111 Capromab Pendetide: Coadministration of Estrogen Derivatives and Indium 111 Capromab Pendetide may alter diagnostic results. Risk X: Avoid

Inducers of CYP3A4 (Moderate) and P-glycoprotein: May decrease serum concentration of Relugolix, Estradiol, and Norethindrone. Risk C: Monitor

Inducers of CYP3A4 (Strong) and P-glycoprotein: May decrease serum concentration of Relugolix, Estradiol, and Norethindrone. Risk X: Avoid

LamoTRIgine: Estrogen Derivatives may decrease serum concentration of LamoTRIgine. Risk C: Monitor

Lasmiditan: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid

Lenalidomide: Estrogen Derivatives may increase thrombogenic effects of Lenalidomide. Risk C: Monitor

Levacetylleucine: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor

Lonafarnib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors). Risk C: Monitor

Lumacaftor and Ivacaftor: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Lumacaftor and Ivacaftor may decrease serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Risk C: Monitor

Melatonin: Estrogen Derivatives may increase serum concentration of Melatonin. Risk C: Monitor

MetyraPONE: Coadministration of Estrogen Derivatives and MetyraPONE may alter diagnostic results. Management: Consider alternatives to the use of the metyrapone test in patients taking estrogen derivatives. Risk D: Consider Therapy Modification

MetyraPONE: Coadministration of Progestins and MetyraPONE may alter diagnostic results. Management: Consider alternatives to the use of the metyrapone test in patients taking progestins. Risk D: Consider Therapy Modification

Mitapivat: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor

Mivacurium: Estrogen Derivatives may increase serum concentration of Mivacurium. Risk C: Monitor

Nonsteroidal Anti-Inflammatory Agents (COX-2 Selective): May increase thrombogenic effects of Estrogen Derivatives. Nonsteroidal Anti-Inflammatory Agents (COX-2 Selective) may increase serum concentration of Estrogen Derivatives. Risk C: Monitor

Ospemifene: Estrogen Derivatives may increase adverse/toxic effects of Ospemifene. Risk X: Avoid

P-glycoprotein/ABCB1 Inhibitors: May increase serum concentration of Relugolix, Estradiol, and Norethindrone. Management: Avoid use of relugolix/estradiol/norethindrone with P-glycoprotein (P-gp) inhibitors. If concomitant use is unavoidable, relugolix/estradiol/norethindrone should be administered at least 6 hours before the P-gp inhibitor. Risk D: Consider Therapy Modification

Pacritinib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor

Pomalidomide: Estrogen Derivatives may increase thrombogenic effects of Pomalidomide. Risk C: Monitor

Pretomanid: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor

Primaquine: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor

Raloxifene: Estrogen Derivatives may increase adverse/toxic effects of Raloxifene. Risk X: Avoid

ROPINIRole: Estrogen Derivatives may increase serum concentration of ROPINIRole. Risk C: Monitor

Sotorasib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Management: Consider avoiding use of sotorasib and narrow therapeutic index/sensitive P-gp substrates. If combined use is unavoidable, monitor for increased toxicities of the substrate and consider a decrease in the substrate dosage. Risk D: Consider Therapy Modification

Sparsentan: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid

Succinylcholine: Estrogen Derivatives may increase serum concentration of Succinylcholine. Risk C: Monitor

Tacrolimus (Systemic): Estrogen Derivatives may increase serum concentration of Tacrolimus (Systemic). Risk C: Monitor

Taurursodiol: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid

Thalidomide: Estrogen Derivatives may increase thrombogenic effects of Thalidomide. Risk C: Monitor

Theophylline Derivatives: CYP1A2 Inhibitors (Weak) may increase serum concentration of Theophylline Derivatives. Risk C: Monitor

Thyroid Products: Estrogen Derivatives may decrease therapeutic effects of Thyroid Products. Risk C: Monitor

TiZANidine: CYP1A2 Inhibitors (Weak) may increase serum concentration of TiZANidine. Management: Avoid the use of tizanidine with weak CYP1A2 inhibitors when possible. If combined, monitor closely for increased tizanidine toxicities (eg, hypotension, bradycardia, drowsiness). Tizanidine dose reduction or discontinuation may be necessary. Risk D: Consider Therapy Modification

Tranexamic Acid: Estrogen Derivatives may increase thrombogenic effects of Tranexamic Acid. Risk X: Avoid

Ulipristal: May decrease therapeutic effects of Progestins. Progestins may decrease therapeutic effects of Ulipristal. Risk X: Avoid

Ursodiol: Estrogen Derivatives may decrease therapeutic effects of Ursodiol. Risk C: Monitor

Venetoclax: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Management: Avoid concomitant use of venetoclax and oral p-glycoprotein (P-gp) substrates if possible. If combined use is unavoidable, administer the P-gp substrate at least 6 hours before venetoclax to minimize the potential for an interaction. Risk D: Consider Therapy Modification

Vimseltinib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors). Management: Avoid concomitant use of vimseltinib and P-gp substrates when possible. If combined, administer vimseltinib at least 4 hours before the P-gp substrate. Risk D: Consider Therapy Modification

Xanomeline: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor

Reproductive Considerations

Discontinue hormonal contraceptives and exclude pregnancy prior to treatment with relugolix/estradiol/norethindrone.

Nonhormonal contraception is recommended during therapy and for 1 week after the last relugolix/estradiol/norethindrone dose.

Use may alter menstrual bleeding patterns, delaying the ability to detect a pregnancy; if pregnancy is suspected during treatment, pregnancy testing is recommended.

Pregnancy Considerations

Based on information from animal reproduction studies and the mechanism of action, exposure to relugolix/estradiol/norethindrone during pregnancy may cause early pregnancy loss.

Outcome data following inadvertent use of relugolix/estradiol/norethindrone during pregnancy is limited (Giudice 2022).

Use is contraindicated during pregnancy. Discontinue relugolix/estradiol/norethindrone if pregnancy occurs during treatment.

Data collection to monitor pregnancy and infant outcomes following inadvertent exposure to Myfembree is ongoing. Health care providers are encouraged to enroll patients exposed to Myfembree during pregnancy in the Pregnancy Registry (855-428-0707); patients may also enroll themselves.

Breastfeeding Considerations

It is not known if relugolix is present in breast milk. Estrogens and progestins are present in breast milk.

Milk production may be decreased; this risk is increased prior to the establishment of breastfeeding. According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.

Monitoring Parameters

Pregnancy status (prior to therapy); pregnancy status during therapy (if pregnancy is suspected); bone mineral density with dual-energy x-ray absorptiometry (prior to therapy and periodically during therapy in patients with heavy menstrual bleeding associated with uterine fibroids; prior to therapy and annually during therapy in patients with moderate to severe pain associated with endometriosis); age appropriate breast and pelvic exams; BP; glycemic control in patients with diabetes or prediabetes; hemoglobin; lipid profile (periodically during therapy); evaluate mental status prior to therapy in patients with a history of depression, suicidal ideation, and mood disorders; monitor for mood changes (including shortly after initiation of therapy); signs and symptoms of hepatic impairment; signs and symptoms of thromboembolic disorders.

Mechanism of Action

Relugolix is a nonpeptide, gonadotropin-releasing hormone antagonist that decreases luteinizing hormone, follicle-stimulating hormone, estradiol, and progesterone, reducing bleeding associated with uterine fibroids. Estradiol may reduce the bone loss associated with relugolix. Norethindrone may protect the uterus from adverse endometrial effects of unopposed estrogen.

In women treated for 24 weeks, a ≥50% decrease in menstrual blood loss from baseline, and a volume of menstrual blood loss <80 mL was observed over the last 35 days of treatment (Al-Hendy 2021).

Pharmacokinetics (Adult Data Unless Noted)

Also refer to individual Estradiol, Norethindrone, and Relugolix monographs for additional information.

Onset: Decreased menstrual bleeding occurs within 4 weeks of initiating treatment in patients with heavy menstrual bleeding associated with uterine fibroids (Al-Hendy 2021). A decrease in dysmenorrhea and nonmenstrual pelvic pain was observed ~4 weeks after treatment initiation with maximal effect at 8 to 12 weeks in patients with moderate to severe endometriosis (Giudice 2022).

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AT) Austria: Ryeqo;
  • (AU) Australia: Ryeqo;
  • (BE) Belgium: Ryeqo;
  • (BG) Bulgaria: Ryeqo;
  • (CH) Switzerland: Ryeqo;
  • (DE) Germany: Ryeqo;
  • (EE) Estonia: Ryeqo;
  • (ES) Spain: Ryeqo;
  • (FI) Finland: Ryeqo;
  • (GB) United Kingdom: Ryeqo;
  • (HU) Hungary: Ryeqo;
  • (IE) Ireland: Ryeqo;
  • (IT) Italy: Ryeqo;
  • (LT) Lithuania: Ryeqo;
  • (LU) Luxembourg: Ryeqo;
  • (LV) Latvia: Ryeqo;
  • (NL) Netherlands: Ryeqo;
  • (NO) Norway: Ryeqo;
  • (PL) Poland: Ryeqo;
  • (PT) Portugal: Ryeqo;
  • (RO) Romania: Ryeqo;
  • (SE) Sweden: Ryeqo;
  • (SI) Slovenia: Ryeqo;
  • (SK) Slovakia: Ryeqo
  1. Al-Hendy A, Lukes AS, Poindexter AN 3rd, et al. Treatment of uterine fibroid symptoms with relugolix combination therapy. N Engl J Med. 2021;384(7):630-642. doi:10.1056/NEJMoa2008283 [PubMed 33596357]
  2. Giudice LC, As-Sanie S, Arjona Ferreira JC, et al. Once daily oral relugolix combination therapy versus placebo in patients with endometriosis-associated pain: two replicate phase 3, randomised, double-blind, studies (SPIRIT 1 and 2). Lancet. 2022;399(10343):2267-2279. doi:10.1016/S0140-6736(22)00622-5 [PubMed 35717987]
  3. Hodson L, Ovesen J, Couch J, et al; US Centers for Disease Control and Prevention, National Institute for Occupational Safety and Health. Managing hazardous drug exposures: information for healthcare settings, 2023. https://doi.org/10.26616/NIOSHPUB2023130. Updated April 2023. Accessed December 27, 2024.
  4. Myfembree (relugolix, estradiol, and norethindrone) [prescribing information]. Marlborough, MA: Sumitomo Pharma America, Inc; July 2024.
  5. Myfembree (relugolix, estradiol, and norethindrone) [product monograph]. Kirkland, Quebec, Canada: Pfizer Canada ULC; October 2023.
  6. Ovesen JL, Sammons D, Connor TH, et al; US Centers for Disease Control and Prevention, National Institute for Occupational Safety and Health. NIOSH list of hazardous drugs in healthcare settings, 2024. https://doi.org/10.26616/NIOSHPUB2025103. Updated December 18, 2024. Accessed December 20, 2024.
  7. United States Pharmacopeia. <800> Hazardous Drugs—Handling in Healthcare Settings. In: USP-NF. United States Pharmacopeia; July 1, 2020. Accessed January 16, 2025. doi:10.31003/USPNF_M7808_07_01
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