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Drug overview for MYFEMBREE (relugolix/estradiol/norethindrone acetate):
Generic name: relugolix/estradiol/norethindrone acetate (REL-ue-GOE-lix/ES-tra-DYE-ol/nor-ETH-in-drone)
Drug class: Estrogens
Therapeutic class: Endocrine
Relugolix, estradiol, and norethindrone acetate (relugolix/estradiol/norethindrone) is a fixed combination of relugolix (a gonadotropin-releasing hormone (GnRH) receptor antagonist), estradiol (an estrogen), and norethindrone acetate (a progestin).
No enhanced Uses information available for this drug.
Generic name: relugolix/estradiol/norethindrone acetate (REL-ue-GOE-lix/ES-tra-DYE-ol/nor-ETH-in-drone)
Drug class: Estrogens
Therapeutic class: Endocrine
Relugolix, estradiol, and norethindrone acetate (relugolix/estradiol/norethindrone) is a fixed combination of relugolix (a gonadotropin-releasing hormone (GnRH) receptor antagonist), estradiol (an estrogen), and norethindrone acetate (a progestin).
No enhanced Uses information available for this drug.
DRUG IMAGES
MYFEMBREE 40 MG-1 MG-0.5 MG TB
The following indications for MYFEMBREE (relugolix/estradiol/norethindrone acetate) have been approved by the FDA:
Indications:
Heavy menstrual bleeding associated with uterine leiomyoma
Pain associated with endometriosis
Professional Synonyms:
None.
Indications:
Heavy menstrual bleeding associated with uterine leiomyoma
Pain associated with endometriosis
Professional Synonyms:
None.
The following dosing information is available for MYFEMBREE (relugolix/estradiol/norethindrone acetate):
Relugolix/estradiol/norethindrone is available as fixed combination tablets containing relugolix 40 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg.
Dosage of norethindrone is expressed in terms of norethindrone acetate.
Dosage of norethindrone is expressed in terms of norethindrone acetate.
Administer relugolix/estradiol/norethindrone orally once daily with or without food at approximately the same time each day. The first dose should be given as soon as possible after the onset of menses within 7 days of the start of menses. The recommended total duration of treatment is 24 months.
If a dose of relugolix/estradiol/norethindrone is missed, take the dose as soon as possible within the same day, and then resume the regular dosing schedule on the following day. Avoid concomitant use of P-glycoprotein (P-gp) inhibitors. If concomitant use cannot be avoided, relugolix/estradiol/norethindrone should be administered at least 6 hours before the P-gp inhibitor. Store relugolix/estradiol/norethindrone tablets at 15-30degreesC.
If a dose of relugolix/estradiol/norethindrone is missed, take the dose as soon as possible within the same day, and then resume the regular dosing schedule on the following day. Avoid concomitant use of P-glycoprotein (P-gp) inhibitors. If concomitant use cannot be avoided, relugolix/estradiol/norethindrone should be administered at least 6 hours before the P-gp inhibitor. Store relugolix/estradiol/norethindrone tablets at 15-30degreesC.
No dosing information available.
No generic dosing information available.
The following drug interaction information is available for MYFEMBREE (relugolix/estradiol/norethindrone acetate):
There are 0 contraindications.
There are 0 severe interactions.
There are 0 moderate interactions.
The following contraindication information is available for MYFEMBREE (relugolix/estradiol/norethindrone acetate):
Drug contraindication overview.
*High risk of arterial, venous thrombotic, or thromboembolic disorders. *Pregnancy. *Known osteoporosis.
*Current or history of breast cancer or other hormone-sensitive malignancies. *Known hepatic impairment or disease. *Undiagnosed abnormal uterine bleeding. *Known hypersensitivity to relugolix, estradiol, norethindrone acetate, or any components in the formulation.
*High risk of arterial, venous thrombotic, or thromboembolic disorders. *Pregnancy. *Known osteoporosis.
*Current or history of breast cancer or other hormone-sensitive malignancies. *Known hepatic impairment or disease. *Undiagnosed abnormal uterine bleeding. *Known hypersensitivity to relugolix, estradiol, norethindrone acetate, or any components in the formulation.
There are 15 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Acute myocardial infarction |
| Antithrombin III deficiency |
| Carcinoma of breast |
| Cerebrovascular accident |
| Deep venous thrombosis |
| Disease of liver |
| Endometrial carcinoma |
| Estrogen-dependent neoplasm |
| Osteoporosis |
| Predisposition to thrombosis |
| Pregnancy |
| Protein C deficiency disease |
| Pulmonary thromboembolism |
| Thromboembolic disorder |
| Thrombophilia |
There are 14 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Bed-ridden |
| Coronary artery disease |
| Depression |
| Family history of malignant tumor of breast |
| Hereditary angioedema |
| Hypertension |
| Hypothyroidism |
| Invasive surgical procedure |
| Malignant neoplasm of the ovary |
| Osteopenia |
| Papilledema |
| Retinal thrombosis |
| Suicidal ideation |
| Tobacco smoker |
There are 6 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Diabetes mellitus |
| Gallbladder disease |
| Hyperglycemia |
| Hyperlipidemia |
| Hypertriglyceridemia |
| Unspecified lump in breast |
The following adverse reaction information is available for MYFEMBREE (relugolix/estradiol/norethindrone acetate):
Adverse reaction overview.
The most common adverse reactions (incidence >=3%) reported with relugolix/estradiol/norethindrone in women with heavy menstrual bleeding associated with uterine fibroids are vasomotor symptoms, uterine bleeding, alopecia, and decreased libido. The most common adverse reactions (incidence >=3%) reported with relugolix/estradiol/norethindrone in women with moderate to severe pain associated with endometriosis are headache, vasomotor symptoms, mood disorders, abnormal uterine bleeding, nausea, toothache, back pain, decreased sexual desire and arousal, arthralgia, fatigue, and dizziness.
The most common adverse reactions (incidence >=3%) reported with relugolix/estradiol/norethindrone in women with heavy menstrual bleeding associated with uterine fibroids are vasomotor symptoms, uterine bleeding, alopecia, and decreased libido. The most common adverse reactions (incidence >=3%) reported with relugolix/estradiol/norethindrone in women with moderate to severe pain associated with endometriosis are headache, vasomotor symptoms, mood disorders, abnormal uterine bleeding, nausea, toothache, back pain, decreased sexual desire and arousal, arthralgia, fatigue, and dizziness.
There are 12 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Osteopenia |
Hypertension |
| Rare/Very Rare |
|---|
|
Anaphylaxis Angioedema Cholecystitis Hypersensitivity drug reaction Increased alanine transaminase Increased aspartate transaminase Suicidal ideation Thromboembolic disorder Thrombotic disorder Uterine leiomyoma degeneration |
There are 14 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Abnormal vaginal bleeding Alopecia Drug-induced hot flash Hyperhidrosis Libido changes Night sweats |
Depression Hypercholesterolemia Hypertriglyceridemia Irritability Symptoms of anxiety |
| Rare/Very Rare |
|---|
|
Hyperglycemia Pelvic pain Urticaria |
The following precautions are available for MYFEMBREE (relugolix/estradiol/norethindrone acetate):
Safety and efficacy of relugolix/estradiol/norethindrone combination therapy have not been established in pediatric patients.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
Relugolix/estradiol/norethindrone is contraindicated during pregnancy. Relugolix/estradiol/norethindrone can cause early pregnancy loss in humans based on its mechanism of action and animal findings. If pregnancy occurs during treatment, the fixed-combination drug should be discontinued.
Human data are insufficient to determine the risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes associated with relugolix/estradiol/norethindrone. In pregnant rabbits, oral exposure to relugolix at exposures equivalent to approximately half of the maximum recommended human dose (40 mg) during organogenesis resulted in spontaneous abortion and total litter loss. However, in rabbits and rats, relugolix exposures ranging from approximately 0.5
to 300 times the human exposure at recommended dosages did not result in fetal malformations. No increase in genital or non-genital birth defects has been identified with exposure to estrogens (e.g., estradiol) and progestins (e.g., norethindrone) before conception or during early pregnancy based on data from epidemiologic studies and meta-analyses. MYFEMBREE Pregnancy Exposure Registry tracks pregnancy outcomes in women exposed to relugolix/estradiol/norethindrone during pregnancy. Patients and providers are encouraged to report exposures during pregnancy by calling 1-855-428-0707.
Human data are insufficient to determine the risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes associated with relugolix/estradiol/norethindrone. In pregnant rabbits, oral exposure to relugolix at exposures equivalent to approximately half of the maximum recommended human dose (40 mg) during organogenesis resulted in spontaneous abortion and total litter loss. However, in rabbits and rats, relugolix exposures ranging from approximately 0.5
to 300 times the human exposure at recommended dosages did not result in fetal malformations. No increase in genital or non-genital birth defects has been identified with exposure to estrogens (e.g., estradiol) and progestins (e.g., norethindrone) before conception or during early pregnancy based on data from epidemiologic studies and meta-analyses. MYFEMBREE Pregnancy Exposure Registry tracks pregnancy outcomes in women exposed to relugolix/estradiol/norethindrone during pregnancy. Patients and providers are encouraged to report exposures during pregnancy by calling 1-855-428-0707.
Relugolix is distributed into milk in rats. It is not known whether relugolix or its metabolites are distributed into human milk, but drugs present in the milk of animals are likely to be present in human milk also. Estrogen and progestin have been detected in the breast milk of women treated with these drugs.
Estrogen plus progestin therapy can reduce milk production; reduction in milk production can occur at any time, but is less likely after breastfeeding is well established. The developmental and health benefits of breastfeeding, the clinical importance of the therapy to the woman, and any potential adverse effects to the nursing infants should be considered when making treatment decisions.
Precaution Exists
Precaution exists. (No data or inconclusive human data.) Use of this drug by breast feeding mothers should be evaluated carefully.
Estrogen plus progestin therapy can reduce milk production; reduction in milk production can occur at any time, but is less likely after breastfeeding is well established. The developmental and health benefits of breastfeeding, the clinical importance of the therapy to the woman, and any potential adverse effects to the nursing infants should be considered when making treatment decisions.
Precaution Exists
Precaution exists. (No data or inconclusive human data.) Use of this drug by breast feeding mothers should be evaluated carefully.
| Drug Name | Excretion Potential | Effect on Infant | Notes |
|---|---|---|---|
| Relugolix-estradiol-norethindrone | Excreted.This drug is known to be excreted in human breast milk. | It is not known whether this drug has an adverse effect on the nursing infant. (No data or inconclusive human data) | Insuff human data avail; all three active components secreted into breastmilk |
The manufacturer makes no specific dosage recommendations for geriatric patients. Clinical trials evaluating relugolix/estradiol/norethindrone combination therapy did not include any patients 65 years of age or older.
Precaution Exists
Geriatric management or monitoring precaution exists.
Precaution Exists
Geriatric management or monitoring precaution exists.
| Drug Name | Narrative | REN | HEP | CARDIO | NEURO | PULM | ENDO |
|---|---|---|---|---|---|---|---|
| Estrogenic Agents (systemic) | General-Use lowest possible dose for shortest duration and in combination with a progestin as indicated to reduce the risk of endometrial hyperplasia and breast cancer. Cardiovascular-May increase risk for thromboembolic events. Avoid use in patients with known, suspected, or history of arterial or venous thromboembolic disease. Neuro/Psych-May increase the risk for dementia. Genitourinary-May aggravate urinary incontinence. | N | N | Y | Y | N | N |
The following prioritized warning is available for MYFEMBREE (relugolix/estradiol/norethindrone acetate):
WARNING: Combination hormone treatment increases the risk of blood clot problems, including clots in the legs, lungs, and heart. Do not use this medication if you smoke cigarettes/use tobacco and are over 35 years old. Smoking raises your risk of stroke, heart attack, blood clots, and high blood pressure from this product.
The risk of these serious problems increases with age and with the number of cigarettes you smoke. Do not smoke or use tobacco.
WARNING: Combination hormone treatment increases the risk of blood clot problems, including clots in the legs, lungs, and heart. Do not use this medication if you smoke cigarettes/use tobacco and are over 35 years old. Smoking raises your risk of stroke, heart attack, blood clots, and high blood pressure from this product.
The risk of these serious problems increases with age and with the number of cigarettes you smoke. Do not smoke or use tobacco.
The following icd codes are available for MYFEMBREE (relugolix/estradiol/norethindrone acetate)'s list of indications:
| Heavy menstrual bleeding assoc. with uterine leiomyoma | |
| D25 | Leiomyoma of uterus |
| D25.0 | Submucous leiomyoma of uterus |
| D25.1 | Intramural leiomyoma of uterus |
| D25.2 | Subserosal leiomyoma of uterus |
| D25.9 | Leiomyoma of uterus, unspecified |
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