Relugolix, estradiol, and norethindrone (Oral route)

Pronunciation:

rel-ue-GOE-lix, es-tra-DYE-ol, nor-ETH-in-drone AS-e-tate

Brand Names:

Myfembree

Dosage Forms:

Tablet

Warnings:

Oral route(Tablet)

Estrogen and progestin combination products, including relugolix/estradiol/norethindrone acetate, increase the risk of thrombotic or thromboembolic disorders including pulmonary embolism (PE), deep vein thrombosis (DVT), stroke and myocardial infarction (MI), especially in women at increased risk for these events. Relugolix/estradiol/norethindrone acetate 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 over 35 years of age who smoke or women with uncontrolled hypertension .

Classifications:

Therapeutic—

Endocrine-Metabolic Agent

Pharmacologic—

Luteinizing Hormone Releasing Hormone Antagonist

Uses of This Medicine:

Relugolix, estradiol, and norethindrone combination is used to manage heavy menstrual bleeding caused by uterine leiomyomas (fibroids) in premenopausal women. It is also used to manage moderate to severe pain caused by endometriosis in premenopausal women.

This medicine is available only with your doctor's prescription.

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Appropriate studies have not been performed on the relationship of age to the effects of relugolix, estradiol, and norethindrone combination in the pediatric population. Safety and efficacy have not been established.

Older adults—

No information is available on the relationship of age to the effects of relugolix, estradiol, and norethindrone combination in geriatric patients.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

Bepridil
Cisapride
Dronedarone
Ketoconazole
Mesoridazine
Pimozide
Piperaquine
Posaconazole
Saquinavir
Sparfloxacin
Terfenadine
Thioridazine
Tranexamic Acid
Ziprasidone

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

Abametapir
Adagrasib
Alfuzosin
Amifampridine
Amiodarone
Amisulpride
Amitriptyline
Amobarbital
Amoxicillin
Ampicillin
Amprenavir
Anagrelide
Apalutamide
Apomorphine
Aprepitant
Aripiprazole
Aripiprazole Lauroxil
Armodafinil
Arsenic Trioxide
Artemether
Asenapine
Astemizole
Atazanavir
Azithromycin
Bacampicillin
Bedaquiline
Belzutifan
Betamethasone
Bexarotene
Boceprevir
Bosentan
Buprenorphine
Bupropion
Buserelin
Butabarbital
Butalbital
Carbamazepine
Carbenicillin
Carvedilol
Cefaclor
Cefadroxil
Cefdinir
Cefditoren
Cefixime
Cefpodoxime
Cefprozil
Ceftazidime
Ceftibuten
Cefuroxime
Cenobamate
Ceritinib
Chloroquine
Chlorpromazine
Ciprofloxacin
Citalopram
Clarithromycin
Clobazam
Clofazimine
Clomipramine
Cloxacillin
Clozapine
Cobicistat
Colesevelam
Conivaptan
Crizotinib
Cyclacillin
Cyclobenzaprine
Cyclosporine
Dabrafenib
Darunavir
Dasatinib
Degarelix
Delamanid
Desipramine
Deslorelin
Deutetrabenazine
Dexamethasone
Dicloxacillin
Dipyrone
Disopyramide
Dofetilide
Dolasetron
Domperidone
Donepezil
Doxepin
Doxycycline
Droperidol
Ebastine
Efavirenz
Elagolix
Elvitegravir
Encorafenib
Entrectinib
Enzalutamide
Eribulin
Erythromycin
Escitalopram
Eslicarbazepine Acetate
Etravirine
Famotidine
Fedratinib
Felbamate
Fexinidazole
Fingolimod
Flecainide
Flibanserin
Fluoxetine
Formoterol
Fosamprenavir
Fosaprepitant
Foscarnet
Fosnetupitant
Fosphenytoin
Galantamine
Gatifloxacin
Gemifloxacin
Glasdegib
Gonadorelin
Goserelin
Granisetron
Grazoprevir
Griseofulvin
Guar Gum
Halofantrine
Haloperidol
Histrelin
Hydroquinidine
Hydroxychloroquine
Hydroxyzine
Ibutilide
Iloperidone
Imipramine
Indinavir
Inotuzumab Ozogamicin
Isotretinoin
Itraconazole
Ivabradine
Ivosidenib
Lapatinib
Lefamulin
Lenvatinib
Lesinurad
Leuprolide
Levofloxacin
Lixisenatide
Lofexidine
Lopinavir
Lorlatinib
Lumacaftor
Lumefantrine
Macimorelin
Mavacamten
Mefloquine
Mephobarbital
Methadone
Methohexital
Methotrimeprazine
Metronidazole
Mifepristone
Minocycline
Mitapivat
Mitotane
Mizolastine
Mobocertinib
Modafinil
Moricizine
Moxifloxacin
Mycophenolate Mofetil
Mycophenolic Acid
Nafarelin
Nafcillin
Nelfinavir
Netupitant
Nevirapine
Nilotinib
Norfloxacin
Octreotide
Ofloxacin
Olanzapine
Ondansetron
Osilodrostat
Osimertinib
Oxacillin
Oxaliplatin
Oxcarbazepine
Oxytetracycline
Paliperidone
Panobinostat
Papaverine
Paroxetine
Pasireotide
Pazopanib
Penicillin G
Penicillin G Procaine
Penicillin V
Pentamidine
Pentobarbital
Perphenazine
Phenobarbital
Phenylbutazone
Phenytoin
Pimavanserin
Pipamperone
Pitolisant
Pixantrone
Ponesimod
Prednisolone
Prednisone
Primidone
Probucol
Procainamide
Prochlorperazine
Promethazine
Propafenone
Protriptyline
Quetiapine
Quinidine
Quinine
Ranolazine
Red Clover
Ribociclib
Rifabutin
Rifampin
Rifapentine
Rilpivirine
Risperidone
Ritonavir
Rufinamide
Saquinavir
Secobarbital
Selpercatinib
Sertindole
Sertraline
Sevoflurane
Simeprevir
Siponimod
Sodium Phosphate
Sodium Phosphate, Dibasic
Sodium Phosphate, Monobasic
Solifenacin
Somatrogon-ghla
Sorafenib
Sotalol
St John's Wort
Sugammadex
Sulpiride
Sultamicillin
Sultopride
Sunitinib
Tacrolimus
Tamoxifen
Tazemetostat
Telaprevir
Telavancin
Telithromycin
Telotristat Ethyl
Tetrabenazine
Tetracycline
Theophylline
Thiopental
Thioridazine
Ticarcillin
Tigecycline
Tipranavir
Tirzepatide
Tizanidine
Tolterodine
Topiramate
Toremifene
Trazodone
Triclabendazole
Trimipramine
Triptorelin
Troglitazone
Ulipristal
Valproic Acid
Vandetanib
Vardenafil
Vemurafenib
Venlafaxine
Verapamil
Vilanterol
Vinflunine
Voclosporin
Voriconazole
Vorinostat
Voxilaprevir
Zotepine
Zuclopenthixol

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

Amitriptyline
Atazanavir
Atorvastatin
Clomipramine
Diazepam
Doxepin
Ginseng
Imipramine
Lamotrigine
Levothyroxine
Licorice
Lorazepam
Parecoxib
Selegiline
Tacrine
Temazepam
Tipranavir
Triazolam
Troleandomycin
Valdecoxib
Voriconazole
Warfarin

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

Caffeine

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

Abnormal or unusual vaginal bleeding or
Blood clots (eg, deep vein thrombosis, pulmonary embolism) or history of or
Breast cancer or history of or
Heart attack, history of or
Heart or blood vessel disease or
Heart rhythm problems (eg, atrial fibrillation) or
Hypertension (high blood pressure), uncontrolled or
Liver disease, severe or
Migraine headache or
Osteoporosis (weak bones) or
Stroke, history of—Should not be used in patients with these conditions.

Cholestatic jaundice (bile problem) during pregnancy or previous pill use (eg, estrogen), history of or
Diabetes or
Dyslipidemia (high cholesterol in the blood) or
Fracture (broken bone), history of or
Gallbladder disease or
Mental problems (eg, depression) or history—Use with caution. May make these conditions worse.

Obesity—Use with caution. May increase risk for more side effects.

Proper Use of This Medicine:

Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

This medicine comes with a patient information leaflet. Read and follow these instructions carefully. Ask your doctor if you have any questions.

Take the tablet at about the same time each day, with or without food.

Use this medicine within 7 days from the start of your menstrual period.

You may receive other medicines (eg, calcium or vitamin D supplements) to help reduce bone loss.

Take this medicine at least 6 hours before taking other medicines called P-gp inhibitors. Ask your doctor about these medicines.

Dosing—

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For oral dosage form (tablet):
- For heavy menstrual bleeding caused by uterine fibroids and moderate to severe pain caused by endometriosis:
  - Adults—One tablet once a day for up to 24 months. Each tablet contains 40 milligrams (mg) relugolix, 1 mg estradiol, and 0.5 mg norethindrone.
  - Children—Use and dose must be determined.

Missed dose—

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage—

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly. Blood and urine tests may be needed to check for unwanted effects.

This medicine may increase your risk of early pregnancy loss. Your doctor may give you a pregnancy test before you start using this medicine to make sure you are not pregnant. Birth control pills may not work as well to prevent pregnancy when used with this medicine. Use another form of birth control (eg, condoms, spermicide) during treatment and for at least 1 week after the last dose. If a pregnancy occurs while using the medicine, tell your doctor right away.

Do not use this medicine if you smoke cigarettes or if you are over 35 years old. If you smoke while using this medicine, you increase your risk of having a heart attack, stroke, or blood clot. Your risk is even higher if you are over age 35, if you have diabetes, high blood pressure, high cholesterol, or if you are overweight. Talk with your doctor about ways to stop smoking. Keep your diabetes under control. Ask your doctor about diet and exercise to control your weight and blood cholesterol level.

Check with your doctor right away if you have pain in the chest, groin, or legs, especially the calves, difficulty with breathing, a sudden, severe headache, slurred speech, a sudden, a sudden loss of coordination, or vision changes while using this medicine.

This medicine can cause your bone mineral density to decrease, which may lead to osteoporosis or weakened bones. Check with your doctor if you have pain in the back, ribs, arms, or legs, or a decrease in your height.

This medicine may increase your risk of having hormone-sensitive cancer, including breast cancer. Check with your doctor right away if you have clear or bloody discharge from the nipple, an inverted nipple, dimpling of the breast skin, a lump in the breast or under the arm, crusting or scaling of the nipple, redness or swelling of the breast, or a sore on the skin of the breast that does not heal.

This medicine may cause some people to be agitated, irritable, or display other abnormal behaviors. It may also cause some people to have suicidal thoughts and tendencies or to become more depressed. Also tell your doctor if you have sudden or strong feelings, including feeling nervous, angry, restless, violent, or scared. If you or your caregiver notice any of these side effects, tell your doctor right away.

Check with your doctor right away if you have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea or vomiting, unusual tiredness or weakness, or yellow eyes or skin. These could be symptoms of a serious liver or gallbladder problem.

This medicine may cause changes in menstrual bleeding, which may decrease your ability to recognize pregnancy. Talk to your doctor if you have concerns.

This medicine may cause thinning or loss of hair. Talk with your doctor if you have any concerns about this.

Make sure any doctor or dentist who treats you knows that you are using this medicine. You may need to stop using this medicine for at least 4 to 6 weeks before having surgery.

Before you have any medical tests, tell the medical doctor in charge that you are taking this medicine. The results of some tests may be affected by this medicine.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common: Heavy non-menstrual vaginal bleeding; longer or heavier menstrual periods; normal menstrual bleeding occurring earlier, possibly lasting longer than expected; unusually heavy or unexpected menstrual bleeding; vaginal bleeding or spotting

Less common: Anxiety; discouragement; feeling sad or empty; hair loss, thinning of hair; irritability; lack of appetite; loss of interest or pleasure; mood swings; trouble concentrating; trouble sleeping; unusual tiredness or weakness

Rare: Pelvic pain; stomach pain, bloating

Incidence not known: Blurred vision; chest pain or tightness; chills; clay-colored stools; cough; dark urine; diarrhea; dizziness or lightheadedness; dry mouth; fainting; fast heartbeat; fever; fruit-like breath odor; headache; hives, itching; increased hunger; increased thirst; increased urination; loss of appetite; loss of consciousness; nausea and vomiting; puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue; skin rash; trouble breathing; unexplained weight loss; unpleasant breath odor; vomiting of blood; yellow eyes or skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common: Feeling of warmth; increased sweating; night sweats; redness of the face, neck, arms, and occasionally, upper chest; toothache

Less common: Back pain; decreased interest in sexual intercourse; difficulty in moving; inability to have or keep an erection; joint pain; loss in sexual ability, desire, drive, or performance; muscle pain or stiffness

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Last Updated: 11/16/2023

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