TheraRadar
Data updated: May 26, 2026

MYFEMBREE (estradiol)

Gonadotropin Releasing Hormone Receptor Antagonists
Women's Health Approved 2021-05-26

Myfembree is a combination of relugolix (a GnRH receptor antagonist), estradiol (an estrogen), and norethindrone acetate (a progestin). It is indicated for premenopausal women to manage heavy menstrual bleeding associated with uterine fibroids and moderate to severe pain associated with endometriosis. Due to the risk of continued, potentially irreversible bone loss, use of this medication is limited to a total duration of 24 months.

Source: FDA Label • SUMITOMO PHARMA AM • Gonadotropin Releasing Hormone Receptor Antagonist

How MYFEMBREE Works

Relugolix competitively blocks GnRH receptors in the pituitary gland, reducing the release of LH and FSH. This leads to decreased production of ovarian estrogen and progesterone, which reduces fibroid-related bleeding and endometriosis pain. To mitigate the side effects of low estrogen, the medication includes estradiol to maintain bone mineral density and norethindrone acetate to protect the uterine lining from the potential adverse effects of unopposed estrogen.

4
Indications
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Phase 3 Trials
5
Years on Market

Details

Status
Prescription
First Approved
2021-05-26
Patent Cliff
2042

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Patent cliff and revenue data

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Routes
ORAL
Dosage Forms
TABLET

Companies

Active Ingredient: ESTRADIOL , NORETHINDRONE ACETATE , RELUGOLIX

MYFEMBREE Approval History

2022
2023
2024
2025
2026
Original
New Indication
New Form
Label Update
7 FDA actions from 2021 to 2025 · 3 indication expansions
Aug 2025 SUPPL
Label · Labeling
Jul 2024 SUPPL
Label · Labeling
Apr 2024 SUPPL
Efficacy

What MYFEMBREE Treats

3 indications

MYFEMBREE is approved for 3 conditions since its original approval in 2021. These indications span multiple therapeutic areas including oncology, immunology, and more.

  • Heavy Menstrual Bleeding
  • Uterine Leiomyoma
  • Endometriosis
Source: FDA Label

MYFEMBREE Boxed Warning

THROMBOEMBOLIC DISORDERS AND VASCULAR EVENTS Estrogen and progestin combinations, including MYFEMBREE, 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 [see Warnings and Precautions ( 5.1 )]. MYFEMBREE is contraindicated in women with current or a history of thrombotic or thromboembolic disorders and in women at increased risk for...

MYFEMBREE Competitive Set

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Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.

Drugs Similar to MYFEMBREE

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Clinical Trial Registry

65 trials
Trial Sponsor ID Phase Status Title
NCT07455903 2025-GAR-001 Ph 2 recruiting Assessing Efficacy of Neoadjuvant ADT in Localized High-Risk Prostate Cancer Patients Utilizing 18F-Flotufolastat PSMA PET/CT
NCT04423211 EA8191 NCI-2020-02686, EA8191 Ph 3 recruiting Treating Prostate Cancer That Has Come Back After Surgery With Apalutamide and Targeted Radiation Based on PET Imaging
NCT05716516 ESTHER STUDY02001740 NCI-2023-05453 Ph 2 recruiting STUDY02001740;22SCH740: Estradiol For ER+ Advanced Breast Cancer (ESTHER)
NCT05050084 NRG-GU010 NCI-2021-08760, NRG-GU010 Ph 3 active not recruiting Two Studies for Patients With Unfavorable Intermediate Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a Higher Gene Risk Score, The Guidance Trial
NCT05053152 NRG-GU011 NCI-2021-09164, NRG-GU011 Ph 2 active not recruiting Testing the Addition of the Drug Relugolix to the Usual Radiation Therapy for Advanced-Stage Prostate Cancer, The NRG Promethean Study
NCT04513717 NRG-GU009 NCI-2020-04705, NRG-GU009 Ph 3 active not recruiting Two Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a High Gene Risk Score, The PREDICT-RT Trial
NCT04523207 results posted CR108875 56021927PCR2041 Ph 2 completed A Study of Apalutamide (Adjuvant Treatment) and Androgen Deprivation Therapy (ADT) in Participants Who Have Undergone Radical Prostatectomy (RP) for Non-metastatic Prostate Cancer and Who Are at High Risk for Metastases
NCT06378866 DIVINE MC230502 R01CA286127, 23-012176 Ph 2 recruiting Stereotactic Body Radiation Therapy Plus Immediate or Delayed Androgen Receptor Pathway Inhibitor and Androgen Deprivation Therapy or Salvage Radiation Therapy for the Treatment of Prostate Cancer, DIVINE Trial
NCT06005610 GETITRIgHT results posted A5403 38806 Ph 2 terminated Estradiol Therapy In Transgender Women to Research Interactions With HIV Therapy
NCT07025369 MC240503 NCI-2025-03965, 25-002008 Ph 2 recruiting Androgen Deprivation Therapy (Relugolix) for the Improvement of Diagnostic Imaging (PSMA PET/CT Scan) in Patients With High Risk or Very High Risk Prostate Cancer, The EnrichPSMA Trial
NCT05457972 STUDY20220578 Ph 4 recruiting Postpartum Vaginal Estrogen for Breastfeeding Patients
NCT06330805 OSU-23069 NCI-2024-00705 Ph 2 recruiting Effects of Relugolix vs Leuprolide on Cardiac Function in Patients With Prostate Cancer
NCT06463457 24-217 Ph 2 active not recruiting Comeback From Long coursE Androgen Deprivation Therapy (ADT) With RElugolix and Darolutamide (CLEARED)
NCT06650579 STUDY00007557 P30CA138292, NCI-2024-07761 Ph 3 recruiting REVELUTION-2: Relugolix+Abiraterone Acetate (AA) Versus Leuprolide+AA Cardiac Trial
NCT05320406 REVELUTION results posted STUDY00003654 NCI-2022-00117, STUDY00003654 Ph 2 active not recruiting RElugolix VErsus LeUprolide Cardiac Trial
NCT06631521 IIR-US-00295 2077841 Ph 1 recruiting Neoadjuvant Darolutamide and Relugolix Combination Preceding Radical Prostatectomy for Prostate Cancer
NCT06671548 QLG1079-301 Ph 3 recruiting Efficacy & Safety Study of Relugolix in Women With Heavy Menstrual Bleeding Associated With Uterine Fibroids
NCT04192266 results posted HSC-MS-23-0497 R33MH111907 Ph 3 completed Estrogen and Fear in PTSD
NCT06499870 NU 24U02 NCI-2024-03934, STU00221219 Ph 2 recruiting Relugolix and Enzalutamide in Combination With Radiation Therapy for the Treatment of Very High Risk Prostate Cancer, OPTIMAL Trial
NCT03689543 results posted 180144 18-M-0144 Ph 2 completed Estrogen Receptor Beta and Mood
NCT05605964 MVT-601-056 Ph 3 completed Randomized Study to Evaluate MACE in Patients With Prostate Cancer Treated With Relugolix or Leuprolide Acetate
NCT04666129 MVT-601-049 Ph 1 completed Study of Relugolix in Men With Metastatic Castration-Sensitive Prostate Cancer or Non-Metastatic or Metastatic Castration-Resistant Prostate Cancer
NCT05765500 22-599 Ph 2 recruiting RecoverPC: Relugolix vs GnRH Agonist in Quality of Life
NCT06253702 2023-0548 1R01HL150361-01, EDUC/KINESIOLOGY Ph 4 completed Brain Blood Flow Responses to Stress: Sex Differences
NCT02238808 PRESTO EER001 Ph 2 active not recruiting A Study to See Whether Estrogen Can Slow the Growth of Some ER Positive Breast Cancers
NCT03751124 results posted MVT-601-035 2018-001368-43 Ph 3 completed Study of Relugolix With Estradiol and Norethindrone Acetate in Women With Heavy Menstrual Bleeding Associated With Uterine Fibroids
NCT03412890 results posted MVT-601-3003 2017-003310-74 Ph 3 completed LIBERTY EXTENSION: Efficacy and Safety Extension Study of Relugolix in Women With Heavy Menstrual Bleeding Associated With Uterine Fibroids
NCT05617820 71836003 Ph 3 completed Study Comparing Estradiol Vaginal Inserts 4mcg To IMVEXXY ® (Estradiol Vaginal Inerts 4 mcg) In The Treatment Of Dyspareunia in Women With Vulvur and Vaginal Atrophy
NCT06129851 STUDY00150674 NCI-2023-09079, STUDY00150674 Ph 2 not yet recruiting Relugolix in Combination With Radiation Therapy for Treating Patients With High Risk Prostate Cancer
NCT03654274 results posted MVT-601-3103 2017-004066-10 Ph 3 completed SPIRIT EXTENSION: Efficacy and Safety Extension Study of Relugolix in Women With Endometriosis-Associated Pain
NCT04225221 results posted 19-2343 R21MH121726 Ph 2 completed Neurobiology of Bulimia Nervosa
NCT04933240 HM20021901 Ph 4 withdrawn Tamoxifen Versus Estradiol for Unscheduled Bleeding in Etonogestrel Implant Users, a Randomized Pilot Trial
NCT03103087 results posted MVT-601-3002 2016-005113-50 Ph 3 completed LIBERTY 2: Efficacy & Safety Study of Relugolix in Women With Heavy Menstrual Bleeding Associated With Uterine Fibroids
NCT03049735 results posted MVT-601-3001 2016-003727-27 Ph 3 completed LIBERTY 1: Efficacy & Safety Study of Relugolix in Women With Heavy Menstrual Bleeding Associated With Uterine Fibroids
NCT01923298 results posted 13-0477-04 EString Ph 2 completed Estradiol Levels in Patients Treated With Estring
NCT03085095 HERO results posted MVT-601-3201 2017-000160-15 Ph 3 completed A Study to Evaluate the Safety and Efficacy of Relugolix in Men With Advanced Prostate Cancer
NCT03493126 results posted 2018H0006 Ph 4 completed Vaginal Estrogen on Postpartum Atrophy, Perineal Pain, and Sexual Function
NCT02995694 results posted 71462901 Ph 3 completed A Study Comparing Estradiol Vaginal Cream to Estrace® Cream in Females With Atrophic Vaginitis
NCT04714554 MVT-601-054 Ph 1 completed A Study of the Effects of Erythromycin on the Pharmacokinetics of Relugolix, Estradiol, and Norethindrone in Healthy Postmenopausal Women and on the Pharmacokinetics of Relugolix in Healthy Adult Men
NCT04978688 MVT-601-1001 Ph 1 completed Study of Relugolix Alone and Relugolix Combined With Hormonal Add-Back Therapy in Healthy Premenopausal Female Participants
NCT01441635 results posted M12-663 Ph 2 completed Safety and Efficacy of Elagolix in Pre-Menopausal Women With Heavy Uterine Bleeding and Uterine Fibroids
NCT03204331 MVT-601-3102 2017-001632-19 Ph 3 completed SPIRIT 2: Efficacy and Safety Study of Relugolix in Women With Endometriosis-Associated Pain
NCT03204318 MVT-601-3101 2017-001588-19 Ph 3 completed SPIRIT 1: Efficacy and Safety Study of Relugolix in Women With Endometriosis-Associated Pain
NCT01895881 EPPA EPPA - 12101906 Ph 2 withdrawn Estrogen Therapy as Prevention in the Progression of Aneurysm (EPPA) Trial
NCT00997893 RISE results posted 2009-0052 5R01MH083782-05 Ph 2 completed Research Investigation of Soy and Estrogen
NCT03848234 EST-S-01 Ph 3 completed Estradiol Patch as add-on to Antipsychotics in Patients With Schizophrenia, Schizoaffective or Schizophreniform Disorder
NCT02455453 results posted 201411005 5R01CA195450-03 Ph 2 completed Assessment of Functional Status of Estrogen Receptors in Breast Cancer by Positron Emission Tomography
NCT01083641 results posted CO09711 H-2009-0172, NCI-2011-00618 Ph 2 terminated Estrogen for Triple Negative Breast Cancer
NCT02255175 PEERS results posted 13-3572 K12HD001441-15, K23MH105569-01A1 Ph 4 completed Perimenopausal Effects of Estradiol on Reward Responsiveness
NCT01942668 REPLENISH results posted TXC12-05 REPLENISH Trial Ph 3 completed A Safety and Efficacy Study of the Combination Estradiol and Progesterone to Treat Vasomotor Symptoms

Showing 50 of 65 trials

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Key Completed Trials

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Completed studies with published results, ranked by significance

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Trial Timeline

Full development history with FDA approval milestones

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Understanding FDA Approval Types
Count Type What it means
- ORIG Original approval - drug first enters market
- SUPPL - Efficacy New indication (new disease/condition approved)
- SUPPL - Labeling Label text changes (warnings, dosing updates)
- SUPPL - Manufacturing Production changes (new facility)
- SUPPL - Chemistry Formulation changes (new dosage strength)

Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.

MYFEMBREE FDA Label Details

Indications & Usage

FDA Label (PDF)

MYFEMBREE is indicated for the treatment of Heavy Menstrual Bleeding; Uterine Leiomyoma; Endometriosis.

⚠️ BOXED WARNING

WARNING: THROMBOEMBOLIC DISORDERS AND VASCULAR EVENTS Estrogen and progestin combinations, including MYFEMBREE, 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 inc...

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7 OB patents · 3 families · 176 international docs across 37 countries

MYFEMBREE Patents & Exclusivity

Latest Patent: Nov 2042
Exclusivity: Jan 2026

Patents (8 active)

US12551447 Expires Nov 5, 2042
US11793812 Expires May 3, 2038
US11033551 Expires Sep 29, 2037
US11957684 Expires Sep 29, 2037
US12325714 Expires Sep 27, 2033
US11795178 Expires Sep 27, 2033
US7300935 Expires Jan 28, 2029
US8058280 Expires Jan 28, 2026

Exclusivity

M-289 Until Jan 2026
Source: FDA Orange Book

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Patent Timeline

  • Cliff: 2042
  • 8 active patents

Trial Analysis

  • Clinical trial tracking
  • Development stage analysis

Competitive Landscape

  • 9 similar drugs
  • Same target/indication analysis
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Data Sources

Data sourced from official FDA and NIH databases. Click links to verify on original sources.