• SKIP TO CONTENT
  • SKIP NAVIGATION
  • Patient Resources
    • Clinical Trial Listings
    • What are Clinical Trials?
    • Become a Clinical Trial Volunteer
    • Useful Resources
    • FDA Approved Drugs
  • Professional Resources
    • Research Center Profiles
    • Market Research
    • Benchmark Reports
    • FDA Approved Drugs
    • Training Guides
    • Books
    • eLearning
    • Events
    • Newsletters
    • White Papers
    • SOPs
  • White Papers
  • Clinical Trial Listings
  • Advertise
  • Sign In
  • Create Account
  • Sign Out
  • My Account
Home » Directories » FDA Approved Drugs » Myfembree (relugolix, estradiol, and norethindrone acetate) tablets

AND
  • A
  • B
  • C
  • D
  • E
  • F
  • G
  • H
  • I
  • J
  • K
  • L
  • M
  • N
  • O
  • P
  • Q
  • R
  • S
  • T
  • U
  • V
  • W
  • X
  • Y
  • Z

Myfembree (relugolix, estradiol, and norethindrone acetate) tablets

  • Profile

Profile

Contact Information

Contact: Myovant Sciences and Pfizer
Website: https://www.myfembree.com/

Currently Enrolling Trials

    Show More

    Myfembree (relugolix, estradiol, and norethindrone acetate) - 2 indications

    Scroll down for more information on each indication:

    • for the management of heavy menstrual bleeding associated with uterine fibroids premenopausal women; approved May of 2021 
    • for the management of moderate to severe pain associated with endometriosis in premenopausal women; approved August of 2022

    General Information

    Myfembree is a combination of relugolix, a gonadotropin-releasing hormone (GnRH) receptor antagonist, estradiol, an estrogen, and norethindrone acetate, a progestin.

    Myfembree is specifically indicated for:

    • the management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women
    • the management of moderate to severe pain associated with endometriosis in premenopausal women

    Myfembree is supplied as a tablet for oral administration. Exclude pregnancy and discontinue hormonal contraceptives prior to initiating Myfembree. Take one tablet orally once daily at approximately the same time, with or without food. Start Myfembree as early as possible after the onset of menses but no later than seven days after menses has started. The recommended total duration of treatment with Myfembree is 24 months

    Mechanism of Action

    Myfembree is a combination of relugolix, estradiol (E2), and norethindrone acetate (NETA).

    Relugolix is a non-peptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased serum concentrations of the ovarian sex hormones estradiol and progesterone and reduced bleeding associated with uterine fibroids.

    Estradiol acts by binding to nuclear receptors that are expressed in estrogen-responsive tissues. As a component of Myfembree, the addition of exogenous estradiol may reduce the increase in bone resorption and resultant bone loss that can occur due to a decrease in circulating estrogen concentrations from relugolix alone.

    Progestins such as norethindrone act by binding to nuclear receptors that are expressed in progesterone responsive tissues. As a component of Myfembree, norethindrone may protect the uterus from the potential adverse endometrial effects of unopposed estrogen.

    Side Effects

    In women with heavy menstrual bleeding associated with uterine fibroids, adverse reactions may include, but are not limited to, the following:

    • vasomotor symptoms
    • uterine bleeding
    • alopecia
    • decreased libido

    In women with moderate to severe pain associated with endometriosis, adverse reactions may include, but are not limited to, the following:

    • headache
    • vasomotor symptoms
    • mood disorders
    • abnormal uterine bleeding
    • nausea
    • toothache
    • back pain
    • decreased sexual desire and arousal
    • arthralgia
    • fatigue
    • dizziness

    The Myfembree drug label comes with the following Black Box Warning: Estrogen and progestin combinations, including Myfembree , increase the risk of thrombotic or thromboembolic disorders, especially in women at increased risk for these events. Myfembree 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.

    Indication 1 - the management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women

    Approved May of 2021

    Clinical Trial Results

    The FDA approval of Myfembree was based on two replicate, 24-week, multinational, randomized, double-blind, placebo-controlled studies in a total of 768 premenopausal women with heavy menstrual bleeding associated with uterine fibroids. Th women were randomized 1:1:1 to receive a once daily relugolix 40 mg tablet plus an over encapsulated tablet of E2 1 mg and NETA 0.5 mg (relugolix+E2/NETA), which is equivalent to 1 tablet of Myfembree, for 24 weeks, placebo for 24 weeks, or relugolix 40 mg monotherapy for 12 weeks followed by Myfembree for 12 weeks. Treatment was initiated within the first seven days after the onset of menses. The primary endpoint was the proportion of women in the Myfembree group compared with women in the placebo group, who achieved menstrual blood loss volume of < 80 mL and at least a 50% reduction from baseline MBL volume over the last 35 days of treatment, as measured by the alkaline hematin method. In both Study L1 and Study L2, a statistically higher proportion of women treated with Myfembree achieved the primary endpoint of both an MBL volume of less than 80 mL and at least a 50% reduction from baseline in MBL volume over the last 35 days of treatment compared with placebo.

    Indication 2 - the management of moderate to severe pain associated with endometriosis in premenopausal women

    Approved August of 2022

    Clinical Trial Results

    FDA approval was based on one-year efficacy and safety data, including 24-week data from the Phase 3 SPIRIT 1 and SPIRIT 2 trials in over 1,200 women. SPIRIT 1 and 2 each met their co-primary endpoints with 75% of women in the Myfembree group in both studies achieving a clinically meaningful reduction in dysmenorrhea compared with 27% and 30% of women in the placebo groups at Week 24, respectively. For non-menstrual pelvic pain, treatment with Myfembree demonstrated a clinically meaningful reduction in pain in 59% and 66% of women, compared with 40% and 43% of women in the placebo groups. The open-label extension study for eligible women who completed either SPIRIT 1 or SPIRIT 2 showed mean bone mineral density loss of less than 1% from baseline through one year of treatment; some patients (19.7%) had losses >3%.

    Approval Date: 2021-05-01
    Company Name: Myovant Sciences and Pfizer
    Back to Listings

    Upcoming Events

    • 14Apr

      MAGI 2024: The Clinical Research Conference

    Featured Products

    • Surviving an FDA GCP Inspection

      Surviving an FDA GCP Inspection: Resources for Investigators, Sponsors, CROs and IRBs

    • Best Practices for Clinical Trial Site Management

      Best Practices for Clinical Trial Site Management

    Featured Stories

    • Jonathan Seltzer

      Thought Leadership: Remote Patient Monitoring Gives New View of Safety in Cardiac Clinical Trials

    • Quality_Compass-360x240.png

      Ask the Experts: Applying Quality by Design to Protocols

    • Obesity Treatment Patient

      Clinical Trials Need Greater Representation of Obese Patients, Experts Say

    • Modernize-360x240.png

      FDA IT Modernization Plan Prioritizes Data-Sharing, AI, Collaboration and More

    Standard Operating Procedures for Risk-Based Monitoring of Clinical Trials

    The information you need to adapt your monitoring plan to changing times.

    Learn More Here
    • About Us
    • Contact Us
    • Privacy Policy
    • Do Not Sell or Share My Data

    Footer Logo

    300 N. Washington St., Suite 200, Falls Church, VA 22046, USA

    Phone 703.538.7600 – Toll free 888.838.5578

    Copyright © 2023. All Rights Reserved. Design, CMS, Hosting & Web Development :: ePublishing