What are the benefits and risks of Myfembree (relugolix, estradiol, and norethindrone acetate)?

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Last updated: February 11, 2025View editorial policy

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From the Guidelines

Myfembree (relugolix, estradiol, and norethindrone acetate) is a beneficial treatment option for managing uterine fibroids, offering a reduction in bleeding symptoms and fibroid size.

Benefits

  • Reduces bleeding symptoms: Myfembree has been shown to decrease bleeding symptoms associated with uterine fibroids, improving patient quality of life 1.
  • Decreases fibroid size: The combination of relugolix, estradiol, and norethindrone acetate in Myfembree can reduce fibroid size, making it a useful treatment option for patients preparing for surgery 1.
  • Mitigates hypoestrogenic effects: The addition of low-dose estrogen and progestin to Myfembree helps mitigate hypoestrogenic effects, such as headaches, hot flushes, and loss of bone mineral density, which are commonly associated with GnRH agonists and antagonists 1.

Risks

  • Fertility suppression: Myfembree can suppress fertility during treatment, and symptoms may rapidly recur after cessation of therapy 1.
  • Hypoestrogenic effects: Although the combination of relugolix, estradiol, and norethindrone acetate in Myfembree mitigates hypoestrogenic effects, patients may still experience these symptoms, particularly if they have a history of hormone-sensitive conditions 1.
  • Potential for hepatotoxicity: While Myfembree itself has not been directly associated with hepatotoxicity, the use of certain progesterone receptor modulators, such as ulipristal acetate, has been linked to reports of hepatotoxicity, highlighting the importance of careful patient selection and monitoring 1.

From the Research

Benefits of Myfembree

  • Myfembree (relugolix, estradiol, and norethindrone acetate) has been shown to decrease menstrual bleeding and improve symptoms of uterine fibroids in women with heavy menstrual bleeding associated with uterine fibroids 2, 3.
  • The combination of relugolix, estradiol, and norethindrone acetate has been found to ameliorate relugolix-induced bone loss and hot flush 2.
  • Myfembree has been approved for the management of heavy menstrual bleeding associated with uterine fibroids in the USA and management of moderate to severe symptoms of uterine fibroids in the EU 2, 4.
  • Treatment with Myfembree for up to 2 years did not induce a clinically meaningful bone loss in the majority of women 2.
  • Myfembree may lessen distress associated with uterine fibroid symptoms and improve health-related quality of life related to uterine fibroids 5.

Risks of Myfembree

  • The most common adverse reaction associated with Myfembree is vasomotor symptoms 2.
  • Relugolix monotherapy is associated with signs and symptoms of a hypoestrogenic state, including bone mineral density loss and vasomotor symptoms 4.
  • Myfembree may have potential risks associated with its use, such as the risk of fibroid recurrence, symptom recurrence, and the subsequent need for reintervention after surgical myomectomy 6.

Efficacy of Myfembree

  • Myfembree has been shown to be effective in reducing menstrual bleeding and improving symptoms of uterine fibroids in women with heavy menstrual bleeding associated with uterine fibroids 2, 3.
  • The efficacy of Myfembree has been demonstrated in two phase 3 LIBERTY trials, which found that relugolix + estradiol/norethisterone substantially decreased menstrual bleeding and improved a range of other uterine fibroid symptoms in women with uterine fibroids-associated heavy menstrual bleeding 2.
  • Myfembree may have the potential to delay the recurrence of fibroid symptoms, prolong the improved quality of life, and delay the need for re-intervention after uterine sparing surgery 6.

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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