What is Ryeqo medication?

Ryeqo Medication: A Treatment for Uterine Fibroids and Endometriosis

Ryeqo is an oral fixed-dose combination medication containing relugolix, estradiol, and norethisterone acetate that is approved for managing moderate to severe symptoms of uterine fibroids in the EU and for heavy menstrual bleeding associated with uterine fibroids in the US (where it's marketed as Myfembree). 1, 2

Composition and Mechanism of Action

Ryeqo contains three active ingredients that work together:

1. Relugolix (40 mg): A gonadotropin-releasing hormone (GnRH) receptor antagonist that:

   • Competitively binds to GnRH receptors
   • Prevents release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH)
   • Reduces ovarian production of estrogen and progesterone
   • Suppresses ovulation and corpus luteum formation 2

2. Estradiol (1 mg): Added to:

   • Prevent bone mineral density loss
   • Reduce vasomotor symptoms (hot flushes)
   • Maintain estradiol in therapeutic range 2

3. Norethisterone acetate (0.5 mg) (also known as norethindrone acetate):

   • Works with estradiol to prevent hypoestrogenic effects
   • Helps maintain bone health 2, 3

Clinical Applications

Ryeqo is approved for:

• In the European Union and United Kingdom:

  • Management of moderate to severe symptoms associated with uterine fibroids in adult premenopausal women 2
  • Symptomatic treatment of endometriosis in adult women of reproductive age with previous medical or surgical treatment for endometriosis 3

• In the United States (as Myfembree):

  • Management of heavy menstrual bleeding associated with uterine fibroids
  • Management of moderate to severe pain associated with endometriosis 2, 3

Clinical Efficacy

For Uterine Fibroids

• In the LIBERTY phase 3 trials, Ryeqo substantially decreased menstrual bleeding and improved other uterine fibroid symptoms 1
• Provides convenient once-daily administration 1

For Endometriosis

• In pivotal phase III trials, Ryeqo significantly improved:
  • Dysmenorrhea (painful menstruation)
  • Non-menstrual pelvic pain
  • Overall pelvic pain and dyspareunia (painful intercourse)
  • Reduced need for analgesics and opioids
  • Improved health-related quality of life 3
• Efficacy was sustained for up to 2 years in long-term studies 3

Safety Profile

• Generally well tolerated with the most common adverse reactions being:

  • Vasomotor symptoms (hot flushes) 1

• Bone health: Treatment for up to 2 years did not induce clinically meaningful bone loss in the majority of women 1, 3

• Advantages over GnRH agonists:

  • The addition of estradiol/norethisterone acetate mitigates the hypoestrogenic effects typically seen with GnRH monotherapy
  • Allows for longer-term treatment without the bone mineral density loss and severe vasomotor symptoms associated with GnRH agonists 2

Administration

• Dosing: One tablet taken orally once daily 1, 2, 3
• Convenience: The once-daily oral dosing regimen offers convenience compared to injectable GnRH agonists 3

Clinical Positioning

Ryeqo represents an important addition to the treatment options for women with:

• Uterine fibroids causing heavy menstrual bleeding
• Moderate to severe endometriosis-associated pain
• May delay or prevent the need for surgical intervention 2

This medication offers an alternative to traditional treatments like combined hormonal contraceptives (used off-label), NSAIDs, and injectable GnRH agonists, with the advantage of oral administration and better tolerability for long-term use.