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GnRH receptor antagonist

Relugolix

Relugolix is an oral gonadotrophin-releasing hormone (GnRH) receptor antagonist; in women's health it is combined with oestradiol and a progestogen to treat symptoms of uterine fibroids and endometriosis.

Dosing — being independently re-sourced

ClinCalc Pro is rebuilding its dose data from primary open sources — the manufacturer SmPC (eMC), the WHO Model Formulary and other official references — under clinician review. This drug's structured dose is not yet published here. Confirm all doses against the product SmPC and your local formulary before prescribing.

Clinical monograph

How it works

It competitively blocks pituitary GnRH receptors, rapidly suppressing the release of LH and FSH and thereby lowering ovarian oestradiol production, with the added oestradiol/progestogen offsetting hypo-oestrogenic effects.

Prescribing in practice

  • Even with add-back hormones, treatment can reduce bone mineral density, so duration should be limited and bone health considered, particularly with risk factors for osteoporosis.
  • Because it can restore ovulation and is contraindicated in pregnancy, effective non-hormonal contraception is needed during use.
  • It is contraindicated in undiagnosed abnormal uterine bleeding and in known or suspected hormone-sensitive malignancy.

Monitoring

Assess bone mineral density where prolonged use or osteoporosis risk applies, and reassess the need for continued treatment periodically.

Counselling the patient

  • Take the tablet once daily at about the same time each day.
  • Use a non-hormonal method of contraception while taking this medicine.
  • Report any unexpected or worsening vaginal bleeding.

Evidence & guidelines

Recommended by NICE for heavy menstrual bleeding due to uterine fibroids and for symptomatic endometriosis on the basis of randomised controlled trials.

Reference: NICE TA832; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.