Relugolix/Estradiol/Norethisterone (Combination)

How it works

Relugolix antagonises pituitary GnRH receptors to suppress ovarian sex hormones, and the bundled estradiol and norethisterone acetate act as add-back to mitigate bone loss and menopausal-type symptoms.

Prescribing in practice

• Reduction in bone mineral density is the principal safety issue, so treatment duration is restricted and bone density monitoring considered with longer courses or where osteoporosis risk is high.
• The oestrogen-progestogen content means combined-hormone cautions apply, with contraindications including hormone-sensitive cancers, a history of thromboembolism, and undiagnosed vaginal bleeding.
• Non-hormonal contraception is recommended as contraceptive cover should not be assumed, and the product must be discontinued if pregnancy is suspected.

Monitoring

Evaluate thromboembolic and cardiovascular risk and blood pressure at baseline and on review, with bone mineral density monitoring during prolonged use.

Counselling the patient

• Take the tablet once daily at a consistent time.
• Use non-hormonal contraception and report any signs of pregnancy.
• Seek urgent advice for chest pain, breathlessness, or a painful swollen leg.

Evidence & guidelines

NICE supports relugolix combination therapy for uterine fibroids and endometriosis, based on the LIBERTY and SPIRIT randomised trials.