Relugolix with estradiol and norethisterone acetate

How it works

Relugolix competitively blocks pituitary GnRH receptors to lower oestrogen and progesterone, while the added estradiol and norethisterone provide hormonal add-back to limit hypo-oestrogenic effects on bone and vasomotor symptoms.

Prescribing in practice

• Bone mineral density loss is the key long-term concern, so duration is limited and BMD assessment considered, especially with extended use or pre-existing osteoporosis risk.
• As it contains an oestrogen-progestogen component it carries combined hormonal contraceptive-type cautions, and it is contraindicated in known, suspected or hormone-dependent malignancy, undiagnosed genital bleeding and a history of venous or arterial thromboembolism.
• It is not a contraceptive of itself in the expected manner and ovulation suppression cannot be assumed early, so non-hormonal contraception is advised; it must be stopped if pregnancy occurs.

Monitoring

Assess cardiovascular and thromboembolic risk and blood pressure before and during treatment, and monitor bone mineral density when prolonged therapy is needed.

Counselling the patient

• Take one tablet at the same time each day with or without food.
• Use a non-hormonal method of contraception and report a missed period or possible pregnancy promptly.
• Tell your doctor about any leg pain or swelling, chest pain, breathlessness, or unusual vaginal bleeding.

Evidence & guidelines

NICE recommends relugolix combination therapy as an option for uterine fibroids and for endometriosis, supported by the LIBERTY and SPIRIT phase 3 trial programmes.