Leuprorelin Acetate

What it is and how it works

Leuprorelin is a synthetic GnRH analogue. Continuous administration, after an initial transient rise in LH and FSH, down-regulates pituitary GnRH receptors and suppresses gonadotrophin secretion, reducing testosterone to castrate levels in men and oestradiol to postmenopausal levels in women.

Indications

Advanced or locally advanced hormone-dependent prostate cancer; endometriosis; uterine fibroids (pre-operative); hormone-receptor-positive breast cancer in pre- and perimenopausal women; central precocious puberty.

Dosage and administration (summary)

Depot formulations given by subcutaneous or intramuscular injection, typically 3.75 mg monthly or 11.25 mg every 3 months (longer-acting formulations also exist); regimen and duration depend on indication and product.

Contraindications

Hypersensitivity to GnRH or its analogues; pregnancy and breast-feeding; undiagnosed abnormal vaginal bleeding.

Warnings and precautions

In prostate cancer, the initial testosterone surge may cause tumour flare (bone pain, urinary obstruction, spinal cord compression); an anti-androgen is given for the first weeks in at-risk patients. Long-term androgen or oestrogen deprivation causes loss of bone mineral density and may increase risk of diabetes, cardiovascular events and QT prolongation; depression and seizures have been reported. Women should use non-hormonal contraception, as ovulation may not be suppressed initially.

Pregnancy

Contraindicated in pregnancy.

Storage and supply

Store below 25 °C (some formulations require refrigeration at 2–8 °C); do not freeze.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.