One of the most widely used GnRH agonists. Its long-acting injections suppress sex hormones in prostate cancer, endometriosis, fibroids, and central precocious puberty.
FDA (US): Approved (1985, Lupron) for advanced prostate cancer; later Lupron Depot for endometriosis, uterine fibroids, and central precocious puberty (and Eligard, Fensolvi, Camcevi)
EMA (EU): Authorized mainly through national procedures in the EU and in Spain (Procrin, Eligard…); Camcevi approved by the EMA (2022) for hormone-dependent advanced prostate cancer
Dose
Prostate cancer: 7.5 mg per month, 22.5 mg every 3 months, or 45 mg every 6 months. Endometriosis: 3.75 mg per month or 11.25 mg every 3 months, maximum 6 months (12 months with 'add-back' hormone replacement therapy). Precocious puberty: according to weight and formulation (FDA prescribing information).
Safety
Hot flashes, sweating, loss of libido, erectile dysfunction or vaginal dryness, mood changes, and loss of bone density with prolonged use. In prostate cancer, possible initial worsening of symptoms. Metabolic and cardiovascular risk with androgen deprivation and possible QT prolongation. Contraindicated in pregnancy. Under medical supervision.
Interactions
Caution with drugs that prolong the QT interval.
Differences between women and men
It is used in both sexes for different purposes: in men for prostate cancer; in women for endometriosis and fibroids (limited to 6 months without 'add-back' because of bone loss); and in boys and girls with central precocious puberty, which is much more common in girls (49 of 54 in one trial). Contraindicated in pregnancy. View the study →
Effect by goal · level of evidence
Central precocious puberty: effective suppression with monthly or quarterly depot
reducesModerateRCT (AA)in people
Suppression with all 3 regimens
In 54 children (49 girls), doses of 7.5 mg monthly and 11.25 or 22.5 mg every 3 months quickly halted puberty for 2 years, with no differences in growth or bone age.
Prostate cancer: slower chemical castration than with antagonists
reducesHighRCT (AA)in people
96% suppression at 1 year
As a comparator in a trial of 610 men, leuprolide 7.5 mg monthly kept testosterone at castrate levels in 96.4% for one year, but none reached it by day 3 (because of the initial surge).
Mimics GnRH. For 1–2 weeks LH and sex hormones rise ('flare'), and then the pituitary gland becomes desensitized and stops stimulating the testes or ovaries. Testosterone or estrogen drop to very low levels for as long as the depot lasts.
What the evidence says
In people
Central precocious puberty: effective suppression with monthly or quarterly depot. In 54 children (49 girls), doses of 7.5 mg monthly and 11.25 or 22.5 mg every 3 months quickly halted puberty for 2 years, with no differences in growth or bone age. PubMed 21798557
Prostate cancer: slower chemical castration than with antagonists. As a comparator in a trial of 610 men, leuprorelin 7.5 mg monthly kept testosterone at castration levels in 96.4% for one year, but none reached it by day 3 (because of the initial surge). PubMed 19035858