Leuprorelin, also known as leuprolide, is a manufactured version of a hormone used to treat prostate cancer, breast cancer, endometriosis, uterine fibroids, and early puberty, to perform chemical castration of violent sex offenders, or as part of transgender hormone therapy. It is given by injection into a muscle or under the skin.Leuprorelin is in the gonadotropin-releasing hormone (GnRH) analogue family of medications. It works by decreasing gonadotropin and therefore decreasing testosterone and estradiol. Common side effects include hot flashes, unstable mood, trouble sleeping, headaches, and pain at the site of injection. Other side effects may include high blood sugar, allergic reactions, and problems with the pituitary gland. Use during pregnancy may harm the baby.Leuprorelin was patented in 1973 and approved for medical use in the United States in 1985. It is on the World Health Organizations List of Essential Medicines. It is sold under the brand name Lupron among others. Medical use
Leuprorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer and breast cancer. It may also be used for estrogen-dependent conditions such as endometriosis or uterine fibroids. It may be used for precocious puberty in both males and females, and to prevent premature ovulation in cycles of controlled ovarian stimulation for in vitro fertilization (IVF).
This use is controversial since the Lupron label advises against using the drug when one is considering pregnancy, due to a risk of birth defects.It may be used to reduce the risk of premature ovarian failure in women receiving cyclophosphamide for chemotherapy.Along with triptorelin and goserelin, it has been used to delay puberty in transgender youth until they are old enough to begin hormone replacement therapy. Researchers have recommended puberty blockers after age 12, when the person has developed to Tanner stages 2–3, and then cross-sex hormones treatment at age 16. This use of the drug is off-label, however, not having been approved by the Food and Drug Administration and without data on long-term effects of this use.They are also sometimes used as alternatives to antiandrogens like spironolactone and cyproterone acetate for suppressing testosterone production in transgender women. It also is used for suppressing estrogen production in transgender men.It is considered a possible treatment for paraphilias. Leuprorelin has been tested as a treatment for reducing sexual urges in pedophiles and other cases of paraphilia.