Leuprolide
Leuprolide (GnRH agonist)
Also known as: Lupron
An FDA-approved GnRH agonist that suppresses sex hormones, used for prostate cancer, endometriosis, and precocious puberty.
Overview
Leuprolide is a long-acting GnRH agonist. Given continuously it first stimulates and then shuts down the pituitary-gonadal axis, dramatically lowering testosterone or estrogen. It is FDA-approved as Lupron for prostate cancer, endometriosis, uterine fibroids, and central precocious puberty. It illustrates the paradox that continuous GnRH stimulation suppresses hormones, the opposite of pulsatile gonadorelin.
Mechanism of action
Continuous GnRH receptor stimulation desensitizes the pituitary, sharply reducing LH, FSH, and downstream sex hormones.
Key studies & citations
- Human1984
Leuprolide versus diethylstilbestrol for metastatic prostate cancer
199 patients: leuprolide suppressed testosterone comparably to DES with far fewer gynecomastia, nausea, edema and thromboembolic events.
New England Journal of Medicine - Human1990
Lupron depot (leuprolide acetate for depot suspension) in the treatment of endometriosis: a randomized, placebo-controlled, double-blind study
Monthly 3.75 mg depot significantly improved dysmenorrhea, pelvic pain and tenderness versus placebo.
Fertility and Sterility
Frequently asked questions
How can leuprolide both stimulate and suppress hormones?
A brief initial flare is followed by desensitization: continuous GnRH signaling shuts the axis down, unlike the pulsatile signaling that sustains it.