Leuprolide

FDA approved

Leuprolide (Lupron Depot, Eligard) is a GnRH agonist first approved by the FDA in 1985. It is used to lower sex hormones in advanced prostate cancer, endometriosis, uterine fibroids and early (central precocious) puberty.

At a glance

Where it acts: Sexual & reproductive
Regulatory status: FDA approvedApproved by the U.S. FDA for at least one medical use.

Mechanism of Action

Leuprolide is a 9-amino acid analog of gonadotropin-releasing hormone. It first stimulates the pituitary, causing a brief surge in LH, FSH and sex hormones, but continuous exposure then desensitizes the receptors, shutting down testosterone and estrogen production.

Typical Dosage (Research)

Prescription-only medicine. Dosing is set by a physician according to the FDA-approved label and the condition being treated.

Side Effects & Risks

Hot flashes, decreased libido, fatigue, injection site reactions, and initial worsening of symptoms during the hormone flare.

Bone density loss with long-term use, cardiovascular and metabolic effects of low testosterone, mood changes, and tumor flare at the start of therapy.

Who Uses Leuprolide

Men with advanced prostate cancer; women with endometriosis or fibroids; children with central precocious puberty.