Leuprolide — Drug Monograph

Brand names: Lupron Depot, Eligard, Camcevi

Drug class: Hormonal Agent

Mechanism of Action

Leuprolide is a synthetic gonadotropin-releasing hormone (GnRH) agonist. Initially, it causes a "flare" or transient increase in the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a surge in testosterone (males) or estrogen (females). With continuous administration, it causes downregulation and desensitization of GnRH receptors in the anterior pituitary. This results in profound suppression of LH and FSH, ultimately reducing sex hormone levels to castrate levels.

FDA Indications

• Palliative treatment of advanced prostatic cancer
• Endometriosis
• Uterine leiomyomata (fibroids) — in combination with iron for anemia
• Central precocious puberty

Common Side Effects

• Hot flashes
• Injection site reactions
• Fatigue
• Decreased libido
• Erectile dysfunction
• Gynecomastia
• Bone pain (initial)
• Sweating
• Weight gain

Clinical Pearl

The "tumor flare" is a critical clinical consideration: in patients with vertebral metastases, the initial testosterone surge can cause spinal cord compression if not mitigated with an antiandrogen. Long-term therapy requires bone health management (calcium, vitamin D, DEXA scans, or bisphosphonates). Eligard is unique because it is mixed in a delivery system that forms a solid implant in the SC space. For breast cancer, leuprolide is used off-label for ovarian function suppression in…

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