Leuprolide is a peptide-based GnRH receptor superagonist used for the palliative treatment of prostate cancer, uterine leiomyomata, endometriosis, and central precocious puberty. Leuprolide is a synthetic 9-residue peptide analogue of gonadotropin-releasing hormone (GnRH).
- Mechanism
- Curator reviewed · 12 references
Gonadotropin-releasing hormone (GnRH) is a naturally occurring decapeptide that modulates the hypothalamic-pituitary-gonadal (HPG) axis. GnRH binds to corresponding receptors (GnRHRs) on the anterior pituitary gonadotropes, which in turn release luteinizing hormone (LH) and follicle-stimulating hormone (FSH); these, in turn, affect the downstream synthesis and release of the sex hormones testosterone, dihydrotestosterone, estrone, and estradiol.
Despite the variety of conditions indicated for treatment with leuprolide, the mechanism of action underlying efficacy is the same in all cases. As a GnRHR agonist, leuprolide binds to and initially activates downstream LH and FSH release; this initial spike in gonadotropin levels is responsible for some of the adverse effects associated with treatment. After 2-4 weeks of treatment, continuous stimulation of GnRHR results in feedback inhibition and significant downregulation of LH, FSH, and their corresponding downstream effects, producing a therapeutic benefit. These effects are reversible upon treatment discontinuation.
- Primary indication
- Leuprolide is indicated for the treatment of advanced prostate cancer and as palliative treatment of advanced prostate cancer.Curator reviewed · 15 structured indications
- First approval
- Canada, 1999 · United States, 1986 · European Union, 2022
- Also known as
- Leuporelin · Leuprorelin
- Code names
- CKD-841
- Brand names
Resolves to
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