Function of leuprolide acetate in disorders of the reproductive system



Leuprolide acetate, an acetate salt with similar structure to luteinizing hormone-releasing hormone (LHRH) secreted by the hypothalamus, is a synthetic agonist analog of gonadotropin-releasing hormone (GnRH). Leuprolide acetate has good biological activity owing to less susceptibility to proteolysis and greater binding affinity to GnRH receptors than the natural hormone. As a result, leuprolide acetate has been considered to be a very safe and tolerable drug and can be used for a variety of clinical applications especially disorders of the reproductive system such as central precocious puberty, prostate cancer and so on.

Pharmacologic action

Leuprolide acetate is widely used in a variety of disorders of the reproductive system. Take prostate cancer as an example, the pharmacologic effect of leuprolide acetate as follows. Dihydrotestosterone promotes the growth of prostate cancer cells. In history, men have been treated for prostate cancer by interrupting the production of testosterone, which is the main source of dihydrotestosterone, with testosterone or estrogen therapy. Leuprolide acetate works by completely blocking the secretion of gonadotropin, thereby stopping the secretion of testosterone. In fact, testosterone has dropped to the level of orchiectomy with the therapy of leuprolide acetate. Leuprolide acetate, taking the place of testosterone and estrogen therapy, is an effective drug for the treatment of prostate cancer and can effectively improve the quality of life of patients.


Leuprolide acetate is one of the most popular GnRH agonists due to its efficacy and diversity of clinical applications. Leuprolide acetate has been proved to be effective in disorders of the reproductive system such as prostate cancer, breast cancer, endometriosis, uterine myoma and central precocious puberty. The basic mechanism of action is that leuprolide acetate suppresses the secretion of gonadotrope. In addition to the above applications, leuprolide acetate is also the potential choice for the treatment of polycystic ovary syndrome, Alzheimer's disease , functional bowel disease, premenstrual syndrome, short stature and even as an alternative for contraception.

Pharmacokinetics and metabolism

Leuprolide acetate, when injected into body, is available in many different dose and administration forms, which is associated with the specific disease. In fact, bioavailability of leuprolide acetate is similar with intravenous or subcutaneous routes of administration. There is less than 5% of the dose which can be recoverable after administration of the 3.75 mg of depot. Leuprolide acetate treatment can induce significant gain in body weight along with increases in neurofilament and myelin basic protein expression and axonal diameter in the spinal cord.


1. Galindo, C. D., Gómez-González, B., Salinas, E., Calderón-Vallejo, D., Hernández-Jasso, I., Bautista, E., & Quintanar, J. L. (2015). Leuprolide acetate induces structural and functional recovery of injured spinal cord in rats. Neural regeneration research, 10(11), 1819.

2. Guzmán-Soto, I., Salinas, E., Hernández-Jasso, I., & Quintanar, J. L. (2012). Leuprolide acetate, a GnRH agonist, improves experimental autoimmune encephalomyelitis: a possible therapy for multiple sclerosis. Neurochemical research, 37(10), 2190-2197.

3. Abouelfadel, Z., & Crawford, E. D. (2008). Leuprorelin depot injection: patient considerations in the management of prostatic cancer. Therapeutics and clinical risk management, 4(2), 513.

4. Wilson, A. C., Vadakkadath Meethal, S., Bowen, R. L., & Atwood, C. S. (2007). Leuprolide acetate: a drug of diverse clinical applications. Expert opinion on investigational drugs, 16(11), 1851-1863.

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