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Leuprolide Acetate

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Leuprorelin; (Des-Gly10,D-Leu6,Pro-NHEt9)-LHRH; Lupron; leuprolide; Enantone
Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt acetate salt
Molecular Formula
Long-term Storage Conditions
As a LH-RH (GnRH) analog, leuprolide may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat precocious puberty, and to control ovarian stimulation in In Vitro Fertilization (IVF).
Leuprolide acetate is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.
Areas of Interest
Hormonal therapy
  • Background
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Leuprolide acetate is a synthetic nonapeptide that is a potent gonadotropin-releasing hormone receptor (GnRHR) agonist used for diverse clinical applications, including the treatment of prostate cancer, endometriosis, uterine fibroids, central precocious puberty and in vitro fertilization techniques. As its basic mechanism of action, leuprolide acetate suppresses gonadotrope secretion of luteinizing hormone and follicle-stimulating hormone that subsequently suppresses gonadal sex steroid production. In addition, leuprolide acetate is presently being tested for the treatment of Alzheimer's disease, polycystic ovary syndrome, functional bowel disease, short stature, premenstrual syndrome and even as an alternative for contraception.

CAS: 50-57-7
Sequence: c[Cys-Tyr-Phe-Gln-Asn-Cys]-Pro-Lys-Gly-NH2
M.W: 1056.2
Molecular Formula: C46H65N13O12S2
CAS: 62305-91-3
Sequence: 6-Me-5-oxothiomorpholinyl-3-carbonyl-His-Pro-NH2
M.W: 408.48
Molecular Formula: C17H24N6O4S
CAS: 76932-56-4 (net)
Sequence: Pyr-His-Trp-Ser-Tyr-D-2-Nal-Leu-Arg-Pro-Gly-NH2 acetate salt
M.W: 1322.5
Molecular Formula: C10H18N2O7
CAS: 1081110-72-6
Sequence: H-Phe-Asn-Ala-Pro-Phe-Asp-Val-Gly-Ile-Lys-Leu-Ser-Gly-Val-Gln-Tyr-Gln-Gln-His-Ser-Gln-Ala-Leu-NH2
M.W: 2546.87
Molecular Formula: C116H176N32O33
CAS: 123583-37-9 (net)
Sequence: H-Ile-Lys-Pro-Glu-Ala-Pro-Gly-Glu-Asp-Ala-Ser-Pro-Glu-Glu-Leu-Asn-Arg-Tyr-Tyr-Ala-Ser-Leu-Arg-His-Tyr-Leu-Asn-Leu-Val-Thr-Arg-Gln-Arg-Tyr-NH2 acetate salt
M.W: 4049.52
Molecular Formula: C180H279N53O54

The use of leuprolide acetate depot in combination with norethindrone acetate 5 mg alone, or with norethindrone acetate and conjugated equine estrogens 0.625 mg, provides effective suppression of pelvic pain symptoms associated with endometriosis while protecting against bone loss.

Hornstein, M. D., Surrey, E. S., Weisberg, G. W., Casino, L. A., & Lupron Add-Back Study Group. (1998). Leuprolide acetate depot and hormonal add-back in endometriosis: a 12-month study. Obstetrics & Gynecology, 91(1), 145-148.

Leuprolide is an established luteinizing hormone–releasing hormone (LHRH) agonist used as first-line treatment in advanced prostate cancer. As different formulations and dosing schedules are likely to have economic implications, we aimed to evaluate their efficacy, safety, and costs in nine European countries: Austria, Belgium, Czech Republic, Hungary, Italy, Latvia, Netherlands, Poland, and Portugal.

Wex, J., Sidhu, M., Odeyemi, I., Abou-Setta, A. M., Retsa, P., & Tombal, B. (2013). Leuprolide acetate 1-, 3-and 6-monthly depot formulations in androgen deprivation therapy for prostate cancer in nine European countries: evidence review and economic evaluation. ClinicoEconomics and outcomes research: CEOR, 5, 257.

A new class of antiandrogen medications, gonadotropin-releasing hormone agonists, offers promise in the treatment of the paraphilias, with substantially less side effects than medroxyprogesterone acetate or cyproterone acetate. This paper reports the results of treatment using a depot suspension of leuprolide acetate on 12 patients with paraphilic disorders or with sexual disorders not otherwise specified to suppress or help these individuals control their deviant sexual behavior or impulses. The method involved uncontrolled observations of individuals treated with depot-leuprolide acetate for various lengths of time, from 6 months to 5 years, with the follow-up intervals ranging from 6 months to 6 years. Leuprolide acetate resulted in a significant suppression of deviant sexual interests and behavior as measured by self-report and was well tolerated. However, the three patients who were on long-term therapy developed bone demineralization, suggesting that this is a significant side effect of prolonged therapy. Leuprolide acetate shows promise as a treatment for the paraphilias.

Krueger, R. B., & Kaplan, M. S. (2001). Depot-leuprolide acetate for treatment of paraphilias: a report of twelve cases. Archives of Sexual Behavior, 30(4), 409-422.

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