Degarelix acetate

Degarelix Acetate is the acetate form of a long-acting, synthetic peptide with gonadotrophin-releasing hormone (GnRH) antagonistic properties. Degarelix targets and blocks GnRH receptors located on the surfaces of gonadotroph cells in the anterior pituitary, thereby reducing secretion of luteinizing hormone (LH) by pituitary gonadotroph cells and so decreasing testosterone production by interstitial (Leydig) cells in the testes.

Name Degarelix acetate	Molecular structural formula
Purity 95%
CAS Number 934016-19-0
Formula C84H107ClN18O18
MW 1692.3
Target GnRH report
Sequence Ac-D-2Nal-D-Phe(4-Cl)-D-3Pal-Ser-Phe(4-S-dihydroorotamido)-D-Phe(4-ureido)-Leu-Lys(iPr)-Pro-D-Ala-NH2
Sequence Shortening XXXSXXLXPA-NH2
InChIKey AUTFSFUMNFDPLH-KYMMNHPFSA-N
References [1] Klotz L, Boccon-Gibod L N, Andreou C, et al. The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer. Bju International, 2008, 102(11):1531-1538 [2] Sciarra A, Fasulo A, Ciardi A, et al. A meta-analysis and systematic review of randomized controlled trials with degarelix versus gonadotropin-releasing hormone agonists for advanced prostate cancer. Medicine, 2016, 95(27): e3845. [3] Tokiwa S, Shimmura H, Nomura S, et al. Degarelix treatment is compatible with diabetes and antithrombotic therapy in patients with prostate cancer. Research & Reports in Urology, 2017, 9:225. [4] Kimura T, Sasaki H, Akazawa K, et al. Gonadotropin-releasing hormone antagonist: A real advantage? Urologic Oncology Seminars & Original Investigations, 2015, 33(7):322-328. [5] Xie L, Li J, Wang X. Updates in prostate cancer detections and treatments – Messages from 2017 EAU and AUA. Asian Journal of Urology, 2017, 5(1):3-7. [6] Alireza H S, Fatemeh R, Ali A S, et al. Degarelix for the treatment of advanced prostate cancer compared with GnRh-Agonists: a systematic review and meta-analysis. Medical Journal of the Islamic Republic of Iran, 2016, 30(1):317-317. [7] Albertsen P C, Klotz L, Tombal B, et al. Cardiovascular Morbidity Associated with Gonadotropin Releasing Hormone Agonists and an Antagonist. European Urology, 2014, 65(3):565-573. [8] Klotz L1, Miller K2, Crawford ED, et al, Disease control outcomes from analysis of pooled individual patient data from five comparative randomised clinical trials of degarelix versus luteinising hormone-releasing hormone agonists，Eur Urol. 2014 Dec;66(6):1101-8. [9] Gittelman M, Pommerville P J, Persson B E, et al. A 1-year, open label, randomized phase II dose finding study of degarelix for the treatment of prostate cancer in North America. Journal of Urology, 2008, 180(5):1986-1992.