Degarelix: A novel gonadotropin-releasing hormone blocker for the treatment of prostate cancer

Future Oncology

Volumn 5, Issue 4, 2009, Pages 433-443

  Anderson, John ^a  

^a ROYAL HALLAMSHIRE HOSPITAL   (United Kingdom)

Author keywords

Adenocarcinoma of the prostate; Degarelix; GnRH antagonist; GnRH blocker; Gonadotropin releasing hormone; Prostate cancer; Prostate specific antigen; PSA; Testosterone

Indexed keywords

ABARELIX; BICALUTAMIDE; DEGARELIX; GONADORELIN AGONIST; GONADORELIN ANTAGONIST; GONADORELIN RECEPTOR; LEUPRORELIN; PROSTATE SPECIFIC ANTIGEN; TESTOSTERONE; ACETYL 2 NAPHTHYLALANYL 3 CHLOROPHENYLALANYL 1 OXOHEXADECYL SERYL 4 AMINOPHENYLALANYL(HYDROOROTYL) 4 AMINOPHENYLALANYL(CARBAMOYL) LEUCYL ILYS PROLYL ALANINAMIDE; ACETYL-2-NAPHTHYLALANYL-3-CHLOROPHENYLALANYL-1-OXOHEXADECYL-SERYL-4-AMINOPHENYLALANYL(HYDROOROTYL)-4-AMINOPHENYLALANYL(CARBAMOYL)-LEUCYL-ILYS-PROLYL-ALANINAMIDE; ANTINEOPLASTIC AGENT; GONADORELIN; OLIGOPEPTIDE;

ADVANCED CANCER; ANDROGEN DEPRIVATION THERAPY; ARTHRALGIA; ARTICLE; BACKACHE; BREAST CANCER; CHILL; CLINICAL TRIAL; CONSTIPATION; DEPRESSION; DISEASE SEVERITY; DRUG APPROVAL; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG HALF LIFE; DRUG HYPERSENSITIVITY; DRUG MECHANISM; DRUG RELEASE; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; DRUG WITHDRAWAL; FATIGUE; HOT FLUSH; HUMAN; HYPERCHOLESTEROLEMIA; HYPERTENSION; INJECTION SITE REACTION; MALE; MULTIPLE CYCLE TREATMENT; PHARMACODYNAMICS; PRIORITY JOURNAL; PROSTATE ADENOCARCINOMA; PROSTATE CANCER; RECEPTOR BLOCKING; SIDE EFFECT; TESTOSTERONE BLOOD LEVEL; URINARY TRACT INFECTION; URTICARIA; WEIGHT GAIN; DRUG ANTAGONISM; PROSTATE TUMOR; REVIEW;

ANTINEOPLASTIC AGENTS; CLINICAL TRIALS AS TOPIC; GONADOTROPIN-RELEASING HORMONE; HUMANS; MALE; OLIGOPEPTIDES; PROSTATIC NEOPLASMS;

EID: 67651238917     PISSN: 14796694     EISSN: 17448301     Source Type: Journal    
DOI: 10.2217/fon.09.24     Document Type: Article

References (33)

1. Ferlay J, Autier P, Boniol M, Heanue M, Colombet M, Boyle P: Estimates of the cancer incidence and mortality in Europe in 2006. Ann. Oncol. 18(3), 581-592 (2007).
2. Etzioni R, Penson DF, Legler JM et al.: Overdiagnosis due to prostate-specific antigen screening: lessons from U.S. prostate cancer incidence trends. J. Natl Cancer Inst. 94(13), 981-990 (2002).
3. Siesling S, van Dijck JA, Visser O, Coebergh JW: Trends in incidence of and mortality from cancer in The Netherlands in the period 1989-1998. Eur. J. Cancer. 39(17), 2521-2530 (2003).
4. Jemal A, Siegel R, Ward E et al.: Cancer statistics. 2008. CA Cancer J. Clin. 58(2), 71-96 (2008).
5. Iversen P: Orchidectomy and oestrogen therapy revisited. Eur. Urol. 34(Suppl. 3), 7-11 (1998).
6. Labrie F, Belanger A, Luu-The V et al.: Gonadotropin-releasing hormone agonists in the treatment of prostate cancer. Endocr. Rev. 26(3), 361-379 (2005).
7. Huirne JA, Lambalk CB: Gonadotropin-releasing-hormone-receptor antagonists. Lancet 358(9295), 1793-1803 (2001).
8. Sasagawa I, Kubota Y, Nakada T et al.: Influence of luteinizing hormone-releasing hormone analogues on serum levels of prostatic acid phosphatase and prostatic specific antigen in patients with metastatic carcinoma of the prostate. Int. Urol. Nephrol. 30(6), 745-753 (1998).
9. Tomera K, Gleason D, Gittelman M et al.: The gonadotropin-releasing hormone antagonist abarelix depot versus luteinizing hormone releasing hormone agonists leuprolide or goserelin: initial results of endocrinological and biochemical efficacies in patients with prostate cancer. J. Urol. 165(5), 1585-1589 (2001).
10. Thompson IM, Zeidman EJ, Rodriguez FR: Sudden death due to disease flare with luteinizing hormone-releasing hormone agonist therapy for carcinoma of the prostate. J. Urol. 144(6), 1479-1480 (1990).
11. Heidenreich H, Aus G, Bolla M et al.; on behalf of the European Association of Urology: EAU guidelines on prostate cancer. Eur. Urol. 53(1), 68-80 (2008).
12. Jockenhovel F, Bhasin S, Steiner BS, Rivier JE, Vale WW, Swerdloff RS: Hormonal effects of single gonadotropin-releasing hormone antagonist doses in men. J. Clin. Endocrinol. Metab. 66(5), 1065-1070 (1988).
13. Salameh W, Bhasin S, Steiner B, McAdams LA, Peterson M, Swerdloff R: Marked suppression of gonadotropins and testosterone by an antagonist analog of gonadotropin-releasing hormone in men. Fertil. Steril. 55(1), 156-164 (1991).
14. Bagatell CJ, Conn PM, Bremner WJ: Single-dose administration of the gonadotropin-releasing hormone antagonist, Nal-Lys (antide) to healthy men. Fertil. Steril. 60(4), 680-685 (1993).
15. Bagatell CJ, Rivier JE, Bremner WJ: Dose effects of the gonadotropin-releasing hormone antagonist, Nal-Glu, combined with testosterone enanthate on gonadotropin levels in normal men. Fertil. Steril. 64(1), 139-145 (1995).
16. Klingmuller D, Schepke M, Enzweiler C, Bidlingmaier F: Hormonal responses to the new potent GnRH antagonist cetrorelix. Acta Endocrinol. 128(1), 15-18 (1993).
17. Broqua P, Riviere PJ, Conn PM, Rivier JE, Aubert ML, Junien JL: Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormone antagonist: degarelix. J. Pharmacol. Exp. Ther. 301(1), 95-102 (2002).
18. Van Poppel H, Nilsson S: Testosterone surge: rationale for gonadotropin-releasing hormone blockers? Urology 71(6), 1001-1006 (2008).
19. Hutchison J, Liao S, Smith J, Phillips A: Clinical pharmacology of azaline B. Gynecol. Endocrinol. 13(Suppl. 1), 9 (1999).
20. Weckermann D, Harzmann R: Hormone therapy in prostate cancer: LHRH antagonists versus LHRH analogues. Eur. Urol. 46(3), 279-283 (2004).
21. Princivalle M, Broqua P, White R et al.: Rapid suppression of plasma testosterone levels and tumor growth in the dunning rat model treated with degarelix, a new gonadotropin-releasing hormone antagonist. J. Pharmacol. Exp. Ther. 320(3), 1113-1118 (2007).
22. Doehn C, Sommerauer M, Jocham D: Drug evaluation: degarelix - a potential new therapy for prostate cancer. IDrugs 9(8), 565-572 (2006).
23. Balchen T, Agerso H, Olesen TK, Jensen J-K, Senderovitz T: Pharmacokinetics, pharmacodybnamics, and safety of a novel fast-acting gonadotropin-releasing hormone receptor blocker, degarelix, in healthy men. Presented at: 8th International Symposium on GnRH Analogues in Cancer and Human Reproduction. Salzburg, Austria, 10-13 February 2005.
24. Jiang G, Stalewski J, Galyean R et al.: GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6. J. Med. Chem. 44(3), 453-467 (2001).
25. Schwach G, Oudry N, Giliberto JP et al.: Biodegradable PLGA microparticles for sustained release of a new GnRH antagonist: part II. In vivo performance. Eur. J. Pharm. Biopharm. 57(3), 441-446 (2004).
26. Schwach G, Oudry N, Delhomme S, Luck M, Lindner H, Gurny R: Biodegradable microparticles for sustained release of a new GnRH antagonist - part I: screening commercial PLGA and formulation technologies. Eur. J. Pharm. Biopharm. 56(3), 327-336 (2003).
27. Koechling W: Effect of various GnRH antagonists on histamine release from human skin. Presented at: 8th International Symposium on GnRH Analogues in Cancer and Human Reproduction. Salzburg, Austria, 10-13 February 2005.
28. Van Poppel H, Tombal B, de la Rosette JJ, Persson BE, Jensen JK, Kold OT: Degarelix: a novel gonadotropin-releasing hormone (GnRH) receptor blocker - results from a 1-yr, multicentre, randomised, Phase 2 dosage-finding study in the treatment of prostate cancer. Eur. Urol. 54(4), 805-813 (2008).
29. Gittelman M, Pommerville PJ, Persson BE, Jensen JK, Olesen TK: A 1-year, open label, randomized Phase II dose finding study of degarelix for the treatment of prostate cancer in North America. J. Urol. 180(5), 1986-1992 (2008).
30. Klotz L, Boccon-Gibod L, Shore ND 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 Int. 102(11), 1531-1538 (2008).
31. Ako D, Shiba M, Arai Y et al.: Skin reactions to 3-month depot type of luteinizing hormone-releasing hormone agonist therapy. JMAJ 49, 48-54 (2006).
32. Eligard (7.5 mg). US product label. Sanofi-Aventis Inc., NJ, USA (November 2007).
33. Conti PD, Atallah AN, Arruda H, Soares BG, El Dib RP, Wilt TJ: Intermittent versus continuous androgen suppression for prostatic cancer. Cochrane Database Syst. Rev. 4, CD005009 (2007).