Degarelix (degarelix for injection)
Company: Ferring
Approval Status: Approved December of 2008
Treatment for: Prostate Cancer
Areas: Nephrology/Urology; Oncology
| General Information | Clinical Results | Side Effects | Mechanism of Action | Literature References | Additional Information |
General Information
Degarelix is a Gonadotropin-releasing hormone (GnRH) receptor antagonist. It binds reversibly to the pituitary GnRH receptors, thereby reducing the release of gonadotropins and consequently testosterone.
Degarelix is specifically indicated for the treatment of advanced prostate cancer.
Degarelix is supplied as a powder to be reconstituted with sterile water for subcutaneous administration in the abdomen. The recommended initial dose of the drug is 240 mg given as two subcutaneous injections of 120 mg at a concentration of 40 mg/mL. The recommended maintenance dose of Degarelix is 80 mg given as one subcutaneous injection at a concentration of 20 mg/mL, every 28 days.
Clinical Results
FDA ApprovalFDA approval of Degarelix was based on the results of a clinical trial. This open-label, multi-center, randomized, parallel-group study enrolled 620 subjects with prostate cancer. The subjects received one of two Degarelix dosing regimens or leuprolide for one year: Group A) Degarelix at a starting dose of 240 mg (40 mg/mL) followed by monthly doses of 160 mg (40 mg/mL) subcutaneously; Group B) Degarelix at a starting dose of 240 mg (40 mg/mL) followed by monthly doses of 80 mg (20 mg/mL) subcutaneously; or Group C) leuprolide 7.5 mg intramuscularly monthly. The primary objective was to demonstrate that Degarelix is effective with respect to achieving and maintaining testosterone suppression to castration levels (T < 50 ng/dL), during 12 months treatment. In Group A (240/160 mg) there were 199 responders and the castration rate was 98.3%; in Group B (240/80 mg) there were 202 responders and the castration rate was 97.2%; and in Group C (leuprolide 7.5 mg) there were 194 responders and the castration rate was 96.4%.
Ongoing Study Commitments
- Ferring has agreed to complete the ongoing extension study FE200486 CS21A entitled “An Open-Label, Multi-Center, Extension Study, Evaluating the Long-Term Safety and Tolerability of Degarelix One Month Dosing Regimen in Patients with Prostate Cancer Requiring Androgen Ablation Therapy".
Protocol Submission: January 2007
Trial Start Date: March 2007
First Annual Report Submission: March 2009
Second Annual Report Submission: March 2010
Third Annual Report Submission: March 2011
Final Report and Dataset Submission: June 2012
Side Effects
Adverse events associated with the use of Degarelix may include, but are not limited to, the following:- hot flashes
- injection site reactions
- weight gain
- increase in liver enzymes
- tiredness
- hypertension
- back and joint pain
- chills
- urinary tract infection
- decreased sex drive and trouble with erectile function
Mechanism of Action
Degarelix is a Gonadotropin-releasing hormone (GnRH) receptor antagonist. It binds reversibly to the pituitary GnRH receptors, thereby reducing the release of gonadotropins and consequently testosterone.
Literature References
Klotz L, Boccon-Gibod L, Shore ND, Andreou C, Persson BE, Cantor P, Jensen JK, Olesen TK, Schröder FH 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 Dec;102(11):1531-8
Gittelman M, Pommerville PJ, Persson BE, Jensen JK, Olesen TK; Degarelix Study Group A 1-year, open label, randomized phase II dose finding study of degarelix for the treatment of prostate cancer in North America. The Journal of Urology 2008 Nov;180(5):1986-92
Van Poppel H, Tombal B, de la Rosette JJ, Persson BE, Jensen JK, Kold Olesen T 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. European Urology 2008 Oct;54(4):805-13
Princivalle M, Broqua P, White R, Meyer J, Mayer G, Elliott L, Bjarnason K, Haigh R, Yea C Rapid suppression of plasma testosterone levels and tumor growth in the dunning rat model treated with degarelix, a new gonadotropin-releasing hormone antagonist. The Journal of Pharmacology and Experimental Therapeutics 2007 Mar;320(3):1113-8
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. The Journal of Pharmacology and Experimental Therapeutics 2002 Apr;301(1):95-102
Additional Information
For additional information regarding Degarelix or prostate cancer, please visit the Degarelix web page.The FDA drug information shown here is licensed from Thomson CenterWatch. The information provided here is for general educational purposes only and does not constitute medical or pharmaceutical advice which should be sought from qualified medical and pharmaceutical advisers.
