Degarelix

Degarelix is an intramuscularly injectable synthetic peptide (molecular formula: C82H103ClN18O16) from the group of GnRH antagonists. Degarelix is used for the treatment of advanced or metastasized hormone-dependent prostate carcinoma.

Degarelix acts via competitive inhibition of the GnRH receptor. This leads to a rapid but reversible interruption of testosterone production. In contrast to treatment with a gonadorelin receptor agonist (see buserelin or triptorelin below), Degarelix does not cause an initial testosterone flooding, which could possibly trigger an aggravation of the clinical picture.

Clinical studies have shown that testosterone and PSA are reduced more rapidly under Abarelix treatment, both in comparison with treatment with gonadorelin receptor agonists (e.g. goserelin, buserelin) and in comparison with maximum androgen blockade (gonadorelin receptor agonists + antiandrogen).

Effects on testosterone levels: under Degarelix therapy, testosterone levels fall to castration levels within a week.

Degarelix can cause anaphylactoid reactions. The side effects of Degarelix are otherwise those of hormone withdrawal. These include hot flushes, impotence, sleep disturbances, reduction of sexual drive, depression as well as weakness, weakness, swelling of the mammary glands and hot flushes. In addition, peripheral oedema, pain, dizziness, headaches, sensitivity disorders and gastrointestinal disturbances were frequent.

Firmagon®

Degarelix has been approved in the USA since December 2008 and in the entire European Union since February 2009.

1. Clinton TN et al (2017) Degarelix versus luteinizing hormone-releasing hormone agonists for the treatment of prostate cancer. Expert Opinion Pharmacother 18:825-832.
2. Klotz L et al (2008) 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 102:1531-1538.
3. Uttley L et al (2017) Degarelix for Treating Advanced Hormone-Dependent Prostate Cancer: An Evidence Review Group Perspective of a NICE Single Technology Appraisal. Pharmacoeconomics 35:717-726.