Degarelix — Drug Monograph
Brand names: Firmagon
Drug class: Hormonal Agent
Mechanism of Action
Degarelix is a selective gonadotropin-releasing hormone (GnRH) receptor antagonist. It binds reversibly to pituitary GnRH receptors, preventing the binding of endogenous GnRH. This results in immediate suppression of LH and FSH secretion, which leads to a rapid reduction in testosterone levels without the initial surge or "flare" seen with GnRH agonists. Castrate levels of testosterone are achieved within 3 days of administration.
FDA Indications
- Treatment of advanced prostate cancer
Common Side Effects
- Injection site reactions (pain, erythema, swelling)
- Hot flashes
- Weight gain
- Increased liver transaminases
- Fatigue
- Chills
- Decreased libido
Clinical Pearl
Degarelix is the preferred agent when rapid testosterone suppression is needed or when a "flare" must be avoided (e.g., severe bone pain or impending cord compression). Unlike leuprolide/goserelin, no antiandrogen "lead-in" is required. However, injection site reactions are nearly universal (about 40% of patients) and can be quite painful; patients should be counseled that redness and a lump at the site are normal. It must be administered every 28 days, which may be less convenient than…
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