Degarelix
Also known as: Firmagon
Degarelix competitively and reversibly blocks pituitary GnRH receptors, immediately reducing LH and FSH release and thereby suppressing testosterone without the initial flare seen with GnRH agonists.
- Drug class
- GnRH receptor antagonist (synthetic decapeptide)
- Primary targets
- Pituitary GnRH receptor, Luteinizing hormone (LH), Follicle-stimulating hormone (FSH), Testosterone
- Dose reference
- Label reference (not a recommendation): 240 mg subcutaneous starting dose (two 120 mg injections), then 80 mg subcutaneous maintenance every 28 days
- Half-life
- ~43 days terminal half-life after the 240 mg starting depot; ~28-29 days for the 80 mg maintenance dose (depot-driven)
- Developer / origin
- Ferring Pharmaceuticals
- Reference year
- 2008
- Evidence score
- 5/5 - Approved, strong clinical evidence
Approved uses
- Treatment of patients with advanced prostate cancer
Approved, strong clinical evidence
Degarelix is FDA-approved (2008) for advanced prostate cancer, supported by the randomized phase 3 CS21 trial (610 patients) showing castrate testosterone suppression (<50 ng/dL) in over 96% of patients from day 28-364 with no initial testosterone surge, plus a detailed FDA label.
Approved medication with substantial human clinical evidence.
Evidence basis
- FDA prescribing information / DailyMed label for FIRMAGON
- Phase 3 randomized trial CS21 (Klotz et al., BJU Int 2008, n=610)
- Phase 3 leuprolide-to-degarelix crossover extension (J Urol 2011)
- Documented pharmacokinetics and post-marketing safety data
Key references
How to read this entry
Dose references and half-life values are pulled from trial protocols, labels, reviews, or published summaries where available. They are context for research and comparison, not a personal dosing recommendation.
Status matters: approved drugs have regulated indications; investigational compounds are still being studied; research-only peptides do not have established human dosing, safety, or efficacy for consumer use.
Degarelix guides
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Compare with related peptides
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Triptorelin
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Triptorelin is a potent GnRH-receptor agonist that first transiently stimulates LH and FSH release, then, with continuous exposure, downregulates and desensitizes pituitary GnRH receptors to suppress gonadotropins and sex steroids.
Goserelin
Zoladex
Goserelin is a synthetic decapeptide GnRH agonist that first stimulates and then, with continuous depot exposure, downregulates pituitary GnRH receptors to suppress LH, FSH and downstream sex steroids toward castrate or postmenopausal levels.
Buserelin
Suprefact
Buserelin is a GnRH receptor superagonist that initially stimulates and then, with continuous non-pulsatile exposure, desensitizes pituitary gonadotrophs to suppress LH, FSH and downstream testosterone or estradiol production.
Nafarelin
Synarel
Nafarelin is a potent GnRH receptor agonist that initially stimulates pituitary LH and FSH release but with continued dosing downregulates the receptor, suppressing gonadotropins and sex steroid production.