Degarelix
Also known as: Firmagon, FE 200486
A GnRH antagonist injection for advanced prostate cancer that lowers testosterone within days without a flare. FDA-approved as Firmagon (2008).
Last updated
Mechanism of Action
Degarelix is a synthetic decapeptide that binds and blocks GnRH receptors in the pituitary. Because it is an antagonist rather than an agonist, it suppresses LH and FSH immediately, without the initial testosterone surge seen with leuprolide or goserelin; most men reach castrate testosterone levels within 3 days. After subcutaneous injection it forms a gel depot that releases drug slowly, allowing monthly maintenance dosing.
- Half-life
- ~53 days (maintenance dose, depot release)
- Administration Routes
- Subcutaneous
- Research Status
- Clinical
Reported Benefits
- Treatment of advanced prostate cancer (androgen deprivation)
- Rapid testosterone suppression without a tumor flare
- Faster PSA reduction than leuprolide in the pivotal trial
Potential Side Effects
- Injection-site reactions (pain, redness, swelling), very common
- Hot flashes, weight gain and fatigue
- Increased liver transaminases
- QT prolongation with androgen deprivation therapy
- Loss of bone density with long-term use
Common Dosing
The labeled regimen is a starting dose given as two subcutaneous abdominal injections, followed by a monthly maintenance injection beginning 28 days later. Injections are given by a healthcare provider. Dosing is set and supervised by the prescribing clinician.
The dosing information above is aggregated from research literature and anecdotal community reports for educational purposes only. It is not a recommendation, prescription, or medical advice. Peptides are sold as research chemicals only and are not intended for human use.
Contraindications
- Known hypersensitivity to degarelix or any component
- Not indicated for women; can cause fetal harm
No documented stacking partners for Degarelix yet.
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The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer
2008
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Cardiovascular Safety of Degarelix Versus Leuprolide in Patients With Prostate Cancer: The Primary Results of the PRONOUNCE Randomized Trial
2021
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Degarelix for treating advanced hormone-sensitive prostate cancer
2021