Degarelix
Also known as: Camcevi, Degarelix acetate, FE200486, Firmagon, IUPHAR:1173
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Summary
Degarelix is a synthetic decapeptide GnRH antagonist administered subcutaneously to achieve rapid testosterone suppression in men with advanced prostate cancer.
Mechanism of Action
Competitive antagonist of the gonadotropin-releasing hormone (GnRH) receptor, suppressing LH and FSH release and lowering testosterone production.
Routes of Administration
Goals & Uses
- Cardiovascular risk reduction vs GnRH agonistsCardiologyModerate
- Prevention of testosterone flareOncology / Hormonal SafetyHigh
- Prostate cancer treatmentOncologyHigh
- Advanced prostate cancer treatmentOncologyHigh
- Neoadjuvant/adjuvant to radiotherapyOncologyModerate
- Rapid testosterone castrationEndocrineHigh
- Androgen deprivation therapy (ADT)EndocrinologyHigh
Contraindications
- Severe hepatic impairmentOrganModerateLiver function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Women and pediatric patientsPopulationHigh
- Hypersensitivity to degarelix or excipientsAllergyHigh
Adverse Effects
- Elevated liver enzymes (AST/ALT)HepatotoxicityUncommon
- Injection site reactionsLocalCommon
- Decreased bone mineral densityMusculoskeletalCommon
- Hot flashesEndocrine / VasomotorCommon
- QT/QTc prolongationCardiovascularUncommon
- Weight gainMetabolicCommonIncrease in body weight
- Cardiovascular eventsSystemicRare
- Elevated liver enzymesHepaticUncommonIncrease in AST/ALT or other hepatic markers
- Injection site reactions (pain, erythema, swelling)LocalCommon
Drug Interactions
- Hormonal therapies (e.g., antiandrogens)Moderate
- Class III antiarrhythmics (amiodarone, sotalol)High
- CYP450 substratesLow
- QT-prolonging agents (e.g., antiarrhythmics, antipsychotics)High
- Class IA antiarrhythmics (quinidine, procainamide)High
Population Constraints
- Patients with congenital long QT syndromeCardiovascularRelative
- Pediatric patientsAgeAbsolute
- Patients with severe hepatic impairmentHepaticRelative
- Elderly patients (≥65 years)Age RelatedRelative
- Patients with severe renal impairmentOrgan ImpairmentRelative
- Patients with severe cardiovascular diseaseCardiovascularRelative
Regulatory Status
- European UnionApprovedApproved: Hormone-sensitive prostate cancerMarketing authorization granted.
- United StatesApprovedApproved: Advanced prostate cancerBrand: Firmagon.
- United KingdomApprovedApproved: Prostate cancerAvailable via NHS.
Approved in the US, EU, and UK for treatment of hormone-sensitive prostate cancer; marketed under the brand name Firmagon.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Degarelix?
Degarelix is a synthetic decapeptide GnRH antagonist administered subcutaneously to achieve rapid testosterone suppression in men with advanced prostate cancer.
What is Degarelix used for?
Degarelix is educationally associated with: Cardiovascular risk reduction vs GnRH agonists, Prevention of testosterone flare, Prostate cancer treatment, Advanced prostate cancer treatment, Neoadjuvant/adjuvant to radiotherapy, Rapid testosterone castration, Androgen deprivation therapy (ADT). Educational only — not medical advice.
How is Degarelix administered?
Recorded routes of administration: Subcutaneous.
What are the potential side effects of Degarelix?
Reported adverse effects include: Elevated liver enzymes (AST/ALT), Injection site reactions, Decreased bone mineral density, Hot flashes, QT/QTc prolongation, Weight gain, Cardiovascular events, Elevated liver enzymes, Injection site reactions (pain, erythema, swelling). This list is not exhaustive — consult a qualified clinician.
Who should avoid Degarelix?
Recorded contraindications: Severe hepatic impairment, Pregnancy, Women and pediatric patients, Hypersensitivity to degarelix or excipients. Consult a qualified clinician before use.