Drug reference

Degarelix

GnRH Analogue · Hormone therapy for prostate cancer

Also known as Degarelix acetate, Firmagon

GnRH AnalogueHormone therapy for prostate cancerATC null

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AmiodaroneSevereDatabaseDDInter
AmisulprideSevereDatabaseDDInter
AnagrelideSevereDatabaseDDInter
Arsenic TrioxideSevereDatabaseDDInter

Mechanism

Degarelix is a gonadotrophin-releasing hormone (GnRH) antagonist that suppresses testosterone. It binds to GnRH receptors in the pituitary, preventing the release of luteinizing hormone and follicle-stimulating hormone. This action rapidly reduces testicular androgen production, leading to medical castration without the initial testosterone flare seen with GnRH agonists.

Indications

Advanced hormone-dependent prostate cancerAdvanced prostate cancerTreatment of advanced and metastatic prostate cancer

Dosing

Adult: Initially 240 mg by subcutaneous injection, administered as 2 injections of 120 mg into the abdominal region, then 80 mg every 28 days by subcutaneous injection.
Renal adjustment: Manufacturer advises caution in severe impairment; no specific information available.
Hepatic adjustment: Manufacturer advises caution; monitor liver function (limited information available).

Pharmacokinetics

Onset

Cmax is achieved after 2 days.

Half-life

42 days for the starting dose and 28 days for the maintenance dose (plasma median t1/2)

Protein binding

90% protein bound

Metabolism

Degraded by proteolysis via the hepatobiliary system.

Excretion

Degraded protein fragments are eliminated in the feces, and unmetabolized drug is eliminated via the kidneys.

Contraindications

Diabetes
Susceptibility to QT-interval prolongation

Side effects

Common

AnaemiaChillsDiarrhoeaDizzinessFatigueFeverGynaecomastiaHeadacheHot flushInfluenza-like illnessInsomniaMusculoskeletal discomfortMusculoskeletal painNauseaSexual dysfunctionSkin reactionsSweat changesTesticular disordersWeight changesAlopeciaAppetite decreasedArrhythmiasBone disordersBreast painCognitive impairmentConstipationDepressionDiabetes mellitusDry mouthDyspnoeaGastrointestinal discomfortGenital discomfortHyperglycaemiaHypertensionHypotensionJoint disordersMalaiseMuscle spasmsMuscle weaknessNumbnessPalpitationsPelvic painPeripheral oedemaRenal impairmentUrinary disordersVision blurredVomitingAnxietyCoughGastrointestinal disordersHair growth abnormalHerpes zosterLibido decreasedLymphedemaOedemaPhotosensitivity reactionThirstInjection site reactionsHot flashesWeight gainIncreases in transaminase and γ-glutamyltransaminase levelsProlonged QT intervalDecreased bone mineral densityInjection site reactions (higher rates compared with GnRH agonists)

Serious