Adult Dosing

Advanced Prostate cancer

• Starting dose: 240 mg SC given as 2 x 120 mg injections at a concentration of 40 mg/mL
• Maintenance dose: 80 mg SC at a concentration of 20 mg/mL q28 days

Reconstitution:

• Starting dose: Inject 3 mL water for injection into 120 mg vial. Keeping the vial in upright position, swirl it gently till the liquid becomes clear. If the powder has not dissolved completely, tilt the vial slightly. Avoid shaking as foam may form. Tilt the vial slightly and keep the needle in the lowest part of the vial. Withdraw 3 mL of 120 mg degarelix without turning the vial upside down. Exchange the reconstitution needle with the administration needle and inject 3 mL of 120 mg degarelix SC at an angle of not less than 45 degrees, immediately after reconstitution. Repeat this procedure for the second injection and inject 3 mL at a different injection site
• Maintenance doses: Inject 4.2 mL water for injection into 80 mg vial. Keeping the vial in upright position, swirl it gently till the liquid becomes clear. If the powder has not dissolved completely, tilt the vial slightly. Avoid shaking as foam may form. Tilt the vial slightly and keep the needle in the lowest part of the vial. Withdraw 3 mL of 120 mg degarelix without turning the vial upside down. Exchange the reconstitution needle with the administration needle and inject 4.2 mL of 80 mg degarelix SC, at an angle of not less than 45 degrees, immediately after reconstitution.

Note:

• Administer the dose subcutaneously and do not administer intravenously

Pediatric Dosing

• Safety and effectiveness in pediatric patients have not been established

[Outline]

• Adult Dosing
• Pediatric Dosing

• Treatment of advanced prostate cancer

• Hypersensitivity to degarelix or any of the ingredients of the product
• Pregnancy

• N/A

Renal Dose Adjustment (Based on CrCl)

• Mild impairment (CrCl 50-80 mL/min): No dose adjustments
• Moderate to severe impairment (CrCl < 50 mL/min): Caution advised, dose adjustments not defined

Hepatic Dose Adjustment

• Mild to moderate impairment (Child Pughs A/B): No dose adjustments
• Severe impairment (Child Pugh C): Caution advised, dose adjustments not defined
• Monitor testosterone levels monthly until medical castration is achieved; then monitor levels every other month

• Women who are or may become pregnant should not be treated with degarelix
• Long-term androgen deprivation therapy prolongs the QT interval; carefully weigh benefits vs potential risks in patients with congenital long QT syndrome, electrolyte abnormalities, CHF, Concurrent Class IA (eg, quinidine, procainamide) or Class III (eg, amiodarone, sotalol) antiarrhythmic medications
• Degarelix suppresses pituitary gonadal system; diagnostic tests of the pituitary gonadotropic and gonadal functions may be affected
• Measure serum prostate-specific antigen (PSA) periodically, measure testosterone serum concentrations if PSA increases
• Monitor LFT, ECG, electrolytes at baseline; testosterone if hepatic impairment q4wk until medical castration achieved, then q8 wks
• Hypersensitivity reactions such as anaphylaxis, urticaria, and angioedema have been reported during postmarketing studies. If a serious hypersensitivity reaction occurs, discontinue therapy immediately if the injection has not been completed, and manage as clinically indicated

Cautions: Use cautiously in

• Renal impairment, severe
• Hepatic impairment, severe
• Congenital long QT syndrome
• Electrolyte abnormalities
• Hypokalemia
• CHF
• Coadministration of Class IA or Class III antiarrhythmic medications

Pregnancy Category:X

Breastfeeding: Degarelix is not indicated for use in women. It is not considered compatible with breastfeeding due to the potential for serious adverse events in nursing infants

• GU: Urinary tract infection, erectile dysfunction, gynecomastia, testicular atrophy
• CNS: Fatigue, asthenia, dizziness, headache, insomnia
• CV: Hot flashes, hypertension, torsades de pointes
• GI: Diarrhea, constipation, nausea
• LABTESTS: Increased gamma-glutamyl transpeptidase, increased transaminase
• LOCAL: Pain, erythema,swelling, induration
• METABOLIC: Increased weight
• MUSC: Back pain, arthralgia
• MISC: Chills, fever, night sweats, hyperhidrosis, decreased bone density, anti-degarelix antibodies

• GnRH receptor antagonist; Binds to the pituitary GnRH receptors; reduces gonadotropin (LH and FSH) release and reducing testicular steroidogenesis (GnRH antagonist action)
• Primarily metabolized in liver; CYP450: None
• Renally excreted: 20-30% (unchanged); feces: 70-80%
• Half-Life: 53 days

US Trade Name(s)

• Firmagon

US Availability

Firmagon

• PWDR for INJ: 80 mg/vial
• PWDR for INJ: 120 mg/vial

Canadian Trade Name(s)

• Firmagon

Canadian Availability

Firmagon

• PWDR for INJ: 80 mg/vial
• PWDR for INJ: 120 mg/vial

UK Trade Name(s)

• Firmagon

UK Availability

Firmagon

• PWDR for INJ: 80 mg/vial
• PWDR for INJ: 120 mg/vial

Australian Trade Name(s)

• Firmagon

Australian Availability

Firmagon

• PWDR for INJ: 80 mg/vial
• PWDR for INJ: 120 mg/vial

[Outline]

Hematology/Oncology

Antineoplastics

Gonadotropin-Releasing Hormone Antagonist