Degarelix

Subcutaneous
Advanced prostate cancer

Add 4.2 or 3 mL of sterile water for injection to a vial containing 80 or 120 mg, respectively, to provide a 20 or 40 mg/mL solution, respectively. Swirl gently, do not shake.

Hypersensitivity. Pregnancy and lactation.

Patient with congenital long QT syndrome, history of or risk factors for QT prolongation (e.g. cardiac failure, electrolyte imbalance) and CV disease; diabetes, risk factors for low BMD. Moderate to severe renal (CrCl <50 mL/min) and severe hepatic impairment.

Significant: Anaemia, hypersensitivity reactions, QT prolongation, decreased BMD, decreased glucose tolerance, CV disease, antibody formation.
Gastrointestinal disorders: Nausea, constipation, diarrhoea.
General disorders and administration site conditions: Chills, fatigue, pyrexia, influenza-like illness, injection site reactions (e.g. erythema, pain), asthenia, night sweats.
Investigations: Increased hepatic transaminases.
Metabolism and nutrition disorders: Increased weight.
Musculoskeletal and connective tissue disorders: Back pain, arthralgia.
Nervous system disorder: Dizziness, headache.
Psychiatric disorders: Insomnia.
Reproductive system and breast disorders: Gynaecomastia, erectile dysfunction, testicular atrophy.
Skin and subcutaneous tissue disorders: Rash, hyperhidrosis.
Vascular disorders: Hot flush, hypertension.
Potentially Fatal: Rarely, anaphylaxis.

SC: X

This drug may cause dizziness and fatigue, if affected, do not drive or operate machinery.

Monitor prostate-specific antigen (PSA), serum testosterone levels, LFTs, serum electrolytes (e.g. Na, K, Ca, Mg), BMD, ECG.

Increased risk of QT prolongation with class IA (e.g. disopyramide) or class III (e.g. amiodarone) antiarrhythmics, antipsychotics, methadone and moxifloxacin.

May interfere with diagnostic test results for gonadotropic and gonadal functions.

Description:
Mechanism of Action: Degarelix, a synthetic decapeptide, reversibly and competitively binds to gonadotropin-releasing hormone (GnRH) receptors in the anterior pituitary gland, thereby decreasing secretion of luteinising hormone (LH) and follicle stimulating hormone (FSH), and subsequently reducing testicular androgen synthesis.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: Within 2 days (loading dose).
Distribution: Volume of distribution: Approx 1 L/kg. Plasma protein binding: Approx 90%.
Metabolism: Undergoes peptide hydrolysis in the hepato-biliary system.
Excretion: Mainly via faeces (approx 70-80%, mainly as peptide fragments); via urine (approx 20-30%). Terminal elimination half-life: Approx 43-53 days (loading dose); approx 28 days (maintenance dose).

Source: National Center for Biotechnology Information. PubChem Database. Degarelix, CID=16136245, https://pubchem.ncbi.nlm.nih.gov/compound/Degarelix (accessed on Jan. 20, 2020)

Store at or below 25°C.
Follow applicable procedures for receiving, handling, administration and disposal. Wear gloves during receiving, unpacking, and placing in storage.

Cancer Hormone Therapy

L02BX02 - degarelix ; Belongs to the class of other hormone antagonists and related agents. Used in the treatment of advanced prostate cancer.

Anon. Degarelix. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 03/04/2018.

Anon. Degarelix. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/04/2018.

Buckingham R (ed). Degarelix. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com . Accessed 03/04/2018.

Firmagon (Ferring Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/04/2018.

Joint Formulary Committee. Degarelix. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/04/2018.