Drug information of Degarelix
Mechanism of effect
Gonadotropin-releasing hormone (GnRH) antagonist which reversibly binds to GnRH receptors in the anterior pituitary gland, blocking the receptor and decreasing secretion of luteinizing hormone (LH) and follicle stimulation hormone (FSH), resulting in rapid androgen deprivation by decreasing testosterone production, thereby decreasing testosterone levels. Testosterone levels do not exhibit an initial surge, or flare, as is typical with GnRH agonists
Hepatobiliary, via peptide hydrolysis
Time to reach the peak
Plasma: Loading dose: SubQ: Within 2 days
Vd: >1000 L
Loading dose: SubQ: ~53 days; Maintenance dose: SubQ: ~31 days (Canadian labeling)
Feces (~70% to 80%, primarily as peptide fragments); urine (~20% to 30%)
Treatment of advanced prostate cancer
Usual Adult Dose for Prostate Cancer
-Initial Dose: 240 mg administered as 2 subcutaneous injections of 120 mg each at a concentration of 40 mg/mL .
-Maintenance Dose: 80 mg administered as 1 subcutaneous injection at a concentration of 20 mg/mL every 28 days.
Known hypersensitivity to degarelix or any component of the formulation; women who are or may become pregnant.
Central nervous system: Fatigue
Endocrine & metabolic: Hot flash, increased gamma-glutamyl transferase, weight loss, weight gain
Hepatic: Increased serum transaminases
Local: Injection site reactions, pain at injection site, erythema at injection site, swelling at injection site, induration at injection site, injection site nodule, injection site infection
Gastrointestinal: Constipation, nausea, diarrhea
Genitourinary: Urinary tract infection, erectile dysfunction, testicular atrophy
Immunologic: Antibody development (antidegarelix)
Neuromuscular & skeletal: Back pain, arthralgia, weakness
Miscellaneous: Night sweats
InteractionsDolasetron , vandetanib , sparfloxacin , Dofetilide , Halofantrine , Grepafloxacin , Haloperidol , Entrectinib , Bepridil , bedaquiline , Gemtuzumab , vemurafenib
Points of recommendation
1-Although this medicine is not for use by women, degarelix should not be used by a woman who is pregnant or breast-feeding, or who may become pregnant .
2-Before you receive degarelix, tell your doctor if you have liver or kidney disease, a personal or family history of "Long QT syndrome," congestive heart failure, or an electrolyte imbalance, such as low or high levels of potassium or magnesium in your blood .
3-Tell your doctor about all other medications you use, especially a heart rhythm medication .
4-Degarelix is usually given once every 28 days .
6-Degarelix is injected under the skin around your stomach.
7-On the day of your injection, avoid wearing a belt, tight waistband, or tight clothing around your stomach where the injection will be given.
8-The first time you receive this medicine, you will be given two injections. At your monthly follow-up visits you will receive only one injection.
9-Administer this drug in the abdominal region only.
10-Vary the injection site periodically to minimize patient discomfort, and administer in abdomen areas not exposed to pressure .
11-Perform a slow, deep subcutaneous injection over 30 seconds .
12-This drug is for subcutaneous injection only; do not administer intravenously or intramuscularly
13-Use this drug only as a first-line androgen deprivation therapy; there is no data available on use of this drug in patients who have failed treatment with GnRH agonists (e.g., leuprorelin, goserelin).
Store at 25°C; excursions permitted to 15°C to 30°C . Use within 1 hour of reconstitution (US labeling). The Canadian labeling recommends immediate administration following reconstitution (preferred); stability has been demonstrated for 2 hours following reconstitution. Do not shake the vials.
Use is contraindicated in women who are or may become pregnant.
Breast feeding warning
excretion in milk unknown/not recommended.