Trade Names:Degarelix- Injection, lyophilized powder for solution 80 mg- Injection, lyophilized powder for solution 120 mg
Binds reversibly to the pituitary gonadotropin-releasing hormone (GnRH) receptors, thereby reducing the release of gonadotropin and consequently testosterone.
C max and AUC are approximately 26 ng/mL and 1,054 ng•day/mL, respectively. T max is 2 days. Pharmacokinetics are strongly influenced by the injection concentration.
Vd after IV (more than 1 L/kg) or subcutaneous (more than 1,000 L) administration indicates drug distribution throughout total body water. Plasma protein binding is approximately 90%.
Metabolism is due to peptide hydrolysis during hepatobiliary system passage.
Excretion is primarily as peptide fragments in the feces (70% to 80%) and approximately 20% to 30% is renally excreted. Median terminal half-life is approximately 53 days. Cl is approximately 9 L/h.
Patients with hepatic function impairment were excluded from trials.Renal function impairment
No pharmacokinetic studies have been performed.
Treatment of advanced prostate cancer.
Women who are or may become pregnant; hypersensitivity to any component of the product.
Subcutaneous Start with 240 mg given as 2 injections of 120 mg at a concentration of 40 mg/mL. The maintenance dose is 80 mg as 1 injection at a concentration of 20 mg/mL.
Store at 59° to 86°F.
None well documented.
Because suppression of the pituitary gonadal system may occur, results of diagnostic test of the pituitary gonadotropic or gonadal functions may be affected.
Hot flashes (26%); hypertension (7%).
Fatigue (6%); asthenia, dizziness, headache, insomnia (1% to 5%).
Diarrhea (at least 1%); constipation (5%); nausea (1% to 5%);.
Urinary tract infection (5%); erectile dysfunction, gynecomastia, testicular atrophy (at least 1%).
Anti-degarelix antibodies (10%).
Increased gamma-glutamyl transpeptidase, increased transaminase (10%).
Pain (28%); erythema (17%); swelling (6%); induration (4%); nodule (3%).
Increased weight (11%).
Back pain (6%); arthralgia (5%).
Chills (5%); fever, night sweats (1% to 5%); hyperhidrosis (at least 1%), decreased bone density.
Monitor prostate-specific antigen (PSA) periodically. If PSA increases, measure testosterone serum concentrations.
Category X .
Safety and efficacy not established.
Use with caution in patients with CrCl less than 50 mL/min.
Use with caution in patients with severe hepatic dysfunction.
Long-term androgen deprivation therapy prolongs the QT interval. Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients with congenital long QT syndrome, electrolyte abnormalities, or CHF and patients taking class 1A (eg, procainamide, quinidine) or class III (eg, amiodarone, sotalol) antiarrhythmic agents.
Has not been reported.
Copyright © 2009 Wolters Kluwer Health.