Product Information
Registration Status: ActiveFIRMAGON POWDER AND SOLVENT FOR SOLUTION FOR INJECTION 80MG is approved to be sold in Singapore with effective from 2013-05-13. It is marketed by FERRING PHARMACEUTICALS PTE LTD, with the registration number of SIN14351P.
This product contains Degarelix 80mg in the form of INJECTION, POWDER, FOR SOLUTION. It is approved for SUBCUTANEOUS use.
This product is manufactured by Rentschler Biotechnologie GmbH (Powder)
Hameln Pharmaceuticals GmbH (Solvent)
Ferring GmbH (Solvent) in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Degarelix is used for the treatment of advanced prostate cancer. Degarelix is a synthetic peptide derivative drug which binds to gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland and blocks interaction with GnRH. This antagonism reduces luteinising hormone (LH) and follicle-stimulating hormone (FSH) which ultimately causes testosterone suppression. Reduction in testosterone is important in treating men with advanced prostate cancer. Chemically, it is a synthetic linear decapeptide amide with seven unnatural amino acids, five of which are D-amino acids. FDA approved on December 24, 2008.
Indication
Degaralix is used for the management of advanced prostate cancer.
Mechanism of Action
GnRH antagonists compete with natural GnRH for binding to GnRH receptors in the pituitary gland. This reversible blinding blocks the release of LH and FSH from the pituitary. The reduction in LH subsequently leads to a rapid and sustained suppression of testosterone release from the testes and subsequently reduces the size and growth of the prostate cancer.
Pharmacokinetics
- Absorption
- Degarelix forms a depot at the site of injection after subcutaneous administration from which the drug slowly released into circulation. After a single bolus dose of 2mg/kg, peak plasma concentrations of degarelix occured within 6 hours at a concentration of 330 ng/mL. Ki = 0.082 ng/mL and 93% of receptors were fully suppressed; MRT = 4.5 days.
- Distribution
- Central compartment: 8.88 - 11.4 L; Peripheral compartment: 40.9 L
- Metabolism
- 70% - 80% of degarelix is subject to peptide hydrolysis during its passage through the hepatobiliary system and then fecally eliminated. No active or inactive metabolites or involvement of CYP450 isozymes.
- Elimination
Clearance
Following subcutaneous administration of degarelix to prostate cancer patients the clearance is approximately 9 L/hr.
Toxicity
The most commonly observed adverse reactions (> 10%) during degarelix therapy included injection site reactions (e.g., pain, erythema, swelling, or induration), hot flashes, increased weight, and increases in serum levels of transaminases and gamma-glutamyltransferase (GGT).
Active Ingredient/Synonyms
Degarelix | Degarelix |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.