Peringatan Keamanan

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).

Degarelix

DB06699

small molecule approved

Deskripsi

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.

Struktur Molekul 2D

Berat 1632.29
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Terminal half-life: 41.5 - 70.2 days; Absorption half-life: 32.9 hours; Half-life from injection site: 1.17 days.
Volume Distribusi Central compartment: 8.88 - 11.4 L; Peripheral compartment: 40.9 L
Klirens (Clearance) Following subcutaneous administration of degarelix to prostate cancer patients the clearance is approximately 9 L/hr.

Absorpsi

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.

Metabolisme

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.

Rute Eliminasi

Fecal (70% to 80%) and renal (20%-30% of unchanged drug)

Interaksi Obat

403 Data
Leuprolide The risk or severity of QTc prolongation can be increased when Degarelix is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Goserelin.
Erythromycin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Erythromycin.
Azithromycin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Azithromycin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Moxifloxacin.
Ranolazine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ranolazine.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Degarelix is combined with Sulfisoxazole.
Amitriptyline The risk or severity of QTc prolongation can be increased when Degarelix is combined with Amitriptyline.
Methadone The risk or severity of QTc prolongation can be increased when Degarelix is combined with Methadone.
Diltiazem The risk or severity of QTc prolongation can be increased when Degarelix is combined with Diltiazem.
Clozapine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Clozapine.
Sulpiride The risk or severity of QTc prolongation can be increased when Degarelix is combined with Sulpiride.
Nimodipine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nimodipine.
Promazine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Prochlorperazine.
Droperidol The risk or severity of QTc prolongation can be increased when Degarelix is combined with Droperidol.
Imipramine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Imipramine.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Chlorpromazine.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Degarelix.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ciprofloxacin.
Fluorouracil The risk or severity of QTc prolongation can be increased when Degarelix is combined with Fluorouracil.
Perflutren The risk or severity of QTc prolongation can be increased when Degarelix is combined with Perflutren.
Cinnarizine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Cinnarizine.
Atropine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Atropine.
Chloroquine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Chloroquine.
Efavirenz The risk or severity of QTc prolongation can be increased when Degarelix is combined with Efavirenz.
Adenosine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Adenosine.
Pentamidine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Pentamidine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Degarelix is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Carbinoxamine.
Dolasetron The risk or severity of QTc prolongation can be increased when Degarelix is combined with Dolasetron.
Roxithromycin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Roxithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Cinoxacin.
Loperamide The risk or severity of QTc prolongation can be increased when Degarelix is combined with Loperamide.
Granisetron The risk or severity of QTc prolongation can be increased when Degarelix is combined with Granisetron.
Ondansetron The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ondansetron.
Levosimendan The risk or severity of QTc prolongation can be increased when Degarelix is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Desloratadine.
Telithromycin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Telithromycin.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Degarelix is combined with Dimenhydrinate.
Primaquine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Primaquine.
Papaverine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Papaverine.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Chlorpheniramine.
Nifedipine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nifedipine.
Levofloxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Levofloxacin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ofloxacin.
Propafenone The risk or severity of QTc prolongation can be increased when Degarelix is combined with Propafenone.
Flecainide The risk or severity of QTc prolongation can be increased when Degarelix is combined with Flecainide.
Clarithromycin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Clarithromycin.
Levacetylmethadol The risk or severity of QTc prolongation can be increased when Degarelix is combined with Levacetylmethadol.
Saquinavir The risk or severity of QTc prolongation can be increased when Degarelix is combined with Saquinavir.
Clomipramine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Clomipramine.
Mibefradil The risk or severity of QTc prolongation can be increased when Degarelix is combined with Mibefradil.
Probucol The risk or severity of QTc prolongation can be increased when Degarelix is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Terlipressin.
Prenylamine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Prenylamine.
Fluspirilene The risk or severity of QTc prolongation can be increased when Degarelix is combined with Fluspirilene.
Lofexidine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Lofexidine.
Azimilide The risk or severity of QTc prolongation can be increased when Degarelix is combined with Azimilide.
Pracinostat The risk or severity of QTc prolongation can be increased when Degarelix is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Degarelix is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Degarelix is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Telavancin.
Pazopanib The risk or severity of QTc prolongation can be increased when Degarelix is combined with Pazopanib.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nemonoxacin.
Panobinostat The risk or severity of QTc prolongation can be increased when Degarelix is combined with Panobinostat.
Nilvadipine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nilvadipine.
Antazoline The risk or severity of QTc prolongation can be increased when Degarelix is combined with Antazoline.
Crizotinib The risk or severity of QTc prolongation can be increased when Degarelix is combined with Crizotinib.
Bedaquiline The risk or severity of QTc prolongation can be increased when Degarelix is combined with Bedaquiline.
Fendiline The risk or severity of QTc prolongation can be increased when Degarelix is combined with Fendiline.
Eperisone The risk or severity of QTc prolongation can be increased when Degarelix is combined with Eperisone.
Butriptyline The risk or severity of QTc prolongation can be increased when Degarelix is combined with Butriptyline.
Ceritinib The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ceritinib.
Lenvatinib The risk or severity of QTc prolongation can be increased when Degarelix is combined with Lenvatinib.
Melperone The risk or severity of QTc prolongation can be increased when Degarelix is combined with Melperone.
Benidipine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Benidipine.
Dexchlorpheniramine maleate The risk or severity of QTc prolongation can be increased when Degarelix is combined with Dexchlorpheniramine maleate.
Amifampridine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Amifampridine.
Mocetinostat The risk or severity of QTc prolongation can be increased when Degarelix is combined with Mocetinostat.
Entinostat The risk or severity of QTc prolongation can be increased when Degarelix is combined with Entinostat.
Gilteritinib The risk or severity of QTc prolongation can be increased when Degarelix is combined with Gilteritinib.
CUDC-101 The risk or severity of QTc prolongation can be increased when Degarelix is combined with CUDC-101.
Simendan The risk or severity of QTc prolongation can be increased when Degarelix is combined with Simendan.
Ricolinostat The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ricolinostat.
Mizolastine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Mizolastine.
Abexinostat The risk or severity of QTc prolongation can be increased when Degarelix is combined with Abexinostat.
Oxatomide The risk or severity of QTc prolongation can be increased when Degarelix is combined with Oxatomide.
Sitafloxacin The risk or severity of QTc prolongation can be increased when Degarelix is combined with Sitafloxacin.
Sultopride The risk or severity of QTc prolongation can be increased when Degarelix is combined with Sultopride.
Otilonium The risk or severity of QTc prolongation can be increased when Degarelix is combined with Otilonium.
Nizofenone The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nizofenone.
Bunaftine The risk or severity of QTc prolongation can be increased when Degarelix is combined with Bunaftine.

Target Protein

Gonadotropin-releasing hormone receptor GNRHR

Referensi & Sumber

Synthesis reference: Carin WINDERSTROM, "KIT AND METHOD FOR PREPARATION OF A DEGARELIX SOLUTION." U.S. Patent US20100286603, issued November 11, 2010.
Artikel (PubMed)
  • PMID: 20110043
    Steinberg M: Degarelix: a gonadotropin-releasing hormone antagonist for the management of prostate cancer. Clin Ther. 2009;31 Pt 2:2312-31. doi: 10.1016/j.clinthera.2009.11.009.
  • PMID: 19602868
    Persson BE, Kold Olesen T, Jensen JK: Degarelix: a new approach for the treatment of prostate cancer. Neuroendocrinology. 2009;90(3):235-44. doi: 10.1159/000228832. Epub 2009 Jul 14.

Contoh Produk & Brand

Produk: 12 • International brands: 0
Produk
  • Degarelix Accord
    Injection, powder, for solution • 80 mg • Subcutaneous • EU • Approved
  • Degarelix Accord
    Injection, powder, for solution • 80 mg • Subcutaneous • EU • Approved
  • Degarelix Accord
    Injection, powder, for solution • 120 mg • Subcutaneous • EU • Approved
  • Firmagon
    Powder, metered • 40 mg/1mL • Subcutaneous • US • Approved
  • Firmagon
    Powder, metered • 20 mg/1mL • Subcutaneous • US • Approved
  • Firmagon
    Injection, powder, lyophilized, for solution; Kit • 40 mg/1mL • Subcutaneous • US • Approved
  • Firmagon
    Injection, powder, lyophilized, for solution; Kit • 20 mg/1mL • Subcutaneous • US • Approved
  • Firmagon
    Powder, for solution • 80 mg / vial • Subcutaneous • Canada • Approved
Menampilkan 8 dari 12 produk.

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