Peringatan Keamanan

In healthy volunteers, the most frequently reported adverse reactions in greater than or equal to 5% of subjects treated with idarucizumab was headache. In patients, the most frequently reported adverse reactions in greater than or equal to 5% of patients treated with idarucizumab were hypokalemia, delirium, constipation, pyrexia, and pneumonia.

Idarucizumab

DB09264

biotech approved

Deskripsi

Idarucizumab is a humanized monoclonal antibody fragment (Fab) derived from an immunoglobulin G1 isotype molecule that binds to and inactivates the oral anticoagulant dabigatran, thereby reversing its anticoagulant effect. As a direct acting oral anticoagulant (DOAC), one of the risks associated with the use of dabigatran includes bleeding, espeically when given to patients at increased risk (elderly, chronic kidney disease, concomitant NSAID or warfarin use, etc).

Approved under the tradename Praxbind (FDA), idarucizumab is indicated for the emergency treatment of dabigatran-associated bleeding in life-threatening or surgically induced situations. Its use is associated with immediate, complete and sustained reversal of the anticoagulant effects of dabigatran.

Idarucizumab protein structure can be viewed below, with disulfide bridges at the following points: H22-H95, H149-H205, H225-L-219, L23-L93, L139-L199.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) initial half-life: 47 minutes terminal half-life: 10.3 h
Volume Distribusi 8.9 L
Klirens (Clearance) 47.0 mL/min

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Several pathways have been described that may contribute to the metabolism of antibodies. All of these pathways involve biodegradation of the antibody to smaller molecules, i.e., small peptides or amino acids which are then reabsorbed and incorporated in the general protein synthesis.

Rute Eliminasi

After intravenous administration of 5 g idarucizumab, 32.1% (gCV 60.0%) of the dose was recovered in urine within a collection period of 6 hours and less than 1% in the following 18 hours. The remaining part of the dose is assumed to be eliminated via protein catabolism, mainly in the kidney.

Interaksi Obat

1089 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Idarucizumab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Idarucizumab.
Estrone Estrone may increase the thrombogenic activities of Idarucizumab.
Dienestrol Dienestrol may increase the thrombogenic activities of Idarucizumab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Idarucizumab.
Mestranol Mestranol may increase the thrombogenic activities of Idarucizumab.
Estriol Estriol may increase the thrombogenic activities of Idarucizumab.
Quinestrol Quinestrol may increase the thrombogenic activities of Idarucizumab.
Hexestrol Hexestrol may increase the thrombogenic activities of Idarucizumab.
Tibolone Tibolone may increase the thrombogenic activities of Idarucizumab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Idarucizumab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Idarucizumab.
Zeranol Zeranol may increase the thrombogenic activities of Idarucizumab.
Equol Equol may increase the thrombogenic activities of Idarucizumab.
Promestriene Promestriene may increase the thrombogenic activities of Idarucizumab.
Methallenestril Methallenestril may increase the thrombogenic activities of Idarucizumab.
Epimestrol Epimestrol may increase the thrombogenic activities of Idarucizumab.
Moxestrol Moxestrol may increase the thrombogenic activities of Idarucizumab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Idarucizumab.
Biochanin A Biochanin A may increase the thrombogenic activities of Idarucizumab.
Formononetin Formononetin may increase the thrombogenic activities of Idarucizumab.
Estetrol Estetrol may increase the thrombogenic activities of Idarucizumab.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Idarucizumab.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Idarucizumab.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Idarucizumab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Idarucizumab.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Idarucizumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Idarucizumab.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Idarucizumab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Idarucizumab.
Trastuzumab The risk or severity of adverse effects can be increased when Trastuzumab is combined with Idarucizumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Idarucizumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Idarucizumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Idarucizumab.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Idarucizumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Idarucizumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Idarucizumab.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Idarucizumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Idarucizumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Idarucizumab.
Natalizumab The risk or severity of adverse effects can be increased when Natalizumab is combined with Idarucizumab.
Palivizumab The risk or severity of adverse effects can be increased when Palivizumab is combined with Idarucizumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Idarucizumab.
Bevacizumab The risk or severity of adverse effects can be increased when Bevacizumab is combined with Idarucizumab.
Technetium Tc-99m arcitumomab The risk or severity of adverse effects can be increased when Technetium Tc-99m arcitumomab is combined with Idarucizumab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Idarucizumab.
Panitumumab The risk or severity of adverse effects can be increased when Panitumumab is combined with Idarucizumab.
Ranibizumab The risk or severity of adverse effects can be increased when Ranibizumab is combined with Idarucizumab.
Galiximab The risk or severity of adverse effects can be increased when Galiximab is combined with Idarucizumab.
Pexelizumab The risk or severity of adverse effects can be increased when Pexelizumab is combined with Idarucizumab.
Afelimomab The risk or severity of adverse effects can be increased when Afelimomab is combined with Idarucizumab.
Epratuzumab The risk or severity of adverse effects can be increased when Epratuzumab is combined with Idarucizumab.
Bectumomab The risk or severity of adverse effects can be increased when Bectumomab is combined with Idarucizumab.
Oregovomab The risk or severity of adverse effects can be increased when Oregovomab is combined with Idarucizumab.
IGN311 The risk or severity of adverse effects can be increased when IGN311 is combined with Idarucizumab.
Adecatumumab The risk or severity of adverse effects can be increased when Adecatumumab is combined with Idarucizumab.
Labetuzumab The risk or severity of adverse effects can be increased when Labetuzumab is combined with Idarucizumab.
Matuzumab The risk or severity of adverse effects can be increased when Matuzumab is combined with Idarucizumab.
Fontolizumab The risk or severity of adverse effects can be increased when Fontolizumab is combined with Idarucizumab.
Bavituximab The risk or severity of adverse effects can be increased when Bavituximab is combined with Idarucizumab.
CR002 The risk or severity of adverse effects can be increased when CR002 is combined with Idarucizumab.
Rozrolimupab The risk or severity of adverse effects can be increased when Rozrolimupab is combined with Idarucizumab.
Girentuximab The risk or severity of adverse effects can be increased when Girentuximab is combined with Idarucizumab.
Obiltoxaximab The risk or severity of adverse effects can be increased when Obiltoxaximab is combined with Idarucizumab.
XTL-001 The risk or severity of adverse effects can be increased when XTL-001 is combined with Idarucizumab.
NAV 1800 The risk or severity of adverse effects can be increased when NAV 1800 is combined with Idarucizumab.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Idarucizumab.
Otelixizumab The risk or severity of adverse effects can be increased when Otelixizumab is combined with Idarucizumab.
AMG 108 The risk or severity of adverse effects can be increased when AMG 108 is combined with Idarucizumab.
Iratumumab The risk or severity of adverse effects can be increased when Iratumumab is combined with Idarucizumab.
Enokizumab The risk or severity of adverse effects can be increased when Enokizumab is combined with Idarucizumab.
Ramucirumab The risk or severity of adverse effects can be increased when Ramucirumab is combined with Idarucizumab.
Farletuzumab The risk or severity of adverse effects can be increased when Farletuzumab is combined with Idarucizumab.
Veltuzumab The risk or severity of adverse effects can be increased when Veltuzumab is combined with Idarucizumab.
Ustekinumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Idarucizumab.
Trastuzumab emtansine The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Idarucizumab.
PRO-542 The risk or severity of adverse effects can be increased when PRO-542 is combined with Idarucizumab.
TNX-901 The risk or severity of adverse effects can be increased when TNX-901 is combined with Idarucizumab.
Inotuzumab ozogamicin The risk or severity of adverse effects can be increased when Inotuzumab ozogamicin is combined with Idarucizumab.
RI 624 The risk or severity of adverse effects can be increased when RI 624 is combined with Idarucizumab.
Stamulumab The risk or severity of adverse effects can be increased when MYO-029 is combined with Idarucizumab.
CT-011 The risk or severity of adverse effects can be increased when CT-011 is combined with Idarucizumab.
Leronlimab The risk or severity of adverse effects can be increased when Leronlimab is combined with Idarucizumab.
Glembatumumab vedotin The risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Idarucizumab.
Olaratumab The risk or severity of adverse effects can be increased when Olaratumab is combined with Idarucizumab.
IPH 2101 The risk or severity of adverse effects can be increased when IPH 2101 is combined with Idarucizumab.
TB-402 The risk or severity of adverse effects can be increased when TB-402 is combined with Idarucizumab.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Idarucizumab.
IMC-1C11 The risk or severity of adverse effects can be increased when IMC-1C11 is combined with Idarucizumab.
Eldelumab The risk or severity of adverse effects can be increased when Eldelumab is combined with Idarucizumab.
Lumiliximab The risk or severity of adverse effects can be increased when Lumiliximab is combined with Idarucizumab.
Canakinumab The risk or severity of adverse effects can be increased when Canakinumab is combined with Idarucizumab.
Nimotuzumab The risk or severity of adverse effects can be increased when Nimotuzumab is combined with Idarucizumab.
Clenoliximab The risk or severity of adverse effects can be increased when Clenoliximab is combined with Idarucizumab.
Tocilizumab The risk or severity of adverse effects can be increased when Tocilizumab is combined with Idarucizumab.
BIIB015 The risk or severity of adverse effects can be increased when BIIB015 is combined with Idarucizumab.
Sonepcizumab The risk or severity of adverse effects can be increased when Sonepcizumab is combined with Idarucizumab.
Motavizumab The risk or severity of adverse effects can be increased when Motavizumab is combined with Idarucizumab.
Elotuzumab The risk or severity of adverse effects can be increased when Elotuzumab is combined with Idarucizumab.
AVE9633 The risk or severity of adverse effects can be increased when AVE9633 is combined with Idarucizumab.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27388764
    Syed YY: Idarucizumab: A Review as a Reversal Agent for Dabigatran. Am J Cardiovasc Drugs. 2016 Aug;16(4):297-304. doi: 10.1007/s40256-016-0181-4.
  • PMID: 27389324
    Yogaratnam D, Ditch K, Medeiros K, Doyno C, Fong JJ: Idarucizumab for Reversal of Dabigatran. Ann Pharmacother. 2016 Jul 7. pii: 1060028016659504.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Praxbind
    Injection • 50 mg/1mL • Intravenous • US • Approved
  • Praxbind
    Solution • 50 mg / mL • Intravenous • Canada • Approved
  • Praxbind
    Injection, solution • 2.5 g/50mL • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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