Peringatan Keamanan

There are no confirmed cases of overdosage with canakinumab.L48006 In the event of an overdose, the patient should be monitored closely and appropriate symptomatic treatment should be administered immediately as clinically indicated.

Canakinumab

DB06168

biotech approved investigational

Deskripsi

Canakinumab is a recombinant, human anti-human-IL-1? monoclonal antibody that belongs to the IgG1/? isotype subclass. It is expressed in a murine Sp2/0-Ag14 cell line and comprised of two 447- (or 448-) residue heavy chains and two 214-residue light chains, with a molecular mass of 145157 Daltons when deglycosylated. Both heavy chains of canakinumab contain oligosaccharide chains linked to the protein backbone at asparagine 298 (Asn 298). Canakinumab binds to human IL-1? and neutralizes its inflammatory activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1alpha or IL-1 receptor antagonist (IL-1ra). Canakinumab is marketed under the brand name Ilaris and indicated for patients 4 years of age and older to treat Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS), which are both part of the Cryopyrin-Associated Periodic Syndromes (CAPS) as well as for patients 2 years of age and older to treat systemic juvenile idiopathic arthritis (SJIA). Clinical trials have established the administration of canakinumab every 2 weeks to be safe and effective, offering a considerable advantage over the existing treatment with the human IL-1 receptor antagonist, anakinra, which must be injected daily and which is often poorly tolerated by patients.

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 26 days
Volume Distribusi The steady-state volume of distribution of canakinumab is variable based on weight - it was estimated to be 6.01 liters in a typical CAPS patient weighing 70 kg, 3.2 liters in a SJIA patient weighing 33 kg, 6.34 liters for a Periodic Fever Syndrome (TRAPS, HIDS/MKD, FMF) patient weighing 70 kg and 7.9 liters in a typical patient with gout flares weighing 93 kg.[L48006]
Klirens (Clearance) The clearance of canakinumab is variable based on weight - it was estimated to be 0.174 L/day in a typical CAPS patient weighing 70 kg, 0.11 L/day in an SJIA patient weighing 33 kg, 0.17 L/day in a Periodic Fever Syndrome (TRAPS, HIDS/MKD, FMF) patient weighing 70 kg and 0.23 L/day in a typical patient with gout flares of body weight 93 kg.[L48006]

Absorpsi

The absolute bioavailability of subcutaneously administered canakinumab is estimated to be 66%.L48006 Peak serum concentration is 16 ± 3.5 mcg/mL and occurs approximately 7 days following a single subcutaneous dose of 150mg.L48006 Exposure to canakinumab increases proportionately to the administered dose.L48006

Metabolisme

Canakinumab, like other therapeutic proteins, is likely degraded via non-specific catabolic processes to smaller peptides and amino acids.

Rute Eliminasi

The route of elimination for canakinumab has not yet been determined.

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1334 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Canakinumab.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Canakinumab.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Canakinumab.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Canakinumab.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Canakinumab.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Canakinumab.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Canakinumab.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Canakinumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Canakinumab.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Canakinumab.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Canakinumab.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Canakinumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Canakinumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Canakinumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Canakinumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Canakinumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Canakinumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Canakinumab.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Canakinumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Canakinumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Canakinumab.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Canakinumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Canakinumab.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Canakinumab.
Cladribine Canakinumab may increase the immunosuppressive activities of Cladribine.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Canakinumab.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Canakinumab.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Canakinumab.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Canakinumab.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Canakinumab.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Canakinumab.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Canakinumab.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Canakinumab.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Canakinumab.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Canakinumab.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Canakinumab.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Canakinumab.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Canakinumab.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Canakinumab.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Canakinumab.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Canakinumab.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Canakinumab.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Canakinumab.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Canakinumab.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Canakinumab.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Canakinumab.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Canakinumab.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Canakinumab.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Canakinumab.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Canakinumab.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Canakinumab.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Canakinumab.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Canakinumab.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Canakinumab.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Canakinumab.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Canakinumab.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Canakinumab.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Canakinumab.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Canakinumab.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Canakinumab.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Canakinumab.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Canakinumab.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Canakinumab.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Canakinumab.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Canakinumab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Canakinumab.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Canakinumab.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Canakinumab.
Abatacept The risk or severity of adverse effects can be increased when Abatacept is combined with Canakinumab.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Canakinumab.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Canakinumab.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Canakinumab.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Canakinumab.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Canakinumab.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Canakinumab.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Canakinumab.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Canakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Canakinumab.
Tocilizumab The risk or severity of adverse effects can be increased when Canakinumab is combined with Tocilizumab.
Rilonacept The risk or severity of adverse effects can be increased when Canakinumab is combined with Rilonacept.
Mepolizumab The risk or severity of adverse effects can be increased when Canakinumab is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Canakinumab is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Canakinumab is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Canakinumab is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Canakinumab is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Canakinumab is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Canakinumab is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Canakinumab is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Canakinumab is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Canakinumab is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Canakinumab is combined with Obinutuzumab.
Secukinumab The risk or severity of adverse effects can be increased when Canakinumab is combined with Secukinumab.
Vedolizumab The risk or severity of adverse effects can be increased when Canakinumab is combined with Vedolizumab.
Siltuximab The risk or severity of adverse effects can be increased when Canakinumab is combined with Siltuximab.
Blinatumomab The risk or severity of adverse effects can be increased when Canakinumab is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Canakinumab is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Canakinumab is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Canakinumab is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Canakinumab is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Canakinumab is combined with Tepoxalin.

Target Protein

Interleukin-1 beta IL1B

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19169963
    Church LD, McDermott MF: Canakinumab, a fully-human mAb against IL-1beta for the potential treatment of inflammatory disorders. Curr Opin Mol Ther. 2009 Feb;11(1):81-9.
  • PMID: 19494217
    Lachmann HJ, Kone-Paut I, Kuemmerle-Deschner JB, Leslie KS, Hachulla E, Quartier P, Gitton X, Widmer A, Patel N, Hawkins PN: Use of canakinumab in the cryopyrin-associated periodic syndrome. N Engl J Med. 2009 Jun 4;360(23):2416-25. doi: 10.1056/NEJMoa0810787.

Contoh Produk & Brand

Produk: 9 • International brands: 0
Produk
  • Ilaris
    Injection, powder, lyophilized, for solution • 150 mg/1mL • Subcutaneous • US • Approved
  • Ilaris
    Injection, solution • 150 mg/1mL • Subcutaneous • US • Approved
  • Ilaris
    Powder, for solution • 150 mg / vial • Subcutaneous • Canada • Approved
  • Ilaris
    Solution • 150 mg / mL • Subcutaneous • Canada • Approved
  • Ilaris
    Injection, powder, for solution • 150 mg • Subcutaneous • EU • Approved
  • Ilaris
    Injection, powder, for solution • 150 mg • Subcutaneous • EU • Approved
  • Ilaris
    Injection, powder, for solution • 150 mg • Subcutaneous • EU • Approved
  • Ilaris
    Injection, solution • 150 mg/ml • Subcutaneous • EU • Approved
Menampilkan 8 dari 9 produk.

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