Peringatan Keamanan

Data regarding overdoses of tocilizumab are not readily available.L12789 Patients experiencing an overdose may develop neutropenia.L12789 In case of overdose, monitor patients for signs of adverse reactions and provide symptomatic and supportive treatment.L12789

Tocilizumab

DB06273

biotech approved

Deskripsi

Tocilizumab is a recombinant humanized monoclonal antibody IL-6 receptor inhibitor used to treat inflammatory and autoimmune conditions.L12789 It was first described in the literature in 2003 when Chugai, a subsidiary of Roche began developing IL-6 inhibiting monoclonal antibodies.A193281 Tocilizumab was granted FDA approval on 8 January 2010 to treat a number of inflammatory and autoimmune disorders, such as different types of arthritis and cytokine release syndrome.L12789 It was later approved by Health Canada on 30 April 2010.L43697 After being investigated to treat severely ill patients with COVID-19,A193278,L12837,L12843 tocilizumab was approved by the European Commission in December 2021 to treat COVID-19 in adults receiving systemic corticosteroids and supplemental oxygen or mechanical ventilation.L40164 Subsequently, it was granted approval by Health Canada and the FDA in October L43697 and December 2022, respectively.L44483 Tocilizumab-bavi, a biosimilar drug, was approved by the FDA in September 2023.L48385

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) The half life of tocilizumab is concentration dependent.[L12789] The terminal half life in rheumatoid arthritis patients is 21.5 days.[L12789] The absorption half life in rheumatoid arthritis and giant cell arteritis patients was 4 days, and in polyarticular juvenile idiopathic arthritis patients and systemic juvenile idiopathic arthritis patients was 2 days.[L12789]
Volume Distribusi In rheumatoid arthritis patients, the central volume of distribution is 3.5L, the peripheral volume of distribution is 2.9L, and the volume of distribution at steady state is 6.4L.[L12789] In giant cell arteritis patients, the central volume of distribution is 4.09L, the peripheral volume of distribution if 3.37L, and the volume of distribution at steady state is 7.46L.[L12789] In pediatric patients with polyarticular juvenile arthritis, the central volume of distribution is 1.98L, the peripheral volume of distribution is 2.1L, and the volume of distribution at steady state is 4.08L.[L12789] In pediatric patients with systemic juvenile idiopathic arthritis, the central volume of distribution is 1.87L, the peripheral volume of distribution is 2.14L, and the volume of distribution at steady state is 4.01L.[L12789]
Klirens (Clearance) The linear clearance in rheumatoid arthritis patients is 12.5mL/h, in giant cell arteritis patients is 6.7mL/h, in polyarticular juvenile idiopathic arthritis patients is 5.8mL/h, and in systemic juvenile idiopathic arthritis is 5.7mL/h.[L12789] Clearance is dose dependent and changes from non linear at low doses to linear at higher doses.[L12789]

Absorpsi

A 162mg subcutaneous dose given weekly has a Cmax of 51.3±23.2µg/mL and an AUC of 8254±3833µg\*h/mL.A193293 A 162mg subcutaneous dose given every 2 weeks has a Cmax of 13±8.3µg/mL and an AUC of 3460±2530µg\*h/mL.A193293 A 162mg subcutaneous dose given every 4 weeks has a Cmax of 154±42µg/mL and an AUC of 39216±14304µg\*h/mL.A193293

Metabolisme

Tocilizumab, like other monoclonal antibodies, is expected to be metabolized to smaller proteins and amino acids by proteolytic enzymes.A19126

Rute Eliminasi

Data regarding the exact route of elimination of monoclonal antibodies is not readily available.A19126,L12789

Interaksi Obat

1378 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Tocilizumab.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Tocilizumab.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Tocilizumab.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Tocilizumab.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Tocilizumab.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Tocilizumab.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Tocilizumab.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Tocilizumab.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Tocilizumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Tocilizumab.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Tocilizumab.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Tocilizumab.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Tocilizumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Tocilizumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Tocilizumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Tocilizumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Tocilizumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Tocilizumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Tocilizumab.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Tocilizumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Tocilizumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Tocilizumab.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Tocilizumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Tocilizumab.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Tocilizumab.
Cladribine Tocilizumab may increase the immunosuppressive activities of Cladribine.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Tocilizumab.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Tocilizumab.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Tocilizumab.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Tocilizumab.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Tocilizumab.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Tocilizumab.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Tocilizumab.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Tocilizumab.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Tocilizumab.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Tocilizumab.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Tocilizumab.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Tocilizumab.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Tocilizumab.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Tocilizumab.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Tocilizumab.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Tocilizumab.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Tocilizumab.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Tocilizumab.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Tocilizumab.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Tocilizumab.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Tocilizumab.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Tocilizumab.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Tocilizumab.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Tocilizumab.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Tocilizumab.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Tocilizumab.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Tocilizumab.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Tocilizumab.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Tocilizumab.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Tocilizumab.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Tocilizumab.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Tocilizumab.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Tocilizumab.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Tocilizumab.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Tocilizumab.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Tocilizumab.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Tocilizumab.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Tocilizumab.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Tocilizumab.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Tocilizumab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Tocilizumab.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Tocilizumab.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Tocilizumab.
Abatacept The risk or severity of adverse effects can be increased when Abatacept is combined with Tocilizumab.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Tocilizumab.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Tocilizumab.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Tocilizumab.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Tocilizumab.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Tocilizumab.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Tocilizumab.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Tocilizumab.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Tocilizumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Tocilizumab.
Canakinumab 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 Tocilizumab is combined with Rilonacept.
Mepolizumab The risk or severity of adverse effects can be increased when Tocilizumab is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Tocilizumab is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Tocilizumab is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Tocilizumab is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Tocilizumab is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Tocilizumab is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Tocilizumab is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Tocilizumab is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Tocilizumab is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Tocilizumab is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Tocilizumab is combined with Obinutuzumab.
Secukinumab The risk or severity of adverse effects can be increased when Tocilizumab is combined with Secukinumab.
Vedolizumab The risk or severity of adverse effects can be increased when Tocilizumab is combined with Vedolizumab.
Siltuximab The risk or severity of adverse effects can be increased when Tocilizumab is combined with Siltuximab.
Blinatumomab The risk or severity of adverse effects can be increased when Tocilizumab is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Tocilizumab is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Tocilizumab is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Tocilizumab is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Tocilizumab is combined with Antilymphocyte immunoglobulin (horse).

Target Protein

Interleukin-6 receptor subunit alpha IL6R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 32278585
    Cellina M, Orsi M, Bombaci F, Sala M, Marino P, Oliva G: Favorable changes of CT findings in a patient with COVID-19 pneumonia after treatment with tocilizumab. Diagn Interv Imaging. 2020 Mar 31. pii: S2211-5684(20)30087-5. doi: 10.1016/j.diii.2020.03.010.
  • PMID: 12669473
    Ding C, Jones G: Technology evaluation: MRA, Chugai. Curr Opin Mol Ther. 2003 Feb;5(1):64-9.
  • PMID: 20608753
    Keizer RJ, Huitema AD, Schellens JH, Beijnen JH: Clinical pharmacokinetics of therapeutic monoclonal antibodies. Clin Pharmacokinet. 2010 Aug;49(8):493-507. doi: 10.2165/11531280-000000000-00000.
  • PMID: 25190079
    Tanaka T, Narazaki M, Kishimoto T: IL-6 in inflammation, immunity, and disease. Cold Spring Harb Perspect Biol. 2014 Sep 4;6(10):a016295. doi: 10.1101/cshperspect.a016295.
  • PMID: 27599663
    Abdallah H, Hsu JC, Lu P, Fettner S, Zhang X, Douglass W, Bao M, Rowell L, Burmester GR, Kivitz A: Pharmacokinetic and Pharmacodynamic Analysis of Subcutaneous Tocilizumab in Patients With Rheumatoid Arthritis From 2 Randomized, Controlled Trials: SUMMACTA and BREVACTA. J Clin Pharmacol. 2017 Apr;57(4):459-468. doi: 10.1002/jcph.826. Epub 2016 Nov 17.

Contoh Produk & Brand

Produk: 51 • International brands: 1
Produk
  • Actemra
    Injection, solution, concentrate • 20 mg/1mL • Intravenous • US • Approved
  • Actemra
    Solution • 80 mg / 4 mL • Intravenous • Canada • Approved
  • Actemra
    Solution • 200 mg / 10 mL • Intravenous • Canada • Approved
  • Actemra
    Solution • 400 mg / 20 mL • Intravenous • Canada • Approved
  • Actemra
    Solution • 162 mg / 0.9 mL • Subcutaneous • Canada • Approved
  • Actemra
    Solution • 162 mg / 0.9 mL • Subcutaneous • Canada • Approved
  • Actemra
    Injection, solution, concentrate • 80 mg/4mL • Intravenous • US • Approved
  • Actemra
    Injection, solution, concentrate • 400 mg/20mL • Intravenous • US • Approved
Menampilkan 8 dari 51 produk.
International Brands
  • RoActemra

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