Peringatan Keamanan

Overdoses of eculizumab are unlikely as it is administered under specialist supervision.L6922 In case of overdose, contact local poison control.L6922

Eculizumab

DB01257

biotech approved investigational

Deskripsi

Eculizumab is a monoclonal antibody that targets complement protein C5.L6919,A2245 Binding to this protein prevents the activation of a complement terminal complex, which is used to treat a number of autoimmune conditions.L6919,A2245,A2246

Eculizumab was granted FDA approval on 16 March 2007.L6919 In Q1 2023, the EMA's Committee for Medicinal Products for Human Use (CHMP) adopted a positive opinion of two formulations of eculizumab indicated for the treatment of paroxysmal nocturnal hemoglobinuria.L46262,L46267

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of eculizumab is 270-375h[L6919] or 272±82h.[A2247]
Volume Distribusi The volume of distribution of eculizumab is 5-8L.[L6919]
Klirens (Clearance) Pharmacokinetic properties in healthy patients have not been determined.[A179908] In patients with rhematoid arthritis, there is an average clearance of 0.26mL/kg/h.[A179908]

Absorpsi

Eculizumab is administered by intravenous infusion so the bioavailability is 100%.L6919 This drug reaches a Cmax of 194±76µg/mL and Ctrough of 97±60µg/mL.L6919 The AUC was calculated to be 24,467.6µg\*h/mL.A179908

Metabolisme

Eculizumab is a monoclonal antibody and is expected to be metabolized to small peptides and amino acids.A179908,A40006

Rute Eliminasi

Monoclonal antibodies are not eliminated in the urine, and only a small amount is excreted in bile.A40006 Most monoclonal antibodies are catabolized in lysosomes to amino acids.A40006

Interaksi Obat

669 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Eculizumab.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Eculizumab.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Eculizumab.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Eculizumab.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Eculizumab.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Eculizumab.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Eculizumab.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Eculizumab.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Eculizumab.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Eculizumab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Eculizumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Eculizumab.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Eculizumab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Eculizumab.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Eculizumab.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Eculizumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Eculizumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Eculizumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Eculizumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Eculizumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Eculizumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Eculizumab.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Eculizumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Eculizumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Eculizumab.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Eculizumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Eculizumab.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Eculizumab.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Eculizumab.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Eculizumab.
Cladribine Eculizumab may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Eculizumab.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Eculizumab.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Eculizumab.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Eculizumab.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Eculizumab.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Eculizumab.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Eculizumab.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Eculizumab.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Eculizumab.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Eculizumab.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Eculizumab.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Eculizumab.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Eculizumab.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Eculizumab.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Eculizumab.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Eculizumab.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Eculizumab.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Eculizumab.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Eculizumab.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Eculizumab.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Eculizumab.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Eculizumab.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Eculizumab.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Eculizumab.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Eculizumab.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Eculizumab.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Eculizumab.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Eculizumab.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Eculizumab.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Eculizumab.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Eculizumab.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Eculizumab.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Eculizumab.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Eculizumab.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Eculizumab.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Eculizumab.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Eculizumab.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Eculizumab.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Eculizumab.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Eculizumab.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Eculizumab.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Eculizumab.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Eculizumab.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Eculizumab.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Eculizumab.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Eculizumab.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Eculizumab.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Eculizumab.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Eculizumab.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Eculizumab.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Eculizumab.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Eculizumab.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Eculizumab.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Eculizumab.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Eculizumab.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Eculizumab.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Eculizumab.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Eculizumab.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Eculizumab.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Eculizumab.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Eculizumab.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Eculizumab.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Eculizumab.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Eculizumab.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Eculizumab.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Eculizumab.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Eculizumab.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Eculizumab.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Eculizumab.

Target Protein

Complement C5 C5

Referensi & Sumber

Artikel (PubMed)
  • PMID: 9171898
    Thomas TC, Rollins SA, Rother RP, Giannoni MA, Hartman SL, Elliott EA, Nye SH, Matis LA, Squinto SP, Evans MJ: Inhibition of complement activity by humanized anti-C5 antibody and single-chain Fv. Mol Immunol. 1996 Dec;33(17-18):1389-401.
  • PMID: 18784156
    Dmytrijuk A, Robie-Suh K, Cohen MH, Rieves D, Weiss K, Pazdur R: FDA report: eculizumab (Soliris) for the treatment of patients with paroxysmal nocturnal hemoglobinuria. Oncologist. 2008 Sep;13(9):993-1000. doi: 10.1634/theoncologist.2008-0086. Epub 2008 Sep 10.
  • PMID: 17989688
    Rother RP, Rollins SA, Mojcik CF, Brodsky RA, Bell L: Discovery and development of the complement inhibitor eculizumab for the treatment of paroxysmal nocturnal hemoglobinuria. Nat Biotechnol. 2007 Nov;25(11):1256-64.
  • PMID: 30758736
    Wijnsma KL, Ter Heine R, Moes DJAR, Langemeijer S, Schols SEM, Volokhina EB, van den Heuvel LP, Wetzels JFM, van de Kar NCAJ, Bruggemann RJ: Pharmacology, Pharmacokinetics and Pharmacodynamics of Eculizumab, and Possibilities for an Individualized Approach to Eculizumab. Clin Pharmacokinet. 2019 Jul;58(7):859-874. doi: 10.1007/s40262-019-00742-8.
  • PMID: 28653357
    Ryman JT, Meibohm B: Pharmacokinetics of Monoclonal Antibodies. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):576-588. doi: 10.1002/psp4.12224. Epub 2017 Jul 29.

Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Bekemv
    Injection, solution, concentrate • 300 mg • Intravenous • EU • Approved
  • Epysqli
    Injection, solution, concentrate • 10 mg/ml • Intravenous • EU • Approved
  • Soliris
    Injection, solution, concentrate • 300 mg/30mL • Intravenous • US • Approved
  • Soliris
    Solution • 10 mg / mL • Intravenous • Canada • Approved
  • Soliris
    Injection, solution, concentrate • 300 mg • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

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