Peringatan Keamanan

Most common adverse events (?10%) are headache, upper respiratory tract infection, nasopharyngitis, and nausea. Doses up to 50 mg/kg have been administered without apparent toxic effect.

Abatacept

DB01281

biotech approved

Deskripsi

Abatacept is a soluble fusion protein, which links the extracellular domain of human cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) to the modified Fc (hinge, CH2, and CH3 domains) portion of human immunoglobulin G1 (IgG1).L20504,L42715 Structurally, abatacept is a glycosylated fusion protein with a MALDI-MS molecular weight of 92,300 Da and it is a homodimer of two homologous polypeptide chains of 357 amino acids each. It is produced through recombinant DNA technology in mammalian CHO cells. The drug has activity as a selective co-stimulation modulator with inhibitory activity on T lymphocytes. Although approved for the treatment of rheumatoid arthritis, Repligen has entered a slightly different formulation of CTLA4-Ig into clinical trials (RG2077).

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) 16.7 (12-23) days in healthy subjects; 13.1 (8-25) days in RA subjects; 14.3 days when subcutaneously administered to adult RA patients.
Volume Distribusi * 0.07 L/kg [RA Patients, IV administration] * 0.09 L/kg [Healthy Subjects, IV administration] * 0.11 L/kg [RA patients, subcutaneous administration]
Klirens (Clearance) * 0.23 mL/h/kg [Healthy Subjects after 10 mg/kg Intravenous Infusion] * 0.22 mL/h/kg [RA Patients after multiple 10 mg/kg Intravenous Infusions] * 0.4 mL/h/kg [juvenile idiopathic arthritis patients]. The mean systemic clearance is 0.28 mL/h/kg when a subcutaneously administered to adult RA patients. The clearance of abatacept increases with increasing body weight.

Absorpsi

When a single 10 mg/kg intravenous infusion of abatacept is administered in healthy subjects, the peak plasma concentration (Cmax) was 292 mcg/mL. When multiple doses of 10 mg/kg was given to rheumatoid arthritis (RA) patients, the Cmax was 295 mcg/mL. The bioavailability of abatacept following subcutaneous administration relative to intravenous administration is 78.6%.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Kidney and liver

Interaksi Obat

1028 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Abatacept.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Abatacept.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Abatacept.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Abatacept.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Abatacept.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Abatacept.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Abatacept.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Abatacept.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Abatacept.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Abatacept.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Abatacept.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Abatacept.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Abatacept.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Abatacept.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Abatacept.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Abatacept.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Abatacept.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Abatacept.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Abatacept.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Abatacept.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Abatacept.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Abatacept.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Abatacept.
Cladribine Abatacept may increase the immunosuppressive activities of Cladribine.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Abatacept.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Abatacept.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Abatacept.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Abatacept.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Abatacept.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Abatacept.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Abatacept.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Abatacept.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Abatacept.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Abatacept.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Abatacept.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Abatacept.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Abatacept.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Abatacept.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Abatacept.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Abatacept.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Abatacept.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Abatacept.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Abatacept.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Abatacept.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Abatacept.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Abatacept.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Abatacept.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Abatacept.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Abatacept.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Abatacept.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Abatacept.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Abatacept.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Abatacept.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Abatacept.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Abatacept.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Abatacept.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Abatacept.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Abatacept.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Abatacept.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Abatacept.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Abatacept.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Abatacept.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Abatacept.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Abatacept.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Abatacept.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Abatacept.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Abatacept.
Stepronin The risk or severity of adverse effects can be increased when Abatacept is combined with Stepronin.
Castanospermine The risk or severity of adverse effects can be increased when Abatacept is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Abatacept is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Abatacept is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Abatacept is combined with Brequinar.
Interferon alfa The risk or severity of adverse effects can be increased when Abatacept is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Abatacept is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Abatacept is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Abatacept is combined with Human interferon omega-1.
Canakinumab The risk or severity of adverse effects can be increased when Abatacept is combined with Canakinumab.
Tocilizumab The risk or severity of adverse effects can be increased when Abatacept is combined with Tocilizumab.
Rilonacept The risk or severity of adverse effects can be increased when Abatacept is combined with Rilonacept.
Mepolizumab The risk or severity of adverse effects can be increased when Abatacept is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Abatacept is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Abatacept is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Abatacept is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Abatacept is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Abatacept is combined with Eribulin.
Teriflunomide The risk or severity of adverse effects can be increased when Abatacept is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Abatacept is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Abatacept is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Abatacept is combined with Obinutuzumab.
Secukinumab The risk or severity of adverse effects can be increased when Abatacept is combined with Secukinumab.
Vedolizumab The risk or severity of adverse effects can be increased when Abatacept is combined with Vedolizumab.
Siltuximab The risk or severity of adverse effects can be increased when Abatacept is combined with Siltuximab.
Blinatumomab The risk or severity of adverse effects can be increased when Abatacept is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Abatacept is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Abatacept is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Abatacept is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Abatacept is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Abatacept is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Abatacept is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Abatacept is combined with Ravulizumab.

Target Protein

T-lymphocyte activation antigen CD80 CD80
T-lymphocyte activation antigen CD86 CD86
Cytotoxic T-lymphocyte protein 4 CTLA4

Referensi & Sumber

Synthesis reference: Sang-Lin Kim, Hyun-Kwang Tan, Sang-Min Lim, Wuk-Sang Ryu, Hahn-Sun Jung, Song-Jae Lee, Cheon-Ik Park, Seung-Hoon Kang, Dong Il Kim, "Plant Recombinant Human CTLA4IG and a Method for Producing the Same." U.S. Patent US20100189717, issued July 29, 2010.
Artikel (PubMed)
  • PMID: 15230295
    Dall'Era M, Davis J: CTLA4Ig: a novel inhibitor of costimulation. Lupus. 2004;13(5):372-6.
  • PMID: 16557658
    Moreland L, Bate G, Kirkpatrick P: Abatacept. Nat Rev Drug Discov. 2006 Mar;5(3):185-6.
  • PMID: 17014006
    Weisman MH, Durez P, Hallegua D, Aranda R, Becker JC, Nuamah I, Vratsanos G, Zhou Y, Moreland LW: Reduction of inflammatory biomarker response by abatacept in treatment of rheumatoid arthritis. J Rheumatol. 2006 Nov;33(11):2162-6. Epub 2006 Oct 1.
  • PMID: 16932686
    Weyand CM, Goronzy JJ: T-cell-targeted therapies in rheumatoid arthritis. Nat Clin Pract Rheumatol. 2006 Apr;2(4):201-10.
  • PMID: 16971318
    Scheinfeld N: Abatacept: A review of a new biologic agent for refractory rheumatoid arthritis for dermatologists. J Dermatolog Treat. 2006;17(4):229-34.
  • PMID: 20080922
    Maxwell LJ, Singh JA: Abatacept for rheumatoid arthritis: a Cochrane systematic review. J Rheumatol. 2010 Feb;37(2):234-45. doi: 10.3899/jrheum.091066. Epub 2010 Jan 15.
  • PMID: 19821401
    Maxwell L, Singh JA: Abatacept for rheumatoid arthritis. Cochrane Database Syst Rev. 2009 Oct 7;(4):CD007277. doi: 10.1002/14651858.CD007277.pub2.
  • PMID: 17212998
    Nogid A, Pham DQ: Role of abatacept in the management of rheumatoid arthritis. Clin Ther. 2006 Nov;28(11):1764-78.
Menampilkan 8 dari 10 artikel.

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