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| http://linked.open...gbank/description
| - 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). 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). (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # Dall'Era M, Davis J: CTLA4Ig: a novel inhibitor of costimulation. Lupus. 2004;13(5):372-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15230295 # Moreland L, Bate G, Kirkpatrick P: Abatacept. Nat Rev Drug Discov. 2006 Mar;5(3):185-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16557658 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17014006 # Weyand CM, Goronzy JJ: T-cell-targeted therapies in rheumatoid arthritis. Nat Clin Pract Rheumatol. 2006 Apr;2(4):201-10. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16932686 # Scheinfeld N: Abatacept: A review of a new biologic agent for refractory rheumatoid arthritis for dermatologists. J Dermatolog Treat. 2006;17(4):229-34. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16971318 # Maxwell LJ, Singh JA: Abatacept for rheumatoid arthritis: a Cochrane systematic review. J Rheumatol. 2010 Feb;37(2):234-45. Epub 2010 Jan 15. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20080922 # Maxwell L, Singh JA: Abatacept for rheumatoid arthritis. Cochrane Database Syst Rev. 2009 Oct 7;(4):CD007277. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19821401 # Nogid A, Pham DQ: Role of abatacept in the management of rheumatoid arthritis. Clin Ther. 2006 Nov;28(11):1764-78. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17212998 # Hervey PS, Keam SJ: Abatacept. BioDrugs. 2006;20(1):53-61; discussion 62. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16573350 # Reynolds J, Shojania K, Marra CA: Abatacept: a novel treatment for moderate-to-severe rheumatoid arthritis. Pharmacotherapy. 2007 Dec;27(12):1693-701. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18041889 # FDA label (en)
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| http://linked.open...gy/drugbank/group
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| http://linked.open...drugbank/halfLife
| - 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. (en)
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| http://linked.open...ugbank/indication
| - For the management of the signs and symptoms of moderate-to-severe active rheumatoid arthritis, inducing major clinical response, slowing the progression of structural damage, and improving physical function in adult patients. It is indicated both as a monotherapy and for use in combination with a continued regimen of DMARDs (not including TNF antagonists). Also used for the management of the signs and symptoms of moderately to severely active polyarticular juvenile idiopathic arthritis in children. (en)
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Abatacept is a selective costimulation modulator, like CTLA-4, the drug has shown to inhibit T-cell (T lymphocyte) activation by binding to CD80 and CD86, thereby blocking interaction with CD28. Blockade of this interaction has been shown to inhibit the delivery of the second co-stimulatory signal required for optimal activation of T-cells. This results in the inhibition of autoimmune T-Cell activation that has been implcated in the pathogenesis of rheumatoid arthritis. (en)
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| http://linked.open...drugbank/packager
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| http://linked.open...y/drugbank/patent
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| http://linked.open...outeOfElimination
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| http://linked.open.../drugbank/synonym
| - CTLA4-Ig (en)
- CTLA4-IgG4m (en)
- CTLA4Ig (en)
- CTLA4IgG4m (en)
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| http://linked.open...drugbank/toxicity
| - 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. (en)
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| http://linked.open...umeOfDistribution
| - * 0.07 L/kg [RA Patients, IV administration] * 0.09 L/kg [Healthy Subjects, IV administration] * 0.11 L/kg [RA patients, subcutaneous administration] (en)
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...ynthesisReference
| - 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. (en)
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| http://linked.open...y/mesh/hasConcept
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| foaf:page
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...ugbank/absorption
| - 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%. (en)
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...drugbank/category
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| http://linked.open...rugbank/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. (en)
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