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Category:Abatacept
Comment taken from DrugBank
Curator Ab +
DefiningCitation http://www.drugbank.ca/drugs/DB01281  +
Definition Abatacept is a soluble fusion protein, whi 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). It is produced through recombinant DNA technology in mammalian cells. The drug has activity as a selective costimulation 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). Pharmacology: Abatacept is the first in a new class of drugs known as Selective Co-stimulation Modulators. Ordinarily, full T-cell activation requires binding of the T-cell receptor to an antigen-MHC complex on the antigen-presenting cell as well as a co-stimulatory signal provided by the binding of the CD28 protein on the surface of the T-cell with the CD80/86 proteins on the surface of the antigen-presenting cell. CTLA4 is a naturally occurring protein which is expressed on the surface of T-cells some hours or days after full T-cell activation and is capable of binding to CD80/86 on antigen-presenting cells with much greater affinity than CD28. Binding of CTLA4-Ig to CD80/86 provides a negative feedback mechanism which results in T-cell deactivation. Abatacept was developed by Bristol-Myers-Squibb and is licensed in the US for the treatment of Rheumatoid Arthritis in the case of inadequate response to anti-TNF-alpha therapy. Mechanism of action: Abatacept is a selective costimulation modulator, shown to inhibit Tcell (T lymphocyte) activation by binding to CD80 and CD86, thereby blocking interaction with CD28. Blockade of this interaction has been shown to inhibit the autoimmune T-Cell activation that has been implcated in the pathogenesis of rheumatoid arthritis. Drug type: Biotech. Drug category: Antirheumatic Agents otech. Drug category: Antirheumatic Agents
Has role Drug +
Id DB01281  +
Label Abatacept  +
Modification dateThis property is a special property in this wiki. 14 April 2014 20:29:44  +
ModifiedDate 14 April 2014  +
RelatedTo T-lymphocyte activation antigen CD86 +, T-lymphocyte activation antigen CD80 +
SuperCategory Molecular entity  +
Synonym CTLA4-Ig  +, CTLA4-IgG4m  +, CTLA4Ig  +, CTLA4IgG4m  +, RG-1046  +, RG-2077  +, RG1046  +, RG2077  +, abatacept  +, Orencia  +, Orencia (Bristol-Myers Squibb)  +
Categories Molecular entity
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