Name: | abatacept |
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PubChem Substance ID: | 10550015 |
Synonyms: |
LEA29Y; LEA 29Y; CD152 antigen; CTLA-4 (antigen) (29-tyrosine,104-glutamic acid) (human extracellular domain-containing fragment) fusion protein with immunoglobulin G1 (human monoclonal Fc domain-containing fragment), bimol. (120->120?)-disulfide; cytotoxic T-lymphocyte antigen 4; BMS-224818; Belatacept; BMS 224818; BMS224818; Belatacept [USAN].
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Name: | abatacept |
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Name (isomeric): | DB01281 |
Drug Type: | biotech |
Synonyms: |
CTLA4-IgG4m; RG-1046; CTLA4Ig; RG1046; CTLA4-Ig; RG-2077; RG2077; CTLA4IgG4m
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Brand: | Orencia (Bristol-Myers Squibb), Orencia |
Category: | Antirheumatic Agents |
CAS number: | 332348-12-6 |
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. |
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Pharmacology: |
Abatacept is the first in a new class of drugs known as Selective Co-stimulation Modulators. Known as a recombinant fusion protein, the drug consists of the extracellular domain of human cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) linked to a modified Fc portion of human immunoglobulin G1 (IgG1. The Fc portion of the ...
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Mechanism of Action: |
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 re...
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Half Life: | 16.7 (12-23) days in healthy subjects, 13.1 (8-25) days in RA subjects. |
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] |
Toxicity: | Doses up to 50 mg/kg have been administered without apparent toxic effect. |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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