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QuickView for abatacept (compound)


PubChem Substance
Name: abatacept
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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DrugBank
Identification
Name: abatacept
Name (isomeric): DB01281
Drug Type: biotech
Synonyms:
CTLA4-IgG4m; RG-1046; CTLA4Ig; RG1046; CTLA4-Ig; RG-2077; RG2077; CTLA4IgG4m
Brand: Orencia (Bristol-Myers Squibb), Orencia
Category: Antirheumatic Agents
CAS number: 332348-12-6
Pharmacology
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.
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
Interactions
Drug interaction:
TrastuzumabTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
ThalidomideThalidomide may increase the adverse effects of Abatacept. Increased risk of serious infection. Concomitant therapy should be avoided.

Targets