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Abatacept
- 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.
- pharmacologypharmacology:
- mechanism: 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.
- toxicity: Doses up to 50 mg/kg have been administered without apparent toxic effect.
- absorprion:
- halflife: 16.7 (12-23) days in healthy subjects, 13.1 (8-25) days in RA subjects.
- roouteelimination:
- volumedistribution: * 0.02-0.13 L/kg [RA Patients] * 0.06-0.13 L/kg [Healthy 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]