abatacept   Click here for help

GtoPdb Ligand ID: 6891

Synonyms: BMS-188667 | CTLA4-IgG4m | Orencia® | RG-1046 | RG-2077
Approved drug Immunopharmacology Ligand
abatacept is an approved drug (FDA (2005), EMA (2005))
Compound class: Peptide or derivative
Comment: Abatacept is a recombinant protein fusing 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) [3]. In essence, abatacept is a CTLA-4 mimetic, that enhances CTLA-4's inhibitory signal to T cells, thereby down-modulating T cell mediated inflammation.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species

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View more information in the IUPHAR Pharmacology Education Project: abatacept

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Summary of Clinical Use Click here for help
Used to treat moderate to severe rheumatoid arthritis and juvenile rheumatoid arthritis. In July 2017, FDA approval was extended to include treatment of active psoriatic arthritis.
A Phase 2 clinical trial (NCT00505375) has been completed, evaluating the ability of abatacept to stop autoimmune destruction of any remaining active β cells in patients recently diagnosed with type 1 diabetes mellitus- see [4] for an explanation of the rationale behind this therapeutic approach, and [1] which points to some of its drawbacks.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Binding of abatacept to CD80/86 (B7 proteins on antigen presenting cells) provides a negative feedback mechanism which results in T-cell deactivation. This action reduces active inflammation.
External links Click here for help
For extended ADME data see the following:

Electronic Medicines Compendium (eMC)
Drugs.com
European Medicines Agency (EMA)