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Synonyms: BMS-188667 | CTLA4-IgG4m | Orencia® | RG-1046 | RG-2077
abatacept is an approved drug (FDA (2005), EMA (2005))
Compound class:
Peptide
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.
Ligand Activity Visualisation ChartsThese 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. ✖
View more information in the IUPHAR Pharmacology Education Project: abatacept |
| No information available. |
Summary of Clinical Use  |
| 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 |
| 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 |
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For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) |
