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

References
1. Davis IC, Randell J, Davis SN. (2015)
Immunotherapies currently in development for the treatment of type 1 diabetes.
Expert Opin Investig Drugs, 24 (10): 1331-41. [PMID:26364507]
2. Douthwaite J, Moisan J, Privezentzev C, Soskic B, Sabbah S, Cohen S, Collinson A, England E, Huntington C, Kemp B et al.. (2017)
A CD80-Biased CTLA4-Ig Fusion Protein with Superior In Vivo Efficacy by Simultaneous Engineering of Affinity, Selectivity, Stability, and FcRn Binding.
J Immunol, 198 (1): 528-537. [PMID:27881707]
3. Linsley PS, Brady W, Urnes M, Grosmaire LS, Damle NK, Ledbetter JA. (1991)
CTLA-4 is a second receptor for the B cell activation antigen B7.
J Exp Med, 174 (3): 561-9. [PMID:1714933]
4. Ludvigsson J. (2016)
Therapies to Preserve β-Cell Function in Type 1 Diabetes.
Drugs, 76 (2): 169-85. [PMID:26645223]
5. Vicente Rabaneda EF, Herrero-Beaumont G, Castañeda S. (2013)
Update on the use of abatacept for the treatment of rheumatoid arthritis.
Expert Rev Clin Immunol, 9 (7): 599-621. [PMID:23899231]