Synonyms: compound 1g [PMID: 24900456] | SAR 1118 | SAR-1118 | SAR-1118-023 | Xiidra®
lifitegrast is an approved drug (FDA (2016))
Compound class:
Synthetic organic
Comment: It is postulated that lifitegrast (SAR 1118) interacts with the lymphocyte function-associated antigen-1 (LFA-1) to inhbit the LFA-1/ICAM-1 adhesion interaction and was approved for the treatment of Dry Ey in 2016 [7,9]. LFA-1 is a heterodimeric member of the β2 integrin family which is essential for adhesion, migration, and proliferation of T cells at sites of inflammation, and is involved in T cell specific immune responses through the formation of adhesive interactions and immunological synapses. Intercellular adhesion molecule‑1 (ICAM‑1) is the cognate ligand of LFA-1.The compound formulation is claimed in patent WO2014100135 [7].
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. ✖ |
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Bioactivity Comments |
No specific binding data are provided in [9] to substantiate the lifitegrast/LFA-1 interaction. Target engagement is inferred from biological assays showing inhibition of T cell adhesion and inhibition of inflammatory mediator secretion. In in vitro assays, lifitegrast inhibits Jurkat T cell and HuT 78 T cell adhesion to immobilised ICAM-Ig with IC50s of 2.98nM and 9nM respectively [9]. Lifitegrast was designed to have minimal systemic exposure, to limit action at sites other than at the site of administration [7]. |
Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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