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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References |
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Liver X receptors as regulators of macrophage inflammatory and metabolic pathways. Biochim Biophys Acta, 1812 (8): 982-94. [PMID:21193033] |
2. Breitenstein W, Huerzeler M, Kelly T, Mancuso R, Schneider G, Weitz-Schmidt G. (2015)
Small molecule lfa-1 inhibitors. Patent number: WO2015189265. Assignee: Allocyte Pharmaceuticals Ag. Priority date: 12/06/2014. Publication date: 17/12/2015. |
3. Giblin PA, Lemieux RM. (2006)
LFA-1 as a key regulator of immune function: approaches toward the development of LFA-1-based therapeutics. Curr Pharm Des, 12 (22): 2771-95. [PMID:16918410] |
4. Kapp TG, Rechenmacher F, Sobahi TR, Kessler H. (2013)
Integrin modulators: a patent review. Expert Opin Ther Pat, 23 (10): 1273-95. [PMID:24050747] |
5. Lam H, Bleiden L, de Paiva CS, Farley W, Stern ME, Pflugfelder SC. (2009)
Tear cytokine profiles in dysfunctional tear syndrome. Am J Ophthalmol, 147 (2): 198-205. e1. [PMID:18992869] |
6. Murphy CJ, Bentley E, Miller PE, McIntyre K, Leatherberry G, Dubielzig R, Giuliano E, Moore CP, Phillips TE, Smith PB et al.. (2011)
The pharmacologic assessment of a novel lymphocyte function-associated antigen-1 antagonist (SAR 1118) for the treatment of keratoconjunctivitis sicca in dogs. Invest Ophthalmol Vis Sci, 52 (6): 3174-80. [PMID:21330663] |
7. Newman M, Hunke W. (2014)
Lfa-1 inhibitor formulations. Patent number: WO2014100135. Assignee: Sarcode Bioscience Inc.. Priority date: 19/12/2012. Publication date: 26/06/2014. |
8. Sheppard JD, Torkildsen GL, Lonsdale JD, D'Ambrosio Jr FA, McLaurin EB, Eiferman RA, Kennedy KS, Semba CP, OPUS-1 Study Group. (2014)
Lifitegrast ophthalmic solution 5.0% for treatment of dry eye disease: results of the OPUS-1 phase 3 study. Ophthalmology, 121 (2): 475-83. [PMID:24289915] |
9. Zhong M, Gadek TR, Bui M, Shen W, Burnier J, Barr KJ, Hanan EJ, Oslob JD, Yu CH, Zhu J et al.. (2012)
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye. ACS Med Chem Lett, 3 (3): 203-6. [PMID:24900456] |