Sodium Lifitegrast

Lifitegrast (SAR 1118) sodium is a potent integrin antagonist. Lifitegrast sodium blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast sodium inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast sodium can be used for researching dry eye disease[1].

αLβ2

[1] Perez VL, et al. Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease. Ocul Surf. 2016 Apr;14(2):207-15. DOI:10.1016/j.jtos.2016.01.001
[2] Sun Y, et al. Corneal inflammation is inhibited by the LFA-1 antagonist, lifitegrast (SAR 1118). J Ocul Pharmacol Ther. 2013 May;29(4):395-402. DOI:10.1089/jop.2012.0102
[3] Rao VR, et al. Delivery of SAR 1118 to the retina via ophthalmic drops and its effectiveness in a rat streptozotocin(STZ) model of diabetic retinopathy (DR). Invest Ophthalmol Vis Sci. 2010 Oct;51(10):5198-204. DOI:10.1167/iovs.09-5144
[4] MIN ZHONG*. Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye[J]. ACS Medicinal Chemistry Letters, 2012, 3 3: 203-206. DOI: 10.1021/ml2002482
[5] CHRISTOPHER J MURPHY. The pharmacologic assessment of a novel lymphocyte function-associated antigen-1 antagonist (SAR 1118) for the treatment of keratoconjunctivitis sicca in dogs.[J]. Investigative ophthalmology & visual science, 2011, 52 6: 3174-3180. DOI: 10.1167/iovs.09-5078