Lifitegrast

Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast 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 inhibits Jurkat T cell attachment to ICAM-1 with an IC₅₀ of 2.98 nM. Lifitegrast can be used for researching dry eye disease^[1]. IC50 & Target: IC50: 2.98 nM (LFA-1)^[1] In Vitro: Lifitegrast (SAR 1118) inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins (lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1), thus lessening overall inflammatory responses^[1].
Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC₅₀ of 2.98 nM^[1]. In Vivo: Lifitegrast (SAR 1118), has potent anti-inflammatory activity on corneal inflammation induced by antibiotic-killed P. aeruginosa and S. aureus in the presence of a silicone hydrogel lens with the optimal application being a 1% solution applied either 2 or 3 times prior^[2].
Lifitegrast (SAR 1118) ophthalmic drops administered thrice daily deliver therapeutic levels of Lifitegrast (SAR 1118) in the retina and can alleviate the retinal complications associated with diabetes^[3].