Lifitegrast

A potent LFA-1/ICAM-1 antagonist with IC50 of 9 nM in HuT78 cells; exhibits good in vitro safety profile and low potency on CYP3A4, CYP2C9 and hERG; development as an ophthalmic solution for treating dry eye.Other Indication Approved (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.Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. (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.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.