NCIt definition : A tetrahydroisoquinoline derivative and lymphocyte function-associated antigen-1 (LFA-1)
antagonist, that can be used as an ophthalmic solution for the treatment of dry eye
disease (DED; keratoconjunctivitis sicca; dry eye syndrome). Upon ocular administration
and although the exact mechanism of action of lifitegrast in DED is not fully known,
lifitegrast targets and binds to the integrin LFA-1, a cell surface protein found
on leukocytes. This prevents the interaction of LFA-1 with its cognate ligand intercellular
adhesion molecule-1 (ICAM-1). As ICAM-1 may be overexpressed in corneal and conjunctival
tissues in DED, the blockage of the LFA-1/ICAM-1 interaction by lifitegrast may inhibit
T-cell adhesion to ICAM-1 and may abrogate the formation of an immunological synapse.
This may prevent T-cell proliferation, activation and migration and the release of
pro-inflammatory cytokines in the corneal and conjunctival tissues. This may reduce
inflammation, protect the corneal surface from inflammatory-mediated damage and reduce
the symptoms of DED.;