Fuzapladib (IS-741), an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site.
Fuzapladib (IS-741) (1 μM, 3 h) can significantly inhibit the adhesion of HL-60 cells to HUVEC under the stimulation of lipopolysaccharide[3].
Fuzapladib (IS-741) (p.o., 50 mg/kg, 7 days) inhibits neutrophil infiltration into inflamed lesions, and is effective for attenuating rat trinitrobenzene sulfonic acid (TNBS) ileitis[4].