BMS-688521

BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC₅₀ of 2.5 nM in the adhesion assay and an IC₅₀ of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model^[1]. In Vitro: BMS-688521 in a mouse specific adhesion assay employed mouse splenocytes and a mouse ICAM-1 expression cell line, b.END3. BMS-688521 has an IC₅₀ of 78 nM, representing an approximately 30-fold decrease in activity relative to the human T-cell/HUVEC assay data (ICIC₅₀=2.5 nM)^[1]. In Vivo: BMS-688521 (1-10 mg/kg; p.o.; BID for a three-day) is efficacious in a mouse allergic eosinophilic lung inflammation model^[1].
BMS-688521 (5 mg/kg; p.o.) treatment shows the C_max, T_max, AUC, F values are 0.32 μM, 1.0 μM, 1.5 μM h, and 50%, respectively^[1].
BMS-688521 (1 mg/kg; i.v.) treatment shows the T_1/2, MRT, CL and Vss values are 1.6 hours, 1.7 hours, 50 mL/mim/kg, and 5.1 L/kg, respectively in BALB/c mice^[1].