BIO-7488 (BIO7488) is the first potent, selective, and CNS-penetrant IRAK4 inhibitor with IC50 of 0.5 nM (1 mM ATP).
BIO-7488 potently inhibits R848 stimulus of 1L-1β production with IC50 of 200 nM in human whole blood assay.
BIO-7488 has limited MDR1 or BCRP efflux liability, supporting the favorable measured rat Kpu,u of 0.3 in rats.
BIO-7488 (10, 30, or 100 mg/kg) demonstrated robust and dose-dependent suppression of multiple cytokines, including IL-1β, TNFα, and IL-6 in LPS challenge rat model.
