SB-242235

Description: SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 uM and has the potential for treatment of cytokine-mediated diseases like autoimmune or inflammatory diseases. SB-242235 showed favorable pharmacokinetic properties. Systemic plasma clearance was high in rat, but in the non-rodent species SB-242235 demonstrated low to moderate clearance with plasma half-lives > 4h. Oral bioavailability in each preclinical species was high. In rat and monkey, SB-242235 demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses.

References: Xenobiotica. 2002 Mar; 32(3):221-33; Osteoarthritis Cartilage. 2000 Nov; 8(6):434-43.