AZD-8330 is a novel, selective, highly efficacious, uncompetitive MEK 1/2 inhibitor. In cell-free kinase assays, AZD-8330 inhibits MEK 1/2 with an IC50 of 7 nM.[1] AZD-8330 has antiviral activity against influenza virus with an EC50 of 40 nM.[2] In a Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model, AZD-8330 (1.25 mg/kg) inhibits ERK phosphorylation by >90% for between 4 and 8 hours.[1] |