Avitinib

Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR) receptor tyrosine kinase. It inhibits EGFR L858R/T790M double mutations with an IC₅₀ value of 0.18 nM which is nearly 43-fold potent over wild-type EGFR (IC₅₀ value of 7.68 nM) in kinase assays. In a xenograft model, oral administration at a daily dose of 500 mg/kg results in complete remission of tumors with EGFR-active and T790M mutations.