AC0010 is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (EGFR) inhibitor, structurally distinct from previously reported pyrimidine-based irreversible EGFR inhibitors such as osimertinib and rociletinib. AC0010 selectively inhibits EGFR active and T790M mutations with up to 298-fold increase in potency compared to wild-type EGFR. In a xenografte model, oral administration of AC0010 at daily dose of 500 mg/kg resulted in complete remission of tumors with EGFR active and T790M mutations for over 143 days with no weight loss. Three major metabolites of AC0010 were tested and showed no wild-type EGFR inhibition and off-target effects such as inhibition of IGF-1R. AC0010 is safe in non-small cell lung cancer (NSCLC) patients at the dose range between 50 mg and 550 mg once per day and no hyperglycemia and other severe adverse effects were detected such as grade 3 QT prolongation. The objective responses were observed in NSCLC patients with EGFR T790M mutation.
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