Nicholaas Stahl

Discovery of Tetrasubstituted Quinazolin-4(3 H )-ones as Wild-type-sparing, Highly Selective PI3KαH1047R Inhibitors

Abstract Inhibiting PI3Kα has demonstrated promising therapeutic effects for patients with HR+/HER2− and PIK3CA-mutated advanced or metastatic breast cancer. However, hyperglycemia and other notable adverse events (AE) associated with concomitant wild-type inhibition remain a cha...