LAE118

LAE118 is a novel allosteric pan-mutant selective PI3Kα inhibitor developed by Laekna. It demonstrates excellent in vitro anti-proliferation activities against both kinase and helical domain mutant PI3Kα cell lines, and remains active against cells resistant to orthosteric PI3Kα inhibitors. In preclinical studies, LAE118 shows strong anti-tumor growth effects in xenograft models at doses much lower than other allosteric inhibitors, with less effect on glucose homeostasis compared to orthosteric PI3Kα inhibitors. It also exhibits good tolerability in preclinical toxicology studies. The drug is currently in IND-enabling stage for the treatment of cancers with PIK3CA mutations, which are prevalent in breast, colorectal, lung, endometrial, and other cancers[2][6][10].