Using Iambic Therapeutics’ AI/HTE platform, researchers at the company have engineered a next-generation HER2 inhibitor with superb selectivity for HER2, as well as broad mutant coverage and brain penetrance. The compound, IAM-1363, binds to HER2 in a type II DFG-out conformation, which represents the first reported type II HER2 tyrosine kinase inhibitor.
Iambic Therapeutics Inc. presented preclinical data on IAM-1363, a selective and irreversible HER2 and pan-HER2 mutant inhibitor in HER2-driven NSCLC models. In vitro studies across a panel of HER2-altered NSCLC cell lines demonstrated that IAM-1363 exhibits potent antiproliferative activity in both HER2-amplified and HER2-mutant models.
