IAM1363

IAM1363 is a highly potent, irreversible, and selective small molecule tyrosine kinase inhibitor (TKI) that targets human epidermal growth factor receptor 2 (HER2) and its oncogenic mutants, while sparing the epidermal growth factor receptor (EGFR). This selectivity minimizes EGFR-mediated toxicities commonly seen with other pan-ERBB or HER2 inhibitors. Designed using an AI-driven drug discovery platform by Iambic Therapeutics, IAM1363 demonstrates over 1000-fold selectivity for HER2 versus EGFR. It exhibits favorable pharmacokinetics, preferential tumor enrichment, effective central nervous system (CNS) penetration—including the ability to cross the blood-brain barrier—and has shown efficacy in preclinical models of both extracranial and intracranial HER2-positive tumors. The drug is being developed primarily for advanced cancers harboring HER2 alterations such as gene mutations or amplifications; these include breast cancer, non-small cell lung cancer (NSCLC), gastric/gastroesophageal junction adenocarcinoma, bladder cancer, and colorectal cancer. Clinical trials are ongoing to evaluate its safety and efficacy as monotherapy and in combination with other targeted therapies[1][2][4][5][6][7][8][9].

Other names

HER2 inhibitor IAM1363HER-2 inhibitor IAM1363HER 2 inhibitor IAM1363IAM-1363IAM1363IAM 1363