Definition

An orally bioavailable, immediate release (IR) capsule formulation containing a selective and irreversible inhibitor of the receptor tyrosine kinase human epidermal growth factor receptor 2 (HER2; ErbB2; HER-2), with potential antineoplastic activity. Upon oral administration, HER2 inhibitor IAM1363 selectively targets, irreversibly binds to and inhibits the activity of wild-type (WT) and various HER2 mutants. This prevents HER2-mediated signaling and may lead to cell death in HER2-expressing tumor cells. HER2, a receptor tyrosine kinase overexpressed on a variety of tumor cell types, plays an important role in tumor cell proliferation and tumor vascularization. IAM1363 is able to penetrate the blood-brain -barrier (BBB) and may be used in HER2-expressing brain tumors and brain metastases. IAM1363 does not inhibit epidermal growth factor receptor (EGFR) and avoids off-target EGFR-mediated toxicity.