tesevatinib + trastuzumab

The combination of tesevatinib and trastuzumab is an investigational drug therapy primarily studied for HER2-positive metastatic breast cancer, with particular interest in its potential for treating brain metastases. Tesevatinib (formerly KD019) is a tyrosine kinase inhibitor (TKI) that targets EGFR, HER2, and SRC, notable for its ability to cross the blood-brain barrier (BBB). Trastuzumab (Herceptin) is a well-established anti-HER2 monoclonal antibody targeting the extracellular domain of HER2 receptors. The rationale for this combination stems from HER2-positive tumors' continued dependence on HER2 signaling even after developing resistance to trastuzumab, and tesevatinib's BBB permeability addressing the unmet need for treating brain metastases as most approved anti-HER2 agents do not efficiently cross the BBB.