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Tucatinib is a small molecule, oral tyrosine kinase inhibitor that selectively targets the human epidermal growth factor receptor 2 (HER2). By binding to the HER2 tyrosine kinase domain, tucatinib blocks downstream signaling pathways such as PI3-kinase and MAP-kinase, which are involved in cell proliferation and survival. This inhibition slows or stops the growth of cancer cells that overexpress HER2. Tucatinib is primarily used in combination with trastuzumab and capecitabine for adults with advanced or metastatic HER2-positive breast cancer, including those with brain metastases who have received prior anti-HER2 therapies. It is also approved in combination with trastuzumab for RAS wild-type HER2-positive unresectable or metastatic colorectal cancer after progression on standard chemotherapy regimens.
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