What's the mechanism of action for tucatinib

Update: 19 Mar,2026 Source: Bigbear Views: 117

Tucatinib (Tukysa) is a human epidermal growth factor receptor-2 (HER2) inhibitor that works by blocking the HER2 protein to help slow or stop cancer cell growth in patients with advanced breast cancer or colorectal cancer. Some cancers have an over-expression of the HER2 protein causing increased growth and spread of cancer cells.

Tucatinib, an oral targeted drug therapy, is very selective for the HER2 protein and works inside the cell. Tucatinib binds to tyrosine kinase (an enzyme) of HER2, reducing PI3-kinase and MAP-kinase signaling. Reduced signaling helps to block cell growth and leads to cell death. Tucatinib is classified as a HER2 tyrosine kinase inhibitor.

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