Skip to main content

What's the mechanism of action for tucatinib?

Medically reviewed by Leigh Ann Anderson, PharmD. Last updated on Jan 15, 2025.

Official Answer by Drugs.com

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.

Related information: List of HER2 Inhibitors

How is tucatinib used?

The FDA approved Tukysa for colorectal cancer under an "accelerated approval". This means that continued approval for this use may depend upon results of further clinical studies looking at its effectiveness in colorectal cancer.

This is not all the information you need to know about Tukysa (tucatinib) for safe and effective use and does not take the place of talking to your doctor about your treatment. Review the full product information here, and discuss this information and any questions you have with your doctor or other health care provider.

Related questions

References
  • Tukysa (tucatinib) product information. Seagen. Bothell, WA. Revised 1/2023. Accessed Jan 25, 2023 at https://docs.seagen.com/TUKYSA_Full_Ltr_Master.pdf
  • Tukysa.com. Mechanism of Action. Seagen Inc. Accessed April 22, 2021 at https://www.tukysahcp.com/videolibrary

Read next

What is the FOLFOX chemo regimen and is it effective?

FOLFOX is a combination chemotherapy regimen primarily used to treat colorectal cancer, in both early-stage and advanced-stage settings. It includes folinic acid (leucovorin), fluorouracil, and oxaliplatin. These drugs work together to destroy cancer cells by disrupting their DNA synthesis and function.

Continue reading

What is the success rate of Keytruda?

In general, PD-1 immune checkpoint inhibitors like Keytruda have been shown to significantly prolong overall survival (OS) in some patients with various cancer types, but Keytruda does not always work for everyone. Continue reading

What is the CAPOX (XELOX) chemotherapy regimen?

The CAPOX chemotherapy regimen includes capecitabine and oxaliplatin. It is a widely used and effective chemotherapy protocol for advanced colorectal and other gastrointestinal cancers. It combines oral capecitabine and intravenous oxaliplatin, administered in 3-week cycles.

Continue reading

See also:

Related medical questions

Drug information

Related support groups