What are the indications for tucatinib/tucatinib?

As a tyrosine kinase inhibitor targeting HER2, Tucatinib has a wide range of clinical indications and is mainly used to treat HER2-positive cancer patients, especially in the treatment of advanced or metastatic cancer. It has shown important clinical value. The use of tucatinib is not limited to breast cancer, but also involves other types of tumors such as colorectal cancer, especially when used in combination with other anti-cancer drugs, showing its strong therapeutic potential.

1. Metastatic breast cancer (MBC)

Tucatinib was first approved for the treatment of metastatic HER2-positive breast cancer in combination with trastuzumab and capecitabine. The applicable patient group is patients with advanced unresectable or metastatic HER2-positive breast cancer who have often experienced multiple treatment failures, including patients with brain metastases. The effect of tucatinib is particularly significant in these patients because it can cross the blood-brain barrier, effectively inhibit HER2-positive breast cancer with brain metastasis, and improve the quality of life and prognosis of patients. Its mechanism of action reduces tumor cell proliferation and survival by selectively inhibiting HER2 signaling.

2. Metastatic colorectal cancer (CRC)

In addition to breast cancer, tucatinib also shows good clinical promise in the treatment of HER2-positive metastatic colorectal cancer. Particularly when combined with trastuzumab, tucatinib has been shown to significantly improve efficacy in patients who have progressed on chemotherapy drugs such as fluoropyrimidine, oxaliplatin, and irinotecan. Tucatinib provides a new treatment option for these patients, especially after the failure of conventional chemotherapy, the treatment of metastatic colorectal cancer patients often faces greater challenges, and the introduction of tucatinib brings hope to these patients.

Reference: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/213411s004lbl.pdf