Tucatinib/tucatinib launch time in China

Tucatinib/Tucatinib is a high-profile drug that has shown remarkable results in the treatment of brain metastases from HER2+ advanced breast cancer. As ofmid-April 2024, tucatinib has not yet been launched in China. In China, drug marketing requires approval from the State Food and Drug Administration. But we can expect that this drug will be approved for marketing in China in the near future, bringing hope to more patients with HER2+ advanced breast cancer.

Tucatinib is an oral, small molecule inhibitor of human epidermal growth factor receptor 2 (HER2), a tyrosine kinase that is overexpressed in some cancers and causes excessive cell growth and proliferation. HER2 is an oncogenic driver that is overexpressed in 15% to 20% of breast cancer cases and more rarely in other solid tumors such as colorectal cancer.

In a large, randomized, double-blind, placebo-controlled trial, the combination of trastuzumab and capecitabine was found to induce objective responses in 60% of patients with refractory metastatic or advanced unresectable HER2-positive breast cancer, including those with brain metastases. Tucatinib combined with trastuzumab and capecitabine was approved in the United States in 2020 by the U.S. Food and Drug Administration (FDA) for adult patients with advanced or metastatic HER2-positive breast cancer after the failure of previous anti-HER2-based regimens.

Unlike monoclonal antibodies, tucatinib can penetrate the blood-brain barrier, which may be the reason for its efficacy in treating brain metastases refractory to anti-HER2 monoclonal antibody therapy. In 2023, the indications of tucatinib will be expanded to the treatment of refractory HER2-positive advanced unresectable metastatic colorectal cancer in combination with trastuzumab.