Tucatinib: an investigational novel therapeutic agent for the treatment of HER-2 colorectal cancer

Introduction: Human epidermal growth factor receptor 2 (HER-2) is an oncogenic driver and target in gastroesophageal and breast cancer; there is also evidence for a role in non-small cell lung cancer (NSCLC). In colorectal cancer (CRC), the incidence of HER-2 overexpression occurs in up to 10% of patients. While its role of HER-2 as a biomarker for prognosis in CRC remains uncertain, it remains of interest as a potential therapeutic target. Tucatinib is an investigational agent which functions as a selective HER-2 inhibitor. Areas covered: In this article, the authors discuss the incidence of HER-2 in CRC and its rationale in the treatment of CRC. An overview of the market is offered, followed by a scientific summary of tucatinib including its clinical development in CRC. Expert opinion: Tucatinib is a selective HER-2 inhibitor that has unique properties which distinguishes it from other HER-2 directed therapies. In the clinical setting, it has demonstrated clinical efficacy of HER-2 inhibition across various solid tumors including CRC. Given the evidence of clinical activity observed with tucatinib in breast cancer and frequency of HER-2 overexpression in CRC, the investigation of tucatinib as a monotherapy and in combination with other therapeutic agents remains of interest.

Automated summary

HER-2 plays an important role in different types of cancers, including gastroesophageal, breast, and colorectal cancer. Tucatinib, as a selective HER-2 inhibitor, has shown potential therapeutic effects in a clinical setting. Although its role as a biomarker for prognosis in colorectal cancer remains uncertain, it is still a potential therapeutic target.