Abstract
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.
Original language | English (US) |
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Pages (from-to) | 437-441 |
Number of pages | 5 |
Journal | Expert Opinion on Investigational Drugs |
Volume | 31 |
Issue number | 5 |
DOIs | |
State | Published - 2022 |
Keywords
- Colorectal cancer
- ERBB2
- HER-2
- ONT-380
- tucatinib
ASJC Scopus subject areas
- Pharmacology
- Pharmacology (medical)