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

Research output: Contribution to journalArticlepeer-review


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 languageEnglish (US)
Pages (from-to)437-441
Number of pages5
JournalExpert Opinion on Investigational Drugs
Issue number5
StatePublished - 2022


  • Colorectal cancer
  • ERBB2
  • HER-2
  • ONT-380
  • tucatinib

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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