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Lapatinib: a dual inhibitor of EGFR and HER2 tyrosine kinase activity

Filippo Montemurro1, Giorgio Valabrega, Massimo Aglietta

  • 1Institute for Cancer Research and Treatment (IRCC), University Division of Medical Oncology and Hematology, Strada Provinciale 142, Km 3.95, 10060 Candiolo, Italy. filippo.montemurro@ircc.it

Expert Opinion on Biological Therapy
|January 26, 2007
PubMed

Insights

Lapatinib effectively treats HER2-positive advanced breast cancer. This oral tyrosine kinase inhibitor shows modest activity in other cancers, prompting further research into predictive factors for patient selection.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Lapatinib is an oral tyrosine kinase inhibitor targeting epidermal growth factor receptor (EGFR) and human EGFR-2 (HER2).
  • Both EGFR and HER2 are frequently altered in various human malignant tumors.
  • As a multitargeting agent, lapatinib has theoretical potential for enhanced antitumor activity and delayed tumor resistance.

Purpose of the Study:

  • To evaluate the clinical activity and safety of lapatinib in cancer patients.
  • To determine the efficacy of lapatinib in HER2-positive advanced breast cancer.
  • To explore the role of lapatinib in other solid tumors and identify predictive factors for treatment efficacy.

Main Methods:

  • Phase I clinical trials assessed the safety and side effect profile of lapatinib.
  • Phase II studies evaluated the clinical activity of lapatinib in advanced breast cancer.
  • Ongoing studies in breast cancer and other solid tumors are collecting biological data for correlative analyses.

Main Results:

  • Lapatinib demonstrated a favorable side effect profile in Phase I trials with limited serious toxicity.
  • Phase II studies indicated meaningful clinical activity in patients with HER2-positive advanced breast cancer.
  • Lapatinib showed modest activity in cancers predominantly driven by EGFR, such as colorectal and head and neck cancers.

Conclusions:

  • Lapatinib is a promising agent for HER2-positive advanced breast cancer.
  • Further research is needed to establish lapatinib's precise role in breast cancer treatment.
  • Correlative studies aim to identify predictive biomarkers for lapatinib efficacy to guide patient selection in clinical practice.

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