A review of Lapatinib, a tyrosine kinase inhibitor, in HER2+ metastatic breast cancer treatment development

Abstract

Metastatic breast cancer continues to have high mortality rates despite the numerous advances in drug therapy. Breast cancer patients have acquired resistance to current treatments, and severe adverse effects, such as cardiotoxicity caused by Trastuzumab, further contribute to the high mortality rate. Therefore, novel drugs with greater specificity and less severe adverse effects must be developed to combat the rise in treatment resistance. Lapatinib, a tyrosine kinase inhibitor, is an attractive drug of choice since lapatinib is not associated with cardiotoxicity, given its greater specificity to HER2 receptors compared to trastuzumab. This review provides a brief overview of tyrosine kinase inhibitors and their overall mechanism of action in treating HER2+ cancers. The study further summarizes the mechanism of action of Lapatinib, its pharmacokinetic properties, its clinical applications, the tools of the act of lapatinib resistance, and recent advances in developing derivatives of Lapatinib to combat lapatinib-acquired resistance.