Mechanisms of Trastuzumab Resistance and Opportunities to Overcome Therapeutic Resistance

Wu, Milos Dokmanovic Wen Jin

doi:10.4172/2155-9929.1000e116

Cited by 1 publication

(1 citation statement)

References 26 publications

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“…It has been suggested that a better understanding of molecular mechanisms underlying primary or acquired resistance to trastuzumab is essential for exploring alternative therapeutic avenues. The administration of tyrosine kinase inhibitors either alone or in combination with trastuzumab or antibody-drug conjugates have been suggested as viable alternatives [33].…”

Section: Monoclonal Antibodies In Her2 Inhibitionmentioning

confidence: 99%

Small Molecule Tyrosine Kinase Inhibitors of ErbB2/HER2/Neu in the Treatment of Aggressive Breast Cancer

2014

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Abstract:The human epidermal growth factor receptor 2 (HER2) is a member of the erbB class of tyrosine kinase receptors. These proteins are normally expressed at the surface of healthy cells and play critical roles in the signal transduction cascade in a myriad of biochemical pathways responsible for cell growth and differentiation. However, it is widely known that amplification and subsequent overexpression of the HER2 encoding oncogene results in unregulated cell proliferation in an aggressive form of breast cancer known as HER2-positive breast cancer. Existing therapies such as trastuzumab (Herceptin ® ) and lapatinib (Tyverb/Tykerb ® ), a monoclonal antibody inhibitor and a dual EGFR/HER2 kinase inhibitor, respectively, are currently used in the treatment of HER2-positive cancers, although issues with high recurrence and acquired resistance still remain. Small molecule tyrosine kinase inhibitors provide attractive therapeutic targets, as they are able to block cell signaling associated with many of the proposed mechanisms for HER2 resistance. In this regard we aim to present a review on the available HER2 tyrosine kinase inhibitors, as well as those currently in development. The use of tyrosine kinase inhibitors as sequential or combinatorial therapeutic strategies with other HER family inhibitors is also discussed.

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Section: Monoclonal Antibodies In Her2 Inhibitionmentioning

confidence: 99%