Drug name: Lapatinib


Related CSCTT Targets

ERBB2 [ref.1, 2]P04626

Lapatinib

Cas.no PubChem ID
231277-92-2 208908
Known Target
Receptor tyrosine-protein kinase erbB-2P04626
Introduction
Lapatinib inhibits the tyrosine kinase activity associated with two oncogenes, EGFR (epidermal growth factor receptor) and HER2/neu (Human EGFR type 2). Over expression of HER2/neu can be responsible for certain types of high-risk breast cancers in women. Like Sorafenib, lapatinib is a protein kinase inhibitor shown to decrease tumor-causing breast cancer stem cells. Lapatinib inhibits receptor signal processes by binding to the ATP-binding pocket of the EGFR/HER2 protein kinase domain, preventing self-phosphorylation and subsequent activation of the signal mechanism

Lapatinib-Structure

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Reference

  • [1] Tumor-initiating cells of HER2-positive carcinoma cell lines express the highest oncoprotein levels and are sensitive to trastuzumab. Magnifico, A., et al. (2009).Clin Cancer Res. 15(6):2010-21.
    19276287. [ 19276287 ]
  • [2] Targeting of preexisting and induced breast cancer stem cells with trastuzumab and trastuzumab emtansine (T-DM1). Diessner, J., et al. (2014).Cell Death Dis. 5:e1149.
    24675467. [ 24675467 ]

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