Lapatinib CAS NO.231277-92-2

Lapatinib is a new targeted treatment drug for breast cancer developed by glaxosmithkline PLC. It is a tyrosine kinase inhibitor, which can effectively inhibit the activity of human epidermal growth factor receptor-1 (ErbB1) and human epidermal growth factor receptor-2 (ErbB2) tyrosine kinase. It is unique in that it works in a variety of ways, preventing breast cancer cells from receiving the signals they need to grow. The mechanism of action is to inhibit the phosphorylation and activation of tumor cells by inhibiting the ATP sites of EGFR(erbb-1) and HER2(erbb-2) in cells, and to block down-regulated signals by the homogenous and heterogeneous dimers of EGFR(erbb-1) and HER2(erbb-1).

 

Molecular targeted therapy for breast cancer is to treat oncogenes and related expression products related to the occurrence and development of breast cancer. Molecular targeted drugs can inhibit or kill tumor cells by blocking the signal transduction of tumor cells or related cells to control the changes of cell gene expression.

 

On March 14, 2007, the U.S. food and drug administration approved rapatinib combined with xilotabine (capecitabine) for the treatment of overexpression of human epidermal factor receptor 2(ErbB2) in patients with advanced or metastatic breast cancer treated with anthracyclines, taxol, and trastuzumab.

 

Clinical trials have shown that the drug also works well in patients with HER2 breast cancer who have developed resistance to roche's Herceptin.

 

Lapatinib is a new targeted anticancer drug. It can act on both her-1 and her-2 targets at the same time, and the biological effect of inhibiting the proliferation and growth of tumor cells generated by this action mode is far greater than that of inhibiting only one of the targets. The so-called targeted therapy drugs refer to the drugs that target certain receptors, genes or key proteins to kill relevant tumor cells.

 

Human ErbB receptor belongs to the type I receptor tyrosine kinase (TK) family. These include ErbB1(EGFR), ErbB2(HER2), ErbB3(HER3), and ErbB4(HER4). Cancer patients with erbb-1 (EGFR) and erbb-2 (her-2) receptors are often overexpressed or otherwise altered. Currently, it is known that human epidermal growth factor receptor-2 (erbb-2, her-2) is a human oncogene closely related to breast cancer, and its high expression in breast cancer often indicates that lymph node metastasis and poor tumor differentiation are likely to be present, and the prognosis is poor. With the further study of her-2, it has become one of the target molecules for the specific treatment of breast cancer.