Lapatinib
China [CN] lapatinib, trade name Tykerb, is an oral reversible small molecule tyrosine kinase inhibitor targeting HER-1/HER-2. Lapatinib has a different mechanism of action from the humanized monoclonal antibody drug Herceptin that has been approved for marketing. It can down-regulate cell proliferation signals by double-blocking the HER-1/HER-2 pathway. The clinical indication is Chemicalbook in combination with capecitabine for the treatment of advanced or metastatic breast cancer with HER2 overexpression and previous treatment including anthracyclines, taxanes and trastuzumab. The effective rate of first-line monotherapy in the advanced stage is approximately 12 to 24%. General clinical guidelines recommend second-line medication. The effective rate of combination therapy with capecitabine is about 26 to 33%, and the maximum clinical benefit rate can reach 71.3%. It is also the most commonly used combination chemotherapy regimen of lapatinib.
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