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LAPATINIB DITOSYLATE: EXPANDING THERAPEUTIC OPTIONS FOR RECEPTOR TYROSINE-PROTEIN KINASE ERBB-2-POSITIVE BREAST CANCER

  作者 Awada, A; Saliba, W; Bozovic-Spasojevic, I  
  选自 期刊  Drugs of today;  卷期  2011年47-5;  页码  335-345  
  关联知识点  
 

[摘要]Receptor tyrosine-protein kinase erbB-2 (HER2)-positive breast cancer is a specific entity with an aggressive behavior Trastuzumab, a monoclonal antibody targeting erbB-2 (HER2) deeply transformed the outcome in patients. Nevertheless, resistance to trastuzumab is still a major concern. Lapatinib ditosylate is an orally available, small molecule targeting the tyrosine activity of the HER2 receptor Lapatinib as a single agent and in combination therapy showed interesting activity in trastuzumab-resistant advanced tumors. In addition, lapatinib use seemed suitable in recurrent locally advanced inflammatory breast cancer and brain metastases. More recently, the Neo-ALTTO (NeoAdjuvant Lapatinib and/or Trastuzumab Treatment Optimisation) trial showed that lapatinib in combination with trastuzumab and paclitaxel significantly improved the pathological complete response in a neoadjuvant setting. Several clinical trials are still ongoing and data that may change current clinical practice are awaited with much interest.

 
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