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by Dr. C.H. Weaver M.D. 9/2019

Pyrotinib plus Xeloda (capecitabine) yielded better overall response rates and delayed cancer progression than Tykerb (lapatinib) plus Xeloda in patients with human epidermal growth factor receptor 2 (HER2)-positive metastatic breast cancer.

Tykerb is a precision cancer medicine that targets two proteins that often function abnormally in breast cancer cells-HER2 and EGFR. When these proteins are over expressed among cancer cells, referred to as HER2-positive and/or EGFR-positive cancers, the proteins tend to function abnormally, resulting in unchecked replication and growth of cancerous cells.

Tykerb is currently approved for use in combination with the chemotherapy agent Xeloda® for the treatment of advanced or metastatic breast cancer in women whose cancer overexpresses HER2 and whose cancer has progressed following prior therapy with an anthracycline, a taxane, and Herceptin® (trastuzumab). (1)

Pyrotinib is a “next generation” pan-HER receptor tyrosine kinase inhibitor that is active against HER positive cancers in both preclinical experiments and humans.

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The purpose of the current clinical trial was to determine if pyrotinib’s “pan inhibiton” might produce superior results compared to standard treatment with Tykerb. In the clinical trial a total of 128 patients with HER-2 positive relapsed or metastatic breast cancer previously treated with taxanes, anthracyclines, and/or Herceptin were treated with either pyrotinib or lapatinib in combination with Xeloda and directly compared.

Overall 79% of pyrotinib treated patients responded to treatment compared to only 57% for those receiving lapatinib. Pyrotinib delayed cancer progression on average 18 months compared with 7 months for lapatinib. Both treatments were well tolerated but caused hand-foot syndrome in ~20% of patients. Pyrotinb was also more likely to cause diarrhea and a low white blood count than lapatinib.

The study results demonstrated the superiority of pyrotinib over Tykerb for the treatment of advanced HER2-positive breast cancer. Upon approval pyrotinib will provide doctors and patients a new and effective treatment for the management of HER2+ breast cancer.


  1. Tykerb® Treatment of Advanced - Metastatic Breast Cancer
  2. J Clin Oncol. 2019 Aug 20. Epub ahead of print