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Does lapatinib, a small-molecule tyrosine kinase inhibitor, constitute a breakthrough in the treatment of breast cancer?

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Abstract

ErbB/HER receptor or its signal transduction pathway is an attractive therapeutic target for breast cancer. Lapatinib, an orally administered dual inhibitor of ErbB1 (EGFR) and ErbB2 (HER2) receptor tyrosine kinases has shown promising results for metastatic breast cancer (MBC). Lapatinib exhibited activity against trastuzumab-refractory MBC and showed an acceptable adverse event profile such as tran-sient mild rash, diarrhea and nausea. The addition of lapatinib to capecitabine resulted in significantly pro-longed time to progression. Large randomized trials using lapatinib following chemotherapy and surgery are ongoing for early stage HER2-overexpressing breast cancer. Various combinations with agents such as paclitaxel, aromatase inhibitors, or other molecular targeted agents are currently being investigated in clinical trials. If these approaches overcome the limitations of trastuzumab, lapatinib will become an effec-tive treatment option for breast cancer in the near future.

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Abbreviations

MBC:

Metastatic breast cancer

EGFR:

Epidermal growth factor receptor

MAPK:

Mitogen-activated protein kinase

PI3K:

Phatidylinositol 3 kinase

IGF-IR:

Insulin-like growth factor-l receptor

Cdk:

Cyclin-dependent kinase

ER:

Estrogen receptor

Al:

Aromatase inhibitor

TAM:

Tamoxifen

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Authors and Affiliations

  1. Department of Medical Oncology, Cancer Institute Hospital, Japanese Foundation for Cancer Research, Japan

    Yoshinori Ito, Nahomi Tokudome, Tsutomu Sugihara, Shunji Takahashi & Kiyohiko Hatake

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  1. Yoshinori Ito
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  2. Nahomi Tokudome
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  3. Tsutomu Sugihara
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  4. Shunji Takahashi
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Correspondence to Yoshinori Ito.

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Ito, Y., Tokudome, N., Sugihara, T. et al. Does lapatinib, a small-molecule tyrosine kinase inhibitor, constitute a breakthrough in the treatment of breast cancer?. Breast Cancer 14, 156–162 (2007). https://doi.org/10.2325/jbcs.971

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