Abstract
Lapatinib is an oral dual tyrosine kinase inhibitor targeting EGFR1 and EGFR2 (HER2). Phase I trials have shown that lapatinib is well tolerated, with mild diarrhea and skin rush as common adverse effects, and low cardiotoxicity. Phase II and III trials provided evidences on clinical effectiveness in advanced or metastatic breast cancer and potential against brain metastases. Lapatinib is active in combination with trastuzumab and in trastuzumab-resistant patients, moreover it has synergistic action with capecitabine. Several clinical trials are in progress to explore the effectiveness of lapatinib in other combinations and against several tumor types.
MeSH terms
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Antibodies, Monoclonal / therapeutic use
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Antibodies, Monoclonal, Humanized
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Antineoplastic Agents
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Antineoplastic Combined Chemotherapy Protocols / therapeutic use
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Breast Neoplasms / drug therapy*
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Breast Neoplasms / metabolism
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Clinical Trials as Topic
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Drug Resistance, Neoplasm
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ErbB Receptors / antagonists & inhibitors
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ErbB Receptors / metabolism
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Female
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Humans
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Lapatinib
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Neoplasms / drug therapy
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Quinazolines / administration & dosage
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Quinazolines / adverse effects
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Quinazolines / pharmacokinetics
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Quinazolines / therapeutic use*
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Receptor, ErbB-2 / antagonists & inhibitors
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Receptor, ErbB-2 / metabolism
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Trastuzumab
Substances
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Antibodies, Monoclonal
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Antibodies, Monoclonal, Humanized
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Antineoplastic Agents
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Quinazolines
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Lapatinib
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EGFR protein, human
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ERBB2 protein, human
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ErbB Receptors
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Receptor, ErbB-2
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Trastuzumab