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Lapatinib

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Information about Lapatinib

  Lapatinib is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors.

Liver safety of Lapatinib

Lapatinib therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury

Mechanism of action of Lapatinib

Lapatinib (la pa' ti nib) is a selective inhibitor of two tyrosine kinase receptors which are associated with tumor growth and angiogenesis.  Lapatinib has special activity against the epidermal growth factor receptor (EGFR) and the human epidermal group factor receptor-2 (HER2).  Tyrosine kinase receptors are often mutated and over expressed in cancer cells, causing unregulated cell growth and proliferation.  Lapatinib is one of several tyrosine kinase inhibitors that have been introduced into cancer chemotherapy and are specially directed at molecular abnormalities that occur in cancer cells.  Inhibition of these receptors can lead to dramatic reversal of progression the cancer, although the efficacy is sometimes limited by the development of tumor resistance caused by mutations in the kinase. 

FDA approval information for Lapatinib

Lapatinib received approval for use in the United States in 2007 for treatment of patients with advanced or metastatic breast cancer whose tumors over express HER2 to be used in combination with capecitabine.  Indications have been broadened somewhat since then. 

Dosage and administration for Lapatinib

Lapatinib is available in tablets of 250 mg under the brand name Tykerb.  The typical dose of lapatinib is 1,250 mg once daily in combination with capecitabine in cycles of 21 days. 

Side effects of Lapatinib

Side effects include rash, diarrhea, nausea, vomiting, fatigue, hand-foot syndrome and pruritus. 

 

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