lapatinib (Tykerb)

  • Pharmacy Author:
    Omudhome Ogbru, PharmD

    Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

  • Medical and Pharmacy Editor: Jay W. Marks, MD
    Jay W. Marks, MD

    Jay W. Marks, MD

    Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.

GENERIC NAME: lapatinib


DRUG CLASS AND MECHANISM: Lapatinib is an oral medication used for treating breast cancer. Lapatinib is classified as a kinase inhibitor. Kinase inhibitors include

Kinase inhibitors prevent the growth of tumors by reducing the action of proteins that control cell division, growth and survival. These proteins usually are present in larger quantities or are more active in cancer cells. By reducing the activity of these proteins, growth and survival of cancer cells are reduced. The FDA approved lapatinib in March, 2007.

PRESCRIBED FOR: Lapatinib is used in combination with capecitabine (Xeloda) for treatment of patients with advanced or metastatic breast cancer that overexpress HER2, a receptor on the surface of cancer cells that promotes the growth of the cells. Before treatment with lapatinib, patients should have been treated with an anthracycline, a taxane, and trastuzumab (Herceptin) and have had their breast cancer progressed while treated with trastuzumab.

Lapatinib also is combined with letrozole (Femara) for the treatment of postmenopausal women who require hormonal therapy for hormone receptor- positive metastatic breast cancer that overexpresses the HER2 receptor.


  • Decreases in left ventricular ejection fraction (LVEF) may occur and impair the function of the heart. Patients should have normal LVEF before starting lapatinib and LVEF should be monitored during treatment.
  • Lapatinib has been associated with liver damage. Liver tests should be obtained before starting treatment, every 4 to 6 weeks during treatment, and as needed thereafter. Dose reduction in patients with severe hepatic impairment should be considered, and treatment should be stopped if patients experience severe changes in liver function tests.
  • Diarrhea, including severe diarrhea, has been reported during treatment.
  • Lapatinib has been associated with interstitial lung disease and pneumonitis. Treatment should be discontinued if patients experience severe pulmonary symptoms.
  • Lapatinib may cause abnormal heartbeats (arrhythmias) in some patients. Electrocardiogram (ECG) and electrolyte monitoring should be considered.
  • Severe cutaneous (skin) reactions have been reported. Treatment should be discontinued if cutaneous reactions are suspected.
Medically Reviewed by a Doctor on 11/5/2015

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