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Mechanisms of Lapatinib Resistance in HER2-driven Breast Cancer

Valentina D'Amato, Lucia Raimondo, Luigi Formisano, Mario Giuliano, Sabino De Placido, Roberta Rosa, Roberto Bianco

Cancer Treat Rev. 2015 Dec;41(10):877-83.

PMID: 26276735

Abstract:

Targeted therapies have been approved for various malignancies but the acquisition of resistance remains a substantial challenge in the clinical management of advanced cancers. Twenty-five per cent of breast cancers overexpress ErbB2/HER2, which confers a more aggressive phenotype and is associated with a poor prognosis. HER2-targeting therapies (trastuzumab, pertuzumab, TDM1 and lapatinib) are available, but a significant fraction of HER2-positive breast cancers eventually relapse or progress. This suggests that acquired or intrinsic resistance enables escape from HER2 inhibition. This review focuses on mechanisms of intrinsic/acquired resistance to lapatinib identified in preclinical and clinical studies. A better understanding of these mechanisms could lead to novel predictive markers of lapatinib response and to novel therapeutic strategies for breast cancer patients.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP231277922 Lapatinib Lapatinib 231277-92-2 Price
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