Lapatinib for Advanced or Metastatic Breast Cancer
Open accessAbstract
Lapatinib is a potent reversible and selective inhibitor of the tyrosine kinase domains of epidermal growth factor receptor and human epidermal growth factor receptor (HER)-2 that exerts its action by competitive binding to the intracellular ATP-binding site of the receptor. It is registered for the treatment of advanced or metastatic HER-2+ breast cancer in combination with capecitabine and for hormone receptor–positive breast cancer in combination with an aromatase inhibitor. Lapatinib administered orally once daily is moderately to well tolerated, with rash and gastrointestinal adverse events as the main toxicities. In studies on the efficacy of lapatinib, direct comparisons between lapatinib and trastuzumab are lacking. Results of ongoing randomized phase III studies with lapatinib or trastuzumab in combination with taxanes as first-line agents for metastatic breast cancer as well as in the neoadjuvant and adjuvant settings are awaited.
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Lapatinib is a highly selective EGFR, ERBB2 and ERBB4 inhibitor that is currently FDA-approved for the treatment of a variety of malignancies.
“Lapatinib is a highly selective EGFR, ERBB2 and ERBB4 inhibitor that is currently FDA-approved for the treatment of a variety of malignancies (59).”
From The drug efflux pump MDR1 promotes intrinsic and acquired resistance to PROTACs in cancer cells (2022) · cites this paper as [59]
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- Authors
- Opdam, F. L., Guchelaar, H.-J., Beijnen, J. H., & Schellens, J. H. M.
- Affiliations
- Leiden University (NL)
- Utrecht University (NL)
- Corresponding author
- Schellens, Jan H.M.
- Venue
- The Oncologist
- Publisher
- Oxford University Press (OUP)
- Published
- 2012-04-01
- Volume
- 17
- Issue
- 4
- Pages
- 536-542
- ISSN
- 1083-7159 (ISSN-L)
- 1549-490X
- PMC
- PMC3336826
- OpenAlex
- W2169052701
- Cited by
- 113
- References
- 33
- Citations by year
- 2026: 8 · 2025: 10 · 2024: 23 · 2023: 9 · 2022: 12 · 2021: 12 · 2020: 4 · 2019: 6 · 2018: 5 · 2017: 3 · 2016: 2 · 2015: 4 · 2014: 5 · 2013: 8 · 2012: 2
- FWCI
- 0.66
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Licence
- academic.oup.com/journals/pages/open_access/funder_policies/chorus/standard_publication_model (vor)
- Locations
- The Oncologist (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Data Archiving and Networked Services (DANS) (submittedVersion)
- Leiden Repository (Leiden University) (submittedVersion)
- Topics
- Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
- Health Sciences › Medicine › Oncology › Cancer Treatment and Pharmacology
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Breast Cancer Treatment Studies
- Keywords
- lapatinib, HER2-positive breast cancer, metastatic breast cancer, tyrosine kinase inhibitors, EGFR, HER2, capecitabine, aromatase inhibitors, hormone receptor-positive breast cancer, trastuzumab, drug toxicity, rash, gastrointestinal adverse effects, taxanes
- MeSH terms
- Lapatinib, Antineoplastic Agents, Antineoplastic Combined Chemotherapy Protocols, Breast Neoplasms, Female, Humans, Neoplasm Metastasis, Quinazolines, Protein Kinase Inhibitors
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