Lapatinib: A Novel Dual Tyrosine Kinase Inhibitor with Activity in Solid Tumors

@article{Nelson2006LapatinibAN,
  title={Lapatinib: A Novel Dual Tyrosine Kinase Inhibitor with Activity in Solid Tumors},
  author={Michael H Nelson and Christian R. Dolder},
  journal={Annals of Pharmacotherapy},
  year={2006},
  volume={40},
  pages={261 - 269}
}
Objective: To review the pharmacology, pharmacokinetics, clinical trials, adverse effects, and drug interactions of lapatinib. Data Sources: A PubMed search was conducted (1966–August 2005) using the following terms: lapatinib, GW572016, and dual tyrosine kinase inhibitor. Additional information sources included meeting abstracts, clinical trial data, and bibliographies from articles identified through PubMed. Study Selection and Data Extraction: Preclinical and clinical trials that evaluated… Expand

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Preliminary evidence of biologic and clinical activity in ErbB1 and/or Erb B2-overexpressing tumors is exhibited, however, the limited sample size of this study and the variability of the biologic endpoints suggest that further work is needed to prioritize biomarkers for disease-directed studies, and underscores the need for improved trial design strategies in early clinical studies of targeted agents. Expand
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Patients with metastatic breast cancer that overexpress the ErbB2 protein 2+ or 3+ were enrolled at escalating dose levels of lapatinib in combination with weekly, standard dosing of trastuzumab, and diarrhea, anorexia, fatigue and rash were the common toxicities. Expand
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Lapatinib was well tolerated at doses ranging from 500 to 1,600 mg once daily and clinical activity was observed in heavily pretreated patients with ErbB1-expressing and/or ErbbB2-overexpressing metastatic cancers, including four PRs in patients with trastuzumab-resistant breast cancers and prolonged stable disease in 10 patients. Expand
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Data indicate that quinazoline and pyrido-[3,4-d]-pyrimidine small molecules have potential use as therapy in the broad population of cancer patients overexpressing ErbB-2 and/or EGFR. Expand
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