The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo.

By D. Rusnak, K. Lackey, K. Affleck, E. Wood, K. Alligood, N. Rhodes, B. Keith, Doris M. Murray, K. Glennon, W. Knight and 3 more. Molecular Cancer Therapeutics, 2001

745 citations recorded by the source corpus.

View Paper: https://www.semanticscholar.org/paper/bbdf0192f9f3c8ecd7654205b448c1844e6b3555

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Citations in the corpus

Tissue-penetrating delivery of compounds and nanoparticles into tumors (2009, unknown): “Mice bearing subcutaneous 22Rv1 tumors were treated similarly for 12 days, and orthotopic BT474 tumors for 20 days.”
Targeting the EGFR signaling pathway in cancer therapy (2012, background): “Also, it was found to exhibit activity against AKT overexpressing human tumor xenografts [93].”
Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells. (2006, background): “Lapatinib inhibits the purified HER-2 and EGFR tyrosine kinase at nanomolar concentration in cellfree biochemical assays and effectively inhibits EGFR and HER-2 phosphorylation as well as tumor cell growth at comparably low nanomolar concentration in selected cell lines with constitutive activity of”
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity. (2007, background): “…for clinical use, including the 4-anilinoquinazolines gefitinib (Iressa) (Wakeling et al., 2002), erlotinib (Tarceva) (Pollack et al., 1999), and lapatinib (Rusnak et al., 2001); the pyrrolopyrimidine AEE788 (Traxler et al., 2004); and the irreversible inhibitor HKI-272 (Tsou et al., 2005).”
Role of Tyrosine Kinase Inhibitors in Cancer Therapy (2005, background): “Lapatinib (GW-572016) Lapatinib is a reversible and specific receptor tyrosine kinase inhibitor of both ErbB1 and ErbB2 and has been shown to have activity against ErbB1 and ErbB2, as well as Akt-overexpressing human tumor xenografts (Rusnak et al., 2001).”
Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. (2005, background): “Lapatinib (GW572016) is anorallyactive smallmolecule that reversibly inhibits ErbB1 and ErbB2 tyrosine kinases, leading to inhibition of MAPK and PI3K signaling in ErbB1-expressing andErbB2-overexpressing tumor cell lines and xenografts.(23,24) Lapatinib-treated tumor cells undergo apoptosis or grow”