Lapatinib






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1 12214266 Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Oncogene 2002 Sep 12 21
2 12964069 Lapatinib ditosylate GlaxoSmithKline. IDrugs 2003 Sep 3
3 14633707 Epidermal growth factor receptor autocrine signaling in RIE-1 cells transformed by the Ras oncogene enhances radiation resistance. Cancer Res 2003 Nov 15 5
4 14737100 Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016. Oncogene 2004 Jan 22 10
5 14751502 Effects of the EGFR/HER2 kinase inhibitor GW572016 on EGFR- and HER2-overexpressing breast cancer cell line proliferation, radiosensitization, and resistance. Int J Radiat Oncol Biol Phys 2004 Feb 1 9
6 14967461 Emerging role of epidermal growth factor receptor inhibition in therapy for advanced malignancy: focus on NSCLC. Int J Radiat Oncol Biol Phys 2004 Mar 1 1
7 15163842 Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist 2004 4
8 15374980 A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res 2004 Sep 15 15
9 15528979 Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW572016, a dual EGFR-ErbB2 inhibitor, in healthy subjects. Invest New Drugs 2005 Jan 4
10 15665275 The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res 2005 Jan 1 13
11 15684311 Study of the biologic effects of lapatinib, a reversible inhibitor of ErbB1 and ErbB2 tyrosine kinases, on tumor growth and survival pathways in patients with advanced malignancies. J Clin Oncol 2005 Apr 10 6
12 15755991 Heregulin-induced activation of HER2 and HER3 increases androgen receptor transactivation and CWR-R1 human recurrent prostate cancer cell growth. Clin Cancer Res 2005 Mar 1 12
13 15833875 Inhibition of HER-2/neu kinase impairs androgen receptor recruitment to the androgen responsive enhancer. Cancer Res 2005 Apr 15 9
14 15857287 Small molecules with EGFR-TK inhibitor activity. Curr Drug Targets 2005 May 2
15 15955900 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. J Clin Oncol 2005 Aug 10 3
16 16020981 Therapeutic targeting of multiple signaling pathways in malignant pleural mesothelioma. Oncology 2005 1
17 16091755 Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells. Oncogene 2005 Sep 15 12
18 16397255 Blockade of EGFR and ErbB2 by the novel dual EGFR and ErbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma GEO cells to apoptosis. Cancer Res 2006 Jan 1 6
19 16452222 Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells. Cancer Res 2006 Feb 1 16
20 16452223 Regulation of survivin by ErbB2 signaling: therapeutic implications for ErbB2-overexpressing breast cancers. Cancer Res 2006 Feb 1 7
21 16682622 A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer. Proc Natl Acad Sci U S A 2006 May 16 15
22 16843263 HER2 kinase domain mutation results in constitutive phosphorylation and activation of HER2 and EGFR and resistance to EGFR tyrosine kinase inhibitors. Cancer Cell 2006 Jul 2
23 16894399 Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer. Drugs Today (Barc) 2006 Jul 10
24 16934227 Receptor tyrosine kinase (RTK) inhibition is effective in chemosensitising EGFR-expressing drug resistant human ovarian cancer cell lines when used in combination with cytotoxic agents. Biochem Pharmacol 2006 Oct 16 2
25 16940802 Identification of potentially useful combinations of epidermal growth factor receptor tyrosine kinase antagonists with conventional cytotoxic agents using median effect analysis. Anticancer Drugs 2006 Sep 1
26 17001557 [Molecular diagnostic and targeted therapy--"Barking dogs are going to bite": presentations from the 42nd Annual Meeting of the American Society of Clinical Oncology, Atlanta 2006]. Zentralbl Gynakol 2006 Oct 1
27 17060407 Prospective study of positron emission tomography for evaluation of the activity of lapatinib, a dual inhibitor of the ErbB1 and ErbB2 tyrosine kinases, in patients with advanced tumors. Jpn J Clin Oncol 2007 Jan 3
28 17092403 Delivery of a healthy baby after first-trimester maternal exposure to lapatinib. Clin Breast Cancer 2006 Oct 3
29 17110623 Lapatinib: current status and future directions in breast cancer. Oncologist 2006 Nov-Dec 2
30 17113234 The 17q12-q21 amplicon: Her2 and topoisomerase-IIalpha and their importance to the biology of solid tumours. Cancer Treat Rev 2007 Feb 2
31 17192538 Lapatinib plus capecitabine for HER2-positive advanced breast cancer. N Engl J Med 2006 Dec 28 6
32 17203189 Synergistic inhibition of breast cancer cell lines with a dual inhibitor of EGFR-HER-2/neu and a Bcl-2 inhibitor. Oncol Rep 2007 Feb 6
33 17208435 Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu). Eur J Cancer 2007 Feb 2
34 17250463 Lapatinib: a dual inhibitor of EGFR and HER2 tyrosine kinase activity. Expert Opin Biol Ther 2007 Feb 11
35 17283152 Lapatinib antitumor activity is not dependent upon phosphatase and tensin homologue deleted on chromosome 10 in ErbB2-overexpressing breast cancers. Cancer Res 2007 Feb 1 13
36 17308062 Lapatinib induces apoptosis in trastuzumab-resistant breast cancer cells: effects on insulin-like growth factor I signaling. Mol Cancer Ther 2007 Feb 18
37 17320695 Combined treatment of bladder cancer cell lines with lapatinib and varying chemotherapy regimens--evidence of schedule-dependent synergy. Urology 2007 Feb 4
38 17341725 Lapatinib moves forward in inflammatory and early HER2-positive breast cancer trials. J Natl Cancer Inst 2007 Mar 7 1
39 17350323 Recent advances in the treatment of salivary gland cancers: emphasis on molecular targeted therapy. Oral Oncol 2007 Sep 2
40 17402790 HER-2-positive breast cancer: hope beyond trastuzumab. BioDrugs 2007 2
41 17407594 relocating job wise? A mathematical model separates quantitatively the cytostatic and cytotoxic effects of a HER2 tyrosine kinase inhibitor. Theor Biol Med Model 2007 Apr 3 2
42 17485900 Does lapatinib, a small-molecule tyrosine kinase inhibitor, constitute a breakthrough in the treatment of breast cancer? Breast Cancer 2007 5
43 17489737 Circulating oncoproteins HER2/neu, EGFR and CAIX (MN) as novel cancer biomarkers. Expert Rev Mol Diagn 2007 May 3
44 17513611 Delineation of molecular mechanisms of sensitivity to lapatinib in breast cancer cell lines using global gene expression profiles. Mol Cancer Ther 2007 May 19
45 17545611 Protein kinase Calpha determines HER2 fate in breast carcinoma cells with HER2 protein overexpression without gene amplification. Cancer Res 2007 Jun 1 4
46 17547474 HER2-positive breast cancer: current and future treatment strategies. Drugs 2007 2
47 17555368 Her signaling in pancreatic cancer. Expert Opin Biol Ther 2007 Jun 2
48 17591827 Lapatinib in breast cancer. Ann Oncol 2007 Jun 5
49 17593621 EGFR and HER-2 antagonists in breast cancer. Anticancer Res 2007 May-Jun 3
50 17635524 Assessment of epidermal growth factor receptor (EGFR, ErbB1) and HER2 (ErbB2) protein expression levels and response to lapatinib (Tykerb, GW572016) in an expanded panel of human normal and tumour cell lines. Cell Prolif 2007 Aug 26