lapatinib

Known as: N-(3-chloro-4-(((3-fluorobenzyl)oxy)phenyl)-6-(5-(((2-methylsulfonyl)ethyl)amino)methyl) -2-furyl)-4-quinazolinamine, N-(3-chloro-4-((3-Fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-4-quinazolinamine, lapatinib [Chemical/Ingredient] 
A synthetic, orally-active quinazoline with potential antineoplastic properties. Lapatinib reversibly blocks phosphorylation of the epidermal growth… (More)
National Institutes of Health

Topic mentions per year

Topic mentions per year

1979-2017
010020030019792017

Related topics

Related topics

15 relations

Broader (3)

Antineoplastic AgentsProtein Kinase InhibitorsQuinazolines
EGFR protein, humanERBB2 protein, humanInhibition of Cell ProliferationPhosphorylation Inhibition
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Narrower (5)

GW 282974XGW 572016GW2016Tykerb
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Related mentions per year

Related mentions per year

1936-2018
19401960198020002020
lapatinib
Antineoplastic Agents
Receptor Protein-Tyrosine Kinases
EGFR protein, human
Positive Regulation of Apoptosis
ERBB2 protein, human

Papers overview

Semantic Scholar uses AI to extract papers important to this topic.
Highly Cited
2012
Highly Cited
2012
Lapatinib with trastuzumab for HER2-positive early breast cancer (NeoALTTO): a randomised, open-label, multicentre, phase 3 trial.
BACKGROUND The anti-HER2 monoclonal antibody trastuzumab and the tyrosine kinase inhibitor lapatinib have complementary… (More)
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Highly Cited
2010
Highly Cited
2010
Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer.
PURPOSE Preclinical studies in ErbB2-positive cell lines demonstrated a synergistic interaction between lapatinib and trastuzumab… (More)
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Highly Cited
2009
Highly Cited
2009
Lapatinib combined with letrozole versus letrozole and placebo as first-line therapy for postmenopausal hormone receptor-positive metastatic breast cancer.
PURPOSE Cross-talk between human epidermal growth factor receptors and hormone receptor pathways may cause endocrine resistance… (More)
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Highly Cited
2009
Highly Cited
2009
Multicenter phase II study of lapatinib in patients with brain metastases from HER2-positive breast cancer.
PURPOSE Brain metastases develop in one third of patients with advanced HER2+ breast cancer. Effective therapy for patients with… (More)
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Highly Cited
2009
Highly Cited
2009
Novel mechanism of lapatinib resistance in HER2-positive breast tumor cells: activation of AXL.
HER2-directed therapies, such as trastuzumab and lapatinib, are important treatments for breast cancer. However, some tumors do… (More)
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Highly Cited
2009
Highly Cited
2009
Lapatinib, a HER2 tyrosine kinase inhibitor, induces stabilization and accumulation of HER2 and potentiates trastuzumab-dependent cell cytotoxicity
Lapatinib is a human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitor (TKI) that has clinical activity in HER2… (More)
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Highly Cited
2008
Highly Cited
2008
Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235.
Small molecule inhibitors of HER2 are clinically active in women with advanced HER2-positive breast cancer who have progressed on… (More)
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Highly Cited
2006
Highly Cited
2006
Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells.
Lapatinib (GW572016) is a selective inhibitor of both epidermal growth factor receptor (EGFR) and HER-2 tyrosine kinases. Here… (More)
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Highly Cited
2005
Highly Cited
2005
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…
PURPOSE This study (EGF10004) assessed the safety/tolerability, pharmacokinetics, and clinical activity of daily oral dosing with… (More)
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Highly Cited
2004
Highly Cited
2004
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.
GW572016 (Lapatinib) is a tyrosine kinase inhibitor in clinical development for cancer that is a potent dual inhibitor of… (More)
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