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GW 572016

Known as: GW-572016, GW572016 
 

Topic mentions per year

Topic mentions per year

2002-2012
05101520022012

Related topics

Related topics

2 relations

Broader (2)

lapatiniblapatinib ditosylate

Related mentions per year

Related mentions per year

1979-2018
197019801990200020102020
GW 572016
lapatinib
lapatinib ditosylate

Papers overview

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Highly Cited
2009
Highly Cited
2009
An unexpected synergist role of P-glycoprotein and breast cancer resistance protein on the central nervous system penetration of the tyrosine kinase inhibitor lapatinib (N-{3-chloro-4-[(3…
Lapatinib is a tyrosine kinase inhibitor approved for use in combination with capecitabine to treat advanced or metastatic breast… (More)
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Highly Cited
2008
Highly Cited
2008
Lapatinib (Tykerb, GW572016) reverses multidrug resistance in cancer cells by inhibiting the activity of ATP-binding cassette subfamily B member 1 and G member 2.
Lapatinib is active at the ATP-binding site of tyrosine kinases that are associated with the human epidermal growth factor… (More)
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Highly Cited
2007
Highly Cited
2007
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…
OBJECTIVE Lapatinib (Tykerb, GW572016), a potent inhibitor of the catalytic activities of epidermal growth factor receptor (EGFR… (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
2005
Highly Cited
2005
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
Antibodies and small molecule tyrosine kinase inhibitors targeting ErbB2 exhibit distinct, noncross resistant mechanisms of… (More)
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Highly Cited
2005
Highly Cited
2005
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.
Effective treatment of estrogen receptor (ER)-positive breast cancers with tamoxifen is often curtailed by the development of… (More)
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Highly Cited
2005
Highly Cited
2005
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.
To realize the full potential of targeted protein kinase inhibitors for the treatment of cancer, it is important to address the… (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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Highly Cited
2002
Highly Cited
2002
Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways
Dual EGFR/erbB2 inhibition is an attractive therapeutic strategy for epithelial tumors, as ligand-induced erbB2/EGFR… (More)
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