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Activity of lapatinib is independent of EGFR expression level in HER2-overexpressing breast cancer cells.

Zhang D, Pal A, Bornmann WG, Yamasaki F, Esteva FJ, Hortobagyi GN, Bartholomeusz C, Ueno NT.

Mol Cancer Ther. 2008 Jul;7(7):1846-50. doi: 10.1158/1535-7163.MCT-08-0168.


An heregulin-EGFR-HER3 autocrine signaling axis can mediate acquired lapatinib resistance in HER2+ breast cancer models.

Xia W, Petricoin EF 3rd, Zhao S, Liu L, Osada T, Cheng Q, Wulfkuhle JD, Gwin WR, Yang X, Gallagher RI, Bacus S, Lyerly HK, Spector NL.

Breast Cancer Res. 2013;15(5):R85.


Effect of lapatinib on the outgrowth of metastatic breast cancer cells to the brain.

Gril B, Palmieri D, Bronder JL, Herring JM, Vega-Valle E, Feigenbaum L, Liewehr DJ, Steinberg SM, Merino MJ, Rubin SD, Steeg PS.

J Natl Cancer Inst. 2008 Aug 6;100(15):1092-103. doi: 10.1093/jnci/djn216. Epub 2008 Jul 29.


Epidermal growth factor-receptor activation modulates Src-dependent resistance to lapatinib in breast cancer models.

Formisano L, Nappi L, Rosa R, Marciano R, D'Amato C, D'Amato V, Damiano V, Raimondo L, Iommelli F, Scorziello A, Troncone G, Veneziani B, Parsons SJ, De Placido S, Bianco R.

Breast Cancer Res. 2014 May 5;16(3):R45. doi: 10.1186/bcr3650.


A class I histone deacetylase inhibitor, entinostat, enhances lapatinib efficacy in HER2-overexpressing breast cancer cells through FOXO3-mediated Bim1 expression.

Lee J, Bartholomeusz C, Mansour O, Humphries J, Hortobagyi GN, Ordentlich P, Ueno NT.

Breast Cancer Res Treat. 2014 Jul;146(2):259-72. doi: 10.1007/s10549-014-3014-7. Epub 2014 Jun 12.


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.

Rusnak DW, Alligood KJ, Mullin RJ, Spehar GM, Arenas-Elliott C, Martin AM, Degenhardt Y, Rudolph SK, Haws TF Jr, Hudson-Curtis BL, Gilmer TM.

Cell Prolif. 2007 Aug;40(4):580-94.


Epidermal growth factor receptor gene copy number may predict lapatinib sensitivity in HER2-positive metastatic breast cancer.

Fabi A, Merola R, Ferretti G, Di Benedetto A, Antoniani B, Ercolani C, Nisticò C, Papaldo P, Ciccarese M, Sperduti I, Vici P, Marino M, Gori S, Botti C, Malaguti P, Cognetti F, Mottolese M.

Expert Opin Pharmacother. 2013 Apr;14(6):699-706. doi: 10.1517/14656566.2013.779672. Epub 2013 Mar 9.


Heparanase mediates a novel mechanism in lapatinib-resistant brain metastatic breast cancer.

Zhang L, Ngo JA, Wetzel MD, Marchetti D.

Neoplasia. 2015 Jan;17(1):101-13. doi: 10.1016/j.neo.2014.11.007.


MET activation mediates resistance to lapatinib inhibition of HER2-amplified gastric cancer cells.

Chen CT, Kim H, Liska D, Gao S, Christensen JG, Weiser MR.

Mol Cancer Ther. 2012 Mar;11(3):660-9. doi: 10.1158/1535-7163.MCT-11-0754. Epub 2012 Jan 11.


Lapatinib-mediated cyclooxygenase-2 expression via epidermal growth factor receptor/HuR interaction enhances the aggressiveness of triple-negative breast cancer cells.

Hsia TC, Tu CY, Chen YJ, Wei YL, Yu MC, Hsu SC, Tsai SL, Chen WS, Yeh MH, Yen CJ, Yu YL, Huang TC, Huang CY, Hung MC, Huang WC.

Mol Pharmacol. 2013 Apr;83(4):857-69. doi: 10.1124/mol.112.082743. Epub 2013 Jan 25.


β1 integrin mediates an alternative survival pathway in breast cancer cells resistant to lapatinib.

Huang C, Park CC, Hilsenbeck SG, Ward R, Rimawi MF, Wang YC, Shou J, Bissell MJ, Osborne CK, Schiff R.

Breast Cancer Res. 2011 Aug 31;13(4):R84. doi: 10.1186/bcr2936.


Novel Hsp90 inhibitor FW-04-806 displays potent antitumor effects in HER2-positive breast cancer cells as a single agent or in combination with lapatinib.

Huang W, Wu QD, Zhang M, Kong YL, Cao PR, Zheng W, Xu JH, Ye M.

Cancer Lett. 2015 Jan 28;356(2 Pt B):862-71. doi: 10.1016/j.canlet.2014.10.040. Epub 2014 Nov 4.


RON confers lapatinib resistance in HER2-positive breast cancer cells.

Wang Q, Quan H, Zhao J, Xie C, Wang L, Lou L.

Cancer Lett. 2013 Oct 28;340(1):43-50. doi: 10.1016/j.canlet.2013.06.022. Epub 2013 Jun 27.


Activated phosphoinositide 3-kinase/AKT signaling confers resistance to trastuzumab but not lapatinib.

O'Brien NA, Browne BC, Chow L, Wang Y, Ginther C, Arboleda J, Duffy MJ, Crown J, O'Donovan N, Slamon DJ.

Mol Cancer Ther. 2010 Jun;9(6):1489-502. doi: 10.1158/1535-7163.MCT-09-1171. Epub 2010 May 25. Erratum in: Mol Cancer Ther. 2011 Nov;10(11):2211.


Human breast cancer cells harboring a gatekeeper T798M mutation in HER2 overexpress EGFR ligands and are sensitive to dual inhibition of EGFR and HER2.

Rexer BN, Ghosh R, Narasanna A, Estrada MV, Chakrabarty A, Song Y, Engelman JA, Arteaga CL.

Clin Cancer Res. 2013 Oct 1;19(19):5390-401. doi: 10.1158/1078-0432.CCR-13-1038. Epub 2013 Aug 15.


Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases.

Medina PJ, Goodin S.

Clin Ther. 2008 Aug;30(8):1426-47. doi: 10.1016/j.clinthera.2008.08.008. Review.


Lapatinib, a dual HER1/HER2 tyrosine kinase inhibitor, augments basal cleavage of HER2 extracellular domain (ECD) to inhibit HER2-driven cancer cell growth.

Vazquez-Martin A, Oliveras-Ferraros C, Cufí S, Del Barco S, Martin-Castillo B, Menendez JA.

J Cell Physiol. 2011 Jan;226(1):52-7. doi: 10.1002/jcp.22333.


Roles of BIM induction and survivin downregulation in lapatinib-induced apoptosis in breast cancer cells with HER2 amplification.

Tanizaki J, Okamoto I, Fumita S, Okamoto W, Nishio K, Nakagawa K.

Oncogene. 2011 Sep 29;30(39):4097-106. doi: 10.1038/onc.2011.111. Epub 2011 Apr 18.


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