Slamon DJ, Godolphin W, Jones LA, Holt JA, Wong SG, Keith DE, Levin WJ, Stewart SG, Udove J, Ullrich A, et al: Studies of the HER-2/neu proto-oncogene in human breast and ovarian cancer. Science. 1989, 244: 707-712. 10.1126/science.2470152.
Article
CAS
PubMed
Google Scholar
Bacus SS, Zelnich CR, Plowman G, Yarden Y: Expression of the erbB-2 family of growth factor receptors and their ligands in breast cancer: Implication for tumor biology and clinical behavior. Am J Clin Pathol. 1994, 102 (4 Suppl 1): S13-S24.
CAS
PubMed
Google Scholar
Slamon DJ, Clark GM, Wong SG, Levin WJ, Ullrich A, McGuire WL: Human breast cancer: correlation of relapse and survival with amplification of the HER-2/neu oncogene. Science. 1987, 235: 177-182. 10.1126/science.3798106.
Article
CAS
PubMed
Google Scholar
Yarden Y, Sliwkowski MX: Untangling the ErbB signaling network. Nat Rev Mol Cell Biol. 2001, 2: 127-137. 10.1038/35052073.
Article
CAS
PubMed
Google Scholar
Hynes N, Lane H: ERBB receptors and cancer: the complexity of targeted inhibitors. Nat Rev Cancer. 2005, 5: 341-354. 10.1038/nrc1609.
Article
CAS
PubMed
Google Scholar
Olayioye MA, Graus-Porta D, Beerli RR, Rohrer J, Gay B, Hynes NE: ErbB-1 and ErbB-2 acquire distinct signaling properties dependent upon their dimerization partner. Mol Cell Biol. 1998, 18: 5042-5051.
Article
CAS
PubMed
PubMed Central
Google Scholar
Cobleigh MA, Vogel CL, Tripathy D, Robert NJ, Scholl S, Fahrenbacher L, Wolter JM, Paton V, Shak S, Lieberman G, et al: Multinational study of the efficacy and safety of humanized anti-Her2 monoclonal antibody in women who have Her2-overexpressing metastatic breast cancer that has progressed after chemotherapy for metastatic disease. J Clin Oncol. 1999, 17: 2639-2648.
CAS
PubMed
Google Scholar
Slamon DJ, Leyland-Jones B, Shak S, Fuchs H, Paton V, Bajamonde A, Fleming T, Eiermann W, Wolter J, Pegram M, et al: Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2. N Engl J Med. 2001, 344: 783-792. 10.1056/NEJM200103153441101.
Article
CAS
PubMed
Google Scholar
Pegram MD, Lipton A, Hayes DF, Weber BL, Baselga JM, Tripathy D, Baly D, Baughman SA, Twaddell T, Glaspy JA, et al: Phase II study of receptor-enhanced chemosensitivity using recombinant humanized anti-p185HER2/neu monoclonal antibody plus cisplatin in patients with HER2/neu-overexpressing metastatic breast cancer refractory to chemotherapy treatment. J Clin Oncol. 1998, 16: 2659-2671.
CAS
PubMed
Google Scholar
Baselga J, Tripathy D, Mendelsohn J, Baughman S, Benz CC, Dantis L, Sklarin NT, Seidman AD, Hudis CA, Moore J, et al: Phase II study of weekly intravenous recombinant humanized anti-p185HER2 monoclonal antibody in patients with HER2/neu-overexpressing metastatic breast cancer. J Clin Oncol. 1996, 14: 737-744.
CAS
PubMed
Google Scholar
Romond EH, Perez EA, Bryant J, Suman VJ, Geyer CE, Davidson NE, Tan-Chiu E, Martino S, Paik S, Kaufman PA, et al: Trastuzumab plus chemotherapy for operable HER2-positive breast cancer. N Engl J Med. 2005, 353: 1673-1684. 10.1056/NEJMoa052122.
Article
CAS
PubMed
Google Scholar
Piccart-Gebhart MJ, Proctor M, Leyland-Jones B, Goldhirsch A, Untch M, Smith I, Gianni L, Baselga J, Bell R, Jackisch C, et al: Trastuzumab after adjuvant chemotherapy in HER2-positive breast cancer. N Engl J Med. 2005, 353: 1659-1672. 10.1056/NEJMoa052306.
Article
CAS
PubMed
Google Scholar
Clynes RA, Towers TL, Presta LG, Ravetch JV: Inhibitory Fc receptors modulates in vivo cytotoxicity against tumor targets. Nat Med. 2000, 6: 443-446. 10.1038/74704.
Article
CAS
PubMed
Google Scholar
Hudziak RM, Lewis GD, Winget M, Fendly BM, Shepard HM, Ullrich A: p185HER2 monoclonal antibody has antiproliferative effects in vitro and sensitizes human breast tumor cells to tumor necrosis factor. Mol Cell Biol. 1989, 9: 1165-1172.
Article
CAS
PubMed
PubMed Central
Google Scholar
Nahta R, Esteva FJ: Herceptin: mechanisms of action and resistance. Cancer Lett. 2006, 232: 123-138. 10.1016/j.canlet.2005.01.041.
Article
CAS
PubMed
Google Scholar
Sliwkowski MX, Lofgren J, Lewis GD, Hotaling TE, Fendly BM, Fox JA: Nonclinical studies addressing the mechanism of action of trastuzumab (herceptin). Semin Oncol. 1999, 26 (4 Suppl 12): 60-70.
CAS
PubMed
Google Scholar
Pietras RJ, Fendly BM, Chazin VR, Pegram MD, Howell SB, Slamon DJ: Antibody to Her-2/neu receptor blocks DNA repair after cisplatin in human breast and ovarian cancer cells. Oncogene. 1994, 9: 1829-1838.
CAS
PubMed
Google Scholar
Smith BL, Chin D, Maltzman W, Crosby K, Hortobagyi GN, Bacus SS: The efficacy of Herceptin therapies is influenced by the expression of other erbB receptors, their ligands and the activation of downstream signalling proteins. Br J Cancer. 2004, 91: 1190-1194.
CAS
PubMed
PubMed Central
Google Scholar
Lu Y, Zi X, Zhao Y, Mascarenhas D, Pollak M: Insulin-like growth factor-1 receptor signaling and resistance to trastuzumab (Herceptin). J Natl Cancer Inst. 2001, 93: 1852-1857. 10.1093/jnci/93.24.1852.
Article
CAS
PubMed
Google Scholar
Nahta R, Yu D, Hong MC, Hortobagyi GN, Esteva FJ: Mechanisms of disease: understanding resistance to HER2-targeted therapy in human breast cancer. Nat Clin Pract Oncol. 2006, 3: 269-280. 10.1038/ncponc0509.
Article
CAS
PubMed
Google Scholar
Nagata Y, Lan K-H, Zhou X, Tan M, Esteva FJ, Sahin AA, Klos KS, Li P, Monia BP, Nguyen NT, et al: PTEN activation contributes to tumor inhibition by trastuzumab, and loss of PTEN predicts trastuzumab resistance in patients. Cancer Cell. 2004, 6: 117-127. 10.1016/j.ccr.2004.06.022.
Article
CAS
PubMed
Google Scholar
Saez R, Molina MA, Ramsey EE, Rojo F, Keenan EJ, Albanell J, Lluch A, Garcia-Conde J, Baselga J, Clinton GM: p95HER-2 predicts worse outcome in patients with HER-2-positive breast cancer. Clin Cancer Res. 2006, 12: 424-431. 10.1158/1078-0432.CCR-05-1807.
Article
CAS
PubMed
Google Scholar
Nahta R, Takahashi T, Ueno NT, Hung MC, Esteva FJ: P27 (kip1) down-regulation is associated with trastuzumab resistance in breast cancer cells. Cancer Res. 2004, 64: 3981-3986. 10.1158/0008-5472.CAN-03-3900.
Article
CAS
PubMed
Google Scholar
Neve RM, Chin K, Fridlyand J, Yeh J, Baehner FL, Fevr T, Clark L, Bayani N, Coppe J-P, Tong F, et al: A collection of breast cancer cell lines for the study of functionally distinct cancer subtypes. Cancer Cell. 2006, 10: 515-527. 10.1016/j.ccr.2006.10.008.
Article
CAS
PubMed
PubMed Central
Google Scholar
Xia W, Mullin RJ, Keith BR, Liu L, Ma H, Rusnak DW, Owens G, Alligood KJ, Spector NL: 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, 21: 6255-6263. 10.1038/sj.onc.1205794.
Article
CAS
PubMed
Google Scholar
Fry DW, Bridges AJ, Denny WA, Doherty A, Greis KD, Hicks JL, Hook KE, Keller PR, Leopold WR, Loo JA, et al: Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci USA. 1998, 95: 12022-12027. 10.1073/pnas.95.20.12022.
Article
CAS
PubMed
PubMed Central
Google Scholar
Fabian MA, Biggs WH, Treiber DK, Atteridge CE, Aziomioara MD, Benedetti MG, Carter TA, Ciceri P, Edeen T, Floyd M, et al: A small molecule-kinase interaction map for clinical kinase inhibitors. Nat Biotechnol. 2005, 23: 329-336. 10.1038/nbt1068.
Article
CAS
PubMed
Google Scholar
Sartor CI, Zhou H, Kozlowska E, Guttridge K, Kawata E, Caskey L, Harrelson J, Hynes N, Ethier S, Calvo B, et al: HER4 mediates ligand-dependent antiproliferative and differentiation responses in human breast cancer cells. Mol Cell Biol. 2001, 21: 4265-4275. 10.1128/MCB.21.13.4265-4275.2001.
Article
CAS
PubMed
PubMed Central
Google Scholar
Bence AK, Anderson EB, Doukas MA, DeSimone PA, Davis GA, Smith DA, Koch KM, Stead AG, Mangum S, Spector NL, et al: Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW57 a dual EGFR-ErbB2 inhibitor, in healthy subjects. Invest New Drugs. 2005, 23: 39-49. 10.1023/B:DRUG.0000047104.45929.ea.
Article
CAS
PubMed
Google Scholar
Nemunaitis J, Eiseman I, Cunningham C, Senzer N, Williams A, Lenehan P, Olson SC, Bycott P, Schlicht M, Zentgraff R, et al: Phase I clinical and pharmacokinetics evaluation of oral CI-1033 in patients with refractory cancer. Clin Cancer Res. 2005, 11: 3846-3853. 10.1158/1078-0432.CCR-04-1950.
Article
CAS
PubMed
Google Scholar
Rabindran SK, Discafani CM, Rosfjord EC, Baxter M, Brawner Floyd M, Golas J, Hallett WA, Johnson BD, Nilakantan R, et al: Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 2004, 64: 3958-3965. 10.1158/0008-5472.CAN-03-2868.
Article
CAS
PubMed
Google Scholar
Wood ER, Truesdale AT, McDonald OB, Yuan D, Hassell A, Dickerson SH, Ellis B, Pennisi C, Horne E, Lackey K, et al: 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, 64: 6652-6659. 10.1158/0008-5472.CAN-04-1168.
Article
CAS
PubMed
Google Scholar
Xia W, Liu L-H, Ho P, Spector NL: 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, 23: 646-653. 10.1038/sj.onc.1207166.
Article
CAS
PubMed
Google Scholar
Baselga J: Skin as a surrogate tissue for pharmacodynamic end points: is it deep enough?. Clin Cancer Res. 2003, 9: 2389-2390.
PubMed
Google Scholar
Malik SN, Siu LL, Rowinsky EK, deGraffenried L, Hammond LA, Rizzo J, Bacus S, Brattain MG, Kreisberg JI, Hidalgo M: Pharma-codynamic evaluation of the epidermal growth factor receptor inhibitor OSI-774 in human epidermis of cancer patients. Clin Cancer Res. 2003, 9: 2478-2486.
CAS
PubMed
Google Scholar
Spector NL, Xia W, Burris HA, Hurwitz H, Claire Dees E, Dowlati A, O'Neil B, Overmoyer B, Liu L, Marcom K, et al: A Study of the biological effects of GW572016, a reversible inhibitor of EGFR (ErbB1) and ErbB2 tyrosine kinases, on tumor growth and survival pathways in patients with advanced malignancies. J Clin Oncol. 2005, 23: 1-11.
Article
Google Scholar
Xia W, Bisi J, Strum J, Liu L, Carrick K, Graham KL, Hardwicke MA, Treece AL, Bacus S, Spector NL: Regulation of survivin by ErbB2 signaling: therapeutic implications for ErbB2-overex-pressing breast cancers. Cancer Res. 2006, 66: 1640-1647. 10.1158/0008-5472.CAN-05-2000.
Article
CAS
PubMed
Google Scholar
Zinner RG, Donato NJ, Nemunaitis JJ, Cunningham CC, Shin HJ, Zentgraf RE, Ayers GD, Glisson BS, Khuri FR, Kies MS, et al: Biomarker modulation in tumor and skin biopsy samples from patients with solid tumors following treatment with the panerbB tyrosine kinase inhibitor CI-1033. Proc Am Soc Clin Oncol. 2002, 21: 58a-
Google Scholar
Guarneri V, Lenihan DJ, Valero V, Durand JB, Durand JB, Broglio K, Hess KR, Michaud LB, Gonzalez-Angulo AM, Hortobagyi GN, et al: Long-term cardiac tolerability of trastuzumab in meta-static breast cancer: the M.D. Anderson Cancer Center experience. J Clin Oncol. 2006, 24: 4107-4115. 10.1200/JCO.2005.04.9551.
Article
CAS
PubMed
Google Scholar
Chien KR: Myocyte survival pathways and cardiomyopathy: implications for trastuzumab cardiotoxicity. Semin Oncol. 2000, 27: 9-14.
CAS
PubMed
Google Scholar
Kerkela R, Grazette L, Yacobi R, Iliescu C, Patten R, Beahm C, Walters B, Shevtsov S, Pesant S, Clubb FJ, et al: Cardiotoxicity of the cancer therapeutic agent imatinib mesylate. Nat Med. 2006, 12: 908-916. 10.1038/nm1446.
Article
PubMed
Google Scholar
Perez EA, Byrne JA, Hammond IW, Rafi R, Martin AM, Berger MS, Zaks TZ, Oliva CR, Roychowdhury DF, Stein SH: Results of an analysis of cardiac function in 2812 patients treated with lapatinib [abstract]: ASCO Annual Meeting Proceedings. J Clin Oncol. 2006, 24 (18S): 583a-
Google Scholar
Geyer CE, Forster J, Lindquist D, Chan S, Romieu CG, Pienkowski T, Jagiello-Gruszfeld A, Crown J, Chan A, Kaufman B, et al: Lapatinib plus capecitabine for HER2-positive advanced breast cancer. N Engl J Med. 2006, 355: 2733-2743. 10.1056/NEJMoa064320.
Article
CAS
PubMed
Google Scholar
Burris HA, Hurwitz HI, Dees EC, Dowlati A, Blackwell KL, O'Neil B, Marcom PK, Ellis MJ, Overmoyer B, Jones SF, et al: 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, 23: 5305-5313. 10.1200/JCO.2005.16.584.
Article
CAS
PubMed
Google Scholar
Jones SF, Burris HA, Yardley DA, Greco FA, Spigel DR, Raefsky EL, Hainsworth JD, Willcutt NT, Calvert SA, Versola MJ, et al: Lapatinib (an oral dual kinase inhibitor) plus weekly or every 3 week paclitaxel [abstract]. San Antonio Breast Cancer Symposium. Breast Cancer Res Treat. 2004, 88 (Suppl 1): 1069a-
Google Scholar
Schwartz G, Chu QSC, Hammond LA, Mita M, Curtright J, Versola MJ, Kock K, Pandite LN, Ho PT, Rowinsky EK: Phase I clinical, biology and pharmacokinetic study of the combination of GW572016 and capecitabine in patients with advanced solid tumors [abstract]: ASCO Annual Meeting Proceedings. J Clin Oncol. 2004, 22 (14S): 3070a-
Google Scholar
Trudeau M, Johnston S, Kaufman B, Blackwell K, Ahmed SB, Boussen H, Frikha M, Ayed FB, El-Hariry I, Spector N: Lapatinib (Tycerb) monotherapy in patients with recurrent inflammatory breast cancer: clinical activity and biological predictors of response. Annals Oncol. 2006, 1400a-Suppl 16
Blackwell KL, Burstein H, Pegram M, Storniolo A, Salazar VM, Maleski JE, Lin X, Spector N, Stein SH, Berger MS: Determining relevant biomarkers from tissue and serum that may predict response to single agent lapatinib in trastuzumab refractory metastatic breast cancer [abstract]: ASCO Annual Meeting Proceedings. J Clin Oncol. 2005, 23 (16S): 3004a-
Google Scholar
Gomez HL, Chavez MA, Doval DC, Chow LW, Wood BA, Berger MS, Sledge GW: A Phase II, randomized trial using the small molecule tyrosine kinase inhibitor lapatinib as a first-line treatment in patients with FISH positive advanced or metastatic breast cancer: ASCO Annual Meeting Proceedings. J Clin Oncol. 2004, 23 (14S): 3046a-
Google Scholar
Wong KK, Fracasso PM, Bukowski RM, Munster PN, Lynch T, Abbas R, Quinn SE, Zacharchuk C, Burris H: HKI-272, an irreversible pan erbB receptor tyrosine kinase inhibitor: preliminary phase 1 results in patients with solid tumors: ASCO Annual Meeting Proceedings. J Clin Oncol. 2006, 24 (18S): 3018a-
Google Scholar
Agus DB, Terlizzi E, Stopfer P, Amelsberg A, Gordon MS: Phase 1 dose escalation study of BIBW-2992, an irreversible dual EGFR/HER2 receptor tyrosine kinase inhibitor, in a continuous schedule in patients with advanced solid tumors: ASCO Annual Meeting Proceedings. J Clin Oncol. 2006, 24 (18S): 2074a-
Google Scholar
Gee JM, Harper ME, Hutcheson IR, Madden TA, Barrow D, Knowlden JM, McClelland RA, Jordan N, Wakeling AE, Nicholson RI: The antiepidermal growth factor receptor agent gefitinib (ZD1839/Iressa) improves antihormone response and prevents development of resistance in breast cancer in vitro. Endocrinology. 2003, 144: 5105-5117. 10.1210/en.2003-0705.
Article
CAS
PubMed
Google Scholar
Arpino G, Weiss H, Lee AV, Schiff R, DePlacido S, Osborne CK, Elledge RM: Estrogen receptor-positive, progesterone receptor-negative breast cancer: association with growth factor receptor expression and tamoxifen resistance. J Natl Cancer Inst. 2005, 97: 1254-1261.
Article
CAS
PubMed
Google Scholar
Lin NU, Carey LA, Liu MC, Younger J, Come SE, Bullitt E, Van Den Abbeele AD, Li X, Hockberg FH, Winer EP: Phase II trial of lapatinib for brain metastases in patients with HER2+ breast cancer. J Clin Oncol. 2006, 24: 503a-10.1200/JCO.2005.05.1458.
Article
Google Scholar
Nahta R, Yuan LXH, Zhang B, Kobayashi R, Esteva FJ: Lapatinib induces apoptosis in trastuzumab-resistant breast cancer cells: effects on insulin-like growth factor-I receptor 1 signaling. Mol Cancer Ther. 2007,
Google Scholar
Xia W, Husain I, Liu L, Bacus S, Saini S, Spohn J, Pry K, Westlund R, Stein S, Spector NL: Lapatinib anti-tumor activity is not dependent upon PTEN in ErbB2-overexpressing breast cancers. Cancer Res. 2007,
Google Scholar
Stephens P, Hunter C, Bignell G, Edkins S, Davies H, Teague J, Stevens C, O'Meara S, Smith R, Parker A, et al: Intragenic ERBB2 kinase mutations in tumors. Nature. 2004, 431: 525-526. 10.1038/431525b.
Article
CAS
PubMed
Google Scholar
Wang SE, Narasanna A, Perez-Torres M, Xiang B, Wu FY, Yang S, Carpenter G, Gazdar AF, Muthuswamy SK, Arteaga CL: HER2 kinase domain mutation results in constitutive phosphorylation and activation of HER2 and EGFR and resistance to EGFR tyrosine kinase inhibitors. Cancer Cell. 2006, 10: 25-38. 10.1016/j.ccr.2006.05.023.
Article
PubMed
Google Scholar
Budman DR, Soong R, Calabro A, Tai J, Diasio R: Identification of potentially useful combinations of epidermal growth factor receptor tyrosine kinase antagonists with conventional cytotoxic agents using median effect analysis. Anti-Cancer Drugs. 2006, 17: 921-928. 10.1097/01.cad.0000224457.36522.60.
Article
CAS
PubMed
Google Scholar
Xia W, Gerard C, Lui L, Baudson N, Ory T, Spector NL: Lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases synergizes with anti-ErbB2 antibodies to inhibit mediators of tumor cell survival and induce apoptosis in ErbB2 overexpressing breast cancer cells. Oncogene. 2005, 24: 6213-6221. 10.1038/sj.onc.1208774.
Article
CAS
PubMed
Google Scholar
Storniolo A, Burris H, Pegram M, Overmoyer B, Mille K, Jones S, Silverman P, Paul E, Loftiss J, Pandite L: A phase I, open-label study of lapatinib (GW572016) plus trastuzumab; a clinically active regimen [abstract]: ASCO Annual Meeting Proceedings. J Clin Oncol. 2005, 16S: 559a-
Google Scholar
Xia W, Bacus S, Hegde P, Husain I, Strum J, Liu L, Paulozzo G, Trusk P, Lyass L, Spector NL: A model of acquired autoresistance to ErbB2 tyrosine kinase inhibitors and a therapeutic strategy to prevent its onset in breast cancer. Proc Natl Acad Sci USA. 2006, 103: 7795-7800. 10.1073/pnas.0602468103.
Article
CAS
PubMed
PubMed Central
Google Scholar
Konecny GE, Meng YG, Untch M, Wang HJ, Bauerfeind I, Epstein M, Stieber P, Vernes JM, Gutierrez J, Hong K, et al: Association between HER-2/neu and vascular endothelial growth factor expression predicts clinical outcome in primary breast cancer patients. Clin Cancer Res. 2004, 10: 1706-1716. 10.1158/1078-0432.CCR-0951-3.
Article
CAS
PubMed
Google Scholar
Miller KD, Trigo JM, Wheeler C, Barge A, Rowbottom J, Sledge G, Baselga J: A multicenter phase II trial of ZD a vascular endothelial growth factor receptor-2 and epidermal growth factor receptor tyrosine kinase inhibition, in patients with previously treated metastatic breast cancer. Clin Cancer Res. 2005, 11: 3369-3376. 10.1158/1078-0432.CCR-04-1923.
Article
CAS
PubMed
Google Scholar