Lapatinib

Recent Results in Cancer Research

Volumn 184, Issue , 2010, Pages 45-59

  Schneider Merck, Tanja ^a   Trepel, Martin ^a  

^a NONE

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATE; ANTHRACYCLINE; CAPECITABINE; CETUXIMAB; EPIDERMAL GROWTH FACTOR RECEPTOR; ERLOTINIB; FLUOROURACIL; FOLINIC ACID; GEFITINIB; GEMCITABINE; GROWTH FACTOR; HUMAN EPIDERMAL GROWTH FACTOR 1; HUMAN EPIDERMAL GROWTH FACTOR 2; IRINOTECAN; LAPATINIB; LETROZOLE; OXALIPLATIN; PACLITAXEL; PROTEIN TYROSINE KINASE; TAXANE DERIVATIVE; TRASTUZUMAB; UNCLASSIFIED DRUG;

ADD ON THERAPY; ANTINEOPLASTIC ACTIVITY; BILE DUCT CANCER; BINDING SITE; BREAST CANCER; CANCER INHIBITION; CLINICAL STUDY; CLINICAL TRIAL; DIARRHEA; DRUG DOSE REDUCTION; DRUG EFFICACY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG WITHDRAWAL; ENDOMETRIUM CANCER; ENZYME ACTIVITY; FATIGUE; HEADACHE; HEART FAILURE; HEART FUNCTION; HEART LEFT VENTRICLE EJECTION FRACTION; HEART OUTPUT; HUMAN; INTERSTITIAL PNEUMONIA; LIVER CIRRHOSIS; LIVER METASTASIS; LIVER TOXICITY; NAUSEA; OVARY CANCER; PANCREAS CANCER; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN FAMILY; RASH; RECOMMENDED DRUG DOSE; REVIEW; SIDE EFFECT; UNSPECIFIED SIDE EFFECT; VOMITING;

ANIMALS; ANTINEOPLASTIC AGENTS; CLINICAL TRIALS AS TOPIC; HUMANS; NEOPLASMS; PROTEIN KINASE INHIBITORS; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; RECEPTOR, ERBB-2;

EID: 77249112567     PISSN: 00800015     EISSN: None     Source Type: Book Series    
DOI: 10.1007/978-3-642-01222-8_4     Document Type: Review

References (88)

1. Atalay G, Cardoso F, Awada A, Piccart MJ (2003) Novel therapeutic strategies targeting the epidermal growth factor receptor (EGFR) family and its downstream effectors in breast cancer. Ann Oncol 14:1346-1363
2. Bence AK, Anderson EB, Halepota MA, Doukas MA, DeSimone PA, Davis GA, Smith DA, Koch KM, Stead AG, Mangum S, Bowen CJ, Spector NL, Hsieh S, Adams VR (2005) Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW572016, a dual EGFR-ErbB2 inhibitor, in healthy subjects. Invest New Drugs 23:39-49
3. Bilancia D, Rosati G, Dinota A, Germano D, Romano R, Manzione L (2007) Lapatinib in breast cancer. Ann Oncol 18(Suppl 6):26-30
4. Blackwell KL, Burstein H, Pegram M, Storniolo AM, Salazar VM, Maleski JE, Lin X, Spector N, Stein SH, Berger MS (2005) Determining relevant biomarkers from tissue and serum that may predict response to single agent lapatinib in trastuzumab refractory metastatic breast cancer. J Clin Oncol 23:3004
5. Blackwell KL, Kaplan EH, Franco SX, Marcom PK, Maleski JE, Sorensen MJ, Berger MS (2004) A phase II, open-label, multicenter study of GW572016 in patients with trastuzumab-refractory metastatic breast cancer. J Clin Oncol 22:3006
6. Burris HA 3rd (2004) Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist 9(Suppl 3):10-15
7. Burris HA 3rd, Hurwitz HI, Dees EC, Dowlati A, Blackwell KL, O'Neil B, Marcom PK, Ellis MJ, Overmoyer B, Jones SF, Harris JL, Smith DA, Koch KM, Stead A, Mangum S, Spector NL (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 with metastatic carcinomas. J Clin Oncol 23:5305-5313
8. Burstein H, Storniolo AM, Franco S, Salazar VM, Sorensen MJ, Stein SH (2004) A phase II, openlabel, multicenter study of lapatinib in two cohorts of patients with advanced or metastatic breast cancer who have progressed while receiving trastuzumab-containing regimens. Annal Oncol 15:1040
9. Cameron D, Casey M, Press M, Lindquist D, Pienkowski T, Romieu CG, Chan S, Jagiello-Gruszfeld A, Kaufman B, Crown J, Chan A, Campone M, Viens P, Davidson N, Gorbounova V, Raats JI, Skarlos D, Newstat B, Roychowdhury D, Paoletti P, Oliva C, Rubin S, Stein S, Geyer CE (2008) A phase III randomized comparison of lapatinib plus capecitabine versus capecitabine alone in women with advanced breast cancer that has progressed on trastuzumab: updated efficacy and biomarker analyses. Breast Cancer Res Treat 112:533-543
10. Cappuzzo F, Toschi L, Finocchiaro G, Ligorio C, Santoro A (2007) Surrogate predictive biomarkers for response to anti-EGFR agents: state of the art and challenges. Int J Biol Markers 22: S10-S23
11. Chu Q, Goldstein L, Murray N, Rowinsky E, Cianfrocca M, Gale M, Ho P, Paul E, Loftiss J, Pandite L (2005) A phase I, open-label study of the safety, tolerability and pharmacokinetics of lapatinib (GW572016) in combination with letrozole in cancer patients. J Clin Oncol 23:3001
12. Citri A, Yarden Y (2006) EGF-ERBB signalling: towards the systems level. Nat Rev Mol Cell Biol 7:505-516
13. Danielsen AJ, Maihle NJ (2002) The EGF/ErbB receptor family and apoptosis. Growth Factors 20:1-15
14. DeBono JS, Schwartz G, Monroe P (2003) Phase I and pharmacokinetics (PK) study of oral GW572016, a potent reversible dual inhibitor of both erbB1 and erbB2 tyrosine kinase (TK), administered in combination with cepecitabine. Proc Am Soc Clin Oncol 22:981a
15. Dees EC, Burris H, Hurwitz H, Dowlati A, Smith D, Koch K, Stead A, Mangum S, Harris J, Spector N (2004) Clinical summary of 67 heavily pretreated patients with metastatic carcinomas treated with GW572016 in a phase Ib study. J Clin Oncol 22:3188
16. DeSimone PA, Bence AK, Anderson EB, Halepota MA, Smith DA, Koch KM, Stead AG, Mangum SG, Spector NL, Davis GA, Doukas MA, Adams VR (2002) A phase I study to investigate the safety, tolerability, and pharmacokinetics of single oral escalating doses of GW572016 in healthy volunteers. Proc Am Soc Clin Oncol 21:375
17. Di Leo A, Gomez HL, Aziz Z, Zvirbule Z, Bines J, Arbushites MC, Guerrera SF, Koehler M, Oliva C, Stein SH, Williams LS, Dering J, Finn RS, Press MF (2008) Phase III, double-blind, randomized study comparing lapatinib plus paclitaxel with placebo plus paclitaxel as first-line treatment for metastatic breast cancer. J Clin Oncol 26:5544-5552
18. Geyer CE, Forster J, Lindquist D, Chan S, Romieu CG, Pienkowski T, Jagiello-Gruszfeld A, Crown J, Chan A, Kaufman B, Skarlos D, Campone M, Davidson N, Berger M, Oliva C, Rubin SD, Stein S, Cameron D (2006a) Lapatinib plus capecitabine for HER2-positive advanced breast cancer. N Engl J Med 355:2733-2743
19. Geyer CE, Forster JK, Cameron D (2006b) A phase III, randomized, open-label, international study comparing lapatinib and capecitabine vs capecitabine in women with refractory advanced or metastatic breast cancer (EGF100151). J Clin Oncol 24:3717-3718
20. Gomez HL, Chavez MA, Doval DC, Chow LWC, Wood BA, Berger MS, Sledge GW (2005) A phase II, randomized trial using the small molecule tyrosine kinase inhibitor lapatinib as a firstline treatment in patients with FISH positive advanced or metastatic breast cancer. J Clin Oncol 23:3046
21. Gomez HL, Doval DC, Chavez MA, Ang PC, Aziz Z, Nag S, Ng C, Franco SX, Chow LW, Arbushites MC, Casey MA, Berger MS, Stein SH, Sledge GW (2008) Efficacy and safety of lapatinib as first-line therapy for ErbB2-amplified locally advanced or metastatic breast cancer. J Clin Oncol 26:2999-3005
22. Graus-Porta D, Beerli RR, Daly JM, Hynes NE (1997) ErbB-2, the preferred heterodimerization partner of all ErbB receptors, is a mediator of lateral signaling. EMBO J 16:1647-1655
23. Gridelli C, Rossi A, Maione P, Ferrara C, Del Gaizo F, Guerriero C, Nicolella D, Palazzolo G, Falanga M, Colantuoni G (2008) New insights in drug development for the non-small cell lung cancer therapy. Front Biosci 13:5108-5119
24. Gril B, Palmieri D, Bronder JL, Herring JM, Vega-Valle E, Feigenbaum L, Liewehr DJ, Steinberg SM, Merino MJ, Rubin SD, Steeg PS (2008) Effect of lapatinib on the outgrowth of metastatic breast cancer cells to the brain. J Natl Cancer Inst 100:1092-1103
25. Ingle JN, Tu D, Pater JL, Martino S, Robert NJ, Muss HB, Piccart MJ, Castiglione M, Shepherd LE, Pritchard KI, Livingston RB, Davidson NE, Norton L, Perez EA, Abrams JS, Cameron DA, Palmer MJ, Goss PE (2006) Duration of letrozole treatment and outcomes in the placebo-controlled NCIC CTG MA.17 extended adjuvant therapy trial. Breast Cancer Res Treat 99:295-300
26. Johnston S, Pegram M, Press M, Pippen J, Pivot X, Gomez H, Florance A, O'Rourke L, Maltzman J, (2008) Lapatinib combined with letrozole vs. letrozole alone for front line postmenopausal hormone receptor positive (HR+) metastatic breast cancer (MBC): first results from the EGF30008 Trial. San Antonio Breast Cancer Symposium (abstract)
27. Johnston SR (2005) Clinical trials of intracellular signal transductions inhibitors for breast cancer- a strategy to overcome endocrine resistance. Endocr Relat Cancer 12(Suppl 1): S145-S157
28. Jones SF, Hainsworth JD, Spigel DR, Peacock NW, Willcutt NT, Pandite LN, Versola MJ, Koch KM, Greco F, Burris HA (2004) A phase I study of the dual kinase inhibitor GW572016 in combination with paclitaxel (EGF10009). J Clin Oncol 22:2083
29. Kaufman B, Trudeau ME, Johnston S, Awada A, Blackwell KL, Bachelot T, Salazar V, Westlund R, Desilvio M, Zaks T (2008) Clinical activity of lapatinib monotherapy in patients with HER2+ relapsed/refractory inflammatory breast cancer (IBC): Final results of the expanded HER2+ cohort in EGF103009. J Clin Oncol 26:636
30. Kim JW, Kim HP, Im SA, Kang S, Hur HS, Yoon YK, Oh DY, Kim JH, Lee DS, Kim TY, Bang YJ (2008) The growth inhibitory effect of lapatinib, a dual inhibitor of EGFR and HER2 tyrosine kinase, in gastric cancer cell lines. Cancer Lett 272:296-306
31. Klapper LN, Kirschbaum MH, Sela M, Yarden Y (2000) Biochemical and clinical implications of the ErbB/HER signaling network of growth factor receptors. Adv Cancer Res 77:25-79
32. Konecny GE, Pegram MD, Venkatesan N, Finn R, Yang G, Rahmeh M, Untch M, Rusnak DW, Spehar G, Mullin RJ, Keith BR, Gilmer TM, Berger M, Podratz KC, Slamon DJ (2006) Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells. Cancer Res 66:1630-1639
33. Lakhai WS, Beijnen JH, Den Boer SS, Westermann AM, Versola M, Koch K, Ho P, Pandite L, Richel DJ, Schellens J (2004) Phase I trial to determine the safety and tolerability of GW572016 in combination with oxaliplatin (OX)/5-fluorouracil (5-FU)/leucovorin (LV) [FOLFOX4] in patients with solid tumors. J Clin Oncol 22:2044
34. Lin NU, Carey LA, Liu MC, Younger J, Come SE, Ewend M, Harris GJ, Bullitt E, Van den Abbeele AD, Henson JW, Li X, Gelman R, Burstein HJ, Kasparian E, Kirsch DG, Crawford A, Hochberg F, Winer EP (2008) Phase II trial of lapatinib for brain metastases in patients with human epidermal growth factor receptor 2-positive breast cancer. J Clin Oncol 26:1993-1999
35. Lin NU, Dieras V, Paul D, Lossignol D, Christodoulou C, Laessig D, Roché H, Zembryki D, Oliva CR, Winer EP (2007) EGF105084, a phase II study of lapatinib for brain metastases in patients (pts) with HER2+ breast cancer following trastuzumab (H) based systemic therapy and cranial radiotherapy (RT). J Clin Oncol 25:1012
36. Lin NU, Winer EP (2004) New targets for therapy in breast cancer: small molecule tyrosine kinase inhibitors. Breast Cancer Res 6:204-210
37. Mackey JR, Kaufman B, Clemens M, Bapsy PP, Vaid A, Wardley A, Tjulandin S, Jahn M, Lehle M, Jones A (2006) Trastuzmab prolongs progressionfree survival in hormone-dependent and HER2-positive metastatic breast cancer. San Antonio breast cancer conference 2006 (abstract 3)
38. Medina PJ, Goodin S (2008) Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Clin Ther 30:1426-1447
39. Mendelsohn J, Baselga J (2003) Status of epidermal growth factor receptor antagonists in the biology and treatment of cancer. J Clin Oncol 21: 2787-2799
40. Midgley R, Flaherty KT, Haller DG, Versola MJ, Smith DA, Koch KM, Pandite L, Kerr DJ, O'Dwyer PJ, Middelton MR (2005) Phase I study of GW572016 (lapatinib), a dual kinase inhibitor, in combination with irinotecan (IR), 5-fluorouracil (FU) and leucovorin (LV). J Clin Oncol 23:3086
41. Milanezi F, Carvalho S, Schmitt FC (2008) EGFR/ HER2 in breast cancer: a biological approach for molecular diagnosis and therapy. Expert Rev Mol Diagn 8:417-434
42. Minami H, Nakagawa K, Kawada K, Mukai H, Tahara M, Kurata T, Uejima H, Nogami T, Sasaki Y, Fukuoka M (2004) A phase I study of GW572016 in patients with solid tumors. J Clin Oncol 22:3048
43. Montemurro F, Valabrega G, Aglietta M (2007) Lapatinib: a dual inhibitor of EGFR and HER2 tyrosine kinase activity. Expert Opin Biol Ther 7:257-268
44. Moy B, Goss PE (2006) Lapatinib: current status and future directions in breast cancer. Oncologist 11:1047-1057
45. Moy B, Goss PE (2007a) Lapatinib-associated toxicity and practical management recommendations. Oncologist 12:756-765
46. Moy B, Goss PE (2007b) TEACH: Tykerb evaluation after chemotherapy. Clin Breast Cancer 7: 489-492
47. Nahleh ZA (2008) Molecularly targeted therapy in breast cancer: the new generation. Recent Patents Anticancer Drug Discov 3:100-104
48. Nahta R, Hortobagyi GN, Esteva FJ (2003) Growth factor receptors in breast cancer: potential for therapeutic intervention. Oncologist 8:5-17
49. Nahta R, Yu D, Hung MC, Hortobagyi GN, Esteva FJ (2006) Mechanisms of disease: understanding resistance to HER2-targeted therapy in human breast cancer. Nat Clin Pract Oncol 3:269-280
50. Nelson MH, Dolder CR (2006) Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Ann Pharmacother 40:261-269
51. O'Shaughnessy J, Blackwell KL, Burstein H, Storniolo AM, Sledge G, Baselga J, Koehler M, Laabs S, Florance A, Roychowdhury D (2008) A randomized study of lapatinib alone or in combination with trastuzumab in heavily pretreated HER2+ metastatic breast cancer progressing on trastuzumab therapy. J Clin Oncol 26:1015
52. Okano J, Gaslightwala I, Birnbaum MJ, Rustgi AK, Nakagawa H (2000) Akt/protein kinase B isoforms are differentially regulated by epidermal growth factor stimulation. J Biol Chem 275: 30934-30942
53. Olayioye MA, Neve RM, Lane HA, Hynes NE (2000) The ErbB signaling network: receptor heterodimerization in development and cancer. EMBO J 19:3159-3167
54. Pandite L, Burris HA, Jones S, Wilding G, Taylor C, Versola MJ, Smith DA, Stead A, Koch KM, Spector NL (2004) A safety, tolerability, and pharmacokinetic (PK) study of GW572016 in patients with solid tumors. J Clin Oncol 22: 3179
55. Parkin DM, Bray F, Ferlay J, Pisani P (2005) Global cancer statistics, 2002. CA Cancer J Clin 55: 74-108
56. Piccart-Gebhart MJ, Procter M, Leyland-Jones B, Goldhirsch A, Untch M, Smith I, Gianni L, Baselga J, Bell R, Jackisch C, Cameron D, Dowsett M, Barrios CH, Steger G, Huang CS, Andersson M, Inbar M, Lichinitser M, Lang I, Nitz U, Iwata H, Thomssen C, Lohrisch C, Suter TM, Ruschoff J, Suto T, Greatorex V, Ward C, Straehle C, McFadden E, Dolci MS, Gelber RD (2005) Trastuzumab after adjuvant chemotherapy in HER2-positive breast cancer. N Engl J Med 353:1659-1672 (Pubitemid 41464705)
57. Prenzel N, Fischer OM, Streit S, Hart S, Ullrich A (2001) The epidermal growth factor receptor family as a central element for cellular signal transduction and diversification. Endocr Relat Cancer 8:11-31
58. Rahman A, Pazdur R, Wang Y, Huang SM, Lesko L (2007) The value meal: Effect of food on lapatinib bioavailability. J Clin Oncol 25: 5333-5334
59. Rapidis AD, Vermorken JB, Bourhis J (2008) Targeted therapies in head and neck cancer: past, present and future. Rev Recent Clin Trials 3: 156-166
60. Ratain MJ, Cohen EE (2007) The value meal: how to save $1, 700 per month or more on lapatinib. J Clin Oncol 25:3397-3398
61. Ravaud A, Hawkins R, Gardner JP, von der Maase H, Zantl N, Harper P, Rolland F, Audhuy B, Machiels JP, Petavy F, Gore M, Schoffski P, El-Hariry I (2008) Lapatinib versus hormone therapy in patients with advanced renal cell carcinoma: a randomized phase III clinical trial. J Clin Oncol 26:2285-2291
62. Reuter CW, Morgan MA, Eckardt A (2007) Targeting EGF-receptor-signalling in squamous cell carcinomas of the head and neck. Br J Cancer 96:408-416
63. Rivera F, Vega-Villegas ME, Lopez-Brea MF (2008) Cetuximab, its clinical use and future perspectives. Anticancer Drugs 19:99-113
64. Rocha-Lima CM, Soares HP, Raez LE, Singal R (2007) EGFR targeting of solid tumors. Cancer Control 14:295-304
65. Romond EH, Perez EA, Bryant J, Suman VJ, Geyer CE Jr, Davidson NE, Tan-Chiu E, Martino S, Paik S, Kaufman PA, Swain SM, Pisansky TM, Fehrenbacher L, Kutteh LA, Vogel VG, Visscher DW, Yothers G, Jenkins RB, Brown AM, Dakhil SR, Mamounas EP, Lingle WL, Klein PM, Ingle JN, Wolmark N (2005) Trastuzumab plus adjuvant chemotherapy for operable HER2-positive breast cancer. N Engl J Med 353:1673-1684
66. Rusnak DW, Affleck K, Cockerill SG, Stubberfield C, Harris R, Page M, Smith KJ, Guntrip SB, Carter MC, Shaw RJ, Jowett A, Stables J, Topley P, Wood ER, Brignola PS, Kadwell SH, Reep BR, Mullin RJ, Alligood KJ, Keith BR, Crosby RM, Murray DM, Knight WB, Gilmer TM, Lackey K (2001) The characterization of novel, dual ErbB-2/EGFR, tyrosine kinase inhibitors: potential therapy for cancer. Cancer Res 61: 7196-7203
67. Safran H, Iannitti D, Miner T, Demel K, Yoo D, Joseph P, Maia-Acuna C, Lockridge L, Evans D, Teresa K (2006) GW572016, gemcitabine and GW572016, gemcitabine, oxaliplatin, a twostage, phase I study for advanced pancreaticobiliary cancer. J Clin Oncol 24:4002
68. Singh BN, Malhotra BK (2004) Effects of food on the clinical pharmacokinetics of anticancer agents: underlying mechanisms and implications for oral chemotherapy. Clin Pharmacokinet 43: 1127-1156
69. Sliwkowski MX (2003) Ready to partner. Nat Struct Biol 10:158-159
70. Spector NL, Blackwell K, Hurley J, Harris JL, Lombardi D, Bacus S, Ahmed SB, Boussen H, Frikha M, Ayed FB (2006) EGF103009, a phase II trial of lapatinib monotherapy in patients with relapsed/refractory inflammatory breast cancer (IBC): Clinical activity and biologic predictors of response. J Clin Oncol 24:502
71. Spector NL, Xia W, Burris III H , Hurwitz H, Dees EC, Dowlati A, O'Neil B, Overmoyer B, Marcom PK, Blackwell KL, Smith DA, Koch KM, Stead A, Mangum S, Ellis MJ, Liu L, Man AK, Bremer TM, Harris J, Bacus S (2005) 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 23: 2502-2512
72. Stemmler J, Schmitt M, Willems A, Bernhard H, Harbeck N, Heinemann V (2006) Brain metastases in HER2-overexpressing metastatic breast cancer: comparative analysis of trastuzumab levels in serum and cerebrospinal fluid. J Clin Oncol 24:1525
73. Stern DF (2000) Tyrosine kinase signalling in breast cancer: ErbB family receptor tyrosine kinases. Breast Cancer Res 2:176-183
74. Storniolo AM, Burris HA 3rd, Pegram M, Overmoyer B, Miller K, Jones S, Silverman P, Paul E, Loftiss J, Pandite L (2005) A phase I, open-label study of lapatinib (GW572016) plus trastuzumab; a clinically active regimen. J Clin Oncol 23:559
75. Storniolo AM, Pegram MD, Overmoyer B, Silverman P, Peacock NW, Jones SF, Loftiss J, Arya N, Koch KM, Paul E, Pandite L, Fleming RA, Lebowitz PF, Ho PT, Burris HA 3rd (2008) Phase I dose escalation and pharmacokinetic study of lapatinib in combination with trastuzumab in patients with advanced ErbB2-positive breast cancer. J Clin Oncol 26:3317-3323
76. Toschi L, Cappuzzo F (2007) Understanding the new genetics of responsiveness to epidermal growth factor receptor tyrosine kinase inhibitors. Oncologist 12:211-220
77. Ulhoa-Cintra A, Greenberg L, Geyer CE (2008) The emerging role of lapatinib in HER2-positive breast cancer. Curr Oncol Rep 10:10-17
78. Valabrega G, Montemurro F, Aglietta M (2007) Trastuzumab: mechanism of action, resistance and future perspectives in HER2-overexpressing breast cancer. Ann Oncol 18:977-984
79. Versola M, Burris HA, Jones S, Wilding G, Taylor C, Pandite L, Smith DA, Stead A, Spector NL (2004) Clinical activity of GW572016 in EGF10003 in patients with solid tumors. J Clin Oncol 22:3047
80. Von Minckwitz G, Zielinski C, Maarteense E, Vogel P, Schmidt M, Eidtmann H, Cufer T, de Jongh FE, Kaufmann M, Loibl S (2008) Capecitabine vs. capecitabine + trastuzumab in patients with HER2-positive metastatic breast cancer progressing during trastuzumab treatment: the TBP phase III study (GBG 26/BIG 3-05). J Clin Oncol 26:1025
81. Witton CJ, Reeves JR, Going JJ, Cooke TG, Bartlett JM (2003) Expression of the HER1-4 family of receptor tyrosine kinases in breast cancer. J Pathol 200:290-297
82. Wood ER, Truesdale AT, McDonald OB, Yuan D, Hassell A, Dickerson SH, Ellis B, Pennisi C, Horne E, Lackey K, Alligood KJ, Rusnak DW, Gilmer TM, Shewchuk L (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. Cancer Res 64:6652-6659
83. Xia W, Gerard CM, Liu L, Baudson NM, Ory TL, Spector NL (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. Oncogene 24:6213-6221
84. Xia W, Liu LH, Ho P, Spector NL (2004) 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 23:646-653
85. Xia W, Mullin RJ, Keith BR, Liu LH, Ma H, Rusnak DW, Owens G, Alligood KJ, Spector NL (2002) Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Oncogene 21:6255-6263
86. Yarden Y (2001) Biology of HER2 and its importance in breast cancer. Oncology 61(Suppl 2):1-13
87. Yarden Y, Sliwkowski MX (2001) Untangling the ErbB signalling network. Nat Rev Mol Cell Biol 2:127-137
88. Zhou Y, Li S, Hu YP, Wang J, Hauser J, Conway AN, Vinci MA, Humphrey L, Zborowska E, Willson JK, Brattain MG (2006) 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 66:404-411