213
Views
21
CrossRef citations to date
0
Altmetric
Reviews

Small-molecule inhibitors of the human epidermal receptor family

, MD, , MD & , MDPhD
Pages 1829-1842 | Published online: 25 Nov 2009

Bibliography

  • Gross ME, Shazer RL, Agus DB. Targeting the HER-kinase axis in cancer. Semin Oncol 2004;31(Suppl 3):9-20
  • Barnes CJ, Kumar R. Epidermal growth factor receptor family tyrosine kinases as signal integrators and therapeutic targets. Cancer Metastasis Rev 2003;22:301-7
  • Riese DJ II, Stern DF. Specificity within the EGF family/ErbB receptor family signaling network. Bioessays 1998;20:41-8
  • Revillion F, Lhotellier V, Hornez L, ErbB/HER ligands in human breast cancer, and relationships with their receptors, the bio-pathological features and prognosis. Ann Oncol 2008;19:73-80
  • Pinkas-Kramarski R, Alroy I, Yarden Y. ErbB receptors and EGF-like ligands: cell lineage determination and oncogenesis through combinatorial signaling. J Mammary Gland Biol Neoplasia 1997;2:97-107
  • Pinkas-Kramarski R, Eilam R, Alroy I, Differential expression of NDF/neuregulin receptors ErbB-3 and ErbB-4 and involvement in inhibition of neuronal differentiation. Oncogene 1997;15:2803-15
  • Wada T, Qian XL, Greene MI. Intermolecular association of the p185neu protein and EGF receptor modulates EGF receptor function. Cell 1990;61:1339-47
  • Bulgaru AM, Mani S, Goel S, Perez-Soler R. Erlotinib (Tarceva): a promising drug targeting epidermal growth factor receptor tyrosine kinase. Expert Rev Anticancer Ther 2003;3:269-79
  • Neal DE, Mellon K. Epidermal growth factor receptor and bladder cancer: a review. Urol Int 1992;48:365-71
  • Pirker R, Pereira JR, Szczesna A, Cetuximab plus chemotherapy in patients with advanced non-small-cell lung cancer (FLEX): an open-label randomised phase III trial. Lancet 2009;373:1525-31
  • Modi S, D'Andrea G, Norton L, A phase I study of cetuximab/paclitaxel in patients with advanced-stage breast cancer. Clin Breast Cancer 2006;7:270-7
  • Xiong HQ, Rosenberg A, LoBuglio A, Cetuximab, a monoclonal antibody targeting the epidermal growth factor receptor, in combination with gemcitabine for advanced pancreatic cancer: a multicenter phase II Trial. J Clin Oncol 2004;22:2610-16
  • Dong M, Nio Y, Guo KJ, Epidermal growth factor and its receptor as prognostic indicators in Chinese patients with pancreatic cancer. Anticancer Res 1998;18:4613-19
  • Perez-Soler R, Chachoua A, Hammond LA, Determinants of tumor response and survival with erlotinib in patients with non-small-cell lung cancer. J Clin Oncol 2004;22:3238-47
  • Moyer JD, Barbacci EG, Iwata KK, Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res 1997;57:4838-48
  • Shepherd FA, Rodrigues Pereira J, Ciuleanu T, Erlotinib in previously treated non-small-cell lung cancer. N Engl J Med 2005;353:123-32
  • Herbst RS, Prager D, Hermann R, TRIBUTE: a phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer. J Clin Oncol 2005;23:5892-9
  • Gatzemeier U, Pluzanska A, Szczesna A, Phase III study of erlotinib in combination with cisplatin and gemcitabine in advanced non-small-cell lung cancer: the Tarceva Lung Cancer Investigation Trial. J Clin Oncol 2007;25:1545-52
  • Cappuzzo F, Stelmakh L, Cicenas S, SATURN: a double-blind, randomized, phase III study of maintenance erlotinib versus placebo following nonprogression with first-line platinum-based chemotherapy in patients with advanced NSCLC 2009 ASCO Annual Meeting: J Clin Oncol 2009;27(Suppl 15): Abstract 8001
  • Herbst RS, Johnson DH, Mininberg E, Phase I/II trial evaluating the anti-vascular endothelial growth factor monoclonal antibody bevacizumab in combination with the HER-1/epidermal growth factor receptor tyrosine kinase inhibitor erlotinib for patients with recurrent non-small-cell lung cancer. J Clin Oncol 2005;23:2544-55
  • Hainsworth J, Herbst R. A phase III, multicenter, placebo-controlled, double-blind, randomized clinical trial to evaluate the efficacy of bevacizumab (Avastin®) in combination with erlotinib (Tarceva®) compared with erlotinib alone for treatment of advanced non-small cell lung cancer after failure of standard first-line chemotherapy (BETA). J Thorac Oncol 2008;3(Suppl 4)
  • Miller VA, Soh C, Kabbinavar F. A randomized, double-blind, placebo-controlled, phase IIIb trial (ATLAS) comparing bevacizumab (B) therapy with or without erlotinib (E) after completion of chemotherapy with B for first-line treatment of locally advanced, recurrent, or metastatic non-small cell lung cancer (NSCLC). J Clin Oncol 2009;27(Suppl 18): Abstract LBA8002
  • Moore MJ, Goldstein D, Hamm J, Erlotinib plus gemcitabine compared with gemcitabine alone in patients with advanced pancreatic cancer: a phase III trial of the National Cancer Institute of Canada Clinical Trials Group. J Clin Oncol 2007;25:1960-6
  • Fukuoka M, Yano S, Giaccone G, Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (the IDEAL 1 trial) [corrected]. J Clin Oncol 2003;21:2237-46
  • Kris MG, Natale RB, Herbst RS, Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial. JAMA 2003;290:2149-58
  • Thatcher N, Chang A, Parikh P, Gefitinib plus best supportive care in previously treated patients with refractory advanced non-small-cell lung cancer: results from a randomised, placebo-controlled, multicentre study (Iressa Survival Evaluation in Lung Cancer). Lancet 2005;366:1527-37
  • Kim ES, Hirsh V, Mok T, Gefitinib versus docetaxel in previously treated non-small-cell lung cancer (INTEREST): a randomised phase III trial. Lancet 2008;372:1809-18
  • Giaccone G, Herbst RS, Manegold C, Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a phase III trial – INTACT 1. J Clin Oncol 2004;22:777-84
  • Herbst RS, Giaccone G, Schiller JH, Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a phase III trial – INTACT 2. J Clin Oncol 2004;22:785-94
  • Sharma SV, Bell DW, Settleman J, Haber DA. Epidermal growth factor receptor mutations in lung cancer. Nat Rev Cancer 2007;7:169-81
  • Paez JG, Janne PA, Lee JC, EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004;304:1497-500
  • Eberhard DA, Johnson BE, Amler LC, Mutations in the epidermal growth factor receptor and in KRAS are predictive and prognostic indicators in patients with non-small-cell lung cancer treated with chemotherapy alone and in combination with erlotinib. J Clin Oncol 2005;23:5900-9
  • Sordella R, Bell DW, Haber DA, Settleman J. Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science 2004;305:1163-7
  • Tracy S, Mukohara T, Hansen M, Gefitinib induces apoptosis in the EGFRL858R non-small-cell lung cancer cell line H3255. Cancer Res 2004;64:7241-4
  • Sequist LV, Martins RG, Spigel D, First-line gefitinib in patients with advanced non-small-cell lung cancer harboring somatic EGFR mutations. J Clin Oncol 2008;26:2442-9
  • Inoue A, Suzuki T, Fukuhara T, Prospective phase II study of gefitinib for chemotherapy-naive patients with advanced non-small-cell lung cancer with epidermal growth factor receptor gene mutations. J Clin Oncol 2006;24:3340-6
  • Yoshida K, Yatabe Y, Park JY, Prospective validation for prediction of gefitinib sensitivity by epidermal growth factor receptor gene mutation in patients with non-small cell lung cancer. J Thorac Oncol 2007;2:22-8
  • Jackman DM, Yeap BY, Sequist LV, Exon 19 deletion mutations of epidermal growth factor receptor are associated with prolonged survival in non-small cell lung cancer patients treated with gefitinib or erlotinib. Clin Cancer Res 2006;12:3908-14
  • Kobayashi S, Boggon TJ, Dayaram T, EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med 2005;352:786-92
  • Pao W, Miller VA, Politi KA, Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med 2005;2:e73
  • Balak MN, Gong Y, Riely GJ, Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors. Clin Cancer Res 2006;12:6494-501
  • Sasaki H, Endo K, Takada M, EGFR exon 20 insertion mutation in Japanese lung cancer. Lung Cancer 2007;58:324-8
  • Yun CH, Mengwasser KE, Toms AV, The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci USA 2008;105:2070-5
  • Keohavong P, DeMichele MA, Melacrinos AC, Detection of K-ras mutations in lung carcinomas: relationship to prognosis. Clin Cancer Res 1996;2:411-18
  • Rodenhuis S, van de Wetering ML, Mooi WJ, Mutational activation of the K-ras oncogene. A possible pathogenetic factor in adenocarcinoma of the lung. N Engl J Med 1987;317:929-35
  • Cho JY, Kim JH, Lee YH, Correlation between K-ras gene mutation and prognosis of patients with nonsmall cell lung carcinoma. Cancer 1997;79:462-7
  • Wallen M, Tomas E, Visakorpi T, Endometrial K-ras mutations in postmenopausal breast cancer patients treated with adjuvant tamoxifen or toremifene. Cancer Chemother Pharmacol 2005;55:343-6
  • Chen C, Liu FK, Qi XP, K-ras mutations in rectal cancer undergone preoperative radiotherapy. Zhonghua Wai Ke Za Zhi 2005;43:710-12
  • Lohr M, Kloppel G, Maisonneuve P, Frequency of K-ras mutations in pancreatic intraductal neoplasias associated with pancreatic ductal adenocarcinoma and chronic pancreatitis: a meta-analysis. Neoplasia 2005;7:17-23
  • Pao W, Wang TY, Riely GJ, KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib. PLoS Med 2005;2:e17
  • Birchmeier C, Birchmeier W, Gherardi E, Vande Woude GF. Met, metastasis, motility and more. Nat Rev Mol Cell Biol 2003;4:915-25
  • Miller CT, Lin L, Casper AM, Genomic amplification of MET with boundaries within fragile site FRA7G and upregulation of MET pathways in esophageal adenocarcinoma. Oncogene 2006;25:409-18
  • Jeffers M, Schmidt L, Nakaigawa N, Activating mutations for the met tyrosine kinase receptor in human cancer. Proc Natl Acad Sci USA 1997;94:11445-50
  • Bean J, Brennan C, Shih JY, MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proc Natl Acad Sci USA 2007;104:20932-7
  • Engelman JA, Zejnullahu K, Mitsudomi T, MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 2007;316:1039-43
  • Press MF, Bernstein L, Thomas PA, HER-2/neu gene amplification characterized by fluorescence in situ hybridization: poor prognosis in node-negative breast carcinomas. J Clin Oncol 1997;15:2894-904
  • McCann AH, Dervan PA, O'Regan M, Prognostic significance of c-erbB-2 and estrogen receptor status in human breast cancer. Cancer Res 1991;51:3296-303
  • Monoclonal antibody approved for metastatic breast cancer. Oncology (Williston Park) 1998;12:1727
  • Junttila TT, Akita RW, Parsons K, Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941. Cancer Cell 2009;15:429-40
  • Cho HS, Mason K, Ramyar KX, Structure of the extracellular region of HER2 alone and in complex with the Herceptin Fab. Nature 2003;421:756-60
  • Reid A, Vidal L, Shaw H, de Bono J. Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu). Eur J Cancer 2007;43:481-9
  • Spector NL, Xia W, Burris H III, 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 2005;23:2502-12
  • Rusnak DW, Lackey K, Affleck K, The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther 2001;1:85-94
  • Geyer CE, Forster J, Lindquist D, Lapatinib plus capecitabine for HER2-positive advanced breast cancer. N Engl J Med 2006;355:2733-43
  • Johnston S, Trudeau M, Kaufman B, Phase II study of predictive biomarker profiles for response targeting human epidermal growth factor receptor 2 (HER-2) in advanced inflammatory breast cancer with lapatinib monotherapy. J Clin Oncol 2008;26:1066-72
  • Burstein HJ, Storniolo AM, Franco S, A phase II study of lapatinib monotherapy in chemotherapy-refractory HER2-positive and HER2-negative advanced or metastatic breast cancer. Ann Oncol 2008;19:1068-74
  • Lin NU, Carey LA, Liu MC, Phase II trial of lapatinib for brain metastases in patients with human epidermal growth factor receptor 2-positive breast cancer. J Clin Oncol 2008;26:1993-9
  • Smylie M, Blumenschein G, Dowlati A, A phase II multicenter trial comparing two schedules of lapatinib (LAP) as first or second line monotherapy in subjects with advanced or metastatic non-small cell lung cancer (NSCLC) with either bronchioalveolar carcinoma (BAC) or no smoking history. 2007
  • Rusnak DW, Alligood KJ, Mullin RJ, 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. Cell Prolif 2007;40:580-94
  • Knowlden JM, Hutcheson IR, Jones HE, Elevated levels of epidermal growth factor receptor/c-erbB2 heterodimers mediate an autocrine growth regulatory pathway in tamoxifen-resistant MCF-7 cells. Endocrinology 2003;144:1032-44
  • Shou J, Massarweh S, Osborne CK, Mechanisms of tamoxifen resistance: increased estrogen receptor-HER2/neu cross-talk in ER/HER2-positive breast cancer. J Natl Cancer Inst 2004;96:926-35
  • Chu I, Blackwell K, Chen S, Slingerland J. 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. Cancer Res 2005;65:18-25
  • Chu QS, Cianfrocca ME, Goldstein LJ, A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer. Clin Cancer Res 2008;14:4484-90
  • Chen FL, Xia W, Spector NL. Acquired resistance to small molecule ErbB2 tyrosine kinase inhibitors. Clin Cancer Res 2008;14:6730-4
  • Nagy P, Friedlander E, Tanner M, Decreased accessibility and lack of activation of ErbB2 in JIMT-1, a herceptin-resistant, MUC4-expressing breast cancer cell line. Cancer Res 2005;65:473-82
  • Xia W, Bacus S, Hegde P, A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer. Proc Natl Acad Sci USA 2006;103:7795-800
  • Sergina NV, Rausch M, Wang D, Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3. Nature 2007;445:437-41
  • Soung YH, Lee JW, Kim SY, Somatic mutations of the ERBB4 kinase domain in human cancers. Int J Cancer 2006;118:1426-9
  • Tvorogov D, Sundvall M, Kurppa K, Somatic mutations of ErbB4: selective loss-of-function phenotype affecting signal transduction pathways in cancer. J Biol Chem 2009;284:5582-91
  • Gordon AN, Finkler N, Edwards RP, Efficacy and safety of erlotinib HCl, an epidermal growth factor receptor (HER1/EGFR) tyrosine kinase inhibitor, in patients with advanced ovarian carcinoma: results from a phase II multicenter study. Int J Gynecol Cancer 2005;15:785-92
  • Rivkin SE, MC, Iriarte D, Phase I/II lapatinib plus carboplatin and paclitaxel in stage III or IV relapsed ovarian cancer patients. J Clin Oncol 2008;26(Suppl): Abstract 5556
  • Oza AM, Eisenhauer EA, Elit L, Phase II study of erlotinib in recurrent or metastatic endometrial cancer: NCIC IND-148. J Clin Oncol 2008;26:4319-25
  • Stoehlmacher J, Geokkurt E, Arnold D, Associations between the EGFR status as well as KRAS mutations and clinical outcome in colorectal cancer (CRC) patients treated with erlotinib monotherapy in 2nd or 3rd line. A study of the Arbeitsgemeinschaft Internistische O. J Clin Oncol 2008;26(Suppl): Abstract 51
  • Fields AL, RD, Henderson CA, An open label multicenter phase II study of oral lapatinib as single agent, second line therapy in patients with metastatic colorectal cancer [Abstract 3583]. J Clin Oncol 2005;23(Suppl):266S
  • Gross ME, Jo S, Agus DB. Update on HER-kinase-directed therapy in prostate cancer. Clin Adv Hematol Oncol 2004;2:53-6,64
  • Di Lorenzo G, Tortora G, D'Armiento FP, Expression of epidermal growth factor receptor correlates with disease relapse and progression to androgen-independence in human prostate cancer. Clin Cancer Res 2002;8:3438-44
  • Dragovich T, McCoy S, Urba G, SWOG 0127: Phase II trial of erlotinib in GEJ and gastric adenocarcinomas. Presented at the ASCO Meeting: Gastrointestinal Cancers Symposium, 2005 [Abstract 49]
  • Iqbal S, GB, Lenz HJ, S0413: a phase II SWOG study of GW572016 (lapatinib) as first line therapy in patients with advanced gastric cancer. ASCO Annual Proceedings Part I. J Clin Oncol 2007;25(18 Suppl)
  • Cohen EE, Rosen F, Stadler WM, Phase II trial of ZD1839 in recurrent or metastatic squamous cell carcinoma of the head and neck. J Clin Oncol 2003;21:1980-7
  • Soulieres D, Senzer NN, Vokes EE, Multicenter phase II study of erlotinib, an oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with recurrent or metastatic squamous cell cancer of the head and neck. J Clin Oncol 2004;22:77-85
  • Siu LL, Soulieres D, Chen EX, Phase I/II trial of erlotinib and cisplatin in patients with recurrent or metastatic squamous cell carcinoma of the head and neck: a Princess Margaret Hospital phase II consortium and National Cancer Institute of Canada Clinical Trials Group Study. J Clin Oncol 2007;25:2178-83
  • Cavalot A, Martone T, Roggero N, Prognostic impact of HER-2/neu expression on squamous head and neck carcinomas. Head Neck 2007;29:655-64
  • Jermann M, Stahel RA, Salzberg M, A phase II, open-label study of gefitinib (IRESSA) in patients with locally advanced, metastatic, or relapsed renal-cell carcinoma. Cancer Chemother Pharmacol 2006;57:533-9
  • Dawson NA, Guo C, Zak R, A phase II trial of gefitinib (Iressa, ZD1839) in stage IV and recurrent renal cell carcinoma. Clin Cancer Res 2004;10:7812-19
  • Hainsworth JD, Sosman JA, Spigel DR, Treatment of metastatic renal cell carcinoma with a combination of bevacizumab and erlotinib. J Clin Oncol 2005;23:7889-96
  • Janne PA, von Pawel J, Cohen RB, Multicenter, randomized, phase II trial of CI-1033, an irreversible pan-ERBB inhibitor, for previously treated advanced non small-cell lung cancer. J Clin Oncol 2007;25:3936-44
  • Campos S, Hamid O, Seiden MV, Multicenter, randomized phase II trial of oral CI-1033 for previously treated advanced ovarian cancer. J Clin Oncol 2005;23:5597-604
  • Wong KK. HKI-272 in non small cell lung cancer. Clin Cancer Res 2007;13:s4593-6
  • Widakowich C, Dinh P, de Azambuja E, HER-2 positive breast cancer: what else beyond trastuzumab-based therapy? Anticancer Agents Med Chem 2008;8:488-96
  • Rabindran SK, Discafani CM, Rosfjord EC, Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res 2004;64:3958-65
  • Yang C, Shih J, Chao T, Use of BIBW 2992, a novel irreversible EGFR/HER2 TKI, to induce regression in patients with adenocarcinoma of the lung and activating EGFR mutations: preliminary results of a single-arm phase II clinical trial. J Clin Oncol 2008:26 (Suppl); Abstract 8026
  • Molife R, d BJS, Bell S, A phase II trial to compare BIBF 1120 or BIBW 2992 monotherapy versus a combination of sequential administration of both medications in patients with hormone refractory prostate cancer. Presented at the ASCO Meeting: Genitourinary Cancers Symposium 2009 [Abstract 203]
  • Janne PA, Schellens JH, Engelman JA, Preliminary activity and safety results from a phase I trial of PF-00299804, an irreversible pan-HER inhibitor, in patients with NSCLC. J Clin Oncol 2008:26 (Suppl); Abstract 8027
  • Erlichman C, Hidalgo M, Boni JP, Phase I study of EKB-569, an irreversible inhibitor of the epidermal growth factor receptor, in patients with advanced solid tumors. J Clin Oncol 2006;24:2252-60
  • Yarden Y. Biology of HER2 and its importance in breast cancer. Oncology 2001;61(Suppl 2):1-13

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.