E7050: A dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models

Cancer Science

Volumn 101, Issue 1, 2010, Pages 210-215

  Nakagawa, Takayuki ^a   Tohyama, Osamu ^a   Yamaguchi, Atsumi ^a   Matsushima, Tomohiro ^a   Takahashi, Keiko ^a   Funasaka, Setsuo ^a   Shirotori, Shuji ^a   Asada, Makoto ^a   Obaishi, Hiroshi ^a  

^a EISAI CO LTD   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

E 7050; N [2 FLUORO 4 [[2 [4 (4 METHYLPIPERAZIN 1 YL)PIPERIDIN 1 YL]CARBONYLAMINOPYRIDIN 4 YL]OXY]PHENYL] N' (4 FLUOROPHENYL)CYCLOPROPANE 1,1 DICARBOXAMIDE TARTRATE; PROTEIN TYROSINE KINASE INHIBITOR; SCATTER FACTOR RECEPTOR; UNCLASSIFIED DRUG; VASCULOTROPIN RECEPTOR 2;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIANGIOGENIC ACTIVITY; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CELL CULTURE; CANCER INHIBITION; CANCER SURVIVAL; CONTROLLED STUDY; DRUG EFFICACY; DRUG MEGADOSE; DRUG POTENCY; DRUG STRUCTURE; DRUG TARGETING; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; MOUSE; NONHUMAN; NUDE MOUSE; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; RECEPTOR BLOCKING; TUMOR REGRESSION; TUMOR XENOGRAFT;

AMINOPYRIDINES; ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DISEASE PROGRESSION; FEMALE; HUMANS; MICE; NEOPLASMS, EXPERIMENTAL; PHOSPHORYLATION; PIPERAZINES; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-MET; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-2; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 71849098261     PISSN: 13479032     EISSN: 13497006     Source Type: Journal    
DOI: 10.1111/j.1349-7006.2009.01343.x     Document Type: Article

References (42)

1. Laird AD, Cherrington JM. Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents. Expert Opin Investig Drugs 2003, 12(1):51-64.
2. Knudsen BS, Vande Woude G. Showering c-MET-dependent cancers with drugs. Curr Opin Genet Dev 2008, 18(1):87-96.
3. Comoglio PM, Giordano S, Trusolino L. Drug development of MET inhibitors: targeting oncogene addiction and expedience. Nat Rev Drug Discov 2008, 7(6):504-16.
4. Christensen JG, Burrows J, Salgia R. c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention. Cancer Lett 2005, 225(1):1-26.
5. Maulik G, Shrikhande A, Kijima T, Ma PC, Morrison PT, Salgia R. Role of the hepatocyte growth factor receptor, c-Met, in oncogenesis and potential for therapeutic inhibition. Cytokine Growth Factor Rev 2002, 13(1):41-59.
6. Stabile LP, Rothstein ME, Keohavong P. Therapeutic targeting of human hepatocyte growth factor with a single neutralizing monoclonal antibody reduces lung tumorigenesis. Mol Cancer Ther 2008, 7(7):1913-22.
7. Shinomiya N, Gao CF, Xie Q. RNA interference reveals that ligand-independent met activity is required for tumor cell signaling and survival. Cancer Res 2004, 64(21):7962-70.
8. Herynk MH, Stoeltzing O, Reinmuth N. Down-regulation of c-Met inhibits growth in the liver of human colorectal carcinoma cells. Cancer Res 2003, 63(11):2990-6.
9. Anderson MR, Harrison R, Atherfold PA. Met receptor signaling: a key effector in esophageal adenocarcinoma. Clin Cancer Res 2006, 12(20 Pt 1):5936-43.
10. Maulik G, Kijima T, Ma PC. Modulation of the c-Met/hepatocyte growth factor pathway in small cell lung cancer. Clin Cancer Res 2002, 8(2):620-7.
11. Trusolino L, Comoglio PM. Scatter-factor and semaphorin receptors: cell signalling for invasive growth. Nat Rev Cancer 2002, 2(4):289-300.
12. Kuniyasu H, Yasui W, Kitadai Y, Yokozaki H, Ito H, Tahara E. Frequent amplification of the c-met gene in scirrhous type stomach cancer. Biochem Biophys Res Commun 1992, 189(1):227-32.
13. 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(3):409-18.
14. Zhao X, Weir BA, LaFramboise T. Homozygous deletions and chromosome amplifications in human lung carcinomas revealed by single nucleotide polymorphism array analysis. Cancer Res 2005, 65(13):5561-70.
15. Di Renzo MF, Olivero M, Giacomini A. Overexpression and amplification of the met/HGF receptor gene during the progression of colorectal cancer. Clin Cancer Res 1995, 1(2):147-54.
16. Tsugawa K, Yonemura Y, Hirono Y. Amplification of the c-met, c-erbB-2 and epidermal growth factor receptor gene in human gastric cancers: correlation to clinical features. Oncology 1998, 55(5):475-81.
17. Nakajima M, Sawada H, Yamada Y. The prognostic significance of amplification and overexpression of c-met and c-erb B-2 in human gastric carcinomas. Cancer 1999, 85(9):1894-902.
18. Engelman JA, Zejnullahu K, Mitsudomi T. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 2007, 316(5827):1039-43.
19. 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 U S A 2007, 104(52):20932-7.
20. Folkman J, Watson K, Ingber D, Hanahan D. Induction of angiogenesis during the transition from hyperplasia to neoplasia. Nature 1989, 339(6219):58-61.
21. Hanahan D, Folkman J. Patterns and emerging mechanisms of the angiogenic switch during tumorigenesis. Cell 1996, 86(3):353-64.
22. Carmeliet P, Jain RK. Angiogenesis in cancer and other diseases. Nature 2000, 407(6801):249-57.
23. Folkman J, Klagsbrun M. Angiogenic factors. Science 1987, 235(4787):442-7.
24. Kanno S, Oda N, Abe M. Roles of two VEGF receptors, Flt-1 and KDR, in the signal transduction of VEGF effects in human vascular endothelial cells. Oncogene 2000, 19(17):2138-46.
25. Kim KJ, Li B, Winer J. Inhibition of vascular endothelial growth factor-induced angiogenesis suppresses tumour growth in vivo. Nature 1993, 362(6423):841-4.
26. Wilhelm SM, Carter C, Tang L. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res 2004, 64(19):7099-109.
27. Mendel DB, Laird AD, Xin X. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res 2003, 9(1):327-37.
28. Asano M, Yukita A, Matsumoto T, Kondo S, Suzuki H. Inhibition of tumor growth and metastasis by an immunoneutralizing monoclonal antibody to human vascular endothelial growth factor/vascular permeability factor121. Cancer Res 1995, 55(22):5296-301.
29. Nakamura K, Taguchi E, Miura T. KRN951, a highly potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, has antitumor activities and affects functional vascular properties. Cancer Res 2006, 66(18):9134-42.
30. Van Belle E, Witzenbichler B, Chen D. Potentiated angiogenic effect of scatter factor/hepatocyte growth factor via induction of vascular endothelial growth factor: the case for paracrine amplification of angiogenesis. Circulation 1998, 97(4):381-90.
31. Gerritsen ME, Tomlinson JE, Zlot C, Ziman M, Hwang S. Using gene expression profiling to identify the molecular basis of the synergistic actions of hepatocyte growth factor and vascular endothelial growth factor in human endothelial cells. Br J Pharmacol 2003, 140(4):595-610.
32. Zhang YW, Su Y, Volpert OV, Vande Woude GF. Hepatocyte growth factor/scatter factor mediates angiogenesis through positive VEGF and negative thrombospondin 1 regulation. Proc Natl Acad Sci U S A 2003, 100(22):12718-23.
33. Matsui J, Yamamoto Y, Funahashi Y. E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer 2008, 122(3):664-71.
34. Smolen GA, Sordella R, Muir B. Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc Natl Acad Sci U S A 2006, 103(7):2316-21.
35. Boku T, Nakane Y, Minoura T. Prognostic significance of serosal invasion and free intraperitoneal cancer cells in gastric cancer. Br J Surg 1990, 77(4):436-9.
36. Kodera Y, Nakanishi H, Yamamura Y. Prognostic value and clinical implications of disseminated cancer cells in the peritoneal cavity detected by reverse transcriptase-polymerase chain reaction and cytology. Int J Cancer 1998, 79(4):429-33.
37. Zeng ZS, Weiser MR, Kuntz E. c-Met gene amplification is associated with advanced stage colorectal cancer and liver metastases. Cancer Lett 2008, 265(2):258-69.
38. Lutterbach B, Zeng Q, Davis LJ. Lung cancer cell lines harboring MET gene amplification are dependent on Met for growth and survival. Cancer Res 2007, 67(5):2081-8.
39. Zou HY, Li Q, Lee JH. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res 2007, 67(9):4408-17.
40. Zhang Y, Kaplan-Lefko PJ, Rex K. Identification of a novel recepteur d'origine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo. Cancer Res 2008, 68(16):6680-7.
41. Martens T, Schmidt NO, Eckerich C. A novel one-armed anti-c-Met antibody inhibits glioblastoma growth in vivo. Clin Cancer Res 2006, 12(20 Pt 1):6144-52.
42. Asano M, Yukita A, Suzuki H. Wide spectrum of antitumor activity of a neutralizing monoclonal antibody to human vascular endothelial growth factor. Jpn J Cancer Res 1999, 90(1):93-100.