E7080 (Lenvatinib), a Multi-Targeted Tyrosine Kinase Inhibitor, Demonstrates Antitumor Activities Against Colorectal Cancer Xenografts

Neoplasia (United States)

Volumn 16, Issue 11, 2014, Pages 972-981

  Wiegering, Armin ^a,b   Korb, Doreen ^a   Thalheimer, Andreas ^a,e   Kämmerer, Ulrike ^a   Allmanritter, Jan ^c   Matthes, Niels ^a   Linnebacher, Michael ^d   Schlegel, Nicolas ^a   Klein, Ingo ^a   Ergün, Süleyman ^c   Germer, Christoph Thomas ^a   Otto, Christoph ^a  

^a UNIVERSITY HOSPITAL WÜRZBURG   (Germany)

^b UNIVERSITY OF WÜRZBURG   (Germany)

^c UNIVERSITY OF WÜRZBURG   (Germany)

^d UNIVERSITY OF ROSTOCK   (Germany)

^e Viszeral und Unfallchirurgie   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

CARBONATE DEHYDRATASE IX; COLLAGEN; K RAS PROTEIN; LENVATINIB; MESSENGER RNA; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; MYC PROTEIN; VASCULOTROPIN; VASCULOTROPIN RECEPTOR; VASCULOTROPIN RECEPTOR 1; VASCULOTROPIN RECEPTOR 3; CARBANILAMIDE DERIVATIVE; KI 67 ANTIGEN; PROTEIN KINASE INHIBITOR; QUINOLINE DERIVATIVE; RAS PROTEIN;

ANGIOGENESIS ASSAY; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIANGIOGENIC ACTIVITY; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER GROWTH; CAPILLARY DENSITY; CELL GROWTH; CELL PROLIFERATION; CELL STIMULATION; CELL VIABILITY; COLORECTAL CANCER; COMPARATIVE STUDY; CONTROLLED STUDY; DRUG EFFICACY; ENDOTHELIUM CELL; EX VIVO STUDY; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; SIGNAL TRANSDUCTION; SUPERNATANT; TUMOR XENOGRAFT; UPREGULATION; ANIMAL; CACO 2 CELL LINE; CELL CULTURE; CELL SURVIVAL; COLORECTAL NEOPLASMS; DRUG EFFECTS; DRUG SCREENING; GENE EXPRESSION; GENETICS; HCT116 CELL LINE; HT 29 CELL LINE; IC50; INBRED MOUSE STRAIN; METABOLISM; MUTATION; NEOVASCULARIZATION, PATHOLOGIC; NUDE MOUSE; PROCEDURES; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; TREATMENT OUTCOME; TUMOR CELL LINE; UMBILICAL VEIN ENDOTHELIAL CELL;

ANIMALS; CACO-2 CELLS; CELL LINE, TUMOR; CELL SURVIVAL; CELLS, CULTURED; COLORECTAL NEOPLASMS; FEMALE; GENE EXPRESSION; HCT116 CELLS; HT29 CELLS; HUMAN UMBILICAL VEIN ENDOTHELIAL CELLS; HUMANS; INHIBITORY CONCENTRATION 50; KI-67 ANTIGEN; MICE, INBRED STRAINS; MICE, NUDE; MUTATION; NEOVASCULARIZATION, PATHOLOGIC; PHENYLUREA COMPOUNDS; PROTEIN KINASE INHIBITORS; QUINOLINES; RAS PROTEINS; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION; TREATMENT OUTCOME; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84937552291     PISSN: 15228002     EISSN: 14765586     Source Type: Journal    
DOI: 10.1016/j.neo.2014.09.008     Document Type: Article

References (46)

1. Siegel R., Desantis C., Jemal A. Colorectal cancer statistics, 2014. CA Cancer J Clin 2014, 64(2):104-117.
2. Lorenz M., Staib-Sebler E., Hochmuth K., Heinrich S., Gog C., Vetter G., Encke A., Muller H.H. Surgical Resection of Liver Metastases of Colorectal Carcinoma: Short and Long-Term Results. Semin Oncol 2000, 27(5 Suppl. 10):112-119.
3. Folkman J. Angiogenesis in cancer, vascular, rheumatoid and other disease. Nat Med 1995, 1(1):27-31.
4. Goel H.L., Mercurio A.M. VEGF targets the tumour cell. Nat Rev Cancer 2013, 13(12):871-882.
5. Cunningham D., Humblet Y., Siena S., Khayat D., Bleiberg H., Santoro A., Bets D., Mueser M., Harstrick A., Verslype C., et al. Cetuximab monotherapy and cetuximab plus irinotecan in irinotecan-refractory metastatic colorectal cancer. N Engl J Med 2004, 4:337-345.
6. Hurwitz H., Fehrenbacher L., Novotny W., Cartwright T., Hainsworth J., Heim W., Berlin J., Baron A., Griffing S., Holmgren E., et al. Bevacizumab Plus Irinotecan, Fluorouracil, and Leucovorin for Metastatic Colorectal Cancer. N Engl J Med 2004, 23:2335-2342.
7. Hubbard J., Grothey A. Antiangiogenesis agents in colorectal cancer. Curr Opin Oncol 2010, 22:374-380.
8. Saltz L.B., Clarke S., Díaz-Rubio E., Scheithauer W., Figer A., Wong R., Koski S., Lichinitser M., Yang T.S., Rivera F., et al. Bevacizumab in combination with oxaliplatin-based chemotherapy as first-line therapy in metastatic colorectal cancer: a randomized phase III study. J Clin Oncol 2008, 26:2013-2019.
9. Bos J.L., Fearon E.R., Hamilton S.R., et al. Prevalence of ras gene mutations in human colorectal cancers. Nature 1987, 327:293-297.
10. Mulder K., Scarfe A., Chua N., Spratlin J. The role of bevacizumab in colorectal cancer: understanding its benefits and limitations. Expert Opin Biol Ther 2011, 11:405-413.
11. Marques I., Araújo A., de Mello R.A. Anti-angiogenic therapies for metastatic colorectal cancer: current and future perspectives. World J Gastroenterol 2013, 19(44):7955-7971.
12. Shamloo B.K., Chhabra P., Freedman A.N., Potosky A., Malin J., Weiss Smith S. Novel adverse events of bevacizumab in the US FDA adverse event reporting system database: a disproportionality analysis. Drug Saf 2012, 35:507-518.
13. Yancopoulos G.D., Davis S., Gale N.W., Rudge J.S., Wiegand S.J., Holash J. Vascular-specific growth factors and blood vessel formation. Nature 2000, 407:242-248.
14. Abou-Elkacem L., Arns S., Brix G., Gremse F., Zopf D., Kiessling F., Lederle W. Regorafenib inhibits growth, angiogenesis, and metastasis in a highly aggressive, orthotopic colon cancer model. Mol Cancer Ther 2013, 12:1322-1331.
15. Grothey A., Van Cutsem E., Sobrero A., Siena S., Falcone A., Ychou M., Humblet Y., Bouché O., Mineur L., Barone C., et al. Regorafenib monotherapy for previously treated metastatic colorectal cancer (CORRECT): an international, multicentre, randomised, placebo-controlled, phase 3 trial. Lancet 2013, 381:303-312.
16. Matsui J., Yamamoto Y., Funahashi Y., Tsuruoka A., Watanabe T., Wakabayashi T., Uenaka T., Asada M. 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):664-671.
17. Okamoto K., Kodama K., Takase K., Sugi N.H., Yamamoto Y., Iwata M., Tsuruoka A. Antitumor activities of the targeted multi-tyrosine kinase inhibitor lenvatinib (E7080) against RET gene fusion-driven tumor models. Cancer Lett 2013, 340(1):97-103.
18. Matsui J., Funahashi Y., Uenaka T., Watanabe T., Tsuruoka A., Asada M. Multi-kinase inhibitor E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of vascular endothelial growth factor-receptor (VEGF-R) 2 and VEGF-R3 kinase. Clin Cancer Res 2008, 14:5459-5465.
19. Ikuta K., Yano S., Trung V.T., Hanibuchi M., Goto H., Li Q., Wang W., Yamada T., Ogino H., Kakiuchi S., et al. E7080, a multi-tyrosine kinase inhibitor, suppresses the progression of malignant pleural mesothelioma with different proangiogenic cytokine production profiles. Clin Cancer Res 2009, 15:7229-7237.
20. Glen H., Mason S., Patel H., Macleod K., Brunton V.G. E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion. BMC Cancer 2011, 22(11):309. 10.1186/1471-2407-11-309.
21. Maletzki C., Stier S., Gruenert U., Gock M., Ostwald C., Prall F., Linnebacher M. Establishment, characterization and chemosensitivity of three mismatch repair deficient cell lines from sporadic and inherited colorectal carcinomas. PLoS One 2012, 7(12):e52485. [Epub 2012 Dec 31]. 10.1371/journal.pone.0052485.
22. Otto C., Kämmerer U., Illert B., Mühling M., Pfetzer N., Wittig R., Ulrich Völker H.U., Thiede A., Coy J.F. Growth of human gastric cancer cells in nude mice is delayed by a ketogenic diet supplemented with omega-3 fatty acids and medium-chain triglycerides. BMC Cancer 2008, 30(8):122. 10.1186/1471-2407-8-122.
23. Illert B., Otto C., Thiede A., Timmermann W. Detection of disseminated tumor cells in nude mice with human gastric cancer. Clin Exp Metastasis 2003, 20(6):549-554.
24. Altun A., Temiz T.K., Balci E., Polat Z.A., Turan M. Effects of tyrosine kinase inhibitor E7080 and eNOS inhibitor L-NIO on colorectal cancer alone and in combination. Chin J Cancer Res 2013, 25(5):572-584.
25. Altun A., Turgut N.H., Kaya T.T. Anticancer effect of COX-2 inhibitor DuP-697 alone and in combination with tyrosine kinase inhibitor (E7080) on colon cancer cell lines. Asian Pac J Cancer Prev 2014, 15(7):3113-3121.
26. Ogino H., Hanibuchi M., Kakiuchi S., Trung V.T., Goto H., Ikuta K., Yamada T., Uehara H., Tsuruoka A., Uenaka T., et al. E7080 suppresses hematogenous multiple organ metastases of lung cancer cells with nonmutated epidermal growth factor receptor. Mol Cancer Ther 2011, 10:1218-1228.
27. Hanahan D., Weinberg R.A. The hallmarks of cancer. Cell 2000, 100(1):57-70.
28. Bergers G., Benjamin L.E. Tumorigenesis and the angiogenic switch. Nat Rev Cancer 2003, 3:401-410.
29. Folkman J., Merler E., Abernathy C., Williams G. Isolation of a tumor factor responsible for angiogenesis. J Exp Med 1971, 133(2):275-288.
30. Albini A., Tosetti F., Li V.W., Noonan D.M., Li W.W. Cancer prevention by targeting angiogenesis. Nat Rev Clin Oncol 2012, 9(9):498-509.
31. Hanahan D., Folkman J. Patterns and emerging mechanisms of the angiogenic switch during tumorigenesis. Cell 1996, 86(3):353-364.
32. Kim K.J., Li B., Winer J., Armanini M., Gillett N., Phillips H.S., Ferrara N. Inhibition of vascular endothelial growth factor-induced angiogenesis suppresses tumour growth in vivo. Nature 1993, 362(6423):841-844.
33. Chen C.T., Hung M.C. Beyond anti-VEGF: dual-targeting antiangiogenic and antiproliferative therapy. Am J Transl Res 2013, 5:393-403.
34. Funovics P., Brostjan C., Nigisch A., Fila A., Grochot A., Mleczko K., Was H., Weigel G., Dulak J., Jozkowicz A. Effects of 15d-PGJ(2) on VEGF-induced angiogenic activities and expression of VEGF receptors in endothelial cells. Prostaglandins Other Lipid Mediat 2006, 79:230-244.
35. Hurley N.E., Schildmeyer L.A., Bosworth K.A., Sakurai Y., Eskin S.G., Hurley L.H., McIntire L.V. Modulating the functional contributions of c-Myc to the human endothelial cell cyclic strain response. J Vasc Res 2010, 47(1):80-90.
36. Adhikary S., Eilers M. Transcriptional regulation and transformation by Myc proteins. Nat Rev Mol Cell Biol 2005, 6(8):635-645.
37. Olive P.L., Aquino-Parsons C., MacPhail S.H., Liao S.Y., Raleigh J.A., Lerman M.I., Stanbridge E.J. Carbonic anhydrase 9 as an endogenous marker for hypoxic cells in cervical cancer. Cancer Res 2001, 61(24):8924-8929.
38. Lock F.E., McDonald P.C., Lou Y., Serrano I., Chafe S.C., Ostlund C., Aparicio S., Winum J.Y., Supuran C.T., Dedhar S. Targeting carbonic anhydrase IX depletes breast cancer stem cells within the hypoxic niche. Oncogene 2013, 32(44):5210-5219.
39. Gatenby R.A., Gillies R.J. Why do cancers have high aerobic glycolysis?. Nat Rev Cancer 2004, 4(11):891-899.
40. Cairns R.A., Harris I.S., Mak T.W. Regulation of cancer cell metabolism. Nat Rev Cancer 2011, 11(2):85-95.
41. Hanahan D., Weinberg R.A. Hallmarks of cancer: the next generation. Cell 2011, 144(5):646-674.
42. Winder T., Lenz H.J. Vascular endothelial growth factor and epidermal growth factor signaling pathways as therapeutic targets for colorectal cancer. Gastroenterology 2010, 138:2163-2176.
43. Amado R.G., Wolf M., Peeters M., Van Cutsem E., Siena S., Freeman D.J., Juan T., Sikorski R., Suggs S., Radinsky R., et al. Wild-type KRAS is required for panitumumab efficacy in patients with metastatic colorectal cancer. J Clin Oncol 2008, 26(10):1626-1634.
44. Yamada K., Yamamoto N., Yamada Y., Nokihara H., Fujiwara Y., Hirata T., Koizumi F., Nishio K., Koyama N., Tamura T. Phase I dose-escalation study and biomarker analysis of E7080 in patients with advanced solid tumors. Clin Cancer Res 2011, 17:2528-2537.
45. Boss D.S., Glen H., Beijnen J.H., Keesen M., Morrison R., Tait B., Copalu W., Mazur A., Wanders J., O'Brien J.P., et al. A phase I study of E7080, a multitargeted tyrosine kinase inhibitor, in patients with advanced solid tumours. Br J Cancer 2012, 106:1598-1604.
46. Molina A.M., Hutson T.E., Larkin J., Gold A.M., Wood K., Carter D., Motzer R., Michaelson M.D. A phase 1b clinical trial of the multi-targeted tyrosine kinase inhibitor lenvatinib (E7080) in combination with everolimus for treatment of metastatic renal cell carcinoma (RCC). Cancer Chemother Pharmacol 2014, 73:181-189.