616
Views
22
CrossRef citations to date
0
Altmetric
Reviews

Emerging VEGF-receptor inhibitors for colorectal cancer

, MD PhD, , MD PhD, , MD PhD, , MD PhD, , MD PhD, & show all
Pages 25-37 | Published online: 06 Dec 2012

Bibliography

  • Siegel R, Ward E, Brawley O, Cancer statistics. CA Cancer J Clin 2011;61:212-36
  • Available from: http://globocan.iarc.fr
  • Jemal A, Bray F, Center MM, Global cancer statistics. CA Cancer J Clin 2011;61:69-90
  • Douillard JY, Cunningham D, Roth AD, Irinotecan combined with fluorouracil compared with fluorouracil alone as first-line treatment for metastatic colorectal cancer: a multicentre randomized trial. Lancet 2000;355:1041-7
  • Saltz LB, Cox JV, Blanke C, Irinotecan plus fluorouracil and leucovorin for metastatic colorectal cancer. N Engl J Med 2000;343:905-14
  • Goldberg RM, Sargent DJ, Morton RF, A randomized controlled trial of fluorouracil plus leucovorin, irinotecan, and oxaliplatin combinations in patients with previously untreated metastatic colorectal cancer. J Clin Oncol 2004;22:23-30
  • Folkman J. Tumor angiogenesis: therapeutic implications. N Engl J Med 1971;285:1182-6
  • Hicklin DJ, Ellis LM. Role of the vascular endothelial growth factor pathway in tumor growth and angiogenesis. J Clin Oncol 2005;23:1011-27
  • Hurwitz H, Fehrenbacher L, Novotny W, Bevacizumab plus irinotecan, fluorouracil, and leucovorin for metastatic colorectal cancer. N Engl J Med 2004;350:2335-42
  • Saltz LB. Irinotecan plus fluorouracil and leucovorin for metastatic colorectal cancer. Irinotecan Study Group. N Engl J Med 2000;343:905-14
  • Goldberg RM. A randomized controlled trial of fluorouracil plus leucovorin, irinotecan, and oxaliplatin combinations in patients with previously untreated metastatic colorectal cancer. J Clin Oncol 2004;22:23-30
  • Kabbinavar FF, Hurwitz HI, Sarkar S, Addition of bevacizumab to fluorouracil.based first-line treatment of metastatic colorectal cancer: pooled analysis of cohorts of older patients from two randomized clinical trials. J Clin Oncol 2009;27:199-205
  • Saltz LB, Clarke S, Diaz-Rubio E, Bevacizumab in combination with oxaliplatin-based chemotherapy as first-line therapy in metastatic colorectal cancer: a randomized phase III study. J Clin Oncol 2008;26:2013-19
  • Fuchs CS, Marshall J, Mitchell E, Randomized, controlled trial of irinotecan plus infusional, bolus, or oral fluoropyrimidines in first-line treatment of metastatic colorectal cancer: results from the BICC-C study. J Clin Oncol 2007;25:4779-86
  • Kopetz S, Hoff PM, Morris JS, Phase II trial of infusional fluorouracil, irinotecan,and bevacizumab for metastatic colorectal cancer: efficacy and circulating angiogenic biomarkers associated with therapeutic resistance. J Clin Oncol 2010;28:453-9
  • Diaz-Rubio E, Gomez A, Massuti B, First-line XELOX plus bevacizumab followed by XELOX plus bevacizumab or single-agent bevacizumab as maintenance therapy in patients with metastatic colorectal cancer: the phase III MACRO TTD study. Oncologist 2012;17:15-25
  • Wagner AD, Arnold D, Grothey AA, Anti-angiogenic therapies for metastatic colorectal cancer. Cochrane Database Syst Rev 2009;CD005392
  • Grothey A, Sugrue MM, Purdie DM, Bevacizumab beyond first progression is associated with prolonged overall survival in metastatic colorectal cancer: results from a large observational cohort study (BRiTE). J Clin Oncol 2008;26:5326-34
  • Arnold D, Andre T, Bennouna J, Bevacizumab plus chemotherapy continued beyond first progression in patients with metastatic colorectal cancer previously treated with bevacizumab plus CT: results of a randomized phase III intergroup study (TML study). J Clin Oncol 2012;30(Suppl):abstract CRA3503
  • Andre T, Van Cutsem E, Schmoll J, A multinational, randomized phase III study of bevacizumab (Bev) with FOLFOX4 or XELOX versus FOLFOX4 alone as adjuvant treatment for colon cancer (CC): Subgroup analyses from the AVANT trial. J Clin Oncol 2011;29(Suppl):abstract 3509
  • Prat A, Casado E, Cortes J. New approaches in angiogenic targeting for colorectal cancer. World J Gastroenterol 2007;13:5857-66
  • Sobrero A, Ackland S, Clarke S, Phase IV study of bevacizumab in combination with infusional fluorouracil, leucovorin and irinotecan (FOLFIRI) in first-line metastatic colorectal cancer. Oncology 2009;77:113-19
  • Takahashi Y, Tucker SL, Kitadai Y, Vessel counts and expression of vascular endothelial growth factor as prognostic factors in node-negative colon cancer. Arch Surg 1997;132:541-6
  • Takahashi Y, Kitadai Y, Bucana CD, Expression of vascular endothelial growth factor and its receptor, KDR, correlates with vascularity, metastasis, and proliferation of human colon cancer. Cancer Res 1995;55:3964-8
  • De Vita F, Orditura M, Lieto E, Elevated perioperative serum vascular endothelial growth factor levels in patients with colon carcinoma. Cancer 2004;2:270-8
  • Cascinu S, Staccioli MP, Gasparini G, Expression of vascular endothelial growth factor can predict event-free survival in stage II colon cancer. Clin Cancer Res 2000;6:2803-7
  • Kerbel RS. Tumor angiogenesis. N Engl J Med 2008;358:2039-49
  • Zhong H, Bowen JP. Antiangiogenesis drug design:multiple pathways targeting tumor vasculature. Curr Med Chem 2006;13:849-62
  • Bergers G, Benjamin LE. Tumorigenesis and the angiogenic switch. Nat Rev Cancer 2003;3:401-10
  • Salmon JS, Lockhart AC, Berlin J. Anti-angiogenic treatment of gastrointestinal malignancies. Cancer Invest 2005;23:712-26
  • Cross MJ, Dixelius J, Matsumotoo T, VEGF-receptor signal transduction. Trends Biochem Sci 2003;28:488-94
  • Joukov V, Pajusola K, Kaipainen A, A novel vascular endotheolial growth factor, VEGF-C, is a ligand for the Flt4 (VEGFR-3) and KDR (VEGFR-2) receptor tyrosine kinases. EMBO J 1996;15:290-8
  • Yamada Y, Nezu J, Shimane M, Molecular cloning of a novel vascular endothelial growth factor, VEGF-D. Genomics 1997;42:483-8
  • Park JE, Keller GA, Ferrara N. The vascular endothelial growth factor (VEGF) isoforms: differential deposition into the subepithelial extra-cellular matrix and bioactivity of extracellular matrix-bound VEGF. Mol Biol Cell 1993;4:1317-26
  • Terman BI, Dougher-Vermazen M, Carrion ME, Identification of the KDR tyrosine kinase as a receptor for vascular endothelial cell growth factor. Biochem Biophys Res Commun 1992;187:1579-86
  • Soker S, Takashima S, Miao HQ, Neuropilin-1 is expressed by endothelial and tumor cells as an isoform-specific receptor for vascular endothelial growth factor. Cell 1998;92:735-45
  • Paavonen K, Puolakkainen P, Jussila L, Vascular endothelial growth factor receptor-3 in lymphangiogenesis in wound healing. Am J Pathol 2000;156:1499-04
  • Olofsson B, Pajusola K, Kaipainen A, Vascular endothelial growth factor B, a novel frowth factor for endothelial cells. Proc Natl Acad Sci USA 1996;93:2576-81
  • Dvorak HF. Vascular permeability factor/vascular endothelial growth factor: a critical cytokine in tumor angiogenesis and a potential target for diagnosis and therapy. J Clin Oncol 2002;20:4368-80
  • Zeng H, Dvorak HF, Mukhopadhyay D. Vascular permeability factor (VPF)/vascular endothelial growth factor (VEGF) receptor-1 down-modulates VPF/VEGF receptor-2-mediated endothelial cell proliferation, but not migration, through phosphatidylinositol 3-kinase-dependent pathways. J Biol Chem 2001;276:26969-79
  • Millauer B, Wizigmann-Voos S, Schnurch H, High affinity VEGF binding and developmental expression suggest Flk-1 as a major regulator of vasculogenesis and angiogenesis. Cell 1993;72:835-46
  • Fong GH, Rossant J, Gertsenstein M, Role of the Flt-1 receptor tyrosine kinase in regulating the assembly of vascular endothelium. Nature 1995;376:66-70
  • Hiratsuka S, Maru Y, Okada A, Involvement of Flt-1 tyrosine kinase (vascular endothelial growth factor receptor-1) in pathological angiogenesis. Cancer Res 2001;61:1207-13
  • Fan F, Wey JS, McCarty MF, Expression and function of vascular endothelial growth factor receptor-1 on human colorectal cancer cells. Oncogene 2005;24:2647-53
  • Kaipainen A, Korhonen J, Mustonen T, Expression of the fms-like tyrosine kinase 4 gene becomes restricted to lymphatic endothelium during development. Proc Natl Acad Sci USA 1995;92:3566-70
  • Mandriota SJ, Jussila L, Jeltsch M, Vascular endothelial growth factor- C-mediated lymphangiogenesis promotes tumour metastasis. EMBO J 2001;20:672-82
  • Stacker SA, Caesar C, Baldwin ME, VEGF-D promotes the metastatic spread of tumor cells via the lymphatics. Nat Med 2001;7:186-91
  • Warren RS, Yuan H, Matli MR, Regulation by vascular endothelial growth factor of human colon cancer tumorigenesis in a mouse model of experimental liver metastasis. J Clin Invest 1995;95:1789-97
  • Ellis LM, Hicklin DJ. VEGF-targeted therapy: mechanism of anti-tumor activity. Nat Rev Cancer 2008;8:579-91
  • Cai ZW, Zhang Y, Borzilleri RM, Discovery of brivanib alaninate ((S)-((R)- 1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f] [1,2,4]triazin- 6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215). J Med Chem 2008;51:1976-80
  • Huynh H, Ngo VC, Fargnoli J, Brivanib alaninate, a dual inhibitor of vascular endothelial growth factor receptor and fibroblast growth factor receptor tyrosine kinases, induces growth inhibition in mouse models of human hepatocellular carcinoma. Clin Cancer Res 2008;14:6146-53
  • Dempke WC, Zippel R. Brivanib, a novel dual VEGF-R2/bFGF-R inhibitor. Anticancer Res 2010;30:4477-83
  • Lieu C, Heymach J, Overman M, Beyond VEGF: inhibition of the fibroblast growth factor pathway and antiangiogenesis. Clin Cancer Res 2011;17:6130-9
  • Ayers M. Comparison of a dual inhibitor of VEGF and FGF signaling, BMS- 582664, to the activity of bevacizumab, an inhibitor exclusively of VEGF signaling, in xenograft models of colon carcinoma [abstract 1618]. AACR Meeting Abstracts; 2007
  • Daniele G, Corral J, Molife LR, FGF receptor inhibitors: role in cancer therapy. Curr Oncol Rep 2012;14:111-19
  • Garrett CR, Siu LL, El-Khoueiry A, Phase I dose-escalation study to determine the safety, pharmacokinetics and pharmacodynamics of brivanib alaninate in combination with full-dose cetuximab in patients with advanced gastrointestinal malignancies who have failed prior therapy. Br J Cancer 2011;105:44-52
  • Siu LL, Shapiro JD, Jonker DJ, Final analysis of the phase III randomized trial of cetuximab (CET) plus either brivanib alaninate (BRIV) or placebo in patients (pts) with chemotherapy refractory, K-RAS wild-type (WT), metastatic colorectal carcinoma (mCRC): the NCIC Clinical Trials Group and AGITG CO.20 trial. J Clin Oncol 2012;30(Suppl):abstract 3504
  • Wedge SR, Kendrew J, Hennequin LF, AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res 2005;65:4389-400
  • Drevs J, Siegert P, Medinger M, Phase I clinical study ofA ZD2171, an oral vascular endothelial growth factor signaling inhibitor, in patients with advanced solid tumors. J Clin Oncol 2007;25:3045-54
  • Chen E, Jonker D, Gauthier I, Phase I study of cediranib in combinationwith oxaliplatin and infusional 5-fluorouracil in patients with advanced colorectal cancer. Clin Cancer Res 2009;15:1481-6
  • Schmoll HJ, Cunningham D, Sobrero A, Cediranib with mFOLFOX6 versus bevacizumab with mFOLFOX6 as first-line treatment for patients with advanced colorectal cancer: a double-blind, randomized phase III study (HORIZON III). J Clin Oncol 2012;29:3588-95
  • Robertson JD, Botwood NA, Rothenberg ML, Phase III trial of FOLFOX plus bevacizumab or cediranib (AZD2171) as first-line treatment of patients with metastatic colorectal cancer: HORIZON III. Clin Colorectal Cancer 2009;8:59-60
  • Hoff PM, Hochhaus A, Pestalozzi B, Cediranib plus FOLFOX/XELOX versus placebo plus FOLFOX/XELOX in patients with previously untreated metastatic colorectal cancer: a randomized, double –blind, phase III study (Horizon II). J Clin Oncol 2012;29:3596-603
  • O’Farrell AM, Abrams TJ, Yuen HA, SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood 2003;101:3597-605
  • 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;9:327-37
  • Castillo-Avila W, Piulats JM, Garcia Del Muro X, Sunitinib inhibits tumor growth and synergizes with cisplatin in orthotopic models of cisplatin-sensitive and cisplatin-resistant human testicular germ cell tumors. Clin Cancer Res 2009;15:3384-95
  • Cumashi A, Tinari N, Rossi C, Sunitinib malate (SU-11248) alone or in combination with low-dose docetaxel inhibits the growth of DU-145 prostate cancer xenografts. Cancer Lett 2008;270:229-33
  • Krystal GW, Honsawek S, Kiewlich D, Indolinone tyrosine kinase inhibitors block Kit activation and growth of small cell lung cancer cells. Cancer Res 2001;61:3660-8
  • Marzola P, Degrassi A, Calderan L, Early antiangiogenic activity of SU11248 evaluated in vivo by dynamic contrast-enhanced magnetic resonance imaging in an experimental model of colon carcinoma. Clin Cancer Res 2005;11:5827-32
  • Faivre S, Delbaldo C, Vera K, Safety, pharmacokinetic, and antitumor activity of SU11248, a novel oral multitarget tyrosine kinase inhibitor, in patients with cancer. J Clin Oncol 2006;24:25-35
  • Saltz LB, Rosen LS, Marshall JL, Phase II trial of sunitinib in patients with metastatic colorectal cancer after failure of standard therapy. J Clin Oncol 2007;25:4793-9
  • Leong S, Eckhardt SG, Chan E, A phase I study of sunitinib in combination with modified FOLFOX 6 (mFOLFOX6) chemotherapy [abstract 285]. ASCO Gastrointestinal Cancers Symposium; 2007
  • Starling N, Vázquez-Mazón F, Cunningham D, Phase I study of sunitinib in combination with FOLFIRI in patients with untreated metastatic colorectal cancer. Ann Oncol 2012;23:119-27
  • Mross K, Büchert M, Fasol U, A preliminary report of a Phase II study of folinic acid, 5-fluorouracil, irinotecan (FOLFIRI) plus sunitinib with toxicity, efficacy, pharmacokinetics, biomarker, imaging data in patients with colorectal cancer with liver metastases as 1st line treatment – a study of the CESAR central european society for anticancer drug research – EWIV**. Int J Clin Pharmacol Ther 2011;1:96-8
  • Wood JM, Bold G, Buchdunger E, PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res 2000;60:2178-89
  • Drevs J, Muller-Driver R, Wittig C, PTK787/ZK 222584, a specific vascular endothelial growth factor-receptor tyrosine kinase inhibitor, affects the anatomy of the tumor vascular bed and the functional vascular properties as detected by dynamic enhanced magnetic resonance imaging. Cancer Res 2002;62:4015-22
  • George D, Jonasch E, Hart L, A phase I, dose escalating and pharmacokinetic (PK) study of the VEGF-receptor inhibitor PTK787/ZK222584 (PTK/ZK) in patients with advanced renal cell or prostate carcinomas. Clin Cancer Res 2001;7:548a
  • Mross K, Drevs J, Muller M, Phase I clinical and pharmacokinetic study of PTK/ZK, a multiple VEGF receptor inhibitor, in patients with liver metastases from solid tumors. Eur J Cancer 2005;41:1291-9
  • Thomas AL, Trarbach T, Bartel C, A phase IB, open-label dose-escalating study of the oral angiogenesis inhibitor PTK787/ZK 222584 (PTK/ZK), in combination with FOLFOX4 chemotherapy in patients with advanced colorectal cancer. Ann Oncol 2007;18:782-8
  • Hecht JR, Trarbach T, Jaeger E, A randomized, double-blind, placebo-controlled, phase III study in patients (Pts) with metastatic a line chemotherapy with oxaliplatin/5-fluorouracil/leucovorin and PTK787/ZK222584 or placebo (CONFIRM-1). J Clin Oncol 2005;23(Suppl):abstract 3
  • Kohne C, Bajetta E, Lin E, Final results of CONFIRM 2: a multinational, randomized, double-blind, phase III study in 2nd line patients (pts) with metastatic colorectal cancer (mCRC) receiving FOLFOX4 and PTK787/ZK222584 (PTK/ZK) or placebo. J Clin Oncol 2007;25(Suppl):abstract 4033
  • Fong TA, Shawver LK, Sun L, SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res 1999;59:99-106
  • Stopeck A, Sheldon M, Vahedian M, Results of a phase I dose-escalating study of the antiangiogenic agent, SU5416, in patients with advanced malignancies. Clin Cancer Res 2002;8:2798-805
  • Rosen L, Mulay M, Mayers A, Phase I dose-escalating trial of SU5416, a novel angiogenesis inhibitor, in patients with advanced malignancies. Proc Am Soc Clin Oncol 1999;18:618a
  • Rosen P, Amado R, Hecht J, A phase I/II study of SU5416 in combination with 5-FU/leucovorin in patients with metastatic colorectal cancer. Proc Am Soc Clin Oncol 2000;18:5a
  • Van Cutsem E, Prenen H, Guillén-Ponce C, A phase I/II open-label, randomized study of BIBF 1120 plus mFOLFOX6 compared to bevacizumab plus mFOLFOX6 in patients with metastatic colorectal cancer [abstract 14LB]. ECCO-ESMO Congress; Stockolm; 2011
  • Spratlin JL, Mulder KE, Mackey JR. Ramucirumab (IMC-1121B): a novel attack on angiogenesis. Future Oncol 2010;6:1085-94
  • Prewett M, Huber J, Li Y, Antivascular endothelial growth factor receptor (fetal liver kinase 1) monoclonal antibody inhibits tumor angiogenesis and growth of several mouse and human tumors. Cancer Res 1999;59:5209-18
  • Spratlin JL, Cohen RB, Eadens M, Phase I pharmacologic and biologic study of ramucirumab (IMC-1121B), a fully human immunoglobulin G1 monoclonal antibody targeting the vascular endothelial growth factor receptor-2. J Clin Oncol 2010;28:780-7
  • Clinicaltrials.gov [Website]. Irinotecan hydrochloride and cetuximab with or without ramucirumab in treating patients with advanced colorectal cancer with progressive disease after treatment with bevacizumab-containing chemotherapy. Available from: http://clinicaltrials.gov/ct2/show/NCT01079780?term_NCT01079780&rank_1 [Accessed 13 December 2010]
  • Chu QS. Aflibercept (AVE0005): an alternative strategy for inhibiting tumor angiogenesis by vascular endothelial growth factors. Expert Opin Biol Ther 2009;9:263-71
  • Fukasawa M, Korc M. Vascular endothelial growth factor-trap suppresses tumorigenicity of multiple pancreatic cancer cell lines. Clin Cancer Res 2004;10:3327-32
  • Kadenhe-Chiweshe A, Papa J, McCrudden KW, Sustained VEGF blockade results in microenvironmental sequestration of VEGF by tumors and persistent VEGF receptor-2 activation. Mol Cancer Res 2008;6:1-9
  • Lockhart AC, Rothenberg ML, Dupont J, Phase I study of intravenous vascular endothelial growth factor trap, aflibercept, in patients with advanced solid tumors. J Clin Oncol 2010;28:207-14
  • Tang P, Cohen SJ, Bjarnason GA, Phase II trial of aflibercept (VEGF Trap) in previously treated patients with metastatic colorectal cancer (MCRC): a PMH phase II consortium trial. J Clin Oncol 2008;26(Suppl):abstract 4027
  • Van Cutsem E, Tabernero J, Lakomy R, Addition of Aflibercept to Fluorouracil, Leucovorin, and Irinotecan Improves Survival in a Phase III Randomized Trial in Patients With Metastatic Colorectal Cancer. J Clin Oncol 2012;30(28):3499-06
  • Allegra CJ, Lakomy R, Tabernero J, Effects of prior bevacizumab (B) use on outcomes from the VELOUR study: a phase III study of aflibercept (Afl) and FOLFIRI in patients (pts) with metastatic colorectal cancer (mCRC) after failure of an oxaliplatin regimen. J Clin Oncol 2012;30(Suppl):abstract 3505
  • Food and Drugs Administration, Drugs approvals and database. Available from: www.fda.org
  • Kies MS, Blumenschein GR Jr, Christensen O, Phase I study of regorafenib (BAY 73-4506), an inhibitor of oncogenic and angiogenic kinases, administered continuously in patients (pts) with advanced refractory non-small cell lung cancer (NSCLC) [abstract]. J Clin Oncol 2010;28(15 Suppl):abstract 7585
  • Strumberg D, Scheulen ME, Frost A, Phase I study of BAY 73-4506, an inhibitor of oncogenic and angiogenic kinases, in patients with advanced refractory colorectal carcinoma (CRC). J Clin Oncol 2009;27(15 Suppl):abstract 3560
  • Grothey A, Sobrero AF, Siena S, Results of a phase III randomized, double-blind, placebo-controlled, multicenter trial (CORRECT) of regorafenib plus best supportive care (BSC) versus placebo plus BSC in patients (pts) with metastatic colorectal cancer (mCRC) who have progressed after standard therapies. J Clin Oncol 2012;30(4 Suppl):abstract LBA385
  • Martinelli E, De Palma R, Orditura M, Anti-EGFR monoclonal antibodies in cancer therapy. J Clin Immunol 2009;158(1):1-9
  • Troiani T, Martinelli E, Orditura M, Beyond bevacizumab: new anti-VEGF strategies in colorectal cancer. Expert Opin Investig Drugs 2012;21(7):949-59

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.