메뉴 건너뛰기




Volumn 15, Issue 12, 2014, Pages 1635-1645

Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy

Author keywords

Angiogenesis; Anti tumor activity; Cancer treatment; Fruquintinib; Tumor xenograft models; Tyrosine kinase inhibitor; VEGFR 1 2 3

Indexed keywords

ANTINEOPLASTIC AGENT; DOCETAXEL; FRUQUINTINIB; OXALIPLATIN; PROTEIN TYROSINE KINASE INHIBITOR; UNCLASSIFIED DRUG; VASCULOTROPIN; VASCULOTROPIN RECEPTOR 1; VASCULOTROPIN RECEPTOR 2; VASCULOTROPIN RECEPTOR 3; ANGIOGENESIS INHIBITOR; BENZOFURAN DERIVATIVE; HMPL-013; PROTEIN KINASE INHIBITOR; QUINAZOLINE DERIVATIVE;

EID: 84920116720     PISSN: 15384047     EISSN: 15558576     Source Type: Journal    
DOI: 10.4161/15384047.2014.964087     Document Type: Article
Times cited : (106)

References (38)
  • 1
    • 0034693879 scopus 로고    scopus 로고
    • Vascular endothelial growth factor receptors in the regulation of angiogenesis and lymphangiogenesis
    • PMID:11114740
    • Karkkainen MJ, Petrova TV. Vascular endothelial growth factor receptors in the regulation of angiogenesis and lymphangiogenesis. Oncogene 2000; 19:5598-605; PMID:11114740; http://dx.doi.org/10.1038/sj. onc.1203855
    • (2000) Oncogene , vol.19 , pp. 5598-5605
    • Karkkainen, M.J.1    Petrova, T.V.2
  • 2
    • 0037967272 scopus 로고    scopus 로고
    • Tumorigenesis and the angiogenic switch
    • PMID:12778130
    • Bergers G, Benjamin LE. Tumorigenesis and the angiogenic switch. Nat Rev Cancer 2003; 3: 401-10; PMID:12778130; http://dx.doi.org/10.1038/ nrc1093
    • (2003) Nat Rev Cancer , vol.3 , pp. 401-410
    • Bergers, G.1    Benjamin, L.E.2
  • 4
    • 43249095919 scopus 로고    scopus 로고
    • Tumor angiogenesis
    • PMID:18463380
    • Kerbel RS. Tumor angiogenesis. N Engl J Med 2008; 358:2039-49; PMID:18463380; http://dx.doi.org/ 10.1056/NEJMra0706596
    • (2008) N Engl J Med , vol.358 , pp. 2039-2049
    • Kerbel, R.S.1
  • 5
    • 0036842215 scopus 로고    scopus 로고
    • Vascular permeability factor/vascular endothelial growth factor: A critical cytokine in tumor angiogenesis and a potential target for diagnosis and therapy
    • PMID:12409337
    • 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; PMID:12409337; http:// dx.doi.org/10.1200/JCO.2002.10.088
    • (2002) J Clin Oncol , vol.20 , pp. 4368-4380
    • Dvorak, H.F.1
  • 6
    • 0028822834 scopus 로고
    • Mutant ras oncogenes upregulate VEGF/VPF expression: Implications for induction and inhibition of tumor angiogenesis
    • PMID:7553632
    • Rak J, Mitsuhashi Y, Bayko L, Filmus J, Shirasawa S, Sasazuki T, Kerbel RS. Mutant ras oncogenes upregulate VEGF/VPF expression: Implications for induction and inhibition of tumor angiogenesis. Cancer Res 1995; 55:4575-80; PMID:7553632
    • (1995) Cancer Res , vol.55 , pp. 4575-4580
    • Rak, J.1    Mitsuhashi, Y.2    Bayko, L.3    Filmus, J.4    Shirasawa, S.5    Sasazuki, T.6    Kerbel, R.S.7
  • 8
    • 84899409082 scopus 로고    scopus 로고
    • Hypoxia-driven osteopontin contributes to breast tumor growth through modulation of HIF1a-mediated VEGF-dependent angiogenesis
    • PMID: 23728336
    • Raja R, Kale S, Thorat D, Soundararajan G, Lohite K, Mane A, Karnik S, Kundu GC. Hypoxia-driven osteopontin contributes to breast tumor growth through modulation of HIF1a-mediated VEGF-dependent angiogenesis. Oncogene 2014; 33:2053-64; PMID: 23728336; http://dx.doi.org/10.1038/onc.2013.171
    • (2014) Oncogene , vol.33 , pp. 2053-2064
    • Raja, R.1    Kale, S.2    Thorat, D.3    Soundararajan, G.4    Lohite, K.5    Mane, A.6    Karnik, S.7    Kundu, G.C.8
  • 10
    • 84878477682 scopus 로고    scopus 로고
    • Overexpression of both VEGF-A and VEGF-C in gastric cancer correlates with prognosis, and silencing of both is effective to inhibit cancer growth
    • PMID:23573305
    • Wang X, Chen X, Fang J, Yang C. Overexpression of both VEGF-A and VEGF-C in gastric cancer correlates with prognosis, and silencing of both is effective to inhibit cancer growth. Int J Clin Exp Pathol 2013; 6:586-97; PMID:23573305
    • (2013) Int J Clin Exp Pathol , vol.6 , pp. 586-597
    • Wang, X.1    Chen, X.2    Fang, J.3    Yang, C.4
  • 11
    • 84876943656 scopus 로고    scopus 로고
    • Clinicopathological correlation and prognostic significance of VEGF-A, VEGF-C, KDR and VEGFR-3 expression in colorectal cancer
    • PMID:23603341
    • Martins SF, Garcia EA, Luz MA, Pardal F, Rodrigues M, Filho AL. Clinicopathological correlation and prognostic significance of VEGF-A, VEGF-C, KDR and VEGFR-3 expression in colorectal cancer. Cancer Genomics Proteomics 2013; 10:55-67; PMID:23603341
    • (2013) Cancer Genomics Proteomics , vol.10 , pp. 55-67
    • Martins, S.F.1    Garcia, E.A.2    Luz, M.A.3    Pardal, F.4    Rodrigues, M.5    Filho, A.L.6
  • 12
    • 84876973578 scopus 로고    scopus 로고
    • Vascular endothelial growth factor (VEGF) expression in locally advanced prostate cancer: Secondary analysis of radiation therapy oncology group (RTOG) 8610
    • PMID:23618468
    • Pan L, Baek S, Edmonds PR, Roach M, Wolkov H, Shah S, Pollack A, Hammond ME, Dicker AP. Vascular endothelial growth factor (VEGF) expression in locally advanced prostate cancer: secondary analysis of radiation therapy oncology group (RTOG) 8610. Radiat Oncol 2013; 8:100; PMID:23618468; http:// dx.doi.org/10.1186/1748-717X-8-100
    • (2013) Radiat Oncol , vol.8
    • Pan, L.1    Baek, S.2    Edmonds, P.R.3    Roach, M.4    Wolkov, H.5    Shah, S.6    Pollack, A.7    Hammond, M.E.8    Dicker, A.P.9
  • 13
    • 66349096698 scopus 로고    scopus 로고
    • VEGF-A and i-NOS expression are prognostic factors in serous epithelial ovarian carcinomas after complete surgical resection
    • PMID:19126566
    • Engels K, du Bois A, Harter P, Fisseler-Eckhoff A, Kommoss F, Stauber R, Kaufmann M, Nekljudova V, Loibl S. VEGF-A and i-NOS expression are prognostic factors in serous epithelial ovarian carcinomas after complete surgical resection. J Clin Pathol 2009; 62:448-54; PMID:19126566; http://dx.doi.org/ 10.1136/jcp.2008.063859
    • (2009) J Clin Pathol , vol.62 , pp. 448-454
    • Engels, K.1    Du Bois, A.2    Harter, P.3    Fisseler-Eckhoff, A.4    Kommoss, F.5    Stauber, R.6    Kaufmann, M.7    Nekljudova, V.8    Loibl, S.9
  • 15
  • 16
    • 84868618639 scopus 로고    scopus 로고
    • Vascular endothelial growth factor (VEGF) and its receptor (VEGFR) signaling in angiogenesis: A crucial target for anti- and pro-angiogenic therapies
    • PMID:22866201
    • Shibuya M. Vascular endothelial growth factor (VEGF) and its receptor (VEGFR) signaling in angiogenesis: a crucial target for anti- and pro-angiogenic therapies. Genes Cancer 2011; 2:1097-105; PMID:22866201; http://dx.doi.org/10.1177/1947601911423031
    • (2011) Genes Cancer , vol.2 , pp. 1097-1105
    • Shibuya, M.1
  • 17
    • 3042634486 scopus 로고    scopus 로고
    • Development of new drugs in angiogenesis
    • PMID:15216914
    • Ziche M, Donnini S, Morbidelli L. Development of new drugs in angiogenesis. Curr Drug Targets 2004; 5:485-93; PMID:15216914; http://dx.doi.org/ 10.2174/1389450043345371
    • (2004) Curr Drug Targets , vol.5 , pp. 485-493
    • Ziche, M.1    Donnini, S.2    Morbidelli, L.3
  • 18
    • 84900802283 scopus 로고    scopus 로고
    • Safety and efficacy of first-line bevacizumab combination therapy in Chinese population with advanced non-squamous NSCLC: Data of subgroup analyses from MO19390 (SAiL) study
    • PMID:24002945
    • Zhou CC, Bai CX, Guan ZZ, Jiang GL, Shi YK, Wang MZ, Wu YL, Zhang YP, Zhu YZ. Safety and efficacy of first-line bevacizumab combination therapy in Chinese population with advanced non-squamous NSCLC: data of subgroup analyses from MO19390 (SAiL) study. Clin Transl Oncol 2014; 16:463-8; PMID:24002945; http://dx.doi.org/10.1007/s12094-013-1102-5
    • (2014) Clin Transl Oncol , vol.16 , pp. 463-468
    • Zhou, C.C.1    Bai, C.X.2    Guan, Z.Z.3    Jiang, G.L.4    Shi, Y.K.5    Wang, M.Z.6    Wu, Y.L.7    Zhang, Y.P.8    Zhu, Y.Z.9
  • 19
    • 84887018257 scopus 로고    scopus 로고
    • A phase II study of erlotinib in combination with bevacizumab versus chemotherapy plus bevacizumab in the first-line treatment of advanced non-squamous non-small cell lung cancer
    • PMID:23992877
    • Ciuleanu T, Tsai CM, Tsao CJ, Milanowski J, Amoroso D, Heo DS, Groen HJ, Szczesna A, Chung CY, Chao TY, et al. A phase II study of erlotinib in combination with bevacizumab versus chemotherapy plus bevacizumab in the first-line treatment of advanced non-squamous non-small cell lung cancer. Lung Cancer 2013; 82:276-81; PMID:23992877; http://dx.doi.org/ 10.1016/j.lungcan.2013.08.002
    • (2013) Lung Cancer , vol.82 , pp. 276-281
    • Ciuleanu, T.1    Tsai, C.M.2    Tsao, C.J.3    Milanowski, J.4    Amoroso, D.5    Heo, D.S.6    Groen, H.J.7    Szczesna, A.8    Chung, C.Y.9    Chao, T.Y.10
  • 20
    • 77957160694 scopus 로고    scopus 로고
    • A phase II study of bevacizumab, oxaliplatin, and docetaxel in locally advanced and metastatic gastric and gastroesophageal junction cancers
    • PMID:20332133
    • El-Rayes BF, Zalupski M, Bekai-Saab T, Heilbrun LK, Hammad N, Patel B, Urba S, Shields AF, Vaishampayan U, Dawson S, et al. A phase II study of bevacizumab, oxaliplatin, and docetaxel in locally advanced and metastatic gastric and gastroesophageal junction cancers. Ann Oncol 2010; 21:1999-2004; PMID:20332133; http://dx.doi. org/10.1093/annonc/mdq065
    • (2010) Ann Oncol , vol.21 , pp. 1999-2004
    • El-Rayes, B.F.1    Zalupski, M.2    Bekai-Saab, T.3    Heilbrun, L.K.4    Hammad, N.5    Patel, B.6    Urba, S.7    Shields, A.F.8    Vaishampayan, U.9    Dawson, S.10
  • 22
    • 34547459725 scopus 로고    scopus 로고
    • Sorafenib and sunitinib: Novel targeted therapies for renal cell cancer
    • PMID:17655513
    • Grandinetti CA, Goldspiel BR. Sorafenib and sunitinib: novel targeted therapies for renal cell cancer. Pharmacotherapy 2007; 27:1125-44; PMID:17655513; http://dx.doi.org/10.1592/phco.27.8.1125
    • (2007) Pharmacotherapy , vol.27 , pp. 1125-1144
    • Grandinetti, C.A.1    Goldspiel, B.R.2
  • 25
    • 84865253075 scopus 로고    scopus 로고
    • Concise drug review: Pazopanib and axitinib
    • PMID:22733795
    • van Geel RM, Beijnen JH, Schellens JH. Concise drug review: pazopanib and axitinib. Oncologist 2012; 17:1081-9; PMID:22733795; http://dx.doi.org/ 10.1634/theoncologist.2012-0055
    • (2012) Oncologist , vol.17 , pp. 1081-1089
    • Van Geel, R.M.1    Beijnen, J.H.2    Schellens, J.H.3
  • 26
    • 84903815337 scopus 로고    scopus 로고
    • Preclinical pharmacokinetics and disposition of a novel selective VEGFR inhibitor fruquintinib (HMPL-013) and the prediction of its human pharmacokinetics
    • PMID:24817647
    • Gu Y, Wang J, Li K, Zhang L, Ren HC, Guo LX, Sai Y, Zhang WH, Su WG. Preclinical pharmacokinetics and disposition of a novel selective VEGFR inhibitor fruquintinib (HMPL-013) and the prediction of its human pharmacokinetics. Cancer Chemoth Pharmacol 2014; 74:95-115; PMID:24817647; http://dx.doi.org/ 10.1007/s00280-014-2471-3
    • (2014) Cancer Chemoth Pharmacol , vol.74 , pp. 95-115
    • Gu, Y.1    Wang, J.2    Li, K.3    Zhang, L.4    Ren, H.C.5    Guo, L.X.6    Sai, Y.7    Zhang, W.H.8    Su, W.G.9
  • 27
    • 84867346245 scopus 로고    scopus 로고
    • Development and strategies of KDR/KDR inhibitors
    • PMID:23043480
    • Huang L, Huang Z, Bai Z, Xie R, Sun L, Lin K. Development and strategies of KDR/KDR inhibitors. Future Med Chem 2012; 4:1839-52; PMID:23043480; http://dx.doi.org/10.4155/fmc.12.121
    • (2012) Future Med Chem , vol.4 , pp. 1839-1852
    • Huang, L.1    Huang, Z.2    Bai, Z.3    Xie, R.4    Sun, L.5    Lin, K.6
  • 28
    • 83255162010 scopus 로고    scopus 로고
    • Vascular endothelial growth factor (VEGF), VEGF receptors and their inhibitors for antiangiogenic tumor therapy
    • PMID:22130231
    • Takahashi S. Vascular endothelial growth factor (VEGF), VEGF receptors and their inhibitors for antiangiogenic tumor therapy. Biol Pharm Bull 2011; 34:1785-8; PMID:22130231; http://dx.doi.org/ 10.1248/bpb.34.1785
    • (2011) Biol Pharm Bull , vol.34 , pp. 1785-1788
    • Takahashi, S.1
  • 29
    • 79957902010 scopus 로고    scopus 로고
    • Signal transduction by vascular endothelial growth factor receptors
    • PMID: 21711246
    • Koch S, Tugues S, Li X, Gualandi L, laesson-Welsh L. Signal transduction by vascular endothelial growth factor receptors. Biochem J 2011; 437:169-83; PMID: 21711246; http://dx.doi.org/10.1042/BJ20110301
    • (2011) Biochem J , vol.437 , pp. 169-183
    • Koch, S.1    Tugues, S.2    Li, X.3    Gualandi, L.4    Laesson-Welsh, L.5
  • 31
    • 0034693879 scopus 로고    scopus 로고
    • Vascular endothelial growth factor receptors in the regulation of angiogenesis and lymphangiogenesis
    • PMID:11114740
    • Karkkainen MJ, Petrova TV. Vascular endothelial growth factor receptors in the regulation of angiogenesis and lymphangiogenesis. Oncogene 2000; 19:5598-605; PMID:11114740; http://dx.doi.org/10.1038/sj. onc.1203855
    • (2000) Oncogene , vol.19 , pp. 5598-5605
    • Karkkainen, M.J.1    Petrova, T.V.2
  • 32
    • 84877909957 scopus 로고    scopus 로고
    • VEGF-c expression in an in vivo model of orthotopic endometrial cancer and retroperitoneal lymph node metastasis
    • PMID:23693075
    • Huang YW, Xu LQ, Luo RZ,Huang X, Hou T, Zhang YN. VEGF-c expression in an in vivo model of orthotopic endometrial cancer and retroperitoneal lymph node metastasis. Reprod Biol Endocrinol 2013; 11:49; PMID:23693075; http://dx.doi.org/10.1186/1477-7827-11-49
    • (2013) Reprod Biol Endocrinol , vol.11
    • Huang, Y.W.1    Xu, L.Q.2    Luo, R.Z.3    Huang, X.4    Hou, T.5    Zhang, Y.N.6
  • 33
    • 84877704806 scopus 로고    scopus 로고
    • The association of VEGF-C expression with tumor lymphatic vessel density and lymph node metastasis in patients with gastric cancer and gastrointestinal stromal tumor
    • PMID:23574654
    • Kigure W, Fujii T, Sutoh T, Morita H, Katoh T, Yajima RN, Yamaguchi S, Tsutsumi S, Asao T, Kuwano H. The association of VEGF-C expression with tumor lymphatic vessel density and lymph node metastasis in patients with gastric cancer and gastrointestinal stromal tumor. Hepatogastroenterology 2013; 60:277-80; PMID:23574654
    • (2013) Hepatogastroenterology , vol.60 , pp. 277-280
    • Kigure, W.1    Fujii, T.2    Sutoh, T.3    Morita, H.4    Katoh, T.5    Yajima, R.N.6    Yamaguchi, S.7    Tsutsumi, S.8    Asao, T.9    Kuwano, H.10
  • 34
    • 84885361721 scopus 로고    scopus 로고
    • MT1-MMP in breast cancer: Induction of VEGF-C correlates with metastasis and poor prognosis
    • PMID:24119788
    • Yao G, He P, Chen L, Hu X, Gu F, Ye C. MT1-MMP in breast cancer: induction of VEGF-C correlates with metastasis and poor prognosis. Cancer Cell Int 2013; 13:98; PMID:24119788; http://dx.doi.org/10.1186/ 1475-2867-13-98
    • (2013) Cancer Cell Int , vol.13
    • Yao, G.1    He, P.2    Chen, L.3    Hu, X.4    Gu, F.5    Ye, C.6
  • 35
    • 27544483545 scopus 로고    scopus 로고
    • Tumor-secreted vascular endothelial growth factor-C is necessary for prostate cancer lymphangiogenesis, but lymphangiogenesis is unnecessary for lymph node metastasis
    • PMID:16267000
    • Wong SY, Haack H, Crowley D, Barry M, Bronson RT, Hynes RO. Tumor-secreted vascular endothelial growth factor-C is necessary for prostate cancer lymphangiogenesis, but lymphangiogenesis is unnecessary for lymph node metastasis. Cancer Res 2005; 65:9789-98; PMID:16267000; http://dx.doi.org/10.1158/ 0008-5472.CAN-05-0901
    • (2005) Cancer Res , vol.65 , pp. 9789-9798
    • Wong, S.Y.1    Haack, H.2    Crowley, D.3    Barry, M.4    Bronson, R.T.5    Hynes, R.O.6
  • 36
    • 84876943656 scopus 로고    scopus 로고
    • Clinicopathological correlation and prognostic significance of VEGF-A, VEGF-C, VEGFR-2 and VEGFR-3 expression in colorectal cancer
    • PMID:23603341
    • Martins SF, Garcia EA, Luz MA, Pardal F, Rodrigues M, Filho AL. Clinicopathological correlation and prognostic significance of VEGF-A, VEGF-C, VEGFR-2 and VEGFR-3 expression in colorectal cancer. Cancer Genomics Proteomics 2013; 10:55-67; PMID:23603341
    • (2013) Cancer Genomics Proteomics , vol.10 , pp. 55-67
    • Martins, S.F.1    Garcia, E.A.2    Luz, M.A.3    Pardal, F.4    Rodrigues, M.5    Filho, A.L.6
  • 37
    • 79955029845 scopus 로고    scopus 로고
    • Lymphangiogenesis and cancer metastasis
    • Al-Rawi MA, Jiang WG. Lymphangiogenesis and cancer metastasis. Front Biosci 2011; 16:23-39; http://dx. doi.org/10.2741/3715
    • (2011) Front Biosci , vol.16 , pp. 23-39
    • Al-Rawi, M.A.1    Jiang, W.G.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.