Targeting EGFR and IGF 1R: A promising combination therapy for metastatic cancer

Frontiers in Bioscience - Scholar

Volumn 5 S, Issue 1, 2013, Pages 231-246

  Singh, Inderpal ^a   Amin, Hina ^a   Rah, Bilal ^a   Goswami, Anindya ^a  

^a CSIR INDIAN INSTITUTE OF INTEGRATIVE MEDICINE   (India)

Author keywords

Combination therapy; EGFR; IGF 1R; Metastasis; Review

Indexed keywords

1 [4 [(5 CYCLOPROPYL 1H PYRAZOL 3 YL)AMINO]PYRROLO[2,1 F][1,2,4]TRIAZIN 2 YL] N (6 FLUORO 3 PYRIDINYL) 2 METHYL 2 PYRROLIDINECARBOXAMIDE; 4 AMINO 5 (3 BENZYLOXYPHENYL) 7 [3 (1 PYRROLIDINYLMETHYL)CYCLOBUTYL] 7H PYRROLO[2,3 D]PYRIMIDINE; 6 (4 HYDROXYPHENYL) 4 (ALPHA METHYLBENZYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDINE; A 928605; ANTINEOPLASTIC AGENT; AVE 1642; CETUXIMAB; CIXUTUMUMAB; CONATUMUMAB; DALOTUZUMAB; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; EVEROLIMUS; FIGITUMUMAB; GANITUMAB; GEFITINIB; GEMCITABINE; IMATINIB; IRINOTECAN; LAPATINIB; LINSITINIB; MDI 573; NERATINIB; NVP AEW 541; PANITUMUMAB; R 1507; ROBATUMUMAB; TRASTUZUMAB; UNCLASSIFIED DRUG; UNINDEXED DRUG; XL 228; EPIDERMAL GROWTH FACTOR RECEPTOR; PROTEIN KINASE INHIBITOR; SOMATOMEDIN C RECEPTOR;

ADRENAL CORTEX CARCINOMA; ADVANCED CANCER; ANTINEOPLASTIC ACTIVITY; ARTICLE; ASTHENIA; BILIARY TRACT CANCER; BONE METASTASIS; BREAST CANCER; BREAST METASTASIS; CANCER COMBINATION CHEMOTHERAPY; CANCER RESISTANCE; CANCER RISK; CANCER SURVIVAL; CHRONIC MYELOID LEUKEMIA; COLON CANCER; COLORECTAL CANCER; CONSTIPATION; DIARRHEA; DRUG INDUCED DISEASE; DRUG POTENTIATION; DRUG TARGETING; DRUG TOLERANCE; EWING SARCOMA; FIBROSARCOMA; GLIOBLASTOMA; GLIOSARCOMA; HEAD AND NECK CANCER; HEAD AND NECK CARCINOMA; HEAD AND NECK SQUAMOUS CELL CARCINOMA; HUMAN; HYPERGLYCEMIA; LIVER CELL CARCINOMA; LIVER METASTASIS; LUNG METASTASIS; LUNG NON SMALL CELL CANCER; LYMPH NODE METASTASIS; METASTASIS; METASTASIS INHIBITION; METASTATIC COLORECTAL CANCER; MONOTHERAPY; MULTIPLE MYELOMA; MYELOID LEUKEMIA; MYELOMA; NONHODGKIN LYMPHOMA; NONHUMAN; OSTEOSARCOMA; OVARY CANCER; OVERALL SURVIVAL; PANCREAS CARCINOMA; PANCREAS TUMOR; PERITONEUM TUMOR; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PROGRESSION FREE SURVIVAL; PROSTATE CANCER; RASH; RECTUM CANCER; SARCOMA; SOLID TUMOR; UTERINE CERVIX CANCER; UTERINE TUBE DISEASE; ANIMAL; DRUG ANTAGONISM; DRUG EFFECT; METABOLISM; MOLECULARLY TARGETED THERAPY; NEOPLASM; PATHOLOGY; REVIEW; SIGNAL TRANSDUCTION;

ANIMALS; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; HUMANS; MOLECULAR TARGETED THERAPY; NEOPLASM METASTASIS; NEOPLASMS; PROTEIN KINASE INHIBITORS; RECEPTOR, EPIDERMAL GROWTH FACTOR; RECEPTOR, IGF TYPE 1; SIGNAL TRANSDUCTION;

EID: 84883670021     PISSN: 19450516     EISSN: 19450524     Source Type: Journal    
DOI: 10.2741/s369     Document Type: Article

References (131)

1. F. Hofmann and C. Garcia-Echeverria: Blocking the insulin-like growth factor-1 receptor as a strategy for targeting cancer. Drug Discov Today 10, 1041-1047 (2005)
2. R. Baserga: The insulin-like growth factor-1 receptor as a target for cancer therapy. Expert Opin Ther Targets 9, 753-768 (2005)
3. S. Yakar, D. Leroith and P. Brodt: The role of the growth hormone/insulin-like growth factor axis in tumor growth and progression: lessons from animal models. Cytokine Growth Factor Rev 16, 407-420 (2005)
4. J. Capdevila, E. Elez, T. Macarulla , F.J. Ramos , M. Ruiz-Echarri and J. Tabernero: Anti-epidermal growth factor receptor monoclonal antibodies in cancer treatment. Cancer Treatment Rev 35, 354-363 (2009)
5. J.D Wu, A.Odman, L.M Higgins, K.Haugk, R.Vessella, D.L Ludwig and S.R Plymate: In vivo effects of the human type I insulin-like growth factor receptor antibody A-12 on androgen dependent and androgen independent xenograft human prostate tumors. Clin Cancer Res 11, 3065-3074 (2005)
6. T.J. Lynch, D.W. Bell, R. Sordella, S. Gurubhagavatula, R.A. Okimoto, B.W. Brannigan, P.L. Harris, S.M. Haserlat, J.G.Supko , F.G. Haluska , D.N. Louis , D.C. Christiani , J. Settleman and D.A. Haber: Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 350, 2129-2139 (2004)
7. G.R. Oxnard, M.E. Arcila, C.S. Sima, G.J. Riely, J. Chmielecki, M.G. Kris, W. Pao, M. Ladanyi and V.A. Miller: Acquired resistance to EGFR tyrosine kinase inhibitors in EGFR-mutant lung cancer: distinct natural history of patients harboring the T790M mutation. Clin Cancer Res 17, 1616-22 (2011)
8. E. Buck, P.C. Gokhale, S. Koujak, E. Brown, A. Eyzaguirre, N. Tao, M. Rosenfeld-Franklin, L. Lerner, M.I. Chiu, R. Wild, D. Epstein, J.A. Pachter and M.R. Miglarese: Compensatory Insulin Receptor (IR) Activation on Inhibition of Insulin-Like Growth Factor-1 Receptor (IGF 1R): Rationale for Co-Targeting IGF 1R and IR in Cancer. Mol Cancer Ther 9, 2652-2664 (2010)
9. A. Camirand, M. Zakikhani, F. Young and M. Pollak: Inhibition of insulin-like growth factor-1 receptor signaling enhances growth-inhibitory and pro-Apoptotic effects of gefitinib (iressa) in human breast cancer cells. Breast Cancer Res 7R, 570-R579 (2005)
10. D. Lu, H. Zhang, H. Koo, J. Tonra, P. Balderes, M. Prewett, E. Corcoran, V. Mangalampalli, R. Bassi, D. Anselma, D. Patel, X. Kang, D. L. Ludwig, D. J. Hicklin, P. Bohlen, L. Witte and Z. Zhu: A fully human recombinant IgG-like bispecific antibody to both the epidermal growth factor receptor and the insulin like growth factor receptor for enhanced antitumor activity. J Biol Chem 280, 19665-19672 (2005)
11. J.P. Steinbach, C. Eisenmann , A. Klumpp, and M. Weller: Co-inhibition of epidermal growth factor receptor and type-1 insulin-like growth factor receptor synergistically sensitizes human malignant glioma cells to CD95L-induced apoptosis. Biochem Biophy Res Comm 32, 1524-530 (2004)
12. L. Goetsch, A. Gonzalez, O. Leger, A. Beck, P.J. Pauwels, J.F. Haeuw and N. Corvaia: Recombinant humanized anti-insulin-like growth factor receptor type-1 antibody (h7C10) enhances the antitumor activity of Vinorelbine and anti-epidermal growth factor receptor therapy against human cancer xenografts. International J Cancer 11, 3316-328 (2005)
13. D. Coppola, A. Ferber, M. Miura, C. Sell, C.D'Ambrosio, R. Rubin, and R. Baserga: A functional insulin-like growth factor 1 receptor is required for the mitogenic and transforming activities of epidermal growth factor receptor. Mol Cell Biol 14, 4588-4595 (1994)
14. J. Mendelsohn: Anti-epidermal growth factor receptor monoclonal antibodies as potential anti-cancer agents. J Steroid Biochem Mol Biol 37, 889-892 (1990)
15. B.D. Manning and L.L. Cantley: AKT/PKB Signaling: Navigating downstream .Cell 129(7), 1261-74 (2007)
16. S.V. Sharma, D.W. Bell, J. Settleman and D.A. Haber: Epidermal growth factor receptor mutations in lung cancer. Nature Rev Cancer 7, 169-181 (2007)
17. Z. Lu, G. Jiang, P. B. Jensen and T. Hunter: Epidermal growth factor-induced tumor cell invasion and metastasis initiated by dephosphorylation and downregulation of focal adhesion kinase. Mol Cell Biol 21, 4016-4031 (2001)
18. A. Pryczynicz, K. Guzinska-Ustymowicz, A. Kemona and Jolanta Czyzewska: Expression of egf and egfr strongly correlates with metastasis of pancreatic ductal carcinoma. Anticancer Res 28, 1399-1404 (2008)
19. T. Shibata , T. Kawano , H. Nagayasu , K. Okumura , M. Arisue , J. Hamada , N. Takeichi and M . Hosokawa: Enhancing effects of epidermal growth factor on human squamous cell carcinoma motility and matrix degradation but not growth. Tumor Biol 17, 168-75 (1996)
20. J.T.Price, H.M. Wilson and N.E. Haites: Epidermal growth factor (EGF) increases the in vitro invasion, motility and adhesion interactions of the primary renal carcinoma cell line, A704. Eur J Cancer 32A, 1977-82 (1996)
21. X. Lu and Y. Kang: Epidermal growth factor signalling and bone metastasis. Br J Cancer 10, 2457-461 (2010)
22. E.L. Rosenthal , T.M. Johnson , E.D Allen , I.J. Apel , A. Punturieri and S.J. Weiss: Role of the Plasminogen Activator and Matrix Metalloproteinase Systems in Epidermal Growth Factorand Scatter Factor-stimulated Invasion of Carcinoma Cells. Cancer Res 58, 5221-5230 (1998)
23. A. Rossi, E. Bria, P. Maione, G. Palazzolo, M. Falanga and C. Gridelli: The role of cetuximab and other epidermal growth factor receptor monoclonal antibodies in the treatment of advanced non-small cell lung cancer. Rev Recent Clin Trials 3, 217-27 (2008)
24. D. Ma and J.Y. Niederkorn: Role of Epidermal Growth Factor Receptor in the Metastasis of Intraocular Melanomas. IOVS 39, 1067-1075 (1998)
25. J.T. Price, T. Tiganis, A. Agarwal, D. Djakiew and E.W. Thompson: Epidermal GrowthFactor Promotes MDA-MB-231 Breast Cancer Cell Migration through a Phosphatidylinositol 3-Kinase and Phospholipase Cdependent Mechanism. Cancer Res 59, 5475-5478 (1999)
26. J. Soh, N. Okumura, W.W. Lockwood, H. Yamamoto, H. Shigematsu, W. Zhang, R.Chari, D.S. Shames, X. Tang, C. MacAulay, M. Varella-Garcia, T. Vooder, I.I. Wistuba, S. Lam, R. Brekken, S. Toyooka, J. D. Minna, W.L. Lam and A.F. Gazdar: Oncogene mutations, copy number gains and mutant allele specific imbalance (MASI) frequently occur together in tumor cells. PLoS One 4e, 7464 (2009)
27. D. Cunningham , Y. Humblet , S. Siena , D. Khayat , H. Bleiberg , A .Santoro , D. Bets , M. Mueser , A. Harstrick , C. Verslype , I. Chau and E. Van Cutsem: Cetuximab monotherapy and cetuximab plus irinotecan in irinotecanrefractory metastatic colorectal cancer. N Engl J Med 351, 337-45 (2004)
28. P. Savagner: Leaving the neighborhood: molecular mechanisms involved during epithelial-mesenchymal transition. Bioessays 23(10), 912-23 (2001)
29. M.P. Cunningham, H. Thomas, C. Marks, M. Green, Z. Fan and H. Modjtahedi: Co-Targeting the EGFR and IGF-IR with anti-EGFR monoclonal antibody ICR62 and the IGF-IR tyrosine kinase inhibitor NVP-AEW541 in colorectal cancer cells. Int J Oncol 33, 1107-13 (2008)
30. J. Zhang, P.L. Yang and N.S. Gray: Targeting cancer with small molecule kinase inhibitors. Nature Rev. Cancer 9, 28-39(2009)
31. T. Mitsudomi and Y. Yatabe: Epidermal growth factor receptor in relation to tumor development: EGFR gene and cancer. FEBS J 27, 301-308 (2010)
32. J.Y. Wu, S.G. Wu, C.H. Yang, C.H. Gow, Y.L. Chang, C.J. Yu, J.Y. Shih and P.C .Yang: Lung cancer with epidermal growth factor receptor exon 20 mutations is associated with poor gefitinib treatment response. Clin Cancer Res 14, 4877-82 (2008)
33. D.L.Reidy, E.Vakiani, M.G. Fakih, M.W. Saif, J. R. Hecht, N. Goodman-Davis, E. Hollywood, J. Shia, J. Schwartz, K. Chandrawansa, A. Dontabhaktuni, H. Youssoufian, D.B. Solit, and L.B. Saltz: Randomized phase II study of the insulin like growth factor-1 receptor inhibitor IMC-A12., with or without cetuximab, in patients with cetuximab or panitumumab refractory metastatic colorectal cancer. J Clin Oncol 28, 4240-46 (2010)
34. J.M. Knowlden, I.R. Hutcheson, D. Barrow, J.M. Gee and R.I. Nicholson: Insulin-like growth factor-I receptor signaling in tamoxifen-resistant breast cancer: a supporting role to the epidermal growth factor receptor. Endocrinology 146(11), 4609-18 (2005)
35. J.M. Knowlden , H.E. Jones, D. Barrow, J.M. Gee, R.I. Nicholson and I.R. Hutcheson: Insulin receptor substrate-1 involvement in epidermal growth factor receptor and insulin-like growth factor receptor signalling: implication for Gefitinib ('Iressa') response and resistance. Breast Cancer Res Treat 111(1), 79-91 (2008)
36. C. Desbois-Mouthon, W. Cacheux, M.J. Blivet-Van Eggelpoël, V. Barbu, L. Fartoux, R. Poupon, C. Housset, O. Rosmorduc: Impact of IGF 1R/EGFR crosstalk on hepatoma cell sensitivity to gefitinib. Int J Cancer 119(11), 2557-66 (2006)
37. E. Buck, A. Eyzaguirre, M. Rosenfeld-Franklin, S. Thomson, M. Mulvihill, S. Barr, E. Brown, M. O'Connor, Y. Yao, J. Pachter, M. Miglarese, D. Epstein, K.K. Iwata, J.D. Haley, N.W. Gibson and Q.S. Ji: Feedback mechanisms promote cooperativity for small molecule inhibitors of epidermal and insulin-like growth factor receptors. Cancer Res 68(20), 8322-32 (2008)
38. H.E. Jones, L. Goddard, J.M. Gee, S. Hiscox, M. Rubini, D. Barrow, J.M. Knowlden, S. Williams, A.E. Wakeling and R.I. Nicholson: Insulin-like growth factor-I receptor signalling and acquired resistance to gefitinib (ZD1839; Iressa) in human breast and prostate cancer cells. Endocr Relat Cancer 11(4), 793-814 (2004)
39. H.E. Jones, J.M. Gee, I.R. Hutcheson, J.M. Knowlden, D. Barrow and R.I. Nicholson: Growth factor receptor interplay and resistance in cancer. Endocr Relat Cancer Suppl 1, S45-51 (2006)
40. H. Ji, X. Zhao, Y. Yuza, T. Shimamura, D. Li, A. Protopopov, B.L. Jung, K. McNamara, H. Xia, K.A. Glatt, R.K. Thomas, H. Sasaki, J.W. Horner, M. Eck, A. Mitchell, Y. Sun, R. Al-Hashem, R.T. Bronson, S.K. Rabindran, C.M. Discafani, E. Maher, G.I. Shapiro, M. Meyerson and K.Wong: Epidermal growth factor receptor variant III mutations in lung tumorigenesis and sensitivity ti tyrosine kinase inhibitors. Proc Natl Acad Sci USA 103, 7817-7822 (2006)
41. Z. Tang, R. Du, S. Jiang, C. Wu, D.S. Barkauskas, J. Richey, J. Molter, M. Lam, C. Flask, S. Gerson, A. Dowlati, L .Liu, Z. Lee, B. Halmos, Y Wang, J.A .Kern and P.C .Ma: Dual MET EGFR combinatorial inhibition against T790M-EGFR-mediated erlotinib-resistant lung cancer. Br J Cancer 99, 911-22 (2008)
42. B. Burtness, M.A. Goldwasser, W. Flood, B. Mattar and A.A. Forastiere: Phase III randomized trial of cisplatin plus placebo compared with cisplatin plus cetuximab in metastatic/recurrent head and neck cancer: an Eastern Cooperative Oncology Group study. J Clin Oncol 23, 8646-54 (2005)
43. D.L. Wheeler, S. Huang, T.J. Kruser, M.M. Nechrebecki, E.A. Armstrong, S. Benavente, V. Gondi, K.T. Hsu and P.M. Harari: Mechanisms of acquired resistance to cetuximab: role of HER (ErbB) family members. Oncogene 27, 3944-56 (2008)
44. U. Gatzemeier, A. Pluzanska, A. Szczesna, E. Kaukel, J. Roubec, F. De Rosa, J.Milanowski, H. Karnicka-Mlodkowski, M. Pesek, P. Serwatowski, R. Ramlau, T. Janaskova , J. Vansteenkiste, J. Strausz, G.M. Manikhas and J. Von Pawel: 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 25, 1545-52 (2007)
45. K. Kelly, K. Chansky, L.E. Gaspar, K.S. Albain, J.Jett, Y.C. Ung, D.H.M. Lau, J.J. Crowley and D.R. Gandara: Phase III trial of maintenance gefitinib or placebo after concurrent chemoradiotherapy and docetaxel consolidation in inoperable stage III non-small-cell lung cancer: SWOG S0023. J Clin Oncol 26, 2450-6 (2008)
46. R. Tandon, S. Kapoor, S. Vali, V. Senthil, D. Nithya, R. Venkataramanan, A Sharma, A. Talwadkar, A. Ray, P.K. Bhatnagar and S.G. Dastidar: Dual epidermal growth factor receptor (EGFR)/insulin-like growth factor-1 receptor (IGF 1R) inhibitor: a novel approach for overcoming resistance in anticancer treatment. Eur J Pharmacol 667,56-65 (2011)
47. C.E. Galer, C.L. Corey, Z. Wang, M.N. Younes, F. Gomez-Rivera, S.A. Jasser, D.L. Ludwig, A.K. El-Naggar , R.S. Weber and J.N. Myers: Dual inhibition of epidermal growth factor receptor and insulin-like growth factor receptor I: reduction of angiogenesis and tumor growth in cutaneous squamous cell carcinoma. Head Neck 33, 189-98 (2011)
48. J. Massague and M.P. Czech: The subunit structures of two distinct receptors for insulin-like growth factors I and II and their relationship to the insulin receptor. J Biol Chem 257, 5038-5045 (1982)
49. T.P.J. Garrett, N.M. McKern, M. Lou, M.J. Frenkel, J.D. Bentley, G.O. Lovrecz, T.C. Elleman, L.J. Cosgrove and C.W. Ward: Crystal structure of the first three domains of the type-1 insulin-like growth factor receptor. Nature 394, 395-399 (1998)
50. A.A. Butler, S. Yakar, I.H. Gewolb, M. Karas, Y. Okubo and D. LeRoith: Insulin-like growth factor-I receptor signal transduction: at the interface between physiology and cell biology. Comp. Biochem .Physiol B Biochem Mol Biol 121, 19-26 (1998)
51. A.A. Samani and P. Brodt: The receptor for the type I insulin-like growth factor and its ligands regulate multiple cellular functions that impact on metastasis. Surg Oncol Clin N Am 10, 289-312 (2001)
52. A. Christoforidis, I. Maniadaki and R. Stanhope: Growth hormone/insulin-like growth Factor-1 axis during puberty. Pediatr Endocrinol Rev 35-10 (2005)
53. G. Wrobel, P. Roerig, F. Kokocinski, K. Neben, M. Hahn, G. Reifenberger and P. Lichter: Microarray-based gene expression profiling of benign, atypical and anaplastic meningiomas identifies novel genes associated with meningioma progression. Int J Cancer 11, 4249-256 (2005)
54. W. Hartmann, A. Koch, H. Brune, A. Waha, U. Schüller, I. Dani, D. Denkhaus, W. Langmann, U. Bode, O.D. Wiestler, K.l Schilling and T. Pietsch: Insulin-like growth factor II is involved in the proliferation control of medulloblastoma and its cerebellar precursor cells. Am J Pathol 166, 1153-1162 (2005)
55. C.M. Perks and J.M. Holly: The insulin-like growth factor (IGF) family and breast cancer. Breast Dis 18, 45-60 (2003)
56. C.M. Perks and J. M. Holly: IGFBPs and breast cancer. Breast Dis 17, 91-104 (2003)
57. J.M. Chan, M.J. Stampfer, E. Giovannucci, P.H. Gann, J. Ma, P. Wilkinson, C.H. Hennekens and M. Pollak: Plasma insulin-like growth factor-I and prostate cancer risk: a prospective study. Science 279, 563-566 (1998)
58. N.M. Probst-Hensch, J.M. Yuan, F.Z. Stanczyk, Y.T. Gao, R.K. Ross and M.C. Yu: IGF-1, IGF-2 and IGFBP-3 in prediagnostic serum: association with colorectal cancer in a cohort of Chinese men in Shanghai. Br J Cancer 85, 1695-1699 (2001)
59. R. Palmqvist, G. Hallmans, E. Riboli, S. Rinaldi, C. Biessy, R. Stenling and R Kaaks: Plasma insulin-like growth factor 1, insulin-like growth factor binding protein 3, and risk of colorectal cancer: a prospective study in northern Sweden. Gut 50, 642-646 (2002)
60. A.F. Chambers, A.C, Groom and I.C. MacDonald: Dissemination and growth of cancer cells in metastatic sites. Nature Rev Cancer 2, 563-572 (2002)
61. P. Toniolo, P.F. Bruning, A. Akhmedkhanov, J.M. Bonfrer, K.L. Koenig, A. Lukanova, R.E. Shore and A. Zeleniuch-Jacquotte: Serum insulin-like growth factor-I and breast cancer. Int J Cancer 88, 828-832 (2000)
62. S.E. Hankinson, W.C. Willett, G.A. Colditz, D.J. Hunter, D.S. Michaud, B. Deroo, B. Rosner, F.E .Speizer and M. Pollak: Circulating concentrations of insulin-like growth factor-I and risk of breast cancer. Lancet 351, 1393-1396 (1998)
63. N.E. Allen, A.W. Roddam, D.S. Allen, I.S. Fentiman, I.S. Silva, J. Peto, J.M.P. Holly and T. J. Key: A prospective study of serum insulin-like growth factor-I (IGF-I), IGF-II, IGF-binding protein-3 and breast cancer risk. Br J Cancer 92, 1283-1287 (2005)
64. P. Stattin, A. Bylund, S. Rinaldi, C. Biessy, H. Déchaud, U.H. Stenman, L. Egevad, E. Riboli, G. Hallmans and R. Kaaks: Plasma insulin-like growth factor-I, insulin-like growth factor-binding proteins,and prostate cancer risk: a prospective study. J Natl Cancer Inst 92, 1910-1917 (2000)
65. H. Yu, M.R. Spitz, J. Mistry, J.Gu, W.K. Hong and X. Wu: Plasma levels of insulin-like growth factor-I and lung cancer risk: a case control analysis. J Natl Cancer Inst 91, 151-156 (1999)
66. J. Ma, M.N. Pollak, E. Giovannucci, J.M. Chan, Y. Tao, C.H. Hennekens and M.J. Stampfer: Prospective study of colorectal cancer risk in men and plasma levels of insulin-like growth factor (IGF)-I and IGF-binding protein-3. J Natl Cancer Inst 91, 620-625 (1999)
67. E. Petridou, P. Koukoulomatis, D.M. Alexe, Z. Voulgaris, E. Spanos and D. Trichopoulos: Endometrial cancer and the IGF system: a case-control study in Greece. Oncology 64, 341-345 (2003)
68. H. Zhao, H.B. Grossman, M.R. Spitz, S.P. Lerner, K. Zhang and X. Wu: Plasma levels of insulin-like growth factor-1 and binding protein-3, and their association with bladder cancer risk. J Urol 169, 714-717 (2003)
69. S. Shiono, G. Ishii, K. Nagai, Y. Murata, K. Tsuta, J. Nitadori, T. Kodama and A. Ochiai: Immunohistochemical prognostic factors in resected colorectal lung metastasis using tissue microarray analysis. Eur J Surg Oncol 32, 308-309 (2006)
70. Y. Xie, B. Skytting and G. Nilsson: Expression of insulinlike growth factor-1 receptor in synovial sarcoma: association with an aggressive phenotype. Cancer Res 59, 3588-3591 (1999)
71. C. All-Ericsson, L. Girnita, S. Seregard, A. Bartolazzi, M.J. Jager and O. Larsson: Insulin-like growth factor-1 receptor in uveal melanoma: a predictor for metastatic disease and a potential therapeutic target. Invest Ophthalmol Vis Sci 43, 1-8 (2002)
72. Y. Jiang, L. Wang, W. Gong, D. Wei, X. Le, J. Yao, J. Ajani, J.L. Abbruzzese, S. Huang and Xie K: A high expression level of insulin-like growth factor I receptor is associated with increased expression of transcription factor Sp1 and regional lymph node metastasis of human gastric cancer. Clin Exp Metastasis 21, 755-764 (2004)
73. P. Kornprat, P. Rehak, J. Rüschoff and C. Langner: Expression of IGF-I, IGF-II, and IGF-IR in gallbladder carcinoma. A systematic analysis including primary and corresponding metastatic tumors. J Clin Pathol 59, 202-206 (2006)
74. D. Feldser, F. Agani and V.I. Narayan: Reciprocal positive regulation of hypoxia-inducible factor 1a and insulin-like growth factor 2. Cancer Res. 59, 3915-3918 (1999)
75. E. Zelzer, Y. Levy, C. Kahana, B.Z. Shilo, M. Rubinstein and B. Cohen: Insulin induces transcription of target genes through the hypoxia-inducible factor HIF-1a/ARNT. EMBO J 17, 5085-5094 (1998)
76. R. Fukuda, K. Hirota, F. Fan, Y.D. Jung, L.M. Ellis and G.L. Semenza: Insulin-like growth factor 1 induces hypoxia-inducible factor 1-mediated vascular endothelial growth factor expression, which is dependent on MAP kinase and phosphatidylinositol 3-kinase signaling in colon cancer cells. J Biol Chem 277, 38205-38211 (2002)
77. S. Shigemastu, K. Yamauchi, Matsumoto, K. Nakajima, S. Iijima, T. Aizawa and K Hashizume: IGF-1 regulates migration and angiogenesis of human endothelial cells. Endocr J, 46 (Supplement) S59-S62 (1999)
78. O.H. Lee, S.K. Bae, M.H. Bae, Y.M. Lee, E.J. Moon, H.J. Cha, Y.G. Kwon and K.W. Kim: Identification of angiogenic properties of insulin-like growth factor II in in vitro angiogenesis models. Br J Cancer 82, 385-391 (2000)
79. J. Grulich-Henn, J. Ritter, S. Mesewinkel, U. Heinrich, M. Bettendorf and K.T. Preissner: Transport of insulin-like growth factor-I across endothelial cell monolayers and it's binding to the sub-endothelial matrix. Exp Clin Endocrinol Diabetes 110, 67-73 (2002)
80. C.L. Arteaga, L.J. Kitten, E.B. Coronado, S. Jacobs, F.C. Kull, Jr, D C Allred and C.K. Osborne: Blockade of the type I somatomedin receptor inhibits growth of human breast cancer cells in athymic mice. J Clin Invest 84, 1418-1423 (1989)
81. D. Sachdev, R. Singh, Y. Fujita-Yamaguchi and D. Yee: Down-regulation of insulin receptor by antibodies against the type I insulin-like growth factor receptor: implications for anti-insulin-like growth factor therapy in breast cancer. Cancer Res 66, 2391-2402 (2006)
82. C.S. Mitsiades, N.S. Mitsiades, C.J. McMullan, V. Poulaki, R. Shringarpure, M. Akiyama, T. Hideshima, D. Chauhan, M. Joseph, T.A. Libermann, C. García-Echeverría, M.A. Pearson, F. Hofmann, K.C. Anderson and A.L. Kung: Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors. Cancer Cell 5, 221-230 (2004)
83. B.D. Cohen, D.A. Baker, C. Soderstrom, G. Tkalcevic, A.M. Rossi, P.E. Miller, M.W. Tengowski , F. Wang, A. Gualberto, J.S. Beebe and J.D. Moyer: Combination therapy enhances the inhibition of tumor growth with the fully human anti-Type 1 insulin-like growth factor receptor monoclonal antibody CP-751, 871. Clin Cancer Res 11, 2063-2073 (2005)
84. A.W. Tolcher, J. Sarantopoulos, A. Patnaik, K. Papadopoulos, C.C. Lin, J. Rodon, B. Murphy, B. Roth, I. McCaffery, K.S. Gorski, B. Kaiser, M. Zhu, H. Deng, G. Friberg and I. Puzanov: Phase I, pharmacokinetic, and pharmacodynamic study of AMG 479, a fully human monoclonal antibody to insulin-like growth factor receptor 1. J Clin Oncol 27, 5800-7 (2009)
85. F. Atzori, J.Tabernero, A. Cervantes, L. Prudkin, J. Andreu, E. Rodríguez-Braun, A. Domingo, J. Guijarro, C. Gamez, J. Rodon, S. Di Cosimo, H. Brown, J. Clark, J.S. Hardwick , R.A. Beckman, W.D. Hanley, K. Hsu, E. Calvo, S. Roselló, R.B. Langdon and J. Baselga: A Phase I Pharmacokinetic and Pharmacodynamic Study of Dalotuzumab (MK-0646), an Anti-Insulin-like Growth Factor-1 Receptor Monoclonal Antibody, in Patients with Advanced Solid Tumors. Clin Cancer Res19, 6304-12 (2011)
86. A. Ullrich, A. Gray, A.W. Tam, T. Yang-Feng, M. Tsubokawa, C. Collins, W. Henzel, T. Le Bon, S. Kathuria and E. Chen: Insulin-like growth factor I receptor primary structure: comparison with insulin receptor suggests structural determinants that define functional specificity. EMBO J 5, 2503-2512 (1986)
87. C.García-Echeverría, M.A. Pearson, A. Marti, T. Meyer, J. Mestan, J. Zimmermann, J. Gao, J. Brueggen, H.G. Capraro, R. Cozens, D.B. Evans, D. Fabbro, P. Furet, D.G. Porta , J. Liebetanz , G. Martiny-Baron , S. Ruetz and F. Hofmann: In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell 5, 231-239 (2004)
88. K. Scotlandi, M.C. Manara, G. Nicoletti, P.L. Lollini, S. Lukas, S. Benini, S. Croci, S. Perdichizzi , D. Zambelli M. Serra, C. García- Echeverría, F. Hofmann and P. Picci: Antitumor activity of the insulin-like growth factor-I receptor kinase inhibitor NVP-AEW541 in musculoskeletal tumors, Cancer Res 65, 3868-3876 (2005)
89. S. Di Cosimo, J. Seoane, M. Guzman, F. Rojo, J. Jimenez, J. Anido, J. Arribas, F. Cognetti and J. Baselga: Combination of the mammalian target of rapamycin (mTOR) inhibitor everolimus (E) with the insulin like growth factor-1-receptor (IGF-1-R) inhibitor NVP-AEW-541: A mechanistic based anti-Tumor strategy. J Clin Oncol 23, (Supplement) Astract 3112 (2005)
90. A. Girnita, L. Girnita, F. del Prete, A. Bartolazzi, O. Larsson and M. Axelson: Cyclolignans as inhibitors of the insulin-like growth factor-1 receptor and malignant cell growth, Cancer Res 64, 236-242 (2004)
91. G. Blum, A. Gazit and A. Levitzki: Development of new insulin-like growth factor-1 receptor kinase inhibitors using catechol mimics. J Biol Chem 278, 40442-40454 (2003)
92. K.E. O'Reilly, F. Rojo, Q.B. She, D. Solit, G.B. Mills, D. Smith, H. Lane, F. Hofmann, D.J. Hicklin, D.L. Ludwig, J. Baselga and N. Rosen: mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. Cancer Res 66, 1500-8(2006)
93. P.J. Beltran, P. Mitchell, G. Moody, Y. Chung, E. Cajulis, B. Belmontes, R. Radinsky and F. Calzone: Effect of AMG 479 on anti-Tumor effects of gemcitabine and erlotinib against pancreatic carcinoma xenograft models. J Clin Oncol 26, (Supplement) Abstract 4617(2008)
94. W.N. Pappano, P.M. Jung, J.A. Meulbroek, Y.C. Wang, R.D. Hubbard, Q. Zhang , M.M. Grudzien, N.B. Soni, E.F. Johnson, G.S. Sheppard, C. Donawho, F.G. Buchanan, S.K. Davidsen, R.L. Bell and J. Wang: Reversal of oncogene transformation and suppression of tumor growth by the novel IGF1R kinase inhibitor A-928605. BMC Cancer 9, 314 (2009)
95. J.L. Wilsbacher, Q. Zhang, L.A. Tucker, R.D. Hubbard, G.S. Sheppard, N.Y. Bamaung, S.D. Fidanze, G.T. Wang, X. Hu, S.K. Davidsen, R.L. Bell and J. Wang: Insulin-like growth factor-1 receptor and ErbB kinase inhibitor combinations block proliferation and induce apoptosis through cyclin D1 reduction and Bax activation. J Biol Chem 283, 23721-23730 (2008)
96. Q.B. She, D. Solit, A. Basso and M.M. Moasser: Resistance to gefetinib in PTEN-null HER-overexpressing tumor cells can be overcome through restoration of PTEN function or pharmacologic modulation of constitutive phosphatidylinositol 3'kinase/Akt pathway signaling. Clin Cancer Res 9, 4340-4346 (2003)
97. J.G. Paez, P.A. Jänne, J.C. Lee, S. Tracy, H. Greulich, S. Gabriel, P. Herman, F.J. Kaye, N. Lindeman, T.J. Boggon, K. Naoki, H. Sasaki, Y. Fujii, M.J. Eck , W.R. Sellers , B.E. Johnson and M. Meyerson: EGFR mutations in lung cancer: Correlation with clinical response to gefitinib therapy, Science 304, 1497-1500 (2004)
98. W. Pao, V. Miller, M. Zakowski, J. Doherty, K. Politi, I. Sarkaria, B. Singh, R. Heelan, V. Rusch, L . Fulton, E. Mardis, D. Kupfer, R. Wilson, M. Kris and H. Varmus: EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci USA 101, 13306-11 (2004)
99. A. Chakravarti, J.S. Loeffler, and N.J. Dyson: Insulinlike growth factor receptor I mediates resistance to antiepidermal growth factor receptor therapy in primary human glioblastoma cells through continued activation of phosphoinositide 3-kinase signalling. Cancer Res 62, 200-207 (2002)
100. M.M. Chitnis, J.S. Yuen, A.S. Protheroe, M. Pollak and V.M. Macaulay: The type 1 insulin-like growth factor receptor pathway. Clin. Cancer Res 14, 6364-6370 (2008)
101. A. Gualberto and M. Pollak: Emerging role of insulin like growth factor receptor inhibitors in oncology: early clinical trial results and future directions. Oncogen 28, 3009-3021 (2009)
102. A.S. Martins, C. Mackintosh, D. H. Martín, M. Campos, T. Hernández, J.L. Ordóñez and E. de Alava E: Insulin-like growth factor I receptor pathway inhibition by ADW742, alone or in combination with imatinib, doxorubicin, or vincristine, is a novel therapeutic approach in Ewing tumor. Clin Cancer Res 12, 3532-40 (2006)
103. P. J. Beltran, P. Mitchell, G. Moody, Y. Chung, E. Cajulis, B. Belmontes, R. Radinsky and F. Calzone: Effect of AMG 479 on anti-Tumor effects of gemcitabine and erlotinib against pancreatic carcinoma xenograft models. J. Clin. Oncol, 26 (Supplement) Abstract 4617 (2008)
104. H. Modjtahedi, D.K. Moscatello, G. Box, M. Green, C. Shotton, D.J. Lamb, L.J. Reynolds, A.J. Wong, C. Dean, H. Thomas and S. Eccles: Targeting of cells expressing wild-Type EGFR and type-III mutant EGFR (EGFRvIII) by anti-EGFR MAb ICR62: a two-pronged attack for tumor therapy. Int J Cancer 105, 273-2780 (2003)
105. U. Gatzemeier, A. Pluzanska, A. Szczesna, E. Kaukel, J. Roubec, F. De Rosa, J. Milanowski, H. Karnicka-Mlodkowski, M. Pesek, P. Serwatowski, R. Ramlau, T. Janaskova , J.Vansteenkiste, J. Strausz, G.M. Manikhas and J. Von Pawel: Insulin-like growth factor-I receptor signaling and resistance to trastuzumab (Herceptin). J Natl Cancer Inst 93, 1852-1857(2001)
106. Jones JI and Clemmons DR: Insulin-like growth factors and their binding proteins: biological actions. Endocr Rev 16, 3-34(1995)
107. M. Hopfner, A.P. Sutter, A. Huether, V. Baradari and H. Scherubl: Tyrosine kinase of insulin growth factor receptor as target for novel treatment and prevention strategies of colorectal cancer.World J Gastroenterol 12, 5635-5643 (2006)
108. Panitumumab combination study with AMG 102 or AMG 479 in wild-Type KRAS mCRC. Sponsor: Amgen; ClinicalTrials.gov Identifier: NCT00788957 110. N.K. Saxena , L. Taliaferro-Smith , B.B. Knight , D. Merlin , F.A. Anania , R.M. O'Regan and D. Sharma: Bidirectional crosstalk between leptin and insulin-like growth factor-I signaling promotes invasion and migration of breast cancer cells via transactivation of epidermal growth factor receptor. Cancer Res 68(23), 9712-22 (2008)
109. C. Desbois-Mouthon, A. Baron, M.J. Blivet-Van Eggelpoël, L. Fartoux, C. Venot, F. Bladt, C. Housset and O. Rosmorduc: Insulin-like growth factor-1 receptor inhibition induces a resistance mechanism via the epidermal growth factor receptor/HER3/AKT signaling pathway: rational basis for cotargeting insulin-like growth factor-1 receptor and epidermal growth factor receptor in hepatocellular carcinoma. Clin Cancer Res 15(17), 5445-56 (2009)
110. F. Huang, A. Greer, W. Hurlburt, X. Han, R. Hafezi, G.M. Wittenberg, K. Reeves, J. Chen, D. Robinson , A. Li, F.Y. Lee, M.M. Gottardis, E. Clark, L. Helman, R.M. Attar, A. Dongre and J.M. Carboni: The mechanisms of differential sensitivity to an insulin-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors. Cancer Res 69(1), 161-170(2009)
111. M. Hewish, I. Chau and D. Cunningham: Insulin-like growth factor 1 receptor targeted therapeutics: novel compounds and novel treatment strategies for cancer medicine. Recent Pat Anticancer Drug Discov 4, 54-72(2009)
112. P.J. Beltran, Y.A. Chung, G. Moody, P. Mitchell, E. Cajulis, S. Vonderfecht, R. Kendall, R. Radinsky and F.J. Calzone: Efficacy of Ganitumab (AMG 479), Alone and in combination with Rapamycin, in Ewing's and Osteogenic Sarcoma Models. J Pharmacol Exp Ther 337, 644-54 (2011)
113. P.J. Beltran, P. Mitchell, Y.A. Chung, E. Cajulis, J. Lu, B. Belmontes, J. Ho, M.M. Tsai, M. Zhu, S. Vonderfecht, R. Baserga, R. Kendall, R. Radinsky and F.J. Calzone: AMG 479, a fully human anti-insulin-like growth factor receptor type I monoclonal antibody, inhibits the growth and survival of pancreatic carcinoma cells. Mol Cancer Ther 8, 1095-1105 (2009)
114. H.M. Rosevear, A.J. Lightfoot and T.S. Griffith: Conatumumab, a fully human mAb against death receptor 5 for the treatment of cancer. Curr Opin Investig Drugs 11, 688-98 (2010)
115. E. Buck & M. Mulvihill: Small molecule inhibitors of the IGF 1R/IR axis for the treatment of cancer. Expert Opin Investig Drugs 20, 605-21 (2011)
116. J. Furukawa, C.J. Wraight, S.M. Freier, E. Peralta, L.M. Atley, B.P. Monia, M.E. Gleave and M.E. Cox: Antisense oligonucleotide targeting of insulin-like growth factor-1 receptor (IGF 1R) in prostate cancer. Prostate 70, 206-18 (2010)
117. M. Spiliotaki, H. Markomanolaki, M. Mela, D. Mavroudis, V. Georgoulias and S. Agelaki: Targeting the insulin-like growth factor I receptor inhibits proliferation and VEGF production of non-small cell lung cancer cells and enhances paclitaxel-mediated anti-Tumor effect. Lung Cancer 73,158-65 (2011)
118. G. Descamps, P. Gomez-Bougie, C. Venot, P. Moreau, R. Bataille and M. Amiot: A humanised anti-IGF 1R monoclonal antibody (AVE1642) enhances Bortezomib-induced apoptosis in myeloma cells lacking CD45. Br J Cancer 100, 366-9 (2009)
119. D. Olmos, S. Postel-Vinay, L.R. Molife, S.H. Okuno, S.M. Schuetze, M.L. Paccagnella, G.N. Batzel, D. Yin, K. Pritchard-Jones, I. Judson, F.P. Worden, A .Gualberto, M. Scurr , J.S. de Bono and P. Haluska: Safety, pharmacokinetics, and preliminary activity of the anti-IGF 1R antibody figitumumab (CP-751,871) in patients with sarcoma and Ewing's sarcoma: a phase 1 expansion cohort study. Lancet Oncol 11, 129-35 (2010)
120. I.M. Collins, P. Beddy and K.J. O'Byrne: Radiological response in an incidental meningioma in a patient treated with chemotherapy combined with CP-751,871, an IGF 1R inhibitor. Acta Oncol 49, 872-4 (2010)
121. L.R. Molife, P.C. Fong, L. Paccagnella, A.H. Reid, H.M. Shaw, L. Vidal, H.T. Arkenau, V. Karavasilis, T.A. Yap, D. Olmos, J. Spicer, S. Postel-Vinay, D. Yin, A. Lipton , L. Demers, K. Leitzel, A. Gualberto and J.S. de Bono: The insulin-like growth factor-I receptor inhibitor figitumumab (CP-751,871) in combination with docetaxel in patients with advanced solid tumors: results of a phase Ib dose-escalation, open-label study. Br J Cancer 103, 332-9 (2010)
122. E.K. H. Rowinsky, Youssoufian, J.R. Tonra, P. Solomon, D. Burtrum and D.L. Ludwig: IMC-A12, a human IgG1 monoclonal antibody to the insulin-like growth factor I receptor, Clin Cancer Res 13, 5549-5555 (2007)
123. M. Scartozzi, M. Bianconi, E. Maccaroni, R. Giampieri, R. Berardi and S. Cascinu: Dalotuzumab, a recombinant humanized mAb targeted against IGF 1R1 for the treatment of cancer. Curr Opin Mol Ther 12, 361-71 (2010)
124. A Study of Ridaforolimus (MK-8669) in Combination With Dalotuzumab (MK-0646) Compared to Standard of Care Treatment in Estrogen Receptor Positive Breast Cancer Patients (MK-8669-041 AM1). Clinical trials.gov.
125. R. Kurzrock, A. Patnaik, J. Aisner, T. Warren, S. Leong, R. Benjamin, S.G. Eckhardt, J.E. Eid, G. Greig, K. Habben, C.D. McCarthy and L. Gore: A phase I study of weekly R1507, a human monoclonal antibody insulinlike growth factor-I receptor antagonist, in patients with advanced solid tumors. Clin Cancer Res 16, 2458-65 (2010)
126. E.A. Kolb, D. Kamara, W. Zhang, J. Lin, P. Hingorani, L. Baker, P. Houghton and R. Gorlick: R1507, a fully human monoclonal antibody targeting IGF 1R, is effective alone and in combination with rapamycin in inhibiting growth of osteosarcoma xenografts. Pediatr Blood Cancer 55, 67-75 (2010)
127. Y. Gong, E. Yao, R. Shen, A. Goel, M. Arcila, J. Teruya-Feldstein, M.F. Zakowski, S. Frankel, M. Peifer, R.K. Thomas, M. Ladanyi and W. Pao: High expression levels of total IGF 1R and sensitivity of NSCLC cells in vitro to an anti-IGF 1R antibody (R1507). PLoS One 4, e7273 (2009)
128. Y. Wang , P. Lipari, X. Wang, J. Hailey, L. Liang, R. Ramos, M. Liu, J.A. Pachter, W.R. Bishop and Y. Wang: A fully human insulin-like growth factor-I receptor antibody SCH 717454 (Robatumumab) has antitumor activity as a single agent and in combination with cytotoxics in pediatric tumor xenografts. Mol Cancer Ther 9, 410-8 (2010)
129. C. Tarn, L. Rink, E. Merkel, D. Flieder, H. Pathak, D. Koumbi, J.R. Testa, B. Eisenberg, M. von Mehren and A.K. Godwin: Insulin-like growth factor 1 receptor is a potential therapeutic target for gastrointestinal stromal tumors. Proc Natl Acad Sci USA 105, 8387-8392(2008)
130. G.K. Abou-Alfa, B.Gansukh, J.F. Chou, J. Shia, M. Capanu, M. Kalin, H.X. Chen, N.J. Zojwalla, S. Katz, D.L. Reidy, D.P. Kelsen and L. Saltz: Phase II study of cixutumumab (IMC-A12, NSC742460; C) in hepatocellular carcinoma (HCC). J Clin Oncol 29, s4043 (2011)
131. J. Wu and A. Xzhu: Targetting insulin-like growth factor axix in hepatocellular carcinoma. J Heamatology Oncol 4, 30 (2011)