Targeting insulin-like growth factor type 1 receptor in cancer therapy

Targeted Oncology

Volumn 4, Issue 4, 2009, Pages 255-266

  Atzori, Francesco ^a   Traina, Tiffany A ^b   Ionta, Maria Teresa ^a   Massidda, Bruno ^a  

^a UNIVERSITY OF CAGLIARI   (Italy)

^b MEMORIAL SLOAN KETTERING CANCER CENTER   (United States)

Author keywords

Clinical trials phase I; Clinical trials phase II; Insulin like growth factor 1 receptor; Monoclonal antibodies; Tyrosine kinase inhibitors

Indexed keywords

3 BROMO 5 TERT BUTYL 4 HYDROXYBENZYLIDENEMALONONITRILE; AMG 479; ANT 429; ANTINEOPLASTIC AGENT; ATL 1101; AVE 1642; BMS 536924; BMS 554417; BORTEZOMIB; BVP 51004; CARBOPLATIN; CETUXIMAB; CISPLATIN; CIXUTUMUMAB; CP 751871; DEFOROLIMUS; DEXAMETHASONE; DOCETAXEL; ERLOTINIB; EXEMESTANE; GEMCITABINE; IMC A 12; INSM 18; IRINOTECAN; MK 0646; MONOCLONAL ANTIBODY; OSI 906; PACLITAXEL; PANITUMUMAB; PF 299804; PREDNISONE; PROTEIN TYROSINE KINASE INHIBITOR; R 1507; ROBATUMUMAB; SCH 717454; SOMATOMEDIN C RECEPTOR; TEMSIROLIMUS; UNCLASSIFIED DRUG; UNINDEXED DRUG; XL 228;

ABDOMINAL PAIN; ACUTE LYMPHOBLASTIC LEUKEMIA; ADRENAL CORTEX CARCINOMA; ALANINE AMINOTRANSFERASE BLOOD LEVEL; AMINOTRANSFERASE BLOOD LEVEL; ANEMIA; ANOREXIA; ANTINEOPLASTIC ACTIVITY; APPETITE; ARTHRALGIA; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; ASTHENIA; BACKACHE; BREAST CANCER; CANCER COMBINATION CHEMOTHERAPY; CANCER HORMONE THERAPY; CANCER RESISTANCE; CANCER RISK; CANCER THERAPY; CHILL; CHRONIC MYELOID LEUKEMIA; CLINICAL TRIAL; COLORECTAL CANCER; COLORECTAL CARCINOMA; CONSTIPATION; COUGHING; DEEP VEIN THROMBOSIS; DIARRHEA; DIGESTIVE SYSTEM CANCER; DIZZINESS; DRUG DOSE ESCALATION; DRUG ERUPTION; DRUG FEVER; DRUG HYPERSENSITIVITY; DRUG RECEPTOR BINDING; DYSPNEA; EWING SARCOMA; FATIGUE; FEBRILE NEUTROPENIA; FECES COLOR; FEVER; FLUSHING; GAMMA GLUTAMYL TRANSFERASE BLOOD LEVEL; GASTROINTESTINAL HEMORRHAGE; HUMAN; HYPERGLYCEMIA; HYPERURICEMIA; HYPOMAGNESEMIA; INFECTION; INJECTION SITE REACTION; LIVER CARCINOMA; LOADING DRUG DOSE; LUNG CANCER; LUNG NON SMALL CELL CANCER; LYMPHOCYTOPENIA; MULTIPLE CYCLE TREATMENT; MULTIPLE MYELOMA; NAIL DISEASE; NAUSEA; NEUROENDOCRINE TUMOR; NEUTROPENIA; NONHUMAN; OSTEOSARCOMA; OVARY CANCER; PAIN; PANCREAS CANCER; PANCREAS CARCINOMA; PARESTHESIA; PNEUMONIA; PRIORITY JOURNAL; PROSTATE CANCER; PROTEIN TARGETING; PRURITUS; PSORIASIS; PURPURA; RASH; REVIEW; SALMONELLOSIS; SARCOMA; SIDE EFFECT; SIGNAL TRANSDUCTION; SYNCOPE; THROMBOCYTOPENIA; TUMOR LYSIS SYNDROME; TUMOR PAIN; VOMITING; WEIGHT REDUCTION;

ANTINEOPLASTIC AGENTS; DRUG DELIVERY SYSTEMS; DRUG SYNERGISM; HUMANS; MALE; NEOPLASMS; PROTEIN KINASE INHIBITORS; RECEPTOR, IGF TYPE 1; SIGNAL TRANSDUCTION;

EID: 72449159103     PISSN: 17762596     EISSN: 1776260X     Source Type: Journal    
DOI: 10.1007/s11523-009-0123-z     Document Type: Review

References (132)

1. MN Pollak ES Schernhammer SE Hankinson 2004 Insulin-like growth factors and neoplasia Nat Rev Cancer 4 505 418 10.1038/nrc1387 1:CAS:528: DC%2BD2cXlt1Oktro%3D 15229476
2. SE Hankinson WC Willett GA Colditz, et al. 1998 Circulating concentrations of insulin-like growth factor-I and risk of breast cancer Lancet 351 9113 1393 1396 10.1016/S0140-6736(97)10384-1 1:STN:280:DyaK1c3lsVansw%3D%3D 9593409 (Pubitemid 28209997)
3. AW Roddam NE Allen P Appleby, et al. 2008 Insulin-like growth factors, their binding proteins, and prostate cancer risk: analysis of individual patient data from 12 prospective studies Ann Intern Med 149 7 461 471 18838726
4. J Ma MN Pollak E Giovannucci, et al. 1999 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 7 620 625 10.1093/jnci/91.7.620 1:CAS:528:DyaK1MXislKgs70%3D 10203281
5. A Ouban P Muraca T Yeatman, et al. 2003 Expression and distribution of insulin-like growth factor-1 receptor in human carcinomas Hum Pathol 34 8 803 908 10.1016/S0046-8177(03)00291-0 1:CAS:528:DC%2BD3sXmslegu7w%3D 14506643 (Pubitemid 37040618)
6. A Camirand M Zakikhani F Young, et al. 2005 Inhibition of insulin-like growth factor-1 receptor signaling enhances growth-inhibitory and proapoptotic effects of gefitinib (Iressa) in human breast cancer cells Breast Cancer Res 7 4 570 579 10.1186/bcr1028
7. HE Jones L Goddard JM Gee, et al. 2004 Insulin-like growth factor-I receptor signaling and acquired resistance to gefitinib (ZD1839; Iressa) in human breast and prostate cancer cells Endocr Relat Cancer 11 4 793 814 10.1677/erc.1.00799 1:CAS:528:DC%2BD2MXhtVartrs%3D 15613453 (Pubitemid 40065552)
8. A Chakravarti JS Loeffler NJ Dyson 2002 Insulin-like growth factor receptor I mediates resistance to anti-epidermal growth factor receptor therapy in primary human glioblastoma cells through continued activation of phosphoinositide 3-kinase signaling Cancer Res 62 1 200 207 1:CAS:528: DC%2BD38XntV2hsA%3D%3D 11782378
9. B Liu M Fang Y Lu, et al. 2001 Fibroblast growth factor and insulin-like growth factor differentially modulate the apoptosis and G1 arrest induced by anti-epidermal growth factor receptor monoclonal antibody Oncogene 20 15 1913 1922 10.1038/sj.onc.1204277 1:CAS:528:DC%2BD3MXivFKht78%3D 11313939 (Pubitemid 32458701)
10. M Sakamoto A Kondo K Kawasaki, et al. 2001 Analysis of gene expression profiles associated with cisplatin resistance in human ovarian cancer cell lines and tissues using cDNA microarray Hum Cell 14 4 305 315 1:STN:280: DC%2BD387ptlOquw%3D%3D 11925933
11. C Shimizu T Hasegawa Y Tani, et al. 2004 Expression of insulin-like growth factor 1 receptor in primary breast cancer: immunohistochemical analysis Hum Pathol 35 12 1537 1542 10.1016/j.humpath.2004.09.005 1:CAS:528: DC%2BD2cXhtVyku7%2FE 15619214 (Pubitemid 40017995)
12. S Abe T Funato S Takahashi, et al. 2006 Increased expression of insulin-like growth factor i is associated with Ara-C resistance in leukemia Tohoku J Exp Med 209 3 217 228 10.1620/tjem.209.217 1:CAS:528: DC%2BD28XntVSrsr4%3D 16778368 (Pubitemid 43905553)
13. F Cappuzzo L Toschi G Tallini GL Ceresoli I Domenichini S Bartolini, et al. 2006 Insulin-like growth factor receptor 1 (IGFR-1) is significantly associated with longer survival in non-small-cell lung cancer patients treated with gefitinib Ann Oncol 17 7 1120 1127 10.1093/annonc/mdl077 1:STN:280:DC%2BD28zotVaksA%3D%3D 16600976 (Pubitemid 43985248)
14. N Friedrich R Haring M Nauck, et al. 2009 Mortality and serum insulin-like growth factor I and insulin-like growth factor binding protein 3 concentrations J Clin Endocrinol Metab 94 5 1732 1739 10.1210/jc.2008-2138 1:CAS:528:DC%2BD1MXlvVCqtbo%3D 19223521
15. MA Rowlands D Gunnell R Harris, et al. 2009 Circulating insulin-like growth factor peptides and prostate cancer risk: a systematic review and meta-analysis Int J Cancer 124 10 2416 2429 10.1002/ijc.24202 1:CAS:528:DC%2BD1MXltFaqt7w%3D 19142965
16. VA Papadimitrakopoulou EN Brown DD Liu, et al. 2006 The prognostic role of loss of insulin-like growth factor-binding protein-3 expression in head and neck carcinogenesis Cancer Lett 239 1 136 143 10.1016/j.canlet.2005.08.009 1:CAS:528:DC%2BD28Xms1agt74%3D 16181731 (Pubitemid 43946585)
17. YS Chang L Wang YA Suh L Mao SJ Karpen FR Khuri, et al. 2004 Mechanisms underlying lack of insulin-like growth factor-binding protein-3 expression in non-small-cell lung cancer Oncogene 23 39 6569 6580 10.1038/sj.onc.1207882 1:CAS:528:DC%2BD2cXmvFGisbw%3D 15247904 (Pubitemid 39265520)
18. L Baglietto DR English JL Hopper, et al. 2007 Circulating insulin-like growth factor-I and binding protein-3 and the risk of breast cancer Cancer Epidemiol Biomarkers Prev 16 4 763 768 10.1158/1055-9965.EPI-06-0960 1:CAS:528:DC%2BD2sXjvV2msr0%3D 17416768 (Pubitemid 46650579)
19. O Nedic V Malenkovic B Dukanovic, et al. 2008 Association of elevated IGFBP-1 with increased IGF-II concentration in patients with carcinoma of the liver Int J Biol Markers 23 4 225 230 1:CAS:528:DC%2BD1MXkvVGltLg%3D 19199270
20. AG Renehan J Jones CS Potten, et al. 2000 Elevated serum insulin-like growth factor (IGF)-II and IGF binding protein-2 in patients with colorectal cancer Br J Cancer 83 10 1344 1350 10.1054/bjoc.2000.1462 1:CAS:528: DC%2BD3cXos12gsr4%3D 11044360
21. B Rikhof J van Doorn AJ Suurmeijer, et al. 2009 Insulin-like growth factors and insulin-like growth factor-binding proteins in relation to disease status and incidence of hypoglycaemia in patients with a gastrointestinal stromal tumour Ann Oncol 20 9 1582 1588 10.1093/annonc/mdp038 1:STN:280:DC%2BD1MrnsVaksw%3D%3D 19276395
22. Y Lin T Jiang K Zhou, et al. 2009 Plasma IGFBP-2 levels predict clinical outcomes of patients with high-grade gliomas Neuro Oncol 10.1215/15228517-2008- 114 19164435
23. M Letsch AV Schally R Busto, et al. 2003 Growth hormone-releasing hormone (GHRH) antagonists inhibit the proliferation of androgen-dependent and -independent prostate cancers Proc Natl Acad Sci U S A 100 3 1250 1255 10.1073/pnas.0337496100 1:CAS:528:DC%2BD3sXhtF2gtbg%3D 12538852 (Pubitemid 36183988)
24. MO Thorner CJ Strasburger Z Wu, et al. 1999 Growth hormone (GH) receptor blockade with a PEG-modified GH (B2036-PEG) lowers serum insulin-like growth factor-I but does not acutely stimulate serum GH J Clin Endocrinol Metab 84 6 2098 2103 10.1210/jc.84.6.2098 1:CAS:528:DyaK1MXjs1OhsLs%3D 10372717
25. I Schreiber M Buchfelder M Droste, et al. 2007 Treatment of acromegaly with the GH receptor antagonist pegvisomant in clinical practice: safety and efficacy evaluation from the German Pegvisomant Observational Study Eur J Endocrinol 156 1 75 82 10.1530/eje.1.02312 1:CAS:528:DC%2BD2sXntlyqtbk%3D 17218728 (Pubitemid 46553905)
26. D Yin F Vreeland LJ Schaaf, et al. 2007 Clinical pharmacodynamic effects of the growth hormone receptor antagonist pegvisomant: implications for cancer therapy Clin Cancer Res 13 3 1000 1009 10.1158/1078-0432.CCR-06-1910 1:CAS:528:DC%2BD2sXhsVyku7k%3D 17289896 (Pubitemid 46340379)
27. J Divisova I Kuiatse Z Lazard, et al. 2006 The growth hormone receptor antagonist pegvisomant blocks both mammary gland development and MCF-7 breast cancer xenograft growth Breast Cancer Res Treat 98 3 315 327 10.1007/s10549-006-9168-1 1:CAS:528:DC%2BD28XnvVGmu7k%3D 16541323 (Pubitemid 44195602)
28. IE McCutcheon A Flyvbjerg H Hill, et al. 2001 Antitumor activity of the growth hormone receptor antagonist pegvisomant against human meningiomas in nude mice J Neurosurg 94 3 487 492 10.3171/jns.2001.94.3.0487 1:CAS:528: DC%2BD3MXhvFKgtbc%3D 11235955
29. M Goya S Miyamoto K Nagai, et al. 2004 Growth inhibition of human prostate cancer cells in human adult bone implanted into nonobese diabetic/severe combined immunodeficient mice by a ligand-specific antibody to human insulin-like growth factors Cancer Res 64 17 6252 6258 10.1158/0008-5472.CAN-04-0919 1:CAS:528:DC%2BD2cXntFCltrg%3D 15342412 (Pubitemid 39129428)
30. CL Arteaga LJ Kitten EB Coronado, et al. 1989 Blockade of the type I somatomedin receptor inhibits growth of human breast cancer cells in athymic mice J Clin Invest 84 5 1418 1423 10.1172/JCI114315 1:CAS:528:DyaL1MXmt1Kjs78%3D 2553774
31. M Pollak 2008 Targeting insulin and insulin-like growth factor signaling in oncology Curr Opin Pharmacol 8 4 384 392 10.1016/j.coph.2008.07.004 1:CAS:528:DC%2BD1cXhtFCktL7L 18674638
32. S Munshi DL Hall M Kornienko, et al. 2003 Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 A resolution Acta Crystallogr D Biol Crystallogr 59 Pt 10 1725 1730 10.1107/S0907444903015415 14501110 (Pubitemid 37245124)
33. M Pollak 2008 Insulin, insulin-like growth factors and neoplasia Best Pract Res Clin Endocrinol Metab 22 4 625 638 10.1016/j.beem.2008.08.004 1:CAS:528:DC%2BD1cXht12rtr7N 18971123
34. F Hofmann C Garcia-Echeverria 2005 Blocking the insulin-like growth factor-I receptor as a strategy for targeting cancer Drug Discov Today 10 15 1041 1047 10.1016/S1359-6446(05)03512-9 1:CAS:528:DC%2BD2MXntVGmsL0%3D 16055020 (Pubitemid 41074142)
35. BD Cohen DA Baker C Soderstrom, et al. 2005 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 5 2063 2073 10.1158/1078-0432.CCR-04-1070 1:CAS:528:DC%2BD2MXitVKrtr0%3D 15756033 (Pubitemid 40471873)
36. P Haluska HM Shaw GN Batzel, et al. 2007 Phase I dose escalation study of the anti insulin-like growth factor-I receptor monoclonal antibody CP-751, 871 in patients with refractory solid tumors Clin Cancer Res 13 19 5834 5840 10.1158/1078-0432.CCR-07-1118 1:CAS:528:DC%2BD2sXhtFSntLrE 17908976 (Pubitemid 47583908)
37. MQ Lacy M Alsina R Fonseca, et al. 2008 Phase I, pharmacokinetic and pharmacodynamic study of the anti-insulinlike growth factor type 1 Receptor monoclonal antibody CP-751, 871 in patients with multiple myeloma J Clin Oncol 26 19 3196 3203 10.1200/JCO.2007.15.9319 1:CAS:528:DC%2BD1cXptlKgtb8%3D 18474873
38. Karp DD, Paz-Ares LG, Blakely LJ et al (2007) Efficacy of the anti-insulin like growth factor I receptor (IGF-IR) antibody CP-751871 in combination with paclitaxel and carboplatin as first-line treatment for advanced non-small cell lung cancer (NSCLC). J Clin Oncol, 2007 ASCO Annual Meeting Proceedings Part I. 25(18S):7506
39. DD Karp MN Pollak RB Cohen PD Eisenberg P Haluska D Yin A Lipton L Demers K Leitzel ML Hixon LW Terstappen L Garland LG Paz-Ares F Cardenal CJ Langer A Gualbert 2009 Safety, pharmacokinetics and pharmacodynamics of the insulin-like growth factor type 1 receptor inhibitor figitumumab (CP-751, 871) in combination with paclitaxel and carboplatin J Thorac Oncol 10.1097/JTO.0b013e3181ba2f1d
40. Study of CP-751,871 in Combination With Sunitinib in Patients With Advanced Solid Tumors. http://clinicaltrials.gov/show/NCT00729833. Accessed 28 Sept 2009
41. A Safety And Efficacy Study Of The Combination Of Oral PF-00299804 And Intravenous CP-751,871 Given Every 3 Weeks. http://clinicaltrials.gov/show/ NCT00728390. Accessed 28 Sept 2009
42. Study Of CP-751,871 In Combination With Cisplatin And Gemcitabine In Chemotherapy-Naïve Patients With Advanced Non-Small Cell Lung Cancer. http://clinicaltrials.gov/show/NCT00560573. Accessed 28 Sept 2009
43. Phase 2 Trial Of CP-751,871 And Docetaxel In Advanced Breast Cancer. http://clinicaltrials.gov/ct2/show/NCT00678626. Accessed 28 Sept 2009
44. Study of CP-751,871 in Combination With Docetaxel and Prednisone in Patients With Hormone Insensitive Prostate Cancer (HRPC). http://clinicaltrials. gov/show/NCT00313781. Accessed 28 Sept 2009
45. Postel-Vinay S, Okuno S, Schuetze S et al (2008) Safety, pharmacokinetics and preliminary activity of the anti-IGF-IR antibody CP-751,871 in patients with sarcoma. 20th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics. Proceedings Eur J Cancer 6(12) 2008, abstract 388
46. Study of CP-751,871 In combination with exemestane in postmenopausal women with Hormone Receptor Positive Advanced Breast Cancer. http://clinicaltrials.gov/show/NCT00372996. Accessed 28 Sept 2009
47. Study Using CP-751,871 In Patients With Stage IV Colorectal Cancer That Has Not Responded To Previous Anti-Cancer Treatments. http://clinicaltrials.gov/ show/NCT00560560. Accessed 28 Sept 2009
48. Trial Of CP-751, 871 And Erlotinib In Refractory Lung Cancer (NSCLC). http://clinicaltrials.gov/show/NCT00673049. Accessed 28 Sept 2009
49. Carboplatin And Paclitaxel With Or Without CP-751, 871 (An IGF-1R Inhibitor) For Advanced NSCLC Of Squamous, Large Cell And Adenosquamous Carcinoma Histology. http://clinicaltrials.gov/show/NCT00596830. Accessed 28 Sept 2009
50. D Burtrum Z Zhu D Lu, et al. 2003 A fully human monoclonal antibody to the insulin-like growth factor I receptor blocks ligand-dependent signaling and inhibits human tumor growth in vivo Cancer Res 63 8912 8921 1:CAS:528: DC%2BD3sXhtVSqtbvL 14695208
51. EK Rowinsky H Youssoufian JR Tonra, et al. 2007 (2007) IMC-A12, a human IgG1 monoclonal antibody to the insulin-like growth factor I receptor Clin Cancer Res 13 18 Pt 2 5549s 5555s 10.1158/1078-0432.CCR-07-1109 1:CAS:528:DC%2BD2sXhtVCitLrO 17875788 (Pubitemid 47510386)
52. Higano CS, Yu EY, Whiting SH et al (2007) A phase I, first in man study of weekly IMC-A12, a fully human insulin like growth factor-I receptor IgG1 monoclonal antibody, in patients with advanced solid tumors. J Clin Oncol 25(18 S): abstract 3505
53. Rothenberg ML et al (2007) Phase I dose-escalation study of the anti-IGF-IR recombinant human IgG1 monoclonal antibody (Mab) IMC-A12, administered every other week to patients with advanced solid tumors. AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics, abstract C84
54. A Five-Tier, Phase 2 Open-Label Study of IMC-A12 Administered as a Single Agent. http://clinicaltrials.gov/show/NCT00668148. Accessed 28 Sept 2009
55. Cixutumumab in Treating Patients With Relapsed or Refractory Solid Tumors. http://clinicaltrials.gov/ct/show/NCT00831844. Accessed 28 Sept 2009
56. A Study of IMC-A12 in Adrenocortical Cancer. http://clinicaltrials.gov/ show/NCT00810537. Accessed 28 Sept 2009
57. Monoclonal Antibody IMC-A12 and Temsirolimus in Treating Patients With Locally Advanced or Metastatic Cancer. http://clinicaltrials.gov/ct/show/ NCT00678223. Accessed 28 Sept 2009
58. Cixutumumab and Temsirolimus in Treating Young Patients With Solid Tumors That Have Recurred or Not Responded to Treatment. http://clinicaltrials.gov/ct/ show/NCT00880282. Accessed 28 Sept 2009
59. IMC-A12 and Temsirolimus in Treating Patients With Locally Recurrent or Metastatic Breast Cancer. http://clinicaltrials.gov/ct/show/NCT00699491. Accessed 28 Sept 2009
60. Monoclonal Antibody IMC-A12 and Doxorubicin in Treating Patients With Unresectable, Locally Advanced, or Metastatic Soft Tissue Sarcoma. http://clinicaltrials.gov/ct/show/NCT00720174. Accessed 28 Sept 2009
61. Study of IMC-A12, Alone or in Combination With Cetuximab, in Patients With Recurrent or Metastatic Squamous Cell Carcinoma (MSCC) of the Head and Neck. http://clinicaltrials.gov/show/NCT00617734. Accessed 28 Sept 2009
62. Capecitabine and Lapatinib With or Without Monoclonal Antibody Therapy in Treating Patients With Previously Treated HER2-Positive Stage IIIB, Stage IIIC, or Stage IV Breast Cancer. http://clinicaltrials.gov/ct/show/NCT00684983. Accessed 28 Sept 2009
63. Study Using IMC-A12 or IMC-1121B Plus Mitoxantrone and Prednisone in Metastatic Androgen-Independent Prostate Cancer, Following Disease Progression on Docetaxel-Based Chemotherapy. http://clinicaltrials.gov/show/NCT00683475. Accessed 28 Sept 2009
64. A Study for Safety and Effectiveness of IMCA12 by Itself or Combined With Antiestrogens to Treat Metastatic Breast Cancer in Patients Who Progressed on Antiestrogen Therapy. http://clinicaltrials.gov/show/NCT00728949. Accessed 28 Sept 2009
65. Mitotane With or Without IMC-A12 in Treating Patients With Recurrent, Metastatic, or Primary Adrenocortical Cancer That Cannot Be Removed By Surgery. http://clinicaltrials.gov/ct/show/NCT00778817. Accessed 28 Sept 2009
66. Erlotinib With or Without IMC-A12 in Treating Patients With Stage III or Stage IV Non-Small Cell Lung Cancer. http://clinicaltrials.gov/ct/show/ NCT00778167. Accessed 28 Sept 2009
67. Study of Effectiveness of IMC-A12 Antibody Combined With Hormone Therapy Prior to Surgery to Treat Prostate Cancer. http://clinicaltrials.gov/show/ NCT00769795. Accessed 28 Sept 2009
68. Multicenter Study of IMC-A12 in Combination With Depot Octreotide in Patients With Carcinoid or Islet Cell Cancer. http://clinicaltrials.gov/show/ NCT00781911. Accessed 28 Sept 2009
69. A Study of Irinotecan and Cetuximab With or Without IMC-A12 for Treatment of People With Colon or Rectum Cancer Who Got Worse After Their First Treatment With Oxaliplatin and Bevacizumab (FC-4). http://clinicaltrials.gov/show/ NCT00845039. Accessed 28 Sept 2009
70. A Study to Test IMC-A12 With and Without Other Standard Chemotherapies in Patients With Lung Cancer Who Have Not Received Chemotherapy Before. http://clinicaltrials.gov/show/NCT00870870. Accessed 28 Sept 2009
71. Beltran P, Mitchell P, Hwang D et al (2007) Inhibition of endocrine IGF-1 signaling in normal murine tissues and human tumor xenografts with AMG 479, a fully human anti IGF-1R monoclonal antibody. AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics, 2007, abstract A67
72. Calzone F, Chung YA, Cajulis E et al (2008) Domain-specific mechanisms of receptor inhibition by AMG 479, a fully-human IGF1R targeted antibody. 99th AACR Annual Meeting 2008, abstract 3994
73. Moody G, Mitchell P, Cajulis E et al (2007) AMG 479, a fully human anti IGF-1 receptor monoclonal antibody, is efficacious against Ewing's sarcoma and osteosarcoma xenografts. AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics, 2007, abstract A64
74. Tolcher AW, Rothenberg ML, Rodon J, et al. A phase I pharmacokinetic and pharmacodynamic study of AMG 479, a fully human monoclonal antibody against insulin-like growth factor type 1 receptor (IGF-1R), in advanced solid tumors. J Clin Oncol2007 ASCO Annual Meeting Proceedings Part I. Vol 25, No. 18 S Suppl; abstr: 3002
75. J Sarantopoulos AC Mita M Mulay, et al. 2008 A phase IB study of AMG-479, a type 1 insulin-like growth factor receptor (IGF1R) anitbody, in combination with panitumumab (P) or gemcitabine (G) J Clin Oncol 26 15S 3583
76. A Phase 2 Study of AMG 479 in Relapsed or Refractory Ewing's Family Tumor and Desmoplastic Small Round Cell Tumors. http://clinicaltrials.gov/show/ NCT00563680. Accessed on 28 Sept 2009
77. Study of AMG 479 as Second Line Therapy in Patients With Recurrent Platinum-Sensitive Ovarian Cancer. http://clinicaltrials.gov/show/NCT00719212. Accessed on 28 Sept 2009
78. A Study of AMG 655 or AMG 479 in Combination With Gemcitabine for Treatment of Metastatic Pancreatic Cancer. http://clinicaltrials.gov/show/ NCT00630552. Accessed on 28 Sept 2009
79. Panitumumab Combination Study With AMG 102 or AMG 479 in Wild-Type KRAS mCRC. http://clinicaltrials.gov/show/NCT00788957. Accessed on 28 Sept 2009
80. A Phase 1b/2 Trial of AMG 479 or AMG 102 in Combination With Platinum-Based Chemotherapy as First-Line Treatment for Extensive Stage Small Cell Lung Cancer. http://clinicaltrials.gov/show/NCT00791154. Accessed on 28 Sept 2009
81. Phase 1b/2 Study of AMG 479 in Combination With Paclitaxel and Carboplatin for 1st Line Treatment of Advanced Squamous Non-Small Cell Lung Cancer. http://clinicaltrials.gov/show/NCT00807612. Accessed on 28 Sept 2009
82. AMG 655 in Combination With AMG 479 in Advanced, Refractory Solid Tumors. http://clinicaltrials.gov/show/NCT00819169. Accessed on 28 Sept 2009
83. Amgen Protocol No. 20060362 - A Study of AMG 479 With Exemestane or Fulvestrant in Postmenopausal Women With Hormone Receptor Positive Locally Advanced or Metastatic Breast Cancer. http://clinicaltrials.gov/show/ NCT00626106. Accessed on 28 Sept 2009
84. Phase 2 Safety & Efficacy of FOLFIRI in Combination With AMG 479 or AMG 655 vs FOLFIRI in KRAS-Mutant Metastatic Colorectal Carcinoma. http://clinicaltrials.gov/show/NCT00813605. Accessed on 28 Sept 2009
85. L Goetsch A Gonzalez O Leger, et al. 2005 Recombinant humanized anti-insulin-like growth factor receptor type I antibody (h7C10) enhances the antitumor activity of vinorelbine and anti-epidermal growth factor receptor therapy against human cancer xenografts Int J Cancer 113 316 328 10.1002/ijc.20543 1:CAS:528:DC%2BD2cXhtFajtb7P 15386423 (Pubitemid 39628325)
86. Atzori F, Tabernero J, Cervantes A et al (2008) A phase I, pharmacokinetic (PK) and pharmacodynamic (PD) study of weekly (qW) MK-0646, an insulin-like growth factor-1 receptor (IGF1R) monoclonal antibody (MAb) in patients (pts) with advanced solid tumors. J Clin Oncol 26(15S): abstract 3519
87. Hidalgo M, Tirado Gomez M, Lewis N et al (2008) A phase I study of MK-0646, a humanized monoclonal antibody against the insulin-like growth factor receptor type 1 (IGF1R) in advanced solid tumor patients in a q2 wk schedule. J Clin Oncol 26(15S): abstract 3520
88. A Study of MK0646 in Breast Cancer Patients. http://clinicaltrials.gov/ show/NCT00759785. Accessed on 28 Sept 2009
89. A Combination Study With MK8669 and MK0646 in Patients With Advanced Cancer. http://clinicaltrials.gov/show/NCT00730379. Accessed on 28 Sept 2009
90. MK-0646 Insulin Growth Factor 1 Receptor Antibody in Stage IIIb or IV Metastatic Non-Squamous Lung Cancer (IMPACT). http://clinicaltrials.gov/show/ NCT00799240. Accessed on 28 Sept 2009
91. Phase I Imaging Study Evaluating MK0646 in Combination With Erlotinib for Patients With Non-Small Cell Lung Cancer. http://clinicaltrials.gov/show/ NCT00729742. Accessed on 28 Sept 2009
92. MK-0646, Etoposide, and Cisplatin in Treating Patients With Extensive-Stage Small Cell Lung Cancer. http://clinicaltrials.gov/ct/show/ NCT00869752. Accessed on 28 Sept 2009
93. Clinical and Translational Study of MK-0646 in Patients With Metastatic Neuroendocrine Tumors (NET). http://clinicaltrials.gov/show/NCT00610129. Accessed on 28 Sept 2009
94. MK-0646 and Gemcitabine +/- Erlotinib for Patients With Advanced Pancreatic Cancer. http://clinicaltrials.gov/show/NCT00769483. Accessed on 28 Sept 2009
95. Study of MK0646 in Combination With Cetuximab and Irinotecan in Metastatic Colorectal Cancer. http://clinicaltrials.gov/show/NCT00614393. Accessed on 28 Sept 2009
96. J Rodon A Patnaik M Stein, et al. 2007 A phase I study of q3W R1507, a human monoclonal antibody IGF-1R antagonist in patients with advanced cancer J Clin Oncol 25 18S 3590
97. A Multiple Ascending Dose Study of R1507 in Children and Adolescents With Advanced Solid Tumors. http://clinicaltrials.gov/show/NCT00560144. Accessed on 28 Sept 2009
98. A Study of R1507 in Patients With Recurrent or Refractory Sarcoma. http://clinicaltrials.gov/show/NCT00642941. Accessed on 28 Sept2009
99. A Study of the Effect of R1507 in Combination With Tarceva (Erlotinib) on Progression-Free Survival in Patients With Stage IIIb/IV Non-Small Cell Lung Cancer (NSCLC). http://clinicaltrials.gov/show/NCT00760929. Accessed on 28 Sept 2009
100. A Study of the Effect of R1507 in Combination With Tarceva (Erlotinib) on Progression-Free Survival in Patients With Stage IIIb/IV Non-Small Cell Lung Cancer (NSCLC) Having Received Tarceva Monotherapy. http://clinicaltrials.gov/ show/NCT00773383. Accessed on 28 Sept 2009
101. A Study of R1507 in Combination With Letrozole in Postmenopausal Women With Advanced Breast Cancer. http://clinicaltrials.gov/show/NCT00796107. Accessed on 28 Sept 2009
102. A Study of R1507 in Combination With Multiple Standard Chemotherapy Treatments in Patients With Advanced Solid Tumors. http://clinicaltrials.gov/ show/NCT00811993. Accessed on 28 Sept 2009
103. EK Maloney JL McLaughlin NE Dagdigian, et al. 2003 An anti-insulin-like growth factor I receptor antibody that is a potent inhibitor of cancer cell proliferation Cancer Res 63 5073 5083 1:CAS:528:DC%2BD3sXms12nsbk%3D 12941837
104. NA Dallas L Xia F Fan, et al. 2009 Chemoresistant colorectal cancer cells, the cancer stem cell phenotype, and increased sensitivity to insulin-like growth factor-I receptor inhibition Cancer Res 69 5 1951 1957 10.1158/0008-5472.CAN-08-2023 1:CAS:528:DC%2BD1MXisFSrtb4%3D 19244128
105. G Descamps P Gomez-Bougie C Venot, et al. 2009 A humanised anti-IGF-1R monoclonal antibody (AVE1642) enhances Bortezomib-induced apoptosis in myeloma cells lacking CD45 Br J Cancer 100 2 366 369 10.1038/sj.bjc.6604839 1:CAS:528:DC%2BD1MXpsVSqtA%3D%3D 19165200
106. P Moreau C Hulin T Facon, et al. 2007 Phase I study of AVE1642 Anti IGF-1R monoclonal antibody in patients with multiple myeloma. ASH Annual Meeting Abstracts Blood 11 1166
107. Tolcher AW, Patnaik A, Till E et al (2008) A phase I study of AVE1642, a humanized monoclonal antibody IGF-1R (Insulin like growth factor 1 receptor) antagonist, in patients (pts) with advanced solid tumor (ST). J Clin Oncol 26(15 S): abstract 3582
108. Dose Finding Study of AVE1642 in Patients With Advanced or Metastatic Liver Carcinoma. http://clinicaltrials.gov/show/NCT00791544. Accessed on 28 Sept 2008
109. EA Kolb R Gorlick PJ Houghton, et al. 2008 Initial testing (stage 1) of a monoclonal antibody (SCH 717454) against the IGF-1 receptor by the pediatric preclinical testing program Pediatr Blood Cancer 50 6 1190 1197 10.1002/pbc.21450 18260118 (Pubitemid 351555543)
110. Seraj J, Tsai M, Seiberling M et al (2007) Evaluation of safety and pharmacokinetics of a fully human IGF-1 receptor antibody, SCH 717454, in healthy volunteers. AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics 2007, Abstract A72
111. A Study to Determine the Activity of SCH 717454 in Subjects With Relapsed Osteosarcoma or Ewing's Sarcoma (Study P04720). http://clinicaltrials.gov/show/ NCT00617890. Accessed on 28 September 2008
112. A Study to Determine the Activity of SCH 717454 in Subjects With Relapsed or Recurrent Colorectal Cancer (Study P04721AM1). http://clinicaltrials.gov/ show/NCT00551213. Accessed on 28 September 2008
113. Hariharan K, Dong J; Demarest S et al (2007) BIIB022, a fully human nonglycosylated γ4P antibody targeting IGF-1R for cancer therapy. AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, 2007, abstract B210
114. Dong J, Tamraz S, Berquist L et al (2008) BIIB022, a human antibody targeting human insulin-like growth factor-1 receptor (IGF-1R), enhances the antitumor activities of Tarceva in non small cell lung carcinoma (NSCLC) and Rapamycin in sarcoma cell lines. Proceedings of the 99th Annual Meeting of the American Association for Cancer Research; 2008. Abstr. 4002.
115. ++ Leukemias with Either Failure to Multiple TKI Therapies or with T315I Mutation ASH Annual Meeting Abstracts Blood 112 3232
116. Smith DC, C. Britten C, Clary DO et al (2009) A phase I study of XL228, a potent IGF1R/AURORA/SRC inhibitor, in patients with solid tumors or hematologic malignancies. J Clin Oncol 27(15S): abstract 3512
117. Harzstark AL, Ryan C, Diamond M et al (2007) A phase I trial of nordihydroguareacetic acid (NDGA) in patients with non-metastatic prostate cancer and rising PSA. J Clin Oncol 25(18S) abstract 15500
118. Pharmacokinetic and Efficacy Study of Nordihydroguaiaretic Acid (NDGA) in Non Metastatic Recurrent Prostate Cancer. http://clinicaltrials.gov/show/ NCT00678015. Accessed on 28 Sept 2008
119. H Werner M Woloschak M Adamo, et al. 1989 Developmental regulation of the rat insulin-like growth factor I receptor gene Proc Natl Acad Sci U S A 86 19 7451 7455 10.1073/pnas.86.19.7451 1:CAS:528:DyaL1MXmtFSjsrs%3D 2477843 (Pubitemid 19254474)
120. S Benyoucef KH Surinya D Hadaschik K Siddle 2007 Characterization of insulin/IGF hybrid receptors: contributions of the insulin receptor L2 and Fn1 domains and the alternatively spliced exon 11sequence to ligand binding and receptor activation Biochem J 403 603 613 10.1042/BJ20061709 1:CAS:528:DC%2BD2sXltVejsb8%3D 17291192 (Pubitemid 46706989)
121. R Lammers A Gray J Schlessinger A Ullrich 1989 Differential signalling potential of insulin- and IGF-1-receptor cytoplasmic domains EMBO J 8 1369 1375 1:CAS:528:DyaL1MXktFyjtbw%3D 2548842
122. A Belfiore 2007 The role of insulin receptor isoforms and hybrid insulin/IGF-I receptors in human cancer Curr Pharm Des 13 671 686 10.2174/138161207780249173 1:CAS:528:DC%2BD2sXlsVagtr8%3D 17346183 (Pubitemid 46510744)
123. Gualberto A, Pollak M (2009) Clinical Development of Inhibitors of the Insulin-like Growth Factor Receptor in Oncology. Curr Drug Targets. Oct 1 epublication
124. A Gualberto DD Karp 2009 Development of the monoclonal antibody figitumumab, targeting the insulin-like growth factor-1 receptor, for the treatment of patients with non-small-cell lung cancer Clin Lung Cancer 10 4 273 280 10.3816/CLC.2009.n.038 1:CAS:528:DC%2BD1MXhtVSms7nF 19632947
125. Olmos D, Molife R, Okuno S, Worden F, Hammer G, Yap T et al (2007) Safety, tolerability and preliminary efficacy of the anti-IGFIR monoclonal antibody CP-751,871 in patients with sarcomas and adrenocortical tumors. Presented at the AACR-NCI-EORTC Molecular Targets and Cancer Therapeutics Meeting, San Francisco, USA, 22-26, October 2007
126. D Cunningham Y Humblet S Siena, et al. 2004 Cetuximab monotherapy and cetuximab plus irinotecan in irinotecan-refractory metastatic colorectal cancer N Engl J Med 351 4 337 345 10.1056/NEJMoa033025 1:CAS:528:DC%2BD2cXlvFGitbk%3D 15269313 (Pubitemid 38944402)
127. S Thomson E Buck F Petti, et al. 2005 Epithelial to mesenchymal transition is a determinant of sensitivity of non-small-cell lung carcinoma cell lines and xenografts to epidermal growth factor receptor inhibition Cancer Res 65 9455 9462 10.1158/0008-5472.CAN-05-1058 1:CAS:528:DC%2BD2MXhtFWmu73E 16230409 (Pubitemid 41508014)
128. G Pandini T Wurch B Akla, et al. 2007 Functional responses and in vivo anti-tumour activity of h7C10: a humanised monoclonal antibody with neutralising activity against the insulin-like growth factor-1 (IGF-1) receptor and insulin/IGF-1 hybrid receptors Eur J Cancer 43 1318 1327 10.1016/j.ejca.2007.03. 009 1:CAS:528:DC%2BD2sXlt1ahtr0%3D 17451939 (Pubitemid 46720250)
129. FHW Huang R Hafezi X Han, et al. 2007 Identification of sensitivity markers for BMS-536924, an inhibitor for insulin-like growth factor-1 receptor. ASCO Ann Meet Proc 2007 J Clin Oncol 25 3506
130. MNLM Pollak A Lipton L Demers 2007 Pharmacodynamic properties of the anti-IGF-IR monoclonal antibody CP-751,871 in cancer patients. ASCO Ann Meet Proc 2007 J Clin Oncol 25 3587 10.1200/JCO.2007.12.4180
131. K Scotlandi 2006 Targeted therapies in Ewing's sarcoma Adv Exp Med Biol 587 13 22 1:CAS:528:DC%2BD1MXhsV2lu7g%3D 17163152
132. Ji QS, Mulvihill M, Franklin M et al (2007) Properties of small molecule IGF-IR kinase inhibitors in preclinical models. AACR Annual Meeting 2007, Los Angeles (CA): abstract 30.9