BMS-754807, a small-molecule inhibitor of insulin-like growth factor-1 receptor/insulin receptor, enhances gemcitabine response in pancreatic cancer

Molecular Cancer Therapeutics

Volumn 11, Issue 12, 2012, Pages 2644-2653

  Awasthi, Niranjan ^a,b   Zhang, Changhua ^a,b   Ruan, Winston ^a,b   Schwarz, Margaret A ^b   Schwarz, Roderich E ^a,b  

^a UNIVERSITY OF TEXAS SOUTHWESTERN MEDICAL CENTER   (United States)

^b UNIVERSITY OF TEXAS SOUTHWESTERN MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

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; CASPASE 3; GEMCITABINE; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE 1; PROTEIN KINASE B; SOMATOMEDIN C RECEPTOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; APOPTOSIS; ARTICLE; CANCER GROWTH; CANCER INHIBITION; CANCER SURVIVAL; CELL PROLIFERATION; CHEMOSENSITIZATION; CONTROLLED STUDY; DRUG EFFICACY; DRUG POTENTIATION; FEMALE; HUMAN; HUMAN CELL; IC 50; IMMUNOBLOTTING; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; PANCREAS ADENOCARCINOMA; PRIORITY JOURNAL; PROTEIN CLEAVAGE; PROTEIN EXPRESSION; SURVIVAL TIME;

ANIMALS; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; APOPTOSIS; CARCINOMA, PANCREATIC DUCTAL; CELL GROWTH PROCESSES; CELL LINE, TUMOR; DEOXYCYTIDINE; DRUG SYNERGISM; FEMALE; HUMANS; IMMUNOHISTOCHEMISTRY; MICE; MICE, NUDE; MICE, SCID; PANCREATIC NEOPLASMS; PYRAZOLES; RANDOM ALLOCATION; RECEPTOR, IGF TYPE 1; SIGNAL TRANSDUCTION; TRIAZINES; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84871368849     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-12-0447     Document Type: Article

References (50)

1. Jemal A, Siegel R, Xu J, Ward E. Cancer statistics, 2010. CA Cancer J Clin 2010;60:277-300.
2. Burris HA III, Moore MJ, Andersen J, Green MR, Rothenberg ML, Modiano MR, et al. Improvements in survival and clinical bene fit with gemcitabine as first-line therapy for patients with advanced pancreas cancer: a randomized trial. J Clin Oncol 1997;15:2403-13. (Pubitemid 27251144)
3. Saif MW. Pancreatic cancer: highlights from the 42nd annual meeting of the American Society of Clinical Oncology, 2006. JOP 2006;7: 337-48. (Pubitemid 44083105)
4. Reni M, Cordio S, Milandri C, Passoni P, Bonetto E, Oliani C, et al. Gemcitabine versus cisplatin, epirubicin, fluorouracil, and gemcitabine in advanced pancreatic cancer: a randomised controlled multicentre phase III trial. Lancet Oncol 2005;6:369-76. (Pubitemid 40753742)
5. Ozawa F, Friess H, Tempia-Caliera A, Kleeff J, Buchler MW. Growth factors and their receptors in pancreatic cancer. Teratog Carcinog Mutagen 2001;21:27-44.
6. Bergmann U, Funatomi H, Yokoyama M, Beger HG, Korc M. Insulinlike growth factor I overexpression in human pancreatic cancer: evidence for autocrine and paracrine roles. Cancer Res 1995;55: 2007-11.
7. Samani AA, Yakar S, LeRoith D, Brodt P. The role of the IGF system in cancer growth and metastasis: overview and recent insights. Endocr Rev 2007;28:20-47. (Pubitemid 46220849)
8. Resnik JL, Reichart DB, Huey K, Webster NJ, Seely BL. Elevated insulin-like growth factor I receptor autophosphorylation and kinase activity in human breast cancer. Cancer Res 1998;58:1159-64. (Pubitemid 28183203)
9. Pollak MN, Schernhammer ES, Hankinson SE. Insulin-like growth factors and neoplasia. Nat Rev Cancer 2004;4:505 -18.
10. Baserga R, Peruzzi F, Reiss K. The IGF-1 receptor in cancer biology. Int J Cancer 2003;107:873- 7.
11. Baserga R. The insulin-like growth factor-I receptor as a target for cancer therapy. Expert Opin Ther Targets 2005;9:753-68. (Pubitemid 41131677)
12. Osborne CK, Bolan G, Monaco ME, Lippman ME. Hormone responsive human breast cancer in long-term tissue culture: effect of insulin. Proc Natl Acad Sci U S A 1976;73:4536-40. (Pubitemid 8013935)
13. Kido Y, Nakae J, Accili D. Clinical review 125: the insulin receptor and its cellular targets. J Clin Endocrinol Metab 2001;86:972-9. (Pubitemid 32322967)
14. Frasca F, Pandini G, Scalia P, Sciacca L, Mineo R, Costantino A, et al. Insulin receptor isoform A, a newly recognized, high-affi nity insulin-like growth factor II receptor in fetal and cancer cells. Mol Cell Biol 1999;19:3278-88. (Pubitemid 29193789)
15. Pandini G, Vigneri R, Costantino A, Frasca F, Ippolito A, Fujita-Yamaguchi Y, et al. Insulin and insulin-like growth factor-I (IGF-I) receptor overexpression in breast cancers leads to insulin/IGF-I hybrid receptor overexpression: evidence for a second mechanism of IGF-I signaling. Clin Cancer Res 1999;5:1935-44. (Pubitemid 29334478)
16. Pandini G, Frasca F, Mineo R, Sciacca L, Vigneri R, Belfiore A. Insulin/ insulin-like growth factor I hybrid receptors have different biological characteristics depending on the insulin receptor isoform involved. J Biol Chem 2002;277:39684-95. (Pubitemid 35190951)
17. Beltran PJ, Mitchell P, Chung YA, Cajulis E, Lu J, Belmontes B, et al. 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 2009;8:1095-105.
18. Ii M, Li H, Adachi Y, Yamamoto H, Ohashi H, Taniguchi H, et al. The efficacy of IGF-I receptor monoclonal antibody against human gastrointestinal carcinomas is independent of k-ras mutation status. Clin Cancer Res 2011;17:5048-59.
19. Haluska P, Shaw HM, Batzel GN, Yin D, Molina JR, Molife LR, et al. 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 2007;13:5834-40. (Pubitemid 47583908)
20. Munshi S, Hall DL, Kornienko M, Darke PL, Kuo LC. Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 A resolution. Acta Crystallogr D Biol Crystallogr 2003;59:1725-30. (Pubitemid 37245124)
21. Carboni JM, Wittman M, Yang Z, Lee F, Greer A, Hurlburt W, et al.BMS- 754807, a small molecule inhibitor of insulin-like growth factor-1R/IR. Mol Cancer Ther 2009;8:3341-9.
22. Huang F, Hurlburt W, Greer A, Reeves KA, Hillerman S, Chang H, et al. Differential mechanisms of acquired resistance to insulin-like growth factor-i receptor antibody therapy or to a small-molecule inhibitor, BMS-754807, in a human rhabdomyosarcoma model. Cancer Res 2010;70:7221-31.
23. Kolb EA, Gorlick R, Lock R, Carol H, Morton CL, Keir ST, et al. Initial testing (stage 1) of the IGF-1 receptor inhibitor BMS-754807 by the pediatric preclinical testing program. Pediatr Blood Cancer 2011; 56:595-603.
24. Awasthi N, Schwarz MA, Verma V, Cappiello C, Schwarz RE. Endothelial monocyte activating polypeptide II interferes with VEGFinduced proangiogenic signaling. Lab Invest 2009;89:38-46.
25. Schwarz RE, Schwarz MA. In vivo therapy of local tumor progression by targeting vascular endothelium with EMAP-II. J Surg Res 2004; 120:64-72. (Pubitemid 38686531)
26. Schwarz RE, McCarty TM, Peralta EA, Diamond DJ, Ellenhorn JD. An orthotopic in vivo model of human pancreatic cancer. Surgery 1999;126:562-7. (Pubitemid 29421045)
27. Awasthi N, Yen PL, Schwarz MA, Schwarz RE. The efficacy of a novel, dual PI3K/mTOR inhibitor NVP-BEZ235 to enhance chemotherapy and antiangiogenic response in pancreatic cancer. J Cell Biochem 2012;113:784-91.
28. Awasthi N, Kirane A, Schwarz MA, Toombs JE, Brekken RA, Schwarz RE. Smac mimetic-derived augmentation of chemotherapeutic response in experimental pancreatic cancer.BMCCancer 2011;11:15.
29. RochaLima CM, Green MR, Rotche R, Miller WH Jr, Jeffrey GM, Cisar LA, et al. Irinotecan plus gemcitabine results in no survival advantage compared with gemcitabine monotherapy in patients with locally advanced or metastatic pancreatic cancer despite increased tumor response rate. J Clin Oncol 2004;22:3776-83.
30. Louvet C, Labianca R, Hammel P, Lledo G, Zampino MG, Andre T, et al. Gemcitabine in combination with oxaliplatin compared with gemcitabine alone in locally advanced or metastatic pancreatic cancer: results of a GERCOR and GISCAD phase III trial. J Clin Oncol 2005;23: 3509- 16.
31. Moore MJ, Goldstein D, Hamm J, Figer A, Hecht JR, Gallinger S, et al. Erlotinib plus gemcitabine compared with gemcitabine alone in patients with advanced pancreatic cancer: a phase III trial of the National Cancer Institute of Canada Clinical Trials Group. J Clin Oncol 2007;25:1960-6. (Pubitemid 46972777)
32. Baserga R. Targeting the IGF-1 receptor: from rags to riches. Eur J Cancer 2004;40:2013-5. (Pubitemid 39165531)
33. Bohula EA, Playford MP, Macaulay VM. Targeting the type 1 insulin-like growth factor receptor as anti-cancer treatment. Anticancer Drugs 2003;14:669-82. (Pubitemid 37357691)
34. Liu JP, Baker J, Perkins AS, Robertson EJ, Efstratiadis A. Mice carrying null mutations of the genes encoding insulin-like growth factor I (Igf-1) and type 1 IGF receptor (Igf1r). Cell 1993;75:59-72. (Pubitemid 23306021)
35. Baserga R, Hongo A, Rubini M, Prisco M, Valentinis B. The IGF-I receptor in cell growth, transformation and apoptosis. Biochim Biophys Acta 1997;1332:F105-26. (Pubitemid 27272620)
36. Tricoli JV, Rall LB, Karakousis CP, Herrera L, Petrelli NJ, Bell GI, et al. Enhanced levels of insulin-like growth factor messenger RNA in human colon carcinomas and liposarcomas. Cancer Res 1986;46:6169-73. (Pubitemid 17221751)
37. Sachdev D, Yee D. Disrupting insulin-like growth factor signaling as a potential cancer therapy. Mol Cancer Ther 2007;6:1-12. (Pubitemid 46206663)
38. Weroha SJ, Haluska P. IGF-1 receptor inhibitors in clinical trials -early lessons. J Mammary Gland Biol Neoplasia 2008;13:471-83.
39. Morgillo F, Kim WY, Kim ES, Ciardiello F, Hong WK, Lee HY. Implication of the insulin-like growth factor-IR pathway in the resistance of non -small cell lung cancer cells to treatment with gefitinib. Clin Cancer Res 2007;13:2795-803. (Pubitemid 46788049)
40. Martins AS, Mackintosh C, Martin DH, Campos M, Hernandez T, Ordonez JL, et al. 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 2006;12:3532-40.
41. Min Y, Adachi Y, Yamamoto H, Ito H, Itoh F, Lee CT, et al. Genetic blockade of the insulin-like growth factor-I receptor: a promising strategy for human pancreatic cancer. Cancer Res 2003;63:6432-41. (Pubitemid 37255193)
42. Haluska P, Carboni JM, Loegering DA, Lee FY, Wittman M, Saulnier MG, et al. In vitro and in vivo antitumor effects of the dual insulin-like growth factor-I/insulin receptor inhibitor, BMS-554417. Cancer Res 2006;66:362-71. (Pubitemid 43166043)
43. Tolcher AW, Mita M, Meropol NJ, von Mehren M, Patnaik A, Padavic K, et al. Phase I pharmacokinetic and biologic correlative study of mapatumumab, a fully human monoclonal antibody with agonist activity to tumor necrosis factor-related apoptosis-inducing ligand receptor-1. J Clin Oncol 2007;25:1390-5. (Pubitemid 46706887)
44. Gualberto A, Pollak M. Emerging role of insulin-like growth factor receptor inhibitors in oncology: early clinical trial results and future directions. Oncogene 2009;28:3009-21.
45. Garofalo RS, Orena SJ, Rafidi K, Torchia AJ, Stock JL, Hildebrandt AL, et al. Severe diabetes, age-dependent loss of adipose tissue, and mild growth deficiency in mice lacking Akt2/PKB beta. J Clin Invest 2003;112:197-208. (Pubitemid 38056356)
46. Sciacca L, Costantino A, Pandini G, Mineo R, Frasca F, Scalia P, et al. Insulin receptor activation by IGF-II in breast cancers: evidence for a new autocrine/paracrine mechanism. Oncogene 1999;18:2471-9. (Pubitemid 29206160)
47. Schwarz RE, Awasthi N, Konduri S, Cafasso D, Schwarz MA. EMAP IIbased antiangiogenic-antiendothelial in vivo combination therapy of pancreatic cancer. Ann Surg Oncol 2010;17:1442-52.
48. Awasthi N, Schwarz MA, Schwarz RE. Combination effects of bortezomib with gemcitabine and EMAP II in experimental pancreatic cancer. Cancer Biol Ther 2010;10:99-107.
49. Awasthi N, Schwarz MA, Schwarz RE. Antitumour activity of sunitinib in combination with gemcitabine in experimental pancreatic cancer.HPB (Oxford) 2011;13:597-604.
50. Von Hoff DD, Ramanathan RK, Borad MJ, Laheru DA, Smith LS, Wood TE, et al. Gemcitabine plus nab-paclitaxel is an active regimen in patients with advanced pancreatic cancer: a phase I/II trial. J Clin Oncol 2011;29:4548-54.