Emerging role of insulin-like growth factor receptor inhibitors in oncology: early clinical trial results and future directions (original) (raw)

References

• Adelaide J, Finetti P, Bekhouche I, Repellini L, Geneix J, Sircoulomb F et al. (2007). Integrated profiling of basal and luminal breast cancers. Cancer Res 67: 11565–11575.
  Article CAS PubMed Google Scholar
• Ahlgren M, Melbye M, Wohlfahrt J, Sorensen TI . (2004). Growth patterns and the risk of breast cancer in women. N Engl J Med 351: 1619–1626.
  CAS PubMed Google Scholar
• Allen GW, Saba C, Armstrong EA, Huang SM, Benavente S, Ludwig DL et al. (2007). Insulin-like growth factor-I receptor signaling blockade combined with radiation. Cancer Res 67: 1155–1162.
  CAS PubMed Google Scholar
• Arteaga CL, Kitten LJ, Coronado EB, Jacobs S, Kull Jr FC, Allred DC et al. (1989). Blockade of the type I somatomedin receptor inhibits growth of human breast cancer cells in athymic mice. J Clin Invest 84: 1418–1423.
  CAS PubMed PubMed Central Google Scholar
• Attard G, Fong PC, Molife R, Reade S, Shaw H, Reid A et al. (2006). Phase I trial involving the pharmacodynamic (PD) study of circulating tumour cells, of CP-751,871 (C), a monoclonal antibody against the insulin-like growth factor 1 receptor (IGF-1R), with docetaxel (D) in patients (p) with advanced cancer. J Clin Oncol 24: 126s.
  Google Scholar
• Atzori F, Tabernero J, Cervantes A, Botero M, Hsu K, Brown H 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: 157s.
  Google Scholar
• Barr S, Buck E, Thomson S, Haley J, Gibson N, Ji Q et al. (2007). The combination of small molecule inhibitors of EGFR and IGF-1R is synergistic in HNSCC and ovarian cancer cell lines. Proc Am Assoc Cancer Res 48: 608.
  Google Scholar
• Baserga R, Peruzzi F, Reiss K . (2003). The IGF-1 receptor in cancer biology. Int J Cancer 107: 873–877.
  CAS PubMed Google Scholar
• Belfiore A . (2007). The role of insulin receptor isoforms and hybrid insulin/IGF-I receptors in human cancer. Curr Pharm Des 13: 671–686.
  CAS PubMed Google Scholar
• Benini S, Manara MC, Baldini N, Cerisano V, Massimo S, Mercuri M et al. (2001). Inhibition of insulin-like growth factor I receptor increases the antitumor activity of doxorubicin and vincristine against Ewing's sarcoma cells. Clin Cancer Res 7: 1790–1797.
  CAS PubMed Google Scholar
• Benyoucef S, Surinya KH, Hadaschik D, Siddle K . (2007). Characterization of insulin/IGF hybrid receptors: contributions of the insulin receptor L2 and Fn1 domains and the alternatively spliced exon 11 sequence to ligand binding and receptor activation. Biochem J 403: 603–613.
  CAS PubMed PubMed Central Google Scholar
• Best CJ, Ludwig DL, Steeg PS . (2006). Breast cancer cell lines resistant to either tamoxifen or Herceptin exhibit sensitivity to the anti-IGF receptor antibody A12 in vitro. Proc Am Assoc Cancer Res 47: 290.
  Google Scholar
• Britten C, Smith D, Bui L, Clary D, Hurwitz H . (2008). A phase I dose de-escalation study of XL228, a potent IGFIR/src inhibitor in patients with advanced malignancies. Presented at the 20th EORTC-NCI-AACR symposium on Molecular Targets and Cancer Therapeutics Congress, 21–24 October 2008, Geneva, Switzerland.
• Buck E, Eyzaguirre A, Rosenfeld-Franklin M, Thomson S, Mulvihill M, Barr S et al. (2008). Feedback mechanisms promote cooperativity for small molecule inhibitors of epidermal and insulin-like growth factor receptors. Cancer Res 68: 8322–8332.
  CAS PubMed Google Scholar
• Cao L, Yu Y, Darko I, Currier D, Mayeenuddin LH, Wan X et al. (2008). Addiction to elevated insulin-like growth factor I receptor and initial modulation of the AKT pathway define the responsiveness of rhabdomyosarcoma to the targeting antibody. Cancer Res 68: 8039–8048.
  CAS PubMed PubMed Central Google Scholar
• Ceda GP, Dall’Aglio E, Maggio M, Lauretani F, Bandinelli S, Falzoi C et al. (2005). Clinical implications of the reduced activity of the GH-IGF-I axis in older men. J Endocrinol Invest. 28 (11 Suppl): 96–100.
  CAS PubMed Google Scholar
• Chan JM, Stampfer MJ, Giovannucci E, Gann PH, Ma J, Wilkinson P et al. (1998). Plasma insulin-like growth factor-I and prostate cancer risk: a prospective study. Science 279: 563–566.
  CAS PubMed Google Scholar
• Chitnis MM, Yuen JS, Protheroe AS, Pollak M, Macaulay VM . (2008). The type 1 insulin-like growth factor receptor pathway. Clin Cancer Res 14: 6364–6370.
  CAS PubMed Google Scholar
• Cohen BD, Baker DA, Soderstrom C, Tkalcevic G, Rossi AM, Miller PE 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: 2063–2073.
  CAS PubMed Google Scholar
• Cortes J, Paquette R, Talpaz M, Pinilla J, Asatiani E, Wetzler M et al. (2008). Preliminary clinical activity in a phase I trial of the BCR-ABL/IGF-1R/aurora kinase inhibitor XL228 in patients with Ph+ leukemias with either failure to multiple TKI therapies or with T315I mutation. Presented at the 50th ASH Annual Meeting and Exposition, San Francisco, USA, 6–9 December 2008, http://ash.confex.com/ash/2008/webprogram/Paper13204.html.
• Cox ME, Gleave ME, Zakikhani M, Bell RH, Piura E, Vickers E et al. (2009). Insulin receptor expression by human prostate cancers. Prostate 69: 33–40.
  CAS PubMed Google Scholar
• De Bono JS, Attard G, Adjei A, Pollak MN, Fong PC, Haluska P et al. (2007). Potential applications for circulating tumor cells expressing the insulin-like growth factor-I receptor. Clin Cancer Res 13: 3611–3616.
  CAS PubMed Google Scholar
• De Bono JS, Attard G, Adjei A, Pollak MN, Fong PC, Haluska P et al. (2008). Activity of the anti-IGF-IR antibody CP-751,871 in combination with docetaxel as first-line treatment for castration-resistant prostate cancer in a randomized phase II trial. Presented at the Molecular Targets and Cancer Therapeutics Congress, 21–24 October 2008, Geneva, Switzerland.
• del Rincon JP, Iida K, Gaylinn BD, McCurdy CE, Leitner JW, Barbour LA et al. (2007). Growth hormone regulation of p85alpha expression and phosphoinositide 3-kinase activity in adipose tissue: mechanism for growth hormone-mediated insulin resistance. Diabetes 56: 1638–1646.
  CAS PubMed Google Scholar
• Diorio C, Pollak M, Byrne C, Masse B, Hebert-Croteau N, Yaffe M et al. (2005). Insulin-like growth factor-I, IGF-binding protein-3, and mammographic breast density. Cancer Epidemiol Biomarkers Prev 14: 1065–1073.
  CAS PubMed Google Scholar
• Dong MQ, Venable JD, Au N, Xu T, Park SK, Cociorva D et al. (2007). Quantitative mass spectrometry identifies insulin signaling targets in C. elegans. Science 317: 660–663.
  CAS PubMed Google Scholar
• Feng Y, Dimitrov DS . (2008). Monoclonal antibodies against components of the IGF system for cancer treatment. Curr Opin Drug Discov Devel 11: 178–185.
  CAS PubMed Google Scholar
• Gebre-Medhin M, Kindblom LG, Wennbo H, Tornell J, Meis-Kindblom JM . (2001). Growth hormone receptor is expressed in human breast cancer. Am J Pathol 158: 1217–1222.
  CAS PubMed PubMed Central Google Scholar
• Girnita A, Girnita L, del PF, Bartolazzi A, Larsson O, Axelson M . (2004). Cyclolignans as inhibitors of the insulin-like growth factor-1 receptor and malignant cell growth. Cancer Res 64: 236–242.
  CAS PubMed Google Scholar
• Glait C, Tencer L, Ravid D, Sarfstein R, Liscovitch M, Werner H . (2006). Caveolin-1 up-regulates IGF-I receptor gene transcription in breast cancer cells via Sp1- and p53-dependent pathways. Exp Cell Res 312: 3899–3908.
  CAS PubMed Google Scholar
• Goodin S. (2008). Development of monoclonal antibodies for the treatment of colorectal cancer. Am J Health Syst Pharm 65: S3–S7.
  CAS PubMed Google Scholar
• Goodwin PJ, Ennis M, Pritchard KI, Trudeau ME, Koo J, Madarnas Y et al. (2002). Fasting insulin and outcome in early-stage breast cancer: results of a prospective cohort study. J Clin Oncol 20: 42–51.
  CAS PubMed Google Scholar
• Gualberto A, Karp DD . (2008). Development of a monoclonal antibody against the IGF-IR for the treatment of non small cell lung cancer (CP-751,871). Clin Lung Cancer June 2009 (in press).
• Gualberto A, Melvin CL, Dean A, Ang AL, Reynolds JM, Lee AV et al. (2008a). Characterization of NSCLC patients responding to anti-IGF-IR therapy. J Clin Oncol 26: 424s.
  Google Scholar
• Gualberto A, Melvin CL, Dean A, Ang AL, Reynolds JM, Lee AV et al. (2008b). IGF-IR markers in NSCLC patients on anti-IGF-IR therapy. Ann Oncol 19: viii62.
  Google Scholar
• Guix M, Faber AC, Wang SE, Olivares MG, Song Y, Qu S et al. (2008). Acquired resistance to EGFR tyrosine kinase inhibitors in cancer cells is mediated by loss of IGF-binding proteins. J Clin Invest 118: 2609–2619.
  CAS PubMed PubMed Central Google Scholar
• Haluska P, Shaw HM, Batzel GN, Yin D, Molina JR, Molife LR 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: 5834–5840.
  CAS PubMed Google Scholar
• Hartog H, Wesseling J, Boezen HM, van der Graaf WT . (2007). The insulin-like growth factor 1 receptor in cancer: old focus, new future. Eur J Cancer 43: 1895–1904.
  CAS PubMed Google Scholar
• Hidalgo M, Tirado Gomez M, Lewis N, Vuky JL, Taylor G, Hayburn JL 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: 158s.
  Google Scholar
• Higano CS, Yu EY, Whiting SH, Gordon MS, Lorusso P, Fox F 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. Presented at the 2007 Prostate Cancer Symposium, Orlando, USA, 22–24 February, 2007 (Abstract 269) http://www.asco.org/ASCO/Abstracts+%26+Virtual+Meeting/Abstracts?&vmview=abst_detail_view&confID=46&abstractID=20331.
• Hochberg Z . (2002). Mechanisms of steroid impairment of growth. Horm Res 58 (Suppl 1): 33–38.
  CAS PubMed Google Scholar
• Huang F, Greer A, Hurlburt W, Han X, Hafezi R, Wittenberg GM et al. (2009). 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: 161–170.
  CAS PubMed PubMed Central Google Scholar
• Hyun T, Yam A, Pece S, Xie X, Zhang J, Miki T et al. (2000). Loss of PTEN expression leading to high Akt activation in human multiple myelomas. Blood. 96: 3560–3568.
  CAS PubMed Google Scholar
• Ji QS, Mulvihill MJ, Rosenfeld-Franklin M, Cooke A, Feng L, Mak G et al. (2007). A novel, potent, and selective insulin-like growth factor-I receptor kinase inhibitor blocks insulin-like growth factor-I receptor signaling in vitro and inhibits insulin-like growth factor-I receptor dependent tumor growth in vivo. Mol Cancer Ther 6: 2158–2167.
  CAS PubMed Google Scholar
• Karp DD, Paz-Ares LG, Novello S, Haluska P, Garland L, Cardenal F et al. (2009). Phase II study of the efficacy of the anti-insulin-like growth factor type 1 receptor antibody CP-751,871 in combination with paclitaxel and carboplatin in previously untreated, locally advanced, or metastatic non-small cell lung cancer. J Clin Oncol 27: 2516–2522.
  CAS PubMed Google Scholar
• Klinakis A, Szabolcs M, Chen G, Xuan S, Hibshoosh H, Efstratiadis A . (2009). Igf1r as a therapeutic target in a mouse model of basal-like breast cancer. Proc Natl Acad Sci USA 106: 2359–2364.
  CAS PubMed PubMed Central Google Scholar
• Kopchick JJ, Parkinson C, Stevens EC, Trainer PJ . (2002). Growth hormone receptor antagonists: discovery, development, and use in patients with acromegaly. Endocr Rev 23: 623–646.
  CAS PubMed Google Scholar
• Lacy MQ, Alsina M, Fonseca R, Paccagnella ML, Melvin CL, Yin D 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: 3196–3203.
  CAS PubMed Google Scholar
• Lammers R, Gray A, Schlessinger J, Ullrich A . (1989). Differential signalling potential of insulin- and IGF-1-receptor cytoplasmic domains. EMBO J. 8: 1369–1375.
  CAS PubMed PubMed Central Google Scholar
• Law JH, Habibi G, Hu K, Masoudi H, Wang MY, Stratford AL et al. (2008). Phosphorylated insulin-like growth factor-i/insulin receptor is present in all breast cancer subtypes and is related to poor survival. Cancer Res 68: 10238–10246.
  CAS PubMed Google Scholar
• Leong S, Gore L, Benjamin R, Warren TL, Eckhardt SG, Camidge DR et al. (2007). A phase I study of R1507, a human monoclonal antibody IGF-1R (insulin-like growth factor receptor) antagonist given weekly inpatients with advanced solid tumors. Presented at the AACR-NCI-EORTC Molecular Targets and Cancer Therapeutics Meeting, San Francisco, USA, 22–26 October 2007, http://www.aacr.org/Uploads/DocumentRepository/2007conf/moltar/mt07_postera.pdf.
• Lindsay CR, Chan E, Evans TR, Campbell S, Bell P, Stephens AW et al. (2009). Phase I dose escalation study of continuous oral dosing of OSI-906, an insulin like growth factor-1 receptor (IGF-1R) tyrosine kinase inhibitor, in patients with advanced solid tumors. J Clin Oncol 27: 15s (suppl; abstr 2559).
  Google Scholar
• Lu Y, Zi X, Zhao Y, Mascarenhas D, Pollak M. (2001). Insulin-like growth factor-I receptor signaling and resistance to trastuzumab (Herceptin). J Natl Cancer Inst 93: 1852–1857.
  CAS PubMed Google Scholar
• Ma J, Li H, Giovannucci E, Mucci L, Qiu W, Nguyen PL et al. (2008). Prediagnostic body-mass index, plasma C-peptide concentration, and prostate cancer-specific mortality in men with prostate cancer: a long-term survival analysis. Lancet Oncol 9: 1039–1047.
  CAS PubMed PubMed Central Google Scholar
• Majeed N, Blouin MJ, Kaplan-Lefko PJ, Barry-Shaw J, Greenberg NM, Gaudreau P et al. (2005). A germ line mutation that delays prostate cancer progression and prolongs survival in a murine prostate cancer model. Oncogene 24: 4736–4740.
  CAS PubMed Google Scholar
• Martin MJ, Melnyk N, Pollard M, Bowden M, Leong H, Podor TJ et al. (2006). The insulin-like growth factor I receptor is required for Akt activation and suppression of anoikis in cells transformed by the ETV6-NTRK3 chimeric tyrosine kinase. Mol Cell Biol 26: 1754–1769.
  CAS PubMed PubMed Central Google Scholar
• Mendelsohn J, Baselga J . (2006). Epidermal growth factor receptor targeting in cancer. Semin Oncol 33: 369–385.
  CAS PubMed Google Scholar
• Moreau P, Hulin C, Facon T, Boccadoro M, Mery-Mignard D, Deslandes A et al. (2007). Phase I study of AVE1642 anti IGF-1R monoclonal antibody in patients with advanced multiple myeloma. Blood. ASH Annual Meeting Abstracts, http://abstracts.hematologylibrary.org/cgi/content/abstract/110/11/1166?maxtoshow=&HITS=10&hits=10&RESULTFORMAT=&fulltext=AVE1642&searchid=1&FIRSTINDEX=0&volume=110&issue=11&resourcetype=HWCIT.
• Morrow LA, O’Brien MB, Moller DE, Flier JS, Moses AC . (1994). Recombinant human insulin-like growth factor-I therapy improves glycemic control and insulin action in the type A syndrome of severe insulin resistance. J Clin Endocrinol Metab 79: 205–210.
  CAS PubMed Google Scholar
• Myal Y, Shiu RP, Bhaumick B, Bala M . (1984). Receptor binding and growth-promoting activity of insulin-like growth factors in human breast cancer cells (T-47D) in culture. Cancer Res 44: 5486–5490.
  CAS PubMed Google Scholar
• Natrajan R, Reis-Filho JS, Little SE, Messahel B, Brundler MA, Dome JS et al. (2006). Blastemal expression of type I insulin-like growth factor receptor in Wilms’ tumors is driven by increased copy number and correlates with relapse. Cancer Res 66: 11148–11155.
  CAS PubMed Google Scholar
• O’Reilly KE, Molife R, Okuno S, Worden F, Hammer G, Yap T et al. (2006). mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. Cancer Res 66: 1500–1508.
  PubMed PubMed Central Google Scholar
• Olmos D, Molife R, Okuno S, Worden F, Hammer G, Yap T et al. (2007). Safety, tolerability and preliminary efficacy of the anti-IGF-IR 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, http://www.aacr.org/Uploads/DocumentRepository/2007conf/moltar/mt07_postera.pdf.
• Olmos D, Okuno S, Schuetze SM, Pacagnella ML, Yin D, Gualberto A et al. (2008). Safety, pharmacokinetics and preliminary activity of the anti-IGF-IR antibody CP-751,871 in patients with sarcoma. J Clin Oncol 26: 553s.
  Google Scholar
• Plymate SR, Haugk K, Coleman I, Woodke L, Vessella R, Nelson P et al. (2007). An antibody targeting the type I insulin-like growth factor receptor enhances the castration-induced response in androgen-dependent prostate cancer. Clin Cancer Res 13: 6429–6439.
  CAS PubMed Google Scholar
• Pollak M . (2008a). Insulin and insulin-like growth factor signalling in neoplasia. Nat Rev Cancer 8: 915–928.
  CAS PubMed Google Scholar
• Pollak M. (2008b). Targeting insulin and insulin-like growth factor signalling in oncology. Curr Opin Pharmacol 8: 384–392.
  CAS PubMed Google Scholar
• Pollak M, Blouin MJ, Zhang JC, Kopchick JJ. (2001). Reduced mammary gland carcinogenesis in transgenic mice expressing a growth hormone antagonist. Br J Cancer 85: 428–430.
  CAS PubMed PubMed Central Google Scholar
• Pollak M, Eisenberg P, Karp D, Cohen R, Kreisman H, Adjei A et al. (2007). Safety and tolerability of the anti-IGF-I receptor antibody CP-751,871 in combination with paclitaxel and carboplatin in patients with advanced solid tumors. AACR Meeting Abstracts (abstract LB-343), http://www.aacrmeetingabstracts.org/cgi/content/meeting_abstract/2007/1_Annual_Meeting/LB-343?maxtoshow=&HITS=10&hits=10&RESULTFORMAT=1&author1=Pollak&title=paclitaxel+carboplatin&andorexacttitle=and&andorexacttitleabs=and&searchid=1&FIRSTINDEX=0&sortspec=relevance&fdate=1/1/2007&tdate=12/31/2007&resourcetype=HWCIT.
• Pollak MN, Perdue JF, Margolese RG, Baer K, Richard M. (1987). Presence of somatomedin receptors on primary human breast and colon carcinomas. Cancer Lett 38: 223–230.
  CAS PubMed Google Scholar
• Pollak MN, Schernhammer ES, Hankinson SE. (2004). Insulin-like growth factors and neoplasia. Nat Rev Cancer 4: 505–518.
  CAS PubMed Google Scholar
• Postel-Vinay S, Okuno S, Schuetze SM, Pacagnella L, Yin D, Gualberto A et al. (2008). Safety, pharmacokinetics and preliminary activity of the anti-IGF-1R antibody CP-751,871 in patients with sarcoma. Presented at the 20th EORTC-NCI-AACR symposium on Molecular Targets and Cancer Therapeutics Congress, 21–24 October 2008, Geneva, Switzerland.
• Rodon J, DeSantos V, Ferry Jr RJ, Kurzrock R. (2008). Early drug development of inhibitors of the insulin-like growth factor-I receptor pathway: lessons from the first clinical trials. Mol Cancer Ther 7: 2575–2588.
  CAS PubMed PubMed Central Google Scholar
• Rodon J, Patnaik A, Stein M, Tolcher A, Ng C, Dias C 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: 160s.
  Google Scholar
• Rothenberg ML, Poplin E, Sandler AB, Rubin EH, Fox F, Schwartz J 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. Presented at the AACR-NCI-EORTC Molecular Targets and Cancer Therapeutics Meeting, San Francisco, USA, 22–26 October 2007, http://www.aacr.org/Uploads/DocumentRepository/2007conf/moltar/mt07_posterc.pdf.
• Russo VC, Gluckman PD, Feldman EL, Werther GA. (2005). The insulin-like growth factor system and its pleiotropic functions in brain. Endocr Rev 26: 916–943.
  CAS PubMed Google Scholar
• Ryan PD, Neven P, Dirix LY, Barrios CH, Miller WH, Fenton D et al. (2008). Safety of the anti-IGF-1R antibody CP-751,871 in combination with exemestane in patients with advanced breast cancer. Presented at the 31st Annual San Antonio Breast Cancer Meeting, San Antonio, USA, 10–14 December 2008.
• Sachdev D, Singh R, Fujita-Yamaguchi Y, Yee D. (2006). 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.
  CAS PubMed Google Scholar
• Sachdev D, Yee D . (2007). Disrupting insulin-like growth factor signaling as a potential cancer therapy. Mol Cancer Ther 6: 1–12.
  CAS PubMed Google Scholar
• Samani AA, Yakar S, LeRoith D, Brodt P. (2007). The role of the IGF system in cancer growth and metastasis: overview and recent insights. Endocr Rev 28: 20–47.
  CAS PubMed Google Scholar
• Sarantopoulos J, Mita AC, Mulay M, Romero O, Lu J, Capilla F et al. (2008). A phase IB study of AMG 479, a type 1 insulin-like growth factor receptor (IGF1R) antibody, in combination with panitumumab (P) or gemcitabine (G). J Clin Oncol 26: 173s.
  Google Scholar
• Sell C, Rubini M, Rubin R, Liu JP, Efstratiadis A, Baserga R. (1993). Simian virus 40 large tumor antigen is unable to transform mouse embryonic fibroblasts lacking type 1 insulin-like growth factor receptor. Proc Natl Acad Sci USA 90: 11217–11221.
  CAS PubMed PubMed Central Google Scholar
• Seraj J, Tsai M, Seiberling M, Cutler D. (2007). Evaluation of safety and pharmacokinetics of a fully human IGF-1 receptor antibody, SCH 717454, in healthy volunteers. Presented at the AACR-NCI-EORTC Molecular Targets and Cancer Therapeutics Meeting, San Francisco, USA, 22-26 October 2007, http://www.aacr.org/Uploads/DocumentRepository/2007conf/moltar/mt07_postera.pdf.
• Shaw RJ, Lamia KA, Vasquez D, Koo SH, Bardeesy N, Depinho RA et al. (2005). The kinase LKB1 mediates glucose homeostasis in liver and therapeutic effects of metformin. Science 310: 1642–1646.
  CAS PubMed PubMed Central Google Scholar
• Slamon DJ, Leyland-Jones B, Shak S, Fuchs H, Paton V, Bajamonde A et al. (2001). Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2. N Engl J Med 344: 783–792.
  CAS PubMed Google Scholar
• Tabernero J. (2008). The role of the IGF-1R inhibitor in CRC. Presented at the 33rd ESMO congress, Stockholm, Sweden, 12–16 September, 2008, http://www.esmo.org/fileadmin/media/presentations/977/1976/Tabernero_ESMO%20symposium%202008_slide%20presentation_d02b.ppt.pdf.
• Tao Y, Pinzi V, Bourhis J, Deutsch E. . (2007). Mechanisms of disease: signaling of the insulin-like growth factor 1 receptor pathway—therapeutic perspectives in cancer. Nat Clin Pract Oncol 4: 591–602.
  CAS PubMed Google Scholar
• Tarn C, Rink L, Merkel E, Flieder D, Pathak H, Koumbi D et al. (2008). Insulin-like growth factor 1 receptor is a potential therapeutic target for gastrointestinal stromal tumors. Proc Natl Acad Sci USA 105: 8387–8392.
  CAS PubMed PubMed Central Google Scholar
• Tolcher AW, Rothenberg ML, Rodon J, Delbeke D, Patnaik A, Nguyen L et al. (2008). A phase I study of AVE1642, a humanized monoclonal antibody IGF-1R (insulin like growth factor1 receptor) antagonist, in patients (pts) with advanced solid tumor (ST). J Clin Oncol 26: 173s.
  Google Scholar
• Tolcher AW, Patnaik A, Till E, Takimoto CH, Papadopoulos KP, Massard C et al. (2007). 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 Oncol 25: 118s.
  Google Scholar
• Wan X, Harkavy B, Shen N, Grohar P, Helman LJ. (2007). Rapamycin induces feedback activation of Akt signaling through an IGF-1R-dependent mechanism. Oncogene 26: 1932–1940.
  CAS PubMed Google Scholar
• Weroha SJ, Haluska P . (2008). IGF-1 receptor inhibitors in clinical trials--early lessons. J Mammary Gland Biol Neoplasia 13: 471–483.
  PubMed PubMed Central Google Scholar
• Wiseman LR, Johnson MD, Wakeling AE, Lykkesfeldt AE, May FE, Westley BR. (1993). Type I IGF receptor and acquired tamoxifen resistance in oestrogen-responsive human breast cancer cells. Eur J Cancer 29A: 2256–2264.
  CAS PubMed Google Scholar
• Witt K . (2008). OSI Pharmaceuticals Oncology Portfolio: R&D Strategy and Update on Pipeline. Securities and Exchange Commission OSI Pharmaceuticals Inc. 8-K form for 11/26/2008, Exhibit 99.1.
• Wolpin BM, Meyerhardt JA, Chan AT, Ng K, Chan JA, Wu K et al. (2009). Insulin, the insulin-like growth factor axis, and mortality in patients with nonmetastatic colorectal cancer. J Clin Oncol 27: 176–185.
  PubMed PubMed Central Google Scholar
• Wu JD, Haugk K, Coleman I, Woodke L, Vessella R, Nelson P et al. (2006). Combined in vivo effect of A12, a type 1 insulin-like growth factor receptor antibody, and docetaxel against prostate cancer tumors. Clin Cancer Res 12: 6153–6160.
  CAS PubMed Google Scholar
• Wu JD, Odman A, Higgins LM, Haugk K, Vessella R, Ludwig DL et al. (2005). in vivo effects of the human type I insulin-like growth factor receptor antibody A12 on androgen-dependent and androgen-independent xenograft human prostate tumors. Clin Cancer Res 11: 3065–3074.
  CAS PubMed Google Scholar
• Wu Y, Cui K, Miyoshi K, Hennighausen L, Green JE, Setser J et al. (2003). Reduced circulating insulin-like growth factor I levels delay the onset of chemically and genetically induced mammary tumors. Cancer Res 63: 4384–4388.
  CAS PubMed Google Scholar
• Yee D. (2006). Targeting insulin-like growth factor pathways. Br J Cancer 94: 465–468.
  CAS PubMed PubMed Central Google Scholar
• Yin D, Paccagnella ML, Lacy MQ, De Bono JS, Haluska P, Gualberto A et al. (2008). Population pharmacokinetics of CP-751,871, a monoclonal antibody against IGF-I receptor, in patients with multiple myeloma or solid tumors. J Clin Oncol 26: 118s.
  Google Scholar
• Yuen JS, Macaulay VM . (2008). Targeting the type 1 insulin-like growth factor receptor as a treatment for cancer. Expert Opin Ther Targets 12: 589–603.
  CAS PubMed Google Scholar
• Zhang H, Pelzer AM, Kiang DT, Yee D. (2007) Down-regulation of type I insulin-like growth factor receptor increases sensitivity of breast cancer cells to insulin. Cancer Res 67: 391–397.
  CAS PubMed Google Scholar
• Zhang L, Zhou W, Velculescu VE, Kern SE, Hruban RH, Hamilton SR et al. (1997). Gene expression profiles in normal and cancer cells. Science 276: 1268–1272.
  CAS PubMed Google Scholar

Download references