{"title":"Drugs targeting insulin-like growth factor 1 receptor","authors":"T. Mayer, L. Harris, M. DiGiovanna","doi":"10.1017/S1470903109990058","DOIUrl":null,"url":null,"abstract":"14622. 59. Wittman M, Carboni J, Attar R, et al. Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J Med Chem 2005; 48(18): 5639–5643. 60. Mulvihill M, Qun-Sheng J, Rosenfeld-Franklin M, et al. The discovery of OSI-906: a novel, potent, orally bioavailable imidazopyrazine-derived insulin-like growth factor-I receptor (IGF-1R) inhibitor with antitumor activity. AACR Annual Meeting 2008: abstract 4893. 61. Burtrum D, Zhu Z, Lu D, et al. 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 2003; 63(24): 8912–8921. 62. Cohen B, Baker D, Soderstrom C, et al. 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 2005; 11(5): 2063–2073. 63. Goetsch L, Gonzalez A, Leger O, et al. A 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 2005; 113(2): 316–328. 64. Maloney E, McLaughlin J, Dagdigian N, et al. An antiinsulin-like growth factor I receptor antibody that is a potent inhibitor of cancer cell proliferation. Cancer Res 2003; 63(16): 5073–5083. 65. Sachdev D, Li S, Hartell J, Fujita-Yamaguchi Y, Miller J, Yee D. A chimeric humanized single-chain antibody against the type I insulin-like growth factor (IGF) receptor renders breast cancer cells refractory to the mitogenic effects of IGF-I. Cancer Res 2003; 63(3): 627–635. 66. Wang Y, Hailey J, Williams D, et al. Inhibition of insulinlike growth factor-I receptor (IGF-IR) signaling and tumor cell growth by a fully human neutralizing anti-IGF-IR antibody. Mol Cancer Ther 2005; 4(8): 1214–1221. 67. Haluska P, Shaw H, Batzel G, 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(19): 5834–5840. Drugs targeting insulin-like growth factor 1 receptor Page 9 of 10 https://www.cambridge.org/core/terms. https://doi.org/10.1017/S1470903109990058 Downloaded from https://www.cambridge.org/core. IP address: 207.241.231.82, on 24 Jul 2018 at 13:47:50, subject to the Cambridge Core terms of use, available at 68. Lacy M, Alsina M, Fonseca R, et al. Phase I, Pharmacokinetic and Pharmacodynamic Study of the AntiInsulin like Growth Factor Type 1 Receptor Monoclonal Antibody CP-751,871 in Patients With Multiple Myeloma. J Clin Oncol 2008; 26(19): 3196–3203. 69. Karp D, Paz-Ares L, Novello P, et al. High activity of the anti-IGF-IR antibody CP-751,871 in combination with paclitaxel and carboplatin in squamous NSCLC. J Clin Oncol 2008; 26: abstract 8015. 70. Hidalgo M, Tirado Gomez M, Lewis N, et al. A phase I study of MK-0646, a humanized monoclonal antibody against the insulin-like growth factor receptor type 1 (IGF-IR) in advanced solid tumor patients in a q2 wk schedule. J Clin Oncol 2008; 26: abstract 3520. 71. Atzori F, Tabernero A, Cervantes A, et al. A phase I, pharmacokinetic (PK) and pharmacodynamic (PD) study of weekly (qW) MK-0646, an insulin-like growth factor-1 receptor (IGF-IR) monoclonal antibody (MAb) in patients (pts) with advanced solid tumors. J Clin Oncol 2008; 26: abstract 3519. 72. Beltran P, Mitchell P, Moody G, et al. AMG-479, a fully human anti IGF-1 receptor antibody, inhibits PI3K/Akt3519. 72. Beltran P, Mitchell P, Moody G, et al. AMG-479, a fully human anti IGF-1 receptor antibody, inhibits PI3K/Akt signaling and exerts potent antitumor effects in combination with EGF-R inhibitors in pancreatic xenograft models. Gastrointestinal Cancers Symposium, American Society of Clinical Oncology, Orlando, FL, USA, 2007: abstract 208. 73. Sarantpoulos J, Mita A, Mulay M, et al. A phase IB study of AMG 479, a type 1 insulin-like growth factor receptor (IGF-1R) antibody, in combination with panitumumab (P) or gemcitabine (G). J Clin Oncol 2008; 26: abstract 3583. 74. Tolcher A, Rothenberg M, Rodon J, et al. A phase I pharmacokinetic and pharmacodynamic study of AMG 479, a fully human monoclonal antibody against insulinlike growth factor type 1 receptor (IGF-1R), in advanced solid tumors. J Clin Oncol 2007; 25: abstract 3002. 75. Rodon J, Patnaik A, Stein M, et al. A phase I study of q3W R1507, a human monoclonal antibody IGF-1R antagonist in patients with advanced cancer. J Clin Oncol 2007; 25: abstract 3590. 76. Rowinsky E, Youssoufian H, Tonra J, Solomon P, Burtrum D, Ludwig D. IMC-A12, a human IgG1 monoclonal antibody to the insulin-like growth factor I receptor. Clin Cancer Res 2007; 13: 5549s–5555s. 77. Higano C, Yu E, Whiting S, et al. 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. Prostate Cancer Symposium, American Society of Clinical Oncology, Orlando, FL, USA, 2007: abstract 269. 78. Tolcher A, Patnaik A, Till E, et al. 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 tumors (ST). J Clin Oncol 2008; 26: abstract 3582. 79. Dong J, Tamraz S, Berquist L, et al. BIIB022, a human antibody targeting human insulin-like growth factor-1 receptor (IGF-1R), enhances the anti-tumor activities of Tarceva in non-small cell lung carcinoma (NSCLC) and rapamycin in sarcoma cell lines. AACR Annual Meeting 2008: abstract 4002. 80. Girnita A, Girnita L, del Prete F, Bartolazzi A, Larsson O, Axelson M. Cyclolignans as inhibitors of the insulin-like growth factor-1 receptor and malignant cell growth. Cancer Res 2004; 64(1): 236–242. 81. Gable K, Maddux B, Penaranda C, et al. Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth. Mol Cancer Ther 2006; 5(4): 1079–1086. 82. D’cunja J, Shalaby T, Rivera P, et al. Antisense treatment of IGF-IR induces apoptosis and enhances chemosensitivity in central nervous system atypical teratoid/ rhabdoid tumours cells. Eur J Cancer 2007; 43(10): 1581–1589. 83. Neuenschwander S, Roberts CJ, LeRoith D. Growth inhibition of MCF-7 breast cancer cells by stable expression of an insulin-like growth factor I receptor antisense ribonucleic acid. Endocrinology 1995; 136(10): 4298–4303. 84. Moses A, Young S, Morrow L, O’Brien M, Clemmons D. Recombinant human insulin-like growth factor I increases insulin sensitivity and improves glycemic control in type II diabetes. Diabetes 1996; 45(1): 91–100. 85. Schmitz F, Hartmann H, Stümpel F, Creutzfeldt W. In vivo metabolic action of insulin-like growth factor I in adult rats. Diabetologia 1991; 34(3): 144–149. 86. Soos M, Whittaker J, Lammers R, Ullrich A, Siddle K. Receptors for insulin and insulin-like growth factor-I can form hybrid dimers. Characterisation of hybrid receptors in transfected cells. Biochem J 1990; 270(2): 383–390. 87. Ullrich A, Gray A, Tam A, et al. Insulin-like growth factor I receptor primary structure: comparison with insulin receptor suggests structural determinants that define functional specificity. EMBO J 1986; 5(10): 2503–2512. 88. Yee D. Targeting insulin-like growth factor pathways. Br J Cancer 2006; 94(4): 465–468. 89. Sachdev D, Yee D. Inhibitors of insulin-like growth factor signaling: a therapeutic approach for breast cancer. J Mammary Gland Biol Neoplasia 2006; 11(1): 27–39. 90. Miyagawa S, Kobayashi M, Konishi N, Sato T, Ueda K. Insulin and insulin-like growth factor I support the proliferation of erythroid progenitor cells in bone marrow through the sharing of receptors. Br J Haematol 2000; 109(3): 555–562. 91. Masuda S, Chikuma M, Sasaki R. Insulin-like growth factors and insulin stimulate erythropoietin production in primary cultured astrocytes. Brain Res 1997; 746(1–2): 63–70. 92. Okajima Y, Matsumura I, Nishiura T, et al. Insulin-like growth factor-I augments erythropoietin-induced proliferation through enhanced tyrosine phosphorylation of STAT5. J Biol Chem 1998; 273: 22877–22883. 93. Huang F, Hurlburt W, Hafezi R, et al. Identification of sensitivity markers for BMS-536924, an inhibitor for insulin-like growth factor-1 receptor. J Clin Oncol 2007; 25: abstract 3506. 94. Warshamana-Greene G, Litz J, Buchdunger E, Garcı́aEcheverrı́a C, Hofmann F, Krystal G. The insulin-like growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy. Clin Cancer Res 2005; 11(4): 1563–1571. Page 10 of 10 T. Mayer et al. https://www.cambridge.org/core/terms. https://doi.org/10.1017/S1470903109990058 Downloaded from https://www.cambridge.org/core. 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引用次数: 1
Abstract
14622. 59. Wittman M, Carboni J, Attar R, et al. Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J Med Chem 2005; 48(18): 5639–5643. 60. Mulvihill M, Qun-Sheng J, Rosenfeld-Franklin M, et al. The discovery of OSI-906: a novel, potent, orally bioavailable imidazopyrazine-derived insulin-like growth factor-I receptor (IGF-1R) inhibitor with antitumor activity. AACR Annual Meeting 2008: abstract 4893. 61. Burtrum D, Zhu Z, Lu D, et al. 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 2003; 63(24): 8912–8921. 62. Cohen B, Baker D, Soderstrom C, et al. 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 2005; 11(5): 2063–2073. 63. Goetsch L, Gonzalez A, Leger O, et al. A 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 2005; 113(2): 316–328. 64. Maloney E, McLaughlin J, Dagdigian N, et al. An antiinsulin-like growth factor I receptor antibody that is a potent inhibitor of cancer cell proliferation. Cancer Res 2003; 63(16): 5073–5083. 65. Sachdev D, Li S, Hartell J, Fujita-Yamaguchi Y, Miller J, Yee D. A chimeric humanized single-chain antibody against the type I insulin-like growth factor (IGF) receptor renders breast cancer cells refractory to the mitogenic effects of IGF-I. Cancer Res 2003; 63(3): 627–635. 66. Wang Y, Hailey J, Williams D, et al. Inhibition of insulinlike growth factor-I receptor (IGF-IR) signaling and tumor cell growth by a fully human neutralizing anti-IGF-IR antibody. Mol Cancer Ther 2005; 4(8): 1214–1221. 67. Haluska P, Shaw H, Batzel G, 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(19): 5834–5840. Drugs targeting insulin-like growth factor 1 receptor Page 9 of 10 https://www.cambridge.org/core/terms. https://doi.org/10.1017/S1470903109990058 Downloaded from https://www.cambridge.org/core. IP address: 207.241.231.82, on 24 Jul 2018 at 13:47:50, subject to the Cambridge Core terms of use, available at 68. Lacy M, Alsina M, Fonseca R, et al. Phase I, Pharmacokinetic and Pharmacodynamic Study of the AntiInsulin like Growth Factor Type 1 Receptor Monoclonal Antibody CP-751,871 in Patients With Multiple Myeloma. J Clin Oncol 2008; 26(19): 3196–3203. 69. Karp D, Paz-Ares L, Novello P, et al. High activity of the anti-IGF-IR antibody CP-751,871 in combination with paclitaxel and carboplatin in squamous NSCLC. J Clin Oncol 2008; 26: abstract 8015. 70. Hidalgo M, Tirado Gomez M, Lewis N, et al. A phase I study of MK-0646, a humanized monoclonal antibody against the insulin-like growth factor receptor type 1 (IGF-IR) in advanced solid tumor patients in a q2 wk schedule. J Clin Oncol 2008; 26: abstract 3520. 71. Atzori F, Tabernero A, Cervantes A, et al. A phase I, pharmacokinetic (PK) and pharmacodynamic (PD) study of weekly (qW) MK-0646, an insulin-like growth factor-1 receptor (IGF-IR) monoclonal antibody (MAb) in patients (pts) with advanced solid tumors. J Clin Oncol 2008; 26: abstract 3519. 72. Beltran P, Mitchell P, Moody G, et al. AMG-479, a fully human anti IGF-1 receptor antibody, inhibits PI3K/Akt3519. 72. Beltran P, Mitchell P, Moody G, et al. AMG-479, a fully human anti IGF-1 receptor antibody, inhibits PI3K/Akt signaling and exerts potent antitumor effects in combination with EGF-R inhibitors in pancreatic xenograft models. Gastrointestinal Cancers Symposium, American Society of Clinical Oncology, Orlando, FL, USA, 2007: abstract 208. 73. Sarantpoulos J, Mita A, Mulay M, et al. A phase IB study of AMG 479, a type 1 insulin-like growth factor receptor (IGF-1R) antibody, in combination with panitumumab (P) or gemcitabine (G). J Clin Oncol 2008; 26: abstract 3583. 74. Tolcher A, Rothenberg M, Rodon J, et al. A phase I pharmacokinetic and pharmacodynamic study of AMG 479, a fully human monoclonal antibody against insulinlike growth factor type 1 receptor (IGF-1R), in advanced solid tumors. J Clin Oncol 2007; 25: abstract 3002. 75. Rodon J, Patnaik A, Stein M, et al. A phase I study of q3W R1507, a human monoclonal antibody IGF-1R antagonist in patients with advanced cancer. J Clin Oncol 2007; 25: abstract 3590. 76. Rowinsky E, Youssoufian H, Tonra J, Solomon P, Burtrum D, Ludwig D. IMC-A12, a human IgG1 monoclonal antibody to the insulin-like growth factor I receptor. Clin Cancer Res 2007; 13: 5549s–5555s. 77. Higano C, Yu E, Whiting S, et al. 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. Prostate Cancer Symposium, American Society of Clinical Oncology, Orlando, FL, USA, 2007: abstract 269. 78. Tolcher A, Patnaik A, Till E, et al. 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 tumors (ST). J Clin Oncol 2008; 26: abstract 3582. 79. Dong J, Tamraz S, Berquist L, et al. BIIB022, a human antibody targeting human insulin-like growth factor-1 receptor (IGF-1R), enhances the anti-tumor activities of Tarceva in non-small cell lung carcinoma (NSCLC) and rapamycin in sarcoma cell lines. AACR Annual Meeting 2008: abstract 4002. 80. Girnita A, Girnita L, del Prete F, Bartolazzi A, Larsson O, Axelson M. Cyclolignans as inhibitors of the insulin-like growth factor-1 receptor and malignant cell growth. Cancer Res 2004; 64(1): 236–242. 81. Gable K, Maddux B, Penaranda C, et al. Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth. Mol Cancer Ther 2006; 5(4): 1079–1086. 82. D’cunja J, Shalaby T, Rivera P, et al. Antisense treatment of IGF-IR induces apoptosis and enhances chemosensitivity in central nervous system atypical teratoid/ rhabdoid tumours cells. Eur J Cancer 2007; 43(10): 1581–1589. 83. Neuenschwander S, Roberts CJ, LeRoith D. Growth inhibition of MCF-7 breast cancer cells by stable expression of an insulin-like growth factor I receptor antisense ribonucleic acid. Endocrinology 1995; 136(10): 4298–4303. 84. Moses A, Young S, Morrow L, O’Brien M, Clemmons D. Recombinant human insulin-like growth factor I increases insulin sensitivity and improves glycemic control in type II diabetes. Diabetes 1996; 45(1): 91–100. 85. Schmitz F, Hartmann H, Stümpel F, Creutzfeldt W. In vivo metabolic action of insulin-like growth factor I in adult rats. Diabetologia 1991; 34(3): 144–149. 86. Soos M, Whittaker J, Lammers R, Ullrich A, Siddle K. Receptors for insulin and insulin-like growth factor-I can form hybrid dimers. Characterisation of hybrid receptors in transfected cells. Biochem J 1990; 270(2): 383–390. 87. Ullrich A, Gray A, Tam A, et al. Insulin-like growth factor I receptor primary structure: comparison with insulin receptor suggests structural determinants that define functional specificity. EMBO J 1986; 5(10): 2503–2512. 88. Yee D. Targeting insulin-like growth factor pathways. Br J Cancer 2006; 94(4): 465–468. 89. Sachdev D, Yee D. Inhibitors of insulin-like growth factor signaling: a therapeutic approach for breast cancer. J Mammary Gland Biol Neoplasia 2006; 11(1): 27–39. 90. Miyagawa S, Kobayashi M, Konishi N, Sato T, Ueda K. Insulin and insulin-like growth factor I support the proliferation of erythroid progenitor cells in bone marrow through the sharing of receptors. Br J Haematol 2000; 109(3): 555–562. 91. Masuda S, Chikuma M, Sasaki R. Insulin-like growth factors and insulin stimulate erythropoietin production in primary cultured astrocytes. Brain Res 1997; 746(1–2): 63–70. 92. Okajima Y, Matsumura I, Nishiura T, et al. Insulin-like growth factor-I augments erythropoietin-induced proliferation through enhanced tyrosine phosphorylation of STAT5. J Biol Chem 1998; 273: 22877–22883. 93. Huang F, Hurlburt W, Hafezi R, et al. Identification of sensitivity markers for BMS-536924, an inhibitor for insulin-like growth factor-1 receptor. J Clin Oncol 2007; 25: abstract 3506. 94. Warshamana-Greene G, Litz J, Buchdunger E, Garcı́aEcheverrı́a C, Hofmann F, Krystal G. The insulin-like growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy. Clin Cancer Res 2005; 11(4): 1563–1571. Page 10 of 10 T. Mayer et al. https://www.cambridge.org/core/terms. https://doi.org/10.1017/S1470903109990058 Downloaded from https://www.cambridge.org/core. IP address: 207.241.231.82, on 24 Jul 2018 at 13:47:50, subject to the Cambridge Core terms of use, available at