Developing c-MET pathway inhibitors for cancer therapy: progress and challenges

Trends in Molecular Medicine

Volumn 16, Issue 1, 2010, Pages 37-45

  Liu, Xiangdong ^a   Newton, Robert C ^a   Scherle, Peggy A ^a  

^a Experimental Station   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [1 (2,6 DICHLORO 3 FLUOROPHENYL)ETHOXY] 5 [1 (4 PIPERIDINYL) 1H PYRAZOL 4 YL] 2 PYRIDINYLAMINE; AMG 102; AMG 208; ANTINEOPLASTIC AGENT; ARQ 197; AV 299; BMS 777607; BMS 907351; DOCETAXEL; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; INCB 28060; JNJ 38877605; JNJ 38877606; METMAB; MGCD 265; MK 2461; MP 470; PF 4317903; PROTEIN TYROSINE KINASE INHIBITOR; RILOTUMUMAB; SCATTER FACTOR; SCATTER FACTOR RECEPTOR; SCATTER FACTOR RECEPTOR INHIBITOR; SCH 900105; TAK 701; TEMOZOLOMIDE; UNCLASSIFIED DRUG; UNINDEXED DRUG; XL 184; XL 880;

ANTINEOPLASTIC ACTIVITY; C MET GENE; CANCER GROWTH; CANCER THERAPY; CARCINOGENESIS; CLINICAL TRIAL; COLORECTAL CANCER; DRUG DOSE ESCALATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG TARGETING; DRUG TOLERABILITY; GENE EXPRESSION; GENE MUTATION; GLIOBLASTOMA; GLIOMA; HEAD AND NECK CANCER; HUMAN; KIDNEY CANCER; KIDNEY CARCINOMA; LARGE CELL LYMPHOMA; LIVER CELL CARCINOMA; LOWER ESOPHAGUS SPHINCTER ADENOCARCINOMA; LUNG NON SMALL CELL CANCER; LUNG SMALL CELL CANCER; METASTASIS; NEOPLASM; NEUROENDOCRINE TUMOR; NONHUMAN; PANCREAS CANCER; PROSTATE CANCER; REVIEW; SIGNAL TRANSDUCTION; SOLID TUMOR; STOMACH CANCER; THYROID CANCER; THYROID MEDULLARY CARCINOMA; TUMOR; UNSPECIFIED SIDE EFFECT;

ANIMALS; HUMANS; NEOPLASMS; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-MET; SIGNAL TRANSDUCTION;

EID: 73449111266     PISSN: 14714914     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.molmed.2009.11.005     Document Type: Review

References (78)

1. Ma W.W., and Adjei A.A. Novel agents on the horizon for cancer therapy. CA Cancer J Clin. 59 (2009) 111-137
2. Greenman C., et al. Patterns of somatic mutation in human cancer genomes. Nature 446 (2007) 153-158
3. Rikova K., et al. Global survey of phosphotyrosine signaling identifies oncogenic kinases in lung cancer. Cell 131 (2007) 1190-1203
4. Birchmeier C., et al. Met, metastasis, motility and more. Nat Rev Mol Cell Biol. 4 (2003) 915-925
5. Ido A., and Tsubouchi H. Translational research to identify clinical applications of hepatocyte growth factor. Hepatol Res. 39 (2009) 739-747
6. Christensen J., et al. c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention. Cancer Lett. 8 (2005) 1-26
7. Liu X., et al. Targeting the c-MET signaling pathway for cancer therapy. Expert Opin Investig Drugs. 17 (2008) 997-1011
8. Giebeler A., et al. c-Met confers protection against chronic liver tissue damage and fibrosis progression after bile duct ligation in mice. Gastroenterology 137 (2009) 297-308
9. Zeng Z.S., et al. c-Met gene amplification is associated with advanced stage colorectal cancer and liver metastases. Cancer Lett. 265 (2008) 258-269
10. Graveel C., et al. Activating Met mutations produce unique tumor profiles in mice with selective duplication of the mutant allele. Proc Natl Acad Sci USA 101 (2004) 17198-17203
11. Ponzo M.G., et al. Met induces mammary tumors with diverse histologies and is associated with poor outcome and human basal breast cancer. Proc Natl Acad Sci USA 106 (2009) 12903-12908
12. Seiwert T.Y., et al. The MET receptor tyrosine kinase is a potential novel therapeutic target for head and neck squamous cell carcinoma. Cancer Res. 69 (2009) 3021-3031
13. Knowles L.M., et al. HGF and c-Met participate in paracrine tumorigenic pathways in head and neck squamous cell cancer. Clin Cancer Res. 15 (2009) 3740-3750
14. Okuda K., et al. Met gene copy number predicts the prognosis for completely resected non-small cell lung cancer. Cancer Sci. 99 (2008) 2280-2285
15. Toiyama Y., et al. Serum hepatocyte growth factor as a prognostic marker for stage II or III colorectal cancer patients. Int J Cancer 125 (2009) 1657-1662
16. Gupta A., et al. Predictive value of plasma hepatocyte growth factor/scatter factor levels in patients with clinically localized prostate cancer. Clin Cancer Res. 14 (2008) 7385-7390
17. Cappuzzo F., et al. Increased MET gene copy number negatively affects survival of surgically resected non-small-cell lung cancer patients. J Clin Oncol. 27 (2009) 1667-1674
18. Kammula U.S., et al. Molecular co-expression of the c-Met oncogene and hepatocyte growth factor in primary colon cancer predicts tumor stage and clinical outcome. Cancer Lett. 248 (2007) 219-228
19. Miyata Y., et al. Phosphorylated hepatocyte growth factor receptor/c-Met is associated with tumor growth and prognosis in patients with bladder cancer: correlation with matrix metalloproteinase-2 and -7 and E-cadherin. Hum Pathol. 40 (2009) 496-504
20. Ma J., et al. Somatic mutation and functional polymorphism of a novel regulatory element in the HGF gene promoter causes its aberrant expression in human breast cancer. J Clin Invest. 119 (2009) 478-491
21. Ma P.C., et al. Expression and mutational analysis of MET in human solid cancers. Genes Chromosomes Cancer 47 (2008) 1025-1037
22. Stein U., et al. MACC1, a newly identified key regulator of HGF-MET signaling, predicts colon cancer metastasis. Nat Med. 15 (2009) 59-67
23. Lee C.T., et al. The prognostic significance of RON and MET receptor coexpression in patients with colorectal cancer. Dis Colon Rectum. 51 (2008) 1268-1274
24. Guo A., et al. Signaling networks assembled by oncogenic EGFR and c-Met. Proc Natl Acad Sci USA 105 (2008) 692-697
25. You W.K., et al. The hepatocyte growth factor/c-Met signaling pathway as a therapeutic target to inhibit angiogenesis. BMB Rep. 41 (2008) 833-839
26. Gu X., et al. Inhibition of HGF/c-MET pathway by ARQ197: characterization of pharmacodynamic markers in vitro and in vivo. The AACR Annual Meeting (2009) Abstract 1748
27. Mekhail T., et al. Final results: A dose escalation phase I study of ARQ197, a selective c-Met inhibitor, in patients with metastatic solid tumors. The ASCO Annual Meeting (2009) Abstract 3548
28. Yap T.A., et al. Final results of a pharmacokinetic (PK) and pharmacodynamic (PD) phase I trial of ARQ 197 incorporating dynamic contrast-enhanced (DCE) magnetic resonance imaging (MRI) studies investigating the antiangiogenic activity of selective c-Met inhibition. The ASCO Annual Meeting (2009) Abstract 3523
29. Laux I., et al. Phase I dose escalation trial (ARQ197-111) evaluating combination of selective c-Met inhibitor ARQ197 and erlotinib. The ASCO Annual Meeting (2009) Abstract 3549
30. Goldberg J., et al. Preliminary results from a phase II study of ARQ197 in patients with microphthalmia transcription factor family (MiT)-associated tumors. The ASCO Annual Meeting (2009) Abstract 10502
31. Zou H.Y., et al. An orally available small-molecule inhibitor of c-MET, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 67 (2007) 4408-4417
32. Christensen J.G., et al. Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma. Mol Cancer Ther. 6 (2007) 3314-3322
33. Timofeevski S.L., et al. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry 48 (2009) 5339-5349
34. Kwak E.L., et al. Clinical activity observed in a phase I dose escalation trial of an oral c-Met and ALK inhibitor, PF-02341066. The ASCO Annual Meeting (2009) Abstract 3509
35. Christensen, J.G. (2008) cMET inhibitor. The AACR Annual Meeting New Drugs on the Horizon 2 (Drug Development Track: Special Session 2). Oral presentation
36. Perera T., et al. JNJ-38877605: a selective Met kinase inhibitor inducing regression of Met-driven tumor models. The AACR Annual Meeting (2008) Abstract 4837
37. Liu X., et al. Discovery and characterization of INCB028060, a novel, potent and selective Met RTK inhibitor for cancer treatment. The AACR Annual Meeting (2008) Abstract 2577
38. Liu L., et al. Novel mechanism of lapatinib resistance in HER2-positive breast cancer cells: activation of AXL. Cancer Res. 69 (2009) 6871-6878
39. Janne P.A., et al. Targeting MET with XL184 to reverse EGFR tyrosine kinase inhibitor (TKI) resistance in NSCLC: impact of preclinical studies on clinical trial design. European J of Cancer. 6 (2008) Abstract 552
40. Eder J.P., et al. Phase I experience with c-MET inhibitor CL880 administered orally to patients (pts) with solid tumors. J Clin Oncol ASCO Annual Meeting Proceedings 25 18S (2007) 3526
41. Shapiro G.I., et al. A phase I dose-escalation study of the safety, pharmacokinetics (PK) and pharmacodynamics of XL880, a VEGFR and MET kinase inhibitor, administered daily to patients (pts) with advanced malignancies. The AACR-NCI-EORTC Symposium on Molecular Targets and Cancer Therapeutics (2007) Abstract B248
42. Srinivasan R., et al. Phase II study of two dosing regimens of GSK1363089 (GSK089), a dual MET/VEGFR2 inhibitor, in patients (pts) with papillary renal carcinoma (PRC). The ASCO Annual Meeting (2009) Abstract 5103
43. Jhawer M., et al. Assessment of two dosing schedules of GSK1363089 (GSK089), a dual MET/VEGFR2 inhibitor, in metastatic gastric cancer (GC): Interim results of a multicenter phase II study. The ASCO Annual Meeting (2009) Abstract 4502
44. Kurzrock R., et al. A phase I study of XL184, a MET, VEGFRs and RET kinase inhibitor, administered orally to patients (pts) with advanced malignancies, including a subgroup of pts with medullary thyroid cancer (MTC). The AACR-NCI-EORTC International Conference, Molecular Targets and Cancer Therapeutics, Discovery, Biology, and Clinical Applications (2007) Abstract 379
45. de Groot J.F., et al. A phase II study of XL184 in patients (pts) with progressive glioblastoma multiforme (GBM) in first or second relapse. The ASCO Annual Meeting (2009) Abstract 2047
46. th World Conference on Lung Cancer (2009) Abstract 7936
47. Beaulieu C., et al. Preclinical development of MGCD265, a potent orally active c-Met/VEGFR multi-target kinase inhibitor. The AACR Annual Meeting (2008) Abstract 4838
48. Kollmannsberger C.K., et al. Phase I study of daily administration of MGCD265 to patients with advanced malignancies (Study 265-101). The ASCO Annual Meeting (2009) Abstract e14525
49. Schroeder G.M., et al. Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily. J Med Chem. 52 (2009) 1251-1254
50. Eder J.P., et al. Novel therapeutic inhibitors of the c-Met signaling pathway in cancer. Clin Cancer Res. 15 (2009) 2207-2214
51. Camacho L.H., et al. First in human phase I study of MK-2461, a small molecule inhibitor of c-Met, for patients with advanced solid tumors. The ASCO Annual Meeting (2008) Abstract 14657
52. Zhang Y., et al. Identification of a novel recepteur d'origine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo. Cancer Res. 68 (2008) 6680-6687
53. Giordano S. Rilotumumab, a mAb against human hepatocyte growth factor for the treatment of cancer. Curr Opin Mol Ther. 11 (2009) 448-455
54. Jun H.T., et al. AMG 102, a fully human anti-hepatocyte growth factor/scatter factor neutralizing antibody, enhances the efficacy of temozolomide or docetaxel in U-87 MG cells and xenografts. Clin Cancer Res. 13 (2007) 6735-6742
55. Gordon M.S., et al. Interim results from a first-in-human study with AMG102, a full human monoclonal antibody that neutralizes hepatocyte growth factor (HGF), the ligand to c-Met receptor, in patients (pts) with advanced solid tumors. The ASCO Annual Meeting (2007) Abstract 3551
56. Rosen P.J., et al. AMG102, an HGF/SF antagonist, in combination with anti-angiogenesis targeted therapies in adult patients with advanced solid tumors. J Clin Oncol. 26 (2008) Abstract 3570
57. Reardon D.A., et al. Phase II study of AMG102, a fully human neutralizing antibody against hepatocyte growth factor/scatter factor, in patients with recurrent glioblastoma multiforme. The ASCO Annual Meeting (2008) Abstract 2051
58. Merchant M., et al. One-armed 5D5 (OA5D5) is a potent humanized HGF-blocking anti-c-Met monovalent antibody that inhibits HGF-dependent activity in vitro and demonstrated anti-tumor efficacy in vivo. The AACR Annual Meeting (2007) Abstract LB-372
59. Jin H., et al. MetMAb, the one-armed 5D5 anti-c-Met antibody, inhibits orthotopic pancreatic tumor growth and improves survival. Cancer Res. 68 (2008) 4360-4368
60. Merchant M., et al. MetMAb significantly enhances anti-tumor activity of anti-VEGF and/or erlotinib in several animal tumor models. The AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics (2008) Abstract 556
61. Martens T., et al. A novel one-armed anti-c-MET antibody inhibits glioblastoma growth in vivo. Clin Cancer Res. 12 (2006) 6144-6152
62. Salgia R., et al. A phase I, open-label, dose-escalation study of the safety and pharmacology of MetMAb, a monovalent antagonist antibody to the receptor c-MET, administered IV in patients with locally advanced or metastatic solid tumors. The AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics (2008) Abstract 441
63. Matteucci E., et al. Nuclear localization of active HGF receptor Met in aggressive MDA-MB-231 breast carcinoma cells. Carcinogenesis 30 (2009) 937-945
64. de Groot J.W., et al. RET as a diagnostic and therapeutic target in sporadic and hereditary endocrine tumors. Endocr Rev. 27 (2006) 535-560
65. Sherman S.I. Molecularly targeted therapies for thyroid cancers. Endocr Pract. 22 (2009) 1-27
66. Mineo R., et al. Activation of the hepatocyte growth factor (HGF)-Met system in papillary thyroid cancer: biological effects of HGF in thyroid cancer cells depend on Met expression levels. Endocrinology 145 (2004) 4355-4365
67. Miletic H., et al. Anti-VEGF therapies for malignant glioma: treatment effects and escape mechanisms. Expert Opin Ther Targets. 13 (2009) 455-468
68. Sharma S.V., et al. Epidermal growth factor receptor mutations in lung cancer. Nat Rev Cancer 7 (2007) 169-181
69. Apperley J.F. Part I: mechanisms of resistance to imatinib in chronic myeloid leukaemia. Lancet Oncol. 8 (2007) 1018-1029
70. Akervall J., et al. Genetic and expression profiles of squamous cell carcinoma of the head and neck correlate with cisplatin sensitivity and resistance in cell lines and patients. Clin Cancer Res. 10 (2004) 8204-8213
71. Ma Y., et al. Identification of genes that modulate sensitivity of U373MG glioblastoma cells to cis-platinum. Anticancer Drugs 17 (2006) 733-751
72. Lal B., et al. Targeting the c-Met pathway potentiates glioblastoma responses to gamma-radiation. Clin Cancer Res. 11 (2005) 4479-4486
73. Engelman J.A., et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 316 (2007) 1039-1043
74. Bean J., et al. MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proc Natl Acad Sci USA 104 (2007) 20932-20937
75. Cappuzzo F., et al. MET increased gene copy number and primary resistance to gefitinib therapy in non-small-cell lung cancer patients. Ann Oncol. 20 (2009) 298-304
76. Yano S., et al. Hepatocyte growth factor induces gefitinib resistance of lung adenocarcinoma with epidermal growth factor receptor-activating mutations. Cancer Res. 68 (2008) 9479-9487
77. Turke A.B., et al. HGF induces transient and stable ligand-independent resistance in gefitinib-sensitive lung cancers. The AACR Annual Meeting (2009) Abstract 1365
78. Agarwal S., et al. Association of constitutively activated hepatocyte growth factor receptor (Met) with resistance to a dual EGFR/Her2 inhibitor in non-small-cell lung cancer cells. Br J Cancer 100 (2009) 941-949