Biochemical and pharmacological characterization of human c-Met neutralizing monoclonal antibody CE-355621

mAbs

Volumn 4, Issue 6, 2012, Pages 710-723

  Michaud, Neil R ^a,c   Jani, Jitesh P ^a   Hillerman, Stephen ^a   Tsaparikos, Konstantinos E ^a   Barbacci Tobin, Elsa G ^a   Knauth, Elisabeth ^a   Putz, Henry ^a   Campbell, Mary ^a   Karam, George A ^a   Chrunyk, Boris ^a   Gebhard, David F ^a   Green, Larry L ^b,d   Xu, Jinghai J ^a   Dunn, Margaret C ^a   Coskran, Tim M ^a   Lapointe, Jean Martin ^a   Cohen, Bruce D ^a   Coleman, Kevin G ^a   Bedian, Vahe ^a,c   Vincent, Patrick ^a   Kajiji, Shama ^a   Steyn, Stefan J ^a   Borzillo, Gary V ^a   Los, Gerrit ^a   more..

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

^b Abgenix Inc   (United States)

^c ASTRAZENECA   (United Kingdom)

^d Ablexis LLC   (United States)

Author keywords

Antibody; Antitumor; c Met; HGF; Xenograft; XenoMouse

Indexed keywords

CE 310083; CE 310393; CE 310397; CE 310400; CE 355621; EPITOPE; MONOCLONAL ANTIBODY; NEUTRALIZING ANTIBODY; SCATTER FACTOR; SCATTER FACTOR RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIGEN BINDING; ARTICLE; BINDING AFFINITY; CANCER CELL; CANCER INHIBITION; CHEMICAL ANALYSIS; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG ISOLATION; FEMALE; FLOW CYTOMETRY; GENE ACTIVATION; GENE OVEREXPRESSION; GLIOBLASTOMA; HUMAN; HUMAN CELL; IC 50; IMMUNOHISTOCHEMISTRY; LIGAND BINDING; MORPHOGENESIS; MOUSE; NONHUMAN; PHENOTYPE; PROTO ONCOGENE; RECEPTOR BLOCKING; RECEPTOR DOWN REGULATION; STOMACH CANCER; TUMOR XENOGRAFT;

EID: 84869748840     PISSN: 19420862     EISSN: 19420870     Source Type: Journal    
DOI: 10.4161/mabs.22160     Document Type: Article

References (58)

1. Michalopoulos GK, DeFrances MC. Liver regeneration. Science 1997; 276:60-6; PMID:9082986; http://dx.doi.org/10.1126/science.276.5309.60
2. Di Renzo MF, Narsimhan RP, Olivero M, Bretti S, Giordano S, Medico E, et al. Expression of the Met/HGF receptor in normal and neoplastic human tissues. Oncogene 1991; 6:1997-2003; PMID:1719465
3. Birchmeier C, Birchmeier W, Gherardi E, Vande Woude GF. Met, metastasis, motility and more. Nat Rev Mol Cell Biol 2003; 4:915-25; http://dx.doi.org/10. 1038/nrm1261; PMID:14685170
4. Bladt F, Riethmacher D, Isenmann S, Aguzzi A, Birchmeier C. Essential role for the c-met receptor in the migration of myogenic precursor cells into the limb bud. Nature 1995; 376:768-71; http://dx.doi.org/10.1038/376768a0; PMID:7651534
5. Schmidt C, Bladt F, Goedecke S, Brinkmann V, Zschiesche W, Sharpe M, et al. Scatter factor/hepatocyte growth factor is essential for liver development. Nature 1995; 373:699-702; http://dx.doi.org/10.1038/373699a0; PMID:7854452
6. Gherardi E, Birchmeier W, Birchmeier C, Vande Woude G. Targeting MET in cancer: Rationale and progress. Nat Rev Cancer 2012; 12:89-103; PMID: 22270953; DOI: 10.1038/nrc3205; 10.1038/nrc3205
7. Maulik G, Shrikhande A, Kijima T, Ma PC, Morrison PT, Salgia R. Role of the hepatocyte growth factor receptor, c-Met, in oncogenesis and potential for therapeutic inhibition. Cytokine Growth Factor Rev 2002; 13:41-59; PMID:11750879; http://dx.doi.org/10.1016/S1359-6101(01)00029-6
8. Gao CF, Vande Woude GF. HGF/SF-Met signaling in tumor progression. Cell Res 2005; 15:49-51; http://dx.doi.org/10.1038/sj.cr.7290264; PMID:15686627
9. Ichimura E, Maeshima A, Nakajima T, Nakamura T. Expression of c-met/HGF receptor in human non-small cell lung carcinomas in vitro and in vivo and its prognostic significance. Jpn J Cancer Res 1996; 87:1063-9; PMID:8957065; http://dx.doi.org/10.1111/j.1349-7006.1996.tb03111.x
10. Han SU, Lee JH, Kim WH, Cho YK, Kim MW. Significant correlation between serum level of hepatocyte growth factor and progression of gastric carcinoma. World J Surg 1999; 23:1176-80; PMID:10501881; http://dx.doi.org/10.1007/ s002689900642
11. Kuba K, Matsumoto K, Date K, Shimura H, Tanaka M, Nakamura T. HGF/NK4, a four-kringle antagonist of hepatocyte growth factor, is an angiogenesis inhibitor that suppresses tumor growth and metastasis in mice. Cancer Res 2000; 60:6737-43; PMID:11118060
12. Tomioka D, Maehara N, Kuba K, Mizumoto K, Tanaka M, Matsumoto K, et al. Inhibition of growth, invasion, and metastasis of human pancreatic carcinoma cells by NK4 in an orthotopic mouse model. Cancer Res 2001; 61:7518-24; PMID:11606388
13. Martin TA, Parr C, Davies G, Watkins G, Lane J, Matsumoto K, et al. Growth and angiogenesis of human breast cancer in a nude mouse tumour model is reduced by NK4, a HGF/SF antagonist. Carcinogenesis 2003; 24:1317-23; http://dx.doi.org/10.1093/carcin/bgg072; PMID:12807719
14. Christensen JG, Burrows J, Salgia R. c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention. Cancer Lett 2005; 225:1-26; http://dx.doi.org/10.1016/j.canlet.2004.09.044; PMID:15922853
15. Cao B, Su Y, Oskarsson M, Zhao P, Kort EJ, Fisher RJ, et al. Neutralizing monoclonal antibodies to hepatocyte growth factor/scatter factor (HGF/SF) display antitumor activity in animal models. Proc Natl Acad Sci U S A 2001; 98:7443-8; http://dx.doi.org/10.1073/pnas.131200498; PMID:11416216
16. Comoglio PM, Giordano S, Trusolino L. Drug development of MET inhibitors: targeting oncogene addiction and expedience. Nat Rev Drug Discov 2008; 7:504-16; http://dx.doi.org/10.1038/nrd2530; PMID:18511928
17. Zou HY, Li Q, Lee JH, Arango ME, McDonnell SR, Yamazaki S, et al. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res 2007; 67:4408-17; http://dx.doi.org/10.1158/0008-5472. CAN-06-4443; PMID:17483355
18. Tu WH, Zhu C, Clark C, Christensen JG, Sun Z. Efficacy of c-Met inhibitor for advanced prostate cancer. BMC Cancer 2010; 10:556; http://dx.doi.org/10. 1186/1471-2407-10-556; PMID:20946682
19. Ma PC, Schaefer E, Christensen JG, Salgia R. A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clin Cancer Res 2005; 11:2312-9; http://dx.doi.org/10.1158/1078-0432. CCR-04-1708; PMID:15788682
20. Jin H, Yang R, Zheng Z, Romero M, Ross J, Bou-Reslan H, et al. MetMAb, the one-armed 5D5 antic-Met antibody, inhibits orthotopic pancreatic tumor growth and improves survival. Cancer Res 2008; 68:4360-8; http://dx.doi.org/10. 1158/0008-5472. CAN-07-5960; PMID:18519697
21. Martens T, Schmidt NO, Eckerich C, Fillbrandt R, Merchant M, Schwall R, et al. A novel one-armed anti-c-Met antibody inhibits glioblastoma growth in vivo. Clin Cancer Res 2006; 12:6144-52; http://dx.doi.org/10.1158/1078-0432.CCR- 05-1418; http://www.ncbi.nl PMID:17062691
22. Burgess T, Coxon A, Meyer S, Sun J, Rex K, Tsuruda T, et al. Fully human monoclonal antibodies to hepatocyte growth factor with therapeutic potential against hepatocyte growth factor/c-Met-dependent human tumors. Cancer Res 2006; 66:1721-9
23. Stabile LP, Rothstein ME, Keohavong P, Jin J, Yin J, Land SR, et al. Therapeutic targeting of human hepatocyte growth factor with a single neutralizing monoclonal antibody reduces lung tumorigenesis. Mol Cancer Ther 2008; 7:1913-22; http://dx.doi.org/10.1158/1535-7163.MCT-07-2169; PMID:18645002
24. Buchanan SG, Hendle J, Lee PS, Smith CR, Bounaud PY, Jessen KA, et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther 2009; 8:3181-90; http://dx.doi.org/10.1158/1535-7163.MCT-09-0477; PMID:19934279
25. Tseng JR, Kang KW, Dandekar M, Yaghoubi S, Lee JH, Christensen JG, et al. Preclinical efficacy of the c-Met inhibitor CE-355621 in a U87 MG mouse xenograft model evaluated by 18F-FDG small-animal PET. J Nucl Med 2008; 49:129-34; http://dx.doi.org/10.2967/jnumed.106.038836; PMID:18077531
26. Green LL. Antibody engineering via genetic engineering of the mouse: XenoMouse strains are a vehicle for the facile generation of therapeutic human monoclonal antibodies. J Immunol Methods 1999; 231:11-23; PMID:10648924; http://dx.doi.org/10.1016/S0022-1759(99)00137-4
27. Graziani A, Gramaglia D, Cantley LC, Comoglio PM. The tyrosine-phosphorylated hepatocyte growth factor/scatter factor receptor associates with phosphatidylinositol 3-kinase. J Biol Chem 1991; 266:22087-90; PMID:1718989
28. Trusolino L, Bertotti A, Comoglio PM. MET signalling: principles and functions in development, organ regeneration and cancer. Nat Rev Mol Cell Biol 2010; 11:834-48; http://dx.doi.org/10.1038/nrm3012; PMID:21102609
29. Jeffers M, Rong S, Anver M, Vande Woude GF. Autocrine hepatocyte growth factor/scatter factor-Met signaling induces transformation and the invasive/ metastastic phenotype in C127 cells. Oncogene 1996; 13:853-6; PMID:8761307
30. Rong S, Bodescot M, Blair D, Dunn J, Nakamura T, Mizuno K, et al. Tumorigenicity of the met protooncogene and the gene for hepatocyte growth factor. Mol Cell Biol 1992; 12:5152-8; PMID:1406687
31. Rong S, Oskarsson M, Faletto D, Tsarfaty I, Resau JH, Nakamura T, et al. Tumorigenesis induced by coexpression of human hepatocyte growth factor and the human met protooncogene leads to high levels of expression of the ligand and receptor. Cell Growth Differ 1993; 4:563-9; PMID:8398896
32. Tajima H, Matsumoto K, Nakamura T. Regulation of cell growth and motility by hepatocyte growth factor and receptor expression in various cell species. Exp Cell Res 1992; 202:423-31; PMID:1327854; http://dx.doi.org/10.1016/0014- 4827(92)90095-P
33. Okano Y, Mizuno K, Osada S, Nakamura T, Nozawa Y. Tyrosine phosphorylation of phospholipase C gamma in c-met/HGF receptor-stimulated hepatocytes: comparison with HepG2 hepatocarcinoma cells. Biochem Biophys Res Commun 1993; 190:842-8; http://dx.doi.org/10.1006/bbrc.1993.1125; PMID:7679901
34. Neaud V, Faouzi S, Guirouilh J, Le Bail B, Balabaud C, Bioulac-Sage P, et al. Human hepatic myofibroblasts increase invasiveness of hepatocellular carcinoma cells: evidence for a role of hepatocyte growth factor. Hepatology 1997; 26:1458-66; http://dx.doi.org/10.1002/hep.510260612; PMID:9397985
35. Gherardi E, Sandin S, Petoukhov MV, Finch J, Youles ME, Ofverstedt LG, et al. Structural basis of hepatocyte growth factor/scatter factor and MET signalling. Proc Natl Acad Sci U S A 2006; 103:4046-51; http://dx.doi.org/10. 1073/pnas.0509040103; PMID:16537482
36. Tolbert WD, Daugherty J, Gao C, Xie Q, Miranti C, Gherardi E, et al. A mechanistic basis for converting a receptor tyrosine kinase agonist to an antagonist. Proc Natl Acad Sci U S A 2007; 104:14592-7; http://dx.doi.org/10. 1073/pnas.0704290104; PMID:17804794
37. Tolbert WD, Daugherty-Holtrop J, Gherardi E, Vande Woude G, Xu HE. Structural basis for agonism and antagonism of hepatocyte growth factor. Proc Natl Acad Sci U S A 2010; 107:13264-9; http://dx.doi.org/10.1073/pnas. 1005183107; PMID:20624990
38. Ohashi K, Marion PL, Nakai H, Meuse L, Cullen JM, Bordier BB, et al. Sustained survival of human hepatocytes in mice: A model for in vivo infection with human hepatitis B and hepatitis delta viruses. Nat Med 2000; 6:327-31; http://dx.doi.org/10.1038/73187; PMID:10700236
39. Carter PJ. Potent antibody therapeutics by design. Nat Rev Immunol 2006; 6:343-57; http://dx.doi.org/10.1038/nri1837; PMID:16622479
40. Tangri S, Mothé BR, Eisenbraun J, Sidney J, Southwood S, Briggs K, et al. Rationally engineered therapeutic proteins with reduced immunogenicity. J Immunol 2005; 174:3187-96; PMID:15749848
41. Abounader R, Ranganathan S, Lal B, Fielding K, Book A, Dietz H, et al. Reversion of human glioblastoma malignancy by U1 small nuclear RNA/ribozyme targeting of scatter factor/hepatocyte growth factor and c-met expression. J Natl Cancer Inst 1999; 91:1548-56; PMID:10491431; http://dx.doi.org/10.1093/ jnci/91.18.1548
42. Smolen GA, Sordella R, Muir B, Mohapatra G, Barmettler A, Archibald H, et al. Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc Natl Acad Sci U S A 2006; 103:2316- 21; http://dx.doi.org/10.1073/pnas.0508776103; PMID:16461907
43. Petrelli A, Circosta P, Granziero L, Mazzone M, Pisacane A, Fenoglio S, et al. Ab-induced ectodomain shedding mediates hepatocyte growth factor receptor down-regulation and hampers biological activity. Proc Natl Acad Sci U S A 2006; 103:5090-5; http://dx.doi.org/10.1073/pnas.0508156103; PMID:16547140
44. Tolgay Ocal I, Dolled-Filhart M, D'Aquila TG, Camp RL, Rimm DL. Tissue microarray-based studies of patients with lymph node negative breast carcinoma show that met expression is associated with worse outcome but is not correlated with epidermal growth factor family receptors. Cancer 2003; 97:1841-8; http://dx.doi.org/10.1002/cncr.11335; PMID:12673709
45. Beck A, Reichert JM, Wurch T. 5th european antibody congress 2009: November 30-december 2, 2009, geneva, switzerland. MAbs 2010; 2:108-28; PMID:20179425; http://dx.doi.org/10.4161/mabs.2.2.11302
46. Greenall SA, Gherardi E, Liu Z, Donoghue JF, Vitali AA, Li Q, et al. Non-agonistic bivalent antibodies that promote c-MET degradation and inhibit tumor growth and others specific for tumor related c-MET. PLoS One 2012; 7:e34658; http://dx.doi.org/10.1371/journal.pone.0034658; PMID:22511956
47. Goetsch L. Antibodies inhibiting c-met dimerization, and therapeutic (anticancer) and diagnostic uses thereof. PCT Int Appl 2009; 2008-EP59026; 2007-301231:175
48. Goetsch L, Wurch T, Bes C. Anti-c-met antibodies for cancer therapy. PCT Int Appl 2011; 2011-EP59139; 2010-791681:119
49. Prat M, Crepaldi T, Pennacchietti S, Bussolino F, Comoglio PM. Agonistic monoclonal antibodies against the Met receptor dissect the biological responses to HGF. J Cell Sci 1998; 111:237-47; PMID:9405310
50. Kong-Beltran M, Stamos J, Wickramasinghe D. The Sema domain of Met is necessary for receptor dimerization and activation. Cancer Cell 2004; 6:75-84; http://dx.doi.org/10.1016/j.ccr.2004.06.013; PMID:15261143
51. Pacchiana G, Chiriaco C, Stella MC, Petronzelli F, De Santis R, Galluzzo M, et al. Monovalency unleashes the full therapeutic potential of the DN-30 anti-Met antibody. J Biol Chem 2010; 285:36149-57; http://dx.doi.org/10.1074/ jbc.M110.134031; PMID:20833723
52. Sharma N, Adjei AA. In the clinic: ongoing clinical trials evaluating c-MET-inhibiting drugs. Ther Adv Med Oncol 2011; 3(Suppl):S37-50; http://dx.doi.org/10.1177/1758834011423403; PMID:22128287
53. Surati M, Patel P, Peterson A, Salgia R. Role of MetMAb (OA-5D5) in c-MET active lung malignancies. Expert Opin Biol Ther 2011; 11:1655-62; http://dx.doi.org/10.1517/14712598.2011.626762; PMID:22047509
54. Belalcazar A, Azaña D, Perez CA, Raez LE, Santos ES. Targeting the Met pathway in lung cancer. Expert Rev Anticancer Ther 2012; 12:519-28; http://dx.doi.org/10.1586/era.12.16; PMID:22500688
55. Catenacci DV, Henderson L, Xiao SY, Patel P, Yauch RL, Hegde P, et al. Durable complete response of metastatic gastric cancer with anti-Met therapy followed by resistance at recurrence. Cancer Discov 2011; 1:573-9; http://dx.doi.org/10.1158/2159-8290.CD-11-0175; PMID:22389872
56. Schwall RH, Adams CW, Zheng Z, Romero M, Mai E, Moffat B, et al. Inhibition of cMet activation by a one-armed antibody. AACR Meeting Abstracts 2004; 2004:327-b-
57. Reyes AE II, Xiang H, Bender B, Haughney P, Oldendorp A, Nijem I, et al. Pharmacokinetics of a novel one-armed antibody to C-met in mice, rats, and monkeys. AAPS PharmSci 2008; 10(S2):587.
58. Institute of Laboratory Animal Resources (U.S.). Guide for the Care and use of Laboratory Animals. Washington, D.C.; Great Britain: National Academy Press, 1996