Seminars in clinical pharmacology: An introduction to met inhibitors for the medical oncologist

Annals of Oncology

Volumn 24, Issue 1, 2013, Pages 14-20

  Fasolo, A ^a   Sessa, C ^a,b   Gianni, L ^a   Broggini, M ^c  

^a SAN RAFFAELE HOSPITAL   (Italy)

^b ONCOLOGY INSTITUTE OF SOUTHERN SWITZERLAND   (Switzerland)

^c MARIO NEGRI INSTITUTE FOR PHARMACOLOGICAL RESEARCH   (Italy)

Author keywords

Inhibitors; MET; MET receptor; Molecule targeted treatment; Target

Indexed keywords

ABIRATERONE; ANTINEOPLASTIC AGENT; BEVACIZUMAB; CABOZANTINIB; CAPECITABINE; CETUXIMAB; CISPLATIN; CRIZOTINIB; DOCETAXEL; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; EPIRUBICIN; ERLOTINIB; FICLATUZUMAB; FLUOROURACIL; FOLINIC ACID; FORETINIB; MOTESANIB; ONARTUZUMAB; OXALIPLATIN; PLACEBO; RILOTUMUMAB; SCATTER FACTOR RECEPTOR; SCATTER FACTOR RECEPTOR INHIBITOR; TEMOZOLOMIDE; TIVANTINIB; UNCLASSIFIED DRUG;

ADVANCED CANCER; ALANINE AMINOTRANSFERASE BLOOD LEVEL; ANOREXIA; ANTINEOPLASTIC ACTIVITY; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; BONE METASTASIS; CANCER PROGNOSIS; CANCER RESEARCH; CANCER RESISTANCE; CANCER STAGING; CASTRATION RESISTANT PROSTATE CANCER; CHEMOTHERAPY INDUCED EMESIS; CLINICAL PHARMACOLOGY; DECREASED APPETITE; DIARRHEA; DIGESTIVE SYSTEM CANCER; DRUG CYTOTOXICITY; DRUG DOSE ESCALATION; DRUG DOSE REDUCTION; DRUG EFFICACY; DRUG ERUPTION; DRUG HALF LIFE; DRUG INTERMITTENT THERAPY; DRUG POTENTIATION; DRUG RECEPTOR BINDING; DRUG RESEARCH; DRUG RESPONSE; DRUG TARGETING; DRUG TOLERABILITY; DRUG WITHDRAWAL; EDEMA; ESOPHAGUS CANCER; FATIGUE; GASTROESOPHAGEAL CANCER; GLIOBLASTOMA; HAND FOOT SYNDROME; HUMAN; HYPERTENSION; LIVER CELL CARCINOMA; LUNG NON SMALL CELL CANCER; MELANOMA; METASTASIS; METASTASIS INHIBITION; MOLECULAR INTERACTION; MOLECULARLY TARGETED THERAPY; MYALGIA; NAUSEA; NONHUMAN; OVARY CANCER; OVERALL SURVIVAL; PANCREAS CANCER; PERIPHERAL EDEMA; PHARMACODYNAMICS; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PHENOTYPE; PRIORITY JOURNAL; PROGRESSION FREE SURVIVAL; PROTEIN EXPRESSION; RANDOMIZED CONTROLLED TRIAL (TOPIC); RECEPTOR UPREGULATION; RECOMMENDED DRUG DOSE; REVIEW; SIDE EFFECT; SIGNAL TRANSDUCTION; SOLID TUMOR; STOMACH CANCER; THYROID MEDULLARY CARCINOMA; TREATMENT DURATION; TRIPLE NEGATIVE BREAST CANCER;

EID: 84871592260     PISSN: 09237534     EISSN: 15698041     Source Type: Journal    
DOI: 10.1093/annonc/mds520     Document Type: Review

References (41)

1. Comoglio PM, Giordano S, Trusolino L. Drug development of MET inhibitors: targeting oncogene addiction and expedience. Nat Rev Drug Discov 2008; 7: 504-516.
2. Trusolino L, Bertotti A, Comoglio PM. MET signalling: principles and functions in development, organ regeneration and cancer. Nat Rev Mol Cell Biol 2010; 11: 834-848.
3. Liu X, Newton RC, Scherle PA. Development of c-MET pathway inhibitors. Expert Opin Investig Drugs 2011; 20: 1225-1241.
4. Yap TA, De Bono JS. Targeting the HGF/c-met axis: State of play. Mol Cancer Ther 2010; 9: 1077-1079.
5. Stella GM, Benvenuti S, Comoglio PM. Targeting the MET oncogene in cancer and metastases. Expert Opin Investig Drugs 2010; 19: 1381-1394.
6. Benvenuti S, Comoglio PM. The MET receptor tyrosine kinase in invasion and metastasis. J Cell Physiol 2007; 213: 316-325.
7. Benvenuti S, Lazzari L, Arnesano A et al. Ron kinase transphosphorylation sustains MET oncogene addiction. Cancer Res 2011; 71: 1945-1955.
8. Engelman JA, Zejnullahu K, Mitsudomi T et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 2007; 316: 1039-1043.
9. Turke AB, Zejnullahu K, Wu YL et al. Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC. Cancer Cell 2010; 17: 77-88.
10. Munshi N, Jeay S, Li Y et al. ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity. Mol Cancer Ther 2010; 9: 1544-1553.
11. Eathiraj S, Palma R, Volckova E et al. Discovery of a novel mode of protein kinase inhibition characterized by the mechanism of inhibition of human mesenchymalepithelial transition factor (c-Met) protein autophosphorylation by ARQ 197. J Biol Chem 2011; 286: 20666-20676.
12. Previdi S, Abbadessa G, Dalo F et al Breast cancer-derived bone metastasis can be effectively reduced through specific c-MET inhibitor tivantinib (ARQ 197) and shRNA c-MET knockdown. Mol Cancer Ther 2011; 11: 214-223.
13. Yakes FM, Chen J, Tan J et al Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth Mol Cancer Ther 2011; 10: 2298-2308.
14. Sennino B, Naylor RM, Tabruyn SP et al Reduction of tumor invasiveness and metastasis and prolongation of survival of RIP-Tag2 mice after inhibition of VEGFR plus c-Met by XL184. Mol Cancer Ther 2009; 8: A13.
15. Ebos JM, Lee CR, Cruz-Munoz W et al. Accelerated metastasis after short-term treatment with a potent inhibitor of tumor angiogenesis. Cancer Cell 2009; 15: 391-395.
16. Paez-Ribes M, Allen E, Hudock J et al. Antiangiogenic therapy elicits malignant progression of tumors to increased local invasion and distant metastasis. Cancer Cell 2009; 15: 220-231.
17. Kataoka Y, Mukohara T, Tomioka H et al. Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks. Invest New Drugs 2012; 4: 1352-1360.
18. Zillhardt M, Park SM, Romero IL et al. Foretinib (GSK1363089), an orally available multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces anoikis, and impairs ovarian cancer metastasis. Clin Cancer Res 2011; 17: 4042-4051.
19. Kwak EL, Bang Y-J, Camidge DR et al. Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. N Engl J Med 2010; 363: 1693-1703.
20. Tanizaki J, Okamoto I, Okamoto K et al. MET tyrosine kinase inhibitor crizotinib (PF-02341066) shows differential antitumor effects in non-small cell lung cancer according to MET alterations. J Thorac Oncol 2011; 6: 1624-1631.
21. Martens T, Schmidt N-O, Eckerich C et al. A novel one-armed anti-c-Met antibody inhibits glioblastoma growth in vivo. Clin Cancer Res 2006; 12: 6144-6152.
22. Jin H, Yang R, Zheng Z et al. MetMAb, the one-armed 5D5 anti-c-Met antibody, inhibits orthotopic pancreatic tumor growth and improves survival. Cancer Res 2008; 68: 4360-4368.
23. Jun HT, Sun J, Rex K 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 2007; 13: 6735-6742.
24. Burgess TL, Sun J, Meyer S et al. Biochemical characterization of AMG 102: a neutralizing, fully human monoclonal antibody to human and nonhuman primate hepatocyte growth factor. Mol Cancer Ther 2010; 9: 400-409.
25. Yap TA, Olmos D, Brunetto AT et al. Phase I trial of a selective c-MET inhibitor ARQ 197 incorporating proof of mechanism pharmacodynamic studies. J Clin Oncol 2011; 29: 1271-1279.
26. Sequist LV, Von Pawel J, Garmey EG et al. Randomized phase II study of erlotinib plus tivantinib versus erlotinib plus placebo in previously treated non-small-cell lung cancer. J Clin Oncol 2011; 29: 3307-3315.
27. Scagliotti GV, Novello S, Schiller JH et al. Rationale and design of MARQUEE: a phase III, randomized, double-blind study of tivantinib plus erlotinib versus placebo plus erlotinib in previously treated patients with locally advanced or metastatic, nonsquamous, non-small-cell lung cancer. Clin Lung Cancer 2012; 5: 391-395.
28. Rimassa L, Porta C, Borbath I et al. Tivantinib (ARQ 197) versus placebo in patients (Pts) with hepatocellular carcinoma (HCC) who failed one systemic therapy: Results of a randomized controlled phase II trial (RCT). J Clin Oncol. 2012; 30: 240.
29. Salgia R, Sherman S, Hong DS et al. A phase I study of XL184, a RET, VEGFR2, and MET kinase inhibitor, in patients ( pts) with advanced malignancies, including pts with medullary thyroid cancer (MTC). ASCO Meeting Abstr 2008; 26: 3522.
30. Buckanovich RJ, Berger R, Sella A et al. Activity of cabozantinib (XL184) in advanced ovarian cancer patients ( pts): results from a phase II randomized discontinuation trial (RDT). ASCO Meeting Abstr 2011; 29: 5008.
31. Hussain M, Smith MR, Sweeney C et al. Cabozantinib (XL184) in metastatic castration-resistant prostate cancer (mCRPC): results from a phase II randomized discontinuation trial. ASCO Meeting Abstr 2011; 29: 4516.
32. Eder JP, Shapiro GI, Appleman LJ et al. A phase I study of foretinib, a multitargeted inhibitor of c-Met and vascular endothelial growth factor receptor 2. Clin Cancer Res 2010; 16: 3507-3516.
33. Salgia R, Peterson A, Eppler S et al. 411 POSTER A phase I, open-label, doseescalation 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. Eur J Cancer Suppl 2008; 6: 129.
34. Catenacci DVT, Henderson L, Xiao S-Y et al. Durable complete response of metastatic gastric cancer with anti-Met therapy followed by resistance at recurrence. Cancer Discov 2011; 1: 573-579.
35. Gordon MS, Sweeney CS, Mendelson DS et al. Safety, pharmacokinetics, and pharmacodynamics of AMG 102, a fully human hepatocyte growth factorneutralizing monoclonal antibody, in a first-in-human study of patients with advanced solid tumors. Clin Cancer Res 2010; 16: 699-710.
36. Rosen PJ, Sweeney CJ, Park DJ et al. A phase Ib study of AMG 102 in combination with bevacizumab or motesanib in patients with advanced solid tumors. Clin Cancer Res 2010; 16: 2677-2687.
37. Iveson T, Donehower RC, Davidenko I et al. 6504 ORAL Safety and efficacy of epirubicin, cisplatin, and capecitabine (ECX) plus rilotumumab (R) as first-line treatment for unresectable locally advanced (LA) or metastatic (M) gastric or esophagogastric junction (EGJ) adenocarcinoma. Eur J cancer 2011; 47: S443.
38. Patnaik A, Weiss GJ, Papadopoulos K et al. Phase I study of SCH 900105 (SC), an anti-hepatocyte growth factor (HGF) monoclonal antibody (MAb), as a single agent and in combination with erlotinib (E) in patients (pts) with advanced solid tumors. ASCO Meeting Abstr 2010; 28: 2525.
39. Spigel DR, Edelman MJ, Mok T et al. The MetLUNG study: a randomized, double-blind, phase III study of onartuzumab (MetMAb) plus erlotinib versus placebo plus erlotinib in patients with advanced, MET-positive non-small cell lung cancer (NSCLC). ASCO Meeting Abstr 2012; 30: TPS7616.
40. Rodig SJ, Shapiro GI. Crizotinib, a small-molecule dual inhibitor of the c-Met and ALK receptor tyrosine kinases. Curr Opin Investig Drugs 2010; 11: 1477-1490.
41. Mok T, Tan E, Park K et al. Randomized phase II study of ficlatuzumab (formerly AV-299), an anti-hepatocyte growth factor (HGF) monoclonal antibody (MAb) in combination with gefitinib (G) in Asian patients (pts) with NSCLC. J Clin Oncol 2011; 29: TSP213.