Tivantinib: A new promising mesenchymal-epithelial transition factor inhibitor in the treatment of hepatocellular carcinoma

Future Oncology

Volumn 9, Issue 2, 2013, Pages 153-165

  Rimassa, Lorenza ^a   Personeni, Nicola ^a   Simonelli, Matteo ^a   Santoro, Armando ^a  

^a HUMANITAS CLINICAL AND RESEARCH CENTER   (Italy)

Author keywords

hepatocellular carcinoma; immunohistochemistry; locally advanced metastatic disease; MET expression; MET inhibitor; second line; tivantinib

Indexed keywords

ERLOTINIB; GEMCITABINE; PLACEBO; SORAFENIB; SUNITINIB; TIVANTINIB;

ABDOMINAL PAIN; ADVANCED CANCER; ANTINEOPLASTIC ACTIVITY; ARTICLE; ASCITES; ASTHENIA; CANCER CELL CULTURE; CANCER CHEMOTHERAPY; CANCER COMBINATION CHEMOTHERAPY; CANCER PATIENT; CANCER SURVIVAL; CHEMOTHERAPY INDUCED ANEMIA; CHEMOTHERAPY INDUCED EMESIS; COLORECTAL CANCER; COUGHING; DECREASED APPETITE; DIARRHEA; DRUG BIOAVAILABILITY; DRUG DOSE COMPARISON; DRUG DOSE ESCALATION; DRUG EFFICACY; DRUG FATALITY; DRUG FEVER; DRUG INDICATION; DRUG MECHANISM; DRUG METABOLISM; DRUG SAFETY; EPITHELIAL MESENCHYMAL TRANSITION; FATIGUE; GASTROINTESTINAL SYMPTOM; HAND FOOT SYNDROME; HUMAN; IMMUNOHISTOCHEMISTRY; IN VITRO STUDY; IN VIVO STUDY; LIVER CELL CARCINOMA; LIVER FAILURE; LUNG NON SMALL CELL CANCER; NAUSEA; NEUTROPENIA; PERIPHERAL EDEMA; PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; PROGRESSION FREE SURVIVAL; SIDE EFFECT; SOLID TUMOR; THROMBOCYTOPENIA; WEIGHT REDUCTION;

ANIMALS; ANTINEOPLASTIC AGENTS; CARCINOMA, HEPATOCELLULAR; CLINICAL TRIALS, PHASE I AS TOPIC; CLINICAL TRIALS, PHASE II AS TOPIC; DRUG EVALUATION, PRECLINICAL; HUMANS; LIVER NEOPLASMS; PYRROLIDINONES; QUINOLINES; TREATMENT OUTCOME;

EID: 84874037058     PISSN: 14796694     EISSN: 17448301     Source Type: Journal    
DOI: 10.2217/fon.12.188     Document Type: Article

References (50)

1. Ann. Surg. Oncol. 19(2), 636-641 (2012).
2. Ashworth T. A case of cancer in which cells similar to those in the tumours were seen in the blood after death. Aust. Med. J. 14(3), 146-149 (1869).
3. Cen P, Ni X, Yang J, Graham DY, Li M. Circulating tumor cells in the diagnosis and management of pancreatic cancer. Biochim. Biophys. Acta 1826(2), 350-356 (2012).
4. Riethdorf S, Fritsche H, Müller V et al. Detection of circulating tumor cells in peripheral blood of patients with metastatic breast cancer: A validation study of the CellSearch system. Clin. Cancer Res. 13(3), 920-928 (2007).
5. Jiao LR, Apostolopoulos C, Jacob J et al. Unique localization of circulating tumor cells in patients with hepatic metastases. J. Clin. Oncol. 27(36), 6160-6165 (2009).
6. Shaw JA, Brown J, Coombes RC et al. Circulating tumor cells and plasma DNA analysis in patients with indeterminate early or metastatic breast cancer. Biomarkers Med. 5(1), 87-91 (2011).
7. Iwanicki-Caron et al. Usefulness of circulating tumor cell detection in pancreatic adenocarcinoma diagnosis. Am. J. Gastro. 108(1), 152-155 (2013).
8. Ren C, Han C, Zhang J et al. Detection of apoptotic circulating tumor cells in advanced pancreatic cancer following 5-fluorouracil chemotherapy. Cancer Biol. Ther. 12(8), 700-706 (2011).
9. De Albuquerque A, Kubisch I, Breier G et al. Multimarker gene analysis of circulating tumor cells in pancreatic cancer patients: A feasibility study. Oncology 82(1), 3-10 (2012).
10. Yu M, Ting DT, Stott SL et al. RNA sequencing of pancreatic circulating tumour cells implicates WNT signalling in metastasis. Nature 487(7408), 510-513 (2012).
11. Rhim AD, Mirek ET, Aiello NM et al. EMT and dissemination precede pancreatic tumor formation. Cell 148(1), 349-361 (2012).
12. Jung K, Fleischhacker M, Rabien A. Cell-free DNA in the blood as a solid tumor biomarker: A critical appraisal of the literature. Clin. Chim. Acta 411(21-22), 1611-1624 (2010).
13. Jahr S, Hentze H, Englisch S et al. DNA fragments in the blood plasma of cancer patients: quantitations and evidence for their origin from apoptotic and necrotic cells. Cancer Res. 61(4), 1659-1665 (2001).
14. Stroun M, Maurice P, Vasioukhin V et al. The origin and mechanism of circulating DNA. Ann. NY Acad. Sci. 906, 161-168 (2000).
15. Lee TH, Montalvo L, Chrebtow V, Busch MP. Quantitation of genomic DNA in plasma and serum samples: higher concentrations of genomic DNA found in serum than in plasma. Transfusion 41(2), 276-282 (2001).
16. Dabritz J, Preston R, Hanfler J, Oettle H. Follow-up study of Kras mutations in the plasma of patients with pancreatic cancer: correlation with clinical features and carbohydrate antigen 19-9. Pancreas 38(5), 534-541 (2009).
17. Dabritz J, Preston R, Hanfler J, Oettle H. Kras mutations in the plasma correspond to computed tomographic findings in patients with pancreatic cancer. Pancreas 41(2), 323-325 (2012).
18. Chen H, Tu H, Meng ZQ, Chen Z, Wang P, Liu LM. K-ras mutational status predicts poor prognosis in unresectable pancreatic cancer. Eur. J. Surg. Oncol. 36(7), 657-662 (2010).
19. Park JW, Baek IH, Kim YT. Preliminary study analyzing the methylated genes in the plasma of patients with pancreatic cancer. Scand. J. Surg. 101(1), 38-44 (2012).
20. Liggett T, Melnikov A, Yi QL et al. Differential methylation of cell-free circulating DNA among patients with pancreatic cancer versus chronic pancreatitis. Cancer 116(7), 1674-1680 (2010).
21. Kong X, Du Y, Wang G et al. Detection of differentially expressed microRNAs in serum of pancreatic ductal adenocarcinoma patients: miR-196a could be a potential marker for poor prognosis. Dig. Dis. Sci. 56(2), 602-609 (2010).
22. Wang P, Zhuang L, Zhang J et al. The serum miR-21 level serves as a predictor for the chemosensitivity of advanced pancreatic cancer, and miR-21 expression confers chemoresistance by targeting FasL. Mol. Oncol. doi:10.1016/j.molonc.2012.10.011 (2012) (Epub ahead of print).
23. Bauer AS, Keller A, Costello E et al. Diagnosis of pancreatic ductal adenocarcinoma and chronic pancreatitis by measurement of microRNA abundance in blood and tissue. PLoS One 7(4), e34151 (2012).
24. Santoro A, Simonelli M, Rodriguez-Lope C et al. A Phase-1b study of tivantinib (ARQ 197) in adult patients with hepatocellular carcinoma and cirrhosis. Br. J. Cancer 108(1), 21-24 (2013).
25. Goldman JW, Laux I, Chai F et al. Phase 1 dose-escalation trial evaluating the combination of the selective MET (mesenchymal-epithelial transition factor) inhibitor tivantinib (ARQ 197) plus erlotinib. Cancer 118(23), 5903-5911 (2012).
26. Adjei AA, Sosman JA, Dy GK et al. A Phase I dose-escalation trial evaluating ARQ 197 administered in combination with sorafenib in adult patients (pts) with advanced solid tumors. Presented at: 46th American Society of Clinical Oncology Annual Meeting. Chicago, IL, USA, 4-8 June 2010 (Abstract 3024).
27. Engelman JA, Zejnullahu K, Mitsudomi T et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 316, 1039-1043 (2007).
28. Martel R, Puzanov I, When WM et al. Safety and efficacy of MET inhibitor tivantinib (ARQ 197) combined with sorafenib in patients (pts) with hepatocellular carcinoma (HCC) from a Phase I study. Presented at: 48th American Society of Clinical Oncology Annual Meeting. Chicago, IL, USA, 1-5 June 2012 (Abstract 4117).
29. Means-Powell JA, Adjei AA, Puzanov I et al. Safety and efficacy of MET inhibitor tivantinib (ARQ 197) combined with sorafenib in patients (pts) with NRAS wildtype or mutant melanoma from a Phase I study. Presented at: 48th American Society of Clinical Oncology Annual Meeting. Chicago, IL, USA, 1-5 June 2012 (Abstract 8519).
30. Puzanov I, Sosman JA, Santoro A et al. Safety and efficacy of MET inhibitor tivantinib (ARQ 197) combined with sorafenib in patients (pts) with renal cell carcinoma (RCC) from a Phase I study. Presented at: 48th American Society of Clinical Oncology Annual Meeting. Chicago, IL, USA, 1-5 June 2012 (Abstract 4545).
31. Camacho LH, Pant S, Saleh MN et al. Phase Ib results of cMET inhibitor ARQ 197 in combination with gemcitabine in a cohort of patients (pts) with advanced breast, ovarian, and uterine tumors. Presented at: 47th American Society of Clinical Oncology Annual Meeting. Chicago, IL, USA, 3-7 June 2011 (Abstract 3077).
32. Camacho LH, Bendell JC, Pant S et al. Phase 1b Results of cMET inhibitor Tivantinib (ARQ 197) in combination with Gemcitabine in a cohort of patients with advanced thoracic tumors. Presented at: 14th World Conference on Lung Cancer. Amsterdam RAI, The Netherlands, 3-7 July 2011 (Abstract).
33. Santoro A, Rimassa L, Borbath I et al. Tivantinib for second-line treatment of advanced hepatocellular carcinoma: A randomised, placebo-controlled Phase 2 study. Lancet Oncol. 14(1), 55-63 (2013).
34. Eisenhauer EA, Therasse P, Bogaerts J et al. New response evaluation criteria in solid tumours: revised RECIST guideline (version 1.1). Eur. J. Cancer 45(2), 228-247 (2009).
35. Cappuzzo F, Marchetti A, Skokan M et al. Increased MET gene copy number negatively affects survival of surgically resected nonsmall-cell lung cancer patients. J. Clin. Oncol. 27, 1667-1674 (2009).
36. 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. 29(24), 3307-3315 (2011).
37. Rodig S, Sequist LV, Schiller JH et al. An exploratory biomarker analysis evaluating the effect of the cMET inhibitor tivantinib (ARQ 197) and erlotinib in NSCLC patients in a randomized, double-blinded Phase 2 study. Presented at: 103rd American Association for Cancer Research Annual Meeting. Chicago, IL, USA, 31 March-4 April 2012 (Abstract 1729).
38. Ma PC, Jagadeeswaran R, Jagadeesh S et al. Functional expression and mutations of cMet and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer. Cancer Res. 65(4), 1479-1488 (2005).
39. Eng C, Bessudo A, Gabrail N et al. Phase I/II study of tivantinib (ARQ 197), irinotecan and cetuximab in patients with KRAS wild-type, previously treated, metastatic colorectal cancer. Presented at: 14th World Congress on Gastrointestinal Cancer. Barcelona, Spain, 27-30 June 2012 (Abstract PD0018).
40. Inno A, Di Salvatore M, Cenci T et al. Is there a role for IGF1R and cMET pathways in resistance to cetuximab in metastatic colorectal cancer? Clin. Colorectal Cancer 10(4), 325-332 (2011).
41. Pan BS, Chan GK, Chenard M et al. MK2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated cMet receptor. Cancer Res. 70(4), 1524-1533 (2010).
42. You H, Ding W, Dang H, Jiang Y, Rountree CB. CMet represents a potential therapeutic target for personalized treatment in hepatocellular carcinoma. Hepatology 54(3), 879-889 (2011).
43. Oliner KS, Tang R, Anderson A et al. Evaluation of MET pathway biomarkers in a Phase II study of rilotumumab (R, AMG 102) or placebo (P) in combination with epirubicin, cisplatin, and capecitabine (ECX) in patients (pts) with locally advanced or metastatic gastric (G) or esophagogastric junction (EGJ) cancer. Presented at: 2012 American Society of Clinical Oncolocy Annual Meeting. Chicago, IL, USA, 1-5 June 2012 (Abstract 4005).
44. Pozner-Moulis S, Cregger M, Camp RL, Rimm DL. Antibody validation by quantitative analysis of protein expression using expression of Met in breast cancer as a model. Lab. Invest. 87(3), 251-260 (2007).
45. Kondo S, Ojima H, Tsuda H et al. Clinical impact of cMet expression and its gene amplification in hepatocellular carcinoma. Int. J. Clin. Oncol. doi: 10.1007/s10147-011-0361-95 (2012) (Epub ahead of print).
46. Perera T, Lavrijssen T, Janssens B et al. JNJ38877605: A selective Met kinase inhibitor inducing regression of Met-driven tumor models. Presented at: 99th American Association for Cancer Research Annual Meeting. Philadelphia, PA, USA, 11-15 April 2008 (Abstract 4837).
47. Verslype C, Cohn AL, Kelley RK et al. Activity of cabozantinib (XL184) in hepatocellular carcinoma: results from a Phase II randomized discontinuation trial (RDT). Presented at: 2012 Gastrointestinal Cancers Symposium. San Francisco, CA, USA, 19-21 January 2012 (Abstract 4007).
48. Personeni N, Bozzarelli S, Pressiani T et al. Usefulness of alpha-fetoprotein response in patients treated with sorafenib for advanced hepatocellular carcinoma. J. Hepatol. 57(1), 101-107 (2012).
49. Qian F, Engst S, Yamaguchi K et al. Inhibition of tumor cell growth, invasion, and metastasis by EXEL2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases. Cancer Res. 69(20), 8009-8016 (2009).
50. Huynh H, Ong R, Soo KC. Foretinib demonstrates anti-tumor activity and improves overall survival in preclinical models of hepatocellular carcinoma. Angiogenesis 15(1), 59-70 (2012).