Phase 1 dose-escalation trial evaluating the combination of the selective MET (mesenchymal-epithelial transition factor) inhibitor tivantinib (ARQ 197) plus erlotinib

Cancer

Volumn 118, Issue 23, 2012, Pages 5903-5911

  Goldman, Jonathan W ^a   Laux, Isett ^a   Chai, Feng ^b   Savage, Ronald E ^b   Ferrari, Dora ^b   Garmey, Edward G ^b   Just, Richard G ^c   Rosen, Lee S ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b ARQULE INC   (United States)

^c Pacific Oncology and Hematology Associates   (United States)

Author keywords

ARQ 197; carcinoma; erlotinib; nonsmall cell lung cancer; proto oncogene proteins c MET

Indexed keywords

EPIDERMAL GROWTH FACTOR RECEPTOR; ERLOTINIB; SCATTER FACTOR RECEPTOR; TIVANTINIB;

ABDOMINAL PAIN; ADULT; AGED; ANEMIA; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BRADYCARDIA; CANCER COMBINATION CHEMOTHERAPY; CANCER SURVIVAL; CLINICAL ARTICLE; COLORECTAL CANCER; CYP2C19 GENE; DEHYDRATION; DIARRHEA; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DOSE ESCALATION; DRUG DOSE INCREASE; DRUG EFFICACY; DRUG ERUPTION; DRUG HALF LIFE; DRUG POTENTIATION; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG TARGETING; DRUG TOLERABILITY; EGFR GENE; EPITHELIAL MESENCHYMAL TRANSITION; FAINTNESS; FATIGUE; FEMALE; GENE; GENOTYPE; HEAD AND NECK CANCER; HOSPITAL PATIENT; HUMAN; LEUKOPENIA; LUNG NON SMALL CELL CANCER; MALE; MAXIMUM PLASMA CONCENTRATION; MAXIMUM TOLERATED DOSE; MET GENE; MULTIPLE CYCLE TREATMENT; NAUSEA; NEUTROPENIA; ONCOGENE; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; PROGRESSION FREE SURVIVAL; RECOMMENDED DRUG DOSE; SICK SINUS SYNDROME; SINUS BRADYCARDIA; SOLID TUMOR; THROMBOCYTOPENIA; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADULT; AGED; AGED, 80 AND OVER; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; CARCINOMA, NON-SMALL-CELL LUNG; FEMALE; HUMANS; LUNG NEOPLASMS; MALE; MIDDLE AGED; NEOPLASMS; PROTO-ONCOGENE PROTEINS C-MET; PYRROLIDINONES; QUINAZOLINES; QUINOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR;

EID: 84869499839     PISSN: 0008543X     EISSN: 10970142     Source Type: Journal    
DOI: 10.1002/cncr.27575     Document Type: Article

References (31)

1. Shepherd FA, Rodrigues Pereira J, Ciuleanu T, et al. National Cancer Institute of Canada Clinical Trials Group. Erlotinib in previously treated non-small-cell lung cancer. N Engl J Med. 2005; 353: 123-132. (Pubitemid 41058344)
2. Moore MJ, Goldstein D, Hamm J, et al. National Cancer Institute of Canada Clinical Trials Group. Erlotinib plus gemcitabine compared with gemcitabine alone in patients with advanced pancreatic cancer: a phase III trial of the National Cancer Institute of Canada Clinical Trials Group. J Clin Oncol. 2007; 25: 1960-1966. (Pubitemid 46972777)
3. Lynch TJ, Bell DW, Sordella R, et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med. 2004; 350: 2129-2139. (Pubitemid 38637993)
4. Paez JG, Janne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science. 2004; 304: 1497-1500. (Pubitemid 38720929)
5. Tsao MS, Sakurada A, Cutz JC, et al. Erlotinib in lung cancer-molecular and clinical predictors of outcome. N Engl J Med. 2005; 353: 133-144. (Pubitemid 41058345)
6. Zhu CQ, da Cunha Santos G, Ding K, et al. National Cancer Institute of Canada Clinical Trials Group Study BR.21. Role of KRAS and EGFR as biomarkers of response to erlotinib in National Cancer Institute of Canada Clinical Trials Group Study BR.21. J Clin Oncol. 2008; 26: 4268-4275.
7. Kobayashi S, Boggon TJ, Dayaram T, et al. EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med. 2005; 352: 786-792. (Pubitemid 40271173)
8. Balak MN, Gong Y, Riely GJ, et al. Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors. Clin Cancer Res. 2006; 12: 6494-6501. (Pubitemid 44799723)
9. Bean J, Brennan C, Shih JY, 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 U S A. 2007; 104: 20932-20937.
10. 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. (Pubitemid 46799492)
11. Yano S, Wang W, Li Q, et al. Hepatocyte growth factor induces gefitinib resistance of lung adenocarcinoma with epidermal growth factor receptor-activating mutations. Cancer Res. 2008; 68: 9479-9487.
12. Tang Z, Du R, Jiang S, et al. Dual MET-EGFR combinatorial inhibition against T790M-EGFR-mediated erlotinib-resistant lung cancer. Br J Cancer. 2008; 99: 911-922.
13. 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.
14. 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.
15. Rosen LS, Senzer N, Mekhail T, et al. A phase I dose-escalation study of Tivantinib (ARQ 197) in adult patients with metastatic solid tumors. Clin Cancer Res. 2011; 17: 7754-7764.
16. Abounader R, Reznik T, Colantuoni C, Martinez-Murillo F, Rosen EM, Laterra J,. Regulation of c-Met-dependent gene expression by PTEN. Oncogene. 2004; 23: 9173-9182. (Pubitemid 40069687)
17. Furge KA, Zhang YW, Vande Woude GF,. Met receptor tyrosine kinase: enhanced signaling through adapter proteins. Oncogene. 2000; 19: 5582-5589.
18. Herynk MH, Zhang J, Parikh NU, Gallick GE,. Activation of Src by c-Met overexpression mediates metastatic properties of colorectal carcinoma cells. J Exp Ther Oncol. 2007; 6: 205-217. (Pubitemid 46789721)
19. Jankowski K, Kucia M, Wysoczynski M, et al. Both hepatocyte growth factor (HGF) and stromal-derived factor-1 regulate the metastatic behavior of human rhabdomyosarcoma cells, but only HGF enhances their resistance to radiochemotherapy. Cancer Res. 2003; 63: 7926-7935. (Pubitemid 37466729)
20. Jücker M, Günther A, Gradl G, et al. The Met/hepatocyte growth factor receptor (HGFR) gene is overexpressed in some cases of human leukemia and lymphoma. Leuk Res. 1994; 18: 7-16.
21. Ma PC, Tretiakova MS, MacKinnon AC, et al. Expression and mutational analysis of MET in human solid cancers. Genes Chromosomes Cancer. 2008; 47: 1025-1037.
22. Rygaard K, Nakamura T, Spang-Thomsen M,. Expression of the proto-oncogenes c-met and c-kit and their ligands, hepatocyte growth factor/scatter factor and stem cell factor, in SCLC cell lines and xenografts. Br J Cancer. 1993; 67: 37-46. (Pubitemid 23034921)
23. Welch WC, Kornblith PL, Michalopoulos GK, et al. Hepatocyte growth factor (HGF) and receptor (c-met) in normal and malignant astrocytic cells. Anticancer Res. 1999; 19: 1635-1640. (Pubitemid 29392716)
24. Guzmán-Ramírez N, Völler M, Wetterwald A, et al. In vitro propagation and characterization of neoplastic stem/progenitor-like cells from human prostate cancer tissue. Prostate. 2009; 69: 1683-1693.
25. Cappuzzo F, Marchetti A, Skokan M, et al. Increased MET gene copy number negatively affects survival of surgically resected non-small-cell lung cancer patients. J Clin Oncol. 2009; 27: 1667-1674.
26. Go H, Jeon YK, Park HJ, Sung SW, Seo JW, Chung DH,. High MET gene copy number leads to shorter survival in patients with non-small cell lung cancer. J Thorac Oncol. 2010; 5: 305-313.
27. Beau-Faller M, Ruppert AM, Voegeli AC, et al. MET gene copy number in non-small cell lung cancer: molecular analysis in a targeted tyrosine kinase inhibitor naïve cohort. J Thorac Oncol. 2008; 3: 331-339. (Pubitemid 351489471)
28. Cappuzzo F, Jänne PA, Skokan M, et al. MET increased gene copy number and primary resistance to gefitinib therapy in non-small-cell lung cancer patients. Ann Oncol. 2009; 20: 298-304.
29. 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.
30. Sequist LV, von Pawel J, Garmey EG, et al. Randomzied 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.
31. Sandler A, Schiller JH, Hirsh V, et al. A phase III, randomized, double-blind, placebo-controlled study of erlotinib plus ARQ 197 versus erlotinib plus placebo in previously treated subjects with locally advanced or metastatic, nonsquamous, non-small cell lung cancer (NSCLC). J Clin Oncol. 2011; 29 (suppl): Abstract TPS217.