A first-in-human study of AMG 208, an oral MET inhibitor, in adult patients with advanced solid tumors

Oncotarget

Volumn 6, Issue 21, 2015, Pages 18693-18706

  Hong, David S ^a   Rosen, Peter ^b   Lockhart, A Craig ^c   Fu, Siqing ^a   Janku, Filip ^a   Kurzrock, Razelle ^a   Khan, Rabia ^a   Amore, Benny ^d   Caudillo, Isaac ^e   Deng, Hongjie ^e   Hwang, Yuying C ^e   Loberg, Robert ^e   Ngarmchamnanrith, Gataree ^e   Beaupre, Darrin M ^e   Lee, Peter ^b  

^a UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

^b Tower Cancer Research Foundation ^*  (United States)

^c WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

^d AMGEN INC   (United States)

^e AMGEN INC   (United States)

Author keywords

First in human; MET; Prostate cancer; Small molecule; Solid tumors

Indexed keywords

AMG 208; ANTINEOPLASTIC AGENT; ASPARTATE AMINOTRANSFERASE; CREATININE; SCATTER FACTOR RECEPTOR; UNCLASSIFIED DRUG; PROTEIN KINASE INHIBITOR; PYRIDAZINE DERIVATIVE; TRIAZOLE DERIVATIVE; TUMOR MARKER;

ACHROMOTRICHIA; ACUTE HEART INFARCTION; ADULT; ADVANCED CANCER; AGED; ANEMIA; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BLADDER CANCER; CANCER OF UNKNOWN PRIMARY SITE; CLINICAL TRIAL; COLON CANCER; CREATININE BLOOD LEVEL; DECREASED APPETITE; DIARRHEA; DRUG DOSE ESCALATION; DRUG EFFICACY; DRUG HALF LIFE; DRUG RESPONSE; DRUG SAFETY; DRUG TOLERABILITY; ESOPHAGUS CANCER; FATIGUE; FEMALE; GALLBLADDER CARCINOMA; HAIR DISEASE; HEAD AND NECK SQUAMOUS CELL CARCINOMA; HUMAN; HYPERGLYCEMIA; HYPERTENSION; HYPOMAGNESEMIA; KIDNEY CANCER; LEUKOPENIA; LUNG EMBOLISM; MAJOR CLINICAL STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; MAXIMUM TOLERATED DOSE; MELANOMA; NAUSEA; NEUTROPENIA; NON SMALL CELL LUNG CANCER; OVARY CANCER; PHARMACODYNAMICS; PROSTATE CANCER; PROTEIN EXPRESSION; QT PROLONGATION; SCATTER FACTOR RECEPTOR GENE; SOLID TUMOR; STOMACH CANCER; THROMBOCYTOPENIA; TREATMENT OUTCOME; UNSPECIFIED SIDE EFFECT; VOMITING; ANTAGONISTS AND INHIBITORS; CHEMICALLY INDUCED; DOSE RESPONSE; FLUORESCENCE IN SITU HYBRIDIZATION; GENETICS; IMMUNOHISTOCHEMISTRY; METABOLIC CLEARANCE RATE; METABOLISM; MIDDLE AGED; NEOPLASMS; ORAL DRUG ADMINISTRATION; PHASE 1 CLINICAL TRIAL; REMISSION; VERY ELDERLY;

ADMINISTRATION, ORAL; ADULT; AGED; AGED, 80 AND OVER; AREA UNDER CURVE; BIOMARKERS, TUMOR; DOSE-RESPONSE RELATIONSHIP, DRUG; FATIGUE; FEMALE; HUMANS; HYPERTENSION; IMMUNOHISTOCHEMISTRY; IN SITU HYBRIDIZATION, FLUORESCENCE; MALE; METABOLIC CLEARANCE RATE; MIDDLE AGED; NAUSEA; NEOPLASMS; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-MET; PYRIDAZINES; REMISSION INDUCTION; TREATMENT OUTCOME; TRIAZOLES;

EID: 84938800976     PISSN: None     EISSN: 19492553     Source Type: Journal    
DOI: 10.18632/oncotarget.4472     Document Type: Article

References (36)

1. Birchmeier C, Birchmeier W, Gherardi E, Vande Woude GF. Met, metastasis, motility and more. Nat Rev Mol Cell Biol. 2003; 4: 915-925.
2. Ma PC, Maulik G, Christensen J, Salgia R. c-Met: structure, functions and potential for therapeutic inhibition. Cancer Metastasis Rev. 2003; 22: 309-325.
3. Gherardi E, Birchmeier W, Birchmeier C, Vande Woude G. Targeting MET in cancer: rationale and progress. Nat Rev Cancer. 2012; 12: 89-103.
4. Tanyi J, Tory K, Rigo Jr J, Nagy B, Papp Z. Evaluation of the tyrosine kinase domain of the Met proto-oncogene in sporadic ovarian carcinomas. Pathol Oncol Res. 1999; 5: 187-191.
5. Tjin EP, Groen RW, Vogelzang I, Derksen PW, Klok MD, Meijer HP, van Eeden S, Pals ST, Spaargaren M. Functional analysis of HGF/MET signaling and aberrant HGF-activator expression in diffuse large B-cell lymphoma. Blood. 2006; 107: 760-768.
6. Moore SR, Persons DL, Sosman JA, Bobadilla D, Bedell V, Smith DD, Wolman SR, Tuthill RJ, Moon J, Sondak VK, Slovak ML. Detection of copy number alterations in metastatic melanoma by a DNA fluorescence in situ hybridization probe panel and array comparative genomic hybridization: a Southwest Oncology Group study (S9431). Clin Cancer Res. 2008; 14: 2927-2935.
7. Nakajima M, Sawada H, Yamada Y, Watanabe A, Tatsumi M, Yamashita J, Matsuda M, Sakaguchi T, Hirao T, Nakano H. The prognostic significance of amplification and overexpression of c-met and c-erb B-2 in human gastric carcinomas. Cancer. 1999; 85: 1894-1902.
8. Ma PC, Jagadeeswaran R, Jagadeesh S, Tretiakova MS, Nallasura V, Fox EA, Hansen M, Schaefer E, Naoki K, Lader A, Richards W, Sugarbaker D, Husain AN, et al. Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer. Cancer Res. 2005; 65: 1479-1488.
9. Di Renzo MF, Olivero M, Giacomini A, Porte H, Chastre E, Mirossay L, Nordlinger B, Bretti S, Bottardi S, Giordano S. Overexpression and amplification of the met/HGF receptor gene during the progression of colorectal cancer. Clin Cancer Res. 1995; 1: 147-154.
10. Di Renzo MF, Olivero M, Martone T, Maffe A, Maggiora P, Stefani AD, Valente G, Giordano S, Cortesina G, Comoglio PM. Somatic mutations of the MET oncogene are selected during metastatic spread of human HNSC carcinomas. Oncogene. 2000; 19: 1547-1555.
11. Linehan WM, Pinto PA, Srinivasan R, Merino M, Choyke P, Choyke L, Coleman J, Toro J, Glenn G, Vocke C, Zbar B, Schmidt LS, Bottaro D, et al. Identification of the genes for kidney cancer: opportunity for disease-specific targeted therapeutics. Clin Cancer Res. 2007; 13: 671s-679s.
12. Bean J, Brennan C, Shih JY, Riely G, Viale A, Wang L, Chitale D, Motoi N, Szoke J, Broderick S, Balak M, Chang WC, Yu CJ, 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. 2007; 104: 20932-20937.
13. Engelman J, Zejnullahu K, Mitsudomi T, Song Y, Hyland C, Park JO, Lindeman N, Gale CM, Zhao X, Christensen J, Kosaka T, Holmes AJ, Rogers AM, et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science. 2007; 316: 1039-1043.
14. Sennino B, Ishiguro-Oonuma T, Wei Y, Naylor RM, Williamson CW, Bhagwandin V, Tabruyn SP, You W-K, Chapman HA, Christensen JG, Aftab DT, McDonald DM. Suppression of tumor invasion and metastasis by concurrent inhibition of c-Met and VEGF signaling in pancreatic neuroendocrine tumors. Cancer Discovery. 2012; 2: 270-287.
15. Smith DC, Smith MR, Sweeney C, Elfiky AA, Logothetis C, Corn PG, Vogelzang NJ, Small EJ, Harzstark AL, Gordon MS, Vaishampayan UN, Haas NB, Spira AI, et al. Cabozantinib in patients with advanced prostate cancer: results of a phase II randomized discontinuation trial. J Clin Oncol. 2013; 31: 412-419.
16. Elisei R, Schlumberger MJ, Müller SP, Schöffski P, Brose MS, Shah MH, Licitra L, Jarzab B, Medvedev V, Kreissl MC, Niederle B, Cohen EE, Wirth LJ, et al. Cabozantinib in progressive medullary thyroid cancer. J Clin Oncol. 2013; 31: 3639-3646.
17. Choueiri TK, Vaishampayan U, Rosenberg JE, Logan TF, Harzstark AL, Bukowski RM, Rini BI, Srinivas S, Stein MN, Adams LM, Ottesen LH, Laubscher KH, Sherman L, et al. Phase II and biomarker study of the dual MET/VEGFR2 inhibitor foretinib in patients with papillary renal cell carcinoma. J Clin Oncol. 2013; 31: 181-186.
18. Exelixis. Exelixis Announces Results from the COMET-1 Phase 3 Pivotal Trial of Cabozantinib in Men with Metastatic Castration-Resistant Prostate Cancer. News Release, September 2, 2014. Available at: http://ir.exelixis.com/phoenix.zhtml?c=120923&p=irolnewsArticle&ID=1962549. Accessed April 10, 2015.
19. Liu T, Mendes DE, Berkman CE. From AR to c-Met: Androgen deprivation leads to a signaling pathway switch in prostate cancer cells. Int J Oncol. 2013; 43: 1125-1130.
20. Lennerz JK, Kwak EL, Ackerman A, Michael M, Fox SB, Bergethon K, Lauwers GY, Christensen JG, Wilner KD, Haber DA, Salgia R, Bang YJ, Clark JW, et al. MET amplification identifies a small and aggressive subgroup of esophagogastric adenocarcinoma with evidence of responsiveness to crizotinib. J Clin Oncol. 2011; 29: 4803-4810.
21. Forde PM, Kelly RJ. Genomic alterations in advanced esophageal cancer may lead to subtype-specific therapies. Oncologist. 2013; 18: 823-832.
22. Salgia R, Patel P, Bothos J, Yu W, Eppler S, Hegde P, Bai S, Kaur S, Nijem I, Catenacci DV, Peterson A, Ratain MJ, Polite B, et al. Phase I dose-escalation study of onartuzumab as a single agent and in combination with bevacizumab in patients with advanced solid malignancies. Clin Cancer Res. 2014; 20: 1666-1675.
23. Gomez-Martin C, Plaza JC, Pazo-Cid R, Salud A, Pons F, Fonseca P, Leon A, Alsina M, Visa L, Rivera F, Galan MC, Del Valle E, Vilardell F, et al. Level of HER2 gene amplification predicts response and overall survival in HER2-positive advanced gastric cancer treated with trastuzumab. J Clin Oncol. 2013; 31: 4445-4452.
24. Burtness B, Bauman JE, Galloway T. Novel targets in HPV-negative head and neck cancer: overcoming resistance to EGFR inhibition. Lancet Oncol. 2013; 14: e302-e309.
25. Katayama R, Aoyama A, Yamori T, Qi J, Oh-hara T, Song Y, Engelman JA, Fujita N. Cytotoxic activity of tivantinib (ARQ 197) is not due solely to c-MET inhibition. Cancer Res. 2013; 73: 3087-3096.
26. Goldman JW, Laux I, Chai F, Savage RE, Ferrari D, Garmey EG, Just RG, Rosen LS. Phase 1 dose-escalation trial evaluating the combination of the selective MET (mesenchymal-epithelial transition factor) inhibitor tivantinib (ARQ 197) plus erlotinib. Cancer. 2012; 118: 5903-5911.
27. Strickler JH, LoRusso P, Yen C-J, Lin C-C, Kang Y-K, Kaminker P, Ansell P, Bhathena A, Wong S, Dudley MW, Naumovski L, Ramanathan RK. Phase 1, open-label, dose-escalation, and expansion study of ABT-700, an anti-C-met antibody, in patients (pts) with advanced solid tumors. J Clin Oncol. 2014; 32: 5s (suppl; abstr 2507).
28. Hong DS, LoRusso P, Hamid O, Beaupre DM, Janku F, Khan R, Kittaneh M, Loberg RD, Amore B, Caudillo I, Hwang YC, Tang R, Ngarmchamnanrith G, et al. First-inhuman study of AMG 337, a highly selective oral inhibitor of MET, in adult patients (pts) with advanced solid tumors. J Clin Oncol. 2014; 32: 5s (suppl; abstr 2508).
29. Bang Y-J, Su W-C, Nam D-H, Lim W-T, Bauer TM, Brana I, Poon RT-P, Hong DS, Lin C-C, Peng B, Zhang Y, Zhao S, Kumar A, et al. Phase I study of the safety and efficacy of INC280 in patients with advanced MET-dependent solid tumors. J Clin Oncol. 2014; 32: 5s (suppl; abstr 2520^).
30. Falchook GS, Hong DS, Amin HM, Fu S, Piha-Paul SA, Janku F, Granda JG, Zheng H, Klevesath MB, Köhler K, Bladt F, Johne A, Kurzrock R. Results of the first-in-human phase I trial assessing MSC2156119J (EMD 1214063), an oral selective c-Met inhibitor, in patients (pts) with advanced solid tumors. J Clin Oncol. 2014; 32: 5s: (suppl; abstr 2521^).
31. Angevin E, Spitaleri G, Hollebecque A, De Pas T, Soria J-C, Harnois M, Mazuir F, Assadourian S, De Marinis F. A first-in-human (FIH) phase I study of SAR125844, a novel selective MET kinase inhibitor, in patients (pts) with advanced solid tumors: Dose escalation results. J Clin Oncol. 2014; 32: 5s (suppl; abstr 2506).
32. Gan HK, Lickliter J, Millward M, Gu Y, SU W, Frigault M, Qi C, MU H. First-in-human phase I study of a selective c-Met inhibitor volitinib (HMP504/AZD6094) in patients with advanced solid tumors. J Clin Oncol. 2014; 32: 5s (suppl; abstr 11111).
33. Schmidt Slørdahl T, Denayer T, Helen Moen S, Standal T, Børset M, Ververken C, Baade Rø T. Anti-c-MET nanobody - a new potential drug in multiple myeloma treatment. Eur J Haematol. 2013; 91: 399-410.
34. Ye L, Ou X, Tian Y, Yu B, Luo Y, Feng B, Lin H, Zhang J, Wu S. Indazoles as potential c-Met inhibitors: design, synthesis and molecular docking studies. Eur J Med Chem. 2013; 65: 112-118.
35. Therasse P, Arbuck SG, Eisenhauer EA, Wanders J, Kaplan RS, Rubinstein L, Verweij J, Van Glabbeke M, van Oosterom AT, Christian MC, Gwyther SG. New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada. J Natl Cancer Inst. 2000; 92: 205-216.
36. Mita AC, Takimoto CH, Mita M, Tolcher A, Sankhala K, Sarantopoulos J, Valdivieso M, Wood L, Rasmussen E, Sun YN, Zhong ZD, Bass MB, Le N, et al. Phase 1 study of AMG 386, a selective angiopoietin 1/2-neutralizing peptibody, in combination with chemotherapy in adults with advanced solid tumors. Clin Cancer Res. 2010; 16: 3044-3056.