Treatment efficacy and resistance mechanisms using the second-generation ALK inhibitor AP26113 in human NPM-ALK-positive anaplastic large cell lymphoma

Molecular Cancer Research

Volumn 13, Issue 4, 2015, Pages 775-783

  Ceccon, M ^a   Mologni, L ^a   Giudici, G ^a   Piazza, R ^a   Pirola, A ^a   Fontana, D ^a   Gambacorti Passerini, C ^a,b  

^a UNIVERSITY OF MILANO BICOCCA   (Italy)

^b SAN GERARDO HOSPITAL   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2 [[2 (ISOPROPYLSULFONYL)PHENYL]AMINO] 4 [[2 METHOXY 4 [4 (4 METHYL 1 PIPERAZINYL) 1 PIPERIDINYL]PHENYL]AMINO] 1,3,5 TRIAZINE; ALECTINIB; CERITINIB; CRIZOTINIB; HYBRID PROTEIN; PROTEIN NPM ALK; UNCLASSIFIED DRUG; VASCULOTROPIN RECEPTOR; [2 [[5 CHLORO 2 [[4 [4 (DIMETHYLAMINO) 1 PIPERIDINYL] 2 METHOXYPHENYL]AMINO] 4 PYRIMIDINYL]AMINO]PHENYL]DIMETHYLPHOSPHINE OXIDE; ANAPLASTIC LYMPHOMA KINASE; BRIGATINIB; ORGANOPHOSPHORUS COMPOUND; P80(NPM-ALK) PROTEIN; PROTEIN TYROSINE KINASE; PYRIMIDINE DERIVATIVE;

AMINO ACID SUBSTITUTION; ARTICLE; CANCER CELL LINE; DRUG EFFICACY; DRUG MECHANISM; HUMAN; HUMAN CELL; IC50; LARGE CELL LYMPHOMA; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; PROTEIN DOMAIN; CHEMISTRY; DNA SEQUENCE; DRUG RESISTANCE; EXOME; GENETICS; LYMPHOMA, LARGE-CELL, ANAPLASTIC; METABOLISM; POINT MUTATION; TUMOR CELL LINE; UPREGULATION;

AMINO ACID SUBSTITUTION; CELL LINE, TUMOR; DRUG RESISTANCE, NEOPLASM; EXOME; HUMANS; INHIBITORY CONCENTRATION 50; LYMPHOMA, LARGE-CELL, ANAPLASTIC; ORGANOPHOSPHORUS COMPOUNDS; POINT MUTATION; PROTEIN-TYROSINE KINASES; PYRIMIDINES; RECEPTOR PROTEIN-TYROSINE KINASES; SEQUENCE ANALYSIS, DNA; UP-REGULATION;

EID: 84928036655     PISSN: 15417786     EISSN: 15573125     Source Type: Journal    
DOI: 10.1158/1541-7786.MCR-14-0157     Document Type: Article

References (36)

1. Morris SW, Kirstein MN, Valentine MB, Dittmer KG, Shapiro DN, Saltman DL, et al. Fusion of a kinase gene, ALK, to a nucleolar protein gene, NPM, in non-Hodgkin's lymphoma. Science 1994;263:1281-4.
2. Coffin CM, Patel A, Perkins S, Elenitoba-Johnson KS, Perlman E, Griffin CA. ALK1 and p80 expression and chromosomal rearrangements involving 2p23 in inflammatory myofibroblastic tumor. Mod Pathol 2001;14: 569-76.
3. Soda M, Choi YL, Enomoto M, Takada S, Yamashita Y, Ishikawa S, et al. Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer. Nature 2007;448:561-6.
4. Van Gaal JC, Flucke UE, Roeffen MH, de Bont ES, Sleijfer S, Mavinkurve-Groothuis AM, et al. Anaplastic lymphoma kinase aberrations in rhabdomyosarcoma: clinical and prognostic implications. J Clin Oncol 2012;30: 308-15.
5. Wang WY, Gu L, Liu WP, Li GD, Liu HJ, Ma ZG. ALK-positive extramedullary plasmacytoma with expression of the CLTC-ALK fusion transcript. Pathol Res Pract 2011;207:587-91.
6. Debelenko LV, Raimondi SC, Daw N, Shivakumar BR, Huang D, Nelson M, et al. Renal cell carcinoma with novel VCL-ALK fusion: new representative of ALK-associated tumor spectrum. Mod Pathol 2011;24:430-42.
7. Murugan AK, Xing M. Anaplastic thyroid cancers harbor novel oncogenic mutations of the ALK gene. Cancer Res 2011;71:4403-11.
8. Ning H, Mitsui H,Wang CQ, Suarez-Farinas M, Gonzalez J, Shah KR, et al. Identification of anaplastic lymphoma kinase as a potential therapeutic target in Basal Cell Carcinoma. Oncotarget 2013;4:2237-48.
9. Lin E, Li L, Guan Y, Soriano R, Rivers CS, Mohan S, et al. Exon array profiling detects EML4-ALK fusion in breast, colorectal, and non-small cell lung cancers. Mol Cancer Res 2009;7:1466-76.
10. Lipson D, Capelletti M, Yelensky R, Otto G, Parker A, Jarosz M, et al. Identification of new ALK and RET gene fusions from colorectal and lung cancer biopsies. Nat Med 2012;18:382-4.
11. Mosse YP, Laudenslager M, Longo L, Cole KA, Wood A, Attiyeh EF, et al. Identification of ALK as a major familial neuroblastoma predisposition gene. Nature 2008;455:930-5.
12. Azarova AM, Gautam G, George RE. Emerging importance of ALK in neuroblastoma. Semin Cancer Biol 2011;21:267-75.
13. Powers C, Aigner A, Stoica GE, McDonnell K, Wellstein A. Pleiotrophin signaling through anaplastic lymphoma kinase is rate-limiting for glioblastoma growth. J Biol Chem 2002;277:14153-8.
14. Hudson L, Kulig K, Young D, McLendon R, Abernethy A. Abstract: "A42: ALK and cMET expression in glioblastoma multiforme: Implications for therapeutic targeting." Abstract: s: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics-Nov 12-16, 2011; San Francisco, CA.
15. Roskoski R Jr. Anaplastic lymphoma kinase (ALK): structure, oncogenic activation, and pharmacological inhibition. Pharmacol Res 2013;68:68-94.
16. Chiarle R, Simmons WJ, Cai H, Dhall G, Zamo A, Raz R, et al. Stat3 is required for ALK-mediated lymphomagenesis and provides a possible therapeutic target. Nat Med 2005;11:623-9.
17. Chiarle R, Voena C, Ambrogio C, Piva R, Inghirami G. The anaplastic lymphoma kinase in the pathogenesis of cancer. Nat Rev Cancer 2008; 8:11-23.
18. Shaw AT, Kim DW, Nakagawa K, Seto T, Crino L, Ahn MJ, et al. Crizotinib versus chemotherapy in advanced ALK-positive lung cancer. N Engl J Med 2013;368:2385-94.
19. Gambacorti-Passerini C, Messa C, Pogliani EM. Crizotinib in anaplastic large-cell lymphoma. N Engl J Med 2011;364:775-6.
20. Gambacorti Passerini C, Farina F, Stasia A, Redaelli S, Ceccon M, Mologni L, et al. Crizotinib in advanced, chemoresistant anaplastic lymphoma kinase-positive lymphoma patients. J Natl Cancer Inst 2014;106:djt378.
21. Deininger MW, Holyoake TL. Can we afford to let sleeping dogs lie? Blood 2005;105:1840-1.
22. Gambacorti-Passerini CB, Gunby RH, Piazza R, Galietta A, Rostagno R, Scapozza L. Molecular mechanisms of resistance to imatinib in Philadelphia-chromosome-positive leukaemias. Lancet Oncol 2003;4:75-85.
23. Choi YL, Soda M, Yamashita Y, Ueno T, Takashima J, Nakajima T, et al. EML4-ALK mutations in lung cancer that confer resistance to ALK inhibitors. N Engl J Med 2010;363:1734-9.
24. Sasaki T, Okuda K, Zheng W, Butrynski J, Capelletti M, Wang L, et al. The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers. Cancer Res 2010;70: 10038-43.
25. Doebele RC, Pilling AB, Aisner DL, Kutateladze TG, Le AT, Weickhardt AJ, et al. Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer. Clin Cancer Res 2012;18:1472-82.
26. Katayama R, Shaw AT, Khan TM, Mino-KenudsonM, Solomon BJ, Halmos B, et al. Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers. Sci Transl Med 2012;4:120ra17.
27. Mologni L. Inhibitors of the anaplastic lymphoma kinase. Expert Opin Investig Drugs 2012;21:985-94.
28. Rivera VM, Anjum R, Wang F, Zhang S, Keats J, Ning Y, et al. Efficacy and pharmacodynamic analysis of AP26113, a potent and selective orally active inhibitor of Anaplastic Lymphoma Kinase (ALK). Washington, D.C.: AACR; 2010.
29. Ceccon M, Mologni L, Bisson W, Scapozza L, Gambacorti-Passerini C. Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors. Mol Cancer Res 2013;11:122-32.
30. Li H, Handsaker B, Wysoker A, Fennell T, Ruan J, Homer N, et al. The Sequence alignment/map format and SAMtools. Bioinformatics 2009;25: 2078-9.
31. Piazza R, Magistroni V, Pirola A, Redaelli S, Spinelli R, Galbiati M, et al. CEQer: a graphical tool for copy number and allelic imbalance detection from whole-exome sequencing data. PLoS One 2013;8:e74825.
32. Redaelli S, Piazza R, Rostagno R, Magistroni V, Perini P, Marega M, et al. Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants. J Clin Oncol 2009;27:469-71.
33. Redaelli S, Mologni L, Rostagno R, Piazza R, Magistroni V, CecconM, et al. Three novel patient-derived BCR/ABL mutants show different sensitivity to second and third generation tyrosine kinase inhibitors. Am J Hematol 2014;87:E125-8.
34. Zhang S, Wang F, Keats J, Ning Y, Wardwell SD, Moran Lauren, et al. AP26113, a potent ALK inhibitor, overcomes mutations in EML4-ALK that confer resistance to PF-02341066. AACR annual meeting, Apr 17-21, 2010; Washington, DC.
35. Katayama R, Khan TM, Benes C, Lifshits E, Ebi H, Rivera VM, et al. Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A 2011;108:7535-40.
36. Heuckmann JM, Holzel M, Sos ML, Heynck S, Balke-Want H, Koker M, et al. ALK mutations conferring differential resistance to structurally diverse ALK inhibitors. Clin Cancer Res 2011;17:7394-401.