Tackling crizotinib resistance: The pathway from drug discovery to the pediatric clinic

Cancer Research

Volumn 75, Issue 14, 2015, Pages 2770-2774

  Tucker, Elizabeth R ^a   Danielson, Laura S ^a   Innocenti, Paolo ^a   Chesler, Louis ^a  

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

6 AMINO 5 [1 (2,6 DICHLORO 3 FLUOROPHENYL)ETHOXY] N [4 (4 METHYL 1 PIPERAZINYLCARBONYL)PHENYL] 3 PYRIDAZINECARBOXAMIDE; ALECTINIB; ANAPLASTIC LYMPHOMA KINASE; ANAPLASTIC LYMPHOMA KINASE INHIBITOR; BRIGATINIB; CERITINIB; CRIZOTINIB; ENTRECTINIB; PF 06463922; TSR 011; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE; PYRAZOLE DERIVATIVE; PYRIDINE DERIVATIVE;

AMINO ACID SUBSTITUTION; ANTINEOPLASTIC ACTIVITY; CANCER RESISTANCE; CLINICAL TRIAL (TOPIC); CONFORMATIONAL TRANSITION; DRUG APPROVAL; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG RESEARCH; DRUG STRUCTURE; ENZYME INHIBITION; ENZYME KINETICS; GENE MUTATION; HUMAN; NEUROBLASTOMA; NON SMALL CELL LUNG CANCER; NONHUMAN; PEDIATRICS; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; REVIEW; SIGNAL TRANSDUCTION; SOMATIC MUTATION; ADULT; ANIMAL; CARCINOMA, NON-SMALL-CELL LUNG; CHILD; DRUG DEVELOPMENT; DRUG EFFECTS; DRUG RESISTANCE; GENETICS; LUNG NEOPLASMS; PHYSIOLOGY; PROCEDURES;

ADULT; ANIMALS; ANTINEOPLASTIC AGENTS; CARCINOMA, NON-SMALL-CELL LUNG; CHILD; DRUG DISCOVERY; DRUG RESISTANCE, NEOPLASM; HUMANS; LUNG NEOPLASMS; NEUROBLASTOMA; PROTEIN KINASE INHIBITORS; PYRAZOLES; PYRIDINES; RECEPTOR PROTEIN-TYROSINE KINASES;

EID: 84942881803     PISSN: 00085472     EISSN: 15387445     Source Type: Journal    
DOI: 10.1158/0008-5472.CAN-14-3817     Document Type: Review

References (30)

1. Morris SW, Naeve C, Mathew P., James PL, Kirstein MN, Cui X, et al ALK, the chromosome 2 gene locus altered by the t(2;5) in non-Hodgkin's lymphoma, encodes a novel neural receptor tyrosine kinase that is highly related to leukocyte tyrosine kinase (LTK). Oncogene 1997; 14: 2175-88.
2. Morris SW, Kirstein MN, Valentine M.B., 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.
3. Soda M, Choi YL, Enomoto M, Takada S., Yamashita Y, Ishikawa S, et al Identification of the transforming EML4-ALK fusion geneinnon-small-cell lung cancer. Nature 2007; 448: 561-6.
4. Bresler SC, Weiser DA, Huwe P.J., Park JH, Krytska K, Ryles H, et al ALK mutations confer differential oncogenic activation and sensitivity to ALK inhibition therapy in neuroblastoma. Cancer Cell 2014; 26: 682-94.
5. Katayama R, Shaw AT, Khan T.M., Mino-Kenudson M, Solomon BJ, Halmos B, et al Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers. Sci Transl Med 2012; 4: 120ra17.
6. 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.
7. Yu HA, Arcila ME, Rekhtman N, Sima C.S., Zakowski MF, Pao W, et al. Analysis of tumor specimensat the timeofacquired resistance to EGFR-TKI therapy in 155 patients with EGFR-mutant lung cancers. Clin Cancer Res 2013; 19: 2240-7.
8. 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.
9. 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.
10. Janoueix-Lerosey I., Lequin D, Brugieres L., Ribeiro A, de Pontual L, Combaret V, et al Somatic and germline activating mutations of the ALK kinase receptor in neuroblastoma. Nature 2008; 455: 967-70.
11. Chen Y, Takita J, Choi Y.L., Kato M., Ohira M, Sanada M, et al Oncogenic mutations of ALK kinase in neuroblastoma. Nature 2008; 455: 971-4.
12. George RE, Sanda T, Hanna M., Frohling S, Luther W 2nd, Zhang J, et al. Activating mutations in ALK provide atherapeutic target in neuroblastoma. Nature 2008; 455: 975-8.
13. Mosse YP, Lim MS, Voss S.D., Wilner K., Ruffner K, Laliberte J, et al Safety and activity of crizotinib for paediatric patients with refractory solid tumours or anaplastic large-cell lymphoma: a Children's Oncology Group phase 1 consortium study. Lancet Oncol 2013; 14: 472-80.
14. Schleiermacher G, Javanmardi N, Bernard V., Leroy Q, Cappo J, Rio Frio T, et al. Emergence of new ALK mutations at relapse of neuroblastoma. J Clin Oncol 2014; 32: 2727-34.
15. Berry T, Luther W, Bhatnagar N., Jamin Y, Poon E, Sanda T., et al. The ALK (F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma. Cancer Cell 2012; 22: 117-30.
16. Heukamp LC, Thor T, Schramm A., De Preter K, Kumps C, De Wilde B, et al. Targeted expression of mutated ALK induces neuroblastoma in transgenic mice. Sci Transl Med 2012; 4: 141ra91.
17. Zhu S, Lee JS, Guo F, Shin J., Perez-Atayde AR, Kutok JL, et al Activated ALK collaborates with MYCN in neuroblastoma pathogenesis. Cancer Cell 2012; 21: 362-73.
18. Sattu K, Hochgrafe F, Wu J., Umapathy G, Schonherr C, Ruuth K., et al. Phosphoproteomic analysis of anaplastic lymphoma kinase (ALK) downstream signaling pathways identifies signal transducer and activator of transcription 3 as a functional target of activated ALK in neuroblastoma cells. FEBS J 2013; 280: 5269-82.
19. Umapathy G, El Wakil A, Witek B, Chesler L, Danielson L, Deng X, et al. The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. Sci Signal 2014; 7: ra102.
20. Schonherr C, Ruuth K, Kamaraj S., Wang CL, Yang HL, Combaret V, et al Anaplastic Lymphoma Kinase (ALK) regulates initiation of transcription of MYCN in neuroblastoma cells. Oncogene 2012; 31: 5193-200.
21. Marsilje TH, Pei W, Chen B., Lu W, Uno T, Jin Y., et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulf onyl)phenyl) pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem 2013; 56: 5675-90.
22. + solid tumours. J Clin Oncol 30, 2012 (suppl; abstr 3007).
23. Friboulet L, Li N, Katayama R., Lee CC, Gainor JF, Crystal AS, et al The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer. Cancer Discov 2014; 4: 662-73.
24. Bossi RT, Saccardo MB, Ardini E, Menichincheri M., Rusconi L, Magnaghi P, et al Crystal structures of anaplastic lymphoma kinase in complex with ATP competitive inhibitors. Biochemistry 2010; 49: 6813-25.
25. Schonherr C, Ruuth K, Yamazaki Y., Eriksson T, Christensen J, Palmer R.H., et al. Activating ALK mutations found in neuroblastoma are inhibited by crizotinib and NVP-TAE684. Biochem J 2011; 440: 405-13.
26. Bresler SC, Wood AC, Haglund E.A., Courtright J., Belcastro LT, Plegaria JS, et al. Differential inhibitor sensitivity of anaplastic lymphoma kinase variants found in neuroblastoma. Sci Transl Med 2011; 3: 108ra14.
27. Lee CC, Jia Y, Li N., Sun X, Ng K, Ambing E., et al. Crystal structure of the ALK (anaplastic lymphoma kinase) catalytic domain. Biochem J 2010; 430: 425-37.
28. Johnson TW, Richardson PF, Bailey S, Brooun A., Burke BJ, Collins MR, et al. Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(m etheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocy-clic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations. J Med Chem 2014; 57: 4720-44.
29. Moreno L, Pearson AD How can attrition rates be reduced in cancer drug discovery? Expert Opin Drug Discov 2013; 8: 363-8.
30. Lovly CM, Heuckmann JM, de Stanchina E, Chen H, Thomas R.K., Liang C., et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors. Cancer Res 2011; 71: 4920-31.