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Volumn 15, Issue 4, 2016, Pages 628-639

Entrectinib, a Pan-TRK, ROS1, and ALK inhibitor with activity in multiple molecularly defined cancer indications

Author keywords

[No Author keywords available]

Indexed keywords

CRIZOTINIB; ENTRECTINIB; ANAPLASTIC LYMPHOMA KINASE; ANTINEOPLASTIC AGENT; BENZAMIDE DERIVATIVE; INDAZOLE DERIVATIVE; ONCOPROTEIN; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE; ROS1 PROTEIN, HUMAN;

EID: 84964355641     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-15-0758     Document Type: Article
Times cited : (261)

References (40)
  • 1
    • 36849065315 scopus 로고    scopus 로고
    • Global survey of phosphotyrosine signalling identifies oncogenic kinases in lung cancer
    • Rikova K, Guo A, Zeng O, Possemato A, Yu J, Haack H, et al. Global survey of phosphotyrosine signalling identifies oncogenic kinases in lung cancer. Cell 2007;131:1190-203.
    • (2007) Cell , vol.131 , pp. 1190-1203
    • Rikova, K.1    Guo, A.2    Zeng, O.3    Possemato, A.4    Yu, J.5    Haack, H.6
  • 2
    • 34547638047 scopus 로고    scopus 로고
    • Identification of the transforming EML4-ALK fusion gene in non-small cell lung cancer
    • 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.
    • (2007) Nature , vol.448 , pp. 561-566
    • Soda, M.1    Choi, Y.L.2    Enomoto, M.3    Takada, S.4    Yamashita, Y.5    Ishikawa, S.6
  • 4
    • 84866178842 scopus 로고    scopus 로고
    • Nerve growth factor and the physiology of pain: Lessons from congenital insensitivity to pain with anhidrosis
    • Indo Y. Nerve growth factor and the physiology of pain: lessons from congenital insensitivity to pain with anhidrosis. Clin Genet 2012;82:341-50.
    • (2012) Clin Genet , vol.82 , pp. 341-350
    • Indo, Y.1
  • 5
    • 77950939830 scopus 로고    scopus 로고
    • Rearrangements of NTRK1 gene in papillary thyroid carcinoma
    • Greco A, Miranda C, Pierotti MA. Rearrangements of NTRK1 gene in papillary thyroid carcinoma. Mol Cell Endocrinol 2010;321:44-9.
    • (2010) Mol Cell Endocrinol , vol.321 , pp. 44-49
    • Greco, A.1    Miranda, C.2    Pierotti, M.A.3
  • 7
    • 34250378582 scopus 로고    scopus 로고
    • Tyrosine kinase inhibitor CEP-701 blocks the NTRK1/NGF receptor and limits the invasive capability of prostate cancer cells in vitro
    • Festuccia C, Muzi P, Gravina GL, Millimaggi D, Speca S, Dolo V, et al. Tyrosine kinase inhibitor CEP-701 blocks the NTRK1/NGF receptor and limits the invasive capability of prostate cancer cells in vitro. Int J Oncol 2007;30:193-200.
    • (2007) Int J Oncol , vol.30 , pp. 193-200
    • Festuccia, C.1    Muzi, P.2    Gravina, G.L.3    Millimaggi, D.4    Speca, S.5    Dolo, V.6
  • 8
    • 0035132668 scopus 로고    scopus 로고
    • Nerve Growth Factor exerts differential effects on the growth of human pancreatic cancer cells
    • Zhu ZW, Friess H, Wang L, Bogardus T, Korc M, Kleeff J, et al. Nerve Growth Factor exerts differential effects on the growth of human pancreatic cancer cells. Clin Cancer Res 2001;7:105-12.
    • (2001) Clin Cancer Res , vol.7 , pp. 105-112
    • Zhu, Z.W.1    Friess, H.2    Wang, L.3    Bogardus, T.4    Korc, M.5    Kleeff, J.6
  • 9
    • 38449108441 scopus 로고    scopus 로고
    • SiRNA directed against TrkA sensitizes human pancreatic cancer cells to apoptosis induced by gemcitabine through an inactivation of PI3K/Akt-dependent pathway
    • Liu D, Zhang Y, Dand C, Ma Q, Lee W, Chen W. siRNA directed against TrkA sensitizes human pancreatic cancer cells to apoptosis induced by gemcitabine through an inactivation of PI3K/Akt-dependent pathway. Oncol Rep 2007;18:673-7.
    • (2007) Oncol Rep , vol.18 , pp. 673-677
    • Liu, D.1    Zhang, Y.2    Dand, C.3    Ma, Q.4    Lee, W.5    Chen, W.6
  • 12
    • 84911955886 scopus 로고    scopus 로고
    • The TPM3-NTRK1 rearrangement is a recurring event in colorectal carcinoma and is associated with tumor sensitivity to TRKA kinase inhibition
    • Ardini E, Bosotti R, Lombardi Borgia A, De Ponti C, Somaschini A, Cammarota R, et al. The TPM3-NTRK1 rearrangement is a recurring event in colorectal carcinoma and is associated with tumor sensitivity to TRKA kinase inhibition. Mol Oncol 2014;8:1495-507.
    • (2014) Mol Oncol , vol.8 , pp. 1495-1507
    • Ardini, E.1    Bosotti, R.2    Lombardi Borgia, A.3    De Ponti, C.4    Somaschini, A.5    Cammarota, R.6
  • 13
    • 84922341647 scopus 로고    scopus 로고
    • TRKing downan old oncogene in a new era of targeted therapy
    • Vaishnavi A, Le AT, Doebele RC. TRKing downan old oncogene in a new era of targeted therapy. Cancer Discov 2015;5:25-34.
    • (2015) Cancer Discov , vol.5 , pp. 25-34
    • Vaishnavi, A.1    Le, A.T.2    Doebele, R.C.3
  • 15
    • 84899526966 scopus 로고    scopus 로고
    • The genomic landscape of diffuse intrinsic pontine glioma and pediatric non-brainstem high-grade glioma
    • Wu G, Diaz AK, Paugh BS, Rankin SL, Ju B, Li Y, et al. The genomic landscape of diffuse intrinsic pontine glioma and pediatric non-brainstem high-grade glioma. Nat Genet 2014;46:444-50.
    • (2014) Nat Genet , vol.46 , pp. 444-450
    • Wu, G.1    Diaz, A.K.2    Paugh, B.S.3    Rankin, S.L.4    Ju, B.5    Li, Y.6
  • 17
    • 19044391610 scopus 로고    scopus 로고
    • Expression of the ETV6-NTRK3 gene fusion as a primary event in human secretory breast carcinoma
    • Tognon C, Knezevich SR, Huntsman D, Roskelley CD, Melnyk N, Mathers JA, et al. Expression of the ETV6-NTRK3 gene fusion as a primary event in human secretory breast carcinoma. Cancer Cell 2002;2:367-76.
    • (2002) Cancer Cell , vol.2 , pp. 367-376
    • Tognon, C.1    Knezevich, S.R.2    Huntsman, D.3    Roskelley, C.D.4    Melnyk, N.5    Mathers, J.A.6
  • 18
    • 84880664490 scopus 로고    scopus 로고
    • Novel targets in non-small cell lung cancer: ROS1 and RET fusions
    • Gainor JF, Shaw AT. Novel targets in non-small cell lung cancer: ROS1 and RET fusions. Oncologist 2013;18:865-75.
    • (2013) Oncologist , vol.18 , pp. 865-875
    • Gainor, J.F.1    Shaw, A.T.2
  • 21
    • 78649475696 scopus 로고    scopus 로고
    • The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers
    • 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.
    • (2010) Cancer Res , vol.70 , pp. 10038-10043
    • Sasaki, T.1    Okuda, K.2    Zheng, W.3    Butrynski, J.4    Capelletti, M.5    Wang, L.6
  • 22
  • 24
    • 84892187259 scopus 로고    scopus 로고
    • The central nervous system as a sanctuary site in ALK-positive non-small cell lung cancer
    • Gainor JF, Ou SH, Logan J, Borges LF, Shaw AT. The central nervous system as a sanctuary site in ALK-positive non-small cell lung cancer. J Thorac Oncol 2013;8:1570-3.
    • (2013) J Thorac Oncol , vol.8 , pp. 1570-1573
    • Gainor, J.F.1    Ou, S.H.2    Logan, J.3    Borges, L.F.4    Shaw, A.T.5
  • 25
    • 84880877176 scopus 로고    scopus 로고
    • Synthesis, structureactivity 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-(isopropylsulfonyl) phenyl) pyrimidine-2, 4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials
    • Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, et al. Synthesis, structureactivity 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-(isopropylsulfonyl) phenyl) pyrimidine-2, 4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem 2013;56:5675-90.
    • (2013) J Med Chem , vol.56 , pp. 5675-5690
    • Marsilje, T.H.1    Pei, W.2    Chen, B.3    Lu, W.4    Uno, T.5    Jin, Y.6
  • 27
    • 84888646015 scopus 로고    scopus 로고
    • Tyrosine kinase gene rearrangements in epithelial malignancies
    • Shaw AT, Hsu PP, Awad MM, Engelman JA. Tyrosine kinase gene rearrangements in epithelial malignancies. Nat Rev Cancer 2013;13:772-87.
    • (2013) Nat Rev Cancer , vol.13 , pp. 772-787
    • Shaw, A.T.1    Hsu, P.P.2    Awad, M.M.3    Engelman, J.A.4
  • 29
    • 84915784462 scopus 로고    scopus 로고
    • Phase 1 open label, dose escalation study of RXDX-101, an oral pan-trk, ROS1, and ALK inhibitor, in patients with advanced solid tumors with relevant molecular alterations
    • 2502
    • De Braud FGM, Pilla L, Niger M, Damian S, Bardazza B, Martinetti A, et al. Phase 1 open label, dose escalation study of RXDX-101, an oral pan-trk, ROS1, and ALK inhibitor, in patients with advanced solid tumors with relevant molecular alterations. J Clin Oncol 2014;32:5s (suppl; abstr 2502).
    • (2014) J Clin Oncol , vol.32 , pp. 5s
    • De Braud, F.G.M.1    Pilla, L.2    Niger, M.3    Damian, S.4    Bardazza, B.5    Martinetti, A.6
  • 30
    • 84946795025 scopus 로고    scopus 로고
    • Alka-372-001: First-in-human, phase I study of entrectinib-an oral pantrk, ROS1, and ALK inhibitor-in patients with advanced solid tumorswith relevant molecular alterations
    • 2517
    • De Braud FGM, Niger M, Damian S, Bardazza B, Martinetti A, Pelosi G, et al. Alka-372-001: first-in-human, phase I study of entrectinib-an oral pantrk, ROS1, and ALK inhibitor-in patients with advanced solid tumorswith relevant molecular alterations. J Clin Oncol 33, 2015(suppl; abstr 2517).
    • (2015) J Clin Oncol , vol.33
    • De Braud, F.G.M.1    Niger, M.2    Damian, S.3    Bardazza, B.4    Martinetti, A.5    Pelosi, G.6
  • 31
    • 84946795026 scopus 로고    scopus 로고
    • STARTRK-1: Phase 1/2a study of entrectinib, an oral Pan-Trk, ROS1, and ALK inhibitor, in patients with advanced solid tumorswith relevant molecular alterations
    • 2596
    • Patel MR, Bauer TM, Liu SV, Drilon A, Wheler J, Shaw A, et al. STARTRK-1: phase 1/2a study of entrectinib, an oral Pan-Trk, ROS1, and ALK inhibitor, in patients with advanced solid tumorswith relevant molecular alterations. J Clin Oncol 33, 2015(suppl; abstr 2596).
    • (2015) J Clin Oncol , vol.33
    • Patel, M.R.1    Bauer, T.M.2    Liu, S.V.3    Drilon, A.4    Wheler, J.5    Shaw, A.6
  • 32
    • 79955560817 scopus 로고    scopus 로고
    • NMSP937, a 4, 5-dihydro-1H-pyrazolo[4, 3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor
    • Beria I, Bossi RT, Brasca MG, Caruso M, Ceccarelli W, Fachin G, et al. NMSP937, a 4, 5-dihydro-1H-pyrazolo[4, 3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett 2011;21:2969-74.
    • (2011) Bioorg Med Chem Lett , vol.21 , pp. 2969-2974
    • Beria, I.1    Bossi, R.T.2    Brasca, M.G.3    Caruso, M.4    Ceccarelli, W.5    Fachin, G.6
  • 33
    • 84874335106 scopus 로고    scopus 로고
    • Cell line identity finding by fingerprinting, an optimized resource for short tandem repeat profile authentication
    • Somaschini A, Amboldi N, Nuzzo A, Scacheri E, Ukmar G, Ballinari D, et al. Cell line identity finding by fingerprinting, an optimized resource for short tandem repeat profile authentication. Genet Test Mol Biomarkers 2013;17:254-9.
    • (2013) Genet Test Mol Biomarkers , vol.17 , pp. 254-259
    • Somaschini, A.1    Amboldi, N.2    Nuzzo, A.3    Scacheri, E.4    Ukmar, G.5    Ballinari, D.6
  • 34
    • 84858701559 scopus 로고    scopus 로고
    • The generation of purinome-targeted libraries as ameans to diversify ATPmimetic chemical classes for lead finding
    • Felder ER, Badari A, Disingrini T, Mantegani S, Orrenius C, Avanzi N, et al. The generation of purinome-targeted libraries as ameans to diversify ATPmimetic chemical classes for lead finding. Mol Divers 2012;16:27-51.
    • (2012) Mol Divers , vol.16 , pp. 27-51
    • Felder, E.R.1    Badari, A.2    Disingrini, T.3    Mantegani, S.4    Orrenius, C.5    Avanzi, N.6
  • 36
    • 85047699293 scopus 로고    scopus 로고
    • Anaplastic lymphoma kinase (ALK) activates Stat3 and protects hematopoietic cells from cell death
    • Zamo A, Chiarle R, Piva R, Howes J, Fan Y, Chilosi M, et al. Anaplastic lymphoma kinase (ALK) activates Stat3 and protects hematopoietic cells from cell death. Oncogene 2002;21:1038-47.
    • (2002) Oncogene , vol.21 , pp. 1038-1047
    • Zamo, A.1    Chiarle, R.2    Piva, R.3    Howes, J.4    Fan, Y.5    Chilosi, M.6
  • 37
    • 84903482432 scopus 로고    scopus 로고
    • Ceritinib in ALK-rearranged non-small cell lung cancer
    • Shaw AT, Engelman JA. Ceritinib in ALK-rearranged non-small cell lung cancer. N Engl J Med 2014;370:2537-9.
    • (2014) N Engl J Med , vol.370 , pp. 2537-2539
    • Shaw, A.T.1    Engelman, J.A.2
  • 38
    • 80054754771 scopus 로고    scopus 로고
    • Phase I trial of lestaurtinib for childrenwith refractory neuroblastoma: A new approaches to neuroblastoma therapy consortium study
    • Minturn JE, Evans AE, Villablanca JG, Yanik GA, Park JR, Shusterman S, et al. Phase I trial of lestaurtinib for childrenwith refractory neuroblastoma: a new approaches to neuroblastoma therapy consortium study. Cancer Chemother Pharmacol 2011;68:1057-65.
    • (2011) Cancer Chemother Pharmacol , vol.68 , pp. 1057-1065
    • Minturn, J.E.1    Evans, A.E.2    Villablanca, J.G.3    Yanik, G.A.4    Park, J.R.5    Shusterman, S.6
  • 39
    • 84896457874 scopus 로고    scopus 로고
    • New routes to targeted therapy of intrahepatic cholangiocarcinomas revealed by nextgeneration sequencing
    • Ross JS, Wang K, Gay L, Al-Rohil R, Rand JV, Jones DM, et al. New routes to targeted therapy of intrahepatic cholangiocarcinomas revealed by nextgeneration sequencing. Oncologist 2014;19:235-42.
    • (2014) Oncologist , vol.19 , pp. 235-242
    • Ross, J.S.1    Wang, K.2    Gay, L.3    Al-Rohil, R.4    Rand, J.V.5    Jones, D.M.6
  • 40
    • 84881245421 scopus 로고    scopus 로고
    • Molecular pathways: ROS1 fusion proteins in cancer
    • Davies KD, Doebele RC. Molecular pathways: ROS1 fusion proteins in cancer. Clin Cancer Res 2013;19:2040-5.
    • (2013) Clin Cancer Res , vol.19 , pp. 2040-2045
    • Davies, K.D.1    Doebele, R.C.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.