Implications of Mutational Analysis for the Management of Patients With Gastrointestinal Stromal Tumors and the Application of Targeted Therapies

REFERENCES

• National Comprehensive Cancer Network. NCCN Clinical Practice Guidelines in Oncology: soft tissue sarcoma V.2.2010. 2009. http://www.nccn.org/professionals/physician_gls/PDF/sarcoma.pdf.
   Google Scholar
• Casali, P.G.; Jost, L.; Reichardt, P.; Schlemmer, M.; Blay, J.Y. Gastrointestinal stromal tumors: ESMO clinical recommendations for diagnosis, treatment and follow-up. Ann Oncol 2009, 20(Suppl 4), iv64–67.
   Google Scholar
• Nilsson, B.; Bümming, P.; Meis-Kindblom, J.M.; Odén, A.; Dortok, A.; Gustavsson, B.; Sablinska, K.; Kindblom, L.G. Gastrointestinal stromal tumors: the incidence, prevalence, clinical course, and prognostication in the preimatinib mesylate era –a population-based study in western Sweden. Cancer 2005, 103(4), 821–829.
   PubMed Web of Science ®Google Scholar
• Din, O.S.; Woll, P.J. Treatment of gastrointestinal stromal tumor: focus on imatinib mesylate. Ther Clin Risk Manag 2008, 4(1), 149–162.
   PubMedGoogle Scholar
• Joensuu, H.; Fletcher, C.; Dimitrijevic, S.; Silberman, S.; Roberts, P.; Demetri, G. Management of malignant gastrointestinal stromal tumours. Lancet Oncol 2002, 3(11), 655–664.
   PubMed Web of Science ®Google Scholar
• DeMatteo, R.P.; Heinrich, M.C.; El-Rifai, W.M.; Demetri, G. Clinical management of gastrointestinal stromal tumors: before and after STI-571. Hum Pathol 2002, 33(5), 466–477.
   PubMed Web of Science ®Google Scholar
• Hornick, J.L.; Fletcher, C.D. The role of KIT in the management of patients with gastrointestinal stromal tumors. Hum Pathol 2007, 38(5), 679–687.
   PubMed Web of Science ®Google Scholar
• Hoeben, A.; Schoffski, P.; Debiec-Rychter, M. Clinical implications of mutational analysis in gastrointestinal stromal tumours. Br J Cancer 2008, 98(4), 684–688.
   PubMed Web of Science ®Google Scholar
• Rubin, B.P. Gastrointestinal stromal tumours: an update. Histopathology 2006, 48(1), 83–96.
   PubMed Web of Science ®Google Scholar
• D’Amato, G.; Steinert, D.M.; McAuliffe, J.C.; Trent, J.C. Update on the biology and therapy of gastrointestinal stromal tumors. Cancer Control 2005, 12(1), 44–56.
   PubMedGoogle Scholar
• Heinrich, M.C.; Corless, C.L.; Duensing, A.; McGreevey, L.; Chen, C.J.; Joseph, N.; Singer, S.; Griffith, D.J.; Haley, A.; Town, A.; Demetri, G.D.; Fletcher, C.D.; Fletcher, J.A. PDGFRA activating mutations in gastrointestinal stromal tumors. Science 2003, 299(5607), 708–710.
   PubMed Web of Science ®Google Scholar
• Debiec-Rychter, M.; Wasag, B.; Stul, M.; De Wever, I.; van Oosterom, A.; Hagemeijer, A.; Sciot, R. Gastrointestinal stromal tumours (GISTs) negative for KIT (CD117 antigen) immunoreactivity. J Pathol 2004, 202(4), 430–438.
   PubMed Web of Science ®Google Scholar
• Pauls, K.; Merkelbach-Bruse, S.; Thal, D.; Buttner, R.; Wardelmann, E. PDGFRalpha- and c-kit-mutated gastrointestinal stromal tumours (GISTs) are characterized by distinctive histological and immunohistochemical features. Histopathology 2005, 46(2), 166–175.
   PubMed Web of Science ®Google Scholar
• Emile, J.F.; Stock, N.; Corless, C.L.; Sciot, R.; Schildhaus, H.U.; Brahimi, S.; Debiec-Rychter, M.; Wardelmann, E.; Coindre, J.M.; Blay, J.Y. Dotlike or Golgi-like KIT and PDGFRA staining in GISTs. Am J Surg Pathol 2009, 33(1), 157–158.
   PubMed Web of Science ®Google Scholar
• Novartis Pharmaceuticals. Gleevec® (imatinib mesylate) prescribing information. February 2010. http://www.pharma.us.novartis.com/product/pi/pdf/gleevec_tabs.pdf.
   Google Scholar
• Blanke, C.D.; Demetri, G.D.; von, M.M.; Heinrich, M.C.; Eisenberg, B.; Fletcher, J.A.; Corless, C.L.; Fletcher, C.D.; Roberts, P.J.; Heinz, D.; Wehre, E.; Nikolova, Z.; Joensuu, H. Long-term results from a randomized phase II trial of standard-versus higher-dose imatinib mesylate for patients with unresectable or metastatic gastrointestinal stromal tumors expressing KIT. J Clin Oncol 2008, 26(4), 620–625.
   PubMed Web of Science ®Google Scholar
• Demetri, G.D.; von Mehren, M.; Blanke, C.D.; Van Den Abbeele, A.D.; Eisenberg, B.; Roberts, P.J.; Heinrich, M.C.; Tuveson, D.A.; Singer, S.; Janicek, M.; Fletcher, J.A.; Silverman, S.G.; Silberman, S.L.; Capdeville, R.; Kiese, B.; Peng, B.; Dimitrijevic, S.; Druker, B.J.; Corless, C.; Fletcher, C.D.; Joensuu, H. Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. N Engl J Med 2002, 347(7), 472–480.
   PubMed Web of Science ®Google Scholar
• Verweij, J.; Casali, P.G.; Zalcberg, J.; LeCesne, A.; Reichardt, P.; Blay, J.Y.; Issels, R.; van Oosterom, A.; Hogendoorn, P.C.; Van Glabbeke, M.; Bertulli, R.; Judson, I. Progression-free survival in gastrointestinal stromal tumours with high-dose imatinib: randomised trial. Lancet 2004, 364(9440), 1127–1134.
   PubMed Web of Science ®Google Scholar
• Van Glabbeke, M.; Verweij, J.; Casali, P.G.; Le Cesne, A.; Hohenberger, P.; Ray-Coquard, I.; Schlemmer, M.; van Oosterom, A.T.; Goldstein, D.; Sciot, R.; Hogendoorn, P.C.; Brown, M.; Bertulli, R.; Judson, I.R. Initial and late resistance to imatinib in advanced gastrointestinal stromal tumors are predicted by different prognostic factors: a European Organisation for Research and Treatment of Cancer–Italian Sarcoma Group–Australasian Gastrointestinal Trials Group study. J Clin Oncol 2005, 23(24), 5795–5804.
   PubMed Web of Science ®Google Scholar
• Abrams, T.J.; Lee, L.B.; Murray, L.J.; Pryer, N.K.; Cherrington, J.M. SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer. Mol Cancer Ther 2003, 2(5), 471–478.
   PubMed Web of Science ®Google Scholar
• Mendel, D.B.; Laird, A.D.; Xin, X.; Louie, S.G.; Christensen, J.G.; Li, G.; Schreck, R.E.; Abrams, T.J.; Ngai, T.J.; Lee, L.B.; Murray, L.J.; Carver, J.; Chan, E.; Moss, K.G.; Haznedar, J.O.; Sukbuntherng, J.; Blake, R.A.; Sun, L.; Tang, C.; Miller, T.; Shirazian, S.; McMahon, G.; Cherrington, J.M. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res 2003, 9(1), 327–337.
   PubMed Web of Science ®Google Scholar
• Murray, L.J.; Abrams, T.J.; Long, K.R.; Ngai, T.J.; Olson, L.M.; Hong, W.; Keast, P.K.; Brassard, J.A.; O’Farrell, A.M.; Cherrington, J.M.; Pryer, N.K. SU11248 inhibits tumor growth and CSF-1R-dependent osteolysis in an experimental breast cancer bone metastasis model. Clin Exp Metastasis 2003, 20(8), 757–766.
   PubMed Web of Science ®Google Scholar
• O’Farrell, A.M.; Abrams, T.J.; Yuen, H.A.; Ngai, T.J.; Louie, S.G.; Yee, K.W.; Wong, L.M.; Hong, W.; Lee, L.B.; Town, A.; Smolich, B.D.; Manning, W.C.; Murray, L.J.; Heinrich, M.C.; Cherrington, J.M. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood 2003, 101(9), 3597–3605.
   PubMed Web of Science ®Google Scholar
• Kim, D.W.; Jo, Y.S.; Jung, H.S.; Chung, H.K.; Song, J.H.; Park, K.C.; Park, S.H.; Hwang, J.H.; Rha, S.Y.; Kweon, G.R.; Lee, S.J.; Jo, K.W.; Shong, M. An orally administered multitarget tyrosine kinase inhibitor, SU11248, is a novel potent inhibitor of thyroid oncogenic RET/papillary thyroid cancer kinases. J Clin Endocrinol Metab 2006, 91(10), 4070–4076.
   PubMed Web of Science ®Google Scholar
• Demetri, G.D.; Huang, X.; Garrett, C.R.; Schöffski, P.; Blackstein, M.E.; Shah, M.H.; Verweij, J.; Tassell, V.; Baum, C.M.; Casali, P. Novel statistical analysis of long-term survival to account for crossover in a phase III trial of sunitinib (SU) vs. placebo (PL) in advanced GIST after imatinib (IM) failure [Abstract]. J Clin Oncol 2008. 26(15S), 559S.
   Google Scholar
• Pfizer Inc. SUTENT® (sunitinib) prescribing information. February 2010. http://www.pfizer.com/files/products/uspi_sutent.pdf.
   Google Scholar
• Miettinen, M.; Majidi, M.; Lasota, J. Pathology and diagnostic criteria of gastrointestinal stromal tumors (GISTs): a review. Eur J Cancer 2002, 38(Suppl. 5), S39–S51.
   PubMedGoogle Scholar
• Fletcher, C.D.; Berman, J.J.; Corless, C.; Gorstein, F.; Lasota, J.; Longley, B.J.; Miettinen, M.; O’Leary, T.J.; Remotti, H.; Rubin, B.P.; Shmookler, B.; Sobin, L.H.; Weiss, S.W. Diagnosis of gastrointestinal stromal tumors: a consensus approach. Hum Pathol 2002, 33(5), 459–465.
   PubMed Web of Science ®Google Scholar
• Miettinen, M.; Lasota, J. Gastrointestinal stromal tumors: review on morphology, molecular pathology, prognosis, and differential diagnosis. Arch Pathol Lab Med 2006, 130(10), 1466–1478.
   PubMed Web of Science ®Google Scholar
• Miettinen, M.; Lasota, J. Gastrointestinal stromal tumors: pathology and prognosis at different sites. Semin Diagn Pathol 2006, 23(2), 70–83.
   PubMed Web of Science ®Google Scholar
• Demetri, G.D.; Benjamin, R.S.; Blanke, C.D.; Blay, J.Y.; Casali, P.; Choi, H.; Corless, C.L.; Debiec-Rychter, M.; DeMatteo, R.P.; Ettinger, D.S.; Fisher, G.A.; Fletcher, C.D.; Gronchi, A.; Hohenberger, P.; Hughes, M.; Joensuu, H.; Judson, I.; Le, C.A.; Maki, R.G.; Morse, M.; Pappo, A.S.; Pisters, P.W.; Raut, C.P.; Reichardt, P.; Tyler, D.S.; Van Den Abbeele, A.D.; von, M.M.; Wayne, J.D.; Zalcberg, J. NCCN Task Force report: management of patients with gastrointestinal stromal tumor (GIST) –update of the NCCN clinical practice guidelines. J Natl Compr Canc Netw 2007, 5(Suppl. 2), S1–S29.
   PubMedGoogle Scholar
• Heinrich, M.C.; Corless, C.L.; Demetri, G.D.; Blanke, C.D.; von Mehren, M.; Joensuu, H.; McGreevey, L.S.; Chen, C.J.; Van Den Abbeele, A.D.; Druker, B.J.; Kiese, B.; Eisenberg, B.; Roberts, P.J.; Singer, S.; Fletcher, C.D.; Silberman, S.; Dimitrijevic, S.; Fletcher, J.A. Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor. J Clin Oncol 2003, 21(23), 4342–4349.
   PubMed Web of Science ®Google Scholar
• Rubin, B.P.; Singer, S.; Tsao, C.; Duensing, A.; Lux, M.L.; Ruiz, R.; Hibbard, M.K.; Chen, C.J.; Xiao, S.; Tuveson, D.A.; Demetri, G.D.; Fletcher, C.D.; Fletcher, J.A. KIT activation is a ubiquitous feature of gastrointestinal stromal tumors. Cancer Res 2001, 61(22), 8118–8121.
   PubMed Web of Science ®Google Scholar
• Debiec-Rychter, M.; Sciot, R.; Le Cesne, A.; Schlemmer, M.; Hohenberger, P.; van Oosterom, A.T.; Blay, J.Y.; Leyvraz, S.; Stul, M.; Casali, P.G.; Zalcberg, J.; Verweij, J.; Van, G.M.; Hagemeijer, A.; Judson, I. KIT mutations and dose selection for imatinib in patients with advanced gastrointestinal stromal tumours. Eur J Cancer 2006, 42(8), 1093–1103.
   PubMed Web of Science ®Google Scholar
• Corless, C.L.; McGreevey, L.; Haley, A.; Town, A.; Heinrich, M.C. KIT mutations are common in incidental gastrointestinal stromal tumors one centimeter or less in size. Am J Pathol 2002, 160(5), 1567–1572.
   PubMed Web of Science ®Google Scholar
• Wardelmann, E.; Losen, I.; Hans, V.; Neidt, I.; Speidel, N.; Bierhoff, E.; Heinicke, T.; Pietsch, T.; Buttner, R.; Merkelbach-Bruse, S. Deletion of Trp-557 and Lys-558 in the juxtamembrane domain of the c-kit protooncogene is associated with metastatic behavior of gastrointestinal stromal tumors. Int J Cancer 2003, 106(6), 887–895.
   PubMed Web of Science ®Google Scholar
• Lasota, J.; Miettinen, M. Clinical significance of oncogenic KIT and PDGFRA mutations in gastrointestinal stromal tumours. Histopathology 2008, 53(3), 245–266.
   PubMed Web of Science ®Google Scholar
• Lasota, J.; Stachura, J.; Miettinen, M. GISTs with PDGFRA exon 14 mutations represent subset of clinically favorable gastric tumors with epithelioid morphology. Lab Invest 2006, 86(1), 94–100.
   PubMed Web of Science ®Google Scholar
• Joensuu, H. Gastrointestinal stromal tumor (GIST). Ann Oncol 2006, 17(Suppl. 10), x280–x286.
   PubMed Web of Science ®Google Scholar
• Corless, C.L.; Fletcher, J.A.; Heinrich, M.C. Biology of gastrointestinal stromal tumors. J Clin Oncol 2004, 22(18), 3813–3825.
   PubMed Web of Science ®Google Scholar
• Miettinen, M.; Lasota, J.; Sobin, L.H. Gastrointestinal stromal tumors of the stomach in children and young adults: a clinicopathologic, immunohistochemical, and molecular genetic study of 44 cases with long-term follow-up and review of the literature. Am J Surg Pathol 2005, 29(10), 1373–1381.
   PubMed Web of Science ®Google Scholar
• Agaram, N.P.; LaQuaglia, M.P.; Ustun, B.; Guo, T.; Wong, G.C.; Socci, N.D.; Maki, R.G.; DeMatteo, R.P.; Besmer, P.; Antonescu, C.R. Molecular characterization of pediatric gastrointestinal stromal tumors. Clin Cancer Res 2008, 14(10), 3204–3215.
   PubMed Web of Science ®Google Scholar
• Prakash, S.; Sarran, L.; Socci, N.; DeMatteo, R.P.; Eisenstat, J.; Greco, A.M.; Maki, R.G.; Wexler, L.H.; LaQuaglia, M.P.; Besmer, P.; Antonescu, C.R. Gastrointestinal stromal tumors in children and young adults: a clinicopathologic, molecular, and genomic study of 15 cases and review of the literature. J Pediatr Hematol Oncol 2005, 27(4), 179–187.
   PubMed Web of Science ®Google Scholar
• Liegl, B.; Kepten, I.; Le, C.; Zhu, M.; Demetri, G.D.; Heinrich, M.C.; Fletcher, C.D.; Corless, C.L.; Fletcher, J.A. Heterogeneity of kinase inhibitor resistance mechanisms in GIST. J Pathol 2008, 216(1), 64–74.
   PubMed Web of Science ®Google Scholar
• Rubin, B.P.; Heinrich, M.C.; Corless, C.L. Gastrointestinal stromal tumour. Lancet 2007, 369(9574), 1731–1741.
   PubMed Web of Science ®Google Scholar
• Debiec-Rychter, M.; Dumez, H.; Judson, I.; Wasag, B.; Verweij, J.; Brown, M.; Dimitrijevic, S.; Sciot, R.; Stul, M.; Vranck, H.; Scurr, M.; Hagemeijer, A.; Van Glabbeke, M.; van Oosterom, A.T. Use of c-KIT/PDGFRA mutational analysis to predict the clinical response to imatinib in patients with advanced gastrointestinal stromal tumours entered on phase I and II studies of the EORTC Soft Tissue and Bone Sarcoma Group. Eur J Cancer 2004, 40(5), 689–695.
   PubMed Web of Science ®Google Scholar
• Heinrich, M.C.; Owzar, K.; Corless, C.L.; Hollis, D.; Borden, E.C.; Fletcher, C.D.; Ryan, C.W.; von, M.M.; Blanke, C.D.; Rankin, C.; Benjamin, R.S.; Bramwell, V.H.; Demetri, G.D.; Bertagnolli, M.M.; Fletcher, J.A. Correlation of kinase genotype and clinical outcome in the North American Intergroup Phase III Trial of imatinib mesylate for treatment of advanced gastrointestinal stromal tumor: CALGB 150105 study by Cancer and Leukemia Group B and Southwest Oncology Group. J Clin Oncol 2008, 26(33), 5360–5367.
   PubMed Web of Science ®Google Scholar
• Nakagomi, N.; Hirota, S. Juxtamembrane-type c-kit gene mutation found in aggressive systemic mastocytosis induces imatinib-resistant constitutive KIT activation. Lab Invest 2007, 87(4), 365–371.
   PubMed Web of Science ®Google Scholar
• Sciot, R.; Debiec-Rychter, M.; Daugaard, S.; Fisher, C.; Collin, F.; Glabbeke, M.V.; Verweij, J.; Blay, J.Y.; Hogendoorn, P.C. Distribution and prognostic value of histopathologic data and immunohistochemical markers in gastrointestinal stromal tumours (GISTs): an analysis of the EORTC phase III trial of treatment of metastatic GISTs with imatinib mesylate. Eur J Cancer 2008, 44(13), 1855–1860.
   PubMed Web of Science ®Google Scholar
• Heinrich, M.C.; Corless, C.L.; Blanke, C.D.; Demetri, G.D.; Joensuu, H.; Roberts, P.J.; Eisenberg, B.L.; von, M.M.; Fletcher, C.D.; Sandau, K.; McDougall, K.; Ou, W.B.; Chen, C.J.; Fletcher, J.A. Molecular correlates of imatinib resistance in gastrointestinal stromal tumors. J Clin Oncol 2006, 24(29), 4764–4774.
   PubMed Web of Science ®Google Scholar
• Wakai, T.; Kanda, T.; Hirota, S.; Ohashi, A.; Shirai, Y.; Hatakeyama, K. Late resistance to imatinib therapy in a metastatic gastrointestinal stromal tumour is associated with a second KIT mutation. Br J Cancer 2004, 90(11), 2059–2061.
   PubMed Web of Science ®Google Scholar
• Antonescu, C.R.; Besmer, P.; Guo, T.; Arkun, K.; Hom, G.; Koryotowski, B.; Leversha, M.A.; Jeffrey, P.D.; Desantis, D.; Singer, S.; Brennan, M.F.; Maki, R.G.; DeMatteo, R.P. Acquired resistance to imatinib in gastrointestinal stromal tumor occurs through secondary gene mutation. Clin Cancer Res 2005, 11(11), 4182–4190.
   PubMed Web of Science ®Google Scholar
• Wardelmann, E.; Thomas, N.; Merkelbach-Bruse, S.; Pauls, K.; Speidel, N.; Buttner, R.; Bihl, H.; Leutner, C.C.; Heinicke, T.; Hohenberger, P. Acquired resistance to imatinib in gastrointestinal stromal tumours caused by multiple KIT mutations. Lancet Oncol 2005, 6(4), 249–251.
   PubMed Web of Science ®Google Scholar
• Wardelmann, E.; Merkelbach-Bruse, S.; Pauls, K.; Thomas, N.; Schildhaus, H.U.; Heinicke, T.; Speidel, N.; Pietsch, T.; Buettner, R.; Pink, D.; Reichardt, P.; Hohenberger, P. Polyclonal evolution of multiple secondary KIT mutations in gastrointestinal stromal tumors under treatment with imatinib mesylate. Clin Cancer Res 2006, 12(6), 1743–1749.
   PubMed Web of Science ®Google Scholar
• Rutkowski, P.; Symonides, M.; Zdzienicki, M.; Siedlecki, J.A. Developments in targeted therapy of advanced gastrointestinal stromal tumors. Recent Patents Anticancer Drug Discov 2008, 3(2), 88–99.
   PubMed Web of Science ®Google Scholar
• Petain, A.; Kattygnarath, D.; Azard, J.; Chatelut, E.; Delbaldo, C.; Geoerger, B.; Barrois, M.; Seronie-Vivien, S.; LeCesne, A.; Vassal, G. Population pharmacokinetics and pharmacogenetics of imatinib in children and adults. Clin Cancer Res 2008, 14(21), 7102–7109.
   PubMed Web of Science ®Google Scholar
• Maki, R.G.; Fletcher, J.A.; Heinrich, M.C.; Morgan, J.A.; George, S.; Desai, J.; Scheu, K.; Fletcher, C.D.; Baum, C.; Demetri, G.D. Results from a continuation trial of SU11248 in patients (pts) with imatinib (IM)-resistant gastrointestinal stromal tumor (GIST) [Abstract]. J Clin Oncol 2005, 23(16S), 818S.
   Google Scholar
• Heinrich, M.C.; Maki, R.G.; Corless, C.L.; Antonescu, C.R.; Harlow, A.; Griffith, D.; Town, A.; McKinley, A.; Ou, W.-B.; Fletcher, J.A.; Fletcher, C.D.M.; Huang, X.; Cohen, D.P.; Baum, C.M.; Demetri, D.G. Primary and secondary kinase genotypes correlate with the biological and clinical activity of sunitinib malate in imatinib-resistant. J Clin Oncol 2008, 26(33), 5352–5359.
   PubMed Web of Science ®Google Scholar
• Demetri, G.D.; van Oosterom, A.T.; Garrett, C.R.; Blackstein, M.E.; Shah, M.H.; Verweij, J.; McArthur, G.; Judson, I.R.; Heinrich, M.C.; Morgan, J.A.; Desai, J.; Fletcher, C.D.; George, S.; Bello, C.L.; Huang, X.; Baum, C.M.; Casali, P.G. Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial. Lancet 2006, 368(9544), 1329–1338.
   PubMed Web of Science ®Google Scholar
• George, S.; Blay, J.Y.; Casali, P.G.; Le, C.A.; Stephenson, P.; DePrimo, S.E.; Harmon, C.S.; Law, C.N.; Morgan, J.A.; Ray-Coquard, I.; Tassell, V.; Cohen, D.P.; Demetri, G.D. Clinical evaluation of continuous daily dosing of sunitinib malate in patients with advanced gastrointestinal stromal tumour after imatinib failure. Eur J Cancer 2009, 45(11), 1959–1968.
   PubMed Web of Science ®Google Scholar
• Reichardt, P.; Kang, Y.; Ruka, W.; Seddon, B.; Guerriero, B.; Breazna, A.; Lowry, S.; Demetri, G.D. Detailed analysis of survival and safety with sunitinib (SU) in a worldwide treatment-use trial of patients with advanced GIST [Abstract]. J Clin Oncol 2008, 26(15S), 565S.
   Google Scholar
• Demetri, D.G.; Casali, P.G.; Blackstein, M. Assessment of soluble KIT as a potential surrogate marker for time to tumour progression in sunitinib-treated patients with advanced gastrointestinal stromal tumour. Presented at 19th International Congress on Anti-Cancer Treatment, Paris, France, 2008.
   Google Scholar
• Prenen, H.; Cools, J.; Mentens, N.; Folens, C.; Sciot, R.; Schöffski, P.; Van, O.A.; Marynen, P.; Debiec-Rychter, M. Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate. Clin Cancer Res 2006, 12(8), 2622–2627.
   PubMed Web of Science ®Google Scholar
• Gajiwala, K.S.; Wu, J.C.; Christensen, J.; Deshmukh, G.D.; Diehl, W.; DiNitto, J.P.; English, J.M.; Greig, M.J.; He, Y.A.; Jacques, S.L.; Lunney, E.A.; McTigue, M.; Molina, D.; Quenzer, T.; Wells, P.A.; Yu, X.; Zhang, Y.; Zou, A.; Emmett, M.R.; Marshall, A.G.; Zhang, H.M.; Demetri, G.D. KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients. Proc Natl Acad Sci U S A 2009, 106(5), 1542–1547.
   PubMed Web of Science ®Google Scholar
• Dewaele, B.; Wasag, B.; Cools, J.; Sciot, R.; Prenen, H.; Vandenberghe, P.; Wozniak, A.; Schoffski, P.; Marynen, P.; Debiec-Rychter, M. Activity of dasatinib, a dual SRC/ABL kinase inhibitor, and IPI-504, a heat shock protein 90 inhibitor, against gastrointestinal stromal tumor-associated PDGFRAD842V mutation. Clin Cancer Res 2008, 14(18), 5749–5758.
   PubMed Web of Science ®Google Scholar
• Reichardt, P. Novel approaches to imatinib- and sunitinib-resistant GIST. Curr Oncol Rep 2008, 10(4), 344–349.
   PubMedGoogle Scholar
• Floris, G.; Debiec-Rychter, M.; Sciot, R.; Stefan, C.; Fieuws, S.; Machiels, K.; Atadja, P.; Wozniak, A.; Faa, G.; Schoffski, P. High efficacy of panobinostat towards human gastrointestinal stromal tumors in a xenograft mouse model. Clin Cancer Res 2009, 15(12), 4066–4076.
   PubMed Web of Science ®Google Scholar