Blay JY, Kang YK, Nishida T, von Mehren M. Gastrointestinal stromal tumours. Nat Rev Dis Primers. 2021;7:22.
Hirota S, Isozaki K, Moriyama Y, Hashimoto K, Nishida T, Ishiguro S, et al. Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors. Science. 1998;279:577–80.
Heinrich MC, Corless CL, Duensing A, McGreevey L, Chen CJ, Joseph N, et al. PDGFRA activating mutations in gastrointestinal stromal tumors. Science. 2003;299:708–10.
Keung EZ, Raut CP. Management of gastrointestinal stromal tumors. Surg Clin North Am. 2017;97:437–52.
Demetri GD, von Mehren M, Blanke CD, Van den Abbeele AD, Eisenberg B, Roberts PJ, et al. Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. N Engl J Med. 2002;347:472–80.
Blanke CD, Rankin C, Demetri GD, Ryan CW, von Mehren M, Benjamin RS, et al. Phase III randomized, intergroup trial assessing imatinib mesylate at two dose levels in patients with unresectable or metastatic gastrointestinal stromal tumors expressing the kit receptor tyrosine kinase: S0033. J Clin Oncol. 2008;26:626–32.
Demetri GD, van Oosterom AT, Garrett CR, Blackstein ME, Shah MH, Verweij J, et al. Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial. Lancet. 2006;368:1329–38.
Demetri GD, Reichardt P, Kang YK, Blay JY, Rutkowski P, Gelderblom H, et al. Efficacy and safety of regorafenib for advanced gastrointestinal stromal tumours after failure of imatinib and sunitinib (GRID): an international, multicentre, randomised, placebo-controlled, phase 3 trial. Lancet. 2013;381:295–302.
Blay JY, Serrano C, Heinrich MC, Zalcberg J, Bauer S, Gelderblom H, et al. Ripretinib in patients with advanced gastrointestinal stromal tumours (INVICTUS): a double-blind, randomised, placebo-controlled, phase 3 trial. Lancet Oncol. 2020;21:923–34.
CAS PubMed PubMed Central Google Scholar
Kurokawa Y, Honma Y, Sawaki A, Naito Y, Iwagami S, Komatsu Y, et al. Pimitespib in patients with advanced gastrointestinal stromal tumor (CHAPTER-GIST-301): a randomized, double-blind, placebo-controlled phase III trial. Ann Oncol. 2022;33:959–67.
Bukowski K, Kciuk M, Kontek R. Mechanisms of Multidrug Resistance in Cancer Chemotherapy. Int J Mol Sci. 2020;21.
Zhou S, Abdihamid O, Tan F, Zhou H, Liu H, Li Z, et al. KIT mutations and expression: current knowledge and new insights for overcoming IM resistance in GIST. Cell Commun Signal. 2024;22:153.
CAS PubMed PubMed Central Google Scholar
Napolitano A, Vincenzi B. Secondary KIT mutations: the GIST of drug resistance and sensitivity. Br J Cancer. 2019;120:577–8.
PubMed PubMed Central Google Scholar
Heinrich MC, Jones RL, George S, Gelderblom H, Schöffski P, von Mehren M, et al. Ripretinib versus sunitinib in gastrointestinal stromal tumor: ctDNA biomarker analysis of the phase 3 INTRIGUE trial. Nat Med. 2024;30:498–506.
CAS PubMed PubMed Central Google Scholar
Serrano C, Bauer S, Gómez-Peregrina D, Kang YK, Jones RL, Rutkowski P, et al. Circulating tumor DNA analysis of the phase III VOYAGER trial: KIT mutational landscape and outcomes in patients with advanced gastrointestinal stromal tumor treated with avapritinib or regorafenib. Ann Oncol. 2023;34:615–25.
George S, Blay JY, Chi P, Jones RL, Serrano C, Somaiah N, et al. The INSIGHT study: a randomized, Phase III study of ripretinib versus sunitinib for advanced gastrointestinal stromal tumor with KIT exon 11 + 17/18 mutations. Future Oncol. 2024;20:1973–82.
PubMed PubMed Central Google Scholar
Hirota S, Ohashi A, Nishida T, Isozaki K, Kinoshita K, Shinomura Y, et al. Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors. Gastroenterology. 2003;125:660–7.
Corless CL, Schroeder A, Griffith D, Town A, McGreevey L, Harrell P, et al. PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib. J Clin Oncol. 2005;23:5357–64.
Debiec-Rychter M, Sciot R, Le Cesne A, Schlemmer M, Hohenberger P, van Oosterom AT, et al. KIT mutations and dose selection for imatinib in patients with advanced gastrointestinal stromal tumours. Eur J Cancer. 2006;42:1093–103.
Heinrich MC, Owzar K, Corless CL, Hollis D, Borden EC, Fletcher CD, et al. 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;26:5360–7.
CAS PubMed PubMed Central Google Scholar
Heinrich MC, Corless CL, Demetri GD, Blanke CD, von Mehren M, Joensuu H, et al. Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor. J Clin Oncol. 2003;21:4342–9.
Nishida T, Kanda T, Nishitani A, Takahashi T, Nakajima K, Ishikawa T, et al. Secondary mutations in the kinase domain of the KIT gene are predominant in imatinib-resistant gastrointestinal stromal tumor. Cancer Sci. 2008;99:799–804.
CAS PubMed PubMed Central Google Scholar
Casali PG, Zalcberg J, Le Cesne A, Reichardt P, Blay JY, Lindner LH, et al. Ten-year progression-free and overall survival in patients with unresectable or metastatic gi stromal tumors: long-term analysis of the European organisation for research and treatment of cancer, Italian sarcoma group, and Australasian gastrointestinal trials group intergroup phase iii randomized trial on imatinib at two dose levels. J Clin Oncol. 2017;35:1713–20.
Toulmonde M, Dinart D, Brahmi M, Verret B, Jean-Denis M, Ducimetière F, et al. Evolution of Patterns of Care and Outcomes in the Real-Life Setting for Patients with Metastatic GIST Treated in Three French Expert Centers over Three Decades. Cancers (Basel). 2023;15.
Schaefer IM, DeMatteo RP, Serrano C. The GIST of advances in treatment of advanced gastrointestinal stromal tumor. Am Soc Clin Oncol Educ Book. 2022;42:1–15.
PubMed PubMed Central Google Scholar
Kelly CM, Gutierrez Sainz L, Chi P. The management of metastatic GIST: current standard and investigational therapeutics. J Hematol Oncol. 2021;14:2.
CAS PubMed PubMed Central Google Scholar
Cassier PA, Fumagalli E, Rutkowski P, Schöffski P, Van Glabbeke M, Debiec-Rychter M, et al. Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era. Clin Cancer Res. 2012;18:4458–64.
Rizzo A, Pantaleo MA, Astolfi A, Indio V, Nannini M. The Identity of PDGFRA D842V-Mutant Gastrointestinal Stromal Tumors (GIST). Cancers (Basel). 2021;13.
Wada R, Arai H, Kure S, Peng WX, Naito Z. “Wild type” GIST: Clinicopathological features and clinical practice. Pathol Int. 2016;66:431–7.
Miselli FC, Casieri P, Negri T, Orsenigo M, Lagonigro MS, Gronchi A, et al. c-Kit/PDGFRA gene status alterations possibly related to primary imatinib resistance in gastrointestinal stromal tumors. Clin Cancer Res. 2007;13:2369–77.
Li K, Cheng H, Li Z, Pang Y, Jia X, Xie F, et al. Genetic progression in gastrointestinal stromal tumors: mechanisms and molecular interventions. Oncotarget. 2017;8:60589–604.
PubMed PubMed Central Google Scholar
Serrano C, Mariño-Enríquez A, Tao DL, Ketzer J, Eilers G, Zhu M, et al. Complementary activity of tyrosine kinase inhibitors against secondary kit mutations in imatinib-resistant gastrointestinal stromal tumours. Br J Cancer. 2019;120:612–20.
CAS PubMed PubMed Central Google Scholar
Hsueh YS, Lin CL, Chiang NJ, Yen CC, Li CF, Shan YS, et al. Selecting tyrosine kinase inhibitors for gastrointestinal stromal tumor with secondary KIT activation-loop domain mutations. PLoS ONE. 2013;8: e65762.
CAS PubMed PubMed Central Google Scholar
Jeffers M, Kappeler C, Kuss I, Beckmann G, Mehnert DH, Fredebohm J, et al. Broad spectrum of regorafenib activity on mutant KIT and absence of clonal selection in gastrointestinal stromal tumor (GIST): correlative analysis from the GRID trial. Gastric Cancer. 2022;25:598–608.
CAS PubMed PubMed Central Google Scholar
Yoshimura C, Nagatoishi S, Kuroda D, Kodama Y, Uno T, Kitade M, et al. Thermodynamic dissection of potency and selectivity of cytosolic hsp90 inhibitors. J Med Chem. 2021;64:2669–77.
Ohkubo S, Kodama Y, Muraoka H, Hitotsumachi H, Yoshimura C, Kitade M, et al. TAS-116, a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models. Mol Cancer Ther. 2015;14:14–22.
Neckers L, Workman P. Hsp90 molecular chaperone inhibitors: are we there yet? Clin Cancer Res. 2012;18:64–76.
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