Regorafenib-resistant KIT mutants

Stable Identifier
Homo sapiens
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Regorafenib is a type II tyrosine kinase inhibitor that is approved for treatment of advanced gastrointestinal stromal tumors with KIT mutations. Regorafenib is effective in imatinib-resistant tumors carrying secondary mutations in exon 14 (gatekeeper mutation), and most KIT secondary mutations encoded by exons 17 and 18 (the activation loop) (Demetri et al, 2013; Serrano et al, 2017, Serrano et al, 2019; reviewed in Roskoski, 2018; Klug et al, 2018; ).
Literature References
PubMed ID Title Journal Year
28478525 Novel Insights into the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors

Morales-Barrera, R, Carles, J, Suárez, C, García-Valverde, A, Olivares, D, Valverde, C, George, S, Serrano, C

Target Oncol 2017
29704617 The role of small molecule Kit protein-tyrosine kinase inhibitors in the treatment of neoplastic disorders

Roskoski, R

Pharmacol. Res. 2018
30792533 Complementary activity of tyrosine kinase inhibitors against secondary kit mutations in imatinib-resistant gastrointestinal stromal tumours

Heinrich, MC, Ketzer, J, Bauer, S, Zhu, M, Presnell, A, Raut, CP, George, S, Mannan, AM, Serrano, C, Yu, C, Sicinska, E, Tao, DL, Rubin, BP, Fletcher, JA, Mariño-Enríquez, A, Demetri, GD, Eilers, G, Czaplinski, JT, McKinley, A

Br. J. Cancer 2019
29964125 Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases

Heinrich, MC, Kent, JD, Klug, LR

Pharmacol. Ther. 2018
12181401 Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors

Joensuu, H, Silberman, SL, Capdeville, R, Peng, B, Heinrich, MC, Singer, S, Roberts, PJ, Blanke, CD, von Mehren, M, Eisenberg, B, Fletcher, JA, Demetri, GD, Kiese, B, Corless, C, Silverman, SG, Fletcher, CD, Druker, BJ, Janicek, M, Dimitrijevic, S, Tuveson, DA, Van den Abbeele, AD

N. Engl. J. Med. 2002
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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