PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 35050442-10 2022 CONCLUSION: These data support the results of the GRID trial, and suggest that patients may benefit from regorafenib in the presence of KIT mutations and without the selection of particular mutation patterns that confer resistance. regorafenib 105-116 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 136-139 35585158-1 2022 Although KIT-mutant GISTs can be effectively treated with tyrosine kinase inhibitors (TKIs), many patients develop resistance to imatinib mesylate (IM) as well as the FDA-approved later-line agents sunitinib, regorafenib and ripretinib. regorafenib 209-220 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 9-12 35050442-0 2022 Broad spectrum of regorafenib activity on mutant KIT and absence of clonal selection in gastrointestinal stromal tumor (GIST): correlative analysis from the GRID trial. regorafenib 18-29 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 49-52 35050442-8 2022 Regorafenib showed PFS benefit across all primary and secondary KIT mutational subgroups examined. regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 64-67 32944848-0 2021 Durable Disease Control with Regorafenib in a Patient with Metastatic KIT-Mutated Colorectal Cancer. regorafenib 29-40 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 70-73 33947686-2 2021 Imatinib, sunitinib, and regorafenib are available as first, second, and third-line targeted therapies, respectively, for metastatic or unresectable KIT-driven GIST. regorafenib 25-36 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 149-152 32052681-3 2021 Regorafenib is an FDA approved oral multi-kinase inhibitor that blocks the activity of multiple protein kinases including those involved in the regulation of tumor angiogenesis [VEGFR1-3, TIE2], tumor microenvironment [PDGFR-beta, FGFR] and oncogenesis (KIT, RET, RAF-1, BRAF). regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 254-257 33307872-6 2021 Sunitinib and regorafenib are inhibitors of multiple tyrosine kinases, including KIT, PDGFRalpha, PDGFRbeta, and VEGFRs, and are approved for the management of imatinib- and imatinib/sunitinib-refractory GIST patients, respectively. regorafenib 14-25 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 81-84 32207565-1 2020 BACKGROUND: Regorafenib is a small molecule multikinase inhibitor that inhibits multiple kinases including BRAF, KIT, PDGFRB, RAF, RET, and VEGFR1-3. regorafenib 12-23 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 113-116 31608707-12 2020 Regorafenib is a multikinase inhibitor targeting BRAF, VEGFR-1/2/3, KIT, TIE-2, PDGFR-beta, fibroblast growth factor receptor 1 (FGFR-1), RET, RAF-1, and p38 MAP kinase. regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 68-71 32024476-9 2020 KIT secondary mutations were the only mechanism of resistance found across 10 imatinib-resistant GIST patients progressing to sunitinib or regorafenib. regorafenib 139-150 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 0-3 31471313-2 2019 Approved KIT inhibitors sunitinib and regorafenib have complementary activity against KIT resistance mutations. regorafenib 38-49 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 9-12 31471313-2 2019 Approved KIT inhibitors sunitinib and regorafenib have complementary activity against KIT resistance mutations. regorafenib 38-49 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 86-89 26865419-4 2016 A novel oral multikinase inhibitor regorafenib inhibits receptor tyrosine kinases expressed on stromal cells (vascular endothelial growth factor receptor 1-3, TIE2, PDGFR-beta, and fibroblast growth factors) and tumor cells (c-KIT, RET, and BRAF). regorafenib 35-46 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 225-230 30684595-2 2019 Sunitinib and regorafenib have been approved as the second and third line therapies to overcome some of these drug-resistance mutations; however, their limited clinical response, toxicity and resistance of the activation loop mutants still makes new therapies bearing different cKIT mutants activity spectrum profile highly demanded. regorafenib 14-25 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 278-282 29764854-2 2018 Treatment with the small-molecule inhibitors imatinib, sunitinib, and regorafenib resulted in resistance (c-KIT mutant tumors) or limited activity (c-KIT wild-type tumors). regorafenib 70-81 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 106-111 29764854-2 2018 Treatment with the small-molecule inhibitors imatinib, sunitinib, and regorafenib resulted in resistance (c-KIT mutant tumors) or limited activity (c-KIT wild-type tumors). regorafenib 70-81 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 148-153 29359239-3 2018 Regorafenib is a potent inhibitor of angiogenic (VEGFR 1-3, PDGFR-b) as well as oncogenic (c-KIT, RET, FGFR, Raf) kinases. regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 91-96 29334307-0 2018 Regorafenib regresses an imatinib-resistant recurrent gastrointestinal stromal tumor (GIST) with a mutation in exons 11 and 17 of c-kit in a patient-derived orthotopic xenograft (PDOX) nude mouse model. regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 130-135 30069758-1 2018 Regorafenib (BAY 73-4506, Stivarga ) is an oral diphenylurea multi-kinase inhibitor that targets angiogenic (VEGFR1-3, TIE2), stromal (PDGFR-beta, FGFR), and oncogenic receptor tyrosine kinases (KIT, RET, and RAF). regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 195-198 30069758-1 2018 Regorafenib (BAY 73-4506, Stivarga ) is an oral diphenylurea multi-kinase inhibitor that targets angiogenic (VEGFR1-3, TIE2), stromal (PDGFR-beta, FGFR), and oncogenic receptor tyrosine kinases (KIT, RET, and RAF). regorafenib 13-24 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 195-198 27371698-14 2016 CONCLUSIONS: Long-term follow-up of patients with metastatic GIST treated with regorafenib suggests particular benefit among patients with primary KIT exon 11 mutations and those with SDH-deficient GIST. regorafenib 79-90 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 147-150 30792533-2 2019 Once resistance emerges, targeting KIT with tyrosine kinase inhibitors (TKIs) sunitinib and regorafenib provides clinical benefit, albeit of limited duration. regorafenib 92-103 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 35-38 28478525-3 2017 Three tyrosine kinase inhibitors (TKIs) with KIT inhibitory activity - imatinib, sunitinib, and regorafenib - are approved to treat advanced GIST and have successfully exploited this addiction to KIT oncogenic signaling, demonstrating remarkable activity in a disease that historically had no successful systemic therapy options. regorafenib 96-107 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 45-48 28478525-3 2017 Three tyrosine kinase inhibitors (TKIs) with KIT inhibitory activity - imatinib, sunitinib, and regorafenib - are approved to treat advanced GIST and have successfully exploited this addiction to KIT oncogenic signaling, demonstrating remarkable activity in a disease that historically had no successful systemic therapy options. regorafenib 96-107 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 196-199 27167336-11 2016 Combinational treatment with KIT inhibitors (imatinib, regorafenib) enhanced the proapoptotic effect. regorafenib 55-66 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 29-32 26419617-1 2016 Regorafenib, an oral small-molecule multi kinase inhibitor, is able to block Vascular Endothelial Growth Factor Receptors (VEGFR-1, 2, and 3), Platelet-Derived Growth Factor Receptors (PDGF), Fibroblast Growth Factor (FGF) receptor 1, Raf, TIE-2, and the kinases KIT, RET, and BRAF. regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 263-266 23610528-2 2013 Regorafenib is an oral small-molecule multi kinase inhibitor, binding to several intracellular kinases, with powerful inhibitory activity against vascular endothelial growth factor receptors (VEGFR-1,VEGFR-2, and VEGFR-3), platelet-derived growth factor receptor, fibroblast growth factor receptor 1, Raf, TIE-2, and the kinases KIT, RET, and BRAF. regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 329-332 24405315-4 2014 Regorafenib, a KIT/PDGFRA/vascular endothelial growth factor receptor (VEGFR) oral kinase inhibitor, has been shown to improve progression-free survival in the third- or fourth-line setting. regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 15-18 24405315-9 2014 Regorafenib activity in this setting is believed to be due to its activity against oncogenic forms of KIT/PDGFRA. regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 102-105 24756792-1 2014 Regorafenib (BAY 73-4506, Stivarga ) is an oral diphenylurea multikinase inhibitor that targets angiogenic (VEGFR1-3, TIE2), stromal (PDGFR-beta, FGFR), and oncogenic receptor tyrosine kinases (KIT, RET, and RAF). regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 194-197 24756792-1 2014 Regorafenib (BAY 73-4506, Stivarga ) is an oral diphenylurea multikinase inhibitor that targets angiogenic (VEGFR1-3, TIE2), stromal (PDGFR-beta, FGFR), and oncogenic receptor tyrosine kinases (KIT, RET, and RAF). regorafenib 13-24 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 194-197 26651387-3 2016 AREAS COVERED: Regorafenib, an oral multitargeted inhibitor with activity against multiple kinases including KIT, RET, RAF1, BRAF, angiogenesis (VEGFR, TIE-2) and those involved in tumor microenvironment (PDGFR and FGFR) was introduced after the successful Phase III GRID (GIST - Regorafenib In progressive Disease) clinical trial. regorafenib 15-26 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 109-112 26327919-1 2015 Regorafenib (Stivarga, BAY 73-4506; Bayer Pharma AG, Berlin, Germany) is an oral multikinase inhibitor that targets the angiogenic tumor microenvironment and oncogenic kinases including vascular endothelial growth factor receptor 2 (VEGFR2), VEGFR1, VEGFR3, fibroblast growth factor receptor 1 (FGFR1), RAF, KIT, RET and BRAF. regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 308-311 26327919-1 2015 Regorafenib (Stivarga, BAY 73-4506; Bayer Pharma AG, Berlin, Germany) is an oral multikinase inhibitor that targets the angiogenic tumor microenvironment and oncogenic kinases including vascular endothelial growth factor receptor 2 (VEGFR2), VEGFR1, VEGFR3, fibroblast growth factor receptor 1 (FGFR1), RAF, KIT, RET and BRAF. regorafenib 13-21 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 308-311 25239608-2 2014 Imatinib, sunitinib, and regorafenib are approved therapies; however, efficacy is often limited by the acquisition of polyclonal secondary resistance mutations in KIT, with those located in the activation (A) loop (exons 17/18) being particularly problematic. regorafenib 25-36 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 163-166 25239608-4 2014 EXPERIMENTAL DESIGN: The cellular and in vivo activities of ponatinib, imatinib, sunitinib, and regorafenib against mutant KIT were evaluated using an accelerated mutagenesis assay and a panel of engineered and GIST-derived cell lines. regorafenib 96-107 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 123-126 24384849-5 2014 Treatment with tyrosine kinase inhibitors (TKIs) such as imatinib, sunitinib, and regorafenib is effective in controlling unresectable disease; however, drug resistance caused by secondary KIT or PDGFRA mutations eventually develops in 90% of cases. regorafenib 82-93 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 189-192 22614970-2 2012 Regorafenib is a structurally unique inhibitor of multiple cancer-associated kinases, including KIT and platelet-derived growth factor receptor (PDGFR), with broad-spectrum anticancer activity in preclinical and early-phase trials. regorafenib 0-11 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 96-99 22421192-1 2012 PURPOSE: Regorafenib is a novel oral multikinase inhibitor of angiogenic (VEGFR1-3, TIE2), stromal (PDGFR-beta, FGFR), and oncogenic kinases (KIT, RET, and RAF). regorafenib 9-20 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 142-145 22577890-1 2012 INTRODUCTION: Regorafenib (BAY 73-4506) is a novel, orally active, diphenylurea multikinase inhibitor of VEGFR1-3, c-KIT, TIE-2, PDGFR-beta, FGFR-1, RET, RAF-1, BRAF and p38 MAP kinase. regorafenib 14-25 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 115-120 22577890-1 2012 INTRODUCTION: Regorafenib (BAY 73-4506) is a novel, orally active, diphenylurea multikinase inhibitor of VEGFR1-3, c-KIT, TIE-2, PDGFR-beta, FGFR-1, RET, RAF-1, BRAF and p38 MAP kinase. regorafenib 27-38 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 115-120 21170960-4 2011 Furthermore, regorafenib inhibits additional angiogenic kinases (VEGFR1/3, platelet-derived growth factor receptor-beta and fibroblast growth factor receptor 1) and the mutant oncogenic kinases KIT, RET and B-RAF. regorafenib 13-24 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 194-197