Gastrointestinal Stromal Tumor

In a retrospective study of 1124 sunitinib-treated gastrointestinal stromal tumor patients, patients with primary KIT exon 11 mutations (n=143) were associated with decreased progression free surviva… (full text at CIViC)

PMID 26772734 · Reichardt et al., 2016 · Open in CIViC

This phase II clinical trial of regorafenib (NCT01068769) examined the long term safety and efficacy of regorafenib in patients with metastatic and/or unresectable gastrointestinal stromal tumors (GIS… (full text at CIViC)

PMID 27371698 · Ben-Ami et al., 2016 · Open in CIViC

Patients with exon 9 mutations treated with a higher dose of imatinib (800mg vs. 400 mg daily) experienced improved progression-free survival compared to those treated with the standard dose (HR:0.392… (full text at CIViC)

PMID 16624552 · Debiec-Rychter et al., 2006 · Open in CIViC

Molecular models predict that deletion of a portion of the juxtamembrane domain relieves steric hindrance and results in higher binding affinity for imatinib.

PMID 21364689 · Pierotti et al., 2011 · Open in CIViC

Molecular models predict that deletion of a portion of the juxtamembrane domain relieves steric hindrance and results in higher binding affinity for imatinib.

PMID 21364689 · Pierotti et al., 2011 · Open in CIViC

In a phase 1/2 trial of 97 gastrointestinal stromal tumor patients, patients with KIT exon 11 mutations (44/77) treated with sunitinib were associated with shorter progression free survival (5.1mo vs.… (full text at CIViC)

PMID 18955458 · Heinrich et al., 2008 · Open in CIViC

In a retrospective study of 1124 sunitinib-treated gastrointestinal stromal tumor patients, patients with primary KIT exon 11 mutations (n=143) were associated with decreased progression free surviva… (full text at CIViC)

In a retrospective study, a Chinese gastrointestinal stromal tumor patient harboring KIT Y553_W557delYEVQW deletion mutation (n=1/2) was associated with improved response to sunitinib treatment after … (full text at CIViC)

PMID 23456621 · Gao et al., 2013 · Open in CIViC

In a phase 1/2 trial of 97 gastrointestinal stromal tumor patients, patients with KIT exon 11 mutations (44/77) treated with sunitinib were associated with shorter progression free survival (5.1mo vs.… (full text at CIViC)

PMID 18955458 · Heinrich et al., 2008 · Open in CIViC

In a retrospective study of 1124 sunitinib-treated gastrointestinal stromal tumor patients, patients with primary KIT exon 11 mutations (n=143) were associated with decreased progression free surviva… (full text at CIViC)

PMID 26772734 · Reichardt et al., 2016 · Open in CIViC

147 patients with advanced, unresectable GISTs were enrolled onto a randomized, phase II clinical study of imatinib (CSTI571-B2222). Specimens from 43 pretreatment and/or imatinib-resistant tumors wer… (full text at CIViC)

PMID 16954519 · Heinrich et al., 2006 · Open in CIViC

A 58-year-old male with NTRK-fusion positive gastrointestinal stromal tumour (GIST) demonstrated initial response to Larotrectinib but progressed after developing a gatekeeper mutation (TRKC F617L).

PMID 30624546 · Hong et al., 2019 · Open in CIViC

In CHO cells with PDGFRA D842I mutation that have shown imatinib resistance, crenolanib was significantly more potent at inhibiting kinase activity than imatinib.

PMID 22745105 · Heinrich et al., 2012 · Open in CIViC

In CHO cells with PDGFRA DI842-843VM mutation that have shown imatinib resistance, crenolanib was significantly more potent at inhibiting kinase activity than imatinib.

PMID 22745105 · Heinrich et al., 2012 · Open in CIViC

In an in vitro study, Ba/F3 cells expressing PDGFRA D842_M844delDIM mutation were associated withsensitivity to dasatinib treatment.(IC50: 10nM). Sensitivity was determined by assessing cell prolifera… (full text at CIViC)

PMID 18794084 · Dewaele et al., 2008 · Open in CIViC

GIST tumors harboring PDGFRA D842V mutation are more likely to be benign than malignant.

PMID 15146165 · Lasota et al., 2004 · Open in CIViC

In a phase 2 trial, patients with gastrointestinal stromal tumor (GIST) harboring with PDGFRA D842V or other exon 18 mutation were treated with Avapritinib which have broad activity against oncogenic … (full text at CIViC)

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In CHO cells with PDGFRA D842V mutation that have shown imatinib resistance, crenolanib was significantly more potent at inhibiting kinase activity than imatinib.

PMID 22745105 · Heinrich et al., 2012 · Open in CIViC

In CHO cells with PDGFRA D842Y mutation that have shown imatinib resistance, crenolanib was significantly more potent at inhibiting kinase activity than imatinib.

PMID 22745105 · Heinrich et al., 2012 · Open in CIViC

In phase I NAVIGATOR trial (NCT02508532) took part 43 patients with GIST harboring a PDGFRA exon 18 mutation, including 38 patients with PDGFRA D842V mutation.For patients harboring a PDGFRA exon 18 … (full text at CIViC)

PMID 30274985 · Gebreyohannes et al., 2019 · Open in CIViC

These four patients were part of a larger cohort of 397 patients with incurable (i.e. metastatic or unresectable) CD117-positive Gastrointestinal stromal tumors (GISTs) enrolled in the North American … (full text at CIViC)

PMID 18955451 · Heinrich et al., 2008 · Open in CIViC

In CHO cells with the PDGFRA deletion I843 mutation that have shown imatinib sensitivity, crenolanib showed no significant difference from imatinib in kinase activity inhibition.

PMID 22745105 · Heinrich et al., 2012 · Open in CIViC

15/127 patients with KIT-WT metastatic gastrointestinal stromal tumors were tested for PDGFRA mutations. 6 GISTs harbored PDGFRA mutations. 1 patient had a deletion of I843. CHO cells expressing this … (full text at CIViC)

PMID 14645423 · Heinrich et al., 2003 · Open in CIViC

In a retrospective study of 23 Taiwanese gastrointestinal stromal tumor patients, a patient with PDGFRA exon 18 mutation (n=1/21) was associated with partial response to sunitinib treatment.

PMID 21547131 · Chen et al., 2011 · Open in CIViC

In this retrospective survey among referral centers and collaborative groups with experience in conducting clinical studies in sarcoma and/or GISTs in Europe, 58 patients were included with advanced P… (full text at CIViC)

PMID 22718859 · Cassier et al., 2012 · Open in CIViC

This prospective study of 127 patients with metastatic gastrointestinal stromal tumors (GISTs) examined the relationship between kinase (KIT and PDGFRA) genotype and treatment outcome for patients enr… (full text at CIViC)

PMID 14645423 · Heinrich et al., 2003 · Open in CIViC

In this phase III trial, 240 patients with histologically confirmed, metastatic or unresectable GIST, with failure of at least previous imatinib and sunitinib were randomized in 2:1 to receive either …

293T cells stably transduced with PDGFRA V561A showed constitutive tyrosine phosphorylation in the absense of ligand; however, when treated with imatinib, this phosphorylation was inhibited similarly … (full text at CIViC)

PMID 12949711 · Hirota et al., 2003 · Open in CIViC

This case study examines one patient from a larger cohort of 397 patients with incurable (i.e. metastatic or unresectable) CD117-positive Gastrointestinal stromal tumors (GISTs) enrolled in the North … (full text at CIViC)

PMID 18955451 · Heinrich et al., 2008 · Open in CIViC

In a gastrointestinal stromal tumor patient harboring PDGFRA W559_R560delWR in-frame deletion mutation, PDGFRA W559_R560delWR was reported to be sensitive to sunitinib treatment. The patient was treat… (full text at CIViC)

PMID 26396737 · Brohl et al., 2015 · Open in CIViC

In an in vitro study, a TT cell line expressing RET C634W mutation demonstrated increased sensitivity to regorafenib treatment (IC50: 34nM vs. 560-3269nM) compared to HepG2, SW620, Colo-205 or A375 ce… (full text at CIViC)

PMID 21170960 · Wilhelm et al., 2011 · Open in CIViC