|
Adenocarcinoma of lung (disorder)
|
|
0.700 |
GeneticVariation
|
CLINVAR |
Acquired resistance to crizotinib from a mutation in CD74-ROS1.
|
23724914 |
2013 |
|
Adenocarcinoma of lung (disorder)
|
|
0.700 |
CausalMutation
|
CLINVAR |
|
|
|
|
Non-Small Cell Lung Carcinoma
|
|
0.030 |
GeneticVariation
|
BEFREE |
Non-small-cell lung cancer (NSCLC) patients harboring ALK or ROS1 rearrangements invariably acquire resistance to the first- and second-generation tyrosine kinase inhibitors (TKIs), most notably ALK G1202R and ROS1 G2032R.
|
30683630 |
2019 |
|
Non-Small Cell Lung Carcinoma
|
|
0.030 |
GeneticVariation
|
BEFREE |
Development of the acquired ROS1 G2032R mutation has been reported as a resistant mechanism to ROS1 inhibitors in ROS1-rearranged (ROS1<sup>+</sup>) NSCLC patients.
|
29477381 |
2018 |
|
Non-Small Cell Lung Carcinoma
|
|
0.030 |
GeneticVariation
|
BEFREE |
In an ongoing phase I trial, the ALK tyrosine kinase inhibitor (TKI) crizotinib shows remarkable initial responses in patients with non-small cell lung cancer (NSCLC) harboring ROS1 fusions; however, cancers eventually develop crizotinib resistance due to acquired mutations such as G2032R in ROS1.
|
25351743 |
2015 |
|
Neoplasms
|
|
0.030 |
GeneticVariation
|
BEFREE |
The ROS1 G2032R mutation was identified in crizotinib-resistant tumors from one patient.
|
25688157 |
2015 |
|
Neoplasms
|
|
0.030 |
GeneticVariation
|
BEFREE |
In vivo, PF-06463922 showed marked antitumor activity in tumor models expressing FIG-ROS1, CD74-ROS1, and the CD74-ROS1(G2032R) mutation.
|
25733882 |
2015 |
|
Neoplasms
|
|
0.030 |
GeneticVariation
|
BEFREE |
We performed a biopsy of a resistant tumor and identified an acquired mutation leading to a glycine-to-arginine substitution at codon 2032 in the ROS1 kinase domain.
|
23724914 |
2013 |
|
Malignant Neoplasms
|
|
0.020 |
GeneticVariation
|
BEFREE |
Here we report that DS-6051b is effective in treating ROS1- or NTRK-rearranged cancer in preclinical models, including crizotinib-resistant ROS1 positive cancer with secondary kinase domain mutations especially G2032R mutation which is highly resistant to crizotinib as well as lorlatinib and entrectinib, next generation ROS1 inhibitors.
|
31399568 |
2019 |
|
Primary malignant neoplasm
|
|
0.020 |
GeneticVariation
|
BEFREE |
Here we report that DS-6051b is effective in treating ROS1- or NTRK-rearranged cancer in preclinical models, including crizotinib-resistant ROS1 positive cancer with secondary kinase domain mutations especially G2032R mutation which is highly resistant to crizotinib as well as lorlatinib and entrectinib, next generation ROS1 inhibitors.
|
31399568 |
2019 |
|
Primary malignant neoplasm
|
|
0.020 |
GeneticVariation
|
BEFREE |
The effect of the identified drug was assessed in the CD74-ROS1-mutant Ba/F3 cells and crizotinib-resistant patient-derived cancer cells (MGH047) harboring G2032R-mutated CD74-ROS1.
|
25351743 |
2015 |
|
Malignant Neoplasms
|
|
0.020 |
GeneticVariation
|
BEFREE |
The effect of the identified drug was assessed in the CD74-ROS1-mutant Ba/F3 cells and crizotinib-resistant patient-derived cancer cells (MGH047) harboring G2032R-mutated CD74-ROS1.
|
25351743 |
2015 |
|
Tumor Cell Invasion
|
|
0.010 |
GeneticVariation
|
BEFREE |
Combination of Twist1 siRNA and crizotinib significantly reduced cell vitality, inhibited cell invasion and migration, and promoted apoptosis in A549-CD74-ROS1 G2032R mutation cells.
|
29477381 |
2018 |