RRC ID 74819
Author Drilon A, Horan JC, Tangpeerachaikul A, Besse B, Ou SI, Gadgeel SM, Camidge DR, van der Wekken AJ, Nguyen-Phuong L, Acker A, Keddy C, Nicholson KS, Yoda S, Mente S, Sun Y, Soglia JR, Kohl NE, Porter JR, Shair MD, Zhu V, Davare MA, Hata AN, Pelish HE, Lin JJ.
Title NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations.
Journal Cancer Discov
Abstract The combined preclinical features of NVL-520 that include potent targeting of ROS1 and diverse ROS1 resistance mutations, high selectivity for ROS1 G2032R over TRK, and brain penetration mark the development of a distinct ROS1 TKI with the potential to surpass the limitations of earlier-generation TKIs for ROS1 fusion-positive patients. This article is highlighted in the In This Issue feature, p. 517.
Volume 13(3)
Pages 598-615
Published 2023-3-1
DOI 10.1158/2159-8290.CD-22-0968
PII 716750
PMID 36511802
PMC PMC9975673
MeSH Aminopyridines Brain Carcinoma, Non-Small-Cell Lung* / genetics Humans Lactams Lactams, Macrocyclic / pharmacology Lung Neoplasms* / genetics Mutation Protein Kinase Inhibitors / pharmacology Protein Kinase Inhibitors / therapeutic use Protein-Tyrosine Kinases / genetics Proto-Oncogene Proteins / genetics Pyrazoles
IF 29.497
Resource
Human and Animal Cells Ba/F3