論文 - 詳細
| RRC ID | 74819 |
|---|---|
| 著者 | 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. |
| タイトル | NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations. |
| ジャーナル | 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. |
| 巻・号 | 13(3) |
| ページ | 598-615 |
| 公開日 | 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 |
| リソース情報 | |
| ヒト・動物細胞 | Ba/F3 |