NVL-520 is a selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations Journal Article
| Authors: | Drilon, A.; Horan, J. C.; Tangpeerachaikul, A.; Besse, B.; Ou, S. H. I.; Gadgeel, S. M.; Camidge, D. R.; van der Wekken, A. J.; Nguyen-Phuong, L.; Acker, A.; Keddy, C.; Nicholson, K. S.; Yoda, S.; Mente, S.; Sun, Y.; Soglia, J. R.; Kohl, N. E.; Porter, J. R.; Shair, M. D.; Zhu, V.; Davare, M. A.; Hata, A. N.; Pelish, H. E.; Lin, J. J. |
| Article Title: | NVL-520 is a selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations |
| Abstract: | SIGNIFICANCE: 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. ©2022 The Authors; Published by the American Association for Cancer Research. |
| Keywords: | oncoprotein; genetics; mutation; proto-oncogene proteins; protein kinase inhibitor; carcinoma, non-small-cell lung; lung neoplasms; protein tyrosine kinase; protein kinase inhibitors; lung tumor; brain; pyrazole derivative; pyrazoles; protein-tyrosine kinases; lactams; lactams, macrocyclic; macrocyclic lactam; non small cell lung cancer; humans; human; lactam; aminopyridines; aminopyridine derivative; ros1 protein, human |
| Journal Title: | Cancer Discovery |
| Volume: | 13 |
| Issue: | 3 |
| ISSN: | 2159-8274 |
| Publisher: | American Association for Cancer Research |
| Date Published: | 2023-03-01 |
| Start Page: | 598 |
| End Page: | 615 |
| Language: | English |
| DOI: | 10.1158/2159-8290.Cd-22-0968 |
| PUBMED: | 36511802 |
| PROVIDER: | scopus |
| PMCID: | PMC9975673 |
| DOI/URL: | |
| Notes: | The MSK Cancer Center Support Grant (P30 CA008748) is acknowledged in the PDF -- Source: Scopus |
