The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations
Open accessAbstract
Significance: Overcoming resistance to targeted kinase inhibitors is a major clinical challenge in oncology. Development of crizotinib resistance through the emergence of a secondary ROS1 mutation, ROS1 G2032R , was observed in patients with ROS1 fusion-positive lung cancer. In addition, a novel ROS1 fusion recently has been identified in glioblastoma. A new agent with robust activity against the ROS1 G2032R mutation and with CNS activity is needed to address these unmet medical needs. Here we report the identification of PF-06463922, a ROS1/anaplastic lymphoma kinase (ALK) inhibitor, with exquisite potency against ROS1 fusion kinases, capable of inhibiting the ROS1 G2032R mutation and FIG-ROS1–driven glioblastoma tumor growth in preclinical models. PF-06463922 demonstrated excellent therapeutic potential against ROS1 fusion-driven cancers, and it currently is undergoing phase I/II clinical trial investigation.
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Cites
Crizotinib in ROS1-Rearranged Non–Small-Cell Lung Cancer
Shaw, A. T., Ou, S.-H. I., Bang, Y.-J., Camidge, D. R., Solomon, B. J., Salgia, R., Riely, G. J., Varella-Garcia, M., Shapiro, G. I., Costa, D. B., et al. (2014) · New England Journal of Medicine · doi:10.1056/nejmoa1406766 · Cited by 1,964
ROS1 Rearrangements Define a Unique Molecular Class of Lung Cancers
Bergethon, K., Shaw, A. T., Ignatius Ou, S.-H., Katayama, R., Lovly, C. M., McDonald, N. T., Massion, P. P., Siwak-Tapp, C., Gonzalez, A., Fang, R., et al. (2012) · Journal of Clinical Oncology · doi:10.1200/jco.2011.35.6345 · Cited by 1,555
Cited by
Shaw, A. T., Felip, E., Bauer, T. M., Besse, B., Navarro, A., Postel-Vinay, S., Gainor, J. F., Johnson, M., Dietrich, J., James, L. P., et al. (2017) · The Lancet Oncology · doi:10.1016/s1470-2045(17)30680-0 · Cited by 659
Drilon, A., Ou, S.-H. I., Cho, B. C., Kim, D.-W., Lee, J., Lin, J. J., Zhu, V. W., Ahn, M.-J., Camidge, D. R., Nguyen, J., et al. (2018) · Cancer Discovery · doi:10.1158/2159-8290.cd-18-0484 · Cited by 504
Scientific Advances in Lung Cancer 2015
Tsao, A. S., Scagliotti, G. V., Bunn, P. A., Carbone, D. P., Warren, G. W., Bai, C., de Koning, H. J., Yousaf-Khan, A. U., McWilliams, A., Tsao, M. S., et al. (2016) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2016.03.012 · Cited by 284
Papadopoulos, K. P., Borazanci, E., Shaw, A. T., Katayama, R., Shimizu, Y., Zhu, V. W., Sun, T. Y., Wakelee, H. A., Madison, R., Schrock, A. B., et al. (2020) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-20-1630 · Cited by 113
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., et al. (2023) · Cancer Discovery · doi:10.1158/2159-8290.cd-22-0968 · Cited by 52
Metadata
- Authors
- Zou, H. Y., Li, Q., Engstrom, L. D., West, M., Appleman, V., Wong, K. A., McTigue, M., Deng, Y.-L., Liu, W., Brooun, A., Timofeevski, S., McDonnell, S. R. P., Jiang, P., Falk, M. D., Lappin, P. B., Affolter, T., Nichols, T., Hu, W., Lam, J., Johnson, T. W., Smeal, T., Charest, A., & Fantin, V. R.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2015-03-02
- Volume
- 112
- Issue
- 11
- Pages
- 3493-3498
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2052546787
- Cited by
- 267
- References
- 2
- FWCI
- 24.26
- Type
- journal article
- Language
- en
- Open access
- green
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- The paper
- Zou, H. Y., Li, Q., Engstrom, L. D., West, M., Appleman, V., Wong, K. A., McTigue, M., Deng, Y.-L., Liu, W., Brooun, A., Timofeevski, S., McDonnell, S. R. P., Jiang, P., Falk, M. D., Lappin, P. B., Affolter, T., Nichols, T., Hu, W., Lam, J., . . . Fantin, V. R. (2015). PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.1420785112
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.