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Cited by 267

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 access
Zou, Helen Y., Li, Qiuhua, Engstrom, Lars D., West, Melissa, Appleman, Vicky, Wong, Katy A., McTigue, Michele, Deng, Ya-Li, Liu, Wei, Brooun, Alexei, Timofeevski, Sergei, McDonnell, Scott R. P., Jiang, Ping, Falk, Matthew D., Lappin, Patrick B., Affolter, Timothy, Nichols, Tim, Hu, Wenyue, Lam, Justine, Johnson, Ted W., Smeal, Tod, Charest, Al, Fantin, Valeria R.·2015·Proceedings of the National Academy of Sciences

Abstract

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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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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CoChat. (2026). Citation check: PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations. https://app.cochat.ai/papers/10.1073/pnas.1420785112
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

Data sources

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.