Defactinib (INN, codenamed VS-6063) is an inhibitor of PTK2, also known as focal adhesion kinase (FAK), Pyk2, and MELK which was developed by Pfizer and licensed to Verastem Oncology as a potential treatment for solid tumors.
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Other names | PF-04554878, VS-6063 |
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Formula | C20H21F3N8O3S |
Molar mass | 510.50 g·mol−1 |
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Development for mesothelioma was discontinued in 2015 due to lack of efficacy in a placebo-controlled phase II trial.[1][2] Subsequent research in patients with specific NF2 mutations also found limited activity.[3]
As of 2022, it remains in trials in combination with other medications for other types of cancer.
References
edit- ^ Nathan VL (2015-09-28). "Verastem stops cancer therapy development; shares plunge" (Press release). Reuters. Retrieved 2022-06-05.
- ^ Fennell DA, Baas P, Taylor P, Nowak AK, Gilligan D, Nakano T, et al. (April 2019). "Maintenance Defactinib Versus Placebo After First-Line Chemotherapy in Patients With Merlin-Stratified Pleural Mesothelioma: COMMAND-A Double-Blind, Randomized, Phase II Study". Journal of Clinical Oncology. 37 (10): 790–798. doi:10.1200/JCO.2018.79.0543. PMID 30785827. S2CID 73478275.
- ^ Jackman DM, Jegede O, Zauderer MG, Mitchell EP, Zwiebel J, Gray RJ, et al. (2021-05-20). "A phase 2 study of defactinib (VS-6063) in patients with NF2 altered tumors: Results from NCI-match (EAY131) subprotocol U.". Journal of Clinical Oncology. 39 (15_suppl). American Society of Clinical Oncology (ASCO): 3087. doi:10.1200/jco.2021.39.15_suppl.3087. ISSN 0732-183X. S2CID 236401789.