ALK inhibitor
ALK inhibitors are potential anti-cancer drugs that act on tumours with variations of anaplastic lymphoma kinase (ALK) such as an EML4-ALK translocation.[1]
EML4-ALK
About 4-7% of non-small cell lung carcinomas (NSCLC) have EML4-ALK translocations.[2]
Approved inhibitors
- crizotinib (Xalkori) and ceritinib (Zykadia), approved by the FDA for treatment of NSCLC.[2][3][4]
- Alectinib (Chugai, NDA has been filed in Japan) (breakthrough status in U.S.) FDA approved Dec 2015.
Clinical trials
Additional ALK inhibitors currently (or soon to be) undergoing clinical trials include:
- Brigatinib (AP26113) (by Ariad) (breakthrough status in U.S.) (also an EGFR inhibitor)
- Entrectinib (Nerviano's NMS-E628, licensed by Ignyta and renamed RXDX-101, in the U.S. orphan drug designation and rare pediatric disease designation for the treatment of neuroblastoma and orphan drug designation for treatment of TrkA-, TrkB-, TrkC-, ROS1- and ALK-positive NSCLC)
- PF-06463922 (Pfizer)
- TSR-011 (Tesaro)
- CEP-37440 (Teva)
- X-396 (Xcovery)
Updates for several of these will be available at the start of June at ASCO 2014.
Discontinued
- ASP-3026 (Astellas)
NPM-ALK
NPM-ALK is a different variation/fusion of ALK that drives anaplastic large-cell lymphomas (ALCLs) and is the target of other ALK inhibitors.[5] [6]
References
- ↑ Nelsen (2010). "ALK Inhibitors: Possible New Treatment for Lung Cancer".
- 1 2 Farmer (2010). "Non-Small-Cell Lung Cancer Standards of Care Challenged by a Cornucopia of New Drugs".
- ↑ Chustecka (2010). "Crizotinib in ALK-NSCLC; Response Rate "Unprecedented"".
- ↑ "FDA Approves Ceritinib for ALK-Positive Lung Cancer". Medscape. April 29, 2014.
- ↑ Galkin; et al. (2007). "Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK".
- ↑ http://www.axonmedchem.com/product/1416tae684.html
External links
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