src: clincancerres.aacrjournals.org
ALK inhibitors are potential anti-cancer drugs that act on tumours with variations of anaplastic lymphoma kinase (ALK) such as an EML4-ALK translocation.
Video ALK inhibitor
EML4-ALK
About 4-7% of non-small cell lung carcinomas (NSCLC) have EML4-ALK translocations.
Approved inhibitors
- crizotinib (Xalkori) (also a ROS1 inhibitor) approved in Aug 2011 by the US FDA for ALK-positive NSCLC.
- ceritinib (Zykadia), approved by the FDA in April 2014 for treatment of NSCLC.
- alectinib (Alecensa) (Chugai, NDA has been filed in Japan) (breakthrough status in U.S.) FDA approved Dec 2015 (accelerated), full approval in 2017 for ALK-positive NSCLC.
Maps ALK inhibitor
Clinical trials
Additional ALK inhibitors currently (or soon to be) undergoing clinical trials include:
- Dalantercept, ACE-041 (Acceleron)
- 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)
src: cancerdiscovery.aacrjournals.org
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.
src: cancerdiscovery.aacrjournals.org
References
src: clincancerres.aacrjournals.org
External links
- alkinhibitors.com
- ALK inhibitor discussion forum
Source of the article : Wikipedia