ALK inhibitor: Difference between revisions
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[[Image:ALK_positive_lung_adenocarcinoma_-_ALK_IHC_--_high_mag.jpg|thumb|right|[[Micrograph]] showing an [[ALK positive lung cancer|ALK positive adenocarcinoma of the lung]]. The ALK [[immunostain]] allows individuals with ALK rearrangements to be identified.]] |
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'''ALK inhibitors''' are potential [[anti-cancer drug]]s that act on tumours with variations of [[anaplastic lymphoma kinase]] (ALK) such as an [[EML4]]-[[Anaplastic lymphoma kinase|ALK]] [[Chromosomal translocation|translocation]].<ref>{{cite web |url=http://www.medscape.com/viewarticle/715243 |title=ALK Inhibitors: Possible New Treatment for Lung Cancer |author=Nelsen |year=2010 }}</ref> |
'''ALK inhibitors''' are potential [[anti-cancer drug]]s that act on tumours with variations of [[anaplastic lymphoma kinase]] (ALK) such as an [[EML4]]-[[Anaplastic lymphoma kinase|ALK]] [[Chromosomal translocation|translocation]].<ref>{{cite web |url=http://www.medscape.com/viewarticle/715243 |title=ALK Inhibitors: Possible New Treatment for Lung Cancer |author=Nelsen |year=2010 }}</ref> |
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Revision as of 01:41, 7 September 2018
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) (also a ROS1 inhibitor) approved in Aug 2011 by the US FDA for ALK-positive NSCLC.[3]
- ceritinib (Zykadia), approved by the FDA in April 2014 for treatment of NSCLC.[2][4]
- alectinib (Alecensa) (Chugai, NDA has been filed in Japan) FDA approved Dec 2015 (accelerated), full approval in 2017 for ALK-positive NSCLC.
- brigatinib (Alunbrig) (Ariad) (also an EGFR inhibitor) approved in April 2017 by the US FDA for ALK-positive NSCLC.[5]
Clinical trials
 | This section needs to be updated. (February 2016) |
Additional ALK inhibitors currently (or soon to be) undergoing clinical trials include:
- Dalantercept, ACE-041 (Acceleron)[6]
- 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
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.[7] [8]
References
- ^ Nelsen (2010). "ALK Inhibitors: Possible New Treatment for Lung Cancer".
- ^ a b 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.
- ^ https://www.fda.gov/Drugs/DevelopmentApprovalProcess/DrugInnovation/ucm537040.htm
- ^ "Dalantercept". AdisInsight. Retrieved 15 February 2017.
- ^ Galkin; et al. (2007). "Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK".
- ^ "Archived copy". Archived from the original on 2010-12-23. Retrieved 2010-10-02.
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