ALK inhibitor

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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[edit]

About 4-7% of non-small cell lung carcinomas (NSCLC) have EML4-ALK translocations.[2]

There are currently two ALK inhibitors, crizotinib (Xalkori) and ceritinib (Zykadia), approved by the FDA for treatment of NSCLC.[2][3][4]

Additional ALK inhibitors currently (or soon to be) undergoing clinical trials include:

  • Brigatinib (AP26113 by Ariad) (breakthrough status in U.S.)
  • 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[edit]

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[edit]

External links[edit]