Harman Patil (Editor)

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.

Contents

EML4-ALK

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

Approved inhibitors

  • crizotinib (Xalkori) and ceritinib (Zykadia), approved by the FDA for treatment of NSCLC.
  • Alectinib (Alecensa) (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:

  • 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)

    • 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.

    References

    ALK inhibitor Wikipedia
    (Text) CC BY-SA


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