Kinase Chemistry – Just a year and a half behind the times.

XL-019 = #14

Posted by kinasepro on May 24, 2007

IND application in the books.

First JAK2 inhibitor in development?

8 Responses to “XL-019 = #14”

  1. Dunno, but those Aussies at Cytopia are coming up again…JAK-tastic

  2. OrgMed said

    Cytopia Jak2 and Jak3. Cool.
    TargeGen Selects Jak2 Inhibitor Lead (TG101348) For Clinical Development As A Potential Therapy For Myeloproliferative Diseases Including Polycythemia.
    Poster 2387 AACR 2007 Discovery and characterization of small molecule inhibitors for Jak2. I heard they are doing Adv.Preclinical?. Great.
    Seems like XL019 (Exelixis) is moving a head.

  3. ALso Cephalons lestaurtinib in Phase 2 trials, which apparently is a JAK2 inhibitor in addition to hitting Flt3

  4. kinasepro said

    mmm good intel,

    So I guess its worth revising the statement to read: First Jak2 selective IND

  5. Was all in the timing my good man, as I happened to be reading “Molecular Mechanisms of cardiotoxicity of tyrosine kinase inhibition” at the time (Nature Reviews Cancer, 2007, 332) where Cephalon CEP-701 get a notable mention.

  6. OrgMed said

    Hello TotallMediicinal: Which is not the case for CEP-701).

    The most advanced JAK inhibitor in clinical development
    is lestaurtinib (CEP-701), which is a relatively
    selective inhibitor of FLT3 and JAK2. There are no
    reports of significant cardiotoxicity in phase I–II trials of
    lestaurtinib in patients with acute myeloid leukaemia and
    activating FLT3 mutations.
    Thats good for Cephalon.

  7. engbiol said

    First JAK selective over other kinases, but how selective is XL019 over JAK3?

    Targegen lookin to file IND on compound reported to be 30-fold selective over JAK3.
    Does it need to be selective over JAK3 though?

  8. engbiol said

    Make that 83X selectivity over JAK3 it seems.

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