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Astex Pharmaceuticals, AŞ Message Board

  • trader0670 trader0670 Jan 24, 2013 11:53 PM Flag

    AT13387 abstract on website now

    • AT13387 exhibits dose dependent systemic exposure and linear
    pharmacokinetics. Half-life of AT13387 in GIST patients across Phase 1 and
    Phase 2, range between 6.8 – 11.2 hours.
    • HSP70 induction of 2-7 fold magnitude was observed representing
    pharmacodynamic evidence of target engagement.
    • AT13387 demonstrated clinical activity after failure of multiple TKI treatment
    with 2 PR of 14 treated patients in Phase1 and Phase 2 thus far.
    • Phase 1 DLTs consisted mainly of multiple Gr 2 Adverse Events of GI toxicities
    (diarrhea, vomiting), systemic infusion reactions, and fatigue. Few patients had
    Gr 3 toxicities and no Gr 4 AEs were reported. Visual disturbances were all Gr 1
    with only 1 patient reported as Gr 3 due to ERG changes. All were transient
    and reversible. Visual disturbances are considered on target pharmacological
    class effects of potent HSP90 inhibition. GIST patients safety profile similar to
    overall enrolled population.
    • AT13387 is a promising agent in GIST, including TKI-resistant c-KIT positive and
    c-Kit negative GIST.
    • Phase 2 study in combination with imatinib is ongoing for imatinib-resistant

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