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PBT 4.6¢

PBT1033 - development

  1. interestingtome

    1,847 Posts.
    Thought you guys would be interested in this thread from ymb
    Originally posted by kadaicher1 • 5 hours ago

    2 users liked this posts users disliked this posts 2

    What is this?
    [Clinical Development of PBT 1033
    1033 was administered to healthy volunteers in a 2-part study comprising single dose administration (Stage A) and multidose administration (Stage B). Overall, 1033 was generally well tolerated as a single dose in young male volunteers and up to 7 days of treatment in elderly healthy volunteers.

    The objectives of the following trials were to determine the safety, tolerability and pharmacokinetics of single and multiple oral doses of 1033 in healthy volunteers. Double-blind studies were conducted. The protocol included safety measures designed to capture the potential human adverse effects. A total of 65 healthy subjects have been exposed to doses of 1033 (41 single dose, 24 multiple dose).]

    interestingtome • 20 minutes ago Remove
    J is correct. This was listed in an earlier patent but here's a summary of results.

    The patent information shows that PBT1033 was selected for advancement up through human clinical testing. PBT1033 exhibited one of the highest AB inhibition rates at 38% as shown in Table 7 It also exhibited a 37% soluble and 29% insoluble AB change rate in the transgenic mouse brain models with greater than 50% BBB penetration. Mean plaque removals were higher than PBT1038, 1051 and 1052.

    The compound was tested in Transgenic HD mice with favorable results prior to clinical testing for safety and tolerability at dosing levels up to 800 mg. Treated mice exhibited significant improvement in rotarod performance, clasping behavior (typical in HD mice), greater body weights, longer life spans, ventricle areas, brain weight and Htt protein aggregates were not detected in treated mice.

    PBT1033 was also tested against glioma cells (brain cancer). The results shown indicate a dose-related reduction in tumor area in mice with most effective reduction at 100 mg dose.

    The clinical testing in humans raised by Kad is interesting indicating safe and tolerable dosing up to 800 mg in healthy elderly humans.

    Here's the conclusion "It will be apparent to the person skilled in the art that while the invention has been described in some detail for the purposes of clarity and understanding, various modifications and alterations to the embodiments and the methods described herein may be made without departing form the scope of the inventive concept disclosed in this specification." More compound tinkering to come.

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