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Ohr Pharmaceutical, Inc. Message Board

  • gs88gs88 gs88gs88 Aug 31, 2013 3:32 AM Flag

    Is this an intellictual property violation?

    If you Google Squalamax---someone is pushing oral squalamine capsules. Marketing states it is from "shark liver" and is "natural". It mentions anti-angiogenesis. about $34 for 100 capsules. I assume an IP violation?

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    • They are selling oil from sharks but the amount of squalamine is infinitesimal, less than 0.01%. Anyway I don't believe that a significant amount of squalaminie can be absorbed by an oral route since the intestinal villi have a outer layer of cells that lie between the lumen and the capillaries and these cells are not going to let a large charged molecule pass through them unless by active transport, which doesn't occur with squalamine.

      • 1 Reply to livermore10
      • Trodusquemine is not charged and is about the same size as squalamine; I think it could be aborbed by an oral route using a sublingual formulation if need be. Here is an abstract from a paper last year on trodusquemine:

        "Trodusquemine (MSI-1436) causes rapid and reversible weight loss in genetic models of obesity. To better predict the potential effects of trodusquemine in the clinic, we investigated the effects of trodusquemine treatment in a murine model of diet-induced obesity (DIO). Trodusquemine suppressed appetite, reduced body weight (BW) in a fat-specific manner, and improved plasma insulin and leptin levels in mice. Screening assays revealed that trodusquemine selectively inhibited protein-tyrosine phosphatase 1B (PTP1B), a key enzyme regulating insulin and leptin signaling. Trodusquemine significantly enhanced insulin-stimulated tyrosine phosphorylation of insulin receptor (IR) β and STAT3, direct targets of PTP1B, in HepG2 cells in vitro and/or hypothalamic tissue in vivo. These data establish trodusquemine as an effective central and peripheral PTP1B inhibitor with the potential to elicit noncachectic fat-specific weight loss and improve insulin and leptin levels."

        Genaera's human trial of trodusquemine was screwed up when they wasted their time doing a study with a subtherapeutic dose of around 6mg IV every 3 days which lowered sugar but not weight. They rolled up the company before having a chance to do a higher dose study using 20mg IV every 3 days but even a higher dose of 30 or 40mg should have been done due to the linear dose response curve of trodusquemine..

        Now suppose trodusquemine could be formulated into a sublingual dose of 100mg twice daily has a bioavailability of 10%; then this would be an effective dose of around 60mg every 3 days. Assuming half if metabolozed by the liver on the first pass, then this is analogous to a 30mg IV every 3 days and that would probably be sufficient to restore insulin and leptin sensitivity.
        .

    • Sorry about the typo. I can't figure out how to edit a posting on the newer yahoo board.

 
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