Nice patent, but essentially useless unless AMRN intends to run new trials with this new lecithin containing formula to show getting EPA into organs via the lymph system can help the disease state of multiple organs, I assume by reducing organ inflammation, which causes things like pancreatitis, impaired kidney function etc. - there's some stuff in the patent suggesting this use would be for cancer, but it doesn't say how EPA could treat cancer. That patent says there's a Fig. 22 that shows how much this new formula increased EPA levels in organs of rats but there are no figures in this file:
Ah - if you download the PDF (link is at top of page) you can see the figures - check pg 169 for Fig 22 - pretty shocking how such a tiny amount of lecithin can increase EPA in organs - for the brain it was +80%, in the lungs by > 100% - it could have helped patients in COVID and BRAVE trials .
The patent is basically too broad - they would have a dozen or more diseases to look at, and they'd have to pick the best one since they can't afford a hit and miss - my money says they don't do more the preclinical work with mice or rats for a year or more. Then taking it all the way to FDA/EMA approval is more money AMRN can't afford unless EU V sales actually start to contribute to earnings, whenever THAT'S going to happen - and I don't mean revs, I mean profits - the level where V sales cover the costs of their EU operations I haven't a clue. Overall, I think we can stick this into the "nice to have but we'll never use it for anything" patent pile, which is pretty damn high at this point.
Here's the relevant section of the patent for increasing EPA in organs:
[0137] Compared to plain EtEPA, enhanced cellular uptake of EPA with LR-EtEPA was also observed in several dense tissues including cells in the lung, heart, brain, kidneys, pancreas, jejunum, and liver. Notably, the superior cellular uptake wasn't accompanied by consistent differences in acellular blood such as plasma, suggesting that even though LR-EtEPA results in acellular blood/plasma EPA levels comparable to plain EtEPA, it is superior at delivering EPA to tissues and increasing tissue/cell-level EPA bioavailability. [0138] Taken together, compared to administration of EtEPA alone, coadministration of phospholipids and/or emulsifiers with EtEPA in the lymph-releasing EPA formulation (LR-EtEPA) shunts EPA to the lymphatic system rather than the portal vein. In doing so, visceral/hepatic first pass loss is reduced, resulting in more efficient drug delivery. Owing to its high perfusion and diminished first pass losses, delivering drugs by the lymphatic route especially enhances lung, heart, and brain incorporation. The lungs and heart essentially become the first pass organs, which means the composition is particularly advantageous for treating cardiopulmonary diseases. The composition also enhances EPA delivery and uptake by coronary, carotid, and vertebral arteries, and hence to the heart and brain, as well as other organs/tissues of the body.
[0139] Moreover, increasing the amount of the additives (e.g., phospholipids and/or emulsifiers) appears to result in significantly more delivery of EPA to lymph (FIG. 2). By altering the ratio of EtEPA to additives from 4:1 (favoring EtEPA) to 1 :1 (i.e., equal parts EtEPA and additives), the cumulative lymph delivery of EPA was significantly higher, and the increase in EPA uptake was prolonged, compared to the lower additive formulation, indicating a robust dose-dependent effect between the amount of phospholipids and the amount of EPA delivered to lymph. The lymphreleasing effects, as well as the corresponding improved bioavailability in lymph and enhanced drug delivery to tissues, of the composition and its additives are expected to apply to other PUFAs and derivatives thereof. Thus, the present technology provides a superior formulation for delivering PUFAs and derivatives thereof to various tissues and cells of the body, which presents great therapeutic potential for a variety of diseases.
The Thought Police: To censor and protect. Craig Bruce
