7 comments

  • bonsai_spool13 minutes ago
    I&#x27;m not a specialist but I think there are some stapled peptides that do show appreciable uptake, so the blog post is not a complete history; this review reports bioavailability of up to 70% for some agents.<p>Nielsen DS et al. 2017. Orally Absorbed Cyclic Peptides. Chemical Reviews.<p><a href="https:&#x2F;&#x2F;sci-hub.ru&#x2F;10.1021&#x2F;acs.chemrev.6b00838" rel="nofollow">https:&#x2F;&#x2F;sci-hub.ru&#x2F;10.1021&#x2F;acs.chemrev.6b00838</a>
  • celltalk3 hours ago
    It’s a great read but is this really the history of oral peptides?
    • Nevermark1 minute ago
      Here is a list of ways bioactivity is achieved:<p>Cyclization + N-methylation — lipophilicity, protease resistance (cyclosporine)<p>D-amino acid substitution — protease evasion (desmopressin)<p>Permeation enhancers — transient tight-junction opening or membrane fluidization (semaglutide&#x2F;SNAC, insulin formulations)<p>Extreme potency — tolerating &lt;1% bioavailability (desmopressin)<p>Minimizing size to di&#x2F;tripeptides — exploiting PepT1 active transport (collagen hydrolysates)<p>Prodrug masking — protecting reactive groups, intracellular unmasking (S-acetyl-glutathione)<p>Local buffering — pH microenvironment control (semaglutide)<p>One I take, PEP19, apparently is unique in being naturally bioactive. Evidence is early stage, but I get better sleep with it, taking 6mg, 3x the recommended dosage. At the higher does it may also promote fat burning and fat browning at night (only 1 study). It only has 10 residues which apparently avoid having typical cleavage points, fragments may retain bioactivity, and it has extreme potency in very small doses so any absorption means a lot.<p>And the big one:<p>Mechanical injection — bypassing the absorption problem entirely (Rani pill)<p>But despite a plethora of peptides, successes are not common.
    • abainbridge2 hours ago
      Yep, I think it is. The point is there&#x27;s almost no history of oral peptides, other than stomachs destroying them.<p>FTA: &quot;So to summarize the state of the art in oral peptide delivery: there are exactly two FDA-approved products that use permeation enhancers to get peptides into your bloodstream through your GI tract. Both achieve sub-1% bioavailability. Both required over a decade of development, thousands of clinical trial participants, and hundreds of millions of dollars.&quot;
      • pstuart1 hour ago
        Would a sublingual dose be possible&#x2F;more effective? Research in other (um, yeah, medicinal!) compounds shows that it can be an effective pathway to the bloodstream rather than trying to survive the digestive system.
        • CGMthrowaway1 hour ago
          Sublingual is even harder. The sublingual mucosa is thin but selective. It strongly favors molecules that are small, lipophilic and uncharged. Semaglutide is about 8-10x too big, highly polar and charged.<p>Injection is really the only method with any substantial bioavailability. BUT, low (&lt;1%) bioavailability does not necessarily mean useless.
        • rodarmor1 hour ago
          It would be hilarious if people wound up snorting or boofing their GLP-1s (≧▽≦)
          • pstuart9 minutes ago
            Insufflation for medicinal purposes if it works and doesn&#x27;t cause harm seem like a win. Less needles == more use.
  • Kaminsk131 day ago
    I&#x27;m not sure why the hims investors ever thought that this was legal
    • InsideOutSanta3 hours ago
      They probably didn&#x27;t, they just took the bet that this was one of the crimes that are currently legal, like crypto scams, environmental crimes, bribery, and tay evasion for the rich.
    • badrequest3 hours ago
      Some of the most profitable ventures this century have been objectively illegal, but when you know you won&#x27;t go to prison for violating the law, why would you care to follow it?
      • pixl971 hour ago
        The process of chlorinating water was first done illegally.
        • CGMthrowaway57 minutes ago
          Also:<p><pre><code> human dissection (grave robbing) translating the Bible into English silk production outside of China (death penalty for exporting worm eggs) rubber production in Asia (seeds smuggled out of Brazil) the Underground Railroad heliocentrism AIDS treatment (see Dallas Buyers Club) Needle exchange programs for IV drug users Ridesharing&#x2F;airbnb&#x2F;napster (obvious ones) SF gay marriage licenses (in defiance of CA law)</code></pre>
        • maxbond45 minutes ago
          &gt; The process of chlorinating water was first done illegally.<p>I tried to find a source on this but it doesn&#x27;t seem to be true? The first chapter of this book describes the history of chlorination: <a href="https:&#x2F;&#x2F;upload.wikimedia.org&#x2F;wikipedia&#x2F;commons&#x2F;f&#x2F;fd&#x2F;Chlorination_of_water_%28IA_chlorinationofwa00race%29.pdf" rel="nofollow">https:&#x2F;&#x2F;upload.wikimedia.org&#x2F;wikipedia&#x2F;commons&#x2F;f&#x2F;fd&#x2F;Chlorina...</a> (which is a source Wikipedia cites) and it doesn&#x27;t appear to mention anything about illegally chlorinating water. After looking in that book I asked ChatGPT to find a source for the claim, and it reported the claim was false. Chlorination was initially controversial but I can&#x27;t find anything claiming it was illegal?
    • kps3 hours ago
      The charitable assumption is that investors weren&#x27;t aware it was a problem.
  • Boot2Root1 day ago
    Appreciate the perspective on the risk of dubious formulations. Consequences are far more than cosmetic.
  • badc0ffee1 hour ago
    Informative article but I feel like it could have benefited from a paragraph about what Hims is. I had never heard of them before.
    • maxbond8 minutes ago
      An online pharmacy that advertises pretty aggressively, with men being the target audience. Hair loss, erectile dysfunction, that sort of thing.<p><a href="https:&#x2F;&#x2F;en.wikipedia.org&#x2F;wiki&#x2F;Hims_%26_Hers_Health" rel="nofollow">https:&#x2F;&#x2F;en.wikipedia.org&#x2F;wiki&#x2F;Hims_%26_Hers_Health</a>
  • ydai05311 day ago
    great read!
  • ftchd3 hours ago
    [flagged]