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Posts tagged with "Drug Development"

  • Analytical Chemistry

    The Entropic Term is Laughing At Us

    There are plenty of things to optimize in a med-chem project other than binding affinity. But if you don’t have at least some level of binding, you may not have a med-chem project. And while from the outside, you might think that understanding how and why compound A binds to a given target while compound… Read More
  • Cancer

    Why Not Target DNA? Well. . .

    There are all sorts of small-molecule drugs that bind to protein targets. Active sites of enzymes are, of course, a big subset of those, but there are plenty of enzymes whose allosteric sites are known to host synthetic ligands as well. Membrane receptor and ion channel proteins get both of those mechanisms too, and then… Read More
  • Drug Development

    AI Will Not Threaten Pharma Patents – Not This Way

    I’d class this letter to Nature as “interesting but wrong”. Here’s the argument: . . .A patent is granted only when a compound’s application can be classified as both ‘new’ and ‘invented’. A highly effective compound thrown up by an AI algorithm could indeed be new. Whether it is ‘invented’, however, is debatab… Read More
  • Analytical Chemistry

    Looking Way Down Into the Cells

    Pharmacokinetics – the study of how drugs are taken up, distributed, metabolized, and cleared – is obviously a key part of drug development. Every drug substance gets handled somewhat differently by the human body, and these differences can completely determine whether you’ve got an effective therapy or not. But the tools we have… Read More
  • Clinical Trials

    Gene Therapy for Duchenne

    I have said unkind things about Sarepta’s drug for Duchenne muscular dystrophy, Exondys (eteplirsen). That’s because I did not think that there was enough information to approve it at the FDA, and I had trouble believing that its biochemical effects were enough to be meaningful in general. I have no reason to modify those opinions… Read More
  • Drug Development

    How to Be a Good Medicinal Chemist

    Longtime medicinal chemist Mark Murcko has a Perspective article out in J. Med. Chem. on “What Makes a Great Medicinal Chemist“. As he makes clear from the beginning, if you’ve been doing this stuff for a while, you’ve likely heard many of these recommendations before. But it’s useful for people starting out, and it… Read More
  • Drug Assays

    Pharmacokinetic Advice From Genentech

    Here’s another solid pharmacokinetics paper, this one from Genentech, with advice on how to extend drug half-life (compare this other recent one). They’re specifically addressing the “make it less lipophilic” rule of thumb that many medicinal chemists have, and they demonstrate that this isn’t exactly a universal law.… Read More
  • Cancer

    Cancer Sequencing Hype And Reality

    This piece in Science says something that needs to be said louder and more publicly. If you live in the US, you’ve surely seen various cancer treatment centers talking about their personalized therapy plans, and especially how they’ll tailor things to your DNA sequence and so on. You would get the impression that we have… Read More
  • Drug Development

    BenevolentAI: Worth Two Billion?

    Regular readers will know that I have no problem believing that AI (in its various forms) will definitely have an impact on drug discovery. And regular readers will also know that I’m quite skeptical that it’s going to have an immediate impact on the high-level functions of drug discovery (what target to go after, what… Read More
  • Drug Assays

    Pharmacokinetic Advice from Merck’s Collection

    Here’s a solid med-chem paper from Merck on the topic of extending half-life for small-molecule drugs. This obviously is most important (and can have the biggest effect) if your compound has a short half-life after dosing to begin with (and plenty of compounds do). As the paper notes, if you have constant clearance for the… Read More
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