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Posts tagged with "Pharmacokinetics"

  • 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

    Finger-Pointing at Celgene

    Just what is going on at Celgene? They’ve had some odd recent setbacks (such as as the failure of Mongersen), and another such acquisition, Ozanimod, had its filing recently rejected by the FDA. Several things about that incident were eyebrow-raisers – for one, it’s rare for a large, established company to get an outright refusal- Read More
  • Chemical News

    Silicon In Drug Molecules, Revisited

    Here’s an update to a post from last year about silicon in drug-like molecules. The Denmark group at Illinois has investigated a range of silicon-containing heterocycles, providing both synthetic routes into the (mostly unknown) structures, and looking at some basic pharmaceutically relevant properties. There’s a lot of work in this pap… 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
  • 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
  • Cardiovascular Disease

    Inhaled Nanoparticles – Good Ones, That Is

    Never give up on drug delivery ideas – that’s one of the big points I get out of this paper. The authors, part of a multi-center team from sites in Italy and Germany, have previously shown that calcium phosphate nanoparticles could be a good carrier for delicate cargo such as microRNAs. Such things tend to… Read More
  • Analytical Chemistry

    Two Molecules, When You Were Expecting Just One

    Here’s a good short review on a subject that doesn’t come up too often in drug discovery, but can be a major headache when it does: atropisomerism. There are all sorts of structural isomers possible for organic compounds, and students in their second-year class have a joyful time learning them and keeping them straight. But… Read More
  • Animal Testing

    Melanocortin: It’s Not Just For Lizards Any More

    If you’re looking for a good example of evolution-as-a-tinkerer, the melanocortin receptors would be a good place to start. From a single starting point, they’ve ended up as a family of related proteins that do completely different things. And the hormones that bind to them have radiated out as well: they’re all derived by process… Read More
  • Chemical Biology

    Poke Holes Through Your Membranes. It’s Fun.

    The cell membrane – the fundamental architecture of living things, the foundation of how our very bodies are organized – is a major pain in the behind. I express this ungrateful opinion merely because over the years it has rejected entry to some of my best ideas for drug candidates, and I bear a grudge. Read More
  • Biological News

    Small Proteins: Into the Gap

    We medicinal chemists are used to thinking about small molecule drugs – it’s what we do. And we’re also comfortable with having a category in our worldview that we assign to “biologics” – proteins, mostly, many of them antibodies, which can also be extremely therapeutically effective under the right conditions. B… Read More
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