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Posts tagged with "Pharmacokinetics"

  • Drug Development

    Taking Your Doses For You

    MIT’s Bob Langer has another idea: he’s looking to change the way that entire courses of treatment are dosed. What if an extended-release formulation, for an oral drug, was really extended release. Days, weeks? Instead of taking pills every morning, what if you took one, well, pill-like thing that emitted the drug substance on schedule… Read More
  • Cancer

    Bind’s Attempts To Remake Chemotherapy

    There’s a lot of effort (and a lot of money) going into targeted nanoparticle drug delivery. And that’s completely understandable, because the way we dose things now, with any luck, will eventually come to seem primitive. So you used to just have people eat the compound, did you, or just poke it into their bloodstream… Read More
  • Drug Development

    Why Not Bromine?

    So here’s a question for the medicinal chemists: how come we don’t like bromoaromatics so much? I know I don’t, but I have trouble putting my finger on just why. I know that there’s a ligand efficiency argument to be made against them – all that weight, for one atom – but there are times… Read More
  • Drug Assays

    Don’t Optimize Your Plasma Protein Binding

    Here’s a very good review article in J. Med. Chem. on the topic of protein binding. For those outside the field, that’s the phenomenon of drug compounds getting into the bloodstream and then sticking to one or more blood proteins. Human serum albumin (HSA) is a big player here – it’s a very abundant blood… Read More
  • Biological News

    Modifying Red Blood Cells As Carriers

    What’s the best carrier to take some sort of therapeutic agent into the bloodstream? That’s often a tricky question to work out in animal models or in the clinic – there are a lot of possibilities. But what about using red blood cells themselves? That idea has been in the works for a few years… Read More
  • Biological News

    Single-Cell Compound Measurements – Now In A Real Animal

    Last year I mentioned an interesting paper that managed to do single-cell pharmacokinetics on olaparib, a poly(ADP) ribose polymerase 1 (PARP1) inhibitor. A fluorescently-tagged version of the drug could be spotted moving into cells and even accumulating in the nucleus. The usual warnings apply: adding a fluorescent tag can disturb the various mole… Read More
  • Drug Assays

    A New Way to Study Hepatotoxicity

    Every medicinal chemist fears and respects the liver. That’s where our drugs go to die, or at least to be severely tested by that organ’s array of powerful metabolizing enzymes. Getting a read on a drug candidate’s hepatic stability is a crucial part of drug development, but there’s an ever bigger prize out there: predicting… Read More
  • Pharmacokinetics

    Dosing by Body Surface Area

    We were talking about allometry around here the other day, which prompts me to mention this paper. It used the reports of resveratrol dosing in animals, crudely extrapolated to humans, to argue that the body surface area normalization (BSA) method was a superior technique for dose estimation across species. Over the years, though, the BSA… Read More
  • Drug Development

    A New Book on Scaffold Hopping

    I’ve been sent a copy of Scaffold Hopping in Medicinal Chemistry, a new volume from Wiley, edited by Nathan Brown of the Institute of Cancer Research in London. There are eighteen chapters – five on identifying and characterizing scaffolds to start with, ten on various computational approaches to scaffold-hopping, and three case histori… Read More
  • In Silico

    A New Metabolism Predictor

    Drug metabolism is a perennial topic for us small-molecule people. Watching your lovingly optimized molecules go through the shredding-machine of the liver is an instructive experience, not least when you consider how hard it would be for you to do some of the chemistry that it does. (For reference and getting up to speed on… Read More
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