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Posts tagged with "Pharmacokinetics"

  • Animal Testing

    A Terrific Paper on the Problems in Drug Discovery

    Here’s a really interesting paper from consultants Jack Scannell and Jim Bosley in PLoS ONE, on the productivity crisis in drug discovery. Several things distinguish it: for one, it’s not just another “whither the drug industry” think piece, of which we have plenty already. This one get quantitative, attempting to figure out… Read More
  • Drug Assays

    Park Your Drug Right Here For a While

    Here’s a ten-year look back at the whole concept of residence times in drug discovery, published by Bob Copeland of Epizyme in Nature Reviews Drug Discovery. He’s the one to write it, since he’s one of the key developers of the whole concept, which certainly seems to have made a home for itself in the… Read More
  • Chemical News

    Cubane to the Rescue

    Medicinal chemists are interested in weird ring systems – I can’t deny it. We like them for several reasons, one of which is that we’re always looking for variations on structural themes that might affect the metabolism or absorption of our drug molecules. And the fact that these variations can lead to new patentable chemical… Read More
  • Drug Development

    More 3-D Drug Printing Excitement

    Chemjobber drew my attention to this a few days ago, rightly noting that someone was indeed falling for a big ol’ pile of hype. There’s an awful lot of breathless stuff out there about “3-D printed drugs”, and this will serve as a fine example. Many of these pieces suffer from one or more of… Read More
  • Cancer

    Another Funny-Looking Structure Comes Through

    Here’s one that I certainly wouldn’t have thought about doing. This recent paper in ACS Medicinal Chemistry Letters describes changing the substituents off the core of a PAK1 inhibitor. Nothing too interesting about that, you’d think: the inhibitor itself is one of your standard-looking kinase inhibitor sausage strings of heteroar… Read More
  • Cancer

    Blasting Your Way In

    Getting drugs of any sort through the blood-brain barrier is never something that can be taken for granted, and if your therapeutic agents is well outside the usual size/polarity bounds, you can pretty much take it for granted that it’s not going in at all. The number of techniques that have been tried to get… Read More
  • Drug Development

    Modeling the Rats, Who Model the Humans

    When you get down to it, one of the biggest problems in drug discovery is that there is (in most cases) no alternative but doing things the hard way. If you want to find out if your drug is going to work for a given disease, there’s no other way to be sure than to… Read More
  • Alzheimer's Disease

    Two Alzheimer’s Updates (Lilly and TauRx)

    When you look at the stock charts of the major pharma companies, there’s not a lot of excitement to be had. Until you get to Eli Lilly, that is. Over the last year, the S&P 500 is up about 5%, and most of the big drug stocks are actually negative (Merck -0.4%, Sanofi down 6%… Read More
  • Drug Assays

    The End of Compound Property Optimization Is At Hand

    Here’s another Big Retrospective Review of drug pipeline attrition. This sort of effort goes back to the now-famous Rule-of-Five work, and readers will recall the Pfizer roundup of a few years back, followed by an AstraZeneca one (which didn’t always recapitulate the Pfizer pfindings, either). This latest is a joint effort to look at th… Read More
  • Infectious Diseases

    A New Fifty-Year-Old Hepatitis C Drug

    Here’s something that might be alarming for the companies that have been piling into the hepatitis C space (Gilead, BMS, Merck and more). But if you’re a hepatitis C patient, or the insurance company of one, it might be welcome. A new report suggests that an existing antihistamine, chlorcyclizine (CCZ), could be an effective therapy. Read More