Derek Lowe's commentary on drug discovery and the pharma industry. An editorially independent blog from the publishers of Science Translational Medicine. All content is Derek’s own, and he does not in any way speak for his employer.

By Derek Lowe

Posts tagged with "Toxicology"

• Animal Testing

  A Toxicological Flag

  14 January, 2019

      Here’s a caution from a new paper out of Manchester. The group had been synthesizing inhibitors of PARG (poly-ADP ribose glycohydrolase), an enzyme involved in DNA repair. The general chemotype is shown at right, but there are a number of variations. That fluorine is a new addition, though. The corresponding cyclopropylmethyl se… Read More

• Analytical Chemistry

  The Sartan Contamination Story

  4 January, 2019

  There’s a chemical contamination story in the generic drug industry that just isn’t going away. Late last summer, some lots of valsartan were recalled due to detection of N-nitrosodimethylamine (NDMA), and the problem has just continued since then. We’ll get into the chemistry of this problem in a minute, but first off, looking at… Read More

• Cancer

  Bromopyruvate Revealed

  14 November, 2018

  3-bromopyruvate is an interesting and controversial compound. It’s been reported to be an active chemotherapy agent, apparently acting via covalent inhibition of glyceraldehyde 3-phosphate dehydrogenase (GAPDH) and subsequent metabolic effects via loss of pyruvate itself. Several years ago, you could come across numerous web pages touting it… Read More

• Biological News

  Real Progress in Parkinson’s

  2 November, 2018

  There have been some potentially significant developments in Parkinson’s disease, which is a good thing to be able to report. As populations age around the world, PD has been on its way up, but therapies for it have not been, despite a good deal of work in the field. But it looks like some clues… Read More

• Clinical Trials

  Digging Into the Genetics of Drug Targets

  12 September, 2018

  Rare diseases – remember years ago, back when those were a case of market failure? When companies were reluctant to work on them because the market size was guaranteed to be small and you’d have to charge, like, a hundred thousand or more a year to make the whole idea financially viable? Which wasn’t going… Read More

• Cancer

  Why Not Target DNA? Well. . .

  28 June, 2018

  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

• Infectious Diseases

  Fluoroquinolone Trouble Untangled

  23 May, 2018

  The fluoroquinolone antibiotics are important drugs indeed – ciprofloxacin is probably the most famous of the bunch, but there’s a whole series of them, and they’re widely used for serious bacterial infections. (I last wrote about them here, with the various arguments about how they were developed in the first place). But for many… Read More

• Drug Assays

  Tecfidera Explained

  30 April, 2018

  One of the more unusual drugs on the market is Tecfidera (dimethyl fumarate). I went into its history a bit in this post, if you’re wondering how a molecule that small and unfunctionalized became a multiple sclerosis drug. As that shows, it went into trials for the disease with quite a bit of clinical rationale… Read More

• Chem/Bio Warfare

  A Poisoning in England: But Which Poison?

  8 March, 2018

  Chemistry doesn’t make the news as often as you might think, and when it does, it’s often in a grim way. Such is the case in the UK right now, with the poisoning of Sergei and Yulia Skripal in Salisbury. For those who don’t know the background of the situation, Skripal was an officer in… Read More

• Cardiovascular Disease

  Inhaled Nanoparticles – Good Ones, That Is

  26 January, 2018

  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