/home/corante/public_html/pipeline/ en-us derekb.lowe@gmail.com 2013-05-07T07:27:44-05:00 hourly 1 2000-01-01T12:00+00:00 http://pipeline.corante.com/archives/2013/05/07/an_update_on_deuterium_drugs.php In case you're wondering how the deuterated-drugs idea is coming along, the answer seems to be "just fine", at least for Concert Pharamaceuticals. They've announced their third collaboration inside of a year, this time with Celgene. And they've got their... 76394@/home/corante/public_html/pipeline/ Pharmacokinetics 2013-05-07T07:27:44-05:00 http://pipeline.corante.com/archives/2013/04/24/watching_parp1_inhibitors_fail_to_work_cell_by_cell.php Here's something that's been sort of a dream of medicinal chemists and pharmacologists, and now can begin to be realized: single-cell pharmacokinetics. For those outside the field, you should know that we spend a lot of time on our drug... 76364@/home/corante/public_html/pipeline/ Pharmacokinetics 2013-04-24T06:32:13-05:00 http://pipeline.corante.com/archives/2013/04/12/nanodrugs_peaked_or_maybe_past.php Nano-everything has been the rule for several years now, to judge from press releases and poster abstracts. But here's an article in Nature Reviews Drug Discovery that's wondering what, exactly, "nanomedicine" has offered so far: . . .Indeed, by some... 76343@/home/corante/public_html/pipeline/ Pharmacokinetics 2013-04-12T11:09:50-05:00 http://pipeline.corante.com/archives/2013/03/13/getting_down_to_proteinprotein_compounds.php Late last year I wrote about a paper that suggested that some "stapled peptides" might not work as well as advertised. I've been meaning to link to this C&E News article on the whole controversy - it's a fine overview... 76274@/home/corante/public_html/pipeline/ Drug Development 2013-03-13T06:37:12-05:00 http://pipeline.corante.com/archives/2013/01/31/in_case_you_were_wondering_what_we_thought_about_the_liver.php Courtesy of the vital site that is TOC ROFL, I wanted to highlight this graphic from this paper in MedChemComm. I always pictured the liver as sort of a sawmill or shredding machine for our drug candidates, with the... 76181@/home/corante/public_html/pipeline/ Pharmacokinetics 2013-01-31T12:12:00-05:00 http://pipeline.corante.com/archives/2013/01/23/eating_a_whole_bunch_of_random_compounds.php Reader Andy Breuninger, from completely outside the biopharma business, sends along what I think is an interesting question, and one that bears on a number of issues: A question has been bugging me that I hope you might answer. My... 76157@/home/corante/public_html/pipeline/ Drug Assays 2013-01-23T11:12:20-05:00 http://pipeline.corante.com/archives/2012/12/17/stapled_peptides_take_a_torpedo.php I wrote here about "stapled peptides", which are small modified helical proteins. They've had their helices stabilized by good ol' organic synthesis, with artificial molecular bridging between the loops. There are several ways to do this, but they all seem... 76078@/home/corante/public_html/pipeline/ Chemical Biology 2012-12-17T11:15:25-05:00 http://pipeline.corante.com/archives/2012/10/23/improving_halflife.php There was a question in the comments from a reader who's picking up med-chem, and I thought it was worth answering out here. I've been meaning to shore up the "Pharma 101" category, and this is a good opportunity. So... 75954@/home/corante/public_html/pipeline/ Pharmacokinetics 2012-10-23T09:12:55-05:00 http://pipeline.corante.com/archives/2012/09/18/going_after_the_big_cyclic_ones.php I wrote last year about macrocyclic compounds and their potential as drugs. Now BioCentury has a review of the companies working in this area, and there are more of them than I thought. Ensemble and Aileron are two that come... 75870@/home/corante/public_html/pipeline/ Drug Development 2012-09-18T07:33:16-05:00 http://pipeline.corante.com/archives/2012/07/19/come_back_thiophene_all_is_forgiven.php A couple of commenters took exception to my words yesterday about thiophene not being a "real" heterocycle. And I have to say, on reflection, that they're right. When I think about it, I have seen an example myself, in a... 75763@/home/corante/public_html/pipeline/ Life in the Drug Labs 2012-07-19T12:02:45-05:00 http://pipeline.corante.com/archives/2012/06/13/live_by_the_bricks_die_by_the_bricks.php I wanted to highlight a couple of recent examples from the literature to show what happens (all too often) when you start to optimize med-chem compounds. The earlier phases of a project tend to drive on potency and selectivity, and... 75699@/home/corante/public_html/pipeline/ Alzheimer's Disease 2012-06-13T07:13:58-05:00 http://pipeline.corante.com/archives/2012/05/24/an_oral_insulin_pill.php Bloomberg has an article on Novo Nordisk and their huge ongoing effort to come up with an orally available form of insulin. That's been a dream for a long time now, but it's always been thought to be very close... 75658@/home/corante/public_html/pipeline/ Diabetes and Obesity 2012-05-24T07:11:00-05:00 http://pipeline.corante.com/archives/2012/05/16/antidepressant_drugs_and_cell_membranes.php How much do we really know about what small drug molecules do when they get into cells? Everyone involved in this sort of research wonders about this question, especially when it comes to toxicology. There's a new paper out in... 75639@/home/corante/public_html/pipeline/ The Central Nervous System 2012-05-16T06:19:03-05:00 http://pipeline.corante.com/archives/2012/04/27/how_do_drugs_get_into_cells_a_vicious_debate.php So how do drug molecules (and others) get into cells, anyway? There are two broad answers: they just sort of slide in through the membranes on their own (passive diffusion), or they're taken up by pores and proteins built for... 75598@/home/corante/public_html/pipeline/ Pharma 101 2012-04-27T08:01:46-05:00 http://pipeline.corante.com/archives/2012/04/04/the_artificial_intelligence_economy.php Now here's something that might be about to remake the economy, or (on the other robotic hand) it might not be ready to just yet. And it might be able to help us out in drug R&D, or it might... 75557@/home/corante/public_html/pipeline/ Drug Development 2012-04-04T07:15:09-05:00