Applying Pharmacology to New Drug Discovery, April 22, 2016 in San Diego, CA by CHI
Reporter: Aviva Lev-Ari, PhD, RN
Applying Pharmacology to New Drug Discovery, April 22, 2016 in San Diego, CA by CHI The system-independent quantification of molecular drug properties for prediction of therapeutic utility April 22, 2016 Over the past 6 six years, the primary cause of new drug candidate failures (50%) has been failure of therapeutic efficacy. Put another way, drug discovery programs do everything right, get the defined candidate molecule, only to have it fail in therapeutic trials. Among the most prevalent reasons proposed for this shortcoming is the lack of translation of in vitro and recombinant drug activity to therapeutic in vivo whole systems. Drug activity in complete systems can be characterized with the application of pharmacological principles which translate drug behaviors in various organs with molecular scales of affinity and efficacy. Pharmacological techniques are unique in that they can convert descriptive data (what we see, potency, activity in a given system) to predictive data (molecular scales of activity that can be used to predict activity in all systems including the therapeutic one, i.e. affinity, efficacy). The predicted outcome of this process is a far lower failure rate as molecules are progressed toward clinical testing. Instructor Terry Kenakin presently is a Professor of Pharmacology in the Department of Pharmacology, University of North Carolina School of Medicine. The course is taught from the perspective of industrial drug discovery; Dr. Kenakin has worked in drug industry for 32 years (7 at Burroughs-Wellcome, RTP, NC and 25 at GlaxoSmithKline, RTP. NC). He is Editor-in-Chief of the Journal of Receptors and Signal Transduction and Co-Editor-in-Chief of Current Opinion in Pharmacology and is on numerous journal Editorial Boards. In addition, he has authored over 200 peer reviewed papers and reviews and has written 10 books on Pharmacology. Course Material Summary sheets, exercises with answers, relevant papers are included as well as a pdf of all slides. The course is based on the book A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery. 4th Edition, Elsevier/Academic Press, 2014. This course will describe pharmacological principles and procedures to quantify affinity, efficacy, biased signaling and allostery to better screen for new drugs and characterize drug candidates in lead optimization assays.
Cambridge Healthtech Institute’s Eleventh Annual Drug Discovery Chemistry is a dynamic conference for medicinal chemists working in pharma and biotech. Focused on discovery and optimization challenges of small molecule drug candidates, this event provides many exciting opportunities for scientists to create a unique program by going back and forth between concurrent meeting tracks to hear presentations most suited to one’s personal interests. New for 2016 is the addition of three symposia on Friday covering the blood-brain barrier, biophysical approaches for drug discovery, and antivirals.
Short Courses Make the most of your time in San Diego by adding on one or more short courses*. Topics include trends in physical properties, GPCRs, peptide therapeutics, immunology, phenotypic screening, crystallography, ligand-receptor molecular interactions, inhibitor design, macrocycles, FBDD, and covalent inhibitors. * separate registration required for short courses |
SOURCE
From: Deborah Shear <pete@healthtech.com>
Date: Friday, January 8, 2016 at 11:42 AM
To: Aviva Lev-Ari <AvivaLev-Ari@alum.berkeley.edu>
Subject: Training Seminar: Applying Pharmacology to New Drug Discovery
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