Forum Topic Clinical Pharmacology
  • Conversation: Applying Pharmacology to New Drug Discovery

    • January 23, 2018 5:34 PM GMT
      • Post(s)

      Applying Pharmacology to New Drug Discovery

       TS2: Applying Pharmacology to New Drug Discovery: The System-Independent Quantification of Molecular Drug Properties for Prediction of Therapeutic Utility The Westin Copley Place | Boston, MA

      Tuesday, June 19 - Wednesday, June 20
      Day 1: 9:00 am – 5:00 pm | Day 2: 9:00 am – 12:00 pm


      Terry Kenakin, PhD, Professor, Department of Pharmacology, University of North Carolina School of Medicine 
      Over the past 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.

      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. In particular, new concepts that have entered the fabric of discovery over the past few years, namely biased signaling and allosteric drug function, will be emphasized as new ways forward to reduce new candidate attrition in the drug discovery process.

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