NEW for 2019 – Short Course
on Medicinal & Bioorganic Chemistry

Medicinal Chemistry Approaches to De-risking Toxicology Issues in Drug Discovery

 (8 Hour Course over 2 Days)
Tuesday 29th January 2019: 12.00 – 4.00 pm (includes boxed Lunch) & Wednesday 30th January 2019: 12.00 – 4.00 pm (includes boxed lunch) – prices below.

Course Description

The discovery of new therapeutic agents is met with significant challenges in preclinical discovery and development.  Both efficacy and safety endpoints must be adequately assessed prior to testing a new investigational agent in humans.  Perhaps the most challenging part of drug discovery is the mitigation of safety risks that arise during most drug discovery optimization efforts.  Successful drug discovery teams will properly design and execute experiments that can best assess and discharge risks prior to first human dose (FHD), in the context of anticipated human drug exposures.  This course highlights the important role that medicinal chemists play in identifying, understanding and mitigating common preclinical safety risks.  Information regarding best practices for avoidance and early detection of common toxicology issues will also be discussed.  Finally, the course will describe some of the common pitfalls in toxicological data interpretation and how to best use the data to inform a lead optimization strategy to deliver safe small molecule drug candidates.

Who should attend?

While the focus is on medicinal chemistry methods, this course will benefit all scientists who participate in the cross functional execution of drug discovery programs.  Medicinal chemists, toxicologists, biologists, pharmacologists, pharmacokineticists and program managers will all gain valuable insights into modern preclinical safety assessment strategies.

Course Content Highlights

Medicinal Chemistry Approaches to De-risking Toxicology Issues in Drug Discovery–Part 1 (4 hrs) – Tuesday 29th January 2019, 12.00 – 4.00 pm (includes boxed lunch)

  • Principles of Toxicology and Safety Assessment
  • The Investigational New Drug (IND) Application
  • Target Assessment, Predictive Toxicology and In Silico Methods
  • Preferred Drug Properties to Minimize Toxicological Risks
  • Mitigating Common On and Off-Target Safety Concerns
  • Case Studies and Problem Sessions

Medicinal Chemistry Approaches to De-risking Toxicology Issues in Drug Discovery–Part 2 (4 hrs) Wednesday 30th January 2019, 12.00 – 4.00 pm (includes boxed lunch)

  • Drug Metabolism and Bioactivation
  • Toxicophores and Structure Alerts
  • Mechanisms and mitigation strategies for Drug Induced Liver Injury (DILI)
  • Safety Assessment and Flow Scheme Design in Lead Optimization
  • Clinical Candidate Selection and FHD Enablement
  • Case Studies and Problem Sessions

Instructor Biography 

Bryan H. Norman received his Ph.D. at Emory University and was an NIH Postdoctoral Fellow at Penn State University.  After three years at Monsanto/Searle, Bryan joined Eli Lilly and Company in 1993, where he led multiple cross functional drug discovery efforts, many of which culminated in clinical candidates for oncology, endocrine and pain indications.  In addition to his expertise in medicinal chemistry, Bryan has significant cross functional drug discovery experience and expertise in additional disciplines, such as biomarkers, pharmacokinetic/pharmacodynamic (PK/PD) relationships, mechanisms of drug metabolism and toxicology.  He has specific expertise in the mechanisms and mitigation strategies to avoid drug-induced liver injury (DILI).  The breadth of his background has led to his service on many Due Diligence teams to assess potential in-license opportunities.  Bryan is a Volume Editor and serves on the Editorial Board of Burger’s Medicinal Chemistry, Drug Discovery and Development.  He is currently on the Board of Directors of the Medicinal and Bioorganic Chemistry Foundation and serves on various grant review committees.  He has published over 45 papers in peer-reviewed scientific journals and given many invited lectures at scientific conferences and universities.  His most recent research interests have focused on the identification of mechanisms associated with drug-induced liver injury and the discovery of novel analgesic agents for use in chronic pain.  He is currently an independent medicinal chemistry consultant and drug discovery course instructor.


Industrial/Academic rates of $500/$300 (for both days)
Industrial/Academic rates of $275/$175 (for one day)
Students attending the conference can attend free of charge

Please book your place or places when you book to attend the conference.

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