Archived: Medicinal Chemistry Strategies to Mitigate Preclinical Safety Risks in Drug Discovery

Date: 14 April - 15 April 2020

Location: San Francisco, USA

Tutors: Dr Bryan H. Norman

The identification of potential 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.  In order to design and make safer drug candidates, medicinal chemists work with cross-functional drug discovery partners to understand, assess and mitigate safety risks associated with potential new drug candidates.  Successful drug discovery teams will properly design and execute experiments that can best assess and discharge risks prior to the first human dose (FHD).  This must be accomplished in the context of anticipated human drug exposures and patient risk-benefit analysis.  Through the lens of modern medicinal chemistry, this course explores the current best practices and methods used to identify, understand and mitigate common preclinical safety risks from both a strategic and tactical perspective.  Importantly, the course also describes proactive approaches that can help medicinal chemists avoid many safety issues and deliver safer small molecule drug candidates.  A key objective of the course is to improve medicinal chemist’s preparedness for participation and leadership on cross-functional drug discovery teams.

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Course Outline

  • 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.
  • Common off-target safety concerns and mitigation.
  • Managing on-target safety concerns.
  • Pharmacokinetics in preclinical safety assessment.
  • Drug metabolism and bioactivation.
  • Toxicophores and Structure Alerts.
  • Mechanisms and mitigation strategies for Drug-Induced Liver Injury (DILI).
  • Preclinical safety biomarkers and translation to the clinic.
  • Clinical candidate selection and FHD enablement.

Who Should Attend

The course content is specifically designed for medicinal chemists.  Other members of cross-functional drug discovery teams, such as toxicologists, biologists, pharmacologists, pharmacokineticists and program managers may also gain valuable insights into medicinal chemistry approaches to preclinical safety avoidance and mitigation.

What's Included

  • Refreshments & lunch daily
  • The comprehensive Course Manual
  • Course Certificate


Queen's University

The presenter was superbly prepared, well-organized, knowledgeable and easily approached for questions.

NC State University

As someone with a background in Synthetic organic chemistry, this course helped me greatly in understanding the medicinal properties and toxicology of potential therapeutics.