In Person

Medicinal Chemistry Strategies to Mitigate Preclinical Safety Risks in Drug Discovery

Perhaps the most challenging part of drug discovery is the mitigation of safety risks that arise during most drug discovery optimization efforts. This course will help drug hunters understand and navigate a path to minimizing drug safety risks, thus improving the probabilities of clinical success.

Philadelphia, PA
Mar 24 - Mar 25, 2020
Boston, MA
Oct 01 - Oct 02, 2020
Prices start at
$1495
Registration Info

About the Course

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 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.

What You Will Learn

  • An overview of the typical safety issues that arise during drug discovery.
  • An understanding of the modern in silico, in vitro and in vivo tools and methods used to assess safety risks.
  • An understanding of  the current avoidance and mitigation strategies that are used to address safety risks in drug discovery.
  • How to apply current industry best practices in safety risk assessment to your project.

Overall, this training will increase student capabilities in the participation and/or leadership of cross-functional drug discovery teams to deliver safer drug candidates.

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.

Course Outline

  • Agenda

    • Principles of toxicology and safety assessment
    • The Investigational New Drug (IND) application.  What preclinical safety data is required?
    • Target assessment, predictive toxicology and in silico methods.  How can we assess and mitigate safety issues earlier in discovery?
    • Preferred drug properties to minimize toxicological risks.  How is toxicology influenced by drug properties?
    • Common off-target safety concerns and mitigation.  Genotoxicity, hERG, related receptors and subtypes.
    • Understanding and managing on-target safety issues.  Hyper-pharmacology, species specificity issues, tissue distribution.
    • Drug exposure and preclinical safety assessment.  Review of principles necessary for toxicological data interpretation.
    • Drug metabolism, bioactivation and reactive metabolites in safety assessment.  Understanding their association with toxicity.
    • Toxicophores and Structure Alerts.  What are the substructures that we should avoid and why?
    • Mechanisms and mitigation strategies for Drug-Induced Liver Injury (DILI).  Reactive metabolites, liver transport inhibitors, other mechanisms.
    • Preclinical safety biomarkers and translation to the clinic.
    • Safety assessment and flow scheme design in lead optimization.  How and when to incorporate safety assessment assays to improve mitigation likelihood and speed delivery to the clinic?
    • Clinical candidate selection and FHD enablement.

Dates, Locations, and Prices

Five for four! Register five people for one course, one person for five courses, or any combination in between and your fifth registration is free. The free registration will be the course of the lowest price. Please note: This discount is only available if you register by fax, phone, or mail and mention this discount and it cannot be combined with any other offer.

In Person

Mar 24 - Mar 25, 2020

Temple University Center City
1515 Market Street
Philadelphia, PA 19102

Early Bird Ends Feb 24 Member $1495 Non-Member $1695
Standard $1695 $1895
Become a member during registration
- Less Details+ More Details

Course Times: 8:30 AM - 5:00 PM; Check-in starts at 7:45 AM on the first day of the course. Course fee includes a course manual and continental breakfast each day. *Early Bird pricing ends four (4) weeks before the start date of the course.

To complete your registration, you will be asked to log in using your ACS ID. If you are not already logged in, you may enter your credentials or create an ID from the next screen.

Log in or Register Now

In Person

Oct 01 - Oct 02, 2020

Metro Meeting Centers - Boston
101 Federal Street, 4th Floor
Boston, MA 02110

Early Bird Ends Sep 01 Member $1495 Non-Member $1695
Standard $1695 $1895
Become a member during registration
- Less Details+ More Details

Course Times: 8:30 AM - 5:00 PM; Check-in starts at 7:45 AM on the first day of the course. Course fee includes a course manual and continental breakfast each day. *Early Bird pricing ends four (4) weeks before the start date of the course.

To complete your registration, you will be asked to log in using your ACS ID. If you are not already logged in, you may enter your credentials or create an ID from the next screen.

Log in or Register Now

About the Instructor(s)

Bryan H. Norman

President, Norman Drug Discovery Training and Consulting, LLC

Bryan H. Norman is an experienced drug hunter with >25 years experience in the pharmaceutical industry as a medicinal chemist. Additionally, he 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). Over the years, Bryan's scientific leadership has resulted in the delivery of many novel clinical candidates for a range of therapeutic indications. He is currently a drug discovery consultant and short course instructor.

Philadelphia, PA
Mar 24 - Mar 25, 2020
Boston, MA
Oct 01 - Oct 02, 2020
Prices start at
$1495
Registration Info