Principles of Drug Metabolism

Why Should You Attend:

Are you and others in your organization aware of the many ways in which drugs can be metabolized? Improving drug metabolic profiles and mitigating metabolism issues are critical aspects of drug discovery optimization. This webinar will highlight the primary metabolic pathways associated with the most common drug metabolizing enzymes. This knowledge will lay the groundwork for a description of the modern methods of improving the metabolic profiles of potential drug candidates.

One of the most difficult parts of discovering a drug is the optimization of pharmacokinetic properties. Drug hunters must be mindful of ADME (absorption, distribution, metabolism and excretion) properties to insure that drug candidates have adequate drug exposures across preclinical species and ultimately humans. Frequently, drug candidates are highly metabolized, limiting exposure to the drug target tissue. Thus, mitigation of metabolism issues is one of the most impactful ways to improve the pharmacokinetic profile of a drug candidate.

This webinar will describe the most common drug metabolizing enzymes (DMEs) and metabolic pathways encountered in drug discovery. Importantly, it will also highlight the assays and mitigation strategies in use to profile, understand and optimize the metabolism of drug candidates. Other important principles, such as minimizing the formation of reactive metabolites and the impact of cytochrome p450 (CYP) inhibitors/activators on drug-drug interactions (DDIs) will also be described.

While the focus is on medicinal chemistry methods, this webinar will benefit all scientists who participate in the cross functional execution of drug discovery programs.

Areas Covered in the Webinar:

• Impact of metabolism on pharmacokinetics
• Oxidative drug metabolizing enzymes (Phase 1)
• Mechanisms, examples, case studies
• Conjugative drug metabolizing enzymes (Phase 2)
• Mechanisms, examples, case studies
• Prodrugs
• In vitro and in vivo assays used to assess drug metabolism
• Sources of metabolic variability
• Genetic polymorphisms
• Cytochrome P450 (CYP) inhibition
• CYP activation
• Drug-Drug Interactions (DDIs), case studies
• Humanized mice

Who Will Benefit:

• Medicinal chemists, toxicologists, biologists, pharmacologists, pharmacokineticists and program managers will all gain valuable insights into modern preclinical safety assessment and mitigation strategies.
• Educational levels: B.S., M.S., Ph.D.
• Best suited for drug discovery researchers in early to mid career.

Free Materials:

• Reference documents
• Rule documents or guidance
• Checklist
• SOP template
• Easy fill in forms
• Articles

Bryan Norman
President, Norman Drug Discovery Training and Consulting LLC

Bryan H. Norman received his Ph.D. in Organic Chemistry 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. In addition to drug discovery training and consulting activities, Bryan is currently an Adjunct Professor at the Indiana University School of Medicine, where he teaches multiple drug discovery topics. He is a Volume Editor and serves on the Editorial Board of Burger’s Medicinal Chemistry, Drug Discovery and Development. Bryan 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, been named an inventor on over 30 U.S. patents 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.

Follow us :