Introduction to Drug Metabolism: Role and Practice in Drug Discovery and Development

Course Code: INDM

Overview

Learn about generating, interpreting, and using drug metabolism data to support drug discovery—from lead selection and optimization to drug registration.

When and Where

Key Topics

• Optimal ADME properties of a drug candidate.
• Common biotransformation reactions and enzymes. Application examples.
• Optimization of lead compounds from the drug metabolism perspective.
• Assessment and minimization of structural liabilities associated with drug metabolism.
• Typical drug metabolism experiments for drug discovery and development.
• Regulatory consideration and PhRMA perspective on drug metabolism (including MIST).

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Course Instructors

Dr. Donglu Zhang is a Principal Scientist at Bristol-Myers Squibb in Princeton, NJ. Dr. Zhang’s research interests include identification of metabolites and metabolism enzymes, investigative metabolism, LC/MS methodologies, microbial biotransformation, and their applications to drug discovery and development. He has frequently taught short courses at ACS and EAS, is a co-editor of the book ‘Drug metabolism in drug design and development, a co-inventor of mass defect filtering technology, and has published >60 peer-reviewed articles.

Dr. Ragu Ramanathan is an Associate Director in the Department of Biotransformation at Bristol-Myers Squibb, Princeton, NJ. With over 20 years of experience in mass spectrometry, Dr. Ramanathan’s primary focus of research involves application of LC-MS for pharmaceutical drug discovery and development. Prior to joining BMS, Dr. Ramanathan worked at Schering-Plough Research Institute and Pfizer Global Research and Development. Dr. Ramanathan earned his BS in Chemistry from the University of Southern Mississippi, a Ph.D. in Chemistry from the University of Florida and trained as a postdoctoral research fellow at the Washington University, St. Louis, Missouri. Dr. Ramanathan’s accomplishments include 35 peer-reviewed papers, 10 book chapters, a book entitled "Mass Spectrometry in Drug Metabolism and Pharmacokinetics" and over 60 oral/poster presentations. Dr. Ramanathan also served as a chairperson for the North Jersey ACS Mass Spectrometry Discussion Group and as a chairman for DMPK sessions of the ASMS and EAS meetings.

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Who Should Attend?

Scientists and managers in the medicinal and analytical chemistry and drug metabolism fields of the pharmaceutical and chemical industries and academic labs who want to learn about the applications of drug metabolism. Attendees should have a basic understanding of organic chemistry, analytical chemistry, and/or biochemistry.

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How You'll Benefit

• Gain practical drug metabolism knowledge.
• Understand how to effectively interpret and use drug metabolism data.
• Recognize drug metabolism issues such as DDI and formation of reactive or toxic metabolites.
• Learn how to minimize drug liabilities associated with drug metabolism.
• Be able to design basic in vitro and in vivo drug metabolism studies.
• Get familiar with drug metabolism packages required for IND and NDA filing and for drug label.
• Become familiar with analytical tools in drug metabolism studies.

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Agenda

• Common metabolic reactions and common metabolism enzymes (CYP, UGT, SULT) and polymorphisms;
• In vitro drug metabolism models;
• Strategy/methodology for screening and minimizing reactive metabolites;
• Reaction phenotyping, CYP inhibition and induction for DDI potential;
• Lead optimization examples.
• Common analytical tools including LC/MS and radioactivity detection;
• Metabolite identification strategies and metabolite profiling in the first-in-man study;
• Design of animal and human ADME studies – comparative metabolic profiling.

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Course Fees

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