Deepen your understanding of how organisms process pharmaceuticals with our Drug Metabolism – Principles and Applications course, offered by the University of Wisconsin–Madison’s Division of Pharmacy Professional Development.
Course Overview:
Drug metabolism is a critical aspect of drug discovery and development, influencing efficacy, safety, and therapeutic outcomes. This self-paced, online course is designed to equip scientists and regulatory professionals with foundational knowledge of drug metabolism processes and their applications in the pharmaceutical industry.
Key Learning Objectives:
Understand Drug-Metabolizing Enzymes: Identify the major enzymes involved in drug metabolism, their distribution, regulation, and species-related differences.
Evaluate Experimental Models: Assess the appropriate application of in vivo and in vitro models and protocols to address drug metabolism and transport issues during the discovery phase.
Interpret Metabolic Pathways: Analyze the significance of various metabolic pathways and their impact on drug disposition.
Apply Preclinical Data: Utilize information from drug discovery to inform preclinical decisions on drug candidates.
Predict Human Drug Disposition: Leverage data from experimental studies to forecast how drugs will behave in the human body.
Navigate Regulatory Expectations: Understand scientific and regulatory requirements for drug metabolism and transport studies, and their role in expediting drug development.
Course Format:
This 100% online, self-paced course comprises approximately 5 hours of recorded lectures and materials, allowing you to learn at your convenience. To boot, there are no assignments to submit, enabling you to focus entirely on absorbing the content.
Who Should Attend?
This course is ideal for scientists, technicians, and regulatory professionals seeking to grasp the essentials of drug metabolism, a pivotal component of the drug development process.
Why Enroll?
By completing this course, you’ll acquire a solid foundation in drug metabolism principles, enhancing your ability to contribute effectively to drug discovery and development projects. This knowledge is crucial for predicting drug behavior, optimizing therapeutic efficacy, and ensuring patient safety.
Join us to advance your expertise in drug metabolism and make a meaningful impact in the pharmaceutical industry.
For more detailed information, please view the course outline below.
Developed & Conducted by the Division of Pharmacy Professional Development, School of Pharmacy, University of Wisconsin-Madison.
Please contact Eric Buxton to qualify for the academic and graduate student rates.
This course is online and self-paced. You may register at any time and complete the curriculum at your own pace.
Course Objectives
The purpose of this online course is to provide the learner with a basic understanding of drug metabolism and its role in drug discovery and development. This self-paced course consists of approximately 5 hours of recorded lectures and materials. There are no assignments to be turned in.
Goals and Objectives
Upon completion of the program the learner will be able to:
Recognize the identity, distribution, regulation and species-related differences of major drug-metabolizing enzymes and transporters;
Evaluate the appropriate application of experimental models and protocols to drug metabolism and transport issues in vivo and in vitro during discovery;
Interpret the relative importance of various metabolic pathways;
Describe how information from the drug discovery phase is used in making preclinical decisions on preclinical drug candidates;
Utilize data from in vitro and in vivo drug metabolism and transport experiments to predict drug disposition in humans; and
Explain scientific and regulatory expectations with respect to drug metabolism and transport studies, and the impact of these studies in accelerating drug development.
Who Should Attend
Scientists, technicians and regulatory professionals who desire to learn the essentials of drug metabolism, a key aspect of the drug development process.
Course Outline
Lecture 1
An Overview of Drug Metabolism
1. Terminology
2. Elimination Routes
Lecture 2
Phase I Enzymes
A. Oxidation
1. Cytochromes P450 Monooxygenase (CYP450) System
a) Structure and Function
b) Gene Families and Substrate Specificity
c) Mechanism of Oxygen Activation
d) Reactions Catalyzed by CYP450’s
e) Induction and Inhibition of CYP450 isoforms
f) Genetic Polymorphism of CYP450 genes
g) Clinical Relevance of CYP450 Induction/Inhibition
2. Flavin Monooxygenases
3. Other Oxidases
a) Aldehyde Oxidase/Dehydrogenase
b) Alcohol Dehydrogenase
Phase II (Conjugation) Enzymes and Adverse Drug Reactions (ADRs) A. Glucuronosyl transferases
1. Modification Sites of Drugs
2. Mechanism and Solubility of Conjugates
3. Location of Enzymes - Transport of Conjugates
4. Genetic Polymorphism
5. Reactive Metabolite Formation
B. Sulfotransferases
1. Competition and Glucuronidation
2. Mechanism and Conjugate Properties
C. Glutathione S-Transferases (GST's)
1. Mechanism of Glutathiione Activation
2. Role of GST's in Detoxication of Potentially Harmful Metabolites
D. Adverse Drug Reactions (ADRs)
Examples of Idiosyncratic Adverse Drug Reactions (IADR) due to Reactive Metabolite (RM) Formation: Toxicity, Immunogenicity and Carcinogenicity
Lecture 4
Transporters
Role
Clinical concerns
Types
Classification of Transporters
1. Genetic
2. ABC
3. Solute (SLC)
Lecture 5
Drug Metabolism in Drug Development A. General Overview
Drug action
Drug disposition
B. Working Through Pre-Clinical Stages
Is the compound being absorbed?
Does metabolism limit exposure?
Distribution to the target tissue?
C. Bringing All of the Data Together
D. Biologics
Instructors
Dan Bow, PhD
Principle Research Scientist
AbbVie
Charles T. Lauhon, PhD
Associate Professor
Assistant Dean for Graduate Studies
School of Pharmacy, University of Wisconsin-Madison
Donald L. McKenzie, PhD
Executive Director of Drug Metabolism
Covance Laboratories
Adjunct Professor
School of Pharmacy, University of Wisconsin-Madison
Program Coordinator
Eric Buxton, PhD
Division of Pharmacy Professional Development 777 Highland Avenue Madison, WI 53705 (608) 262-2431 FAX (608) 265-2259 eric.buxton@wisc.edu
