University of Wisconsin–Madison

Drug Metabolism – Principles and Applications

drug metabolilsm in drug discovery

Drug metabolism is how organisms break down drugs. Developing effective new drugs requires a thorough understanding of how the drugs will act once they are administered to the patient. This learn-at-your-own-pace online course is designed to provide scientists and regulatory professionals with a basic understanding of drug metabolism and its role in drug discovery and development.

For detailed information, please view the course outline below.

Developed & Conducted by the Division of Pharmacy Professional Development, School of Pharmacy, University of Wisconsin-Madison.

Registration Information


Refund Policy

Course date:Jan 1, 2021 - Jun 30, 2024
Course fee:

$600 Regular registration

$300 Academic Rate/non-profit
$150 Graduate Student rate

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:

  1. Recognize the identity, distribution, regulation and species-related differences of major drug-metabolizing enzymes and transporters;
  2. Evaluate the appropriate application of experimental models and protocols to drug metabolism and transport issues in vivo and in vitro during discovery;
  3. Interpret the relative importance of various metabolic pathways;
  4. Describe how information from the drug discovery phase is used in making preclinical decisions on preclinical drug candidates;
  5. Utilize data from in vitro and in vivo drug metabolism and transport experiments to predict drug disposition in humans; and
  6. 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

B.  Reduction

1.  Aldehyde/Keto Reductases

2.  Aldehyde dehydrogenases – reverse reaction

C.  Hydrolysis

1.  Carboxyesterases
2.  Esterase Sensitive Prodrugs
3.  Epoxide Hydrolase

Lecture 3

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


  1. Role
  2. Clinical concerns
  3. Types
  4. Classification of Transporters
    1.    Genetic
    2.    ABC
    3.    Solute (SLC)
Lecture 5

Drug Metabolism in Drug Development
A.  General Overview

  1. Drug action
  2. Drug disposition

B. Working Through Pre-Clinical Stages

  1.  Is the compound being absorbed?
  2. Does metabolism limit exposure?
  3. Distribution to the target tissue?

C. Bringing All of the Data Together


D. Biologics



Dan Bow, PhD
Principle Research Scientist

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

Customized Course Request