ADMET

2018-2019

Course Objective

To get familiar with the biochemical and physiological processes
underlying the pharmacokinetics and adverse side effects of drugs,
and strategies to improve ADMET-properties by structural modification

Course Content

Of the thousands of novel compounds that are developed by drug discovery
project teams, only a fraction have the appropriate pharmacokinetic
properties to become a drug product. Pharmacokinetics is determined by
the complex processes involved in absorption (A), distribution (D),
metabolism (M) and excretion (E) of the drug, the so-called ADME-
processes. Furthermore, 20% of the drug entering the clinical
development phase fail, because of unwanted/toxic (T) side-effects.
In this course, the students will be familiarized with:
• the pharmacokinetic concepts and the mathematical models by which the
time-course of plasma- and tissueconcentration of a drug can be
described and which plays an important role in identification of the
pharmacokinetic defect(s) of a drug.
• experimental and computational approaches used to predict the ADMET-
properties of a new chemical entity;
• the relationship between physico-chemical properties (pKa, logP, logD,
solubility, permeability, etc) and ADME-properties, and analytical-
chemical approaches to determine physico-chemical properties;
• role of drug metabolism and transporters in pharmacokinetics:
metabolic stability, drug-drug interactions, active metabolites, genetic
polymorphisms
• strategies to improve ADME-properties by structural modification of
compounds;
• Covalent drugs

Teaching Methods

lectures and case studies.

Method of Assessment

Written exam and case reports.

Literature

Recommended book: ‘Drug-like properties: concepts, structure design and
methods.
From ADME to Toxicity optimization.’ Eds. E.H. Kerns and L. Di,
Academic Press, 2008, ISBN: 978-0-1236-9520-8.

Additional course material will be provided via Canvas

Target Audience

mDDS-BCCA, mDDS-CMCT, mDDS-DD&S, mDDS-DDSA, mDDS-DDTF, mDDS-C-var, mDDS-
E-var, mDDS-M-var

Custom Course Registration

Registration via VU-Net.

General Information

Course Code X_432721
Credits 6 EC
Period P1
Course Level 400
Language of Tuition English
Faculty Faculty of Science
Course Coordinator dr. J.N.M. Commandeur
Examiner dr. J.N.M. Commandeur
Teaching Staff dr. J. Kool
dr. J.N.M. Commandeur
dr. D.J. Scholten
dr. S.J. Dekker

Practical Information

You need to register for this course yourself

Last-minute registration is available for this course.

Teaching Methods Lecture
Target audiences

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