Course ObjectiveTo 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 ContentOf 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
• strategies to improve ADME-properties by structural modification of
• Covalent drugs
Teaching Methodslectures and case studies.
Method of AssessmentWritten exam and case reports.
LiteratureRecommended book: ‘Drug-like properties: concepts, structure design and
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 AudiencemDDS-BCCA, mDDS-CMCT, mDDS-DD&S, mDDS-DDSA, mDDS-DDTF, mDDS-C-var, mDDS-
Custom Course RegistrationRegistration via VU-Net.
|Language of Tuition||English|
|Faculty||Faculty of Science|
|Course Coordinator||dr. J.N.M. Commandeur|
|Examiner||dr. J.N.M. Commandeur|
dr. D.J. Scholten
dr. J. Kool
dr. J.N.M. Commandeur
dr. S.J. Dekker
dr. D.J. Scholten
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