ADMET

2019-2020
Dit vak wordt in het Engels aangeboden. Omschrijvingen kunnen daardoor mogelijk alleen in het Engels worden weergegeven.

Doel vak

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

Inhoud vak

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

Onderwijsvorm

lectures and case studies.

Toetsvorm

Written exam and case reports.

Literatuur

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

Doelgroep

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

Afwijkende intekenprocedure

Registration via VU-Net.

Algemene informatie

Vakcode X_432721
Studiepunten 6 EC
Periode P1
Vakniveau 400
Onderwijstaal Engels
Faculteit Faculteit der Bètawetenschappen
Vakcoördinator dr. J.N.M. Commandeur
Examinator dr. J.N.M. Commandeur
Docenten dr. J. Kool
dr. J.N.M. Commandeur
dr. D.J. Scholten
dr. S.J. Dekker

Praktische informatie

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Werkvormen Hoorcollege
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