Drug Discovery and Preclinical Development

Method course
Swedish or English
Luke Odell and Pär Matsson
Medicinal Chemistry and Pharmacy
BMC, Husargatan 3, Rum D3:416b (PM) and B5:422b (LO)
Box 580 (PM) and 573 (LO), 751 23 UPPSALA
Spring 2016, Contact us for exact dates
2 weeks

The course outlines the principles, concepts and applications of drug discovery and early drug development. These include; lead discovery and development, modern methods in drug design including QSAR and computer-aided molecular modeling, and profiling and optimization of pharmaceutical (ADMET) properties. The course will consist of a mixture of lectures, demonstrations, and hands-on exercises. Current literature in the field of medicinal chemistry and ADMET profiling will be discussed.
For PhD level students in the biomedical fields who want to learn the principles of preclinical drug development.

The aim of this course is to teach the principles of drug-target interaction and ADMET (drug absorption, distribution, metabolism, excretion and toxicity), and how these properties are assessed and optimized in drug discovery. Modern methods in drug design will be discussed, as will experimental and computational methods for assessing membrane permeability, solubility in biorelevant media, interactions with transport proteins and metabolic stability of drugs. The course also aims to give an understanding of how medicinal chemists think and approach problems in the design of new drugs. At the end of the course, the students should be well versed in the principles of drug design, how a drug’s ADMET properties affects its pharmacokinetics and therapeutic potential, state-of-the-art techniques for ADMET profiling and how target interaction and ADMET profiling techniques are integrated into the modern drug discovery process.

The course will provide an understanding of:
• The theoretical background and the underlying molecular mechanisms of drug-target binding, human drug absorption, distribution, metabolism, excretion and toxicity
• The underlying principles of medicinal chemistry
• How the chemical properties of a drug influences its ADMET profile
• Modern techniques used to assess and optimize ADMET in drug discovery
• How the chemical and biological properties of a drug molecule are optimized

Written examination at the conclusion of the course.

Graham L. Patrick, An introduction to Medicinal Chemistry.
Oxford University Press, 4th edition, 2009. ISBN 978-0-19-923447-9.
Edward H. Kerns and Li Di, Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization. Academic Press, 2008. ISBN 978-0-1236-9520-8.

Luke Odell, Pär Matsson, Christian Sköld, Per Artursson, Mats Larhed, Anders Karlén and invited lecturers.

Pär Matsson
Uppsala University
Dept of Pharmacy
BMC, Box 580
SE-751 23 Uppsala
Phone: +46 18 471 4630

Luke Odell
Uppsala University
Dept of Medicinal Chemistry
Organic Pharmaceutical Chemistry
BMC, Box 574
SE-751 23 Uppsala
Phone: +46 18 471 4297

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