Full course description
Student will become acquainted with the different strategies of drug discovery from early stages in which molecules are screened in low to high throughput screens from representative chemical or virtual libraries; subsequently, the obtained hit molecules are optimized with respect to pharmacodynamics and pharmacokinetics (ADME) to first lead compounds for in vivo testing in healthy animals and animal models of disease; this is followed by further optimization until eventually candidate molecules for registration and clinical development are defined. Patenting may occur at any point along that time-line and has to take the compound life cycle and later clinical development failures into account. Next to small molecule discovery, attention will be given to the recent development of recombinant human(ised) therapeutic antibodies. As a prerequisite for these rather standard processes, classical and possible future strategies of target identification and validation will be presented and analysed. In this context, important issues regarding the translational value of in vitro vs. in vivo models will be discussed.
Students will be able:
- to give a good rational/definition of a medicinal drug;
- to explain the different targets that drugs can have. This can be receptors, enzymes, second messengers, and biological targets;
- understand the characteristic features of drugs how they bind to the different type of targets (in the brain);
- to explain how high-throughput screening is done and how different tets models can be used for this purpose;
- to explain what the use of in vivo and in vitro models has in the drug discovery program. Students will know the principles of selecting a good test battery for a drug discovery program. They will be able to apply concepts as construct-, external-, and predictive validity;
- to write a research discovery plan starting form novel target, to drug finding, to drug testing;
- to understand the requirements for proposing a drug candidate for clinical development.