Biochemical Pharmaceutics

Course goals

At the end of the course students can:

1. Understand the interaction of small molecules with their target (protein);
2. Judge the chemical entities and properties of a small molecule relevant for binding, adsorption, distribution, metabolism, excretion and toxicology (ADME(T));
3. Understand how binding of a small molecule interferes with the activity and changes the structure of the target (protein);
4. Explain drug-target binding by graphical representation, interpret and conclude based on the graphical representation how a small molecule binds the target in terms of affinity, specificity, selectivity, and (ant)agonism;
5. Describe what is meant by ‘biologics’ or ‘biotherapeutics’ and mention several examples of this class of drug molecules;
6. Describe the differences between small molecules and biologics;
7. Design and conduct experiments to conclude about affinity and specificity of drug-target binding interactions and analyse the obtained results;
8. Understand the drug design cycle.

Content

Introduction:
The course will introduce you how medicines, including both small molecules and biologics, influence the function of their target proteins. The emphasis will be on receptor-ligand interactions (pharmacodynamics), but attention will also be paid to other processes that are relevant for the action of a drug in the body, such as absorption, distribution and secretion (pharmacokinetics).

Set up of the course:
In a molecular pharmacological manner, the chemical processes relevant to the binding of a drug to a receptor will be explained. These processes will be elucidated by discussing the chemical properties, binding characteristics and mechanism of action of small molecyule drugs such as non-steroidal anti-inflammatory drugs (diclofenac, ibuprofen) . andrenergic drugs and biologics such as nanobodies, monoclonal antibodies , therapueticv proteins and vaccins. In a number of lectures, the biochemical properties of drugs and biologics in relation to the molecular binding will be explained. In the associated tutorials, the emphasis is on the processing of experimental data and the mathematical analyzes that are performed to correctly describe the effect of the drug. Experimental data are analyzed using simulation, calculation and graphical methods to describe processes such as binding, enzyme kinetics and pharmacological response. In addition, a binding experiment and an enzyme-kinetics experiment will be performed, in which the student has to draw conclusions about the effect of a drug based on the data obtained. The theoretical knowledge obtained from the work and lectures should be put into practice, with the emphasis on data analyses. Finally, groups will work on a receptor dossier that describes the chemical properties, binding and effect of a self-selected drug. The emphasis is on the thorough analysis and description of the scientific pharmacological literature, and the results of the findings will be presented at a mini symposium.

Relation to other courses:
This course provides deeper knowledge on pharmaceutical and biochemical research and extends on the knowledge acquired in the foundation courses MBLS-103 ‘Organic Chemistry of Drug Molecules’, MBLS-104 ‘Physical Chemistry for Life Sciences, and MBLS-105 ‘Biomolecular Chemistry'. This elective course fits the profile Molecules & Medicine, and introduces students to pharmaceutical research and is a first introduction to drug development. Hence, this course connects to other courses in the bachelor program College of Pharmaceutical Sciences (CPS), and to the master program Drug Innovation.

This course is open to Pharmacy and College of Pharmaceutical Sciences (CPS) students (including first-year students) as a free-elective course.

Teaching format course (estimation):
Lectures = 20%
Tutorials = 10%
Practicals = 20-%
Presenting = 0%
Writing = 10%
Self study=40%

The course content is studied globally following the book “Ïntroduction to the Pharmaceutical Sciences” via the cycle of a pre-lecture, an introduction learning module, followed by a lecture. After self-study the student participates in an interactive group lecture, followed by a group tutorial. After several weeks students prepare for the practical by following an e-module and prepare a labjournal. Prior to during and after the practical the labjournal is monitored and graded. Individual e-assessments are provided to students to be enable them to monitor their progress throughout the duration of the course.

Grading (see course manual for details):
Exam 1 (30%)
Exam 2 (45%)
Writing (15%)
Practical (10%)

For the each of the exams a 5.0 is the minimal grade to pass, for the average of the 2 exams a 5.5 is the minimal grade.
Attendance of the prelab activities and practicals is mandatory and for the average grade of the three practicals a 5.5 is the minimal grade