FA806: Drug Transporters in ADME

Students taking the course are expected to:

• Have knowledge, skills and competences of basic biochemistry, molecular biology, pharmacology and physiology.
• Have knowledge, skills and competences of pharmaceutics corresponding to a bachelor level.
• Have knowledge, skills and competences of procedures for working in a lab and lab safety.
• Skills to make simple calculations and statistical analyse

• To give competences required for participating in project groups developing drugs.
•  To give competences required for discussing the evaluation and approval of drug substances and drug products.
• To give competences in evaluating the interaction with drug transporters and the implications for drug delivery, pharmacokinetics and drug-drug interactions
• To provide skills in conducting experimental approaches to investigate drug – transporter interaction
• To provide competences in analyzing and discussing data involving transporters and transporter kinetics.
• To provide competences in sound and critical communication of ADMET properties and transporter findings.
• To give skills about classifying transporters with regard to types, structure, function, and expression in different tissues of the body
• To give competences about planning, conducting and discussing experiments aimed at investigating ADMET properties and transport interaction.

• To give competences required for participating in project groups working in drug development programs
• To give competences required for discussing and approving the use of drug substances and drug products.
• To give skills and competences such as for example in vitro-in vivo correlation and PBPK modeling discussing the interaction with drug transporters and the implications for drug delivery, pharmacokinetics and drug-drug interactions
• To provide skills in substantiate and calculate the kinetics of drug transporters in barrier tissues and to conduct experiments with in-vitro barrier tissues as well as to interpret experimental flux data
• To provide skills in conducting experimental approaches to investigate drug – transporter interaction
• To provide competences in analyzing/discussion data involving transporters and transporter kinetics.
• To provide skills in sound and critical communication of ADME properties and transporter findings.
• To give knowledge about classifying transporters with regard to transporter type, structure, function, and expression in different tissues of the body
• To give competences about planning, conducting and evaluating experiments aimed at investigating ADME properties and transport interactions.

The course is based on lectures, lab exercises and e-classes that revolve around central subjects in the field of drug transporters in ADMET. The lectures cover a range of subjects, from individual transporter kinetics, to overall ADMET properties of drug compounds and the effect of transporter interactions on these. The following topics will be covered in the lectures; Membrane transporter structure and function, the concepts of flux, permeability and carrier-mediated transepithelial transport kinetics, in vitro and in vivo methods for studying drug transport by membrane transporters, pharmacokinetics and the ADME concepts, drug uptake and efflux transporters in the small intestine, liver and kidney and their interplay with metabolizing enzymes, drug uptake and efflux transporters in the blood-brain barrier and their role in CNS drug delivery, , FDA and EMA guidelines for transporter interactions.

• Bente Steffansen, Birger Brodin and Carsten Uhd Nielsen: Molecular Biopharmaceutics: Aspects of Drug Characterisation, Drug Delivery and Dosage Form Evaluation, Pharmaceutical Press, 2010.
  
• Course materials (E-Learn).

See Blackboard for syllabus lists and additional literature references.