FA806: Drug Transporters in ADME
Study Board Pharmacy
Teaching language: Danish or English depending on the teacher, but English if international students are enrolled
EKA: N570006112, N570006102
Assessment: Second examiner: None, Second examiner: Internal
Grading: Pass/Fail, 7-point grading scale
Offered in: Odense
Offered in: Autumn
Level: Master
STADS ID (UVA): N570006101
ECTS value: 5
Date of Approval: 08-04-2025
Duration: 1 semester
Version: Approved - active
Internal Course Code
Comment
Teaching language: For lectures: English. For work in the lab: Danish or English dependent on teacher responsible, however always English if international students take part.
Limited number of seats:
The course has a limited number of seats (16). If more than 16 students have registered timely, FKF will give priority to the students registered (method 2), and a waiting list may be established. Pharmacy students enrolled at the technological profile will be given preference.
Entry requirements
A bachelor degree in natural or health sciences in the area of pharmacy, biology, chemistry or medical related sciences.
Academic preconditions
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
Participant limit
Course introduction
The aim of the course is that the students become able to define and classify drug transporting membrane proteins, and describe their role in determining ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) properties of drug substances. Furthermore, that the students can describe transporters role in tissue-specific drug delivery and exemplify how transporters impact on pharmacokinetic profiles of their drug substrates/inhibitors. Furthermore, that the students can describe the regulatory implications of transporter interactions and drug-drug interactions.
The overall aim of the course, is thus that the participants are able to a) experimentally determine kinetic parameters related to transporters b) substantiate the role of drug transporters in overall ADMET properties of a drug compound c) describe the regulatory aspects of transporter interactions of selected drug compounds d) discuss original scientific literature within the field.
The above-mentioned elements are important for pharmacist working in the setting of drug discovery and drug development in the pharmaceutical industry as well as for clinical pharmacists and pharmacists working in public administration (e.g. Danish Agency of Medicines or Department of Health or Environment) that relate to the use and approval of drug products.
Expected learning outcome
The learning objectives of the course is that the student demonstrates the ability to:
- To define when a drug is interacting with a transporter
- To calculate flux values, IC50 values, Km values and Ki values for passive and actively transported drugs, respectively
- To describe the role of transporters in ADME and pharmacokinetics
- To interpret/discuss experimental data on flux and transporter kinetic
- To predict, simulate and discuss when drug-transporter interacting result in drug-drug interactions or dose-dependent tissue accumulation or absorption
- To reflect/discuss about the consequences of drugs interacting with transporters or metabolising enzymes for tissue specific drug delivery and ADMET properties
- To suggest strategies for optimising ADMET properties based on knowledge about drug interaction with transporters and/or enzymes.
Content
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.
The exercises cover selected aspects of the curriculum.
The topics of the exercises will be;
In vitro analysis of drug uptake transporter activity, In vitro analysis of drug efflux transporter activity exemplified by studies on the efflux pump P-glycoprotein, calculations of transporter kinetics from in vitro studies, calculations of transporter involvement in oral absorption using computer-based modeling.
In the exercises, students work in groups of 2-3 . Following the exercise, the results are used for preparing a written project report on the subject of the exercise, including background and literature studies. The reports, in total 3, will made by the group that performed the practical exercise. The project reports have to be handed in to-, and will be screened by a course teacher. The results found must be reported clearly and precisely in keeping with the conventions in force in English-language journals.
The e-classes are for calculation and estimation of kinetical parameters that are fundamental for understanding ADME and transporters. Thus students should be able to make basic calculations of e.g. flux, permeability, Km, Vmax , efflux ratio.
Literature
- 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 itslearning for syllabus lists and additional literature references.
Examination regulations
Prerequisites for participating in the exam a)
Timing
Fall
Tests
Laboratory exercises and reports
EKA
N570006112
Assessment
Second examiner: None
Grading
Pass/Fail
Identification
Full name and SDU username
Language
Normally, the same as teaching language
Examination aids
To be announced during the course
ECTS value
0
Additional information
Examinatipon consists of participation in all laboratory exercises and preparation, submission of 3 reports based on lab work
Participation in all laboratory exercises is a prerequisite for taking part in exam a)
Participation in all laboratory exercises is a prerequisite for taking part in exam a)
Exam element a)
Timing
January
Prerequisites
| Type | Prerequisite name | Prerequisite course |
|---|---|---|
| Examination part | Prerequisites for participating in the exam a) | N570006101, FA806: Drug Transporters in ADME |
Tests
Oral exam
EKA
N570006102
Assessment
Second examiner: Internal
Grading
7-point grading scale
Identification
Student Identification Card - Name
Language
Normally, the same as teaching language
Duration
30 minuttes
Examination aids
Allowed, a closer description of the exam rules will be posted in itslearning
ECTS value
5
Additional information
The exam is based on presenting 1 randomly selected report out of the three and a following discussion of the context relevant to the course.
Indicative number of lessons
Teaching Method
Planned lessons:
Total number of planned lessons: 48
Hereof:
Common lessons in classroom/auditorium: 28
Common lessons in laboratory: 20
In Common lessons in classroom/auditorium in the auditorium, the teacher reviews key topics in the form of a lecture and there is two-way communication regarding central topics where the lecturer asks professional questions. During the Team lessons in the classroom, it is primarily training in terms defining behavior terms, calculations and task review. When reviewing assignments, it is not the teacher who reviews the assignments, but this is done in collaboration with the students. The students are expected to have prepared, and there will be more assignments than can be reviewed. There are suggested solutions for each hour. During Team lessons in the laboratory, the students do experiments that require preparation, and reports are drawn up based on the exercises.
Other planned teaching activities:
- Reading of text book material and scientific paper
- Calculation and presentation of results obtained during the laboratory work
- Evaluation of experimental obtained data
- Preparation of scientific rapport based on the lab work
Teacher responsible
Timetable
Administrative Unit
Team at Registration
Offered in
Recommended course of study
Transition rules
Transitional arrangements describe how a course replaces another course when changes are made to the course of study.
If a transitional arrangement has been made for a course, it will be stated in the list.
See transitional arrangements for all courses at the Faculty of Science.