Pre-clinical drug metabolism and pharmacokinetics (DMPK) is the science that describes the fate of a substance in the body. At Actelion, DMPK supports medicinal chemistry in the early phase of a project in the design of new molecules, that have a good chance of oral activity and reaching the site of action.

DMPK is an integral part of the pre-clinical development process. Selected drug candidates are studied in a number of in vivo and in vitro experiments to characterize the physiological and molecular processes that govern the drug's absorption, distribution, metabolism and elimination. Together with data from pharmacology and toxicology, a safety profile of the drug candidate is created in order to identify any potential risk before the drug is first given to man and to streamline the design of the early clinical trials.

Pharmacokinetics

From the monitoring of the time course of drug appearance and disappearance in blood and other organs, scientists develop a detailed understanding of the processes that govern the absorption of a drug into, the distribution within, and the removal from the body.

At Actelion an approach of combining in vivo experiments with in vitro studies on drug absorption and transport is applied in order to gain a detailed understanding of a drug candidate's characteristics. This knowledge is then used to support the optimal design of further experiments in toxicology studies.

Metabolism

Metabolism is the science describing the (bio)chemical modification of a drug which is part of the removal process from the body but which might also have toxicological consequences. Subcellular and cellular systems, such as recombinant liver enzymes, liver microsomes and hepatocytes, are useful tools to study in vitro the nature and rate of metabolic processes in different animals species and man.