engleski

Metabolic stability as a challenge facing drug- oriented research

Drug metabolism studies were previously performed at a late stage of drug development process and very often not until the phase of clinical studies. Therefore, inadequate metabolism and pharmacokinetic parameters frequently presented the major reason of failure for new chemical entities (NCEs). Nowadays, introduction of in vitro approaches into drug metabolism enables the characterization of the metabolic properties of lead candidates at early preclinical studies even in a small-scale academic laboratory. In the framework of the lecture, plans for new perspective testing based on determination of metabolic stability and biotransformation of NCEs with special emphasis on designed cholinesterase-acting compounds will be presented. Using the example of research on interactions between conventional cytostatic and cannabinoids, evidence will be provided to which extent metabolism research is important for better understanding of the biological (pharmacological or therapeutic and/or toxic) effect of a drug. This research was supported by the Croatian Science Foundation UIP-2017-05-7260.

NCE, cannabionids, preclinical, small-scale, biotransformation

nije evidentirano