DMPK - Articles and news items

Drug Metabolism and Pharmacokinetics – an overview

Issue 6 2009, Past issues / 12 December 2009 /

The journey from molecular target and early drug lead to the clinic is an arduous one with many hurdles to cross prior to developing a successful clinical candidate. The high rate of attrition of drug molecules has forced drug researchers to pay greater attention to drug metabolism and pharmacokinetics (DMPK) of lead molecules at even the earliest stages of drug discovery. Throughout the development of a successful molecule the researcher must bear in mind three important questions: will enough drug reach the target (pharmacokinetics)? What form will it arrive in (metabolism)? And what will it do when it gets there (pharmacodynamics)? These are the main questions that the DMPK scientist attempts to answer.

Drug-drug interactions: tools for drug transporter protein studies

Issue 4 2009, Past issues / 30 July 2009 /

Drug transporters are membrane proteins involved in the uptake or efflux of drugs by several tissues such as the intestine, liver, kidney and brain. They can have a significant impact on the pharmacokinetics of endogenous and exogenous compounds. Also, co-administered drugs or nutrients can influence the transporter activity which may lead to changes in the pharmacokinetics of drugs and, as a result, possibly to reduced efficacy or increased toxicity (so called drug-drug or drug-nutrient interactions). For this reason the regulatory authorities US Food and Drug Administration (FDA) and European Medicines Agency (EMEA) request data on the effects of novel drugs on transporter protein activity.


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