for Physical Chemists by Physical Chemists


Oxidative and metabolic stability of drugs: assessment by a novel Electroactive Pharmaceutical Screening System

Dr Iwo Gatlik- Gatlik Ltd, Basel, Switzerland

Assessing the oxidative and especially metabolic stability of new chemical entities is at the center of drug discovery processes. The Electroactive Pharmaceutical Screening (EPS) system represents a new methodology mimicking CYP biotransformation reactions of electrochemically active drugs. Using arrays of miniaturized chambers the EPS screening system facilitates assessment of the oxidative and metabolic stability of drug candidates and the prediction of in vivo hepatic clearance. Over 100 drugs with human in vivo hepatic clearance values have been measured by the EPS device revealing a strong correlation.

The EPS method is based on electrochemically induced parallel oxidation reactions of screened compounds and the analysis of follow-up products. The EPS device does not require any enzymes or organic materials and is not restricted to certain compound types. This innovative technique allows more informed and accurate decisions about synthesis and lead selection in the early stages of discovery.

Figure 1. A series of voltammograms for the oxidation of Paracetamol in phosphate buffer solution after baseline correction obtained with the EPS System.

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Last modified: 28 April 2008