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Microfluidic electrosynthesis: a novel technology for the synthesis of drug metabolites

corresponding

ANDREW MANSFIELD
Head of Flow Chemistry, Syrris Ltd

Abstract

Understanding how drugs are metabolized by the body is an important part of drug development, and is key to establishing any undesirable side effects. To ensure safety and bioavailability, the absorption, distribution, metabolism and excretion (ADME) characteristics of a candidate drug must be thoroughly investigated before it can be taken forward for further development. Fully understanding these in vivo processes requires the synthesis of a number of drug metabolites for in vitro testing, but this is often an expensive and time-consuming process. Flow electrochemistry is emerging as a powerful and effective solution to overcome these issues, helping to accelerate ADME studies and drug development pipelines.


Preclinical development of a candidate drug is a drawn out process, often lasting many years. As economic conditions continue to push pharmaceutical companies to develop new drugs more quickly and cost-effectively, there is increasing pressure to accelerate these preclinical investigations and reduce time-to-market. ADME studies are currently making significant progress in this area, thanks to the development of novel techniques for the synthesis of drug metabolites.


FOLLOWING NATURE

Hepatic oxidation is usually one of the first steps in the metabolism and excretion of small molecule drugs. 

This oxidation reaction is most often catalyzed by the CYP450 family of enzymes present in the liver, which employ a porphyrin-coordinated iron ion in the active site. Identification and characterization of these primary metabolites is crucial to understanding the pharmacokinetics and pharmacodynamics of new drug candidates, but has traditionally required the use of animal models to perform the oxidation. This limits both the scale and scope of ADME studies, due to the amount of material that can be pr ...


 

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