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Drug metabolite synthesis using electrochemistry

Development in progress • Protected by patent
This device enables oxidation reactions for active ingredients to be continuously produced through electrochemistry to identify, stabilize and isolate their metabolites.

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Market benefits

  • Less costly (continuous production, disposable electrodes)
  • Faster than biological methods
  • More efficient thanks to the stabilization step

Issue

Launching any new drug onto the market requires regulatory pre-clinical studies, with a focus on identifying the metabolites of the active ingredients.

When a drug is administered, the active ingredient normally undergoes an initial processing step through the cells of the liver. This is an oxidation reaction that is catalyzed through hepatic enzymes known as cytochrome P450.

Methods currently used in pre-clinical studies use hepatocytes, microsomes, and natural or synthetic catalysts to identify the oxidized metabolites of active ingredients. These biological methods are unable to obtain stable metabolites or large quantities (several ?g). Once these are identified, these must then be synthesized in even greater quantities to evaluate their toxicity through in-vitro and in-vivo tests on mice.

In summary, current biological tests are laborious, expensive, and non-exhaustive. Furthermore, some metabolites are very difficult to identify and isolate as they are very unstable. Analyzing drugs with metabolites with a half-life that is too short for analysis is thus very difficult.

Solution

We have developed an electrochemical device that can carry out oxidation reactions, stabilization, and is able to synthesize sufficient quantities from an active ingredient in solution. The purpose of this is to mimic biological reactions (principally oxidation) that mainly take place in the liver (hepatocytes) after the drug is ingested, using electrochemistry. Thanks to the stabilization compartment, the device can continuously identify and continuously produce metabolites that are naturally unstable.

This electrochemical device uses single-use screen-printed electrodes (PVC or cellulose) that ensure optimal system performance at a lower cost.

Our "industrialized" method also enables continuous, rapid synthesis (around 100 mg/h), limiting the mobilization time for clinicians and at a low equipment cost (screen-printed electrodes).

In addition, the stabilization system makes it easier to analyze drugs with highly unstable metabolites.