SUMMER 2017
Drug Discovery World
Long-read sequencing offers path to more accurate drug metabolism profiles
By Dr Jenny Ekholm

In the complex drug discovery process, one of the looming questions for any new compound is how it will be metabolised in a human body. While there are several methods for evaluating this, one of the most common involves CYP2D6, the enzyme encoded by the cytochrome P450-2D6 gene.

This enzyme is involved in metabolising a quarter of all commonly used medications, making it an important target for ADME and pharmacogenomics studies. It is known to activate some drugs and to play a role in the deactivation or excretion of others.

The CYP2D6 gene harbours many variants that contribute to the differences in how people metabolise everything from antipsychotic therapies to painkillers. From a pharmacology perspective, it is critical to understand the function of this gene in order to develop the best possible compounds, determine optimal dosing protocols, and target drugs to the right patient population...

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