For many drugs, this first requires metabolism or biotransformation, which takes place partly in the gut wall during uptake, but primarily in the liver.
In phase I metabolism, a molecule is functionalized, for example, through oxidation, reduction or hydrolysis. In phase II metabolism, the functionalized drug molecule is further transformed in so-called conjugation reactions.

These include for example, glucuronidation and sulfation, as well as conjugation with glutathione. It should be noted that the metabolism in animals might be different from that in humans, and therefore the prediction of human pharmacokinetics and metabolism from animal data might not be straightforward.

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