Overview Of Biotransformation

Various drug metabolizing enzymes (DMEs) lead to formation of metabolites. Metabolites can be:

• Inactive towards the target, as is seen in most cases

• Active, either on-target, such as fluoxetine^norfluoxetine, or off-target

• Toxic, such as acetaminophen^N-acetyl-p-quinoneimine (NAPQI) at high doses

• The ultimate drug, such as the conversion of prodrug (e.g., 5-fluorouracil)!drug (e.g., fluorouridine triphosphate and fluorodeoxyuridine triphosphate).

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