Abstract
This chapter discusses enzyme activation of drugs, mechanisms of drug activation, and bioprecursor prodrugs. The term “prodrug” is a pharmacologically inactive compound that is converted into an active drug by a metabolic biotransformation. The prodrug to drug conversion occurs before absorption, during absorption, after absorption, or at a specific site in the body. The targeting of drugs for a specific site in the body by conversion to a prodrug is plausible when the physicochemical properties of the parent drug and prodrug are optimal for the target. A bioprecursor prodrug is a compound that is metabolized by molecular modification into a new compound, which is the active principle to the active drug. Hydrolysis is a mechanism for bioprecursor prodrug activation, which requires additional activation to become the active drug. Drug design is typically initiated with approaches to maximize the pharmacodynamic properties of prodrug molecules. Therefore, it is possible to alter the structure of compound to improve its pharmacokinetic properties and transforming compound into a promising drug candidate.
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