Abstract

Chapter 9 focuses on the prodrug approach to overcoming problems frequently encountered in drug design, such as poor solubility or absorption, short duration of action, toxicity, patient acceptability, formulation problems, or impaired access to the site of action. Building from the foundation laid by Chapter 8, Chapter 9 describes how various intrinsic metabolic processes can be harnessed to promote release of the active drug from its prodrug form, often at or near the intended site of action. Two types of prodrug approaches, the attachment of a small molecule or macromolecular carrier group to the drug and modification of the drug to a masked form, are described.

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