ABSTRACT
Drug discovery is an exceedingly complex and demanding enterprise aiming to select a drug candidate that displays promising efcacy, safety, and marketing potential for clinical trials. The initial phase of the drug discovery process is devoted to increase pharmacological potency with high afnity and selective ligands at the target. This initial phase often results in lead compounds with less than optimal biopharmaceutical and pharmacokinetic properties, or properties more frequently referred to as ADME (absorption, distribution, metabolism, and excretion) properties. Designing prodrugs, when used appropriately, has the potential to enable a suitable drug candidate with the optimal ADME properties and pharmacological potency to be selected for development faster and with less overall costs. Fortunately, prodrugs are becoming an integral part of many drug discovery efforts.
