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β-Glucuronidase-mediated prodrug activation is a targeted drug delivery strategy that exploits the enzymatic activity of β-glucuronidase to selectively activate prodrugs at specific sites, most notably within the tumor microenvironment. This approach aims to increase therapeutic efficacy while minimizing systemic toxicity by converting relatively non-toxic, hydrophilic glucuronide prodrugs into their active cytotoxic forms only where β-glucuronidase is present in high concentrations.
Enzymatic cleavage of glucuronide prodrugs by β-glucuronidase, releasing the active drug.
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