Long considered as no more than biological waste meant to be eliminated in urine, glucuronides have recently contributed to tremendous developments in the biomedical field, particularly against cancer. While glucuronide prodrugs monotherapy and antibody-directed enzyme prodrug therapy have been around for some time, new facets have emerged that combine the unique properties of glucuronides notably in the fields of antibody-drug conjugates and nanomedicine. In both cases, glucuronides are utilized as a vector to improve pharmacokinetics and confer localized activation of potent drugs at tumor sites while also decreasing systemic toxicity. Here we will discuss some of the most promising strategies using glucuronides to promote successful anti-tumor therapeutic treatments.
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