Glucuronidation

Glucuronidation catalyzed by uridine 5′-diphospho-glucuronosyltransferase (UGT) is the most common phase II metabolism. The UGTs can severely limit a drug's exposure and generate reactive metabolites, leading to toxicity. This chapter provides a brief overview of the current understanding of the UGT enzyme family, followed by various medicinal chemistry strategies to address this metabolic liability and select examples from the literature.