Abstract：Glucuronidation as a major phase II reaction plays important roles in biotransformation, metabolism and disposition of drugs, such as nicotine, morphine, and Tamoxifen used for curing breast cancer. This paper reviews the recent research development in drug glucuronidation. The tissue distribution, polymorphism, and substrate diversity of UDP-Glucuronosyltransferases (UGTs) for glucuronidation, products of drug glcuronidation, and pharmacology and toxicology of glucuronidation for drug metabolism are discussed, together with the risks of de-glucuronidation, the distribution and significances of UGTs in brain, the individual differences, species differences of drug glucuronidation, the analysis methods for drug glucuronides, and different research results obtained for drug glucuronidation. This review will provide some food for thought in understanding the recent developments of glucuronidation in drug disposition and metabolism, and it will be useful for further researches on the drug glucuronidation and metabolism, efficacy and toxic side effects of drugs, and the relation between drug glucuronidation and the occurrence of cancers. It is important not only to understand the roles of glucuronidation in drug metabolism, but also to develop new drugs with high efficacy, quick metabolism, and small risk of side toxic effects.