The metabolic transformation of the drugs containing carboxylic acid groups can lead to the  formation of acyl glucuronide metabolites through catalysis by glucuronosyltransferase, and produce pro-acyl glucuronide intermediate metabolites with electronic activity.  Then, protein or DNA adducts appeared after a series of non-enzyme or enzyme reactions.  These adducts would change the protein activity and potentially lead to idiosyncratic and genotoxicity.  In this paper, we discussed the chemical activity, drug-induced mechanisms, distribution and toxicity resulting from this metabolic activation for these drugs, and stated the status and   prospects of research in this field.