The constitutive androstane receptor (CAR, NR1I3) is a member of the nuclear receptor superfamily. Initially recognized as a xenobiotic receptor, CAR has been increasingly appreciated for its endobiotic functions in influencing glucose and lipid metabolism, whose dysregulations are implicated in the most prevalent metabolic disorders, such as obesity and type 2 diabetes. Given the metabolic benefits of CAR activation, CAR may represent an attractive therapeutic target to manage obesity and type 2 diabetes. Further studies are necessary to understand the mechanisms of action of CAR in metabolic diseases and to determine the human relevance of the antidiabetic effect of CAR.