Lisdexamfetamine dimesylate is a long-acting central nervous system stimulating agent, a therapeutically inactive d-amphetamine prodrug, used in the treatment of attention-deficit/hyperactivity disorder and binge eating disorder. Impurities in the drug are closely related to the adverse reactions and can produce fatal immune response. Due to the strict regulatory requirements and lisdexamfetamine biotransformation in human body, the development of precise method for analysis is critical to ensuring the drug’s quality and safety.