Lisdexamfetamine dimesylate: the first long-acting prodrug stimulant treatment for attention deficit/hyperactivity disorder

BACKGROUND: Lisdexamfetamine dimesylate is the first long-acting prodrug stimulant and is indicated for the treatment of attention deficit/hyperactivity disorder. Lisdexamfetamine dimesylate is a therapeutically inactive molecule. METHODS: Following oral ingestion, it is converted to L-lysine and active d-amphetamine, which is responsible for the therapeutic effect. Lisdexamfetamine dimesylate was developed with the goal of providing a long duration of effect with the potential for less abuse-related liking. RESULTS: In controlled clinical trials lisdexamfetamine dimesylate demonstrated a significant efficacy and extended duration of action as well as a safety profile consistent with other once-daily stimulants (mixed amphetamine salts extended release). In addition, abuse liability studies have shown that lisdexamfetamine dimesylate has lower abuse-related liking scores compared with equipotent doses of immediate-release d-amphetamine.