Pharmacokinetic evaluation of eltoprazine

INTRODUCTION: Approvals and availability of drugs and delivery systems to treat attention-deficit/hyperactivity disorder (ADHD) have increased steadily in the last decade. The development of new pharmacological agents to treat ADHD symptoms in adults allows for both single and combination therapy for optimal efficacy. Eltoprazine hydrochloride, a serotonergic agent currently under development, is the focus of the current paper. AREAS COVERED: This paper provides an overview of the pharmacokinetics (PK) of the non-stimulant medication eltoprazine. The PK profile of eltoprazine, based on standard PK sampling accompanied by safety monitoring, is described. A literature search and review of the studies published on eltoprazine were carried out using the PubMed database up to November 2010. EXPERT OPINION: Although clinical studies of eltoprazine did not conclusively demonstrate its efficacy in treating pathological aggression in humans, eltoprazine has shown to be a well-tolerated drug in both healthy volunteers and patients across several indications studied thus far. More recently, the role of eltoprazine in reducing symptoms of ADHD in adults has been explored in a clinical trial. Future research may provide endophenotypical characteristics to help identify specific subgroups of patients with ADHD, who can benefit from the development of eltoprazine, to maximize efficacy while minimizing adverse reactions.