Asenapine: A Review of the Data

Abstract

of the two recently approved antipsychotics in the United States. A subsequent issue will report on iloperidone. Asenapine is the latest agent to receive FDAapproval for both the acute treatment of schizophrenia andmanic or mixed episodes associated with bipolar I disorder in adults. It is marketed in the United States under the trade name Saphris (Schering Corp.) and is administered sublingually (SL). The recommended starting and target dose for schizophrenia is 5 mg twice daily, and the recommended starting dose for bipolar I disorder is 10 mg twice daily. The safety of asenapine at doses greater than 10 mg SLBID has not been assessed in clinical trials. This review will consider asenapine’s neuroreceptor profile, the data to support its utility in managing various symptoms associated with these disorders, and how asenapinemay distinguish itself from other agents in its class. PHARMACODYNAMICS Asenapine is a dibenzo-oxepino pyrrole, possessing a unique structure and a “broader spectrum” of neuroreceptor activity with differing affinity and antagonistic properties from other agents in its class (e.g., risperidone, olanzapine) (Figure 1). In this context, it has affinity and specificity for various receptors, including: