Evaluation of the clinical efficacy of asenapine in schizophrenia

Abstract

Importance of the field: Asenapine is a new atypical antipsychotic medication with high affinity for D₂ and 5HT_2A receptors that has been approved by the FDA in adults for the acute treatment of schizophrenia in the USA. The purpose of this review is to describe the compound and examine whether it addresses some of the unmet clinical needs in treating schizophrenia.

Areas covered in this review: The development of asenapine is described with attention to its chemistry, pharmacodynamic and pharmacokinetic profile. Preclinical and clinical trials of safety and efficacy are reviewed. The advantages and disadvantages of asenapine relative to other antipsychotic medications are discussed.

What the reader will gain: Asenapine will be evaluated for whether it: i) causes a reduction in symptoms of schizophrenia; ii) has a side-effect profile minimizing extrapyramidal symptoms, weight gain and cardiac effects; and iii) affects negative and/or cognitive symptoms.

Take home message: Asenapine is a recently approved agent with an acceptable cardiometabolic profile and exhibits similar efficacy as other antipsychotic medications, primarily on positive symptoms of schizophrenia. Relatively less weight gain compared with other agents may confer a notable advantage. Sublingual administration may have positive and negative effects on patient compliance. Potential ‘pro-cognitive’ effects of asenapine are preliminary and require more investigation.

Keywords::

• antipsychotic
• asenapine
• bipolar disorder
• dopamine
• SAPHRIS
• schizophrenia
• serotonin

Acknowledgment

The authors would like to thank Dr Kaimana MacDonald for his helpful opinions.