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 D 2 and 5HT 2A receptors that has been approved by the FDA in adults for the acute treatment of schizophrenia in the United States. 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. Pre-clinical 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: a) causes a reduction in symptoms of schizophrenia; b) has a side-effect profile minimizing extrapyramidal symptoms, weight gain, and cardiac effects; and c) affects negative and/or cognitive symptoms.Take home message-Asenapine is a recently approved agent with an acceptable cardiometabolic profile that exhibits similar efficacy as other antipsychotic medications, primarily on positive symptoms of schizophrenia. Relatively less weight gain compared to 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 further investigation.

Supersensitivity Psychosis and Its Response to Asenapine in a Patient with Delusional Disorder

“…The choice of asenapine as a treatment modality in this patient was based on the fact that, like ziprasidone and aripiprazole, it is associated with lower rates of weight gain. However, there are theoretical reasons to believe that this drug may be useful in supersensitivity psychoses per se, because asenapine is a potent antagonist of serotonin 5-HT2A receptors [ 20 ], and 5-HT2A blockade may reduce the D2 receptor supersensitivity responsible for these patients' symptoms [ 21 ].…”

Predictive animal models of mania: hits, misses and future directions

“…The use of this model for developing antipsychotic treatment in schizophrenia has been covered elsewhere (Geyer and Moghaddam, 2002). A recent example, however, is the new atypical antipsychotic asenapine, initially approved for schizophrenia and now also approved for treating mania in BD (Minassian and Young, 2010). Early studies indicated that asenapine reversed the dopaminergic‐induced hyperactivity model of schizophrenia, consistent with other antipsychotics (Ellenbroek, 1993; Moore et al ., 1997; Geyer and Ellenbroek, 2003; Sun et al ., 2009).…”

Unmet treatment needs in schizophrenia patients: is asenapine a potential therapeutic option?

“…In addition, potential negative and cognitive symptoms resulting from asenapine need to be more closely investigated. The correct interpretation of data derived from the short-term trials is not easy, and meta-analytical studies are required to better understand these controversial points [138].…”