Asenapine: a review of acute and extension phase data in bipolar disorder.

The second generation atypical antipsychotic, asenapine (Saphris), was approved by the US FDA (August 2009) for the acute treatment of manic or mixed episodes with or without psychotic features associated with bipolar I disorder in adults as well as the acute treatment of schizophrenia. Asenapine exhibits a high affinity for and antagonism at several serotonergic (5-HT(2A-C), 5HT(5A), 5HT(6), 5HT(7)), dopaminergic (D(2), D(3)), alpha-adrenergic (α(1) and α(2)), and histaminergic (H1, H2) receptor subtypes. Asenapine is the first atypical antipsychotic formulated as a fast-dissolving, rapidly absorbed sublingual tablet. Asenapine was evaluated in adults with bipolar I disorder, manic or mixed episodes with or without psychotic features. Two identically designed 3-week registration trials confirmed the efficacy of asenapine relative to placebo in studies that included olanzapine as an active control. The placebo-subtracted rate of EPS (excluding akathisia) is 5% whereas the placebo-subtracted rate of akathisia was 2%. The placebo-subtracted rate of clinically significant weight gain (≥7%) with asenapine was approximately 5% during the 3-week acute mania trials. A 9- extension trial indicated that 19% of asenapine patients will experience clinically significant weight gain. Clinically significant metabolic abnormalities were not observed during the acute and/or extension trials. Asenapine can be associated with somnolence (asenapine 24%, placebo 6%) and does not appear to be associated with clinically significant changes in vital signs, laboratory parameters, or electrocardiographic changes. Bipolar depression and recurrence prevention studies are required to fully characterize this novel agent's position in the treatment of bipolar disorder.
AuthorsRoger S McIntyre
JournalCNS neuroscience & therapeutics (CNS Neurosci Ther) Vol. 17 Issue 6 Pg. 645-8 (Dec 2011) ISSN: 1755-5949 [Electronic] England
PMID20950326 (Publication Type: Journal Article, Review)
Copyright© 2010 Blackwell Publishing Ltd.
Chemical References
  • Antipsychotic Agents
  • Heterocyclic Compounds with 4 or More Rings
  • Receptors, Serotonin
  • Asenapine
  • Acute Disease
  • Antipsychotic Agents (pharmacokinetics, pharmacology, therapeutic use)
  • Bipolar Disorder (drug therapy, psychology)
  • Double-Blind Method
  • Heterocyclic Compounds with 4 or More Rings (pharmacokinetics, pharmacology, therapeutic use)
  • Humans
  • Randomized Controlled Trials as Topic
  • Receptors, Serotonin (metabolism)

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