Cath Lab Digest

Saphris
(asenapine)

Saphris (asenapine) is an atypical antipsychotic indicated for acute treatment of schizophrenia in adults and acute treatment of manic or mixed episodes associated with bipolar I disorder in adults. Asenapine is administered via 5-mg or 10-mg sublingual tablets that are placed under the tongue and allowed to dissolve completely. For schizophrenia, the recommended starting dose of asenapine is 5 mg twice daily. For bipolar disorder the recommended starting dose is 10 mg twice daily, and the dose can be decreased to 5 mg twice daily if patients experience adverse effects.

A novel psychopharmacologic agent, asenapine is a dopamine D2 receptor modulator that controls positive symptoms of schizophrenia. According to the Food and Drug Administration (FDA) asenapine is well tolerated and has a favorable safety profile. The receptor binding profile of asenapine demonstrates the highest affinity for blocking serotonin receptors, followed by dopamine, alpha-adrenergic, and histamine receptors, with minimal affinity for muscarinic receptors. The exact mechanism of action of asenapine, as with other drugs having efficacy in schizophrenia and bipolar disorder, is unknown.

The efficacy of asenapine in treating schizophrenia was studied in 3 short-term placebo-controlled and active-drug controlled clinical trials. In 2 of the trials Saphris demonstrated superior efficacy compared to an inactive pill (placebo) in reducing the symptoms of schizophrenia.

The efficacy of asenapine in the treatment of bipolar disorder was studied in 2 short-term placebo-controlled and active-drug controlled clinical trials in which asenapine was shown to be superior to placebo in treating symptoms of bipolar disorder.

This First Report – Managed Care Product Spotlight provides a summary of results from a clinical trial of asenapine in acute schizophrenia that was reviewed as part of the FDA approval of Saphris. In addition, we have summarized results from a clinical trial of asenapine in patients experiencing manic or mixed episodes in bipolar mania.

SCHIZOPHRENIA TRIAL
Below is summary of results from a phase 3 trial that evaluated the efficacy, tolerability, and safety of asenapine—Efficacy and Tolerability of Asenapine in Acute Schizophrenia: A Placebo- and Risperidone-Controlled Trial.

Reference: Potkin SG, Cohen M, Panagides J. J Clin Psychiatry. 2007;68:1492-1500.

Study Objectives:
The trial was designed to assess the efficacy, tolerability, and safety of asenapine, compared with placebo and risperidone, for the treatment of acute schizophrenia.

Method
The study was conducted from August 2001 to May 2002. In the double-blind, double-dummy, 3-arm, fixed-dose, 6-week, placebo-controlled, and risperidone-controlled trial patients were randomly assigned to receive either 5 mg of sublingual asenapine twice daily, placebo twice daily, or 3 mg of risperidone twice daily. Patients first completed a 3- to 7-day single-blind placebo washout phase that established their adherence to study treatment; if they were >75% adherent they were randomly assigned to treatment with asenapine, placebo, or risperidone.