Asenapine is a novel psychopharmacological agent that binds with high affinity and specificity to numerous
dopamine,
serotonin,
noradrenaline (
norepinephrine) and
histamine receptor subtypes. It is being developed for the treatment of
schizophrenia and bipolar
mania. In two randomized, controlled trials of
asenapine monotherapy and in one randomized, controlled trial of adjunctive
asenapine therapy in adult patients with bipolar I disorder, sublingual
asenapine produced significantly greater reductions from baseline than placebo in clinician-assessed Young
Mania Rating Scale (YMRS) total score at 3 weeks. In two randomized, controlled trials in adult patients with acute
schizophrenia, treatment with
asenapine reduced from baseline the clinician-assessed Positive and Negative Syndrome Scale (PANSS) total score to a significantly greater extent than placebo at 6 weeks. In schizophrenic patients with predominant, persistent, negative symptoms,
asenapine at 26 weeks reduced the Negative Symptom Assessment (NSA-16) total score from baseline to an extent similar to that observed with
olanzapine. Sublingual
asenapine was generally well tolerated in clinical trials, with most treatment-emergent adverse events being of mild to moderate severity. Incidence rates of clinically significant
weight gain, extrapyramidal symptoms,
hyperprolactinaemia and alterations in
glucose or lipid metabolism were generally low.