Cariprazine, a new, orally active dopamine D_2/3receptor partial agonist for the treatment of schizophrenia, bipolar mania and depression

Abstract

Cariprazine is a novel drug with partial agonist activity at dopamine D2/3 receptors and six- to eightfold higher affinity for human dopamine D3 over D2 receptors. Results from several placebo-controlled Phase II/III trials in patients with a The Diagnostic and Statistical Manual of Mental Disorders IV diagnosis of schizophrenia or bipolar I disorder suggest that cariprazine is superior to placebo with respect to antipsychotic and antimanic activity. Reports concerning safety and tolerability of cariprazine are mainly favorable, although the rates of treatment-associated adverse events, which most commonly included akathisia and extrapyramidal symptom, are rather high. However, only minor alterations of clinical laboratory values, prolactin concentrations and ECG parameters are reported in cariprazine-treated patients. A new drug application to the U.S. F DA for cariprazine for the treatment of both schizophrenia and manic or mixed episodes associated with bipolar I disorder was submitted in November 2012. A more precise assessment of the clinical properties of this new drug will require additional studies, aimed to compare and contrast cariprazine with other antipsychotic agents.

Canadian Network for Mood and Anxiety Treatments (CANMAT) 2016 Clinical Guidelines for the Management of Adults with Major Depressive Disorder

“…148,149 Other investigational drugs for MDD include novel atypical antipsychotics such as cariprazine. 150 …”

Treatment of Antipsychotic-Related Akathisia Revisited

“…8 A remarkably high rate of akathisia (roughly 10%-20%), especially in patients with affective disorders, was associated with the partial dopamine D2/D3 receptor agonist aripiprazole, leading to the recognition of akathisia as one of aripiprazole's most frequent and troublesome side effects. 7 A similar high incidence was recently revealed with another partial dopamine D2/D3 receptor agonist, cariprazine, 9 suggesting that partial dopamine agonists may exhibit a particularly high propensity for inducing akathisia. Notably, children and adolescents are particularly sensitive to SGA-induced EPS.…”

Bedeutung des Arzneimittelmarktneuordnungsgesetzes für die Psychopharmakotherapie

“…Das heißt, sie werden innerhalb des ersten Jahres nach Markteinführung wieder verschwinden, oder, was sich jetzt abzuzeichnen beginnt, sie werden erst gar nicht eingeführt. Einige Beispiele seien hier exemplarisch genannt: [18]. Dennoch werden in der klinischen Praxis die Patienten, die mit Cariprazin behandelt werden, ganz andere sein, als die, die mit Risperidon zufriedener sind.…”