title: Cariprazine, a new, orally active dopamine D2/3 receptor 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.
authors.affiliation: Department of Psychiatry, Psychotherapy and Psychosomatics, Medical Faculty, RWTH Aachen University, Aachen, Germany and.
authors.forename: Tanja
authors.initials: T
authors.lastname: Veselinović
authors.forename: Michael
authors.initials: M
authors.lastname: Paulzen
authors.forename: Gerhard
authors.initials: G
authors.lastname: Gründer
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001714:Bipolar Disorder / Q000188:drug therapy* / Q000523:psychology; D002986:Clinical Trials as Topic / Q000379:methods; D003866:Depressive Disorder / Q000188:drug therapy* / Q000523:psychology; D018491:Dopamine Agonists / Q000008:administration & dosage / Q000737:chemistry; D054333:Drug Partial Agonism; D006801:Humans; D010879:Piperazines / Q000008:administration & dosage* / Q000737:chemistry; D017448:Receptors, Dopamine D2 / Q000819:agonists*; D050637:Receptors, Dopamine D3 / Q000819:agonists*; D012559:Schizophrenia / Q000188:drug therapy*; D012565:Schizophrenic Psychology
chemical_list: D018491:Dopamine Agonists; D010879:Piperazines; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; C533287:cariprazine