The Novel Antipsychotic Cariprazine (RGH-188): State-of-the-Art in the Treatment of Psychiatric Disorders.

Abstract

Cariprazine (RGH-188) is a novel antipsychotic drug that exerts partial agonism of dopamine D2/D3 receptors with preferential binding to D3 receptor, antagonism of 5HT2B receptors and partial agonism of 5HT1A. Currently, cariprazine is in late-stage clinical development (phase III clinical trials) in patients with schizophrenia (S) and in patients with bipolar disorder (BD), as well as an adjunctive treatment in patients with Major Depressive Disorder (MDD) and drug-resistant MDD. Cariprazine has completed phase III trials for the acute treatment of schizophrenia and bipolar mania, phase II trials for the bipolar depression and MDD whilst it is undergoing phase III trials as an adjunct to antidepressants. The present review aims at proving a comprehensive summary of the current evidence on the safety, tolerability and efficacy of cariprazine in the treatment of schizophrenia, BD (manic/mixed/ depressive episode) and MDD. A systematic search was conducted on PubMed/Medline/ Scopus and the database on Clinical Trials from inception until April 2015 by typing a set of specified keywords. Available evidence seems to support cariprazine efficacy in the treatment of cognitive and negative symptoms of schizophrenia. Preliminary findings suggest its antimanic activity whilst it is still under investigation its efficacy in the treatment of bipolar depression and MDD. Furthermore, the available data seems not to allow judgements about its antipsychotic potential in comparison with currently prescribed antipsychotics. Further studies should be carried out to better investigate its pharmacodynamic and clinical potential, particularly as alternative to current antipsychotic drugs.

• Authors: Domenico De Berardis, Laura Orsolini, Felice Iasevoli, Emiliano Prinzivalli, Andrea de Bartolomeis, Nicola Serroni, Monica Mazza, Alessandro Valchera, Michele Fornaro, Roberta Vecchiotti, Alessandro Carano, Gianna Sepede, Federica Vellante, Ilaria Matarazzo, Maurizio Pompili, Giampaolo Perna, Chiara Conti, Cristina Segura-García, Giovanni Martinotti, Massimo Di Giannantonio
• Journal: Current pharmaceutical design (Curr Pharm Des) Vol. 22 Issue 33 Pg. 5144-5162 ( 2016) ISSN: 1873-4286 [Electronic] United Arab Emirates
• PMID: 27396597 (Publication Type: Journal Article, Review)

Chemical References

• Antipsychotic Agents
• Piperazines
• cariprazine

Topics

• Animals
• Antipsychotic Agents (chemistry, therapeutic use)
• Bipolar Disorder (drug therapy)
• Depressive Disorder, Major (drug therapy)
• Humans
• Piperazines (chemistry, therapeutic use)
• Schizophrenia (drug therapy)