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.
Keywords: Cariprazine, RGH-188, MP-214, Dopamine D3/D2 ligand, Schizophrenia, Bipolar Disorder, Major Depressive Disorder, antipsychotic.
Current Pharmaceutical Design
Title:The Novel Antipsychotic Cariprazine (RGH-188): State-of-the-Art in the Treatment of Psychiatric Disorders
Volume: 22 Issue: 33
Author(s): Alessandro Carano, Massimo Di Giannantonio, Giovanni Martinotti, Cristina Segura-García, Chiara Conti, Giampaolo Perna, Maurizio Pompili, Ilaria Matarazzo, Federica Vellante, Gianna Sepede, Domenico De Berardis, Roberta Vecchiotti, Michele Fornaro, Alessandro Valchera, Monica Mazza, Nicola Serroni, Andrea de Bartolomeis, Emiliano Prinzivalli, Felice Iasevoli and Laura Orsolini
Affiliation:
Keywords: Cariprazine, RGH-188, MP-214, Dopamine D3/D2 ligand, Schizophrenia, Bipolar Disorder, Major Depressive Disorder, antipsychotic.
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.
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Carano Alessandro, Giannantonio Di Massimo, Martinotti Giovanni, Segura-García Cristina, Conti Chiara, Perna Giampaolo, Pompili Maurizio, Matarazzo Ilaria, Vellante Federica, Sepede Gianna, Berardis De Domenico, Vecchiotti Roberta, Fornaro Michele, Valchera Alessandro, Mazza Monica, Serroni Nicola, Bartolomeis de Andrea, Prinzivalli Emiliano, Iasevoli Felice and Orsolini Laura, The Novel Antipsychotic Cariprazine (RGH-188): State-of-the-Art in the Treatment of Psychiatric Disorders, Current Pharmaceutical Design 2016; 22 (33) . https://dx.doi.org/10.2174/1381612822666160701084447
DOI https://dx.doi.org/10.2174/1381612822666160701084447 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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