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Literature DB >> 26510944

Cariprazine: First Global Approval.

Abstract

Cariprazine (Vraylar) is an oral atypical antipsychotic originated by Gedeon Richter. It is a potent dopamine D3 and D2 receptor partial agonist, which preferentially binds to the D3 receptor. Cariprazine also has partial agonist activity at serotonin 5-HT1A receptors. In September 2015, cariprazine received its first global approval in the USA for the treatment of schizophrenia and for the acute treatment of manic or mixed episodes associated with bipolar I disorder. It is also in development in a variety of countries for the treatment of schizophrenia with predominant negative symptoms (phase III), as adjunctive therapy for major depressive disorder (phase II/III) and for the treatment of bipolar depression (phase II). This article summarizes the milestones in the development of cariprazine leading to this first approval for schizophrenia and manic or mixed episodes associated with bipolar I disorder.

Entities: Chemical Disease

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Year: 2015 PMID： 26510944 DOI： 10.1007/s40265-015-0494-7

Source DB: PubMed Journal: Drugs ISSN： 0012-6667 Impact factor: 9.546

14 in total

1. Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: II. behavioural characterisation of RG-15.

Authors: István Gyertyán; Katalin Sághy; Judit Laszy; Ottilia Elekes; Rita Kedves; Larisza I Gémesi; Gabriella Pásztor; Mária Zájer-Balázs; Margit Kapás; Eva Agai Csongor; György Domány; Béla Kiss; Zsolt Szombathelyi
Journal: Naunyn Schmiedebergs Arch Pharmacol Date: 2008-06-12 Impact factor: 3.000

2. Efficacy and safety of low- and high-dose cariprazine in acute and mixed mania associated with bipolar I disorder: a double-blind, placebo-controlled study.

Authors: Joseph R Calabrese; Paul E Keck; Anju Starace; Kaifeng Lu; Adam Ruth; István Laszlovszky; György Németh; Suresh Durgam
Journal: J Clin Psychiatry Date: 2015-03 Impact factor: 4.384

Review 3. The role of dopamine D(3) receptors in antipsychotic activity and cognitive functions.

Authors: Gerhard Gross; Karla Drescher
Journal: Handb Exp Pharmacol Date: 2012

4. An evaluation of the safety and efficacy of cariprazine in patients with acute exacerbation of schizophrenia: a phase II, randomized clinical trial.

Authors: Suresh Durgam; Anju Starace; Dayong Li; Raffaele Migliore; Adam Ruth; György Németh; István Laszlovszky
Journal: Schizophr Res Date: 2014-01-10 Impact factor: 4.939

5. Efficacy and Safety of Cariprazine in Acute Exacerbation of Schizophrenia: Results From an International, Phase III Clinical Trial.

Authors: John M Kane; Stephen Zukin; Yao Wang; Kaifeng Lu; Adam Ruth; Krisztián Nagy; István Laszlovszky; Suresh Durgam
Journal: J Clin Psychopharmacol Date: 2015-08 Impact factor: 3.153

6. Cariprazine in the treatment of acute mania in bipolar I disorder: a double-blind, placebo-controlled, phase III trial.

Authors: Gary S Sachs; William M Greenberg; Anju Starace; Kaifeng Lu; Adam Ruth; István Laszlovszky; György Németh; Suresh Durgam
Journal: J Affect Disord Date: 2014-11-24 Impact factor: 4.839

7. Cariprazine, a dopamine D(3)-receptor-preferring partial agonist, blocks phencyclidine-induced impairments of working memory, attention set-shifting, and recognition memory in the mouse.

Authors: Ross Zimnisky; Gloria Chang; István Gyertyán; Béla Kiss; Nika Adham; Claudia Schmauss
Journal: Psychopharmacology (Berl) Date: 2012-10-19 Impact factor: 4.530

8. The efficacy and tolerability of cariprazine in acute mania associated with bipolar I disorder: a phase II trial.

Authors: Suresh Durgam; Anju Starace; Dayong Li; Raffaele Migliore; Adam Ruth; György Németh; István Laszlovszky
Journal: Bipolar Disord Date: 2014-07-24 Impact factor: 6.744

9. Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: I. neurochemical characterisation of RG-15.

Authors: Béla Kiss; István Laszlovszky; Attila Horváth; Zsolt Némethy; Eva Schmidt; Gyula Bugovics; Károly Fazekas; István Gyertyán; Eva Agai-Csongor; György Domány; Zsolt Szombathelyi
Journal: Naunyn Schmiedebergs Arch Pharmacol Date: 2008-06-13 Impact factor: 3.000

6. Calbindin Deficits May Underlie Dissociable Effects of 5-HT₆ and mGlu₇ Antagonists on Glutamate and Cognition in a Dual-Hit Neurodevelopmental Model for Schizophrenia.

Authors: Sinead E Shortall; Angus M Brown; Eliot Newton-Mann; Erin Dawe-Lane; Chanelle Evans; Maxine Fowler; Madeleine V King
Journal: Mol Neurobiol Date: 2020-06-12 Impact factor: 5.682

6 in total

Cariprazine: First Global Approval.

1. Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: II. behavioural characterisation of RG-15.

2. Efficacy and safety of low- and high-dose cariprazine in acute and mixed mania associated with bipolar I disorder: a double-blind, placebo-controlled study.

Review 3. The role of dopamine D(3) receptors in antipsychotic activity and cognitive functions.

4. An evaluation of the safety and efficacy of cariprazine in patients with acute exacerbation of schizophrenia: a phase II, randomized clinical trial.

5. Efficacy and Safety of Cariprazine in Acute Exacerbation of Schizophrenia: Results From an International, Phase III Clinical Trial.

6. Cariprazine in the treatment of acute mania in bipolar I disorder: a double-blind, placebo-controlled, phase III trial.

7. Cariprazine, a dopamine D(3)-receptor-preferring partial agonist, blocks phencyclidine-induced impairments of working memory, attention set-shifting, and recognition memory in the mouse.

8. The efficacy and tolerability of cariprazine in acute mania associated with bipolar I disorder: a phase II trial.

9. Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: I. neurochemical characterisation of RG-15.

10. Cariprazine exerts antimanic properties and interferes with dopamine D2 receptor β-arrestin interactions.

Review 1. New Antipsychotic Medications in the Last Decade.

2. Perils of Pragmatic Psychiatry: How We Can Do Better.

Review 3. Progress and Pitfalls in Developing Agents to Treat Neurocognitive Deficits Associated with Schizophrenia.

Review 4. Second Generation Antipsychotics in the Treatment of Major Depressive Disorder: An Update.

5. Cariprazine, A Dopamine D₂/D₃ Receptor Partial Agonist, Modulates ABCG2-Mediated Multidrug Resistance in Cancer.

6. Calbindin Deficits May Underlie Dissociable Effects of 5-HT₆ and mGlu₇ Antagonists on Glutamate and Cognition in a Dual-Hit Neurodevelopmental Model for Schizophrenia.