A5060763145- Schizophrenia research and treatment
- Bipolar Disorder and Treatment
- Neurotransmitter Receptor Influence on Behavior
- Treatment of Major Depression
- Receptor Mechanisms and Signaling
- Anxiety, Depression, Psychometrics, Treatment, Cognitive Processes
- Child and Adolescent Psychosocial and Emotional Development
- Neuroscience and Neuropharmacology Research
- Pharmaceutical studies and practices
- Attention Deficit Hyperactivity Disorder
- Functional Brain Connectivity Studies
- Health Systems, Economic Evaluations, Quality of Life
- Mental Health Treatment and Access
- Mental Health and Psychiatry
- Electroconvulsive Therapy Studies
- Mental Health Research Topics
- Pharmacological Receptor Mechanisms and Effects
- Obsessive-Compulsive Spectrum Disorders
- Gastrointestinal motility and disorders
- Genetic Mapping and Diversity in Plants and Animals
- Pharmacological Effects and Toxicity Studies
- Medical Imaging Techniques and Applications
- Neuroscience and Music Perception
- Cyclopropane Reaction Mechanisms
- Neuroendocrine regulation and behavior
Gedeon Richter (Hungary)
2012-2022
Case Western Reserve University
2015
University Hospitals Cleveland Medical Center
2015
Universitat de Barcelona
2015
Creative Commons
2015
New York State Office of Mental Health
1996
Nathan Kline Institute for Psychiatric Research
1990-1994
Cariprazine {RGH-188; trans-N-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-N',N'-dimethylurea hydrochloride}, a novel candidate antipsychotic, demonstrated approximately 10-fold higher affinity for human D(3) versus D(2L) and D(2S) receptors (pKi 10.07, 9.16, 9.31, respectively). It displayed high at serotonin (5-HT) type 2B (pK(i) 9.24) with pure antagonism. had lower rat hippocampal 5-HT(1A) 8.59 8.34, respectively) low intrinsic efficacy. 5-HT(2A) 7.73). Moderate or...
Objective: The authors evaluated the efficacy, safety, and tolerability of cariprazine, an atypical antipsychotic candidate, in adult patients with acute bipolar I depression. Method: This was 8-week multinational, multicenter, randomized, double-blind, placebo-controlled, parallel-group, fixed-dose study disorder experiencing a current major depressive episode. Patients were randomly assigned (1:1:1:1) to receive placebo or cariprazine at 0.75, 1.5, 3.0 mg/day. primary secondary efficacy...
Cariprazine is an orally active and potent D3 D2 partial agonist with preferential binding to receptors in development for the treatment of schizophrenia bipolar mania. This study (NCT00694707) evaluated efficacy safety cariprazine patients acute exacerbation schizophrenia.This was a multinational, double-blind, randomized, placebo- active-controlled, fixed-dose trial. Patients were randomized receive placebo, 1.5mg/d, 3.0mg/d, 4.5mg/d, or risperidone 4.0mg/d (for assay sensitivity) 6 weeks...
This phase III study evaluated the efficacy and safety of cariprazine, a dopamine D3 D2 receptor partial agonist with preferential binding to receptors, in patients acute exacerbation schizophrenia. Patients were randomized 6-week double-blind treatment placebo, cariprazine 3 6 mg/d, or 9 mg/d. Primary secondary efficacy: change from baseline week Positive Negative Syndrome Scale total Clinical Global Impressions-Severity scores, respectively, analyzed using mixed-effects model for repeated...
This phase 3 study evaluated the efficacy, safety, and tolerability of cariprazine in patients with acute exacerbation schizophrenia.This multinational, randomized, double-blind, placebo- active-controlled was conducted from April 2010 to December 2011. Patients who met DSM-IV-TR criteria for schizophrenia were randomized placebo (n = 153), mg/d 155), 6 157), or aripiprazole 10 152) weeks double-blind treatment. The primary secondary efficacy parameters mean change baseline week Positive...
This Phase III, randomized, double-blind, placebo-controlled study investigated the efficacy and tolerability of flexibly-dosed cariprazine in patients with acute manic or mixed episodes associated bipolar I disorder. Patients were randomized to 3 weeks double-blind treatment 3–12 mg/day (n=158) placebo (n=154). The primary parameter was change from baseline Week Young Mania Rating Scale (YMRS) total score. secondary Clinical Global Impressions-Severity (CGI-S) Mean YMRS score significantly...
Objectives Cariprazine, an orally active and potent dopamine D 3 2 receptor partial agonist with preferential binding to receptors, is being developed for the treatment of schizophrenia bipolar mania. This Phase II trial evaluated efficacy, safety, tolerability cariprazine versus placebo in acute manic or mixed episodes associated I disorder. Methods was a multinational, randomized, double‐blind, placebo‐controlled, flexible‐dose study 3–12 mg/day patients Following washout, received three...
Abstract Rationale Second-generation antipsychotics occupy dopamine D 2 receptors and act as antagonists or partial agonists at these receptors. While drugs alleviate positive symptoms in patients with schizophrenia, they are less effective for treating cognitive deficits negative symptoms. Dopamine 3 highly expressed areas of the brain thought to play a role regulation motivation reward-related behavior. Consequently, receptor has become target combination antagonism treat schizophrenia....
Article Abstract Objective: This phase 3 trial evaluated the efficacy, safety, and tolerability of low- high-dose cariprazine in patients meeting DSM-IV-TR criteria for acute manic or mixed episodes associated with bipolar I disorder. Method: multicenter, randomized, double-blind, placebo-controlled, parallel-group, fixed/flexible-dose study was conducted from February 2010 to December 2011. Patients were randomly assigned placebo, 3-6 mg/d, 6-12 mg/d weeks double-blind treatment. Primary...
Article AbstractBackground: Cariprazine is an atypical antipsychotic currently under investigation as adjunctive therapy in patients with major depressive disorder (MDD) who have inadequate response to standard antidepressant therapy.Method: A randomized, double-blind, placebo-controlled, flexible-dose study was conducted from December 2011 2013 adults met DSM-IV-TR criteria for MDD and had response. Eligible were randomized 8-week treatment placebo (n = 269), cariprazine 1-2 mg/d 274), or...
Abstract Background: Negative symptoms in schizophrenia are heterogeneous and multidimensional; effective treatments lacking. Cariprazine, a dopamine D 3 -preferring /D 2 receptor partial agonist serotonin 5-HT 1A agonist, was significantly more than risperidone treating negative prospectively designed trial patients with persistent, predominant symptoms. Methods: Using post hoc analyses, we evaluated change from baseline at week 26 individual items of the Positive Syndrome Scale (PANSS)...
Abstract Objective To investigate the effect of cariprazine on cognitive symptom change across bipolar I disorder and schizophrenia. Methods Post hoc analyses 3- to 8-week pivotal studies in depression mania were conducted; one schizophrenia trial including Cognitive Drug Research System attention battery was also analyzed. Outcomes interest: Montgomery-Åsberg Depression Rating Scale [MADRS], Functioning Assessment Short Test [FAST], Positive Negative Syndrome [PANSS]). LSMDs from baseline...
Cariprazine, a dopamine D3/D2 receptor partial agonist with preference for D3 receptors, has demonstrated efficacy in randomized controlled trials schizophrenia. This multinational, randomized, double-blind, placebo-controlled, parallel-group study evaluated the efficacy, safety, and tolerability of cariprazine relapse prevention adults schizophrenia; total duration was up to 97 weeks. Schizophrenia symptoms were treated/stabilized 3–9 mg/d during 20-week open-label treatment consisting an...
Schizophrenia is a chronic and debilitating neuropsychiatric disorder that often requires long-term pharmacotherapy to manage symptoms prevent relapse. Cariprazine potent dopamine D3 D2 receptor partial agonist FDA-approved in the US for treatment of schizophrenia manic or mixed episodes associated with bipolar I adults; recommended dose range 1.5-6 mg/d.To further characterize safety cariprazine, data from two 48-week open-label, flexible-dose extension studies were pooled post hoc...
This 6-week, double-blind, placebo-controlled, proof-of-concept study evaluated the efficacy, safety, and tolerability of low-dose (1.5-4.5 mg/day) high-dose (6-12 cariprazine in patients with acute exacerbation schizophrenia (NCT00404573). The primary efficacy measure was change Positive Negative Syndrome Scale (PANSS) total score, analyzed using a last observation carried forward approach. Other measures included Clinical Global Impression-Severity (secondary) PANSS subscales (additional)....
Objective Cariprazine, a dopamine D 3 /D 2 partial agonist atypical antipsychotic with preferential binding to receptors, is approved for the treatment of schizophrenia and manic or mixed episodes associated bipolar I disorder. The efficacy safety cariprazine was established in three randomized, double-blind, placebo-controlled, 6-week trials patients acute exacerbation schizophrenia. This 53-week study evaluated long-term tolerability Methods multicenter, open-label, flexible-dose 3–9 mg/d...
Cariprazine, a potent dopamine D3 and D2 receptor partial agonist antipsychotic with preferential binding to receptors, is Food Drug Administration approved for treating schizophrenia manic or mixed episodes of bipolar I disorder. A post-hoc safety/tolerability analysis data from the four acute trials in cariprazine clinical development program (NCT00404573; NCT00694707; NCT01104766; NCT01104779) was carried out using overall safety population (all patients who received ≥1 dose study drug)...
Cariprazine, a dopamine D3/D2 receptor partial agonist antipsychotic, demonstrated efficacy and tolerability in 6-week, randomized, placebo-controlled schizophrenia trials. Schizophrenia is chronic disorder that requires continuous treatment; therefore, the long-term safety profile of antipsychotic agents an important factor guiding clinician decisions. This single-arm, open-label extension study evaluated cariprazine patients with schizophrenia. Patients enrolled this completed placebo-...
This 19-week, double-blind, placebo-controlled, randomized phase 2 study evaluated the efficacy, safety, and tolerability of adjunctive cariprazine (0.1-0.3 1.0-2.0 mg/day) as an antidepressant treatment for adults with treatment-resistant major depressive disorder (MDD) (NCT00854100). The primary endpoint was change in Montgomery-Åsberg Depression Rating Scale (MADRS) total score secondary Clinical Global Impression-Intensity score. Additional efficacy parameters were also assessed. A 231...
Background: Long-term treatment with antipsychotic agents is indicated for patients schizophrenia, but associated adverse events (AEs) that contribute to medication discontinuation and nonadherence. Understanding drug safety profiles critical avoid unwanted side effects. Cariprazine a potent dopamine D 3 /D 2 receptor partial agonist approved the of adults schizophrenia (EU, US) acute manic/mixed depressive episodes bipolar I disorder (US). Methods: Post hoc analyses were conducted...