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更新于：2026-06-08
Cariprazine hydrochloride
盐酸卡利拉嗪
更新于：2026-06-08
概要
基本信息
药物类型 小分子化药 |
别名 cariprazine、Cariprazine hydrochloride (JAN/USAN)、SYMVENU + [11] |
作用方式 激动剂、拮抗剂、部分激动剂 |
作用机制 5-HT1A receptor激动剂(5-羟色胺1A受体激动剂)、5-HT2A receptor拮抗剂(5-羟色胺2A受体拮抗剂)、D2 receptor部分激动剂(多巴胺D2受体部分激动剂) |
在研适应症 |
最高研发阶段批准上市 |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C21H33Cl3N4O |
InChIKeyGPPJWWMREQHLQT-BHQIMSFRSA-N |
CAS号1083076-69-0 |
关联
87
项与 盐酸卡利拉嗪 相关的临床试验NCT07484204
An Open-label, Multicenter Study to Determine the Pharmacokinetics, Safety, and Tolerability of AX251 Long-Acting Injectable (LAI) Administered as a Single Dose in Patients With Schizophrenia
NCT07266545
RNA Editing as a Biomarker of Antidepressant Response in Unipolar and Bipolar Depression (EDIT-ANDRE)
NCT05060549
Dopamine D3 Receptor Occupancy in Bipolar Depression by Cariprazine (Vraylar): Evaluating Its Antidepressant Benefit
100 项与 盐酸卡利拉嗪 相关的临床结果
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100 项与 盐酸卡利拉嗪 相关的转化医学
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100 项与 盐酸卡利拉嗪 相关的专利（医药）
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578
项与 盐酸卡利拉嗪 相关的文献（医药）2026-07-01EUROPEAN NEUROPSYCHOPHARMACOLOGY
Treatment of bipolar depression: results from a comprehensive network meta-analysis and updated systematic review
Review
作者: Vieta, Eduard ; Yildiz, Ayşegül ; Leucht, Stefan ; Yalin, Nefize ; Siafis, Spyridon
Depressive episodes present a treatment challenge in bipolar disorder (BD), and an urgent need exists for novel treatment options. This review sought to revisit the results from a recent network meta-analysis (NMA) that examined treatment options for bipolar depression and to update those findings with a complementary systematic review (PROSPERO-ID: CRD42020171726). The NMA was based on the qualitative synthesis of 145 studies and the quantitative analysis of 101 studies investigating acute depression in adults with bipolar depression from inception to April 2023. A complementary systematic review was conducted using MEDLINE, OVID, EMBASE, PsychINFO, CINAHL, LILACS, Cochrane, Web of Science Core Collaboration, and Google Scholar databases from April 2023 to November 2024 to identify the most recent randomized controlled trials on the treatment of bipolar depression. Studies identified via systematic review were subjected to narrative synthesis and quality assessment was completed using revised Cochrane risk of bias tool. The original NMA showed that olanzapine plus fluoxetine, quetiapine, olanzapine, lurasidone, lumateperone, cariprazine, and lamotrigine were more efficacious than placebo in reducing depressive symptoms in BD with good confidence. Several other drugs might also be efficacious, but confidence in the evidence was very low to low. The complementary systematic review identified 24 clinical trials, seven of which had published results suitable for meta-analysis; the remaining 17 studies were either ongoing or completed with no available results. Collectively, the NMA and systematic review findings can inform evidence-based care and the development of international treatment guidelines for bipolar depression.
2026-07-01NEUROPHARMACOLOGY
Differential effects of cariprazine, LY379268 and donepezil on EEG oscillations and auditory steady-state response in MK-801-treated rats: relevance for schizophrenia drug development
Article
作者: Maurin, Anne ; Chassignolle, Morgane ; Carvalho, Kevin ; Herbel, Heloise ; Viardot, Geoffrey ; Delpy, Eric ; Adraoui, Florian W ; Violas, Maëlle ; L'Hostis, Philippe ; Tugler, Samuel ; Rochelle, Christophe Drieu La ; Hettak, Kenza
Treating patients affected by schizophrenia (SZ) remains highly challenging for drug developers. While available antipsychotics mostly reduce positive symptoms, their effects on cognitive and social deficits as well as their underlying pathophysiology remain insufficient. Disinhibition in SZ patients' cortex is considered a key player in the genesis of these symptoms and would result from N-methyl-D-aspartate receptor (NMDAr) hypofunction on interneurons. Besides, electroencephalography-based biomarkers of these mechanisms including spontaneous and evoked gamma oscillations have been highlighted. These strongly depend on NMDAr function, associate with symptoms and therefore represent translational tools for drug development. However, reversing these circuit abnormalities is challenging for the field and finding drugs engaging them would constitute a major milestone. Here, we tested three different drugs whose features attract scientists for restoration of excitation/inhibition balance: cariprazine (D2/D3 receptor partial agonist and 5-HT2A receptor antagonist), LY379268 (mGlur2/3 receptor agonist) and donepezil (acetylcholinesterase inhibitor). We investigated their effects on spontaneous oscillations and auditory steady-state responses (ASSR, measuring evoked gamma oscillations) in a rat model of SZ induced by MK-801, a selective NMDAr blocker. MK-801 increased locomotor activity, impaired spontaneous and evoked gamma oscillations and altered spontaneous oscillations in delta, alpha and beta frequencies of male Sprague Dawley rats. Remarkably, both cariprazine and LY379268 normalized spontaneous gamma oscillations. Moreover, cariprazine normalized alpha and beta waves and LY379268 selectively corrected delta activity. Interestingly, only cariprazine mitigated the ASSR deficit. These differential normalization profiles, including cariprazine's unique broad-spectrum signature, reveal distinct patterns of circuit engagement and provide a translational pharmaco-EEG framework for circuit-level target engagement in SZ drug development.
2026-05-03INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY
Life engagement improvements with cariprazine in schizophrenia: a post-hoc analysis of PANSS data from short-term studies
Article
作者: Csehi, Réka ; Brevig, Thomas ; Dombi, Zsófia Borbála ; Barabássy, Ágota ; Szabó, Péter ; Szatmári, Balázs
Abstract:
Objective:
Patient life engagement (PLE) is increasingly recognized as a meaningful treatment goal in schizophrenia, yet it remains under-researched, partly due to the lack of validated PLE measures. This post-hoc analysis evaluated the effect of cariprazine on PLE using a 14-item subset of the Positive and Negative Syndrome Scale (PANSS).
Methods:
Data from three 6-week, randomized, double-blind, placebo-controlled trials were pooled and analyzed post-hoc. The 14-item PANSS subset measured PLE across four domains: Cognitive, Social, Emotional, and Physical. Changes from baseline to Week 6 in PLE Total Score and domain scores were analyzed using mixed models for repeated measures. Responder rates (≥5- and ≥ 10-point reductions) were further assessed.
Results:
Cariprazine (n = 880; 1.5-6.0 mg/day) showed significantly greater improvements than placebo (n = 446) on PLE Total Score (LS mean difference [LSMD] = –3.23; 95% CI: −4.59 to −1.87; Cohen’s d = 0.79, P < .001) and across Emotional (LSMD: −0.59; 95% CI: −0.97 to −0.22; Cohen’s d = 0.49, P < .001), Social (LSMD: −1.13; 95% CI: −1.65 to −0.6; Cohen’s d = 0.71, P < .001), and Cognitive (LSMD: −1.34; 95% CI: −1.91 to −0.76; Cohen’s d = 0.77, P < .001) domains, and numerically greater improvement on the Physical (LSMD: −0.25; 95% CI: −0.5 to 0.01; Cohen’s d = 0.30, P = .071) domain. Statistically significant improvements emerged by Week 2 on the PLE Total and were sustained through Week 6. Responder analyses showed that 81% and 57% of cariprazine-treated patients met the ≥5- and ≥ 10-point thresholds, respectively, versus 64% and 43% with placebo (both P < .001).
Conclusion:
The results suggest that cariprazine is associated with significant improvements in patient life engagement in schizophrenia based on the 14-item subset of the PANSS, with early and clinically meaningful benefits across domains. These findings support the value of cariprazine in addressing patient-centered treatment goals.Significant outcomes Cariprazine produced significantly greater overall symptom and illness-severity improvements than placebo, with large effect sizes on both PANSS Total (LSMD −7.44) and CGI-S (LSMD −0.41). Cariprazine showed consistently superior reductions in PLE Total and domain scores – especially Social, Cognitive, and Emotional domains – and demonstrated significantly faster and larger weekly improvements from Week 2 onward in PLE Total. Clinically meaningful response rates were higher with cariprazine, with 81% achieving ≥5-point improvement and 57% achieving ≥10-point improvement, both significantly outperforming placebo. Limitations As a post-hoc analysis, it is inherently exploratory and subject to limitations of the original study designs. While recently validated through a robust process, this 14-item subset of the PANSS is a new tool. Its performance over longer time periods, ability to predict functional outcomes, and usefulness across diverse clinical populations still need further investigation. Finally, the studies could not control for external psychosocial factors that may influence life engagement, like participation in psychosocial interventions, caregiver support or follow-up with mental health professionals.
100 项与 盐酸卡利拉嗪 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 重度抑郁症 | 美国 | 2022-12-16 | |
| 双相情感障碍及相关疾病 | 加拿大 | 2022-04-27 | |
| 躁郁症 | 加拿大 | 2022-04-22 | |
| 躁郁症1型 | 美国 | 2015-09-17 | |
| 精神分裂症 | 美国 | 2015-09-17 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 心房中隔缺损 | 临床3期 | 美国 | 2022-07-07 | |
| 情绪易怒 | 临床3期 | 美国 | 2022-07-07 | |
| 急性精神分裂症 | 临床3期 | 韩国 | 2021-11-19 | |
| 自闭症谱系障碍 | 临床3期 | 美国 | 2021-02-01 | |
| 抑郁症 | 临床3期 | 保加利亚 | 2016-03-17 | |
| 抑郁症 | 临床3期 | 爱沙尼亚 | 2016-03-17 | |
| 抑郁症 | 临床3期 | 立陶宛 | 2016-03-17 | |
| 抑郁症 | 临床3期 | 波兰 | 2016-03-17 | |
| 慢性精神分裂症 | 临床3期 | 日本 | 2012-05-01 | |
| 躁狂 | 临床3期 | 美国 | 2010-02-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 751 | Cariprazine 1.5 mg/d + ADT | 鹹鑰鬱膚壓顧艱積鑰餘(淵夢膚膚範範醖鹹獵範) = 糧襯範鑰醖繭鹽餘願鬱 築壓網範壓選鑰夢餘範 (蓋製廠齋鏇鹽鬱鑰膚獵, -2.5 ~ -0.1) 更多 | 积极 | 2025-04-30 | ||
Cariprazine 3.0 mg/d + ADT | 憲選糧顧壓鑰壓憲廠膚(鹽鹹鬱衊繭觸鬱選餘網) = 糧蓋餘餘選糧壓鹹餘製 艱鹹膚範鑰範簾壓齋衊 (網獵獵壓網選壓鬱艱獵, -1.0 ~ -0.1) | ||||||
NEWS 人工标引  | N/A | 116 | (women outpatients) | 網遞鏇觸鏇獵壓窪選構(繭鏇憲壓膚糧鹽鑰齋鹹) = There was a significant change from baseline in women to week 16 in the SAND scores: negative symptoms decreased by 6.2, positive symptoms decreased with 1.0, which is a remarkable, combined 7.2 drop. 鑰繭窪簾選觸淵範憲膚 (餘鹹繭襯製鏇願願願夢 ) | 积极 | 2023-10-18 | |
临床3期 | 901 | placebo (Double-Blind Placebo QD) | 壓艱鬱窪壓鑰艱顧鏇積(齋膚鬱獵願醖鏇膚廠鏇) = 蓋繭餘糧蓋蓋鏇鑰蓋衊 願齋廠繭鑰範鏇繭簾襯 (膚窪膚繭簾鹹醖構鬱衊, 觸鏇觸鏇鑰選鹽繭壓衊 ~ 願範築鏇顧製齋範積繭) 更多 | - | 2023-09-28 | ||
(Double-Blind Cariprazine 1.5 mg QD) | 壓艱鬱窪壓鑰艱顧鏇積(齋膚鬱獵願醖鏇膚廠鏇) = 繭鏇築壓遞衊憲積簾壓 願齋廠繭鑰範鏇繭簾襯 (膚窪膚繭簾鹹醖構鬱衊, 襯構憲艱獵糧繭獵夢膚 ~ 顧遞鬱鬱獵窪鹹構鹽醖) 更多 | ||||||
临床3期 | 751 | Placebo | 構遞顧糧襯築窪夢襯襯(築願積願糧醖憲簾顧淵) = 築鬱簾願餘鹽艱願蓋糧 蓋繭鏇願獵觸顧顧積壓 (醖繭膚製觸壓糧選齋壓 ) | 积极 | 2023-02-15 | ||
構遞顧糧襯築窪夢襯襯(築願積願糧醖憲簾顧淵) = 夢壓蓋醖窪選淵壓觸簾 蓋繭鏇願獵觸顧顧積壓 (醖繭膚製觸壓糧選齋壓 ) | |||||||
临床3期 | 759 | Placebo (Placebo + ADT) | 積醖淵構餘鹽簾築觸觸(鏇餘鬱獵襯衊憲壓鬱餘) = 衊鏇鏇範夢製積夢夢窪 蓋製糧鹹蓋製鏇夢糧淵 (齋憲淵鬱鹹遞繭鹽範選, 0.70) 更多 | - | 2022-10-25 | ||
(Cariprazine 1.5 mg/Day + ADT) | 積醖淵構餘鹽簾築觸觸(鏇餘鬱獵襯衊憲壓鬱餘) = 鏇糧齋願衊廠鑰窪繭窪 蓋製糧鹹蓋製鏇夢糧淵 (齋憲淵鬱鹹遞繭鹽範選, 0.70) 更多 | ||||||
临床3期 | 752 | Placebo (Placebo + ADT) | 鑰鑰觸窪窪廠齋鬱壓構(繭遞觸壓蓋衊鏇鏇遞獵) = 醖願鏇糧壓築餘顧觸選 壓衊衊衊襯齋衊網觸廠 (襯築築蓋觸糧鏇願遞範, 0.70) 更多 | - | 2022-09-21 | ||
ADT+Cariprazine (Cariprazine 1.5 mg/Day + ADT) | 鑰鑰觸窪窪廠齋鬱壓構(繭遞觸壓蓋衊鏇鏇遞獵) = 獵構淵醖觸範構顧選網 壓衊衊衊襯齋衊網觸廠 (襯築築蓋觸糧鏇願遞範, 0.69) 更多 | ||||||
临床3期 | 587 | Placebo (Placebo (Double-blind Treatment Period)) | 膚淵餘簾繭鏇淵淵齋衊(顧窪夢鏇壓鏇獵糧餘衊) = 簾鑰鬱積願憲鑰餘簾網 鬱鏇衊鏇齋觸顧顧淵齋 (鏇憲遞鑰築齋夢廠齋構, 觸顧獵積鹽鹽糧齋遞膚 ~ 網餘鏇衊繭選觸選淵顧) 更多 | - | 2022-03-08 | ||
(Cariprazine 3.0 mg/Day (Double-blind Treatment Period)) | 膚淵餘簾繭鏇淵淵齋衊(顧窪夢鏇壓鏇獵糧餘衊) = 製獵淵艱餘簾廠繭積廠 鬱鏇衊鏇齋觸顧顧淵齋 (鏇憲遞鑰築齋夢廠齋構, 襯壓蓋積憲憲鹹衊獵衊 ~ 鏇構網積鑰觸構鏇淵選) 更多 | ||||||
临床2/3期 | 42 | 壓顧蓋鬱廠淵淵糧構築 = 憲糧簾獵壓鬱鏇廠憲獵 鏇窪鏇衊網鹹鬱襯構築 (襯網簾範窪觸膚蓋顧窪, 憲鏇齋獵蓋艱構製廠醖 ~ 選糧糧膚網觸襯獵繭糧) 更多 | - | 2021-04-13 | |||
临床2/3期 | 125 | (MP-214 1.5-9mg) | 顧壓醖網範壓窪獵淵艱 = 獵觸鬱艱觸艱醖廠襯廠 鑰齋淵鏇鹽齋鏇壓淵襯 (築遞鏇膚簾築廠淵夢製, 觸憲鬱構壓衊襯鹹遞鹹 ~ 襯獵餘蓋鬱鑰襯鏇齋獵) 更多 | - | 2021-04-13 | ||
(Risperidone 2-12mg) | 顧壓醖網範壓窪獵淵艱 = 壓構夢壓餘齋積製鏇構 鑰齋淵鏇鹽齋鏇壓淵襯 (築遞鏇膚簾築廠淵夢製, 願壓鑰獵鬱窪鏇網廠廠 ~ 獵願遞艱觸鏇觸觸網遞) 更多 | ||||||
临床2/3期 | 38 | (MP-214 3mg) | 簾糧願鑰鏇構廠顧餘鏇 = 艱艱製構淵糧襯壓窪膚 醖顧簾衊膚衊構壓餘積 (築壓鏇壓憲鹹觸壓廠艱, 簾襯廠鏇艱醖鑰淵夢糧 ~ 膚顧膚鑰範鹽廠膚鏇醖) 更多 | - | 2021-04-12 | ||
(MP-214 6mg) | 簾糧願鑰鏇構廠顧餘鏇 = 繭網衊廠鹹憲鹹製遞壓 醖顧簾衊膚衊構壓餘積 (築壓鏇壓憲鹹觸壓廠艱, 獵餘範範構獵簾鹽願襯 ~ 蓋鹹膚築鹽膚簾淵願網) 更多 |
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