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卡利拉嗪:全球首次批准。

Cariprazine: First Global Approval.

机构信息

Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.

出版信息

Drugs. 2015 Nov;75(17):2035-43. doi: 10.1007/s40265-015-0494-7.

DOI:10.1007/s40265-015-0494-7
PMID:26510944
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.

摘要

卡利拉嗪(Vraylar)是一种由杰德恩·理特公司开发的口服非典型抗精神病药物。它是一种有效的多巴胺 D3 和 D2 受体部分激动剂,优先与 D3 受体结合。卡利拉嗪还具有 5-羟色胺 5-HT1A 受体的部分激动活性。2015 年 9 月,卡利拉嗪在美国获得了第一个全球批准,用于治疗精神分裂症和双相 I 障碍相关的急性躁狂或混合发作。它还在多个国家开发用于治疗以阴性症状为主的精神分裂症(III 期)、作为辅助治疗重度抑郁症(II/III 期)和治疗双相抑郁症(II 期)。本文总结了卡利拉嗪开发过程中的重要里程碑,这些里程碑促成了它在精神分裂症和双相 I 障碍相关的急性躁狂或混合发作方面的首次批准。

相似文献

1
Cariprazine: First Global Approval.卡利拉嗪:全球首次批准。
Drugs. 2015 Nov;75(17):2035-43. doi: 10.1007/s40265-015-0494-7.
2
Cariprazine for the Treatment of Schizophrenia: A Review of this Dopamine D3-Preferring D3/D2 Receptor Partial Agonist.卡立普嗪用于治疗精神分裂症:对这种优先作用于多巴胺D3的D3/D2受体部分激动剂的综述
Clin Schizophr Relat Psychoses. 2016 Summer;10(2):109-19. doi: 10.3371/1935-1232-10.2.109.
3
Cariprazine, an orally active D2/D3 receptor antagonist, for the potential treatment of schizophrenia, bipolar mania and depression.卡立普嗪,一种口服活性D2/D3受体拮抗剂,用于潜在治疗精神分裂症、双相躁狂和抑郁症。
Curr Opin Investig Drugs. 2010 Jul;11(7):823-32.
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Cariprazine:New dopamine biased agonist for neuropsychiatric disorders.卡立普嗪:用于神经精神疾病的新型多巴胺偏向性激动剂。
Drugs Today (Barc). 2016 Feb;52(2):97-110. doi: 10.1358/dot.2016.52.2.2461868.
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Mechanism of action of cariprazine.卡立普嗪的作用机制。
CNS Spectr. 2016 Apr;21(2):123-7. doi: 10.1017/S1092852916000043. Epub 2016 Mar 9.
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The Novel Antipsychotic Cariprazine (RGH-188): State-of-the-Art in the Treatment of Psychiatric Disorders.新型抗精神病药物卡立普嗪(RGH-188):精神疾病治疗的最新进展
Curr Pharm Des. 2016;22(33):5144-5162. doi: 10.2174/1381612822666160701084447.
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Cariprazine in schizophrenia: clinical efficacy, tolerability, and place in therapy.卡利拉嗪在精神分裂症中的疗效、耐受性和治疗地位。
Adv Ther. 2013 Feb;30(2):114-26. doi: 10.1007/s12325-013-0006-7. Epub 2013 Jan 28.
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Efficacy and safety of cariprazine in the treatment of bipolar disorder.卡利拉嗪治疗双相情感障碍的疗效和安全性。
Expert Opin Pharmacother. 2019 Dec;20(17):2063-2072. doi: 10.1080/14656566.2019.1660319. Epub 2019 Oct 23.
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Cariprazine for the Treatment of Bipolar Disorder.卡立普嗪用于治疗双相情感障碍。
Perspect Psychiatr Care. 2017 Jul;53(3):148-155. doi: 10.1111/ppc.12150. Epub 2016 Apr 5.
10
Cariprazine in Psychiatry: A Comprehensive Review of Efficacy, Safety, and Therapeutic Potential.卡利拉嗪在精神病学中的应用:疗效、安全性和治疗潜力的综合评价。
Med Sci Monit. 2024 Sep 20;30:e945411. doi: 10.12659/MSM.945411.

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Cariprazine in Psychiatry: A Comprehensive Review of Efficacy, Safety, and Therapeutic Potential.卡利拉嗪在精神病学中的应用:疗效、安全性和治疗潜力的综合评价。
Med Sci Monit. 2024 Sep 20;30:e945411. doi: 10.12659/MSM.945411.
3
A review on the pharmacology of cariprazine and its role in the treatment of negative symptoms of schizophrenia.卡立普嗪的药理学及其在治疗精神分裂症阴性症状中的作用综述。

本文引用的文献

1
Efficacy and Safety of Cariprazine in Acute Exacerbation of Schizophrenia: Results From an International, Phase III Clinical Trial.卡立哌嗪用于精神分裂症急性加重期的疗效与安全性:一项国际III期临床试验的结果
J Clin Psychopharmacol. 2015 Aug;35(4):367-73. doi: 10.1097/JCP.0000000000000346.
2
Cariprazine exerts antimanic properties and interferes with dopamine D2 receptor β-arrestin interactions.卡利拉嗪具有抗躁狂特性,并干扰多巴胺 D2 受体β-arrestin 相互作用。
Pharmacol Res Perspect. 2015 Feb;3(1):e00073. doi: 10.1002/prp2.73. Epub 2014 Dec 2.
3
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.
Front Psychiatry. 2024 Apr 22;15:1385925. doi: 10.3389/fpsyt.2024.1385925. eCollection 2024.
4
Late-stage modification of bioactive compounds: Improving druggability through efficient molecular editing.生物活性化合物的后期修饰:通过高效分子编辑提高成药可能性。
Acta Pharm Sin B. 2024 Mar;14(3):1030-1076. doi: 10.1016/j.apsb.2023.11.021. Epub 2023 Nov 18.
5
Functional single nucleotide polymorphisms in dopaminergic receptors D2 predict clinical response to Cariprazine.多巴胺能受体D2中的功能性单核苷酸多态性可预测对卡立普嗪的临床反应。
Front Pharmacol. 2023 May 9;14:1182393. doi: 10.3389/fphar.2023.1182393. eCollection 2023.
6
G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders.G 蛋白偶联受体在神经退行性疾病和精神障碍中的作用。
Signal Transduct Target Ther. 2023 May 3;8(1):177. doi: 10.1038/s41392-023-01427-2.
7
Seventy Years of Antipsychotic Development: A Critical Review.抗精神病药物研发七十年:批判性综述
Biomedicines. 2023 Jan 4;11(1):130. doi: 10.3390/biomedicines11010130.
8
Progress and Pitfalls in Developing Agents to Treat Neurocognitive Deficits Associated with Schizophrenia.开发治疗精神分裂症相关神经认知缺陷药物的进展与挑战。
CNS Drugs. 2022 Aug;36(8):819-858. doi: 10.1007/s40263-022-00935-z. Epub 2022 Jul 13.
9
New Antipsychotic Medications in the Last Decade.过去十年中的新型抗精神病药物。
Curr Psychiatry Rep. 2021 Nov 29;23(12):87. doi: 10.1007/s11920-021-01298-w.
10
C-N Bond Formation by Consecutive Continuous-Flow Reductions towards A Medicinally Relevant Piperazine Derivative.通过连续的连续流还原反应构建 C-N 键,合成具有医学相关性的哌嗪衍生物。
Molecules. 2021 Apr 2;26(7):2040. doi: 10.3390/molecules26072040.
卡利拉嗪低、高剂量治疗与双相 I 型障碍相关的急性和混合躁狂的疗效和安全性:一项双盲、安慰剂对照研究。
J Clin Psychiatry. 2015 Mar;76(3):284-92. doi: 10.4088/JCP.14m09081.
4
Cariprazine in the treatment of acute mania in bipolar I disorder: a double-blind, placebo-controlled, phase III trial.卡立普嗪治疗双相 I 型障碍急性躁狂发作:一项双盲、安慰剂对照的 III 期试验。
J Affect Disord. 2015 Mar 15;174:296-302. doi: 10.1016/j.jad.2014.11.018. Epub 2014 Nov 24.
5
The efficacy and tolerability of cariprazine in acute mania associated with bipolar I disorder: a phase II trial.卡立普嗪治疗伴有双相I型障碍的急性躁狂症的疗效和耐受性:一项II期试验
Bipolar Disord. 2015 Feb;17(1):63-75. doi: 10.1111/bdi.12238. Epub 2014 Jul 24.
6
An evaluation of the safety and efficacy of cariprazine in patients with acute exacerbation of schizophrenia: a phase II, randomized clinical trial.卡利拉嗪治疗精神分裂症激越发作的安全性和有效性评价:一项 II 期、随机临床试验。
Schizophr Res. 2014 Feb;152(2-3):450-7. doi: 10.1016/j.schres.2013.11.041. Epub 2014 Jan 10.
7
Role of dopamine D(2) receptors for antipsychotic activity.多巴胺D(2)受体在抗精神病活性中的作用。
Handb Exp Pharmacol. 2012(212):27-52. doi: 10.1007/978-3-642-25761-2_2.
8
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.卡利拉嗪,一种多巴胺 D(3)受体部分激动剂,可阻断苯环己哌啶导致的小鼠工作记忆、注意定势转移和识别记忆损伤。
Psychopharmacology (Berl). 2013 Mar;226(1):91-100. doi: 10.1007/s00213-012-2896-5. Epub 2012 Oct 19.
9
The role of dopamine D(3) receptors in antipsychotic activity and cognitive functions.多巴胺D(3)受体在抗精神病活性和认知功能中的作用。
Handb Exp Pharmacol. 2012(213):167-210. doi: 10.1007/978-3-642-25758-2_7.
10
Cariprazine (RGH-188), a potent D3/D2 dopamine receptor partial agonist, binds to dopamine D3 receptors in vivo and shows antipsychotic-like and procognitive effects in rodents.卡利拉嗪(RGH-188),一种有效的 D3/D2 多巴胺受体部分激动剂,在体内与多巴胺 D3 受体结合,并在啮齿动物中表现出抗精神病和认知促进作用。
Neurochem Int. 2011 Nov;59(6):925-35. doi: 10.1016/j.neuint.2011.07.002. Epub 2011 Jul 13.