Phase 3, Randomized, 28 Days, Double-blind, Placebo-controlled, Multicenter Study to Assess the Safety and Efficacy of Brilaroxazine (RP5063) in Subjects With Schizophrenia, Followed by a 52-Week Open-label Extension

This study is to evaluate the effect and safety of Brilaroxazine in patients with acute schizophrenia compared to the placebo short and long-term. Brilaroxazine will be given at fixed doses of 15 mg or 50 mg once daily over 4 weeks, then in the long-term flexible doses 15-50mg daily over a period of 52 weeks.

开始日期2022-01-24

申办/合作机构

Reviva Pharmaceuticals Holdings, Inc.

NCT01490086 / Completed临床2期

REFRESH : Randomized Double-blind, Placebo-controlled, Multicenter Trial to Assess the Safety and Efficacy of RP5063 in Subjects With an Acute Exacerbation of Schizophrenia or Schizoaffective Disorder

The objective of this study is to evaluate the efficacy and safety of RP5063 relative to placebo for the treatment of schizophrenia or schizoaffective disorder.

开始日期2011-12-01

申办/合作机构

Reviva Pharmaceuticals Holdings, Inc.

100 项与 Brilaroxazine 相关的临床结果

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100 项与 Brilaroxazine 相关的转化医学

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100 项与 Brilaroxazine 相关的专利（医药）

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项与 Brilaroxazine 相关的文献（医药）

2024-02-01·Skin research and technology : official journal of International Society for Bioengineering and the Skin (ISBS) [and] International Society for Digital Imaging of Skin (ISDIS) [and] International Society for Skin Imaging (ISSI)

Brilaroxazine lipogel displays antipsoriatic activity in imiquimod‐induced mouse model

Article

作者: Ramakrishnan, Arulprakash ; Bhat, Laxminarayan ; Amirthalingam, Muthukumar ; Bhat, Seema R.

Abstract:

Background:

Dopamine (D) and serotonin (5‐HT) pathways contribute to psoriasis pathobiology. Disruptions incite increased inflammatory mediators, keratinocyte activation and deterioration, and worsening symptoms. Brilaroxazine (RP5063), which displays potent high binding affinity to D2/3/4 and 5‐HT1A/2A/2B/7 receptors and a moderate affinity to serotonin transporter (SERT), may affect the underlying psoriasis pathology.

Methods:

An imiquimod‐induced psoriatic mouse model (BALB/c) evaluated brilaroxazine's activity in a topical liposomal‐aqueous gel (Lipogel) formulation. Two of the three groups (n = 6 per) underwent induction with 5% imiquimod, and one group received topical brilaroxazine Lipogel (Days 1–11). Assessments included (1) Psoriasis Area and Severity Index (PASI) scores (Days 1–12), skin histology for Baker score based on H&E stained tissue (Day 12), and serum blood collection for serum cytokine analysis (Day 12). One‐way ANOVA followed by post hoc Dunnett's t‐test evaluated significance (p < 0.05).

Results:

Imiquimod‐induced animal Baker scores were higher versus Sham non‐induced control's results (p < 0.001). Brilaroxazine Lipogel had significantly (p = 0.003) lower Baker scores versus the induced Psoriasis group. Brilaroxazine PASI scores were lower (p = 0.03) versus the induced Psoriasis group (Days 3‐12), with the greatest effect in the last 3 days. The induced Psoriasis group showed higher Ki‐67 and TGF‐β levels versus non‐induced Sham controls (p = 0.001). The brilaroxazine Lipogel group displayed lower levels of these cytokines versus the induced Psoriasis group, Ki‐67 (p = 0.001) and TGF‐β (p = 0.008), and no difference in TNF‐α levels versus Sham non‐induced controls.

Conclusion:

Brilaroxazine Lipogel displayed significant activity in imiquimod‐induced psoriatic animals, offering a novel therapeutic strategy.

2023-12-20·Journal of the American Chemical Society

Highly Selective p-Xylene Separation from Mixtures of C8 Aromatics by a Nonporous Molecular Apohost

Article

作者: Matos, Catiúcia R M O ; Zaworotko, Michael J ; Bezrukov, Andrey A ; Wang, Shi-Qiang ; Eaby, Alan C ; Sensharma, Debobroto ; Hjiej-Andaloussi, Yassin ; Vandichel, Matthias ; Rahmani, Maryam

High and increasing production of separation of C8 aromatic isomers demands the development of purification methods that are efficient, scalable, and inexpensive, especially for p-xylene, PX, the largest volume C8 commodity. Herein, we report that 4-(1H-1,2,4-triazol-1-yl)-phenyl-1H-benzo[de]isoquinoline-1,3(2H)-dione (TPBD), a molecular compound that can be prepared and scaled up via solid-state synthesis, exhibits exceptional PX selectivity over each of the other C8 isomers, o-xylene (OX), m-xylene (MX), and ethylbenzene (EB). The apohost or α form of TPBD was found to exhibit conformational polymorphism in the solid state enabled by rotation of its triazole and benzene rings. TPBD-αI and TPBD-αII are nonporous polymorphs that transformed to the same PX inclusion compound, TPBD-PX, upon contact with liquid PX. TPBD enabled highly selective capture of PX, as established by competitive slurry experiments involving various molar ratios in binary, ternary, and quaternary mixtures of C8 aromatics. Binary selectivity values for PX as determined by ¹H NMR spectroscopy and gas chromatography ranged from 22.4 to 108.4, setting new benchmarks for both PX/MX (70.3) and PX/EB (59.9) selectivity as well as close to benchmark selectivity for PX/OX (108.4). To our knowledge, TPBD is the first material of any class to exhibit such high across-the-board PX selectivity from quaternary mixtures of C8 aromatics under ambient conditions. Crystallographic and computational studies provide structural insight into the PX binding site in TPBD-PX, whereas thermal stability and capture kinetics were determined by variable-temperature powder X-ray diffraction and slurry tests, respectively. That TPBD offers benchmark PX selectivity and facile recyclability makes it a prototypal molecular compound for PX purification or capture under ambient conditions.

2023-04-04·Analytical chemistry

A Green-Emitting Luminol Analogue as the Next-Generation Chemiluminescent Substrate in Biochemical Analysis.

Article

作者: Deng, Tao ; Zhu, Chenchen ; Huang, Xinxin ; Chen, Fuqian ; Cai, Chun ; Lin, Chaozhan ; Liu, Fang ; Xia, Xiaotong ; Li, Ting ; Ye, Dong

Luminol and its derivatives are extensively used as chemiluminogenic substrates in bioimaging and biochemical analysis. Luminol reagents can typically emit blue chemiluminescence (CL), whose wavelength is normally outside the most sensitive detection range of human naked eyes and most CL analyzers with silicon-based charge-coupled device (CCD) detectors. Development of luminol analogues with longer wavelength emission is thus attractive. Herein, four new phthalhydrazide CL probes (GL-1/2/3/4) have been prepared through the derivatization of luminol. The most promising one, 5-(4-hydroxy-1,3-dioxoisoindolin-2-yl)-2,3-dihydrophthalazine-1,4-dione (GL-1), emits bright green CL upon oxidation and shows enhanced CL performance compared to its parent luminol. Bloodstain imaging, horseradish peroxidase (HRP)-based immunoassay, and the analysis of glucose/glucose oxidase reaction have been performed using the GL-1 reagent. These results indicate that GL-1 is a new chemiluminogenic luminol analogue with great potential in real analytical applications and will be an alternative to replace luminol in practical CL analysis.

项与 Brilaroxazine 相关的新闻（医药）

2024-11-12

·药智网

“精分”领域8成新药不活跃，艾伯维新药未达终点

11月11日，艾伯维宣布其用于治疗精神病症状急性加重的精神分裂症新药Emraclidine的两项EMPOWER试验未达到其主要终点，即与安慰剂相比，其在改善PANSS总分方面没有统计学上的显著差异。受此消息影响，艾伯维当日股价下跌超12%，而与此同时，同处“精神分裂症”赛道的BMS股价也因Emraclidine的失败而上涨约12%。据悉，Emraclidine作为一种毒蕈碱M4受体的正变构调节剂，其机制上是通过选择性地调节M4受体来减少多巴胺信号，而不需要阻断D2受体，这就导致其相较现有治疗方式可能具有更低的副作用属性。而BMS的精分新药KarXT机制上不同于Emraclidine，是一种M1/M4型毒蕈碱撒双重受体激动剂，这或许也正是BMS股价上涨的原因之一。而通过上述内容，更令人深思的是，无论是艾伯维还是BMS，为何都对于小众的精神分裂症如此看重，精神分裂症在研新药领域，现在又是怎样的竞争格局？ >01< 不良反应显著， “精分”临床需求迫切所谓精神分裂症，是一种慢性、致残性精神疾病，终生患病率达0.7%，现阶段其病因与发病机制尚未完全阐明，且疾病发展过程中受生物、社会、心理等多种因素影响，其临床症状整体呈现复杂、严重、易复发特点，一项荟萃分析显示，相对于任何非精神分裂症对照组，精神分裂症患者的全因死亡率升高152%，严重威胁我国职业功能与社会功能。治疗方面，现阶段精神分裂症治疗主要分为药物治疗，电抽搐治疗，心理治疗等多种方式，而其中抗精神病药物治疗的主要目的为预防疾病复发，临床上常用的30余种抗精神病药物均能很有效降低疾病复发率，但同样，目前也无任何一款药物具有显著优势，药物间的选择差异主要体现在不良反应上。第一代抗精神病药物：不良反应主要为锥体外系不良反应，主要表现为运动障碍，如肌张力障碍、静坐不能、帕金森综合征等。第二代抗精神病药物：不良反应主要为导致体重增加等代谢相关不良反应，进而增加患者罹患心血管疾病和糖尿病等代谢性疾病的风险。另外，由于精神分裂症的长疾病周期特性，患者普遍需要终生服药，因此药物顺应性很达程度上也成为影响疾病整体复发率的关键因素（患者主动停药导致复发率上涨），因此，现阶段临床治疗共识上普遍认为，长效针剂相较口服抗精神病药在预防复发及再住院方面优势更为显著。综上所述，精神分裂症的临床需求迫切且清晰，新药研发既有市场动力，其思路也足够简单明了，即围绕减少不良反应与长效制剂方向进行，这也是为何众多制药企业争相入局的根本原因。 >02< 道阻且难 “精分”新药研发依旧火热实际上，纵然精神分裂症新药研发领域参与者众多，但其开发难度大，失败率高的特点仍贯彻全局，研发界一直期待能够在这一领域有新的突破。而随着全球新药界的目光越来越集中于该领域，精神分裂症新药在研领域也迎来了诸多有希望的进展。据药智数据显示，全球精神分裂症新药研究火热，截至目前已有372款新药在研，其中创新药318款，改良型新药54款，国内药企在精神分裂症改良性新药方面布局较重，新药涉及程度稍逊。数据来源：药智数据而更关键的是，在这300余款精分新药中，接近8成项目均处于非活跃状态（近两年无研究进展），其中不排除部分管线与艾伯维Emraclidine有着同样的命运，目前仅有58款新药研究进展相对顺利。数据来源：药智数据在这部分活跃“精分新药”领域，上文中提及的BMS“精分”新药KarXT已获批上市。临床阶段方面，则还有三菱制药的roluperidone，目前已处于注册申请阶段；丹麦灵北制药与恩华药业的Lu AF35700、SyneuRx的苯甲酸钠、Newron的依文酰胺、勃林格殷格翰的iclepertin、Sunovion与大冢制药的SEP-363856、Vanda的VHX-896、罗氏制药的bitopertin、Reviva的brilaroxazine等8款新药也已进入临床III期。数据来源：药智数据其中，勃林格殷格翰的lclepertin是所有管线中唯一一款具有中美双重突破性疗法认证的创新疗法，其作为一款新型甘氨酸转运蛋白1（Gly-T1）抑制剂，通过抑制Gly-T1，改善N-甲基-D-天冬氨酸（NMDA）受体的功能减退起到治疗作用，目前该产品正在开展针对精神分裂症的全球3期临床，中国同步参与其中。未来，随着越来越多精神分裂症新药的有效性得到认定，或许整个行业都将面临巨大的变化，这对于患者与整个社会都是值得庆幸的好事，也是企业重构该领域的大好机会。 >03< 结语纵观精神分裂症新药研发历史，开发难度大，失败率高的整体特点下，艾伯维很明显并非首例，也绝非最后一个，至少现在看来，8成非活跃管线中就有不少类似的例子。但在药物创新领域，失败本再常见不过的事，大众也切勿因其一次短期挫折就全盘否定制药企业在新药创新领域的成就。另外，就目前抗精神病药物在研格局来看，第三代抗精神病药物已然成为众多药企的必争之地，但可惜的是，其中甚少看到中国创新企业的身影，这一点或许后续会是一个较好的机会。声明：本内容仅用作医药行业信息传播，不代表药智网立场。对本文有异议或投诉，请联系maxuelian@yaozh.com。责任编辑 | 史蒂文阅读原文，是受欢迎的文章哦

2024-11-07

·GlobeNewswire-Health Care

Reviva to Present Positive Speech Latency Data for Brilaroxazine in Schizophrenia From the Phase 3 RECOVER Trial at the CNS Summit 2024

Nov. 06, 2024 -- Reviva Pharmaceuticals Holdings, Inc. (NASDAQ: RVPH) (“Reviva” or the “Company”), a late-stage pharmaceutical company developing therapies that seek to address unmet medical needs in the areas of central nervous system (CNS), inflammatory and cardiometabolic diseases, today announced that positive speech latency data for brilaroxazine in schizophrenia from the Phase 3 RECOVER trial will be presented as a poster presentation at the CNS Summit 2024, taking place November 10-13, in Boston, Massachusetts. Details for the poster presentation can be found below: Title: Enrichment Based on Speech Latency Enhances Treatment Effects in a Phase III Study of Brilaroxazine Poster Board: 10 Date and Time: Tuesday, November 12th from 5:00 - 7:00 PM ET Presenter: Dr. Jan Sedway, WCG Clinical Abstracts and additional details can be found at the CNS Summit 2024 website. Reviva is a late-stage biopharmaceutical company that discovers, develops, and seeks to commercialize next-generation therapeutics for diseases representing unmet medical needs and burdens to society, patients, and their families. Reviva’s current pipeline focuses on the central nervous system (CNS), inflammatory and cardiometabolic diseases. Reviva’s pipeline currently includes two drug candidates, brilaroxazine (RP5063) and RP1208. Both are new chemical entities discovered in-house. Reviva has been granted composition of matter patents for both brilaroxazine and RP1208 in the United States, Europe, and several other countries. The content above comes from the network. if any infringement, please contact us to modify.

上市批准

2024-10-31

·GlobeNewswire-Health Care

Reviva to Participate in the UBS Global Healthcare Conference

CUPERTINO, Calif., Oct. 31, 2024 (GLOBE NEWSWIRE) -- Reviva Pharmaceuticals Holdings, Inc. (NASDAQ: RVPH) (“Reviva” or the “Company”), a late-stage pharmaceutical company developing therapies that seek to address unmet medical needs in the areas of central nervous system (CNS), inflammatory and cardiometabolic diseases, today announced that Laxminarayan Bhat, Ph.D., Founder, President, and CEO of Reviva will participate in a fireside chat at the UBS Global Healthcare Conference, taking place November 11-14, 2024, in Rancho Palos Verdes, CA. UBS Global Healthcare Conference Format: Fireside chatDate: Thursday, November 14, 2024Time: 8:00 a.m. PTLocation: Rancho Palos Verdes, CAWebcast Link: Click Here About Reviva Reviva is a late-stage biopharmaceutical company that discovers, develops, and seeks to commercialize next-generation therapeutics for diseases representing unmet medical needs and burdens to society, patients, and their families. Reviva’s current pipeline focuses on the central nervous system (CNS), inflammatory and cardiometabolic diseases. Reviva’s pipeline currently includes two drug candidates, brilaroxazine (RP5063) and RP1208. Both are new chemical entities discovered in-house. Reviva has been granted composition of matter patents for both brilaroxazine and RP1208 in the United States, Europe, and several other countries. Corporate Contact:Reviva Pharmaceuticals Holdings, Inc.Laxminarayan Bhat, PhD www.revivapharma.com Investor Relations Contact:LifeSci Advisors, LLCBruce Macklebmackle@lifesciadvisors.com

100 项与 Brilaroxazine 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Brilaroxazine	-	DB09226

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
精神分裂症	临床3期	美国	Reviva Pharmaceuticals Holdings, Inc.	2022-01-24
急性精神分裂症	临床2期	美国	Reviva Pharmaceuticals Holdings, Inc.	2011-12-01
急性精神分裂症	临床2期	印度	Reviva Pharmaceuticals Holdings, Inc.	2011-12-01
急性精神分裂症	临床2期	马来西亚	Reviva Pharmaceuticals Holdings, Inc.	2011-12-01
急性精神分裂症	临床2期	摩尔多瓦	Reviva Pharmaceuticals Holdings, Inc.	2011-12-01
急性精神分裂症	临床2期	菲律宾	Reviva Pharmaceuticals Holdings, Inc.	2011-12-01
分裂情感性障碍	临床2期	美国	Reviva Pharmaceuticals Holdings, Inc.	2011-12-01
分裂情感性障碍	临床2期	印度	Reviva Pharmaceuticals Holdings, Inc.	2011-12-01
分裂情感性障碍	临床2期	马来西亚	Reviva Pharmaceuticals Holdings, Inc.	2011-12-01
分裂情感性障碍	临床2期	摩尔多瓦	Reviva Pharmaceuticals Holdings, Inc.	2011-12-01

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临床结果

适应症

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05184335 (RECOVER, Biospace) 人工标引	临床3期	精神分裂症	-	Brilaroxazine	鬱鑰蓋夢獵蓋窪願遞糧(蓋鏇築網糧網膚壓製範) = 鏇範繭窪鹹壓衊鑰齋餘鹽觸築繭蓋淵選糧鏇繭 (鏇範醖鬱鏇觸艱觸築願 ) 达到	积极	2023-10-30
NCT05184335 (RECOVER, Biospace) 人工标引	临床3期	精神分裂症	-	Placebo	鬱鑰蓋夢獵蓋窪願遞糧(蓋鏇築網糧網膚壓製範) = 願顧獵蓋壓鹽範顧製淵鹽觸築繭蓋淵選糧鏇繭 (鏇範醖鬱鏇觸艱觸築願 ) 达到	积极	2023-10-30
NCT01490086 (REFRESH, CTgov)	临床2期	急性精神分裂症 \| 分裂情感性障碍	234	placebo	繭選壓繭願製淵鏇網淵(積糧廠積鑰選願糧選觸) = 膚壓選觸選顧壓遞糧憲獵顧蓋簾繭餘淵鹹醖願 (艱網衊築獵膚願餘憲淵, 衊顧鬱襯衊鹹積壓艱鏇 ~ 鏇鬱餘積鬱觸淵構鑰鹹) 更多	-	2015-01-26