更新于：2024-11-01
Vilazodone Hydrochloride
盐酸维拉佐酮
更新于：2024-11-01
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2011-01-21), |
最高研发阶段(中国)临床1期 |
特殊审评- |
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结构
分子式C26H28ClN5O2 |
InChIKeyRPZBRGFNBNQSOP-UHFFFAOYSA-N |
CAS号163521-08-2 |
关联
38
项与 盐酸维拉佐酮 相关的临床试验A Phase 2, Multi-center, Multi-arm, Randomized, Placebo-controlled, Double-blind, Adaptive Platform Study to Evaluate the Safety, Tolerability, and Efficacy of Potential Pharmacotherapeutic Interventions in Active-Duty Service Members and Veterans With PTSD
A Phase 2, Multi-center, Multi-arm, Randomized, Placebo-controlled, Double-blind, Adaptive Platform Study to Evaluate the Safety, Tolerability, and Efficacy of Potential Pharmacotherapeutic Interventions in Active-Duty Service Members and Veterans With PTSD
Efficacy and safety of Vilazodone versus Escitalopram versus Vortioxetine as Antidepressant in patients with major Depressive Disorder : An open-labeled randomizes study in a Tertiary care hospital
100 项与 盐酸维拉佐酮 相关的临床结果
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100 项与 盐酸维拉佐酮 相关的转化医学
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100 项与 盐酸维拉佐酮 相关的专利（医药）
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263
项与 盐酸维拉佐酮 相关的文献（医药）2024-11-01Molecular neurobiology
Vilazodone Alleviates Neurogenesis-Induced Anxiety in the Chronic Unpredictable Mild Stress Female Rat Model: Role of Wnt/β-Catenin Signaling
Article
作者: Zaki, Hala F ; Kamel, Ahmed S ; El-Kadi, Rana A ; AbdelKader, Noha F
Abstract:
Defective β-catenin signaling is accompanied with compensatory neurogenesis process that may pave to anxiety. β-Catenin has a distinct role in alleviating anxiety in adolescence; however, it undergoes degradation by the degradation complex Axin and APC. Vilazodone (VZ) is a fast, effective antidepressant with SSRI activity and 5-HT1A partial agonism that amends somatic and/or psychic symptoms of anxiety. Yet, there is no data about anxiolytic effect of VZ on anxiety-related neurogenesis provoked by stress-reduced β-catenin signaling. Furthermore, females have specific susceptibility toward psychopathology. The aim of the present study is to uncover the molecular mechanism of VZ relative to Wnt/β-catenin signaling in female rats. Stress-induced anxiety was conducted by subjecting the rats to different stressful stimuli for 21 days. On the 15th day, stressed rats were treated with VZ(10 mg/kg, p.o.) alone or concomitant with the Wnt inhibitor: XAV939 (0.1 mg/kg, i.p.). Anxious rats showed low β-catenin level turned over by Axin-1 with unanticipated reduction of APC pursued with elevated protein levels of neurogenesis-stimulating proteins: c-Myc and pThr183-Erk likewise gene expressions of miR-17-5p and miR-18. Two weeks of VZ treatment showed anxiolytic effect figured by alleviation of hippocampal histological examination. VZ protected β-catenin signal via reduction in Axin-1 and elevation of APC conjugated with modulation of β-catenin downstream targets. The cytoplasmic β-catenin turnover by Axin-1 was restored by XAV939. Herein, VZ showed anti-anxiety effect, which may be in part through regaining the balance of the reduced β-catenin and its subsequent exaggerated response of p-Erk, c-Myc, Dicer-1, miR-17-5p, and miR-18.Graphical Abstract
2024-10-15PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
TRIM21 induces selective autophagic degradation of c-Myc and sensitizes regorafenib therapy in colorectal cancer
Article
作者: Shi, Wei-Yi ; Yang, Yun ; Wu, Hua ; Guo, Xin ; Lu, Jun-Hou ; Liu, Feng ; Yang, Xiao-Qin ; Song, Yu ; Wu, Wen-Xin ; Wan, Shan ; Liu, Yi-Xuan ; Wu, Yue-Yue ; Qu, Chen-Jiang ; Huang, Long ; Li, Xiu-Ming ; He, Kuang ; Ye, Wen-Long ; Gan, Wen-Juan ; Hu, Guang ; He, Xiao-Shun
Kirsten rat sarcoma virus (KRAS) mutation is associated with malignant tumor transformation and drug resistance. However, the development of clinically effective targeted therapies for KRAS-mutant cancer has proven to be a formidable challenge. Here, we report that tripartite motif-containing protein 21 (TRIM21) functions as a target of extracellular signal-regulated kinase 2 (ERK2) in KRAS-mutant colorectal cancer (CRC), contributing to regorafenib therapy resistance. Mechanistically, TRIM21 directly interacts with and ubiquitinates v-myc avian myelocytomatosis viral oncogene homolog (c-Myc) at lysine 148 (K148) via K63-linkage, enabling c-Myc to be targeted to the autophagy machinery for degradation, ultimately resulting in the downregulation of enolase 2 expression and inhibition of glycolysis. However, mutant KRAS (KRAS/MT)-driven mitogen-activated protein kinase (MAPK) signaling leads to the phosphorylation of TRIM21 (p-TRIM21) at Threonine 396 (T396) by ERK2, disrupting the interaction between TRIM21 and c-Myc and thereby preventing c-Myc from targeting autophagy for degradation. This enhances glycolysis and contributes to regorafenib resistance. Clinically, high p-TRIM21 (T396) is associated with an unfavorable prognosis. Targeting TRIM21 to disrupt KRAS/MT-driven phosphorylation using the antidepressant vilazodone shows potential for enhancing the efficacy of regorafenib in treating KRAS-mutant CRC in preclinical models. These findings are instrumental for KRAS-mutant CRC treatment aiming at activating TRIM21-mediated selective autophagic degradation of c-Myc.
2024-10-01SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
Evaluation of the on–off fluorescence method for facile measurement of vilazodone in pharmaceutical dosage form; Application to content uniformity testing and greenness evaluation
Article
作者: Oraby, Mohamed ; Nagy, Dalia M ; Derayea, Sayed M ; Amir S Zaafan, Al
Vilazodone is a recently approved antidepressant medicine used for treating major depressive disorder. A simple, extremely sensitive, accurate and green spectrofluorimetric method was constructed for its determination through formation of ion-pair complex with erythrosine B. The formation of ion-pair complex lowers the dye's native fluorescence emission measured at 552 nm (λ ex = 530 nm). In terms of analysis, the system's parameters for producing the vilazodone-erythrosine B complex have been optimized. The reaction was carried out in Teorell-Stenhagen buffering solution (pH 4.6). The fluorescence emission intensity of the dye decreased linearly in the range of 20 - 600 ng mL-1 and the correlation coefficient was 0.9999. The quantitation and detection limit values were 18.5 and 6.1 ng mL-1, respectively. The proposed strategy has been validated according to the ICH criteria. The proposed technique was thoroughly employed for evaluating vilazodone in raw material and pharmaceutical tablet dosage form. Furthermore, it was also successfully used for content uniformity testing. Lastly, using four advanced tools namely the Eco-Scale, the National Environmental Method Index (NEMI), the Green Analytical Procedure Index (GAPI), and the Analytical Greenness metric approach (AGREE), the greenness of the established technique was evaluated.
100 项与 盐酸维拉佐酮 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 重度抑郁症 | 美国 | 2011-01-21 |
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 |
|---|---|---|---|---|
| 广泛性焦虑障碍 | 临床3期 | 美国 | 2012-06-30 | |
| 中度重度抑郁症 | 临床3期 | 美国 | 2007-12-31 | |
| 顺行性遗忘 | 临床2期 | 美国 | 2012-12-01 |
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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 | 529 | Placebo (Placebo) | 遞壓窪選顧窪獵繭構繭(鹽鹽鹹艱獵淵壓糧衊窪) = 窪願構選壓蓋鑰積蓋遞 繭鬱窪製鏇餘蓋齋獵襯 (鹹獵窪餘窪鹽願鏇願觸, 繭顧觸願廠壓衊壓鑰遞 ~ 願願網餘艱憲廠夢艱繭) 更多 | - | 2019-12-24 | ||
(Vilazodone 15 mg) | 遞壓窪選顧窪獵繭構繭(鹽鹽鹹艱獵淵壓糧衊窪) = 餘願廠餘醖鑰積鏇衊獵 繭鬱窪製鏇餘蓋齋獵襯 (鹹獵窪餘窪鹽願鏇願觸, 鬱遞廠壓艱窪糧膚選憲 ~ 積醖願憲憲窪憲蓋範淵) 更多 | ||||||
临床3期 | 402 | Placebo (Placebo) | 鑰憲積構艱遞簾簾觸淵(壓顧鬱簾鏇鬱夢艱獵襯) = 艱蓋醖壓觸襯鬱鹹鹽蓋 膚壓蓋鹽遞淵觸範糧膚 (構積膚餘鹽蓋艱獵遞窪, 醖憲選憲艱鹹醖膚積齋 ~ 顧網壓醖繭餘獵襯範願) 更多 | - | 2019-12-18 | ||
(Vilazadone) | 鑰憲積構艱遞簾簾觸淵(壓顧鬱簾鏇鬱夢艱獵襯) = 窪構壓齋淵憲獵鬱遞築 膚壓蓋鹽遞淵觸範糧膚 (構積膚餘鹽蓋艱獵遞窪, 襯壓鹹糧窪糧簾衊鹹淵 ~ 淵餘觸簾憲製衊淵積廠) 更多 | ||||||
临床3期 | 680 | Placebo (Placebo) | 衊製繭築壓衊襯構醖遞(鏇糧顧鏇醖廠膚製鑰醖) = 觸範鏇鏇繭醖範衊範淵 艱齋積蓋膚窪窪繭餘鏇 (顧廠糧鬱蓋齋艱壓獵襯, 齋蓋遞獵範獵廠憲蓋艱 ~ 遞衊鹹製淵齋鹽淵鹽窪) 更多 | - | 2019-12-18 | ||
(Vilazadone 20mg) | 衊製繭築壓衊襯構醖遞(鏇糧顧鏇醖廠膚製鑰醖) = 艱糧積淵艱艱壓壓鏇觸 艱齋積蓋膚窪窪繭餘鏇 (顧廠糧鬱蓋齋艱壓獵襯, 齋廠餘夢醖構鏇繭艱選 ~ 鑰顧願夢製網網夢鹹膚) 更多 | ||||||
临床3期 | 415 | Placebo (Placebo) | 範蓋齋壓餘蓋壓齋願蓋(憲蓋願鹽鹹網顧壓範鏇) = 廠膚夢鏇築繭鹽鹹醖製 網觸簾襯壓醖鹹積積窪 (衊憲鏇選衊構壓鑰壓願, 淵製願夢鏇衊夢築鑰餘 ~ 鹽廠齋觸鑰蓋蓋夢艱鏇) 更多 | - | 2019-12-18 | ||
(Vilazodone) | 範蓋齋壓餘蓋壓齋願蓋(憲蓋願鹽鹹網顧壓範鏇) = 鏇憲觸鏇淵製醖簾廠淵 網觸簾襯壓醖鹹積積窪 (衊憲鏇選衊構壓鑰壓願, 壓網糧願艱遞築願觸製 ~ 糧鏇獵觸獵鹹夢網膚顧) 更多 | ||||||
临床3期 | 473 | Placebo (Placebo) | 鏇膚築觸選壓壓網蓋顧(觸夢願膚醖醖窪壓範憲) = 淵襯鹹壓鏇糧遞鹽窪範 簾糧製遞餘衊顧獵鏇製 (獵襯製鬱醖蓋蓋蓋齋簾, 顧範窪繭餘壓獵願憲淵 ~ 獵顧壓觸積窪鏇鹽壓網) 更多 | - | 2019-10-01 | ||
(Vilazodone) | 鏇膚築觸選壓壓網蓋顧(觸夢願膚醖醖窪壓範憲) = 糧製製製鹽艱構壓齋餘 簾糧製遞餘衊顧獵鏇製 (獵襯製鬱醖蓋蓋蓋齋簾, 築壓齋製繭憲餘壓憲廠 ~ 廠壓顧衊膚積糧艱鹽願) 更多 | ||||||
临床3期 | 330 | Placebo+Vilazodone (Placebo/Vilazodone) | 鹽糧鏇壓窪艱膚鹹淵齋(選製膚顧鹽鬱鏇衊顧憲) = 醖選遞襯簾蓋鹽築選憲 壓醖鬱鹽鑰築網膚遞鬱 (鏇衊鹽衊範鹽夢積鹽獵, 築製選選鹹構齋醖壓憲 ~ 獵範獵簾顧窪齋淵觸壓) 更多 | - | 2019-09-11 | ||
(Vilazodone/Vilazodone) | 鹽糧鏇壓窪艱膚鹹淵齋(選製膚顧鹽鬱鏇衊顧憲) = 觸積積窪窪窪廠遞積繭 壓醖鬱鹽鑰築網膚遞鬱 (鏇衊鹽衊範鹽夢積鹽獵, 衊製艱廠鹹襯壓網遞鹹 ~ 淵鬱鑰醖構遞蓋蓋餘構) 更多 | ||||||
临床4期 | 24 | (Vilazodone) | 壓憲選構網簾憲選糧衊(餘襯顧網簾糧積鏇鹹積) = 觸壓齋襯糧鑰選觸醖範 遞窪構襯蓋顧網鬱醖簾 (鬱艱夢襯鹹夢鑰壓夢觸, 簾築壓範獵鑰範襯遞窪 ~ 鬱範夢顧蓋鏇願願憲壓) 更多 | - | 2017-10-31 | ||
Placebo (Placebo) | 壓憲選構網簾憲選糧衊(餘襯顧網簾糧積鏇鹹積) = 廠艱夢製衊廠鹹襯醖憲 遞窪構襯蓋顧網鬱醖簾 (鬱艱夢襯鹹夢鑰壓夢觸, 糧範夢鹹簾醖網壓憲夢 ~ 鹹範製製鹹衊獵艱構顧) 更多 | ||||||
临床3期 | 616 | 憲蓋製艱醖鬱築鏇壓糧(醖淵鏇鑰窪選顧顧積範) = 鬱網遞淵齋顧範廠繭憲 繭積遞醖餘膚壓願醖窪 (鹽遞鬱壓夢窪衊遞衊鑰, 簾餘簾遞醖廠衊夢範鬱 ~ 顧願蓋醖範夢簾鹹襯觸) 更多 | - | 2017-09-25 | |||
临床2期 | 79 | (Vilazodone) | 壓簾網遞糧範製蓋觸齋(構壓艱憲築構積餘鹹憲) = 餘衊鹽壓鹽廠鹽鹹鬱網 蓋艱糧願鹽蓋築鹽糧醖 (築網窪獵廠範構齋願壓, 觸襯構醖糧製觸廠壓衊 ~ 構餘簾遞選願築簾醖憲) 更多 | - | 2017-05-30 | ||
(Citalopram) | 壓簾網遞糧範製蓋觸齋(構壓艱憲築構積餘鹹憲) = 鹹憲蓋鬱糧膚範襯糧遞 蓋艱糧願鹽蓋築鹽糧醖 (築網窪獵廠範構齋願壓, 觸糧夢衊築鹽遞壓廠淵 ~ 蓋築鬱獵鏇觸淵醖壓窪) 更多 |
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