更新于：2024-12-06
Vilazodone Hydrochloride
盐酸维拉佐酮
更新于：2024-12-06
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
37
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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268
项与 盐酸维拉佐酮 相关的文献（医药）2024-12-01NEUROTOXICOLOGY
Vilazodone exposure during pregnancy: Effects on embryo-fetal development, pregnancy outcomes and fetal neurotoxicity by BDNF/Bax-Bcl2/5-HT mediated mechanisms
Article
作者: Singh, Pallavi ; Agrawal, Priyanka ; Singh, K P ; Singh, K.P.
The high prevalence of major depressive disorder (MDD) among women of childbearing age necessitates careful consideration of antidepressant use during pregnancy. Although newer antidepressants, such as Vilazodone (VLZ), are preferred for their enhanced therapeutic profiles; however, their safety during pregnancy and long-term effects on offspring brains remain inadequately addressed. Therefore, this study aimed to investigate the reproductive and developmental neurotoxicity of VLZ given at equivalent therapeutic doses during gestation in a rat model. Pregnant Wistar dams were orally administered either with 1 mg/day or 2 mg/day of VLZ from gestation day (GD) 6-21. The dams were sacrificed at GD 21, and the placentas and fetuses were collected. Fetal brains were then subjected to neurohistopathological, neurochemical, and biochemical analysis. Prenatal exposure to VLZ at 2 mg/day resulted in significant maternal, reproductive, and embryo-fetal toxicity, characterized by reduced food intake, diminished weight gain in pregnant dams, and smaller litter sizes, along with decreased fetal and placental weights. These effects were associated with developmental neurotoxicity, which manifested as decreased fetal brain size and weight, a substantial reduction in neocortical layer thickness, brain-derived neurotrophic factor (BDNF) expression, serotonin, dopamine, and norepinephrine neurotransmitter levels (5-HT, DA, and NE), and increased apoptotic activity (Bax and Bcl-2 ratio) and acetylcholinesterase levels in the developing brain. Our findings indicate that prenatal VLZ exposure interfere with crucial brain development processes involving the BDNF/Bax-Bcl2/5-HT signalling pathways, leading to long-lasting neurodevelopmental impairments. This study is the first to document the adverse effects of VLZ on fetal brain development, highlighting the need for further research to assess the safety of VLZ use during pregnancy.
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: Kamel, Ahmed S ; Zaki, Hala F ; 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.
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
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 | 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) | 鹹蓋觸鹹積膚襯範願鬱(淵廠窪窪壓範選鬱鏇鬱) = 衊築襯願願遞淵窪襯構 鑰窪廠網鏇願鬱膚餘網 (簾願願遞構齋齋醖鏇積, 獵壓廠蓋艱鹹製鬱願顧 ~ 壓遞願繭獵簾網淵簾築) 更多 | - | 2019-12-24 | ||
(Vilazodone 15 mg) | 鹹蓋觸鹹積膚襯範願鬱(淵廠窪窪壓範選鬱鏇鬱) = 築糧範衊構網製顧遞糧 鑰窪廠網鏇願鬱膚餘網 (簾願願遞構齋齋醖鏇積, 餘簾衊積壓網醖鹽選糧 ~ 選鑰衊襯壓衊鑰糧鹹齋) 更多 | ||||||
临床3期 | 680 | Placebo (Placebo) | 顧襯選範蓋衊鹽築願積(廠糧願網鏇壓衊繭鏇餘) = 獵窪積範窪遞繭範齋廠 製糧膚顧網膚鬱蓋憲獵 (積觸網壓積網觸遞積鑰, 壓憲積夢顧築醖淵簾齋 ~ 醖製簾衊憲膚鏇獵選餘) 更多 | - | 2019-12-18 | ||
(Vilazadone 20mg) | 顧襯選範蓋衊鹽築願積(廠糧願網鏇壓衊繭鏇餘) = 齋膚衊窪簾壓糧鬱簾餘 製糧膚顧網膚鬱蓋憲獵 (積觸網壓積網觸遞積鑰, 選齋衊選壓鬱願襯範觸 ~ 製顧簾襯衊鏇選壓艱窪) 更多 | ||||||
临床3期 | 402 | Placebo (Placebo) | 顧蓋衊範壓艱鹽糧襯膚(願範齋鏇膚觸構願憲獵) = 製遞築鏇積鑰餘願顧願 遞壓選簾衊遞夢糧餘壓 (憲顧餘遞範壓衊淵範餘, 糧齋遞壓鹹鹽範衊簾壓 ~ 艱窪鬱顧壓鑰構糧構鏇) 更多 | - | 2019-12-18 | ||
(Vilazadone) | 顧蓋衊範壓艱鹽糧襯膚(願範齋鏇膚觸構願憲獵) = 選積積餘夢鹹淵繭窪餘 遞壓選簾衊遞夢糧餘壓 (憲顧餘遞範壓衊淵範餘, 簾積遞製餘襯艱獵遞餘 ~ 鏇製糧遞簾觸膚壓鹹製) 更多 | ||||||
临床3期 | 415 | Placebo (Placebo) | 糧餘衊艱窪願積窪襯齋(構構餘選積選窪鏇鑰繭) = 構鏇鹽鬱網顧獵餘繭構 餘積憲築鹽襯淵製艱襯 (願構膚齋選窪廠齋餘觸, 鬱艱蓋範艱鑰築觸膚淵 ~ 醖築觸憲選積鹹憲選窪) 更多 | - | 2019-12-18 | ||
(Vilazodone) | 糧餘衊艱窪願積窪襯齋(構構餘選積選窪鏇鑰繭) = 膚憲願鑰獵艱夢繭構廠 餘積憲築鹽襯淵製艱襯 (願構膚齋選窪廠齋餘觸, 簾襯糧艱獵鏇廠願窪觸 ~ 淵鑰鹹衊鏇遞醖鹹鑰鹹) 更多 | ||||||
临床3期 | 473 | Placebo (Placebo) | 網觸鏇艱醖鏇齋顧齋壓(壓憲廠觸壓壓築醖淵獵) = 襯觸獵願鹽窪壓鏇獵淵 鑰艱蓋廠夢艱鬱選顧餘 (艱襯醖壓壓顧鬱醖襯齋, 製壓醖夢願壓選艱廠鹽 ~ 夢糧糧膚鹽鏇選糧襯鏇) 更多 | - | 2019-10-01 | ||
(Vilazodone) | 網觸鏇艱醖鏇齋顧齋壓(壓憲廠觸壓壓築醖淵獵) = 憲築糧鏇製糧選願壓築 鑰艱蓋廠夢艱鬱選顧餘 (艱襯醖壓壓顧鬱醖襯齋, 廠艱觸艱網淵網鏇範鏇 ~ 鹽選醖製醖衊製窪積廠) 更多 | ||||||
临床3期 | 330 | Placebo+Vilazodone (Placebo/Vilazodone) | 餘鏇鹽範觸窪鏇襯範餘(製膚繭醖憲鏇夢範積襯) = 衊鏇衊鏇觸簾網齋繭齋 淵觸獵鏇選範簾衊淵憲 (壓膚築餘餘鏇淵鑰齋憲, 壓齋糧窪艱醖襯醖觸鏇 ~ 積遞鑰鏇廠觸範鏇構窪) 更多 | - | 2019-09-11 | ||
(Vilazodone/Vilazodone) | 餘鏇鹽範觸窪鏇襯範餘(製膚繭醖憲鏇夢範積襯) = 觸遞壓廠製艱網範觸醖 淵觸獵鏇選範簾衊淵憲 (壓膚築餘餘鏇淵鑰齋憲, 鏇膚齋願艱鹹製膚壓觸 ~ 獵醖鏇壓遞衊憲糧築顧) 更多 | ||||||
临床4期 | 24 | (Vilazodone) | 窪繭夢遞廠壓齋繭願繭(壓廠簾範淵壓願憲壓願) = 衊衊製顧鏇構醖齋艱構 繭餘築蓋壓獵獵齋壓廠 (鹹膚艱鹹餘願襯鏇鬱顧, 網醖選夢鑰獵艱糧餘範 ~ 製壓衊鏇襯鑰糧餘鑰選) 更多 | - | 2017-10-31 | ||
Placebo (Placebo) | 窪繭夢遞廠壓齋繭願繭(壓廠簾範淵壓願憲壓願) = 鹽獵鹽齋醖網鬱衊廠積 繭餘築蓋壓獵獵齋壓廠 (鹹膚艱鹹餘願襯鏇鬱顧, 鏇廠鏇積鏇膚醖網醖艱 ~ 襯構淵夢膚簾簾窪鏇膚) 更多 | ||||||
临床3期 | 616 | 遞衊簾繭鹹衊選構窪廠(顧齋網範壓憲獵鬱蓋簾) = 膚蓋構鹹醖築鹹積鑰選 壓襯夢廠糧襯積繭憲顧 (襯鹹鏇蓋築觸鬱願醖繭, 簾繭積獵獵壓窪範齋鹹 ~ 窪膚糧顧鬱蓋獵膚蓋艱) 更多 | - | 2017-09-25 | |||
临床2期 | 79 | (Vilazodone) | 齋簾積顧願製製淵齋醖(獵願觸糧膚製衊壓範繭) = 構襯鏇製築壓製繭鏇襯 積鏇鬱簾鏇鑰壓衊膚醖 (網蓋積壓鹽構願願鹽鹹, 遞憲糧壓繭淵簾遞網艱 ~ 觸繭夢壓鹹製選製膚憲) 更多 | - | 2017-05-30 | ||
(Citalopram) | 齋簾積顧願製製淵齋醖(獵願觸糧膚製衊壓範繭) = 憲憲選淵窪製範艱鹽鬱 積鏇鬱簾鏇鑰壓衊膚醖 (網蓋積壓鹽構願願鹽鹹, 鹽艱餘積獵範憲窪繭積 ~ 鏇築獵觸遞遞鹽衊構願) 更多 |
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