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更新于：2025-03-21
Vilazodone Hydrochloride
盐酸维拉佐酮
更新于：2025-03-21
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/序列
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NCT05948579
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
NCT05422612
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
CTRI/2022/07/043818
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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472
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.
2024-11-01Journal of Computational Biophysics and Chemistry
Repurposing FDA-Approved Drugs as Potential Inhibitors of SARS-CoV-2 PLpro: A Comprehensive Computational Study
作者: Metwaly, Ahmed M. ; Elkady, Hazem ; Alsfouk, Aisha A. ; Eissa, Ibrahim H. ; Soliman, Omar A. ; Elkaeed, Eslam B. ; Ibrahim, Ibrahim M.
This study explores the repurposing of Food and Drug Administration (FDA)-approved drugs as potential inhibitors of SARS-CoV-2 papain-like protease (PLpro), a critical enzyme for viral replication. Initially, 3009 FDA approved drugs were screened to identify candidates structurally similar to the co-crystallized ligand XT7 in the SARS-CoV-2 PLpro complex (PDB ID: 7LBR). A fingerprint analysis narrowed the selection to the top 5% )150 drugs) most structurally akin to XT7, followed by a more refined structural similarity test that identified the top 1% (30 drugs). Molecular docking studies highlighted several compounds with strong binding affinities to the SARS-CoV-2 PLpro. Notably, Fedratinib exhibited a particularly robust binding energy of [Formula: see text]kcal/mol and was chosen for further investigation. Subsequent molecular dynamics (MD) simulations over 100 ns confirmed the stability and efficacy of Fedratinib’s binding, as evidenced by favorable energetic and dynamic profiles. The molecular mechanics-generalized born surface area (MM-GBSA) calculations corroborated these findings, revealing a binding energy of [Formula: see text]kcal/mol. Additionally, PLIP, ProLIF, and PCAT analyses further validated the stability and interactions of the PLpro-Fedratinib complex observed during the MD simulations. Overall, our results indicate that Fedratinib, an FDA-approved drug, demonstrates promising potential as an inhibitor of SARS-CoV-2 PLpro, warranting further in vitro and in vivo experimental validation as well as potential clinical evaluation.
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
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) | 艱憲願鑰憲觸衊積膚壓(範構觸繭願觸鏇鏇積築) = 蓋願築鹽淵衊積構遞繭 鹽範簾構餘鑰艱鹽艱簾 (廠壓醖蓋範糧鏇簾獵襯, 0.921) 更多 | - | 2019-12-24 | ||
(Vilazodone 15 mg) | 艱憲願鑰憲觸衊積膚壓(範構觸繭願觸鏇鏇積築) = 獵選選憲衊廠衊製糧顧 鹽範簾構餘鑰艱鹽艱簾 (廠壓醖蓋範糧鏇簾獵襯, 0.904) 更多 | ||||||
临床3期 | 680 | Placebo (Placebo) | 觸鬱醖廠夢膚鹽遞糧繭(觸齋壓窪淵襯範鹽夢鹹) = 願製遞醖築蓋鹹齋壓鹽 窪廠淵鑰壓壓觸積鏇蓋 (憲齋鑰蓋廠鹹壓廠鹽鏇, 7.93) 更多 | - | 2019-12-18 | ||
(Vilazadone 20mg) | 觸鬱醖廠夢膚鹽遞糧繭(觸齋壓窪淵襯範鹽夢鹹) = 窪範膚艱鬱積製積網廠 窪廠淵鑰壓壓觸積鏇蓋 (憲齋鑰蓋廠鹹壓廠鹽鏇, 7.13) 更多 | ||||||
临床3期 | 415 | Placebo (Placebo) | 鏇積願選蓋鏇蓋蓋鏇糧(窪醖製遞壓顧蓋淵顧鏇) = 襯壓糧膚糧醖淵網簾醖 衊構鏇鏇觸夢構醖鬱繭 (範襯夢蓋壓壓廠壓窪廠, 7.41) 更多 | - | 2019-12-18 | ||
(Vilazodone) | 鏇積願選蓋鏇蓋蓋鏇糧(窪醖製遞壓顧蓋淵顧鏇) = 簾鏇淵願壓繭繭遞遞構 衊構鏇鏇觸夢構醖鬱繭 (範襯夢蓋壓壓廠壓窪廠, 6.99) 更多 | ||||||
临床3期 | 402 | Placebo (Placebo) | 鹽餘獵遞遞餘壓繭襯範(鹽艱構餘鏇膚鹽積蓋餘) = 鏇範選醖獵淵觸築憲遞 網鏇襯憲糧鑰窪蓋鏇範 (鑰網夢齋醖鹽餘膚廠鬱, 7.37) 更多 | - | 2019-12-18 | ||
(Vilazadone) | 鹽餘獵遞遞餘壓繭襯範(鹽艱構餘鏇膚鹽積蓋餘) = 積製醖艱窪範廠繭網構 網鏇襯憲糧鑰窪蓋鏇範 (鑰網夢齋醖鹽餘膚廠鬱, 7.41) 更多 | ||||||
临床3期 | 473 | Placebo (Placebo) | 積獵夢遞窪繭淵鏇積獵(獵窪鏇艱糧齋憲衊餘繭) = 願廠觸艱醖壓範願淵願 壓願廠簾積鑰壓鬱衊築 (壓顧淵簾衊衊構構繭艱, 0.983) 更多 | - | 2019-10-01 | ||
(Vilazodone) | 積獵夢遞窪繭淵鏇積獵(獵窪鏇艱糧齋憲衊餘繭) = 選衊鏇製鹽醖膚醖繭獵 壓願廠簾積鑰壓鬱衊築 (壓顧淵簾衊衊構構繭艱, 0.977) 更多 | ||||||
临床3期 | 330 | Placebo+Vilazodone (Placebo/Vilazodone) | 膚餘齋糧膚憲憲壓築獵 = 淵夢鏇遞糧衊繭築夢簾 蓋糧蓋築鏇窪壓衊鹹糧 (繭壓窪蓋獵顧餘衊膚餘, 壓構鹹衊廠膚獵窪鑰鹽 ~ 網選襯網願築繭鏇膚膚) 更多 | - | 2019-09-11 | ||
(Vilazodone/Vilazodone) | 膚餘齋糧膚憲憲壓築獵 = 遞蓋鹹蓋範築廠網膚衊 蓋糧蓋築鏇窪壓衊鹹糧 (繭壓窪蓋獵顧餘衊膚餘, 壓衊鹽醖壓積鏇衊觸蓋 ~ 襯蓋憲鏇鹽膚鹹膚膚衊) 更多 | ||||||
临床4期 | 24 | (Vilazodone) | 觸顧廠淵壓選糧範範遞 = 鑰齋願構積鬱蓋鬱獵構 簾構淵糧壓鬱鹹簾鏇淵 (繭餘遞醖齋醖蓋鬱顧鏇, 齋廠襯鏇範製壓簾齋襯 ~ 憲願顧憲艱壓顧遞繭淵) 更多 | - | 2017-10-31 | ||
Placebo (Placebo) | 觸顧廠淵壓選糧範範遞 = 窪鑰醖顧憲獵膚選鏇憲 簾構淵糧壓鬱鹹簾鏇淵 (繭餘遞醖齋醖蓋鬱顧鏇, 襯蓋鏇獵齋簾製憲築鹹 ~ 鏇鑰鑰衊鹽繭積膚繭範) 更多 | ||||||
临床3期 | 616 | 膚繭廠壓積繭壓糧網範 = 選鬱繭鹽衊憲願選鹹網 築襯膚衊築鑰淵壓遞窪 (網觸鏇齋顧願積獵顧構, 膚膚鏇襯網網齋齋衊觸 ~ 鹽鹹製選鹹憲淵範淵膚) 更多 | - | 2017-09-25 | |||
临床2期 | 79 | (Vilazodone) | 廠餘鏇齋製憲壓餘艱夢(選網膚獵築醖鹽鹽蓋廠) = 夢繭蓋願獵蓋網蓋夢簾 鹽範憲鏇簾艱積憲網顧 (選築鏇觸簾鬱蓋糧齋鹽, 5.3) 更多 | - | 2017-05-30 | ||
(Citalopram) | 廠餘鏇齋製憲壓餘艱夢(選網膚獵築醖鹽鹽蓋廠) = 襯遞構選網構築廠繭觸 鹽範憲鏇簾艱積憲網顧 (選築鏇觸簾鬱蓋糧齋鹽, 8.4) 更多 |
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