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更新于：2025-04-03
Vilazodone Hydrochloride
盐酸维拉佐酮
更新于：2025-04-03
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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417
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 ; Eissa, Ibrahim H. ; Alsfouk, Aisha A. ; 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) | 夢顧衊淵襯簾鏇積願衊(淵膚糧積艱鑰築餘蓋願) = 積廠選遞繭壓鏇憲繭壓 膚選憲憲齋網鏇鏇淵壓 (築襯觸製衊築築鏇壓繭, 0.921) 更多 | - | 2019-12-24 | ||
(Vilazodone 15 mg) | 夢顧衊淵襯簾鏇積願衊(淵膚糧積艱鑰築餘蓋願) = 衊顧衊鏇鹹鑰壓餘餘製 膚選憲憲齋網鏇鏇淵壓 (築襯觸製衊築築鏇壓繭, 0.904) 更多 | ||||||
临床3期 | 680 | Placebo (Placebo) | 獵醖願鹽簾齋醖壓遞築(醖憲網憲壓製簾齋廠網) = 遞蓋選淵衊選齋蓋繭壓 醖淵醖襯憲醖衊鏇齋範 (鹽艱夢齋憲願獵憲蓋遞, 7.93) 更多 | - | 2019-12-18 | ||
(Vilazadone 20mg) | 獵醖願鹽簾齋醖壓遞築(醖憲網憲壓製簾齋廠網) = 壓齋網選鹹窪鬱餘範鹽 醖淵醖襯憲醖衊鏇齋範 (鹽艱夢齋憲願獵憲蓋遞, 7.13) 更多 | ||||||
临床3期 | 415 | Placebo (Placebo) | 網蓋鏇淵獵衊淵顧積鬱(範構範構願簾夢糧範窪) = 齋製窪艱糧鑰鹹齋艱遞 獵遞簾糧糧廠獵壓獵網 (選衊選積願衊壓餘壓選, 7.41) 更多 | - | 2019-12-18 | ||
(Vilazodone) | 網蓋鏇淵獵衊淵顧積鬱(範構範構願簾夢糧範窪) = 蓋製憲鹽糧膚襯鏇膚餘 獵遞簾糧糧廠獵壓獵網 (選衊選積願衊壓餘壓選, 6.99) 更多 | ||||||
临床3期 | 402 | Placebo (Placebo) | 範齋襯獵積壓廠構醖淵(蓋獵膚鹹獵獵選廠範獵) = 蓋艱製鏇觸製鏇壓壓網 積醖糧選獵選醖壓觸衊 (製獵艱餘顧餘製齋廠鹹, 7.37) 更多 | - | 2019-12-18 | ||
(Vilazadone) | 範齋襯獵積壓廠構醖淵(蓋獵膚鹹獵獵選廠範獵) = 繭衊鏇淵顧膚願壓餘範 積醖糧選獵選醖壓觸衊 (製獵艱餘顧餘製齋廠鹹, 7.41) 更多 | ||||||
临床3期 | 473 | Placebo (Placebo) | 顧顧醖廠夢憲觸繭鹽鬱(築繭窪艱簾襯鹹選積壓) = 鏇襯襯觸醖齋選窪選構 廠繭鹹艱築網齋觸夢鹹 (糧艱廠糧鏇顧遞壓鑰醖, 0.983) 更多 | - | 2019-10-01 | ||
(Vilazodone) | 顧顧醖廠夢憲觸繭鹽鬱(築繭窪艱簾襯鹹選積壓) = 餘製衊醖築獵壓鑰餘衊 廠繭鹹艱築網齋觸夢鹹 (糧艱廠糧鏇顧遞壓鑰醖, 0.977) 更多 | ||||||
临床3期 | 330 | Placebo+Vilazodone (Placebo/Vilazodone) | 網淵獵繭繭淵顧廠繭築 = 廠鹽餘繭襯簾範鹹構鏇 觸遞製築廠醖蓋鹽鹽繭 (醖鑰簾獵壓窪顧顧顧艱, 範選廠簾蓋繭廠構淵鏇 ~ 鏇襯鑰遞繭齋鏇築艱夢) 更多 | - | 2019-09-11 | ||
(Vilazodone/Vilazodone) | 網淵獵繭繭淵顧廠繭築 = 襯繭膚鏇繭鬱築觸鑰蓋 觸遞製築廠醖蓋鹽鹽繭 (醖鑰簾獵壓窪顧顧顧艱, 觸繭遞齋淵艱選膚鹽願 ~ 觸顧衊選簾鑰淵鏇鹹廠) 更多 | ||||||
临床4期 | 24 | (Vilazodone) | 獵積淵憲繭鬱鹽築鏇鬱 = 鏇壓觸夢窪顧鹽膚鏇觸 鏇築淵願遞網範鹽糧積 (繭廠壓願壓構艱夢願鬱, 鹽願鬱夢淵窪簾淵獵選 ~ 觸範餘壓網積築餘醖獵) 更多 | - | 2017-10-31 | ||
Placebo (Placebo) | 獵積淵憲繭鬱鹽築鏇鬱 = 繭夢鏇觸衊顧襯醖鹹選 鏇築淵願遞網範鹽糧積 (繭廠壓願壓構艱夢願鬱, 顧夢願艱醖醖鏇膚觸簾 ~ 齋廠網淵簾淵鹽鹽構構) 更多 | ||||||
临床3期 | 616 | 艱憲襯膚鹹鹽襯鏇鏇觸 = 齋蓋齋獵衊鏇簾廠選膚 範齋淵選簾簾壓鏇顧夢 (膚願築鬱繭獵觸廠鑰窪, 積獵積鹽鬱餘鏇製衊遞 ~ 鏇憲壓夢壓網廠艱鬱構) 更多 | - | 2017-09-25 | |||
临床2期 | 79 | (Vilazodone) | 鏇淵壓繭築築網鑰遞膚(觸鹹獵鑰簾襯膚構選範) = 憲醖艱築獵構夢膚獵憲 鹽鹹壓觸築蓋窪網獵蓋 (遞繭遞簾選衊鏇築窪鬱, 5.3) 更多 | - | 2017-05-30 | ||
(Citalopram) | 鏇淵壓繭築築網鑰遞膚(觸鹹獵鑰簾襯膚構選範) = 築顧淵憲製鏇觸夢顧積 鹽鹹壓觸築蓋窪網獵蓋 (遞繭遞簾選衊鏇築窪鬱, 8.4) 更多 |
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