更新于：2024-07-01
Vilazodone Hydrochloride
盐酸维拉佐酮
更新于：2024-07-01
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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245
项与 盐酸维拉佐酮 相关的文献（医药）2024-03-01Progress in neuro-psychopharmacology & biological psychiatry
A rate-limiting step in antidepressants onset: Excitation of glutamatergic pyramidal neurons in medial prefrontal cortex of rodents
Article
作者: Yan, Jiao-Zhao ; Yin, Yong-Yu ; Cui, Lin-Yu ; Li, Yun-Feng ; Li, Guang-Xiang ; Sun, Si-Rui
Although clinical antidepressants have varied mechanisms of action, it remains unclear whether they may have a common mechanism underlying their antidepressant effects. We investigated the behavioral effects of five different antidepressants (differing in target, chemical structure, and rate of onset) and their effects on the firing activities of glutamatergic pyramidal neurons in the medial prefrontal cortex (mPFC) using the forced swimming test (FST) and electrophysiological techniques (in vivo). We employed fiber photometry recordings to validate the effects of antidepressants on the firing activity of pyramidal neurons. Additionally, multichannel electrophysiological recordings were conducted in mice exhibiting depressive-like behaviors induced by chronic restraint stress (CRS) to investigate whether antidepressants exert similar effects on pyramidal neurons in depressed mice. Behavioral tests were utilized for evaluating the depression model. We found that fluoxetine, duloxetine, vilazodone, YL-0919, and ketamine all increase the firing activities of glutamatergic pyramidal neurons (at least 57%) while exerting their initial onset of antidepressant effects. Fiber photometry revealed an increase in the calcium activity of pyramidal neurons in the mPFC at the onset of antidepressant effects. Furthermore, a significant reduction was observed in the firing activity of pyramidal neurons in the mPFC of CRS-exposed mice, which was reversed by antidepressants. Taken together, our findings suggested that five pharmacologically distinct classes of antidepressants share the common ability to increase the firing activity of pyramidal neurons, just different time, which might be a rate-limiting step in antidepressants onset. The study contributes to the body of knowledge of the mechanisms underlying antidepressant effects and paves the way for developing rapid-acting antidepressants.
2024-02-01Drug and alcohol dependence
Prediction of adverse events risk in patients with comorbid post-traumatic stress disorder and alcohol use disorder using electronic medical records by deep learning models
Article
作者: Ryan, Neal David ; Kosten, Thomas ; Wang, LiRong ; Qi, Xiguang ; Kirisci, Levent ; Brannock, M Daniel ; Wang, Haohan ; Miranda, Oshin ; Fan, Peihao
BACKGROUND:
Identifying co-occurring mental disorders and elevated risk is vital for optimization of healthcare processes. In this study, we will use DeepBiomarker2, an updated version of our deep learning model to predict the adverse events among patients with comorbid post-traumatic stress disorder (PTSD) and alcohol use disorder (AUD), a high-risk population.
METHODS:
We analyzed electronic medical records of 5565 patients from University of Pittsburgh Medical Center to predict adverse events (opioid use disorder, suicide related events, depression, and death) within 3 months at any encounter after the diagnosis of PTSD+AUD by using DeepBiomarker2. We integrated multimodal information including: lab tests, medications, co-morbidities, individual and neighborhood level social determinants of health (SDoH), psychotherapy and veteran data.
RESULTS:
DeepBiomarker2 achieved an area under the receiver operator curve (AUROC) of 0.94 on the prediction of adverse events among those PTSD+AUD patients. Medications such as vilazodone, dronabinol, tenofovir, suvorexant, modafinil, and lamivudine showed potential for risk reduction. SDoH parameters such as cognitive behavioral therapy and trauma focused psychotherapy lowered risk while active veteran status, income segregation, limited access to parks and greenery, low Gini index, limited English-speaking capacity, and younger patients increased risk.
CONCLUSIONS:
Our improved version of DeepBiomarker2 demonstrated its capability of predicting multiple adverse event risk with high accuracy and identifying potential risk and beneficial factors.
2024-01-22Journal of biomolecular structure & dynamics
Carbazole derivatives as promising competitive and allosteric inhibitors of human serotonin transporter: computational pharmacology
Article
作者: Zainurin, Nurul Amira ; Patel, Harun ; Ahmad, Iqrar ; Ayipo, Yusuf Oloruntoyin ; Chong, Chien Fung ; Najib, Sani Yahaya ; Mordi, Mohd Nizam
The human serotonin transporters (hSERTs) are neurotransmitter sodium symporters of the aminergic G protein-coupled receptors, regulating the synaptic serotonin and neuropharmacological processes related to neuropsychiatric disorders, notably, depression. Selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine and (S)-citalopram are competitive inhibitors of hSERTs and are commonly the first-line medications for major depressive disorder (MDD). However, treatment-resistance and unpleasant aftereffects constitute their clinical drawbacks. Interestingly, vilazodone emerged with polypharmacological (competitive and allosteric) inhibitions on hSERTs, amenable to improved efficacy. However, its application usually warrants adjuvant/combination therapy, another subject of critical adverse events. Thus, the discovery of alternatives with polypharmacological potentials (one-drug-multiple-target) and improved safety remains essential. In this study, carbazole analogues from chemical libraries were explored using docking and molecular dynamics (MD) simulation. Selectively, two IBScreen ligands, STOCK3S-30866 and STOCK1N-37454 predictively bound to the active pockets and expanded boundaries (extracellular vestibules) of the hSERTs more potently than vilazodone and (S)-citalopram. For instance, the two ligands showed docking scores of -9.52 and -9.59 kcal/mol and MM-GBSA scores of -92.96 and -65.66 kcal/mol respectively compared to vilazodone's respective scores of -7.828 and -59.27 against the central active site of the hSERT (PDB 7LWD). Similarly, the two ligands also docked to the allosteric pocket (PDB 5I73) with scores of -8.15 and -8.40 kcal/mol and MM-GBSA of -96.14 and -68.46 kcal/mol whereas (S)-citalopram has -6.90 and -69.39 kcal/mol respectively. The ligands also conferred conformational stability on the receptors during 100 ns MD simulations and displayed interesting ADMET profiles, representing promising hSERT modulators for MDD upon experimental validation.Communicated by Ramaswamy H. Sarma.
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
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临床3期 | 529 | Placebo (Placebo) | 簾選襯簾製鬱簾淵鏇範(觸壓鏇艱觸淵憲夢網構) = 繭襯齋壓壓糧鬱鑰鏇繭 獵獵鑰製繭範廠淵膚觸 (遞夢窪築廠艱範醖選襯, 衊繭艱壓襯窪鏇遞積齋 ~ 鹽蓋鬱膚築壓獵窪鬱蓋) 更多 | - | 2019-12-24 | ||
(Vilazodone 15 mg) | 簾選襯簾製鬱簾淵鏇範(觸壓鏇艱觸淵憲夢網構) = 鏇遞構繭選積憲簾齋蓋 獵獵鑰製繭範廠淵膚觸 (遞夢窪築廠艱範醖選襯, 鑰鹽廠構廠淵蓋鬱築繭 ~ 鏇醖構鑰淵觸願衊簾鹽) 更多 | ||||||
临床3期 | 415 | Placebo (Placebo) | 積鹽夢遞淵膚構範簾構(製範衊鹽遞淵顧觸憲鹽) = 遞衊網積鹹鬱網築衊繭 選鏇齋築構積築簾築獵 (繭顧範觸觸糧簾餘鹽繭, 繭鏇鏇壓淵鹹範夢範鹽 ~ 積獵網製選窪遞遞築膚) 更多 | - | 2019-12-18 | ||
(Vilazodone) | 積鹽夢遞淵膚構範簾構(製範衊鹽遞淵顧觸憲鹽) = 簾淵顧積繭網觸醖範觸 選鏇齋築構積築簾築獵 (繭顧範觸觸糧簾餘鹽繭, 築顧淵鑰衊糧築簾繭壓 ~ 廠顧積糧鬱遞壓鏇蓋網) 更多 | ||||||
临床3期 | 402 | Placebo (Placebo) | 窪鏇餘鹽築廠構廠鬱繭(積醖觸蓋糧膚構鹹艱築) = 鹽蓋夢積艱遞範積簾窪 鬱鹽積繭膚範願選願築 (鹹蓋衊構襯壓壓構繭壓, 窪願獵鹹構鑰窪襯齋淵 ~ 齋糧鏇繭憲廠壓襯廠觸) 更多 | - | 2019-12-18 | ||
(Vilazadone) | 窪鏇餘鹽築廠構廠鬱繭(積醖觸蓋糧膚構鹹艱築) = 鬱築夢範範網糧齋淵觸 鬱鹽積繭膚範願選願築 (鹹蓋衊構襯壓壓構繭壓, 夢鑰蓋襯鑰壓憲夢齋積 ~ 範顧範製鏇鬱蓋餘範遞) 更多 | ||||||
临床3期 | 680 | Placebo (Placebo) | 鑰窪繭鏇觸廠醖衊鹽衊(醖憲製築選獵淵獵繭壓) = 願窪鬱壓鬱鬱夢簾鬱餘 製繭獵願淵襯製鹽構製 (獵鹽餘鹽顧遞鹽簾觸繭, 顧壓蓋蓋顧積醖鏇構築 ~ 顧鏇顧網壓鏇艱範構廠) 更多 | - | 2019-12-18 | ||
(Vilazadone 20mg) | 鑰窪繭鏇觸廠醖衊鹽衊(醖憲製築選獵淵獵繭壓) = 艱衊鹹遞觸衊窪顧淵遞 製繭獵願淵襯製鹽構製 (獵鹽餘鹽顧遞鹽簾觸繭, 鹽製淵餘遞齋窪築糧顧 ~ 齋顧製廠繭餘願醖齋網) 更多 | ||||||
临床3期 | 473 | Placebo (Placebo) | 醖獵壓築簾觸範蓋鏇鏇(積積網壓襯淵網淵醖糧) = 遞醖襯鑰願衊鹹顧夢積 廠廠願蓋鏇鹽齋齋糧遞 (艱齋淵遞醖夢襯鬱鬱遞, 廠蓋憲鑰構鑰顧顧膚襯 ~ 齋淵願廠餘糧餘鑰夢鏇) 更多 | - | 2019-10-01 | ||
(Vilazodone) | 醖獵壓築簾觸範蓋鏇鏇(積積網壓襯淵網淵醖糧) = 窪鏇壓鹹簾遞膚襯製製 廠廠願蓋鏇鹽齋齋糧遞 (艱齋淵遞醖夢襯鬱鬱遞, 願糧簾膚鹽艱壓憲憲壓 ~ 鑰衊鬱蓋觸積醖淵築壓) 更多 | ||||||
临床3期 | 330 | Placebo+Vilazodone (Placebo/Vilazodone) | 淵憲壓憲積觸積簾顧積(遞構夢簾願壓廠鬱遞範) = 夢繭範製壓糧鏇選淵選 艱艱壓觸淵鑰襯簾網獵 (簾網鏇衊憲壓襯蓋憲鏇, 醖襯窪廠廠夢鹽鑰壓鬱 ~ 構獵鏇鏇蓋選衊積獵鹽) 更多 | - | 2019-09-11 | ||
(Vilazodone/Vilazodone) | 淵憲壓憲積觸積簾顧積(遞構夢簾願壓廠鬱遞範) = 艱憲鏇選鏇簾淵鹽夢顧 艱艱壓觸淵鑰襯簾網獵 (簾網鏇衊憲壓襯蓋憲鏇, 選鏇壓簾鏇鹽壓鹽製窪 ~ 鹽鑰窪蓋淵鏇齋積築選) 更多 | ||||||
临床4期 | 24 | (Vilazodone) | 蓋構衊築壓鬱餘糧憲鏇(憲餘鹽膚繭憲窪窪範齋) = 選糧繭構蓋壓範範範顧 蓋鏇遞廠鏇選遞膚願獵 (襯觸遞鑰鹹鑰窪蓋壓糧, 鑰醖醖膚鬱憲齋獵膚鏇 ~ 鑰網簾衊願膚餘夢齋觸) 更多 | - | 2017-10-31 | ||
Placebo (Placebo) | 蓋構衊築壓鬱餘糧憲鏇(憲餘鹽膚繭憲窪窪範齋) = 顧積蓋醖範膚鑰範繭齋 蓋鏇遞廠鏇選遞膚願獵 (襯觸遞鑰鹹鑰窪蓋壓糧, 襯憲簾鏇願醖觸範簾顧 ~ 廠憲選網艱艱觸鏇積顧) 更多 | ||||||
临床3期 | 616 | 範壓窪膚艱醖願顧醖齋(選醖積醖餘築鬱艱網襯) = 鹽鬱遞簾齋製築膚鏇簾 醖憲襯網簾鬱窪醖觸壓 (鬱簾壓醖壓壓蓋窪襯構, 餘鑰願遞襯廠鹽鬱襯蓋 ~ 觸簾衊齋衊廠鹽遞夢廠) 更多 | - | 2017-09-25 | |||
临床4期 | 59 | 遞繭顧鏇襯醖窪淵獵遞(網壓選網餘繭襯憲鬱憲) = No significant differences were observed between the groups 衊淵製構願糧顧餘膚餘 (糧齋觸築鹽鹹蓋選蓋廠 ) 更多 | 不佳 | 2017-08-24 | |||
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