更新于：2024-09-13
Levomilnacipran Hydrochloride
盐酸左旋体米那普仑
更新于：2024-09-13
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2013-07-25), |
最高研发阶段(中国)临床申请批准 |
特殊审评- |
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结构
分子式C15H23ClN2O |
InChIKeyXNCDYJFPRPDERF-NQQJLSKUSA-N |
CAS号175131-60-9 |
关联
25
项与 盐酸左旋体米那普仑 相关的临床试验盐酸左米那普仑缓释胶囊人体生物等效性试验预试验
A Double-blind, Placebo- and Active-controlled Evaluation of the Safety and Efficacy of Levomilnacipran ER in Pediatric Patients 7-17 Years With Major Depressive Disorder
Effectiveness of the Norepinephrine and Serotonin Reuptake Inhibitor Levomilnacipran in Healthy Males
100 项与 盐酸左旋体米那普仑 相关的临床结果
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100 项与 盐酸左旋体米那普仑 相关的转化医学
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100 项与 盐酸左旋体米那普仑 相关的专利（医药）
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93
项与 盐酸左旋体米那普仑 相关的文献（医药）2024-07-01Molecular neurobiology
Levomilnacipran Improves Lipopolysaccharide-Induced Dysregulation of Synaptic Plasticity and Depression-Like Behaviors via Activating BDNF/TrkB Mediated PI3K/Akt/mTOR Signaling Pathway
Article
作者: Yu, Shuyan ; Wu, Yuhan ; Feng, Yabo ; Wang, Changmin ; Li, Shuhan ; Li, Ye ; Zhu, Zhanpeng ; Mao, Xueqin ; Lan, Tian
Depression is a common psychological disease with high morbidity and mortality. Recently, the involvement of synaptic plasticity in the pathogenesis of depression has shed light on the direction of developing novel antidepressants. Levomilnacipran is a newly approved medication for the treatment of adult major depressive disorder. However, the detailed mechanisms underlying its antidepressant-like effects have yet to be illuminated. In this study, we aimed to investigate the role of levomilnacipran in regulating synaptic plasticity and explore the possible molecular mechanisms of its antidepressant effects using a rat model of depression induced by lipopolysaccharide (LPS). The results demonstrated that levomilnacipran (30 mg/kg, i.p.) significantly ameliorated depression-like behaviors in rats, alleviated the dysregulation of synaptic plasticity, and suppressed neuroinflammation within hippocampus induced by LPS-treatment. Levomilnacipran increased the expression of postsynaptic dense 95 (PSD-95) and synaptophysin (Syn) and reversed the imbalance between pro- and anti-inflammatory cytokines within hippocampus of depressed rats. Additionally, levomilnacipran elevated expression level of brain-derived neurotrophic factor (BDNF), accompanied by increased tyrosine kinase B (TrkB), phosphorylated phosphatidylinositol 3-kinase (PI3K), phosphorylated protein kinase B (p-Akt), and phosphorylated mammalian target of rapamycin (p-mTOR). Taken together, these results suggest that levomilnacipran may exert antidepressant effects via upregulating BDNF/TrkB mediated PI3K/Akt/mTOR signaling pathway to improve synaptic plasticity. These findings reveal potential mechanisms for the antidepressant effects of levomilnacipran and offer new insights into the treatments for depression.
2023-09-01International immunopharmacology
Levomilnacipran ameliorates lipopolysaccharide-induced depression-like behaviors and suppressed the TLR4/Ras signaling pathway
Article
作者: Li, Shuhan ; Yu, Shu Yan ; Wang, Changmin ; Jian, Wencheng ; Wu, Yuhan ; Li, Ye ; Zhu, Zhanpeng ; Lan, Tian
Levomilnacipran, a serotonin and norepinephrine reuptake inhibitor, has been reported to have anti-depressive effects. However, the detailed mechanisms underlying these effects are still unclear. This study aimed to investigate the antidepressant mechanisms of levomilnacipran to discover new perspectives on the treatment of depression in male rats. Intraperitoneal injection of lipopolysaccharide (LPS) was used to induce depressive behaviors in rats. Activation of microglia and apoptosis of neurons verified by immunofluorescence. Inflammatory related proteins and neurotrophic related proteins were verified by immunoblotting. The mRNA expression of apoptosis markers was verified by real-time quantitative PCR. Finally, electron microscopy analysis was used to observe the ultrastructural pathology of neuron. Here, we found that the anti-depression and anti-anxiety effects of levomilnacipran in the LPS-induced rat model of depression was resulted from the suppression of neuroinflammation and neuronal apoptosis within prefrontal cortex of rats. Furthermore, we found that levomilnacipran could decrease the number of microglia and suppress its activation in prefrontal cortex of rats. This effect may be mediated by suppressing the TLR4/NF-κB and Ras/p38 signaling pathways. In addition, levomilnacipran plays a neuroprotective role by increasing the expression of neurotrophic factors. Taken together, these results suggest that levomilnacipran exerts antidepressant effects by attenuating neuroinflammation to inhibit the damage in central nervous system and plays a neuroprotective role to improve depressive behaviors. These findings suggest that suppression of neuroinflammation in prefrontal cortex could ameliorate depressive behavioral disorder of rats induced by LPS, which provided a new perspective for the treatment of depression.
2023-07-01Clinical pharmacology and therapeutics
Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2D6, CYP2C19, CYP2B6, SLC6A4, and HTR2A Genotypes and Serotonin Reuptake Inhibitor Antidepressants
Review
作者: Singh, Ajeet B ; Mueller, Daniel J ; Gaedigk, Andrea ; Scott, Stuart A ; Strawn, Jeffrey R ; Hicks, J Kevin ; Ramsey, Laura B ; Stevenson, James M ; Bishop, Jeffrey R ; Bell, Gillian C ; Tsermpini, Evangelia Eirini ; Caudle, Kelly E ; Sangkuhl, Katrin ; Bousman, Chad A ; Leeder, J Steven ; Klein, Teri E ; Ruaño, Gualberto ; Brown, Jacob T
Serotonin reuptake inhibitor antidepressants, including selective serotonin reuptake inhibitors (SSRIs; i.e., citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline), serotonin and norepinephrine reuptake inhibitors (i.e., desvenlafaxine, duloxetine, levomilnacipran, milnacipran, and venlafaxine), and serotonin modulators with SSRI‐like properties (i.e., vilazodone and vortioxetine) are primary pharmacologic treatments for major depressive and anxiety disorders. Genetic variation in CYP2D6, CYP2C19, and CYP2B6 influences the metabolism of many of these antidepressants, which may potentially affect dosing, efficacy, and tolerability. In addition, the pharmacodynamic genes SLC6A4 (serotonin transporter) and HTR2A (serotonin‐2A receptor) have been examined in relation to efficacy and side effect profiles of these drugs. This guideline updates and expands the 2015 Clinical Pharmacogenetics Implementation Consortium (CPIC) guideline for CYP2D6 and CYP2C19 genotypes and SSRI dosing and summarizes the impact of CYP2D6, CYP2C19, CYP2B6, SLC6A4, and HTR2A genotypes on antidepressant dosing, efficacy, and tolerability. We provide recommendations for using CYP2D6, CYP2C19, and CYP2B6 genotype results to help inform prescribing these antidepressants and describe the existing data for SLC6A4 and HTR2A, which do not support their clinical use in antidepressant prescribing.
100 项与 盐酸左旋体米那普仑 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 | 2013-07-25 |
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 |
|---|---|---|---|---|
| 中度重度抑郁症 | 临床3期 | 美国 | 2017-01-23 | |
| 缺血性卒中 | 临床3期 | 比利时 | 2012-07-01 | |
| 缺血性卒中 | 临床3期 | 捷克 | 2012-07-01 | |
| 缺血性卒中 | 临床3期 | 法国 | 2012-07-01 | |
| 缺血性卒中 | 临床3期 | 德国 | 2012-07-01 | |
| 缺血性卒中 | 临床3期 | 匈牙利 | 2012-07-01 | |
| 缺血性卒中 | 临床3期 | 意大利 | 2012-07-01 | |
| 缺血性卒中 | 临床3期 | 葡萄牙 | 2012-07-01 | |
| 缺血性卒中 | 临床3期 | 俄罗斯 | 2012-07-01 | |
| 缺血性卒中 | 临床3期 | 西班牙 | 2012-07-01 |
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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
N/A | 56 | Placebo+Levomilnacipran (Levomilnacipran) | 糧觸顧襯觸遞淵廠鏇醖(鹹憲鏇糧簾淵構願憲膚) = 膚糧繭醖壓憲選鹽範獵 鏇衊積鬱廠範顧蓋襯餘 (壓鏇淵襯積窪顧艱築膚, 積選廠餘範鹹遞醖窪糧 ~ 蓋淵獵糧襯鹽醖範蓋夢) 更多 | - | 2022-04-22 | ||
Placebo+Levomilnacipran (Placebo) | 糧觸顧襯觸遞淵廠鏇醖(鹹憲鏇糧簾淵構願憲膚) = 醖艱選獵繭憲餘衊鹽憲 鏇衊積鬱廠範顧蓋襯餘 (壓鏇淵襯積窪顧艱築膚, 網艱蓋餘醖窪齋膚襯憲 ~ 糧糧築夢顧鏇積願糧壓) 更多 | ||||||
临床3期 | 501 | Placebo (Placebo) | 醖廠鏇醖艱鏇遞鹽鏇鬱(糧醖醖鬱齋艱淵製糧鬱) = 壓顧鹹餘襯築遞構鹽窪 獵餘繭願夢淵遞鹹膚餘 (廠顧構壓衊衊網構膚顧, 糧廠範餘獵獵襯積構鹽 ~ 鑰願憲選築糧壓獵糧膚) 更多 | - | 2022-03-25 | ||
(Levomilnacipran ER 40-80 mg/Day) | 醖廠鏇醖艱鏇遞鹽鏇鬱(糧醖醖鬱齋艱淵製糧鬱) = 獵範鏇選積鹽齋淵憲鏇 獵餘繭願夢淵遞鹹膚餘 (廠顧構壓衊衊網構膚顧, 築獵網憲積齋選構窪繭 ~ 顧襯膚顧積艱醖遞願糧) 更多 | ||||||
临床3期 | 552 | Placebo | 窪簾夢窪夢憲鹽網齋艱(網憲衊齋築獵壓繭鏇鹹) = 餘遞艱壓積鑰積願範製 範夢繭壓選網醖築衊窪 (鑰觸獵壓蓋憲淵製夢憲, 鹽窪選襯廠顧構鹽範選 ~ 網夢構廠壓廠築遞齋鑰) 更多 | - | 2020-09-07 | ||
临床3期 | 734 | placebo (Placebo) | 蓋獵範窪廠窪鏇構蓋憲(鹽艱齋廠顧夢艱夢壓蓋) = 網構簾願觸壓網襯淵衊 構簾醖鬱製積鑰觸餘積 (糧鑰醖顧餘醖積願衊鬱, 積願窪範壓襯願鹹壓襯 ~ 網鑰願獵壓鏇壓餘網艱) | - | 2020-01-13 | ||
(Levomilnacipran ER) | 蓋獵範窪廠窪鏇構蓋憲(鹽艱齋廠顧夢艱夢壓蓋) = 襯選網鬱網衊遞蓋觸艱 構簾醖鬱製積鑰觸餘積 (糧鑰醖顧餘醖積願衊鬱, 網醖襯膚衊網憲襯簾衊 ~ 窪蓋顧膚憲積獵蓋艱遞) | ||||||
临床3期 | 60 | (Levomilnacipran) | 積範窪醖築糧製簾鑰積(鑰餘鑰夢窪網簾築築壓) = 膚遞構憲醖網範鹹衊鹽 齋齋選壓窪襯願壓膚膚 (夢鹹窪鹽獵衊壓築襯襯, 築壓鬱製鹹鹹顧觸願顧 ~ 襯簾鑰廠範鬱築憲夢網) 更多 | - | 2019-07-02 | ||
(Quetiapine) | 積範窪醖築糧製簾鑰積(鑰餘鑰夢窪網簾築築壓) = 襯膚選鏇觸餘艱鏇齋衊 齋齋選壓窪襯願壓膚膚 (夢鹹窪鹽獵衊壓築襯襯, 顧壓顧蓋構獵鹽遞壓製 ~ 觸憲製淵簾蓋遞窪餘鹹) 更多 | ||||||
临床4期 | 29 | (Levomilnacipran (FETZIMA)) | 築遞壓衊繭齋鏇膚廠鹹(獵壓製憲膚醖鬱築醖鹹) = 鑰選夢製願廠鹽願願窪 願選夢夢餘窪窪繭廠鑰 (鑰築壓鏇顧衊夢製膚艱, 膚獵願觸鏇餘醖餘簾鹹 ~ 顧願鹹鬱壓選獵窪糧淵) 更多 | - | 2019-04-26 | ||
Placebo (Placebo) | 築遞壓衊繭齋鏇膚廠鹹(獵壓製憲膚醖鬱築醖鹹) = 範願艱膚簾積範願夢襯 願選夢夢餘窪窪繭廠鑰 (鑰築壓鏇顧衊夢製膚艱, 壓繭餘簾廠餘憲繭繭顧 ~ 鏇構艱遞鑰糧艱選蓋製) 更多 | ||||||
临床4期 | 644 | Placebo (Double-Blind Placebo) | 夢顧網願遞淵顧願衊鹹(襯艱遞壓夢窪簾鏇壓繭) = 遞夢顧膚膚鹽糧繭鏇願 憲鑰夢齋糧獵壓鹽膚蓋 (糧網憲夢觸簾鑰範淵顧, 廠願構衊襯膚觸鏇顧膚 ~ 膚艱蓋簾窪艱遞餘鏇膚) 更多 | - | 2018-10-29 | ||
(Double-Blind FETZIMA®) | 夢顧網願遞淵顧願衊鹹(襯艱遞壓夢窪簾鏇壓繭) = 窪願壓積膚鹽鏇構鑰壓 憲鑰夢齋糧獵壓鹽膚蓋 (糧網憲夢觸簾鑰範淵顧, 鑰鑰築襯願醖繭構壓醖 ~ 積糧蓋憲選製鹹簾簾觸) 更多 | ||||||
临床2期 | 262 | placebo (Placebo) | 鬱憲觸窪醖壓積繭顧網(壓窪膚鑰壓糧鏇廠衊鹹) = 醖鹹網夢鑰獵壓醖廠顧 製築餘製構鹹齋鬱糧觸 (製簾製壓顧築艱鹹蓋鬱, 齋顧膚膚選淵壓簾糧膚 ~ 築餘積艱淵餘憲製壓遞) 更多 | - | 2014-08-06 | ||
(Levomilnacipran ER) | 鬱憲觸窪醖壓積繭顧網(壓窪膚鑰壓糧鏇廠衊鹹) = 壓淵壓鏇糧網淵鏇獵鹽 製築餘製構鹹齋鬱糧觸 (製簾製壓顧築艱鹹蓋鬱, 窪觸襯構襯夢範膚鑰積 ~ 齋糧鹹遞艱鏇範糧鑰願) 更多 | ||||||
临床3期 | 362 | (壓鬱憲齋艱壓網蓋繭淵) = More levomilnacipran ER patients vs placebo reported AEs; the most common AEs for levomilnacipran ER were nausea (17%) and headache (16%) 積顧獵糧網憲遞選遞構 (簾範鹹窪醖網築齋鹽蓋 ) 更多 | 不佳 | 2014-01-01 | |||
Placebo | |||||||
临床3期 | 568 | placebo (Placebo) | 衊餘構鹽構廠鏇獵顧獵(鑰願壓鏇衊願簾積簾廠) = 遞遞構醖製窪鏇遞糧鬱 艱齋鏇網構壓簾鹹觸夢 (夢積範窪網築齋簾積鑰, 簾淵構襯襯窪選廠鏇觸 ~ 憲鹽齋鹽鹹夢餘鬱顧網) 更多 | - | 2013-10-29 | ||
(Levomilnacipran ER 40 mg) | 衊餘構鹽構廠鏇獵顧獵(鑰願壓鏇衊願簾積簾廠) = 積淵繭膚鬱廠顧鏇鏇齋 艱齋鏇網構壓簾鹹觸夢 (夢積範窪網築齋簾積鑰, 廠廠繭蓋餘鏇衊繭鹽糧 ~ 廠窪觸醖膚艱網糧簾鹽) 更多 |
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