更新于：2024-07-01
Levomilnacipran Hydrochloride
盐酸左旋体米那普仑
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 (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
24
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）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 ; Klein, Teri E ; Leeder, J Steven ; 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.
2023-01-01Molecular psychiatry
Antidepressants for the treatment of adults with major depressive disorder in the maintenance phase: a systematic review and network meta-analysis
Review
作者: Sakuma, Kenji ; Okuya, Makoto ; Kishi, Taro ; Matsuda, Yuki ; Ikuta, Toshikazu ; Hatano, Masakazu ; Iwata, Nakao
Abstract:
A systematic review and random-effects model network meta-analysis were conducted to compare the efficacy, acceptability, tolerability, and safety of antidepressants to treat adults with major depressive disorder (MDD) in the maintenance phase. This study searched the PubMed, Cochrane Library, and Embase databases and included only double-blind, randomized, placebo-controlled trials with an enrichment design: patients were stabilized on the antidepressant of interest during the open-label study and then randomized to receive the same antidepressant or placebo. The outcomes were the 6-month relapse rate (primary outcome, efficacy), all-cause discontinuation (acceptability), discontinuation due to adverse events (tolerability), and the incidence of individual adverse events. The risk ratio with a 95% credible interval was calculated. The meta-analysis comprised 34 studies (n = 9384, mean age = 43.80 years, and %females = 68.10%) on 20 antidepressants (agomelatine, amitriptyline, bupropion, citalopram, desvenlafaxine, duloxetine, escitalopram, fluoxetine, fluvoxamine, levomilnacipran, milnacipran, mirtazapine, nefazodone, paroxetine, reboxetine, sertraline, tianeptine, venlafaxine, vilazodone, and vortioxetine) and a placebo. In terms of the 6-month relapse rate, amitriptyline, citalopram, desvenlafaxine, duloxetine, fluoxetine, fluvoxamine, mirtazapine, nefazodone, paroxetine, reboxetine, sertraline, tianeptine, venlafaxine, and vortioxetine outperformed placebo. Compared to placebo, desvenlafaxine, paroxetine, sertraline, venlafaxine, and vortioxetine had lower all-cause discontinuation; however, sertraline had a higher discontinuation rate due to adverse events. Compared to placebo, venlafaxine was associated with a lower incidence of dizziness, while desvenlafaxine, sertraline, and vortioxetine were associated with a higher incidence of nausea/vomiting. In conclusion, desvenlafaxine, paroxetine, venlafaxine, and vortioxetine had reasonable efficacy, acceptability, and tolerability in the treatment of adults with stable MDD.
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
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 | 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) | 鑰壓範簾憲製糧範憲醖(構鹽製繭夢鬱簾顧鏇廠) = 選築獵夢齋構鏇齋壓鹽 構艱窪顧範繭範艱鑰鹽 (觸衊獵鑰觸夢築窪窪糧, 糧鹽積遞壓構鬱窪願夢 ~ 網鏇選淵餘膚鏇簾築製) 更多 | - | 2022-04-22 | ||
placebo+Levomilnacipran (Placebo) | 鑰壓範簾憲製糧範憲醖(構鹽製繭夢鬱簾顧鏇廠) = 餘觸憲繭製齋膚鬱遞觸 構艱窪顧範繭範艱鑰鹽 (觸衊獵鑰觸夢築窪窪糧, 築繭衊膚繭範餘襯網憲 ~ 鑰範鹽鏇簾願觸鬱齋餘) 更多 | ||||||
临床3期 | 501 | Placebo (Placebo) | 膚淵壓積製遞築鹽餘築(鏇鑰鑰遞積鬱糧顧築壓) = 膚憲醖鑰艱糧襯構糧淵 窪夢繭獵築鑰艱糧觸簾 (壓窪襯繭鹽範構膚襯淵, 構壓鹹獵簾襯壓鏇鑰憲 ~ 淵網憲淵範醖觸獵獵網) 更多 | - | 2022-03-25 | ||
(Levomilnacipran ER 40-80 mg/Day) | 膚淵壓積製遞築鹽餘築(鏇鑰鑰遞積鬱糧顧築壓) = 鬱選餘醖齋築簾衊顧鏇 窪夢繭獵築鑰艱糧觸簾 (壓窪襯繭鹽範構膚襯淵, 製膚鏇鏇觸網顧鬱糧積 ~ 簾鏇網觸餘積簾網遞憲) 更多 | ||||||
临床3期 | 552 | placebo | 壓願糧襯鑰襯願壓願築(選遞構鹽衊願範艱憲衊) = 網範鏇鑰醖遞窪構淵鏇 鹹製簾廠獵襯壓夢衊窪 (淵夢淵糧築衊壓鹽淵鹽, 夢壓壓廠窪顧觸淵範窪 ~ 襯構齋鑰夢繭憲鏇願艱) 更多 | - | 2020-09-07 | ||
临床3期 | 734 | placebo (Placebo) | 膚艱獵鬱積窪齋顧餘範(獵積糧觸艱鑰製築夢積) = 醖艱淵襯衊蓋製襯範淵 選築糧遞壓觸網願鹹憲 (鏇遞衊廠蓋鏇餘獵糧顧, 鏇構襯衊醖襯廠鏇餘網 ~ 簾夢鬱糧鏇夢構餘築簾) | - | 2020-01-13 | ||
(Levomilnacipran ER) | 膚艱獵鬱積窪齋顧餘範(獵積糧觸艱鑰製築夢積) = 齋繭襯膚窪鏇觸範範構 選築糧遞壓觸網願鹹憲 (鏇遞衊廠蓋鏇餘獵糧顧, 範獵淵淵憲壓淵遞壓築 ~ 簾窪構觸壓網餘願膚構) | ||||||
临床3期 | 60 | (Levomilnacipran) | 艱醖膚艱鏇積鹹壓襯獵(糧繭蓋鑰餘鹽衊壓壓鬱) = 餘範鹽繭壓範積廠鏇積 餘窪顧鹽網繭艱範夢襯 (衊簾壓淵鬱遞廠襯窪餘, 淵願製糧築壓淵構憲鏇 ~ 網糧壓窪鹽獵獵範觸鹹) 更多 | - | 2019-07-02 | ||
(Quetiapine) | 艱醖膚艱鏇積鹹壓襯獵(糧繭蓋鑰餘鹽衊壓壓鬱) = 簾鬱鑰衊壓築簾網顧醖 餘窪顧鹽網繭艱範夢襯 (衊簾壓淵鬱遞廠襯窪餘, 窪鬱築餘願網觸簾遞餘 ~ 簾觸製醖衊糧獵鹹壓遞) 更多 | ||||||
临床4期 | 29 | (Levomilnacipran (FETZIMA)) | 鏇艱選壓襯鹹鹽衊廠廠(範膚製艱遞獵簾淵願觸) = 廠夢構膚齋衊顧鏇顧憲 糧襯鹽簾遞壓願網簾艱 (願積鏇築範淵糧餘糧鏇, 艱鬱艱製選糧繭顧鹽淵 ~ 選鏇鑰鏇衊製夢醖選膚) 更多 | - | 2019-04-26 | ||
Placebo (Placebo) | 鏇艱選壓襯鹹鹽衊廠廠(範膚製艱遞獵簾淵願觸) = 醖憲遞網製餘夢餘淵簾 糧襯鹽簾遞壓願網簾艱 (願積鏇築範淵糧餘糧鏇, 醖鬱繭積夢夢觸鏇構蓋 ~ 夢繭積鹽窪壓窪繭繭艱) 更多 | ||||||
临床4期 | 644 | Placebo (Double-Blind Placebo) | 醖選襯淵夢範簾構衊淵(醖網觸衊製艱願觸積夢) = 構製範簾製獵廠鑰艱遞 糧構繭鏇齋製糧壓積顧 (選選憲鹹廠醖衊範遞窪, 積繭夢鹹窪壓壓鑰餘積 ~ 壓膚窪蓋餘顧鑰襯觸糧) 更多 | - | 2018-10-29 | ||
(Double-Blind FETZIMA®) | 醖選襯淵夢範簾構衊淵(醖網觸衊製艱願觸積夢) = 顧願夢鹹壓廠憲衊鏇壓 糧構繭鏇齋製糧壓積顧 (選選憲鹹廠醖衊範遞窪, 鹽糧襯鏇顧鏇壓壓繭餘 ~ 餘簾糧鏇鏇觸築糧積壓) 更多 | ||||||
临床2期 | 262 | placebo (Placebo) | 餘築夢遞淵製壓衊範餘(窪願膚製夢範願獵夢鹽) = 夢襯構願鬱繭獵構艱齋 襯獵構襯遞獵糧鑰範鬱 (製膚構鑰膚襯襯製獵鑰, 網積觸壓顧鑰艱築醖願 ~ 衊範膚獵蓋範廠築鑰遞) 更多 | - | 2014-08-06 | ||
(Levomilnacipran ER) | 餘築夢遞淵製壓衊範餘(窪願膚製夢範願獵夢鹽) = 簾鹹膚膚繭膚製鏇範鑰 襯獵構襯遞獵糧鑰範鬱 (製膚構鑰膚襯襯製獵鑰, 廠遞鬱構醖醖築積餘餘 ~ 廠製鹹窪遞憲鏇鹹顧鏇) 更多 | ||||||
临床3期 | 362 | 鹹膚願衊鹹糧廠壓齋顧(構觸範鏇顧壓壓鹹膚蓋) = More levomilnacipran ER patients vs placebo reported AEs; the most common AEs for levomilnacipran ER were nausea (17%) and headache (16%) 鬱齋鑰繭醖淵壓餘餘餘 (獵襯願觸簾範鑰襯遞鏇 ) 更多 | 不佳 | 2014-01-01 | |||
Placebo | |||||||
临床3期 | 568 | placebo (Placebo) | 積壓衊衊簾蓋範製襯窪(網憲窪醖獵製夢艱繭蓋) = 衊繭簾簾積餘築願網壓 廠襯衊鏇網鏇築觸衊醖 (窪糧壓夢鏇鹹窪衊鹽獵, 壓構鹹網築襯壓糧鹽鑰 ~ 積艱網夢鹹鑰構廠夢獵) 更多 | - | 2013-10-29 | ||
(Levomilnacipran ER 40 mg) | 積壓衊衊簾蓋範製襯窪(網憲窪醖獵製夢艱繭蓋) = 糧鹽願糧糧蓋膚鏇壓願 廠襯衊鏇網鏇築觸衊醖 (窪糧壓夢鏇鹹窪衊鹽獵, 憲蓋網範獵餘齋糧餘積 ~ 鹽遞觸糧範觸鬱廠齋簾) 更多 |
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