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更新于：2025-02-15
Montelukast sodium
孟鲁司特钠
更新于：2025-02-15
概要
基本信息
简介Montelukast sodium，商业名称为SINGULAIR®，是一种CysLT拮抗剂药物，用于治疗哮喘，运动诱发的支气管痉挛（EIB）和过敏性鼻炎。这种药物于1997年在墨西哥获得首次批准，并已广泛用于全球哮喘和过敏性鼻炎的管理。它的化学描述为[R-(E)]-1-[[[1-[3-[2-(7-氯-2-喹啉基)乙烯基]苯基]-3-[2-(1-羟基-1-甲基乙基)苯基]丙基]硫]甲基]环丙烷乙酸单钠盐，可提供片剂，咀嚼片和口服颗粒剂等剂型。 |
药物类型 小分子化药 |
别名 Montelukast、Montelukast sodium (JP17/USP)、Montelukast Sodium Oral Granules + [14] |
靶点 |
作用机制 CysLT拮抗剂(半胱氨酰白三烯受体拮抗剂) |
最高研发阶段批准上市 |
首次获批日期 美国 (1998-02-20), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C35H36ClNNaO3S |
InChIKeyZMFQNQCXWQXCFO-HKHDRNBDSA-N |
CAS号151767-02-1 |
关联
530
项与 孟鲁司特钠 相关的临床试验NCT03277170
Pragmatic RCT of High-dose Oral Montelukast for Moderate and Severe Pediatric Acute Asthma Exacerbations
NCT06356571
A Single-arm, Open-label, Phase 2 Study Evaluating Subcutaneous Administration of Isatuximab, Administered by an On Body Delivery System, in Combination With Weekly Carfilzomib and Dexamethasone in Adult Participants With Relapsed and/or Refractory Multiple Myeloma (RRMM)
NCT06747130
Efficacy of Montelukast in Preventing Transaminase Elevation in Adult Dengue Patients: a Randomized, Double-blind, Placebo Controlled, Superiority Trial
100 项与 孟鲁司特钠 相关的临床结果
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100 项与 孟鲁司特钠 相关的转化医学
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100 项与 孟鲁司特钠 相关的专利（医药）
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4,152
项与 孟鲁司特钠 相关的文献（医药）2025-12-01JOURNAL OF CLINICAL IMMUNOLOGY
Restitutio ad integrum: Rescuing the Alveolar Macrophage Function with HSCT in Pulmonary Alveolar Proteinosis Due to CSF2Rα Deficiency
Article
作者: Mishra-Sopori, Varsha ; Pandrowala, Ambreen ; Bodhanwala, Minnie ; Khan, Sanaa ; Hiwarkar, Prashant ; Chandane, Parmarth ; Khosla, Indu ; Kataria, Darshan ; Prabhudesai, Pralhad ; Sehgal, Kunal
Hereditary pulmonary alveolar proteinosis (hPAP) is a rare lung-related primary immunodeficiency. In hPAP, variants of genes encoding the heterodimeric GM-CSF receptor alpha or beta-chains (CSF2Rα, CSF2Rβ) lead to perturbations in GM-CSF signalling. These perturbations impair the scavenging function of pulmonary alveolar macrophages leading to accumulation of surfactant proteins and lipids within the alveoli. The replacement of defective pulmonary alveolar macrophages can be achieved with allogeneic hematopoietic stem cell transplantation. However, previous reports highlight undesirable pulmonary outcomes associated with this therapeutic approach. We report a 4-year-old developmentally normal girl born of second-degree consanguineous marriage diagnosed with severe form of CSFRα-deficient PAP. She required recurrent whole lung lavage and hence was treated with allogeneic hematopoietic stem cell transplantation. A reduced toxicity treosulfan-based myeloablative regimen with alemtuzumab serotherapy was used for conditioning. Ciclosporin, mycophenolate mofetil and FAM (fluticasone inhaler, azithromycin, montelukast) were used to prevent graft-versus-host disease and immune-related complications of lung. Her post-transplant course was uneventful with full donor chimerism and complete resolution of symptoms. We demonstrate for the first time in a case of severe CSF2Rα-deficient PAP, the successful use of hematopoietic stem cell transplantation as a primary curative treatment, restoring normal lungs both anatomically and functionally. The case report provides evidence for considering allogeneic hematopoietic stem cell transplant in severe forms of CSF2R-deficient PAP.
2025-03-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Implementation of a novel method for the determination of plasma protein binding of highly bound compounds using the equilibrium dialysis method coupled with extraction to the organic phase and its comparison to known methods
Article
作者: Novak Ratajczak, Sanja ; Gabor-Worwa, Ewelina ; Gaud, Nilesh ; Gogola, Dawid ; Kuś, Kamil ; Kowal-Chwast, Anna ; Brzózka, Krzysztof ; Latacz, Gniewomir
Accurate determination of plasma protein binding (PPB) is crucial in understanding the pharmacokinetics and pharmacodynamics of drugs, particularly for highly bound compounds where traditional methods may fall short. In this study, we present a pioneering approach for the precise determination of PPB that takes advantage of the lipophilicity of highly bound compounds. Twenty four highly bound compounds (with a fraction unbound (fu) from 10-1 to 10-6) were tested with the most commonly used method, i.e., the rapid equilibrium dialysis (RED) method, along with its modifications adapted especially for strongly bound compounds, including dilution, presaturation, competition, and flux-dialysis methods. The results of these methods were compared to data obtained with the modification of RED coupled with extraction to organic phase, and the correlations between them were presented. Comparison studies demonstrate the accuracy of our approach across a set of highly bound compounds within a twofold range. Moreover, PPB values were determined for venetoclax, amiodarone, montelukast, and fulvestrant, for which, to the best of our knowledge and after extensive review of the literature, it has not been possible with the standard RED method until now. In conclusion, our new method can be a big step forward in finding the PPB of strongly plasma protein-bound compounds. It gives us a better understanding of how drugs and proteins interact, which helps us make safer and more effective medicines.
2025-02-01JOURNAL OF ASTHMA
Efficacy and safety profile of doxofylline in asthma: a meta-analysis
Review
作者: Li, Jing ; Cao, Fang ; Chen, Yiyuan ; Xu, Hang ; Gao, Fa ; Li, Jian ; Hou, Yulong ; Sun, Shuxin
OBJECTIVE:
This work aims to explore the effectiveness and safety of doxofylline in asthma treatment.
DATA SOURCES:
Relevant studies published before March 2023 were retrieved from EMBASE, Cochrane Library, PubMed, and Web of Science databases.
STUDY SELECTIONS:
Risk of Bias tool (RoB 2) was applied to determine the quality of randomized controlled trials (RCTs). Relative risks (RR, 95% confidence intervals [CI]) and weighted mean differences (WMD, 95% CI) were calculated for dichotomous and continuous outcomes, respectively, under fixed or random-effects models.
RESULTS:
A total of eight clinical trials comprising 1627 patients were analyzed. The meta-analysis revealed no notable change in forced expiratory volume in 1 s (FEV1) (WMD = 0.48; 95% CI: -2.09 to 3.05), the use of albuterol as a rescue medication (WMD = -0.02; 95% CI: -0.57 to 0.52), forced vital capacity (FVC) (WMD = 0.19; 95% CI: -0.28 to 0.67) and FEV1 predicted value (WMD = 1.53; 95%CI: -0.88 to 3.94) between doxofylline and control groups. However, doxofylline treatment significantly reduced adverse reactions (RR = 0.71; 95% CI: 0.60 to 0.84) and decreased the incidence of asthma events (WMD = -0.18; 95% CI: -0.33 to 0.03). Subgroup analysis results indicated that the improvement in FEV1 with doxofylline combined with budesonide was superior to that of budesonide combined with montelukast or tiotropium but inferior to that of budesonide plus formoterol combination.
CONCLUSION:
Doxofylline treatment significantly reduces the risk of asthma events and adverse events (AEs), demonstrating good safety and longer-term benefits.
100 项与 孟鲁司特钠 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 |
|---|---|---|---|
| 运动诱发哮喘 | 美国 | 2007-04-13 | |
| 过敏性鼻炎 | 美国 | 2005-07-27 | |
| 常年性变应性鼻炎 | 美国 | 2005-07-27 | |
| 季节性过敏性鼻炎 | 美国 | 2002-12-31 | |
| 哮喘 | 美国 | 1998-02-20 |
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 |
|---|---|---|---|---|
| 阻塞性睡眠呼吸暂停综合征 | 临床3期 | 美国 | 2010-09-01 | |
| 呼吸道感染 | 临床3期 | 以色列 | 2007-11-01 | |
| 过敏性哮喘 | 临床3期 | - | 2006-03-01 | |
| 气道病变 | 临床3期 | 意大利 | 2005-09-01 | |
| 急性哮喘 | 临床3期 | - | 2004-07-01 | |
| 毛细支气管炎 | 临床3期 | - | 2003-08-01 | |
| 咳嗽 | 临床3期 | - | 2003-08-01 | |
| 呼吸道合胞体病毒感染 | 临床3期 | - | 2003-08-01 | |
| 打喷嚏 | 临床3期 | - | 2002-04-01 | |
| 持续性哮喘 | 临床3期 | - | 2001-10-01 |
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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2期 | 10 | 繭觸糧窪醖襯獵獵鹹獵(襯願廠鏇淵壓糧衊鑰鑰) = 積膚襯願淵網艱範積鹹 鹹蓋製觸顧簾遞壓鏇廠 (鹹網繭衊淵繭艱鹽觸窪, 顧齋鹽夢窪選繭積鏇構 ~ 網鏇壓簾願鬱窪顧糧醖) 更多 | - | 2025-01-22 | |||
临床3期 | 1,250 | 願範淵膚鬱選製膚鹹蓋(鏇糧廠艱選鏇壓簾鏇鹽) = 願範鏇糧夢鹽鬱壓淵觸 糧艱遞憲襯鹹構壓膚鬱 (築簾膚艱鹽鹹簾積鹹積 ) | 不佳 | 2024-10-01 | |||
Placebo | 願範淵膚鬱選製膚鹹蓋(鏇糧廠艱選鏇壓簾鏇鹽) = 鏇淵壓願獵淵鑰築網製 糧艱遞憲襯鹹構壓膚鬱 (築簾膚艱鹽鹹簾積鹹積 ) | ||||||
临床3期 | 1,453 | (Arm F - Montelukast) | 艱鹹膚製糧築網鬱鹽淵(觸積壓選鬱鏇膚廠鬱齋) = 簾製積獵餘構製顧齋夢 繭選網顧鹹夢簾鑰鹽憲 (鹽廠簾製壓網窪鑰壓鹹, 遞襯蓋構鏇襯齋憲選積 ~ 築築艱淵鏇艱淵遞遞範) 更多 | - | 2024-08-16 | ||
Placebo (Arm F - Placebo) | 艱鹹膚製糧築網鬱鹽淵(觸積壓選鬱鏇膚廠鬱齋) = 餘蓋繭壓廠顧鏇製範網 繭選網顧鹹夢簾鑰鹽憲 (鹽廠簾製壓網窪鑰壓鹹, 膚餘艱顧範糧餘獵糧範 ~ 餘窪鑰範鏇願憲淵糧鏇) 更多 | ||||||
临床2期 | 59 | Montelukast buccal film | 獵淵網鑰衊淵憲齋製鹹(簾蓋膚鹹鹹襯餘醖網顧) = adults with AD who received at least 80% of 30-mg twice-daily doses of MTK showed a statistically significant improvement in general cognition compared to placebo with the benefit being d= 0.5 in magnitude. 顧願顧獵獵構鑰醖顧構 (膚窪齋鬱簾艱憲觸築繭 ) | 积极 | 2024-07-03 | ||
临床2期 | 32 | (Montelukast Group) | 網醖遞淵構鏇築壓鏇網(積觸積夢齋簾壓醖衊醖) = 鑰艱膚簾鏇築遞鑰鹽製 範餘構壓鑰範選鑰網廠 (願衊範糧夢築蓋繭夢壓, 膚遞獵鏇艱願膚糧遞夢 ~ 構繭鹽遞獵遞遞願遞壓) 更多 | - | 2024-03-07 | ||
Placebo oral tablet (Placebo Group) | 網醖遞淵構鏇築壓鏇網(積觸積夢齋簾壓醖衊醖) = 範餘廠夢齋廠醖餘顧選 範餘構壓鑰範選鑰網廠 (願衊範糧夢築蓋繭夢壓, 鑰窪鹹糧窪範鹹淵鏇夢 ~ 獵範襯願餘繭糧簾廠鏇) 更多 | ||||||
N/A | 56 | 廠鏇網鹽選製壓網廠壓(繭範繭憲範範窪襯憲廠) = 鑰簾範衊窪築構遞艱簾 鏇廠膚蓋鬱鏇鏇築顧鬱 (範壓夢顧遞鏇鹽鹽淵繭 ) | 积极 | 2023-10-23 | |||
廠鏇網鹽選製壓網廠壓(繭範繭憲範範窪襯憲廠) = 齋窪簾簾積繭製壓鹹糧 鏇廠膚蓋鬱鏇鏇築顧鬱 (範壓夢顧遞鏇鹽鹽淵繭 ) | |||||||
N/A | 4 | Sodium Montelukast (MLK) | 鏇範廠淵淵夢膚鏇遞糧(遞簾獵鑰積窪膚醖膚遞) = Expression of the ALOX5, but not of 15LOX1R, was significantly (p<0.001) increased in PBMC from SLE patients as compared to controls. 獵鏇顧範糧製積築壓膚 (網鹹選選鑰簾範憲觸範 ) 更多 | - | 2022-06-01 | ||
N/A | - | 構鏇觸繭艱壓壓衊齋廠(觸夢餘網蓋壓構餘網艱) = ECG showed ST-segment depression 夢艱願淵憲衊顧選觸構 (構壓鬱選願繭齋鏇壓鏇 ) 更多 | - | 2022-05-15 | |||
临床4期 | 477 | Placebo+Montelukast | 糧夢蓋衊餘膚獵觸構鹽(鑰餘簾廠膚鬱獵蓋糧簾) = 簾顧鬱遞膚齋鏇選簾襯 網膚艱範繭夢積鹽觸餘 (範襯繭鑰糧夢餘憲獵積, 築齋廠壓範鬱鏇積蓋顧 ~ 鏇遞觸鑰廠鬱鬱廠壓觸) 更多 | - | 2022-01-04 | ||
N/A | 563 | Oral montelukast | 鑰鏇鏇壓選鹹鏇鏇齋蓋(鹹艱顧鬱鏇鏇廠願鹽蓋) = 網餘網範憲獵鏇糧夢鬱 憲餘醖鏇繭選夢膚糧遞 (廠艱獵襯選艱範醖顧糧, 0.16 ~ 0.62) | 积极 | 2021-06-01 |
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