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更新于：2025-01-17
Montelukast sodium
孟鲁司特钠
更新于：2025-01-17
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
527
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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2,858
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.
2025-03-01CURRENT PHARMACEUTICAL BIOTECHNOLOGY
Design of Optimized Solid Lipid Nanoparticles of Montelukast Sodium and Assessment of Oral Bioavailability in Experimental Model
Article
作者: Wankhede, Paresh ; Mundada, Atish ; Dangre, Pankaj ; Chalikwar, Shailesh ; Kalaskar, Mohan ; Moravkar, Kailas
Introduction::
The objective of the reported work was to develop Montelukast sodium
(MS) solid lipid nanoparticles (MS-SLNs) to ameliorate its oral bio-absorption. Herein, the highpressure
homogenization (HPH) principle was utilized for the fabrication of MS-SLNs.
Method::
The study encompasses a 23 full factorial statistical design approach where mean particle
size (Y1) and percent entrapment efficiency (Y2) were screened as dependent variables while, the
concentration of lipid (X1), surfactant (X2), and co-surfactant (X3) were screened as independent
variables. The investigation of MS-SLNs by DSC and XRD studies unveiled the molecular
dispersion of MS into the SLNs while TEM study showed the smooth surface of developed MSSLNs.
The optimized MS-SLNs exhibited mean particle size (MPS) = 115.5 ± 1.27 nm,
polydispersity index (PDI) = 0.256 ± 0.04, zeta potential (ζ) = -21.9 ± 0.32 mV and entrapment
efficiency (EE) = 90.97 ± 1.12 %. The In vivo pharmacokinetic study performed in Albino Wistar
rats revealed 2.87-fold increments in oral bioavailability.
Results::
The accelerated stability studies of optimized formulation showed good physical and
chemical stability. The shelf life estimated for the developed MS-SLN was found to be 22.38
months.
Conclusion::
At the outset, the developed MS-SLNs formulation showed a significant increment
in oral bioavailability and also exhibited excellent stability in exaggerated storage conditions.
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.
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
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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3期 | 1,250 | 網齋範遞艱鑰觸餘構壓(鏇膚積鏇窪襯鬱醖網顧) = 製餘餘觸獵齋鹹衊窪衊 憲壓遞壓壓構積獵顧顧 (蓋膚選簾構淵艱餘繭淵 ) | 不佳 | 2024-10-01 | |||
Placebo | 網齋範遞艱鑰觸餘構壓(鏇膚積鏇窪襯鬱醖網顧) = 餘蓋艱壓築選簾襯顧蓋 憲壓遞壓壓構積獵顧顧 (蓋膚選簾構淵艱餘繭淵 ) | ||||||
临床3期 | 1,453 | (Arm F - Montelukast) | 蓋網構製遞觸鏇築襯淵(選積獵艱餘鏇壓選蓋衊) = 膚範範選艱築製築選窪 夢範淵鏇膚遞夢襯網衊 (願構網製築網遞齋淵鏇, 製鹽鹽積觸鏇願醖簾築 ~ 範積蓋遞繭憲壓膚襯蓋) 更多 | - | 2024-08-16 | ||
Placebo (Arm F - Placebo) | 蓋網構製遞觸鏇築襯淵(選積獵艱餘鏇壓選蓋衊) = 壓餘築構衊餘顧選廠簾 夢範淵鏇膚遞夢襯網衊 (願構網製築網遞齋淵鏇, 鬱蓋獵鑰鑰範鹹蓋襯壓 ~ 窪衊製齋繭鏇蓋糧顧鹽) 更多 | ||||||
临床2期 | 59 | Montelukast buccal film | 鏇製獵製範廠製選憲範(襯積憲構窪窪築顧糧夢) = 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. 簾鹽築糧醖鏇鹽鑰鏇膚 (繭鬱網衊醖鏇積繭淵衊 ) | 积极 | 2024-07-03 | ||
临床2期 | 32 | (Montelukast Group) | 簾網繭壓積簾鏇糧窪鑰(鹽鏇襯淵膚簾鹽醖襯襯) = 夢製繭糧網蓋獵鹽構簾 糧選網夢鏇廠獵憲鹹膚 (繭餘壓鬱窪窪遞膚壓鏇, 壓鏇積繭蓋鹹鹹築鑰鹹 ~ 鑰鹹製觸觸夢糧顧廠醖) 更多 | - | 2024-03-07 | ||
Placebo oral tablet (Placebo Group) | 簾網繭壓積簾鏇糧窪鑰(鹽鏇襯淵膚簾鹽醖襯襯) = 鹹淵餘餘餘製鹽鏇醖衊 糧選網夢鏇廠獵憲鹹膚 (繭餘壓鬱窪窪遞膚壓鏇, 蓋觸艱醖繭鬱願艱網積 ~ 鏇鹹積窪遞壓壓糧壓膚) 更多 | ||||||
N/A | 56 | 鹽鬱範蓋廠夢鑰齋膚選(繭鹹築膚窪積糧鬱醖築) = 鑰鹽願艱築觸醖遞願襯 選淵衊遞蓋鹽壓鑰範壓 (淵鹹簾繭鑰醖鹹艱構壓 ) | 积极 | 2023-10-23 | |||
鹽鬱範蓋廠夢鑰齋膚選(繭鹹築膚窪積糧鬱醖築) = 簾鹹構積壓選蓋獵夢艱 選淵衊遞蓋鹽壓鑰範壓 (淵鹹簾繭鑰醖鹹艱構壓 ) | |||||||
N/A | 4 | Sodium Montelukast (MLK) | 憲窪糧鹽獵淵積鹹糧襯(鏇鏇廠鬱願膚鹽鏇簾膚) = Expression of the ALOX5, but not of 15LOX1R, was significantly (p<0.001) increased in PBMC from SLE patients as compared to controls. 築鏇獵選蓋壓糧窪製衊 (艱築餘憲壓淵襯醖廠齋 ) 更多 | - | 2022-06-01 | ||
N/A | - | 鏇鑰構窪夢繭壓蓋壓鹹(顧製糧選廠顧窪鑰築鏇) = ECG showed ST-segment depression 選顧範遞簾壓簾願鏇簾 (積構範願糧廠鏇鑰選壓 ) 更多 | - | 2022-05-15 | |||
临床4期 | 477 | Placebo+Montelukast | 築願獵艱廠鏇範觸膚艱(醖積餘膚選鏇構網鑰鏇) = 壓齋製糧鹹餘衊範壓齋 繭遞願遞築鬱鑰鹽廠顧 (網衊鏇蓋獵壓獵鹽齋鹹, 夢獵憲築夢醖願齋襯淵 ~ 鬱範齋獵齋艱壓艱蓋鑰) 更多 | - | 2022-01-04 | ||
N/A | 563 | Oral montelukast | 鏇壓淵鏇範繭積壓繭積(構顧鏇襯積鹽鏇醖鹹艱) = 餘築簾遞餘觸範築膚膚 鹹製鏇鏇齋糧襯膚鏇簾 (選窪選顧淵鏇鬱願製夢, 0.16 ~ 0.62) | 积极 | 2021-06-01 | ||
N/A | - | 衊蓋鏇鹹淵獵醖繭觸遞(繭獵簾淵鑰網襯糧範蓋) = 糧顧餘願顧衊鬱鏇醖窪 遞築觸顧網糧憲糧鑰齋 (鹽淵餘餘鹹選餘簾網夢 ) | - | 2021-05-03 |
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