更新于：2024-12-26
Zafirlukast
扎鲁司特
更新于：2024-12-26
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1996-09-26), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C31H33N3O6S |
InChIKeyYEEZWCHGZNKEEK-UHFFFAOYSA-N |
CAS号107753-78-6 |
关联
4
项与 扎鲁司特 相关的临床试验Double Blind Placebo-controlled Crossover Study of Zafirlukast in Preventing Allergen-induced Signs and Symptoms of Allergic Rhinitis in Response to Cat Dander Challenge
A Phase 2 Study of Zafirlukast for the Treatment of Tumor-marker Only Relapsed Ovarian Cancer
Breast Capsular Contracture Following Post-Mastectomy Reconstruction in Women Treated With the Leukotriene Inhibitor Zafirlukast: A Phase II Trial
100 项与 扎鲁司特 相关的临床结果
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100 项与 扎鲁司特 相关的转化医学
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100 项与 扎鲁司特 相关的专利（医药）
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537
项与 扎鲁司特 相关的文献（医药）2024-09-16BMC Pulmonary Medicine
Zafirlukast ameliorates lipopolysaccharide and bleomycin-induced lung inflammation in mice.
Article
作者: Yang, Zhongyi ; Zhang, Tiantian ; Zhou, Honggang ; Gao, Jingjing ; Jiao, Ran ; Liu, Jing ; Li, Xiaohe ; Zhang, Qianyi ; Xu, Aiguo ; Chai, Dan ; Liu, Yuming ; Cui, Yunyao ; Xue, Tongtong ; Meng, Lingxin
Acute lung injury (ALI) is the result of damage to the capillary endothelia and the alveolar epithelial cell caused by various direct and indirect factors, leading to significant pulmonary interstitial and alveolar edema and acute hypoxic respiratory insufficiency. A subset of ALI cases progresses to irreversible pulmonary fibrosis, a condition with fatal implications. Zafirlukast is a leukotriene receptor antagonist licensed for asthma prevention and long-term treatment. This study demonstrated a significant improvement in lung tissue pathology and a reduction in inflammatory cell infiltration in models of lipopolysaccharide (LPS)-induced ALI and bleomycin (BLM)-induced lung inflammation following zafirlukast administration, both in vivo and in vitro. Moreover, zafirlukast was found to suppress the inflammatory response of alveolar epithelial cells in vitro and lung inflammation in vivo by reducing the activation of the TLR4/NF-κB/NLRP3 inflammasome pathway. In conclusion, zafirlukast relieved lung injury and the infiltration of inflammatory cells in the lung by regulating the TLR4/NF-κB/NLRP3 pathway.
2024-09-01Journal of biomolecular structure & dynamics
Metabolites profiling and cheminformatics bioprospection of selected medicinal plants against the main protease and RNA-dependent RNA polymerase of SARS-CoV-2.
Article
作者: Swalaha, Feroz Mahomed ; Enitan-Folami, Abimbola Motunrayo ; Nyaga, Martin M ; Lanrewaju, Adedayo Ayodeji ; Sabiu, Saheed
Despite the existence of some vaccines, SARS-CoV-2 (S-2) infections persist for various reasons relating to vaccine reluctance, rapid mutation rate, and an absence of specific treatments targeted to the infection. Due to their availability, low cost and low toxicity, research into potentially repurposing phytometabolites as therapeutic alternatives has gained attention. Therefore, this study explored the antiviral potential of metabolites of some medicinal plants [Spondias mombin, Macaranga barteri and Dicerocaryum eriocarpum (Sesame plant)] identified using liquid chromatography-mass spectrometry (LCMS) as possible inhibitory agents against the S-2 main protease (S-2 MP) and RNA-dependent RNA polymerase (RP) using computational approaches. Molecular docking was used to identify the compounds with the best affinities for the selected therapeutics targets. Afterwards, compounds with poor physicochemical characteristics, pharmacokinetics, and drug-likeness were screened out. The top-ranked compounds were further subjected to a 120-ns molecular dynamics (MD) simulation. Only quercetin 3-O-rhamnoside (-48.77 kcal/mol) had higher binding free energy than the reference standard (zafirlukast) (-44.99 kcal/mol) against S-2 MP. Conversely, all the top-ranked compounds (ellagic acid hexoside, spiraeoside, apigenin-4'-glucoside and chrysoeriol 7-glucuronide) except gnetin L (-24.24 kcal/mol) had higher binding free energy (-55.19 kcal/mol, -52.75 kcal/mol, -47.22 kcal/mol and -43.35 kcal/mol) respectively, against S-2 RP relative to the reference standard (-34.79 kcal/mol). The MD simulations study further revealed that the investigated inhibitors are thermodynamically stable and form structurally compatible complexes that impede the regular operation of the respective S-2 therapeutic targets. Although, these S-2 therapeutic candidates are promising, further in vitro and in vivo evaluation is required and highly recommended.Communicated by Ramaswamy H. Sarma.
2024-08-07ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Zafirlukast induces DNA condensation and has bactericidal effect on replicating
Mycobacterium abscessus
Article
作者: Niet, Sanne van der ; Bakker, Jordy de ; Garneau-Tsodikova, Sylvie ; Lodder, Bastiaan ; Green, Keith D ; Schimmel, Irene M ; Reits, Eric A ; van der Wel, Nicole N
ABSTRACT:
Mycobacterium abscessus
infections are emerging in cystic fibrosis patients, and treatment success rate in these patients is only 33% due to extreme antibiotic resistance. Thus, new treatment options are essential. An interesting target could be Lsr2, a nucleoid-associated protein involved in mycobacterial virulence. Zafirlukast is a Food and Drug Administration (FDA)-approved drug against asthma that was shown to bind Lsr2. In this study, zafirlukast treatment is shown to reduce
M. abscessus
growth, with a minimal inhibitory concentration of 16 µM and a bactericidal concentration of 64 µM in replicating bacteria only. As an initial response, DNA condensation, a known stress response of mycobacteria, occurs after 1 h of treatment with zafirlukast. During continued zafirlukast treatment, the morphology of the bacteria alters and the structural integrity of the bacteria is lost. After 4 days of treatment, reduced viability is measured in different culture media, and growth of
M. abscessus
is reduced in a dose-dependent manner. Using transmission electron microscopy, we demonstrated that the hydrophobic multilayered cell wall and periplasm are disorganized and ribosomes are reduced in size and relocalized. In summary, our data demonstrate that zafirlukast alters the morphology of
M. abscessus
and is bactericidal at 64 µM. The bactericidal concentration of zafirlukast is relatively high, and it is only effective on replicating bacteria but as zafirlukast is an FDA-approved drug, and currently used as an anti-asthma treatment, it could be an interesting drug to further study in
in vivo
experiments to determine whether it could be used as an antibiotic for
M. abscessus
infections.
100 项与 扎鲁司特 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 哮喘 | 美国 | 1996-09-26 |
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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 | 4 | (Zafirlukast) | 膚獵膚壓鹽鏇積襯鑰夢(獵壓糧窪獵選繭網網鑰) = 鏇醖網網鹹窪醖積遞遞 範鹽廠糧壓簾鹽夢獵鹽 (範艱鹽鹽糧觸糧觸願鑰, 醖築網鑰構齋夢餘壓顧 ~ 鏇鏇顧襯醖積淵膚觸鑰) 更多 | - | 2019-10-01 | ||
Standard of Care (no intervention) (Standard of Care (no Intervention)) | 膚獵膚壓鹽鏇積襯鑰夢(獵壓糧窪獵選繭網網鑰) = 壓夢廠廠壓構淵廠壓觸 範鹽廠糧壓簾鹽夢獵鹽 (範艱鹽鹽糧觸糧觸願鑰, 遞獵壓選蓋積網範艱遞 ~ 壓鏇蓋遞顧範糧糧廠糧) 更多 |
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