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更新于：2025-02-21
Zafirlukast
扎鲁司特
更新于：2025-02-21
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/序列
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NCT06069063
Double Blind Placebo-controlled Crossover Study of Zafirlukast in Preventing Allergen-induced Signs and Symptoms of Allergic Rhinitis in Response to Cat Dander Challenge
NCT04339140
A Phase 2 Study of Zafirlukast for the Treatment of Tumor-marker Only Relapsed Ovarian Cancer
NCT02950480
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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943
项与 扎鲁司特 相关的文献（医药）2025-01-01JOURNAL OF MEDICAL VIROLOGY
Antiviral and Immunomodulatory Effects of Zafirlukast Against Flaviviruses via Inhibition of the TNF Signaling Pathway
Article
作者: Balasubramaniam, Vinod RMT. ; Gilbert‐Jaramillo, Javier ; Adnan, Nur Amelia Azreen ; Komarasamy, Thamil Vaani ; James, William S.
ABSTRACT:
The two most clinically important members of the flavivirus genus, Zika virus (ZIKV) and dengue virus (DENV) pose a significant public health challenge. They cause a range of diseases in humans, from hemorrhagic to neurological manifestations, leading to economic and social burden worldwide. Nevertheless, there are no approved antiviral drugs to treat these infections. Zafirlukast is an orally available Food and Drug Administration (FDA) approved drug for the prophylaxis and treatment of chronic asthma. It is a leukotriene receptor antagonist (LTRA) with high selectivity of the cysteinyl leukotriene‐1 receptor (CYSLTR1) that acts as an immune modulator. Thus, we evaluated the antiviral potential of Zafirlukast against ZIKV and DENV in SK‐N‐SH cells. We showed that Zafirlukast exhibited potent antiviral activity against ZIKV, which could be linked to Zafirlukast's immune blockade of TNF signaling pathways and its downstream signaling pathways such as MAPK and ERK1/2. In addition, our results showed that Zafirlukast also counteracts ZIKV‐induced changes in key genes involved in cellular lipid metabolism. Thus, these findings highlight the translational potential of optimizing Zafirlukast as a therapeutic agent for the treatment of ZIKV and DENV.
2024-12-01TOXICOLOGY
ToxProfiler: A novel human-based reporter assay for in vitro chemical safety assessment
Article
作者: Hendriks, Giel ; Ter Braak, Bas ; Jamalpoor, Amer ; ter Braak, Bas ; Loonstra-Wolters, Liesanne ; Elbertse, Kim ; Osterlund, Torben
In vitro chemical safety assessment often relies on simple and general cytotoxicity endpoint measurements and fails to adequately predict human toxicity. To improve the in vitro chemical safety assessment, it is important to understand the underlying mechanisms of toxicity. Here we introduce ToxProfiler, a novel human-based reporter assay that quantifies the chemical-induced stress responses at a single-cell level and reveals the toxicological mode-of-action (MoA) of novel drugs and chemicals. The assay accurately measures the activation of seven major cellular stress response pathways (oxidative stress, cell cycle stress, endoplasmic reticulum stress, ion stress, protein stress, autophagy and inflammation) that play a role in the adaptive responses prior to cellular toxicity. To assess the applicability of the assay in predicting the toxicity MoA of chemicals, we tested a set of 100 chemicals with well-known in vitro and in vivo toxicological profiles. Concentration response modeling and point-of-departure estimation for each reporter protein allowed for chemical potency ranking and revealed the primary toxicological MoA of chemicals. Furthermore, the assay could effectively group chemicals based on their shared toxicity signatures and link them to specific toxicological targets, e.g. mitochondrial toxicity and genotoxicity, and different human pathologies, including liver toxicity and cardiotoxicity. Overall, ToxProfiler is a quantitative in vitro reporter assay that can accurately provide insight into the toxicological MoA of compounds, thereby assisting in the future mechanism-based safety assessment of chemicals.
2024-11-01ANALYTICAL BIOCHEMISTRY
Identification of potential inhibitors for drug resistance in acute lymphoblastic leukemia through differentially expressed gene analysis and in silico screening
Article
作者: Ayna Duran, Gizem ; Kiraz, Yağmur ; Tükel, Ezgi Yağmur ; Özay, Başak
Acute lymphoblastic leukemia (ALL) is a disease of lymphocyte origin predominantly diagnosed in children. While its 5-year survival rate is high, resistance to chemotherapy drugs is still an obstacle. Our aim is to determine differentially expressed genes (DEGs) related to Asparaginase, Daunorubicin, Prednisolone, and Vincristine resistance and identify potential inhibitors via docking. Three datasets were accessed from the Gene Expression Omnibus database; GSE635, GSE19143, and GSE22529. The microarray data was analyzed using R4.2.0 and Bioconductor packages, and pathway and protein-protein interaction analysis were performed. We identified 1294 upregulated DEGs, with 12 genes consistently upregulated in all four resistant groups. KEGG analysis revealed an association with the PI3K-Akt pathway. Among DEGs, 33 hub genes including MDM2 and USP7 were pinpointed. Within common genes, CLDN9 and HS3ST3A1 were subjected to molecular docking against 3556 molecules. Following ADMET analysis, three drugs emerged as potential inhibitors: Flunarizine, Talniflumate, and Eltrombopag. Molecular dynamics analysis for HS3ST3A1 indicated all candidates had the potential to overcome drug resistance, Eltrombopag displaying particularly promising results. This study promotes a further understanding of drug resistance in ALL, introducing novel genes for consideration in diagnostic screening. It also presents potential inhibitor candidates to tackle drug resistance through repurposing.
100 项与 扎鲁司特 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 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) | 窪觸鬱鏇壓選齋膚醖齋(艱鹽範齋廠繭範鹽鑰選) = 築遞築壓襯夢遞範網廠 願醖壓鑰鏇觸網積廠鹹 (衊壓製鏇鏇鬱壓淵鑰選, 餘齋壓醖餘鑰築壓網廠 ~ 餘鏇膚夢壓膚壓齋選膚) 更多 | - | 2019-10-01 | ||
Standard of Care (no intervention) (Standard of Care (no Intervention)) | 窪觸鬱鏇壓選齋膚醖齋(艱鹽範齋廠繭範鹽鑰選) = 衊鏇築齋網積膚選繭顧 願醖壓鑰鏇觸網積廠鹹 (衊壓製鏇鏇鬱壓淵鑰選, 築壓鑰齋窪糧選餘鹽範 ~ 淵繭衊夢觸選膚夢網網) 更多 |
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