预约演示
更新于：2025-07-15
Zafirlukast
扎鲁司特
更新于：2025-07-15
概要
基本信息
药物类型 小分子化药 |
别名 4-(5-cyclopentyloxycarbonylamino-1-methyl-1H-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide、cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate、Zafirlukast (JAN/USAN/INN) + [8] |
靶点 |
作用方式 拮抗剂 |
作用机制 CysLT1拮抗剂(半胱氨酰白三烯受体-1拮抗剂) |
在研适应症 |
非在研适应症- |
原研机构 |
权益机构- |
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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933
项与 扎鲁司特 相关的文献（医药）2025-07-01Journal of Allergy and Clinical Immunology-In Practice
Efficacy and Safety of Maintenance Regimens for Adolescent and Adult Asthmatics With Exercise-Induced Bronchospasm: Systematic Review and Network Meta-Analysis
Review
作者: Wongsa, Chamard ; Lumkul, Lalita ; Thongngarm, Torpong ; Vichara-Anont, Irin ; Phinyo, Phichayut
BACKGROUND:
Exercise-induced bronchospasm (EIB) commonly coexists with asthma. However, the data on the efficacy of maintenance therapies for asthma with EIB are scarce.
OBJECTIVE:
This network meta-analysis assessed the comparative efficacy and safety of maintenance regimens for asthmatics with EIB.
METHODS:
We searched PubMed, Scopus, Embase, the Cochrane Center of Controlled Trials, and Google Scholar for randomized controlled trials (RCTs) that addressed the efficacy and safety of maintenance treatments in adolescent and adult asthmatics with EIB from inception to April 2024. The primary outcome was the change in forced expiratory volume in 1 second postexercise after maintenance therapy. The secondary outcome focused on treatment-related adverse events (AEs).
RESULTS:
Eleven RCTs involving 1054 patients were included. Low-dose inhaled corticosteroid (ICS)-montelukast significantly improved EIB with a mean difference (95% confidence interval) of 14.96% (9.61, 20.31), followed by low- to medium-dose (LM-dose) ICS-salmeterol 13.7% (8.68, 18.72), high-dose ICS 13.30% (1.34, 25.26), montelukast 11.35% (5.76, 16.95), ICS-vilanterol 9.24% (4.41, 14.07), zafirlukast 8.80% (2.28, 15.32), LM-dose ICS 7.55% (3.48, 11.63), and as-needed ICS-formoterol 6.91% (2.07, 11.75). Low-dose ICS-montelukast and LM-dose ICS-salmeterol were comparably effective. There were no significant efficacy differences among ICS monotherapy, as-needed ICS-formoterol, and antileukotrienes. Antileukotrienes were inferior to ICS monotherapy in reducing asthma exacerbation. Long-acting β2-agonist (LABA)-induced tachyphylaxis may occur despite using alongside ICS.
CONCLUSION:
Low-dose ICS and as-needed ICS-formoterol were equally effective in managing asthmatics with EIB. The addition of antileukotrienes or LABA to ICS should be considered for more severe cases, with close monitoring to assess treatment response and detect potential tachyphylaxis or AEs.
2025-06-16NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
Targeting inflammation-driven tumor progression with Zafirlukast via modulation of Jagged-1/Notch-1/Hes-1, Wnt-4/β-catenin, and VEGF signaling pathways in mice.
Article
作者: Jamil, Lubna ; Salama, Lamiaa A ; El-Dessouki, Ahmed M ; Elhusseiny, Shaza M ; Farghly, Ahmed Mohamed ; Mansour, Dina F ; Ibrahim, Samar ; Hafez, Shaimaa M ; Saleh, Asmaa ; Abdoh, Hammad Yahia ; Hafez, Mohamed M ; Selim, Heba Mohammed Refat M ; Raslan, Nahed A ; Galal, Omneya ; Mahmoud, Nihal A
AIM:
This study investigated the potential of Zafirlukast, an inhibitor of cysteinyl leukotriene receptors, to suppress the progression of Solid Ehrlich Carcinoma (SEC) by modulating inflammation-driven oncogenic pathways, with a particular focus on the inhibition of the Jagged-1/Notch-1/Hes-1 and Wnt-4/β-catenin signaling pathways.
METHODS:
Fifty female Swiss albino mice were randomly assigned to one control group and four SEC-bearing groups. Zafirlukast was given orally at daily doses of 5 mg/kg and 10 mg/kg for two weeks, while doxorubicin (DOX) was administered intraperitoneally at 5 mg/kg, three times a week for two weeks. Tumor volume and weight were assessed, and hematological, histopathological, immunohistochemical, and molecular markers were analyzed using western blot, RT-PCR, and ELISA.
RESULTS:
Zafirlukast markedly reduced tumor volume and mass, with the most pronounced effect observed at the 10 mg/kg dose, by modulating inflammation-driven oncogenic pathways and restoring hematological abnormalities. Treatment with Zaf significantly reduced proinflammatory cytokines (NF-κB, IL-6, TNF-α, iNOS), oxidative stress, and angiogenic mediators (VEGF, MMP-2, MMP-9) (p < 0.01). Furthermore, it downregulated proliferation markers (Cyclin D1, PCNA) and activated pro-apoptotic signaling pathways (Tp53, Bax, Caspase-3) (p < 0.01). RT-PCR analysis confirmed the downregulation of oncogenic genes including DLL4, Jagged-1, Notch-1, Hes-1, Wnt-4, GSK3β, and β-catenin (p < 0.01). Histopathological examination revealed areas of necrosis, reduced neovascularization, and decreased tumor cell proliferation in the treated groups.
CONCLUSION:
Zafirlukast exhibits potent anti-tumor activity by targeting multiple oncogenic pathways, highlighting its potential as a therapeutic option for solid tumors and warranting further clinical investigation.
2025-06-01BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
Both carvedilol and cimetidine alleviate cisplatin-induced nephrotoxicity via downregulating OCT2
Article
作者: Jiao, Xiaoyan ; Wu, Huan ; Ning, Yichun ; Sun, Zhaoxing ; Ji, Ji ; Yu, Xiaofang ; Ding, Xiaoqiang ; Cheng, Xin ; Xu, Xiaoliang ; Lu, Min
BACKGROUND:
Cisplatin is a common chemotherapy agent for solid tumors but severe nephrotoxicity limits its application, with no effective pharmacological treatments. Organic cation transporter 2 (OCT2) is involved in cisplatin uptake in kidneys. This study aimed to find drugs with promising clinical applications that could prevent cisplatin-induced acute kidney injury (Cis-AKI) by inhibiting OCT2.
METHODS:
The mRNA level of OCT2 was examined in human induced pluripotent stem cells (iPSCs) from Cis-AKI patients and paired non-AKI patients. The association between OCT2 and Cis-AKI was investigated by HEK293FT cells and kidney organoids. We screened potential compounds exhibiting protective effects against Cis-AKI in US Food and Drug Administration-approved drugs through virtual screening and activity screening. Subsequently, we determined the effects of these compounds on OCT2 expression, cisplatin uptake, and apoptosis in cells, kidney organoids and mice. A549 and HeLa cells were adopted to observe the influence of drugs on the anti-tumor function of cisplatin.
RESULTS:
Compared to non-AKI patients, the OCT2 mRNA levels of iPSCs from Cis-AKI patients were elevated. OCT2 exhibits similar expression patterns in kidney organoids and human kidney tissues. Furthermore, the overexpression of OCT2 in kidney organoids and HEK293FT cells exacerbated the injury caused by cisplatin. Carvedilol and cimetidine were identified as potent OCT2 inhibitors by drug screening. Further analysis revealed that the pretreatment of carvedilol or cimetidine downregulated OCT2, reduced cisplatin uptake, and alleviated cisplatin-induced apoptosis, but the combination of the two drugs didn't further improve these outcomes. Additionally, carvedilol and cimetidine didn't compromise the cisplatin-induced cell death in A549 and HeLa cells.
CONCLUSION:
Our study confirmed that carvedilol and cimetidine exert protective effects against Cis-AKI by inhibiting OCT2, without altering the anti-tumor effects of cisplatin.
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) | 簾艱窪鏇繭餘築顧簾醖(醖膚鏇顧簾齋積夢鏇壓) = 餘廠艱範淵鬱積鹽觸窪 製鏇襯觸夢餘網醖製繭 (鹽鏇顧膚獵齋遞簾鹽鏇, 淵簾鹽繭遞鬱餘蓋蓋壓 ~ 夢齋齋鹽餘膚醖廠遞夢) 更多 | - | 2019-10-01 | ||
Standard of Care (no intervention) (Standard of Care (no Intervention)) | 簾艱窪鏇繭餘築顧簾醖(醖膚鏇顧簾齋積夢鏇壓) = 範艱廠鹽齋鑰觸鏇築簾 製鏇襯觸夢餘網醖製繭 (鹽鏇顧膚獵齋遞簾鹽鏇, 獵膚願衊鹹鑰膚淵顧遞 ~ 憲醖餘窪廠獵範襯鑰構) 更多 |
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