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更新于：2025-05-16
Zafirlukast
扎鲁司特
更新于：2025-05-16
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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927
项与 扎鲁司特 相关的文献（医药）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.
2025-04-01ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY
Development of Zafirlukast Analogues for Improved Antithrombotic Activity Through Thiol Isomerase Inhibition
Article
作者: Sage, Tanya ; Szahaj, Melanie K. ; Chandrika, Nishad Thamban ; Keovilay, Justine A. ; Wurl, Sienna E. ; Garneau-Tsodikova, Sylvie ; Howard, Kaitlind C. ; Hou, Caixia ; Kennedy, Daniel R. ; Tsodikov, Oleg V. ; Gibbins, Jonathan M. ; Khan, Sabeeya ; Taylor, Kirk A.
BACKGROUND::
Thiol isomerases play essential and nonredundant roles in platelet activation, aggregation, and thrombus formation. Thiol isomerase inhibitors have the potential to overcome the 2 major drawbacks of current antithrombotic therapies, as they target both arterial and venous thrombosis without enhancing bleeding risks. Recently, a Food and Drug Administration–approved drug, zafirlukast (ZAF), was shown to be a promising pan-thiol isomerase inhibitor. The objective of this study is to develop analogues of ZAF with optimized thiol isomerase inhibition and antithrombotic activity.
METHODS::
Thirty-five ZAF analogues were tested in an insulin turbidometric assay for thiol isomerase inhibition. Analogues were tested for platelet activation, aggregation, P-selectin expression, and laser-induced thrombosis in mice and compared with the parent compound.
RESULTS::
Of the 35 analogues, 12 retained activity, with 1, compound 21, that demonstrated a greater potency than that of ZAF, 5 had a similar potency to that of ZAF, and 6 had a weaker potency. Analogues demonstrated inhibition of platelet aggregation and P-selectin expression as compared with ZAF, consistent with their potencies. ZAF and compound 21 were shown to be reversible inhibitors of thiol isomerases, and not cytotoxic to cultured, lung, liver, and kidney cells. Finally, in an in vivo assessment of thrombus formation, compound 21 was able to significantly inhibit thrombus formation without affecting bleeding times.
CONCLUSIONS::
A ZAF analogue, compound 21, with properties superior to those of ZAF was synthesized, demonstrating improved inhibition of platelet activation, aggregation, and thrombus formation as compared with the parent ZAF. This approach could yield a promising clinical candidate for treatment and prophylaxis of arterial and venous thrombosis.
2025-02-01Journal 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
Article
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 (FEV1) post-exercise following maintenance therapy. The secondary outcome focused on treatment-related adverse events (AEs).
RESULTS:
Eleven RCTs involving 1,054 patients were included. Low-dose inhaled corticosteroids (ICS)-montelukast significantly improved EIB with a mean difference (95% CI) of 14.96% (9.61, 20.31), followed by low-to-medium (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, 16.63), 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 anti-leukotrienes. Anti-leukotrienes 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. Adding anti-leukotrienes or LABA to ICS should be considered for more severe cases, with close monitoring to assess treatment response and detect potential tachyphylaxis or AEs.
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) | 醖顧夢顧積繭壓製築膚(蓋網齋艱夢憲積襯鹽鑰) = 醖願憲艱衊獵製鑰餘齋 艱築積鑰齋顧壓遞選鑰 (鹽觸構觸鏇簾壓遞襯壓, 餘積簾繭衊糧願範憲簾 ~ 壓糧獵築齋糧簾齋鏇餘) 更多 | - | 2019-10-01 | ||
Standard of Care (no intervention) (Standard of Care (no Intervention)) | 醖顧夢顧積繭壓製築膚(蓋網齋艱夢憲積襯鹽鑰) = 鬱製廠獵獵糧簾鏇醖醖 艱築積鑰齋顧壓遞選鑰 (鹽觸構觸鏇簾壓遞襯壓, 齋壓鹹簾繭鏇繭繭鏇築 ~ 構網築淵糧鹽蓋淵鹽鏇) 更多 |
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