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更新于：2026-05-30
Enalaprilat
更新于：2026-05-30
概要
基本信息
在研机构- |
权益机构- |
最高研发阶段撤市 |
首次获批日期 美国 (1988-02-09), |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C18H28N2O7 |
InChIKeyMZYVOFLIPYDBGD-MLZQUWKJSA-N |
CAS号84680-54-6 |
关联
10
项与 Enalaprilat 相关的临床试验NCT05259137
Intra-lesional ACE Inhibitor for Treatment of Hypertrophic Scars
ChiCTR1900025446
Study for the safety and effectiveness of Wen-Yang Zhen-Shuai granule in treatment of chronic heart failure (Yang deficiency and water flooding syndrome)
ChiCTR1800018841
A real world study for the treatment of acute stroke
100 项与 Enalaprilat 相关的临床结果
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100 项与 Enalaprilat 相关的转化医学
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100 项与 Enalaprilat 相关的专利（医药）
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1,171
项与 Enalaprilat 相关的文献（医药）2026-08-01JOURNAL OF PHARMACEUTICAL SCIENCES
Zeolitic imidazolate frameworks for delivery of repurposed drugs with anti-chikungunya activity
Article
作者: Deshpande, Atharva Manoj ; Polash, Shakil Ahmed ; Cherian, Sarah ; Jagtap, Rutuja ; Parashar, Deepti ; Alagarasu, Kalichamy ; Kakade, M B ; Patil, Poonam ; Shukla, Ravi
Chikungunya virus (CHIKV) is a major global concern due to its emergence and re-emergence and the lack of effective antiviral treatments. Conventional antiviral drugs struggle with poor bioavailability, rapid degradation, and cytotoxicity, limiting their effectiveness. Nanoparticle-based drug delivery systems, particularly Zeolitic Imidazolate Frameworks (ZIF-C), have shown potential in improving the therapeutic outcomes of antiviral drugs. We encapsulated four repurposed drugs - Enalaprilat, Lomibuvir, Metyrapone, and Resveratrol within ZIF-C. Cytotoxicity assay of the formulations (ZIF-C(E), ZIF-C(L), ZIF-C(M), and ZIF-C(R)) show that free Enalaprilat, Lomibuvir, Metyrapone, and Resveratrol are toxic above 1.56 µM, 6.25 µM, 200 µM, and 12.5 µM, respectively, while their ZIF-C counterparts maintain >90 % cell viability even at 50-100 µM. Antiviral studies further show that ZIF-C(E), ZIF-C(L), ZIF-C(M), and ZIF-C(R) reduce CHIKV viral titers by 3.8, 3.8, 2.9, and 3.9 logs, respectively, with reference to virus control (VC), while the free drugs Enalaprilat, Lomibuvir, Metyrapone, and Resveratrol show 0.7, 0.7, 0.01, and 0.8 log reduction, respectively. Empty ZIF-C nanoparticles exhibit negligible antiviral effects. The results suggest that encapsulation within ZIF-C nanoparticles can help improve the stability, delivery, and effectiveness of antiviral drugs. This could be a promising strategy for treating CHIKV and other viral infections.
2026-04-01Cell Reports Medicine
Enalaprilat reverses neutrophil polarization imbalance via targeting taurine-STING axis for treatment of diabetic wounds
Article
作者: Wang, Mengwen ; Mi, Bobin ; Zhao, Yanli ; Qin, Yating ; Zhao, Yanzhi ; Lu, Li ; Zhang, Shengming ; Zhong, Xiaodan ; Zha, Kangkang ; Liu, Guohui ; Liao, Jiewen ; Al-Smadi, Fawwaz ; Zhou, Juan ; Wang, Guangji ; Xiong, Yuan
Persistent inflammation derived from neutrophil activation drives delayed healing of diabetic wounds. Herein, a dissolvable alginate methacryloyl-based microneedle patch functionalized with polypeptide CFLFLFK-NH2-coupled manganese/zinc ion metal-organic framework (MnZn-MOF) loading enalaprilat (Ena) (TMZE@A-MN) is developed. Ena promotes neutrophil repolarization from pro-inflammatory N1 to anti-inflammatory N2 state by inhibiting nuclear factor (NF)-κB axis and activating Smad3 pathway, attributed to Ena-induced level elevation of taurine and subsequently STING signaling cascade suppression, thus causing macrophage phenotype switching and endothelial cell ferroptosis repression. Due to identifiable property of CFLFLFK-NH2 on neutrophil membrane receptors, the delivery system endows Ena with targeting inhibitory roles in neutrophil activation. In addition, MnZn-MOFs possess free radical-eliminating performance and can effectively combat the growth of methicillin-resistant Staphylococcus aureus and Escherichia coli. In vivo evaluation on diabetic murine and porcine wounds also demonstrates that the TMZE@A-MN accelerates wound healing process. Consequently, the targeted microneedle delivery system holds great promise for diabetic wound treatment.
2026-01-01FEBS Journal
Molecular basis of domain‐specific angiotensin I‐converting enzyme inhibition by the antihypertensive drugs enalaprilat, ramiprilat, trandolaprilat, quinaprilat and perindoprilat
Article
作者: Ramasamy, Vinasha ; Acharya, K. Ravi ; Gregory, Kyle S. ; Sturrock, Edward D.
Angiotensin I‐converting enzyme (ACE) is a dipeptidyl carboxypeptidase with two homologous catalytic domains [N‐ and C‐domains (nACE and cACE)] that can cleave a range of substrates. cACE primarily cleaves the inactive decapeptide angiotensin I into the potent vasopressor angiotensin II, whereas nACE preferentially cleaves the antifibrotic tetrapeptide
N
‐acetyl‐seryl‐aspartyl‐lysyl‐proline (Ac‐SDKP). Several ACE inhibitors, which bind to both cACE and nACE active sites, are used clinically for the treatment of hypertension; however, serious side effects are seen in ~ 20–25% of patients due to nonselective inhibition. To improve ACE inhibitor side effect profiles, the design and development of selective inhibitors of cACE or nACE is desirable for the treatment of hypertension or fibrosis. The detailed molecular basis through which the clinically available ACE inhibitors bind and inhibit cACE and nACE was unknown. Thus, in this study, we have characterised the structural and kinetic basis for the interaction between cACE and nACE with enalaprilat, ramiprilat, trandolaprilat, quinaprilat and perindoprilat. The inhibitors display nanomolar inhibition of both domains, with moderate‐to‐low cACE‐selectivity. Trandolaprilat possesses the highest affinity for both nACE and cACE, whereas quinaprilat displayed the largest cACE‐selectivity. None of the binding modes of the inhibitors extend beyond the S1–S2′ subsites to make use of the unique nACE/cACE residues that have been shown to influence domain selectivity. These findings supplement our understanding of ACE inhibition by the clinically used ACE inhibitors, and this information should be useful in the future design of more domain‐selective inhibitors for the treatment of hypertension and cardiovascular diseases.
100 项与 Enalaprilat 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D03769 | Enalaprilat |
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 |
|---|---|---|---|
| 高血压 | 美国 | 1988-02-09 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 291 | 遞積鑰積醖獵淵繭衊襯 = 衊窪構衊繭糧鏇築鑰艱 齋觸鹹鹹鑰顧繭廠窪網 (選鹽鬱襯襯觸製積憲夢, 鏇蓋餘構選淵窪觸艱鹽 ~ 窪窪鑰壓製積壓鏇壓壓) 更多 | - | 2017-12-11 | |||
(ACEI Continuation) | 遞積鑰積醖獵淵繭衊襯 = 膚憲範窪築網積襯憲願 齋觸鹹鹹鑰顧繭廠窪網 (選鹽鬱襯襯觸製積憲夢, 積膚顧顧蓋願壓網鑰獵 ~ 憲願築膚糧獵壓廠積糧) 更多 | ||||||
N/A | 30 | Head up tilt (HUT) (ARM 1) | 艱遞鬱襯觸壓鏇餘顧鏇(簾醖構遞鑰積窪選糧艱) = 壓襯糧糧壓艱鑰蓋廠齋 獵觸獵醖鹽鏇顧製夢選 (顧構夢獵廠繭鹽壓選齋, 37) 更多 | - | 2014-06-23 | ||
Head up tilt (HUT)+1.25 mg enalaprilat IV (ARM 2) | 艱遞鬱襯觸壓鏇餘顧鏇(簾醖構遞鑰積窪選糧艱) = 選鹹壓廠襯鏇憲顧憲壓 獵觸獵醖鹽鏇顧製夢選 (顧構夢獵廠繭鹽壓選齋, 15) 更多 |
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