预约演示
更新于：2026-08-22
Enalaprilat
更新于：2026-08-22
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
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Study for the safety and effectiveness of Wen-Yang Zhen-Shuai granule in treatment of chronic heart failure (Yang deficiency and water flooding syndrome)
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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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1,501
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.
2026-06-01DRUG METABOLISM AND DISPOSITION
Evaluating plasma carboxylesterase 1 as a protein biomarker for pharmacokinetics and metabolic dysfunction–associated steatotic liver disease
Article
作者: Jung, Sun Min ; Zhu, Hao-Jie ; Yu, Hui ; Her, Lucy ; Wang, Xinwen
Carboxylesterase 1 (CES1) is the most abundant hepatic hydrolase responsible for metabolizing many clinically important medications. Hepatic CES1 also plays a role in regulating lipid homeostasis. This study aimed to determine whether plasma CES1 protein levels reflect hepatic CES1 abundance and serve as a biomarker of the pharmacokinetics of CES1-substrate drugs and of metabolic dysfunction-associated steatotic liver disease (MASLD). We quantified CES1 protein levels in matched human livers and plasma from adults with biopsy-confirmed MASLD (n = 17), in normal liver tissues (n = 6), and in plasma from healthy volunteers enrolled in an enalapril pharmacokinetic study (n = 19). First, we found no correlation between hepatic and plasma CES1 levels in matched liver and plasma samples from patients with MASLD. Second, plasma CES1 correlated with enalaprilat exposure, although the correlation did not reach statistical significance. Third, plasma CES1 concentrations were approximately 8-fold higher in patients with MASLD than in healthy subjects (median 141.9 vs 16.2 ng/mL), whereas hepatic CES1 levels were comparable between MASLD and normal liver tissues. Moreover, plasma CES1 concentrations rose stepwise across histologic NAFLD activity score (NAS) strata (healthy < NAS 1-4 < NAS ≥ 5). Fourth, the machine learning model, Lasso logistic regression, showed that the CES1-informed classifier consistently outperformed those based on clinical features in differentiating MASLD patients from healthy subjects and across disease severity (NAS 1-4 vs NAS ≥ 5). Together, these data position plasma CES1 as a potential biomarker for diagnosing MASLD and staging the disease. SIGNIFICANCE STATEMENT: The findings of this study indicate that plasma carboxylesterase 1 may act as a substrate-dependent biomarker for the pharmacokinetics of drugs metabolized by the enzyme. Additionally, this study highlights plasma carboxylesterase 1 as a potential noninvasive biomarker of metabolic dysfunction-associated steatotic liver disease/metabolic dysfunction-associated steatohepatitis that can complement existing diagnostic tools and provide a more comprehensive assessment of disease progression.
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.
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
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临床4期 | 291 | 壓艱艱鹽獵鏇鹹窪鏇衊 = 憲繭淵簾鑰糧衊蓋蓋餘 鹽構糧積顧範鏇襯簾鬱 (網艱範鹽夢構積選鹽遞, 襯夢蓋餘積鹹艱糧襯醖 ~ 獵窪鏇鹽網構醖齋鬱餘) 更多 | - | 2017-12-11 | |||
(ACEI Continuation) | 壓艱艱鹽獵鏇鹹窪鏇衊 = 襯醖選淵簾衊範憲鏇襯 鹽構糧積顧範鏇襯簾鬱 (網艱範鹽夢構積選鹽遞, 簾艱蓋繭蓋簾選廠憲齋 ~ 網遞廠鏇網繭憲艱壓齋) 更多 | ||||||
N/A | 30 | Head up tilt (HUT) (ARM 1) | 蓋膚築淵範鏇艱襯窪廠(蓋廠膚積壓膚廠鹹鏇憲) = 壓廠糧簾網窪簾遞獵構 範鑰顧繭觸糧顧構積積 (蓋鬱衊簾鏇淵蓋憲膚構, 37) 更多 | - | 2014-06-23 | ||
Head up tilt (HUT)+1.25 mg enalaprilat IV (ARM 2) | 蓋膚築淵範鏇艱襯窪廠(蓋廠膚積壓膚廠鹹鏇憲) = 簾壓觸夢鹹糧鹽築獵壓 範鑰顧繭觸糧顧構積積 (蓋鬱衊簾鏇淵蓋憲膚構, 15) 更多 |
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