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更新于：2026-08-29
Enalaprilat
更新于：2026-08-29
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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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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1,499
项与 Enalaprilat 相关的文献（医药）2026-11-01COLLOIDS AND SURFACES B-BIOINTERFACES
Size-dependent interfacial retention of vaterite particles under tear flow: Linking hydrodynamic detachment to ocular pharmacodynamics
Article
作者: Zhu, C ; Pallaeva, T N ; Beznos, O V ; Trushina, D B ; Chen, X Z ; Artemov, V V ; Kasyanov, I A ; Popova, E V ; Bukreeva, T V ; Abalymov, A A ; Mikheev, A V ; Burmistrov, I A ; Kost, O A
Rapid precorneal clearance remains a major limitation of topical ocular therapy, yet the fundamental physical mechanisms governing particle retention under tear flow are poorly understood. Current delivery strategies primarily rely on empirical optimization of surface chemistry, while the role of particle size in interfacial stability under dynamic conditions remains largely unexplored. Here, we establish a mechanistic size-retention-pharmacodynamic framework for porous vaterite particles designed as mucoadhesive ocular drug carriers. Two structurally equivalent particle fractions were engineered: micron-sized (3.8 ± 0.5 µm) and submicron (0.65 ± 0.15 µm) particles with preserved vaterite phase stability in simulated tear fluid, porous architecture, comparable surface physicochemical properties, matched enalaprilat loading (∼5 wt%), and diffusion-controlled release kinetics. This design enabled isolation of particle size as the primary variable governing interfacial behavior. Under tear-mimicking flow on mucin-coated substrates, submicron particles exhibited ∼1.8-fold slower washout compared to micron-sized counterparts. This difference is consistent with a size-dependent balance between hydrodynamic torque and adhesive stabilization, where detachment propensity increases with particle diameter. Ex vivo corneal experiments under ∼100 × accelerated physiological tear flow revealed convergence of retention (∼10% surface coverage after 2 h), indicating a transition from physics-dominated to biology-dominated interfacial behavior on native tissue. Most importantly, these interfacial effects were associated with improved therapeutic performance in vivo. Submicron enalaprilat-loaded particles produced a more sustained intraocular pressure reduction and an approximately 2.1-fold increase in cumulative intraocular pressure-lowering effect compared to free drug, whereas micron-sized particles showed no clear improvement. Developed formulations demonstrated good cytocompatibility and excellent ocular tolerability in vitro and in vivo. Overall, this work identifies particle size as a key parameter of interfacial retention under flow and suggests that reducing hydrodynamic detachment at mucosal interfaces can enhance ocular pharmacodynamic performance without increasing the administered drug dose. The presented framework provides a basis for rational design of interface-controlled drug delivery systems beyond empirical formulation approaches.
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.
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 | 鑰積獵艱糧繭蓋鏇衊餘 = 積鏇醖遞淵選壓鑰構廠 壓艱積獵繭範獵鏇壓蓋 (壓膚夢範繭選蓋鬱鏇餘, 夢簾築窪遞壓憲艱鹽願 ~ 願鑰範膚艱築鏇糧齋積) 更多 | - | 2017-12-11 | |||
(ACEI Continuation) | 鑰積獵艱糧繭蓋鏇衊餘 = 願選範遞簾鬱製鏇遞膚 壓艱積獵繭範獵鏇壓蓋 (壓膚夢範繭選蓋鬱鏇餘, 簾遞鹽觸獵選積繭積範 ~ 膚築窪艱鬱齋膚鑰網廠) 更多 | ||||||
N/A | 30 | Head up tilt (HUT) (ARM 1) | 鏇窪膚衊憲窪糧鑰醖觸(窪淵顧築鹹蓋蓋鏇範襯) = 構簾壓蓋醖糧鏇廠鹽鹽 膚繭鏇獵窪築襯蓋齋鏇 (襯製鏇網廠願窪選淵壓, 37) 更多 | - | 2014-06-23 | ||
Head up tilt (HUT)+1.25 mg enalaprilat IV (ARM 2) | 鏇窪膚衊憲窪糧鑰醖觸(窪淵顧築鹹蓋蓋鏇範襯) = 鹽構顧衊夢壓選觸鹹膚 膚繭鏇獵窪築襯蓋齋鏇 (襯製鏇網廠願窪選淵壓, 15) 更多 |
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