预约演示
更新于：2026-02-28
Esflurbiprofen
艾司氟比洛芬
更新于：2026-02-28
概要
基本信息
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
登录后查看时间轴
结构/序列
分子式C15H13FO2 |
InChIKeySYTBZMRGLBWNTM-JTQLQIEISA-N |
CAS号51543-39-6 |
关联
22
项与 艾司氟比洛芬 相关的临床试验NCT07307794
Characterisation of Adhesion Performance of a Newly Developed Esflurbiprofen Topical System (EFTS) - a Phase I, Open-label Study in Healthy Subjects.
TCTR20251201010
Efficacy of Esflurbiprofen transdermal patch for postoperative pain control in elderly patients undergoing hip fracture surgery: A triple-blinded randomized controlled trial
CTR20253906
评估受试制剂艾氟洛芬贴剂与参比制剂艾氟洛芬贴剂（Loqoa Tape）作用于健康成年受试者的吸收药代动力学研究
100 项与 艾司氟比洛芬 相关的临床结果
登录后查看更多信息
100 项与 艾司氟比洛芬 相关的转化医学
登录后查看更多信息
100 项与 艾司氟比洛芬 相关的专利（医药）
登录后查看更多信息
447
项与 艾司氟比洛芬 相关的文献（医药）2026-06-01COLLOIDS AND SURFACES B-BIOINTERFACES
Enhanced transdermal delivery of S-flurbiprofen-lidocaine ionic liquid-loaded emulgel for synergistic anti-inflammation and analgesia
Article
作者: Hao, Chao ; Zhang, Guisen ; He, Jie ; Xu, Xiaqian ; Wang, Yiwen ; Gao, Lanting ; Zhang, Jian ; Wang, Chenchen ; Xie, Keke ; Zhu, Anqi
An S-flurbiprofen (SFP)-lidocaine (LDC) ionic liquid (IL)-loaded emulgel (SFP-LDC-IL-EMG) was developed for enhanced transdermal delivery and synergistic anti-inflammation and analgesia. SFP-LDC IL was synthesized from SFP and LDC at a molar ratio of 1:1, dissolved in isopropyl myristate (IPM, oil phase) and incorporated into water phase to create a nanoemulsion. The nanoemulsion was then dispersed into sodium carboxymethyl cellulose (CMC-Na) gel matrix to form the final product of SFP-LDC-IL-EMG, which was characterized via rheology, morphology and stability in detail. Rheological assessment revealed that SFP-LDC-IL-EMG was a typical elastic gel with shear-thinning behavior, which maintains comparable viscosity and gel network integrity to blank emulgel. Ex vivo transdermal delivery of SFP-LDC-IL-EMG demonstrated 8 h cumulative permeation of 931.3 ± 68.7 µg/cm2 for SFP and 1094.2 ± 91.4 µg/cm2 for LDC, representing 4.5-fold and 3.3-fold enhancements over those of SFP-EMG and LDC-EMG. The in vivo therapeutic performance of SFP-LDC-IL-EMG was evaluated in a carrageenan-induced paw edema model, which revealed potent and rapid anti-inflammation with a peak paw swelling inhibition rate of 85.9 % and superior analgesic efficacy with maximum possible effect of 94.9 %. Histopathological examination of SFP-LDC-IL-EMG-treated animals showed minimal inflammatory cell infiltration with tissue morphology closely resembling normal groups. These findings establish SFP-LDC-IL-EMG as a promising topical delivery system combining IL-mediated transdermal enhancement with synergistic pharmacological mechanisms for effective localized inflammation and pain management.
2026-03-01ACTA PHARMACOLOGICA SINICA
Esflurbiprofen exerts a fast-onset antidepressant effect by blocking SERT-nNOS interaction
Article
作者: Peng, Ye ; Wang, Sha-Sha ; Chen, Nai-Hong ; Chen, Yu-Qi ; Chu, Shi-Feng ; Wang, Wen-Fei ; Ye, Jun-Rui ; Zhou, Run ; Yuan, Ruo-Lan ; Zhang, Zhao
Selective serotonin reuptake inhibitors (SSRIs) are characterized by delayed therapeutic onset largely due to their reliance on the desensitization of 5-HT1A autoreceptors (5-HT1ARautos) within the dorsal raphe nucleus (DRN). It has been shown that dissociation of serotonin transporter (SERT) and neuronal nitric oxide synthase (nNOS) interaction selectively modulates 5-HT1ARautos, thereby facilitating fast-onset antidepressant responses. Targeting the atypical disk large/ZO-1 (PDZ) domain has been implicated in the SERT-nNOS interaction. In this study, we established a drug screening system based on mBRET combined with biological tests to find SERT-nNOS interaction blockers (SNIBs). During screening the compound libraries, 9 top candidates were found to be capable of binding to the PDZ domain of nNOS. We then identified esflurbiprofen as a promising fast-onset antidepressant candidate. Pharmacodynamic studies revealed that esflurbiprofen effectively penetrated the DRN following systemic administration. Esflurbiprofen (10, 20, 40 mg/kg, i.p., once every 4 days) dose-dependently ameliorated depressive-like behaviors in mice subjected to chronic social defeat stress (CSDS) and chronic restraint stress (CRS). In rs-fMRI analysis, we found that esflurbiprofen enhanced the functional connectivity of emotion-related neural networks in CSDS mice. We further demonstrated that esflurbiprofen disrupted the SERT-nNOS complex in the DRN, augmented membrane-associated SERT, and reduced the concentration of 5-HT in the extracellular space of the DRN. This cascade subsequently enhanced serotonergic neuronal firing through the inhibition of negative feedback mediated by 5-HT1ARautos, culminating in an augmented release of 5-HT from serotonergic neurons projecting to the prefrontal cortex and hippocampus. These results highlight the potential of esflurbiprofen to induce rapid antidepressant effects by targeting the SERT-nNOS interaction within the DRN.
2025-07-01JOURNAL OF BIOMEDICAL MATERIALS RESEARCH PART A
Development and Evaluation of an Innovative S‐Flurbiprofen‐Diethylamine Emulgel With Superior Transdermal Delivery and Analgesic Activity
Article
作者: Wang, Xingyin ; Hao, Chao ; Zhu, Xiaoqian ; Zhang, Guisen ; Zhang, Jian ; Yin, Chaoyang ; Yin, Mingyue ; Wang, Chenchen ; Xiao, Yang ; Han, Jinmeng ; Zhu, Anqi ; Zeng, Yuyu
ABSTRACT:
This study aimed to develop an innovative (S‐flurbiprofen)‐diethylamine (SFP‐DEA) emulgel formulation via incorporating SFP as the active pharmaceutical ingredient within a carbomer 940 gel matrix. SFP‐DEA emulgel was synthesized by dissolving SFP‐DEA in the aqueous phase of an oil‐in‐water (O/W) emulsion, followed by dispersion into a carbomer 940 gel matrix. The physicochemical stability of SFP‐DEA emulgel was evaluated via centrifuge, temperature swing test, high temperature, and long‐term storage at ambient conditions. Ex vivo SFP transdermal delivery of SFP‐DEA emulgel was evaluated using a Franz diffusion cell combined with excised rat skin. The in vivo analgesic activity and skin irritation test of SFP‐DEA emulgel were evaluated using a mouse knee osteoarthritis model and healthy rats, respectively. Results demonstrated that SFP‐DEA emulgel showed robust physicochemical stability and retain a final SFP content of 1.5% (w/w). Ex vivo transdermal study demonstrated that EMG5 (the emulgel optimized with laurocapram and menthol as penetration enhancers) achieved an 8‐h cumulative SFP transdermal flux of 741.28 μg/cm2 (44.23% of the administered dose), which is 27.94‐fold higher than that of Loqoa (SFP tapes). In addition, SFP‐DEA emulgel demonstrated rapid analgesic efficacy, with an 84.36% pain inhibition rate within 30 min in the osteoarthritis model, and elicited no signs of skin irritation in rats. In conclusion, the SFP‐DEA emulgel developed herein exhibits high stability, enhanced transdermal delivery, preliminary analgesic activity, and favorable safety profiles, positioning it as a promising topical therapeutic candidate.
100 项与 艾司氟比洛芬 相关的药物交易
登录后查看更多信息
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 踝损伤 | 临床3期 | 德国 | 2025-03-06 | |
| 挫伤 | 临床3期 | 德国 | 2025-02-12 | |
| 前臂损伤 | 临床3期 | 德国 | 2025-02-12 | |
| 肱骨骨折 | 临床3期 | 德国 | 2025-02-12 | |
| 疼痛 | 临床3期 | 德国 | 2025-02-12 | |
| 软组织挫伤 | 临床3期 | 德国 | 2025-02-12 | |
| 膝关节炎 | 临床3期 | 印尼 | 2018-02-05 | |
| 运动损伤 | 临床2期 | 德国 | 2021-03-25 | |
| 肌痛 | 临床2期 | 德国 | 2021-03-25 | |
| 扭伤和拉伤 | 临床2期 | 德国 | 2021-03-25 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 200 | (Active Arm) | 遞獵獵積夢醖艱築糧鑰(範觸餘簾淵簾蓋範衊淵) = 獵遞衊鏇鹽蓋餘艱獵觸 鹹選鏇製簾遞繭膚鑰廠 (獵鹽鬱構築膚蓋鬱願蓋, 11.1) 更多 | - | 2023-09-28 | ||
(Control Drug) | 遞獵獵積夢醖艱築糧鑰(範觸餘簾淵簾蓋範衊淵) = 膚鬱醖艱壓憲鬱齋窪襯 鹹選鏇製簾遞繭膚鑰廠 (獵鹽鬱構築膚蓋鬱願蓋, 11.9) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用