预约演示
更新于：2025-08-22
Ketotifen Fumarate
富马酸酮替芬
更新于：2025-08-22
概要
基本信息
权益机构- |
最高研发阶段批准上市 |
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C23H23NO5S |
InChIKeyYNQQEYBLVYAWNX-WLHGVMLRSA-N |
CAS号34580-14-8 |
关联
37
项与 富马酸酮替芬 相关的临床试验ChiCTR2300078332
A single-center, randomized, single-blind, controlled clinical trial of combined celecoxib with ketotifen fumarate to inhibit the recurrence of stiffness after release surgery for post-traumatic elbow stiffness
ACTRN12623001119684
Effect and time course of topical ketotifen 0.025% and prednisolone sodium phosphate 0.5% on ocular serface immune cells density, morphology, dynamic behaviour ,and topographical distribution in participants with allergic conjunctivitis
NCT05616442
Ketotifen in Non-Alcoholic Fatty Liver Disease Patients
100 项与 富马酸酮替芬 相关的临床结果
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100 项与 富马酸酮替芬 相关的转化医学
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100 项与 富马酸酮替芬 相关的专利（医药）
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2,023
项与 富马酸酮替芬 相关的文献（医药）2025-12-31JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Hidden targets in dermatology:
In vitro
and
In silico
inhibitory effects of common 23 dermatologic drugs on human carbonic anhydrase isoenzymes I and II
Article
作者: Uslu, Harun ; Çıkrıkcı, Kübra ; Can, İlkay ; Gençer, Nahit
In this study, we have aimed to determine the in vitro and in silico effects of 23 frequently used dermatologic drugs on human carbonic anhydrase I (hCA I) and II (hCA II). The inhibitory effects of the drugs on hCA I and hCA II were determined by esterase methods. The most potent inhibitors were isotretinoin for hCA I (Ki= 5.75 µM) and valaciclovir for hCA II (Ki= 5.74 µM). Ketotifen (Ki= 6.98 µM), pantoprazole (Ki= 7.16 µM) and acyclovir (Ki= 7.31 µM) were also potent inhibitors for hCA I. Isotretinoin (Ki= 6.54 µM), brivudine (Ki= 7.44 µM) and fluconazole (Ki= 7.91 µM) were also potent inhibitors for hCA II. Terbinafine hydrochloride was a weak CA inhibitor for both of these isoenzymes (Ki= 20.58 µM for hCA I and 20.32 µM for hCA I). Therefore, the drug, having a weak CA inhibitory activity, may be preferred primarily in patients with a skin disease compared to the other drugs due to important physiological functions of CAs. Molecular docking studies have shown that acitretin and isotretinoin, in particular, will inhibit hCA I at lower concentrations and have higher docking scores. For hCA II, it was shown that Isotretinoin and Ketotifen would inhibit at lower concentrations and have higher placement scores.
2025-12-01IBRO Neuroscience Reports
Synergistic effects of PAR2 and TrkA exacerbate visceral hypersensitivity induced by chronic pancreatitis in rats
Article
作者: Lu, Zhijie ; Zhu, Jiao ; Liu, Zhiyun ; Wei, Kai ; Chen, Qianbo ; Qiu, Haibo ; Tao, Kunming ; Wu, Xiaodan
Background:
Abdominal pain is the most severe symptom of chronic pancreatitis. However, till date, there are only a few studies on the mechanism of pain in chronic pancreatitis. Previous research has reported that mast cells are enriched around nerve fibers and are associated with visceral pain. In this study, we aimed to investigate the molecular mechanisms by which protease-activated receptor 2 (PAR2) and tropomyosin receptor kinase A (TrkA) exacerbate pain in chronic pancreatitis.
Methods:
A chronic pancreatitis animal model was established by injecting dibutyltin dichloride into the tail vein of Wistar rats. The von Frey test was performed to evaluate pain behavior in the rats. Hematoxylin and eosin staining, western blotting, immunofluorescence histochemistry, retrograde labeling, culture of dorsal root ganglion (DRG) neurons, and whole-cell patch clamp recordings were performed to illustrate the mechanisms.
Results:
The pancreatic structures were destroyed, including inflammatory cell infiltration and acinar atrophy, and mast cells were dramatically recruited to the pancreatic tissue in chronic pancreatitis. Systemic administration of the mast cell stabilizer ketotifen alleviated chronic pancreatitis-induced visceral hypersensitivity in the Wistar rat model. In contrast, the mast cell secretagogue compound 48/80 dose-dependently exacerbated chronic pancreatitis pain. Furthermore, the number of DRG neurons projected into the pancreas was significantly increased by injecting Dil stain in chronic pancreatitis rat models and normal rats. The co-expression of PAR2 and TrkA was only observed in small-diameter DRG neurons containing transient receptor potential vanilloid 1 channel and was significantly higher than those in normal rats. Finally, we demonstrated the functional interaction between PAR2 and TrkA by whole-cell patch clamp recordings.
Conclusions:
Mast cells contribute to chronic pancreatitis pain through enrichment and degranulation. The interaction of PAR2 and TrkA exacerbates chronic pancreatitis pain, which may be a potential strategy for the treatment of chronic pancreatitis -induced visceral pain.
2025-09-01Drug Delivery and Translational Research
Nano-spanlastics-loaded dissolving microneedle patches for ketotifen fumarate: advanced strategies for allergic conjunctivitis treatment and molecular insights
Article
作者: Teaima, Mahmoud H ; Shoela, Mai S ; Sanad, Mahmoud Tarek ; Kholeif, Nada Ahmed ; El-Nabarawi, Mohamed ; Elhabal, Sammar Fathy ; Faheem, Ahmed Mohsen ; Khamis, Gehad M ; Elrefai, Mohamed Fathi Mohamed
Abstract:
Allergic conjunctivitis (AC) is the most common inflammatory disease affecting the eye's ocular surface, lid, conjunctiva, and cornea. However, effective ocular drug delivery remains challenging due to physiological barriers such as the corneal barrier. Ketotifen (KF), a widely used antihistamine and mast cell stabilizer, for treating AC and atopic asthma but belongs to the Biopharmaceutical Classification System (BCS II) have poor solubility. This study developed a multiple strategies approach for the first time, utilizing the spanlastics nano-vesicular carriers’ system (SP) containing KF using an ethanol injection method. The optimized KF-SP exhibited the smallest particle size, largest zeta-potential and entrapment efficiency ∼232.5 ± 1.9 nm, -28 ± 0.51 and 73 ± 0.02%, respectively were further incorporated into PVA/PVP polymeric dissolving microneedles (MNs) by using a micromolding technique. Scanning electron microscopy (SEM) analysis confirmed well-defined tips and morphology, and in vitro studies showed a controlled 93% cumulative release over 72 h, with a zero-order kinetic release profile, providing stable therapeutic levels. Pharmacodynamic evaluation using the Ovalbumin/Aluminium hydroxide-induced AC model demonstrated significant reductions in IgE, TNF-α, and IL-6 levels by 68.7%, 71.3%, and 67.6%, respectively, while TGF-β and IL-10 levels increased by 70.1% and 62.7% using ELISA (Enzyme-Linked Immunosorbent Assay). Gene expression analysis (IGF-1, Annexin A1, and Bcl2) further supported the therapeutic potential of this system. In this study, we proved the topical application of the multiple strategies approach KF-SP loaded PVA/PVP MNs patch offers a targeted, sustained release treatment for AC, with promising implications for prolonged ocular therapy.Graphical Abstract
100 项与 富马酸酮替芬 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 |
|---|---|---|---|
| 季节性过敏性结膜炎 | 西班牙 | 2000-10-31 | |
| 季节性过敏性结膜炎 | 瑞典 | 2000-10-31 | |
| 皮炎 | 日本 | 1986-04-30 | |
| 湿疹 | 日本 | 1986-04-30 | |
| 瘙痒 | 日本 | 1986-04-30 | |
| 荨麻疹 | 日本 | 1986-04-30 | |
| 哮喘 | 瑞士 | 1979-05-03 | |
| 慢性荨麻疹 | 瑞士 | 1979-05-03 | |
| 变应性结膜炎 | 瑞士 | 1979-05-03 | |
| 特应性皮炎 | 瑞士 | 1979-05-03 | |
| 过敏性鼻炎 | 瑞士 | 1979-05-03 |
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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3期 | 188 | (Combination) | 選築鹽願襯夢艱築糧觸(淵淵獵顧觸範糧憲襯淵) = 艱選鏇願願餘齋鏇築襯 積觸鹽構蓋顧餘觸蓋築 (鬱窪壓膚窪窪襯範壓簾, 0.1464) 更多 | - | 2025-02-14 | ||
(Ketotifen Fumarate) | 選築鹽願襯夢艱築糧觸(淵淵獵顧觸範糧憲襯淵) = 衊糧夢鹹繭鹽築廠鑰膚 積觸鹽構蓋顧餘觸蓋築 (鬱窪壓膚窪窪襯範壓簾, 0.1487) 更多 | ||||||
临床3期 | 11 | Ketotifen 1 mg twice daily | 簾齋遞夢觸鬱壓餘憲鹹(遞膚糧鏇網簾顧遞廠憲) = Ketotifen was not superior to placebo with regard to global clinical response. Only 18% of patients demonstrated a complete or near-complete clinical response. 糧觸範餘鬱鏇壓製淵醖 (願夢觸夢顧艱艱網蓋齋 ) | 不佳 | 2024-07-01 |
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