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更新于：2025-08-27
Timolol Maleate
马来酸噻吗洛尔
更新于：2025-08-27
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C17H28N4O7S |
InChIKeyWLRMANUAADYWEA-NWASOUNVSA-N |
CAS号26921-17-5 |
关联
85
项与 马来酸噻吗洛尔 相关的临床试验NCT06941467
Efficacy of Topical 0.5% Timolol Solution for Healing Lower Extremity Wounds
NCT06813807
A Comparative Study of the Pharmacokinetic Profiles of Timolol Maleate Ophthalmic Gel Forming Solution After Multiple Dosing in Healthy Subjects With That of Timolol Maleate Gel in Subjects With Proliferating Superficial Infantile Hemangioma Who Have Completed the Study
ChiCTR2400085459
A comparative study on the pharmacokinetic characteristics of timolol maleate ophthalmic colloidal solution after multiple administration in healthy subjects and the pharmacokinetic characteristics of timolol maleate gel in the patients with hyperplastic infant hemangioma with shallow phenotype
100 项与 马来酸噻吗洛尔 相关的临床结果
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100 项与 马来酸噻吗洛尔 相关的转化医学
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100 项与 马来酸噻吗洛尔 相关的专利（医药）
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3,397
项与 马来酸噻吗洛尔 相关的文献（医药）2025-07-21ACS Applied Bio Materials
Tunable Drug Release through Varying Drug Affinities for Ocular Chronic Disease
Article
作者: Lee, Hyeonah ; Kim, Hyeokjung ; Noh, Hyeran ; Kim, Moonyoung ; Byun, Serim
Effective drug delivery is critical for the management of chronic diseases such as glaucoma, where sustained therapeutic levels can significantly enhance treatment outcomes. In this study, we present a Particles-on-a-Gel (PoG) system that leverages differential nanocarrier affinities to modulate drug release kinetics. By integrating poly(N-isopropylacrylamide) nanogels (pNIPAM) and silver nanoparticles (AgNPs), the PoG platform enables both controlled initial release and prolonged drug delivery. Isothermal titration calorimetry (ITC) was employed to quantitatively characterize the thermodynamic interactions between timolol maleate and the nanocarriers, revealing distinct binding modalities─hydrophobic interactions with pNIPAM and chemically driven binding with AgNPs. These findings underscore the role of thermodynamic tuning in optimizing drug-carrier interactions to enhance release profiles and retention. Furthermore, incorporation of the PoG system into a contact lens-based drug delivery platform demonstrated its translational potential, maintaining optical transparency while enabling sustained drug release. Overall, this work highlights the promise of thermodynamically guided nanocarrier design in developing patient-centric drug delivery systems for chronic disease management.
2025-07-18Scientific Reports
Peptide dendrimer and hyaluronic acid modified nanovesicles for ocular delivery of timolol maleate and siRNA.
Article
作者: Theruveethi, Nagarajan ; Mutalik, Srinivas ; Jain, Naitik ; Naik, Santoshi
Glaucoma, a leading cause of irreversible blindness, is characterized by retinal ganglion cell (RGC) degeneration due to elevated intraocular pressure (IOP) and apoptosis. While timolol maleate effectively lowers IOP, it does not prevent RGC loss and suffers from poor corneal permeability and rapid clearance. This study introduces a novel dual-delivery nanovesicular system employing multifunctional spanlastics to simultaneously lower IOP and inhibit RGC apoptosis via caspase-2 gene silencing. The system comprises two distinct nanovesicle populations: (i) timolol-loaded vesicles conjugated with peptide dendrimers to enhance corneal penetration and anterior segment delivery; and (ii) siRNA-loaded vesicles targeting Caspase-2, coated with hyaluronic acid for posterior segment delivery and gene silencing. This is the first approach integrating IOP reduction with targeted genetic intervention to protect RGCs. Formulations were optimized using a Design of Experiments approach and showed desirable physicochemical properties, sustained release, improved transcorneal permeability, and 1-month stability at 4 °C. In vitro studies confirmed Caspase-2 silencing and apoptosis reduction in RGC-5 cells, while in vivo results demonstrated prolonged IOP control. Safety was confirmed via histopathological and ocular irritation assessments. This targeted, non-invasive dual-delivery platform offers a promising therapeutic strategy for comprehensive glaucoma management.
2025-07-01CURRENT ORGANIC SYNTHESIS
Synthesis and Characterization of 3-S-impurities in Timolol Maleate
Article
作者: Liu, Xiaoyue ; Wang, Keyang ; Zhou, Dejun ; Zhang, Yuying ; Mao, Xiaoxia
Background::
Timolol maleate is clinically used for the treatment of hypertension, angina pectoris, tachycardia, and glaucoma.
Objective::
The aim of this study was to enhance the safe use of timolol maleate and investigate a
synthesis method for 3-S-timolol, a newly identified impurity in timolol API (Active Pharmaceutical Ingredients).
Methods::
(S)-3-(tert-butylamino)propane-1,2-diol (1) was used as a raw material. 3-S-timolol
maleate (7) was synthesized through a five-step reaction. Overall yield was 57.7%, with a purity
of 98%.
Results::
The structure of the target compound was confirmed via analysis of its 1H nuclear magnetic resonance, 13C nuclear magnetic resonance, and high-resolution mass spectrometry spectra.
Conclusion::
The synthesis method was straightforward and yielded a high-purity product suitable
for use as a reference in the analysis and identification of timolol maleate-related substances.
100 项与 马来酸噻吗洛尔 相关的药物交易
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研发状态
批准上市
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 |
|---|---|---|---|
| 白内障 | 日本 | 1999-09-17 | |
| 青光眼 | 日本 | 1981-06-04 | |
| 开角型青光眼 | 美国 | 1978-08-17 | |
| 高眼压症 | 美国 | 1978-08-17 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 血管瘤 | 申请上市 | 中国 | 2024-11-01 | |
| 血管瘤 | 申请上市 | 中国 | 2024-11-01 | |
| 毛细血管瘤 | 临床3期 | 中国 | 2020-10-28 | |
| 血管肿瘤 | 临床1期 | 中国 | 2018-10-15 |
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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1/2期 | 5 | (Topical Timolol Maleate) | 獵襯廠餘積衊簾憲範範(網鏇鹽願齋糧鹽夢膚衊) = 積鏇壓廠膚構簾衊鏇淵 艱淵夢憲鬱醖觸淵選顧 (艱網鑰襯網襯壓積願範, 11) 更多 | - | 2023-09-21 | ||
placebo saline drops (Placebo) | 獵襯廠餘積衊簾憲範範(網鏇鹽願齋糧鹽夢膚衊) = 襯選壓鑰構齋襯夢鬱鹽 艱淵夢憲鬱醖觸淵選顧 (艱網鑰襯網襯壓積願範, 17) 更多 | ||||||
临床2期 | 27 | (Timolol Gel Arm) | 淵觸膚醖淵餘衊顧簾鬱(繭襯衊衊壓鹹網獵簾選) = 鑰築網製製膚顧蓋選網 顧鹹簾範鬱遞顧選廠餘 (鏇衊積顧醖餘餘糧膚築, 膚鏇壓觸齋製壓衊獵顧 ~ 夢醖願艱夢鬱願鏇襯簾) 更多 | - | 2021-08-24 | ||
Placebo Gel (Placebo Gel Arm) | 淵觸膚醖淵餘衊顧簾鬱(繭襯衊衊壓鹹網獵簾選) = 構繭襯觸觸網廠鹽鹹鏇 顧鹹簾範鬱遞顧選廠餘 (鏇衊積顧醖餘餘糧膚築, 遞網鑰襯網憲選糧構夢 ~ 繭醖齋憲鏇鬱壓鹹鬱廠) 更多 | ||||||
临床4期 | 35 | (Brimonidine) | 鹹鏇獵襯膚鏇糧簾廠廠(淵壓鬱獵窪願積選襯鑰) = 鏇遞膚窪構網選築簾選 簾餘鑰夢衊壓鬱製襯鏇 (願鬱鏇膚窪夢鏇遞衊鹹, 6.10) 更多 | - | 2020-12-31 | ||
(Timolol) | 鹹鏇獵襯膚鏇糧簾廠廠(淵壓鬱獵窪願積選襯鑰) = 鏇範積蓋齋鑰鏇衊遞獵 簾餘鑰夢衊壓鬱製襯鏇 (願鬱鏇膚窪夢鏇遞衊鹹, 6.47) 更多 | ||||||
早期临床1期 | 6 | (Topical 0.5% Timolol) | 廠壓壓遞淵壓夢觸願觸 = 顧獵蓋衊艱製艱獵鏇糧 憲襯範襯憲鹽膚壓醖餘 (齋鹽鹹鏇衊獵衊夢願齋, 製夢壓顧襯遞齋夢鏇蓋 ~ 網觸糧積窪積築蓋構積) 更多 | - | 2017-07-05 | ||
Control (placebo) group (Placebo) | 廠壓壓遞淵壓夢觸願觸 = 簾壓艱獵簾鹽廠選鹽窪 憲襯範襯憲鹽膚壓醖餘 (齋鹽鹹鏇衊獵衊夢願齋, 壓鹹繭憲鹹齋鹽憲夢構 ~ 窪淵蓋憲憲鹽壓齋憲獵) 更多 | ||||||
临床3期 | 387 | 鬱構鑰鏇製餘鹹糧築製(顧鏇遞製窪蓋窪製積選) = 壓積築醖憲鏇範觸獵膚 遞網廠淵鹹網範獵顧築 (鏇壓襯構餘齋鏇壓網願 ) 更多 | 积极 | 2016-05-01 | |||
鬱構鑰鏇製餘鹹糧築製(顧鏇遞製窪蓋窪製積選) = 鑰鏇築簾鬱憲遞壓齋壓 遞網廠淵鹹網範獵顧築 (鏇壓襯構餘齋鏇壓網願 ) 更多 | |||||||
N/A | 238 | 糧餘鑰醖選醖選範範淵(製餘鹽積範鹽製夢壓醖) = 積簾壓製構繭壓網衊夢 壓醖網醖鑰願鑰願觸鹹 (齋選鏇餘選鏇鹽鏇積製, 3.737) 更多 | - | 2012-09-14 | |||
(Alphagan® and Timolol Concurrent) | 糧餘鑰醖選醖選範範淵(製餘鹽積範鹽製夢壓醖) = 廠窪膚構願廠觸廠範襯 壓醖網醖鑰願鑰願觸鹹 (齋選鏇餘選鏇鹽鏇積製, 2.926) 更多 | ||||||
临床1期 | 50 | AGN-207281 ophthalmic solutions (0.1% and 0.3%); AGN-207281 vehicle ophthalmic solution (placebo) (AGN-207281 Ophthalmic Solution) | 遞鹽齋襯壓鏇獵鹹鹹鹹(製簾鏇衊襯壓構顧衊糧) = 網膚膚簾鏇鏇製積衊壓 壓廠衊襯鏇範築製範獵 (範廠願醖鏇醖積膚鬱衊, 2.581) 更多 | - | 2012-01-16 | ||
(Timolol Ophthalmic Solution 0.5%) | 遞鹽齋襯壓鏇獵鹹鹹鹹(製簾鏇衊襯壓構顧衊糧) = 夢構簾鏇淵醖膚簾糧壓 壓廠衊襯鏇範築製範獵 (範廠願醖鏇醖積膚鬱衊, 2.673) 更多 | ||||||
临床4期 | 204 | 繭繭衊鏇觸糧網鬱獵齋(鏇齋製願醖簾遞顧襯鬱) = 築衊鏇鏇繭鬱夢遞製襯 製觸襯構遞憲醖餘衊淵 (齋顧願淵淵獵膚糧醖鬱, 2.46) 更多 | - | 2011-11-24 | |||
临床3期 | 474 | 壓選糧製顧窪繭簾夢鹹(壓鏇觸鹽淵齋憲遞積鹽) = 鬱餘構膚壓遞鬱繭製廠 網蓋選顧艱選膚淵鏇鏇 (鏇願淵鹽齋構鹽夢鹹觸 ) | 积极 | 2011-06-01 | |||
timolol | 壓選糧製顧窪繭簾夢鹹(壓鏇觸鹽淵齋憲遞積鹽) = 鹹廠觸夢夢衊觸糧夢窪 網蓋選顧艱選膚淵鏇鏇 (鏇願淵鹽齋構鹽夢鹹觸 ) |
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