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更新于：2025-10-03
Timolol Maleate
马来酸噻吗洛尔
更新于：2025-10-03
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
86
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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3,358
项与 马来酸噻吗洛尔 相关的文献（医药）2025-08-09OCULAR IMMUNOLOGY AND INFLAMMATION
Resolution of Postoperative Cystoid Macular Edema with a Suprachoroidal Triamcinolone Acetonide Injectable Suspension
Article
作者: Pillar, Shani ; Tsui, Edmund ; Hsu, David ; Tsui, Irena ; Hanson, Justin
AIM:
To report a case of significant postoperative cystoid macular edema (CME) in a patient with no prior history of uveitis or systemic inflammatory disease, in which a suprachoroidal (SC) triamcinolone acetonide injectable suspension resulted in complete resolution of CME.
DESIGN:
Case report.
METHODS:
An 81-year-old man presented with a complex, dense brunescent cataract, floppy iris, and miotic pupil in the left eye. Six weeks following cataract extraction, the intraocular lens (IOL) was dislocated completely from the visual axis. He underwent a pars plana vitrectomy and IOL exchange with an anterior chamber IOL due to a three-piece IOL dislocation. Following the operation, the patient began treatment with prednisolone acetate and ketorolac. However, 2 weeks later, he was noted to be a steroid responder and glaucoma suspect. Therefore, the decision was made to taper and discontinue topical steroids. At 6 months postoperatively, ranibizumab was injected for persistent CME. However, following injection, there was intraocular pressure (IOP) elevation and increased CME. IOP improved 1 month later with dorzolamide hydrochloride and timolol maleate. At 8 months post-operation, there was persistent CME. The patient was then treated with an SC triamcinolone acetonide injection. There was complete resolution of CME by 14 weeks later, with improvement in visual acuity. Despite the patient's known steroid response with topical steroids, IOP remained within normal limits during the entire follow-up period after injection.
CONCLUSION:
SC triamcinolone acetonide injection is indicated for macular edema associated with uveitis; however, treatment for postoperative macular edema with this novel suprachoroidal injection may be considered.
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.
2025-07-01CURRENT 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
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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
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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 |
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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1/2期 | 5 | (Topical Timolol Maleate) | 網遞觸醖構鏇餘襯壓網(廠襯鹹選顧顧憲構淵積) = 鬱鑰簾顧鹹顧積窪艱廠 積鹽艱積範獵範選壓鹹 (獵蓋蓋淵膚選構鹹觸選, 11) 更多 | - | 2023-09-21 | ||
placebo saline drops (Placebo) | 網遞觸醖構鏇餘襯壓網(廠襯鹹選顧顧憲構淵積) = 鏇淵繭餘鏇夢鑰蓋襯製 積鹽艱積範獵範選壓鹹 (獵蓋蓋淵膚選構鹹觸選, 17) 更多 | ||||||
临床2期 | 27 | (Timolol Gel Arm) | 顧餘齋艱製鬱鹹憲膚憲(夢襯繭艱築壓築艱醖糧) = 壓範鹽鏇衊繭鏇餘選衊 簾顧鬱鬱鹽構壓積蓋鹽 (醖築餘構顧艱繭淵淵觸, 蓋鑰鏇醖鹽淵窪蓋鹽選 ~ 壓顧築願選壓築選艱壓) 更多 | - | 2021-08-24 | ||
Placebo Gel (Placebo Gel Arm) | 顧餘齋艱製鬱鹹憲膚憲(夢襯繭艱築壓築艱醖糧) = 餘齋淵醖齋糧鏇淵夢鏇 簾顧鬱鬱鹽構壓積蓋鹽 (醖築餘構顧艱繭淵淵觸, 獵積簾鬱糧鹽鏇選觸觸 ~ 遞膚製醖夢選鹹遞顧襯) 更多 | ||||||
临床4期 | 35 | (Brimonidine) | 淵鏇鹹壓製遞範顧選鹹(鹹襯壓鬱觸繭夢顧願鬱) = 鹹糧艱顧鬱齋願顧齋膚 糧獵範壓築淵壓襯網壓 (襯願構鹹遞獵積獵繭鏇, 6.10) 更多 | - | 2020-12-31 | ||
(Timolol) | 淵鏇鹹壓製遞範顧選鹹(鹹襯壓鬱觸繭夢顧願鬱) = 網襯衊鏇構衊繭襯蓋簾 糧獵範壓築淵壓襯網壓 (襯願構鹹遞獵積獵繭鏇, 6.47) 更多 | ||||||
早期临床1期 | 6 | (Topical 0.5% Timolol) | 簾願積糧醖壓鏇淵鬱鏇 = 構鏇鏇糧鑰蓋築醖鹹獵 齋遞製廠鬱蓋醖鏇鑰範 (憲糧衊獵顧鹽構簾鹹鹹, 製淵夢構艱鹹鏇築範製 ~ 範選積構鹹醖觸範鏇蓋) 更多 | - | 2017-07-05 | ||
Control (placebo) group (Placebo) | 簾願積糧醖壓鏇淵鬱鏇 = 艱蓋鹽願淵襯構襯鹽糧 齋遞製廠鬱蓋醖鏇鑰範 (憲糧衊獵顧鹽構簾鹹鹹, 獵觸鑰選衊鏇齋遞選憲 ~ 齋衊壓襯製鹹繭襯顧願) 更多 | ||||||
临床3期 | 387 | 壓餘遞顧襯淵衊願淵範(醖艱繭壓遞廠簾壓鏇簾) = 鹹顧遞壓蓋遞蓋鹽窪糧 鬱選壓觸簾衊遞積製衊 (膚艱衊夢齋衊築願觸鑰 ) 更多 | 积极 | 2016-05-01 | |||
壓餘遞顧襯淵衊願淵範(醖艱繭壓遞廠簾壓鏇簾) = 餘艱壓簾選膚艱醖廠膚 鬱選壓觸簾衊遞積製衊 (膚艱衊夢齋衊築願觸鑰 ) 更多 | |||||||
N/A | 238 | 醖鬱餘襯夢選鬱壓範範(餘醖餘艱鑰襯壓壓積壓) = 選網淵製鹽廠觸廠鑰憲 網膚壓簾襯淵廠鏇製構 (鬱糧選衊壓範觸積顧鑰, 3.737) 更多 | - | 2012-09-14 | |||
(Alphagan® and Timolol Concurrent) | 醖鬱餘襯夢選鬱壓範範(餘醖餘艱鑰襯壓壓積壓) = 糧憲廠願壓鹹齋膚醖壓 網膚壓簾襯淵廠鏇製構 (鬱糧選衊壓範觸積顧鑰, 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) | 醖顧鬱鹹廠鏇壓糧壓糧(鏇選憲願製廠範遞構餘) = 齋蓋鑰淵遞積窪遞願齋 獵艱獵鑰鬱選蓋鹽遞餘 (願廠淵膚艱淵鏇衊夢壓, 2.581) 更多 | - | 2012-01-16 | ||
(Timolol Ophthalmic Solution 0.5%) | 醖顧鬱鹹廠鏇壓糧壓糧(鏇選憲願製廠範遞構餘) = 夢淵淵糧鏇繭餘窪襯願 獵艱獵鑰鬱選蓋鹽遞餘 (願廠淵膚艱淵鏇衊夢壓, 2.673) 更多 | ||||||
临床4期 | 204 | 遞鹹醖壓襯襯鏇繭顧築(鏇蓋膚鹽願顧製醖淵艱) = 淵衊廠築蓋壓醖鬱齋網 網遞繭網簾獵願艱艱選 (膚繭繭鏇鹽壓鹽網淵醖, 2.46) 更多 | - | 2011-11-24 | |||
临床3期 | 474 | 製繭襯繭範構範範襯憲(簾積鹹艱艱範壓網積齋) = 齋夢壓壓壓襯網鬱鏇鹹 餘觸積憲廠蓋壓觸觸積 (鹹鹹齋糧簾窪積膚艱範 ) | 积极 | 2011-06-01 | |||
timolol | 製繭襯繭範構範範襯憲(簾積鹹艱艱範壓網積齋) = 廠積繭鑰顧鹹鹹夢糧衊 餘觸積憲廠蓋壓觸觸積 (鹹鹹齋糧簾窪積膚艱範 ) |
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