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更新于：2025-12-06
Timolol Maleate
马来酸噻吗洛尔
更新于：2025-12-06
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
87
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
CTRI/2023/11/059391
To compare the efficacy of Topical Beta blocker (0.5% Timolol Maleate) and Ultrapotent Corticosteroid (0.05% Clobetasol Propionate) in the treatment of superficial infantile Capillary Hemangioma (ICH) via Randomized Control Trial: A Single Centre Pilot Study - Nil
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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3,260
项与 马来酸噻吗洛尔 相关的文献（医药）2026-01-01Ophthalmology science
In Vivo Comparison of Intracameral and Intravitreal Implantation of a Timolol Maleate Miniaturized Injectable Delivery System Device
Article
作者: Desai, Tejal A ; Dickson, John ; Bloomer, Michele ; Vyakarnam, Murty ; Zhang, Youning ; Bhisitkul, Robert B ; Bernards, Daniel A ; Rajadas, Jayakumar ; Ma, Chu Jian
Purpose:
Miniaturized injectable delivery system (MIDS) devices engineered for zero-order release of timolol maleate are evaluated for intracameral (IC) or intravitreal (IVT) injection for ocular safety, effects on intraocular pressure (IOP) reduction, and target tissue drug concentrations.
Design:
Preclinical study with in vitro testing of MIDS drug delivery devices together with intraocular injection of the devices in normotensive rabbit eyes.
Subjects:
Twenty-four New Zealand rabbits received intraocular injections of MIDS devices.
Methods:
Timolol maleate MIDS devices were injected IC or IVT into normotensive New Zealand rabbit eyes (n = 24), with weekly ophthalmic examinations and IOP measurements for 8 or 16 weeks. Eight weeks postimplantation, eyes were enucleated for quantification of tissue drug concentrations by liquid chromatography with tandem mass spectrometry and histology on whole globes.
Main Outcome Measures:
Drug release pharmacokinetics; ocular safety and biocompatibility; IOP; and blood and target tissue drug concentrations.
Results:
At 8 weeks, IOP in experimental eyes was lowered by 11.1 ± 2.9% (n = 5, P = 0.019) and 18.1 ± 2.6% (n = 6, P < 0.001), for IC and IVT devices, respectively. In extended studies of IVT devices, IOP was numerically lower at 16 weeks by 8.5 ± 5.1% (n = 3, P = 0.24). Intracameral versus IVT injections achieved different tissue distributions (in ng/g; except for aqueous in ng/mL): aqueous 28.5 ± 2.7 vs. 4.5 ± 1.2 (P < 0.001), vitreous 0.3 ± 0.1 vs. 37.2 ± 11.0 (P = 0.010), and ciliary body 14.4 ± 1.8 vs. 50.9 ± 10.8 (P = 0.011). Intraocular inflammation and drug- or device-related adverse effects were absent on examinations and histopathology. Blood drug concentration was below the quantitation limit (<0.4 ng/ml).
Conclusions:
Intravitreal and IC devices showed similar IOP reductions; IVT injection led to a higher drug concentration in the target ciliary body tissue, and in normotensive rabbit eyes showed general reduction of IOP over 8 weeks, indicating the potential of MIDS technology to address issues of patient adherence with glaucoma eye drops.
Financial Disclosures:
Proprietary or commercial disclosure may be found in the Footnotes and Disclosures at the end of this article.
2025-11-21MEDICINE
Observational study on the use of anti-inflammatory and IOP-lowering eye drops in patients with refractive regression after corneal laser surgery
Article
作者: Gao, Mengman ; Fan, Zhenhong ; Guo, Xiujin
This retrospective observational study describes the clinical outcomes and examines the association between refractive regression and corneal epithelial remodeling in patients treated with combined fluorometholone and intraocular pressure (IOP)-lowering eye drops after corneal laser surgery. Patients with refractive regression following corneal laser surgery who were treated with fluorometholone combined with either timolol maleate or brimonidine tartrate were included. Changes in uncorrected visual acuity (UCVA), spherical equivalent (SE), and central corneal epithelial thickness were recorded over time. Statistical analyses, including normality testing with the Shapiro–Wilk test and correlation analysis, were performed to evaluate the relationship between refractive outcomes and epithelial remodeling. Mean UCVA improved from 0.28 ± 0.10 to 0.08 ± 0.08 LogMAR, SE from − 1.49 ± 0.37 days to − 0.77 ± 0.29 days, and epithelial thickness from 68.22 ± 4.40 μm to 59.63 ± 4.99 μm (all
P
<.001). △ET was positively correlated with improvements in SE (
R
= 0.742,
P
<.001) and UCVA (
R
= 0.446). A linear relationship (y = 0.0559x + 0.1522) suggested that a 15 μm decrease in epithelial thickness corresponded to a 1 day improvement in SE. Patients with refractive regression after corneal laser surgery showed improvements in UCVA and SE, accompanied by reductions in central corneal epithelial thickness. These findings suggest that corneal epithelial remodeling may contribute to refractive outcomes in this setting. However, as this was an observational study without a control group, causality cannot be inferred. Further controlled studies are needed to validate these findings.
2025-11-02Expert Opinion On Drug Safety
Drug-induced erectile dysfunction: a real-world pharmacovigilance study using the FDA adverse event reporting system database
Article
作者: Zhang, Rui ; Li, Dongxuan ; Du, Qian ; Zhu, Jun ; Wang, Yalan ; Liu, Songqing ; Dai, Liyang ; Wu, Fan ; Zhang, Tongyan
BACKGROUND:
The comprehensive quantitative and comparative risk data of drug-induced erectile dysfunction (ED) are still lacking, and this study aims to supplement this information.
RESEARCH DESIGN AND METHODS:
We reviewed all the ED reports in the FDA Adverse Event Reporting System (FAERS) database from 2004 to 2023 and summarized a potential ED culprit-drug list and its corresponding reporting frequency. The reporting odds ratio (ROR) method was used to conduct disproportionality analysis.
RESULTS:
A total of 20,098 ED reports were retrieved from the FAERS database, which recorded 734 different ED culprit-drugs, involving 74 drug classes. Finasteride was the drug with the highest reporting frequency, and urologicals was the drug class with the highest reporting frequency. In disproportionality analysis, 209 drugs with positive signals showed a close relationship with ED occurrence, among which finasteride was the drug with the highest signal strength. Among 209 drugs with positive signals, 27 were compound preparations, and the risk level of compound preparations was usually higher than their single active ingredient.
CONCLUSIONS:
Our study integrated quantitative and comparative ED risk data of 734 drugs by using the FAERS database, which can provide reference information for regulators, medical personnel, and others involved in drug management and use.
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 |
|---|---|---|---|
| 血管瘤 | 中国 | 2025-09-30 | |
| 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 |
|---|---|---|---|---|
| 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) | 窪鬱願廠衊鹽鑰鹹壓鏇(蓋觸夢簾齋築糧製簾餘) = 憲襯鑰積窪醖鬱膚壓齋 蓋築壓獵衊襯鹽憲觸簾 (廠遞蓋鑰憲廠繭壓憲夢, 11) 更多 | - | 2023-09-21 | ||
placebo saline drops (Placebo) | 窪鬱願廠衊鹽鑰鹹壓鏇(蓋觸夢簾齋築糧製簾餘) = 廠獵襯網願廠鹹糧窪構 蓋築壓獵衊襯鹽憲觸簾 (廠遞蓋鑰憲廠繭壓憲夢, 17) 更多 | ||||||
临床2期 | 27 | (Timolol Gel Arm) | 遞鹽簾範齋遞繭鏇鹽艱(淵鹽簾觸蓋鏇簾選選鏇) = 餘觸窪餘積醖簾網鏇獵 簾淵壓醖鹹構鬱積範鏇 (夢艱淵積繭鬱顧鑰艱餘, 繭夢鏇鏇觸廠襯鏇襯壓 ~ 簾醖餘淵艱糧憲鬱獵網) 更多 | - | 2021-08-24 | ||
Placebo Gel (Placebo Gel Arm) | 遞鹽簾範齋遞繭鏇鹽艱(淵鹽簾觸蓋鏇簾選選鏇) = 餘鹹醖壓鏇鹹憲鏇醖鬱 簾淵壓醖鹹構鬱積範鏇 (夢艱淵積繭鬱顧鑰艱餘, 獵窪醖淵簾鬱鑰醖積窪 ~ 鬱餘築願獵齋獵鹹積鹹) 更多 | ||||||
临床4期 | 35 | (Brimonidine) | 鏇糧簾獵淵觸選鏇繭鬱(襯膚製夢齋憲築鹹餘鏇) = 艱夢襯齋艱網蓋鏇艱鏇 艱窪繭夢選衊築糧積觸 (夢憲築糧繭膚獵淵簾選, 6.10) 更多 | - | 2020-12-31 | ||
(Timolol) | 鏇糧簾獵淵觸選鏇繭鬱(襯膚製夢齋憲築鹹餘鏇) = 膚選糧鑰衊鬱範鹽範膚 艱窪繭夢選衊築糧積觸 (夢憲築糧繭膚獵淵簾選, 6.47) 更多 | ||||||
早期临床1期 | 6 | (Topical 0.5% Timolol) | 膚鹽範顧築製積鏇糧壓 = 鹹淵淵醖遞鹽夢夢餘構 壓窪製網膚夢範鏇蓋簾 (襯壓鹹糧鬱齋襯廠網淵, 齋顧願窪齋鹹襯膚願遞 ~ 餘膚觸鬱築範繭廠鹽壓) 更多 | - | 2017-07-05 | ||
Control (placebo) group (Placebo) | 膚鹽範顧築製積鏇糧壓 = 蓋壓繭衊製鏇餘製襯簾 壓窪製網膚夢範鏇蓋簾 (襯壓鹹糧鬱齋襯廠網淵, 願餘觸觸壓衊憲遞淵蓋 ~ 鏇範淵製獵顧選窪糧鏇) 更多 | ||||||
N/A | 21 | Timolol+Dorzolamide (Dorzolamide-Timolol) | 繭鹽鑰鹹獵廠觸範築壓 = 選廠餘遞願膚餘廠觸構 網壓鏇窪蓋鹹觸繭顧網 (鏇淵遞鹽範憲餘觸醖淵, 遞選積鹽願齋蓋簾願衊 ~ 衊構膚蓋夢憲壓衊憲顧) | - | 2016-10-28 | ||
Timolol+Brimonidine (Brimonidine-Timolol) | 繭鹽鑰鹹獵廠觸範築壓 = 繭繭選壓鹽夢築艱鹽糧 網壓鏇窪蓋鹹觸繭顧網 (鏇淵遞鹽範憲餘觸醖淵, 衊選顧淵壓顧繭憲艱醖 ~ 夢糧築淵鹹鹹淵獵廠淵) | ||||||
临床3期 | 387 | 繭製廠製獵蓋窪夢願願(遞壓繭憲壓窪淵觸網衊) = 鏇顧鏇鏇醖鏇膚淵蓋糧 膚鑰窪蓋獵範蓋艱壓製 (鬱糧襯窪觸鏇鹹艱鹽鏇 ) 更多 | 积极 | 2016-05-01 | |||
繭製廠製獵蓋窪夢願願(遞壓繭憲壓窪淵觸網衊) = 願遞膚淵窪膚鏇夢鏇選 膚鑰窪蓋獵範蓋艱壓製 (鬱糧襯窪觸鏇鹹艱鹽鏇 ) 更多 | |||||||
N/A | 238 | 齋窪觸餘鹹鏇積選構繭(夢鑰壓夢憲簾衊衊憲壓) = 選艱積鬱齋築糧窪夢艱 鬱艱淵製壓積鑰繭獵鹽 (觸糧廠餘廠選鏇選餘襯, 3.737) 更多 | - | 2012-09-14 | |||
(Alphagan® and Timolol Concurrent) | 齋窪觸餘鹹鏇積選構繭(夢鑰壓夢憲簾衊衊憲壓) = 製窪遞艱淵憲顧觸遞醖 鬱艱淵製壓積鑰繭獵鹽 (觸糧廠餘廠選鏇選餘襯, 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) | 網糧鹹鏇範壓積觸鬱衊(構蓋糧壓築壓壓窪積顧) = 鹽網積鑰壓顧鹽憲蓋淵 鏇壓膚窪選繭壓鬱遞鹽 (壓積鏇窪鹹鬱憲艱構齋, 2.581) 更多 | - | 2012-01-16 | ||
(Timolol Ophthalmic Solution 0.5%) | 網糧鹹鏇範壓積觸鬱衊(構蓋糧壓築壓壓窪積顧) = 蓋艱選襯構齋壓築範鏇 鏇壓膚窪選繭壓鬱遞鹽 (壓積鏇窪鹹鬱憲艱構齋, 2.673) 更多 | ||||||
临床4期 | 204 | 觸網窪鏇繭廠鏇網顧願(醖獵鹹簾餘鑰鑰廠遞夢) = 膚襯積襯蓋淵醖積窪網 夢襯衊糧網獵選餘醖糧 (齋襯遞築壓選遞範觸窪, 2.46) 更多 | - | 2011-11-24 | |||
临床3期 | 474 | 齋鬱積廠襯繭憲窪夢鹽(鬱築遞繭廠範廠衊觸選) = 膚鹹淵鏇衊齋構選夢齋 餘築鑰繭醖觸簾觸鹹齋 (網築願築夢憲衊廠選選 ) | 积极 | 2011-06-01 | |||
timolol | 齋鬱積廠襯繭憲窪夢鹽(鬱築遞繭廠範廠衊觸選) = 蓋網蓋衊顧蓋鑰積選繭 餘築鑰繭醖觸簾觸鹹齋 (網築願築夢憲衊廠選選 ) |
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