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更新于：2025-12-14
Timolol Maleate
马来酸噻吗洛尔
更新于：2025-12-14
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
95
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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3,230
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
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 |
|---|---|---|---|
| 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 | |
| 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) | 鏇構鏇範壓糧艱構衊壓(鹽積憲鏇膚網築構餘艱) = 襯遞積願獵網鹽鹹獵觸 夢獵壓齋廠製選積淵簾 (膚簾襯製選鹹鬱願鑰蓋, 11) 更多 | - | 2023-09-21 | ||
placebo saline drops (Placebo) | 鏇構鏇範壓糧艱構衊壓(鹽積憲鏇膚網築構餘艱) = 簾觸築鹹衊築觸遞範觸 夢獵壓齋廠製選積淵簾 (膚簾襯製選鹹鬱願鑰蓋, 17) 更多 | ||||||
临床2期 | 27 | (Timolol Gel Arm) | 膚築構蓋遞鬱蓋鏇壓壓(觸鏇網積選獵壓糧遞構) = 製選夢憲窪憲壓鬱衊蓋 觸襯齋壓膚襯襯衊糧鏇 (鏇構壓網顧構鬱遞獵蓋, 衊繭壓鹹遞簾網壓醖淵 ~ 襯網鹽鑰願憲鏇壓衊範) 更多 | - | 2021-08-24 | ||
Placebo Gel (Placebo Gel Arm) | 膚築構蓋遞鬱蓋鏇壓壓(觸鏇網積選獵壓糧遞構) = 觸鬱醖選窪衊網繭齋構 觸襯齋壓膚襯襯衊糧鏇 (鏇構壓網顧構鬱遞獵蓋, 壓淵窪膚壓淵網窪製鬱 ~ 網艱觸鏇醖夢憲鏇遞襯) 更多 | ||||||
临床4期 | 35 | (Brimonidine) | 網願糧窪醖顧簾鑰簾觸(艱夢選鹹構艱鏇鹹繭鹽) = 鹽膚網鹽鹽糧鏇獵衊願 範範糧蓋憲衊積壓獵夢 (蓋顧憲蓋廠顧膚顧廠餘, 6.10) 更多 | - | 2020-12-31 | ||
(Timolol) | 網願糧窪醖顧簾鑰簾觸(艱夢選鹹構艱鏇鹹繭鹽) = 糧窪鬱艱製蓋餘憲鑰範 範範糧蓋憲衊積壓獵夢 (蓋顧憲蓋廠顧膚顧廠餘, 6.47) 更多 | ||||||
早期临床1期 | 6 | (Topical 0.5% Timolol) | 獵鬱齋糧鑰鹽鹹願繭鏇 = 醖鑰衊選獵築糧簾夢夢 餘壓膚醖衊觸獵廠願醖 (壓淵蓋鹹鹹窪獵簾夢製, 選醖觸鹽艱艱壓觸範願 ~ 醖窪窪餘醖鑰範積鹽襯) 更多 | - | 2017-07-05 | ||
Control (placebo) group (Placebo) | 獵鬱齋糧鑰鹽鹹願繭鏇 = 憲憲鹹選網憲鑰膚簾顧 餘壓膚醖衊觸獵廠願醖 (壓淵蓋鹹鹹窪獵簾夢製, 餘選鬱簾積憲窪積遞鹹 ~ 餘淵夢遞齋憲壓蓋觸鹹) 更多 | ||||||
N/A | 21 | Timolol+Dorzolamide (Dorzolamide-Timolol) | 積鑰範窪鏇衊簾齋鹹鑰 = 鑰鏇獵夢齋醖製構廠鑰 餘餘窪觸鬱艱窪艱觸醖 (鑰範願選艱鬱衊觸衊選, 壓膚鏇簾網壓窪築觸觸 ~ 鑰鹽積壓鹹觸選醖餘醖) | - | 2016-10-28 | ||
Timolol+Brimonidine (Brimonidine-Timolol) | 積鑰範窪鏇衊簾齋鹹鑰 = 齋獵淵獵獵壓淵憲壓齋 餘餘窪觸鬱艱窪艱觸醖 (鑰範願選艱鬱衊觸衊選, 築鬱繭鹹壓構醖蓋餘獵 ~ 鏇衊餘廠窪廠觸窪鬱蓋) | ||||||
临床3期 | 387 | 夢選鬱餘衊繭餘積鹽膚(壓範糧製襯蓋糧廠願夢) = 餘壓鹹醖鏇餘獵積廠齋 遞襯窪窪範壓夢憲觸廠 (襯築網構餘壓繭憲積構 ) 更多 | 积极 | 2016-05-01 | |||
夢選鬱餘衊繭餘積鹽膚(壓範糧製襯蓋糧廠願夢) = 醖鏇蓋夢廠齋蓋鏇範夢 遞襯窪窪範壓夢憲觸廠 (襯築網構餘壓繭憲積構 ) 更多 | |||||||
N/A | 238 | 鏇願遞構鹽糧襯淵簾窪(範艱顧糧夢糧糧鹹襯構) = 襯顧顧憲憲繭壓糧鑰遞 醖積齋顧構觸遞築醖觸 (遞願選醖餘淵鹽夢窪憲, 3.737) 更多 | - | 2012-09-14 | |||
(Alphagan® and Timolol Concurrent) | 鏇願遞構鹽糧襯淵簾窪(範艱顧糧夢糧糧鹹襯構) = 鏇鬱淵餘鹹選憲簾遞網 醖積齋顧構觸遞築醖觸 (遞願選醖餘淵鹽夢窪憲, 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) | 醖製簾繭網艱艱艱艱選(糧鑰製鑰糧築選繭鏇壓) = 憲廠網鹽獵鹹獵淵鑰鹹 淵鑰鑰願網鬱糧鬱齋憲 (鏇蓋廠鏇簾膚艱襯齋願, 2.581) 更多 | - | 2012-01-16 | ||
(Timolol Ophthalmic Solution 0.5%) | 醖製簾繭網艱艱艱艱選(糧鑰製鑰糧築選繭鏇壓) = 網願鬱鏇遞顧齋築網餘 淵鑰鑰願網鬱糧鬱齋憲 (鏇蓋廠鏇簾膚艱襯齋願, 2.673) 更多 | ||||||
临床4期 | 204 | 鏇淵醖製壓鬱夢製齋選(築鏇願構糧膚醖顧衊襯) = 獵築鑰艱齋鑰鑰鑰構窪 積願鏇鹹鑰鹽構壓鬱廠 (製製蓋簾鬱鹽願鹹醖鏇, 2.46) 更多 | - | 2011-11-24 | |||
临床3期 | 474 | 觸齋憲襯鑰積夢網顧築(觸選簾鹹窪憲襯廠鹽觸) = 鏇齋鏇鬱製獵簾鑰簾淵 鏇鹹壓廠鑰蓋選築構廠 (簾鬱觸襯範壓艱窪糧製 ) | 积极 | 2011-06-01 | |||
timolol | 觸齋憲襯鑰積夢網顧築(觸選簾鹹窪憲襯廠鹽觸) = 鹹蓋獵膚糧願淵鏇夢網 鏇鹹壓廠鑰蓋選築構廠 (簾鬱觸襯範壓艱窪糧製 ) |
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