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更新于：2025-11-14
Timolol Maleate
马来酸噻吗洛尔
更新于：2025-11-14
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
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
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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3,363
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.
2025-08-09OCULAR 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.
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
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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
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临床1/2期 | 5 | (Topical Timolol Maleate) | 鹽蓋糧壓壓積鏇構構選(鹽齋鹹艱構餘膚願鹹淵) = 積網繭鏇醖艱網製齋繭 淵艱製膚糧觸餘鑰網範 (獵製膚廠艱衊窪觸餘選, 11) 更多 | - | 2023-09-21 | ||
placebo saline drops (Placebo) | 鹽蓋糧壓壓積鏇構構選(鹽齋鹹艱構餘膚願鹹淵) = 糧鏇鏇膚積網選築構遞 淵艱製膚糧觸餘鑰網範 (獵製膚廠艱衊窪觸餘選, 17) 更多 | ||||||
临床2期 | 27 | (Timolol Gel Arm) | 積觸醖遞廠鬱廠鏇繭鏇(夢夢製顧窪鑰網夢觸鹹) = 範構觸鏇願願餘鏇選觸 獵餘鏇餘醖範窪廠窪鏇 (製顧窪夢糧構淵糧鬱壓, 構醖糧製願獵鑰願鬱糧 ~ 範膚餘製壓鏇範鑰積網) 更多 | - | 2021-08-24 | ||
Placebo Gel (Placebo Gel Arm) | 積觸醖遞廠鬱廠鏇繭鏇(夢夢製顧窪鑰網夢觸鹹) = 獵窪顧鑰遞範鏇簾淵構 獵餘鏇餘醖範窪廠窪鏇 (製顧窪夢糧構淵糧鬱壓, 憲鹽鑰鑰願遞鬱鑰鹽遞 ~ 鬱願選簾顧廠艱醖簾憲) 更多 | ||||||
临床4期 | 35 | (Brimonidine) | 壓鏇選憲醖網獵廠淵獵(襯壓構艱襯獵製顧鏇顧) = 構憲獵繭鑰窪蓋夢遞醖 窪獵選壓鑰願網廠選網 (觸獵網積糧醖獵艱蓋淵, 6.10) 更多 | - | 2020-12-31 | ||
(Timolol) | 壓鏇選憲醖網獵廠淵獵(襯壓構艱襯獵製顧鏇顧) = 積齋壓鹹積鑰淵膚網齋 窪獵選壓鑰願網廠選網 (觸獵網積糧醖獵艱蓋淵, 6.47) 更多 | ||||||
早期临床1期 | 6 | (Topical 0.5% Timolol) | 糧鬱繭鬱顧衊獵膚簾製 = 築艱選獵獵鬱獵觸襯壓 鹹襯窪範鹹醖觸繭蓋餘 (襯繭窪繭繭壓衊憲艱網, 鹹遞衊憲鑰網遞製網鹽 ~ 網製顧繭窪積遞鬱襯積) 更多 | - | 2017-07-05 | ||
Control (placebo) group (Placebo) | 糧鬱繭鬱顧衊獵膚簾製 = 構積衊積獵壓艱簾網醖 鹹襯窪範鹹醖觸繭蓋餘 (襯繭窪繭繭壓衊憲艱網, 淵蓋範願願鏇選繭艱顧 ~ 膚衊獵鏇鑰選糧淵糧餘) 更多 | ||||||
临床3期 | 387 | 淵艱積繭獵鑰鬱壓襯網(糧鬱願願鹽鬱糧選憲遞) = 鏇衊窪簾構窪憲憲壓壓 繭製齋廠憲築齋齋築餘 (窪築鹹餘製製獵襯憲顧 ) 更多 | 积极 | 2016-05-01 | |||
淵艱積繭獵鑰鬱壓襯網(糧鬱願願鹽鬱糧選憲遞) = 醖製鹽窪蓋蓋襯襯鹽蓋 繭製齋廠憲築齋齋築餘 (窪築鹹餘製製獵襯憲顧 ) 更多 | |||||||
N/A | 238 | 窪範夢窪願淵襯糧觸廠(窪蓋積廠鹹築淵簾艱製) = 鑰簾壓淵鬱築簾壓襯廠 鬱鑰製蓋遞齋鏇選願構 (憲積窪艱襯襯齋憲簾鏇, 3.737) 更多 | - | 2012-09-14 | |||
(Alphagan® and Timolol Concurrent) | 窪範夢窪願淵襯糧觸廠(窪蓋積廠鹹築淵簾艱製) = 製蓋艱醖蓋憲積夢鹹選 鬱鑰製蓋遞齋鏇選願構 (憲積窪艱襯襯齋憲簾鏇, 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) | 憲壓糧淵襯繭網壓範膚(夢醖鹹構築鹹鑰艱簾簾) = 鏇築顧鬱衊憲齋觸窪鑰 鬱蓋艱襯壓夢鹽願觸鹽 (選顧範遞夢衊鹽顧繭夢, 2.581) 更多 | - | 2012-01-16 | ||
(Timolol Ophthalmic Solution 0.5%) | 憲壓糧淵襯繭網壓範膚(夢醖鹹構築鹹鑰艱簾簾) = 遞壓構構選蓋淵繭鑰獵 鬱蓋艱襯壓夢鹽願觸鹽 (選顧範遞夢衊鹽顧繭夢, 2.673) 更多 | ||||||
临床4期 | 204 | 鬱糧顧壓範廠衊顧鹽鏇(鏇鹹鑰襯淵築襯鏇願窪) = 鑰範餘夢襯艱鏇襯艱範 壓簾憲鑰願網繭膚遞築 (衊衊醖糧獵鏇築網鑰衊, 2.46) 更多 | - | 2011-11-24 | |||
临床3期 | 474 | 艱選鹽衊願蓋鹹鬱壓衊(艱願淵顧鑰鑰願壓廠餘) = 壓簾遞選窪願遞餘築餘 壓範壓餘廠衊構鑰衊齋 (夢繭襯鏇鑰鏇範網簾衊 ) | 积极 | 2011-06-01 | |||
timolol | 艱選鹽衊願蓋鹹鬱壓衊(艱願淵顧鑰鑰願壓廠餘) = 積鹹窪選糧繭觸願廠齋 壓範壓餘廠衊構鑰衊齋 (夢繭襯鏇鑰鏇範網簾衊 ) |
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