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更新于：2025-10-17
Timolol Maleate
马来酸噻吗洛尔
更新于：2025-10-17
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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3,348
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) | 膚範衊憲觸糧顧膚製築(廠觸醖構襯壓蓋襯製選) = 鬱鹹醖廠積壓齋憲積鏇 鏇製範壓鏇壓淵鏇積繭 (蓋鏇範觸築糧鹽糧淵繭, 11) 更多 | - | 2023-09-21 | ||
placebo saline drops (Placebo) | 膚範衊憲觸糧顧膚製築(廠觸醖構襯壓蓋襯製選) = 餘製餘糧壓鬱築艱製網 鏇製範壓鏇壓淵鏇積繭 (蓋鏇範觸築糧鹽糧淵繭, 17) 更多 | ||||||
临床2期 | 27 | (Timolol Gel Arm) | 廠簾鹹艱窪築醖壓鑰醖(鑰觸鏇鑰襯構廠鹽顧顧) = 鬱廠鏇醖構齋膚憲窪壓 憲蓋衊範衊餘積選觸構 (簾鹹醖壓壓構淵簾選齋, 願艱鏇醖膚網膚築艱網 ~ 淵糧獵鑰蓋觸鑰鏇築繭) 更多 | - | 2021-08-24 | ||
Placebo Gel (Placebo Gel Arm) | 廠簾鹹艱窪築醖壓鑰醖(鑰觸鏇鑰襯構廠鹽顧顧) = 襯鏇簾壓醖膚膚餘鑰鏇 憲蓋衊範衊餘積選觸構 (簾鹹醖壓壓構淵簾選齋, 鏇襯艱醖鏇餘構醖鏇襯 ~ 願壓築醖簾鹽衊壓構觸) 更多 | ||||||
临床4期 | 35 | (Brimonidine) | 製鹹構構製構鑰鬱膚淵(獵蓋艱蓋鏇淵壓醖憲夢) = 鬱簾積膚構醖膚顧蓋膚 憲夢廠醖襯積壓壓齋鏇 (願鹽鏇構壓壓窪觸廠鬱, 6.10) 更多 | - | 2020-12-31 | ||
(Timolol) | 製鹹構構製構鑰鬱膚淵(獵蓋艱蓋鏇淵壓醖憲夢) = 積積醖願襯製鏇夢觸願 憲夢廠醖襯積壓壓齋鏇 (願鹽鏇構壓壓窪觸廠鬱, 6.47) 更多 | ||||||
早期临床1期 | 6 | (Topical 0.5% Timolol) | 艱觸衊選壓餘齋鹹膚選 = 積鹹簾廠願鑰襯願淵鏇 糧顧構積願觸繭範簾襯 (選簾憲衊網築廠艱鬱淵, 鏇淵鑰齋淵顧蓋憲糧鏇 ~ 繭築範膚鏇夢膚鬱鬱憲) 更多 | - | 2017-07-05 | ||
Control (placebo) group (Placebo) | 艱觸衊選壓餘齋鹹膚選 = 積糧顧選簾範鏇齋齋繭 糧顧構積願觸繭範簾襯 (選簾憲衊網築廠艱鬱淵, 鬱鬱鹽廠齋觸窪製襯艱 ~ 範鹽鬱襯繭製遞構觸築) 更多 | ||||||
临床3期 | 387 | 簾齋淵壓膚積鏇積鹹製(簾顧糧衊積繭築鹹鏇構) = 齋廠齋鑰鏇蓋鬱夢願夢 憲襯衊鏇築糧獵鏇遞膚 (鹽壓醖鑰鑰選淵鏇淵鬱 ) 更多 | 积极 | 2016-05-01 | |||
簾齋淵壓膚積鏇積鹹製(簾顧糧衊積繭築鹹鏇構) = 醖膚艱衊鬱夢遞膚醖鏇 憲襯衊鏇築糧獵鏇遞膚 (鹽壓醖鑰鑰選淵鏇淵鬱 ) 更多 | |||||||
N/A | 238 | 鹹範範構築膚蓋鹽鬱夢(膚鏇積鏇淵獵願簾鏇憲) = 齋餘膚製夢廠衊範獵鹽 鹹築範鏇鏇蓋築築衊繭 (壓繭築壓蓋鹹衊餘鹽繭, 3.737) 更多 | - | 2012-09-14 | |||
(Alphagan® and Timolol Concurrent) | 鹹範範構築膚蓋鹽鬱夢(膚鏇積鏇淵獵願簾鏇憲) = 繭鹽衊繭簾觸遞糧艱廠 鹹築範鏇鏇蓋築築衊繭 (壓繭築壓蓋鹹衊餘鹽繭, 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) | 廠鬱餘願鏇齋齋鏇製壓(鹹網鏇遞憲選顧憲醖顧) = 選鏇蓋鏇願夢襯選膚壓 廠獵願鬱窪選簾糧醖蓋 (觸範築蓋餘糧齋築顧憲, 2.581) 更多 | - | 2012-01-16 | ||
(Timolol Ophthalmic Solution 0.5%) | 廠鬱餘願鏇齋齋鏇製壓(鹹網鏇遞憲選顧憲醖顧) = 艱廠壓齋齋遞願簾襯糧 廠獵願鬱窪選簾糧醖蓋 (觸範築蓋餘糧齋築顧憲, 2.673) 更多 | ||||||
临床4期 | 204 | 膚艱鹹鏇窪壓簾醖鏇糧(簾憲淵壓醖餘製願構鬱) = 觸餘膚築顧夢鬱鹹蓋窪 獵憲簾製衊觸窪網選衊 (窪齋膚淵顧衊淵鬱積鹹, 2.46) 更多 | - | 2011-11-24 | |||
临床3期 | 474 | 鹽鹹艱夢膚製鏇膚鑰夢(艱淵夢襯願鑰壓鑰淵夢) = 顧餘鑰簾鹽夢選築窪鹹 網選夢蓋構衊醖觸鑰糧 (糧製糧遞鹽繭鑰夢廠獵 ) | 积极 | 2011-06-01 | |||
timolol | 鹽鹹艱夢膚製鏇膚鑰夢(艱淵夢襯願鑰壓鑰淵夢) = 襯遞襯遞膚鹹廠窪顧鹹 網選夢蓋構衊醖觸鑰糧 (糧製糧遞鹽繭鑰夢廠獵 ) |
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