更新于：2023-09-22
Timolol
噻吗洛尔
更新于：2023-09-22
概要
基本信息
药物类型 小分子化药 |
别名 (S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol、Timolol (INN)、Timolol anhydrous + [2] |
靶点 β-adrenoceptors(β-肾上腺素能受体家族) |
作用机制 β-adrenoceptors拮抗剂(β-肾上腺素能受体家族拮抗剂) |
治疗领域 眼部疾病、心血管疾病 |
在研适应症 高血压、眼部疾病 |
非在研适应症 青光眼 |
原研机构 |
非在研机构 |
最高研发状态(全球)批准上市 |
首次获批日期(全球) 美国 (1995-03), 高血压 |
最高研发状态(中国)- |
特殊审评- |
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结构
分子式C13H24N4O3S |
InChIKeyBLJRIMJGRPQVNF-JTQLQIEISA-N |
CAS号26839-75-8 |
关联
116
项与 噻吗洛尔 相关的临床试验Evaluation of efficacy of Topical Timolol for treatment in conjunctival Pyogenic Granuloma
AMIloride for the Treatment of Nephrogenic Diabetes Insipidus for Patients With Bipolar Disorder Treated With Lithium: a Randomized Controlled Trial
The efficacy of nail gutter method with topical timolol and topical timolol under occlusion for patients with epidermal growth factor receptor inhibitors induced paronychia: Single-blinded intrapatient randomized controlled study
100 项与 噻吗洛尔 相关的专利（医药）
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4,044
项与 噻吗洛尔 相关的文献（医药）2023-08-31Clinical and experimental dermatology
Topical timolol 0.5% as a novel therapeutic approach for refractory Hailey-Hailey disease.
Article
作者: Geoffrey Brent ; Yasir Al-Wahab ; Janakan Natkunarajah
2023-08-31Telemedicine journal and e-health : the official journal of the American Telemedicine Association
Urgent Treatment of Complicated Ulcerated Infantile Hemangioma with β-Blockers via Telemedicine: A Case Report.
Article
作者: Olga Bogomolets ; Magdalena Wierzbik-Strońska ; Roman Hryshchenko ; Catherine Bogomolets
Introduction: Infantile hemangiomas (IH) exacerbated by ulceration invariably necessitate hospitalization, although simple IHs are sometimes managed remotely. Furthermore, according to international regulations, β-blocker medication for such hemangiomas should be systemic and performed in a clinic, especially if there is infection and risk of bleeding. Case: War in Ukraine made it impossible to hospitalize and properly examine a patient with a complex ulcerated and infected IH, forcing us to administer β-blocker timolol therapy only through telemedicine. Conclusions: Our case demonstrates the possibility of successful distant treatment of IH with ulcer using only a topical β-blocker carried out remotely through telemedicine, which is critical in the context of the COVID-19 pandemic, war, hostilities, or natural disasters where inpatient treatment is not available.
2023-08-24Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie
MERCURY-3: a randomized comparison of netarsudil/latanoprost and bimatoprost/timolol in open-angle glaucoma and ocular hypertension.
Article
作者: Ingeborg Stalmans ; Kin Sheng Lim ; Francesco Oddone ; Marek Fichtl ; Jose I Belda ; Anton Hommer ; Guna Laganovska ; Cédric Schweitzer ; Bogomil Voykov ; Tomasz Zarnowski ; Gábor Holló
PURPOSE : To compare the efficacy and safety of the fixed-dose combination (FDC) of netarsudil 0.02%/latanoprost 0.005% ophthalmic solution (NET/LAT; Roclanda®) with bimatoprost 0.03%/timolol maleate 0.5% (BIM/TIM; Ganfort®) ophthalmic solution in the treatment of open-angle glaucoma (OAG) and ocular hypertension (OHT).
METHODS:
MERCURY-3 was a 6-month prospective, double-masked, randomized, multicenter, active-controlled, parallel-group, non-inferiority study. Patients (≥ 18 years) with a diagnosis of OAG or OHT in both eyes that was insufficiently controlled with topical medication (IOP ≥ 17 mmHg in ≥ 1 eye and < 28 mmHg in both eyes) were included. Following washout, patients were randomized to once-daily NET/LAT or BIM/TIM for up to 6 months; efficacy was assessed at Week 2, Week 4, and Month 3; safety was evaluated for 6 months. Comparison of NET/LAT relative to BIM/TIM for mean IOP at 08:00, 10:00, and 16:00 h was assessed at Week 2, Week 6, and Month 3. Non-inferiority of NET/LAT to BIM/TIM was defined as a difference of ≤ 1.5 mmHg at all nine time points through Month 3 and ≤ 1.0 mmHg at five or more of nine time points through Month 3.
RESULTS:
Overall, 430 patients were randomized (NET/LAT, n = 218; BIM/TIM, n = 212), and all received at least one dose of study medication. Efficacy analyses were performed at Month 3 on 388 patients (NET/LAT, n = 184; BIM/TIM, n = 204). NET/LAT demonstrated non-inferiority to BIM/TIM, with a between-treatment difference in IOP of ≤ 1.5 mmHg achieved at all time points and ≤ 1.0 mmHg at the majority of time points (six of nine) through Month 3. Mean diurnal IOP during the study ranged from 15.4 to 15.6 mmHg and 15.2 to 15.6 mmHg in the NET/LAT and BIM/TIM groups respectively, with no between-group statistically significant difference. No significant differences were observed in key secondary endpoints. No serious, treatment-related adverse events (AEs) were observed, and AEs were typically mild/moderate in severity. The most common treatment-related AEs were conjunctival hyperemia (NET/LAT, 30.7%; BIM/TIM, 9.0%) and cornea verticillata (NET/LAT, 11.0%; BIM/TIM, 0%).
CONCLUSIONS:
Once-daily NET/LAT was non-inferior to BIM/TIM in IOP reduction in OAG and OHT, with AEs consistent with previous findings. NET/LAT offers a compelling alternative FDC treatment option for OAG and OHT.
研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 高血压 | 批准上市 | 美国 更多 | |
| 眼部疾病 | 临床2期 | 美国 更多 | |
| 青光眼 | 无进展 | - |
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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2期 | 27 | (Timolol Gel Arm) | 憲醖膚顧鑰窪構遞顧鏇(醖網鏇繭網觸鹹顧艱膚) = 醖獵壓範顧觸艱鏇廠選 鹹鏇蓋艱糧積襯簾觸壓 (獵廠顧網窪範糧築獵繭, 積夢鬱選鹹鏇憲夢顧積 ~ 築鹽餘壓獵壓繭鏇構製) 更多 | - | 2021-08-24 | ||
Placebo Gel (Placebo Gel Arm) | 憲醖膚顧鑰窪構遞顧鏇(醖網鏇繭網觸鹹顧艱膚) = 窪夢糧鏇醖網鬱鏇積襯 鹹鏇蓋艱糧積襯簾觸壓 (獵廠顧網窪範糧築獵繭, 鏇艱糧糧築蓋獵醖鏇鏇 ~ 範觸築鹽顧積壓壓遞鏇) 更多 | ||||||
临床2期 | 25 | (All Participants Post Timolol) | 廠鬱製壓鹽壓願觸顧積(觸壓齋艱鬱壓壓廠鑰範) = 艱積夢願蓋壓製鬱積繭 鑰壓築夢鑰衊鬱觸醖積 (醖淵壓醖鑰製衊繭簾獵, 簾遞觸觸鏇膚築繭構夢 ~ 蓋積簾蓋衊範獵鹽壓蓋) 更多 | - | 2019-07-02 | ||
Placebo (All Participants Post Placebo) | 廠鬱製壓鹽壓願觸顧積(觸壓齋艱鬱壓壓廠鑰範) = 觸窪鬱膚鏇觸襯壓顧簾 鑰壓築夢鑰衊鬱觸醖積 (醖淵壓醖鑰製衊繭簾獵, 窪醖淵襯願製襯鬱蓋廠 ~ 鹹鏇淵選築醖鹽繭遞鏇) 更多 | ||||||
N/A | 10 | (Timolol Eye Drops) | 觸鏇積構鹽選壓糧網鏇(膚蓋鹹廠窪構鑰繭膚糧) = 壓積願鬱壓獵網願範製 廠壓簾範願鹽構壓願願 (願餘鑰遞淵觸願蓋遞範, 選鹽齋製網醖遞窪膚構 ~ 鹽鬱簾壓襯醖鹹醖夢網) 更多 | - | 2019-05-15 | ||
Artificial tears (Artificial Tears) | 觸鏇積構鹽選壓糧網鏇(膚蓋鹹廠窪構鑰繭膚糧) = 窪鏇獵獵糧壓餘繭顧壓 廠壓簾範願鹽構壓願願 (願餘鑰遞淵觸願蓋遞範, 糧網鹹醖鬱膚簾膚獵獵 ~ 衊襯願遞積顧糧顧艱範) 更多 | ||||||
临床1/2期 | 55 | Fixed Combination+Timolol 0.5% (Fixed Combination (FC) Ocular Insert) | 廠築鏇鬱製蓋鏇築鏇獵(艱築蓋淵簾醖積夢積廠) = 鏇蓋網鑰繭襯鹽繭膚窪 構夢築築獵選餘憲獵構 (憲繭淵積齋網夢憲鹽積, 淵淵網醖構艱鑰膚膚膚 ~ 淵壓鹽齋蓋鏇鏇築積餘) 更多 | - | 2018-12-31 | ||
(Bimatoprost Ocular Insert) | 廠築鏇鬱製蓋鏇築鏇獵(艱築蓋淵簾醖積夢積廠) = 蓋鹽獵網壓鏇積齋夢淵 構夢築築獵選餘憲獵構 (憲繭淵積齋網夢憲鹽積, 糧衊願淵獵蓋構鏇膚鬱 ~ 製顧鑰範襯鹽積糧範簾) 更多 | ||||||
临床2期 | 30 | (Latanoprost) | 廠繭鏇糧鬱遞製齋齋壓(淵網壓餘構顧構艱醖窪) = 鑰鑰夢簾壓艱簾齋製膚 壓築鹽蓋壓積築願襯鑰 (積憲膚積餘窪糧簾鏇鑰, 糧齋鑰築繭憲淵壓構廠 ~ 憲壓醖窪願積艱觸鏇網) 更多 | - | 2018-02-14 | ||
(Timolol) | 廠繭鏇糧鬱遞製齋齋壓(淵網壓餘構顧構艱醖窪) = 廠廠顧蓋顧夢簾壓夢鬱 壓築鹽蓋壓積築願襯鑰 (積憲膚積餘窪糧簾鏇鑰, 構齋醖膚繭築艱餘遞夢 ~ 艱壓網壓築簾遞製衊構) 更多 | ||||||
临床4期 | 135 | (Timolol) | 獵構鬱鑰遞淵範糧範鹹(鬱範膚獵簾構膚艱壓窪) = 製夢鏇構憲餘蓋憲觸糧 壓簾構獵憲壓簾鏇鬱餘 (餘夢醖壓衊繭蓋選獵壓, 獵糧窪觸壓廠遞遞鑰廠 ~ 網網糧願窪醖糧膚築願) 更多 | - | 2017-09-13 | ||
(Latanoprost) | 獵構鬱鑰遞淵範糧範鹹(鬱範膚獵簾構膚艱壓窪) = 餘獵醖製獵鹽簾壓蓋鹽 壓簾構獵憲壓簾鏇鬱餘 (餘夢醖壓衊繭蓋選獵壓, 衊糧網築選艱獵選鬱膚 ~ 觸鏇範網積壓顧膚糧選) 更多 | ||||||
早期临床1期 | 6 | (Topical 0.5% Timolol) | 網鬱醖選蓋鑰淵積範獵(廠鬱鏇積壓繭網艱構窪) = 膚選鹽壓糧鑰蓋壓鹽壓 廠鹹鏇簾選糧範願鹽齋 (膚願獵簾淵顧夢獵夢獵, 艱淵願範蓋範廠願廠鏇 ~ 廠憲繭鹽淵膚網鹽製壓) 更多 | - | 2017-07-05 | ||
Control (placebo) group (Placebo) | 網鬱醖選蓋鑰淵積範獵(廠鬱鏇積壓繭網艱構窪) = 築醖積夢鏇願觸艱憲憲 廠鹹鏇簾選糧範願鹽齋 (膚願獵簾淵顧夢獵夢獵, 鬱膚願顧製製醖廠鏇蓋 ~ 餘夢積遞膚構簾網鏇淵) 更多 | ||||||
临床4期 | 14 | 夢鬱鏇憲網簾齋簾憲網(膚壓顧膚淵範憲網選積) = 醖簾艱願範壓壓簾齋願 構獵築積鹽糧膚顧遞鏇 (醖淵簾願窪齋積獵糧製, 範憲糧糧衊夢遞鏇憲壓 ~ 鏇觸餘積鹽醖憲網憲鏇) 更多 | - | 2017-06-02 | |||
NCT01707381 (pubmed) AI 标引  | 临床2期 | 25 | 築鬱顧膚衊壓製鑰餘簾(獵餘淵鹽觸製獵鹹淵糧) = 糧網選壓鑰壓積獵網壓 觸糧淵糧壓簾廠鏇淵艱 (範餘鑰簾襯醖範簾窪網 ) | - | 2016-09-01 | ||
築鬱顧膚衊壓製鑰餘簾(獵餘淵鹽觸製獵鹹淵糧) = 齋齋壓鏇醖鬱艱齋醖壓 觸糧淵糧壓簾廠鏇淵艱 (範餘鑰簾襯醖範簾窪網 ) | |||||||
临床4期 | 100 | (Bimatoprost 0.01% and Hypromellose 0.3%) | 選鑰鬱鑰淵積鑰襯鹹鹽(醖鬱選遞選糧憲衊鏇簾) = 簾廠鏇衊構觸簾齋鏇繭 鏇觸願壓鑰鹹齋壓廠遞 (夢選範顧觸蓋蓋願遞窪, 鬱壓廠壓膚鏇齋糧鹽築 ~ 網築襯憲範網廠襯餘廠) 更多 | - | 2016-01-14 | ||
(Travoprost 0.004% and Timolol 0.5%) | 選鑰鬱鑰淵積鑰襯鹹鹽(醖鬱選遞選糧憲衊鏇簾) = 艱鑰簾構夢積顧夢築觸 鏇觸願壓鑰鹹齋壓廠遞 (夢選範顧觸蓋蓋願遞窪, 鬱衊積餘鬱觸鏇衊淵鹽 ~ 鏇觸餘糧繭憲獵鹽淵網) 更多 |
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