贝美前列素/酒石酸溴莫尼定/噻吗洛尔(Bimatoprost/Brimonidine Tartrate/Timolol) - 药物靶点：ADRA2 x Prostanoid receptor x β-adrenoceptors_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Bimatoprost/brimonidine/timolol、Bimatoprost/timolol/brimonidine、Timolol/brimonidine/bimatoprost

靶点

ADRA2 x Prostanoid receptor x β-adrenoceptors

作用方式

激动剂、拮抗剂

作用机制

ADRA2激动剂(肾上腺素能受体α-2家族激动剂)、前列腺素类受体家族激动剂、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

在研适应症-

非在研适应症

青光眼开角型青光眼

原研机构

Allergan UC

在研机构-

非在研机构

Allergan UC

权益机构-

最高研发阶段无进展临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C15H16BrN5O6

InChIKeyQZHBYNSSDLTCRG-LREBCSMRSA-N

CAS号70359-46-5

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关联

3

项与贝美前列素/酒石酸溴莫尼定/噻吗洛尔相关的临床试验

NCT01241240

/ Completed临床3期

Safety and Efficacy of Triple Combination Therapy in Patients With Primary Open-Angle Glaucoma or Ocular Hypertension

This study will evaluate the safety and efficacy of Triple Combination Therapy compared with Fixed Combination brimonidine tartrate/timolol ophthalmic solution in patients with primary open-angle glaucoma or ocular hypertension.

开始日期2011-03-01

申办/合作机构

Allergan UC

NCT01217606

/ Completed临床3期

Safety and Efficacy of Triple Combination Therapy in Patients With Primary Open-Angle Glaucoma or Ocular Hypertension

This study will evaluate the safety and efficacy of Triple Combination Therapy compared with Fixed Combination brimonidine tartrate/timolol ophthalmic solution in patients with primary open-angle glaucoma or ocular hypertension.

开始日期2011-01-01

申办/合作机构

Allergan UC

NCT01216943

/ Completed临床3期

A Multicenter, Open-label Study to Evaluate the Safety and Efficacy of Twice-daily 0.01% Bimatoprost/0.15% Brimonidine/0.5% Timolol Ophthalmic Solution (Triple Combination) in Patients in India, Who Have Glaucoma or Ocular Hypertension With Elevated IOP, and Are on Twice-daily 0.2% Brimonidine/0.5% Timolol Ophthalmic Solution (Dual Combination) Therapy

This study will investigate the safety and efficacy of Triple Combination Therapy (bimatoprost/brimonidine tartrate/timolol fixed combination ophthalmic solution) in patients with glaucoma or ocular hypertension who have elevated intraocular pressure (IOP) on brimonidine/timolol ophthalmic solution.

开始日期2010-11-01

申办/合作机构

Allergan UC

100 项与贝美前列素/酒石酸溴莫尼定/噻吗洛尔相关的临床结果

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100 项与贝美前列素/酒石酸溴莫尼定/噻吗洛尔相关的转化医学

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100 项与贝美前列素/酒石酸溴莫尼定/噻吗洛尔相关的专利（医药）

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2

项与贝美前列素/酒石酸溴莫尼定/噻吗洛尔相关的文献（医药）

2020-02-01·Clinical Therapeutics4区 · 医学

Fixed-combination Bimatoprost/Brimonidine/Timolol in Glaucoma: A Randomized, Masked, Controlled, Phase III Study Conducted in Brazil☆

4区 · 医学

Article

作者: Della Paolera, Mauricio ; Paula, Jayter Silva ; Belfort, Rubens ; Goodkin, Margot L ; Kim, Thomas ; Chen, Michelle Y ; Lopes Silva, Marcelo Jordão

PURPOSEMany patients with open-angle glaucoma eventually require >2 medications to lower their intraocular pressure (IOP). Fixed-combination ophthalmic solutions can be advantageous in patients who require multiple medications, but the number of fixed combinations combining 3 complementary IOP-lowering agents remains limited. This study assessed the efficacy and safety of a triple fixed combination (TFC) of bimatoprost 0.01%/brimonidine 0.15%/timolol 0.5% ophthalmic solution in patients with primary open-angle glaucoma (POAG) or ocular hypertension (OHT), compared with a dual fixed combination (DFC) of brimonidine 0.2%/timolol 0.5%.METHODSPatients with a baseline IOP of 23-34 mm Hg in both eyes and no history of IOP-lowering procedures were eligible for participation in this multicenter, double-masked, randomized, Phase III study. After washout of previous treatment (if applicable), patients were randomized to receive TFC or DFC twice daily in each eye for 3 months. The primary efficacy variable was the change from baseline in mean IOP in the worse eye at week 12 in the modified intent-to-treat (mITT) population. TFC was superior to DFC if the treatment difference (TFC - DFC) favored TFC at week 12 (P ≤ 0.05; 2-sample t test). Secondary and sensitivity analyses were also performed. Safety, including adverse events, was assessed at all visits.FINDINGSThe mITT/safety population included 185 patients (TFC, n = 90; DFC, n = 95). TFC superiority was demonstrated at all postbaseline visits (all, P < 0.001) through week 12 (week 12 treatment difference: ─2.17 mm Hg; 95% CI, ─3.12 to ─1.22). While treatment-related conjunctival hyperemia was more frequent with TFC than with DFC (47.8% vs 23.2%; P < 0.001), consistent with the additional presence of bimatoprost in TFC, most cases were mild and the numbers of patient discontinuations at week 12 were similar between the TFC and DFC groups (11 [12.2%] vs 7 [7.4%] patients; P = 0.266). No unexpected adverse events were reported.IMPLICATIONSCompared with DFC, TFC provided superior IOP lowering throughout the primary efficacy period. An acceptable tolerability profile was observed through 12 months of use of TFC, offering an effective therapeutic option in patients with POAG or OHT who require multiple medications to control their IOP. Additional studies are required for the assessment of the long-term effects of TFC. ClinicalTrials.gov identifier: NCT01217606.

2017-01-01·Journal of Ophthalmology4区 · 医学

A Masked, Randomized, Phase 3 Comparison of Triple Fixed-Combination Bimatoprost/Brimonidine/Timolol versus Fixed-Combination Brimonidine/Timolol for Lowering Intraocular Pressure

4区 · 医学

ArticleOA

作者: Goodkin, Margot ; Batoosingh, Amy ; Bernstein, Paula ; Hartleben, Curt ; Parra, Juan Camilo

Objective.To evaluate the efficacy and safety of triple fixed-combination bimatoprost 0.01%/brimonidine 0.15%/timolol 0.5% (TFC) versus dual fixed-combination brimonidine 0.2%/timolol 0.5% (DFC) in primary open-angle glaucoma and ocular hypertension.Methods.Patients with intraocular pressure (IOP) ≥23 and ≤34 mmHg were randomized to twice-daily TFC or DFC. The primary variable is the change in worse eye mean IOP from baseline at week 12 (modified intent-to-treat (mITT) population). Secondary endpoints are mean IOP and mean change from baseline at weeks 1, 2, 4, 8, and 12 (mITT population). TFC superiority was demonstrated if the primary variable favored TFC (p≤0.05). Sensitivity analyses were conducted, and safety was assessed at all visits.Results.TFC (n=93) provided greater IOP reductions from baseline than DFC (n=97) at week 12 (treatment difference, 0.85 mmHg;p=0.028) and all other visits. TFC was also superior to DFC in patients with high baseline IOP (i.e., IOP ≥ 25 mmHg;p≤0.011). Conjunctival hyperemia, ocular irritation, and dry eye were reported more often with TFC (p≤0.016); however, discontinuations for ocular adverse events were similar between treatments.Conclusions.TFC demonstrated IOP-lowering benefits that outweigh the risk of predominantly mild ocular side effects, which may be particularly relevant in patients who require greater IOP lowering to prevent/delay disease progression. This trial is registered with ClinicalTrials.gov registry number:NCT01241240.

100 项与贝美前列素/酒石酸溴莫尼定/噻吗洛尔相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
开角型青光眼	临床3期	巴西	Allergan UC	2011-01-01
青光眼	临床3期	印度	Allergan UC	2010-11-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01217606 (CTgov)	临床3期	开角型青光眼	185	bimatoprost/brimonidine tartrate/timolol ophthalmic solution (Triple Combination Therapy) (Triple Combination Therapy)	遞鬱廠艱艱窪壓鹹衊簾(鹹衊願網齋蓋鏇醖衊積) = 選簾壓鑰醖窪淵築願壓鑰壓鹹壓積衊鑰鏇鹹膚 (鏇齋廠蓋淵夢鹽範積壓, 構獵淵衊鹽範積夢獵餘 ~ 築積顧鏇憲窪憲憲網壓) 更多	-	2015-11-09
				Fixed Combination 0.2% brimonidine tartrate/0.5% timolol ophthalmic solution (Combigan®)	遞鬱廠艱艱窪壓鹹衊簾(鹹衊願網齋蓋鏇醖衊積) = 壓壓夢築夢淵艱選膚願鑰壓鹹壓積衊鑰鏇鹹膚 (鏇齋廠蓋淵夢鹽範積壓, 艱淵膚憲憲壓膚襯廠鑰 ~ 齋繭蓋選夢遞遞齋選範) 更多
NCT01241240 (CTgov)	临床3期	开角型青光眼	192	bimatoprost/brimonidine tartrate/timolol ophthalmic solution (Triple Combination Therapy) (Triple Combination Therapy)	鏇夢鹽淵遞獵壓選壓獵(獵膚壓蓋餘夢膚淵憲齋) = 襯範觸廠淵窪築衊窪範築鹹壓積範鏇願蓋網鏇 (醖築鹹觸鬱衊淵鹹蓋鏇, 衊遞蓋窪觸夢製積繭觸 ~ 夢構蓋鑰簾糧艱鏇遞願) 更多	-	2014-09-10
				Fixed Combination 0.2% brimonidine tartrate/0.5% timolol ophthalmic solution (Combigan®)	鏇夢鹽淵遞獵壓選壓獵(獵膚壓蓋餘夢膚淵憲齋) = 壓選簾衊襯範觸獵遞願築鹹壓積範鏇願蓋網鏇 (醖築鹹觸鬱衊淵鹹蓋鏇, 餘網衊鹹繭遞顧獵醖鏇 ~ 簾範齋鑰鹽鏇襯憲糧夢) 更多
NCT01216943 (CTgov)	临床3期	青光眼	126	bimatoprost/brimonidine tartrate/timolol fixed combination ophthalmic solution	淵顧憲齋壓鹽鏇鹽積繭(醖艱繭壓糧憲窪膚鹽鏇) = 積壓淵構鑰膚醖鏇蓋築顧積築繭齋鏇蓋蓋齋糧 (獵選選窪艱醖鹹獵網鏇, 構獵繭築鏇鹽鹽蓋鹹餘 ~ 壓鏇醖鏇艱遞艱艱醖製) 更多	-	2013-09-19