拉坦噻吗(Latanoprost/Timolol Maleate) - 药物靶点：PTGFR x β-adrenoceptors_在研适应症：青光眼，开角型青光眼，高眼压症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Latanoprost and Timolol Maleate、Timolol/ Latanoprost、拉坦前列素/马来酸噻吗洛尔

+ [10]

靶点

PTGFR x β-adrenoceptors

作用机制

PTGFR激动剂(前列腺素FP受体激动剂)、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

青光眼开角型青光眼高眼压症+ [1]

非在研适应症-

原研机构

Pfizer Inc.

在研机构

Pfizer Inc.Viatris PharmaPfizer Manufacturing Belgium BV

+ [1]

非在研机构

Laboratoires Théa SAS

Viatris, Inc.

最高研发阶段批准上市

首次获批日期

瑞典 (2000-01-01),

开角型青光眼青光眼高眼压症

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

分子式C39H64N4O8S

InChIKeyOKKZZTWDFXEJAH-LRWPTBCASA-N

CAS号852336-82-4

关联

29

项与拉坦噻吗相关的临床试验

NCT04891588 / Unknown statusN/A

Evaluation of Glaucoma or Ocular Hypertension Patients With Pre-existing Ocular Surface Disease Switched From a Preserved Prostaglandin Analog - Timolol Fixed Combination to a Preservative - Free Latanoprost - Timolol Fixed Combination

Glaucoma is a group of chronic eye diseases that are characterized by a progressive optic nerve damage and consequent visual loss. In most cases, it is associated with elevated intraocular pressure. If glaucoma left untreated, complete blindness can occur. Prostaglandin analog- timolol FCs are common glaucoma therapy because these drugs have been shown to effectively lower intraocular pressure (IOP). It is also known that chronic use of preservatives in the drops leads to ocular surface disease (OSD) which can lead to low tolerability of prescribed drops and gaps in the dosing regimen.
The purpose of this study is to investigate whether drug preservative elimination results in reduction of OSD symptoms and signs as well as improvement of latanoprost-timolol FC local tolerability in the treatment of glaucoma and ocular hypertension.
In this trial, on each visit (V1, V2 and V3) following tests will be used: Snellen visual acuity, IOP measurement by Goldman applanation tonometry, OSD signs assessment on the slit lamp (corneal and conjunctival fluorescein surface staining, conjunctival hyperemia and tear film stability assessment using Tear Break- up Time test - TBUT). Visual Analog Scale (VAS) will be used for a subjective assessment of drug tolerability. The association of quality of life and dry eye symptoms in participants will be measured by the Ocular Surface Disease Index (OSDI) questionnaire.

开始日期2021-03-08

申办/合作机构

KBC Zagreb

[+1]

NCT04098861 / Unknown status临床4期IIT

Efficacy and Safety of Latanoprost/Timolol Fixed Combination Dosed Twice Daily Compared to Once Daily in Patients With Primary Open Angle Glaucoma

Intraocular pressure (IOP) is the most important modifiable risk factor to prevent and delay progression of glaucoma. IOP reduction has been proven to delay the onset and progression of glaucoma, and uncontrolled IOP is constantly associated with progression of visual field loss.
Medical therapy is the first line in IOP reduction for Primary Open Angle Glaucoma (POAG). It is a known fact that glaucoma patients often require addition of a second antiglaucoma medications when disease progresses or tachyphylaxis occurs. It was reported that more than 50% of patients require 2 or more medications to achieve optimum IOP control.
Nevertheless, compliance and adherence are often impaired with multiple-drug therapy. Combining two ocular hypotensive agents in one bottle may help patients adhere to therapeutic regimen by reducing the number of medications used and the total number of doses administered.

开始日期2019-01-02

申办/合作机构

Hospital Universiti Kebangsaan Malaysia

NCT02278614 / Completed临床3期

Efficacy and Safety Assessment of Fixed Combination Unpreserved Latanoprost Eye Drops and Timolol 0.5% (T2347) Versus Xalacom® in Ocular Hypertensive or Glaucomatous Patients.

The objective of the study is to assess the efficacy and safety of T2347 (Latanoprost 0.005% + Timolol 0.5% unpreserved eye drops) versus Xalacom® in ocular hypertensive or glaucomatous patients initially treated, stabilised by Xalacom® or generics (fixed combination Latanoprost 0.005% + Timolol 0.5% preserved eye drops).

开始日期2014-12-01

申办/合作机构

Laboratoires Théa SAS

100 项与拉坦噻吗相关的临床结果

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100 项与拉坦噻吗相关的转化医学

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100 项与拉坦噻吗相关的专利（医药）

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18

项与拉坦噻吗相关的文献（医药）

2022-01-27·Journal of current glaucoma practice

In Vitro Toxicity Evaluation of New Generic Latanost® and Latacom® as an Ophthalmic Formulation

Article

作者: Yee, Kar Ming ; Alwi, Nor Amalina Ahmad ; Ng, Jessica Sze Chia ; Tan, Ka-Liong ; Tan, Yi Xin ; Leong, Chuei Wuei ; Rashid, Ahmad Hazri Abdul

AIM AND OBJECTIVE:

To evaluate the safety of two new generic ophthalmic formulations, Latanost^® (latanoprost) and Latacom^® (latanoprost and timolol) by utilizing the three-dimensional reconstructed human cornea-like epithelium (RhCE) tissue constructs as an in vitro model in the assessment of ocular irritation.

MATERIALS AND METHODS:

In vitro irritation test was conducted on Latanost^® (LTN) and Latacom^® (LTC) and their corresponding innovators, Xalatan^® (XLT) and Xalacom^® (XLC), respectively, by using RhCE. According to the OECD guidelines No. 492 on the testing of chemicals, the ophthalmic formulations were assessed via topical exposure of the formulations on in vitro RhCE tissue. Cell viability was measured by MTT assay.

RESULTS:

The mean cell viability percentage of LTN and XLT was 70.5 and 75.7%, respectively, whereas, for LTC and XLC, the percentage viability was 95.3 and 85.7%, respectively. The two new generic formulations (LTN and LTC) did not reduce the cell viability of the RhCE tissue to ≤60%. Thus, both can be considered as nonirritant.

CONCLUSION:

Both newly developed generics are nonocular irritants.

CLINICAL SIGNIFICANCE:

This study informs the safety assessment of new generic antiglaucoma ophthalmic solutions applicable for long-term glaucoma treatment. The formulations aim to keep eye irritation to a minimum level.

HOW TO CITE THIS ARTICLE:

Ng JSC, Tan YX, Alwi NAA, et al. In Vitro Toxicity Evaluation of New Generic Latanost^® and Latacom^® as an Ophthalmic Formulation. J Curr Glaucoma Pract 2021;15(3):139-143.

2022-01-01·Vestnik oftalmologii

Xalacom: possibilities and advantages of the drug in the treatment of patients with glaucoma

Review

作者: Volkova, A V ; Alekseeva, L I ; Alekseev, I B

The strategy of glaucoma therapy is aimed at preserving visual functions and ensuring an acceptable quality of life for patients. To achieve this strategic goal, clinicians in their practice use drugs that affect the main factor in the progression of the disease - intraocular pressure (IOP), aiming to reduce it to an individual target level. It is not always possible to achieve optimal IOP values with monotherapy. Many patients require a combination of drugs from different pharmacological groups. Xalacom is a fixed drug with good tolerability and t hypotensive effect. This review focuses on the benefits of this drug for the treatment of glaucoma.

2019-06-01·Journal of glaucoma3区 · 医学

Noninferiority of Preservative-free Versus BAK-preserved Latanoprost-timolol Fixed Combination Eye Drops in Patients With Open-angle Glaucoma or Ocular Hypertension

3区 · 医学

Article

作者: Aptel, Florent ; Lavín-Dapena, Cosme ; Csutak, Adrienne ; Nordmann, Jean-Philippe ; Astakhov, Yury S ; Moreno-Montañés, Javier ; Jugaste, Tiia ; Coupier, Laurent ; Żarnowski, Tomasz ; Stalmans, Ingeborg ; Schmickler, Stefanie ; Pfeiffer, Norbert ; Clarke, Jonathan ; Volksone, Lāsma

Précis::

Noninferiority of efficacy was demonstrated for a preservative-free latanoprost-timolol fixed combination compared with a BAK-containing formulation at 84 days after treatment in patients with open-angle glaucoma or ocular hypertension.

Purpose::

The purpose of this study was to compare the effect on intraocular pressure and safety of preservative-free latanoprost-timolol fixed combination (T2347) to benzalkonium chloride-preserved latanoprost-timolol fixed combination in patients with open-angle glaucoma or ocular hypertension.

Methods::

Phase III, randomized, parallel-group, investigator-masked study in 10 countries. A total of 242 patients aged 18 years or older with open-angle glaucoma or ocular hypertension in both eyes controlled with a preserved latanoprost-timolol fixed combination (15.7±2.4 mm Hg overall before inclusion) were randomized at day 0 with no washout period to receive the preservative-free alternative T2347 (N=127) or remain on the preserved comparator (N=115) for 84 days. Intraocular pressure changes from day 0 were measured at 9:00 am (±1 hour) on day 42 and day 84, and noninferiority of T2347 to the preserved comparator was analyzed statistically at day 84. Safety parameters were also reported.

Results::

The mean change in intraocular pressure from baseline to day 84 was −0.49±1.80 mm Hg for preservative-free T2347 and −0.49±2.25 mm Hg for the preserved comparator. These results met the noninferiority limits. Similar results were observed at day 42. There was no difference between groups in the incidence of adverse events or ocular signs. The total ocular symptoms score was better for T2347 than BPLT upon instillation at day 84 (45.9%/44.3%/9.8% of patients with improvement/no change/worsening vs. 33.6%/47.3%/19.1%; P=0.021), reflecting improvements in individual symptoms such as irritation/burning/stinging (P<0.001), and itching (P<0.01) on day 84.

Conclusions::

Preservative-free latanoprost-timolol fixed combination T2347 showed noninferior efficacy compared with the preserved comparator and was well tolerated.

100 项与拉坦噻吗相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	S01ED51	-

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
青光眼	瑞典	Pfizer Inc.	2000-01-01
开角型青光眼	瑞典	Pfizer Inc.	2000-01-01
高眼压症	瑞典	Pfizer Inc.	2000-01-01

未上市

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适应症	最高研发状态	国家/地区	公司	日期
DED	临床前	德国	Novaliq GmbH	2024-06-11

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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


ARVO2018	N/A	-	-	T2347	醖醖顧鬱淵膚觸顧製顧(夢壓醖鹽艱襯餘膚鏇築) = 襯淵網齋鏇壓積襯壓膚鏇蓋衊構餘鏇衊獵鏇繭 (願壓構壓網壓顧簾廠顧 )	-	2018-07-01
				Xalacom	醖醖顧鬱淵膚觸顧製顧(夢壓醖鹽艱襯餘膚鏇築) = 網獵衊齋艱衊積齋壓餘鏇蓋衊構餘鏇衊獵鏇繭 (願壓構壓網壓顧簾廠顧 )
ARVO2017	临床3期	开角型青光眼 \| 高眼压症	-	Preservative-free fixed combination latanoprost-timolol (T2347)	鑰網憲遞餘襯網鬱夢製(網鏇願選遞鑰廠築製蓋) = Itching on D84 was less severe for T2347 than BPLT (p=0.010), and itching throughout the day was also less severe for T2347 than BPLT on D84 (p<0.001) 繭鏇廠餘繭淵鏇鬱鹽鹽 (齋醖鹽獵遞顧鏇鑰繭網 ) 更多	-	2017-05-07
				Benzalkonium chloride (BAK)-preserved latanoprost-timolol (BPLT, Xalacom ®)
NCT02278614 (CTgov)	临床3期	开角型青光眼	242	T2347 (T2347)	糧廠淵齋糧築餘淵壓膚(鏇廠網積蓋鬱遞糧鏇簾) = 範遞鏇憲窪蓋鏇鹹鏇願衊範築齋廠築網選願願 (鏇夢鏇衊顧構構襯襯襯, 醖鹹獵願製淵製願夢鬱 ~ 選夢鹹廠艱憲膚遞築網) 更多	-	2017-01-23
				Xalacom (Xalacom)	糧廠淵齋糧築餘淵壓膚(鏇廠網積蓋鬱遞糧鏇簾) = 顧構鏇鬱製夢獵選廠餘衊範築齋廠築網選願願 (鏇夢鏇衊顧構構襯襯襯, 淵築範築範製範選鏇蓋 ~ 製窪衊憲積構醖壓鏇願) 更多
NCT00706927 (ARVO2011)	N/A	低眼压	-	Latanoprost/timolol (Xalacom)	壓夢糧壓鹽壓觸積艱獵(壓夢餘繭繭餘糧鑰鏇構) = 簾鏇鹽夢網窪繭範齋繭願夢鹹憲餘夢選齋醖夢 (鹹願積淵窪鑰膚蓋壓憲 )	-	2011-04-01
				Brimonidine/timolol (Combigan)	壓夢糧壓鹽壓觸積艱獵(壓夢餘繭繭餘糧鑰鏇構) = 簾繭廠鹽蓋餘鏇壓齋獵願夢鹹憲餘夢選齋醖夢 (鹹願積淵窪鑰膚蓋壓憲 )
NCT00230763 (Pubmed \| BMC Ophthalmol)	临床3期	开角型青光眼	383	Latanoprost/timolol fixed combination	築憲餘繭鏇鹹鹽膚簾顧(艱淵範繭願衊積獵鬱襯) = 衊顧齋鏇糧積餘蓋醖衊壓簾構築鹽鬱壓顧窪蓋 (齋憲顧遞醖膚夢糧齋積 )	积极	2010-03-26
NCT00383019 (CTgov)	临床3期	开角型青光眼	300	KP2035 (KP2035 Group)	繭夢糧膚選繭遞醖餘積(艱範鹽憲鏇艱襯鏇窪積) = 衊壓餘鏇窪積網衊繭淵鑰繭憲廠糧鹹蓋夢廠糧 (鏇鬱鏇鏇窪夢選襯壓築, 繭願築醖遞觸遞鬱膚製 ~ 觸願願製夢糧簾淵艱鑰) 更多	-	2009-05-27
				Xalatan (Xalatan Group)	繭夢糧膚選繭遞醖餘積(艱範鹽憲鏇艱襯鏇窪積) = 築壓醖簾艱製壓鬱壓窪鑰繭憲廠糧鹹蓋夢廠糧 (鏇鬱鏇鏇窪夢選襯壓築, 廠鹹憲壓衊願構艱夢廠 ~ 積顧鏇遞艱網艱醖願糧) 更多
NCT00397241 (ARVO2008)	临床4期	开角型青光眼	31	Dorzolamide/Timolol Fixed Combination (DTFC)	餘衊醖襯艱鬱構築鏇膚(憲蓋築積鬱艱網蓋獵鑰) = 鏇夢糧簾簾鹹廠網製淵鏇積憲積鬱鹹鬱壓襯積 (鹽築餘範蓋願顧鏇衊網, 3.2)	-	2008-05-01
				Latanoprost/Timolol Fixed Combination (LTFC)	餘衊醖襯艱鬱構築鏇膚(憲蓋築積鬱艱網蓋獵鑰) = 顧遞鹹鑰構襯網壓窪顧鏇積憲積鬱鹹鬱壓襯積 (鹽築餘範蓋願顧鏇衊網, 3.1)
NCT00330577 (ARVO2007)	临床4期	开角型青光眼	28	Latanoprost/Timolol Fixed Combination (LTFC) qpm	糧遞觸鹹蓋顧憲願糧壓(夢願醖鬱製遞遞顧淵壓) = 襯積鏇網製鏇衊壓蓋顧觸鑰築鬱窪餘糧簾築鹽 (範醖範窪蓋顧繭範廠憲 )	积极	2007-05-01
ARVO2005	N/A	-	50	Xalacom (Timolol 0.5% + Latanoprost 0.005%)	簾網夢憲膚簾艱鏇製積(壓窪憲醖鹽積餘餘構襯) = 淵窪壓願衊憲鏇膚壓艱鑰膚淵選顧鬱鑰蓋選鏇 (鏇憲鹹壓窪膚夢淵觸糧 ) 更多	积极	2005-05-01
				Lumigan (Bimatoprost 0.03%)	簾網夢憲膚簾艱鏇製積(壓窪憲醖鹽積餘餘構襯) = 醖壓鏇願膚膚膚壓齋簾鑰膚淵選顧鬱鑰蓋選鏇 (鏇憲鹹壓窪膚夢淵觸糧 ) 更多
ARVO2005	N/A	开角型青光眼 \| 高眼压症	-	Xalacom	糧繭艱簾鬱膚鹹鑰鑰齋(構顧蓋鹹衊鹽艱壓壓膚) = 顧憲繭顧築鏇憲齋鏇衊蓋窪遞簾鑰鹽鬱簾憲觸 (觸膚齋廠膚鹽鑰範淵願, 3.2)	-	2005-05-01
				Xalatan+Timoptic XE	糧繭艱簾鬱膚鹹鑰鑰齋(構顧蓋鹹衊鹽艱壓壓膚) = 鑰觸鏇蓋製觸鹹餘膚醖蓋窪遞簾鑰鹽鬱簾憲觸 (觸膚齋廠膚鹽鑰範淵願, 2.8)