Taprenepag isopropyl(Taprenepag isopropyl) - 药物靶点：EP2 x Opioid receptors_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Taprenepag、Taprenepag isopropyl (USAN)

+ [3]

靶点

EP2 x Opioid receptors

作用机制

EP2激动剂(前列腺素EP2受体激动剂)、Opioid receptors激动剂(阿片样受体激动剂)

治疗领域

眼部疾病

在研适应症-

非在研适应症

开角型青光眼

原研机构

Pfizer Inc.

在研机构-

非在研机构

Pfizer Inc.

最高研发阶段无进展临床2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

分子式C27H28N4O5S

InChIKeyNVPXUFQLKWKBHK-UHFFFAOYSA-N

CAS号1005549-94-9

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关联

4

项与 Taprenepag isopropyl 相关的临床试验

ACTRN12612000880842 / Completed临床1期

A Phase 1, Single-Center, Dose-Ranging, Multi-Treatment Study to Determine the Safety and Pharmacokinetics of Single Oral Dose Combinations of PF329 and Nafamostat Mesilate in Healthy Subjects

开始日期2012-09-24

申办/合作机构

Signature Therapeutics, Inc.

ACTRN12610000721000 / Completed临床1期

A Phase 1, Single-Center, Dose-Escalation and Fixed-Dose Crossover, Cohort Study to Determine the Safety and Pharmacokinetics of a Single Oral Dose of PF329 versus oral hydromorphone hydrochloride (HCl) in Healthy Subjects

开始日期2010-10-25

申办/合作机构-

NCT00934089 / Completed临床2期

A Phase 2, Single-masked, Randomized, Crossover Study Of The 24-hour Intraocular Pressure Lowering And Systemic Exposure of Pf-04217329 Alone And In Combination With Latanoprost

This study will characterize the effect of PF-04217329, alone and in combination with latanoprost, on circadian intraocular pressure and blood pressure in glaucoma patients. Blood samples will be collected to measure the amount of active metabolite of PF-04217329 in the plasma following dosing.

开始日期2010-01-01

申办/合作机构

Pfizer Inc.

100 项与 Taprenepag isopropyl 相关的临床结果

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100 项与 Taprenepag isopropyl 相关的转化医学

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100 项与 Taprenepag isopropyl 相关的专利（医药）

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7

项与 Taprenepag isopropyl 相关的文献（医药）

2023-10-01·Journal of Ocular Pharmacology and Therapeutics

Ocular Treatments Targeting Separate Prostaglandin Receptors in Mice Exhibit Alterations in Intraocular Pressure and Optic Nerve Lipidome

Article

作者: Sharif, Najam A ; Arcuri, Jennifer ; Elbaz, Abdelrahman ; Bhattacharya, Sanjoy K

Background: Prostaglandin (PG) receptor agonists are the first-line eyedrop medication treatment for glaucoma. The pathophysiology of this disease is not completely known, and elevated intraocular pressure (IOP) is the key risk factor. The membranes of the axons (of the retinal ganglion cells) passing through the optic nerve (ON) head experience significant damage. Lipids are an essential component of the cell's membranes, and their profile changes owing to neurodegeneration. In this investigation, three agonists for distinct PG receptors were used to lower IOP and to determine their effect on the ON lipids. We utilized DBA/2J mice as a model of progressive IOP increase and C57BL/6J mice as a model of ON crush. Methods: DBA/2J and C57BL/6J mice were treated daily for 2 weeks with Latanoprost, PF-04217329, or Rivenprost. The IOP was measured every 2 days and pattern electroretinogram was conducted for DBA/2J throughout the study. Lipidomics of ONs were performed for each model and treatment group. Results: Of the tested compounds, Latanoprost and Rivenprost were the most effective agents decreasing IOP in DBA/2J mice. Triglyceride levels increased in the ONs of DBA/2J mouse model, but phosphatidylethanolamine levels underwent highest level changes in the C57BL/6J mouse model when treated with Latanoprost. Conclusions: Topical ocular FP- and EP4-receptor agonists appreciably lowered IOP in the DBA/2J mice representing pigmentary glaucoma. The observed changes in ON lipidomics in the different models of neurodegeneration suggest possible use of such measures in the development of more effective medicines for both IOP reduction and ON protection.

2022-05-03·Proceedings of the National Academy of Sciences1区 · 综合性期刊

Agonists of prostaglandin E ₂ receptors as potential first in class treatment for nephronophthisis and related ciliopathies

1区 · 综合性期刊

Article

作者: Saunier, Sophie ; Porée, Esther ; Delous, Marion ; Krug, Pauline ; Fila, Marc ; Salomon, Rémi ; Briseño-Roa, Luis ; Garcia, Hugo ; Viau, Amandine ; Serafin, Alice S. ; Sin-Monnot, Soraya ; Cagnard, Nicolas ; Lyonnet, Stanislas ; Billot, Katy ; Annereau, Jean-Philippe ; Del Nery, Elaine ; Mahaut, Clémentine ; Benmerah, Alexandre ; Roy, Stéphanie ; Silbermann, Flora ; Garfa-Traore, Meriem ; Birgy, Éléonore ; Antignac, Corinne ; Deleglise, Bérangère ; Rodriguez, Pamela C. ; Jabot-Hanin, Fabienne ; Mehraz, Manon ; Ceccarelli, Salomé ; Furio, Laetitia

Significance Juvenile nephronophthisis (NPH) is a renal ciliopathy due to a dysfunction of primary cilia for which no curative treatment is available. This paper describes the identification of agonists of prostaglandin E 2 receptors as a potential therapeutic approach for the most common NPHP1 -associated ciliopathies. We demonstrated that prostaglandin E 1 rescues defective ciliogenesis and ciliary composition in NPHP1 patient urine-derived renal tubular cells and improves ciliary and kidney phenotypes in our NPH zebrafish and Nphp1 −/− mouse models. In addition, Taprenepag alleviates the severe retinopathy observed in Nphp1 −/− mice. Finally, transcriptomic analyses pointed out several pathways downstream the prostaglandin receptors as cell cycle progression, extracellular matrix, or actin cytoskeleton organization. Altogether, our findings provide an alternative for treatment of NPH.

2019-04-01·British Journal of Pharmacology2区 · 医学

Prostaglandin analogues and nitric oxide contribution in the treatment of ocular hypertension and glaucoma

2区 · 医学

Review

作者: Brambilla, Stefania ; Impagnatiello, Francesco ; Almirante, Nicoletta ; Bastia, Elena ; Bergamini, Michael V W ; Kothe, Angela C ; Duquesroix, Brigitte

In patients with ocular hypertension or glaucoma, all treatments aim to lower intraocular pressure (IOP) by modulating aqueous humour (AH) production and/or uveoscleral and trabecular meshwork/Schlemm's canal AH drainage. PG analogues are considered to be the ‘gold standard’ treatment and are the most frequently used IOP‐lowering agents. Recent data support an important role for NO in regulating IOP. Thus, novel PG analogues carrying a NO‐donating moiety were recently advanced. Latanoprostene bunod (LBN) and NCX 470, NO‐donating derivatives of latanoprost and bimatoprost, respectively, are examples of such compounds. LBN ophthalmic solution, 0.024% (Vyzulta™), showed greater IOP‐lowering efficacy compared with that of Xalatan® (latanoprost ophthalmic solution, 0.005%) or 0.5% timolol maleate in clinical settings. NCX 470 was found to be more effective than bimatoprost in animal models of ocular hypertension and glaucoma. Selective EP2 receptor agonists (i.e. taprenepag isopropyl, omidenepag isopropyl and aganepag isopropyl) and non‐selective prostanoid receptor agonists (i.e. ONO‐9054, sepetaprost isopropyl) that concomitantly stimulate FP and EP3 receptors have also been shown to hold promise as effective IOP‐lowering agents.Linked ArticlesThis article is part of a themed section on Eicosanoids 35 years from the 1982 Nobel: where are we now? To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v176.8/issuetoc

100 项与 Taprenepag isopropyl 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D09969	-	-	DB12623

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2期	美国	Pfizer Inc.	2007-12-11

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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


NCT00934089 (CTgov)	临床2期	开角型青光眼	31	Taprenepag+Latanoprost (Taprenepag+Latanoprost)	範憲齋獵蓋鬱選繭鏇廠(壓艱繭積夢鏇夢鹽艱襯) = 壓網顧製鹽醖構鏇網選膚築艱鬱鬱鏇築繭範鏇 (憲憲製範膚繭餘淵鏇鑰, 鹹築齋夢壓醖簾網餘鑰 ~ 遞淵糧鏇獵選鑰衊鑰鹽) 更多	-	2021-05-03
				Taprenepag+Latanoprost (Taprenepag+Latanoprost Vehicle)	範憲齋獵蓋鬱選繭鏇廠(壓艱繭積夢鏇夢鹽艱襯) = 簾壓選淵獵齋糧積顧艱膚築艱鬱鬱鏇築繭範鏇 (憲憲製範膚繭餘淵鏇鑰, 範積願選獵窪廠觸鬱餘 ~ 窪積蓋願製鏇夢鹽簾壓) 更多
NCT00934089 (ARVO2011)	临床2期	-	30	Taprenepag Isopropyl 0.01%	(網選築廠憲襯齋鑰艱築) = 網構齋憲鹹蓋繭選積鏇選襯鏇獵窪選壓艱膚顧 (選糧憲壓窪築鏇夢襯壓 ) 更多	-	2011-04-01
				Taprenepag Isopropyl 0.01% + Latanoprost 0.005%	(網選築廠憲襯齋鑰艱築) = 夢鏇憲鹽構壓獵齋鬱淵選襯鏇獵窪選壓艱膚顧 (選糧憲壓窪築鏇夢襯壓 ) 更多