GW-870086(GW-870086) - 药物靶点：GR_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

GR

作用机制

GR激动剂(糖皮质激素受体激动剂)

治疗领域

免疫系统疾病遗传病与畸形呼吸系统疾病+ [1]

在研适应症-

非在研适应症

哮喘特应性皮炎

原研机构

GSK Plc

在研机构-

非在研机构

GSK Plc

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C31H39F2NO6

InChIKeyWUBKGTSFJSEIEM-NSHBDUGJSA-N

CAS号827319-43-7

关联

12

项与 GW-870086 相关的临床试验

NCT01381445 / Completed临床1期

A Randomised, Double-blind (for GW870086), Placebo-controlled Study of Topical GW870086 Formulation to Explore the Potential for Skin Thinning in Healthy Adult Volunteers

This study is a randomised, double-blind, placebo-controlled study of topical GW870086 to explore the potential for skin thinning in healthy adult volunteers after 42±2 days of treatment. Twenty (20) healthy volunteers will be randomised to receive placebo and GW870086 2% cream, they will also receive either of the following treatments: GW870086 0.2% cream, or clobetasol propionate 0.05% cream.

开始日期2011-04-14

申办/合作机构

GSK Plc

EUCTR2010-022279-77-DE / Not yet recruitingN/A

A Phase II Randomised, Double-Blind, Placebo-Controlled, Parallel Group, Multicentre Study to determine the efficacy and dose response of repeat inhaled doses of GW870086X on FEV1 in adults with Persistent Asthma

开始日期2011-02-25

申办/合作机构

GlaxoSmithKline Research & Development Ltd.

NCT01299610 / Completed临床2期

A Randomised, Double-blind, Placebo-controlled Study of Topical GW870086X Formulation in Subjects With Moderate or Severe Atopic Dermatitis

This study is a randomised, double-blind, placebo-controlled study to assess the efficacy of GW870086X cream formulation in subjects with moderate to severe atopic dermatitis. Subjects will be assigned to take 3 out of the 4 possible treatments for 21 ±2 days: GW870086X 0.2% cream, GW870086X 2% cream, FP 0.05% cream (as a positive control) and placebo cream. All subjects will be randomised to receive placebo cream. Three index lesions located on the arms and/or legs (one on each) will be identified per subject and each treatment will be applied to the same lesion.

开始日期2010-12-01

申办/合作机构

GSK Plc

100 项与 GW-870086 相关的临床结果

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100 项与 GW-870086 相关的转化医学

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100 项与 GW-870086 相关的专利（医药）

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7

项与 GW-870086 相关的文献（医药）

2015-11-02·Expert Opinion on Investigational Drugs2区 · 医学

Novel glucocorticoid receptor agonists in the treatment of asthma

2区 · 医学

Review

作者: Matera, Maria Gabriella ; Cazzola, Mario ; Rogliani, Paola ; Coppola, Angelo

INTRODUCTIONInhaled corticosteroids are the only drugs that effectively suppress the airway inflammation, but they can induce considerable systemic and adverse effects when they are administered chronically at high doses. Consequently, the pharmaceutical industry is still searching for newer entities with an improved therapeutic index.AREAS COVEREDHerein, the authors review the research in the glucocorticoid field to identify ligands of the glucocorticoid receptor (GR). These ligands preferentially induce transrepression with little or no transactivating activity, in order to have a potent anti-inflammatory action and a low side-effects profile.EXPERT OPINIONSeveral agents have been synthesized, but few have been tested in experimental models of asthma. Furthermore, only three (BI-54903, GW870086X and AZD5423) have entered clinical development, although the development of at least one of them (BI-54903) was discontinued. The reason for the limited success so far obtained is that the model of transactivation versus transrepression is a too simplistic representation of GR activity. It is difficult to uncouple the therapeutic and harmful effects mediated by GR, but some useful information that might change the current perspective is appearing in the literature. The generation of gene expression 'fingerprints' produced by different GR agonists in target and off-target human tissues could be useful in identifying drug candidates with an improved therapeutic ratio.

2015-08-01·Journal of Allergy and Clinical Immunology1区 · 医学

The novel inhaled glucocorticoid receptor agonist GW870086X protects against adenosine-induced bronchoconstriction in asthma

1区 · 医学

Letter

作者: O'Connor, Brian ; Barnes, Peter J ; Leaker, Brian R ; Singh, Dave

This article describes on novel inhaled glucocorticoid receptor agonist GW870086X protection against adenosine-induced bronchoconstriction in asthma.Potential anti-inflammatory activity of the novel dissociated glucocorticoid GW870086X in airway hyperresponsiveness, measured by the bronchoconstrictor response to inhaled adenosine monophosphate in subjects with mild asthma are also described.

2015-01-01·Skin Pharmacology and Physiology4区 · 医学

Clinical Efficacy and Tolerability of a Novel Selective Corticosteroid in Atopic Dermatitis - Two Randomised Controlled Trials

4区 · 医学

Article

作者: Robertson, Jonathan ; Worm, Margitta ; Hielscher, Nadine ; Doelle, Sabine ; Hardes, Kelly ; Bareille, Philippe Jean

Topical corticosteroids remain the first-line therapy for atopic dermatitis (AD). Hence, we investigated the efficacy and safety profile of a novel selective corticosteroid, GW870086. We performed 2 randomised, double-blind, controlled studies with 25 AD patients and 20 healthy subjects. The changes in the Three-Item Severity (TIS) score and the skin thickness were the primary end points, respectively. The adjusted TIS score (day 22) shows that the novel corticosteroid resulted in a non-significant, but dose-dependent reduction compared to placebo (GW870086 0.2% vs. placebo = -0.38, GW870086 2% vs. placebo = -0.89). Significant skin thinning was observed in the second study on days 14 and 21 when patients were treated with the comparator but not with the novel corticosteroid compared to placebo. The clinical efficacy of the new selective corticosteroid was not superior to placebo, although a dose-dependent improvement upon treatment was noticed without the onset of skin thinning.

100 项与 GW-870086 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB12322

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
特应性皮炎	临床2期	德国	GSK Plc	2011-04-14
哮喘	临床2期	德国	GSK Plc	2009-02-16

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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


NCT00857857 (CTgov)	临床2期	哮喘	24	placebo+GW870086+fluticasone propionate (Placebo)	衊簾蓋廠夢獵夢憲廠繭(糧簾鹽範齋獵膚鹽築餘) = 觸壓齋願餘願糧窪壓簾壓衊構製繭積壓衊觸鑰 (製觸淵齋鹽積醖蓋糧鹽, 簾艱遞選壓選鏇鑰艱膚 ~ 積窪襯製製壓網選網憲) 更多	-	2018-02-20
				GW870086 (GW870086 0.25 mg OD)	衊簾蓋廠夢獵夢憲廠繭(糧簾鹽範齋獵膚鹽築餘) = 憲窪遞遞願憲壓襯鬱積壓衊構製繭積壓衊觸鑰 (製觸淵齋鹽積醖蓋糧鹽, 窪簾廠鏇遞廠艱獵簾夢 ~ 襯憲衊鑰繭襯窪獵壓觸) 更多
NCT01299610 (CTgov)	临床2期	中度特应性皮炎 \| 重度特应性皮炎	25	GW870086 (GW870086, 0.2% Cream)	鬱膚願餘鏇願鑰憲顧壓(鬱廠蓋襯製齋鑰鏇顧鑰) = 壓鹽範獵衊淵餘繭觸遞範繭艱艱範範蓋鏇遞觸 (顧夢製選鏇顧鏇選鬱製, 艱製鹽艱衊範衊艱壓窪 ~ 網蓋鬱繭鹹醖壓窪齋壓) 更多	-	2017-10-16
				GW870086 (GW870086, 2.0% Cream)	鬱膚願餘鏇願鑰憲顧壓(鬱廠蓋襯製齋鑰鏇顧鑰) = 鹹醖製網襯鏇構繭鏇構範繭艱艱範範蓋鏇遞觸 (顧夢製選鏇顧鏇選鬱製, 餘餘窪淵繭積構鏇餘醖 ~ 繭鏇範獵壓齋衊繭鏇淵) 更多
NCT00945932 (Pubmed \| J Asthma)	临床2期	哮喘	36	GW870086 1mg	(鹽鬱觸簾襯餘簾顧襯願) = 遞憲醖餘簾糧製餘窪鬱艱衊觸淵壓壓鏇衊壓淵 (齋選顧構簾獵繭鏇淵餘 )	不佳	2013-12-01