RV-568(RV-568) - 药物靶点：SRC x p38α x p38γ_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

SRC x p38α x p38γ

作用机制

SRC抑制剂(酪氨酸蛋白激酶SRC抑制剂)、p38α抑制剂(P38 α 丝裂原活化蛋白激酶抑制剂)、p38γ抑制剂(P38 丝裂原活化蛋白激酶-γ抑制剂)

治疗领域

免疫系统疾病感染耳鼻咽喉疾病+ [1]

在研适应症-

非在研适应症

慢性阻塞性肺疾病呼吸道合胞体病毒感染季节性过敏性鼻炎+ [1]

原研机构

RespiVert Ltd.

在研机构-

非在研机构

Janssen Research & Development LLC

RespiVert Ltd.

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C34H36N6O4

InChIKeyRTDCVLCTBQDLBW-UHFFFAOYSA-N

CAS号1220626-82-3

关联

5

项与 RV-568 相关的临床试验

NCT01867762 / Completed临床2期

A Phase 2, Randomized, Double-blind, Placebo-controlled, Efficacy and Safety Study of Inhaled JNJ 49095397 (RV568) in Subjects With Moderate to Severe Chronic Obstructive Pulmonary Disease

The purpose of this study is to assess the effectiveness and safety of JNJ 49095397 in participants with symptomatic moderate to severe chronic obstructive pulmonary disease (COPD).

开始日期2013-09-09

申办/合作机构

Janssen Research & Development LLC

NCT01661244 / Completed临床1期

A Randomised, Double-blind, Placebo-controlled, Two Part Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Treatment With Single and Repeat Doses of Inhaled RV568 in Healthy Volunteers

RV568 is being developed as a possible treatment of smoking related lung disease (also known as Chronic Obstructive Pulmonary Disease - COPD).
The main purpose of this study is to examine the safety and tolerability of a new inhaled formulation of RV568 in healthy volunteers. The study will be run in two parts; Part A and Part B. Part A (Cohorts 1, 2 & 3) will investigate 6 different dose levels of RV568 given as a single dose and Part B (Cohorts 4 & 5) will investigate 2 different dose levels of RV568 given once a day for 14 days.

开始日期2012-09-01

申办/合作机构

RespiVert Ltd.

NCT01475292 / Completed临床2期

A Randomised, Double-blind, Placebo-controlled, Parallel Group Study to Evaluate the Safety and Tolerability of Treatment With Repeat Doses of Inhaled RV568 in Patients With COPD

RV568 is being developed as a possible treatment of diseases such as smoking related lung disease (also known as Chronic Obstructive Pulmonary Disease - COPD) and asthma.
The main purpose of this study is to examine the safety of RV568 in COPD patients. Two dose strengths of RV568 and a placebo will be tested in this study, which will be given by inhaling a liquid suspension from a nebuliser once a day for 2 weeks.

开始日期2011-11-01

申办/合作机构

RespiVert Ltd.

100 项与 RV-568 相关的临床结果

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100 项与 RV-568 相关的转化医学

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100 项与 RV-568 相关的专利（医药）

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3

项与 RV-568 相关的文献（医药）

2017-10-01·European Respiratory Journal1区 · 医学

RV568, a narrow-spectrum kinase inhibitor with p38 MAPK-α and -γ selectivity, suppresses COPD inflammation

1区 · 医学

Article

作者: Singh, Dave ; Russell, Paul ; Charron, Catherine E ; Kizawa, Yasuo ; Lea, Simon ; Ito, Kazuhiro ; Brindley, Charlie

Novel anti-inflammatory approaches targeting chronically activated kinase pathways in chronic obstructive pulmonary disease (COPD) are needed. We evaluated RV568, a p38 mitogen-activated protein kinase-α and -γ and SRC family kinase inhibitor, in cellular andin vivomodels relevant to COPD and examined its safety and efficacy in COPD patients.The anti-inflammatory activities of RV568 were tested in primary cultured monocytes, macrophages and bronchial epithelial cells andin vivoin lipopolysaccharide and cigarette smoke-exposed murine models. RV568 was evaluated in a 14-day trial in COPD patients.RV568 showed potent anti-inflammatory effects in monocytes and macrophages, which were often greater than those of corticosteroids or the p38 inhibitor Birb796. RV568 combined with corticosteroid had anti-inflammatory effects suggestive of a synergistic interaction in poly I:C-stimulated BEAS-2B cells and in the cigarette smoke model. In COPD patients, inhaled RV568 (50 µg and 100 µg) improved pre-bronchodilator forced expiratory volume in 1 s (69 mL and 48 mL respectively) and significantly reduced sputum malondialdehyde (p<0.05) compared to placebo, although there were no changes in sputum cell counts. Adverse events during RV568 and placebo treatment were similar.RV568 shows potent anti-inflammatory effects on cell and animal models relevant to COPD. RV568 was well-tolerated and demonstrated a modest clinical benefit in a 14-day COPD clinical trial.

2015-03-04·Expert Opinion on Investigational Drugs2区 · 医学

Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease

2区 · 医学

Review

作者: Norman, Peter

INTRODUCTIONThe p38 protein kinases, in particular p38α and p38β, regulate the production of multiple inflammatory mediators. Consequentially, considerable effort has been focused on trying to develop p38 inhibitors for the treatment of inflammatory diseases. Some 20 p38 inhibitors have progressed to clinical development, mostly for the treatment of rheumatoid arthritis, but with little success. Increasingly, interest has turned to their use in other indications and notably chronic obstructive pulmonary disease (COPD).AREAS COVEREDIn this review, the author discusses the eight p38 inhibitors that have been clinically evaluated. Acumapimod is the only one of four orally delivered inhibitors that remains in active development while Phase II results of PH-797804 and losmapimod are compared. The activity of two inhibitors designed for inhaled delivery, RV-568 and PF-03715455, is compared but little is known about AZD-7624 or the discontinued GSK-610677.EXPERT OPINIONResults from animal models provide a clear rationale for developing p38 inhibitors for COPD, and appear to be (partially) validated by the efficacy seen with PH-797804 and losmapimod. Inhaled delivery provides the opportunity to enhance p38 inhibition in the lung while reducing unwanted systemic effects of p38 inhibition. Validation of this hypothesis should come from the results of the recently completed Phase II study with RV-568.

2014-12-01·Expert Opinion on Therapeutic Patents2区 · 医学

Respivert’s multikinase inhibitors, an evaluation of WO2014033446 to WO2014033449

2区 · 医学

Article

作者: Norman, Peter

These four patent applications all claim that N-aryl-N'-pyrazol-5-yl urea derivatives , related to RV-568, which are inhibitors of p38, Syk and Src kinases. All four applications claim their use in the treatment of inflammatory diseases, notably asthma and chronic obstructive pulmonary disease. The four applications are primarily differentiated by the claimed substitution of the pyrazole ring. This is accompanied by differential kinase specificity profiles. Many of the exemplified compounds show reduced potency as p38 inhibitors but high potency as inhibitors of Syk and/or Src kinases.

100 项与 RV-568 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
呼吸道合胞体病毒感染	临床2期	英国	RespiVert Ltd.	2010-10-01
季节性过敏性鼻炎	临床2期	奥地利	RespiVert Ltd.	2010-10-01
季节性鼻炎	临床前	奥地利	RespiVert Ltd.	2010-10-01
慢性阻塞性肺疾病	药物发现	英国	RespiVert Ltd.	2011-11-01