Z-160(Z-160) - 药物靶点：N-type calcium channel_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [2]

靶点

N-type calcium channel

作用机制

N-type calcium channel抑制剂(Calcium channel inhibitor N-types inhibitors)

治疗领域

神经系统疾病

在研适应症-

非在研适应症

腰骶神经根病变疱疹后神经痛

原研机构

EPIRUS Biopharmaceuticals, Inc.

在研机构-

非在研机构

Zalicus Pharmaceuticals 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C32H32N2O

InChIKeyVCPMZDWBEWTGNW-UHFFFAOYSA-N

CAS号41332-24-5

关联

2

项与 Z-160 相关的临床试验

NCT01757873 / Completed临床2期

A Phase 2, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study to Evaluate the Efficacy and Safety of Z160 in Subjects With Postherpetic Neuralgia

This study will compare Z160 and placebo in patients with Postherpetic Neuralgia for safety and efficacy for a period of 6 weeks.

开始日期2012-12-01

申办/合作机构

Zalicus Pharmaceuticals Ltd.

NCT01655849 / Completed临床2期

A Phase 2, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study to Evaluate The Efficacy and Safety of Z160 in Subjects With Neuropathic Pain From Lumbosacral Radiculopathy

This study will compare Z160 and placebo in patients with Lumbosacral Radiculopathy for safety and efficacy for a period of 6 weeks.

开始日期2012-08-01

申办/合作机构

Zalicus Pharmaceuticals Ltd.

100 项与 Z-160 相关的临床结果

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100 项与 Z-160 相关的转化医学

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100 项与 Z-160 相关的专利（医药）

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3

项与 Z-160 相关的文献（医药）

2018-07-01·Bioorganic & Medicinal Chemistry3区 · 医学

Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels

3区 · 医学

Article

作者: Anjali Sairaman ; Kellie L. Tuck ; Fernanda Caldas Cardoso ; Anjie Bispat ; Peter J. Duggan ; Richard J. Lewis

Both N- and T-type calcium ion channels have been implicated in pain transmission and the N-type channel is a well-validated target for the treatment of neuropathic pain. An SAR investigation of a series of substituted aminobenzothiazoles identified a subset of five compounds with comparable activity to the positive control Z160 in a FLIPR-based intracellular calcium response assay measuring potency at both Ca_V2.2 and Ca_V3.2 channels. These compounds may form the basis for the development of drug leads and tool compounds for assessing in vivo effects of variable modulation of Ca_V2.2 and Ca_V3.2 channels.

2009-11-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Scaffold-based design and synthesis of potent N-type calcium channel blockers

4区 · 医学

Article

作者: Hossein Pajouhesh ; Terrance P. Snutch ; Gerald W. Zamponi ; Lester A. Mitscher ; David Dolphin ; Zhong-Ping Feng ; Francesco Belardetti ; Yanbing Ding ; Lingyun Zhang ; Hassan Pajouhesh

The therapeutic agents flunarizine and lomerizine exhibit inhibitory activities against a variety of ion channels and neurotransmitter receptors. We have optimized their scaffolds to obtain more selective N-type calcium channel blockers. During this optimization, we discovered NP118809 and NP078585, two potent N-type calcium channel blockers which have good selectivity over L-type calcium channels. Upon intraperitoneal administration both compounds exhibit analgesic activity in a rodent model of inflammatory pain. NP118809 further exhibits a number of favorable preclinical characteristics as they relate to overall pharmacokinetics and minimal off-target activity including the hERG potassium channel.

2004-11-01·Chest1区 · 医学

Zafirlukast Treatment for Acute Asthma

1区 · 医学

Article

作者: Phillip E. Korenblat ; Emil Skobeloff ; Robert A. Silverman ; Steven G. Simonson ; Yusong Chen ; Catherine M. Bonuccelli ; Christopher J. Miller ; Richard M. Nowak

CONTEXTAcute asthma causes nearly 2 million hospital emergency department (ED) visits in the United States annually, and hospitalization after an ED visit and relapse after ED discharge are common.OBJECTIVETo evaluate the adding of therapy with zafirlukast to standardized care for patients with acute asthma in the ED and a 28-day follow-up period.DESIGN AND PATIENTSA total of 641 patients presenting to the ED with acute asthma were randomized to receive either single-dose zafirlukast, 160 mg (Z160) [162 patients], zafirlukast, 20 mg (Z20) [158 patients]), or placebo (321 patients) as adjunct treatment to standard care in this double-blind, multicenter trial. Assessments, including spirometry and symptom scores, were obtained before each albuterol treatment and at 4 h. Patients who were discharged from the ED after 4 h continued outpatient therapy over a 28-day period and received either Z20 bid (276 patients) or placebo (270 patients) in addition to prednisone, albuterol, and their previous asthma medications. FEV(1) was measured at clinic visits on days 10 and 28. Patients recorded outpatient clinical data twice daily on a home diary card.MAIN OUTCOME MEASURESthe effect of zafirlukast on relapse after ED discharge. Other assessments were the rate of extended care (ie, ED stay for > 4 h or hospitalization), FEV(1), and symptoms.RESULTSAt the end of the outpatient period, 65 of 276 patients (23.6%) treated with zafirlukast and 78 of 270 patients (28.9%) treated with placebo relapsed (p = 0.047; absolute reduction, 5.3%; relative reduction, 18.3%). At the end of the ED period, 16 of 162 patients (9.9%) treated with Z160, 26 of 158 patients (16.5%) treated with Z20, and 48 of 321 patients (15.0%) treated with placebo required extended care (p = 0.052; absolute reduction with Z160 compared to placebo, 5.1%; relative reduction, 34%). These findings were supported by a significant improvement in FEV(1) and dyspnea in the ED with the use of Z160 therapy, and by greater improvement in FEV(1) and symptoms during the outpatient period for patients treated with Z20.CONCLUSIONSWhen added to standardized care, therapy with Z20 bid reduced the risk of relapse compared with placebo over a 28-day treatment period. One dose of Z160 in the ED also reduced the rate of extended care.

100 项与 Z-160 相关的药物交易

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