Stroquinan(Stroquinan) - 药物靶点：Reactive oxygen species x SOD1_在研适应症：急性缺血性卒中_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Otaplimastat

+ [3]

靶点

Reactive oxygen species x SOD1

作用机制

活性氧抑制剂、SOD1刺激剂(超氧化物歧化酶刺激剂)

治疗领域

神经系统疾病心血管疾病

在研适应症

急性缺血性卒中

非在研适应症-

原研机构

Shinpoong Pharmaceutical Co., Ltd. ESOA

在研机构

Shin Poog Pharmaceutical Co., Ltd. Shinpoong Pharmaceutical Co., Ltd.

非在研机构-

最高研发阶段临床3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C28H34N6O5

InChIKeySJZBPVOSFYUHFV-UHFFFAOYSA-N

CAS号1176758-04-5

关联

4

项与 Stroquinan 相关的临床试验

NCT06660719 / Not yet recruiting临床3期

A Multi-Center, Randomized, Double-Blind, Parallel, Placebo-Controlled, Phase III Clinical Study to Evaluate Efficacy and Safety of SP-8203 (Otaplimastat) in Patients with Acute Ischemic Stroke Requiring Thrombolytic Therapy As Standard of Care

This clinical study is designed to evaluate the efficacy and safety of the combination therapy of SP-8203 (otaplimastat) and thrombolytic standard of care in acute ischemic stroke patient.
As a standard of care, thrombolytic therapy (for instance, recombinant tissue plasminogen activator) will be administered. When reperfusion is not achieved in spite of thrombolytic therapy, endovascular therapy can be performed.

开始日期2024-12-30

申办/合作机构

Shin Poog Pharmaceutical Co., Ltd.

NCT04479449 / Completed临床2期

A Prospective, Randomized, Double-blind Phase 2b Clinical Trial to Investigate the Efficacy and Safety of SP-8203 in Patients With Acute Ischemic Stroke Requiring Recombinant Tissue Plasminogen Activator (rtPA) Standard of Care

This clinical trial is designed to evaluate the efficacy and safety of the combination therapy of SP-8203 (Otaplimastat) and recombinant tissue Plasminogen Activator (rtPA) standard of care. In this clinical trial, rtPA will be injected intravenously using an infusion device. If reperfusion is not occur in spite of rtPA therapy, endovascular therapy can be performed.

开始日期2019-03-18

申办/合作机构

Shin Poog Pharmaceutical Co., Ltd.

NCT02787278 / Completed临床2期

A Prospective, Randomized, Double-blinded Phase IIa Clinical Trial to Investigate the Safety and Efficacy of Two Doses of SP-8203 in Patients With Ischemic Stroke Requiring rtPA Standard of Care

The current study aims to evaluate the safety of SP-8203, designing in two stages (stage-1, stage-2) to evaluate the safety and efficacy of the combination therapy of SP-8203 and rtPA for the occurrence of cerebral hemorrhage in patients with acute ischemic stroke receiving rtPA standard of care.

开始日期2016-06-05

申办/合作机构

Shin Poog Pharmaceutical Co., Ltd.

100 项与 Stroquinan 相关的临床结果

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100 项与 Stroquinan 相关的转化医学

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100 项与 Stroquinan 相关的专利（医药）

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4

项与 Stroquinan 相关的文献（医药）

2012-10-01·Xenobiotica4区 · 医学

Pharmacokinetic interaction between metoprolol and SP-8203 in rats: competitive inhibition for the metabolism of metoprolol by SP-8203 via hepatic CYP2D subfamily

4区 · 医学

Article

作者: Il Whan Cho ; Seung Yon Han ; Young-Won Chin ; Young Hee Choi ; Insoo Yoon ; Myung Gull Lee

1. The occurrence of cerebral ischemia is prevalent in patients with hypertension and the combination drug therapy is needed. Thus, the pharmacokinetic interaction between metoprolol (anti-hypertension drug) and SP-8203 (a new drug candidate for cerebral ischemia) with respect to the metabolism via CYP isozymes was evaluated. 2. Metoprolol and SP-8203 were administered intravenously or orally to rats. Concentrations (I) of each drug in the liver and intestine in in vivo studies, the disappearance and apparent K(i) of each drug in in vitro microsomes and [I]/K(i) ratios for each drug were determined. In addition, the disappearance of each drug via CYPs in rat and human microsomes were measured. 3. The AUC and CL(NR) of intravenously administered metoprolol with SP-8203 were significantly greater and slower, respectively, than without SP-8203. However, pharmacokinetic parameters of oral metoprolol and intravenous/oral SP-8203 were not altered. 4. The hepatic metabolism of metoprolol via CYP2D was inhibited by SP-8203 in a competitive manner. However, the intestinal metabolism of metoprolol was not influenced by SP-8203. SP-8203 was not metabolized via CYP isozymes in rats and then co-administration of metoprolol did not affect the metabolism of SP-8203.

2011-11-01·Pharmacology Biochemistry and Behavior4区 · 心理学

SP-8203 shows neuroprotective effects and improves cognitive impairment in ischemic brain injury through NMDA receptor

4区 · 心理学

Article

作者: Hye Sun Kim ; Yoo Hun Suh ; Hyun Su Hong ; Su Jin Noh ; Ki Sung Lee ; Jong Min Lee ; Il Hwan Cho ; Chul Kyu Lee

The extracts of earth worms, Eisenia andrei, have been used as a therapeutic agent for stroke in the traditional medicine. It is also reported that the protease fraction separated from the extracts has strong anti-thrombotic activity. Besides anti-thrombotic actions, we found that SP-8203, N-[3-(2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)propyl]-N-{4-[3-(2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)propylamino]butyl}acetamide, derived from the extracts of earth worms blocked N-methyl-(D)-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. The neuroprotective effects of SP-8203 were attributable to prevention of Ca(2+) influx through NMDA receptors. The systemic administration of SP-8203 markedly reduced neuronal death following middle cerebral artery occlusion in rats. SP-8203 significantly improved spatial learning and memory in the water maze test. These results provided strong pharmacological basis for its potential therapeutic roles in cerebral ischemia.

2011-03-01·Pharmacology Biochemistry and Behavior4区 · 心理学

SP-8203 reduces oxidative stress via SOD activity and behavioral deficit in cerebral ischemia

4区 · 心理学

Article

作者: Chul Kyu Lee ; Su Jin Noh ; Il Hwan Cho ; Hye Sun Kim ; Yoo Hun Suh ; Sang Hyung Lee ; Ki Young Shin

Both oxidative stress and excessive activation of glutamate receptors are implicated as major causes of ischemic brain injury. However, the existing N-methyl-D-aspartate (NMDA) receptor antagonists have not exerted good clinical outcome, most likely because they do not protect neurons against oxidative stress. Thus, more effective glutamate antagonists and antioxidants are needed for the treatment of ischemic stroke. In previous study, SP-8203, derived from earth worms, showed the blocking effect of NMDA receptor. We provided evidence that SP-8203 could also suppress the oxidative stress in this study. In vitro, 250 μM H2O2 was treated to SH-SY5Y cells after the pre-treatment of SP-8203 (2, 20 and 200 μM). SP-8203 significantly suppressed H2O2-induced cell death and reactive oxygen species production. In addition, we investigated the effects of SP-8203 in middle cerebral artery (MCA) occluded rat model. SP-8203 (5 and 10 mg/kg) was administered intraperitoneally to rats before and after the MCA occlusion and was injected daily for 10 days. After 10 days, SP-8203 remarkably reduced brain infarct volume and lipid peroxidation products in the MCA-occluded rats but MK-801 didn't. Moreover, SP-8203 significantly improved neurological deficits such as shortening of latency time in Rota rod performance. However, MK-801 didn't improve behavioral deficits. Therefore, SP-8203 may be more effective for multiple-target mechanisms of ischemic stroke.

100 项与 Stroquinan 相关的药物交易

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