Delving into the Latest Updates on Stroquinan with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Otaplimastat

+ [3]

Target

Reactive oxygen species x SOD1

Action

inhibitors, stimulants

Mechanism

Reactive oxygen species inhibitors, SOD1 stimulants(Superoxide dismutase stimulants)

Therapeutic Areas

Nervous System DiseasesCardiovascular Diseases

Active Indication

Acute Ischemic Stroke

Inactive Indication-

Originator Organization

Shinpoong Pharmaceutical Co., Ltd. ESOA

Active Organization

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

Inactive Organization-

Drug Highest PhasePhase 3

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC28H34N6O5

InChIKeySJZBPVOSFYUHFV-UHFFFAOYSA-N

CAS Registry1176758-04-5

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.

Start Date14 Feb 2025

Sponsor / Collaborator

Shin Poog Pharmaceutical Co., Ltd.

NCT04479449

/ CompletedPhase 2

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.

Start Date18 Mar 2019

Sponsor / Collaborator

Shin Poog Pharmaceutical Co., Ltd.

NCT02787278

/ CompletedPhase 2

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.

Start Date05 Jun 2016

Sponsor / Collaborator

Shin Poog Pharmaceutical Co., Ltd.

100 Clinical Results associated with Stroquinan

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100 Translational Medicine associated with Stroquinan

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100 Patents (Medical) associated with Stroquinan

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12

Literatures (Medical) associated with Stroquinan

01 Feb 2021·Journal of Neurology, Neurosurgery & Psychiatry

The future of neuroprotection in stroke

Review

Author: Chamorro, Ángel ; Lo, Eng H ; van Leyen, Klaus ; Renú, Arturo ; Lyden, Patrick D

Investigators acknowledge the limitations of rodent or non-human primate stroke models, hundreds of putative neuroprotectants have been evaluated in preclinical models, but not one has entered the clinical realm. Initial studies focused on the neuron, but in recent years the focus has widened to also include other neural cells including astrocytes, pericytes and endothelial cells, which together form the neurovascular unit. Some new developments raise renewed hope for neuroprotection: the appearance of new compounds with multiple mechanisms of action, or the promulgation of new standards for a rigorous preclinical testing. At the bedside in the last 5 years, uric acid and nerinetide are the only compounds tested for clinical efficacy in randomised controlled trials (RCTs), where all patients had to receive reperfusion therapies, either intravenous thrombolysis and/or mechanical thrombectomy. In addition, otaplimastat, 3K3A-activated protein C (APC), intra-arterial verapamil and intra-arterial hypothermia were also assessed in combination with reperfusion therapy, but in RCTs that only included feasibility or safety outcomes. Some of these compounds yielded promising results which are discussed in this review. Altogether, a deeper knowledge of the mechanisms involved in the ischaemic death process at the neurovascular unit, an improved preselection and evaluation of drugs at the preclinical stage and the testing of putative neuroprotectants in enriched clinical studies of patients receiving reperfusion therapies, might prove more effective than in the past to reverse a dismal situation that has lasted already too long.

01 Feb 2020·Annals of Neurology

Safety and Efficacy of Otaplimastat in Patients with Acute Ischemic Stroke Requiring tPA (SAFE‐TPA): A Multicenter, Randomized, Double‐Blind, Placebo‐Controlled Phase 2 Study

Article

Author: Sung, Sang Min ; Kim, Byung Su ; Hwang, Yang Ha ; Kim, Eung‐Gyu ; Kim, Jong S. ; Kim, Won‐Ki ; Lee, Kyung Bok ; Chang, Dae‐il ; Lee, Eun‐Jae ; Ryu, Jei‐Man ; Oh, Kyungmi ; Ju, Chung ; Park, Jong‐Ho

ObjectiveOtaplimastat is a neuroprotectant that inhibits matrix metalloprotease pathway, and reduces edema and intracerebral hemorrhage induced by recombinant tissue plasminogen activator (rtPA) in animal stroke models. We aimed to assess the safety and efficacy of otaplimastat in patients receiving rtPA.MethodsThis was a phase 2, 2‐part, multicenter trial in stroke patients (19–80 years old) receiving rtPA. Intravenous otaplimastat was administered <30 minutes after rtPA. Stage 1 was a single‐arm, open‐label safety study in 11 patients. Otaplimastat 80 mg was administered twice daily for 3 days. Stage 2 was a randomized, double‐blind, placebo‐controlled study involving 69 patients, assigned (1:1:1) to otaplimastat 40 mg, otaplimastat 80 mg, or a placebo. The primary endpoint was the occurrence of parenchymal hematoma (PH) on day 1. Secondary endpoints included serious adverse events (SAEs), mortality, and modified Rankin scale (mRS) distribution at 90 days (clinicaltrials.gov identifier: NCT02787278).ResultsNo safety issues were encountered in stage 1. The incidence of PH during stage 2 was comparable: 0 of 22 with the placebo, 0 of 22 with otaplimastat 40 mg, and 1 of 21 with the 80 mg dose. No differences in SAEs (13%, 17%, 14%) or death (8.3%, 4.2%, 4.8%) were observed among the 3 groups. Three adverse events (chills, muscle rigidity, hepatotoxicity) were judged to be related to otaplimastat.InterpretationIntravenous otaplimastat adjunctive therapy in patients receiving rtPA is feasible and generally safe. The functional efficacy of otaplimastat needs to be investigated with further large trials. ANN NEUROL 2020;87:233–245

01 Mar 2019·Journal of Chromatographic ScienceQ4 · CHEMISTRY

Optimized liquid chromatography–tandem mass spectrometry for Otaplimastat quantification in rat plasma and brain tissue

Q4 · CHEMISTRY

Article

Author: Oh, Ju-Hee ; Shin, Naree ; Lee, Ji Hyeon ; Kim, Miri ; Lee, Seolhee ; Kim, Min Chang ; Park, Taehoon ; Lee, Joo Hyun ; Lee, Young-Joo

An optimized liquid chromatography-tandem mass spectrometry method for simple and sensitive quantification of Otaplimastat in rat plasma and brain tissue was developed and validated. Protein precipitation with acetonitrile was selected for sample preparation method based on recovery and matrix effect. The chromatographic separation of the sample was performed on a reverse-phase AQ column with an isocratic mobile phase consisting of 10 mM ammonium acetate (pH 4.0) and acetonitrile (50:50, v/v). The analyte was quantified by multiple reaction monitoring with a Waters Quattro micro™ API mass spectrometer. The lower limits of quantification were 20 ng/mL in plasma and 2 ng/g in brain, with the relative standard deviation % of 7.6 and 8.0% for plasma and brain samples, respectively. Acceptable intra-day and inter-day precisions and accuracies were obtained. Otaplimastat was sufficiently stable under all relevant analytical conditions, including a temperature of 4°C for 24 hr, room temperature 20°C for 24 hr, -80°C for 10 days and three freeze-thaw cycles (each at -80°C for 24 hr), for rat plasma and brain tissue. The validated method was successfully used to measure Otaplimastat concentrations in rat plasma and brain samples.

100 Deals associated with Stroquinan

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute Ischemic Stroke	Phase 3	United States	Shin Poog Pharmaceutical Co., Ltd.	14 Feb 2025

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04479449 \| NCT02787278 (Company_Website) Manual	Phase 2	Acute Ischemic Stroke	226	Otaplimastat	jqyoqtcvqm(ccputyciuj): Difference (%) = -89 View more	Positive	13 Feb 2025
				Placebo
NCT02787278 (SAFE-TPA, Pubmed) Manual	Phase 2	Acute Ischemic Stroke	80	Otaplimastat	(moovnayain) = The incidence of PH during stage 2 was comparable: 0 of 22 with the placebo, 0 of 22 with otaplimastat 40 mg, and 1 of 21 with the 80 mg dose. okwwabxgmi (vcsqqckocc ) View more	Positive	01 Feb 2020
				Placebo