Delving into the Latest Updates on Irsogladine Maleate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Irsogladine maleate (JP17)

+ [7]

Target

cGMP-PDE

Action

inhibitors

Mechanism

cGMP-PDE inhibitors(3',5'-cyclic phosphodiesterase inhibitors)

Therapeutic Areas

Digestive System Disorders

Active Indication

Acute gastritisChronic gastritisStomach Ulcer

Inactive Indication-

Originator Organization

Nippon Shinyaku Co., Ltd.

Active Organization

Nippon Shinyaku Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (20 Sep 1988),

Stomach Ulcer

Regulation-

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Structure/Sequence

Molecular FormulaC13H11Cl2N5O4

InChIKeyPJLVTVAIERNDEQ-BTJKTKAUSA-N

CAS Registry84504-69-8

View All Structures (2)

All patients who met the inclusion criteria and agreed to participate in the study underwent baseline capsule endoscopy. Patients with intestinal mucosal injury detected during the initial capsule endoscopy were randomly divided into isoladin maleate group or magnesium aluminum carbonate control group using computer-generated random numbers. Patients in the isoladine maleate group received 4 mg isoladine maleate (Gesellon, Japan) every morning for 4 weeks (or 8 weeks, duration to be determined); Magnesium aluminum carbonate control group received 1 g magnesium aluminum carbonate every morning, afternoon and evening for 4 weeks (or 8 weeks, course to be determined). After treatment, capsule endoscopy was performed again to evaluate the healing of intestinal mucosa.

Start Date01 Apr 2022

Sponsor / Collaborator

Lee's Pharmaceutical Holdings Ltd.

CTR20190535

/ CompletedNot Applicable

马来酸伊索拉定片的人体生物等效性研究

[Translation] Study on the bioequivalence of irsogladine maleate tablets in healthy volunteers

研究目的包括如下：评估受试制剂马来酸伊索拉定片（规格：4mg，齐鲁制药有限公司生产）和参比制剂马来酸伊索拉定片（Gaslon N）（规格：4mg，Nippon Shinyaku Co.,Ltd.）作用于空腹和餐后状态下健康成年受试者的生物等效性。评估受试制剂马来酸伊索拉定片（4mg）在健康受试者中的安全性。

[Translation]

The study objectives include the following: To evaluate the bioequivalence of the test preparation Isoladine Maleate Tablets (Specification: 4 mg, produced by Qilu Pharmaceutical Co., Ltd.) and the reference preparation Isoladine Maleate Tablets (Gaslon N) (Specification: 4 mg, Nippon Shinyaku Co., Ltd.) in healthy adult subjects in the fasting and fed state. To evaluate the safety of the test preparation Isoladine Maleate Tablets (4 mg) in healthy subjects.

Start Date02 Jan 2019

Sponsor / Collaborator

Qilu Pharmaceutical Co., Ltd.

NCT03509831

/ Unknown statusPhase 1

A Randomized, Open-label, Crossover Clinical Study to Assess the Safety and the Pharmacokinetic Characteristics of INT-2150 After Oral Administration to Healthy Adult Male Subjects

Assess the Safety and the Pharmacokinetic Characteristics of INT-2150 after Oral Administration to Healthy Adult Male Subjects

Start Date02 Nov 2017

Sponsor / Collaborator

KUKJE PHARMA Co., Ltd.

100 Clinical Results associated with Irsogladine Maleate

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100 Translational Medicine associated with Irsogladine Maleate

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100 Patents (Medical) associated with Irsogladine Maleate

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200

Literatures (Medical) associated with Irsogladine Maleate

10 Jan 2025·The Journal of Organic Chemistry

Sustainable Synthesis of Substituted 1,3,5-Triazines by [ONO]-Pincer-Supported Nickel(II) Complexes via an Acceptorless Dehydrogenative Coupling Strategy

Article

Author: Malecki, Jan Grzegorz ; Rengan, Ramesh ; Pennamuthiriyan, Anandaraj

A facile, cost-effective, and sustainable synthesis of substituted triazines from primary alcohols by newly synthesized nickel pincer-type complexes (1-3) has been described. Herein, we report the synthesis of a set of three well-defined Ni(II) O^N^O pincer-type complexes, structurally characterized by analytical, spectral, and X-ray diffraction techniques. Further, the nickel complexes are explored as efficient catalysts (4 mol %) for the construction of 2,4,6-substituted 1,3,5-triazines from readily available alcohols via an acceptorless dehydrogenative coupling (ADC) strategy. A wide range of substituted triazine derivatives (33 examples) has been synthesized from the coupling of alcohols and benzamidine/guanidine hydrochloride with a maximum isolated yield of 92% under mild conditions, with eco-friendly H₂O and H₂ gas as the only byproducts. A plausible mechanism has been proposed based on a sequence of control experiments. Interestingly, the short synthesis of the antiulcer drug irsogladine and the large-scale synthesis of 2,4-diphenyl-6-(p-tolyl)-1,3,5-triazine highlight the convenience of the current methodology.

01 Dec 2021·Molecular MedicineQ2 · MEDICINE

Identifying FDA-approved drugs with multimodal properties against COVID-19 using a data-driven approach and a lung organoid model of SARS-CoV-2 entry

Q2 · MEDICINE

ArticleOA

Author: Nixon, Douglas F ; Schwartz, Robert E ; Iñiguez, Luis P ; Chen, Shuibing ; Powell, Timothy R ; Marston, Jez L ; Duarte, Rodrigo R R ; Bram, Yaron ; Han, Yuling ; Copertino, Dennis C

AbstractBackgroundVaccination programs have been launched worldwide to halt the spread of COVID-19. However, the identification of existing, safe compounds with combined treatment and prophylactic properties would be beneficial to individuals who are waiting to be vaccinated, particularly in less economically developed countries, where vaccine availability may be initially limited.MethodsWe used a data-driven approach, combining results from the screening of a large transcriptomic database (L1000) and molecular docking analyses, with in vitro tests using a lung organoid model of SARS-CoV-2 entry, to identify drugs with putative multimodal properties against COVID-19.ResultsOut of thousands of FDA-approved drugs considered, we observed that atorvastatin was the most promising candidate, as its effects negatively correlated with the transcriptional changes associated with infection. Atorvastatin was further predicted to bind to SARS-CoV-2’s main protease and RNA-dependent RNA polymerase, and was shown to inhibit viral entry in our lung organoid model.ConclusionsSmall clinical studies reported that general statin use, and specifically, atorvastatin use, are associated with protective effects against COVID-19. Our study corroborrates these findings and supports the investigation of atorvastatin in larger clinical studies. Ultimately, our framework demonstrates one promising way to fast-track the identification of compounds for COVID-19, which could similarly be applied when tackling future pandemics.

14 Oct 2021·Journal of Medicinal ChemistryQ1 · MEDICINE

Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors

Q1 · MEDICINE

Article

Author: Yokoyama, Takeshi ; Kashihara, Mirai ; Mizuguchi, Mineyuki

Transthyretin (TTR) is a causative protein of TTR amyloidosis (ATTR amyloidosis), a general term for diseases characterized by deposition of TTR amyloid fibrils in specific organs. ATTR amyloidosis can be ameliorated by stabilization of the TTR tetramer through the binding of small molecules. Here, we show that the clinical anthelmintic drugs bithionol (42) and triclabendazole (43) potently inhibit aggregation of the amyloidogenic variant V30M-TTR. A competitive binding assay using a fluorescence probe showed that the binding affinity of 42 with V30M-TTR was significantly higher than that of the first-in-class drug tafamidis (1), and the binding affinity of 43 was similar to that of 1. The crystallographic and thermodynamic analysis revealed that 42 efficiently occupied the halogen-binding grooves of TTR, resulting in the favorable binding entropy. Multifaceted in vitro studies of anthelmintic drugs have the potential to reposition these drugs as ATTR amyloidosis inhibitors.

100 Deals associated with Irsogladine Maleate

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External Link

KEGG	Wiki	ATC	Drug Bank
D01658	Irsogladine Maleate	A02B	DB13056

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Acute gastritis	Japan	Nippon Shinyaku Co., Ltd.	07 Sep 1994
Chronic gastritis	Japan	Nippon Shinyaku Co., Ltd.	07 Sep 1994
Stomach Ulcer	Japan	Nippon Shinyaku Co., Ltd.	20 Sep 1988