Delving into the Latest Updates on Sodium ilaprazole with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

壹丽安

Target

Proton pump

Action

inhibitors

Mechanism

Proton pump inhibitors

Therapeutic Areas

Digestive System DisordersOther Diseases

Active Indication

Peptic Ulcer HemorrhageHemorrhagePeptic Ulcer+ [4]

Inactive Indication

Stress ulcer

Originator Organization

Livzon Group Livzon Pharmaceutical Factory

Active Organization

Livzon Group Livzon Pharmaceutical Factory

Lizhu Group Lizhu Medicine Research Institute

Inactive Organization

Livzon Pharmaceutical Group, Inc.

Drug Highest PhaseApproved

First Approval Date

China (28 Dec 2017),

Peptic Ulcer Hemorrhage

RegulationPriority Review (China)

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Structure/Sequence

Molecular FormulaC19H18N4NaO2S

InChIKeyMBRFHFBLZWUGKR-UHFFFAOYSA-N

CAS Registry172152-50-0

主要目的：通过评价使用注射用艾司奥美拉唑钠和注射用艾普拉唑钠预防重症受试者发生临床显著意义的上消化道出血的比例，对比其在预防重症受试者应激性溃疡出血的疗效；次要目的：评估和比较使用注射用艾司奥美拉唑钠和注射用艾普拉唑钠发生任何上消化道出血的比例；评估和比较使用注射用艾司奥美拉唑钠和注射用艾普拉唑钠发生任何上消化道出血的时间（单位：小时）；评价注射用艾普拉唑钠用于重症受试者的安全性和耐受性。

[Translation]

main purpose: To evaluate the proportion of clinically significant upper gastrointestinal bleeding in severe subjects using esomeprazole sodium for injection and ilaprazole sodium for injection, and compare their effectiveness in preventing stress ulcers in severe subjects Curative effect on bleeding; Secondary purposes: To assess and compare the proportion of any upper gastrointestinal bleeding occurring with esomeprazole sodium for injection and ilaprazole sodium for injection; To assess and compare the time (in hours) to the occurrence of any upper gastrointestinal bleeding with esomeprazole sodium for injection and ilaprazole sodium for injection; To evaluate the safety and tolerability of ilaprazole sodium for injection in critically ill subjects.

Start Date16 Jul 2021

Sponsor / Collaborator

Livzon Group Livzon Pharmaceutical Factory

NCT05841394

/ CompletedPhase 3

A Multi-center, Double-blinding, Parallel and Positive-controlled Phase III Clinical Trial for Efficacy and Safety Evaluation of Ilaprazole Sodium for Injection on Treatment of Prevention of Stress Ulcer Bleeding (Ilaprazole i.v. vs Esomeprazole, i.v.)

The purpose of this study is to evaluate the efficacy of the study drug (Ilaprazole Sodium for Injection) for potential effect on preventing stress ulcer bleeding in vulnerable population by comparing the radio of upper gastrointestinal bleeding when they are administered Ilaprazole Sodium for Injection and Esomeprazole Sodium for Injection respectively.

Start Date16 Jul 2021

Sponsor / Collaborator

Livzon Pharmaceutical Group, Inc.

CTR20133004

/ RecruitingPhase 2

注射用艾普拉唑钠治疗消化性溃疡出血有效性和安全性的多中心、随机、双盲、阳性药物平行对照Ⅱ期临床试验

[Translation] A multicenter, randomized, double-blind, positive drug parallel controlled phase II clinical trial on the efficacy and safety of ilaprazole sodium injection in the treatment of peptic ulcer bleeding

探索注射用艾普拉唑钠治疗消化性溃疡出血/预防再出血的疗效和安全性，为Ⅲ期临床试验提供依据

[Translation]

To explore the efficacy and safety of ilaprazole sodium for injection in the treatment of peptic ulcer bleeding/prevention of rebleeding and provide a basis for Phase III clinical trials

Start Date20 Feb 2014

Sponsor / Collaborator

Livzon Group Livzon Pharmaceutical Factory

[+1]

100 Clinical Results associated with Sodium ilaprazole

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100 Translational Medicine associated with Sodium ilaprazole

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100 Patents (Medical) associated with Sodium ilaprazole

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4

Literatures (Medical) associated with Sodium ilaprazole

01 Jul 2022·European Journal of Pharmacology

Identifying chronic alcoholism drug disulfiram as a potent DJ-1 inhibitor for cancer therapeutics

Article

Author: Yuan, Meng ; Zhang, Mingyang ; He, Qiaojun ; Jiang, Li ; Wen, Yuanmei ; He, Peihao ; Wu, Qian ; Yang, Bo ; Cao, Ji

As a key regulator involved in tumor development and progression, DJ-1 has been proposed as a potential therapeutic target against cancer. Also, the development of DJ-1 inhibitors holds great interests in cancer treatment. In the current study, by utilizing a small molecule covalent compounds library screening, we found that disulfiram (DSF), an FDA-approved chronic alcoholism drug, is a potent DJ-1 inhibitor. Glyoxalase assay and microscale thermophoresis analysis suggested that DSF exhibits strong inhibitory activity and high affinity to DJ-1 protein. Additionally, DSF similarly inhibited the methylglyoxal detoxification function of DJ-1 protein at the intracellular level. Notably, we discovered that DSF could significantly enhance N-(4-hydroxyphenyl) retinamide-based proliferation inhibition and apoptosis induction in different types of cancer cell lines, but not in normal tissue lines. Thus, our data suggest DSF functions as a potential inhibitor targeting DJ-1, which may provide a potential synergistic treatment option for cancer therapy.

01 Apr 2020·European Journal of Pharmaceutics and BiopharmaceuticsQ2 · MEDICINE

The study of intestinal absorption and biodistribution in vivo of proton pump inhibitors

Q2 · MEDICINE

Article

Author: Jin, Zhaolei ; Li, Qingpo ; Jiang, Xindong ; Li, Chunlong ; Hou, Xuemei ; Shen, Tianxiang ; Ji, Qiuzhi ; Wang, Wei ; Long, Hongxin ; Qiu, Weigen ; You, Jian

The major therapeutic strategy for acid-related gastrointestinal diseases in clinic is to reduce the excretion of gastric acid by oral administration of proton-pump inhibitors (PPIs). However, it is quite a challenge to study the oral absorption behaviors of PPIs considering their extreme instability under gastrointestinal environment. As a result, little information has been reported on PPI oral absorption so far, hindering the further development of PPI-contained oral preparations. Here, we first investigated the degradation rate of three representative PPIs, including ilaprazole, ilaprazole sodium and rabeprazole sodium. Then a modified in situ intestine absorption method in rat was established: through the temperature control by the heat exchangers, the perfusate was kept at physiological temperature only when passing through the intestine while it was maintained at 4 °C outside the intestine. Therefore PPIs could maintained sufficiently high stability under proper temperature control. Our data demonstrated that both ilaprazole and ilaprazole sodium exhibited significantly higher absorption efficiency than rabeprazole sodium did through the comparison of their apparent permeability coefficients and steady-state plasma concentrations after perfusion in the duodenum, jejunum, ileum and colon, mainly attributing to their more suitable oil-water partition coefficient. The duodenum could be the best site for the oral absorption of PPIs. Ilaprazole outperformed its sodium salt form with its stable absorption behavior in tested four intestinal segments. Furthermore, after intravenous or oral administration, ilaprazole exhibited a longer residence time and a higher accumulation in the stomach than in most of other tissues/organs. However, it was also found that the accumulation was heterogeneous and mainly located in mucosa cells of the stomach. Our further study indicated that there was no significant difference on the oral absorption efficiency of ilaprazole between female and male rats but ilaprazole underwent a faster metabolism in male rats after oral absorption. Our study provided a valuable guidance for the design of oral formulation and the optimization of PPI-contained formulations.

PLOS ONE

Physical compatibility of Xuebijing injection with 53 intravenous drugs during simulated Y-site administration

Article

Author: Ding, Haiwen ; Li, Peifang ; Huang, Ying ; Tong, Tong ; Liu, Sheng

ObjectiveXuebijing injection (XBJ) is a commonly used herbal medicine injection in China. However, the physical compatibility of XBJ with other intravenous drugs remains unclear. The purpose of this research is to evaluate physical compatibility of Xuebijing injection (XBJ) with 53 intravenous drugs (including 31 Chinese medicine injections and 22 chemicals) during simulated Y-site administration.MethodsY-site administration was simulated in vitro by admixing 0.33 ml/ml XBJ with an equal volume of other diluted 53 intravenous drugs, respectively. Physical compatibility including visual inspection, Tyndall beam, particle limits, turbidity, pH, chromacity value, spectroscopic absorption of 550 nm and 420 nm (A550 nmand A420 nm) were observed and assessed at 0, 1, 2, and 4 h. Physical compatibility was defined as all solutions with no color changes, no gas evolution, particulate formation and no Tyndall beam within 4 hours, turbidity changes <0.5 nephelometric turbidity unit (NTU) compared to 0 h, particle limits allowed by the Chinese Pharmacopoeia (Ch.P) 2020 edition, pH changes <10% compared to 0, chromacity value changes <200 compared to 0 h, or photometrical changes of A420 nm<0.0400 or A550 nm<0.0100 compared to 0 h.ResultsXBJ was physically incompatible with 27 of the 53 intravenous drugs tested, 26 were compatible with XBJ for 4 h.ConclusionsXBJ should not be simultaneously co-administered with 27 of the 53 intravenous drugs during simulated Y-site. If coadministration was inevitable, flushing tube with NS or D5W before and after infusion of XBJ was needed. Assessment included visual inspection, Tyndall beam, turbidity measurement, particle counts, pH measurement, chromacity value measurement and absorption of A550 nmwere proved to be valid and robust for the quality control of infusion and compatibility of Chinese herbal injection.

100 Deals associated with Sodium ilaprazole

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External Link

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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Peptic Ulcer Hemorrhage	China	Livzon Group Livzon Pharmaceutical Factory	28 Dec 2017

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hemorrhage	Phase 3	China	Livzon Group Livzon Pharmaceutical Factory	30 Oct 2014
Hemorrhage	Phase 3	China	Lizhu Group Lizhu Medicine Research Institute	30 Oct 2014
Peptic Ulcer	Phase 3	China	Livzon Group Livzon Pharmaceutical Factory	30 Oct 2014
Peptic Ulcer	Phase 3	China	Lizhu Group Lizhu Medicine Research Institute	30 Oct 2014
Stress ulcer	Phase 2	China	Livzon Pharmaceutical Group, Inc.	16 Jul 2021
Duodenal Ulcer	Phase 2	China	Lizhu Group Lizhu Medicine Research Institute	10 Oct 2014
Duodenal Ulcer	Phase 2	China	Livzon Group Livzon Pharmaceutical Factory	10 Oct 2014
Gastric mucosal lesion	Phase 1	China	Livzon Group Livzon Pharmaceutical Factory	23 Oct 2015
Gastric mucosal lesion	Phase 1	China	Lizhu Group Lizhu Medicine Research Institute	23 Oct 2015
Stomach Ulcer	Phase 1	China	Livzon Group Livzon Pharmaceutical Factory	23 Oct 2015