Prednisolone sodium metazoate(Prednisolone sodium metazoate) - 药物靶点：GR_专利_临床

概要

基本信息

药物类型

小分子化药

别名

COLAL-PRED、Prednisolone 21-(sodium 3-sulfobenzoate)、Prednisolone metasulfobenzoate sodium

+ [4]

靶点

GR

作用机制

GR激动剂(糖皮质激素受体激动剂)

治疗领域

免疫系统疾病神经系统疾病消化系统疾病+ [1]

在研适应症-

非在研适应症

溃疡性结肠炎多发性硬化症

原研机构

Alizyme Plc

在研机构-

非在研机构

Alizyme Plc

Prometheus Biosciences, Inc.

最高研发阶段无进展临床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C28H32O9S

InChIKeyWVKSUFYQOHQCMM-YGZHYJPASA-N

CAS号3694-41-5

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关联

3

项与 Prednisolone sodium metazoate 相关的临床试验

NCT00676832 / Completed临床2期

A Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Dose-Ranging Study of COLAL-PRED in the Treatment of Patients With Moderate to Severe Ulcerative Colitis

The purpose of this study is to determine whether COLAL-PRED is a safe and effective treatment for patients with moderate to severe ulcerative colitis.

开始日期2008-05-01

申办/合作机构

Prometheus Biosciences, Inc.

NCT00299013 / Completed临床3期

A Multicentre, Randomised, Double Blind, Double Dummy, Active Comparator Controlled, Parallel Group Study of COLAL-PRED® in the Treatment of Moderate Acute Ulcerative Colitis

The purpose of this study is to investigate whether a novel dosage form of a prednisolone ester, called COLAL-PRED®, is useful in the treatment of ulcerative colitis.

开始日期2006-03-01

申办/合作机构

Alizyme Plc

ISRCTN14133410 / CompletedN/A

A safety and efficacy study of a novel formulation of prednisolone metasulfobenzoate (predocol) in the induction of remission and maintenance in patients with ulcerative colitis

开始日期2000-11-01

申办/合作机构-

100 项与 Prednisolone sodium metazoate 相关的临床结果

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100 项与 Prednisolone sodium metazoate 相关的转化医学

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100 项与 Prednisolone sodium metazoate 相关的专利（医药）

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20

项与 Prednisolone sodium metazoate 相关的文献（医药）

2023-07-14·Pharmaceutics

Formulation and Evaluation of Prednisolone Sodium Metazoate-Loaded Mucoadhesive Quatsomal Gel for Local Treatment of Recurrent Aphthous Ulcers: Optimization, In Vitro, Ex Vivo, and In Vivo Studies.

Article

作者: Abdellatif, Menna M ; Kassem, Ashraf ; Refai, Hanan ; El-Nabarawi, Mohamed A

This study aims to formulate a buccal mucoadhesive gel containing prednisolone sodium metazoate-loaded quatsomes for efficient localized therapy of recurrent aphthous ulcers. Quatsomes were prepared using a varied concentration of quaternary ammonium surfactants (QAS) and cholesterol (CHO). A 2³ factorial design was conducted to address the impact of independent variables QAS type (X₁), QAS to CHO molar ratio (X₂), and sonication time (X₃). The dependent variables were particle size (PS; Y₁), polydispersity index (PDI; Y₂), zeta potential (ZP; Y₃), entrapment efficiency percent (EE%; Y₄) and percent of drug released after 6 h (Q6%: Y₅). Then, the selected quatsomes formula was incorporated into different gel bases to prepare an optimized mucoadhesive gel to be evaluated via in vivo study. The PS of the developed quatsomes ranged from 69.47 ± 0.41 to 113.28 ± 0.79 nm, the PDI from 0.207 ± 0.004 to 0.328 ± 0.004, ZP from 45.15 ± 0.19 to 68.1 ± 0.54 mV, EE% from 79.62 ± 1.44 to 98.60% ± 1.22 and Q6% from 58.39 ± 1.75 to 94.42% ± 2.15. The quatsomal mucoadhesive gel showed rapid recovery of ulcers, which was confirmed by the histological study and the evaluation of inflammatory biomarkers. These results assured the capability of the developed quatsomal mucoadhesive gel to be a promising formulation for treating buccal diseases.

2022-02-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Novel benzothiazole-based dual VEGFR-2/EGFR inhibitors targeting breast and liver cancers: Synthesis, cytotoxic activity, QSAR and molecular docking studies

4区 · 医学

Review

作者: El Kerdawy, Ahmed M ; Naglah, Ahmed M ; Abd El-Meguid, Eman A ; Moustafa, Gaber O ; Awad, Hanem M

A novel series of benzothiazole-based derivatives linked to various amino acids and their corresponding ethyl ester analogues were prepared and were initially evaluated for their anticancer activity againstMCF-7 and HepG-2 and were further assessed as VEGFR-2 inhibitors. All the newly synthesized benzothiazole derivatives showed promising cytotoxic activities against the tested cell lines. Derivatives exhibited potent cytotoxic and VEGFR-2 inhibitory activities were then evaluated further as anticancer agents against the resistant MDA-MB-231 and as EGFR inhibitors. The carboxylic acid derivatives 10-12 and their ester analogues 21-23 displayed the highest anticancer activities with IC₅₀ of 0.73-0.89 µM, against MCF-7 and IC₅₀ of 2.54-2.80 µM, against HepG-2; compared to doxorubicin (IC₅₀ = 1.13 and 2.75 µM, respectively); also they showed safety towards the normal cell line, the ethyl ester derivatives 21-23 showed a potent activity against the resistant MDA-MB-231 cell line with IC₅₀ of 5.45-7.28 µM, relative to doxorubicin (IC₅₀ = 7.46 µM) surpassing their carboxylic acid analogues 10-12 (IC₅₀ of 8.88-11.02 µM). Furthermore, the promising derivatives 10-12 and 21-23 displayed promising VEGFR-2 inhibitory activity (IC₅₀ = 0.15-0.19 µM) comparable to that of sorafenib (IC₅₀ = 0.12 µM). Against EGFR, the ethyl ester derivatives 21-23 showed superior inhibitory activity relative to the used reference standard, erlotinib, with IC₅₀ of 0.11-0.16 vs. 0.18 µM, respectively. The QSAR study revealed that the molecular bulkiness and molecular partial charge distribution govern the kinase inhibition potency in this series. Furthermore, the molecular docking study in VEGFR-2 active site showed that the novel synthesized benzothiazole derivatives adopted the common binding pattern of type II PK inhibitors.

2019-10-01·Virologica Sinica2区 · 医学

Development of a Specific CHIKV-E2 Monoclonal Antibody for Chikungunya Diagnosis

2区 · 医学

Article

作者: Poo, Haryoung ; Lee, Hee-Jung ; Yang, Jihyun ; Kim, Jaemoo ; Kim, Young Bong ; Kim, Sehyun

Chikungunya fever is a vector-borne viral disease transmitted to humans by chikungunya virus (CHIKV)-infected mosquitoes. There have been many outbreaks of CHIKV infection worldwide, and the virus poses ongoing risks to global health. To prevent and control CHIKV infection, it is important to improve the current CHIKV diagnostic approaches to allow for the detection of low CHIKV concentrations and to correctly distinguish CHIKV infections from those due to other mosquito-transmitted viruses, including dengue virus (DENV), Japanese encephalitis virus (JEV), and Zika virus (ZIKV). Here, we produced monoclonal antibodies (mAbs) against the CHIKV envelope 2 protein (CHIKV-E2) and compared their sensitivity and specificity with commercially available mAbs using enzyme-linked immunosorbent assays (ELISA). Two anti-CHIKV-E2 mAbs, 19-1 and 21-1, showed higher binding affinities to CHIKV-E2 protein than the commercial mAbs did. In particular, the 19-1 mAb had the strongest binding affinity to inactivated CHIKV. Moreover, the 19-1 mAb had very little cross-reactivity with other mosquito-borne viruses, such as ZIKV, JEV, and DENV. These results suggest that the newly produced anti-CHIKV-E2 mAb, 19-1, could be used for CHIKV diagnostic approaches.

100 项与 Prednisolone sodium metazoate 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D08413	Prednisolone sodium metazoate	-	DB05340

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
溃疡性结肠炎	临床3期	捷克	Alizyme Plc	2006-03-01
溃疡性结肠炎	临床3期	瑞典	Alizyme Plc	2006-03-01
溃疡性结肠炎	临床3期	波兰	Alizyme Plc	2006-03-01
溃疡性结肠炎	临床3期	西班牙	Alizyme Plc	2006-03-01
溃疡性结肠炎	临床3期	英国	Alizyme Plc	2006-03-01
溃疡性结肠炎	临床3期	丹麦	Alizyme Plc	2006-03-01
溃疡性结肠炎	临床3期	法国	Alizyme Plc	2006-03-01
溃疡性结肠炎	临床3期	比利时	Alizyme Plc	2006-03-01
溃疡性结肠炎	临床3期	意大利	Alizyme Plc	2006-03-01
溃疡性结肠炎	临床3期	澳大利亚	Alizyme Plc	2006-03-01