头孢他美钠(Cefetamet Sodium) - 药物靶点：PBPs_在研适应症：细菌感染，急性支气管炎，咽喉炎_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Sodium cefetamet、cefetamet sodium salt

靶点

PBPs

作用方式

抑制剂

作用机制

PBPs抑制剂(细菌青霉素结合蛋白家族抑制剂)

治疗领域

感染口颌疾病耳鼻咽喉疾病+ [1]

在研适应症

细菌感染急性支气管炎咽喉炎+ [2]

非在研适应症-

原研机构

四川方向药业有限责任公司

在研机构

海南伊顺药业有限公司

四川方向药业有限责任公司四川抗菌素工业研究所有限公司

非在研机构-

权益机构-

最高研发阶段临床1期

首次获批日期-

最高研发阶段(中国)临床1期

特殊审评-

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结构/序列

分子式C14H15N5O5S2

InChIKeyMQLRYUCJDNBWMV-GHXIOONMSA-N

CAS号65052-63-3

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关联

3

项与头孢他美钠相关的临床试验

CTR20130539

/ Not yet recruiting临床1期

评价注射用头孢他美钠在健康成年志愿者中的耐受性的随机、开放、非对照、单一剂量递增的I期研究

以健康成年受试者为研究对象，对四川方向药业有限责任公司研制的注射用头孢他美钠（规格为0.5g/片、1.0g/片）进行单次给药和多次给药的耐受性研究，观察人体对注射用头孢他美钠的耐受程度和安全性，确定头孢他美钠静脉给药对健康人群的最大耐受剂量（MTD），为临床用药及新药注册提供依据。

开始日期-

申办/合作机构

四川方向药业有限责任公司

[+1]

CTR20131264

/ Completed临床1期

注射用头孢他美钠单次给药临床药代动力学/药效学研究；

通过健康志愿受试者分别单次恒速静脉滴注低、中、高剂量注射用头孢他美钠，考察其在中国健康人体内的药代动力学特征，并结合体外抗菌活性测定结果，进行注射用头孢他美钠PK/PD研究，为制定II期临床试验用药方案提供依据。

开始日期2012-03-07

申办/合作机构

海南伊顺药业有限公司

[+1]

CTR20131864

/ Active, not recruiting临床1期

单中心、随机、盲法、安慰剂平行对照注射用头孢他美钠在健康人体单次和多次给药的I期临床耐受性试验；

观察健康人体单次和多次接受注射用头孢他美钠的安全性和耐受性，评估注射用头孢他美钠在健康人体单次和多次给药的安全剂量范围，确定健康人体单次和多次用药的最大耐受量，为制定I期药代动力学研究及II期临床试验给药方案提供依据。

开始日期2011-10-31

申办/合作机构

海南伊顺药业有限公司

[+1]

100 项与头孢他美钠相关的临床结果

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100 项与头孢他美钠相关的转化医学

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100 项与头孢他美钠相关的专利（医药）

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257

项与头孢他美钠相关的文献（医药）

2025-06-01·Chemometrics and Intelligent Laboratory Systems

AQbD approach for the development of an analytical procedure for the separation of cephalosporin drugs and their degradation products

作者: Lourenco, Felipe Rebello ; Passarin, Paula Beatriz Silva ; Yonamine, Mauricio ; Okamoto, Rogerio Takao ; Dorr, Fabiane

In the pharmaceutical industry, anal. procedures are used to conduct research, development and quality control of drugs and medicines.Given the importance of the Anal. Quality by Design (AQbD) approach in the rational development of anal. procedures, especially by minimizing the need for experiments, acquiring and improving knowledge during development and ensuring the flexibility of the method, this study aimed to develop an anal. procedure, based on AQbD principles, for the identification and quantification of different cephalosporins, as well as to create a tool for defining the method operable design region.The initial screening phase of anal. development was carried out using an in silico tool developed in a previous study.During the anal. development phase, a forced degradation study was performed using Liquid Chromatog. Coupled to Mass Spectrometry (LC-MS) to identify cephalosporin degradation products.The developed method, along with its Method Operable Design Region (MODR), was validated, resulting in a robust and flexible anal. procedure for identifying and quantifying different cephalosporins in accordance with AQbD principles.The proposed tool considers multiple chromatog. responses, target uncertainty and desired confidence level, simplifying the verification of compliance with quality requirements defined in Anal. Target Profile, offering a reliable process that adapts to parameter changes, maintaining the quality of results.

2024-12-01·European Journal of Medicinal Chemistry

Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds

Article

作者: Šácha, Pavel ; Šimková, Adéla ; Konvalinka, Jan ; Staňurová, Jana ; Wichterle, Filip ; Čermáková, Kateřina ; Bušek, Petr ; Kryštůfek, Robin ; Vaníčková, Zdislava

Fibroblast activation protein (FAP) has been extensively studied as a cancer biomarker for decades. Recently, small-molecule FAP inhibitors have been widely adopted as a targeting moiety of experimental theranostic radiotracers. Here we present a fast qPCR-based analytical method allowing FAP inhibition screening in a high-throughput regime. To identify clinically relevant compounds that might interfere with FAP-targeted approaches, we focused on a library of FDA-approved drugs. Using the DNA-linked Inhibitor Antibody Assay (DIANA), we tested a library of 2667 compounds within just a few hours and identified numerous FDA-approved drugs as novel FAP inhibitors. Among these, prodrugs of cephalosporin antibiotics and reverse transcriptase inhibitors, along with one elastase inhibitor, were the most potent FAP inhibitors in our dataset. In addition, by employing FAP DIANA in the quantification mode, we were able to determine FAP concentrations in human plasma samples. Together, our work expands the repertoire of FAP inhibitors, analyzes the potential interference of co-administered drugs with FAP-targeting strategies, and presents a sensitive and low-consumption ELISA alternative for FAP quantification with a detection limit of 50 pg/ml.

2024-04-17·Scientific reports

Non-animal models for blood–brain barrier permeability evaluation of drug-like compounds

Article

作者: Preissner, Robert ; Dixit, Vaibhav A ; Dehnbostel, Frederic O ; Banerjee, Priyanka

AbstractDiseases related to the central nervous system (CNS) are major health concerns and have serious social and economic impacts. Developing new drugs for CNS-related disorders presents a major challenge as it actively involves delivering drugs into the CNS. Therefore, it is imperative to develop in silico methodologies to reliably identify potential lead compounds that can penetrate the blood–brain barrier (BBB) and help to thoroughly understand the role of different physicochemical properties fundamental to the BBB permeation of molecules. In this study, we have analysed the chemical space of the CNS drugs and compared it to the non-CNS-approved drugs. Additionally, we have collected a feature selection dataset from Muehlbacher et al. (J Comput Aided Mol Des 25(12):1095–1106, 2011. 10.1007/s10822-011-9478-1) and an in-house dataset. This information was utilised to design a molecular fingerprint that was used to train machine learning (ML) models. The best-performing models reported in this study achieved accuracies of 0.997 and 0.98, sensitivities of 1.0 and 0.992, specificities of 0.971 and 0.962, MCCs of 0.984 and 0.958, and ROC-AUCs of 0.997 and 0.999 on an imbalanced and a balanced dataset, respectively. They demonstrated overall good accuracies and sensitivities in the blind validation dataset. The reported models can be applied for fast and early screening drug-like molecules with BBB potential. Furthermore, the bbbPythoN package can be used by the research community to both produce the BBB-specific molecular fingerprints and employ the models mentioned earlier for BBB-permeability prediction.

100 项与头孢他美钠相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB13504

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
细菌感染	临床1期	中国	四川方向药业有限责任公司	2015-06-12
急性支气管炎	临床1期	中国	四川抗菌素工业研究所有限公司	2011-10-31
急性支气管炎	临床1期	中国	海南伊顺药业有限公司	2011-10-31
咽喉炎	临床1期	中国	四川抗菌素工业研究所有限公司	2011-10-31
咽喉炎	临床1期	中国	海南伊顺药业有限公司	2011-10-31
肺炎	临床1期	中国	海南伊顺药业有限公司	2011-10-31
肺炎	临床1期	中国	四川抗菌素工业研究所有限公司	2011-10-31
扁桃体炎	临床1期	中国	海南伊顺药业有限公司	2011-10-31
扁桃体炎	临床1期	中国	四川抗菌素工业研究所有限公司	2011-10-31