Delving into the Latest Updates on Cefetamet Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Sodium cefetamet, cefetamet sodium salt

Target

PBPs

Action

inhibitors

Mechanism

PBPs inhibitors(Bacterial penicillin-binding protein inhibitors)

Therapeutic Areas

Infectious DiseasesMouth and Tooth DiseasesOtorhinolaryngologic Diseases+ [1]

Active Indication

Bacterial InfectionsAcute BronchitisPharyngolaryngitis+ [2]

Inactive Indication-

Originator Organization

Sichuan Direction Pharmaceutical Co. Ltd.

Active Organization

Hainan Yishun Pharmaceutical Co. Ltd.

Sichuan Direction Pharmaceutical Co. Ltd.Sichuan Antimicrobial Industry Research Institute

Inactive Organization-

License Organization-

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC14H15N5O5S2

InChIKeyMQLRYUCJDNBWMV-GHXIOONMSA-N

CAS Registry65052-63-3

View All Structures (2)

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。

[Translation]

Healthy adult subjects were used as research subjects to conduct single and multiple dosing tolerance studies on ceftriaxone sodium for injection (specifications: 0.5g/tablet and 1.0g/tablet) developed by Sichuan Xiangfang Pharmaceutical Co., Ltd., to observe the human body's tolerance and safety to ceftriaxone sodium for injection, and to determine the maximum tolerated dose (MTD) of ceftriaxone sodium for intravenous administration in healthy people, so as to provide a basis for clinical use and new drug registration.

Start Date-

Sponsor / Collaborator

Sichuan Direction Pharmaceutical Co. Ltd.

[+1]

CTR20131264

/ CompletedPhase 1

注射用头孢他美钠单次给药临床药代动力学/药效学研究；

[Translation] Clinical pharmacokinetic/pharmacodynamic study of single-dose cefetamet sodium for injection;

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。

[Translation]

The pharmacokinetic characteristics of ceftriaxone sodium for injection in healthy Chinese subjects were investigated by single constant-rate intravenous infusion of low, medium and high doses of ceftriaxone sodium for injection in healthy volunteers. Combined with the results of in vitro antibacterial activity assay, a PK/PD study of ceftriaxone sodium for injection was conducted to provide a basis for formulating the medication regimen for Phase II clinical trials.

Start Date07 Mar 2012

Sponsor / Collaborator

Hainan Yishun Pharmaceutical Co. Ltd.

[+1]

CTR20131864

/ Active, not recruitingPhase 1

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；

[Translation] A single-center, randomized, blinded, placebo-controlled phase I clinical tolerance trial of single and multiple doses of cefetamet sodium for injection in healthy humans;

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。

[Translation]

To observe the safety and tolerability of single and multiple administrations of ceftriaxone sodium for injection in healthy humans, evaluate the safe dosage range of single and multiple administrations of ceftriaxone sodium for injection in healthy humans, determine the maximum tolerated dose of single and multiple administrations in healthy humans, and provide a basis for formulating the dosing regimen for Phase I pharmacokinetic studies and Phase II clinical trials.

Start Date31 Oct 2011

Sponsor / Collaborator

Hainan Yishun Pharmaceutical Co. Ltd.

[+1]

100 Clinical Results associated with Cefetamet Sodium

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100 Translational Medicine associated with Cefetamet Sodium

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100 Patents (Medical) associated with Cefetamet Sodium

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257

Literatures (Medical) associated with Cefetamet Sodium

01 Jun 2025·Chemometrics and Intelligent Laboratory Systems

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

Author: 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.

01 Dec 2024·European Journal of Medicinal Chemistry

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

Article

Author: 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.

17 Apr 2024·Scientific reports

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

Article

Author: 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 Deals associated with Cefetamet Sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB13504

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Phase 1	China	Sichuan Direction Pharmaceutical Co. Ltd.	12 Jun 2015
Acute Bronchitis	Phase 1	China	Sichuan Antimicrobial Industry Research Institute	31 Oct 2011
Acute Bronchitis	Phase 1	China	Hainan Yishun Pharmaceutical Co. Ltd.	31 Oct 2011
Pharyngolaryngitis	Phase 1	China	Sichuan Antimicrobial Industry Research Institute	31 Oct 2011
Pharyngolaryngitis	Phase 1	China	Hainan Yishun Pharmaceutical Co. Ltd.	31 Oct 2011
Pneumonia	Phase 1	China	Hainan Yishun Pharmaceutical Co. Ltd.	31 Oct 2011
Pneumonia	Phase 1	China	Sichuan Antimicrobial Industry Research Institute	31 Oct 2011
Tonsillitis	Phase 1	China	Hainan Yishun Pharmaceutical Co. Ltd.	31 Oct 2011
Tonsillitis	Phase 1	China	Sichuan Antimicrobial Industry Research Institute	31 Oct 2011