Delving into the Latest Updates on Norvancomycin Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Chemical drugs

Synonyms

NVCM

Target

Peptidoglycan

Action

inhibitors

Mechanism

Peptidoglycan inhibitors

Therapeutic Areas

Infectious Diseases

Active Indication

Bacterial Infections

Inactive Indication-

Originator Organization

North China Pharmaceutical Huasheng Co., Ltd.

Active Organization

North China Pharmaceutical Huasheng Co., Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

China (01 Jan 1995),

Bacterial Infections

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC65H73Cl2N9O24

InChIKeyNUAQIRUAZSJTAI-YRPZDAAMSA-N

CAS Registry91700-98-0

An analytical assay based on ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) technique for absolute quantification of vancomycin in complexed biological matrix was developed in this study. Reversed phase column with gradient elution was chosen for chromatographic separation of vancomycin and internal standard (IS) norancomycin. Sample pretreatment was performed by micro-solid phase extraction (μ-SPE) with Oasis® MAX μElution Plate (I.D., 30 μm). Multiple reaction monitoring (MRM) transition was chosen for monitoring of the analytes. For vancomycin, mass-to-charge ratio (m/z) of the MRM transition was 725.3→144.1; For norvancomycin, m/z of the MRM transition was 718.3→144.2. The running time was 3 minutes for each sample. The UHPLC-MS/MS method showed a good linear relationship (R²≥0.995) in the concentration range of 0.5-100 μg/mL. The intra- and inter-day accuracies (relative error, RE) are within the range of -3.44 %-1.50 % and precisions are between 3.48 % and 10.19 %. μ-SPE could enrich the analytes and decrease the endogenous interferences, thereby improving the selectivity and sensitivity of the method. The analytical assay is selective, accurate and reproducible. The assay was successfully applied to therapeutic drug monitoring of vancomycin in clinical application.

28 Nov 2024·Journal of Medicinal Chemistry

Single Amine or Guanidine Modification on Norvancomycin and Vancomycin to Overcome Multidrug-Resistance through Augmented Lipid II Binding and Increased Membrane Activity

Article

Author: Zou, Xiangman ; Chen, Zhifu ; Zhang, Jinyong ; Guan, Dongliang ; Li, Fang ; Li, Yi ; Zhang, Jingwen ; Luo, Youhong ; Bian, Xiaolei ; Wang, Xiaowen ; Wang, Hui ; Xie, Yuanyuan

Vancomycin and norvancomycin have diminished antibacterial efficacy due to acquired or intrinsic resistance from mutations in the terminal dipeptide of lipid II in Gram-positive bacteria or failure to penetrate into the periplasm in Gram-negative bacteria. Herein, we rationally designed and synthesized a series of vancomycin analogues bearing single amine or guanidine functionality, altering various linkers and modification sites, to combat the resistance. Extensive antibacterial screening was performed to delineate a comprehensive SAR. Many derivatives revitalized the activity in vitro, exhibiting a 4-128-fold or 2-16-fold enhancement against the acquired or intrinsic resistance with lower toxicity. Significantly, the optimal compound 4g demonstrated greater pharmacokinetic and pharmacodynamic profiles. Further studies uncovered additional independent and synergistic mechanisms for 4g, including the enhanced membrane activity and augmented inhibition of peptidoglycan biosynthesis via increased lipid II binding, highlighting its potential as a future lead candidate to replenish the glycopeptide antibiotic arsenal.

16 Nov 2024·Critical Reviews in Analytical Chemistry

Macrocyclic Antibiotics as Effective Chiral Selectors in Liquid Chromatography for Enantiomeric Separation of Pharmaceutical Compounds: A Review

Review

Author: Salman, Basma E. ; Mahmoud, Abdelrahman ; El-Sayed, Doaa H. ; Alzarak, Tasneem M. ; Bakr, Hanan H. ; Fouad, Ali ; Adel, Shahd E.

Chiral separation techniques play a crucial role in the pharmaceutical industry, where the enantiomeric purity of drugs can have a significant impact on their efficacy and safety. Macrocyclic antibiotics are highly effective chiral selectors used in various chiral separation techniques, including LC, HPLC, SMB, and TLC, offering reproducible results and a wide range of applications. However, developing robust and efficient immobilization mechanisms for these chiral selectors remains a challenge. This review article focuses on various immobilization approaches, such as immobilization, coating, encapsulation, and photosynthesis, that have been applied to immobilize macrocyclic antibiotics on their support. Commercially available macrocyclic antibiotics for conventional liquid chromatography include Vancomycin, Norvancomycin, Eremomycin, Teicoplanin, Ristocetin A, Rifamycin, Avoparcin, Bacitracin, and others. In addition, capillary (nano) liquid chromatography has also been used in chiral separation utilizing Vancomycin, Polymyxin B, Daptomycin, and Colistin Sulfate. Macrocyclic antibiotic-based CSPs have been extensively applied due to their reproducible results, ease of use, and broad range of applications, capable of separating a large number of racemates.

100 Deals associated with Norvancomycin Hydrochloride

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	J01	-

R&D Status

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Bacterial Infections	China	North China Pharmaceutical Huasheng Co., Ltd.	01 Jan 1995

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ARVO2020	Not Applicable	-	-	norvancomycin (Continuous Topical Ocular Instillation Drug Delivery (CTOIDD))	(pnabqamtnn) = rzvnzulupo kenqffrxry (xodojxndik )	-	01 Jun 2020