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Second-generation glycopeptide antibiotic research
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Second-generation glycopeptide antibiotic research
Author: Shang Xin-Yan Juan Li-ju-jun XU Ji-Yang Dai-Jie Chen
Abstract With the continuing escalation of drug-resistant bacteria, vancomycin-resistant enterococci, a high degree of resistance to glycopeptide antibiotics in the emergence of Staphylococcus aureus, giving the clinical anti-infective therapy has brought great difficulties. Development of new glycopeptide antibiotics without delay. People to vancomycin and other natural glycopeptide antibiotics, chemical modification, has been a series of valuable derivatives, in which oritavancin, dalbavancin and telavancin has entered Phase Ⅲ clinical and registration of new medicines. In this paper, the second-generation glycopeptide antibiotics structural features, pharmacodynamics and pharmacokinetic characteristics and clinical application are reviewed.
Keywords: second-generation glycopeptide antibiotic Oritavancin Dalbavancin Telavancin
ABSTRACT Development of resistance to antibacterial agents, especially the advent of vancomycin resistant Enterococcus (VRE) and glycopeptide resistant Staphylococcus aureus (GRSA) is a mounting problem that continues to compromise the clinical effectiveness of anti infectious drugs. It is essential to develop new glycopeptide antibiotics. Three of these new derivatives obtained by semi synthesis starting from natural compounds, are now in clinical development (oritavancin and telavancin, as derivatives of vancomycin; and dalbavancin, as a derivative of teicoplanin). The review focuses on the structures , pharmacokinetic and pharmacodynamic parameters and the clinical research status related to the second generation glycopeptide antibiotics.
KEY WORDS The second generation glycopeptide antibiotics; Oritavancin; Dalbavancin; Telavancin
Ever since penicillin was discovered and used in clinical after the lifting of antibiotics for human bacterial infec
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