Department of Drug Science, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
Molecules. 2021 May 2;26(9):2671. doi: 10.3390/molecules26092671.
The present work aims to examine the worrying problem of antibiotic resistance and the emergence of multidrug-resistant bacterial strains, which have now become really common in hospitals and risk hindering the global control of infectious diseases. After a careful examination of these phenomena and multiple mechanisms that make certain bacteria resistant to specific antibiotics that were originally effective in the treatment of infections caused by the same pathogens, possible strategies to stem antibiotic resistance are analyzed. This paper, therefore, focuses on the most promising new chemical compounds in the current pipeline active against multidrug-resistant organisms that are innovative compared to traditional antibiotics: Firstly, the main antibacterial agents in clinical development (Phase III) from 2017 to 2020 are listed (with special attention on the treatment of infections caused by the pathogens , including multidrug-resistant isolates, and ), and then the paper moves on to the new agents of pharmacological interest that have been approved during the same period. They include tetracycline derivatives (eravacycline), fourth generation fluoroquinolones (delafloxacin), new combinations between one β-lactam and one β-lactamase inhibitor (meropenem and vaborbactam), siderophore cephalosporins (cefiderocol), new aminoglycosides (plazomicin), and agents in development for treating drug-resistant TB (pretomanid). It concludes with the advantages that can result from the use of these compounds, also mentioning other approaches, still poorly developed, for combating antibiotic resistance: Nanoparticles delivery systems for antibiotics.
本研究旨在探讨抗生素耐药性和多药耐药菌的出现这一令人担忧的问题,这些问题现在在医院中已经非常普遍,并且有可能阻碍全球传染病的控制。在仔细研究了这些现象以及使某些细菌对原本有效治疗由同一病原体引起的感染的特定抗生素产生耐药性的多种机制后,分析了遏制抗生素耐药性的可能策略。因此,本文重点关注目前针对多药耐药菌的最有前途的新型化学化合物,这些化合物与传统抗生素相比具有创新性:首先,列出了 2017 年至 2020 年临床开发(III 期)的主要抗菌药物(特别关注针对病原体引起的感染的治疗,包括多药耐药株),然后本文转向同期批准的具有药理作用的新型药物。它们包括四环素衍生物(依拉环素)、第四代氟喹诺酮类药物(德拉沙星)、一种β-内酰胺和一种β-内酰胺酶抑制剂的新组合(美罗培南和维巴他滨)、铁载体头孢菌素(头孢地尔)、新型氨基糖苷类药物(普拉佐米星)以及用于治疗耐药结核病的药物(普雷托马尼德)。最后,本文总结了使用这些化合物可能带来的优势,同时还提到了其他方法,这些方法仍在开发中,用于对抗抗生素耐药性:抗生素纳米颗粒给药系统。