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Oral meropenem for superbugs: challenges and opportunities
Drug Discovery Today ( IF 6.5 ) Pub Date : 2020-11-13 , DOI: 10.1016/j.drudis.2020.11.004
Aun Raza 1 , Shih Chen Ngieng 2 , Fekade Bruck Sime 1 , Peter J Cabot 2 , Jason A Roberts 3 , Amirali Popat 4 , Tushar Kumeria 5 , James R Falconer 2
Affiliation  

An increase in the number of multidrug-resistant microbial strains is the biggest threat to global health and is projected to cause >10 million deaths by 2055. The carbapenem family of antibacterial drugs are an important class of last-resort treatment of infections caused by drug-resistant bacteria and are only available as an injectable formulation. Given their instability within the gut and poor permeability across the gut wall, oral carbapenem formulations show poor bioavailability. Meropenem (MER), a carbapenem antibiotic, has broad-spectrum antibacterial activity, but suffers from the above-mentioned issues. In this review, we discuss strategies for improving the oral bioavailability of MER, such as inhibiting tubular secretion, prodrug formulations, and use of nanomedicine. We also highlight challenges and emerging approaches for the development of oral MER.



中文翻译:

超级细菌口服美罗培南:挑战与机遇

耐多药微生物菌株数量的增加是对全球健康的最大威胁,预计到 2055 年将导致超过 1000 万人死亡。 碳青霉烯类抗菌药物是一类重要的药物引起感染的最后手段抗性细菌,仅可作为注射剂使用。鉴于它们在肠道内的不稳定性和穿过肠道壁的渗透性差,口服碳青霉烯制剂显示出较差的生物利用度。美罗培南(MER)是一种碳青霉烯类抗生素,具有广谱抗菌活性,但存在上述问题。在这篇综述中,我们讨论了提高 MER 口服生物利用度的策略,例如抑制肾小管分泌、前药制剂和纳米药物的使用。

更新日期:2020-11-13
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