Oral meropenem for superbugs: challenges and opportunities.

Aun Raza, Shih Chen Ngieng, Fekade Bruck Sime, Peter J Cabot, Jason A Roberts, Amirali Popat, Tushar Kumeria, James R Falconer

Drug discovery today 2021 Feb

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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. Copyright © 2020 Elsevier Ltd. All rights reserved.

Citation

Aun Raza, Shih Chen Ngieng, Fekade Bruck Sime, Peter J Cabot, Jason A Roberts, Amirali Popat, Tushar Kumeria, James R Falconer. Oral meropenem for superbugs: challenges and opportunities. Drug discovery today. 2021 Feb;26(2):551-560