Oral meropenem for superbugs: challenges and opportunities

Drug Discov Today. 2021 Feb;26(2):551-560. doi: 10.1016/j.drudis.2020.11.004. Epub 2020 Nov 13.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / pharmacokinetics
  • Anti-Bacterial Agents / pharmacology
  • Bacterial Infections / drug therapy*
  • Bacterial Infections / epidemiology
  • Bacterial Infections / microbiology
  • Biological Availability
  • Drug Development
  • Drug Resistance, Multiple, Bacterial
  • Global Health
  • Humans
  • Meropenem / administration & dosage*
  • Meropenem / pharmacokinetics
  • Meropenem / pharmacology

Substances

  • Anti-Bacterial Agents
  • Meropenem