Faropenem: Pharmacological profile

Faropenem is an orally administered penem antibiotic which demonstrates broad-spectrum antimicrobial activity against many Gram-positive and Gram-negative aerobes and anaerobes. Faropenem is resistant to hydrolysis by nearly all β-lactamases, including ESBLs and AmpC β-lactamases.11Schreuck KN, Wiebe R, Karlowsky JA, et al. Faropenem: Review of a new oral penem. Expert Rev Anti Infect Ther. 2007;5(2):185–198. Faropenem medoxomil (the prodrug form) is inherently stable to most β-lactamases produced by Haemophilus influenzae, Moraxella catarrhalis and S. aureus.22Siegert R, Berg O, Gehanno P, et al. Comparison of the efficacy and safety of faropenem daloxate and cefuroxime axetil for the treatment of acute bacterial maxillary sinusitis in adults. Eur Arch Otorhinolaryngol. 2003;260(4):186–194.

Pharmacodynamics:

Faropenem is characterized by pronounced β-lactamase stability compared to other cephalosporins and imipenem. It is highly stable against hydrolysis by various β-lactamases from Bacteroides fragilisstrains and the rate of faropenem hydrolysis by metallo-β-lactamases is 5 times lower than that for imipenem.33Dalhoff A, Nasu T, Okamoto K. Beta-lactamase stability of faropenem. Chemotherapy. 2003;49(5):229– 236. Faropenem, like other β-lactam antibiotics, interferes with penicillin-binding proteins (PBPs) activity involved in the final phase of peptidoglycan synthesis (Figure 1). PBPs catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death.44Faropenem sodium. Product data sheet. Available at www.toku-e.com/ConvertHtmlToPdf. and?product=643. Accessed on May 05, 2023