Residual β-lactam antibiotics in the gastrointestinal tract

Residual β-lactam antibiotics in the gastrointestinal tract represent a therapeutic target for preventing the adverse effects of systemic antibiotic therapy on the gut microbiome. When antibiotics like penicillins or cephalosporins are administered systemically, a significant fraction can enter the intestinal lumen through biliary excretion or incomplete absorption (Kokai-Kun et al., 2017, Lancet Infect Dis). These residual antibiotics kill beneficial commensal bacteria, leading to gut dysbiosis and a loss of colonization resistance against pathogens like Clostridioides difficile (de Gunzburg et al., 2018, J Infect Dis). Therapeutic agents such as Ribaxamase (SYN-004) are designed to target and degrade these antibiotics specifically within the upper gastrointestinal tract using orally delivered, non-absorbable beta-lactamase enzymes (Whalen et al., 2018, Gene). Other approaches include the use of adsorbents like DAV132 to sequester the antibiotics and prevent their interaction with the colonic microbiota (Burdet et al., 2017, J Antimicrob Chemother). By neutralizing these antibiotics in the gut, these therapies aim to prevent antibiotic-associated diarrhea and the emergence of antimicrobial resistance while preserving the systemic efficacy of the primary treatment.

Other names

Residual intestinal antibioticsGut β-lactamsExcess gastrointestinal antibioticsResidual colonic antibiotics

Enzymatic hydrolysis of the β-lactam ring or physical sequestration via adsorption to neutralize antibiotic activity in the intestinal lumen.