β-lactam-containing prodrug

A β-lactam-containing prodrug is not a biological target but a chemical strategy in which an active drug is covalently linked to a β-lactam ring or scaffold. This design allows the prodrug to remain inactive until it encounters and is cleaved by bacterial β-lactamase enzymes, which releases the active agent (e.g., ciprofloxacin or an antimicrobial peptide) specifically at sites of β-lactamase-producing, often drug-resistant, bacteria. This approach leverages the widespread problem of β-lactamase-mediated antibiotic resistance to achieve selective drug delivery, reduce off-target effects, and mitigate adverse impacts on the microbiome[3][4]. Prodrugs of this kind can utilize various β-lactam cores, most often cephalosporins, and have been explored primarily in the context of infection, especially urinary tract infections and other settings where β-lactamase-producing pathogens are prevalent[3][4]. This is not a defined therapeutic target, but a prodrug scaffold used to target the enzymatic function of β-lactamase-positive bacteria.

Other names

β-lactam prodrugβ-lactamase-activated prodrugβ-lactam-based prodrugcephalosporin prodrug (when cephalosporin is the β-lactam core)

Remain inactive until enzymatic cleavage of the β-lactam motif by bacterial β-lactamase releases the active drug. Enables selective killing of β-lactamase-expressing (typically resistant) bacteria.