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Mecillinam is a narrow-spectrum amidinopenicillin antibiotic with a unique mechanism of action that distinguishes it from other beta-lactams. While most penicillins and cephalosporins primarily target Penicillin-Binding Proteins 1 and 3 (PBP1 and PBP3) to inhibit cell wall synthesis, mecillinam binds with high affinity and specificity to Penicillin-Binding Protein 2 (PBP2). This binding interferes with the maintenance of the rod-like shape of Gram-negative bacteria, causing them to transform into large, fragile spherical cells (spheroplasts) that eventually undergo osmotic lysis. It is particularly potent against Enterobacteriaceae, including *Escherichia coli*, *Klebsiella*, and *Salmonella* species, but lacks significant activity against Gram-positive bacteria and *Pseudomonas aeruginosa*. Developed by Leo Pharma, mecillinam is used parenterally for serious infections, while its pivaloyloxymethyl ester prodrug, pivmecillinam, is used orally for uncomplicated urinary tract infections.
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