In vitro evaluation of tigemonam, a novel oral monobactam.
Tigemonam, a novel, orally administered monobactam, exhibited potent and specific activity in vitro against members of the family Enterobacteriaceae, Haemophilus influenzae, and Neisseria gonorrhoeae. Its activity was variable to poor against gram-positive bacteria, Acinetobacter spp., Pseudomonas aeruginosa, and anaerobes. Within its spectrum of activity, tigemonam was far superior to oral antibiotics currently available, including amoxicillin-clavulanic acid, cefaclor, and trimethoprim-sulfamethoxazole. In addition, tigemonam was superior to cefuroxime, which is under development as an oral pro-drug, and more active than cefixime against several genera of the Enterobacteriaceae. The activity of tigemonam against the enteric bacteria, Haemophilus species, and Neisseria species was, in general, comparable to that of the quinolone norfloxacin. The excellent activity of tigemonam against beta-lactamase-producing bacteria reflected its marked stability to hydrolysis by isolated enzymes. The expanded spectrum of activity against gram-negative bacteria observed with tigemonam thus extends oral beta-lactam coverage to include members of the Enterobacteriaceae that are intrinsically or enzymatically resistant to broad-spectrum penicillins and cephalosporins.
D000150:Acinetobacter / Q000187:drug effects; D001419:Bacteria / Q000187:drug effects*; D004755:Enterobacteriaceae / Q000187:drug effects* / Q000201:enzymology; D006193:Haemophilus influenzae / Q000187:drug effects; D007700:Kinetics; D008826:Microbial Sensitivity Tests; D008997:Monobactams / Q000378:metabolism / Q000494:pharmacology*; D009344:Neisseria gonorrhoeae / Q000187:drug effects; D011550:Pseudomonas aeruginosa / Q000187:drug effects / Q000201:enzymology; D001618:beta-Lactamases / Q000378:metabolism
D008997:Monobactams; C052020:tigemonam; D001618:beta-Lactamases