In-vitro activity of tigemonam, an oral monobactam, against gram-negative rods, including variants in beta-lactamase-production.
Tigemonam was compared in vitro with other orally active beta-lactams, aztreonam and ciprofloxacin against a selection of Gram-negative clinical isolates and laboratory-derived beta-lactamase-producing variants. Of the orally active beta-lactams, tigemonam was the most potent, with a spectrum of activity similar to that of aztreonam. This included stability to plasmid-mediated beta-lactamases and poor induction of chromosomal beta-lactamases. The susceptibility to Class I enzymes was only clinically significant for derepressed Enterobacter cloacae mutants. Tigemonam may have a valuable role in the management of infection caused by enterobacteria, particularly if bioavailability following oral administration is confirmed in human subjects.
Brown
J
J
Department of Medical Microbiology, London Hospital Medical College, UK.
Yang
Y J
YJ
Livermore
D M
DM
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D004755:Enterobacteriaceae / Q000187:drug effects / Q000201:enzymology; D004790:Enzyme Induction; D006090:Gram-Negative Bacteria / Q000187:drug effects* / Q000201:enzymology; D008997:Monobactams / Q000494:pharmacology*; D001618:beta-Lactamases / Q000096:biosynthesis* / Q000378:metabolism
D000900:Anti-Bacterial Agents; D008997:Monobactams; C052020:tigemonam; D001618:beta-Lactamases