New antimicrobial agents are urgently needed for clinical use due to the increasing prevalence and spread of multidrug-resistant bacteria that are commonly responsible for serious and life-threatening diseases. The need to develop new agents that effectively overcome existing mechanisms of resistance displayed by bacteria resistant to currently available drugs has become paramount. Tigecycline, the first in a new class of antimicrobials, the glycylcyclines, is an analogue of minocycline with additional properties that negate most mechanisms mediating resistance to the tetracyclines. In vitro testing has revealed that tigecycline has activity against vancomycin-resistant enterococci, methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae and many species of multidrug-resistant Gram-negative bacteria, although resistance to tigecycline by Pseudomonas aeruginosa and reduced susceptibility among Proteus species do occur. Tigecycline is being evaluated in multicentre Phase III clinical trials for therapy of many serious and life-threatening infections in which multidrug-resistant bacterial organisms may be found. Tigecycline appears to hold promise as a novel expanded spectrum antibiotic.