This brief review summarizes recently published data on the pharmacokinetics and pharmacodynamics of tigecycline in man. Significant pharmacokinetic data are now available from the studies of infected patients, as is information on tissue distribution. Importantly, drug exposure-response relationships have been established for complicated skin and skin structure infections and intra-abdominal infection. These studies highlight the difficulties of undertaking pharmacodynamic studies in humans where account must be taken of both mixed pathogen infections and the potential impact of surgery. These data help to define the clinical role for tigecycline.