THE CHEMISTRY AND BIOLOGICAL PROFILE OF TROVAFLOXACIN

The fluoroquinolone antibacterials are noted for their activity after oral administration and potent activity against Gram-negative pathogen s. Trovafloxacin (CP-99,219) is a new quinolone antibacterial characte rized by a novel 3-azabicyclo[3.1.0]hexyl substituent at the C-7 posit ion, which was discovered in the course of a programme targeting impro ved activity compared with ciprofloxacin against Gram-positive aerobic organisms and anaerobes, as well as an extended elimination half-life . An overview of the chemical properties of trovafloxacin is given. Tr ovafloxacin exhibits excellent potency against Gram-positive organisms and anaerobes, while retaining the potent Gram-negative activity of c iprofloxacin, Its pharmacokinetic properties in humans have been shown to be compatible with a once-daily dosing regimen. The combined spect rum and pharmacokinetics of trovafloxacin have been demonstrated to re sult in excellent efficacy in both animal models of infections and hum an clinical trials. Phase II and Phase III programmes have been comple ted.