Moxifloxacin (BAY 12-8039) is an investigational 8-methoxy-fluoroquinolone with broad-spectrum gram-positive and gram-negative activity. To determine the absolute bioavailability of moxifloxacin, this open-label, randomized, crossover study compared the pharmacokinetic characteristics of a single 100-mg dose administered either orally or intravenously as a 60-minute infusion in 10 healthy male volunteers (mean age [+/- SD], 29.3+/-7.1 years; mean weight [+/- SD], 77.7+/-8.7 kg). Geometric mean values for oral/IV moxifloxacin were as follows: peak serum concentration, 1.15/1.34 mg/L, and area under the concentration-time curve over 48 hours, 9.86/10.89 mg x h/L. The geometric mean absolute bioavailability of oral moxifloxacin was 91.8%. Mean renal clearance was approximately 2.3 L/h after administration of both the single oral and IV formulations, which suggests lack of active tubular secretion of moxifloxacin. Both the oral and IV formulations were well tolerated, with 5 reported possible or probable drug-related adverse events; they included headache, nausea, and localized urticaria. In summary, a single oral dose of moxifloxacin was extensively absorbed in healthy young men. Further studies are necessary in actual patients to confirm the viability of IV to oral conversion at the same dose of moxifloxacin.