TABLE 1.

Pharmacokinetic parameters of caspofungin and total radioactivity in mice, rats, rabbits, and monkeys after an intravenous dosea

SpeciesDose (mg/kg)Parent compoundTotal radioactivityAUC ratio, parent/totalCaspofungin concn in plasma 24 h after a single intravenous dose (μg/ml)
Clearance from plasma (ml/min/kg)Vss (liters/kg)t1/2α (h)t1/2β (h)AUC0-∞ (μg · h/ml)t1/2β (h)AUC0-∞ (μg eq · h/ml)
Mouse50.29 ± 0.070.45 ± 0.174.4 ± 1.246.9 ± 2.8296.4 ± 67.854.8 ± 2.8407.1 ± 48.50.73 ± 0.091.76 ± 0.67
Rat20.43 ± 0.020.50 ± 0.105.9 ± 0.459.7 ± 14.577.1 ± 4.262.8 ± 4.2157.9 ± 13.80.49 ± 0.050.46 ± 0.09
Rabbit51.05 ± 0.250.28 ± 0.051.2 ± 0.211.7 ± 8.582.9 ± 21.3151.4 ± 10.0647.6 ± 66.30.13 ± 0.020.20 ± 0.06
Monkey50.30 ± 0.030.30 ± 0.025.5 ± 0.644.7 ± 7.2278.3 ± 26.1199.7 ± 14.61,658.9 ± 119.70.17 ± 0.032.29 ± 0.33
  • a Data are means ± standard deviations for three mice, rats, and monkeys and four rabbits.