TABLE 2

Pharmacokinetic properties of BIBX1382 in human and male cynomolgus monkey

Data are reported as a range (human) or as mean (S.D.) from n = 3 monkeys.

SpeciesSubjectsRouteDosePlasma Clearance ml/min per kg (S.D.)Volume of Distribution L/kg (S.D.)Cmax nM (S.D.)AUC nM*h (SD)Absolute Bioavailability % (range)
Humana11 (4M, 7F)i.v. infusion25–200 mg25-5510-208.5–34.5
p.o.25–200 mg0.03–0.410.1–2.55 (2–12)
Cynomolgus Monkeyb3 (M)i.v. bolus1 mg/kg118 (28)39 (6)350 (80)
3 (M)p.o.2 mg/kg12.7 (3.8)43 (25)6 (3–10)
  • Cmax, maximal plasma concentration; AUC, area under the concentration-time curve; M, male; F, female.

  • a Data reported in Dittrich et al., 2002 [Cmax and AUC(0–24) values are dose normalized].

  • b AUC reported as AUClast.