TABLE 1

Lersivirine pharmacokinetic parameter values (geometric means and intersubject variability)

PK Parameter (Units)Lersivirine (Plasma)Total Drug-Related Radioactivity (Plasma)Total Drug-Related Radioactivity (Whole Blood)
n444
AUCinf (ng · h/ml)a,b4100 (19)39,130 (4)18,650 (7)
Cmax (ng/ml)a,b1010 (40)6042 (21)2767 (27)
Tmax (h)c1.50 (0.50–3.00)1.50 (1.00–3.00)1.50 (1.00–3.00)
t½ (h)d5.83 (26)9.41 (30)9.91 (19)
CL/F (l/h)b122 (18)12.78 (4)26.81 (7)
Vz/F (liter)b994 (24)169.4 (26)37,804 (15)
  • AUCinf, area under the plasma concentration-time profile from time zero extrapolated to infinite time; CL/F, apparent clearance; Cmax, maximum plasma concentration; t½, terminal half-life; Tmax, time to reach maximum concentration; VZ/F, apparent volume of distribution.

  • a Units for radioactive compound are ng-Eq · h/g for AUCinf and ng-Eq/g for Cmax.

  • b Geometric mean (percentage coefficient of variation).

  • c Median (range).

  • d Arithmetic mean (percentage coefficient of variation).