TABLE 1

Literature values of plasma clearance, half-life, unbound fraction in plasma, blood/plasma concentration ratio, and metabolic enzymes in humans for the model compounds examined in this analysis

Rb values of fasudil, lamotrigine, and sulindac were assumed to be 1 due to unavailable data from the literature. References are in Supplemental Tables 1 and 2.

CompoundsCLt or CLoralt1/2fuRbMetabolic Enzymes
ml · min1 · kg1h
Dapsone0.48220.251.04CYP2C9, CYP3A4, NAT
6-Deoxypenciclovir*,11811.2AO
Diclofenac3.51.40.0050.55CYP2C9, UGT2B7, UGT1A9
Fasudil73.20.260.511AO
Ibuprofen0.821.60.0060.55CYP2C9, UGT2B7
Ketoprofen1.62.10.0080.55UGT2B7
Lamotrigine*0.30.451UGT1A4, UGT2B7
Mirtazapine8.0150.150.67CYP1A2, CYP2D6, CYP3A4
(S)-Naproxen0.10.010.55CYP2C9, CYP1A2, UGT2B7
Salbutamol7.73.90.9250.96SULT1A3
Sulindac*3.30.0691AO
(S)-Warfarin0.055290.0150.55CYP2C9
Zaleplon161.10.40.99AO, CYP3A4
  • * From oral administration data.

  • Calculated as famciclovir, which is prodrug of 6-deoxypenciclovir.

  • –, Unavailable data from intravenous administration.