TABLE 2

Characteristics of the human i.v. pharmacokinetic parameters and plasma protein binding for 670 compounds


Parameter

N

%
VDss
   Compounds less than 0.1 l/kg 17 2.5
   Compounds between 0.1 and 0.7 l/kg 260 39
   Compounds between 0.7 and 2 l/kg 197 29
   Compounds between 2 and 10 l/kg 143 21
   Compounds 10 l/kg or greater 53 7.9
CL
   Compounds less than 1 ml/min/kg 104 16
   Compounds between 1 and 5 ml/min/kg 262 39
   Compounds between 5 and 15 ml/min/kg 200 30
   Compounds between 15 and 21 ml/min/kg 48 7.2
   Compounds greater than 21 ml/min/kg 56 8.4
Half-life (t1/2)
   Compounds less than 1 h 64 10
   Compounds between 1 and 4 h 266 40
   Compounds between 4 and 12 h 185 28
   Compounds between 12 and 24 h 73 11
   Compounds greater than 24 h 82 12
Plasma protein binding
   Compounds greater than 99.9% bound 41 7.4
   Compounds between 99 and 99.9% bound 28 5.1
   Compounds between 90 and 99% bound 116 21
   Compounds between 50 and 90% bound 167 30
   Compounds less than 50% bound
202
36