Table 1.

Pharmacokinetic variables of CCT018159 analogues following individual administration to mice at 20 mg/kg

CompoundTissueRouteAUClast (h*nmol/L)AUCINF (h*nmol/L)Cmax (nmol/L)CL/F, obs (L/h)HL (h)Vz/F, obs (Liter)FTissue/plasma AUC
CCT018159Plasmai.v.8,6108,82324,2080.1290.390.073
CCT018159Plasmap.o.1552062755.500.695.4710.018
CCT066950Plasmai.v.2,4082,7387,0880.5800.170.146
CCT066950Plasmap.o.5051,5481,3551.0250.781.1570.210
CCT066950Liveri.v.1,0811,2434,4301.2770.170.3210.4
CCT066950Liverp.o.319ND*1,957ND*ND*ND*0.6
CCT066950Kidneyi.v.10,55110,82166,6070.1470.090.0204.4
CCT066950Kidneyp.o.2,1882,64110,6040.6010.170.1494.3
CCT066950Spleeni.v.7,1518,33823,5820.1900.190.0513.0
CCT066950Spleenp.o.1,3041,7085,0480.9300.220.2902.6
CCT066952Plasmai.v.1,6901,7507,0980.8160.440.520
CCT066952Plasmap.o.1271954637.3370.293.0360.075
CCT066963Plasmai.v.8,3588,40035,8330.1400.260.052
CCT066963Plasmap.o.2293311,0023.5540.251.2640.027
CCT066965Plasmai.v.8,9129,01457,2350.1280.350.065
CCT066965Plasmap.o.2,6413,3636,8630.3430.670.3320.296
  • Abbreviations: AUClast, AUC up to the time of the last measurable concentration; AUCINF, AUC from the time of dosing extrapolated to infinity; Cmax, maximum concentration; CL, total body clearance; HL terminal half-life; Vz, volume of distribution based on the terminal phase.

  • * Not determined (not enough time points with compounds detected).