TABLE 5.

Physicochemical and pharmacokinetic properties of EC/11770^a

Parameter	Value
CLND solubility (μM)	349
ChromLogD pH 7.4	0.97
AMP pH 7.4 (nm/sec)	275
Mouse and human hepatic microsomes stability (in vitro)
Mouse in vitro CLint (ml/min/g tissue)  Human in vitro CLint (ml/min/g tissue)	<0.5 <0.5
Mouse pharmacokinetic parameters (in vivo)b
Intravenous administration, 1 mg/kg
In vivo CL (ml/min/kg)   Vss (liter/kg)   t1/2 (h)   AUCinf (ng h/ml)	5.0 (0.1) 2.4 (0.1) 5.3 (0.3) 3,338 (79)
Oral administration, 1 mg/kg & 10 mg/kg
Cmax_1 mg/kg (ng/ml)   Cmax_10 mg/kg (ng/ml)   Tmax_1 mg/kg (h)   Tmax_10 mg/kg (h)   AUC0–24_1 mg/kg (ng h/ml)   AUC0–24_10 mg/kg (ng h/ml)   DNAUC0–24_1 mg/kg (ng h/ml per mg/kg)   DNAUC0–24_10 mg/kg (ng h/ml per mg/kg)   %F_1 mg/kg   %F_10 mg/kg	341 (51) 4,393 (1,260) 1.0−2.0 0.75−2.0 3,556 (179) 40,532 (9,083) 3,556 (179) 4,053 (908) ∼100 ∼100

^aCLND solubility, aqueous solubility via chemiluminescent nitrogen detection; AMP, artificial membrane permeability; CL_int, intrinsic clearance; in vivo CL, in vivo clearance; V_ss, volume of distribution at steady state; t_1/2, half-life; AUC_inf, area under the concentration-time curve extrapolated to infinite; C_max, highest concentration of drug in the blood; T_max, time taken to reach C_max; AUC_0–24, area under the concentration-time curve from time 0 to 24 h; DNAUC, dose-normalized area under the concentration-time curve; %F, bioavailability.

^bAverage (SD). T_max is expressed as a range of values. %F is expressed as a percentage.