Table 5.

Summary PK parameters of functional enoticumab following the first IV infusion

0.75 mg/kg1 mg/kg1.5 mg/kg3 mg/kg
Q2WQ2WQ2WQ2W
n = 6n = 6n = 3n = 6
Parameter/UMean (±SD)Mean (±SD)Mean (±SD)Mean (±SD)
t 1/2 Day4.00 (0.738)5.13 (1.51)6.28 (0.762)7.74 (1.00)
CLL/d/kg0.00801 (0.00316)0.00774 (0.00368)0.00534 (0.00101)0.00422 (0.000404)
V ss L/kg0.0443 (0.0169)0.0559 (0.0177)0.0466 (0.0141)0.0444 (0.00811)
C max mg/L20.9 (7.27)24.3 (4.09)40.2 (2.63)99.7 (16.9)
C max/dosekg/L27.8 (9.70)24.3 (4.09)26.8 (1.75)33.2 (5.62)
t max Day0.189 (0.137)2.40 (5.79)0.0796 (0.0940)0.188 (0.139)
AUClast Day/mg/L94.3 (43.5)118 (67.3)233 (63.8)522 (67.0)
AUClast/doseDay/kg/L126 (57.9)118 (67.3)156 (42.5)174 (22.3)
0.25 mg/kg 0.5 mg/kg 1 mg/kg 2 mg/kg 4 mg/kg
Q3W Q3W Q3W Q3W Q3W
n = 7 n = 6 n = 6 n = 6 n = 6
Parameter/U Mean (±SD) Mean (±SD) Mean (±SD) Mean (±SD) Mean (±SD)
t 1/2 Day1.73 (0.399)3.13 (0.747)4.30 (1.61)6.89 (1.90)9.25 (2.31)
CLL/d/kg0.0173 (0.00841)0.00917 (0.00242)0.00577 (0.00151)0.00478 (0.00168)0.00534 (0.00237)
V ss L/kg0.0399 (0.0156)0.0408 (0.0134)0.0361 (0.00566)0.0445 (0.0120)0.0646 (0.0208)
C max mg/L6.06 (1.83)14.1 (4.00)33.7 (9.58)53.9 (13.3)96.7 (17.7)
C max/dosekg/L24.3 (7.30)28.1 (8.00)33.7 (9.58)27.0 (6.64)24.2 (4.43)
t max Day0.0450 (0.0343)0.0634 (0.0646)0.113 (0.0682)0.255 (0.381)0.0799 (0.0449)
AUClast Day/mg/L16.2 (7.70)49.6 (18.4)175 (42.1)404 (118)687 (218)
AUClast/doseDay/kg/L65.0 (30.8)99.2 (36.7)175 (42.1)202 (59.0)172 (54.6)

Abbreviations: CL, clearance; C max, maximum concentration; t 1/2, half-life; t max, time to maximum concentration; V ss, volume of distribution at steady state.