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Table 4 Pharmacokinetic parameters for recaticimab

From: PCSK9 inhibitor recaticimab for hypercholesterolemia on stable statin dose: a randomized, double-blind, placebo-controlled phase 1b/2 study

 

75 mg Q4W (N=10)

150 mg Q4W (N=17)

150 mg Q8W (N=10)

300 mg Q8W (N=15)

300 mg Q12W (N=10)

450 mg Q12W (N=20)

After first dose

 Tmax (day)

9.0 (3.9, 14.0)

9.0 (6.0, 20.9)

7.0 (4.0, 14.0)

8.9 (2.0, 22.0)

9.0 (6.0, 21.0)

6.0 (3.9, 22.0)

 Cmax (μg/mL)

5.7 (43.7%)

12.1 (35.9%)

9.8 (41.0%)

31.4 (23.6%)

28.4 (44.0%)

43.2 (39.9%)

 AUC0-τ (day·μg/mL)

126 (45%)

260 (41%)

299 (37%)

1010 (26%)

1180 (40%)

1640 (46%)

 AUClast (day·μg/mL)

123 (42%)

258 (37%)

299 (37%)

1010 (26%)

1180 (40%)

1640 (46%)

After last dose

 Tmax (day)

7.0 (5.9, 15.0)

7.0 (3.9, 28.0)

7.0 (3.0, 17.0)

7.0 (3.9, 32.2)

7.5 (7.0, 14.0)

7.0 (4.0, 28.9)

 Cmax (μg/mL)

8.7 (42.5%)

24.4 (33.9%)

13.0 (62.7%)

31.7 (41.9%)

32.0 (32.4%)

41.1 (27.0%)

 t1/2 (day)

22.0 (27.3%)

22.1 (28.0%)

18.6 (11.8%)

21.7 (25.7%)

19.9 (24.8%)

27.4 (33.2%)

 AUC0-τ (day·μg/mL)

197 (44%)

553 (37%)

411 (54%)

1130 (47%)

1150 (31%)

1770 (36%)

 AUClast (day·μg/mL)

327 (59%)

988 (41%)

460 (55%)

1310 (48%)

1150 (31%)

1760 (36%)

 AUC0-∞ (day·μg/mL)

367 (56%)

1090 (47%)

487 (53%)

1430 (51%)

1300 (38%)

2090 (43%)

 CL/F (L/day)

0.4 (44.4%)

0.3 (37.2%)

0.4 (54%)

0.3 (47.1%)

0.3 (30.6%)

0.3 (36.1%)

 Vz/F (L)

12.0 (33.8%)

8.4 (30.2%)

9.8 (56.4%)

8.3 (50.2%)

7.2 (18.6%)

10.1 (28.6%)

 Ctrough (μg/mL)

4.8 (53.8%)

13.4 (46.1%)

1.9 (45.8%)

7.5 (61.2%)

3.0 (97.8%)

4.0 (111.1%)

  1. Data are median (range) for Tmax and geometric mean (CV%) for other parameters
  2. CV coefficient of variation, Tmax time to reach maximum serum concentration, Cmax maximum serum concentration, AUC0-τ area under the plasma concentration-time profile from time zero to the treatment, AUClast AUC from time zero to the last concentration measurement, AUC0-∞ AUC from time zero to infinity, t1/2 half-life, CL/F apparent total clearance, Vz/F apparent volume of distribution, and Ctrough trough concentration