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Table 3 Plasma pharmacokinetics of single and multiple dosing of dalpiciclib

From: A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer

  50 mg QD 75 mg QD 100 mg QD 125 mg QD 150 mg QD 175 mg QD
Single dosing n = 3 n = 3 n = 10 n = 10 n = 10 n = 3
Tmax, h 3.0 (2.0–4.0) 3.0 (3.0–3.0) 2.5 (2.0–4.0) 3.5 (2.0–6.0) 3.5 (2.0–4.0) 4.0 (3.0–4.0)
Cmax, ng/mL 12.2 (57.3) 20.3 (37.3) 46.8 (27.5) 46.6 (56.8) 63.6 (64.4) 114 (37.8)
AUC0-t, h*ng/mL 482 (40) 572 (13) 1170 (20) 1480 (38) 1880 (57) 3080 (24)
t1/2z, h 51.0 (13.6) 46.9 (8.0) 49.7 (16.6) 43.7 (23.5) 51.4 (23.2) 40.3 (22.4)
CL/F, L/h 89.8 (39.2) 117 (15.7) 76.1 (20.7) 76.6 (37.8) 70.5 (51.9) 52.8 (21.8)
Vz/F, L 6610 (40) 7900 (12) 5450 (25) 4830 (45) 5230 (71) 3080 (39)
Multiple dosing n = 3 n = 3 n = 9 n = 9 n = 9 n = 3
Tmax, h 4.0 (4.0–6.0) 3.0 (3.0–4.0) 3.0 (2.0–6.0) 4.0 (2.0–6.0) 4.0 (2.0–8.0) 3.0 (3.0–3.0)
Cmax, ng/mL 41.1 (23.9) 53.4 (9.4) 87.0 (48.5) 115 (28.7) 126 (30.0) 155 (57.8)
AUCss, h*ng/mL 615 (27) 792 (18) 1410 (53) 2020 (32) 2230 (24) 2730 (48)
t1/2z, h 46.9 (11.9) 52.3 (6.3) 48.2 (20.3) 44.9 (21.2) 44.9 (17.5) 45.1 (6.6)
CLss/F, L/h 81.4 (26.9) 94.7 (18.0) 71.0 (52.5) 62.0 (31.8) 67.2 (23.9) 64.1 (47.8)
Vz/F, L 5510 (35) 6920 (31) 4930 (67) 4010 (30) 4350 (32) 4170 (48)
Racc(AUC) 3.4 (41.3) 3.0 (22.1) 2.7 (35.9) 3.3 (60.0) 2.7 (52.8) 1.9 (37.7)
  1. Data are median (range) for Tmax and geometric mean (geometric coefficient of variation%) for others
  2. Tmax time to reach Cmax, Cmax peak plasma concentration, AUC0-t area under the curve from time 0 to the last measurable concentration, AUCss area under the curve for dose interval, t1/2 terminal half-life, CL/F apparent clearance, Vz/F apparent volume of distribution, Rac (AUC) accumulation ratio for AUC