Table 3.

Pharmacokinetics of arctigenin (AG) and arctigenin glucuronide (AGG) in patients with advanced pancreatic cancer receiving GBS‐01. (A) Single dose pharmacokinetics parameter of AG; (B) Single dose pharmacokinetics parameter of AGG; (C) Multiple dose pharmacokinetics parameter of AG at level 3; (D) Multiple dose pharmacokinetics parameter of AGG at level 3; (E) Contents of AG and AGG in urine on day 1 of treatment

	Cpmax, ng/mL	T max, h	AUC0–t, ng·h/mL	t 1/2, h
(A)
Level 1 (n = 3)	16.97 ± 3.44	1.00 ± 0.50	248.58 ± 206.30	7.18
Level 2 (n = 3)	24.83 ± 8.51	0.50 ± 0.00	142.36 ± 57.23	3.06 ± 2.94
Level 3 (n = 9)	66.56 ± 26.81	0.87 ± 0.62	487.97 ± 368.86	5.68 ± 6.34
(B)
Level 1 (n = 3)	4.40 ± 0.23 (×103)	1.04 ± 0.41	44.10 ± 4.79 (×103)	5.13 ± 0.72
Level 2 (n = 3)	9.05 ± 2.06 (×103)	0.67 ± 0.24	62.71 ± 21.24 (×103)	15.93 ± 9.37
Level 3 (n = 9)	15.91 ± 6.94 (×103)	1.60 ± 0.61	157.07 ± 74.44 (×103)	6.98 ± 5.66
(C)
Day 1 (n = 9)	66.56 ± 26.81	0.87 ± 0.62	487.97 ± 368.86	5.68 ± 6.34
Day 8 (n = 9)	82.92 ± 47.58	1.06 ± 0.88	694.92 ± 260.70	4.42 ± 3.91
(D)
Day 1 (n = 9)	15.91 ± 6.94 (×103)	1.60 ± 0.61	157.07 ± 74.44 (×103)	6.98 ± 5.66
Day 8 (n = 9)	15.30 ± 7.20 (×103)	2.08 ± 1.54	176.67 ± 100.09 (×103)	7.29 ± 4.57

	AG, μmol†	AGG, μmol†	Total dose of AG + AGG of orally administered GBS‐01, μmol†
(E)
Level 1	0.12 ± 0.05	148.8 ± 16.51	287
Level 2	1.26 ± 1.05	444.1 ± 121.64	718
Level 3	1.58 ± 2.47	428.59 ± 265.29	1148

†Expressed as a molar concentration for comparison. Molecular weight: AG, 372.41; AGG, 548. GBS‐01 dose level 1, 3.0 g q.d. (n = 3); dose level 2, 7.5 g q.d. (n = 3); dose level 3, 12.0 g q.d. (n = 9). All values shown as mean ± SD. AUC_{0 –t}, area under the plasma concentration–time curve from 0 h to time; Cp_max, peak exposure; T _max, time to maximum concentration.