Table 1 Average non-compartmental pharmacokinetic parameters and excretion ratio of 175Lu-DOTA-PSMA-GUL after intravenous injection in rats (n = 5–7).

From: Determination of pharmacokinetics and tissue distribution of a novel lutetium-labeled PSMA-targeted ligand, 177Lu-DOTA-PSMA-GUL, in rats by using LC–MS/MS

Parameters

1 mg/kg

2 mg/kg

5 mg/kg

t1/2 (h)

0.32 ± 0.02

0.30 ± 0.03

0.33 ± 0.09

C0 (ng/mL)

9267.42 ± 2673.59

14,960.22 ± 3104.40*

46,720.92 ± 13,829.91*

AUCall (ng·h/mL)

1841.19 ± 266.36

3029.00 ± 350.80*

8038.10 ± 1055.28*

AUCinf (ng·h/mL)

1857.48 ± 270.08

3047.45 ± 346.00*

8076.44 ± 1063.99*

Vz (L/kg)

0.25 ± 0.03

0.29 ± 0.05

0.30 ± 0.09

CL (mL/min/kg)

9.13 ± 1.30

11.04 ± 1.15

10.46 ± 1.30

MRT (h)

0.34 ± 0.02

0.32 ± 0.03

0.32 ± 0.02

VSS (L/kg)

0.19 ± 0.03

0.21 ± 0.04

0.20 ± 0.03

Furine (%)

58.71 ± 21.26

54.59 ± 25.98

59.89 ± 22.82

Ffeces (%)

5.46 ± 4.11

1.08 ± 0.76

6.41 ± 3.68

  1. *p < 0.05 vs. 1 mg/kg; p < 0.05 vs. 2 mg/kg.