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Table 2 Biodistribution (0.3 MBq/0.075 nmol) of 177 Lu-labelled BN analogues in nude mice bearing PC-3 tumour

From: PEGylation, increasing specific activity and multiple dosing as strategies to improve the risk-benefit profile of targeted radionuclide therapy with 177Lu-DOTA-bombesin analogues

 

177Lu-DOTA-Lys-BN

177Lu-DOTA-PEG 5k-Lys-BN

177Lu-DOTA-Lys-BN

177Lu-DOTA-PEG 5k-Lys-BN

Tissue

1 h p.i.

24 h p.i.

1 h p.i.

24 h p.i.

1 h p.i. blocked

1 h p.i. blocked

Blood

0.24 ± 0.07

0.00 ± 0.00

1.54 ± 0.33*

0.01 ± 0.00*

  

Heart

0.14 ± 0.06

0.01 ± 0.01

0.49 ± 0.05

0.04 ± 0.01

  

Lung

0.36 ± 0.08

0.02 ± 0.01

1.10 ± 0.15

0.13 ± 0.02

  

Spleen

0.42 ± 0.12

0.18 ± 0.04

0.72 ± 0.02

0.19 ± 0.03

  

Kidneys

2.86 ± 0.63

1.41 ± 0.14

4.89 ± 1.33

1.84 ± 0.52

  

Pancreas

8.68 ± 1.95

4.27 ± 0.85

9.62 ± 2.39

4.87 ± 1.11

0.49 ± 0.22**

0.98 ± 0.59*

Stomach

0.72 ± 0.19

0.10 ± 0.02

1.12 ± 0.15

0.22 ± 0.07

  

Small intestine

1.38 ± 0.41

0.16 ± 0.03

1.18 ± 0.22

0.17 ± 0.12

  

Colon

1.64 ± 0.40

0.36 ± 0.09

2.19 ± 0.91

0.45 ± 0.21

0.36 ± 0.07**

0.66 ± 0.14

Liver

0.26 ± 0.09

0.09 ± 0.02

0.57 ± 0.04

0.16 ± 0.09

  

Muscle

0.20 ± 0.24

0.01 ± 0.00

0.31 ± 0.06

0.42 ± 0.69

  

Bone

0.36 ± 0.24

0.02 ± 0.01

0.70 ± 0.06

0.58 ± 0.44

  

Tumour

1.88 ± 0.47

0.54 ± 0.30

3.43 ± 0.63*

1.04 ± 0.04

0.55 ± 0.03*

1.02 ± 0.34**

  1. *P < 0.05; **P < 0.01. Data in percentage of injected dose per gram of tissue (%ID/g), expressed as mean ± SD at 1 and 24 h p.i. (n = 3 to 4).