TABLE 2

Peak percentage of injected dose per gram Three animals per group ± S.D.


Tissue

Peak Total 3H Cmax

Peak Total 14C Cmax

Peak Soluble 14C Cmax
% ID/g (time)
Tumor 40.9 ± 9.7 (1 day) 82.3 ± 27.2 (2 days) 51.9 ± 13.1 (2 days)
Serum 42.0 ± 5.4 (1 h) 38.2 ± 6.6 (1 h) 0.3 ± 0.1 (10 days)
Kidney 6.8 ± 0.8 (1 h) 6.1 ± 0.7 (1 h) 0.9 ± 0.2 (1 h)
Liver 5.1 ± 1.2 (1 h) 10.3 ± 0.8 (4 h) 3.6 ± 0.7 (4 h)
Spleen 4.0 ± 0.9 (1 h) 3.1 ± 0.6 (1 h) 0.6 ± 0.4 (8 h)
Heart 3.4 ± 0.4 (1 h) 4.7 ± 0.9 (1 h) 0.1 ± 0.1 (4 h)
Muscle 0.9 ± 0.8 (1 h) 0.8 ± 0.7 (1 h) 0.1 ± 0.0 (8 h)
Brain 0.6 ± 0.1 (1 h) 0.5 ± 0.1 (1 h) 0.1 ± 0.0 (1 h)
Bone 0.4 ± 0.1 (1 h) 0.1 ± 0.0 (1 h) N.D.a
Bone marrow 0.1 ± 0.1 (1 h) 0.1 ± 0.1 (1 h) 0.1 ± 0.0 (8 h)
Lung 8.6 ± 1.2 (4 h) 6.0 ± 2.1 (4 h) 0.2 ± 0.2 (1 day)
Pancreas 3.4 ± 2.4 (4 h) 2.4 ± 2.5 (4 h) 0.1 ± 0.1 (1 h)
Bladder 1.8 ± 0.7 (4 h) 1.4 ± 0.8 (4 h) 0.6 ± 0.3 (1 day)
Ovary 1.6 ± 0.2 (4 h) 1.4 ± 0.1 (4 h) 0.2 ± 0.0 (8 h)
Stomach 1.3 ± 0.3 (4 h) 0.5 ± 0.2 (4 h) 0.1 ± 0.1 (1 day)
Intestine contents 0.7 ± 0.3 (4 h) 11.3 ± 4.4 (4 h) 9.0 ± 3.5 (4 h)
Skin 3.0 ± 0.8 (8 h) 2.5 ± 0.7 (8 h) N.D.a
Intestine
2.1 ± 0.1 (8 h)
3.0 ± 0.9 (4 h)
1.3 ± 0.9 (4 h)
  • a N.D., not determined, because the processing method for bone and skin allowed only total auristatin to be obtained