TABLE 3

Exposure to total and unconjugated auristatin from 0 to 10 days


Tissue

Total Auristatin Exposurea

Unconjugated Auristatin Exposurea

Ratio of Unconjugated to Total Auristatinb
nM * day
Tumor 2540 ± 590 1510 ± 360 0.593 ± 0.010
Serum 319 ± 28 13.1 ± 0.9 0.0415 ± 0.0060
Kidney 45.6 ± 2.9 8.0 ± 0.2 0.176 ± 0.011
Liver 81.1 ± 0.2 20.4 ± 2.8 0.252 ± 0.036
Spleen 23.0 ± 1.4 7.4 ± 1.5 0.318 ± 0.045
Heart 47.0 ± 7.7 3.5 ± 0.3 0.076 ± 0.020
Muscle 11.2 ± 1.5 3.1 ± 0.4 0.279 ± 0.007
Brain 7.9 ± 0.4 3.1 ± 0.3 0.390 ± 0.054
Bone 2.3 ± 0.3 N.D.c N.D.c
Bone marrow 1.0 ± 0.1 0.7 ± 0.1 0.651 ± 0.009
Lung 68.9 ± 7.3 6.5 ± 0.8 0.094 ± 0.007
Pancreas 21.1 ± 1.1 2.9 ± 0.6 0.137 ± 0.029
Bladder 38.7 ± 10.2 18.5 ± 1.6 0.511 ± 0.183
Ovary 21.6 ± 1.0 8.9 ± 1.0 0.414 ± 0.055
Stomach 8.9 ± 0.6 4.7 ± 0.6 0.529 ± 0.097
Intestine contents 83.4 ± 23.4 67.7 ± 19.0 0.812 ± 0.054
Skin 48.9 ± 4.6 N.D.c N.D.c
Intestine
32.7 ± 3.3
11.6 ± 2.2
0.354 ± 0.030
  • a Three animals per group ± S.D.

  • b Ratio for three individual animals ± S.D.

  • c N.D., not determined because the processing method for bone and skin allowed only total auristatin to be obtained