Skip to main content
. 2016 Sep;44(9):1517–1523. doi: 10.1124/dmd.116.070631

TABLE 1 .

Total antibody (mAb) and catabolite concentrations in tissues of WSU-DLCL2 xenograft mice following a single 5-mg/kg i.v. dose of anti-CD22-cyclopropyl-disulfide-PBD-dimer, or anti-CD22-cyclobutyl-disulfide-PBD-dimer ADCs (n = 2)

Catabolites PBD-dimer and cyclopropyl-thiol and were not detected in tissues of mice dosed with vehicle. ND = not detected.

ADC Time PBD-dimer
Cyclopropyl-thiol
mAb
Plasma Liver Tumor Plasma Liver Tumor Plasma Liver Tumor
h nM nM nM nM nM nM nM nM nM
Cyclobutyl-containing 24 0.43 0.26 1.03 NA NA NA 370 24.8 43.5
0.55 0.55 2.09 NA NA NA 342 19.5 25.0
96 <LLOQ <LLOQ 1.93 NA NA NA 285 20.9 25.3
<LLOQ <LLOQ 2.05 NA NA NA 272 21.1 56.0
Cyclopropyl-containing 24 ND ND ND 0.74 1.42 7.58 294 28.4 59.4
ND ND ND 0.57 0.63 6.76 216 18.6 27.4
96 ND ND ND <LLOQ <LLOQ 4.33 349 23.4 23.5
ND <LLOQ ND 0.30 0.34 4.69 331 16.6 16.6

NA, not applicable; LLOQ, lower limit of quantitation, 0.24 nM for both analytes in homogenates (nanomolar concentration in tumor and liver was estimated on the basis of an assumption of tissue density of 1 g/ml).