TABLE 3

Radiation-Absorbed Dose Estimates to Cell Nucleus by 111In-NLS-Trastuzumab Localized in Compartments of MDA-MB-361 Human Breast Cancer Cell*

Cell compartmentà (Bq × s)S ([Gy/Bq × s] × 104)Radiation dose to cell nucleus D (Gy)
Membrane14,5001.782.58
Cytoplasm2,1003.180.67
Nucleus4,10060.3024.72
Total27.97
  • * Cellular radiation dosimetry model of Goddu et al. (34) was used to estimate radiation-absorbed dose (D) to cell nucleus: D = Ã × S, where S is radiation-absorbed dose in nucleus (Gy) per unit of cumulated radioactivity in source compartment, Ã (Bq × s).

  • Assumes rapid localization of 111In-NLS-trastuzumab in compartment and rate of elimination corresponding to radioactive decay of radionuclide, 111In. Ã = A0/λ, where A0 is amount of radioactivity localized in compartment at time 0 and λ is radioactive decay constant for 111In (2.83 × 10−6/s).

  • Based on targeting a MDA-MB-361 human BC cell with diameter of 10 μm and nucleus with diameter of 6 μm to receptor saturation with 111In-NLS-trastuzumab. At concentrations of radioligand leading to receptor saturation, ∼60 mBq 111In-NLS-trastuzumab would be bound to each MDA-MB-361 cell at specific activity of 3.6 × 1010 MBq/mol.