Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant...
Patent
1987-10-30
1988-11-01
Terapane, John F.
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
424 8591, A61K 4300, A61K 39395, A61N 500
Patent
active
H00005452
ABSTRACT:
The present invention involves labeling monoclonal antibodies with intermediate half-life radionuclides which decay to much shorter half-life daughters with desirable high energy beta emissions. Since the daughter will be in equilibrium with the parent, it can exert an in-situ tumoricidal effect over a prolonged period in a localized fashion, essentially as an "in-vivo generator". This approach circumvents the inverse relationship between half-life and beta decay energy. Compartmental modeling was used to determine the relative distribution of dose from both parent and daughter nuclei in target and non-target tissues. Actual antibody biodistribution data have been used to fit realistic rate constants for a model containing tumor, blood, and non-tumor compartments. These rate constants were then used in a variety of simulations for two generator systems, Ba-128/Cs-128 (t.sub.1/2 =2.4d/3.6m) and Pd-112/Ag-112 (t.sub.1/2 =0.9d/192m). The results show that higher tumor/background dose ratios may be achievable by virtue of the rapid excretion of a chemically different daughter during the uptake and clearance phases. This modeling also quantitatively demonstrates the favorable impact on activity distribution of a faster monoclonal antibody tumor uptake, especially when the antibody is labeled with a radionuclide with a comparable half-life.
REFERENCES:
patent: 3663177 (1972-05-01), Arino et al.
patent: 4550508 (1985-02-01), Srivastava et al.
patent: 4665897 (1987-05-01), Lemelson
patent: 4707440 (1987-11-01), Stavrianopoulos
Mausner Leonard F.
Srivastava Suresh G.
Straub Rita F.
Bogosian Margaret C.
Gottlieb Paul A.
Hightower Judson R.
Terapane John F.
The United States of America as represented by the United States
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