Bone marrow suppressing agents

Patent Number: 4976950

This patent has 2 independent claims, the first covering a method of suppressing the bone marrow, the second covering a sterile injectable capable of suppressing the bone marrow. The method by which this patent teaches to suppress the bone marrow is through administration of a sterile composition containing the radionuclide Yttrium-90 complexed with at least one macrocycle aminophosphonic acid ligand containing the 1,4,7,10-tetraazacyclododecane moiety or a physiologically acceptable salt thereof, wherein the phosphorous of said ligand is attached to the amine nitrogen through an alkylene moiety and wherein the radionuclide in dosage form is present in an amount containing from about 18 to about 1850 megabecquerels per kilogram of body weight of said mammal. It appears that complexing the radionuclide to macrocyclic aminophosphonic acid is to selectively cause the source of radiation to enter the bone. A similar approach (it looks like, anyway) is described in (Appelbaum FR, et al. Specific marrow ablation before marrow transplantation using an aminophosphonic acid conjugate 166Ho-EDTMP. Blood. 1992 Sep 15;80(6):1608-13.)

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