Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer
AssigneeCornell University
InventorsJohn W. BABICH, Justin WILSON, Nikki THIELE, James KELLY, Shashikanth PONNALA
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Abstract
The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (“PSMA”) where the compounds are represented by the following: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt thereof, wherein M1 is independently at each occurrence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.
Claims22
A method of treating a subject, wherein the method comprises administering to the subject a targeting compound of Formula II
- or a pharmaceutically acceptable salt thereof, wherein
- M1 is an alpha-emitting radionuclide;
- Z1 is H or -L3-R22;
- Z2 is OH or NH-L4_R24,
- Z3 is H or -L6-R28,
- α is 0 or 1;
- X1 is O, NH, or S;
- L3, L4, L5, and L6 are independently at each occurrence a bond or a linker group;
- and
- R22, R24, R26, and R28 each independently comprises an antibody, antibody fragment, an antigen-binding fragment, a Fibroblast Activation Protein alpha (FAP-alpha) binding moiety, a binding peptide, a binding polypeptide, a binding protein, an enzyme, a nucleobase-containing moiety, or a lectin.
Dependencies are inferred from the claim text.