Chelator compositions for radiometals and methods of using same
AssigneesTriumf, Provincial Health Services Authority, The University of British Columbia
InventorsHua YANG, Feng GAO, Paul SCHAFFER, Zheliang YUAN, Chengcheng ZHANG, Francois BENARD, Luke WHARTON
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Abstract
A chelator having the general structure (I) for chelating ra-diometals such as 225Ac under mild conditions is provided. (I) The chelator can be coupled to a biological targeting moiety to facilitate targeted delivery of the chelated radiometal in a mammalian subject.
Claims44
An in vivo radioisotope targeting construct comprising a biological targeting moiety and a chelator having the structure (I), (II) or (III):
- wherein:
- X1 and X2 are independently O, N or S;
- R2, R3, R4, R5 and R6 are independently not present or a functional group that can be used to couple the chelator to the biological targeting moiety.
An in vivo radioisotope targeting construct comprising 2,2’,2”,2”’-(1,10-dioxa-4,7,13,16-tetraazacyclooctadecane-4,7,13,16-tetrayl)tetraacetic acid as a chelator.
A metal chelate comprising a metal and a chelator having the following structure (I), (II) or (III):
- wherein:
- X1 and X2 are independently O, N or S;
- R2, R3, R4, R5 and R6 are independently not present or a functional group that can be used to couple the chelator to a biological targeting moiety;
- and wherein the metal is selected from the group consisting of:
- 225Ac, 213Bi, 68Ga, 155Tb, 177Lu, 111In, or 137Cs.
A method of forming a metal chelate comprising combining a chelator having the structure (I), (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX) below with a radiometal in an aqueous solution at a temperature of between 15° C. and 25° C.
- wherein:
- X1 and X2 are independently O, N or S;
- R2, R3, R4, R5 and R6 are independently not present or a functional group that can be used to couple the chelator to a biological targeting moiety;
- R1 when present represents a biological targeting moiety;
- and
- L when present represents a linker.
Dependencies are inferred from the claim text.