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US 6,663,866 B1Granted
Stable radioiodine conjugates and methods for their synthesis
AssigneeImmunomedics, Inc.
InventorSerengulam V. Govindan
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Abstract
Methods are described for conjugating radioiodinated peptides to non-metabolizable carbohydrates with improved yields and qualities of conjugates. Radioiodinated residualizing antibody conjugates comprising a carbohydrate-appended peptide are also provided. The instant radioiodinated residualizing antibody conjugates are particularly stable in vivo and are suitable for radioimmunodetection and radioimmunotherapy.
Claims14
A carbohydrate-appended peptide useful for radioiodinating an antibody, comprising:
- (a) a peptide that comprises at least one D-tyrosine, an amino terminus, a carboxy terminus formed from a D-lysine and no contiguous L-amino acids between the D-tyrosine and the carboxy terminus;
- (b) a reducing carbohydrate conjugated to the peptide via an ε-amino group of the D-lysine to form a carbohydrate-appended peptide;
- and
- (c) a linker group for covalently binding said carbohydrate-appended peptide to an antibody.
1 more element
A carbohydrate-appended peptide useful for radioiodinating an antibody, comprising:
- (a) a peptide that comprises at least one D-tyrosine, an amino terminus, a carboxy terminus, and no contiguous L-amino acids between the D-tyrosine and the carboxy terminus and wherein the carboxy terminus is a D-lysine, D-arginine or D-orthnithine;
- (b) a reducing carbohydrate conjugated to the peptide via the ε-amino group of the D-lysine or the side chain of D-arginine or D-ornithine to form a carbohydrate-appended peptide;
- and
- (c) a linker group for covalently binding said carbohydrate-appended peptide to an antibody.
1 more element
Dependencies are inferred from the claim text.