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US 6,855,308 B2Granted
PACAP compositions and methods for tumor imaging and therapy
AssigneeThomas Jefferson University
InventorMadhukar L. Thakur
Life of this patent
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Abstract
Tumors expressing VPAC receptors can be imaged or treated with compounds comprising PACAP, or a biologically active PACAP fragment or analog.
Claims45
A method of detecting tumors expressing VPAC receptors in a subject who has, or is suspected of having, such a tumor, said method comprising:
- (1) administering an effective amount of an imaging compound of formulae A or B to the subject;
- and
- (2) generating a scintigraphic image of at least part of the subject, wherein formulae A and B are:
- M(I)-X1-P-X2 (A)
- X1-P-X2-M(I) (B)
- wherein:
- M is a chelating agent, provided that in formula A, when X1 is zero and P is PACAP27 (SEQ ID NO:
- 2), M is not a polyamino-polycarboxylic acid chelating agent;
- (I) is an imaging radionuclide conjugated to M;
- X1 is from zero to twenty natural or synthetic amino acids;
- P is PACAP, or an analog or fragment thereof which exhibits PACAP biological activity;
- and
- X2 is from zero to twenty natural or synthetic amino acids.
10 more elements
A method of inhibiting or reversing the growth of a tumor expressing VPAC receptors in a subject who has such a tumor, comprising administering an effective amount of a composition of formulae C or D to the subject, wherein formulae C and D are
- M(T)-X1-P-X2 (C)
- X1-P-X2-M(T) (D)
- and wherein:
- M is a chelating agent;
- (T) is a therapeutic radionuclide conjugated to M;
- X1 is from zero to twenty natural or synthetic amino acids;
- P is PACAP or an analog or fragment thereof which exhibits PACAP biological activity;
- and
- X2 is from zero to twenty natural or synthetic amino acids.
6 more elements
A compound of formulae A, B, C or D:
- M(I)-X1-P-X2 (A)
- X1-P-X2-M(I) (B)
- M(T)-X1-P-X2 (C)
- X1-P-X2-M(T) (D)
- wherein:
- M is a chelating agent;
- , provided that in formula A, when X1 is zero and P is
- PACAP27 (SEQ ID NO;
- 2), M is not a polyamino-polycarboxylic acid chelating agent;
- (I) is an imaging radionuclide conjugated to M in formulae A and B;
- (T) is a therapeutic radionuclide conjugated to M in formulae C and D;
- X1 is from zero to twenty natural or synthetic amino acids;
- P is PACAP, or an analog or fragment thereof which exhibits PACAP biological activity;
- and
- X2 is from zero to twenty natural or synthetic amino acids.
12 more elements
Dependencies are inferred from the claim text.