Radiolabled vasoactive intestinal peptide analogs for imaging and therapy
AssigneesThomas Jefferson University, Temple University of the Commonwealth System of Higher Education
InventorMadhukar (Mathew) L. Thakur
Life of this patent
Estimating the term…
Abstract
This invention relates to a radiodiagnostic agent to image tumors. A composition for a tumor imaging agent, a method and kit for preparing a tumor imaging agent, and a radiolabeling reagent for preparing the tumor imaging agent are provided. Methods of using the tumor imaging agent to detect tumors are also provided
Claims17
A composition having formula I or II:
- M—Z—X1—P—X2 (I)X1—P—X2—Z—M (II)
- wherein:
- M is a radiolabeling moiety comprised of four amino acids capable of complexing with a selected radionuclide in an N4 configuration;
- Z is a linker comprising one or more natural or synthetic amino acids;
- X1 is from zero to twenty natural or synthetic amino acids;
- P is a peptide comprising a sequence His Ser Asp Ala Val Phe Thr Asp Asn Tyr Thr Arg Leu Arg Lys Gln Met Ala Val Lys Lys Tyr Leu Asn Ser Ile Leu Asn (SEQ ID NO:
- 1), or an analog or fragment thereof;
- wherein said analog, or fragment thereof, retains the biological activity of SEQ.ID.NO:
- 1 and
- X2 is from zero to twenty natural or synthetic amino acids.
A reagent for radiolabeling a tumor imaging agent comprising four amino acids which can covalently link a selected radionuclide to the amino group of each amino acid to form an N4 configuration.
A kit for preparing a tumor imaging agent comprising:
- a carrier for receiving one or more containers;
- a first container comprising a sealed vial containing a predetermined quantity of a tumor imaging agent;
- and
- a second container comprising one or more subcontainers capable of holding a reducing agent and a buffer.
A method for preparing a tumor imaging agent, which method comprises the steps of:
- synthesizing a tumor specific sequence;
- linking the tumor specific sequence to a radiolabeling moiety to produce a composition having the formula:
- X1—P—X2—Z—M
- wherein:
- X1 is from zero to twenty natural or synthetic amino acids;
- P is a peptide comprising a sequence His Ser Asp Ala Val Phe Thr Asp Asn Tyr Thr Arg Leu Arg Lys Gln Met Ala Val Lys Lys Tyr Leu Asn Ser Ile Leu Asn (SEQ ID NO:
- 1), or an analog or fragment thereof;
- X2 is from zero to twenty natural or synthetic amino acids;
- Z is a linker comprising one or more natural or synthetic amino acids;
- and
- M is a radiolabeling moiety comprised of four amino acids capable of complexing with a selected radionuclide in an N4 configuration;
- and combining the composition with a sufficient amount of a selected radiolabel to form a tumor imaging agent.
Dependencies are inferred from the claim text.