Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – In an organic compound
Patent
1996-05-06
2000-04-18
Dees, Jose' G.
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
In an organic compound
424 111, 424 165, 424 91, 534 10, 534 14, 530300, 530311, 530317, A61K 5100, A61M 3614
Patent
active
060512067
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to therapeutic agents and peptides, radiotherapeutic agents and peptides, radiodiagnostic agents and peptides, and methods for producing such labeled radiodiagnostic and radiotherapeutic agents. Specifically, the invention relates to cyclic peptide derivatives and analogues of somatostatin, and embodiments of such peptides labeled with gamma-radiation emitting isotopes such as technetium-99m (Tc-99m), as well as methods and kits for making, radiolabeling and using such peptides to image sites in a mammalian body. The invention also relates to peptide derivatives and analogues of somatostatin labeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re), and methods and kits for making, radiolabeling and using such peptides therapeutically in a mammalian body.
2. Description of the Prior Art
Somatostatin is a tetradecapeptide that is endogenously produced by the hypothalamus and pancreas in humans and other mammals. The peptide has the formula: ##STR1## (Single letter abbreviations for amino acids can be bound in G. Zubay, Biochemistry (2d ed.), 1988, (MacMillan Publishing: New York), p. 33). This peptide exerts a wide variety of biological effects in vivo. It is known to act physiologically on the central nervous system, the hypothalamus, the pancreas, and the gastrointestinal tract.
Somatostatin inhibits the release of insulin and glucagon from the pancreas, inhibits growth hormone release from the hypothalamus, and reduces gastric secretions. Thus, somatostatin has clinical and therapeutic applications for the alleviation of a number of ailments and diseases, both in humans and other animals. Native somatostatin is of limited utility, however, due to its short half-life in vivo, where it is rapidly degraded by peptidases. For this reason, somatostatin analogues having improved in vivo stability have been developed in the prior art.
Freidinger, U.S. Pat. No. 4,235,886 disclose cyclic hexapeptide somatostatin analogues useful in the treatment of a number of diseases in humans.
Coy and Murphy, U.S. Pat. No. 4,485,101 disclose synthetic dodecapeptide somatostatin analogues.
Freidinger, U.S. Pat. No. 4,611,054 disclose cyclic hexapeptide somatostatin analogues useful in the treatment of a number of diseases in humans.
Nutt, U.S. Pat. No. 4,612,366 disclose cyclic hexapeptide somatostatin analogues useful in the treatment of a number of diseases in humans.
Coy et al., U.S. Pat. No. 4,853,371 disclose synthetic octapeptide somatostatin analogues.
Coy and Murphy, U.S. Pat. No. 4,871,717 disclose synthetic heptapeptide somatostatin analogues.
Coy et al., U.S. Pat. No. 4,904,642 disclose synthetic octapeptide somatostatin analogues.
Taylor et al., U.S. Pat. No. 5,073,541 disclose a method of treating small cell lung cancer.
Brady, European Patent Application No. 83111747.8 discloses dicyclic hexapeptide somatostatin analogues useful in the treatment of a number of human diseases.
Bauer et al., European Patent Application No. 85810617.2 disclose somatostatin derivatives useful in the treatment of a number of human diseases.
Eck and Moreau, European Patent Application No. 90302760.5 disclose therapeutic octapeptide somatostatin analogues.
Coy and Murphy, International Patent Application Serial No. PCT/US90/07074 disclose somatostatin analogues for therapeutic uses.
Schally et al., European Patent Application Serial No. EPA 911048445.2 disclose cyclic peptides for therapeutic use.
Bodgen and Moreau, International Patent Application Serial No. PCT/US92/01027 disclose compositions and methods for treating proliferative skin disease.
Somatostatin exerts it effects by binding to specific receptors expressed at the cell surface of cells comprising the central nervous system, the hypothalamus, the pancreas, and the gastrointestinal tract. These high-affinity somatostatin binding sites have been found to be abundantly expressed at the cell surface of most endocrine-active tumors arising from these tissues. Ex
REFERENCES:
patent: 4224199 (1980-09-01), Meyers et al.
patent: 4235886 (1980-11-01), Freidinger
patent: 4444690 (1984-04-01), Fritzberg
patent: 4472509 (1984-09-01), Gansow et al.
patent: 4485101 (1984-11-01), Coy et al.
patent: 4608251 (1986-08-01), Mia
patent: 4611054 (1986-09-01), Freidinger
patent: 4612366 (1986-09-01), Nutt
patent: 4650787 (1987-03-01), Schally et al.
patent: 4725577 (1988-02-01), Schally et al.
patent: 4853371 (1989-08-01), Coy et al.
patent: 4871717 (1989-10-01), Coy et al.
patent: 4904642 (1990-02-01), Coy et al.
patent: 5073541 (1991-12-01), Taylor et al.
patent: 5084442 (1992-01-01), Felix et al.
patent: 5095111 (1992-03-01), Lever et al.
patent: 5196510 (1993-03-01), Rodwell et al.
patent: 5212072 (1993-05-01), Blalock et al.
patent: 5225180 (1993-07-01), Dean et al.
patent: 5443816 (1995-08-01), Zamora et al.
patent: 5508020 (1996-04-01), Dean et al.
patent: 5556939 (1996-09-01), Flanagan et al.
patent: 5632969 (1997-05-01), Flanagan et al.
patent: 5716596 (1998-02-01), Dean et al.
patent: 5783170 (1998-07-01), Dean
Kessler et al., "Dimerisation of cyclic hexapeptides: strong increase of biological activity." Peptides 1988, pp. 664-666 (1989).
Byrne & Tolman, "Technetium-99m Bifunctional Chelating Agent--Thiolactone for Coupling to Biomolecules, N2S2 Ligand for Chalation to Technetium." J. Nucl. Med. 24:126 (1983).
Khaw, et al. "Technetium-99m Labeling of Antibodies to Cardiac Myosin Fab and to Human Fibrinogen." J. Nucl. Med. 23:1011-1019 (1982).
Rhodes, "Considerations in the Radiolabeling of Albumin." Sem. Nucl. Med. 4:281-293 (1974).
Zubay, Biochemistry (2nd. ed.), 1988 (MacMillan Publishing: New York), p. 33.
Spanevello et al (1991), Tetrahedron Letters, vol. 32, No. 36, pp. 4675-4678, "Synthesis of Novel Highty Potent Cyclic--Hexapeptide Analogs of Somatostatin. Potential Application of Orthogonal Protection for Affinity Chromatography."
Dean Richard T.
Lister-James John
McBride William
Dees Jos,e G.
Diatide, Inc
Jones Dameron
McDaniels Patricia A.
Noonan Kevin E.
LandOfFree
Radiolabeled somatostatin-derived peptides for imaging and thera does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Radiolabeled somatostatin-derived peptides for imaging and thera, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Radiolabeled somatostatin-derived peptides for imaging and thera will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2334280