A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 47/48 (2006.01) A61K 51/08 (2006.01) C07K 7/06 (2006.01) C07K 14/245 (2006.01) G01N 33/574 (2006.01) G01N 33/60 (2006.01)
Patent
CA 2439579
A peptide-chelate conjugate with affinity for the ST receptor is disclosed, wherein the chelate is tetradentate. A low-molecular weight heat-stable toxin is produced by enterotoxic strains of E. Coli. This toxin, known as ST peptide, mediates acute diarrheal disease by binding to its receptor on colorectal cells and stimulating guanylate cyclase. Gastrointestinal mucosal cells specifically express the ST receptor and the expression persist after colonic and rectal mucosal cells undergo malignant neoplasic transformation. The peptide-chelate conjugate of the invention may be labelled with a radiometal to provide a metal complex. In a preferred embodiment, the radiometal is 99mtc, and the chelating agent is selected from: diaminedioxime, diaminediphenol, N3S, N4 and N2S2 Ligands. A radiopharmaceutical composition comprising the metal complex is provided, which is suitable for the diagnostic imaging of colorectal cancer. Also provided for in the invention is a kit for the preparation of the radiopharmaceutical preparation.
L'invention concerne un conjugué peptide-chélate présentant une certaine affinité pour le récepteur ST, conjugué dans lequel chélate représente tétradentate. Ledit conjugué peptide-chélate peut être marqué à l'aide d'un radiométal pour l'obtention d'un complexe métallique. Cette invention concerne également une composition radiopharmaceutique, renfermant ledit complexe métallique et convenant à l'imagerie diagnostique du cancer colorectal, ainsi qu'un coffret servant à l'élaboration de ladite préparation pharmaceutique.
Bacon Edward Richard
Cuthbertson Alan
Desai Vinay Chandrakant
Dixon Mark
Kasina Sudakhar
Amersham Plc
Fetherstonhaugh & Co.
Ge Healthcare Limited
LandOfFree
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