Nihon Medi-physics Company, Limited

Ge Healthcare Limited

Yoshifumi Shirakami

Ikuya Seki

Yoshitoshi Itaya

Koichi Hanaoka

Nobuo Ueda

Anthony Eamon Storey

Keietsu Takahashi

Miki Kurami

Komei Washino

Takayoshi Kawaguchi

Yoshihito Minosako

Georg Brauers

Koichi Homma

A stabilized radiopharmaceutical composition, a kit including same, and a method for making same, where the radiopharmaceutical is (i) susceptible to either reductive degradation or radiolysis and which includes a metal complex of a radionuclide with a ligand, (ii) a first stabilizer for the radiopharmaceutical which is an amino-substituted aromatic carboxylic acid or a salt, ester or amide thereof, and (iii) a second stabilizer for the radiopharmaceutical which is a diphosphonic acid or salt thereof. The first and second stabilizers are present in an amount effective to stabilize the radiopharmaceutical, and the radiopharmaceutical is not a metal complex of the diphosphonic acid.

Stabiliser for radiopharmaceuticals

A compound that comprises Met-Leu-Phe or Nle-Leu-Phe serving as the leukocyte-binding site of a formyl peptide receptor (FPR), a binding part comprising Ser or Thr that increases the binding ratio to monocytes and lymphocytes in all leukocytes, a group that can be labeled with a radioactive metal or a paramagnetic metal, and spacers binding the three moieties together shows binding properties specific to all leukocytes, i.e., neutrophils, monocytes and lymphocytes both in vivo and in vitro. Owing to this characteristic, this compound is highly useful in SPECT image diagnosis, PET image diagnosis, MRI image diagnosis and the like, for imaging sites of inflammation.

Compound binding to leukocytes and medicinal composition containing the compound in labeled state as the active ingredient

A peptide having affinity with tumor or a salt thereof, which comprises an amino acid sequence containing 20 or less amino acid residues, said amino acid sequence being described as X.sub.1 -YCAREPPT-X.sub.2 wherein A, C, E, P, R, T and Y represent amino acid residues expressed by standard one-letter symbols, each of amino acid residues A, C, R and Y in the amino acid sequence YCAR may be in either L-form or D-form, X.sub.1 represents a basic organic compound having 1-3 amino groups, and X.sub.2 represents any given amino acid sequence, is provided together with a radioactive diagnostic agent and a radioactive therapeutic agent containing the above peptide or a salt thereof. The present tumor affinity peptide is high in radioactive metal labeling yield, useful for imaging and treating pathological tissues such as of breast cancer, ovarian cancer and colon cancer of mammals including human, and difficult to be readily metabolized in organisms and to accumulate in normal tissues especially at kidney and liver.

Tumor affinity peptide, and radioactive diagnostic agent and radioactive

A peptide having affinity with inflammation is disclosed, which contains at least one of the following amino acid sequences:

Peptide having inflammation affinity and radioactive diagnostic

The invention provides, inter alia, metal radionuclide-labelled reagent comprising a metal radionuclide coordinated with a metal chelate forming peptide having an amino acid sequence of three amino acid residues represented by: X1-X2-Cys, wherein X1 represents an Asp residue, a Tyr residue or a Lys residue; X2 represents an amino acid residue other than a Cys residue and a Pro residue, provided that X2 does not represent a Gly residue when X1 represents an Asp residue; wherein functional groups at the N-terminus, C-terminus and side chain may be optionally substituted with protecting groups; and wherein each of the amino acid residues may be either D-form or L-form.

Metal chelate forming peptides and use thereof represented by three

The invention provides a metal chelate forming peptide having an amino acid sequence of three amino acid residues represented by: X1-X2-Cys, wherein X1 represents an amino acid residue other than Cys residue; X2 represents an amino acid residue other than Cys residue and Pro residue; functional groups at the N-terminus, C-terminus and side chain may be substituted with protecting groups; and each of the amino acid residues may be any of D-form and L-form. Further, the invention provides a complex of the peptide with a physiologically active peptide, protein or other substance; a labeled reagent obtained by labeling the peptide or the complex with a metal radionuclide; and a radiodiagnostic and radiotherapeutic composition comprising the metal radionuclide-labeled reagent.

Metal chelate forming peptides and use thereof

A radioactive diagnostic or therapeutic agent, which comprises a metallic element-labeled high molecular compound which comprises one unit of (1) a polyamine compound having at least three amino groups in the side chains per molecule, at least two units of (2) a chelate-forming compound having a carboxyl group, at least one unit of (3) a physiologically active substance and (4) at least two radioactive metallic elements, each unit of the chelate-forming compound (2) and the physiologically active substance (3) being combined to any of the amino groups in the side chains of the polyamine compound (1) and each of the radioactive metallic element (4) being chelate-bonded to the chelate-forming compound (2).

Growing community of inventors

Ichihara, Japan

Yoshifumi Shirakami