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1. WO1996040291 - RADIOLABELED PEPTIDE COMPOSITIONS FOR SITE-SPECIFIC TARGETING

Publication Number WO/1996/040291
Publication Date 19.12.1996
International Application No. PCT/US1996/009384
International Filing Date 06.06.1996
Chapter 2 Demand Filed 03.01.1997
IPC
A61K 51/08 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier
04Organic compounds
08Peptides, e.g. proteins
C07K 14/655 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
655Somatostatins
CPC
A61K 51/083
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
08Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
083the peptide being octreotide or a somatostatin-receptor-binding peptide
A61K 51/088
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
08Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
088conjugates with carriers being peptides, polyamino acids, proteins
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07K 14/6555
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
655Somatostatins
6555at least 1 amino acid in D-form
Applicants
  • MALLINCKRODT MEDICAL, INC. [US]/[US]
Inventors
  • SRINIVASAN, Ananthachari
  • DYSZLEWSKI, Mary, Marmion
  • BUGAJ, Joseph, E.
Agents
  • MCBRIDE, Thomas, P.
Priority Data
08/480,37307.06.1995US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) RADIOLABELED PEPTIDE COMPOSITIONS FOR SITE-SPECIFIC TARGETING
(FR) COMPOSITIONS DE PEPTIDES RADIOMARQUES POUR LE CIBLAGE SPECIFIQUE D'UN SITE
Abstract
(EN)
This invention relates to radiolabeled peptide compositions for radiopharmaceutical use and, more specifically, to radiolabeled peptides for diagnostic or therapeutic use having an unmodified carboxy terminal amino acid. The radiopharmaceutical composition may be used for targeting a selected biological site. The radiolabeled peptide is characterized by having its carboxy terminal amino acid in its carboxylic acid form and the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent. The radiopharmaceutical composition preferably comprises a radiolabeled peptide selected from the group consisting of somatostatin, an analog of somatostatin, a derivative of somatostatin and peptides capable of binding to the somatostatin receptor, where the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent has its carboxy terminal amino acid in its carboxylic acid form.
(FR)
Cette invention concerne des compositions de peptides radiomarqués destinées à un usage radiopharmaceutique et, de manière plus spécifique, à des peptides radiomarqués destinés à des fins diagnostiques ou thérapeutiques, et possédant un acide aminé non modifié à terminaison carboxy. Cette composition radiopharmaceutique peut être utilisée pour cibler un site biologique choisi. Le peptide radiomarqué se caractérise par le fait que son acide aminé à terminaison carboxy se présente sous sa forme acide carboxylique, le peptide étant couplé à un radionucléide à vocation diagnostique ou thérapeutique par un agent chélateur. Cette composition radiopharmaceutique comprend, de préférence, un peptide radiomarqué choisi dans le groupe constitué de la somatostatine, d'un analogue de somatostatine, d'un dérivé de somatostatine, et de peptides capables de se lier au récepteur de somatostatine, le peptide étant couplé à un radionucléide à vocation diagnostique ou thérapeutique par un agent chélateur, tandis que son acide aminé à terminaison carboxy se présente sous sa forme acide carboxylique.
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