Bombesin analog peptide antagonist conjugates

a technology of analog peptides and conjugates, which is applied in the direction of peptide/protein ingredients, drug compositions, and therapeutics, can solve the problems of unsatisfactory radioscintigraphic imaging and radiotherapeutic purposes, unsatisfactory uptake, and need to be improved. to achieve the effect of inhibiting the effect of the agonis
US20150265733A1Inactive Publication Date: 2015-09-24UNIVSSPITAL BASEL +1
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Patent Information

Authority / Receiving Office
US · United States
Patent Type
Applications(United States)
Current Assignee / Owner
UNIVSSPITAL BASEL
Publication Date
2015-09-24
Estimated Expiration
Not applicable · inactive patent

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Abstract

To provide a diagnostic and therapeutic medicament, a bombesin analog peptide antagonist conjugate is provided which has general Formula (I), wherein A is a metal chelator comprising at least one radionuclide metal, B is a spacer linked to N-terminal of C or a covalent bond and C is a bombesin analog peptide antagonist having a sequence as claimed, where further x is an Integer from 1 to 3 and n is an integer from 1 to 6.[A−(B)n]x−C
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Description

INTRODUCTION

[0001] The invention relates to therapeutic or diagnostic / imaging radiopharmaceuticals, the preparation and use thereof wherein the therapeutic or diagnostic radiopharmaceuticals are defined as binding moieties having an affinity for and are capable of binding to bombesin receptors and more particularly to gastrin releasing peptide (GRP) receptor. The binding moieties are labeled to metal complexing group for alpha-, beta-, gamma- and positron emitting isotopes. The use includes treating a subject, having a neoplastic disease comprising the step of administering to the subject an effective amount of a therapeutic radiopharmaceutical having a metal chelated with a chelating group attached to a moiety capable of binding to bombesin receptors and more particularly to gastrin releasing peptide (GRP) receptor over-expressed on tumor cells. The use includes diagnosing or imaging a subject having a neoplastic disease using a diagnostic / imaging radiopharmaceutical having a metal ...

Claims

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