You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 29, 2024

Details for Patent: 5,981,477


✉ Email this page to a colleague

« Back to Dashboard


Title: Peptide-metal chelate conjugates
Abstract:This invention relates to diagnostic and radiodiagnostic agents, including radiolabeled scintigraphic imaging agents, and therapeutic and radiotherapeutic agents. The invention provides such agents and reagents for preparing such agents, and methods for producing and using such reagents. Specifically, the invention provides radiolabeled imaging agents and non-radioactively labeled imaging agents for imaging sites in a mammalian body and reagents for preparing these imaging agents. The invention also provides radiolabeled therapeutic agents, as well as non-radioactively labeled therapeutic agents, and reagents and methods for preparing these agents. The agents and reagents provided comprise a specific binding peptide, covalently linked to a metal ion-complexing moiety. Reagents, methods and kits for making such reagents, methods for labeling such reagents, and methods for using such labeled reagents are provided.
Inventor(s): Dean; Richard T. (Bedford, NH)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:Mar 13, 1998
Application Number:09/039,116
Claims:1. A method of treating an animal bearing a somatostatin receptor-expressing tumor, comprising the step of:

administering to said animal a therapeutically effective amount of a pharmaceutical composition comprising a somatostatin receptor-binding peptide having a formula:

wherein

X is a metal ion complexing moiety having formula

wherein

B is a thiol-containing moiety that is cysteine, homocysteine, isocysteine, or penicillamine;

(amino acid).sub.n and (amino acid).sub.m are each independently any primary .alpha.- or .beta.-amino acid that does not comprise a thiol group;

Z is --OH or --NH.sub.2 ;

n is an integer between 2 and 5;

m is an integer between 0 and 5.

2. A method of radioisotope guided surgery, comprising the steps of:

a) administering to an animal bearing a somatostatin receptor-expressing tumor an effective amount of a pharmaceutical composition comprising a technetium-99m labeled somatostatin receptor-binding peptide having a formula:

wherein

X is a metal ion complexing moiety having formula

wherein

B is a thiol-containing moiety that is cysteine, homocysteine, isocysteine, or penicillamine;

(amino acid).sub.n and (amino acid).sub.m are each independently any primary .alpha.- or .beta.-amino acid that does not comprise a thiol group;

Z is --OH or --NH.sub.2 ;

n is an integer between 2 and 5;

m is an integer between 0 and 5; and

b) excising tissue containing neoplastic or metastatic cells identified by localization of radioactivity from the pharmaceutical composition.

3. A method of imaging a site within a mammalian body comprising the steps of:

a) administering an effective diagnostic amount of a pharmaceutical composition comprising a technetium-99m-labeled somatostatin receptor-binding peptide having a formula:

wherein

X is a metal ion complexing moiety having formula

wherein

B is a thiol-containing moiety that is cysteine, homocysteine, isocysteine, or penicillamine;

(amino acid).sub.n and (amino acid).sub.m are each independently any primary .alpha.- or .beta.-amino acid that does not comprise a thiol group;

Z is --OH or --NH.sub.2 ;

n is an integer between 2 and 5;

m is an integer between 0 and 5; and

b) detecting a radioactive signal from the technetium-99m localized at the site.

4. A method of radioisotope guided surgery, comprising the steps of:

a) administering to an animal bearing a somatostatin receptor-expressing tumor an effective amount of a pharmaceutical composition comprising an iodine-123-labeled or iodine-125-labeled somatostatin receptor-binding peptide having a formula:

wherein

X is a metal ion complexing moiety having formula

wherein

B is a thiol-containing moiety that is cysteine, homocysteine, isocysteine, or penicillamine;

(amino acid).sub.n and (amino acid).sub.m are each independently any primary .alpha.- or .beta.-amino acid that does not comprise a thiol group;

Z is --OH or --NH.sub.2 ;

n is an integer between 2 and 5;

m is an integer between 0 and 5; and

b) excising tissue containing neoplastic or metastatic cells identified by localization of radioactivity from the pharmaceutical composition.

5. A method of treating an animal bearing a somatostatin receptor-expressing tumor, comprising the step of:

administering to said animal a therapeutically effective amount of a pharmaceutical composition comprising a cytotoxic radioisotope and a somatostatin receptor-binding peptide having a formula:

wherein

X is a metal ion complexing moiety having formula

wherein

B is a thiol-containing moiety that is cysteine, homocysteine, isocysteine, or penicillamine;

(amino acid).sub.n and (amino acid).sub.m are each independently any primary .alpha.- or .beta.-amino acid that does not comprise a thiol group;

Z is --OH or --NH.sub.2 ;

n is an integer between 2 and 5;

m is an integer between 0 and 5.

6. The method of claim 5, wherein the radioisotope is selected from the group consisting of copper-67, iodine-125, iodine-131, rhenium-186, rhenium-188, tin-117m, and astatine-211.

7. A method of treating an animal bearing a somatostatin receptor-expressing tumor, comprising the step of:

administering to said animal a therapeutically effective amount of a pharmaceutical composition comprising a non-radioactive metal ion and a somatostatin receptor-binding peptide having a formula:

wherein

X is a metal ion complexing moiety having formula

wherein

B is a thiol-containing moiety that is cysteine, homocysteine, isocysteine, or penicillamine;

(amino acid).sub.n and (amino acid).sub.m are each independently any primary .alpha.- or .beta.-amino acid that does not comprise a thiol group;

Z is --OH or --NH.sub.2 ;

n is an integer between 2 and 5;

m is an integer between 0 and 5.

8. The method of claim 7, wherein the metal ion is selected from the group consisting of copper, zinc, and rhenium.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.