Homing agents

Patent metadata

Field	Value
Publication number	US-11052163-B2
Application number	US-201715711780-A
Country	US
Kind code	B2
Filing date	Sep 21, 2017
Priority date	May 3, 2013
Publication date	Jul 6, 2021
Grant date	Jul 6, 2021

Abstract

The present disclosure provides peptide constructs for diagnostic imaging and therapeutic applications, using pegylated peptides which exhibit specific binding for a target molecule of interest, such as a biomarker of a disease or disorder.

First claim

What is claimed is:

1. A p-armed multimer, wherein p is 4 and each arm of the multimer comprises:
a polymer comprising n PEG monomers, wherein n is 9;
a homing molecule that is SEQ ID NO: 1;
a chelating agent that is N2S2; and
a linker consisting of glutamic acid;

wherein the polymer, the homing molecule and the chelating agent are each attached to the linker and wherein at least one of the polymer, the homing molecule or the chelating agent is attached to a side chain of an amino acid in the linker; and
wherein each arm of the multimer is bound to the other arms of the multimer via an end of the polymer not attached to the linker.

2. A p-armed multimer of claim 1 , wherein the amino acid side chain is directly attached to one of the polymer, homing molecule or chelating agent.

3. A p-armed multimer of claim 1 , wherein the amino acid side chain is attached via click chemistry to one of the polymer, homing molecule or chelating agent.

4. A p-armed multimer of claim 1 , wherein the homing molecule is linked to the C-terminus of glutamic acid, and the polymer is linked via an amino acid side chain of glutamic acid.

5. A p-armed multimer of claim 1 , further comprising a radionuclide bonded to the chelating agent on at least one arm.

6. A p-armed multimer of claim 5 , further comprising a radionuclide bonded to the chelating agent on at least one arm.

7. A radiopharmaceutical composition comprising a p-armed multimer of claim 5 , together with a pharmaceutically-acceptable carrier.

8. A p-armed multimer of claim 1 , wherein the homing molecule is attached to the linker via a hydrophilic moiety.

9. A method for detecting intradevice thrombus in a subject having an implanted mechanical circulation assist device, the method comprising:
(a) administering into the bloodstream of the subject an effective amount of a p-armed multimer of claim 5 ;
(b) allowing the p-armed multimer to bind thrombus; and
(c) detecting a signal from the radionuclide of the p-armed multimer localized at a site of thrombus.

10. The method of claim 9 , wherein the method further comprises quantifying intradevice thrombus by: (d) determining the amount of p-armed multimer localized at a site of thrombus from the signal detected, wherein the amount of p-armed multimer is indicative of the size of the thrombus.

Assignees

• Lanza Gregory M
• Achilefu Samuel I
• Hufang Cui Grace
• Univ Washington

Inventors

• Lanza Gregory M
• Achilefu Samuel I
• Hufang Cui Grace

Classifications

• A61K49/085

  conjugated systems · CPC title

• C07K7/06

  having 5 to 11 amino acids · CPC title

• A61K49/0032

  Methine dyes, e.g. cyanine dyes · CPC title

• A61K51/065

  conjugates with carriers being macromolecules · CPC title

• A61K51/088 Primary

  conjugates with carriers being peptides, polyamino acids or proteins (antibodies A61K51/10) · CPC title