Compositions and methods for non-invasive imaging

Patent metadata

Field	Value
Publication number	US-9511155-B2
Application number	US-201314395345-A
Country	US
Kind code	B2
Filing date	Apr 17, 2013
Priority date	Apr 17, 2012
Publication date	Dec 6, 2016
Grant date	Dec 6, 2016

Abstract

The present invention relates to a novel composition useful in targeted diagnostic and/or therapy of a target site, such as cancerous tissue. The composition and methods disclosed herein find particular use in diagnosing and imaging cancerous tissue. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.

First claim

We claim:

1. A liposomal imaging agent composition comprising: (a) liposomes in a pharmaceutically acceptable medium, said liposomes each having an interior space and a membrane separating said interior from said medium, said membrane comprising one or more lipids; and (b) a compound comprising a chelated metal ion, M, as shown in formula (II) in at least one liposome of the liposomes of (a):

in which M is a copper cation detectable within the liposomal imaging agent.

2. The composition of claim 1 , wherein M is a radioisotope of the copper cation.

3. The composition of claim 2 , wherein the radioisotope is a radioisotope of Cu 2+ .

4. The composition of claim 3 wherein the radioisotope of Cu 2+ is 64 Cu or 67 Cu.

5. The composition of claim 1 , comprising:
liposomes in a pharmaceutically acceptable medium, said liposomes each having an interior space and a membrane separating said interior from said medium, said membrane comprising DSPC, cholesterol and PEG-DSPE.

6. The composition of claim 1 , wherein the liposome membrane comprises DSPC, Cholesterol and PEG-DSPE in a weight ratio of 3:1:1.

7. A liposomal imaging agent comprising a detectable 64 Cu:4-DEAP-ATSC encapsulated in a liposome, the liposome having a liposome membrane comprising DSPC, Cholesterol and PEG-DSPE.

8. The liposomal imaging agent of claim 7 , having an external pH of 5-8.

9. The liposomal imaging agent of claim 7 , having an external pH of about 7.4.

10. The liposomal imaging agent of claim 7 , further comprising a nonpolymeric anionic trapping agent encapsulated within the liposome.

11. The liposomal imaging agent of claim 7 , further comprising sucrose octasulfate encapsulated within the liposome.

12. The liposomal imaging agent of claim 7 , wherein the liposome membrane comprises DSPC, Cholesterol and PEG-DSPE in a 3:1:1 weight ratio.

13. The liposomal imaging agent of claim 12 , further comprising sucrose octasulfate encapsulated within the liposome.

14. The liposomal imaging agent of claim 7 , comprising Cu 2+ in an amount providing radioactivity detectable within a patient.

15. An imaging agent comprising a compound of formula (II) encapsulated in a liposome, in an amount providing detectable radioactivity within a patient, here M is a Cu 2+ radioisotope

16. The imaging agent of claim 15 , wherein the liposome comprises a PEGylated lipid.

17. The imaging agent of claim 15 , wherein the liposome comprises DSPC, Cholesterol and PEG-DSPE.

18. The imaging agent of claim 17 , further comprising sucrose octasulfate encapsulated with the compound of formula (II) within the liposome and having an external pH of about 7.4.

19. The imaging agent of claim 17 , having an external pH of 5-8.

Assignees

• Merrimack Pharmaceuticals Inc

Inventors

• Drummond Daryl C
• Kirpotin Dmitri B
• Wickham Thomas
• Hendriks Bart S
• Agresta Samuel
• Lee Helen
• Gaddy Daniel F

Classifications

• A61K51/1234 Primary

  Liposomes · CPC title

• A61K31/4745

  condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48) · CPC title

• A61K9/1271

  Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911}) · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K51/0478 Primary

  complexes from non-cyclic ligands, e.g. EDTA, MAG3 · CPC title