Granted Patent B1

US 12,343,409 · App. 18/770,529 · Granted Jul 1, 2025

Inventors: Manuel Sturzbecher-Höhne (Berlin, DE); Dennis Mewis (Berlin, DE); Marion Huber (Berlin, DE)

Assignee: Ariceum Therapeutics GmbH

A61K51/0482A61K47/22

Abstract

Claims (21)

1. A method of preparing a liquid radiopharmaceutical composition comprising a radiopharmaceutical compound according to Formula I

or a pharmaceutically acceptable salt thereof,

the method comprising:

providing a liquid radiopharmaceutical pre-composition comprising:

i. a precursor compound according to Formula II

or a pharmaceutically acceptable salt thereof;

ii. a buffer, wherein the buffer provides the liquid radiopharmaceutical pre-composition with a pH of about 8.0 to about 8.9; and

iii. a [ 225 Ac]Ac 3+ salt;

heating the liquid radiopharmaceutical pre-composition to generate a labelled composition;

cooling the labelled composition; and

diluting the labelled composition with a formulation solution; wherein the formulation solution comprises a formulation buffer that provides the liquid radiopharmaceutical composition with a pH of about 8.0 to about 8.9.

2. A method according to claim 1 , wherein the heating of the liquid radiopharmaceutical pre-composition is for at least about 75° C.

3. A method according to claim 1 , wherein the heating of the liquid radiopharmaceutical pre-composition is for at least about 20 minutes.

4. A method according to claim 1 , wherein the labelled composition is diluted between 5 times and 100 times with the formulation solution.

5. A method according to claim 1 , wherein at least part of cooling the labelled composition occurs on diluting the labelled composition with the formulation solution.

6. A method according to claim 1 , wherein the radiopharmaceutical compound is present at a concentration equivalent to about 0.1 MBq/mL to about 0.5 MBq/mL based on the total volume of the liquid radiopharmaceutical composition.

7. A method according to claim 1 , wherein the buffer and formulation buffer are present at a combined concentration of between about 1 mM to about 100 mM based on the total volume of the liquid radiopharmaceutical composition.

8. A method according to claim 1 , wherein the liquid radiopharmaceutical composition comprises a stabiliser selected from ascorbic acid, gentisic acid, glutathione, methionine, hydroquinone, polyoxyethylene (20) sorbitan monooleate, or structural analogues thereof, or pharmaceutically acceptable salts thereof, or combinations thereof.

9. A method according to claim 8 , wherein the stabiliser is ascorbic acid or a pharmaceutically acceptable ascorbate.

10. A method according to claim 8 , wherein the stabiliser is present at a concentration of greater than 350 mM based on the total volume of the liquid radiopharmaceutical composition.

11. A method according to claim 1 , wherein the liquid radiopharmaceutical composition retains a radiochemical purity of >91% after 168 hours at ambient temperature.

Assignments (1)

Priority Claims (1)

References Cited (13)