IP Library › Granted Patent US 12685790
Granted Patent B2
US 12685790 · App. 17/753,762 · Granted Jul 21, 2026

Stable, concentrated radiopharmaceutical composition

Inventors: Donato Barbato (Ivrea, IT); Lorenza Fugazza (Ivrea, IT); Maurizio F. Mariani (Ivrea, IT); Francesca Orlandi (Ivrea, IT); Lorenzo Sacchetti (Turin, IT); Mattia Tedesco (Alba, IT)
Assignee: Novartis AG
A61K51/088A61K47/12
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Quick Facts
Patent No.
US 12685790
App. No.
17/753,762
Granted
Jul 21, 2026
Kind
B2
Abstract

The present disclosure relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.

Claims (26)

1 . A pharmaceutical composition comprising:

(a) a complex formed by

(ai) a radionuclide 177 Lu, and

(aii) a compound of formula I

 and;

(b) at least two stabilizers against radiolytic degradation which are gentisic acid or salts thereof and ascorbic acid or salts thereof,

wherein the concentration ratio in μg/mL between gentisic acid or salts thereof and ascorbic acid or salts thereof is between 1:16 and 1:10; and

(c) optionally a surfactant.

2 . The pharmaceutical composition according to claim 1 , wherein said radionuclide is present at a concentration providing a volumetric radioactivity of at least 370 MBq/mL at End Of Processing±37 MBq/mL.

3 . The pharmaceutical composition according to claim 1 , wherein said gentisic acid or salts thereof is present in a concentration of least 1000 μg/mL.

4 . The pharmaceutical composition according to claim 1 , wherein said ascorbic acid or salts thereof is present in a concentration of at least 10000 μg/mL.

5 . The pharmaceutical composition according to claim 1 , wherein said pharmaceutical formulation has a radiochemical purity higher than 95% up to 72 hours.

6 . The pharmaceutical composition of claim 1 further comprising macrogol 15 hydroxystearate as a surfactant.

7 . The pharmaceutical composition according to claim 6 , further comprising at least one other pharmaceutically acceptable excipient selected from buffer and/or solvent, and/or pH adjuster.

8 . A pharmaceutical composition consisting of:

(a) a complex formed by

(ai) radionuclide 177 Lutetium (Lu-177), and

(aii) NeoB of formula (I):

 and;

(b) gentisic acid or salts thereof and ascorbic acid or salts thereof;

(c) Macrogol 15 Hydroxystearate;

(d) acetate buffer;

(e) water for injection;

(f) NaOH; and

(g) DTPA,

wherein the concentration ratio in μg/mL between gentisic acid or salts thereof and ascorbic acid or salts thereof is between 1:16 and 1:10.