Granted Patent B2

US 12,685,790 · App. 17/753,762 · Granted Jul 21, 2026

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

Abstract

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.

Assignments (2)

Priority Claims (1)

Continuity (1)

References Cited (16)