Granted Patent B2

US 12,702,711 · App. 19/376,547 · Granted Aug 11, 2026

Inventors: Susanne Joerg (Binningen, CH); Kathrin Serno-Schersch (Basel, CH)

Assignee: NOVARTIS AG

A61K39/39591C07K16/244H04L5/0016H04L5/0023H04L5/0051C07K2317/21

Abstract

Claims (71)

1 . A liquid pharmaceutical composition comprising:

(i) about 150 mg/mL secukinumab;

(ii) 2.5 mM to 134 mM methionine;

(iii) a non-ionic stabilizer; and

(iv) a surfactant;

wherein the composition has a pH of about 5.2 to about 6.4; and

wherein upon storage of the liquid pharmaceutical composition at 2-8° C. for about 24 months, at least one of the following criteria is met:

(a) no more than 5% of secukinumab main variant is degraded as measured by reverse phase-high performance liquid chromatography (RP-HPLC); and

(b) no more than 5% of secukinumab pre-main peak variant is formed as measured by RP-HPLC.

2 . The composition of claim 1 , wherein upon storage of the liquid pharmaceutical composition at 2-8° C. for about 24 months, at least one of the following criteria is additionally met:

(a) no more than 5% of secukinumab main variant is degraded as measured by cation exchange chromatography (CEX);

(b) no more than 5% of secukinumab basic variants are formed as measured by CEX; and

(c) no more than 5% of secukinumab acidic variants are formed as measured by CEX.

3 . The composition of claim 2 , wherein upon storage of the liquid pharmaceutical composition at 2-8° C. for about 24 months, at least one of the following criteria is additionally met:

(a) no more than 5% of secukinumab monomer is degraded as measured by size exclusion chromatography (SEC);

(b) no more than 5% secukinumab aggregates are formed as measured by SEC; and

(c) no more than 5% secukinumab degradation products are formed as measured by SEC.

4 . The composition of claim 1 , wherein the composition comprises a buffer selected from gluconate, histidine, citrate, phosphate, succinate, acetate, Tris, glycine, arginine, and a combination thereof.

5 . The composition of claim 2 , wherein the composition comprises a buffer selected from gluconate, histidine, citrate, phosphate, succinate, acetate, Tris, glycine, arginine, and a combination thereof.

6 . The composition of claim 3 , wherein the composition comprises a buffer selected from gluconate, histidine, citrate, phosphate, succinate, acetate, Tris, glycine, arginine, and a combination thereof.

7 . The composition of claim 4 , wherein the non-ionic stabilizer is mannitol, trehalose, raffinose, maltose, sorbitol, or a combination thereof.

8 . The composition of claim 5 , wherein the non-ionic stabilizer is mannitol, trehalose, raffinose, maltose, sorbitol, or a combination thereof.

9 . The composition of claim 6 , wherein the non-ionic stabilizer is mannitol, trehalose, raffinose, maltose, sorbitol, or a combination thereof.

10 . The composition of claim 7 , wherein the surfactant is polysorbate 20 or polysorbate 80.

11 . The composition of claim 8 , wherein the surfactant is a polysorbate 20 or polysorbate 80.

12 . The composition of claim 9 , wherein the surfactant is a polysorbate 20 or polysorbate 80.

13 . The composition of claim 10 , wherein:

(a) the buffer is at a concentration of 10 mM to 30 mM;

(b) the non-ionic stabilizer is at a concentration of about 175 mM to about 350 mM; and

(c) the surfactant is at a concentration of 0.01% (w/v) to 0.1% (w/v).

14 . The composition of claim 11 , wherein:

(a) the buffer is at a concentration of 10 mM to 30 mM;

(b) the non-ionic stabilizer is at a concentration of about 175 mM to about 350 mM; and

(c) the surfactant is at a concentration of 0.01% (w/v) to 0.1% (w/v).

15 . The composition of claim 12 , wherein:

(a) the buffer is at a concentration of 10 mM to 30 mM;

(b) the non-ionic stabilizer is at a concentration of about 175 mM to about 350 mM; and

(c) the surfactant is at a concentration of 0.01% (w/v) to 0.1% (w/V).

16 . The composition of claim 13 , wherein:

(a) the buffer comprises citrate;

(b) the non-ionic stabilizer is sorbitol; and

(c) the surfactant is polysorbate 80.

17 . The composition of claim 14 , wherein:

(a) the buffer comprises citrate;

(b) the non-ionic stabilizer is sorbitol; and

(c) the surfactant is polysorbate 80.

18 . The composition of claim 15 , wherein:

(a) the buffer comprises citrate;

(b) the non-ionic stabilizer is sorbitol; and

(c) the surfactant is polysorbate 80.

19 . The composition of claim 13 , wherein:

(a) the buffer comprises histidine;

(b) the non-ionic stabilizer is trehalose; and

(c) the surfactant is polysorbate 80.

20 . The composition of claim 14 , wherein:

(a) the buffer comprises histidine;

(b) the non-ionic stabilizer is trehalose; and

(c) the surfactant is polysorbate 80.

21 . The composition of claim 15 , wherein:

(a) the buffer comprises histidine;

(b) the non-ionic stabilizer is trehalose; and

(c) the surfactant is polysorbate 80.

22 . The composition of claim 16 , wherein the methionine is at a concentration from about 10 mM to about 67 mM.

23 . The composition of claim 17 , wherein the methionine is at a concentration from about 10 mM to about 67 mM.

24 . The composition of claim 18 , wherein the methionine is at a concentration from about 10 mM to about 67 mM.

25 . The composition of claim 19 , wherein the methionine is at a concentration from about 10 mM to about 67 mM.

26 . The composition of claim 20 , wherein the methionine is at a concentration from about 10 mM to about 67 mM.

27 . The composition of claim 21 , wherein the methionine is at a concentration from about 10 mM to about 67 mM.

28 . The composition of claim 3 , wherein the secukinumab has at least 2.0 mol free thiol (SH) per mol secukinumab upon storage the liquid pharmaceutical composition at 2-8° C. for about 24 months.

29 . The composition of claim 12 , wherein the secukinumab has at least 2.0 mol free thiol (SH) per mol secukinumab upon storage the liquid pharmaceutical composition at 2-8° C. for about 24 months.

30 . The composition of claim 15 , wherein the secukinumab has at least 2.0 mol free thiol (SH) per mol secukinumab upon storage the liquid pharmaceutical composition at 2-8° C. for about 24 months.

Assignments (3)

Continuity (5)

References Cited (400)