Method for preparing antibody-containing formulation

Patent metadata

Field	Value
Publication number	US-2026022194-A1
Application number	US-202519350318-A
Country	US
Kind code	A1
Filing date	Oct 6, 2025
Priority date	Dec 1, 2021
Publication date	Jan 22, 2026
Grant date	—

Abstract

Provided is a pharmaceutical formulation with reduced particle formation, comprising an anti-coagulation factor IXa/X antibody (bispecific monoclonal antibody) that substitutes for coagulation factor VIII, or an anti-IL-6 receptor antibody that inhibits binding to the interleukin 6 receptor. Provided is a pharmaceutical formulation comprising an aqueous solution comprising a polyoxyethylene polyoxypropylene glycol (poloxamer),
wherein the poloxamer is represented by formula I:

wherein a and c are independently an integer selected from 75 to 85;
b is an integer selected from 22 to 33; and a, b and c are average values over the entire poloxamer,

and,
the poloxamer comprises poloxamer molecules comprising 34 or more (C 3 H 6 O) in the molecule at a ratio of 3% (w/w) or more of the total poloxamer.

First claim

1 - 17 . (canceled)

18 . A pharmaceutical formulation comprising an aqueous solution comprising:
a monoclonal antibody comprising either (i) the H chains of SEQ ID NOs: 1 and 2 and the L chain of SEQ ID NO: 3, or (ii) the H chain of SEQ ID NO: 4 and the L chain of SEQ ID NO: 5, and a surfactant selected from polysorbate 20, polysorbate 80, poloxamer 188, and poloxamer 237,
wherein an aqueous solution comprising the surfactant at a concentration of 0.5 mg/mL has a
surface tension of 52 mN/m or less.

19 . The pharmaceutical formulation of claim 18 , wherein the surfactant is a poloxamer that is represented by formula I:

wherein:
a and c are independently a number selected from 75 to 85;
b is a number selected from 22 to 40; and
a, b, and c are average values over the entire poloxamer.

20 . The pharmaceutical formulation of claim 18 , wherein the surfactant is a polysorbate selected from polysorbate 20 and polysorbate 80.

21 . The pharmaceutical formulation of claim 20 , wherein the surfactant is polysorbate 80.

22 . The pharmaceutical composition of claim 18 , wherein the surfactant is a poloxamer, and the degree of unsaturation of the poloxamer is less than 0.018 mEq/g.

23 . The pharmaceutical composition of claim 19 , wherein b is a number selected from 22 to 33.

24 . The pharmaceutical composition of claim 19 , wherein b is a number selected from 25 to 30.

25 . The pharmaceutical composition of claim 19 , wherein b is a number selected from 35 to 40.

26 . The pharmaceutical composition of claim 19 , wherein the number-average molecular weight of the poloxamer is in the range of 7680 to 9510.

27 . The pharmaceutical formulation of claim 18 , wherein the concentration of the surfactant in the pharmaceutical formulation is in the range of 0.001 to 100 mg/mL.

28 . The pharmaceutical formulation of claim 18 , wherein the concentration of the antibody in the pharmaceutical formulation is in the range of 10 to 300 mg/mL.

29 . The pharmaceutical formulation of claim 18 , wherein the pharmaceutical formulation comprises one or more pharmaceutically acceptable excipients selected from sugars, sugar alcohols, buffering agents, preservatives, carriers, antioxidants, chelating agents, natural polymers, synthetic polymers, cryoprotectants, extenders, and stabilizers.

30 . The pharmaceutical formulation of claim 18 , wherein the surfactant is poloxamer 188 or poloxamer 237.

31 . A method for reducing the formation of particles in an aqueous solution comprising a monoclonal antibody having (a) the H chains of SEQ ID NOs: 1 and 2 and the L chain of SEQ ID NO: 3, or (b) the H chain of SEQ ID NO: 4 and the L chain of SEQ ID NO: 5,
the method comprising adding a surfactant to the aqueous solution, wherein the surfactant is polysorbate 20, polysorbate 80, poloxamer 188 or poloxamer 237, and wherein an aqueous solution comprising the surfactant at a concentration of 0.5 mg/mL has a surface tension of 52 mN/m or less.

Assignees

• Chugai Pharmaceutical Co Ltd
• Hoffmann La Roche

Inventors

• Soeda Kohei
• Fukuda Masakazu
• Takahashi Masaya
• Imai Hirotaka
• Saitoh Satoshi
• Duboeuf Jeremy
• RAVURI Kishore
• Kopf Robert
• Chen Wei
• Oltra Nuria Sancho

Classifications

• A61K39/0005

  Vertebrate antigens (from snakes A61K39/38) · CPC title

• C07K2317/24

  containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered · CPC title

• C07K2317/31

  multispecific · CPC title

• C07K16/2866

  against receptors for cytokines, lymphokines, interferons · CPC title

• C07K2317/94

  Stability, e.g. half-life, pH, temperature or enzyme-resistance · CPC title