Antibody biopharmaceutical formulations including polymer excipients

Patent metadata

Field	Value
Publication number	US-12472260-B2
Application number	US-202418654883-A
Country	US
Kind code	B2
Filing date	May 3, 2024
Priority date	May 23, 2022
Publication date	Nov 18, 2025
Grant date	Nov 18, 2025

Abstract

Polyacrylamide-based copolymers act as stabilizing excipients in formulations of antibody biopharmaceutical agents without interacting directly with the antibody or altering its pharmacokinetic properties. The polyacrylamide-based copolymers confer a substantial stability benefit to high concentration compositions of a variety of antibodies by precluding adsorption of the antibody to the interfaces of the composition, preventing undesirable aggregation events and maintaining the binding activity of the antibody. Such antibody compositions are useful in methods of administering the composition to a subject.

First claim

The invention claimed is:

1 . A composition comprising:
a random copolymer consisting of:
a water-soluble carrier monomer selected from N-(3-methoxypropyl) acrylamide (MPAM) and 4-acryloylmorpholine (MORPH); and
a functional dopant monomer that is N-isopropylacrylamide (NIP);
wherein the random copolymer comprises from 10% to 28% by weight of NIP; and
an antibody.

2 . The composition of claim 1 , wherein the water-soluble carrier monomer is MORPH.

3 . The composition of claim 2 , wherein the random copolymer comprises from 20% to 26% by weight of NIP.

4 . The composition of claim 1 , wherein the water-soluble carrier monomer is MPAM.

5 . The composition of claim 1 , wherein the degree of polymerization of the random copolymer is from 10 to 500.

6 . The composition of claim 1 , wherein the molecular weight of the random copolymer is from 2,000 to 10,000 g/mol.

7 . The composition of claim 1 , wherein the degree of polymerization of the random copolymer is from 20 to 200, and the molecular weight of the random copolymer is from 2,000 to 10,000 g/mol.

8 . The composition of claim 3 , wherein the average molecular weight (Mn) of the random copolymer is from 2,000 to 10,000 g/mol, and the degree of polymerization of the random copolymer is from 20 to 200.

9 . The composition of claim 1 , wherein the random copolymer comprises 23% by weight of NIP.

10 . The composition of claim 1 , wherein the random copolymer comprises:
74% to 80% by weight of MORPH; and 20% to 26% by weight of NIP; the average molecular weight (Mn) of the random copolymer is from 1,000 g/mol to 5,000 g/mol; and the degree of polymerization of the random copolymer is 10 to 50.

11 . The composition of claim 2 , wherein the random copolymer comprises 77% by weight of MORPH and 23% by weight of NIP.

12 . A composition comprising:
a polyacrylamide-based copolymer comprising:
a water-soluble carrier monomer selected from MPAM and MORPH; and
a functional dopant monomer that is N-phenylacrylamide (PHE); and
an antibody.

13 . The composition of claim 12 , wherein the water-soluble carrier monomer is MPAM.

14 . The composition of claim 12 , wherein the water-soluble carrier monomer is MORPH.

15 . The composition of claim 12 , wherein the copolymer comprises from 2% to 16% by weight of PHE.

16 . The composition of claim 12 , wherein the degree of polymerization is from 10 to 500.

17 . The composition of claim 16 , wherein the degree of polymerization is from 20 to 200; and the molecular weight of the copolymer is from 2,000 to 10,000 g/mol.

18 . A composition comprising:
a polyacrylamide-based copolymer consisting of:
a water-soluble carrier monomer that is N-(3-methoxy-propyl) acrylamide (MPAM); and
a functional dopant monomer that is N-isopropylacrylamide (NIP); and
an antibody.

19 . The composition of claim 18 , wherein the copolymer is a random copolymer that comprises from 2% to 30% by weight of NIP.

20 . The composition of claim 18 , wherein the degree of polymerization of the copolymer is from 10 to 500.

21 . The composition of claim 18 , wherein the degree of polymerization of the copolymer is from 20 to 200, and the molecular weight of the copolymer is from 2,000 to 10,000 g/mol.

22 . The composition of claim 3 , wherein the random copolymer comprises 22%, 23%, or 24% by weight of NIP.

23 . The composition of claim 22 , wherein the molecular weight of the random copolymer is from 4,000 g/mol to 10,000 g/mol.

24 . The composition of claim 23 , wherein the molecular weight of the random copolymer is from 6,000 g/mol to 10,000 g/mol.

25 . The composition of claim 23 , wherein the molecular weight of the random copolymer is from 4,000 g/mol to 7,000 g/mol.

Assignees

• Univ Leland Stanford Junior

Inventors

• Appel Eric A
• Mann Joseph L
• Klich John
• Kasse Catherine M

Classifications

• C07K16/1145

  Env proteins, e.g. gp41, gp110/120, gp160, V3, principal neutralising domain [PND] or CD4-binding site · CPC title

• A61K39/39591

  Stabilisation, fragmentation · CPC title

• A61K9/08

  Solutions {(composition of solutions A61K47/00)} · CPC title

• A61P31/18

  for HIV · CPC title

• A61K9/1075

  Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence) · CPC title