Stabilized antibody compositions

Patent metadata

Field	Value
Publication number	US-10273298-B2
Application number	US-201414907254-A
Country	US
Kind code	B2
Filing date	Jul 23, 2014
Priority date	Jul 23, 2013
Publication date	Apr 30, 2019
Grant date	Apr 30, 2019

Abstract

The invention provides novel compositions of antibodies based on liquid vehicles selected from semifluorinated alkanes. The use of these vehicles provides for improved stability and shelf-life of antibodies and their derivatives. The compositions are useful for topical administration or for parenteral injection.

First claim

The invention claimed is:

1. A composition comprising an antigen-binding polypeptide or protein and a liquid vehicle, wherein the liquid vehicle comprises a semifluorinated alkane of the formula
RFRH
wherein RF is a linear perfluorinated hydrocarbon segment with 4 to 12 carbon atoms, and wherein RH is a linear alkyl group with 4 to 8 carbon atoms; and wherein the antigen-binding polypeptide or protein is incorporated in the composition such as to form a dispersion or suspension;
wherein the composition is substantially free of water.

2. The composition of claim 1 , wherein the antigen-binding polypeptide or protein is selected from a monoclonal antibody, polyclonal antibody, an antibody fragment, a fusion protein comprising an antibody fragment, an antibody-drug conjugate, or any combination thereof.

3. The composition of claim 2 , wherein the antibody fragment is a fragment antigen-binding (Fab), a single-chain variable fragment (scFv), a single-domain antibody, a minibody, or a diabody.

4. The composition of claim 2 , wherein the monoclonal antibody is a chimeric, humanized, or human antibody.

5. The composition of claim 1 , wherein the antigen-binding polypeptide or protein has a molecular mass of at least 90 kDa.

6. The composition of claim 1 , wherein the semifluorinated alkane is selected from F4H5, F4H6, F4H8, F6H4, F6H6, F6H8, and F6H10.

7. The composition of claim 1 , wherein the composition consists essentially of the antigen-binding polypeptide or protein and the liquid vehicle, the liquid vehicle consisting of one or more semi-fluorinated alkanes of the formula RFRH, wherein RF is a linear perfluorinated hydrocarbon segment with 4 to 12 carbon atoms, and wherein RH is a linear alkyl group with 4 to 8 carbon atoms.

8. The composition of claim 1 , wherein the composition retains at least 85% of its initial antigen-binding activity during storage of 6 months at a temperature of between RT to 40° C.

9. The composition of claim 1 , wherein the antigen-binding polypeptide or protein is at a concentration of at least 0.5 mg/mL.

10. The composition of claim 1 , wherein the antigen-binding polypeptide or protein is an angiogenesis inhibitor, an anti-proliferative agent or a TNF inhibitor.

11. The composition of claim 2 , wherein the semifluorinated alkane is selected from F4H5, F4H6, F4H8, F6H4, F6H6, F6H8, and F6H10.

12. The composition of claim 11 , wherein the composition consists essentially of the antigen-binding polypeptide or protein and the liquid vehicle, the liquid vehicle consisting of one or more semi-fluorinated alkanes selected from F4H5, F4H6, F4H8, F6H4, F6H6, F6H8, and F6H10.

13. The composition according to claim 1 , wherein the antigen-binding polypeptide or protein is not dissolved in the SFA.

14. The composition according to claim 1 , wherein the composition is formulated for topical administration to the eye, ear or nose or for parenteral administration.

Assignees

• Novaliq Gmbh

Inventors

• Günther Bernhard
• Scherer Dieter
• Pettigrew Anthony
• Graf Gesche

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P9/14

  Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers · CPC title

• A61P35/00

  Antineoplastic agents · CPC title