Stabilized antibody compositions

Patent metadata

Field	Value
Publication number	US-2016159902-A1
Application number	US-201414907254-A
Country	US
Kind code	A1
Filing date	Jul 23, 2014
Priority date	Jul 23, 2013
Publication date	Jun 9, 2016
Grant date	—

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

1 . 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.

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 is substantially free of water.

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 . A method for treating or preventing a disease or condition in a patient in need thereof, comprising the step of administering to the patient an effective amount of a composition according to claim 1 .

11 . The method of claim 10 , wherein the composition is administered by subcutaneous, dermal, intramuscular, or locoregional injection.

12 . A method of stabilizing an antigen-binding polypeptide or protein, comprising the step of mixing the antigen-binding polypeptide or protein with a liquid vehicle comprising 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, such as to form a suspension or a dispersion.

13 . The method of claim 12 , wherein the antigen-binding polypeptide or protein retains at least 85% of initial antigen-binding activity during storage of 6 months at a temperature between RT to 40° C.

14 . The method of claim 10 , wherein the disease or condition is cancer or an autoimmune disease.

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

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

17 . The composition of claim 16 , wherein the composition is substantially free of water.

18 . The method of claim 12 , wherein the antigen-binding polypeptide or protein is a monoclonal antibody, a polyclonal antibody, an antibody fragment, a fusion protein comprising an antibody fragment, an antibody-drug conjugate, or any combination thereof.

19 . The method of claim 18 , wherein the semifluorinated alkane is selected from F4H5, F4H6, F4H8, F6H4, F6H6, F6H8, and F6H10.

20 . The method of claim 19 , wherein the antigen-binding polypeptide or protein is at a concentration of at least 0.5 mg/mL.

Assignees

• Novaliq Gmbh

Inventors

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

Classifications

• A61P9/14

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

• A61P37/06

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

• A61P35/00

  Antineoplastic agents · CPC title

• A61P43/00

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

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title