PHARMACEUTICAL COMPOSITIONS CONTAINING sc(Fv)2

Patent metadata

Field	Value
Publication number	US-2016168259-A1
Application number	US-201514967475-A
Country	US
Kind code	A1
Filing date	Dec 14, 2015
Priority date	Jun 10, 2005
Publication date	Jun 16, 2016
Grant date	—

Abstract

The present inventor discovered stabilizing agents/stabilizing conditions for suppressing isomerization reactions of sc(Fv)2. It was also discovered that the above-mentioned isomerization reactions can be suppressed through use of freeze-dried formulations. As disclosed herein, by applying the discovered stabilizing agents/stabilizing conditions or the freeze-dried formulation, the isomerization reaction of an sc(Fv)2-type molecule from the bivalent scFv type to the single chain diabody type, and/or the isomerization reaction from a single chain diabody type to a bivalent scFv type can be suppressed in both directions or one direction.

First claim

1 .- 12 . (canceled)

13 . A pharmaceutical sc(Fv)2 composition comprising a specific conformational isomer of sc(Fv)2, the specific conformational isomer of sc(Fv)2 being either a bivalent scFv-type sc(Fv)2 or a single chain diabody type sc(Fv)2, wherein at least 80% of the sc(Fv)2 in the composition is in the form of the specific conformational isomer.

14 . The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition comprises at least one substance selected from the group consisting of a salt, an amino sugar, a sugar alcohol, an amino acid, and a pH adjusting agent.

15 . The pharmaceutical composition of claim 14 , wherein the substance is a salt selected from the group consisting of sodium chloride and magnesium chloride.

16 . The pharmaceutical composition of claim 14 , wherein the substance is the amino sugar 1-deoxy-1-methylamino-D-glucitol.

17 . The pharmaceutical composition of claim 14 , wherein the substance is the sugar alcohol mannitol.

18 . The pharmaceutical composition of claim 14 , wherein the substance is the amino acid lysine.

19 . The pharmaceutical composition of claim 14 , wherein the substance is a pH adjusting agent selected from the group consisting of a sodium citrate buffer and histidine hydrochloride.

20 . The pharmaceutical composition of claim 13 , wherein the composition has a pH of 4.5 to 9.0.

21 . The pharmaceutical composition of claim 13 , wherein the composition has a pH of 6.0 to 9.0.

22 . The pharmaceutical composition of claim 13 , wherein the composition has a salt concentration of 50 mM to 1000 mM.

23 . The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition is in the form of a freeze-dried formulation.

24 . The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition is in the form of a spray-dried formulation.

25 . The pharmaceutical composition of claim 13 , wherein the specific conformational isomer constitutes 90% or more of the sc(Fv)2 present in the pharmaceutical sc(Fv)2 composition.

26 . The pharmaceutical composition of claim 13 , wherein the specific conformational isomer constitutes 95% or more of the sc(Fv)2 present in the pharmaceutical sc(Fv)2 composition.

27 . The pharmaceutical composition of claim 13 , wherein the specific conformational isomer is a bivalent scFv-type sc(Fv)2.

28 . The pharmaceutical composition of claim 13 , wherein the specific conformational isomer is a single chain diabody type sc(Fv)2.

Assignees

• Chugai Pharmaceutical Co Ltd

Inventors

• Igawa Tomoyuki

Classifications

• A61P43/00

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

• A61K39/39591

  Stabilisation, fragmentation · CPC title

• C07K2317/622

  Single chain antibody (scFv) · CPC title

• C07K16/2869

  against hormone receptors (for antibodies against neuromediator receptors C07K16/286) · CPC title

• C07K16/2866

  against receptors for cytokines, lymphokines, interferons · CPC title