US 10,894,089 B2 · Long-acting insulin or insulin analogue conjugate

Abstract

The present invention relates to insulin and/or an insulin analogue conjugate, and a use thereof, wherein the insulin and/or insulin analogue have improved in vivo durability and stability by linking the same with an Fc region of immunoglobulin. The insulin and/or an insulin analogue conjugate of the present invention show an in vivo activity similar to that of insulin. In addition, the insulin and/or insulin analogue conjugate of the present invention are long-acting formulations of insulin and/or the analogue thereof, in which serum half-life is remarkably increased, and therefore, the present invention provides remarkable insulin and/or an insulin analogue conjugate, which do not induce hypoglycemia, a drawback of insulin treatment.

Claims15

Dependent claims

A long-acting conjugate of the following Formula 1:

X-La-F1:Y-La-F2, Formula 1
wherein, in the above Formula,
X is a wild-type insulin A-chain or analogue thereof;
L is a linker;
a is 0 or a natural number, with the proviso that each L is independent from each other when a is 2 or greater;
:
is a chemical bond between F1 and F2;
Y is a wild-type insulin B-chain or analogue thereof;
and
F1 and F2 each comprise a single chain polypeptide of immunoglobulin constant region and have an FcRn-binding site,
wherein the chemical bond between F1 and F2 is a disulfide bond, and the long-acting conjugate forms a heterodimer via the disulfide bond, and
wherein F1 is conjugated to carboxyl end of X via the linker L, and F2 is conjugated to carboxyl end of Y via the linker L.

9 more elements

Dependencies are inferred from the claim text.

Facts

Application

15/551,489Filed 17 Feb 2016

Priority

KR 10-2015-002409117 Feb 2015

Published

US 2018/0161448 A114 Jun 2018

Granted

19 Jan 2021

Term ends

Not estimatedThe source records don’t support an estimate.

Classification20 codes

A61K 47/6811
Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates: the drug being a protein or peptide, e.g. transferrin or…
A61K 38/28
Hormones: insulins
A61K 47/50
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents…: the…
A61K 47/60
Obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes: the organic…

Long-acting insulin or insulin analogue conjugate

Life of this patent

Long-acting insulin or insulin analogue conjugate

Life of this patent

Abstract

Claims15