Anti-PCSK9 antibodies

Patent metadata

Field	Value
Publication number	US-11111313-B2
Application number	US-201716334767-A
Country	US
Kind code	B2
Filing date	Sep 12, 2017
Priority date	Sep 20, 2016
Publication date	Sep 7, 2021
Grant date	Sep 7, 2021

Abstract

The present disclosure provides monoclonal antibodies against Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9), which can block the binding of PCSK9 to low-density lipoprotein (LDL) receptor, and therefore lower the level low-density lipoprotein cholesterol (LDL-C). The antibodies of disclosure provide very potent agents for the treatment of multiple Cardiovascular diseases (CVDs).

First claim

What is claimed is:

1. An isolated antibody or an antigen binding fragment thereof, comprising: a heavy chain variable region comprising an HCDR1 comprising SEQ ID NO: 13, an HCDR2 comprising SEQ ID NO: 15, and an HCDR3 comprising SEQ ID NO: 17; and a light chain variable region comprising an LCDR1 comprising SEQ ID NO: 19, an LCDR2 comprising SEQ ID NO: 21, and an LCDR3 comprising SEQ ID NO: 23, wherein the isolated antibody or an antigen binding fragment thereof specifically binds to Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9).

2. The antibody or an antigen binding fragment thereof of claim 1 , comprising:
a heavy chain variable region comprising SEQ ID NO: 77 and a light chain variable region comprising SEQ ID NO: 79.

3. The antibody or an antigen binding fragment thereof of claim 1 , which is a fully human monoclonal antibody.

4. The antibody or antigen-binding fragment thereof of claim 1 , which is a camelized single domain antibody, a diabody, a scFv, an scFv dimer, a BsFv, a dsFv, a (dsFv)2, a dsFv-dsFv′, an Fv fragment, a Fab, a Fab′, a F(ab′)2, a disulfide stabilized diabody (ds diabody), a nanobody, a domain antibody, or a bivalent domain antibody.

5. The antibody or antigen-binding fragment thereof of claim 1 , further comprising an immunoglobulin constant region.

6. The antibody or antigen-binding fragment thereof of claim 1 , further comprising a conjugate.

7. A pharmaceutical composition comprising the antibody or antigen-binding fragment thereof of claim 1 and one or more pharmaceutically acceptable carriers.

8. A kit comprising the antibody or antigen-binding fragment thereof of claim 1 .

9. An isolated polynucleotide encoding the antibody or an antigen binding fragment thereof of claim 1 .

10. A vector comprising the isolated polynucleotide of claim 9 .

11. An isolated host cell comprising the vector of claim 10 .

12. A method of expressing an antibody or antigen-binding fragment thereof, comprising culturing the host cell of claim 11 under conditions at which the polynucleotide is expressed.

Assignees

• Wuxi Biologies Ireland Ltd
• Wuxi Biologics Ireland Ltd

Inventors

• Liu Jieying
• Li Jing

Classifications

• C07K2317/94

  Stability, e.g. half-life, pH, temperature or enzyme-resistance · CPC title

• A61P3/06

  Antihyperlipidemics · CPC title

• C07K2317/33

  Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity · CPC title

• C07K16/40 Primary

  against enzymes · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title