# US 11,111,313 B2 · Anti-PCSK9 antibodies

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- Number: US 11,111,313 B2
- Document ID: US11111313B2
- Status: Granted
- Kind: B2
- Application number: 16/334,767
- Filed: 2017-09-12
- Published: 2019-08-01
- Granted: 2021-09-07
- Earliest claimed: 2016-09-20
- Assignees: Wuxi Biologics Ireland Limited
- Applicants: WuXi Biologies Ireland Limited
- Inventors: Jieying Liu; Jing Li
- Web page: https://patentgrep.com/patent/US11111313B2

## CPC

- C07K 16/40: against enzymes
- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/06: Antihyperlipidemics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 37/04: Immunostimulants
- C12N 9/6454: {Dibasic site splicing serine proteases, e.g. kexin (3.4.21.61); furin (3.4.21.75) and other proprotein convertases}
- A61K 2039/505: {comprising antibodies}
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- C07K 2317/21: from primates, e.g. man
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/33: Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- C07K 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## 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).

## Claims

### Claim 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).

### Claim 2 (depends on 1)

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.

### Claim 3 (depends on 1)

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

### Claim 4 (depends on 1)

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.

### Claim 5 (depends on 1)

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

### Claim 6 (depends on 1)

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

### Claim 7 (depends on 1)

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

### Claim 8 (depends on 1)

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

### Claim 9 (depends on 1)

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

### Claim 10 (depends on 9)

A vector comprising the isolated polynucleotide of claim 9.

### Claim 11 (depends on 10)

An isolated host cell comprising the vector of claim 10.

### Claim 12 (depends on 11)

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.