# US 10,246,507 B2 · Polypeptide, anti-VEGF antibody, and anti-c-Met/anti-VEGF bispecific antibodies comprising the same

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- Number: US 10,246,507 B2
- Document ID: US10246507B2
- Status: Granted
- Kind: B2
- Application number: 14/869,636
- Filed: 2015-09-29
- Published: 2016-03-31
- Granted: 2019-04-02
- Earliest claimed: 2014-09-29
- Assignees: Samsung Electronics Co., Ltd.
- Applicants: Samsung Electronics Co., Ltd.
- Inventors: Seung Hyun Lee; Soo Yeon Jung; Bo Gyou Kim; Seung Ja Oh; Ji Min Lee
- Web page: https://patentgrep.com/patent/US10246507B2

## CPC

- C07K 16/22: against growth factors {; against growth regulators}
- A61P 35/00: Antineoplastic agents
- C07K 16/2863: {against receptors for growth factors, growth regulators}
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 39/39558: {against tumor tissues, cells, antigens}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/31: multispecific
- C07K 2317/622: Single chain antibody (scFv)
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- 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 2319/74: containing a fusion for binding to a cell surface receptor
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)

## Abstract

A polypeptide, an anti-VEGF antibody and an anti-c-Met/anti-VEGF bispecific antibody, which includes the polypeptide, a pharmaceutical composition including the antibody, and a method of treating cancer using the antibody.

## Claims

### Claim 1

An anti-VEGF antibody or an antigen-binding fragment thereof comprising
a CDR-H1 comprising the amino acid sequence of SEQ ID NO: 110, a CDR-H2 comprising the amino acid sequence of SEQ ID NO: 121, a CDR-H3 comprising the amino acid sequence of SEQ ID NO: 129, a CDR-L1 comprising the amino acid sequence of SEQ ID NO: 137, a CDR-L2 comprising the amino acid sequence of SEQ ID NO: 145, and a CDR-L3 comprising the amino acid sequence of SEQ ID NO: 151.

### Claim 2 (depends on 1)

The anti-VEGF antibody or an anti-VEGF antigen-binding fragment of claim 1, wherein the anti-VEGF antibody or the anti-VEGF antigen-binding fragment comprises
a heavy chain variable region comprising the amino acid sequence of SEQ ID NO: 159 and a light chain variable region comprising the amino acid sequence of SEQ ID NO: 167.

### Claim 3 (depends on 1)

The anti-VEGF antibody or an antigen-binding fragment thereof of claim 1, which is an anti-VEGF scFv comprising SEQ ID NO: 175.

### Claim 4 (depends on 1)

A pharmaceutical composition comprising the anti-VEGF antibody or an antigen-binding fragment thereof of claim 1, and a pharmaceutically acceptable carrier.

### Claim 5 (depends on 1)

A method of treating a cancer in a subject, comprising administering a therapeutically effective amount of the anti-VEGF antibody or the antigen-binding fragment thereof of claim 1 to the subject to inhibit cancer cell growth, thereby treating the cancer.

### Claim 6 (depends on 1)

The anti-VEGF antibody or an antigen-binding fragment thereof of claim 1, which is an scFv, (scFv)2, scFvFc, Fab, or Fab′.

### Claim 7

An anti-c-Met/anti-VEGF bispecific antibody comprising an anti-c-Met antibody that comprises two heavy chains and two light chains and an scFv of the anti-VEGF antibody linked to the C-terminus of each anti-c-Met antibody heavy chain, wherein the anti-c-Met heavy chain comprises
a CDR-H1 comprising the amino acid sequence of SEQ ID NO: 1, a CDR-H2 comprising the amino acid sequence of SEQ ID NO: 2, a CDR-H3 comprising the amino acid sequence of SEQ ID NO: 3;
the anti-c-Met light chain comprises a CDR-L1 comprising the amino acid sequence of SEQ ID NO: 10, a CDR-L2 comprising the amino acid sequence of SEQ ID NO: 11, and a CDR-L3 comprising the amino acid sequence of SEQ ID NO: 13;
and the anti-VEGF scFv comprises a CDR-H1 comprising the amino acid sequence of SEQ ID NO: 110, a CDR-H2 comprising the amino acid sequence of SEQ ID NO: 121, a CDR-H3 comprising the amino acid sequence of SEQ ID NO: 129, a CDR-L1 comprising the amino acid sequence of SEQ ID NO: 137, a CDR-L2 comprising the amino acid sequence of SEQ ID NO: 145, and a CDR-L3 comprising the amino acid sequence of SEQ ID NO: 151.

### Claim 8 (depends on 7)

The anti-c-Met/anti-VEGF bispecific antibody of claim 7, wherein the anti-c-Met heavy chain comprises
SEQ ID NO: 17, and
the anti-c-Met light chain comprises SEQ ID NO: 18.

### Claim 9 (depends on 7)

An anti-c-Met/anti-VEGF bispecific antibody of claim 7, wherein the anti-c-Met heavy chain comprises
SEQ ID NO: 62, the 18th to 462nd positions of SEQ ID NO: 62, SEQ ID NO: 64, the 18th to 461st positions of SEQ ID NO: 64, SEQ ID NO: 66, or the 18th to 460th positions of SEQ ID NO: 66; and
the anti-c-Met light chain comprises SEQ ID NO: 68, the 21st to 240th positions of SEQ ID NO: 68, SEQ ID NO: 70, or the 21st to 240th positions of SEQ ID NO: 70.

### Claim 10 (depends on 7)

A pharmaceutical composition comprising the anti-c-Met/anti-VEGF bispecific antibody of claim 7, and a pharmaceutically acceptable carrier.

### Claim 11 (depends on 7)

A method of treating a cancer in a subject, comprising administering a therapeutically effective amount of-the anti-c-Met/anti-VEGF bispecific antibody of claim 7 to the subject to inhibit cancer cell growth, thereby treating the cancer.

### Claim 12 (depends on 7)

The anti-c-Met/anti-VEGF bispecific antibody of claim 7, wherein the anti-VEGF scFv comprises SEQ ID NO: 175.