# US 10,246,517 B2 · Antibody binding to carbonic anhydrase and use thereof

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- Number: US 10,246,517 B2
- Document ID: US10246517B2
- Status: Granted
- Kind: B2
- Application number: 15/344,764
- Filed: 2016-11-07
- Published: 2017-11-30
- Granted: 2019-04-02
- Earliest claimed: 2016-05-30
- Assignees: Aprogen Kic Inc.
- Applicants: Aprogen KIC Inc.
- Inventors: Yoo Ri Moon; Gil Yong Ji
- Web page: https://patentgrep.com/patent/US10246517B2

## CPC

- C07K 16/3015: {Breast}
- A61K 33/24: Heavy metals; Compounds thereof
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/6855: {the tumour determinant being from breast cancer cell}
- A61K 47/6871: {the antibody targeting an enzyme}
- A61P 35/00: Antineoplastic agents
- C07K 16/30: from tumour cells
- C07K 16/3023: {Lung}
- C07K 16/40: against enzymes
- G01N 33/57515: of the breast
- G01N 33/5758: {involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/14: Specific host cells or culture conditions, e.g. components, pH or temperature
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/34: Identification of a linear epitope shorter than 20 amino acid residues or of a conformational epitope defined by amino acid residues
- C07K 2317/41: Glycosylation, sialylation, or fucosylation
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- C07K 2317/732: Antibody-dependent cellular cytotoxicity [ADCC]
- C07K 2317/734: Complement-dependent cytotoxicity [CDC]
- C07K 2317/90: characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
- G01N 2333/988: Lyases (4.), e.g. aldolases, heparinase, enolases, fumarase
- 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
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

Provided is an antibody that recognizes and binds to carbonic anhydrase or antigen-binding fragment, a nucleic acid molecule coding for the antibody or antigen-binding fragment, a vector carrying the nucleic acid molecule, a host cell including the nucleic acid molecule or the vector, and use of the antibody or antigen-binding fragment thereof in the alleviation, prevention, treatment or diagnosis of solid cancers.

## Claims

### Claim 1

An antibody or an antigen-binding fragment thereof, binding to carbonic anhydrase, wherein the antibody or antigen-binding fragment thereof comprises a CDR-H1 comprising SEQ ID NO: 14; a CDR-H2 comprising SEQ ID NO: 15; a CDR-H3 comprising SEQ ID NO: 16; a CDR-L1 comprising SEQ ID NO: 17; a CDR-L2 comprising SEQ ID NO: 18; and a CDR-L3 comprising SEQ ID NO: 19.

### Claim 2 (depends on 1)

The antibody or antigen-binding fragment thereof according to claim 1, wherein the antibody or antigen-binding fragment thereof binds to an epitope which is a peptide consisting of 14 to 93 consecutive amino acids containing the amino acid sequence of SEQ ID NO: 3 among amino acid sequence of SEQ ID NO: 5.

### Claim 3 (depends on 2)

The antibody or antigen-binding fragment thereof according to claim 2, wherein the epitope is a peptide consisting of 19 to 93 consecutive amino acids containing the amino acid sequence of SEQ ID NO: 4 among amino acid sequence of SEQ ID NO: 5.

### Claim 4 (depends on 3)

The antibody or antigen-binding fragment thereof according to claim 3, wherein the epitope is a peptide consisting of 14 to 19 consecutive amino acids containing the amino acid sequence of SEQ ID NO: 3 among amino acid sequence of SEQ ID NO: 4.

### Claim 5 (depends on 3)

The antibody or antigen-binding fragment thereof according to claim 3, wherein the epitope is a peptide consisting of 7 to 93 consecutive amino acids containing the amino acid sequence of SEQ ID NOs: 3 or 4.

### Claim 6 (depends on 1)

The antibody or antigen-binding fragment thereof according to claim 1, wherein the antibody or antigen binding fragment comprises:
a heavy chain variable region comprising SEQ ID NO: 20; and
a light chain variable region comprising SEQ ID NO: 21.

### Claim 7 (depends on 1)

The antibody or antigen-binding fragment thereof according to claim 1, wherein the antibody or antigen-binding fragment thereof is coupled to a labeling agent, a toxin, or an anti-tumor drug.

### Claim 8 (depends on 7)

The antibody or antigen-binding fragment thereof according to claim 7, wherein the labeling agent is selected from the group consisting of a radioisotope, a hapten or a fluorescent, a chromogen, and a dye.

### Claim 9 (depends on 7)

The antibody or antigen-binding fragment thereof according to claim 7, wherein the toxin is selected from the group consisting of a radioisotope, a small molecule, a peptide, and a protein.

### Claim 10 (depends on 7)

The antibody or antigen-binding fragment thereof according to claim 7, wherein the antibody or antigen-binding fragment thereof is coupled with the toxin to form a fusion protein.

### Claim 11 (depends on 7)

The antibody or antigen-binding fragment thereof according to claim 7, wherein the antibody or antigen-binding fragment thereof is partially or completely defucosylated.

### Claim 12 (depends on 1)

A pharmaceutical composition, comprising the antibody or antigen-binding fragment thereof according to claim 1.

### Claim 13 (depends on 1)

A composition for detecting a solid cancer that comprises the antibody or antigen-binding fragment thereof according to claim 1 and that the a sample is determined as the solid cancer showing a positive reaction to the antibody or antigen-binding fragment thereof.

### Claim 14 (depends on 13)

The composition for detecting a solid cancer according to claim 13, wherein the antibody or the antigen-binding fragment is coupled to labeling agents.

### Claim 15 (depends on 14)

The composition for detecting a solid cancer according to claim 14, wherein the solid cancer is breast cancer, lung cancer, colorectal cancer, stomach cancer, prostate cancer, and liver cancer.

### Claim 16 (depends on 15)

The composition for detecting a solid cancer according to claim 15, wherein the positive reaction is detected by enzyme reaction, fluorescence, luminescence or radiation.