# US 2014/0193899 A1 · Monoclonal antibodies to fibroblast growth factor receptor 2

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- Number: US 2014/0193899 A1
- Document ID: US20140193899A1
- Status: Published application
- Kind: A1
- Application number: 14/071,520
- Filed: 2013-11-04
- Published: 2014-07-10
- Earliest claimed: 2008-11-07
- Assignees: Galaxy Biotech, LLC
- Applicants: Galaxy Biotech, LLC
- Inventors: Kyung Jin Kim; Wei-meng Zhao; Hangil Park; Maximiliano Vasquez
- Web page: https://patentgrep.com/patent/US20140193899A1

## CPC

- C07K 16/2863: {against receptors for growth factors, growth regulators}
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 35/00: Antineoplastic agents
- G01N 33/5759: {involving compounds localised on the membrane of tumour or cancer cells}
- A61K 2039/505: {comprising antibodies}
- 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 2317/51: Complete heavy chain or Fd fragment, i.e. VH + CH1
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- G01N 2333/71: for growth factors; for growth regulators
- 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
- 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)
- 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

The present invention is directed toward a monoclonal antibody to fibroblast growth factor receptor 2, a pharmaceutical composition comprising same, and methods of treatment comprising administering such a pharmaceutical composition to a patient.

## Claims

### Claim 1

Synthetic genes encoding heavy and light chain variable regions of a humanized or human monoclonal antibody (mAb) which binds to FGFR2IIIb but not FGFR2IIIc and inhibits growth of a human tumor xenograft in a mouse.

### Claim at position 2

2-4. (canceled)

### Claim 5 (depends on 1)

The synthetic genes of claim 1, wherein the mAb is a Fab or F(ab′)2 fragment or single-chain antibody.

### Claim at position 4

6-7. (canceled)

### Claim 8

Synthetic genes encoding a monoclonal antibody (mAb) that competes for binding to FGFR2 with an antibody selected from the group of GAL-FR21, GAL-FR22 and GAL-FR23.

### Claim 9 (depends on 8)

The synthetic genes of claim 8, wherein the mAb inhibits growth of a SNU-16 human tumor xenograft in a mouse.

### Claim 10 (depends on 8)

The synthetic genes of claim 8, wherein the mAb is chimeric or humanized.

### Claim 11 (depends on 8)

The synthetic genes of claim 8, wherein the mAb is a humanized GAL-FR21 or GAL-FR22 mAb.

### Claim 12 (depends on 8)

The synthetic genes of claim 8, wherein the mAb is human.

### Claim at position 10

13-15. (canceled)

### Claim 16

Synthetic genes encoding heavy and light chain variable region of a humanized antibody comprising a humanized light chain comprising CDRs from the sequence in FIG. 13A (GAL-FR21) and a humanized heavy chain comprising CDRs from the sequence of FIG. 13B (GAL-FR21), or comprising a humanized light chain comprising CDRs from the sequence in FIG. 16A (GAL-FR22) and a humanized heavy chain comprising CDRs from the sequence of FIG. 16B (GAL-FR22).

### Claim 17 (depends on 16)

The synthetic genes of claim 16, wherein the humanized antibody, comprises the three light chain CDRs shown in FIG. 13A (GAL-FR21) and the three heavy chain CDRs shown in FIG. 13B (GAL-FR21), or comprising the three light chain CDRs shown in FIG. 16A (GAL-FR22) and the three heavy chain CDRs shown in FIG. 16B (GAL-FR22).

### Claim 18 (depends on 17)

The synthetic genes of claim 17 wherein the light chain variable region has at least 95% sequence identity to the sequence shown in FIG. 13A (HuGAL-FR21) and the heavy chain variable region has at least 95% sequence identity to the sequence shown in FIG. 13B (HuGAL-FR21).

### Claim 19 (depends on 18)

The synthetic genes of claim 18, wherein residues H27, H28, H30, H48, and H67 by Kabat numbering are occupied by the residue occupying the corresponding position of the heavy chain shown in FIG. 13B (GAL-FR21).

### Claim 20 (depends on 19)

The synthetic genes of claim 19 wherein the light chain variable region has the sequence shown in FIG. 13A (HuGAL-FR21) and the heavy chain variable region has the sequence shown in FIG. 13B (HuGAL-FR21).

### Claim 21 (depends on 1)

The synthetic genes of claim 1 as components of an expression vector than expresses the variable regions linked to constant regions.

### Claim 22 (depends on 8)

The synthetic genes of claim 8 as components of an expression vector that expresses the variable regions linked to constant regions.

### Claim 23 (depends on 16)

The synthetic genes of claim 16 as components of an expression vector that expresses the variable regions linked to constant regions.