# US 11,306,152 B2 · Anti-podoplanin antibody

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- Number: US 11,306,152 B2
- Document ID: US11306152B2
- Status: Granted
- Kind: B2
- Application number: 16/498,411
- Filed: 2017-03-30
- Published: 2021-04-22
- Granted: 2022-04-19
- Earliest claimed: 2017-03-30
- Assignees: Tohoku University; Zenogen Pharma Co., Ltd.
- Applicants: Tohoku University; Zenogen Pharma Co., Ltd.
- Inventors: Yukinari Kato; Mika Kato; Shinji Yamada; Satoshi Ogasawara; Takuro Nakamura
- Web page: https://patentgrep.com/patent/US11306152B2

## CPC

- C07K 16/28: against receptors, cell surface antigens or cell surface determinants
- C07K 16/30: from tumour cells
- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 35/00: Antineoplastic agents
- C07K 7/06: having 5 to 11 amino acids
- C07K 14/745: Blood coagulation or fibrinolysis factors
- C07K 16/3092: {against tumour-associated mucins}
- C07K 16/36: against blood coagulation factors
- C12N 5/10: Cells modified by introduction of foreign genetic material
- C12N 15/09: Recombinant DNA-technology
- A61K 2039/505: {comprising antibodies}
- 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 2317/565: Complementarity determining region [CDR]
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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 invention provides a cancer cell-specific anti-podoplanin antibody or an antigen-binding fragment thereof having an epitope in a Thr85-containing region of an amino acid sequence of human podoplanin represented by SEQ ID NO: 1, the Thr85 having a sialylated O-glycan added thereto.

## Claims

### Claim 1

A cancer cell-specific anti-podoplanin antibody or antigen-binding fragment thereof, comprising the following six CDR amino acid sequences:
heavy chain CDR1:
(SEQ ID NO: 2)
GFTFSNAAMY
heavy chain CDR2:
(SEQ ID NO: 3)
RIRSKPNNYATYYTDSVKG
heavy chain CDR3:
(SEQ ID NO: 4)
TVGGNNYAAAY
light chain CDR1:
(SEQ ID NO: 5)
RSSQSLVHSNGNTYLE
light chain CDR2:
(SEQ ID NO: 6)
KVSNRFS
light chain CDR3:
(SEQ ID NO: 7)
FQVTHDPFT.

### Claim 2 (depends on 1)

The cancer cell-specific anti-podoplanin antibody or antigen-binding fragment thereof according to claim 1, having one or more N-glycans bound to an Fc region thereof and having no fucose bound to N-acetylglucosamine at a reducing end of the N-glycan(s).

### Claim 3 (depends on 1)

A nucleic acid encoding the cancer cell-specific anti-podoplanin antibody or antigen-binding fragment thereof according to claim 1.

### Claim 4 (depends on 3)

An expression vector, comprising the nucleic acid as claimed in claim 3.

### Claim 5 (depends on 4)

A transformant, comprising the expression vector as claimed in claim 4.

### Claim 6 (depends on 1)

A pharmaceutical composition, comprising, as an effective ingredient thereof, the cancer cell-specific anti-podoplanin antibody or antigen-binding fragment thereof as claimed in claim 1.

### Claim 7 (depends on 1)

A pharmaceutical composition, comprising, as an effective ingredient thereof, the cancer cell-specific anti-podoplanin antibody or antigen-binding fragment thereof as claimed in claim 1 to which a substance having an anti-cancer activity has been bound.

### Claim 8 (depends on 6)

A method of treating cancer, wherein said cancer expresses podoplanin, in a subject, which comprises administering to the subject the pharmaceutical composition according to claim 6.

### Claim 9 (depends on 7)

A method of treating cancer, wherein said cancer expresses podoplanin, in a subject, which comprises administering to the subject the pharmaceutical composition according to claim 7.

### Claim 10

A cancer cell-specific anti-podoplanin antibody or antigen-binding fragment thereof, comprising the following six CDR amino acid sequences:
heavy chain CDR1:
(SEQ ID NO: 2)
GFTFSNAAMY,
heavy chain CDR2:
(SEQ ID NO: 3)
RIRSKPNNYATYYTDSVKG,
heavy chain CDR3:
(SEQ ID NO: 4)
TVGGNNYAAAY,
light chain CDR1:
(SEQ ID NO: 5)
RSSQSLVHSNGNTYLE,
light chain CDR2:
(SEQ ID NO: 6)
KVSNRFS,
and
light chain CDR3:
(SEQ ID NO: 7)
FQVTHDPFT;
wherein the heavy chain has an amino acid sequence that:
is represented by SEQ ID NO: 8 or 10;
is obtained by addition, substitution, or deletion of one to several amino acids from the amino acid sequence represented by SEQ ID NO: 8 or 10;
has 80% or more identity to the amino acid sequence represented by SEQ ID NO: 8 or 10; and
wherein the light chain has an amino acid sequence that:
is represented by SEQ ID NO: 9 or 11;
is obtained by addition, substitution or deletion of one to several amino acids from the amino acid sequence represented by SEQ ID NO: 9 or 11, or
has 80% or more identity to the amino acid sequence represented by SEQ ID NO: 9 or 11.

### Claim 11 (depends on 10)

The cancer cell-specific anti-podoplanin antibody or antigen-binding fragment thereof according to claim 10, having one or more N-glycans bound to an Fc region thereof and having no fucose bound to N-acetylglucosamine at a reducing end of the N-glycan(s).

### Claim 12 (depends on 10)

A nucleic acid encoding the cancer cell-specific anti-podoplanin antibody or antigen-binding fragment thereof according to claim 10.

### Claim 13 (depends on 11)

An expression vector, comprising the nucleic acid as claimed in claim 11.

### Claim 14 (depends on 13)

A transformant, comprising the expression vector as claimed in claim 13.

### Claim 15 (depends on 10)

A pharmaceutical composition, comprising, as an effective ingredient thereof, the cancer cell-specific anti-podoplanin antibody or antigen-binding fragment thereof as claimed in claim 10.

### Claim 16 (depends on 10)

A pharmaceutical composition, comprising, as an effective ingredient thereof, the cancer cell-specific anti-podoplanin antibody or antigen-binding fragment thereof as claimed in claim 10 to which a substance having an anti-cancer activity has been bound.

### Claim 17 (depends on 15)

A method of treating cancer, wherein said cancer expresses podoplanin, in a subject, which comprises administering to the subject the pharmaceutical composition according to claim 15.

### Claim 18 (depends on 16)

A method of treating cancer, wherein said cancer expresses podoplanin, in a subject, which comprises administering to the subject the pharmaceutical composition according to claim 16.