# US 12,215,168 B2 · Anti-A2AP antibodies and uses thereof

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- Number: US 12,215,168 B2
- Document ID: US12215168B2
- Status: Granted
- Kind: B2
- Application number: 18/525,736
- Filed: 2023-11-30
- Published: 2024-05-23
- Granted: 2025-02-04
- Earliest claimed: 2020-09-15
- Assignees: Bayer Aktiengesellschaft
- Applicants: Bayer Aktiengesellschaft
- Inventors: Stefan Heitmeier; Julia Glunz; Melanie Fischer; Cindy Schulenburg; Hannah Jörißen; Christoph Thiel; Andreas Wilmen; Ernst Weber
- Web page: https://patentgrep.com/patent/US12215168B2

## CPC

- C07K 16/38: against protease inhibitors of peptide structure
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 11/00: Drugs for disorders of the respiratory system
- C12N 15/63: Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
- A61K 2039/505: {comprising antibodies}
- 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 2317/52: Constant or Fc region; Isotype
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/622: Single chain antibody (scFv)
- 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: 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 relates to an isolated antibody or antigen-binding fragment thereof that binds to human A2AP. The isolated antibody or antigen-binding fragment according to the present invention i) cross-reacts with rabbit and/or cynomolgus A2AP, ii) does not inhibit human plasmin activity, and iii) increases plasmin mediated clot lysis in the presence of A2AP.

## Claims

### Claim 1

An isolated antibody or antigen-binding fragment thereof capable of binding to alpha 2 antiplasmin (A2AP) and inhibiting the activity of A2AP, comprising:
a heavy chain antigen-binding region that comprises an H-CDR1 comprising SEQ ID NO: 6, an H-CDR2 comprising SEQ ID NO: 8, and an H-CDR3 comprising SEQ ID NO: 13 and a light chain antigen-binding region that comprises an L-CDR1 comprising SEQ ID NO: 9, an L-CDR2 comprising SEQ ID NO: 10, and an L-CDR3 comprising SEQ ID NO:18.

### Claim 2 (depends on 1)

The isolated antibody or antigen-binding fragment according to claim 1, comprising a variable heavy chain domain comprising SEQ ID NO: 32 and a variable light chain domain comprising SEQ ID NO: 38.

### Claim 3 (depends on 2)

The isolated antibody or antigen-binding fragment according to claim 2, which is a human, humanized or chimeric antibody or antigen-binding fragment.

### Claim 4 (depends on 1)

The isolated antibody or antigen-binding fragment according to claim 1, wherein the isolated antibody is an IgG antibody.

### Claim 5 (depends on 4)

The isolated antibody or antigen-binding fragment according to claim 4, comprising a heavy chain comprising SEQ ID NO: 55 and a light chain comprising SEQ ID NO: 57.

### Claim 6 (depends on 5)

The isolated antibody or antigen-binding fragment according to claim 5, wherein the IgG antibody is an IgG1 or an IgG4 antibody.

### Claim 7 (depends on 5)

The isolated antibody or antigen-binding fragment according to claim 5, which is a human, humanized or chimeric antibody or antigen-binding fragment.

### Claim 8 (depends on 4)

The isolated antibody or antigen-binding fragment according to claim 4, wherein the IgG antibody is an IgG1 or an IgG4 antibody.

### Claim 9 (depends on 4)

The isolated antibody or antigen-binding fragment according to claim 4, wherein the antigen-binding fragment is selected from the group consisting of an scFv, Fab, Fab′ fragment, and a F(ab′)2 fragment.

### Claim 10 (depends on 1)

The isolated antibody or antigen-binding fragment according to claim 1, which is an scFv, Fab, Fab′ fragment or a F(ab′)2 fragment.

### Claim 11 (depends on 1)

The isolated antibody or antigen-binding fragment according to claim 1, which is a monoclonal antibody or antigen-binding fragment.

### Claim 12 (depends on 1)

The isolated antibody or antigen-binding fragment according to claim 1, which is a human, humanized or chimeric antibody or antigen-binding fragment.

### Claim 13 (depends on 1)

An antibody conjugate, comprising the isolated antibody or antigen binding fragment according to claim 1.

### Claim 14 (depends on 1)

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

### Claim 15 (depends on 1)

A kit comprising the isolated antibody or antigen-binding fragment according to claim 1, a conjugate thereof, or a pharmaceutical composition comprising the isolated antibody or antigen-binding fragment, the conjugate, or the pharmaceutical composition, and instructions for use.