# US 10,246,502 B2 · IL22 immunoconjugates

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- Number: US 10,246,502 B2
- Document ID: US10246502B2
- Status: Granted
- Kind: B2
- Application number: 15/608,689
- Filed: 2017-05-30
- Published: 2017-10-26
- Granted: 2019-04-02
- Earliest claimed: 2015-07-16
- Assignees: Philogen S.P.A.
- Applicants: Philogen S.P.A.
- Inventors: Franziska Sophie Bootz; Dario Neri
- Web page: https://patentgrep.com/patent/US10246502B2

## CPC

- C07K 14/54: Interleukins [IL]
- A61K 38/20: Interleukins [IL]
- A61K 47/6813: {the drug being a peptidic cytokine, e.g. an interleukin or interferon}
- A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant}
- A61K 47/6851: {the antibody targeting a determinant of a tumour cell}
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- 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 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/02: Immunomodulators
- C07K 16/18: against material from animals or humans
- C07K 16/30: from tumour cells
- C07K 19/00: Hybrid peptides {, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes}
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- A61K 2039/505: {comprising antibodies}
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/622: Single chain antibody (scFv)
- C07K 2317/626: Diabody or triabody
- C07K 2319/33: fusions for targeting to specific cell types, e.g. tissue specific targeting, targeting of a bacterial subspecies
- C07K 2319/70: containing domain for protein-protein interaction
- 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

## Abstract

The application relates to a conjugate comprising interleukin-22 (IL22) and an antibody molecule. The antibody molecule preferably binds an antigen associated with angiogenesis, such as the ED-A isoform of fibronectin. In particular, the application relates to the therapeutic use of such conjugates in the treatment of a disease/disorder, such as autoimmune diseases, including inflammatory bowel disease (IBD).

## Claims

### Claim 1

A conjugate comprising interleukin-22 (IL22) and an antibody molecule, wherein the antibody molecule comprises an antigen-binding site which binds the Extra Domain-A (ED-A) of fibronectin and comprises the complementarity determining regions (CDRs) of antibody F8 set forth in SEQ ID NOs 1-6, and wherein the IL22 comprises the sequence set forth in SEQ ID NO: 11.

### Claim 2 (depends on 1)

A conjugate according to claim 1, wherein IL22 is conjugated to the N-terminus of the antibody molecule.

### Claim 3 (depends on 2)

A conjugate according to claim 2, wherein IL22 is conjugated to the N-terminus of the antibody molecule via an amino acid linker.

### Claim 4 (depends on 3)

The conjugate according to claim 3, wherein the amino acid linker is 10 to 20 amino acids long.

### Claim 5 (depends on 1)

The conjugate according to claim 1, wherein the antibody molecule is an antigen-binding fragment.

### Claim 6 (depends on 5)

The conjugate according to claim 5, wherein the antigen-binding fragment is a diabody.

### Claim 7 (depends on 5)

The conjugate according to claim 5, wherein the antigen-binding fragment comprises a single chain Fv (scFv).

### Claim 8 (depends on 5)

The conjugate according to claim 5, wherein the antigen-binding fragment comprises the VH and VL domains of antibody F8 set forth in SEQ ID NOs 7 and 8.

### Claim 9 (depends on 8)

The conjugate according to claim 8, wherein the VH domain and the VL domain of the antigen-binding fragment are linked by a 5 to 12 amino acid linker.

### Claim 10 (depends on 9)

The conjugate according to claim 9, wherein the antigen-binding fragment comprises the amino acid sequence of F8 set forth in SEQ ID NO: 10.

### Claim 11 (depends on 5)

The conjugate according to claim 5, wherein the IL22 is linked to the antigen-binding fragment by an amino acid linker.

### Claim 12 (depends on 5)

The conjugate according to claim 5, wherein the antigen-binding fragment comprises a single chain Fv (scFv) and, wherein the IL22 is linked to the N-terminus of the VH domain of the scFv via an amino acid linker.

### Claim 13 (depends on 5)

The conjugate according to claim 5, wherein the conjugate comprises the amino acid sequence set forth in SEQ ID NO: 16.

### Claim 14

A conjugate which binds to the ED-A of fibronectin, wherein the conjugate comprises the amino acid sequence set forth in SEQ ID NO: 16.

### Claim 15

A conjugate comprising IL22 and an scFv, wherein the scFv comprises an antigen-binding site which binds the ED-A of fibronectin and comprises the CDRs of antibody F8 set forth in SEQ ID NOs 1-6, and wherein the IL22 comprises the sequence set forth in SEQ ID NO: 11 and is linked to the N-terminus of the VH domain of the scFv via an amino acid linker.