# US 10,479,824 B2 · Single chain FC polypeptides

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- Number: US 10,479,824 B2
- Document ID: US10479824B2
- Status: Granted
- Kind: B2
- Application number: 12/374,213
- Filed: 2007-07-24
- Published: 2009-12-10
- Granted: 2019-11-19
- Earliest claimed: 2006-07-25
- Assignees: Ucb Biopharma Sprl
- Applicants: Alastair David Griffiths Lawson; Paul Edward Stephens
- Inventors: Alastair David Griffiths Lawson; Paul Edward Stephens
- Web page: https://patentgrep.com/patent/US10479824B2

## CPC

- C07K 16/00: Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- 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 9/14: Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
- A61P 11/06: Antiasthmatics
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/10: for osteoporosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 31/10: Antimycotics
- A61P 31/12: Antivirals
- A61P 33/00: Antiparasitic agents
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/734: Complement-dependent cytotoxicity [CDC]
- 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

## Abstract

The present invention relates to single chain polypeptides comprising one or more immunoglobulin Fc domains. In particular the present invention relates to single-chain Fc polypeptides in which at least one functional Fc domain is formed within the polypeptide chain.

## Claims

### Claim 1

An isolated monovalent polypeptide, comprising a single chain Fc polypeptide, and a monovalent binding domain;
wherein the single chain Fc polypeptide N to C-terminal sequence is:
a first CH2 domain linked via its C-terminus to an N-terminus of a first CH3 domain, and the first CH3 domain is linked at its C-terminus via at least one amino acid linker comprising repeat units of GSGGS (SEQ ID NO:92), GGGGS (SEQ ID NO:93), and GGGS (SEQ ID NO94) to the N-terminus of a second CH2 domain and the second CH2 domain linked at its C-terminus to the N-terminus of a second CH3 domain;
wherein the single chain Fc polypeptide does not contain cysteine amino acid residues in a hinge region;
wherein Fc domains in the single chain Fc polypeptide consist of two CH2 domains and two CH3 domains, wherein the first CH2 domain is intra-molecularly dimerised with the second CH2 domain and the first CH3 domain is intra-molecularly dimerised with the second CH3 domain within the single chain Fc polypeptide;
wherein the two CH2 domains and the two CH3 domains form a functional Fc domain within the single chain Fc polypeptide via at least one linker of 15 to 50 or 30 to 130 amino acids in length, or combinations thereof; and
wherein the single chain Fc polypeptide is linked at its N terminus to one biologically active molecule that is a monovalent binding protein selected from the group consisting of scFv, Fab, Fab', VHH, and Fv,
with the proviso that when the single chain polypeptide Fc is linked to the biologically active molecule via a linker, the linker does not contain cysteine amino acid residues.

### Claim 2 (depends on 1)

The polypeptide of claim 1, wherein the at least one linker forming the functional single chain Fc polypeptide optionally comprises one or more amino acids selected from glycine, serine, alanine and threonine.

### Claim 3 (depends on 2)

The polypeptide of claim 2, wherein the at least one linker forming the functional single chain Fc polypeptide comprises the sequence given in SEQ ID NO:62.

### Claim 4 (depends on 3)

The polypeptide of claim 3, wherein the linker comprises all or part of an antibody hinge sequence or a modified antibody hinge sequence.

### Claim 5 (depends on 1)

The polypeptide of claim 1, wherein the biologically active molecule and the single chain Fc polypeptide are linked by a peptide linker of between 1 and 100 amino acids in length.

### Claim 6 (depends on 1)

The polypeptide of claim 1 to which one or more effector molecules are attached.

### Claim 7 (depends on 1)

A pharmaceutical composition comprising the single chain Fc polypeptide of claim 1, in combination with one or more of a pharmaceutically acceptable excipient, diluent or carrier.

### Claim 8 (depends on 7)

The pharmaceutical composition of claim 7, additionally comprising other active ingredients.

### Claim 9 (depends on 1)

The polypeptide of claim 1, wherein the linker is 50 to 100 amino acids in length.