# US 9,750,820 B2 · IgG Fc fragment for a drug carrier and method for the preparation thereof

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- Number: US 9,750,820 B2
- Document ID: US9750820B2
- Status: Granted
- Kind: B2
- Application number: 14/327,120
- Filed: 2014-07-09
- Published: 2015-01-22
- Granted: 2017-09-05
- Earliest claimed: 2003-11-13
- Assignees: Hanmi Science Co., Ltd.
- Applicants: Hanmi Science Co., Ltd.
- Inventors: Sung Youb Jung; Jin Sun Kim; Geun Hee Yang; Se Chang Kwon; Gwan Sun Lee
- Web page: https://patentgrep.com/patent/US9750820B2

## CPC

- A61K 47/68: the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K 47/6811: {the drug being a protein or peptide, e.g. transferrin or bleomycin}
- A61K 47/6813: {the drug being a peptidic cytokine, e.g. an interleukin or interferon}
- A61K 47/6835: {the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site}
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/06: of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
- A61P 5/10: of the posterior pituitary hormones, e.g. oxytocin, ADH
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 7/06: Antianaemics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 14/505: Erythropoietin [EPO]
- C07K 14/535: Granulocyte CSF; Granulocyte-macrophage CSF
- C07K 14/56: IFN-alpha
- C07K 14/61: Growth hormone [GH], i.e. somatotropin
- C07K 16/46: Hybrid immunoglobulins (hybrids of an immunoglobulin with a peptide not being an immunoglobulin C07K19/00)
- C07K 19/00: Hybrid peptides {, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes}
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/732: Antibody-dependent cellular cytotoxicity [ADCC]
- C07K 2317/734: Complement-dependent cytotoxicity [CDC]
- C07K 2319/30: Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
- 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
- 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)

## Abstract

Disclosed is an IgG Fc fragment useful as a drug carrier. A recombinant vector expressing the IgG Fc fragment, a transformant transformed with the recombinant vector, and a method of preparing an IgG Fc fragment are disclosed. When conjugated to a certain drug, the IgG Fc fragment improves the in vivo duration of action of the drug and minimizes the in vivo activity reduction of the drug.

## Claims

### Claim 1

An IgG Fc fragment as a drug carrier, wherein the IgG Fc fragment is covalently linked to a drug through a non-peptide linker, wherein the non-peptide linker is a polyethylene glycol, polypropylene glycol, copolymers of ethylene glycol and propylene glycol, polyoxyethylated polyols, polyvinyl alcohol, dextran, polyvinyl ether, polylactic acid, polylactic-glycolic acid, a lipid polymer, a chitin, or hyaluronic acid, and wherein the IgG Fc fragment is aglycosylated and consists of the amino acid sequence of SEQ ID NO: 23.

### Claim 2 (depends on 1)

The Fc fragment as set forth in claim 1, wherein the aglycosylated IgG Fc fragment is a recombinant human IgG Fc fragment.

### Claim 3 (depends on 1)

A composition comprising the Fc fragment of claim 1.

### Claim 4

An IgG Fc fragment as a drug carrier, the IgG Fc fragment being covalently linked to a drug through a non-peptide linker, wherein the non-peptide linker is a polyethylene glycol having a molecular weight of 3.4 kDa or 10 kDa, wherein the IgG Fc fragment is aglycosylated and consists of the amino acid sequence of SEQ ID NO: 23.