# US 12,600,789 B2 · Modified antibody constant region

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- Number: US 12,600,789 B2
- Document ID: US12600789B2
- Status: Granted
- Kind: B2
- Application number: 17/720,937
- Filed: 2022-04-14
- Published: 2022-08-11
- Granted: 2026-04-14
- Earliest claimed: 2007-09-26
- Assignees: Chugai Seiyaku Kabushiki Kaisha
- Applicants: Chugai Seiyaku Kabushiki Kaisha
- Inventors: Tomoyuki Igawa; Hirotake Shiraiwa
- Web page: https://patentgrep.com/patent/US12600789B2

## CPC

- C07K 16/2866: {against receptors for cytokines, lymphokines, interferons}
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/00: Drugs for immunological or allergic disorders
- C07K 16/00: Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/524: CH2 domain
- C07K 2317/526: CH3 domain
- C07K 2317/53: Hinge
- C07K 2317/71: Decreased effector function due to an Fc-modification
- C07K 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- 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 inventors succeeded in improving the antibody constant region to have increased stability under acid conditions, reduced heterogeneity originated from disulfide bonds in the hinge region, reduced heterogeneity originated from the H chain C terminus, and increased stability at high concentrations as well as in discovering novel constant region sequences having reduced Fcγ receptor-binding, while minimizing the generation of novel T-cell epitope peptides. As a result, the present inventors successfully discovered antibody constant regions with improved physicochemical properties (stability and homogeneity), immunogenicity, safety, and pharmacokinetics.

## Claims

### Claim 1

An antibody heavy chain constant region comprising the amino acid sequence of SEQ ID NO: 5.

### Claim 2 (depends on 1)

An antibody comprising the antibody heavy chain constant region of claim 1.

### Claim 3 (depends on 2)

The antibody of claim 2, wherein the antibody is an anti-IL-6 receptor antibody, anti-IL-31 receptor antibody, or anti-RANKL antibody.

### Claim 4 (depends on 1)

A pharmaceutical composition comprising the antibody heavy chain constant region of claim 1.

### Claim 5

An antibody heavy chain constant region comprising the amino acid sequence of SEQ ID NO: 7.

### Claim 6 (depends on 5)

An antibody comprising the antibody heavy chain constant region of claim 5.

### Claim 7 (depends on 6)

The antibody of claim 6, wherein the antibody is an anti-IL-6 receptor antibody, anti-IL-31 receptor antibody, or anti-RANKL antibody.

### Claim 8 (depends on 5)

A pharmaceutical composition comprising the antibody heavy chain constant region of claim 5.