# US 12,215,146 B2 · Antibody variants

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- Number: US 12,215,146 B2
- Document ID: US12215146B2
- Status: Granted
- Kind: B2
- Application number: 16/648,185
- Filed: 2018-09-11
- Published: 2020-08-13
- Granted: 2025-02-04
- Earliest claimed: 2017-09-19
- Assignees: Tillotts Pharma AG
- Applicants: Tillotts Pharma AG
- Inventors: Esther Maria Furrer
- Web page: https://patentgrep.com/patent/US12215146B2

## CPC

- C07K 16/241: {Tumor Necrosis Factors}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/41: Glycosylation, sialylation, or fucosylation
- C07K 2317/524: CH2 domain
- C07K 2317/526: CH3 domain
- C07K 2317/72: Increased effector function due to an Fc-modification
- C07K 2317/732: Antibody-dependent cellular cytotoxicity [ADCC]
- C07K 2317/734: Complement-dependent cytotoxicity [CDC]
- C07K 2317/74: Inducing cell proliferation
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/77: Internalization into the cell
- 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)

## Abstract

The present invention relates to antibodies which bind to TNFα and exhibit modified FcRn-binding. The antibodies of the invention have good effector functions and/or pharmacokinetic properties.

## Claims

### Claim 1

An antibody comprising a TNFα-binding domain and an FcRn-binding site, wherein said antibody has a high affinity to human FcRn at pH 6, said high affinity being characterized by a dissociation equilibrium constant (KD) of less than 500 nM, further wherein said antibody has no affinity or a low affinity to human FcRn at pH 7.4, said low affinity being characterized by a KD of greater than 10 μM, further wherein the amino acid sequence of the antibody comprises the amino acids 380A and 434A, wherein the numbering of amino acid residues is according to the EU index, further wherein the antibody comprises (i) a VL domain comprising a CDR1 region having the amino acid sequence as shown in SEQ ID NO:3, a CDR2 region having the amino acid sequence as shown in SEQ ID NO:4, and a CDR3 region having the amino acid sequence as shown in SEQ ID NO:5, and (ii) a VH domain comprising a CDR1 region having the amino acid sequence as shown in SEQ ID NO:6, a CDR2 region having the amino acid sequence as shown in SEQ ID NO:7, and a CDR3 region having the amino acid sequence as shown in SEQ ID NO:8.

### Claim 2 (depends on 1)

The antibody of claim 1, wherein the amino acid sequence of the antibody further comprises the amino acid 307T, wherein the numbering of amino acid residues is according to the EU index.

### Claim 3 (depends on 1)

The antibody of claim 1, wherein said antibody binds to human TNFα with a KD of less than 100 pM.

### Claim 4 (depends on 1)

The antibody of claim 1, wherein said antibody is a non-fucosylated antibody.

### Claim 5 (depends on 1)

A pharmaceutical composition comprising the antibody of claim 1 in combination with a pharmaceutically acceptable carrier.