# US 9,040,041 B2 · Modified FC molecules

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- Number: US 9,040,041 B2
- Document ID: US9040041B2
- Status: Granted
- Kind: B2
- Application number: 12/794,560
- Filed: 2010-06-04
- Published: 2010-09-30
- Granted: 2015-05-26
- Earliest claimed: 2005-10-03
- Assignees: Xencor, Inc.
- Applicants: John R. Desjarlais; Sher Bahadur Karki; Gregory Alan Lazar; John O. Richards; Gregory L. Moore; David F. Carmichael
- Inventors: John R. Desjarlais; Sher Bahadur Karki; Gregory Alan Lazar; John O. Richards; Gregory L. Moore; David F. Carmichael
- Web page: https://patentgrep.com/patent/US9040041B2

## CPC

- C07K 16/00: Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
- C07K 16/2863: {against receptors for growth factors, growth regulators}
- C07K 16/2887: {against CD20}
- C07K 16/30: from tumour cells
- C07K 2317/41: Glycosylation, sialylation, or fucosylation
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/72: Increased effector function due to an Fc-modification
- C07K 2317/732: Antibody-dependent cellular cytotoxicity [ADCC]
- C07K 2317/77: Internalization into the cell
- 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

The present invention relates to Fc variants with optimized Fc receptor binding properties, methods for their generation, Fc polypeptides comprising Fc variants with optimized Fc receptor binding properties, and methods for using Fc variants with optimized Fc receptor binding properties.

## Claims

### Claim 1

A method of enhancing mediation of ADCP (antibody dependent cellular phagocytosis) comprising contacting a antibody with a macrophage expressing FcyRIIa, wherein said antibody comprises an Fc variant of a human parent Fc polypeptide, wherein said Fc variant comprises an amino acid substitution at position 236 in the Fc region as compared to the human parent Fc polypeptide, wherein said substitution is alanine, said Fc variant is an engineered glycoform with reduced fucose content as compared to the human parent Fc polypeptide, and said Fc variant exhibits an increase in affinity for FcγRIIa over FcγRIIb, thereby resulting in the binding of said Fc variant to FcyRIIa, wherein said increased affinity is relative to the affinity exhibited by the human parent Fc polypeptide and wherein the numbering is according to the EU index.

### Claim 2 (depends on 1)

The method of claim 1, wherein said antibody is selected from the group consisting of a human antibody, a humanized antibody, and a monoclonal antibody.

### Claim 3 (depends on 1)

The method of claim 1, wherein said antibody has specificity for a target antigen selected from the group consisting of Ep-CAM, CD19, CD20, CD22, CD30, CD33, CD40, CD40L, CD52, Her2/neu, EGFR, IGF-1 R, EpCAM, MUC1, GD3, CEA, CA 125, HLA-DR, MUC18, and prostate specific membrane antigen (PMSA).