# US 12,006,371 B2 · Humanized anti-MUC1* antibodies

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- Number: US 12,006,371 B2
- Document ID: US12006371B2
- Status: Granted
- Kind: B2
- Application number: 17/817,525
- Filed: 2022-08-04
- Published: 2023-06-15
- Granted: 2024-06-11
- Earliest claimed: 2015-02-10
- Assignees: Minerva Biotechnologies Corporation
- Applicants: Minerva Biotechnologies Corporation
- Inventors: Cynthia Bamdad; Benoit Smagghe
- Web page: https://patentgrep.com/patent/US12006371B2

## CPC

- C07K 16/3092: {against tumour-associated mucins}
- A61K 40/11: T-cells, e.g. tumour infiltrating lymphocytes [TIL] or regulatory T [Treg] cells; Lymphokine-activated killer [LAK] cells
- A61K 40/31: Chimeric antigen receptors [CAR]
- A61K 40/32: T-cell receptors [TCR]
- A61K 40/4257: {Mucins, e.g. MUC-1}
- A61P 35/00: Antineoplastic agents
- A61K 2239/21: Transmembrane domain
- C07K 14/7051: {T-cell receptor (TcR)-CD3 complex}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/34: Identification of a linear epitope shorter than 20 amino acid residues or of a conformational epitope defined by amino acid residues
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/622: Single chain antibody (scFv)
- C07K 2319/02: containing a signal sequence
- C07K 2319/03: containing a transmembrane segment
- C07K 2319/30: Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present application discloses humanized antibodies and antibody like proteins and fragments thereof.

## Claims

### Claim 1

A polypeptide comprising an anti-MUC1* antibody fragment, wherein the anti-MUC1* antibody fragment comprises a heavy chain variable region and a light chain variable region that have complementarity determining regions (CDRs) in the heavy chain variable region and the light chain variable region as follows:
CDR1 heavy chain SEQ ID NO: 123,
CDR1 light chain SEQ ID NO: 173,
CDR2 heavy chain SEQ ID NO: 127,
CDR2 light chain SEQ ID NO: 177,
CDR3 heavy chain SEQ ID NO: 131, and
CDR3 light chain SEQ ID NO: 181;
wherein the heavy chain variable region comprises an amino acid sequence that has at least 90% sequence identity to SEQ ID NO: 145 and the light chain variable region comprises an amino acid sequence that has at least 90% sequence identity to SEQ ID NO: 195; and
wherein the polypeptide binds to a receptor on an immune cell.

### Claim 2 (depends on 1)

The polypeptide of claim 1, wherein the heavy chain variable region comprises an amino acid sequence that has at least 95% sequence identity to SEQ ID NO: 145 and the light chain variable region comprises an amino acid sequence that has at least 95% sequence identity to SEQ ID NO: 195.

### Claim 3 (depends on 1)

The polypeptide of claim 1, wherein the heavy chain variable region comprises an amino acid sequence that has at least 98% sequence identity to SEQ ID NO: 145 and the light chain variable region comprises an amino acid sequence that has at least 98% sequence identity to SEQ ID NO: 195.

### Claim 4 (depends on 1)

The polypeptide of claim 1, wherein the heavy chain variable region comprises the amino acid sequence according to SEQ ID NO: 145 and the light chain variable region comprises the amino acid sequence according to SEQ ID NO: 195.

### Claim 5 (depends on 1)

The polypeptide of claim 1, wherein the heavy chain variable region and a light chain variable region are connected by a linker.

### Claim 6 (depends on 5)

The polypeptide of claim 5, wherein the linker comprises the amino acid sequence according to SEQ ID NO: 402.

### Claim 7 (depends on 1)

The polypeptide of claim 1, wherein the anti-MUC1* antibody fragment comprises a single chain variable fragment (scFv).

### Claim 8 (depends on 7)

The polypeptide of claim 7, wherein the scFv comprises an amino acid sequence that has at least 90% sequence identity to any one of SEQ ID NOs: 239, 241, 243, 396, or 398.

### Claim 9 (depends on 7)

The polypeptide of claim 7, wherein the scFv comprises an amino acid sequence that has at least 95% sequence identity to any one of SEQ ID NOs: 239, 241, 243, 396, or 398.

### Claim 10 (depends on 7)

The polypeptide of claim 7, wherein the scFv comprises an amino acid sequence that has at least 98% sequence identity to any one of SEQ ID NOs: 239, 241, 243, 396, or 398.

### Claim 11 (depends on 7)

The polypeptide of claim 7, wherein the scFv comprises an amino acid sequence according to any one of SEQ ID NOs: 239, 241, 243, 396, or 398.

### Claim 12 (depends on 7)

The polypeptide of claim 7, wherein the scFv is selected for its ability to bind to a MUC1* peptide, wherein the MUC1* peptide comprises the amino acid sequence of SEQ ID NO: 2, SEQ ID NO: 620, or SEQ ID NO: 621.

### Claim 13 (depends on 7)

The polypeptide of claim 7, wherein the scFv is selected for its ability to bind to a MUC1* positive cancer or a MUC1* transfected cell.

### Claim 14 (depends on 13)

The polypeptide of claim 13, wherein the MUC1* positive cancer cell comprises MUC1* positive breast cancer cells.

### Claim 15 (depends on 13)

The polypeptide of claim 13, wherein the MUC1* positive cancer cell comprises MUC1* positive prostate cancer cells.

### Claim 16 (depends on 7)

The polypeptide of claim 7, wherein the scFv is selected for its ability to inhibit growth of MUC1* positive cancer cells.

### Claim 17 (depends on 16)

The polypeptide of claim 16, wherein the MUC1* positive cancer cells comprise MUC1* positive breast cancer cells.

### Claim 18 (depends on 1)

The polypeptide of claim 1, wherein the immune cell comprises a T cell.

### Claim 19 (depends on 18)

The polypeptide of claim 18, wherein the receptor on the immune cell comprises CD3.

### Claim 20 (depends on 19)

The polypeptide of claim 19, wherein the polypeptide further comprises an amino acid sequence with at least 90% sequence identity to SEQ ID NO: 390 or SEQ ID NO: 388.

### Claim 21 (depends on 19)

The polypeptide of claim 19, wherein the polypeptide further comprises an amino acid sequence with at least 95% sequence identity to SEQ ID NO: 390 or SEQ ID NO: 388.

### Claim 22 (depends on 19)

The polypeptide of claim 19, wherein the polypeptide further comprises an amino acid sequence with at least 98% sequence identity to SEQ ID NO: 390 or SEQ ID NO: 388.

### Claim 23 (depends on 19)

The polypeptide of claim 19, wherein the polypeptide further comprises the amino acid sequence of SEQ ID NO: 390 or SEQ ID NO: 388.

### Claim 24 (depends on 1)

The polypeptide of claim 1, wherein the polypeptide comprises an amino acid sequence with at least 95% sequence identity to SEQ ID NO: 239 and an amino acid sequence with at least 95% sequence identity to SEQ ID NO: 390.

### Claim 25 (depends on 1)

The polypeptide of claim 1, wherein the polypeptide comprises an amino acid sequence with at least 95% sequence identity to SEQ ID NO: 239 and an amino acid sequence with at least 95% sequence identity to SEQ ID NO: 388.

### Claim 26 (depends on 1)

The polypeptide of claim 1, wherein the polypeptide comprises an amino acid sequence with at least 95% sequence identity to SEQ ID NO: 398 and an amino acid sequence with at least 95% sequence identity to SEQ ID NO: 388.

### Claim 27 (depends on 1)

The polypeptide of claim 1, wherein the polypeptide comprises the amino acid sequence of SEQ ID NO: 239, the amino acid sequence of SEQ ID NO: 400, and the amino acid sequence of SEQ ID NO: 390.

### Claim 28 (depends on 1)

The polypeptide of claim 1, wherein the polypeptide comprises the amino acid sequence of SEQ ID NO: 239, the amino acid sequence of SEQ ID NO: 400, and the amino acid sequence of SEQ ID NO: 388.

### Claim 29 (depends on 1)

The polypeptide of claim 1, wherein the polypeptide comprises the amino acid sequence of SEQ ID NO: 398, the amino acid sequence of SEQ ID NO: 400, and the amino acid sequence of SEQ ID NO: 388.
