# US 2019/0375819 A1 · Glycosylated transferrin receptor 1 tumor antigen

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- Number: US 2019/0375819 A1
- Document ID: US20190375819A1
- Status: Published application
- Kind: A1
- Application number: 16/346,061
- Filed: 2017-10-30
- Published: 2019-12-12
- Earliest claimed: 2016-10-29
- Applicants: Rhode Island Hospital
- Inventors: Jisu Li; Jason Shapiro; Jack R. Wands
- Web page: https://patentgrep.com/patent/US20190375819A1

## CPC

- C07K 14/70582: {CD71}
- A61K 39/001102: {Receptors, cell surface antigens or cell surface determinants}
- A61K 39/001129: {Molecules with a "CD" designation not provided for elsewhere}
- A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant}
- A61K 47/6859: {the tumour determinant being from liver or pancreas cancer cell}
- A61K 49/0058: {Antibodies}
- A61K 51/1027: {against receptors, cell-surface antigens or cell-surface determinants}
- A61K 51/1057: {the tumor cell being from liver or pancreas}
- A61P 35/00: Antineoplastic agents
- C07K 14/705: Receptors; Cell surface antigens; Cell surface determinants {(tumour specific antigens C07K14/4748)}
- C07K 16/2881: {against CD71}
- C07K 16/44: against material not provided for elsewhere {, e.g. haptens, metals, DNA, RNA, amino acids}
- G01N 33/575: for cancer
- G01N 33/5758: {involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites}
- G01N 33/5759: {involving compounds localised on the membrane of tumour or cancer cells}
- A61K 2039/82: {Colon}
- A61K 2039/844: {Liver}
- C07K 2317/41: Glycosylation, sialylation, or fucosylation
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- G01N 2800/50: Determining the risk of developing a disease
- 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
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

This invention relates to compositions and methods for treating or diagnosing cancer.

## Claims

### Claim 1

A composition or method comprising a purified human transferrin receptor 1 (TFR1) protein or a purified cell surface glycosylated peptide fragment thereof, for use as a biomarker for detection of malignancy.

### Claim 2 (depends on 1)

The composition of claim 1, wherein said TFR1 protein or peptide fragment thereof comprises glycosylation at an aberrant site compared to a wild type TFR1 protein.

### Claim 3 (depends on 1)

The compositon of claim 1, wherein said protein or peptide fragment does not comprise a N-linked glycosylation at amino acid position 251, 317, or 727 of SEQ ID NO:1.

### Claim 4 (depends on 1)

The composition of claim 1, wherein said protein or peptide fragment comprises an N-linked glycosylation at amino acid position 50 or 55 of SEQ ID NO:1.

### Claim 5 (depends on 1)

The composition of claim 1, wherein said protein or peptide fragment comprises an O-linked glycosylation at amino acid position 104 of SEQ ID NO:1.

### Claim 6

A purified monoclonal antibody that binds to a human transferrin receptor 1 (TFR1) for use in immunotherapy, as a vehicle for delivery of anti-tumor compounds, or as a diagnostic agent, wherein said antibody binds to an aberrant glycosylation site of said TFR1.

### Claim 7 (depends on 6)

The monoclonal antibody of claim 6, wherein said TFR1 comprises glycosylation at an aberrant site compared to a wild type TFR1 protein.

### Claim 8 (depends on 6)

The monoclonal antibody of claim 6, wherein said antibody comprises AF-20.

### Claim 9 (depends on 6)

The monoclonal antibody of claim 6, wherein said antibody does not comprise AF-20.

### Claim 10 (depends on 1)

The composition or method of claim 1, wherein said TFR1 or glycosylated peptide thereof, is in the absence of other compounds with which it naturally occurs in a mammal, said compounds being selected from the group consisting of Heat Shock Protein 90 (HSP90) and/or a Na+/K+ ATPase or Mg++ ATPase (Transporting ATPase).

### Claim 11

A method for delivering a cargo molecule to a subject, the method comprising:
administering an antibody conjugated to said cargo molecule to the subject,
wherein the antibody binds to a glycosylated human transferrin receptor-1 antigen, and
wherein said cargo molecule is selected from the group consisting of a therapeutic agent or a detectable label.

### Claim 12 (depends on 11)

The method of claim 11, wherein said therapeutic agent comprises a cytotoxic compound.

### Claim 13 (depends on 11)

The method of claim 11, wherein said detectable label comprises a fluorescent compound or a radioisotope.

### Claim 14 (depends on 11)

The method of claim 11, wherein said subject is characterized as comprising a malignancy.

### Claim 15 (depends on 11)

The method of claim 11, wherein said antibody comprises AF-20.

### Claim 16 (depends on 11)

The method of claim 11, wherein said antibody does not comprise AF-20.

### Claim 17 (depends on 1)

The composition or method of claim 1, wherein said receptor or peptide thereof comprises asparagine (N)-linked glycosylation.

### Claim 18

A purified glycosylated TFR1 antigen epitope comprising N-linked glycosylation at amino acid position 50 of SEQ ID NO:1 or amino acid position 55 of SEQ ID NO:1.

### Claim 19

A purified glycosylated TFR1 antigen epitope comprising O-linked glycosylation at amino acid position 104 of SEQ ID NO:1.

### Claim 20 (depends on 18, 19)

The antigen epitope of claim 18 or 19, wherein said epitope comprises a length of at least 5 consecutive amino acids of SEQ ID NO:1.

### Claim 21

A method of diagnosing a malignancy, comprising contacting a bodily tissue or fluid of a subject with an antibody that binds to TFR1, wherein said TFR1 comprises glycosylation at an aberrant site compared to a wild type TFR1 protein.

### Claim 22 (depends on 21)

The method of claim 21, further comprising administering to said subject a cancer therapeutic composition.

### Claim 23 (depends on 11, 21)

The method of claim 11 or 21, wherein said subject comprises or is at risk of developing a colon cancer, a liver cancer, or a lung cancer.