# US 2023/0069760 A1 · Anti-vtcn1 antibodies and antibody drug conjugates

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2023/0069760 A1
- Document ID: US20230069760A1
- Status: Published application
- Kind: A1
- Application number: 16/606,246
- Filed: 2018-04-19
- Published: 2023-03-02
- Earliest claimed: 2017-04-19
- Assignees: Bluefin BioMedicine, Inc.
- Applicants: Bluefin BioMedicine, Inc.
- Inventors: Ailan Guo; Svetlana Popova; Scott Michael Lonning; Jason G. Beaudet
- Web page: https://patentgrep.com/patent/US20230069760A1

## CPC

- A61K 31/7068: having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/68031: {the drug being an auristatin}
- A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant}
- A61K 47/6851: {the antibody targeting a determinant of a tumour cell}
- A61P 35/00: Antineoplastic agents
- C07K 16/2818: {against CD28 or CD152}
- C07K 16/2827: {against B7 molecules, e.g. CD80, CD86}
- A61K 2039/505: {comprising antibodies}
- A61K 2039/507: {Comprising a combination of two or more separate antibodies}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/33: Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- C07K 2317/732: Antibody-dependent cellular cytotoxicity [ADCC]
- 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
- 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
- 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

Disclosed herein are anti-V-set domain containing T cell activation inhibitor 1 (VTCN1) antibodies and antibody drug conjugates (ADCs), including compositions and methods of using said antibodies and ADCs.

## Claims

### Claim at position 1

-297. (canceled)

### Claim 298

An anti-VTCN1 antibody, or antigen-binding portion thereof, comprising
a heavy chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 239, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 238, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 237, and a light chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 227, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 226, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 225;
a heavy chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 251, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 250, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 249, and a light chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 255, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 254, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 253;
a heavy chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 267, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 266, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 265, and a light chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 271, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 270, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 269;
a heavy chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 267, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 285, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 284, and a light chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 287, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 254, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 269;
a heavy chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 267, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 280, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 279, and a light chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 282, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 254, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 269; or
a heavy chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 215, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 214, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 213, and a light chain variable region comprising a CDR3 domain comprising the amino acid sequence of SEQ ID NO: 219, a CDR2 domain comprising the amino acid sequence of SEQ ID NO: 218, and a CDR1 domain comprising the amino acid sequence of SEQ ID NO: 217.

### Claim 299

An anti-VTCN1 antibody, or antigen-binding portion thereof, comprising
a heavy chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 236 and a light chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 224;
a heavy chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 248 and a light chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 252;
a heavy chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 264 and a light chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 268;
a heavy chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 283 and a light chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 286;
a heavy chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 278 and a light chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 281; or
a heavy chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 212 and a light chain variable domain comprising an amino acid sequence set forth in SEQ ID NO: 216.

### Claim 300

An anti-VTCN1 antibody, or antigen-binding portion thereof, comprising a heavy chain comprising an amino acid sequence set forth in SEQ ID NO: 236, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 236, and/or a light chain comprising an amino acid sequence set forth in SEQ ID NO: 224, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 224;
a heavy chain comprising an amino acid sequence set forth in SEQ ID NO: 248, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 248, and/or a light chain comprising an amino acid sequence set forth in SEQ ID NO: 252, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 252;
a heavy chain comprising an amino acid sequence set forth in SEQ ID NO: 264, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 264, and/or a light chain comprising an amino acid sequence set forth in SEQ ID NO: 268, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 268;
a heavy chain comprising an amino acid sequence set forth in SEQ ID NO: 283, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 283, and/or a light chain comprising an amino acid sequence set forth in SEQ ID NO: 286, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 286;
a heavy chain comprising an amino acid sequence set forth in SEQ ID NO: 278, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 278, and/or a light chain comprising an amino acid sequence set forth in SEQ ID NO: 281, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 281; or
a heavy chain comprising an amino acid sequence set forth in SEQ ID NO: 212, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 212, and/or a light chain comprising an amino acid sequence set forth in SEQ ID NO: 216, or a sequence having at least 90%, 95%, 96%, 97%, 98%, or 99% identity to SEQ ID NO: 216.

### Claim 301 (depends on 298)

An antibody, or antigen-binding portion thereof, that binds to the same epitope as the antibody, or antigen-binding portion thereof, of claim 298.

### Claim 302 (depends on 298)

The antibody, or antigen binding portion thereof, of claim 298, wherein the antibody, or antigen binding portion thereof, is a human or humanized antibody.

### Claim 303 (depends on 298)

The antibody, or antigen binding portion thereof, of claim 298, wherein the antibody, or antigen binding portion thereof, is an IgG1 or IgG4 isotype.

### Claim 304 (depends on 298)

The antibody, or antigen binding portion thereof, of claim 298, wherein the antibody, or antigen binding portion thereof, has a KD of 200 nM or less.

### Claim 305 (depends on 298)

The antibody, or antigen binding portion thereof, of claim 298, wherein the antibody, or antigen binding portion thereof, is multispecific.

### Claim 306 (depends on 298)

The antibody, or antigen binding portion thereof, of claim 298, wherein the antibody, or antigen binding portion thereof, is bispecific.

### Claim 307 (depends on 298)

An isolated nucleic acid encoding an antibody, or antigen binding portion thereof, of claim 298.

### Claim 308 (depends on 298)

A pharmaceutical composition comprising the antibody, or antigen binding portion thereof, of claim 298 and a pharmaceutically acceptable carrier.

### Claim 309 (depends on 298)

A method for treating cancer, comprising administering a therapeutically effective amount of the antibody or antigen binding portion thereof of claim 298, to a subject in need thereof.

### Claim 310 (depends on 309)

The method of claim 309, wherein the cancer is selected from the groups consisting of triple negative breast cancer (TNBC), renal cancer, ovarian cancer, NSCLC, endometrial cancer, and liver cancer.

### Claim 311 (depends on 298)

A method for inhibiting or decreasing solid tumor growth in a subject having a solid tumor, said method comprising administering an effective amount of an anti-VTCN1 antibody, or antigen binding portion thereof, of claim 298, to the subject having the solid tumor, such that the solid tumor growth is inhibited or decreased.

### Claim 312 (depends on 311)

The method of claim 311, wherein the tumor is selected from the groups consisting of triple negative breast cancer (TNBC), renal cancer, and ovarian cancer.

### Claim 313 (depends on 311)

The method of claim 311, wherein the antibody or antigen binding portion thereof, is administered in combination with an additional agent or an additional therapy.

### Claim 314 (depends on 313)

The method of claim 313, wherein the additional agent or additional therapy is an immune checkpoint inhibitor, an antibody, radiation, one or more chemotherapeutic agent, an inhibitor of activity or cell number of meyloid derived suppressor cells (MDSCs), a DNA alkylator, a PARP inhibitor, IL-6, interferon-gamma (IFN-γ), an agent which is capable of decreasing T regulatory cells and/or increasing effector T cell:T regulatory cell ratio, gemcitabine, or a combination thereof.