# US 11,028,172 B1 · Anti-TIGIT antibodies and uses thereof

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- Number: US 11,028,172 B1
- Document ID: US11028172B1
- Status: Granted
- Kind: B1
- Application number: 17/117,969
- Filed: 2020-12-10
- Granted: 2021-06-08
- Earliest claimed: 2020-11-10
- Assignees: Lepu Biopharma Co., Ltd.
- Applicants: Lepu Biopharma Co., Ltd.
- Inventors: Wenci Gong; Yiwei Tou
- Web page: https://patentgrep.com/patent/US11028172B1

## CPC

- C07K 16/2809: {against the T-cell receptor (TcR)-CD3 complex}
- A61P 35/00: Antineoplastic agents
- C07K 16/2803: {against the immunoglobulin superfamily}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/31: multispecific
- C07K 2317/33: Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity
- C07K 2317/55: Fab or Fab'
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/622: Single chain antibody (scFv)
- 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
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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

Provided are anti-TIGIT antibodies and fragments thereof. The antibodies and fragments thereof specifically bind to the TIGIT protein. Methods of using the antibodies or fragments thereof for treating and diagnosing diseases such as cancer and viral infections are also provided.

## Claims

### Claim 1

An antibody or antigen-binding fragment thereof, wherein the antibody or fragment thereof has specificity to a T cell immunoreceptor with Ig and ITIM domains (TIGIT) protein and comprises a heavy chain variable region (VH) comprising a VH CDR1 comprising the amino acid sequence of SEQ ID NO:1, a VH CDR2 comprising the amino acid sequence of SEQ ID NO:2, and a VH CDR3 comprising the amino acid sequence of SEQ ID NO:3, and a light chain variable region (VL) comprising a VL CDR1 comprising the amino acid sequence of SEQ ID NO:4, a VL CDR2 comprising the amino acid sequence of SEQ ID NO:5, and a VL CDR3 comprising the amino acid sequence of SEQ ID NO:6.

### Claim 2 (depends on 1)

The antibody or fragment thereof of claim 1, further comprising a Fc fragment.

### Claim 3 (depends on 2)

The antibody or fragment thereof of claim 2, wherein the Fc fragment is an human IgG1 Fc fragment.

### Claim 4 (depends on 1)

The antibody or fragment thereof of claim 1, which is humanized.

### Claim 5 (depends on 1)

The antibody or fragment thereof of claim 1, wherein the VH comprises an amino acid sequence selected from the group consisting of SEQ ID NO:9-14 and the VL comprises an amino acid sequence selected from the group consisting of SEQ ID NO:15-18.

### Claim 6 (depends on 5)

The antibody or fragment thereof of claim 5, wherein the VH comprises the amino acid sequence of SEQ ID NO:11 and the VL comprises the amino acid sequence of SEQ ID NO:15.

### Claim 7 (depends on 5)

The antibody or fragment thereof of claim 5, wherein the VH comprises the amino acid sequence of SEQ ID NO:10 and the VL comprises the amino acid sequence of SEQ ID NO:16.

### Claim 8 (depends on 1)

The antibody or fragment thereof of claim 1, which is antibody-dependent cellular cytotoxicity (ADCC)-competent.

### Claim 9 (depends on 1)

A bispecific antibody comprising a fragment of claim 1 and a second antigen-binding fragment having a second specificity.

### Claim 10 (depends on 9)

The bispecific antibody of claim 9, wherein the second specificity is to a molecule on an immune cell or a tumor antigen.

### Claim 11 (depends on 9)

The bispecific antibody of claim 9, wherein the second specificity is to a molecule selected from the group consisting of CD33, CD47, CD73, Her2, EGFR, CEA VEGF, CD155, CD112, CD113, PVRL3, PVRIG, CD3, CTLA-4, GITR, 4-1BB, PD-L1, PD-1, LAG-3, CD28, CD122, TIM3, OX-40, OX40L, CD40, CD40L, LIGHT, ICOS, ICOSL, GITR, GITRL, CD27, VISTA, B7H3, B7H4, HEVM, BTLA, KIR, and combinations thereof.

### Claim 12 (depends on 9)

The bispecific antibody of claim 9, wherein the fragment and the second antigen-binding fragment each is independently selected from a Fab fragment or a single-chain variable fragment (scFv).

### Claim 13 (depends on 1)

A composition comprising the antibody or fragment thereof of claim 1 and a pharmaceutically acceptable carrier.

### Claim 14 (depends on 1)

One or more polynucleotides encoding the antibody or fragment thereof of claim 1.

### Claim 15 (depends on 14)

An isolated cell comprising the one or more polynucleotide of claim 14.

### Claim 16 (depends on 1)

A method of treating cancer in a patient in need thereof, comprising administering to the patient the antibody or fragment thereof of claim 1.

### Claim 17 (depends on 16)

The method of claim 16, wherein the cancer is selected from the group consisting of bladder cancer, breast cancer, colorectal cancer, endometrial cancer, esophageal cancer, head and neck cancer, kidney cancer, leukemia, liver cancer, lung cancer, lymphoma, melanoma, pancreatic cancer, prostate cancer, and thyroid cancer.

### Claim 18 (depends on 1)

A method of treating or inhibiting infection in a patient in need thereof, comprising administering to the patient the antibody or fragment thereof of claim 1.

### Claim 19 (depends on 1)

A method of treating cancer in a patient in need thereof, comprising (a) treating a T or NK cell, in vitro, with the antibody or fragment thereof of claim 1; and (b) administering the treated T or NK cell to the patient.

### Claim 20 (depends on 19)

The method of claim 19, further comprising, prior to step (a), isolating the T or NK cell from an individual.