# US 11,439,705 B2 · Anti-TIGIT antibodies

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- Number: US 11,439,705 B2
- Document ID: US11439705B2
- Status: Granted
- Kind: B2
- Application number: 16/413,557
- Filed: 2019-05-15
- Published: 2019-10-17
- Granted: 2022-09-13
- Earliest claimed: 2017-07-27
- Assignees: iTeos Belgium SA
- Applicants: iTeos Belgium SA
- Inventors: Anthony Cooper; Christophe Queva; Sofie Denies; Catherine Hoofd; Julia Cuende; Gregory Driessens; Florence Lambolez
- Web page: https://patentgrep.com/patent/US11439705B2

## CPC

- C07K 16/28: against receptors, cell surface antigens or cell surface determinants
- A61K 39/39541: {against normal tissues, cells}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/00: Antineoplastic agents
- C07K 16/2803: {against the immunoglobulin superfamily}
- C07K 16/2818: {against CD28 or CD152}
- C07K 16/2821: {against ICAM molecules, e.g. CD50, CD54, CD102}
- C07K 16/2827: {against B7 molecules, e.g. CD80, CD86}
- C07K 16/2878: {against the NGF-receptor/TNF-receptor superfamily, e.g. CD27, CD30, CD40, CD95}
- C07K 16/4208: {against an idiotypic determinant on Ig}
- C12N 15/85: for animal cells
- 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 2317/515: Complete light chain, i.e. VL + CL
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/732: Antibody-dependent cellular cytotoxicity [ADCC]
- C07K 2317/75: Agonist effect on antigen
- 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 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

Anti-TIGIT antibodies and antigen binding fragments thereof that inhibit TIGIT-mediated signalling are provided, together with combinations comprising said antibodies or antigen binding fragments thereof and methods for their use.

## Claims

### Claim 1

A method for treating cancer, the method comprising administering to a human patient in need thereof an effective amount of a pharmaceutical composition comprising a pharmaceutically acceptable carrier and an isolated antibody or antigen binding fragment thereof which binds to a human T cell Immunoreceptor with Ig and ITIM domains (TIGIT), wherein the antibody or antigen binding fragment comprises a heavy chain variable domain (VH) comprising a HCDR1, a HCDR2, and a HCDR3, and a light chain variable domain (VL) comprising a LCDR1, a LCDR2 and a LCDR3, wherein:
the LCDR1 comprises SEQ ID NO: 61, the LCDR2 comprises SEQ ID NO:62, and the LCDR3 comprises SEQ ID NO:63; and
the HCDR1 comprises SEQ ID NO: 16, the HCDR2 comprises SEQ ID NO:17, and the HCDR3 comprises SEQ ID NO:18.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the VH comprises an amino acid sequence with at least 95%, 97%, 98% or 99% sequence identity to SEQ ID NO:221 wherein all differences are located in a framework region of the VH; and the VL comprises an amino acid sequence with at least 95%, 97%, 98% or 99% sequence identity to SEQ ID NO:222 wherein all differences are located in a framework region of the VL.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the VH comprises SEQ ID NO:221 and the VL comprises SEQ ID NO:222.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the antibody is a human IgG antibody.

### Claim 5 (depends on 1)

The method according to claim 1, wherein the antibody is a human IgG1 antibody.

### Claim 6 (depends on 1)

The method according to claim 1, wherein the effective amount of the pharmaceutical composition is effective for selective depletion of TIGIT-expressing T-regulatory (T-reg) cells in the subject.

### Claim 7 (depends on 1)

The method of claim 1, wherein the cancer is a lung cancer.

### Claim 8

A method for increasing patient survival in a human patient in need of depletion of T reg cells, the method comprising administering to the human patient an effective amount of a pharmaceutical composition comprising a pharmaceutically acceptable carrier and an isolated antibody or antigen binding fragment thereof which binds to a human T cell Immunoreceptor with Ig and ITIM domains (TIGIT), wherein the antibody or antigen binding fragment comprises a heavy chain variable domain (VH) comprising a HCDR1, a HCDR2, and a HCDR3, and a light chain variable domain (VL) comprising a LCDR1, a LCDR2 and a LCDR3, wherein:
the LCDR1 comprises SEQ ID NO: 61, the LCDR2 comprises SEQ ID NO:62, and the LCDR3 comprises SEQ ID NO:63; and
the HCDR1 comprises SEQ ID NO: 16, the HCDR2 comprises SEQ ID NO:17, and the HCDR3 comprises SEQ ID NO:18.

### Claim 9 (depends on 8)

The method according to claim 8, wherein the VH comprises SEQ ID NO:221 and the VL comprises SEQ ID NO:222.

### Claim 10

A method for decreasing tumor volume, the method comprising administering to a human patient in need thereof an effective amount of a pharmaceutical composition comprising a pharmaceutically acceptable carrier and an isolated antibody or antigen binding fragment thereof which binds to a human T cell Immunoreceptor with Ig and ITIM domains (TIGIT), wherein the antibody or antigen binding fragment comprises a heavy chain variable domain (VH) comprising a HCDR1, a HCDR2, and a HCDR3, and a light chain variable domain (VL) comprising a LCDR1, a LCDR2 and a LCDR3, wherein:
the LCDR1 comprises SEQ ID NO: 61, the LCDR2 comprises SEQ ID NO:62, and the LCDR3 comprises SEQ ID NO:63; and
the HCDR1 comprises SEQ ID NO: 16, the HCDR2 comprises SEQ ID NO:17, and the HCDR3 comprises SEQ ID NO:18.

### Claim 11 (depends on 10)

The method according to claim 10, wherein the VH comprises SEQ ID NO:221 and the VL comprises SEQ ID NO:222.

### Claim 12 (depends on 8)

The method according to claim 8, wherein the antibody is a human IgG1 antibody.

### Claim 13 (depends on 8)

The method according to claim 8, wherein the human patient has lung cancer.

### Claim 14 (depends on 10)

The method according to claim 10, wherein the antibody is a human IgG1 antibody.

### Claim 15 (depends on 10)

The method according to claim 10, wherein the human patient has lung cancer.