# US 10,501,532 B2 · Carbohydrate antibodies, pharmaceutical compositions and uses thereof

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

- Number: US 10,501,532 B2
- Document ID: US10501532B2
- Status: Granted
- Kind: B2
- Application number: 15/288,562
- Filed: 2016-10-07
- Published: 2017-04-13
- Granted: 2019-12-10
- Earliest claimed: 2015-10-07
- Assignees: Obi Pharma, Inc.
- Applicants: Obi Pharma, Inc.
- Inventors: Cheng-Der Tony Yu; Jiann-Shiun Lai; I-Ju Chen
- Web page: https://patentgrep.com/patent/US10501532B2

## CPC

- C07K 16/18: against material from animals or humans
- A61P 35/00: Antineoplastic agents
- C07K 16/30: from tumour cells
- C07K 16/44: against material not provided for elsewhere {, e.g. haptens, metals, DNA, RNA, amino acids}
- A61K 2039/505: {comprising antibodies}
- A61K 2039/80: {Vaccine for a specifically defined cancer}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/567: Framework region [FR]
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- 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

The present invention provides antibodies or the antigen-binding portion thereof to a tumor-associate carbohydrate antigen. Also disclosed herein are pharmaceutical compositions and methods for the inhibition of cancer cells in a subject in need thereof. The pharmaceutical compositions comprise an antibody or an antigen-binding portion thereof and at least one pharmaceutically acceptable carrier.

## Claims

### Claim 1

An antibody, or an antigen-binding portion thereof, that binds to a carbohydrate antigen, comprising a heavy chain variable region and a light chain variable region comprising:
a heavy chain complementarity determining region HC-CDR1 selected from the group consisting of:
(i) SEQ ID NO:1,
(ii) SEQ ID NO: 1 wherein amino acid residue 3 is substituted with an arginine (S028R, and
(iii) SEQ ID NO: 1 wherein amino acid residue 6 is substituted with an arginine (T031R),
a heavy chain complementarity determining region HC-CDR2 selected from the group consisting of:
(i) SEQ ID NO: 2,
(ii) SEQ ID NO: 2 wherein amino acid residue 6 is substituted with a glycine (DO57G), and
(iii) SEQ ID NO: 2 wherein amino acid residue 12 is substituted with a tyrosine (P063Y),
a heavy chain complementarity determining region HC-CDR3 selected from the group consisting of:
(i) SEQ ID NO: 3, and
(i) SEQ ID NO: 3 wherein amino acid residue 6 is substituted with an arginine (D105R),
a light chain complementarity determining region LC-CDR1 selected from the group consisting of:
(i) SEQ ID NO: 7,
(ii) SEQ ID NO: 7 wherein amino acid residue 1 is substituted with a tryptophan (R024W), and
(iii) SEQ ID NO: 7 wherein amino acid residue 9 is substituted with a glutamine (M032Q),
a light chain complementarity determining region LC-CDR2 selected from the group consisting of:
(i) SEQ ID NO: 8,
(ii) SEQ ID NO: 8 wherein amino acid residue 1 is substituted with a glycine (A049G), and
(iii) SEQ ID NO: 8 wherein amino acid residue 5 is substituted with a lysine (L053K), and
a light chain complementarity determining region LC-CDR3 selected from the group consisting of:
(i) SEQ ID NO: 9, and
(ii) SEQ ID NO: 9 wherein amino acid residue 6 is substituted with an arginine (N093R),
wherein the antibody, or an antigen-binding portion thereof, comprises at least one of the amino acid substitutions in a CDR region selected from the group consisting of S028R, T031R, D057G, P063Y, D105R, R024W, M032Q, A049G, L053K and N093R.

### Claim 2 (depends on 1)

The antibody or antibody binding portion thereof of claim 1, further comprises at least one of the following frameworks:
(a) a heavy chain framework (HC-FW1) having a sequence 90% to 100% homologous to SEQ ID NO: 4,
(b) a heavy chain framework (HC-FW2) having a sequence 90% to 100% homologous to SEQ ID NO: 5,
(c) a heavy chain framework (HC-FW3) having a sequence 90% to 100% homologous to SEQ ID NO: 6,
(d) a heavy chain framework (HC-FW2) having a sequence 90% to 100% homologous to SEQ ID NO: 5, wherein amino acid residue 9 in HC-FW2 is glycine and not substituted,
(e) a light chain framework (LC-FW1) having a sequence 90% to 100% homologous to SEQ ID NO: 10,
(f) a light chain framework (LC-FW2) having a sequence 90% to 100% homologous to SEQ ID NO: 11,
(g) a light chain framework (LC-FW3) having a sequence 90% to 100% homologous to SEQ ID NO: 12,
(h) a light chain framework (LC-FW2) having a sequence 90% to 100% homologous to SEQ ID NO: 11, wherein amino acid residue 12 in LC-FW2 is proline and not substituted, and/or
(i) a light chain framework (LC-FW2) having a sequence 90% to 100% homologous to SEQ ID NO: 11, wherein amino acid residue 13 in LC-FW2 is tryptophan and not substituted.

### Claim 3 (depends on 1)

The antibody or the antigen binding portion thereof of claim 1, wherein the carbohydrate antigen is Globo H, stage-specific embryonic antigen 3 (SSEA-3), stage-specific embryonic antigen 4 (SSEA-4), Gb4, Gb3, sLex, Lex, sLea, Lea, LeY, polysialic acid (PSA), sTn, Tn, TF, GD1, GD2,GD3, Fucosyl GM1, GM1, GM2, GM3, GDla, GM2, 6Gal-HS03-SiaLex or 6GluNAc-HS03-SiaLex.

### Claim 4 (depends on 1)

A pharmaceutical composition, comprising: the antibody or the antigen binding portion thereof of claim 1 and a pharmaceutical acceptable carrier.