# US 10,869,927 B2 · Human endothelin receptor antibody and use thereof

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- Number: US 10,869,927 B2
- Document ID: US10869927B2
- Status: Granted
- Kind: B2
- Application number: 16/538,509
- Filed: 2019-08-12
- Published: 2019-12-05
- Granted: 2020-12-22
- Earliest claimed: 2015-12-01
- Assignees: Gmax Biopharm LLC
- Applicants: Gmax Biopharm LLC.
- Inventors: Cheng Zhang; Hua Zhang; Xiaofeng Wang; Chenjiang Yao; Yan Jiang; Min Wang; Xinxin Shi; Hao Pan; Shuqian Jing
- Web page: https://patentgrep.com/patent/US10869927B2

## CPC

- A61K 39/39558: {against tumor tissues, cells, antigens}
- A61P 9/12: Antihypertensives
- C07K 16/26: against hormones {; against hormone releasing or inhibiting factors}
- C07K 16/28: against receptors, cell surface antigens or cell surface determinants
- C12N 5/10: Cells modified by introduction of foreign genetic material
- C12N 5/12: Fused cells, e.g. hybridomas
- C12N 15/63: Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
- A61K 2039/505: {comprising antibodies}
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 35/00: Antineoplastic agents
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/30: characterized by aspects of specificity or valency
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/70: characterized by effect upon binding to a cell or to an 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
- 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)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

The present invention discloses an antibody specifically binding to a human endothelin receptor and uses thereof, where the antibody can inhibit the functions of the human endothelin receptor. The present invention includes the preparation, cloning, expression, and characterization of the antibody. The present invention can be used to effectively treat pulmonary arterial hypertension, a disease associated with pulmonary arterial hypertension, and a reproductive organ cancer in a human.

## Claims

### Claim 1

An antibody that specifically binds to a human endothelin receptor comprising:
light chain CDR1 amino acid sequence: SEQ ID NO: 24;
light chain CDR2 amino acid sequence: SEQ ID NO: 44;
light chain CDR3 amino acid sequence: SEQ ID NO: 62;
heavy chain CDR1 amino acid sequence: SEQ ID NO: 84;
heavy chain CDR2 amino acid sequence: SEQ ID NO: 108; and
heavy chain CDR3 amino acid sequence: SEQ ID NO: 130.

### Claim 2 (depends on 1)

The antibody of claim 1, comprising
light chain variable domain amino acid sequence: SEQ ID NO: 154; and
heavy chain variable domain amino acid sequence: SEQ ID NO: 182.

### Claim 3 (depends on 2)

The antibody of claim 2, further comprising an amino acid sequence selected from:
(a) light chain constant region amino acid sequence: SEQ ID NO: 194;
(b) light chain constant region amino acid sequence: SEQ ID NO: 196;
(c) heavy chain constant region amino acid sequence: SEQ ID NO: 198;
(d) light chain constant region amino acid sequence: SEQ ID NO: 194 and heavy chain constant region amino acid sequence: SEQ ID NO: 198; and
(e) light chain constant region amino acid sequence: SEQ ID NO: 196 and heavy chain constant region amino acid sequence: SEQ ID NO: 198.

### Claim 4 (depends on 1)

The antibody of claim 1, wherein the antibody comprises:
a light chain variable domain amino acid sequence encoded by a polynucleotide sequence that is at least 80% identical to SEQ ID NO: 153; and a heavy chain variable domain amino acid sequence encoded by a polynucleotide sequence that is at least 80% identical to SEQ ID NO: 181.

### Claim 5 (depends on 1)

The antibody of claim 1, wherein the antibody is a murine antibody, a human antibody or a humanized antibody.

### Claim 6 (depends on 1)

A pharmaceutical composition comprising the antibody of claim claim 1 and a pharmaceutically acceptable excipient.

### Claim 7 (depends on 6)

The pharmaceutical composition of claim 6, wherein the antibody is a murine antibody or a humanized antibody.

### Claim 8 (depends on 6)

A kit of treating pulmonary arterial hypertension, a disease associated with pulmonary arterial hypertension, and a reproductive organ cancer, comprising the pharmaceutical composition of claim 6 and a label or instructions for use.

### Claim 9 (depends on 6)

A method of treating pulmonary arterial hypertension in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition of claim 6.