# US 12,594,334 B2 · ETAR antibody, and pharmaceutical compositions and use thereof

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

- Number: US 12,594,334 B2
- Document ID: US12594334B2
- Status: Granted
- Kind: B2
- Application number: 18/155,644
- Filed: 2023-01-17
- Published: 2023-11-02
- Granted: 2026-04-07
- Earliest claimed: 2016-05-31
- Assignees: Gmax Biopharm LLC
- Applicants: Gmax Biopharm LLC.
- Inventors: Cheng Zhang; Kesuo Fan; Yong Guo; Chenjiang Yao; Hua Zhang; Xiaofeng Wang; Shuqian Jing
- Web page: https://patentgrep.com/patent/US12594334B2

## CPC

- A61K 39/39591: {Stabilisation, fragmentation}
- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/183: {Amino acids, e.g. glycine, EDTA or aspartame}
- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 35/00: Antineoplastic agents
- C07K 16/28: against receptors, cell surface antigens or cell surface determinants
- C07K 16/2869: {against hormone receptors (for antibodies against neuromediator receptors C07K16/286)}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- 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

Provided herein are a stable solution formulation of an ETAR antibody, and use thereof in treating, preventing, or alleviating one or more symptoms of pulmonary arterial hypertension or one or more symptoms of cancer of a reproductive organ.

## Claims

### Claim 1

A stable pharmaceutical solution formulation of an ETAR antibody, comprising an ETAR antibody and a buffer, wherein the formulation has a pH approximately ranging from 5 to 7; and wherein the ETAR antibody comprises light chain CDR1 amino acid sequence: SEQ ID NO: 8; light chain CDR2 amino acid sequence: SEQ ID NO: 32; light chain CDR3 amino acid sequence: SEQ ID NO: 50; heavy chain CDR1 amino acid sequence: SEQ ID NO: 70; heavy chain CDR2 amino acid sequence: SEQ ID NO: 92; and heavy chain CDR3 amino acid sequence: SEQ ID NO: 116.

### Claim 2 (depends on 1)

The formulation of claim 1, wherein the ETAR antibody comprises light chain variable domain amino acid sequence SEQ ID NO: 162 and heavy chain variable domain amino acid sequence SEQ ID NO: 190.

### Claim 3 (depends on 1)

The formulation of claim 1, wherein the ETAR antibody comprises light chain variable domain amino acid sequence SEQ ID NO: 138 and heavy chain variable domain amino acid sequence SEQ ID NO: 166.

### Claim 4 (depends on 1)

The formulation of claim 1, wherein the ETAR antibody further comprises light chain constant domain amino acid sequence SEQ ID NO: 194 or SEQ ID NO: 196; and heavy chain constant domain amino acid sequence SEQ ID NO: 198.

### Claim 5 (depends on 1)

The formulation of claim 1, wherein the ETAR antibody comprises a murine ETAR antibody or a humanized ETAR antibody.

### Claim 6 (depends on 1)

The formulation of claim 1, wherein the ETAR antibody comprises a monoclonal ETAR antibody.

### Claim 7 (depends on 1)

The formulation of claim 1, wherein the concentration of the ETAR antibody is approximately ranging from 10 to 200 mg/mL or from 10 to 100 mg/mL.

### Claim 8 (depends on 1)

The formulation of claim 1, wherein the concentration of the buffer is approximately ranging from 1 mM to 200 mM, from 2 mM to 50 mM, or from 5 mM to 25 mM.

### Claim 9 (depends on 1)

The formulation of claim 1, wherein the buffer comprises a salt of citric acid or histidine.

### Claim 10 (depends on 1)

The formulation of claim 1, further comprising a surfactant.

### Claim 11 (depends on 10)

The formulation of claim 10, wherein the surfactant comprises a polysorbate.

### Claim 12 (depends on 11)

The formulation of claim 11, wherein the surfactant comprises polysorbate 20 or polysorbate 80.

### Claim 13 (depends on 10)

The formulation of claim 10, wherein the concentration of the surfactant is approximately ranging from 0.001 to 1 weight/volume percent, from 0.01 to 0.5 weight/volume percent, or from 0.01 to 0.1 weight/volume percent.

### Claim 14 (depends on 1)

The formulation of claim 1, further comprising an amino acid protectant.

### Claim 15 (depends on 14)

The formulation of claim 14, wherein the amino acid protectant comprises arginine or a salt thereof.

### Claim 16 (depends on 14)

The formulation of claim 14, wherein the concentration of the amino acid protectant is approximately ranging from 1 mM to 500 mM or from 10 mM to 200 mM.

### Claim 17 (depends on 1)

The formulation of claim 1, further comprising a polyol protectant.

### Claim 18 (depends on 17)

The formulation of claim 17, wherein the concentration of the polyol protectant is approximately ranging from 0.1 to 50 weight/volume percent, from 1 to 20 weight/volume percent, or from 1 to 10 weight/volume percent.

### Claim 19 (depends on 1)

The formulation of claim 1, further comprising a metal chelator.

### Claim 20 (depends on 19)

The formulation of claim 19, wherein the concentration of the metal chelator is approximately ranging from 0.001 mM to 1 mM, from 0.005 mM to 0.5 mM, or from 0.01 mM to 0.2 mM.

### Claim 21 (depends on 1)

A method of reducing pulmonary arterial hypertension in a subject, comprising administering to the subject a therapeutically effective amount of the formulation of claim 1.