# US 2020/0399315 A1 · Ultra-pure agonists of guanylate cyclase c, method of making and using same

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- Number: US 2020/0399315 A1
- Document ID: US20200399315A1
- Status: Published application
- Kind: A1
- Application number: 16/921,450
- Filed: 2020-07-06
- Published: 2020-12-24
- Earliest claimed: 2013-06-05
- Assignees: Bausch Health Ireland Limited
- Applicants: Bausch Health Ireland Limited
- Inventors: Kunwar Shailubhai; Stephen Comiskey; Rong Feng; Juncai Bai; Ruoping Zhang; Jun Jia; Junfeng Zhou; Qiao Zhao; Guoqing Zhang
- Web page: https://patentgrep.com/patent/US20200399315A1

## CPC

- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- A61K 38/10: Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- B01D 15/424: {Elution mode}
- C07K 1/14: Extraction; Separation; Purification
- C12N 9/88: Lyases (4.)
- C12Y 406/01002: Guanylate cyclase (4.6.1.2)
- 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)
- B01D: SEPARATION (separating solids from solids by wet methods B03B, B03D; by pneumatic jigs or tables B03B; by other dry methods B07; magnetic or electrostatic separation of solid materials from solid materials or fluids, separation by high-voltage electric fields B03C; centrifuges, vortex apparatus B04; presses per se for squeezing-out liquid from liquid-containing material B30B9/02; treatment of water C02F, e.g. softening by ion-exchange C02F1/42; {arrangements of air intake cleaners in gas turbine plants F02C7/05} ; arrangements or mounting of filters in air-conditioning, air-humidification or ventilation F24F13/28)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- C12Y: ENZYMES

## Abstract

The invention provides processes of purifying a peptide including a GCC agonist sequence selected from the group consisting of SEQ ID NOs: 1-251 described herein. The processes include a solvent exchange step before a freeze-drying (lyophilization) step.

## Claims

### Claim at position 1

-28. (canceled)

### Claim 29

An oral formulation comprising:
(a) a purified peptide comprising the Guanylate Cyclase-C(GCC) agonist of amino acid sequence of SEQ ID NO: 1, wherein the purified peptide is substantially free of trifluoroacetic acid (TFA); and
(b) one or more pharmaceutically acceptable excipients, wherein the one or more pharmaceutically acceptable excipients comprises microcrystalline cellulose.

### Claim 30 (depends on 29)

The oral formulation of claim 29, wherein the purified peptide comprises less than 0.05% TFA by weight of the purified peptide.

### Claim 31 (depends on 29)

The oral formulation of claim 29, comprising 0.01 mg to 10 mg of the purified peptide.

### Claim 32 (depends on 31)

The oral formulation of claim 31, comprising 0.1 mg to 5 mg of the purified peptide.

### Claim 33 (depends on 32)

The oral formulation of claim 32, comprising 3 mg of the purified peptide.

### Claim 34 (depends on 29)

The oral formulation of claim 29, wherein the purified peptide has an average particle size of 80-120 μm.

### Claim 35 (depends on 29)

The oral formulation of claim 29, wherein the one or more pharmaceutically acceptable excipients further comprises magnesium stearate.