# US 11,298,370 B2 · Prophylactic or therapeutic agent for inflammatory bowel disease

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- Number: US 11,298,370 B2
- Document ID: US11298370B2
- Status: Granted
- Kind: B2
- Application number: 16/607,681
- Filed: 2018-04-24
- Published: 2020-06-18
- Granted: 2022-04-12
- Earliest claimed: 2017-04-24
- Applicants: Hirofumi Yamamoto; Masaki Mori
- Inventors: Hirofumi Yamamoto; Masaki Mori
- Web page: https://patentgrep.com/patent/US11298370B2

## CPC

- A61K 31/7105: Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 9/143: {with inorganic compounds}
- A61K 47/51: the non-active ingredient being a modifying agent
- A61K 47/6923: {the form being an inorganic particle, e.g. ceramic particles, silica particles, ferrite or synsorb}
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- 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)

## Abstract

The purpose of the present invention is to provide a therapeutic agent which is for inflammatory bowel disease and exhibits superior prophylactic or therapeutic effects on inflammatory bowel disease by using miR-29a and/or miR-29b. The prophylactic or therapeutic agent for inflammatory bowel disease comprises composite particles in which miR-29a and/or miR-29b is/are carried on carbonate apatite particles, and said agent is administered systemically.

## Claims

### Claim 1

A method of treating an inflammatory bowel disease, comprising systemically administering composite particles having miR-29a and/or miR-29b carried on a carbonate apatite particle to a patient in need of treatment of the inflammatory bowel disease, wherein the carbonate apatite particles have an average particle diameter of 400 nm to 3000 nm, wherein the miR-29a and/or miR-29b is internalized into cells of an inflammatory bowel disease lesion and into dendritic cells localizing on a mucosa of the lesion, wherein the inflammatory bowel disease is effectively improved by an action of the miR-29a and/or miR-29b uptake directly into the cells of the lesion and by an action of the dendritic cells that have taken up the miR-29a and/or miR-29b.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the systemic administration is intravascular administration.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the composite particles comprise miR-29a.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the composite particles comprise miR-29b.

### Claim 5 (depends on 1)

The method according to claim 1, wherein the composite particles comprise miR-29a and miR-29b.

### Claim 6 (depends on 1)

The method according to claim 1, wherein the systemic administration is subcutaneous administration.

### Claim 7 (depends on 1)

The method according to claim 1, wherein the carbonate apatite particles have an average particle diameter of greater than 50 nm and 3000 nm or smaller.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the miR-29a and/or miR-29b carried on the carbonate apatite particles is selected from the group consisting of a mature miRNA, a hairpin type precursor miRNA (pri-miRNA), and a pre-miRNA in which a part of the pri-miRNA is cleaved.

### Claim 9 (depends on 1)

The method according to claim 1, wherein the miR-29a and/or the miR-29b are adsorbed to and carried on the carbonate apatite particle through an ionic bond or a hydrogen bond.

### Claim 10 (depends on 1)

The method according to claim 1, wherein the inflammatory bowel disease is ulcerative colitis.

### Claim 11 (depends on 1)

The method according to claim 1, wherein the inflammatory bowel disease is Crohn's disease.
