Double stranded RNA specifically inhibiting expression of IL-23 and pharmaceutical composition comprising same

Patent metadata

Field	Value
Publication number	US-12442001-B2
Application number	US-202117916060-A
Country	US
Kind code	B2
Filing date	Apr 2, 2021
Priority date	Apr 3, 2020
Publication date	Oct 14, 2025
Grant date	Oct 14, 2025

Abstract

The present invention provides a novel siRNA specifically inhibiting the expression of IL-23 and a pharmaceutical composition comprising the siRNA specifically a double stranded RNA comprising a sense strand and an antisense strand wherein each strand has 19 to 30 nucleotides and comprises the base sequence selected from SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5 or SEQ ID NO: 6 or a complementary base sequence thereof and a pharmaceutical composition comprising the double stranded RNA.

First claim

The invention claimed is:

1. A double stranded RNA comprising a sense strand and an antisense strand, wherein each of the strands has 19 to 30 nucleotides and comprises a base sequence selected from SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5 or SEQ ID NO: 6 or a complementary base sequence thereof.

2. The double stranded RNA according to claim 1 , wherein each of the strands has 19 to nucleotides.

3. The double stranded RNA according to claim 1 , wherein one or more nucleotides within each of the strands are chemically modified or the 5′-terminal or 3′-terminal nucleotide in each of the strands is chemically modified.

4. The double stranded RNA according to claim 3 , wherein said chemical modification is selected from the group consisting of phosphorothioate modification, 2′-F modification, 2′-OMe modification, 2′-MOE modification, LNA modification and ENA modification.

5. The double stranded RNA according to claim 1 , which comprises 1 to 10 deoxyribonucleotides in the 3′-end of the sense strand and the 5′-end of the antisense strand.

6. The double stranded RNA according to claim 5 , which comprises 2 thymidines (dTs) in the 3′-end of the sense strand and the 5′-end of the antisense strand.

7. The double stranded RNA according to claim 1 for specifically inhibiting the expression of IL-23.

8. A pharmaceutical composition comprising the double stranded RNA according to claim 1 .

9. The pharmaceutical composition according to claim 8 , which further comprises an aliphatic carboxylic acid-based ionic liquid.

10. The pharmaceutical composition according to claim 9 , wherein the aliphatic carboxylic acid-based ionic liquid is a mixed ionic liquid comprising two or more aliphatic carboxylic acid-based ionic liquids.

11. The pharmaceutical composition according to claim 10 , wherein the mixed ionic liquid is
a) one or more aliphatic carboxylic acid-based ionic liquids of 2 to 7 carbon atoms consisting of a lower aliphatic carboxylic acid of 2 to 7 carbon atoms and any of ethanolamine, diethanolamine or triethanolamine, and
b) an aliphatic carboxylic acid-based ionic liquid of 2 to 20 carbon atoms in which the solubility of the double stranded RNA is 1 w/w % or less.

12. The pharmaceutical composition according to claim 8 which is a transdermal absorption preparation.

13. The pharmaceutical composition according to claim 8 for treating a disease associated with the expression of IL-23.

14. The pharmaceutical composition according to claim 13 , wherein the disease is psoriasis.

Assignees

• Medrx Co Ltd

Inventors

• Miwa Yasushi
• Hamamoto Hidetoshi
• Ishida Tatsuhiro

Classifications

• C12N2310/30

  Chemical structure · CPC title

• C12N2310/11

  Antisense · CPC title

• A61P17/06 Primary

  Antipsoriatics · CPC title

• C12N2320/51

  modulating the chemical stability, e.g. nuclease-resistance · CPC title

• C12N2320/11

  for the determination of target sites, i.e. of active nucleic acids · CPC title