IP Library Granted Patent US 10,590,423
Granted Patent B2
US 10,590,423 · App. 16/042,833 · Granted Mar 17, 2020

Treatment of age-related macular degeneration using RNA complexes that target MyD88 or TLR3

Inventors: Dong-ki Lee (Seoul, KR); Sun Woo Hong (Seoul, KR); Isu Hong (Seoul, KR); Jihye Hwang (Geonggi-Do, KR)
Assignee: OliX Pharmaceuticals, Inc.
C12N15/1138C12N15/113C12N2310/14C12N2310/315C12N2310/321C12N2320/32
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Quick Facts
Patent No.
US 10,590,423
App. No.
16/042,833
Granted
Mar 17, 2020
Kind
B2
Abstract

In certain aspects, provided herein are RNA complexes that inhibit Myeloid differentiation primary response gene 88 (MyD88) and/or Toll-like receptor 3 (TLR3) and are useful in the treatment of age-related macular degeneration (AMD). In certain aspects, provided herein are pharmaceutical compositions comprising such RNA complexes and methods of using such RNA complexes and pharmaceutical compositions.

Claims (23)

1. A method of treating age-related macular degeneration (AMD) in a subject, comprising administering to the subject an RNA duplex of an antisense strand of at least 19 nucleotides (nt) in length and a sense strand of 16 nt in length, wherein:

the sequence of the antisense strand comprises SEQ ID NO: 54 or SEQ ID NO: 56;

the sequence of the sense strand is SEQ ID NO: 53 or SEQ ID NO: 55;

a cholesterol moiety is attached to the 3′ end of the sense strand; and

the antisense strand and the sense strand form a complex in which the 5′ end of the antisense strand and the 3′ end of the sense strand form a blunt end.

2. The method of claim 1 , wherein the antisense strand is 19 to 21 nt in length.

3. The method of claim 1 , wherein the antisense strand is 24 to 121 nt in length.

4. The method of claim 1 , wherein the RNA duplex is capable of inhibiting MyD88 expression by a cell.

5. The method of claim 1 , wherein the RNA duplex is delivered to cells using a delivery vehicle.

6. The method of claim 1 , wherein the RNA duplex further comprises a 2′-O-methylated nucleoside and/or a phosphorothioate bond.

7. The method of claim 6 , wherein the RNA duplex comprises a 2′-O-methylated nucleoside positioned at the 3′ end of the sense strand and/or at the 3′ end of the antisense strand.

8. The method of claim 6 , wherein the RNA duplex comprises a phosphorothioate bond.

9. The method of claim 1 , wherein the RNA duplex is capable of penetrating the cellular membrane of a cell in the absence of a delivery vehicle.

10. The method of claim 1 , wherein the sequence of the antisense strand is SEQ ID NO: 54 or SEQ ID NO: 95, and sequence of the sense strand is SEQ ID NO: 53.

11. The method of claim 1 , wherein the sequence of the antisense strand is SEQ ID NO: 56 or SEQ ID NO: 98, and the sequence of the sense strand is SEQ ID NO: 55.

12. The method of claim 3 , wherein the RNA duplex comprises a 2′-O-methylated nucleoside positioned at the 3′ end of the sense strand and/or at the 3′ end of the antisense strand.

13. The method of claim 1 , wherein the AMD is wet AMD.

14. The method of claim 1 , wherein the AMD is dry AMD.

15. The method of claim 1 , comprising administering a second agent for treatment of AMD.

16. The method of claim 15 , wherein the second agent is an anti-vascular endothelial growth factor (VEGF) therapeutic.

17. The method of claim 1 , comprising administering the RNA complex duplex to the eye of the subject.

18. The method of claim 1 , wherein the RNA complex duplex is administered by intravitreal injection.

19. The method of claim 1 , wherein the RNA duplex is administered as a pharmaceutically acceptable formulation.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 29, 2020
From: LEE, DONG-KI; HONG, SUN WOO; HONG, ISU; HWANG, JIHYE
To: OLIX PHARMACEUTICALS, INC.
Reel/Frame 051659/0482 →
Continuity (3)
Division 15352322 · Nov 15, 2016
Provisional Application 62255878 · Nov 16, 2015
Related Publication 20180327755A1 · Nov 15, 2018
Cited By (1)
US 12,686,867