IP Library Granted Patent US 11,236,339
Granted Patent B2
US 11,236,339 · App. 16/306,831 · Granted Feb 1, 2022

Modulation of GYS1 expression

Inventors: Tamar R. Grossman (La Jolla, CA); Susan M. Freier (San Diego, CA); Berge Minassian (Toronto, CA); Saija Ahonen (Toronto, CA)
Assignees: Ionis Pharmaceuticals, Inc.; The Hospital for Sick Children
C12N15/1137A61K31/7088A61K45/06A61P3/08A61P25/28C12N15/113C12N2310/11C12N2310/315C12N2310/321C12N2310/3341C12N2310/341C12N2320/30
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Quick Facts
Patent No.
US 11,236,339
App. No.
16/306,831
Granted
Feb 1, 2022
Kind
B2
Abstract

Provided herein are methods, compounds, and compositions for reducing expression of GYS1 in an individual. Such methods, compounds, and compositions are useful to treat, prevent, delay, or ameliorate a glycogen storage disease or disorder in an individual in need.

Claims (25)

1. A method of treating Lafora disease in an individual having Lafora disease comprising administering to the individual a compound comprising a modified oligonucleotide consisting of 15 to 30 nucleosides, wherein the modified oligonucleotide has a nucleobase sequence at least 95% complementary to an equal length portion of the nucleobase sequence of any one of SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, or SEQ ID NO: 5, wherein at least one internucleoside linkage of the modified oligonucleotide is a phosphorothioate internucleoside linkage, and wherein Lafora bodies are reduced in a cell in the individual, thereby treating the Lafora disease in the individual.

2. The method of claim 1 , wherein the compound is single-stranded.

3. The method of claim 1 , wherein the modified oligonucleotide comprises at least one modified nucleobase or at least one modified sugar moiety.

4. The method of claim 3 , wherein the at least one modified nucleobase is a 5-methylcytosine.

5. The method of claim 3 , wherein the at least one modified sugar moiety is a bicyclic sugar moiety.

6. The method of claim 1 , wherein the modified oligonucleotide comprises:

a gap segment consisting of linked deoxynucleosides;

a 5′ wing segment consisting of linked nucleosides; and

a 3′ wing segment consisting of linked nucleosides;

wherein the gap segment is positioned immediately adjacent to and between the 5′ wing segment and the 3′ wing segment and wherein each nucleoside of each wing segment comprises a modified sugar.

7. The method of claim 6 , wherein the modified sugar moiety of each wing segment is a 2′-O-methyoxyethyl, and wherein each cytosine of said modified oligonucleotide is a 5-methylcytosine.

8. The method of claim 5 , wherein the bicyclic sugar moiety comprises a 4′-CH(CH 3 )—O-2′ bridge or a 4′-(CH 2 )n-O-2′ bridge, wherein n is 1 or 2.

9. The method of claim 3 , wherein the at least one modified sugar moiety is a non-bicyclic moiety.

10. The method of claim 9 , wherein the non-bicyclic moiety is selected from 2′-F, 2′-OMe, and 2′-MOE.

11. The method of claim 1 , wherein the modified oligonucleotide comprises at least one modified nucleoside comprising a sugar surrogate.

12. The method of claim 11 , wherein the sugar surrogate is selected from morpholino and PNA.

13. The method of claim 1 , wherein the modified oligonucleotide is a gapmer.

14. The method of claim 1 , wherein the modified oligonucleotide comprises:

a gap segment consisting of 7-12 linked deoxynucleosides;

a 5′ wing segment consisting of 1-5 linked nucleosides; and

a 3′ wing segment consisting of 1-5 linked nucleosides;

wherein the gap segment is positioned immediately adjacent to and between the 5′ wing segment and the 3′ wing segment and wherein each nucleoside of each wing segment comprises a modified sugar.

15. The method of claim 1 , wherein at least one internucleoside linkage of the modified oligonucleotide is a phosphodiester internucleoside linkage.

16. The method of claim 1 , wherein the modified oligonucleotide consists of 15-25, 16-20, 18-22, or 18-20 linked nucleosides.

17. The method of claim 1 , wherein the individual is a human.

Continuity (3)
Provisional Application 62430106 · Dec 5, 2016
Provisional Application 62351396 · Jun 17, 2016
Related Publication 20190194666A1 · Jun 27, 2019