IP Library Granted Patent US 10,472,628
Granted Patent B2
US 10,472,628 · App. 15/847,631 · Granted Nov 12, 2019

Lipid formulated compositions and methods for inhibiting expression of Serum Amyloid A gene

Inventors: Antonin de Fougerolles (Brookline, MA); Tatiana Novobrantseva (Wellesley, MA); Gregory Hinkle (Plymouth, MA)
Assignee: Alnylam Pharmaceuticals, Inc.
C12N15/113A61K31/713C12N2310/11C12N2310/14C12N2310/321C12N2310/344C12N2310/3515
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Quick Facts
Patent No.
US 10,472,628
App. No.
15/847,631
Granted
Nov 12, 2019
Kind
B2
Abstract

The invention relates to a double-stranded ribonucleic acid (dsRNA) targeting a Serum Amyloid A (SAA) gene, and methods of using the dsRNA to inhibit expression of SAA.

Claims (22)

1. A double-stranded ribonucleic acid (dsRNA), wherein said dsRNA comprises a sense strand consisting of the nucleotide sequence of SEQ ID NO:189 and an antisense strand consisting of the nucleotide sequence of SEQ ID NO:190.

2. The dsRNA of claim 1 , wherein the sense strand consists of SEQ ID NO:33 and the antisense strand consists of SEQ ID NO:34.

3. The dsRNA of claim 1 , comprising at least one modified nucleotide.

4. The dsRNA of claim 1 , comprising at least one modified nucleotide selected from the group consisting of: a 2′-O-methyl modified nucleotide, a nucleotide comprising a 5′-phosphorothioate group, a terminal nucleotide linked to a cholesteryl derivative or dodecanoic acid bisdecylamide group, a 2′-deoxy-2′-fluoro modified nucleotide, a 2′-deoxy-modified nucleotide, a locked nucleotide, an abasic nucleotide, a 2′-amino-modified nucleotide, a 2′-alkyl-modified nucleotide, a morpholino nucleotide, a phosphoramidate, a 2′-O-methylcytidine-5′-phosphate, a 2′-O-methyluridine-5′-phosphate, and a non-natural base comprising nucleotide.

5. The dsRNA of claim 1 , comprising a dTdT overhang on the 3′ end of each strand.

6. The dsRNA of claim 1 , wherein the dsRNA is conjugated to a ligand.

7. The dsRNA of claim 1 , wherein the dsRNA is formulated in a lipid formulation.

8. The dsRNA of claim 1 , wherein administration of the dsRNA to a cell results in 92% inhibition of SAA mRNA expression as measured by a real time PCR assay or 85% inhibition of SAA mRNA expression as measured by a branched DNA assay or 100% inhibition of SAA protein expression as measured by a ELISA assay compared to an siRNA control.

9. The dsRNA of claim 1 , wherein the dsRNA has an IC50 of less than 10 pM as measured by a branched DNA assay.

10. A cell comprising the dsRNA of claim 1 .

11. A vector comprising a nucleotide sequence encoding at least one strand of the dsRNA of claim 1 .

12. A cell comprising the vector of claim 11 .

13. A pharmaceutical composition for inhibiting expression of an SAA gene comprising the dsRNA of claim 1 .

14. A method of inhibiting SAA expression in a cell, the method comprising:

(a) introducing into the cell the dsRNA of claim 1 ; and

(b) maintaining the cell produced in step (a) for a time sufficient to obtain degradation of the mRNA transcript of an SAA gene, thereby inhibiting expression of the SAA gene in the cell.

15. The method of claim 14 , wherein the method is performed in vitro.

16. A pharmaceutical composition for inhibiting expression of an SAA gene comprising the dsRNA of claim 2 .

17. A method of inhibiting SAA expression in a cell, the method comprising:

(a) introducing into the cell the dsRNA of claim 2 ; and

(b) maintaining the cell produced in step (a) for a time sufficient to obtain degradation of the mRNA transcript of an SAA gene, thereby inhibiting expression of the SAA gene in the cell.

18. The method of claim 17 , wherein the method is performed in vitro.

Assignments (2)
SECURITY INTEREST Recorded Oct 1, 2025
From: ALNYLAM PHARMACEUTICALS, INC.; SIRNA THERAPEUTICS, INC.
To: BANK OF AMERICA, N.A.
Reel/Frame 072996/0337 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 25, 2018
From: DE FOUGEROLLES, ANTONIN; NOVOBRANTSEVA, TATIANA; HINKLE, GREGORY
To: ALNYLAM PHARMACEUTICALS, INC.
Reel/Frame 044733/0819 →
Cited By (2)
US 12,378,560 US 12,691,166