IP Library Granted Patent US 11,149,273
Granted Patent B2
US 11,149,273 · App. 16/592,644 · Granted Oct 19, 2021

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 11,149,273
App. No.
16/592,644
Granted
Oct 19, 2021
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 (19)

1. A double-stranded ribonucleic acid (dsRNA), wherein said dsRNA comprises a sense strand and an antisense strand, wherein each strand is 15-30 nucleotides in length, and wherein the antisense strand comprises a region of complementarity which is complementary to an mRNA encoding Serum amyloid A (SAA) and is complementarity to at least 15 contiguous nucleotides of SEQ ID NO:283.

2. The dsRNA of claim 1 , wherein the sense strand consists of the nucleotide sequence of SEQ ID NO:283 and the antisense strand consists of SEQ ID NO:284.

3. The dsRNA of claim 1 , wherein the sense strand consists of SEQ ID NO:127 and the antisense strand consists of SEQ ID NO:128.

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

5. 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.

6. The dsRNA of claim 1 , wherein each strand is 21 nucleotides in length.

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

8. The dsRNA of claim 1 , wherein the region of complementarity is 19-21 nucleotides in length.

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

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

11. The dsRNA of claim 1 , wherein upon administration of the dsRNA, the SAA gene is suppressed by at least 60%.

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

13. A cell comprising the dsRNA of claim 1 .

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

15. A cell comprising the vector of claim 14 .

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

17. 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.

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 Apr 20, 2020
From: DE FOUGEROLLES, ANTONIN; NOVOBRANTSEVA, TATIANA; HINKLE, GREGORY
To: ALNYLAM PHARMACEUTICALS, INC.
Reel/Frame 052445/0269 →