IP Library › Granted Patent US 12,460,206
Granted Patent B2
US 12,460,206 · App. 17/586,850 · Granted Nov 4, 2025

PCSK9 iRNA compositions and methods of use thereof

Inventors: Anna Borodovsky (Melrose, MA); Kallanthottathil G. Rajeev (Wayland, MA); Kevin Fitzgerald (Brookline, MA); Maria Frank-Kamenetsky (Brookline, MA); William Querbes (Boston, MA); Martin A. Maier (Belmont, MA); Klaus Charisse (Acton, MA); Satyanarayana Kuchimanchi (Acton, MA); Muthiah Manoharan (Weston, MA); Stuart Milstein (Arlington, MA)
Assignee: Alnylam Pharmaceuticals, Inc.
C12N15/1137A61K31/713A61K47/549C12Y304/21C12N2310/14C12N2310/312C12N2310/315C12N2310/321C12N2310/322C12N2310/343C12N2310/351C12N2310/3515C12N2320/35
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Quick Facts
Patent No.
US 12,460,206
App. No.
17/586,850
Granted
Nov 4, 2025
Kind
B2
Abstract

The invention relates to RNAi agents, e.g., double-stranded RNAi agents, targeting the PCSK9 gene, and methods of using such RNAi agents to inhibit expression of PCSK9 and methods of treating subjects having a lipid disorder, such as a hyperlipidemia.

Claims (7)

1 . A pharmaceutical composition comprising a double stranded RNAi agent that inhibits the expression of Proprotein convertase subtilisin kexin 9 (PCSK9) in a cell, comprising

an antisense strand consisting of the nucleotide sequence of 5′-asCfsaAfAfAfgCfaAfaAfcAfgGfuCfuagsasa-3′ (SEQ ID NO:1663), and

a sense strand consisting of the nucleotide sequence of 5′-csusagacCfuGfudTuugcuuuugu-3′ (SEQ ID NO:1657) and a ligand,

wherein the ligand is conjugated to the 3′-end of the nucleotide sequence of the sense strand as shown in the following schematic

wherein a, c, g, and u are 2′-O-methyl (2′-OMe) A, C, G, and U, respectively; Af, Cf, Gf, and Uf are 2′-fluoro A, C, G, and U, respectively; s is a phosphorothioate linkage; dT is 2′-deoxythymidine; and X is O,

in a sterile aqueous solution.

2 . The pharmaceutical composition of claim 1 , wherein the composition is for subcutaneous use.

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 Feb 16, 2022
From: BORODOVSKY, ANNA; RAJEEV, KALLANTHOTTATHIL G.; FITZGERALD, KEVIN; FRANK-KAMENETSKY, MARIA; QUERBES, WILLIAM; MAIER, MARTIN; CHARISSE, KLAUS; KUCHIMANCHI, SATYANARAYANA; MANOHARAN, MUTHIAH; MILSTEIN, STUART
To: ALNYLAM PHARMACEUTICALS, INC
Reel/Frame 059028/0036 →
Continuity (7)
Continuation 16155965 · Oct 10, 2018
Continuation 14650128
Provisional Application 61892188 · Oct 17, 2013
Provisional Application 61886916 · Oct 4, 2013
Provisional Application 61793530 · Mar 15, 2013
Provisional Application 61733518 · Dec 5, 2012
Related Publication 20230002772A1 · Jan 5, 2023
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