IP Library › Granted Patent US 12,667,619
Granted Patent B2
US 12,667,619 · App. 17/050,042 · Granted Jun 30, 2026

Integrin targeting ligands and uses thereof

Inventors: Zhen Li (Westfield, NJ); Jeffrey Carlson (Madison, WI); Anthony Nicholas (Oregon, WI); Xiaokai Li (Middleton, WI); Dongxu Shu (Madison, WI); Matthew Fowler-Watters (Madison, WI)
Assignee: Arrowhead Pharmaceuticals, Inc.
A61K47/545A61K47/60A61P35/00C12N15/113C12N2310/14
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Quick Facts
Patent No.
US 12,667,619
App. No.
17/050,042
Filed
Oct 23, 2020
Granted
Jun 30, 2026
Kind
B2
Art Unit
1625
USPC
546/168
Abstract

Compounds having affinity for integrins, the synthesis of these compounds, and the use of these compounds as ligands to facilitate the delivery of cargo molecules to cells expressing integrins are described. The described integrin targeting ligands have serum stability and affinity for αvβ3 integrin and/or αvβ5 integrin, and are suitable for conjugation to cargo molecules, such as such as oligonucleotide-based therapeutic agents (e.g., RNAi agents), to facilitate delivery of the cargo molecules to cells and tissues, such as tumor cells, that express integrin αvβ3, integrin αvβ5, or both integrin αvβ3 and integrin αvβ5. Compositions that include integrin targeting ligands and methods of use are also described.

Claims (9)

1 . An integrin targeting group comprising the structure:

wherein indicates any suitable scaffold or linker that can be used to bind a ligand to an RNAi agent, indicates the RNAi agent, and “avb 3 ligand” is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2 . A composition comprising the integrin targeting group of claim 1 , and a pharmaceutically acceptable excipient.

3 . A method of delivering one or more RNAi agents to a cell expressing integrin αvβ3, in a subject, the method comprising administering to the subject a composition of claim 2 .

4 . A method of delivering one or more RNAi agents to a cell or tissue of a subject in vivo, the method comprising administering to the subject a composition of claim 2 .

5 . A method of inhibiting the expression of a target gene in a cell that expresses integrin αvβ3, in vivo, the method comprising administering to a subject an effective amount of a composition of claim 2 .

6 . The method of claim 5 , wherein the target gene is EPAS1 (HIF2 alpha).

7 . The method of claim 5 , wherein the cell is a clear cell renal carcinoma tumor cell.

Assignments (3)
SECURITY INTEREST Recorded Aug 7, 2024
From: ARROWHEAD PHARMACEUTICALS, INC.
To: SIXTH STREETLENDING PARTNERS, AS THE ADMINISTRATIVE AGENT
Reel/Frame 068510/0363 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 28, 2021
From: LI, ZHEN
To: ARROWHEAD PHARMACEUTICALS, INC.
Reel/Frame 055064/0012 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 28, 2021
From: CARLSON, JEFFREY; NICHOLAS, ANTHONY; LI, XIAOKAI; SHU, DONGXU; FOWLER-WATTERS, MATTHEW
To: ARROWHEAD PHARMACEUTICALS, INC.
Reel/Frame 055064/0262 →
Continuity (3)
Provisional Application 62790372 · Jan 9, 2019
Provisional Application 62663763 · Apr 27, 2018
Related Publication 20210093725A1 · Apr 1, 2021
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