IP Library › Granted Patent US 12,618,067
Granted Patent B2
US 12,618,067 · App. 17/995,722 · Granted May 5, 2026

Targeted delivery of an inhibitor of miR-21 to macrophages for the treatment of pulmonary fibrosis

Inventors: Stefan Engelhardt (Munich, DE); Deepak Prabhu Ramanujam (Munich, DE)
Assignee: Technische Universität München
C12N15/113A61K47/549A61P11/00C12N2310/141
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Quick Facts
Patent No.
US 12,618,067
App. No.
17/995,722
Granted
May 5, 2026
Kind
B2
Abstract

The present invention relates to a composition for use in the treatment of pulmonary fibrosis of a subject, wherein the composition comprises an inhibitor of miR-21 and a moiety that delivers said inhibitor of miR-21 to a macrophage. Further, the composition may be administered by a pulmonary administration. In particular aspects, said subject to be treated suffers from pulmonary fibrosis and further has a lung disease or disorder, wherein the lung disease or disorder may be a corona virus disease. Furthermore, the invention relates to a composition, wherein the composition comprises an inhibitor of miR-21 and a moiety that delivers said inhibitor of miR-21 to a lung macrophage.

Claims (23)

1 . A method of treating pulmonary fibrosis associated with and/or caused by a viral infection, the method comprising administering to a subject in need thereof a composition comprising an inhibitor of miR-21 and a moiety that delivers said inhibitor of miR-21 selectively to a lung macrophage, wherein said moiety comprises mannose, wherein the inhibitor of miR-21 is conjugated to said moiety via a linker, and wherein:

(i) the linker is:

wherein * represents a bond to the moiety that delivers said inhibitor of miR-21 selectively to a lung macrophage and ** represents a bond to the inhibitor of miR-21; and/or

(ii) the moiety that delivers said inhibitor of miR-21 to a macrophage is:

wherein the linker is attached at the anomeric carbon at the lower right hand part of the structure.

2 . The method of claim 1 , wherein the selectively delivery means a selective and preferential binding to said macrophage over non-target cells.

3 . The method of claim 1 , wherein the composition is administered by a pulmonary administration.

4 . The method of claim 3 , wherein the composition is administered by an aerosolized composition to the lung of the subject by inhalation or by other means of local administration to the lung, bronchi and/or airways.

5 . The method of claim 1 , wherein the viral infection is a corona virus infection.

6 . The method of claim 1 , wherein the pulmonary fibrosis is associated with and/or caused by pulmonary support or mechanical ventilation, optionally following Adult/Acute Respiratory Distress Syndrome (ARDS).

7 . The method of claim 1 , wherein the composition is administered to the subject at least about 5 days after Adult/Acute Respiratory Distress Syndrome (ARDS).

8 . The method of claim 1 , wherein the composition is administered by intraarterial administration.

9 . The method of claim 1 , wherein the inhibitor of miR-21 comprises or is an antisense miRNA-21.

10 . The method of claim 9 , wherein the antisense miRNA-21 is an oligonucleotide that comprises a sequence complementary to miR-21.

11 . The method of claim 9 , wherein the antisense miRNA-21 is a locked nucleic acid (LNA) or a phosphorothioated LNA/DNA mixmer.

12 . The method of claim 1 , wherein the inhibitor of miR-21 is selected from SEQ ID NO:1, SEQ ID NO:2, SEQ ID NO:3, SEQ ID NO: 7, SEQ ID NO:8 and SEQ ID NO: 9.

13 . The method of claim 1 , wherein the composition contains the following compound, wherein the LNA-antimiR-21 is SEQ ID NO:1:

14 . The method of claim 7 , wherein the composition is further to be administered to the subject at least about 19 days after Adult/Acute Respiratory Distress Syndrome (ARDS).

15 . The method of claim 8 , wherein the composition is administered by intracardial administration, intracoronary administration, and/or by administration via inhalation.

16 . The method of claim 12 , wherein the inhibitor of miR-21 is bound to the linker via the phosphor atom of a terminal phosphorothioate group.

17 . The method of claim 1 , wherein the linker is:

wherein * represents a bond to the moiety that delivers said inhibitor of miR-21 selectively to a lung macrophage and ** represents a bond to the inhibitor of miR-21; and the moiety that delivers said inhibitor of miR-21 to a macrophage is:

wherein the linker is attached at the anomeric carbon at the lower right hand part of the structure.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 21, 2023
From: ENGELHARDT, STEFAN; RAMANUJAM, DEEPAK PRABHU
To: TECHNISCHE UNIVERSITÄT MÜNCHEN
Reel/Frame 064015/0613 →
Priority Claims (1)
EP 20169160 · Apr 9, 2020 · regional
Continuity (1)
Related Publication 20230287413A1 · Sep 14, 2023
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