IP Library Granted Patent US 12,350,247
Granted Patent B2
US 12,350,247 · App. 18/295,907 · Granted Jul 8, 2025

Use of APE1/Ref-1 inhibitors for treatment of retinal diseases

Inventors: Mark R. Kelley (Zionsville, IN); Melissa L. Fishel (Fishers, IN)
Assignee: Indiana University Research and Technology Corporation
A61K31/201A61K31/165A61K31/18A61K31/192A61K31/20A61K31/282A61K31/337A61K31/343A61K31/501A61K31/519A61K31/7068A61K31/713A61K33/243A61K45/06A61P35/00
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Quick Facts
Patent No.
US 12,350,247
App. No.
18/295,907
Granted
Jul 8, 2025
Kind
B2
Abstract

Combination therapies including a Apurinic/Apyrimidinic Endonuclease/reduction-oxidation (redox) Factor-1 (APE1/Ref-1) inhibitor specific to inhibit the redox function of APE1/Ref-1 are disclosed herein. The Combination therapies can be used for treating various cancers, as well as other angiogenesis-mediated diseases (e.g., retinal diseases, cardiovascular diseases).

Claims (7)

1. A method of treating retinopathy of prematurity (ROP) in a subject in need thereof, the method comprising administering to the subject [(2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methylidene]-N,N-diethylpentanamide] (APX2009).

2. The method as set forth in claim 1 further comprising administering a second therapeutic agent.

3. The method as set forth in claim 2 , wherein the second therapeutic agent is selected from the group consisting of doxorubicin, endostatin, 5-fluorouracil (5-FU), bortezomib, ispinesib mesylate, SN-38, topotecan, paclitaxel, bryostatin 1, trametinib, LAQ824, vinblastine, BEZ235, panobinostat, methotrexate, temsirolimus, FK866, afatinib, tozasertib, irinotecan, GSK2126458, CPI-613, γ-secretase inhibitors, DLL4-inhibiting antibodies, and combinations thereof.

4. A method of treating neovascularization in a subject in need thereof, the method comprising administering to the subject [(2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methylidene]-N,N-diethylpentanamide] (APX2009).

5. The method as set forth in claim 4 , wherein the neovascularization is selected from the group consisting of retinal neovascularization and choroidal neovascularization (CNV).

6. The method as set forth in claim 4 further comprising administering a second therapeutic agent.

7. The method as set forth in claim 6 , wherein the second therapeutic agent is selected from the group consisting of doxorubicin, endostatin, 5-fluorouracil (5-FU), bortezomib, ispinesib mesylate, SN-38, topotecan, paclitaxel, bryostatin 1, trametinib, LAQ824, vinblastine, BEZ235, panobinostat, methotrexate, temsirolimus, FK866, afatinib, tozasertib, irinotecan, GSK2126458, CPI-613, γ-secretase inhibitors, DLL4-inhibiting antibodies, and combinations thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 5, 2023
From: KELLEY, MARK R.; FISHEL, MELISSA L.
To: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
Reel/Frame 063227/0650 →
Continuity (5)
Division 17026671 · Sep 21, 2020
Continuation 16092812
Provisional Application 62521082 · Jun 16, 2017
Provisional Application 62473528 · Mar 20, 2017
Related Publication 20230293471A1 · Sep 21, 2023
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