IP Library › Granted Patent US 11,351,130
Granted Patent B2
US 11,351,130 · App. 16/850,436 · Granted Jun 7, 2022

Prevention and reversal of inflammation induced DNA damage

Inventors: Mark R. Kelley (Zionsville, IN); Jill Fehrenbacher (Indianapolis, IN)
Assignee: Indiana University Research and Technology Corporation
A61K31/192A61K31/165A61K31/201A61K31/555A61K33/243A61K45/06A61N5/00A61P25/02A61K31/282
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Quick Facts
Patent No.
US 11,351,130
App. No.
16/850,436
Granted
Jun 7, 2022
Kind
B2
Abstract

Methods of reducing neuronal sensitivity, thereby reducing inflammation and chronic pain, in subjects having diabetes are disclosed herein. Particularly disclosed are methods of administrating the apurinic/apyrimidinic endonuclease 1 redox factor 1 (APE 1/Ref-1) inhibitor, APX3330, to enhance the DNA base excision repair (BER) pathway, thereby reducing neuronal sensitivity to inflammatory mediators and alleviating inflammatory or chronic pain.

Claims (14)

1. A method of treating inflammation and chronic pain in a subject suffering from diabetes, the method comprising administering to the subject an effective amount of an apurinic/apyrimidinic endonuclease 1 redox factor 1 (APE1/Ref-1) inhibitor and at least one additional therapeutic agent selected from the group consisting of platinum drugs, taxanes, doxorubicin, alkaloids, thalidomide, lenolidomide, pomalidomide, bortexomib, carfilzomib, eribulin, ionizing radiation, cisplatin, oxaliplatin and combinations thereof, wherein the APE1/Ref-1 inhibitor is selected from the group consisting of 3-[5-(2,3-dimethoxy-6-methyl-1,4-benzoquinoyl)]-2-nonyl-2-propenoic acid], (APX3330); [(2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methylidene]-N,N-diethylpentanamide] (APX2009), (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N,N-dimethylpentanamide] (APX2007), (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N-methoxypentanamide] (APX2014), (2E)-2-(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N,N,2-trimethylprop-2-enamide (APX2032), pharmaceutically acceptable salts and pharmaceutically acceptable solvates thereof, and combinations thereof, pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, which selectively inhibits the amino terminal portion of APE1.

2. The method as set forth in claim 1 , wherein the APE1/Ref-1 inhibitor is selected from the group consisting of 3-[5-(2,3-dimethoxy-6-methyl-1,4-benzoquinoyl)]-2-nonyl-2-propenoic acid], (APX3330); [(2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methylidene]-N,N-diethylpentanamide] (APX2009) and (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N-methoxypentanamide] (APX2014).

3. The method as set forth in claim 1 , wherein the at least one additional therapeutic agent is selected from the group consisting of platinum drugs, ionizing radiation and combinations thereof.

4. The method as set forth in claim 1 , wherein the APE1/Ref-1 inhibitor is APX3330 and the subject is administered from about 5 μM to about 50 μM APX3330.

5. A method of enhancing the DNA base excision repair (BER) pathway in a subject suffering from diabetes, the method comprising administering to the subject an effective amount of an apurinic/apyrimidinic endonuclease 1 redox factor 1 (APE1/Ref-1) inhibitor and at least one additional therapeutic agent selected from the group consisting of platinum drugs, taxanes, doxorubicin, alkaloids, thalidomide, lenolidomide, pomalidomide, bortexomib, carfilzomib, eribulin, ionizing radiation, cisplatin, oxaliplatin and combinations thereof, wherein the APE1/Ref-1 is selected from the group consisting of 3-[5-(2,3-dimethoxy-6-methyl-1,4-benzoquinoyl)]-2-nonyl-2-propenoic acid], (APX3330); [(2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methylidene]-N,N-diethylpentanamide] (APX2009), (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N,N-dimethylpentanamide] (APX2007), (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N-methoxypentanamide] (APX2014), (2E)-2-(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N,N,2-trimethylprop-2-enamide (APX2032), pharmaceutically acceptable salts and pharmaceutically acceptable solvates thereof, and combinations thereof, pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, which selectively inhibits the amino terminal portion of APE1.

6. The method as set forth in claim 5 , wherein the APE1/Ref-1 inhibitor is selected from the group consisting of 3-[5-(2,3-dimethoxy-6-methyl-1,4-benzoquinoyl)]-2-nonyl-2-propenoic acid], (APX3330); [(2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methylidene]-N,N-diethylpentanamide] (APX2009) and (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N-methoxypentanamide] (APX2014).

7. The method as set forth in claim 5 , wherein the at least one additional therapeutic agent is selected from the group consisting of platinum drugs, ionizing radiation and combinations thereof.

8. The method as set forth in claim 5 , wherein the APE1/Ref-1 inhibitor is APX3330 and the subject is administered from about 5 μM to about 50 μM APX3330.

9. A method of treating inflammation and chronic pain in a subject suffering from diabetes, the method comprising administering to the subject an effective amount of an apurinic/apyrimidinic endonuclease 1 redox factor 1 (APE1/Ref-1) inhibitor selected from the group consisting of [(2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methylidene]-N,N-diethylpentanamide] (APX2009), (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N,N-dimethylpentanamide] (APX2007), (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N-methoxypentanamide] (APX2014), (2E)-2-(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N,N,2-trimethylprop-2-enamide (APX2032), pharmaceutically acceptable salts and pharmaceutically acceptable solvates thereof, and combinations thereof, pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, which selectively inhibits the amino terminal portion of APE1.

10. The method as set forth in claim 9 further comprising administering at least one additional therapeutic agent selected from the group consisting of platinum drugs, taxanes, doxorubicin, alkaloids, thalidomide, lenolidomide, pomalidomide, bortexomib, carfilzomib, eribulin, ionizing radiation and combinations thereof.

11. The method as set forth in claim 9 further comprising administering at least one additional therapeutic agent selected from the group consisting of cisplatin and oxaliplatin to the subject.

12. A method of enhancing the DNA base excision repair (BER) pathway in a subject suffering from diabetes, the method comprising administering to the subject an effective amount of an apurinic/apyrimidinic endonuclease 1 redox factor 1 (APE1/Ref-1) inhibitor selected from the group consisting of [(2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methylidene]-N,N-diethylpentanamide] (APX2009), (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N,N-dimethylpentanamide] (APX2007), (2E)-2-[(3-methoxy-1,4-dioxo-1,4-dihydronapthalen-2-yl)methylidene]-N-methoxypentanamide] (APX2014), (2E)-2-(3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N,N,2-trimethylprop-2-enamide (APX2032), pharmaceutically acceptable salts and pharmaceutically acceptable solvates thereof, and combinations thereof, pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, which selectively inhibits the amino terminal portion of APE1.

13. The method as set forth in claim 12 further comprising administering at least one additional therapeutic agent selected from the group consisting of platinum drugs, taxanes, doxorubicin, alkaloids, thalidomide, lenolidomide, pomalidomide, bortexomib, carfilzomib, eribulin, ionizing radiation and combinations thereof.

14. The method as set forth in claim 12 further comprising administering at least one additional therapeutic agent selected from the group consisting of cisplatin and oxaliplatin to the subject.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 16, 2020
From: KELLEY, MARK R.; FEHRENBACHER, JILL
To: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
Reel/Frame 052417/0506 →
Continuity (3)
Continuation 16092816
Provisional Application 62486033 · Apr 17, 2017
Related Publication 20200253904A1 · Aug 13, 2020
Cited By (2)
US 12,312,308 US 12,350,247