IP Library Granted Patent US 10,925,963
Granted Patent B2
US 10,925,963 · App. 15/189,655 · Granted Feb 23, 2021

Combination artemisinin and chemiluminescent photodynamic therapy and uses therefor

Inventors: Daniel E. Goldberg (St. Louis, MO); Paul Sigala (St. Louis, MO)
A61K41/0061A61K31/197A61K31/366A61K31/502Y02A50/30
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Quick Facts
Patent No.
US 10,925,963
App. No.
15/189,655
Granted
Feb 23, 2021
Kind
B2
Abstract

Photodynamic therapy-based methods of treating diseases such as cancer and malaria are disclosed. These methods include administering 5-aminolevulinic acid (ALA), luminol and artemisinin (ART). ART and ALA administered in combination with luminol can kill malaria parasites without host toxicity. In some aspects, the methods further include administration of a luminol enhancer such as 4-iodophenol. The disclosed methods can also be used to remove potential malaria pathogens from the blood supply.

Claims (20)

1. A method of killing intraerythrocytic parasites, the method comprising contacting the parasites with therapeutically effective amount of a combination of 5-aminolevulinic acid or a derivative thereof, luminol or a derivative thereof, and artemisinin or a derivative thereof.

2. The method of claim 1 , further comprising administering a therapeutically effective amount of 4-iodophenol.

3. The method of claim 1 , wherein the artemisinin or derivative thereof is selected from the group consisting of artemisinin, artesunate, artemether, dihydroartesmisinin, artelinic acid, and artemotil.

4. The method of claim 1 , wherein the artemisinin or derivative thereof is dihydroartesmisinin.

5. The method of claim 1 , wherein the artemisinin or derivative thereof is administered at a sub-therapeutic dose.

6. The method of claim 5 , wherein the sub-therapeutic dose is ≤10% of the EC 50 of the artemisinin or derivative thereof.

7. The method of claim 1 , wherein the luminol or derivative thereof is selected from the group consisting of lumino, luminol sodium salt, luminol hemihydrate, luminol hydrochloride, isoluminol, isoluminol monohydrate, and N-(4-aminobutyl)-N-ethyl-isoluminol (ASEI).

8. The method of claim 1 , wherein the 5-aminolevulinic acid or derivative thereof is selected from the group consisting of 5-aminolevulinic acid (5-ALA), methylaminolevulinate, hexylaminolevulinate, 5-ALA esters, and 5-ALA amides.

9. The method of claim 1 , wherein the killing of intraerythrocytic parasites is indicative by pyknosis.

10. The method of claim 1 , wherein the parasites are drug-resistant.

11. The method of claim 1 , wherein the parasites are artemisinin-resistant.

12. A method of treating blood-stage malaria, the method comprising administering to a subject in need thereof, therapeutically effective amount of a combination of 5-aminolevulinic acid or a derivative thereof, luminol or a derivative thereof, and artemisinin or a derivative thereof.

13. The method of claim 12 , further comprising administering a therapeutically effective amount of 4-iodophenol.

14. The method of claim 12 , wherein the artemisinin or derivative thereof is selected from the group consisting of artemisinin, artesunate, artemether, dihydroartesmisinin, artelinic acid, and artemotil.

15. The method of claim 12 , wherein the artemisinin or derivative thereof is dihydroartesmisinin.

16. The method of claim 12 , wherein the artemisinin or derivative thereof is administered at a sub-therapeutic dose.

17. The method of claim 16 , wherein the sub-therapeutic dose is ≤10% of the EC 50 of the artemisinin or derivative thereof.

18. The method of claim 12 , wherein the luminol or derivative thereof is selected from the group consisting of lumino, luminol sodium salt, luminol hemihydrate, luminol hydrochloride, isoluminol, isoluminol monohydrate, and isoluminol ABEI.

19. The method of claim 12 , wherein the 5-aminolevulinic acid or derivative thereof is selected from the group consisting of 5-aminolevulinic acid (5-ALA), methylaminolevulinate, hexylaminolevulinate, 5-ALA esters, and 5-ALA amides.

20. The method of claim 12 , wherein the parasites are artemisinin-resistant.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 14, 2017
From: GOLDBERG, DANIEL E.; SIGALA, PAUL
To: WASHINGTON UNIVERSITY
Reel/Frame 043008/0222 →
CONFIRMATORY LICENSE Recorded Jul 18, 2016
From: WASHINGTON UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 039361/0210 →
Continuity (2)
Provisional Application 62183042 · Jun 22, 2015
Related Publication 20160367674A1 · Dec 22, 2016