IP Library Granted Patent US 10,898,496
Granted Patent B2
US 10,898,496 · App. 16/194,030 · Granted Jan 26, 2021

Targeting NC

Inventor: J. Marc Simard (Baltimore, MD)
Assignees: University of Maryland, Baltimore; The United States of America as Represented by the Department of Veterans Affairs
A61K31/57G01N33/6872A61K31/427A61K31/565A61K38/00
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,898,496
App. No.
16/194,030
Granted
Jan 26, 2021
Kind
B2
Abstract

The present invention concerns protection of an organ or tissue outside of the central nervous system following an ischemic episode. In particular aspects, the invention concerns organ preservation for transplantation, angina pectoris, kidney reperfusion injury, and so forth. In specific embodiments, the organ is subjected to an inhibitor of an NC Ca-ATP channel that is regulated by SUR1. Exemplary inhibitors include sulfonylurea compounds, such as glibenclamide, for example.

Claims (21)

1. A method of treating a subject suffering from cerebral edema or intracranial pressure following hemorrhagic infarction comprising administering an inhibitor of an NC Ca-ATP channel that is a SUR1 antagonist and/or a TRPM4 antagonist as a loading bolus dose followed by a constant infusion of a maintenance dose, wherein the bolus dose by weight is 30-90 times the weight amount of the maintenance dose administered per minute or wherein the SUR1 antagonist is administered to the subject in a dosage of less than 3.5 mg per day.

2. The method of claim 1 , wherein the SUR1 antagonist is glibenclamide (glyburide), tolbutamide, acetohexamide, chlorpropamide, tolazimide, glipizide, gliquidone, repaglinide, nateglinide, meglitinide, gliclazide, glimepiride, repaglinide, nateglinide, mitiglinide, a pharmaceutically acceptable salt thereof, or an active metabolite thereof.

3. The method of claim 1 , wherein the TRPM4 antagonist is selected from the group consisting of flufenamic acid, mefanimic acid, niflumic acid, and antagonists of VEGF, MMP, NOS, TNFα, NFkB, and/or thrombin.

4. The method of claim 1 , wherein said inhibitor is delivered by intravenous, subcutaneous, intramuscular, intracutaneous, intragastric or oral administration.

5. The method of claim 1 , wherein the inhibitor is administered prior to an ischemic episode, concurrent with an ischemic episode, or both.

6. The method of claim 1 , wherein the inhibitor is administered following an ischemic episode.

7. The method of claim 1 , wherein the SUR1 antagonist is administered to the subject in a dosage of less than 3.5 mg per day.

8. The method of claim 1 , wherein the SUR1 antagonist is administered to the subject at a dosage of less than 0.8 mg/kg body weight within a 24 hour period.

9. The method of claim 1 , wherein the maintenance dose is administered as a constant infusion.

10. The method of claim 1 , wherein the maintenance dose is administered for six or more hours.

11. The method of claim 1 , wherein the maintenance dose is administered for twenty-four or more hours.

12. The method of claim 1 , wherein the method further comprises delivery of an additional therapeutic agent.

13. The method of claim 12 , wherein the additional therapeutic agent comprises an antacid, an immunosuppressant, an antiviral compound, an antibacterial compound, an antifungal compound, or a combination or mixture thereof.

14. The method of claim 12 , wherein the additional therapeutic agent comprises anti-thymocyte globulin, basiliximab, methylprednisolone, tacrolimus, mycophenolate mofetil, prednisone, sirolimus, rapamycin, azathioprine, or a mixture thereof.

15. The method of claim 1 , wherein the subject has not undergone decompressive craniotomy.

16. The method of claim 1 , wherein the SUR1 antagonist is glibenclamide or a pharmaceutically acceptable salt thereof.

17. A method of treating a subject suffering from acute ischemic stroke in a cerebral artery comprising administering an inhibitor of an NC Ca-ATP channel that is a SUR1 antagonist and/or a TRPM4 antagonist as a loading bolus dose followed by a constant infusion of a maintenance dose, wherein the bolus dose by weight is 30-90 times the weight amount of the maintenance dose administered per minute or wherein the SUR1 antagonist is administered to the subject in a dosage of less than 3.5 mg per day.

18. The method of claim 17 , wherein the cerebral artery is the middle cerebral artery.

19. The method of claim 17 , wherein the SUR1 antagonist is glibenclamide or a pharmaceutically acceptable salt thereof.

20. A method of reducing matrix metalloproteinases following stroke comprising administering an inhibitor of an NC Ca-ATP channel that is a SUR1 antagonist and/or a TRPM4 antagonist as a loading bolus dose followed by a constant infusion of a maintenance dose, wherein the bolus dose by weight is 30-90 times the weight amount of the maintenance dose administered per minute.

21. The method of claim 20 , wherein the SUR1 antagonist is glibenclamide or a pharmaceutically acceptable salt thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 19, 2018
From: SIMARD, J. MARC
To: UNIVERSITY OF MARYLAND, BALTIMORE
Reel/Frame 047538/0986 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 19, 2018
From: UNIVERSITY OF MARYLAND, BALTIMORE
To: THE UNITED STATES OF AMERICA AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS
Reel/Frame 048570/0713 →
Continuity (7)
Continuation 15369056 · Dec 5, 2016
Continuation 12522444
Provisional Application 61012613 · Dec 10, 2007
Provisional Application 60952396 · Jul 27, 2007
Provisional Application 60923378 · Apr 13, 2007
Provisional Application 60880119 · Jan 12, 2007
Related Publication 20190117672A1 · Apr 25, 2019
Cited By (2)
US 12,508,217 US 12,714,660