IP Library Granted Patent US 10,137,100
Granted Patent B2
US 10,137,100 · App. 15/335,242 · Granted Nov 27, 2018

Administration of serine protease inhibitors to the stomach

Inventors: Geert W. Schmid-Schonbein (Del Mar, CA); Yung-Tsai (Andrew) Lee (Taipei, TW); Jeng Wei (Taipei, TW)
Assignees: The Regents of the University of California; Inflammagen, LLC
A61K31/195A61K9/0053A61K31/10A61K31/145A61K31/155A61K31/185A61K31/19A61K31/216A61K31/24A61K31/661A61K31/765A61K38/1722A61K38/57A61K47/02A61K47/10A61K9/08
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Quick Facts
Patent No.
US 10,137,100
App. No.
15/335,242
Granted
Nov 27, 2018
Kind
B2
Abstract

The inventors have unexpectedly discovered that shock and/or potential multi-organ failure due to shock can be effectively treated by administration of liquid high-dose protease inhibitor formulations to a location upstream of where pancreatic proteases are introduced into the gastrointestinal tract. Most preferably, administration is directly to the stomach, for example, via nasogastric tube under a protocol effective to treat shock by such administration without the need of providing significant quantities of the protease inhibitor to the jejunum and/or ileum.

Claims (21)

1. A method of treating shock in a mammal in need thereof comprising orally administering to the mammal a therapeutically effective amount of an aqueous pharmaceutical composition comprising: (i) tranexamic acid, (ii) polyethylene glycol-3350, and (iii) electrolytes.

2. The method of claim 1 , wherein the composition comprises about 2 grams to about 20 grams of tranexamic acid.

3. The method of claim 1 , wherein the composition comprises 0.16 wt % to 1.80 wt % of tranexamic acid.

4. The method of claim 1 , wherein the shock is traumatic shock, septic shock, cardiogenic shock, or hypovolemic shock.

5. The method of claim 1 , wherein the shock is caused by (i) a surgical intervention, (ii) complications from radiation treatment, (iii) complications from chemotherapy treatment, (iv) organ perforation, (v) chylothorax, (vi) a bacterial infection, (vii) damage from a mechanical ventilator, or (viii) dialysis.

6. The method of claim 1 , wherein the shock is a developing shock or an acute shock.

7. The method of claim 1 , comprising orally administering the composition through a nasogastric tube.

8. The method of claim 1 , wherein the composition is administered as a single undivided dose.

9. The method of claim 1 , wherein the composition is administered as a divided dose.

10. The method of claim 1 , wherein the composition is administered daily for 2 days to 21 days.

11. A method of treating shock in a mammal in need thereof comprising orally administering to the mammal a therapeutically effective amount of an aqueous pharmaceutical composition comprising: (i) a protease inhibitor, (ii) polyethylene glycol-3350, and (iii) electrolytes.

12. The method of claim 11 , wherein the shock is traumatic shock, septic shock, cardiogenic shock, or hypovolemic shock.

13. The method of claim 11 , wherein the shock is caused by (i) a surgical intervention, (ii) complications from radiation treatment, (iii) complications from chemotherapy treatment, (iv) organ perforation, (v) chylothorax, (vi) a bacterial infection, (vii) damage from a mechanical ventilator, or (viii) dialysis.

14. The method of claim 11 , wherein the protease inhibitor is a serine protease inhibitor, a cysteine protease inhibitor, a threonine protease inhibitor, an aspartate protease inhibitor, a glutamate protease inhibitor, a matrix metalloprotease inhibitor, or a combination of two or more thereof.

15. The method of claim 14 , wherein the protease inhibitor is the serine protease inhibitor.

16. The method of claim 11 , wherein the protease inhibitor is a serpin, an alpha 1-antitrypsin, an alpha-2-macroglobulin, 6-amidino-2-naphthyl p-guanidinobenzoate dimethanesulfate, gabexate monomethanesulfonate, diisopropylfluorophosphate, p-(amidinophenyl)methanesulfonyl fluoride, tranexamic acid, 4-(2-aminoethyl)benzenesulfonyl fluoride, or camostate.

17. The method of claim 11 , wherein the composition comprises about 2 grams to about 20 grams of the protease inhibitor.

18. The method of claim 11 , wherein the composition comprises 0.16 wt % to 1.80 wt % of the protease inhibitor.

19. The method of claim 1 , wherein the composition has a volume of about 500 ml to about 1000 ml.

20. The method of claim 11 , comprising orally administering the composition through a nasogastric tube.

21. The method of claim 11 , wherein the composition has a volume of about 500 ml to about 1000 ml.

Assignments (3)
MERGER Recorded Jan 9, 2020
From: INFLAMMAGEN, LLC
To: LEADING BIOSCIENCES, INC.
Reel/Frame 051471/0780 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 11, 2018
From: SCHMID-SCHONBEIN, GEERT W.; CHANG, MARISOL; CABRALES, PEDRO
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 046842/0800 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 11, 2018
From: LEE, YUNG-TSAI (ANDREW); WEI, JENG
To: INFLAMMAGEN, LLC
Reel/Frame 046842/0987 →
Continuity (4)
Division 13825779
Provisional Application 61529052 · Aug 30, 2011
Provisional Application 61385798 · Sep 23, 2010
Related Publication 20170231935A1 · Aug 17, 2017