IP Library Granted Patent US 10,639,354
Granted Patent B2
US 10,639,354 · App. 15/576,647 · Granted May 5, 2020

Treatment of hyperinsulinemic hypoglycemia with exendin (9-39)

Inventors: Tracey L. McLaughlin (Stanford, CA); Colleen M. Craig (Stanford, CA)
A61K38/2278A61K9/0019A61K9/08A61K9/10A61K38/17A61K38/22A61K38/26A61K45/06A61P3/08
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 10,639,354
App. No.
15/576,647
Granted
May 5, 2020
Kind
B2
Abstract

Compositions and methods for treating hyperinsulinemic hypoglycemia, such as hyperinsulinemic hypoglycemia after bariatric surgery or gastrointestinal surgery, are provided. In some embodiments, an effective amount of the glucagon-like peptide-1 receptor antagonist exendin(9-39) is subcutaneously administered twice per day.

Claims (23)

1. A method for treating hyperinsulinemic hypoglycemia in a patient, the method comprising subcutaneously administering to the patient in need thereof a composition comprising a therapeutically effective amount of exendin(9-39) twice-per-day (BID), wherein the therapeutically effective amount is in the range of 10-30 mg exendin(9-39), wherein the composition is administered in a single injection with an injectate volume of 0.5 ml to 1 ml.

2. The method of claim 1 , wherein the therapeutically effective amount of exendin(9-39) administered twice-per-day is selected from a dosage in the range of 10-20 mg, a dosage in the range of 10-15 mg, a dosage of 10 mg, a dosage of 15 mg, a dosage of 20 mg, and a dosage of 30 mg.

3. The method of claim 2 , further comprising administering a first daily administration in the morning and a second daily administration in the evening, and wherein the first daily administration comprising a morning injectate, the second daily administration comprises an evening injectate, and the second daily administration is at least 8 hours after the first daily administration.

4. The method of claim 3 , wherein the first daily administration is administered at a first time selected from before the morning meal, at least 1 hour before the morning meal, 60 to 90 minutes before the morning meal, and during a first period from one hour before the morning meal to one hour after the morning meal.

5. The method of claim 3 , wherein the second daily administration is administered at a second time selected from 60 to 90 minutes before the evening meal, within two hours of bedtime, during a second period from after the evening meal and to before bedtime, and from 9 to 15 hours after the morning administration.

6. The method of claim 1 , wherein the patient has previously had bariatric surgery or gastrointestinal surgery.

7. The method of claim 6 , wherein the bariatric surgery is selected from the group consisting of Roux-en-Y Gastric Bypass surgery, Vertical Sleeve Gastrectomy, placement of an endosleeve device, duodenal mucosal resurfacing, partial bypass of the duodenum, vagal nerve blockade, and pyloroplasty.

8. The method of claim 6 , wherein the gastrointestinal surgery is selected from the group consisting of gastrectomy, Nissen Fundoplication, and esophagectomy.

9. The method of claim 1 , wherein the composition is formulated with a pharmaceutically acceptable diluent or carrier and one or both of a preservative and pH adjustment agent.

10. A method for treating hyperinsulinemic hypoglycemia in a patient, the method comprising subcutaneously administering to the patient in need thereof a composition comprising a therapeutically effective amount of exendin(9-39) twice-per-day (BID), wherein the therapeutically effective amount is in the range of 10-30 mg exendin(9-39), wherein the composition is a solution or suspension that comprises exendin(9-39) at a concentration range selected from 4-20 mg/ml, 10-20 mg/ml, 8-16 mg/ml, and 13-16 mg/ml.

11. A method for treating hyperinsulinemic hypoglycemia in a patient, the method comprising subcutaneously administering to the patient in need thereof a composition comprising a therapeutically effective amount of exendin(9-39) twice-per-day (BID), wherein the therapeutically effective amount is in the range of 10-30 mg exendin(9-39), wherein administration results in a steady state plasma exendin(9-39) concentration of at least 100 ng/ml as measured by liquid chromatography-mass spectrometry.

12. A method for treating hyperinsulinemic hypoglycemia in a patient, the method comprising subcutaneously administering to the patient in need thereof a composition comprising a therapeutically effective amount of exendin(9-39) twice-per-day (BID), wherein the therapeutically effective amount is in the range of 10-30 mg exendin(9-39), wherein the therapeutically effective amount of exendin(9-39) administered twice-per-day is selected from a dosage in the range of 10-20 mg, a dosage in the range of 10-15 mg, a dosage of 10 mg, a dosage of 15 mg, a dosage of 20 mg, and a dosage of 30 mg, and wherein each of the twice-per-day administrations result in a Cmax of 100 ng/ml.

13. A method for treating hyperinsulinemic hypoglycemia in a patient, the method comprising subcutaneously administering to the patient in need thereof a composition comprising a therapeutically effective amount of exendin(9-39) twice-per-day (BID), wherein the therapeutically effective amount is in the range of 10-30 mg exendin(9-39), wherein the therapeutically effective amount of exendin(9-39) administered twice-per-day is selected from a dosage in the range of 10-20 mg, a dosage in the range of 10-15 mg, a dosage of 10 mg, a dosage of 15 mg, a dosage of 20 mg, and a dosage of 30 mg, and, wherein the amount of exendin(9-39) in the evening injectate is greater than the amount of exendin(9-39) in the morning injectate.

14. The method of claim 13 , wherein the amount of exendin(9-39) in the evening injectate is 5 mg-10 mg greater than the amount of exendin(9-39) in the morning injectate.

15. The method of claim 14 , wherein the amount of exendin(9-39) in the morning injectate is selected from 10 mg, 15 mg, and 20 mg.

16. The method of claim 13 , wherein a concentration of exendin(9-39) in the morning injectate is unequal to a concentration of exendin(9-39) in the evening injectate.

17. The method of claim 16 wherein the concentration of exendin(9-39) in the morning injectate is higher than the concentration of exendin(9-39) in the evening injectate.

18. The method of claim 13 , wherein a Tmax of the exendin(9-39) after the second daily administration is longer than a Tmax of the exendin(9-39) after the first daily administration.

19. The method of claim 18 , wherein the concentration of exendin(9-39) in the morning injectate is selected from 4-20 mg/ml, 10-20 mg/ml, 8-16 mg/ml, and 13-16 mg/ml.

20. The method of claim 18 , wherein the concentration of exendin(9-39) in the evening injectate is selected from 4-20 mg/ml, 10-20 mg/ml, 8-16 mg/ml, and 13-16 mg/ml.

21. A method for treating hyperinsulinemic hypoglycemia in a patient, the method comprising subcutaneously administering to the patient in need thereof a composition comprising a therapeutically effective amount of exendin(9-39) twice-per-day (BID), wherein the therapeutically effective amount is in the range of 10-30 mg exendin(9-39), wherein subcutaneous administration twice-per-day comprises administering a morning injectate and an evening injectate, and the amount of exendin(9-39) administered is the same in the morning and evening injectates and the concentration of exendin(9-39) is greater in the evening injectate compared to the morning injectate.

22. The method of claim 21 wherein the concentration of exendin(9-39) in morning injectate is 15 mg/ml and the concentration of exendin(9-39) in the evening injectate is 20 mg/ml.

23. A method for treating hyperinsulinemic hypoglycemia in a patient, the method comprising subcutaneously administering to the patient in need thereof a composition comprising a therapeutically effective amount of exendin(9-39) twice-per-day (BID), wherein the therapeutically effective amount is in the range of 10-30 mg exendin(9-39), wherein the composition is administered to the patient for at least 30 days.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 23, 2018
From: MCLAUGHLIN, TRACEY L.; CRAIG, COLLEEN M.
To: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
Reel/Frame 045325/0780 →
Continuity (4)
Provisional Application 62329850 · Apr 29, 2016
Provisional Application 62254175 · Nov 11, 2015
Provisional Application 62165743 · May 22, 2015
Related Publication 20180117122A1 · May 3, 2018
Cited By (2)
US 12,220,444 US 12,697,390