You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 29, 2024

Details for Patent: 8,318,669


✉ Email this page to a colleague

« Back to Dashboard


Title:Method of regulating glucose metabolism, and reagents related thereto
Abstract: The present invention provides methods for modification and regulation of glucagon-like peptide 1 (GLP-1) metabolism by administering therapeutically effective amounts of an inhibitor of dipeptidylpeptidase IV (DPIV) or a pharmaceutically acceptable salt thereof, where the inhibitor has a Ki for inhibition of DPIV of 10 nM or less; and the inhibitor is administered in an amount sufficient to inhibit DPIV proteolysis of GLP-1 but not sufficient to suppress the immune system of the animal.
Inventor(s): Bachovchin; William W. (Cambridge, MA), Plaut; Andrew G. (Lexington, MA), Drucker; Daniel J. (Toronto, CA)
Assignee: Trustees of Tufts College (Boston, MA) New England Medical Center Hospitals, Inc. (Boston, MA) 1149336 Ontario, Inc. (Toronto, Ontario, CA)
Filing Date:Nov 09, 2010
Application Number:12/942,313
Claims:1. A method for modifying metabolism of glucagon-like peptide 1 (GLP-1), comprising administering orally to an animal in need thereof a therapeutically effective amount of an inhibitor of dipeptidylpeptidase IV (DPIV) or a pharmaceutically acceptable salt thereof once daily, wherein the inhibitor has a Ki for inhibition of DPIV of 10 nM or less; the duration of the therapeutic effect is at least about 24 hours; and the inhibitor is administered in an amount sufficient to inhibit DPIV proteolysis of GLP-1 but not sufficient to suppress the immune system of the animal.

2. The method of claim 1, wherein the inhibitor has a Ki for inhibition of DPIV of 1.0 nM or less.

3. The method of claim 2, wherein the inhibitor has a Ki for inhibition of DPIV of 0.1 nM or less.

4. The method of claim 3, wherein the inhibitor has a Ki for inhibition of DPIV of 0.01 nM or less.

5. The method of claim 1, wherein the inhibitor has an EC.sub.50 for modification of GLP-1 metabolism at least one order of magnitude less than its EC.sub.50 for immunosuppression.

6. The method of claim 5, wherein the inhibitor has an EC.sub.50 for modification of GLP-1 metabolism at least two orders of magnitude less than its EC.sub.50 for immunosuppression.

7. The method of claim 1, wherein the inhibitor has a molecular weight less than 5000 amu.

8. The method of claim 7, wherein the inhibitor has a molecular weight less than 2000 amu.

9. The method of claim 8, wherein the inhibitor has a molecular weight less than 1000 amu.

10. The method of claim 1, wherein said inhibition of DPIV proteolysis of GLP-1 treats Type II diabetes.

11. The method of claim 1, wherein the duration of the therapeutic effect is about 24 hours.

12. The method of claim 1, wherein the animal is a human.

13. The method of claim 1, wherein the inhibitor is administered in the form of a tablet.

14. The method of claim 1, wherein the inhibitor is administered in the form of a coated tablet.

15. The method of claim 1, wherein the animal is a human; and the duration of the therapeutic effect is about 24 hours.

16. The method of claim 1, wherein the animal is a human; and the inhibitor has a molecular weight less than 1000 amu.

17. The method of claim 1, wherein the animal is a human; and the inhibitor is administered in the form of a tablet.

18. The method of claim 1, wherein the animal is a human; and the inhibitor is administered in the form of a coated tablet.

19. The method of claim 1, wherein the inhibitor has a molecular weight less than 1000 amu; and the duration of the therapeutic effect is about 24 hours.

20. The method of claim 1, wherein the inhibitor has a molecular weight less than 1000 amu; and the inhibitor is administered in the form of a tablet.

21. The method of claim 1, wherein the inhibitor has a molecular weight less than 1000 amu; and the inhibitor is administered in the form of a coated tablet.

22. The method of claim 1, wherein the duration of the therapeutic effect is about 24 hours; the animal is a human; and the inhibitor is administered in the form of a tablet.

23. The method of claim 1, wherein the duration of the therapeutic effect is about 24 hours; the animal is a human; and the inhibitor is administered in the form of a coated tablet.

24. The method of claim 1, wherein the duration of the therapeutic effect is about 24 hours; the animal is a human; the inhibitor is administered in the form of a tablet; and the inhibitor has a molecular weight less than 1000 amu.

25. The method of claim 1, wherein the duration of the therapeutic effect is about 24 hours; the animal is a human; the inhibitor is administered in the form of a coated tablet; and the inhibitor has a molecular weight less than 1000 amu.

26. The method of claim 1, wherein the duration of the therapeutic effect is about 24 hours; the animal is a human; the inhibitor is administered in the form of a tablet; the inhibitor has a molecular weight less than 1000 amu; and said inhibition of DPIV proteolysis of GLP-1 treats Type II diabetes.

27. The method of claim 1, wherein the duration of the therapeutic effect is about 24 hours; the animal is a human; the inhibitor is administered in the form of a coated tablet; the inhibitor has a molecular weight less than 1000 amu; and said inhibition of DPIV proteolysis of GLP-1 treats Type II diabetes.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.