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Last Updated: April 23, 2024

Claims for Patent: 8,563,690


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Summary for Patent: 8,563,690
Title:Modulation of platelet aggregation
Abstract: Methods and compositions for inhibition of platelet cell aggregation are described. In particular, compositions comprising cell permeant RGT peptides, such as RGT bound to a lipid moiety are provided. Compositions may be used in the treatment and prevention of clot related diseases such as stroke and myocardial infarction.
Inventor(s): Du; Xiaoping (Willowbrook, IL), Xi; Xiaodong (Shanghai, CN)
Assignee: The Board of Trustees of the University of Illinois (Urbana, IL)
Application Number:12/611,446
Patent Claims:1. A composition comprising a peptide consisting of the amino acid sequence RGT and a lipid covalently bound to the amino-terminus of said peptide.

2. The composition of claim 1, wherein the lipid is a fatty acid.

3. The composition of claim 2, wherein the fatty acid is a saturated fatty acid.

4. The composition of claim 3, wherein the saturated fatty acid is a myristic acid or palmitic acid.

5. The composition of claim 4, wherein the saturated fatty acid is myristic acid.

6. A pharmaceutical composition comprising a composition according to claim 1 in a pharmaceutically acceptable carrier.

7. A method for inhibiting platelet aggregation in a subject comprising administering to the subject the composition of claim 1, said composition administered in an amount effective to inhibit platelet aggregation.

8. The method of claim 7, wherein the lipid is a fatty acid.

9. The method of claim 8, wherein the fatty acid is a saturated fatty acid.

10. The method of claim 9, wherein the saturated fatty acid is a myristic acid or palmitic acid.

11. The method of claim 9, wherein the saturated fatty acid is myristic acid.

12. The method of claim 7, wherein the RGT peptide inhibits or reduces phosphorylation of integrin .beta.3 in a platelet cell.

13. The method according to claim 7, further comprising administering a therapeutic drug to the subject before, after or concurrently with the composition.

14. The method according to claim 13, wherein the therapeutic drug is clopidogrel, ticlopidine, cilostazol, abciximab, eptifibatide, tirofiban, defibrotide, dipyridamole or aspirin.

15. The method of claim 7, wherein the subject has atherosclerosis.

16. The method of claim 7, wherein, the composition is administered to the subject by oral, nasal, topical, orthotopic, intradermal, subcutaneous, intramuscular, intraperitoneal or intravenous administration.

17. The method of claim 16, wherein the composition administered to a subject by intravenous administration.

18. The method of claim 7, wherein the composition further comprises a pharmaceutically acceptable carrier.

19. A method for reducing the occurrence of a secondary ischemic event in a subject comprising administering to a subject who has suffered a primary ischemic event a therapeutically effective amount of the composition of claim 1.

20. The method of claim 19, wherein the primary and/or secondary ischemic event is angina, reocclusion after percutaneous transluminal coronary angioplasty, restenosis, thrombotic stroke, transient ischemic attack, reversible ischemic neurological deficit or intermittent claudication.

21. A method for reducing the size of a blood clot in a subject comprising administering to the subject the composition of claim 1, said composition administered in an amount effective to reduce the size of a blood clot.

22. The method of claim 21, wherein the lipid is a fatty acid.

23. The method of claim 22, wherein the fatty acid is a saturated fatty acid.

24. The method of claim 22, wherein the saturated fatty acid is a myristic acid or palmitic acid.

25. The method of claim 24, wherein the saturated fatty acid is myristic acid.

26. The method of claim 21, wherein the RGT amino acid sequence inhibits or reduces phosphorylation of integrin .beta.3 in a platelet cell.

27. The method according to claim 21, further comprising administering a therapeutic drug to the subject before, after or concurrently with the composition.

28. The method according to claim 27, wherein the therapeutic drug is an anticoagulant.

29. The method according to claim 28, wherein the anticoagulant is warfarin, acenocoumarol, phenprocoumon, phenindione, heparin, fondaparinux, idraparinux, argatroban, lepirudin, bivalirudin or dabigatran.

30. The method according to claim 27, wherein the therapeutic drug is a thrombolytic drug.

31. The method according to claim 30, wherein the thrombolytic drug is streptokinase, tissue plasminogen activator (tPA), urokinase, Reteplase, tenecteplase, anistreplase or brinase.

32. The method of claim 21, wherein, the composition is administered to the subject by oral, nasal, topical, orthotopic, intradermal, subcutaneous, intramuscular, intraperitoneal or intravenous administration.

33. The method of claim 32, wherein the composition is administered to the subject by intravenous administration.

34. The method of claim 21, wherein the composition further comprises a pharmaceutically acceptable carrier.

35. The method of claim 21, wherein the subject has pulmonary embolism, venous thrombosis, deep vein thrombosis, portal vein thrombosis, renal vein thrombosis, jugular vein thrombosis, Budd-Chiari syndrome, Paget-Schroetter disease, cerebral venous sinus thrombosis, arterial thrombosis, thrombotic stroke or myocardial infarction.

Details for Patent 8,563,690

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Microbix Biosystems Inc. KINLYTIC urokinase For Injection 021846 01/16/1978 ⤷  Try a Trial 2028-11-03
Janssen Biotech, Inc. REOPRO abciximab Injection 103575 12/22/1994 ⤷  Try a Trial 2028-11-03
Chiesi Usa, Inc. RETAVASE reteplase For Injection 103786 10/30/1996 ⤷  Try a Trial 2028-11-03
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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