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Last Updated: April 19, 2024

Details for Patent: 8,889,115


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Title:Ion binding polymers and uses thereof
Abstract: The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising potassium binding polymers and pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hyperkalemia, such as hyperkalemia caused by renal failure and/or the use of hyperkalemia causing drugs.
Inventor(s): Charmot; Dominique (Campbell, CA), Chang; Han-Ting (Livermore, CA), Klaerner; Gerrit (Los Gatos, CA), Buysse; Jerry M. (Los Altos, CA), Liu; Mingjun (Campbell, CA)
Assignee: Relypsa, Inc. (Redwood City, CA)
Filing Date:Oct 09, 2012
Application Number:13/647,894
Claims:1. A method for removing potassium from a patient in need thereof comprising administering a potassium-binding polymer in an oral dosage form to a patient having renal insufficiency, the patient being treated for the renal insufficiency with a potassium-sparing diuretic, an angiotensin-converting enzyme inhibitor, an angiotensin receptor blocker, a non-steroidal anti-inflammatory drug, heparin, or trimethoprim and the potassium-binding polymer comprising a crosslinked cation exchange polymer in a bead form, wherein the potassium-binding polymer comprises a crosslinked cation exchange polymer comprising acid groups in their acid or salt form, the acid groups having an electron-withdrawing substituent attached to a carbon atom alpha or beta to the acid group.

2. The method of claim 1 wherein the electron-withdrawing substituent is selected from the group consisting of a hydroxyl group, an ether group, an ester group, and a halide atom.

3. The method of claim 1 wherein the acid group is carboxylic.

4. The method of claim 1 wherein the acid group is phosphonic.

5. The method of claim 3 wherein the potassium-binding polymer comprises a crosslinked carboxylic polymer having fluoride attached to the carbon atom alpha to the carboxylic acid group.

6. The method of claim 1 wherein the potassium-binding polymer comprises a Ca.sup.2+ cationic counterion.

7. The method of claim 1 wherein the patient is being treated with an angiotensin-converting enzyme inhibitor.

8. The method of claim 1 wherein the patient is being treated with an angiotensin receptor blocker.

9. The method of claim 1 wherein the patient suffers from hyperkalemia.

10. The method of claim 1 wherein the potassium-binding polymer and the potassium-sparing diuretic, the angiotensin-converting enzyme inhibitor, the angiotensin receptor blocker, the non-steroidal anti-inflammatory drug, heparin, or trimethoprim are administered simultaneously.

11. A method for removing potassium from a patient in need thereof comprising administering a therapeutically effective amount of a potassium-binding polymer in an oral dosage form to a patient having renal insufficiency, the patient being treated for the renal insufficiency with a potassium-sparing diuretic, an angiotensin-converting enzyme inhibitor, an angiotensin receptor blocker, a non-steroidal anti-inflammatory drug, heparin, or trimethoprim and the potassium-binding polymer being a crosslinked alpha-fluoroacrylic acid polymer.

12. The method of claim 11 wherein the crosslinked alpha-fluoroacrylic acid polymer has a swelling ratio of less than 3.

13. The method of claim 11 wherein the alpha-fluoroacrylic acid polymer is crosslinked with divinylbenzene, ethylene bisacrylamide, N,N'-bis(vinylsulfonylacetyl)ethylene diamine, 1,3-bis(vinylsulfonyl)2-propanol, vinylsulfone, N,N'-methylenebisacrylamide polyvinyl ether, polyallylether, or a combination thereof.

14. The method of claim 11 wherein the potassium-binding polymer is in a bead form.

15. The method of claim 11 wherein the patient is being treated with an angiotensin-converting enzyme inhibitor.

16. The method of claim 11 wherein the patient is being treated with an angiotensin receptor blocker.

17. A method for removing potassium from a patient in need thereof, the patient suffering from congestive heart failure (CHF), the method comprising administering a potassium-binding polymer in an oral dosage form to the patient, the potassium-binding polymer comprising a crosslinked cation exchange polymer in a bead form, wherein the potassium-binding polymer comprises a crosslinked cation exchange polymer comprising acid groups in their acid or salt form, the acid groups having an electron-withdrawing substituent attached to a carbon atom alpha or beta to the acid group.

18. The method of claim 17 wherein the electron-withdrawing substituent is selected from the group consisting of a hydroxyl group, an ether group, an ester group, and a halide atom.

19. The method of claim 17 wherein the acid group is carboxylic.

20. The method of claim 17 wherein the acid group is phosphonic.

21. The method of claim 19 wherein the potassium-binding polymer comprises a crosslinked carboxylic polymer having fluoride attached to the carbon atom alpha to the carboxylic acid group.

22. The method of claim 17 wherein the patient is also being treated with a potassium-sparing diuretic.

23. The method of claim 17 wherein the patient is also being treated with an angiotensin-converting enzyme inhibitor.

24. The method of claim 22 wherein the potassium-binding polymer and the potassium-sparing diuretic are administered simultaneously.

25. The method of claim 23 wherein the potassium-binding polymer and the angiotensin-converting enzyme inhibitor are administered simultaneously.

26. A method for removing potassium from a patient in need thereof, the patient suffering from congestive heart failure (CHF), the method comprising administering a potassium-binding polymer in an oral dosage form to the patient, the potassium-binding polymer being a crosslinked alpha-fluoroacrylic acid polymer.

27. The method of claim 26 wherein the crosslinked alpha-fluoroacrylic acid polymer has a swelling ratio of less than 3.

28. The method of claim 26 wherein the alpha-fluoroacrylic acid polymer is crosslinked with divinylbenzene, ethylene bisacrylamide, N,N'-bis(vinylsulfonylacetyl)ethylene diamine, 1,3-bis(vinylsulfonyl)2-propanol, vinylsulfone, N,N'-methylenebisacrylamide polyvinyl ether, polyallylether, or a combination thereof.

29. The method of claim 26 wherein the potassium-binding polymer is in a bead form.

30. The method of claim 26 wherein the patient is also being treated with a potassium-sparing diuretic.

31. The method of claim 26 wherein the patient is also being treated with an angiotensin-converting enzyme inhibitor.

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