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Claims for Patent: 8,623,826

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Claims for Patent: 8,623,826

Title:Compositions and methods for treating centrally mediated nausea and vomiting
Abstract: Provided are methods for treating nausea and vomiting in patients undergoing chemotherapy, radiotherapy, or surgery, comprising the co-administration of netupitant, palonosetron and dexamethasone.
Inventor(s): Trento; Fabio (Como, IT), Cantoreggi; Sergio (Cagiallo, CH), Rossi; Giorgia (Como, IT), Cannella; Roberta (Varese, IT), Bonadeo; Daniele (Varese, IT)
Assignee: Helsinn Healthcare S.A. (Lugano/Pazallo, CH)
Application Number:13/077,462
Patent Claims: 1. A method of treating both nausea and vomiting for five consecutive days in a patient in need thereof, comprising: a) administering to said patient on day one netupitant or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount which enters the systemic circulation, crosses the blood brain barrier and occupies at least 70% of neurokinin-1 (NK.sub.1) receptors in the striatum seventy-two hours after said administration; b) administering to said patient on day one a therapeutically effective amount of palonosetron or a pharmaceutically acceptable salt thereof; and c) administering to said patient on day one a first dose of dexamethasone which is ineffective against chemotherapy induced nausea and vomiting (CINV) when administered alone, but effective against CINV when administered in combination with said netupitant, wherein said first dose of dexamethasone comprises from 50 to 70% of a minimum effective dose when administered alone against CINV; steps a b and (c) are effective to treat both nausea and vomiting during the period defined by days one through five; and steps (a), (b) and (c) are effective to treat both nausea and vomiting to a greater extent during the period defined by days one through five than steps (b) and (c) alone.

2. The method of claim 1, further comprising: d) administering to said patient, on days two, three and four, a second dose of dexamethasone which is ineffective against vomiting when administered alone against vomiting, but effective against vomiting when administered in combination with steps (a) and (b), wherein said second dose comprises from 40 to 60% of a minimum effective dose when administered alone against vomiting.

3. The method of claim 1 or 2, wherein said netupitant occupies at least 80% of NK.sub.1 receptors in the striatum seventy-two hours after said administration.

4. The method of claim 1, wherein only one dose of netupitant or a pharmaceutically acceptable salt thereof is administered during said five days.

5. The method of claim 1, wherein only one dose of netupitant or a pharmaceutically acceptable salt thereof is administered during said five days, and said one dose is administered orally.

6. The method of claim 1, wherein said therapeutically effective amount of netupitant comprises from about 200 to about 400 mg of netupitant or a pharmaceutically acceptable salt thereof.

7. The method of claim 1, wherein said therapeutically effective amount of netupitant comprises about 300 mg of netupitant as a free base.

8. The method of claim 1, wherein said therapeutically minimum effective dose of dexamethasone when administered alone comprises from about 16 mg to about 20 mg of dexamethasone.

9. The method of claim 1, wherein only one dose of said palonosetron or a pharmaceutically acceptable salt thereof is administered during said five days.

10. The method of claim 1, wherein said therapeutically effective amount of palonosetron or pharmaceutically acceptable salt thereof is from about 0.25 to about 0.75 mg based on the weight of the free base.

11. The method of claim 1, wherein said palonosetron is administered as palonosetron hydrochloride, and said therapeutically effective amount of said palonosetron hydrochloride is about 0.56 mg of palonosetron hydrochloride, corresponding to about 0.5 mg of palonosetron as a free base.

12. The method of claim 1, wherein said palonosetron is administered orally.

13. The method of claim 1, comprising orally administering: a) about 300 mg of netupitant as a free base on day one; b) about 0.56 mg of palonosetron hydrochloride, corresponding to about 0.5 mg of palonosetron as a free base, on day one; and c) about 12 mg of dexamethasone on day one.

14. The method of claim 1, comprising orally administering: a) about 300 mg of netupitant as a free base on day one; b) about 0.56 mg of palonosetron hydrochloride (corresponding to about 0.5 mg of palonosetron as a free base) on day one; c) about 12 mg of dexamethasone on day one; and d) about 8 mg of dexamethasone on days two, three and four.

15. The method of claim 1, wherein said nausea and vomiting is chemotherapy induced nausea and vomiting ("CINV"), radiation therapy induced nausea and vomiting ("RINV"), or post-operative nausea and vomiting ("PONV").

16. The method of claim 1, wherein said nausea and vomiting is induced by moderately or highly emetogenic chemotherapy.

17. The method of claim 1, comprising administering moderately or highly emetogenic chemotherapy within from about one hour to about two hours of said administration of said netupitant or pharmaceutically acceptable salt thereof.

18. The method of claim 1, comprising treating nausea and vomiting in response to highly emetogenic chemotherapy during the acute phase, or in response to highly emetogenic chemotherapy during the delayed phase, or in response to moderately emetogenic chemotherapy during the acute phase, or in response to moderately emetogenic chemotherapy during the delayed phase.

19. A method of treating both nausea and vomiting in a human subject in need thereof during the acute or delayed phases of chemotherapy induced nausea and vomiting (CINV) in response to moderately or highly emetogenic chemotherapy, comprising administering to said subject before said chemotherapy a therapeutically effective amount of netupitant or a pharmaceutically acceptable salt thereof and a therapeutically effective amount of palonosetron or a pharmaceutically acceptable salt thereof.

20. The method of claim 19, comprising orally administering from about 200 to about 400 mg of netupitant or a pharmaceutically acceptable salt thereof, and from about 0.25 to about 0.75 mg of palonosetron or a pharmaceutically acceptable salt thereof.

21. The method of claim 19, comprising orally administering about 300 mg of netupitant as the free base and about 0.56 mg of palonosetron hydrochloride.

22. The method of claim 19, further comprising, if said patient is undergoing highly emetogenic chemotherapy, administering a sub-therapeutic dose of dexamethasone on days one, two, three and four, wherein day one is the day on which netupitant and palonosetron, or pharmaceutically acceptable salts thereof, are administered.

23. The method of claim 19, further comprising, if said patient is undergoing highly emetogenic chemotherapy, orally administering 12 mg of dexamethasone on day one and 8 mg of dexamethasone on days two, three and four, wherein day one is the day on which netupitant and palonosetron, or pharmaceutically acceptable salts thereof, are administered.

24. The method of claim 1, wherein said netupitant or pharmaceutically acceptable salt thereof and said palonosetron or pharmaceutically acceptable salt thereof are synergistically effective to antagonize NK1 activity.

25. The method of claim 19, wherein said netupitant or pharmaceutically acceptable salt thereof and said palonosetron or pharmaceutically acceptable salt thereof are synergistically effective to antagonize NK1 activity.
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