IP Library Granted Patent US 10,828,297
Granted Patent B2
US 10,828,297 · App. 15/923,050 · Granted Nov 10, 2020

Compositions and methods for treating centrally mediated nausea and vomiting

Inventors: Fabio Trento (Pare, IT); Sergio Cantoreggi (Cagiallo, CH); Giorgia Rossi (Cernobbio, IT); Roberta Cannella (Varese, IT); Daniele Bonadeo (Casalzuigno, IT)
Assignee: Helsinn Healthcare SA
A61K31/496A61K9/0053A61K9/2054A61K9/4808A61K9/4858A61K31/4178A61K31/473A61K31/573A61K45/06Y10S514/872
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Quick Facts
Patent No.
US 10,828,297
App. No.
15/923,050
Granted
Nov 10, 2020
Kind
B2
Abstract

Provided are compositions and methods for treating or preventing nausea and vomiting in patients undergoing chemotherapy, radiotherapy, or surgery.

Claims (23)

1. A method of preventing acute and delayed nausea and vomiting in a subject receiving highly emetogenic cancer chemotherapy comprising inducing in said subject therapeutically effective blood levels of palonosetron and netupitant in a combination regimen with dexamethasone.

2. A method of achieving complete response during the acute and delayed phases of chemotherapy induced nausea and vomiting in a subject receiving highly emetogenic cancer chemotherapy comprising inducing in said subject therapeutically effective blood levels of palonosetron and netupitant in a combination regimen with dexamethasone.

3. A method of preventing nausea during the acute and delayed phases of chemotherapy induced nausea and vomiting in a subject receiving highly emetogenic cancer chemotherapy comprising inducing in said subject therapeutically effective blood levels of palonosetron and netupitant in a combination regimen with dexamethasone.

4. The method of claim 1 , wherein said blood levels are induced by an intravenous anti-emetic regimen administered prior to said chemotherapy.

5. The method of claim 1 , wherein (a) said blood levels are induced by an intravenous anti-emetic regimen administered prior to said chemotherapy, and (2) said blood levels are equivalent to blood levels induced by 50 to 500 mg of netupitant free base and 0.075 to 1.0 mg palonosetron hydrochloride administered orally.

6. The method of claim 1 , wherein (a) said blood levels are induced by an intravenous anti-emetic regimen administered prior to said chemotherapy, and (2) said blood levels are equivalent to blood levels induced by 300 mg of netupitant free base and 0.56 mg palonosetron hydrochloride administered orally.

7. The method of claim 1 , wherein said netupitant occupies at least 70% of said patient's striatum NK1 receptors seventy-two hours after said administration.

8. The method of claim 1 , wherein said method achieves complete response in said subject.

9. The method of claim 1 , wherein said method achieves no emesis in said subject.

10. The method of claim 1 , wherein said method achieves no rescue medication in said subject.

11. The method of claim 1 , wherein said method prevents nausea in said subject.

12. The method of claim 1 , wherein said blood levels of netupitant are independently effective to prevent acute and delayed nausea and vomiting in a subject receiving highly emetogenic cancer chemotherapy.

13. The method of claim 2 , wherein said blood levels are induced by an intravenous anti-emetic regimen administered prior to said chemotherapy.

14. The method of claim 2 , wherein (a) said blood levels are induced by an intravenous anti-emetic regimen administered prior to said chemotherapy, and (2) said blood levels are equivalent to blood levels induced by 50 to 500 mg of netupitant free base and 0.075 to 1.0 mg palonosetron hydrochloride administered orally.

15. The method of claim 2 , wherein (a) said blood levels are induced by an intravenous anti-emetic regimen administered prior to said chemotherapy, and (2) said blood levels are equivalent to blood levels induced by 300 mg of netupitant free base and 0.56 mg palonosetron hydrochloride administered orally.

16. The method of claim 2 , wherein said netupitant occupies at least 70% of said patient's striatum NK1 receptors seventy-two hours after said administration.

17. The method of claim 2 , wherein said method prevents nausea in said subject.

18. The method of claim 2 , wherein said blood levels of netupitant are independently effective to produce complete response in a subject receiving highly emetogenic cancer chemotherapy.

19. The method of claim 3 , wherein said blood levels are induced by an intravenous anti-emetic regimen administered prior to said chemotherapy.

20. The method of claim 3 , wherein (a) said blood levels are induced by an intravenous anti-emetic regimen administered prior to said chemotherapy, and (2) said blood levels are equivalent to blood levels induced by 50 to 500 mg of netupitant free base and 0.075 to 1.0 mg palonosetron hydrochloride administered orally.

21. The method of claim 3 , wherein (a) said blood levels are induced by an intravenous anti-emetic regimen administered prior to said chemotherapy, and (2) said blood levels are equivalent to blood levels induced by 300 mg of netupitant free base and 0.56 mg palonosetron hydrochloride administered orally.

22. The method of claim 3 , wherein said netupitant occupies at least 70% of said patient's striatum NK1 receptors seventy-two hours after said administration.

23. The method of claim 3 , wherein said blood levels of netupitant are independently effective to prevent nausea in a subject receiving highly emetogenic cancer chemotherapy.

Assignments (3)
RELEASE OF SECURITY INTEREST Recorded Sep 20, 2023
From: HAMILTON SA LLC
To: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
Reel/Frame 064961/0567 →
SECURITY INTEREST Recorded Dec 30, 2022
From: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
To: HAMILTON SA LLC
Reel/Frame 062254/0888 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 23, 2018
From: TRENTO, FABIO; CANTOREGGI, SERGIO; ROSSI, GIORGIA; CANNELLA, ROBERTA; BONADEO, DANIELE; BRAGLIA, RICCARDO
To: HELSINN HEALTHCARE SA
Reel/Frame 045336/0334 →
Continuity (7)
Continuation 15003327 · Jan 21, 2016
Continuation 14069970 · Nov 1, 2013
Continuation 13077462 · Mar 31, 2011
Continuation PCTIB2010003106 · Nov 18, 2010
Provisional Application 61262470 · Nov 18, 2009
Provisional Application 61382709 · Sep 14, 2010
Related Publication 20180256567A1 · Sep 13, 2018