IP Library › Granted Patent US 9,511,063
Granted Patent B2
US 9,511,063 · App. 13/875,874 · Granted Dec 6, 2016

Antineoplastic combinations containing HKI-272 and vinorelbine

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Quick Facts
Patent No.
US 9,511,063
App. No.
13/875,874
Granted
Dec 6, 2016
Kind
B2
Abstract

A combination of HKI-272 compound and a vinorelbine compound in the treatment of a neoplasm is provided. Regimens, kits, and methods for treatment of neoplasm, including breast cancer including metastatic breast cancer, and lung cancer, using this combination, optionally in combination with other anti-neoplastic agents, or immune modulators are also described.

Claims (51)

1. A method for treating a neoplasm in a patient in need thereof, consisting of administering to the patient:

i) an effective amount of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or an ester, ether, carbamate, or a pharmaceutically acceptable salt thereof; and

ii) vinorelbine, or a pharmaceutically acceptable salt thereof;

wherein the neoplasm is selected from the group consisting of a lung cancer and breast cancer.

2. The method of claim 1 , wherein the method administers an effective amount of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or a pharmaceutically acceptable salt thereof.

3. The method of claim 2 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered in a unit dose.

4. The method of claim 3 , wherein said unit dose is a tablet.

5. The method of claim 2 , wherein one or both of the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, and the vinorelbine are delivered intravenously or orally to said patient.

6. The method of claim 2 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered in an amount of at least about 120 mg.

7. The method of claim 6 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered in an amount of at least about 160 mg.

8. The method of claim 7 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered in an amount of at least about 240 mg.

9. The method of claim 2 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered daily.

10. The method of claim 2 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered at least once daily.

11. The method of claim 2 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered on day 1 of said regimen.

12. The method of claim 2 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered for at least 2 continuous weeks.

13. The method of claim 2 , wherein the method administers vinorelbine.

14. The method of claim 13 , wherein the vinorelbine is administered in a unit dose.

15. The method of claim 13 , wherein the vinorelbine is administered in an amount of at least about 20 mg/L.

16. The method of claim 13 , wherein the vinorelbine is administered in an amount of about 20 to about 25 mg/L.

17. The method of claim 2 , wherein the administering steps occur concurrently, sequentially, simultaneously, in a specified order, or according to a specific temporal relationship.

18. The method of claim 2 , wherein the neoplasm is metastatic.

19. The method of claim 2 , wherein the neoplasm is an advanced solid tumor.

20. The method of claim 2 , wherein the patient has a neutrophil count of at least 1500, a platelet count of at least 100,000/L, or both.

21. The method of claim 13 , wherein the vinorelbine is administered in an amount of between 5-500 mg.

22. The method of claim 2 , wherein the neoplasm overexpresses or amplifies HER-2.

23. The method of claim 2 , wherein the neoplasm is lung cancer.

24. The method of claim 2 , wherein the neoplasm is breast cancer.

25. The method of claim 2 , wherein the neoplasm is metastatic breast cancer.

26. A method for treating a HER-2 positive breast cancer in a patient in need thereof, consisting of administering to the patient:

i) an effective amount of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or an ester, ether, carbamate, or a pharmaceutically acceptable salt thereof; and

ii) vinorelbine, or a pharmaceutically acceptable salt thereof.

27. The method of claim 26 , wherein the method administers an effective amount of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or a pharmaceutically acceptable salt thereof.

28. The method of claim 27 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered in a unit dose.

29. The method of claim 28 , wherein said unit dose is a tablet.

30. The method of claim 27 , wherein one or both of the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, and the vinorelbine are delivered intravenously or orally to said patient.

31. The method of claim 27 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered in an amount of at least about 120 mg.

32. The method of claim 31 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered in an amount of at least about 160 mg.

33. The method of claim 32 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered in an amount of at least about 240 mg.

34. The method of claim 27 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered daily.

35. The method of claim 27 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered at least once daily.

36. The method of claim 27 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered on day 1 of said regimen.

37. The method of claim 27 , wherein the (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, or pharmaceutically acceptable salt thereof, is administered for at least 2 continuous weeks.

38. The method of claim 27 , wherein the method administers vinorelbine.

39. The method of claim 38 , wherein the vinorelbine is administered in a unit dose.

40. The method of claim 38 , wherein the vinorelbine is administered in an amount of at least about 20 mg/L.

41. The method of claim 38 , wherein the vinorelbine is administered in an amount of about 20 to about 25 mg/L.

42. The method of claim 38 , wherein the vinorelbine is administered in an amount of between 5-500 mg.

43. The method of claim 27 , wherein the administering steps occur concurrently, sequentially, simultaneously, in a specified order, or according to a specific temporal relationship.

44. The method of claim 27 , wherein the HER-2 positive breast cancer is HER-2 positive metastatic breast cancer.

45. The method of claim 27 , wherein the HER-2 positive breast cancer is an advanced solid tumor.

46. The method of claim 27 , wherein the patient has a neutrophil count of at least 1500, a platelet count of at least 100,000/L, or both.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 12, 2014
From: ZACHARCHUK, CHARLES MICHAEL
To: WYETH
Reel/Frame 033091/0041 →
CHANGE OF NAME Recorded Jun 12, 2014
From: WYETH
To: WYETH LLC
Reel/Frame 033136/0741 →