IP Library Granted Patent US 10,111,868
Granted Patent B2
US 10,111,868 · App. 15/341,594 · Granted Oct 30, 2018

Antineoplastic combinations containing HKI-272 and vinorelbine

Inventor: Charles Michael Zacharchuk (Westford, MA)
Assignee: WYETH LLC
A61K31/475A61K9/20A61K31/436A61K31/437A61K31/4709A61K31/4745A61N5/10
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Quick Facts
Patent No.
US 10,111,868
App. No.
15/341,594
Granted
Oct 30, 2018
Kind
B2
Abstract

A combination of HKI-272 compound and a vinorelbine compound in the treatment of a neoplasm is provided. Regimens, kits, and method 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 (22)

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

i) 100-300 mg 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; and

ii) vinorelbine, or a pharmaceutically acceptable salt thereof;

wherein the neoplasm:

a) overexpresses or amplifies HER-2; and

b) is selected from the group consisting of prostate cancer, myeloma, head and neck cancer, transitional cell carcinoma, and small cell and large cell neuroendocrine carcinoma of the uterine cervix.

2. The method of claim 1 , 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.

3. The method of claim 2 , wherein said unit dose is a tablet.

4. The method of claim 1 , 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 administered delivered intravenously or orally to said patient.

5. The method of claim 1 , 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.

6. The method of claim 1 , 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.

7. The method of claim 1 , 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.

8. The method of claim 1 , 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.

9. The method of claim 1 , 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 a dosing regimen.

10. The method of claim 1 , 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.

11. The method of claim 1 , wherein the vinorelbine is administered in a unit dose.

12. The method of claim 1 , wherein the vinorelbine is administered in an amount of at least about 20 mg/L.

13. The method of claim 1 , wherein the vinorelbine is administered in an amount of about 20 to about 25 mg/L.

14. The method of claim 1 , wherein the vinorelbine is administered in an amount of between 5-500 mg.

15. The method of claim 1 , wherein the patient has a neutrophil count of at least 1500, a platelet count of at least 100,000/L, or both.

16. The method of claim 1 , wherein the neoplasm is metastatic.

17. The method of claim 1 , wherein the neoplasm is an advanced solid tumor.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2018
From: ZACHARCHUK, CHARLES MICHAEL
To: WYETH
Reel/Frame 044991/0782 →
CHANGE OF NAME Recorded Feb 21, 2018
From: WYETH
To: WYETH LLC
Reel/Frame 045403/0056 →
Continuity (5)
Continuation 13875874 · May 2, 2013
Continuation 13404390 · Feb 24, 2012
Continuation 12486153 · Jun 17, 2009
Provisional Application 61073330 · Jun 17, 2008
Related Publication 20170231972A1 · Aug 17, 2017