IP Library Granted Patent US 10,028,958
Granted Patent B2
US 10,028,958 · App. 14/690,001 · Granted Jul 24, 2018

Methods of treating cancer with a combination of selected MEK1/2 and AXL inhibitors

Inventors: Miles Aaron Miller (Boston, MA); Madeleine Oudin (Boston, MA); Aaron Samuel Meyer (Boston, MA); Frank B. Gertler (Boston, MA); Linda G. Griffith (Cambridge, MA); Douglas A. Lauffenburger (Cambridge, MA)
Assignee: Massachusetts Institute of Technology
A61K31/519A61K31/381A61K31/437A61K31/44A61K31/502A61K31/506A61K31/5025A61K31/5377A61K31/5383A61K39/3955A61K45/06C07K16/38C07K2317/76
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Quick Facts
Patent No.
US 10,028,958
App. No.
14/690,001
Granted
Jul 24, 2018
Kind
B2
Abstract

Methods, compounds and kits relating to treating cancer, reducing kinase inhibitor or resistance, and reducing or preventing diminished ectodomain shedding are described.

Claims (25)

1. A method of treating a cancer in an individual comprising administering a therapeutically effective amount of a MEK1/2 inhibitor and an AXL inhibitor,

wherein the MEK1/2 inhibitor is selected from the group consisting of PD325901, AZD6244 (selumetinib), and trametinib (GSK1120212): and

wherein the AXL inhibitor is selected from the group consisting of R428, MP-470 (amuvatinib), and XL-880 (foretinib).

2. The method of claim 1 , further comprising administering an additional therapeutic agent.

3. A method of treating a cancer in an individual comprising administering a therapeutically effective amount of a MEK1/2 inhibitor, an AXL inhibitor and a tissue inhibitor of metalloproteinase 1 (TIMP1) inhibitor.

4. The method of claim 3 , wherein the tissue inhibitor of metalloproteinase 1 (TIMP1) inhibitor is a TIMP1 neutralizing antibody.

5. The method of claim 1 , wherein the cancer is a carcinoma, sarcoma, lymphoma, leukemia, or blastoma.

6. The method of claim 5 , wherein the carcinoma is a breast cancer, a melanoma, a lung cancer or an ovarian cancer.

7. The method of claim 6 , wherein the breast cancer expresses low estrogen receptor, progesterone receptor, HER2, or a combination thereof triple-negative breast cancer (TNBC).

8. The method of claim 5 , wherein the blastoma is glioblastoma multiforme.

9. The method of claim 1 , wherein the MEK1/2 inhibitor is administered to the individual at or near the same time as the AXL inhibitor.

10. The method of claim 1 , wherein the MEK1/2 inhibitor is administered before or after administration of the AXL inhibitor to the individual.

11. The method of claim 1 , wherein the MEK1/2 inhibitor and the AXL inhibitor are administered to the individual in a single formulation.

12. The method of claim 1 , wherein the MEK1/2 inhibitor and the AXL inhibitor are administered to the individual in different formulations.

13. The method of claim 1 , wherein administering the MEK1/2 inhibitor and AXL inhibitor reduces tumor growth in the individual.

14. The method of claim 1 , wherein administering the MEK1/2 inhibitor and AXL inhibitor reduces metastasis in the individual.

15. A method of treating a cancer in an individual comprising administering a therapeutically effective amount of a MEK inhibitor, an AXL inhibitor, and a BRAF inhibitor,

wherein the MEK1/2 inhibitor is selected from the group consisting of PD325901, AZD6244 (selumetinib), and trametinib (GSK1120212); and

wherein the AXL inhibitor is selected from the group consisting of R428, MP-470 (amuvatinib), and XL-880 (foretinib).

16. The method of claim 1 , wherein the AXL inhibitor is R428.

17. The method of claim 1 , wherein the MEK1/2 inhibitor is PD325901 or AZD6244 (selumetinib).

18. The method of claim 15 , wherein the MEK1/2 inhibitor is PD325901 or AZD6244 (selumetinib).

19. The method of claim 1 , wherein the MEK1/2 inhibitor is PD325901 or AZD6244 (selumetinib) and wherein the AXL inhibitor is R428.

20. The method of claim 15 , wherein the AXL inhibitor R428.

21. The method of claim 15 , wherein the MEK1/2 inhibitor is PD325901 or AZD6244 (selumetinib) and wherein the AXL inhibitor is R428.

Assignments (5)
CONFIRMATORY LICENSE Recorded Nov 18, 2019
From: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
To: THE GOVERNMENT OF THE UNITED STATES, AS REPRESENTED BY THE SECRETARY OF THE ARMY
Reel/Frame 051041/0929 →
CONFIRMATORY LICENSE Recorded Nov 18, 2019
From: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
To: THE GOVERNMENT OF THE UNITED STATES, AS REPRESENTED BY THE SECRETARY OF THE ARMY
Reel/Frame 051041/0947 →
CONFIRMATORY LICENSE Recorded Aug 17, 2016
From: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
To: US ARMY, SECRETARY OF THE ARMY
Reel/Frame 039707/0719 →
CONFIRMATORY LICENSE Recorded Jul 5, 2016
From: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 039252/0962 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 3, 2016
From: GERTLER, FRANK B.; GRIFFITH, LINDA G.; LAUFFENBURGER, DOUGLAS A.; MEYER, AARON SAMUEL; MILLER, MILES AARON; OUDIN, MADELEINE
To: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Reel/Frame 037657/0763 →
Continuity (3)
Provisional Application 62073887 · Oct 31, 2014
Provisional Application 61981741 · Apr 19, 2014
Related Publication 20160067250A1 · Mar 10, 2016