IP Library › Granted Patent US 9,539,245
Granted Patent B2
US 9,539,245 · App. 14/819,871 · Granted Jan 10, 2017

Combination of immunotherapies with activators of Tie-2

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Quick Facts
Patent No.
US 9,539,245
App. No.
14/819,871
Granted
Jan 10, 2017
Kind
B2
Abstract

The present invention relates to combination therapies comprising at least one activator of Tie-2 and immunotherapies that target immune checkpoints. Combination therapies of the disclosure can provide therapeutic effects not obtained with singly-administered immunotherapies. Combination therapies can be used to increase the therapeutic efficacy of an immunotherapy, to provide lower dosages of an immunotherapy being administered, to lower a toxicity of an immunotherapy, or to manage a side effect of an immunotherapy.

Claims (46)

1. A method of treating cancer, the method comprising administering to a subject in need thereof:

a) a therapeutically-effective amount of a Tie-2 activator; and

b) a therapeutically-effective amount of a modulator of an immune checkpoint molecule.

2. The method of claim 1 , wherein the Tie-2 activator binds a phosphatase.

3. The method of claim 1 , wherein the Tie-2 activator inhibits a phosphatase.

4. The method of claim 1 , wherein the Tie-2 activator binds HPTPβ.

5. The method of claim 1 , wherein the Tie-2 activator inhibits HPTPβ.

6. The method of claim 1 , wherein the Tie-2 activator is:

or a pharmaceutically-acceptable salt thereof.

7. The method of claim 1 , wherein the immune checkpoint molecule is LAGS.

8. The method of claim 1 , wherein the immune checkpoint molecule is BTLA.

9. The method of claim 1 , wherein the immune checkpoint molecule is KIR.

10. The method of claim 1 , wherein the immune checkpoint molecule is CTLA4.

11. The method of claim 1 , wherein the immune checkpoint molecule is ICOS.

12. The method of claim 1 , wherein the immune checkpoint molecule is TIM3.

13. The method of claim 1 , wherein the immune checkpoint molecule is A2aR.

14. The method of claim 1 , wherein the immune checkpoint molecule is PD-1.

15. The method of claim 1 , wherein the modulator of the immune checkpoint molecule is ipilimumab.

16. The method of claim 1 , wherein the modulator of the immune checkpoint molecule is nivolumab.

17. The method of claim 1 , wherein the modulator of the immune checkpoint molecule is tremelimumab.

18. The method of claim 1 , wherein the modulator of the immune checkpoint molecule is A-dmDT390-bisFv(UCHT1).

19. The method of claim 1 , wherein the therapeutically-effective amount of the Tie-2 activator is from about 1 mg to about 100 mg.

20. The method of claim 1 , wherein the therapeutically-effective amount of the Tie-2 activator is about 15 mg.

21. The method of claim 1 , wherein the Tie-2 activator and the modulator of the immune checkpoint molecule are administered in the same unit dosage form.

22. The method of claim 1 , wherein the subject is human.

23. A pharmaceutical composition comprising:

a) a Tie-2 activator; and

b) a modulator of an immune checkpoint molecule, wherein the Tie-2 activator and the modulator of the immune checkpoint molecule are in the same unit dosage form.

24. The pharmaceutical composition of claim 23 , wherein the Tie-2 activator binds a phosphatase.

25. The pharmaceutical composition of claim 23 , wherein the Tie-2 activator inhibits a phosphatase.

26. The pharmaceutical composition of claim 23 , wherein the Tie-2 activator binds HPTPβ.

27. The pharmaceutical composition of claim 23 , wherein the Tie-2 activator inhibits HPTPβ.

28. The pharmaceutical composition of claim 23 , wherein the Tie-2 activator is:

or a pharmaceutically-acceptable salt thereof.

29. The pharmaceutical composition of claim 23 , wherein the immune checkpoint molecule is LAG3.

30. The pharmaceutical composition of claim 23 , wherein the immune checkpoint molecule is BTLA.

31. The pharmaceutical composition of claim 23 , wherein the immune checkpoint molecule is KIR.

32. The pharmaceutical composition of claim 23 , wherein the immune checkpoint molecule is CTLA4.

33. The pharmaceutical composition of claim 23 , wherein the immune checkpoint molecule is ICOS.

34. The pharmaceutical composition of claim 23 , wherein the immune checkpoint molecule is TIM3.

35. The pharmaceutical composition of claim 23 , wherein the immune checkpoint molecule is A2aR.

36. The pharmaceutical composition of claim 23 , wherein the immune checkpoint molecule is PD-1.

37. The pharmaceutical composition of claim 23 , wherein the modulator of the immune checkpoint molecule is ipilimumab.

38. The pharmaceutical composition of claim 23 , wherein the modulator of the immune checkpoint molecule is nivolumab.

39. The pharmaceutical composition of claim 23 , wherein the modulator of the immune checkpoint molecule is tremelimumab.

40. The pharmaceutical composition of claim 23 , wherein the modulator of the immune checkpoint molecule is A-dmDT390-bisFv(UCHT1).

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 9, 2021
From: AERPIO PHARMACEUTICALS, INC.
To: EYEPOINT PHARMACEUTICALS, INC.
Reel/Frame 057448/0033 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 17, 2020
From: AERPIO THERAPEUTICS LLC
To: AERPIO PHARMACEUTICALS, INC.
Reel/Frame 052432/0789 →
CHANGE OF NAME Recorded Jul 31, 2019
From: AERPIO THERAPEUTICS, INC.
To: AERPIO THERAPEUTICS LLC
Reel/Frame 049924/0458 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 21, 2015
From: PETERS, KEVIN
To: AERPIO THERAPEUTICS, INC.
Reel/Frame 036393/0015 →