IP Library Granted Patent US 10,604,569
Granted Patent B2
US 10,604,569 · App. 16/180,850 · Granted Mar 31, 2020

Humanized monoclonal antibodies that target protein tyrosine phosphatase-beta (HPTP-β/VE-PTP)

Inventors: Kevin Peters (Cincinnati, OH); Michael Allen Flynn (Ann Arbor, MI)
Assignee: AERPIO PHARMACEUTICALS, INC.
C07K16/28A61K39/3955C07K16/22C07K16/2896A61K2039/505A61K2039/507A61K2039/54A61K2039/545C07K2317/24C07K2317/33C07K2317/51C07K2317/515C07K2317/75C07K2317/76C07K2317/92
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Quick Facts
Patent No.
US 10,604,569
App. No.
16/180,850
Granted
Mar 31, 2020
Kind
B2
Abstract

The disclosure provides compositions and methods for the treatment of ocular conditions associated with angiogenesis comprising administering an antibody that targets a tyrosine phosphatase inhibitor in a subject.

Claims (50)

1. An antibody comprising:

a) a heavy chain that comprises: a sequence that is SEQ ID NO: 54; a sequence that is SEQ ID NO: 55; and a sequence that is SEQ ID NO: 56, wherein the sequence that is SEQ ID NO: 54; the sequence that is SEQ ID NO: 55; and the sequence that is SEQ ID NO: 56 are contained within a sequence that is at least 91% identical to any one of SEQ ID NOs: 9-12; and

b) a light chain that comprises: a sequence that is SEQ ID NO: 57; a sequence that is SEQ ID NO: 58; and a sequence that is SEQ ID NO: 59,

wherein the antibody binds human protein tyrosine phosphatase-beta (HPTP-β).

2. The antibody of claim 1 , wherein the antibody inhibits HPTP-β.

3. The antibody of claim 1 , wherein the antibody binds a first fibronectin type III (FN3) repeat of an extracellular domain of HPTP-β.

4. The antibody of claim 1 , wherein the sequence that is SEQ ID NO: 54; the sequence that is SEQ ID NO: 55; and the sequence that is SEQ ID NO: 56 are contained within a sequence that is any one of SEQ ID NOs: 9-12.

5. The antibody of claim 1 , wherein the sequence that is SEQ ID NO: 54; the sequence that is SEQ ID NO: 55; and the sequence that is SEQ ID NO: 56 are contained within a sequence that is at least 91% identical to SEQ ID NO: 9.

6. The antibody of claim 1 , wherein the sequence that is SEQ ID NO: 54; the sequence that is SEQ ID NO: 55; and the sequence that is SEQ ID NO: 56 are contained within a sequence that is at least 91% identical to SEQ ID NO: 10.

7. The antibody of claim 1 , wherein the sequence that is SEQ ID NO: 54; the sequence that is SEQ ID NO: 55; and the sequence that is SEQ ID NO: 56 are contained within a sequence that is at least 91% identical to SEQ ID NO: 11.

8. The antibody of claim 1 , wherein the sequence that is SEQ ID NO: 54; the sequence that is SEQ ID NO: 55; and the sequence that is SEQ ID NO: 56 are contained within a sequence that is at least 91% identical to SEQ ID NO: 12.

9. A pharmaceutical composition comprising a therapeutically effective amount of an antibody comprising:

a) a heavy chain that comprises: a sequence that is SEQ ID NO: 54; a sequence that is SEQ ID NO: 55; and a sequence that is SEQ ID NO: 56, wherein the sequence that is SEQ ID NO: 54; the sequence that is SEQ ID NO: 55; and the sequence that is SEQ ID NO: 56 are contained within a sequence that is at least 91% identical to any one of SEQ ID NOs: 9-12; and

b) a light chain that comprises: a sequence that is SEQ ID NO: 57; a sequence that is SEQ ID NO: 58; and a sequence that is SEQ ID NO: 59; and

a pharmaceutically-acceptable carrier,

wherein the antibody binds HPTP-β.

10. The pharmaceutical composition of claim 9 , wherein the composition is formulated for ophthalmic administration.

11. The pharmaceutical composition of claim 9 , wherein the composition is formulated for intravitreal administration.

12. The pharmaceutical composition of claim 9 , wherein the composition is formulated for intravenous administration.

13. The pharmaceutical composition of claim 9 , wherein the composition is formulated for subcutaneous administration.

14. The pharmaceutical composition of claim 9 , wherein the composition is formulated for topical administration.

15. The pharmaceutical composition of claim 9 , wherein the therapeutically effective amount of the antibody is from about 0.25 mg to about 200 mg.

16. The pharmaceutical composition of claim 9 , wherein the therapeutically effective amount of the antibody is from about 1 mg to about 50 mg.

17. The pharmaceutical composition of claim 9 , wherein the therapeutically effective amount of the antibody is from about 1 mg/kg to about 10 mg/kg.

18. The pharmaceutical composition of claim 9 , wherein the sequence that is SEQ ID NO: 54; the sequence that is SEQ ID NO: 55; and the sequence that is SEQ ID NO: 56 are contained within a sequence that is any one of SEQ ID NOs: 9-12.

19. An antibody comprising:

a) a heavy chain that comprises: a sequence that is SEQ ID NO: 54; a sequence that is SEQ ID NO: 55; and a sequence that is SEQ ID NO: 56; and

b) a light chain that comprises: a sequence that is SEQ ID NO: 57; a sequence that is SEQ ID NO: 58; and a sequence that is SEQ ID NO: 59, wherein the sequence that is SEQ ID NO: 57; the sequence that is SEQ ID NO: 58; and the sequence that is SEQ ID NO: 59 are contained within a sequence that is at least 83% identical to any one of SEQ ID NOs: 20-23,

wherein the antibody binds HPTP-β.

20. The antibody of claim 19 , wherein the antibody inhibits HPTP-β.

21. The antibody of claim 19 , wherein the antibody binds a first FN3 repeat of an extracellular domain of HPTP-β.

22. The antibody of claim 19 , wherein the sequence that is SEQ ID NO: 57; the sequence that is SEQ ID NO: 58; and the sequence that is SEQ ID NO: 59 are contained within a sequence that is any one of SEQ ID NOs: 20-23.

23. The antibody of claim 19 , wherein the sequence that is SEQ ID NO: 57; the sequence that is SEQ ID NO: 58; and the sequence that is SEQ ID NO: 59 are contained within a sequence that is at least 83% identical to SEQ ID NO: 20.

24. The antibody of claim 19 , wherein the sequence that is SEQ ID NO: 57; the sequence that is SEQ ID NO: 58; and the sequence that is SEQ ID NO: 59 are contained within a sequence that is at least 83% identical to SEQ ID NO: 21.

25. The antibody of claim 19 , wherein the sequence that is SEQ ID NO: 57; the sequence that is SEQ ID NO: 58; and the sequence that is SEQ ID NO: 59 are contained within a sequence that is at least 83% identical to SEQ ID NO: 22.

26. The antibody of claim 19 , wherein the sequence that is SEQ ID NO: 57; the sequence that is SEQ ID NO: 58; and the sequence that is SEQ ID NO: 59 are contained within a sequence that is at least 83% identical to SEQ ID NO: 23.

27. A pharmaceutical composition comprising a therapeutically effective amount of an antibody comprising:

a) a heavy chain that comprises: a sequence that is SEQ ID NO: 54; a sequence that is SEQ ID NO: 55; and a sequence that is SEQ ID NO: 56; and

b) a light chain that comprises: a sequence that is SEQ ID NO: 57; a sequence that is SEQ ID NO: 58; and a sequence that is SEQ ID NO: 59, wherein the sequence that is SEQ ID NO: 57; the sequence that is SEQ ID NO: 58; and the sequence that is SEQ ID NO: 59 are contained within a sequence that is at least 83% identical to any one of SEQ ID NOs: 20-23; and

a pharmaceutically-acceptable carrier,

wherein the antibody binds HPTP-β.

28. The pharmaceutical composition of claim 27 , wherein the composition is formulated for ophthalmic administration.

29. The pharmaceutical composition of claim 27 , wherein the composition is formulated for intravitreal administration.

30. The pharmaceutical composition of claim 27 , wherein the composition is formulated for intravenous administration.

31. The pharmaceutical composition of claim 27 , wherein the composition is formulated for subcutaneous administration.

32. The pharmaceutical composition of claim 27 , wherein the composition is formulated for topical administration.

33. The pharmaceutical composition of claim 27 , wherein the therapeutically effective amount of the antibody is from about 0.25 mg to about 200 mg.

34. The pharmaceutical composition of claim 27 , wherein the therapeutically effective amount of the antibody is from about 1 mg to about 50 mg.

35. The pharmaceutical composition of claim 27 , wherein the therapeutically effective amount of the antibody is from about 1 mg/kg to about 10 mg/kg.

36. The pharmaceutical composition of claim 27 , wherein the sequence that is SEQ ID NO: 57; the sequence that is SEQ ID NO: 58; and the sequence that is SEQ ID NO: 59 are contained within a sequence that is any one of SEQ ID NOs: 20-23.

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 049914/0399 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 6, 2018
From: PETERS, KEVIN; FLYNN, MICHAEL ALLEN
To: AERPIO THERAPEUTICS, INC.
Reel/Frame 047418/0438 →