IP Library Granted Patent US 11,028,183
Granted Patent B2
US 11,028,183 · App. 16/156,382 · Granted Jun 8, 2021

HER2/neu-specific antibodies and methods of using same

Inventors: Leslie S. Johnson (Darnestown, MD); Ling Huang (Bethesda, MD); Nadine Tuaillon (Smithland, KY); Ezio Bonvini (Potomac, MD)
Assignee: MacroGenics, Inc.
C07K16/32A61K39/39558A61K45/06A61K2039/505A61K2039/54C07K2317/24C07K2317/51C07K2317/515C07K2317/71C07K2317/732C07K2317/92
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Quick Facts
Patent No.
US 11,028,183
App. No.
16/156,382
Granted
Jun 8, 2021
Kind
B2
Abstract

This invention relates to antibodies that specifically bind HER2/neu, and particularly chimeric 4D5 antibodies to HER2/neu, which have reduced glycosylation as compared to known 4D5 antibodies. The invention also relates to methods of using the 4D5 antibodies and compositions comprising them in the diagnosis, prognosis and therapy of diseases such as cancer, autoimmune diseases, inflammatory disorders, and infectious disease.

Claims (45)

1. A method of treating a HER2/neu-expressing cancer in a patient in need thereof having a CD16A Fc Receptor comprising a Phe at position 158, comprising administering to said patient a therapeutically effective amount of an antibody that binds human HER2/neu and comprises:

(A) an immunoglobulin light chain comprising an amino acid sequence of SEQ ID NO: 2; and

(B) an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 9, SEQ ID NO: 11, or SEQ ID NO: 13.

2. The method of claim 1 , wherein said antibody is administered by intravenous infusion.

3. The method of claim 1 , comprising the further step of administering a second therapeutic agent simultaneously or sequentially with said antibody.

4. The method of claim 3 , wherein said second therapeutic agent and said antibody are administered no more than 12 hours apart, or no more than 24 hours apart, or no more than 96 hours apart.

5. The method of claim 3 , wherein said second therapeutic agent is selected from the group consisting of an anti-angiogenic agent, an anti-neoplastic agent, a chemotherapeutic agent, and a cytotoxic agent.

6. The method of claim 3 , wherein said second therapeutic agent is selected from the group consisting of an anti-mitotic agent, a hormone therapy agent, and an aromatase inhibitor.

7. The method of claim 1 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

8. The method of claim 2 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

9. The method of claim 3 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

10. The method of claim 4 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

11. The method of claim 5 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

12. The method of claim 6 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

13. A method of treating a HER2/neu-expressing cancer in a patient in need thereof having a CD16A Fc Receptor comprising a Phe at position 158, comprising administering to said patient a therapeutically effective amount of a pharmaceutical composition comprising an antibody that binds human HER2/neu and comprises:

(A) an immunoglobulin light chain comprising an amino acid sequence of SEQ ID NO: 2; and

(B) an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 9, SEQ ID NO: 11, or SEQ ID NO: 13; and

(C) a pharmaceutically acceptable carrier and/or an excipient.

14. The method of claim 13 , further comprising the steps of:

providing said pharmaceutical composition as a sterile liquid in a hermetically sealed container; and

extracting said pharmaceutical composition from said hermetically sealed container prior to said administering step.

15. The method of claim 14 wherein the concentration of said antibody in said sterile liquid is at least 1 mg/ml.

16. The method of claim 13 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

17. The method of claim 14 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

18. The method of claim 15 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

19. The method of claim 14 , wherein the concentration of said antibody in said sterile liquid is at least 2.5 mg/ml.

20. The method of claim 14 , wherein the concentration of said antibody in said sterile liquid is at least 5 mg/ml.

21. The method of claim 14 , wherein the concentration of said antibody in said sterile liquid is at least 8 mg/ml.

22. The method of claim 14 , wherein the concentration of said antibody in said sterile liquid is at least 10 mg/ml.

23. The method of claim 14 , wherein the concentration of said antibody in said sterile liquid is at least 15 mg/ml.

24. The method of claim 14 , wherein the concentration of said antibody in said sterile liquid is at least 25 mg/ml.

25. The method of claim 14 , wherein the concentration of said antibody in said sterile liquid is at least 50 mg/ml.

26. The method of claim 14 , wherein the concentration of said antibody in said sterile liquid is at least 100 mg/ml.

27. The method of claim 14 , wherein the concentration of said antibody in said sterile liquid is at least 150 mg/ml.

28. The method of claim 14 , wherein the concentration of said antibody in said sterile liquid is at least 200 mg/ml.

29. The method of claim 19 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

30. The method of claim 20 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

31. The method of claim 21 wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

32. The method of claim 22 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

33. The method of claim 23 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

34. The method of claim 24 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

35. The method of claim 25 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

36. The method of claim 26 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

37. The method of claim 27 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

38. The method of claim 28 , wherein said antibody comprises an immunoglobulin heavy chain comprising an amino acid sequence of SEQ ID NO: 11.

Assignments (5)
RELEASE OF SECOND LIEN PATENT SECURITY AGREEMENT RECORDED AT R/F 069451/0158 Recorded Jan 8, 2025
From: NEWSTONE CAPITAL PARTNERS, LLC
To: TERSERA THERAPEUTICS LLC
Reel/Frame 069840/0730 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 18, 2024
From: MACROGENICS, INC.
To: TERSERA THERAPEUTICS LLC
Reel/Frame 069626/0659 →
SECURITY INTEREST Recorded Dec 2, 2024
From: TERSERA THERAPEUTICS LLC
To: NEWSTONE CAPITAL PARTNERS, LLC
Reel/Frame 069451/0158 →
FIRST LIEN PATENT SECURITY AGREEMENT Recorded Nov 26, 2024
From: TERSERA THERAPEUTICS LLC
To: ANTARES CAPITAL LP, AS AGENT
Reel/Frame 069447/0210 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 30, 2019
From: JOHNSON, LESLIE S.; HUANG, LING; TUAILLON, NADINE; BONVINI, EZIO
To: MACROGENICS, INC.
Reel/Frame 048189/0904 →
Continuity (6)
Continuation 15266421 · Sep 15, 2016
Continuation 14994892 · Jan 13, 2016
Continuation 14332239 · Jul 15, 2014
Division 12933885
Provisional Application 61041649 · Apr 2, 2008
Related Publication 20190233539A1 · Aug 1, 2019