IP Library Granted Patent US 9,938,346
Granted Patent B2
US 9,938,346 · App. 15/248,562 · Granted Apr 10, 2018

Monospecific and bispecific anti-IGF-1R and anti-ErbB3 antibodies

Inventors: Jason Baum (Needham, MA); Bryan Johnson (Natick, MA); Alexey Alexandrovich Lugovskoy (Woburn, MA); Lihui Xu (Chestnut Hill, MA); Neeraj Kohli (Brighton, MA); Jonathan Basil Fitzgerald (Arlington, MA); Sharlene Adams (Waltham, MA)
Assignee: Merrimack Pharmaceuticals, Inc.
C07K16/2863C07K16/2869C07K16/30C07K16/32C07K16/40C07K16/468A61K2039/505C07K2317/31C07K2317/33C07K2317/35C07K2317/52C07K2317/565C07K2317/60C07K2317/622C07K2317/76C07K2317/92C07K2317/94
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Quick Facts
Patent No.
US 9,938,346
App. No.
15/248,562
Granted
Apr 10, 2018
Kind
B2
Abstract

Provided are monospecific and bispecific antibodies that are useful as anti-neoplastic agents and that bind specifically to human IGF-1R and human ErbB3. Exemplary antibodies inhibit signal transduction through either or both of IGF-1R and ErbB3. Exemplary polyvalent proteins comprise at least one anti-IGF-1R binding site and at least one anti-ErbB3 binding site. In certain embodiments the binding sites may be linked through an immunoglobulin constant region. AntiErbB3 and anti-IGF-1R antibodies (e.g., monoclonal antibodies) are also provided.

Claims (24)

1. An antibody or antigen-binding portion thereof having an IGF-1R binding site comprising heavy and light chain variable regions, wherein the heavy chain variable region comprises a CDR1 comprising amino acids 26-35 of SEQ ID NO: 226, a CDR2 comprising amino acids 51-66 of SEQ ID NO: 226, and a CDR3 comprising amino acids 99-111 of SEQ ID NO: 226, and the light chain variable region comprises a CDR1 comprising amino acids 24-34 of SEQ ID NO: 204, a CDR2 comprising amino acids 50-56 of SEQ ID NO: 204, and a CDR3 comprising amino acids 89-97 of SEQ ID NO: 204.

2. The antibody or antigen-binding portion thereof of claim 1 , wherein the antibody or antigen-binding portion thereof is a monoclonal antibody.

3. The antibody or antigen-binding portion thereof of claim 1 , wherein the antibody or antigen-binding portion thereof is a bispecific antibody.

4. The antibody or antigen-binding portion thereof of claim 3 , wherein the bispecific antibody further comprises an ErbB3 binding site.

5. The antibody or antigen-binding portion thereof of claim 4 , wherein the ErbB3 binding site comprises heavy and light chain variable regions, wherein the heavy chain variable region comprises a CDR1 comprising amino acids 492-501 of SEQ ID NO: 226, a CDR2 comprising amino acids 517-532 of SEQ ID NO: 226, and a CDR3 comprising amino acids 565-577 of SEQ ID NO: 226, and the light chain variable region comprises a CDR1 comprising amino acids 634-644 of SEQ ID NO: 226, a CDR2 comprising amino acids 660-666 of SEQ ID NO: 226, and a CDR3 comprising amino acids 699-709 of SEQ ID NO: 226.

6. An antibody or antigen-binding portion thereof having an ErbB3 binding site comprising heavy and light chain variable regions, wherein the heavy chain variable region comprises a CDR1 comprising amino acids 492-501 of SEQ ID NO: 226, a CDR2 comprising amino acids 517-532 of SEQ ID NO: 226, and a CDR3 comprising amino acids 565-577 of SEQ ID NO: 226, and the light chain variable region comprises a CDR1 comprising amino acids 634-644 of SEQ ID NO: 226, a CDR2 comprising amino acids 660-666 of SEQ ID NO: 226, and a CDR3 comprising amino acids 699-709 of SEQ ID NO: 226.

7. The antibody or antigen-binding portion thereof of claim 6 , wherein the antibody or antigen-binding portion thereof is a monoclonal antibody.

8. The antibody or antigen-binding portion thereof of claim 6 , wherein the antibody or antigen-binding portion thereof is a bispecific antibody.

9. The antibody or antigen-binding portion thereof of claim 8 , wherein the bispecific antibody further comprises an IGF-1R binding site.

10. The antibody or antigen-binding portion thereof of claim 9 , wherein the IGF-1R binding site comprises heavy and light chain variable regions, wherein the heavy chain variable region comprises a CDR1 comprising amino acids 26-35 of SEQ ID NO: 226, a CDR2 comprising amino acids 51-66 of SEQ ID NO: 226, and a CDR3 comprising amino acids 99-111 of SEQ ID NO: 226, and the light chain variable region comprises a CDR1 comprising amino acids 24-34 of SEQ ID NO: 204, a CDR2 comprising amino acids 50-56 of SEQ ID NO: 204, and a CDR3 comprising amino acids 89-97 of SEQ ID NO: 204.

11. The antibody or antigen-binding portion thereof of claim 1 , wherein the antibody is an IgG, IgE, IgM, IgD, IgA, or IgY antibody.

12. The antibody or antigen-binding portion thereof of claim 11 , wherein the antibody is an IgG antibody.

13. The antibody or antigen-binding portion thereof of claim 12 , wherein the antibody is an IgG1, IgG2, IgG3, or IgG4 antibody.

14. A composition comprising the antibody or antigen-binding portion thereof of claim 1 and a pharmaceutically acceptable carrier.

15. The composition of claim 14 , wherein the carrier is suitable for injection or infusion.

16. A method of treating a cancer comprising administering to a subject in need thereof a therapeutically effective amount of the antibody or antigen-binding portion thereof of claim 1 .

17. A kit comprising the antibody or antigen-binding portion thereof of claim 1 .

18. The antibody or antigen-binding portion thereof of claim 6 , wherein the antibody is an IgG, IgE, IgM, IgD, IgA, or IgY antibody.

19. The antibody or antigen-binding portion thereof of claim 18 , wherein the antibody is an IgG antibody.

20. The antibody or antigen-binding portion thereof of claim 19 , wherein the antibody is an IgG1, IgG2, IgG3, or IgG4 antibody.

21. A composition comprising the antibody or antigen-binding portion thereof of claim 6 and a pharmaceutically acceptable carrier.

22. The composition of claim 21 , wherein the carrier is suitable for injection or infusion.

23. A method of treating a cancer comprising administering to a subject in need thereof a therapeutically effective amount of the antibody or antigen-binding portion thereof of claim 6 .

24. A kit comprising the antibody or antigen-binding portion thereof of claim 6 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 27, 2016
From: BAUM, JASON; JOHNSON, BRYAN; LUGOVSKOY, ALEXEY ALEXANDROVICH; XU, LIHUI; KOHLI, NEERAJ; FITZGERALD, JONATHAN BASIL; ADAMS, SHARLENE
To: MERRIMACK PHARMACEUTICALS, INC.
Reel/Frame 040150/0964 →
Continuity (8)
Continuation 14857344 · Sep 17, 2015
Continuation 13778984 · Feb 27, 2013
Continuation 13451135 · Apr 19, 2012
Provisional Application 61619244 · Apr 2, 2012
Provisional Application 61539297 · Sep 26, 2011
Provisional Application 61558192 · Nov 10, 2011
Provisional Application 61477089 · Apr 19, 2011
Related Publication 20170051063A1 · Feb 23, 2017