IP Library Granted Patent US 12,102,680
Granted Patent B2
US 12,102,680 · App. 16/806,658 · Granted Oct 1, 2024

Anti-TIGIT antibodies

Inventors: Sybil M. G. Williams (Wayland, MA); Drake LaFace (Half Moon Bay, CA); Laurence Fayadat-Dilman (Sunnyvale, CA); Gopalan Raghunathan (San Diego, CA); Linda Liang (Mountain View, CA); Wolfgang Seghezzi (Mountain View, CA)
Assignee: Merck Sharp & Dohme LLC
A61K39/39541A61K39/3955A61K45/06C07K16/28C07K16/2803C07K16/2818A61K2039/505A61K2039/507C07K2317/21C07K2317/24C07K2317/34C07K2317/52C07K2317/56C07K2317/565C07K2317/73C07K2317/74C07K2317/76C07K2317/92
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Quick Facts
Patent No.
US 12,102,680
App. No.
16/806,658
Granted
Oct 1, 2024
Kind
B2
Abstract

The present invention relates to anti-TIGIT antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.

Claims (48)

1. A method of treating a human subject with cancer in need thereof, comprising administering to the subject an effective amount of a monoclonal antibody or antigen binding fragment thereof that binds to human TIGIT, wherein the monoclonal antibody and antigen binding fragment thereof comprise a heavy chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:88, a heavy chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:89, a heavy chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:90, a light chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:91, a light chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:92, and a light chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:93,

optionally in association with a further therapeutic agent or therapeutic procedure.

2. A method of treating a human subject having an infection or infectious disease, comprising administering to the subject an effective amount of a monoclonal antibody or antigen binding fragment thereof that binds to human TIGIT, wherein the monoclonal antibody and antigen binding fragment thereof comprise a heavy chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:88, a heavy chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:89, a heavy chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:90, a light chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:91, a light chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:92, and a light chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:93,

optionally in association with a further therapeutic agent or therapeutic procedure.

3. A method of treating a human subject with cancer in need thereof, comprising administering to the subject an effective amount of a monoclonal antibody or antigen binding fragment thereof that binds to human TIGIT, wherein the monoclonal antibody and antigen binding fragment thereof comprise a heavy chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:88, a heavy chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:134, a heavy chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:90, a light chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:91, a light chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:92, and a light chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:93.

4. The method of claim 3 , wherein the monoclonal antibody and antigen binding fragment thereof comprise:

a) a heavy chain variable region comprising the amino acid sequence of SEQ ID NO:128 and a light chain variable region comprising the amino acid sequence of SEQ ID NO:132;

b) a heavy chain variable region comprising the amino acid sequence of SEQ ID NO:127 and a light chain variable region comprising the amino acid sequence of SEQ ID NO:130;

c) a heavy chain variable region comprising the amino acid sequence of SEQ ID NO:128 and a light chain variable region comprising the amino acid sequence of SEQ ID NO:133;

d) a heavy chain variable region comprising at least 97% identity to SEQ ID NO: 128 and a light chain variable region comprising at least 97% identity to SEQ ID NO: 132, wherein any sequence variations occur in the framework regions of the monoclonal antibody;

e) a heavy chain variable region comprising at least 97% identity to SEQ ID NO:127 and a light chain variable region comprising at least 97% identity to SEQ ID NO: 130, wherein any sequence variations occur in the framework regions of the monoclonal antibody; or

f) a heavy chain variable region comprising at least 97% identity to SEQ ID NO:128 and a light chain variable region comprising at least 97% identity to SEQ ID NO: 133, wherein any sequence variations occur in the framework regions of the monoclonal antibody.

5. The method of claim 1 , wherein the monoclonal antibody and antigen binding fragment thereof comprise a heavy chain variable region comprising at least 97% identity to the amino acid sequence of SEQ ID NO: 94 and a light chain variable region comprising at least 97% identity to the amino acid sequence of SEQ ID NO:95.

6. The method of claim 3 , wherein the monoclonal antibody and antigen binding fragment thereof comprise two heavy chains and two light chains.

7. The method of claim 3 , wherein the monoclonal antibody comprises a human IgG1 constant domain and a human kappa constant domain.

8. The method of claim 7 , wherein the human IgG1 constant domain comprises SEQ ID NO: 86 and the human kappa constant domain comprises SEQ ID NO: 56.

9. A method of treating a human subject having an infection or infectious disease, comprising administering to the subject an effective amount of a monoclonal antibody or antigen binding fragment thereof that binds to human TIGIT, wherein the monoclonal antibody and antigen binding fragment thereof comprise a heavy chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:88, a heavy chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:134, a heavy chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:90, a light chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:91, a light chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:92, and a light chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:93.

10. The method of claim 9 , wherein the monoclonal antibody and antigen binding fragment thereof comprise:

a) a heavy chain variable region comprising the amino acid sequence of SEQ ID NO:128 and a light chain variable region comprising the amino acid sequence of SEQ ID NO:132;

b) a heavy chain variable region comprising the amino acid sequence of SEQ ID NO:127 and a light chain variable region comprising the amino acid sequence of SEQ ID NO:130;

c) a heavy chain variable region comprising the amino acid sequence of SEQ ID NO:128 and a light chain variable region comprising the amino acid sequence of SEQ ID NO:133;

d) a heavy chain variable region comprising at least 97% identity to SEQ ID NO:128 and a light chain variable region comprising at least 97% identity to SEQ ID NO: 132, wherein any sequence variations occur in the framework regions of the monoclonal antibody;

e) a heavy chain variable region comprising at least 97% identity to SEQ ID NO: 127 and a light chain variable region comprising at least 97% identity to SEQ ID NO: 130, wherein any sequence variations occur in the framework regions of the monoclonal antibody; or

f) a heavy chain variable region comprising at least 97% identity to SEQ ID NO:128 and a light chain variable region comprising at least 97% identity to SEQ ID NO: 133, wherein any sequence variations occur in the framework regions of the monoclonal antibody.

11. The method of claim 3 , wherein the monoclonal antibody and antigen binding fragment thereof comprise a heavy chain variable region comprising the amino acid sequence of SEQ ID NO:128 and a light chain variable region comprising the amino acid sequence of SEQ ID NO:132.

12. The method of claim 9 , wherein the monoclonal antibody and antigen binding fragment thereof comprise a heavy chain variable region comprising the amino acid sequence of SEQ ID NO:128 and a light chain variable region comprising the amino acid sequence of SEQ ID NO:132.

13. The method of claim 12 , wherein the monoclonal antibody and antigen binding fragment thereof comprise a human IgG1 constant domain comprising SEQ ID NO: 86 and a human kappa constant domain comprising SEQ ID NO: 56.

14. A method of treating a human subject with cancer in need thereof, comprising administering to the subject (a) an effective amount of a monoclonal antibody that binds to human TIGIT and (b) an effective amount of pembrolizumab, wherein the monoclonal antibody comprises two heavy chains and two light chains;

wherein each of the heavy chains comprises a heavy chain variable region comprising the amino acid sequence of SEQ ID NO: 128; and

wherein each of the light chains comprises a light chain variable region comprising the amino acid sequence of SEQ ID NO:132.

15. The method of claim 14 , wherein the monoclonal antibody comprises a human IgG1 constant domain and a human kappa constant domain.

16. The method of claim 15 , wherein the human IgG1 constant domain comprises SEQ ID NO: 86 and the human kappa constant domain comprises SEQ ID NO: 56.

17. The method of claim 16 , wherein the cancer is lung cancer.

18. The method of claim 17 , wherein the cancer is non-small cell lung cancer.

19. A method of treating a human subject with cancer in need thereof, comprising administering to the subject (a) an effective amount of a monoclonal antibody that binds to human TIGIT and (b) an effective amount of pembrolizumab,

wherein the monoclonal antibody comprises two heavy chains and two light chains; and

wherein the monoclonal antibody comprises a heavy chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:88, a heavy chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:134, a heavy chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:90, a light chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:91, a light chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:92, and a light chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:93.

20. The method of claim 19 , wherein the monoclonal antibody comprises a human IgG1 constant domain and a human kappa constant domain.

21. The method of claim 20 , wherein the human IgG1 constant domain comprises SEQ ID NO: 86 and the human kappa constant domain comprises SEQ ID NO: 56.

22. The method of claim 21 , wherein the cancer is lung cancer.

23. The method of claim 22 , wherein the cancer is non-small cell lung cancer.

24. The method of claim 8 , wherein the cancer is lung cancer.

25. The method of claim 24 , wherein the cancer is non-small cell lung cancer.

26. The method of claim 11 , wherein the monoclonal antibody or antigen binding fragment thereof is a monoclonal antibody, wherein the monoclonal antibody comprises two heavy chains and two light chains.

27. The method of claim 26 , wherein the monoclonal antibody comprises a human IgG1 constant domain and a human kappa constant domain.

28. The method of claim 27 , wherein the human IgG1 constant domain comprises SEQ ID NO: 86 and the human kappa constant domain comprises SEQ ID NO: 56.

29. The method of claim 28 , wherein the cancer is lung cancer.

30. The method of claim 29 , wherein the cancer is non-small cell lung cancer.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 6, 2024
From: WILLIAMS, SYBIL M.G.; LAFACE, DRAKE; FAYADAT-DILMAN, LAURENCE; RAGHUNATHAN, GOPALAN; LIANG, LINDA; SEGHEZZI, WOLFGANG
To: MERCK SHARP & DOHME CORP.
Reel/Frame 067327/0691 →
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
Continuity (5)
Division 15817691 · Nov 20, 2017
Continuation 15121624
Provisional Application 62126733 · Mar 2, 2015
Provisional Application 62038912 · Aug 19, 2014
Related Publication 20200270346A1 · Aug 27, 2020