IP Library Granted Patent US 12697385
Granted Patent B2
US 12697385 · App. 17/224,865 · Granted Aug 4, 2026

Combination therapy for cancer with anti-B7-H4 antibodies and anti-PD-1 antibodies

Inventors: Sandeep P. Inamdar (South San Francisco, CA); Helen L. Collins (South San Francisco, CA); Hong Xiang (South San Francisco, CA); Xiang Zhang (South San Francisco, CA); Neyssa Marina (South San Francisco, CA)
Assignee: FIVE PRIME THERAPEUTICS, INC.
A61K39/3955A61P35/00A61K39/00A61K2039/505A61K2039/507A61K2039/545C07K16/2818C07K16/2827C07K2317/24C07K2317/41C07K2317/51C07K2317/515C07K2317/565C07K2317/76
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Quick Facts
Patent No.
US 12697385
App. No.
17/224,865
Granted
Aug 4, 2026
Kind
B2
Abstract

The present disclosure provides methods of administering antibodies and antigen-binding fragments thereof that specifically bind to human B7-H4 to a subject in need thereof, for example, a cancer patient, in combination with a PD-1/PD-L1 antagonist, such as an anti-PD-1 antibody.

Claims (51)

1 . A method of treating a solid tumor in a human subject, the method comprising administering to the subject

(i) about 0.1 to about 20 mg/kg of an anti-B7-H4 antibody or antigen-binding fragment thereof that specifically binds to human B7-H4 and comprises a heavy chain variable region (VH) complementarity determining region (CDR) 1 comprising the amino acid sequence of SEQ ID NO:5, a VH CDR2 comprising the amino acid sequence of SEQ ID NO: 6, a VH CDR3 comprising the amino acid sequence of SEQ ID NO:7, a light chain variable region (VL) CDR1 comprising the amino acid sequence of SEQ ID NO:8, a VL CDR2 comprising the amino acid sequence of SEQ ID NO:9, and a VL CDR3 comprising the amino acid sequence of SEQ ID NO: 10; and

(ii) about 200 mg of an anti-PD-1 antibody or antigen-binding fragment thereof comprising a VH CDR1 comprising the amino acid sequence of SEQ ID NO:34, a VH CDR2 comprising the amino acid sequence of SEQ ID NO:35, a VH CDR3 comprising the amino acid sequence of SEQ ID NO:36, a VL CDR1 comprising the amino acid sequence of SEQ ID NO: 37, a VL CDR2 comprising the amino acid sequence of SEQ ID NO:38, and a VL CDR3 comprising the amino acid sequence of SEQ ID NO:39.

2 . The method of claim 1 , wherein about 20 mg/kg of the anti-B7-H4 antibody or antigen-binding fragment thereof is administered to the subject.

3 . The method of claim 1 , wherein about 10 mg/kg of the anti-B7-H4 antibody or antigen-binding fragment thereof is administered to the subject.

4 . The method of claim 1 , wherein about 3 mg/kg of the anti-B7-H4 antibody or antigen-binding fragment thereof is administered to the subject.

5 . The method of claim 1 , wherein about 1 mg/kg of the anti-B7-H4 antibody or antigen-binding fragment thereof is administered to the subject.

6 . The method of claim 1 , wherein about 0.3 mg/kg of the anti-B7-H4 antibody or antigen-binding fragment thereof is administered to the subject.

7 . The method of claim 1 , wherein about 0.1 mg/kg of the anti-B7-H4 antibody or antigen-binding fragment thereof is administered to the subject.

8 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof and the anti-PD-1 antibody or antigen-binding fragment thereof are administered concurrently.

9 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof and the anti-PD-1 antibody or antigen-binding fragment thereof are administered sequentially.

10 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof is administered about once every three weeks.

11 . The method of claim 1 , wherein the anti-PD-1 antibody or antigen-binding fragment thereof is administered about once every three weeks.

12 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof and the anti-PD-1 antibody or antigen-binding fragment thereof are each administered about once every three weeks.

13 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof comprises a VH comprising the amino acid sequence set forth in SEQ ID NO:11 and/or a VL comprising the amino acid sequence set forth in SEQ ID NO: 12.

14 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof comprises a heavy chain constant region and/or a light chain constant region.

15 . The method of claim 14 , wherein the heavy chain constant region is a human immunoglobulin IgG1 heavy chain constant region and/or wherein the light chain constant region is a human immunoglobulin IgGκ light chain constant region.

16 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof comprises a heavy chain constant region comprising the amino acid sequence set forth in SEQ ID NO:25 and/or a light chain constant region comprising the amino acid sequence set forth in SEQ ID NO:23.

17 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof comprises a heavy chain comprising the amino acid sequence set forth in SEQ ID NO:21 and/or a light chain comprising the amino acid sequence set forth in SEQ ID NO:22.

18 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof is a human antibody or antigen-binding fragment thereof.

19 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof is a full length antibody.

20 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof is an antigen-binding fragment.

21 . The method of claim 20 , wherein the antigen-binding fragment comprises a Fab, Fab′, F(ab′) 2 , single chain Fv (scFv), disulfide linked Fv, V-NAR domain, IgNar, intrabody, IgGΔCH2, minibody, F(ab′) 3 , tetrabody, triabody, diabody, single-domain antibody, DVD-Ig, Fcab, mAb 2 , (scFv) 2 , or scFv-Fc.

22 . The method of claim 1 , wherein the anti-PD-1 antibody or antigen-binding fragment thereof comprises a VH comprising the amino acid sequence of SEQ ID NO:32 and a VL comprising the amino acid sequence SEQ ID NO:33.

23 . The method of claim 1 , wherein the anti-PD-1 antibody or antigen-binding fragment thereof is pembrolizumab.

24 . The method of claim 1 , the method comprising administering to the subject

(i) 3, 10 or 20 mg/kg of an anti-B7-H4 antibody or antigen-binding fragment thereof that specifically binds to human B7-H4 and comprises a VH comprising the amino acid sequence set forth in SEQ ID NO:11 and a VL comprising the amino acid sequence set forth in SEQ ID NO: 12, wherein the anti-B7-H4 antibody or antigen-binding fragment thereof is not detectably fucosylated; and

(ii) 200 mg of pembrolizumab;

wherein (i) and (ii) are administered intravenously as separate formulations on the same day.

25 . The method of claim 24 , wherein the anti-B7-H4 antibody comprises a heavy chain comprising the amino acid sequence set forth in SEQ ID NO:21 and a light chain comprising the amino acid sequence set forth in SEQ ID NO:22.

26 . The method of claim 1 , the method comprising administering to the subject

(i) about 20 mg/kg of an anti-B7-H4 antibody that specifically binds to human B7-H4 and comprises a VH comprising the amino acid sequence of SEQ ID NO: 11 and a VL comprising the amino acid sequence of SEQ ID NO: 12; and

(ii) about 200 mg of an anti-PD-1 antibody comprising a VH comprising the amino acid sequence of SEQ ID NO:32 and a VL comprising the amino acid sequence of SEQ ID NO:33, wherein the anti-B7-H4 antibody and the anti-PD-1 antibody are administered intravenously about once every three weeks.

27 . The method of claim 26 , wherein the anti-B7-H4 antibody comprises a heavy chain comprising the amino acid sequence set forth in SEQ ID NO: 21 and a light chain comprising the amino acid sequence set forth in SEQ ID NO:22.

28 . The method of claim 26 , wherein the anti-PD-1 antibody comprises a heavy chain comprising the amino acid sequence set forth in SEQ ID NO: 30 and a light chain comprising the amino acid sequence set forth in SEQ ID NO:31.

29 . The method of claim 27 , wherein the anti-PD-1 antibody comprises a heavy chain comprising the amino acid sequence set forth in SEQ ID NO: 30 and a light chain comprising the amino acid sequence set forth in SEQ ID NO:31.

30 . The method of claim 1 , wherein the solid tumor is selected from the group consisting of breast cancer, ductal carcinoma, endometrial carcinoma, ovarian cancer, urothelial cancer, non-small cell lung cancer, pancreatic cancer, thyroid cancer, kidney cancer and bladder cancer.

31 . The method of claim 30 , wherein the solid tumor is triple negative breast cancer.

32 . The method of claim 30 , wherein the solid tumor is a hormone-receptor (HR)-positive breast cancer.

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

34 . The method of claim 1 , wherein the patient has not received prior therapy with a PD-1/PD-L1 antagonist.

35 . The method of claim 1 , wherein the method further comprises monitoring the number of immune cells in the tumor and/or monitoring cytokine levels in the subject.

36 . The method of claim 1 , wherein the anti-B7-H4 antibody or antigen-binding fragment thereof is present in a pharmaceutical composition comprising a pharmaceutically acceptable excipient, wherein at least 95% of the anti-B7-H4 antibodies or antigen-binding fragments thereof in the composition are afucosylated.

37 . The method of claim 36 , wherein fucosylation of the anti-B7-H4 antibody or antigen-binding fragment thereof is undetectable in the composition.

38 . The method of claim 36 , the method comprising administering to the subject

(a) a pharmaceutical composition comprising (i) anti-B7-H4 antibodies that specifically bind to human B7-H4 and comprise a VH comprising the amino acid sequence of SEQ ID NO: 11 and a VL comprising the amino acid sequence of SEQ ID NO: 12 and (ii) a pharmaceutically acceptable excipient, wherein at least 95% of the anti-B7-H4 antibodies thereof in the composition are afucosylated, and wherein about 20 mg/kg of the antibodies are administered; and

(b) a pharmaceutical composition comprising an anti-PD-1 antibody or antigen-binding fragment thereof comprising a VH comprising the amino acid sequence of SEQ ID NO:32 and a VL comprising the amino acid sequence of SEQ ID NO:33 and a pharmaceutically acceptable excipient, wherein about 200 mg of the antibody or antigen-binding fragment thereof is administered,

wherein (a) and (b) are administered intravenously about once every three weeks.

39 . The method of claim 38 , wherein the anti-B7-H4 antibodies comprise a heavy chain comprising the amino acid sequence set forth in SEQ ID NO: 21 and a light chain comprising the amino acid sequence set forth in SEQ ID NO:22.

40 . The method of claim 38 , wherein the anti-PD-1 antibody comprises a heavy chain comprising the amino acid sequence set forth in SEQ ID NO: 30 and a light chain comprising the amino acid sequence set forth in SEQ ID NO:31.

41 . The method of claim 39 , wherein the anti-PD-1 antibody comprises a heavy chain comprising the amino acid sequence set forth in SEQ ID NO: 30 and a light chain comprising the amino acid sequence set forth in SEQ ID NO:31.