IP Library Granted Patent US 12678498
Granted Patent B2
US 12678498 · App. 17/655,519 · Granted Jul 14, 2026

FGFR/PD-1 combination therapy for the treatment of cancer

Inventors: Jayaprakash Karkera (Germantown, MD); Suso Jesus Platero (Washington Crossing, PA); Raluca Verona (Swarthmore, PA); Matthew V. Lorenzi (Philadelphia, PA)
Assignee: ASTEX THERAPEUTICS LTD
A61K39/3955A61K31/498A61K45/06C07K16/2818C12Q1/6886G01N33/57492C12Q2600/158G01N2333/70596G01N2800/52
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Quick Facts
Patent No.
US 12678498
App. No.
17/655,519
Granted
Jul 14, 2026
Kind
B2
Abstract

Provided herein are combination therapies for the treatment of cancer. In particular, the disclosed methods are directed to treatment of cancer in a patient comprising administering an antibody that blocks the interaction between PD-1 and PD-L1 and an FGFR inhibitor, wherein the antibody that blocks the interaction between PD-1 and PD-L1 and the FGFR inhibitor are administered if one or more FGFR variants are present in a biological sample from the patient.

Claims (46)

1 . A method of treating cancer in a patient comprising:

administering to the patient a pharmaceutically effective amount of an antibody that blocks the interaction between PD-1 and PD-L1;

monitoring the efficacy of the antibody; and

if the antibody is not efficacious,

evaluating a biological sample from the patient for a presence of one or more FGFR variants, wherein the one or more FGFR variants comprise an FGFR mutation, and wherein the FGFR mutation is FGFR3 G370C; and

administering to the patient a pharmaceutically effective amount of an FGFR inhibitor if the one or more FGFR variants are present in the sample, wherein the FGFR inhibitor is the compound of formula (I):

or a pharmaceutically acceptable salt thereof.

2 . The method of claim 1 , wherein the evaluating step further comprises measuring an expression level of PD-L1 in a biological sample and wherein the second administering step comprises administering the FGFR inhibitor if:

the biological sample has a PD-L1 expression corresponding to an H-score of about 0 to about 99; or

the biological sample has a PD-L1 expression level that is lower than a reference PD-L1 expression level.

3 . The method of claim 1 , wherein the biological sample is blood, lymph fluid, bone marrow, a solid tumor sample, or any combination thereof.

4 . The method of claim 1 , wherein the cancer is lung cancer, bladder cancer, gastric cancer, breast cancer, ovarian cancer, head and neck cancer, esophageal cancer, glioblastoma, or any combination thereof.

5 . The method of claim 4 , wherein the cancer is bladder cancer.

6 . The method of claim 1 , wherein the one or more FGFR variants further comprise an FGFR fusion gene.

7 . The method of claim 1 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 R248C.

8 . The method of claim 1 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 S249C.

9 . The method of claim 1 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 Y373C.

10 . The method of claim 1 , wherein the antibody that blocks an interaction between PD-1 and PD-L1 is an anti-PD-1 antibody, an anti-PD-L1 antibody, or a combination thereof.

11 . The method of claim 2 , wherein the cancer is lung cancer, bladder cancer, gastric cancer, breast cancer, ovarian cancer, head and neck cancer, esophageal cancer, glioblastoma, or any combination thereof.

12 . The method of claim 11 , wherein the cancer is bladder cancer.

13 . The method of claim 2 , wherein the one or more FGFR variants further comprise an FGFR fusion gene.

14 . The method of claim 2 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 R248C.

15 . The method of claim 2 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 S249C.

16 . The method of claim 2 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 Y373C.

17 . The method of claim 2 , wherein the antibody that blocks an interaction between PD-1 and PD-L1 is an anti-PD-1 antibody, an anti-PD-L1 antibody, or a combination thereof.

18 . The method of claim 3 , wherein the cancer is lung cancer, bladder cancer, gastric cancer, breast cancer, ovarian cancer, head and neck cancer, esophageal cancer, glioblastoma, or any combination thereof.

19 . The method of claim 18 , wherein the cancer is bladder cancer.

20 . The method of claim 3 , wherein the one or more FGFR variants further comprise an FGFR fusion gene.

21 . The method of claim 3 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 R248C.

22 . The method of claim 3 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 S249C.

23 . The method of claim 3 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 Y373C.

24 . The method of claim 3 , wherein the antibody that blocks an interaction between PD-1 and PD-L1 is an anti-PD-1 antibody, an anti-PD-L1 antibody, or a combination thereof.

25 . The method of claim 1 , wherein the biological sample:

has a PD-L1 expression corresponding to an H-score of less than 20; or

has a PD-L1 expression level that is lower than a reference PD-L1 expression level.

26 . The method of claim 25 , where the biological sample has a PD-L1 expression corresponding to an H-score of less than 20.

27 . The method of claim 1 , wherein the FGFR inhibitor is the compound of formula (I):

28 . The method of claim 27 , wherein the cancer is lung cancer, bladder cancer, gastric cancer, breast cancer, ovarian cancer, head and neck cancer, esophageal cancer, glioblastoma, or any combination thereof.

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

30 . The method of claim 29 , wherein the one or more FGFR variants further comprise an FGFR fusion gene.

31 . The method of claim 29 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 R248C.

32 . The method of claim 29 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 S249C.

33 . The method of claim 29 , wherein the one or more FGFR variants comprise at least one additional FGFR mutation, which is FGFR3 Y373C.

34 . The method of claim 29 , wherein the antibody that blocks an interaction between PD-1 and PD-L1 is an anti-PD-1 antibody, an anti-PD-L1 antibody, or a combination thereof.

35 . The method of claim 29 , wherein the biological sample is a solid tumor sample.

36 . The method of claim 3 , wherein the biological sample is a solid tumor sample.