IP Library › Granted Patent US 10,946,093
Granted Patent B2
US 10,946,093 · App. 15/399,118 · Granted Mar 16, 2021

Methods of treating cancer using PD-1 axis binding antagonists and MEK inhibitors

Inventor: Melissa Junttila (South San Francisco, CA)
Assignee: Genentech, Inc.
A61K39/3955A61K31/4523A61K39/39558C07K16/2803C07K16/2827A61K2039/505A61K2039/542C07K2317/52C07K2317/56C07K2317/72C07K2317/73C07K2317/76
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Quick Facts
Patent No.
US 10,946,093
App. No.
15/399,118
Granted
Mar 16, 2021
Kind
B2
Abstract

The present invention describes combination treatment comprising a PD-1 axis binding antagonist and a MEK inhibitor and methods for use thereof, including methods of treating conditions where enhanced immunogenicity is desired such as increasing tumor immunogenicity for the treatment of cancer.

Claims (27)

1. A method for treating or delaying progression of a melanoma that is resistant to a B-raf antagonist in an individual, the method comprising administering to the individual an effective amount of a PD-L1 binding antagonist and a MEK inhibitor, wherein:

the individual has been previously treated with the B-raf antagonist for melanoma and the melanoma is resistant to the B-raf antagonist,

the MEK inhibitor is GDC-0973 or a pharmaceutically acceptable salt or solvate thereof, and

the PD-L1 antagonist is an anti-PD-L1 antibody comprising a heavy chain comprising HVR-H1 sequence of SEQ ID NO: 15, HVR-H2 sequence of SEQ ID NO: 16, and HVR-H3 sequence of SEQ ID NO: 3; and a light chain comprising HVR-L1 sequence of SEQ ID NO: 17, HVR-L2 sequence of SEQ ID NO: 18, and HVR-L3 sequence of SEQ ID NO: 19.

2. The method of claim 1 , further comprising diagnosing the individual as having a melanoma that is resistant to the B-raf antagonist, wherein the diagnosing occurs prior to administering the effective amount of the PD-L1 binding antagonist and the MEK inhibitor.

3. The method of claim 1 , wherein the melanoma in the individual has progressed within 1 month, 6 months, 1 year, or 5 years after completing a B-raf antagonist-based therapy regimen.

4. The method of claim 1 , wherein the B-raf antagonist is a small molecule inhibitor.

5. The method of claim 4 , wherein the B-raf antagonist is dabrafenib, vemurafenib, GSK 2118436, RAF265, XL281, ARQ736, BAY73-4506, sorafenib, PLX4720, PLX-3603, GSK2118436, GDC-0879, or N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide.

6. The method of claim 4 , wherein the B-raf antagonist is a selective B-raf antagonist of B-raf V600.

7. The method of claim 6 , wherein the selective B-raf antagonist of B-raf V600 is a selective antagonist of B-raf V600E.

8. The method of claim 6 , wherein the selective B-raf antagonist of B-raf V600 is a selective antagonist of B-raf V600E, B-raf V600K, and/or V600D.

9. The method of claim 6 , wherein the selective B-raf antagonist of B-raf V600 is a selective antagonist of B-raf V600R.

10. The method of claim 1 , wherein the melanoma contains a BRAF V600E mutation, a BRAF wildtype, a KRAS wildtype, or an activating KRAS mutation.

11. The method of claim 1 , wherein the treatment results in a sustained response in the individual after cessation of the treatment.

12. The method of claim 1 , wherein the melanoma is metastatic.

13. The method of claim 1 , wherein the PD-L1 binding antagonist inhibits the binding of PD-L1 to PD-1, PD-L1 to B7-1, or PD-L1 to both PD-1 and B7-1.

14. The method of claim 1 , wherein the anti-PD-L1 antibody is a monoclonal antibody.

15. The method of claim 1 , wherein the anti-PD-L1 antibody is an antibody fragment selected from the group consisting of Fab, Fab′-SH, Fv, scFv, and F(ab′) 2 fragments.

16. The method of claim 1 , wherein the anti-PD-L1 antibody is a humanized antibody.

17. The method of claim 1 , wherein the PD-L1 binding antagonist is YW243.55.S70 or atezolizumab.

18. The method of claim 1 , wherein the anti-PD-L1 antibody comprises a heavy chain variable region comprising the amino acid sequence of SEQ ID NO: 24 and a light chain variable region comprising the amino acid sequence of SEQ ID NO: 21.

19. The method of claim 1 , wherein the MEK inhibitor is administered continuously.

20. The method of claim 1 , wherein the MEK inhibitor is administered intermittently.

21. The method of claim 1 , wherein the MEK inhibitor is administered before the PD-L1 binding antagonist.

22. The method of claim 1 , wherein the MEK inhibitor is administered simultaneously with the PD-L1 binding antagonist.

23. The method of claim 1 , wherein the MEK inhibitor is administered after the PD-L1binding antagonist.

24. The method of claim 1 , wherein the PD-L1 binding antagonist and/or the MEK inhibitor is administered intravenously, intramuscularly, subcutaneously, topically, orally, transdermally, intraperitoneally, intraorbitally, by implantation, by inhalation, intrathecally, intraventricularly, or intranasally.

Continuity (3)
Continuation PCTCN2015040582 · Jul 15, 2015
Provisional Application 62024988 · Jul 15, 2014
Related Publication 20170112925A1 · Apr 27, 2017
Cited By (2)
US 12,685,772 US 12,723,074