# US 10,946,024 B2 · Method for treating cancer

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- Number: US 10,946,024 B2
- Document ID: US10946024B2
- Status: Granted
- Kind: B2
- Application number: 16/444,579
- Filed: 2019-06-18
- Published: 2020-01-09
- Granted: 2021-03-16
- Earliest claimed: 2014-10-16
- Assignees: Epizyme, Inc.
- Applicants: Epizyme, Inc.
- Inventors: Heike Keilhack
- Web page: https://patentgrep.com/patent/US10946024B2

## CPC

- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61K 31/45: having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
- A61K 31/453: containing a six-membered ring with oxygen as a ring hetero atom
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61K 31/5375: 1,4-Oxazines, e.g. morpholine
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (MHC), or cancer, characterized by aberrant, misregulated, or increased Enhancer of Zeste Homolog 2 (EZH2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an EZH2 inhibitor.

## Claims

### Claim 1

A method for screening the effectiveness of a treatment of immune evasion, cancer-cell induced immune dysfunction, reduced immune response, or decreased expression of a major histocompatibility complex (MHC) in a human subject in need thereof comprising:
(1) obtaining a first and a second biological sample from the subject;
(2) contacting the second biological sample with an EZH2 inhibitor;
(3) assaying the first and the second biological sample for expression of a MHC; and
(4) comparing expression of the MHC in the first biological sample to expression of the MHC in the second biological sample;
wherein the treatment comprises an EZH2 inhibitor; and
wherein if the second biological sample has increased expression of the MHC when compared to expression in the first biological sample, then the treatment comprising the EZH2 inhibitor is more likely to be effective in the subject.

### Claim 2 (depends on 1)

The method of claim 1, wherein the subject has aberrant, misregulated, or increased EZH2 activity.

### Claim 3 (depends on 1)

The method of claim 1, wherein the subject has a chromosomal translocation t(x;18)(p11.2;q11.2).

### Claim 4 (depends on 3)

The method of claim 3, wherein the translocation causes a SS18-SSX fusion gene.

### Claim 5 (depends on 1)

The method of claim 1, wherein the subject has reduced function or expression of INI1.

### Claim 6 (depends on 5)

The method of claim 5, wherein the subject has reduced function and expression of INI1.

### Claim 7 (depends on 1)

The method of claim 1, wherein the EZH2 inhibitor is Compound A, having the following formula:
and pharmaceutically acceptable salts thereof.

### Claim 8 (depends on 1)

The method of claim 1, wherein the EZH2 inhibitor is selected from the group consisting of
and pharmaceutically acceptable salts thereof.

### Claim 9 (depends on 1)

The method of claim 1, wherein the method further comprises administering an additional chemotherapeutic compound.

### Claim 10 (depends on 9)

The method of claim 9, wherein the additional chemotherapeutic compound is selected from the group consisting of a PD-1 inhibitor, a PD-L1 inhibitor, and a CTLA-4 inhibitor.

### Claim 11 (depends on 1)

The method of claim 1, wherein the MEW is human leukocyte antigen (HLA), wherein the HLA is selected from the group consisting of HLA-A, HLA-B, HLA-C, HLA-DM alpha, HLA-DM beta, HLA-DO alpha, HLA-DO beta 1, HLA-DP alpha 1, HLA-DP beta 1, HLA-DR alpha, HLA-DR beta 1, HLA-DR beta 3, HLA-DR beta 4, HLA-E, HLA-F, HLA-G, HLA-K, and HLA-L.