METHOD OF TREATING CANCER
The present invention relates to methods of treating cancer by administering an EZH2 inhibitor or a pharmaceutical composition thereof to the subject in need thereof.
1 - 8 . (canceled)
9 . A method for treating or alleviating a symptom of a cancer comprising administering to a subject in need thereof a therapeutically effective amount of an EZH2 inhibitor, wherein the cancer is associated with a chromosomal translocation t(x;18)(p11.2;q11.2) or a SS18-SSX fusion gene.
10 . The method of claim 9 , wherein the inhibitor is Compound A, having the following formula:
or a pharmaceutically acceptable salt thereof.
11 . The method of claim 9 , wherein the inhibitor is selected from the group consisting of
and pharmaceutically acceptable salts thereof.
12 . The method of claim 9 , further comprising a step of detecting the presence of a chromosomal translocation t(x;18)(p11.2;q11.2) or a SS18-SSX fusion gene in a sample from the subject before the administering step.
13 . A method for treating or alleviating a symptom of a cancer associated with (i) aberrant, misregulated, or increased EZH2 activity, or (ii) reduced or absent function of INI1, comprising administering to a subject in need thereof a therapeutically effective amount of an EZH2 inhibitor.
14 - 15 . (canceled)
16 . The method of claim 13 , wherein the inhibitor is Compound A, having the following formula:
or a pharmaceutically acceptable salt thereof.
17 . The method of claim 13 , wherein the inhibitor is selected from the group consisting of
and pharmaceutically acceptable salts thereof.
18 . The method of claim 13 , wherein the cancer is selected from the group consisting of synovial sarcoma, epithelioid sarcoma, extraskeletal myxoid chondrosarcoma, and atypical chordoma.
19 . The method of claim 18 , wherein the cancer is synovial sarcoma.
20 . The method of claim 19 , wherein the synovial sarcoma is characterized by aberrant EZH2 activity.
21 . The method of claim 19 , wherein the synovial sarcoma is characterized by misregulated EZH2 activity.
22 . The method of claim 19 , wherein the synovial sarcoma is characterized by increased EZH2 activity.
23 . The method of claim 18 , wherein the cancer is extraskeletal myxoid chondrosarcoma.
24 . The method of claim 18 , wherein the cancer is atypical chordoma.
25 . The method of claim 24 , wherein the atypical chordoma is characterized by aberrant, misregulated or increased EZH2 activity.
26 . A method of treating a cancer in a subject, the method comprising:
(1) detecting the presence of a chromosomal translocation t(x;18)(p11.2;q11.2) or a SS18-SSX fusion gene in a sample in a biological sample obtained from the subject, thereby identifying the cancer as sensitive to treatment with an EZH2 inhibitor; and
(2) administering to the subject a therapeutically effective amount of an EZH2 inhibitor.
27 . The method of claim 26 , wherein the inhibitor is Compound A, having the following formula:
or a pharmaceutically acceptable salt thereof.
28 . The method of claim 26 , wherein the inhibitor is selected from the group consisting of
and pharmaceutically acceptable salts thereof.
29 . The method of claim 26 , wherein the cancer is selected from the group consisting of synovial sarcoma, epithelioid sarcoma, extraskeletal myxoid chondrosarcoma, and atypical chordoma.
30 . The method of claim 29 , wherein the cancer is synovial sarcoma.