Method for treating cancer
The present disclosure relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase EZH2, and methods of cancer therapy using the EZH2 inhibitor(s).
1. A method for treating an INI1-negative tumor comprising administering a therapeutically effective amount of an EZH2 inhibitor to a subject in need thereof, wherein the INI1-negative tumor is selected from epithelioid malignant peripheral nerve sheath tumor, and myoepithelial carcinoma.
2. The method of claim 1 , wherein the INI1-negative tumor is epithelioid malignant peripheral nerve sheath tumor.
3. The method of claim 1 , wherein the INI1-negative tumor is myoepithelial carcinoma.
4. The method of claim 1 , wherein the EZH2 inhibitor is administered orally.
5. The method of claim 1 , wherein the subject is a human being.
6. The method of claim 1 , wherein the subject is younger than 18 years.
7. The method of claim 1 , wherein the EZH2 inhibitor is compound (A), having the following formula:
or a pharmaceutically acceptable salt thereof.
8. The method of claim 1 , wherein the EZH2 inhibitor is administered to the subject at a dose of about 100 mg to about 3200 mg daily.
9. The method of claim 1 , wherein the EZH2 inhibitor is administered to the subject at a dose of about 100 mg BID to about 1600 mg BID.
10. The method of claim 1 , wherein the EZH2 inhibitor is administered to the subject at a dose of about 100 mg BID, 200 mg BID, 400 mg BID, 800 mg BID, or about 1600 mg BID.
11. The method of claim 8 , wherein the EZH2 inhibitor is administered to the subject at a dose of 800 mg BID.
12. The method of claim 1 , wherein the EZH2 inhibitor is selected from the group consisting of
and pharmaceutically acceptable salts thereof.
13. The method of claim 12 , wherein the EZH2 inhibitor is:
or a pharmaceutically acceptable salt thereof.
14. A method for treating an INI1-negative tumor comprising administering a therapeutically effective amount of an EZH2 inhibitor to a subject in need thereof, wherein the INI1-negative tumor is selected from epithelioid malignant peripheral nerve sheath tumor, and myoepithelial carcinoma;
wherein the EZH2 inhibitor is selected from the group consisting of
and pharmaceutically acceptable salts thereof.
15. The method of claim 7 , wherein the EZH2 inhibitor is administered orally.
16. The method of claim 7 , wherein the subject is a human being.
17. The method of claim 7 , wherein the EZH2 inhibitor is administered to the subject at a dose of about 100 mg to about 3200 mg daily.
18. The method of claim 7 , wherein the EZH2 inhibitor is administered to the subject at a dose of about 100 mg BID to about 1600 mg BID.
19. The method of claim 14 , wherein the INI1-negative tumor is epithelioid malignant peripheral nerve sheath tumor.
20. The method of claim 14 , wherein the INI1-negative tumor is myoepithelial carcinoma.
21. The method of claim 14 , wherein the EZH2 inhibitor is administered orally.
22. The method of claim 14 , wherein the subject is a human being.