EZH2 inhibitors for treating lymphoma
View Patent ↗The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and their use for the treatment of cancer.
1. A method for treating non-Hodgkin's lymphoma (NHL) comprising administering a therapeutically effective amount of an EZH2 inhibitor to a subject in need thereof, wherein the NHL is primary mediastinal large B-cell lymphoma (PMBCL), and wherein the EZH2 inhibitor is administered to the subject at a dose of about 100 mg to about 3200 mg daily.
2. The method of claim 1 , Wherein the EZH2 inhibitor is administered orally.
3. The method of claim 1 , wherein the subject is a human being.
4. The method of claim 3 , wherein the EZH2 inhibitor is EPZ-6438 having the following formula:
or a pharmaceutically acceptable salt thereof.
5. 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.
6. 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.
7. The method of claim 6 , wherein the EZH2 inhibitor is administered to the subject at a dose of 800 mg BID.
8. The method of claim 3 , wherein the EZH2 inhibitor is:
or a pharmaceutically acceptable salt thereof.
9. The method of claim 8 , wherein the EZH2 inhibitor is:
or a pharmaceutically acceptable salt thereof.
10. The method of claim 1 , wherein the PMBCL is relapsed or refractory to at least one prior therapy.
11. The method of claim 10 , wherein the PMBCL is multiply refractory.
12. The method of claim 1 , wherein the EZH2 inhibitor is administered orally, wherein the subject is a human, and wherein the EZH2 inhibitor is EPZ-6438 having the following formula:
or a pharmaceutically acceptable salt thereof.
13. The method of claim 12 , wherein the EZH2 inhibitor is administered to the subject at a dose of about 100 mg BID to about 1600 mg BID.
14. The method of claim 12 , 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.
15. The method of claim 12 , wherein the EZH2 inhibitor is administered to the subject at a dose of 800 mg BID.
16. The method of claim 1 , wherein the EZH2 inhibitor is administered orally, wherein the subject is a human, and wherein the EZH2 inhibitor is EPZ-6438 having the following formula:
or a pharmaceutically acceptable salt thereof.
17. The method of claim 16 , wherein the EZH2 inhibitor is administered to the subject at a dose of about 100 mg BID to about 1600 mg BID.
18. The method of claim 16 , 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.
19. The method of claim 16 , wherein the EZH2 inhibitor is administered to the subject at a dose of 800 mg BID.