Method for treating cancer

• US 10,493,076 B2
• Filed: 08/24/2016
• Issued: 12/03/2019
• Est. Priority Date: 08/24/2015
• Status: Active Grant

• Current Assignee: Epizyme, Inc. (Ipsen Sa)
• Original Assignee: Epizyme, Inc. (Ipsen Sa)
• Inventors: Keilhack, Heike, Knutson, Sarah K.
• Primary Examiner(s): Davis, Brian J
• Application Number:
  US15/754,684
• Publication Number:
  US 20180235975A1
• Time in Patent Office: 1,196 Days
• Field of Search: None
• CPC Class Codes: A61K 31/4412 having oxo groups directly attached to the heterocyclic ring
• CPC Class Codes: A61K 31/4545 containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• CPC Class Codes: A61K 31/5377 not condensed and containing further heterocyclic rings, e.g. timolol
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

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).

Claims

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:

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

13. The method of claim 12, wherein the EZH2 inhibitor is:

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.

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

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.