Inhibitors of human ezh2, and methods of use thereof
US-2017065600-A1 · Mar 9, 2017 · US
EZH2 inhibitors for treating lymphoma
US10166238B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10166238-B2 |
| Application number | US-201515319535-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 17, 2015 |
| Priority date | Jun 17, 2014 |
| Publication date | Jan 1, 2019 |
| Grant date | Jan 1, 2019 |
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- Title
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Abstract
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The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and their use for the treatment of cancer.
First claim
Opening claim text (preview).
What is claimed is: 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.
Assignees
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Classifications
Antineoplastic agents · CPC title
specific for leukemia · CPC title
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
- A61K31/4412Primary
having oxo groups directly attached to the heterocyclic ring · CPC title
linked by a chain containing hetero atoms as chain links · CPC title
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Frequently asked questions
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- What does patent US10166238B2 cover?
- The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and their use for the treatment of cancer.
- Who is the assignee on this patent?
- Epizyme Inc, Eisai R&D Man Co Ltd
- What technology area does this patent fall under?
- Primary CPC classification A61K31/4412. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Jan 01 2019 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).