The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
May. 10, 2016

Filed:

Nov. 13, 2014
Applicant:

Epizyme, Inc., Cambridge, MA (US);

Inventors:

Robert A. Copeland, Lexington, MA (US);

Victoria M. Richon, Wellesley, MA (US);

Margaret D. Scott, Beverly, MA (US);

Christopher J. Sneeringer, San Francisco, CA (US);

Kevin W. Kuntz, Woburn, MA (US);

Sarah K. Knutson, Cambridge, MA (US);

Roy M. Pollock, Medford, MA (US);

Assignee:

Epizyme, Inc., Cambridge, MA (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61P 35/00 (2006.01); C12Q 1/68 (2006.01); A61K 31/7076 (2006.01); C07D 473/34 (2006.01); C12Q 1/48 (2006.01); G01N 33/50 (2006.01); G01N 33/574 (2006.01); C07D 493/04 (2006.01); A61P 35/02 (2006.01);
U.S. Cl.
CPC ...
A61K 31/7076 (2013.01); C07D 473/34 (2013.01); C07D 493/04 (2013.01); C12Q 1/48 (2013.01); C12Q 1/6876 (2013.01); G01N 33/5011 (2013.01); G01N 33/57426 (2013.01); G01N 2333/91011 (2013.01);
Abstract

The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.


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