Patent ID: 9175331
Filing Date: 2015-11-03
Classification: A61K,A61P,C07D,C12Q,G01N,Y10T

Abstract:
1. A method for treating cancer or myelodysplastic syndromes (MDS) in a subject having a Enhancer of Zeste Homolog 2 (EZH2) mutation in the substrate pocket domain of SEQ ID NO: 6, wherein SEQ ID NO: 6 comprises a mutation at amino acid position Y641 of EZH2 of SEQ ID NO: 1, wherein the mutation at amino acid position Y641 is selected from the group consisting of a substitution of phenylalanine (F) for the wild type residue tyrosine (Y) at amino acid position 641 of SEQ ID NO: 1 (Y641 F); a substitution of histidine (H) for the wild type residue tyrosine (Y) at amino acid position 641 of SEQ ID NO: 1 (Y641 H); a substitution of asparagine (N) for the wild type residue tyrosine (Y) at amino acid position 641 of SEQ ID NO: 1 (Y641 N); and a substitution of serine (S) for the wild type residue tyrosine (Y) at amino acid position 641 of SEQ ID NO: 1 (Y641 S); comprising administering to said subject a therapeutically effective amount of an EZH2 inhibitor, wherein the EZH2 inhibitor is or a pharmaceutically acceptable salt thereof.