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Epigenetics refers to mechanisms that lead to activity or inactivity of selective genetic functions due to acquired genetic modification not accompanied by changes in the underlying gene sequence. The term also refers to the study of such mechanisms. Examples of acquired genetic modification in this field include changes in gene expression caused by DNA methylation and changes in genetic expression caused by the chemical modification of amino acids in histones (methylation, acetylation, phosphorylation, etc.). Dacogen® (decitabine), which is marketed by Eisai in the United States, is a DNA methylation inhibitor, and is approved in the United States as a therapeutic agent that contributes to the quality of life of patients living with myelodysplastic syndromes (MDS).

EZH2 is one of the proteins that make up the histone methyltransferases (HMTs) that alter gene expression. EZH2 is known to methylate lysine 27 of the protein H3 (H3K27), H3 being one of the five major histone groups (H1, H2A, H2B, H3 and H4) that together help to store DNA in eukaryotic cell nuclei. H3K27 methylation is also known to suppress gene transcription. Recently, several change-of-function genetic mutations, including Y461, have been reported in EZH2 in lymphomas.

Following advances in human biology, initiatives aimed at achievements in personalized medicine through early development of new drugs and companion diagnostics based on optimum therapeutic hypotheses are progressing steadily. Eisai is actively seeking out therapeutic hypotheses linked to personalized medicine while strengthening networks with scientists at the cutting edge of their respective fields, and is increasing its sensitivities in regard to future trends in scientific technology and both in-house and external inventions and discoveries. At its research subsidiary H3 Biomedicine Inc. in the Boston area of the United States, for example, Eisai is rising to meet challenges in targeting new therapeutic hypotheses by identifying strong potential therapeutic targets through genetics-based approaches to cancer and the creation of novel anticancer agents using first-in-class compounds. Furthermore, Eisai has concentrated all functions aimed at possible developments in this field, from biomarker discovery research to companion diagnostics development, into its Biomarker and Personalized Medicine Core Function Unit, and through collaborations with other drug creation units such as its Oncology Product Creation unit, is continuing endeavors toward further realizing personalized medicine.

Epizyme, Inc. is leading the creation of small molecule histone methyltransferase inhibitors (HMTi), a new class of personalized therapeutics for patients with genetically defined cancers. Genetic alterations in HMTs, a family of epigenetic enzymes, drive multiple human diseases. Its approach represents the future of healthcare by matching better medicines with the right patients.

Headquartered in Basel, Switzerland, Roche is a leader in research-focused healthcare with combined strengths in pharmaceuticals and diagnostics. Roche is the world’s largest biotech company with truly differentiated medicines in oncology, virology, inflammation, metabolism and CNS. Roche is also the world leader in in-vitro diagnostics, tissue-based cancer diagnostics and a pioneer in diabetes management. Roche's personalized healthcare strategy aims at providing medicines and diagnostic tools that enable tangible improvements in the health, quality of life and survival of patients. In 2011, Roche had over 80,000 employees worldwide and invested over 8 billion Swiss francs in R&D. The Group posted sales of 42.5 billion Swiss francs. Genentech, United States, is a wholly owned member of the Roche Group. Roche has a majority stake in Chugai Pharmaceutical, Japan. For more information:.

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