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January 10, 2011

GSK Pays Epizyme $20M Up Front as Part of Histone Methyltransferase Inhibitor Deal

  • Epizyme will receive $20 million up front from GlaxoSmithKline as part of a worldwide deal focused on the discovery, development, and marketing of small molecule inhibitors of histone methyltransferases (HMTs). The collaboration will exploit Epizyme’s HMT discovery platform and chemical library to identify and develop HMT therapeutics against a set of targets for cancer and other diseases.

    Under terms of the agreement Epizyme will carry out all research activities up to the selection of a development candidate for each target, after which GSK will take over all further development and commercialization activities. Epizyme could receive over $630 million in milestones if products against all targets in the collaboration reach the market, plus double-digit sales royalties.

    The deal comes just a few days after Epizyme announced the award of a $1 million grant from the Multiple Myeloma Research Foundation (MMRF), to help fund the development of personalized therapies for patients with genetically defined cancers, including multiple myeloma.

    Epizyme is exploiting its platform to develop selective small molecule inhibitors of specific enzymes within the 96-member HMT target class The firm claims it has used its HMT-focused RNAi library and proprietary small molecule inhibitors to define the roles of specific HMTs in different cancers, and the effects of inhibiting these enzymes in a disease setting. Having subsequently ranked the 96 human HMTs in terms of disease relevance and commercial opportunity, Epizyme has also identified a top-tier set of HMTs for drug discovery and development.

    Its resulting preclinical pipeline of HMT inhibitor is headed by DOT1L, for the treatment of MLL-rearranged leukemia, and EZH2, for the potential treatment of non-Hodgkin lymphoma and certain breast cancer subtypes. A third candidate, HMT3, is also in preclinical development against a hematological malignancy.

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