Product Name: LY-2334737 Request LY-2334737
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LY2334737 is an oral gemcitabine prodrug in which gemcitabine is linked to valproic acid via an amide bond, enabling it to bypass hydrolysis in enterocytes and portal circulation, thereby avoiding the extensive first pass metabolism that occurs with unmodified gemcitabine. Circulating levels of LY2334737 are detectable several hours after oral administration. In addition, a gradual release of gemcitabine following cleavage of the amide bond may ensure that more cancer cells are exposed to effective cytotoxic levels of gemcitabine as they enter G1/S phase of the cell cycle, to enhance efficacy. The lower peak plasma concentrations of gemcitabine that are achieved with LY2334737 may also result in lower toxicity when compared to bolus intravenous gemcitabine, thus resulting in a high therapeutic index. Phase I trials of this agent either as monotherapy or in combination with other agents are currently underway. Exploration of the role of this compound in the therapy of mature T-cell and NKcell lymphomas is planned. (Source: Shonukan A.H. Dantzig S. Kloeker-Rhoades I. Garcia-Ribas Development of LY2334737, an oral gemcitabine prodrug for continuous administration. Perspectives for the therapy of mature T-cell and NK-cell lymphomas Hematology Meeting Reports 2009;3(1):69 ).
Storage Conditions: 2ºC to 8 ºC, or -20ºC for 3 years.