DMPK

Eric Solon Co-presents Poster at AACR (American Association for Cancer Research) Annual Meeting showing the Tissue Disposition Profile of a 2nd Generation Hypomethylating Agent - April, 2014

Hypomethylating agents inhibit DNA methylation and are under investigation for use in treating certain types of cancer such as myelodysplastic syndromes. SGI-110 from Astex Pharmaceuticals is a 2nd generation hypomethylating agent, a dinucleotide of 1st generation agent decitabine (DAC) and deoxyguanosine. SGI-110 is resistant to deamination by cytidinedeaminase and is in clinical development for the treatment of hematologic malignancies and solid tumors.

The objective of this study was to characterize the mass balance and tissue distribution of [14C]SGI-110 compared to IV [14C]DAC, and to evaluate the potential uptake into cells of SGI-110 in parent form prior to its conversion to the active metabolite DAC. The results? SGI 110 appears to deliver active metabolite decitabine to key tissues, including bone marrow, more efficiently than decitabine itself.

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