2014 AACR: SGI-110 SQ provides superior disposition profile for active metabolite decitabine

Summary

  • SGI‐110 is a 2nd generation hypomethylating agent. It is a dinucleotide of decitabine (DAC) and deoxyguanosine; is resistant to deamination by cytidine deaminase and is in clinical evelopment for hematologic malignancies and solid tumors
  • Clinical PK data for SGI‐110 show lasting exposures (8 hr+) in parent form
  • Due to the slow release from SGI‐110 after SQ injection, exposure window for the active metabolite decitabine is prolonged compared to IV DAC, which is the proposed basis for the improved clinical activity emerging from early clinical trials with SGI‐110
  • The objective of this study was to characterize the mass balance and tissue distribution of [14C]SGI‐110 compared to IV [14C]DAC and evaluate the potential uptake into cells of SGI‐110 in parent form prior to conversion to active metabolite DAC

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2014 AACR: SGI-110 SQ provides superior disposition profile for active metabolite decitabine