Tissue Distribution Study of MGCD0103 in Rat by UPLC-MS/MS

MGCD0103 (Mocetinostat), an isotope-selective of histone deacetylase (HDACi) inhibitor, has been clinically evaluated for the treatment of hematologic malignancies and advanced solid tumors, alone and in combination with standard-of-care agents. MGCD0103 in rat plasma and various tissues was determinated by a simple and selective ultra performance liquid chromatography method coupled with tandem mass spectrometry (UPLC-MS/MS). An electrospray ionization source was applied and operated in positive ion mode; multiple reactions monitoring (MRM) mode was used for quantification. The method has been successfully applied in tissue distribution study of MGCD0103. The results also show that MGCD0103 was rapidly absorbed and widely distributed in various tissues. The level of MGCD0103 in kidney was the highest, followed by liver, plasma and spleen.