Drug metabolism assessed as UGT1A1-mediated compound glucuronidation in pooled mixed-gender human liver microsomes at 50 uM preincubated at 37 degC for 3 mins before UDPGA addition by HPLC method
Activity of human UGT1A1 expressed in microsomes isolated from baculovirus infected insect cell assessed as enzyme-mediated (2S,3S,4S,5R,6R)-3,4,5-trihydroxy-6-(5-(4-((6-methoxy-1-methyl-1H-benzo[d]imidazol-2-yl)methoxy)benzyl)-2,4-dioxothiazolidin-3-yl)tetrahydro-2H-pyran-2-carboxylic acid formation at 20 uM after 4 hrs by radio-HPLC/LC-MS/MS analysis in presence of UDPGA
Drug metabolism in UDPGA-fortified human liver microsomes assessed as UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid) formation after 120 mins by radio-HPLC analysis
Drug metabolism in UDPGA-fortified human liver microsomes assessed as UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid) formation after 120 mins measured per mg of protein by radio-HPLC analysis
Drug metabolism in UDPGA-fortified human liver microsomes assessed as intrinsic clearance for UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid) formation after 120 mins measured per mg of protein by radio-HPLC analysis
Drug metabolism assessed as human recombinant UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid) formation after 120 mins by radio-HPLC analysis
Drug metabolism in human intestinal microsomes assessed as UGT1A1-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis
Ratio of UGT1A1-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A1-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM
Drug metabolism assessed as human recombinant UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid) formation after 120 mins measured per mg of protein by radio-HPLC analysis