Microsomes/UGT Enzymes + UDPGA | Ezetimibe Concentration (μM) | % Conversion (% Total Profiled Radioactivity) | ||
---|---|---|---|---|
Phenolic glucuronide (SCH 60663) | Benzylic glucuronide (SCH 488128) | |||
Liver | 5 | 100 | ND | |
25 | 47.8 | 2.32 | ||
Jejunum donor HJ-004 | 25 | 42.5 | 41.3 | |
Jejunum donor HJ-025 | 100 | 41.8 | 41.4 | |
UGT1A1 | 100 | 79.5 | ND | |
UGT1A3 | 100 | 73.4 | ND | |
UGT1A4 | 100 | ND | 0.78 | |
UGT1A6 | 100 | ND | ND | |
UGT1A7 | 100 | ND | ND | |
UGT1A9 | 100 | 0.21 | 0.48 | |
UGT1A10 | 100 | ND | ND | |
UGT2B7 | 100 | 0.51 | 5.96 | |
UGT2B15 | 100 | 6.09 | ND | |
Insect control | 100 | ND | ND |
ND, not detected.