Uptake clearances of [14C]S-8921G by human hepatocytes and contribution of OATP1B1, OATP1B3, and NTCP to the hepatic uptake of [14C]S-8921G Uptake clearances (CLhep) were calculated by subtracting CL (2–0.5 min) in the presence of excess unlabeled substrate from that in the presence of tracer substrate. Values in parentheses represent the ratio of the OATP1B1-, OATP1B3-, or NTCP-mediated uptake clearance relative to the sum of the estimated clearance mediated by OATP1B1, OATP1B3, and NTCP.
Hepatocytes | Predicted Clearance | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| OATP1B1 | OATP1B3 | NTCP | |||||||||
| μl/min/106 cells | % | μl/min/106 cells | % | μl/min/106 cells | % | ||||||
| Lot | |||||||||||
| ETR | 35.1 | 60.6 | 20.9 | 36.2 | 1.83 | 3.2 | |||||
| UYII | 38.8 | 62.4 | 22.0 | 35.5 | 1.33 | 2.1 | |||||
| PFQI | 47.8 | 64.6 | 24.4 | 33.0 | 1.78 | 2.4 | |||||