Kinetic parameters describing the uptake of RSV into cynomolgus monkey and human primary hepatocytes and OATP-expressing HEK-293 cells
| Hepatocytesa | ||||||
|---|---|---|---|---|---|---|
| Cynomolgus Monkey | Human | |||||
| Km (µM) | 6.7 ± 0.8 | 10.3 ± 1.9 | ||||
| Vmax (pmol/min/106cells) | 172.3 ± 9.5 | 114.3 ± 11.6 | ||||
| Vmax/Km (µl/min/106cells) | 25.7 | 11.0 | ||||
| Pdiff (µl/min/106cells) | 0.7 ± 0.1 | 0.5 ± 0.1 | ||||
| [(Vmax/Km)/(Vmax/Km + Pdiff)]•100%b | 97 | 96 | ||||
| HEK-293 Cellsa,c | ||||||
| cOATP1B1 | hOATP1B1 | cOATP1B3 | hOATP1B3 | cOATP2B1 | hOATP2B1 | |
| Km (µM) | 14.4 ± 3.0 | 15.3 ± 3.0 | 14.5 ± 2.0 | 13.5 ± 2.0 | 9.6 ± 0.8 | 10.6 ± 1.0 |
HEK-293, human embryonic kidney 293 cells; Km, Michaelis-Menten constant that corresponds to the substrate concentration at which the uptake rate is half of Vmax; OATP, organic anion–transporting peptide; Pdiff, nonsaturable clearance via passive diffusion; RSV, rosuvastatin; Vmax, maximum transport rate.
↵a Data represent mean ± S.D. of the parameter estimate after non-linear fitting of the data (see Materials and Methods).
↵b Data indicate that >95% of total uptake is mediated by active transport.
↵c Vmax values of RSV uptake into OATP-expressing HEK-293 cells are not reported in the absence of specific OATP protein expression data.