TABLE 3

Pemetrexed influx kinetics as a function of pH

Pemetrexed Km and Vmax values are based upon analysis of initial uptake rates in PCFT-transfected HepG2 cells. Data are the mean ± S.E.M. from three independent experiments. The Km values for MTX and folic acid were reported previously (Qiu et al., 2006) and are listed in the table for the purpose of comparison.

pH Pemetrexed INFLUX Influx, Km
Km Vmax MTX Folic Acid
μM pmol/mg protein/2 min μM
5.5 0.8 ± 0.1 227 ± 6 3.4 1.3
6.0 3.4 1.5
6.5 2.1 ± 0.2 174 ± 6 7.3 2.7
7.0 4.6 ± 0.9 175 ± 10 16.3 6.0
7.1 5.9 ± 0.9 165 ± 8
7.2 12.5 ± 0.8 161 ± 4
7.4 12.7 ± 1.2 141 ± 5 131 56.2