[Pharmacokinetics of Nolaterex in tumor cells].

OBJECTIVE: To investigate the relationship of the transportation characteristics of Nolaterex, a new anti-cancer drug, with its sensitivity in tumor cells. METHODS: The sensitivities of 3 tumor cell lines (C6, SRS-82 and LoVo) to nolaterex were determined by growth inhibition test. After Nolaterex exposure, the intracellular drug concentration was measured by high-performance liquid chromatography. RESULTS: C6 was the most sensitive among the 3 cell lines, and the IC50 values of SRS-82 and LoVo cells were 6.8-fold and 13.8-fold higher, respectively, than that of C6 cells. In all the 3 cell lines, linear relationship between intracellular and extracellular drug concentrations was noted. The intracellular steady-state level achieved in C6 was significantly higher than the levels in the other two cell lines. CONCLUSIONS: The results indicate that nolaterex quickly enters the cells, and different cell lines may have different nolaterex-transporting capacities, thus partially accounting for different states of sensitivity of the tumor cells to nolaterex.