[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.
Li
Yi-lei
YL
Institute of Pharmaceutical Science, First Military Medical University, Guangzhou 510515, China.
Zhao
Ai-guo
AG
Wu
Shu-guang
SG
D000964:Antimetabolites, Antineoplastic / Q000493:pharmacokinetics*; D005493:Folic Acid Antagonists / Q000493:pharmacokinetics*; D006801:Humans; D009369:Neoplasms / Q000378:metabolism*; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors*; D014407:Tumor Cells, Cultured
D000964:Antimetabolites, Antineoplastic; D005493:Folic Acid Antagonists; D013940:Thymidylate Synthase