Pharmacokinetics of etanidazole (SR-2508) in bladder and cervical cancer: Evidence of diffusion from urine

Awwad, Hassan K.; Badawy, Samy El; Baki, Hoda Abd El; Zaghloul, Mohammed; Osman, Abd El Moneim; Akouh, Hany; Fairchild, Karen D.

doi:10.1016/0360-3016(89)90921-8

Cited by 6 publications

(1 citation statement)

References 3 publications

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“…These authors quote values of Ci/Ce of 0.2-0 . The QC, values obtained in this study for both drugs are well in the range of the published values for animal tumours, human tumour xenografts and tumours in patients , White et al 1980, Hill et al 1983, Coleman et al 1984, Minchinton and Stratford 1986, Newman et al 1986, Dische et al 1986b, Walton et al 1987, Dische 1987, Awwad et al 1989, Bleehen et al 1989, Laurent et al 1989, Lespinasse et al 1989 .They also agree well with pharmacokinetic 6 to 1 .…”

Section: Discussionsupporting

confidence: 87%

Relationship between Intracellular Concentration and Radiosensitizing Effect of Pimonidazole and Etanidazole on Two Human Melanoma Cell Lines

Gamoussi

Stratford

Guichard

1993

International Journal of Radiation Biology

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A study on the uptake and radiosensitizing properties of pimonidazole (PIMO) and etanidazole (ETA) was made in vitro with two melanoma cell lines: Na11+ and Na11-. The amelanotic Na11- was derived from the pigmented Na11+ cell line and was characterized by the complete absence of pigmentation in vitro. Plateau-phase cells were heavily pigmented for the Na11+ line whereas exponential cells showed a lower melanin content. Radiosensitivity was studied using an in vitro colony assay; intracellular drug concentration was determined by HPLC. For both cell lines the uptake of PIMO was always higher than the uptake of ETA, and slightly higher in hypoxia than in air. The uptake of PIMO was exceptionally high in plateau-phase cells of the pigmented Na11+ cell line. The radiosensitizing effect of ETA did not differ greatly as a function of the cell kinetics in both cell lines, whereas the radiosensitizing effect of PIMO was cell line-dependent. Sensitization of exponential cells by PIMO was similar in both cell lines but significantly less in plateau-phase cells, with the heavily pigmented Na11+ cell line being least affected, despite a three-fold increase in PIMO uptake observed in plateau cells relative to exponentially growing Na11+ cells. The uptake of PIMO may be related to the high melanin content of plateau-phase Na11+ cells and therefore this in vitro model may be useful for predicting the effects of agents such as PIMO towards melanotic melanomas in vivo.

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