Figure 4.

Pharmacokinetic study of eribulin in a mouse brain tumor model. Eribulin concentrations in plasma, transplanted brain tumor tissue and contralateral normal brain tissue from mice with intracerebral U87MG tumors. A, Mice with U87MG brain tumors were killed at 15 min, 1, 2, 4, 6 and 24 h after a single intravenous injection of eribulin (0.5 mg/kg, n = 3 for each time point). Plasma, tumor tissue and contralateral normal brain tissue were harvested and immediately frozen for measurement of eribulin concentration. Eribulin concentration in plasma gradually decreased after injection and became undetectable after 24 h. The concentration of eribulin in non–tumoral brain tissue was very low and undetectable after 2 h. In contrast, eribulin concentration in the brain tumor tissue was almost as high as that in plasma 15 minutes after injection,and remained high up to 24 h. B, The tumor/plasma ratio of eribulin gradually increased for up to 6 h (plasma concentration undetectable after 24 h). See supplementary data for tissue/plasma concentration of eribulin (Figure S2)