Binding of Toremifene to Human Serum Proteins

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Abstract
The in vitro protein binding of toremifene in human serum was measured by ultracentrifugation using 3H-toremifene together with unlabeled toremifene, 50, 500, and 5000 ng/ml. Of the total radioactivity 99.7 percent was bound to the proteins independent of the concentration of the unlabeled drug. Binding of toremifene to different protein fractions was studied by adding 3H-toremifene and 500 ng/ml of cold toremifene to normal serum. The radioactivity was localized using a position-sensitive proportional counter. After that the proteins were visualized by staining. Of the total protein bound radioactivity 92 percent was bound to albumin, about 6 percent to .beta.1 globulin fraction and about 2 percent to a fraction between albumin and .alpha.1 globulins, part of this probably to .alpha.1 acid glycoprotein.

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