Abstract
Using [3H]-vinorelbine, we demonstrated the presence of saturable and time-dependent high-affinity binding sites on human platelets and lymphocytes. The dissociation constant and binding-site values observed were 200±38 nM, 20.0±2.2 amol/platelet, and 155±20 amol/lymphocyte, respectively. Among other blood components, saturable low-affinity binding of vinorelbine to alpha1-acid glycoprotein, serum albumin, and lipoproteins was observed. The binding to erythocytes was nonsaturable. Given the relative concentrations of these carriers, vinorelbine mainly distributes in the platelet compartment in blood (>70%), and the amount of free vinorelbine in plasma relative to the total amount in blood is <2%. It is suggested that because of the preferential retention of vinorelbine by platelets, variations in the platelet count are very likely to produce changes in the free blood fraction of vinorelbine.
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Urien, S., Brée, F., Breillout, F. et al. Vinorelbine high-affinity binding to human platelets and lymphocytes: distribution in human blood. Cancer Chemother. Pharmacol. 32, 231–234 (1993). https://doi.org/10.1007/BF00685841
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DOI: https://doi.org/10.1007/BF00685841