Summary
The binding of vinblastine (VLB) to recrystallized human α1-acid glycoprotein (α1-AGP) dissolved in phosphate-buffered saline (pH 7.4) was determined at different drug concentrations using the technique of continuous ultrafiltration. Vinblastine was extremely highly bound (>99.0%) at a drug concentration of 4.0 μmol·l-1, dropping to under 60% at 65.0 μmol·l-1. Binding was best described by a two-class model with higher-(9.4 μM-1) and lower-(0.1 μM-1) affinity sites but with a similar number of binding sites (1.5 as against 1.1 lower-affinity sites). These results strongly suggest that α1-AGP would be a major binding protein for VLB in plasma.
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Steele, W.H., Haughton, D.J. & Barber, H.E. Binding of vinblastine to recrystallized human α1-acid glycoprotein. Cancer Chemother. Pharmacol. 10, 40–42 (1982). https://doi.org/10.1007/BF00257236
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DOI: https://doi.org/10.1007/BF00257236