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Protein binding of 2-chloro 2′-deoxyadenosine (cladribine) in healthy subjects and in patients with leukaemia

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Abstract

The plasma protein binding of 2-chloro-2′-deoxyadenosine (CdA) at 37°;C was studied by ultrafiltration in 5 healthy volunteers, in 11 patients with haematological malignancies and in purified protein preparations. In the patients, the binding of CdA to plasma proteins was 25.0% and in healthy subjects it was 21.1%. In a solution of human serum albumin (40 g·1−1), 24.3% CdA was bound, but less than 5% was bound in a solution of α1-acid-glycoprotein (0.7 g·1−1). No dependence of binding on the concentration of CdA was found within a range 25–1000 nmol·1−1.

In conclusion, due to its limited binding to plasma proteins, any change in the binding of CdA is unlikely to have a major influence on its pharmacological effect.

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Albertioni, F., Herngren, L., Juliusson, G. et al. Protein binding of 2-chloro 2′-deoxyadenosine (cladribine) in healthy subjects and in patients with leukaemia. Eur J Clin Pharmacol 46, 563–564 (1994). https://doi.org/10.1007/BF00196117

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  • DOI: https://doi.org/10.1007/BF00196117

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