Protein binding of 2-chloro 2'-deoxyadenosine (cladribine) in healthy subjects and in patients with leukaemia.
The plasma protein binding of 2-chloro-2'-deoxyadenosine (CdA) at 37 degrees 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.l-1), 24.3% CdA was bound, but less than 5% was bound in a solution of alpha 1-acid-glycoprotein (0.7 g.l-1). No dependence of binding on the concentration of CdA was found within a range 25-1000 nmol.l-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.
Albertioni
F
F
Department of Clinical Pharmacology, Karolinska Hospital, Stockholm, Sweden.
Herngren
L
L
Juliusson
G
G
Liliemark
J
J
D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D001798:Blood Proteins / Q000378:metabolism*; D017338:Cladribine / Q000378:metabolism*; D005260:Female; D006801:Humans; D007938:Leukemia / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D011485:Protein Binding
D001798:Blood Proteins; D017338:Cladribine