The binding of the antimalarial arteether to human plasma proteins in‐vitro

Abstract— The binding of the novel antimalarial drug, arteether, to human plasma, pure albumin and α1‐acid glycoprotein has been investigated by ultrafiltration, using [14C]arteether. The protein binding in plasma obtained from 11 healthy male subjects ranged from 73·4 to 81·8% bound, with a mean of 78·7 ± 2·1%. The binding of drug in plasma was mainly accounted for by binding to albumin and α1‐acid glycoprotein. Scatchard analysis of the binding data revealed that the binding affinity of arteether to α1‐acid glycoprotein is much greater (20‐fold) than that to albumin. This suggests that α1‐acid glycoprotein is the more important binding protein in plasma. This may have clinical importance due to alterations in plasma protein binding in patients with malaria, as the concentration of α1‐acid glycoprotein is markedly increased during malarial infection. 1992 Royal Pharmaceutical Society of Great Britain