Recombinant human granulocyte-macrophage colony-stimulating factor: effect of glycosylation on pharmacokinetic parameters

the pharmacokinetic behaviour of the non-glycosylated, bacterially-derived recombinant human granulocyte-macrophage colony-stimulating factor (rhgm-csf) and the glycosylated mammalian product was studied after intra and extra vascular administration of a single dose in rodents. each route of administration gave a different rhgm-csf concentration-time profile. after extra vascular administration of equivalent doses, a higher peak concentration and faster elimination were observed in the group treated with the e. coli-derived cytokine. the faster elimination resulted in a return to pre-treatment plasma levels after 12 hrs, versus 48 hrs following the administration of glycosylated rhgm-csf. after intravascular administration, clearance of rhgm-csf was significantly decreased by the presence of carbohydrates. non-significant differences in the terminal phase of the biphasic kinetics were found, but the distribution phase was significantly longer for the glycosylated form