The effects of dose and route of administration on the pharmacokinetics of granulocyte-macrophage colony-stimulating factor

Eur J Cancer. 1990;26(10):1064-9. doi: 10.1016/0277-5379(90)90053-v.


The pharmacokinetics of granulocyte-macrophage colony stimulating factor (GM-CSF) (0.3-30 micrograms/kg) were studied after subcutaneous bolus (n = 16) or intravenous bolus (n = 5) injection or 2 h intravenous infusion (n = 12). Each method of administration gave a different GM-CSF concentration-time profile. Highest peak serum concentrations (Cmax) followed the intravenous bolus, and the time GM-CSF persisted at a concentration greater than 1 ng/ml (t greater than 1 ng/ml) was longer after a subcutaneous than after an intravenous injection. Area under the concentration-time curve (AUC), Cmax and t greater than 1 ng/ml all increased with dose for each method of administration. After intravenous administration, there was a two-phase decline in concentration. The half-life (t1/2) of the terminal phase following an intravenous bolus ranged from 0.24 to 1.18 h and, following intravenous infusion, from 0.62 to 9.07 h and appeared to increase with dose. The apparent clearance was greatest following subcutaneous injection at doses below 3 micrograms/kg, suggesting a saturable mechanism or different bioavailability. Only 0.001%-0.2% of the injected dose appeared in the urine as immunoreactive GM-CSF.

Publication types

  • Clinical Trial
  • Comparative Study
  • Controlled Clinical Trial

MeSH terms

  • Adult
  • Aged
  • Dose-Response Relationship, Drug
  • Drug Evaluation
  • Female
  • Granulocyte-Macrophage Colony-Stimulating Factor / administration & dosage
  • Granulocyte-Macrophage Colony-Stimulating Factor / pharmacokinetics*
  • Granulocyte-Macrophage Colony-Stimulating Factor / urine
  • Humans
  • Infusions, Intravenous
  • Injections, Intravenous
  • Injections, Subcutaneous
  • Male
  • Middle Aged
  • Neoplasms / drug therapy


  • Granulocyte-Macrophage Colony-Stimulating Factor