Pharmacokinetics and pharmacodynamics of IFN-beta 1a in healthy volunteers

J Interferon Cytokine Res. 2000 Oct;20(10):857-66. doi: 10.1089/10799900050163226.


The pharmacokinetics of recombinant human interferon-beta1a (IFN-beta1a) (Rebif, Ares-Serono, Geneva, Switzerland) were investigated in healthy volunteers following intravenous (i.v.) administration of increasing single doses of the drug (22 microg/6 million international units [MIU], 44 microg/12 MIU, and 66 microg/18 MIU); i.v., intramuscular (i.m.), and subcutaneous (s.c.) administration of a 66-microg dose; and repeated s.c. administration of four 66-microg doses at 48-h intervals. The disposition of IFN-beta1a followed triexponential decay after i.v. administration (half-lives 3 min, 42 min, and 22 h, respectively). After s.c. and i. m. administration, absorption was the rate-limiting factor in the terminal phase. The median absolute bioavailabilities were 30% and 27%, respectively. The accumulation ratio after repeated s.c. injections was 2.4, and a terminal half-life of 66 h was observed. Intracellular 2-5A synthetase activity and serum neopterin and beta2-microglobulin concentrations increased after all IFN-beta1a injections and remained elevated following every-other-day administration. The local tolerance was good, and the systemic tolerance was satisfactory.

Publication types

  • Clinical Trial

MeSH terms

  • Adolescent
  • Adult
  • Area Under Curve
  • Female
  • Humans
  • Injections, Intramuscular
  • Injections, Intravenous
  • Interferon Type I / administration & dosage
  • Interferon Type I / adverse effects
  • Interferon Type I / pharmacokinetics
  • Interferon Type I / pharmacology
  • Interferon-beta / administration & dosage
  • Interferon-beta / adverse effects
  • Interferon-beta / pharmacokinetics*
  • Interferon-beta / pharmacology*
  • Male
  • Maximum Tolerated Dose
  • Recombinant Proteins


  • Interferon Type I
  • Recombinant Proteins
  • Interferon-beta