Pharmacokinetic and tumor distribution characteristics of temsirolimus in patients with recurrent malignant glioma Academic Article uri icon


MeSH Major

  • Anticonvulsants
  • Antineoplastic Agents
  • Brain Neoplasms
  • Glioma
  • Sirolimus


  • Drugs that induce cytochrome P450 3A4, such as EIAEDs, significantly affect the pharmacokinetics of temsirolimus and its active metabolite, sirolimus. Total exposure to temsirolimus and sirolimus was lower in the EIAED group at the maximum tolerated dose of 250 mg compared with the non-EIAED group at the maximum tolerated dose of 170 mg. However, brain tumor tissue concentrations of temsirolimus and sirolimus were relatively comparable in both groups of patients at their respective dose levels. Correlative analyses of the tissue for the inhibition of the key regulators (p70S6 kinase and 4E-binding protein 1) of mammalian target of rapamycin are necessary to define the therapeutic significance of the altered exposure to temsirolimus.

publication date

  • December 15, 2007



  • Academic Article



  • eng

PubMed Central ID

  • PMC4918812

Digital Object Identifier (DOI)

  • 10.1158/1078-0432.CCR-07-0781

PubMed ID

  • 18094423

Additional Document Info

start page

  • 7401

end page

  • 6


  • 13


  • 24