Exploring new frontiers: Sirolimus as a pharmacokinetic modulator in advanced cancer patients

Massimiliano Veroux, Tiziano Tallarita, Daniela Corona, Antonino D'Assoro, Pierfrancesco Veroux

Research output: Contribution to journalReview articlepeer-review

1 Scopus citations


The mTOR pathway mediates many biologic functions such as transcriptional and translational control, and is a target for anticancer drug development. mTOR inhibitors, such as sirolimus (SRL), display immunosuppressive and antiproliferative properties, and the use of SRL in kidney transplant recipients reduces the risk of post-transplant cancer. However, its use in advanced cancer patients has not been fully evaluated. The authors review the study by Cohen et al., evaluating the dose for oral, weekly SRL alone or in combination with grapefruit juice or ketoconazole to achieve the desired whole-blood concentration with antitumoral activity. This study demonstrates that SRL can be feasibly administered orally once weekly and displays a similar pharmacokinetic profile compared with other mTOR inhibitors. This study encouraged the use of SRL in advanced cancer patients and can stimulate clinical trials with a larger number of patients, evaluating the role of SRL as a new targeted therapy in cancer patients.

Original languageEnglish (US)
Pages (from-to)17-20
Number of pages4
JournalExpert review of anticancer therapy
Issue number1
StatePublished - Jan 2013


  • cancer
  • grapefruit juice
  • ketoconazole
  • once weekly
  • oral
  • sirolimus
  • transplantation

ASJC Scopus subject areas

  • Oncology
  • Pharmacology (medical)


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