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[Everolimus (RAD001) and solid tumours: a 2008 summary]

A Lévy1, L Albiges Sauvin, C Massard

  • 1Département de médecine, service des innovations thérapeutiques précoces (SITEP), Institut Gustave-Roussy, Villejuif.

Bulletin Du Cancer
|December 19, 2008
PubMed

Insights

Everolimus, an inhibitor of mammalian target of rapamycin (mTOR), demonstrates significant anti-angiogenic and anti-proliferative effects in preclinical cancer models. Clinical data show antitumor activity, particularly in metastatic renal cell cancer, with good tolerability.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Mammalian target of rapamycin (mTOR) is a key regulator of cell growth and proliferation.
  • mTOR signaling is implicated in various human cancers.
  • Everolimus is an oral mTOR inhibitor derived from rapamycin.

Purpose of the Study:

  • To review preclinical data and clinical results of everolimus (RAD001).
  • To evaluate the anti-angiogenic and anti-proliferative activity of everolimus.
  • To discuss the tolerability and antitumor effects of everolimus in malignancies.

Main Methods:

  • Review of preclinical studies on human tumor cell lines and xenograft models.
  • Analysis of clinical trial data for everolimus in cancer patients.
  • Assessment of adverse events and antitumor responses.

Main Results:

  • Everolimus exhibits significant anti-angiogenic and anti-proliferative activity in preclinical models.
  • Clinical studies demonstrate antitumor activity, including tumor regression and stable disease.
  • Everolimus is generally well-tolerated, with manageable side effects.

Conclusions:

  • Everolimus shows promising antitumor activity across various malignancies, especially metastatic renal cell cancer.
  • The compound is well-tolerated, with reversible adverse events.
  • Further clinical development of everolimus is warranted.

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