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Enzastaurin

Shuo Ma1, Steven T Rosen

  • 1Division of Hematology/Oncology, Department of Medicine, Robert H. Lurie Comprehensive Cancer Center, Northwestern University, Chicago, Illinois 60611, USA.

Current Opinion in Oncology
|October 2, 2007
PubMed
Abstract

Insights

Enzastaurin, an oral antitumor drug, shows promise in treating advanced cancers by inhibiting protein kinase Cbeta and the AKT pathway. Clinical trials indicate it is well-tolerated and effective, particularly in diffuse large B-cell lymphoma.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Enzastaurin is a novel oral antitumor agent targeting protein kinase Cbeta.
  • It has shown potential in early-phase trials for various advanced cancers.

Purpose of the Study:

  • To review the mechanism of action, development, and clinical results of Enzastaurin.
  • To assess its efficacy and safety in hematologic malignancies and solid tumors.

Main Methods:

  • Preclinical studies evaluated antitumor effects on cancer cell lines and xenografts.
  • Phase I and II clinical trials assessed safety, dosage, and efficacy in cancer patients.

Main Results:

  • Enzastaurin inhibits protein kinase Cbeta and the phosphoinositide-3 kinase/AKT pathway.
  • The recommended oral dose is 525 mg/day, with good tolerability and no significant grade 3 or 4 toxicities.
  • Phase II studies in diffuse large B-cell lymphoma demonstrated prolonged freedom from progression.

Conclusions:

  • Enzastaurin is an emerging and promising antitumor treatment.
  • It can be safely used long-term in combination with chemotherapy for various advanced cancers.

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