Enzastaurin

Shuo Ma, Steven T. Rosen*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

32 Scopus citations

Abstract

PURPOSE OF REVIEW: Enzastaurin - a novel oral antitumor agent that selectively inhibits protein kinase Cβ activity - has demonstrated promise in phase I and II trials in various advanced cancers, and is being investigated in multiple hematologic malignancies and solid tumors. RECENT FINDINGS: Enzastaurin (LY317615) was initially developed as an antiangiogenic cancer therapy. Subsequent preclinical studies showed its antitumor effect by inhibiting tumor proliferation and inducing apoptosis on multiple cancer cell lines as well as xenograft models. Enzastaurin not only inhibits protein kinase Cβ activity but also suppresses signaling through the phosphoinositide-3 kinase/AKT pathway. Based on the phase I study, 525 mg/day is the recommended dose for oral enzastaurin. It is well tolerated at this dose, with no clinically significant grade 3 or 4 toxicities. A recent phase II study of enzastaurin in patients with relapsed or refractory diffuse large B-cell lymphoma showed enzastaurin to be associated with prolonged freedom from progression. Several preliminary studies showed promising results in patients with various advanced cancers and suggested that enzastaurin can be safely used long term in combination with traditional chemotherapies. SUMMARY: Enzastaurin is emerging as a promising new antitumor treatment. This review addresses the mechanism of action, development, preclinical studies, and clinical study results with enzastaurin.

Original languageEnglish (US)
Pages (from-to)590-595
Number of pages6
JournalCurrent opinion in oncology
Volume19
Issue number6
DOIs
StatePublished - Nov 1 2007

Keywords

  • Angiogenesis
  • Enzastaurin
  • LY317615
  • Protein kinase Cβ inhibitor

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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