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Enzastaurin

Yi-Bin Chen1, Ann S LaCasce

  • 1Dana Farber Cancer Institute, Massachusetts General Hospital, GRB 740, 44 Binney Street, Boston, MA 02115, USA.

Expert Opinion on Investigational Drugs
|May 22, 2008
PubMed
Abstract

Insights

Enzastaurin, an inhibitor of protein kinase C (PKC), shows promise in treating various cancers. Clinical trials indicate a favorable toxicity profile, particularly for B-cell lymphomas.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Enzastaurin is a novel antineoplastic and antiangiogenic agent.
  • It functions by inhibiting protein kinase C (PKC).

Purpose of the Study:

  • To review the scientific rationale for enzastaurin's use in oncology.
  • To summarize current clinical evidence for enzastaurin in cancer treatment.

Main Methods:

  • Systematic literature review using keywords 'protein kinase C-beta' and 'enzastaurin'.
  • Characterization of the therapeutic target protein kinase C-beta.
  • Review of in-vitro, Phase I, and Phase II data, focusing on hematologic malignancies.

Main Results:

  • Preliminary Phase I trials demonstrated a favorable toxicity profile for enzastaurin.
  • Enzastaurin has been investigated in Phase II and III studies for solid and hematologic malignancies.

Conclusions:

  • The rationale for using enzastaurin is most promising in B-cell lymphomas.
  • Ongoing studies continue to evaluate enzastaurin in various cancer types.

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