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Farnesyl transferase inhibitors in myeloid malignancies

Jeffrey E Lancet1, Judith E Karp

  • 1University of Rochester, James P. Wilmot Cancer Center, 601 Elmwood Avenue, Box 704 Rochester, NY 14642, USA. jeffrey_lancet@urmc.rochester.edu

Blood Reviews
|June 24, 2003
PubMed

Insights

Farnesyl transferase inhibitors (FTIs) show promise in treating myeloid cancers like acute myelogenous leukemia (AML). Early trials indicate target inhibition, low toxicity, and good response rates, warranting further investigation.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Farnesyl transferase inhibitors (FTIs) are a new class of anti-cancer drugs.
  • They work by inhibiting farnesyl protein transferase (FPT), a key enzyme in cancer cell proliferation and survival.
  • Hematologic malignancies, especially myeloid cancers, are potential targets due to overexpression of FPT-dependent pathways like Ras, MAPK, and AKT.

Purpose of the Study:

  • To evaluate the efficacy and safety of FTIs in myeloid malignancies.
  • To identify downstream signaling targets affected by FTIs.
  • To establish the optimal role of FTIs in AML and other myeloid disorders, including combination therapies.

Main Methods:

  • Phase I clinical trials were conducted using FTIs in patients with acute myelogenous leukemia (AML) and other myeloid malignancies.
  • Enzyme inhibition, toxicity, and response rates were assessed.
  • Phase II trials are ongoing to further clarify response rates and identify specific downstream signaling pathways modulated by FTIs.

Main Results:

  • Phase I trials demonstrated successful enzyme target inhibition with FTIs.
  • The agents exhibited low toxicity profiles in initial studies.
  • Promising response rates were observed in patients with myeloid malignancies, including AML.

Conclusions:

  • FTIs represent a promising therapeutic strategy for hematologic malignancies, particularly AML.
  • Further Phase II trials are crucial for confirming efficacy and understanding the precise mechanisms of action.
  • FTIs may be integrated into current treatment regimens and combined with other signal transduction inhibitors for enhanced outcomes.

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