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Tipifarnib: farnesyl transferase inhibition at a crossroads

Ruben A Mesa1

  • 1Division of Hematology and Internal Medicine, Mayo Clinic, Rochester, MN 55905, USA. mesa.ruben@mayo.edu

Expert Review of Anticancer Therapy
|March 1, 2006
PubMed

Insights

Tipifarnib, an oral farnesyl transferase inhibitor, shows promise in myeloid malignancies like myelodysplastic syndrome and acute myeloid leukemia. While ineffective in solid tumors, ongoing trials explore its combination therapy potential.

Area of Science:

  • Oncology
  • Pharmacology

Background:

  • Tipifarnib is an oral farnesyl transferase inhibitor targeting farnesylated proteins implicated in cancer.
  • It has been investigated across various solid tumors and myeloid malignancies.

Purpose of the Study:

  • To evaluate the efficacy and tolerability of tipifarnib in treating different types of cancer.
  • To identify specific cancer types where tipifarnib demonstrates therapeutic potential.

Main Methods:

  • Phase I, II, and III clinical trials were conducted for tipifarnib.
  • Dosing schedules and combination therapies were explored to optimize treatment outcomes.

Main Results:

  • Tipifarnib monotherapy trials for breast, colorectal, lung, brain, pancreatic, and urothelial cancers were disappointing.
  • Significant activity was observed in myelodysplastic syndrome, myelofibrosis, and acute myeloid leukemia, with response rates of 20-30%.

Conclusions:

  • Tipifarnib shows limited efficacy as a monotherapy for most solid tumors.
  • It demonstrates notable clinical activity in specific myeloid malignancies, offering a potential new treatment avenue for patients with limited options.

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