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Renaissance of farnesyltransferase inhibitors in cancer

József Tímár1, Balázs Hegedűs2,3, Marcell Baranyi2

  • 1Department of Pathology, Forensic and Insurance Medicine, Semmelweis University, Budapest, Hungary. jtimar@gmail.com.

Journal of Translational Medicine
|May 29, 2026
PubMed
Abstract

Insights

Farnesyltransferase inhibitors (FTIs) show renewed promise in treating cancers, particularly when combined with other targeted therapies. Future clinical trials must use predictive markers to ensure successful implementation and avoid past failures.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Development

Background:

  • Prenylation, including geranylgeranylation and farnesylation, is crucial for RAS protein regulation.
  • Farnesyltransferase inhibitors (FTIs) were developed based on this understanding and tested in various cancers.
  • Initial clinical trials with FTIs were unsuccessful, halting their development.

Purpose of the Study:

  • To explore the renewed potential of farnesyltransferase inhibitors (FTIs) in oncology.
  • To highlight novel preclinical findings supporting FTI efficacy in combination therapies.
  • To emphasize the importance of predictive markers for future FTI clinical trials.

Main Methods:

  • Review of clinical trial outcomes and recent preclinical findings.
  • Analysis of FTI applications in progeria syndromes and HRAS-mutant head and neck cancers.
  • Investigation of FTI potential in combination with KRAS, EGFR, and multikinase inhibitors.

Main Results:

  • FTIs have seen a resurgence with approvals in rare diseases and specific cancer types.
  • Preclinical data suggest FTIs can enhance the efficacy of novel KRAS inhibitors and other targeted therapies.
  • Ongoing trials are exploring FTIs for viral infections like HDV, RSV, and SARS.

Conclusions:

  • Farnesyltransferase inhibitors (FTIs) are experiencing a "second chance" in oncology.
  • Successful clinical implementation requires avoiding past mistakes, specifically the lack of predictive markers.
  • Future trials must incorporate predictive biomarkers to optimize FTI therapy outcomes.
Keywords:
Farnesyltransferase inhibitorHRASPrenylationRAS inhibitorTarget therapy

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