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Background <p>Prenylation (geranylgeranylation or farnesylation) plays an important role in the regulation of RAS proteins. This observation led to development of farnesyltransferase inhibitors (FTI) which were extensively tested in clinical studies of various cancer types. Unfortunately, these studies failed and the development of these drugs stalled.</p> Main body <p>The renaissance of FTIs started with the approval of lonafarnib in children’s progeria syndromes and continued with the approval of tipifarnib in HRAS-mutant head and neck cancers. Although there are several trials running on various viral infections (HDV, RSV, SARS), their future in oncology is based on the novel preclinical findings that FTIs can potentiate the efficacy of novel KRAS inhibitors or other target therapies such as EGFR- or multikinase inhibitors.</p> Conclusions <p>The „second chance” for FTIs is here but the successful clinical implementation of FTIs can only be achieved if the design of the new clinical trials do not repeat mistakes of the past: application of these drugs without predictive markers.</p>

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Renaissance of farnesyltransferase inhibitors in cancer

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2026年5月28日

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  • József Tímár,
  • Balázs Hegedűs,
  • Marcell Baranyi

摘要

Background

Prenylation (geranylgeranylation or farnesylation) plays an important role in the regulation of RAS proteins. This observation led to development of farnesyltransferase inhibitors (FTI) which were extensively tested in clinical studies of various cancer types. Unfortunately, these studies failed and the development of these drugs stalled.

Main body

The renaissance of FTIs started with the approval of lonafarnib in children’s progeria syndromes and continued with the approval of tipifarnib in HRAS-mutant head and neck cancers. Although there are several trials running on various viral infections (HDV, RSV, SARS), their future in oncology is based on the novel preclinical findings that FTIs can potentiate the efficacy of novel KRAS inhibitors or other target therapies such as EGFR- or multikinase inhibitors.

Conclusions

The „second chance” for FTIs is here but the successful clinical implementation of FTIs can only be achieved if the design of the new clinical trials do not repeat mistakes of the past: application of these drugs without predictive markers.