Renaissance of farnesyltransferase inhibitors

In case of RAS proteins prenylation (geranylation or farnesylation) plays an important role in their functional activity. This led to development of farnesyltransferase inhibitors (FTI) which were extensively tested in various cancer type clinically but they failed in the past and these drugs have been forgotten. 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. There are several trials running on various viral infections (HDV, RSV, SARS) but their future in oncology could be based on those novel preclinical findings that FTIs can potentiate the efficacy of novel KRAS inhibitors.