tipifarnib + cytarabine + daunorubicin

This combination therapy consists of the farnesyltransferase inhibitor tipifarnib (Zarnestra) administered alongside standard induction chemotherapy agents cytarabine and daunorubicin. Tipifarnib works by inhibiting the farnesyltransferase enzyme, which is responsible for the post-translational modification (farnesylation) of proteins like Ras, thereby preventing their localization to the cell membrane and subsequent signaling. This specific regimen was investigated by the University Health Network, Toronto, in a Phase I dose-escalation study targeting older patients (aged 55 and older) with previously untreated acute myeloid leukemia (AML). While tipifarnib was initially developed by Johnson & Johnson and later licensed to Kura Oncology, its development for AML faced regulatory hurdles, including a 2005 FDA 'not approvable' letter for monotherapy in elderly AML.

Brand names

Zarnestra

Other names

Tipifarnib + Cytarabine + DaunorubicinZarnestra + Cytarabine + DaunorubicinZ-University Health Network, Toronto-leukemia (acute myeloid)