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Tipifarnib (also known as Zarnestra or R115777), an orally bioavailable quinolone analog of imidazole heterocyclics, is a potent and specific nonpeptidomimetic competitive inhibitor of farnesyltransferase (FTase), an enezyme mediating post-translational farnesylation of multiple protein substrates involved in tumor cell proliferation. It has demonstrated inhibition of growth and proliferation of a broad range of human tumor models (either wild-type or mutated RAS) via cytostatic rather than cytotoxic activity both in vitro and in vivo. It cell-type dependently induces apoptosis in some neoplastic cell lineages other than acute myeloid leukemia (AML), including multiple myeloma (MM) cell lines and MM cultures from patients.

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