darlifarnib

An orally bioavailable inhibitor of farnesyl transferase, with potential antineoplastic activity. Upon oral administration, darlifarnib targets, binds to and inhibits the enzyme farnesyl transferase. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits Ras-dependent signaling and inhibits the proliferation of tumor cells in which Ras is overexpressed and/or mutated. Ras plays an important role in cell signaling, division and differentiation. Mutations of Ras may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.