Farnesyl Transferase Inhibitors for Patients with Lung Cancer

摘要: The ras family of genes have been identified as potential targets for therapeutic intervention because somatic mutations in different human cancers. They are mutated non-small cell lung cancer (NSCLC) ∼20% the time. enzyme farnesyl transferase is involved posttranslational modification proteins by covalently linking a group to protein. This permits protein be translocated surface membrane, allowing signaling increased proliferation and inhibition apoptosis. class inhibitors designed block farnesylation prevent mature thus inhibit facilitate Multiple agents that developed, two tested patients with three Phase II trials. R115777 has studied NSCLC relapsed small (SCLC) after chemotherapy. There single trial L-778,123 untreated NSCLC. No objective tumor responses stage IIIB/IV were seen these studies. also no among 22 SCLC treated R115777. median survival 44 was ∼8 months, whereas it 11 months 23 L-778,123. well tolerated studies but showed significant activity single-agent therapy or NSLC.