Farnesyl protein transferase (FPT) inhibition is an interesting and promising approach to non-cytotoxic anticancer therapy. Research in this area has resulted in several orally active compounds that are currently in clinical evaluation. This review focuses on FPT inhibitors in clinical trials and concentrates on the benzocycloheptapyridine class, with details on the discovery and development of SCH 66336, currently in Phase II clinical trials.
Keywords: Farnesyl Protein Transferase Inhibition, Anti-tumor Therapy, farnesyl protein transferase, Farnesylation, Geranlylgeranylation, carboxymethyl transferase, FPT Enzyme Assay, COS Assay, Pharmacokinetic Assay (PK), Potent FPT Inhibitors
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