Title: Sch-66336 (Sarasar®) and Other Benzocycloheptapyridyl Farnesyl Protein Transferase Inhibitors: Discovery, Biology and Clinical Observations
Volume: 3
Issue: 10
Author(s): Arthur G. Taveras, Paul Kirschmeier and Charles M. Baum
Affiliation:
Keywords:
Sch-66336, Benzocycloheptapyridyl Farnesyl Protein, anti-cancer agents
Abstract: Farnesyl Protein Transferase as a target for therapeutic intervention is currently under investigation in human clinical trials. Sch-66336 (sarasar®), a benzocycloheptapyridyl Farnesyl Transferase Inhibitor (FTI), has been found to be effective in cellular proliferation assays and in in vivo oncology models both as a single agent and in combination with other anti-cancer agents. Clinically, early evidence is being generated that suggests efficacy in humans, particularly in patients with leukemia. Herein, we review the biology of FPT, the discovery of Sch-66336 and other benzocycloheptapyridyl FTIs, and the clinical evaluation of Sch-66336 for the treatment of leukemia and solid tumors.
