Sch-66336 (Sarasar�) and Other Benzocycloheptapyridyl Farnesyl Protein Transferase Inhibitors: Discovery, Biology and Clinical Observations

A.G. Taveras; P. Kirschmeier; C.M. Baum
June 2003
Current Topics in Medicinal Chemistry;Jun2003, Vol. 3 Issue 10, p1103
Academic Journal
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.


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