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

Author(s): Arthur G. Taveras, Paul Kirschmeier, Charles M. Baum

Journal Name: Current Topics in Medicinal Chemistry

Volume 3 , Issue 10 , 2003

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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.

Keywords: Sch-66336, Benzocycloheptapyridyl Farnesyl Protein, anti-cancer agents

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Article Details

Year: 2003
Page: [1103 - 1114]
Pages: 12
DOI: 10.2174/1568026033452104
Price: $65

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