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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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

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

Volume 3, Issue 10, 2003

Page: [1103 - 1114] Pages: 12

DOI: 10.2174/1568026033452104

Price: $65


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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