Drug intelligence / Profile preview

BMS-214662

Development stage
Phase 1
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Intravenous
01

Overview

BMS-214662 is a potent, selective small molecule inhibitor of protein farnesyltransferase (FTase), developed by Bristol Myers Squibb for antineoplastic therapy. It is a nonsedating benzodiazepine derivative that inhibits the post-translational farnesylation of proteins involved in signal transduction—most notably Ras proteins—thereby disrupting Ras function and inducing apoptosis in susceptible tumor cells. The drug has demonstrated broad-spectrum cytotoxicity against human solid tumor cell lines and was investigated in clinical trials for various cancers including acute leukemias, myelodysplastic syndromes (MDS), and advanced solid tumors. Although it reached phase II clinical trials for several indications, further development appears to have been discontinued[1][3][5][6][7].

Other names
(3R)-3-benzyl-1-(1H-imidazol-5-ylmethyl)-4-thiophen-2-ylsulfonyl-3,5-dihydro-2H-1,4-benzodiazepine-7-carbonitrileUNII-L2U9GFD244UNII-L-2U9GFD244UNII-L 2U9GFD244
02

Targets

FTase (Protein Farnesyltransferase)

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