Drug intelligence / Profile preview

letrozole + tipifarnib

Development stage: Unknown
Lead developer: Janssen Research & Development
Modality: Small Molecules
Administration: Oral

Overview

Letrozole + tipifarnib is a combination therapy that pairs letrozole, an aromatase inhibitor, with tipifarnib, a farnesyltransferase inhibitor. Letrozole works by reducing estrogen production through inhibition of the aromatase enzyme, while tipifarnib inhibits farnesyltransferase, an enzyme involved in the post-translational modification of proteins, including RAS proteins. This combination was studied for the treatment of advanced breast cancer in patients who had progressed after antiestrogen therapy, with the hypothesis that adding tipifarnib might improve response rates compared to letrozole alone.

Targets

FTase (Protein Farnesyltransferase)CYP19A1 (Aromatase)

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