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letrozole + tipifarnib
- Development stage
- Phase 2
- Lead developer
- Janssen Research & Development
- Modality
- Small Molecules
- Administration
- Oral
01
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.
02
Targets
CYP19A1 (Aromatase)FTase (Protein Farnesyltransferase)
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