Drug intelligence / Profile preview

lonafarnib + anastrozole

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

**Lonafarnib + anastrozole** is a combination therapy of a farnesyltransferase inhibitor (lonafarnib) and an aromatase inhibitor (anastrozole). Lonafarnib inhibits the enzyme farnesyltransferase, thereby blocking the post-translational farnesylation of proteins including Ras and other farnesylated proteins involved in cell signaling, proliferation, and survival. Anastrozole inhibits aromatase, an enzyme crucial for the biosynthesis of estrogen, thus reducing estrogen levels and limiting the growth of hormone-sensitive breast cancer cells. This combination was developed and clinically investigated for the treatment of advanced hormone-sensitive breast cancer, aiming to increase efficacy by cotargeting estrogen-dependent and Ras-mediated growth pathways[1][2][6].

Other names
lonafarnib + anastrozole
02

Targets

FTase (Protein Farnesyltransferase)CYP19A1 (Aromatase)

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