Drug intelligence / Profile preview

exemestane + ruxolitinib

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

A combination therapy consisting of exemestane, an aromatase inhibitor, and ruxolitinib, a JAK1/JAK2 inhibitor. Exemestane works by irreversibly binding to the active site of the aromatase enzyme, resulting in permanent inhibition of estrogen production, while ruxolitinib inhibits Janus Associated Kinases (JAKs) JAK1 and JAK2, which mediate signaling of cytokines and growth factors important for hematopoiesis and immune function. This combination is being investigated for the treatment of estrogen receptor-positive breast cancer.

02

Targets

CYP19A1 (Aromatase)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)TYK2 (Tyrosine kinase 2)

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