Drug intelligence / Profile preview

everolimus + letrozole + palbociclib

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

A combination of three drugs used for the treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer. Palbociclib is a CDK4/6 inhibitor that prevents cells from transitioning from G1 phase to S phase of the cell cycle. Letrozole is an aromatase inhibitor that reduces estrogen production. Everolimus is an mTOR inhibitor that targets resistance mechanisms to prolong response duration for endocrine therapy. This specific three-drug combination aims to provide multiple mechanisms to overcome resistance in advanced breast cancer.

02

Targets

CYP19A1 (Aromatase)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)Mechanistic target of rapamycin complex 1

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