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everolimus + letrozole + palbociclib

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

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.

Targets

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

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