Drug intelligence / Profile preview

everolimus + exemestane + palbociclib

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

Overview

This is a combination therapy consisting of three drugs—everolimus, exemestane, and palbociclib—used in the treatment of hormone receptor-positive (HR+), HER2-negative advanced or metastatic breast cancer. Everolimus is an mTOR inhibitor that blocks the mammalian target of rapamycin pathway, which is involved in cell growth and proliferation. Exemestane is an aromatase inhibitor that reduces estrogen production. Palbociclib is a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that prevents cell cycle progression by inhibiting CDK4 and CDK6 enzymes[2][3]. The combination has been investigated for patients with disease progression after prior endocrine therapy or CDK4/6 inhibitors[2]. The triplet regimen aims to overcome resistance to standard endocrine therapies by targeting multiple pathways simultaneously.

Other names
everolimus/exemestane/palbociclibpalbociclib/everolimus/exemestaneexemestane plus everolimus and palbociclib
02

Targets

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

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