Drug intelligence / Profile preview

palbociclib + anastrozole + letrozole + exemestane + hydroxychloroquine

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

Overview

This combination regimen is being investigated by Sun Yat-Sen Memorial Hospital for the treatment of hormone receptor-positive (HR+), HER2-negative advanced breast cancer. It consists of the CDK4/6 inhibitor palbociclib, an aromatase inhibitor (anastrozole, letrozole, or exemestane), and the autophagy inhibitor hydroxychloroquine. The rationale for adding hydroxychloroquine is to inhibit autophagy, a survival mechanism by which cancer cells may develop resistance to CDK4/6 inhibition and endocrine therapy. The regimen is being evaluated in a Phase III trial comparing standard and high-dose palbociclib combinations to standard endocrine therapy plus palbociclib to determine if the addition of an autophagy inhibitor can improve clinical outcomes in patients with advanced disease.

Other names
Hydroxychloroquine and High-Dose Palbociclib in HR+/HER2- Advanced Breast Cancer
02

Targets

V-ATPase (Vacuolar-type H+-ATPase)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)CYP19A1 (Aromatase)

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