Drug intelligence / Profile preview

fulvestrant + palbociclib + pertuzumab + trastuzumab

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intramuscular, Oral, Intravenous, Subcutaneous
01

Overview

A combination therapy regimen consisting of four distinct agents targeting multiple cancer pathways: fulvestrant (an estrogen receptor antagonist), palbociclib (a CDK4/6 inhibitor), and the dual HER2-targeted antibodies pertuzumab and trastuzumab. This combination approach is designed for HER2-positive breast cancer, particularly in cases that are also hormone receptor positive. The pertuzumab and trastuzumab components bind to different domains of HER2, creating a synergistic effect in blocking HER2 signaling pathways.

02

Targets

HER2 ECD II (Human epidermal growth factor receptor 2 domain II)CDK4 (Cyclin-dependent kinase 4)ESR1 (ERα)CDK6 (Cyclin-dependent kinase 6)GPER1 (G protein-coupled estrogen receptor 1)ESR2 (ERβ)

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