Drug intelligence / Profile preview

vistusertib + palbociclib + fulvestrant

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

This is a combination therapy consisting of **vistusertib** (a dual mTORC1/2 inhibitor, also known as AZD2014), **palbociclib** (a selective CDK4/6 inhibitor, brand name Ibrance), and **fulvestrant** (a selective estrogen receptor degrader, brand name Faslodex). The rationale for the combination is that co-inhibition of the mTOR pathway (by vistusertib), the CDK4/6-Rb pathway (by palbociclib), and estrogen receptor signaling (by fulvestrant) may achieve a more profound and sustained inhibition of growth in estrogen receptor–positive (ER+) breast cancers, including those with resistance to endocrine therapy[1][5]. Preclinical studies and early clinical trials suggest that the triple regimen can induce tumor regression and long-term growth inhibition by convergently suppressing mTOR, RB-E2F, and estrogen receptor pathways, without marked increases in apoptosis over dual therapy[1].

Brand names
Ibrance + Faslodex
Other names
AZD2014 + Ibrance + Faslodex
02

Targets

CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)mTOR (Mammalian target of rapamycin kinase)ER (Estrogen receptor)

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