Drug intelligence / Profile preview

fulvestrant + palbociclib + taselisib

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

Overview

The combination of fulvestrant, palbociclib, and taselisib is an investigational triplet therapy for advanced breast cancer. Fulvestrant is a selective estrogen receptor degrader (SERD) that blocks and degrades the estrogen receptor, thereby inhibiting hormone-driven tumor growth. Palbociclib is a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that prevents cell cycle progression from G1 to S phase, leading to cell cycle arrest in cancer cells. Taselisib is a selective phosphoinositide 3-kinase (PI3K) inhibitor targeting the PI3K pathway—specifically PIK3CA mutations—which are common in hormone receptor-positive breast cancers. This triplet regimen has shown promising efficacy and manageable safety in patients with heavily pretreated PIK3CA-mutant, estrogen receptor-positive (ER+), HER2-negative advanced breast cancer[1][5][7]. The combination aims to overcome resistance mechanisms by simultaneously targeting hormonal signaling, cell cycle regulation, and PI3K pathway activation.

02

Targets

CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)PIK3CA (Phosphoinositide 3-kinase alpha)ESR1 (ERα)

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