Drug intelligence / Profile preview

bazedoxifene + palbociclib

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

Overview

Bazedoxifene + palbociclib is an investigational combination therapy for hormone receptor-positive, HER2-negative (HR+/HER2-) advanced breast cancer. Bazedoxifene is a third-generation selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD), while palbociclib is a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. This combination targets both the estrogen signaling pathway and cell cycle progression, aiming to overcome endocrine resistance in breast cancer. Clinical studies have shown that this regimen has clinical efficacy and an acceptable safety profile in heavily pretreated patients with advanced HR+/HER2- breast cancer[1][6]. The primary mechanism involves inhibition of the estrogen receptor by bazedoxifene and blockade of CDK4/6-mediated cell cycle progression by palbociclib.

02

Targets

ESR1 (ERα)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)

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