Drug intelligence / Profile preview

bireociclib + fulvestrant

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

Overview

**Bireociclib (XZP-3287) is an oral small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), developed by Xuanzhu Biopharmaceutical. It selectively inhibits CDK4 and CDK6, blocking phosphorylation of the retinoblastoma protein (Rb) in early G1 phase, thereby preventing cell cycle progression from G1 to S phase and inducing cell cycle arrest[1][2][3]. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds to estrogen receptors and accelerates their degradation, leading to inhibition of estrogen signaling. The combination of bireociclib with fulvestrant is being investigated for the treatment of hormone receptor-positive (HR+), HER2-negative advanced or metastatic breast cancer in patients who have progressed on prior endocrine therapy[2][3][4]. Clinical trials have shown that this combination demonstrates superior efficacy compared to fulvestrant alone in this patient population with a manageable safety profile[2][4].**

Brand names
Xuanyuening
Other names
XZP-3287 + fulvestrantbireociclib + fulvestrant
02

Targets

ESR2 (ERβ)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)ESR1 (ERα)

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