Drug intelligence / Profile preview

dalpiciclib + fulvestrant + letrozole + pyrotinib

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

Overview

This is a multi-drug combination regimen consisting of four agents used in the treatment of advanced or metastatic breast cancer, particularly in patients with hormone receptor-positive and/or HER2-positive disease. **Dalpiciclib** is an oral small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression from G1 to S phase, thereby inhibiting tumor cell proliferation[3][5]. **Fulvestrant** is a selective estrogen receptor degrader (SERD) that binds to estrogen receptors and accelerates their degradation, leading to downregulation of estrogen signaling. **Letrozole** is an aromatase inhibitor that suppresses estrogen synthesis by inhibiting the aromatase enzyme. **Pyrotinib** is an irreversible pan-ErbB tyrosine kinase inhibitor targeting HER1 (EGFR), HER2, and HER4 receptors; it blocks downstream signaling pathways involved in tumor growth[6][9][10]. This combination targets multiple oncogenic pathways—cell cycle regulation via CDK4/6 inhibition, hormonal signaling via ER antagonism/degradation and aromatase inhibition, and growth factor receptor signaling via pan-HER blockade—making it potentially effective against tumors with complex resistance mechanisms.

Brand names
Paudina
Other names
dalpiciclib + fulvestrant + letrozole + pyrotinib
02

Targets

CDK4 (Cyclin-dependent kinase 4)GPER1 (G protein-coupled estrogen receptor 1)ESR1 (ERα)CYP19A1 (Aromatase)CDK6 (Cyclin-dependent kinase 6)ESR2 (ERβ)

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