Drug intelligence / Profile preview

palbociclib + ribociclib + fulvestrant

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

Overview

Palbociclib, ribociclib, and fulvestrant are used in combination as a treatment regimen for hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer. Palbociclib and ribociclib are both selective inhibitors of cyclin-dependent kinases 4 and 6 (CDK4/6), which block cell cycle progression from G1 to S phase by preventing phosphorylation of the retinoblastoma protein. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds to estrogen receptors and accelerates their degradation, thereby inhibiting estrogen signaling in breast cancer cells. This combination targets both cell proliferation pathways and hormone-driven tumor growth[1][2][5][6].

Other names
none
02

Targets

ESR1 (ERα)CDK6 (Cyclin-dependent kinase 6)TAR (HIV-1 TAR RNA)ESR2 (ERβ)CDK4 (Cyclin-dependent kinase 4)CDK2 (Cyclin-dependent kinase 2)

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