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fulvestrant + palbociclib + rogaratinib
- Development stage
- Discontinued
- Lead developer
- Bayer
- Modality
- Small Molecules
- Administration
- Intramuscular, Oral
01
Overview
This is an investigational combination therapy consisting of fulvestrant, palbociclib, and rogaratinib. Fulvestrant is a selective estrogen receptor degrader that antagonizes and degrades the estrogen receptor, used in hormone receptor-positive breast cancer. Palbociclib is a small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression in cancer cells. Rogaratinib is an oral pan-fibroblast growth factor receptor (FGFR) inhibitor targeting FGFR1–4, developed to inhibit tumor growth driven by FGFR overexpression or amplification. The triple blockade aims to overcome resistance mechanisms in advanced hormone receptor-positive, HER2-negative breast cancer with FGFR1/2 amplification or overexpression—particularly after progression on prior CDK4/6 inhibitor plus aromatase inhibitor therapy. The combination has been studied in phase I clinical trials for safety and preliminary efficacy; while it showed feasibility regarding safety profile, efficacy was modest and development was discontinued[3][5][4].
- Brand names
- Ibrance (for palbociclib)Faslodex (for fulvestrant)
- Other names
- None
02
Targets
FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)CDK4 (Cyclin-dependent kinase 4)FGFR2 (Keratinocyte growth factor receptor)CDK6 (Cyclin-dependent kinase 6)FGFR1 (Fibroblast growth factor receptor 1)ESR1 (ERα)
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