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abemaciclib + fulvestrant + pyrotinib
- Development stage
- Unknown
- Lead developer
- Sichuan Cancer Hospital
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
This triplet combination therapy is being investigated for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-positive (HER2+) metastatic breast cancer. It consists of abemaciclib, a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6); fulvestrant, a selective estrogen receptor degrader (SERD); and pyrotinib, an irreversible pan-HER tyrosine kinase inhibitor targeting EGFR, HER2, and HER4. The combination aims to provide a comprehensive blockade of the cross-talking signaling pathways—HER2, ER, and the cell cycle—that drive tumor progression and contribute to therapeutic resistance in this specific breast cancer subtype. Clinical evaluation is being led by institutions such as Sichuan Cancer Hospital, exploring the efficacy and safety of this regimen in patients who have progressed on prior therapies.
- Brand names
- Verzenio + Faslodex + AiRuiNi
- Other names
- Pyrotinib plus Abemaciclib and Fulvestrant
02
Targets
DYRK1B (Dual specificity tyrosine-phosphorylation-regulated kinase 1B)ERBB2 (Erb-b2 receptor tyrosine kinase 2)CDK9 (Cyclin-dependent kinase 9)HIPK3CDK6 (Cyclin-dependent kinase 6)HIPK2 (Homeodomain-interacting protein kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)CDK4 (Cyclin-dependent kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)ESR1 (ERα)
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