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neratinib + fulvestrant
- Development stage
- Unknown
- Lead developer
- Puma Biotechnology
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
Neratinib + fulvestrant is a combination regimen of two pharmaceutical drugs: neratinib, an oral, irreversible pan-HER tyrosine kinase inhibitor, and fulvestrant, an injectable estrogen receptor antagonist. This combination is being investigated for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2 (HER2)-mutated, metastatic breast cancer that is HER2 non-amplified. Neratinib targets and inhibits HER2, HER4, and EGFR kinases and is thought to overcome mechanisms of endocrine resistance mediated by HER2 mutations. Fulvestrant binds to estrogen receptors (ER), antagonizes their signaling, and accelerates their degradation, thereby blocking estrogen-driven tumor growth. The combination is intended to target both ER and HER2-driven pathways, potentially improving outcomes for patients with HER2-mutant HR+ breast cancer who have progressed on prior endocrine therapy.
- Brand names
- Nerlynx + Faslodex
- Other names
- neratinib and fulvestrantNerlynx and Faslodex
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)ESR1 (ERα)EGFR T790M (Epidermal growth factor receptor T790M mutant)ESR2 (ERβ)
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