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apatinib + fulvestrant
- Development stage
- Unknown
- Lead developer
- Hengrui Pharmaceutical
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
A combination therapy consisting of apatinib, a selective small molecule tyrosine kinase inhibitor (TKI) of vascular endothelial growth factor receptor-2 (VEGFR-2), and fulvestrant, a selective estrogen receptor degrader (SERD). This regimen is primarily investigated for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Apatinib inhibits tumor angiogenesis by blocking VEGFR-2 signaling, while fulvestrant binds to and promotes the degradation of the estrogen receptor, thereby inhibiting estrogen-mediated tumor growth. The combination is designed to overcome endocrine resistance by simultaneously targeting angiogenic and hormonal pathways. Clinical development of this combination has been notably advanced through investigator-initiated trials at institutions such as Sun Yat-Sen Memorial Hospital.
- Brand names
- AiTan + Faslodex
- Other names
- rivoceranib + fulvestrantapatinib mesylate + fulvestrant
02
Targets
VEGFR2 (Vascular endothelial growth factor receptor 2)ER (Estrogen receptor)
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