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fulvestrant + risovalisib
- Development stage
- Unknown
- Lead developer
- Haihe
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
The combination of fulvestrant and risovalisib is being investigated for the treatment of PIK3CA-mutated, hormone receptor-positive (HR+), HER2-negative advanced breast cancer. Fulvestrant is a selective estrogen receptor downregulator (SERD) that works by degrading estrogen receptor alpha, with activity in tamoxifen-resistant breast cancer models. Risovalisib (also known as CYH33) is a novel PI3Kα inhibitor that has shown superior inhibitory activity compared to alpelisib in multiple cancer cell lines and tumor xenograft models. This combination represents a targeted approach for patients with PIK3CA mutations, which are a common mechanism of resistance to endocrine therapy with or without CDK4/6 inhibitors in HR+/HER2- advanced breast cancer.
- Other names
- risovalisib mesylate + fulvestrant
02
Targets
PIK3CA (Phosphoinositide 3-kinase alpha)ESR1 (ERα)
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