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fulvestrant + zotatifin
- Development stage
- Phase 2
- Lead developer
- Effector Therapeutics
- Modality
- Small Molecules
- Administration
- Intramuscular, Intravenous
01
Overview
Fulvestrant + zotatifin is a combination therapy being investigated for the treatment of estrogen receptor-positive (ER+)/human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Zotatifin is a potent and sequence-selective small molecule inhibitor of the RNA helicase eIF4A that works by suppressing expression of a network of cancer-driving proteins, including cyclins D and E, CDKs 2, 4, and 6, and select RTKs as well as KRAS. Fulvestrant is an established selective estrogen receptor degrader (SERD). The combination has shown ability to lower ER expression and suppress tumor growth in patients with ER+ breast cancer, particularly in those who have developed resistance to prior therapies.
- Other names
- ZF doublet
02
Targets
ESR1 (ERα)EIF4A2 (Eukaryotic translation initiation factor 4A2)
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