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GS-5829 + fulvestrant
- Development stage
- Phase 1
- Lead developer
- Gilead Sciences
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
GS-5829 + fulvestrant is a combination therapy consisting of GS-5829 (also known as alobresib), an oral bromodomain and extraterminal (BET) inhibitor, and fulvestrant, a selective estrogen receptor degrader (SERD). This combination was investigated for the treatment of advanced estrogen receptor positive, HER2-negative (ER+/HER2-) breast cancer. GS-5829 works by inhibiting BET proteins, which are functionally linked to pathways important in cellular viability and cancer development. BET inhibition selectively suppresses key oncogenic drivers and may be an attractive therapeutic target for ER+ breast cancer. Fulvestrant acts by binding to and degrading estrogen receptors, thereby blocking estrogen signaling in breast cancer cells.
02
Targets
BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)BRD4 (Bromodomain-containing protein 4)ESR1 (ERα)
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