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fulvestrant + molibresib
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Intramuscular, Oral
01
Overview
Fulvestrant + molibresib is an investigational combination therapy evaluated for the treatment of hormone receptor-positive, human epidermal growth factor receptor 2-negative (HR+/HER2-) advanced or metastatic breast cancer. Fulvestrant is a selective estrogen receptor degrader that binds to and accelerates degradation of the estrogen receptor, blocking estrogen signaling in breast cancer cells. Molibresib is a small molecule inhibitor of the bromodomain and extra-terminal domain (BET) family proteins, including BRD2, BRD3, BRD4, and BRDT; it disrupts chromatin remodeling and gene expression by interfering with recognition of acetylated histones. The rationale for this combination was to overcome endocrine resistance in HR+/HER2− metastatic breast cancer by targeting both hormonal signaling and epigenetic regulation. In phase I/II clinical studies, this combination did not demonstrate clinically meaningful activity but provided important safety data[1][2][5].
- Brand names
- Faslodex (for fulvestrant)
- Other names
- I-bet Compound (for molibresib)I-bet762 (for molibresib)Molibresib Besylate (for molibresib)
02
Targets
BRD4 (Bromodomain-containing protein 4)BRD3 (Bromodomain-containing protein 3)BRD2 (Bromodomain-containing protein 2)ESR1 (ERα)BRDT (Bromodomain testis-specific protein)ESR2 (ERβ)
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