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alobresib + exemestane
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Alobresib + exemestane is an **experimental combination therapy** for advanced breast cancer, specifically evaluated in hormone receptor-positive and/or estrogen receptor-positive settings. **Alobresib** (GSK2879552) is a small molecule inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A), an epigenetic modulator thought to play a role in cancer cell proliferation and resistance to endocrine therapy. **Exemestane** is a steroidal aromatase inhibitor that irreversibly blocks the conversion of androgens to estrogens, thereby reducing estrogen-driven proliferation in breast cancer. The combination targets **tumor progression involving both estrogen suppression (via exemestane) and epigenetic regulation (via alobresib)**. The combination is under investigation in early phase clinical trials for breast cancer that has progressed following prior endocrine therapy.
- Other names
- alobresib + exemestane
02
Targets
BRD4 (Bromodomain-containing protein 4)CYP19A1 (Aromatase)BRD3 (Bromodomain-containing protein 3)BRD2 (Bromodomain-containing protein 2)BRDT (Bromodomain testis-specific protein)AR (Adrenergic receptors)
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