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GDC-0152
- Development stage
- Discontinued
- Lead developer
- Genentech
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
GDC-0152 is a small molecule investigational drug developed as a second mitochondrial activator of caspases (Smac) mimetic and inhibitor of apoptosis proteins (IAPs) antagonist. It binds to the BIR3 domains of several IAP family members, including XIAP, cIAP1, cIAP2, and ML-IAP. By antagonizing these proteins, GDC-0152 promotes the degradation of cIAP1 and induces activation of caspase pathways leading to apoptosis in cancer cells. This mechanism results in decreased viability of various tumor cell types and has shown potential antineoplastic activity in preclinical models. The drug has been studied primarily for the treatment of solid tumors[1][2][3][4][5].
- Other names
- Smac mimetic GDC-0152DIABLO/SMAC mimetic
02
Targets
BIRC7BIRC2 (Cellular inhibitor of apoptosis protein 1)BIRC3 (Baculoviral IAP repeat-containing protein 3)XIAP
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