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Drug intelligence / Profile preview
napabucasin + ipilimumab
- Development stage
- Phase 1
- Lead developer
- Sumitomo Pharma America
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
napabucasin + ipilimumab is an investigational combination of a small molecule cancer stemness inhibitor (napabucasin, also known as BBI608) and a monoclonal antibody immune checkpoint inhibitor (ipilimumab). Napabucasin targets and inhibits STAT3-driven gene transcription involved in maintaining cancer stem cells, thereby potentially reducing tumor self-renewal and resistance. Ipilimumab is a fully human monoclonal antibody against CTLA-4, enhancing T-cell-mediated antitumor immunity by blocking the checkpoint protein CTLA-4 and fostering T-cell activation. The rationale for combining these drugs is to jointly suppress tumor stemness (via STAT3 inhibition) and augment cytotoxic immune responses against cancer cells. The combination is under clinical investigation for advanced and refractory solid tumors, especially melanoma and other advanced cancers.
- Other names
- BBI608 + ipilimumab
02
Targets
CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)CYP2C8 (Cytochrome P450 2C8)NQO1STAT3 (Signal Transducer and Activator of Transcription 3)
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