Drug intelligence / Profile preview

napabucasin + ipilimumab

Development stage
Unknown
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

STAT3 (Signal Transducer and Activator of Transcription 3)NQO1CYP1A2 (Cytochrome P450 1A2)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)CYP2B6 (Cytochrome P450 2B6)ABCG2 (Breast cancer resistance protein)CYP2C8 (Cytochrome P450 2C8)

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