Drug intelligence / Profile preview

capecitabine + napabucasin

Development stage
Phase 2
Lead developer
Sumitomo Pharma America
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Capecitabine + napabucasin is an investigational combination therapy for cancer. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU), a nucleoside metabolic inhibitor that interferes with DNA synthesis and inhibits tumor cell proliferation. Napabucasin (also known as BBI-608) is an orally administered small molecule hypothesized to inhibit multiple oncogenic pathways by targeting cancer stemness pathways, including the STAT3 pathway. Napabucasin increases reactive oxygen species (ROS) in cancer cells beyond cytotoxic thresholds, leading to cell death. This combination has been explored in clinical trials for advanced or metastatic gastrointestinal cancers such as pancreatic and colorectal cancers[1][4][8][9].

02

Targets

STAT3 (Signal Transducer and Activator of Transcription 3)TS (Thymidylate synthase)

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