Drug intelligence / Profile preview

napabucasin

Development stage
Phase 3
Lead developer
Sumitomo Pharma America
Modality
Small Molecules
Administration
Oral
01

Overview

Napabucasin is an orally administered small molecule cancer stemness inhibitor with potential antineoplastic activity. It primarily targets and inhibits the signal transducer and activator of transcription 3 (STAT3) pathway, which is overactivated in many cancers and plays a key role in cancer stem cell-mediated tumor propagation. By inhibiting STAT3 and other pathways involved in cancer cell "stemness," napabucasin aims to suppress the growth of both cancer stem cells (CSCs) and heterogeneous tumor cells. This mechanism may help overcome resistance to conventional chemotherapies. Napabucasin has been investigated as monotherapy and in combination with standard chemotherapy agents for various solid tumors including colorectal carcinoma, pancreatic adenocarcinoma, gastric cancer, liver cancer, glioblastoma, malignant melanoma, non-small cell lung cancer (NSCLC), gastrointestinal cancers, and other solid tumors[1][3][4].

Other names
napabucasin2-acetylfuro-1,4-naphthoquinone2-acetylnaphtho[2,3-b]furan-4,9-dione2-acetylbenzo[f][1]benzofuran-4,9-dioneNapabucasinaNapabucasine
02

Targets

SLC47A1 (Multidrug and toxin extrusion transporter 1)ABCG2 (Breast cancer resistance protein)OAT1 (Organic anion transporter 1)CYP1A2 (Cytochrome P450 1A2)STAT3 (Signal Transducer and Activator of Transcription 3)NQO1SLC22A8 (Organic anion transporter 3)CTNNB1 (Beta-catenin)OCT2 (Organic cation transporter 2)CYP2B6 (Cytochrome P450 2B6)CYP2C8 (Cytochrome P450 2C8)

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