Drug intelligence / Profile preview

napabucasin + paclitaxel

Development stage
Unknown
Lead developer
Sumitomo Pharma
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Napabucasin + paclitaxel is an investigational combination therapy consisting of napabucasin, a first-in-class small molecule cancer stemness inhibitor, and paclitaxel, a well-established microtubule-stabilizing chemotherapeutic agent. Napabucasin acts primarily by inhibiting STAT3-driven gene transcription and spherogenesis in cancer stem cells, thereby targeting tumor cell self-renewal and resistance mechanisms. Paclitaxel disrupts mitosis by stabilizing microtubules. The combination has been studied in multiple advanced solid tumors—including metastatic breast cancer, platinum-resistant ovarian cancer, melanoma, and gastric/gastroesophageal junction (GEJ) adenocarcinoma—based on preclinical evidence of synergistic antitumor activity. Clinical trials have shown the regimen to be generally well tolerated with some encouraging signs of efficacy; however, large phase III studies did not demonstrate significant survival benefit over standard therapies[2][5][6][7][8].

Other names
napabucasin + PTXnapabucasin plus paclitaxel
02

Targets

MicrotubuleSTAT3 (Signal Transducer and Activator of Transcription 3)

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