ArticleCancer chemotherapy and pharmacology2020
Phase 1 study of napabucasin, a cancer stemness inhibitor, in patients with advanced solid tumors.
Article in Cancer chemotherapy and pharmacology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers, 1 of them a synthesis that pooled it.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
23 citing papers in PubMed, 1 synthesis or guideline pooled it, 45 citations in OpenAlex.
- Worldwide research trends on bone metastases of lung cancer: a bibliometric analysis.Frontiers in oncology · 2024Pooled it
- Molecular pathways linking the gut microbiome to antitumor immunity.Trends in microbiology · 2026Review
- STAT3 signaling inhibitors for cancer treatment.Trends in pharmacological sciences · 2026Review
- Translational insights and clinical challenges of targeting cancer stem cells.Signal transduction and targeted therapy · 2026Review
- From Signaling Pathways to Combination Therapy: Bioactive Compounds against Cancer Stem Cells.Stem cell reviews and reports · 2026Review
- Bone Metastasis in Estrogen Receptor-Positive Breast Cancer: Molecular Insights and Therapeutic Advances.International journal of molecular sciences · 2026Review
- Identification of ITGA2 as a methylation-regulated oncogene through a CeRNA network in papillary thyroid carcinoma.Discover oncology · 2025Article
- 2-oxoglutarate:acceptor oxidoreductase-catalyzed redox cycling effectively targets coccoid forms of Helicobacter pylori.Nature communications · 2025Article
- STAT3 and the STAT3‑regulated inhibitor of apoptosis protein survivin as potential therapeutic targets in colorectal cancer (Review).Biomedical reports · 2024Review
- Unraveling the complexity of STAT3 in cancer: molecular understanding and drug discovery.Journal of experimental & clinical cancer research : CR · 2024Review
- Natural STAT3 Inhibitors for Cancer Treatment: A Comprehensive Literature Review.Recent patents on anti-cancer drug discovery · 2024Review
- Molecularly Stratified Treatment Options in Primary Refractory DLBCL/HGBL with MYC and BCL2 or BCL6 Rearrangements (HGBL, NOS with MYC/BCL6).Targeted oncology · 2023Article
- The Anticancer Effect of Napabucasin (BBI608), a Natural Naphthoquinone.Molecules (Basel, Switzerland) · 2023Review
- Article
- Genomic features and its potential implication in bone oligometastatic NSCLC.BMC pulmonary medicine · 2023Article
- Proteomic time course of breast cancer cells highlights enhanced sensitivity to Stat3 and Src inhibitors prior to endocrine resistance development.Cancer gene therapy · 2023Article
- Primary refractory plasmablastic lymphoma: A precision oncology approach.Frontiers in oncology · 2023Article
- IL-20RB mediates tumoral response to osteoclastic niches and promotes bone metastasis of lung cancer.The Journal of clinical investigation · 2022Article
- The emerging era of personalized medicine in advanced colorectal cancer.Journal of gastroenterology and hepatology · 2022Review
- Article
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeNapabucasin is a cancer stemness inhibitor that targets a number of oncogenic pathways, including signal transducer and activator of transcription 3 (STAT3). Phase 1/2 studies suggest tolerability and anti-tumor activity in various types of cancer; a Phase 3 study of napabucasin plus standard therapy in colorectal cancer is ongoing. This is a Phase 1 dose-escalation study in patients with advanced solid tumors, and the first study of napabucasin in Japanese patients.
methodsPatients received napabucasin 480, 960, or 1440 mg daily in 28-day cycles until disease progression or intolerable toxicity. Primary objectives were to determine dose-limiting toxicities (DLTs), maximum tolerated dose (MTD), and the pharmacokinetic (PK) profile of napabucasin. Blood samples were taken for PK analysis on Days 1, 2, 8, and 15 of Cycle 1, and Days 29 and 30 of Cycle 2. Secondary objectives were to assess napabucasin antitumor activity, and the relationship between biomarkers and antitumor activity. JapicCTI-No: JapicCTI-132152.
resultsEnrolled were 14 patients (480 mg [n = 3], 960 mg [n = 4], 1440 mg [n = 7]). One patient experienced a DLT (Grade 3, anorexia). MTD was 1440 mg/day. Most common drug-related adverse events were diarrhea (n = 9), nausea (n = 4), vomiting (n = 3), and anorexia (n = 3). Napabucasin showed a similar PK profile to previous studies and no abnormal accumulation was observed. Following treatment, two patients had stable disease; the remaining 12 had progressive disease.
conclusionNapabucasin was well-tolerated at doses up to 1440 mg/day in Japanese patients with advanced solid tumors; the PK profile was comparable to that reported previously.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.