☆ 4.6 Review

The Anticancer Effect of Napabucasin (BBI608), a Natural Naphthoquinone

MOLECULES (2023)

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Summary: Melanoma, the deadliest form of skin cancers, has unsatisfying clinical outcomes despite recent efforts in immunotherapeutic strategies. Factors such as side-effects, immunosuppressive tumor microenvironment, and tumor heterogeneity hinder efficient cancer immunotherapy. Nanotechnology-based approaches have been developed to enhance efficacy and reduce toxicity. Recent studies have shown the revolutionary potential of nanomaterials in immunotherapy for melanoma. This review highlights the integration of nanotechnology and cancer immunotherapy in melanoma treatment, emphasizing the therapeutic advantages for patients.

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Summary: In this study, patients with colorectal cancer were divided into two groups, one receiving combination therapy of napabucasin and FOLFIRI, and the other receiving FOLFIRI alone. The results showed that the addition of napabucasin to FOLFIRI did not significantly improve overall survival compared to the control group.

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STAT3 inhibitor Napabucasin abrogates MDSC immunosuppressive capacity and prolongs survival of melanoma-bearing mice

Rebekka Bitsch et al.

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Targeting STAT3 Signaling Facilitates Responsiveness of Pancreatic Cancer Cells to Chemoradiotherapy

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Inhibition of STAT3 prevents bone metastatic progression of prostate cancer in vivo

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Summary: This study demonstrated the effectiveness of the STAT3 inhibitor Napabucasin in impairing metastatic potential of PC cells and preventing metastatic establishment in tibial bones in mice. Napabucasin treatment also significantly reduced tumor burden in established bone CRPC and altered gene expression in the bone marrow niche towards maintenance of hematopoietic stem cells and the myeloid lineage.

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Napabucasin Induces Mouse Bone Loss by Impairing Bone Formation via STAT3

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2-Methoxy-6-acetyl-7-methyljuglone (MAM) induced programmed necrosis in glioblastoma by targeting NAD(P)H: Quinone oxidoreductase 1 (NQO1)

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Napabucasin, a novel inhibitor of STAT3, inhibits growth and synergises with doxorubicin in diffuse large B-cell lymphoma

Xue Li et al.

CANCER LETTERS (2020)

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The synergistic anticancer effects of ReoT3D, CPT-11, and BBI608 on murine colorectal cancer cells

Abouzar Babaei et al.

DARU-JOURNAL OF PHARMACEUTICAL SCIENCES (2020)

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Article Biochemistry & Molecular Biology

To inhibit TrxR1 is to inactivate STAT3-Inhibition of TrxR1 enzymatic function by STAT3 small molecule inhibitors

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REDOX BIOLOGY (2020)

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Article Pharmacology & Pharmacy

Napabucasin Reduces Cancer Stem Cell Characteristics in Hepatocellular Carcinoma

Ya Li et al.

FRONTIERS IN PHARMACOLOGY (2020)

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Antibiotics for cancer treatment: A double-edged sword

Yuan Gao et al.

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The Cancer Stem Cell Inhibitor Napabucasin (BBI608) Shows General Cytotoxicity in Biliary Tract Cancer Cells and Reduces Cancer Stem Cell Characteristics

Marlena Beyreis et al.

CANCERS (2019)

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Napabucasin (BBI608) eliminate AML cells in vitro and in vivo via inhibition of Stat3 pathway and induction of DNA damage

Silei Bi et al.

EUROPEAN JOURNAL OF PHARMACOLOGY (2019)

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Napabucasin, a novel STAT3 inhibitor suppresses proliferation, invasion and stemness of glioblastoma cells

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Bioactivation of Napabucasin Triggers Reactive Oxygen Species-Mediated Cancer Cell Death

Fieke E. M. Froeling et al.

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Highlighted STAT3 as a potential drug target for cancer therapy

Haeri Lee et al.

BMB REPORTS (2019)

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BBI608 inhibits cancer sternness and reverses cisplatin resistance in NSCLC

Lauren MacDonagh et al.

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Inhibition of STAT3 blocks protein synthesis and tumor metastasis in osteosarcoma cells

Dongqing Zuo et al.

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The NQO1 bioactivatable drug, -lapachone, alters the redox state of NQO1+pancreatic cancer cells, causing perturbation in central carbon metabolism

Molly A. Silvers et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2017)

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Meeting Abstract Oncology

BBI608-201GBM: A phase Ib/II clinical study of napabucasin (BBI608) in combination with temozolomide (TMZ) for adult patients with recurrent glioblastoma (GBM).

Warren P. Mason et al.

JOURNAL OF CLINICAL ONCOLOGY (2017)

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Meeting Abstract Oncology

CanStem303C trial: A phase III study of napabucasin (BBI-608) in combination with 5-fluorouracil (5-FU), leucovorin, irinotecan (FOLFIRI) in adult patients with previously treated metastatic colorectal cancer (mCRC).

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JOURNAL OF CLINICAL ONCOLOGY (2017)

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Napabucasin: An Update on the First-in-Class Cancer Stemness Inhibitor

Joleen M. Hubbard et al.

DRUGS (2017)

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2-Methoxy-6-acetyl-7-methyljuglone (MAM), a natural naphthoquinone, induces NO-dependent apoptosis and necroptosis by H2O2-dependent JNK activation in cancer cells

Wen Sun et al.

FREE RADICAL BIOLOGY AND MEDICINE (2016)

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Meeting Abstract Oncology

A phase Ib study of cancer stem cell (CSC) pathway inhibitor BBI-608 in combination with gemcitabine and nab-paclitaxel (nab-PTX) in patients (pts) with metastatic pancreatic ductal adenocarcinoma (mPDAC).

Safi Shahda et al.

JOURNAL OF CLINICAL ONCOLOGY (2016)

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Cancer stem cell signaling pathways

William H. Matsui

MEDICINE (2016)

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Suppression of prostate cancer progression by cancer cell stemness inhibitor napabucasin

Yiming Zhang et al.

CANCER MEDICINE (2016)

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Suppression of cancer relapse and metastasis by inhibiting cancer stemness

Youzhi Li et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2015)

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Meeting Abstract Oncology

Phase Ib/II study of cancer stem cell (CSC) inhibitor BBI608 combined with paclitaxel in advanced gastric and gastroesophageal junction (GEJ) adenocarcinoma.

Carlos Becerra et al.

JOURNAL OF CLINICAL ONCOLOGY (2015)

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Angoline: A selective IL-6/STAT3 signaling pathway inhibitor isolated from Zanthoxylum nitidum

Jiawei Liu et al.

PHYTOMEDICINE (2014)

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Meeting Abstract Oncology

A phase 1b study of the cancer stem cell inhibitor BBI608 administered with paclitaxel in patients with advanced malignancies

Matthew Hitron et al.

JOURNAL OF CLINICAL ONCOLOGY (2014)

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Article Endocrinology & Metabolism

Osteoblast/osteocyte-specific inactivation of Stat3 decreases load-driven bone formation and accumulates reactive oxygen species

Hongkang Zhou et al.

BONE (2011)

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A Perspective on Cancer Cell Metastasis

Christine L. Chaffer et al.

SCIENCE (2011)

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Selective p38α Inhibitors Clinically Evaluated for the Treatment of Chronic Inflammatory Disorders

David M. Goldstein et al.

JOURNAL OF MEDICINAL CHEMISTRY (2010)

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Targeting NAD(P)H:quinone oxidoreductase (NQO1) in pancreatic cancer

AM Lewis et al.

MOLECULAR CARCINOGENESIS (2005)

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Recommended guidelines for the treatment of cancer treatment-induced diarrhea

AB Benson et al.

JOURNAL OF CLINICAL ONCOLOGY (2004)

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