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DRUG:

CBT-1 (tetrandrine)

i
Other names: NSC-77037
Associations
Trials
Company:
CBA Pharma
Drug class:
P-glycoprotein inhibitor, Ca2+ channel antagonist, MDR modulator
Associations
Trials
8d
Effective components of Coptidis Rhizoma and Cinnamomi Cortex in the treatment of renal cell carcinoma and their mechanism of action. (PubMed, Medicine (Baltimore))
Three components (quercetin, oleic acid, tetrandrine) were highlighted as particularly effective...In conclusion, the therapeutic effect of the HL-RG combination against RCC is primarily mediated by its bioactive components, QUE, OA, and TET. These components regulate the HIF-1 signaling pathway, activating genes involved in the cellular response to hypoxia and modulating the expression of proteins that control glucose metabolism, cell proliferation, and angiogenesis.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • CCND1 (Cyclin D1) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • EGF (Epidermal growth factor) • TGFB1 (Transforming Growth Factor Beta 1) • MMP9 (Matrix metallopeptidase 9) • CAT (Catalase)
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CBT-1 (tetrandrine)
20d
Exploring the mechanism of Stephania tetrandra S. Moore in the treatment of cisplatin resistance against ovarian cancer through integration of network pharmacology and molecular docking. (PubMed, Medicine (Baltimore))
Cisplatin resistance is a major contributor to treatment failure in ovarian cancer (OC). Molecular dynamics simulations demonstrated that hesperidin, cissamine and tetrandrine exhibited strong binding affinities toward AURKA, vitamin D receptor, and TTK. Future studies are encouraged to focus on the experimental validation of these compounds and delve deeper into the possible mechanisms of drug resistance, aiming to improve their therapeutic effectiveness and real-world applicability.
Journal
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BCL2 (B-cell CLL/lymphoma 2) • AURKA (Aurora kinase A) • DNMT1 (DNA methyltransferase 1) • CDK1 (Cyclin-dependent kinase 1) • SMAD7 (SMAD Family Member 7) • TTK (TTK Protein Kinase)
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cisplatin • CBT-1 (tetrandrine)
1m
Study on the clinical efficacy and mechanism of tetrandrine in the treatment of patients with lumbar disc herniation (ChiCTR2500108829)
P=N/A, N=64, Not yet recruiting, Affiliated hangzhou first people's hospital, zhejiang university school of medicine; Hangzhou First People's Hospital
New trial
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CBT-1 (tetrandrine)
1m
A single-center exploratory study on the efficacy and safety of tetrandrine tablets in the treatment of interstitial lung disease associated with rheumatoid arthritis (ChiCTR2500107574)
P=N/A, N=60, Not yet recruiting, The First Affiliated Hospital of Army Medical University (Southwest Hospital); The First Affiliated Hospital of Army Medical University (Southwest Hos
New trial
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Rituxan (rituximab) • cyclophosphamide • prednisone • tofacitinib • CBT-1 (tetrandrine)
2ms
Lactoferrin functionalized bovine serum albumin nanoparticles for synergistic chemo-gene therapy of lung cancer: Co-delivery of tetrandrine and miRNA-126. (PubMed, Int J Biol Macromol)
Histopathological findings further verify the superiority of Lf-miRNA-126-Tet@ANPs. These results highlight Lf-miRNA-126-Tet@ANPs as a promising nanoplatform for chemo-gene targeted delivery against lung cancer.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • STAT3 (Signal Transducer And Activator Of Transcription 3)
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CBT-1 (tetrandrine)
2ms
Investigating C7 modified tetrandrine derivatives for synthesis anti-hepatocellular carcinoma activity and mechanistic insights. (PubMed, Sci Rep)
Notably, compound 15 demonstrated significant antiproliferative activity against all tested cell lines, with IC50 values ranging from 3.28 to 6.16 µM, which is superior to the first-line clinical drug 5-fluorouracil. With its remarkable antitumor activity, excellent synthetic process characteristics, and clear apoptosis-inducing mechanism, compound 15 has emerged as a highly promising clinical candidate. This C-7 modification platform provides a viable path for transforming natural product derivatives into clinical therapies for HCC treatment.
Journal
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BCL2 (B-cell CLL/lymphoma 2) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • FLT1 (Fms-related tyrosine kinase 1) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3)
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5-fluorouracil • CBT-1 (tetrandrine)
3ms
Precision targeted cancer-associated fibroblast nano-regulator enhanced chemo-immunotherapy for triple-negative breast cancer. (PubMed, Biomaterials)
Here, we designed a nanoparticle co-modified with anisamide and CAF cell membrane (CAFm) to load tetrandrine as a CAF nano-regulator (TET@ACNP), which is able to precisely target and modulate CAFs...TET@ACNP was able to inhibit CAFs activation and reduce collagen secretion, thereby breaking the physical barrier to facilitate the penetration of the first-line chemotherapeutic agent docetaxel (DTX) and the infiltration of cytotoxic T lymphocytes...Our study proposes a comprehensive therapeutic strategy based on the precise targeting and regulation of CAFs in combination with chemotherapy to achieve multifaceted inhibition of TNBC. This is expected to be a universal platform to improve the therapeutic efficacy of different chemotherapeutic agents in various types of stroma-rich tumors.
Journal • IO biomarker
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IGF2 (Insulin-like growth factor 2)
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docetaxel • CBT-1 (tetrandrine)
5ms
Combination therapy in cancer: The potential of tetrandrine as a polytherapy for acute myeloid leukemia. (PubMed, Biochim Biophys Acta Rev Cancer)
This review aims to explore the potential mechanisms of tetrandrine treatment in AML, drawing on information gained through tetrandrine treatment in solid cancer. The main focus will be interactions with genes, protein, and pathways commonly dysregulated in AML, namely Tumour Protein 53 (TP53), C-Myc (MYC), Kirsten Rate Sarcoma Virus (KRAS), Vascular Endothelial Growth Factor (VEGF), Fms-like tyrosine kinase 3 (FLT3) and Nuclear Receptor Subfamily 4A1 (NR4A1) as well as the NOD-, LRR- and pyrin domain-containing protein 3 (NLRP3)-inflammasome and calcium-calmodulin (CaM)-dependent protein kinase II (CaMKII).
Review • Journal
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KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • FLT3 (Fms-related tyrosine kinase 3) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • NLRP3 (NLR Family Pyrin Domain Containing 3) • NR4A1 (Nuclear Receptor Subfamily 4 Group A Member 1)
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CBT-1 (tetrandrine)
7ms
Multifunctional Mesoporous Titanium Dioxide Nanodrug for Corneal Haze Treatment and Its Mechanism. (PubMed, Biomater Res)
In this study, we discovered that Tet@TiO2 and tetrandrine (Tet), but not TiO2, displayed a characteristic absorption peak at 282 nm...Compared with those in the control and TiO2 groups, the α-smooth muscle actin, connective tissue growth factor, and type III collagen fibers in the Tet@TiO2 group decreased more significantly after fluorometholone eye drop and Tet treatment, indicating that Tet@TiO2 can effectively inhibit the expression of these inflammatory factors during corneal haze formation. Moreover, Tet@TiO2 showed good, sustained antibacterial properties. More importantly, we found that Tet@TiO2 could effectively down-regulate the expression of phosphatidylinositol 3-kinase (PI3K), protein kinase B (AKT), and B-cell lymphoma-2 (Bcl-2) and up-regulate the expression of Bcl-2-associated X protein (Bax) by modulating the inflammatory PI3K-AKT-Bax/Bcl-2 signaling pathway after corneal surface refractive surgery to effectively prevent and treat corneal haze by reducing the expression of inflammatory factors.
Journal • IO biomarker
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BAX (BCL2-associated X protein) • CTGF (Connective tissue growth factor)
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CBT-1 (tetrandrine)
7ms
Phytochemical intervention in BCRP-driven cancer drug resistance: A comprehensive review. (PubMed, Biochim Biophys Acta Rev Cancer)
Compounds such as tetrandrine and resveratrol have shown promise in sensitizing drug-resistant cancer cells. Understanding the complex interplay between BCRP regulation and these signaling pathways is essential for the development of effective therapeutic strategies to counteract cancer. Targeting multiple pathways or employing combination therapies may offer new avenues to overcome MDR and improve treatment outcomes for cancer patients.
Review • Journal
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CTNNB1 (Catenin (cadherin-associated protein), beta 1)
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CBT-1 (tetrandrine)
7ms
Plant Alkaloids as Promising Anticancer Compounds with Blood-Brain Barrier Penetration in the Treatment of Glioblastoma: In Vitro and In Vivo Models. (PubMed, Molecules)
The toxic and adverse effect analysis suggests that alkaloids such as noscapine, lycorine, capsaicin, chelerythrine, caffeine, boldine, and colchicine show favorable therapeutic potential. However, tetrandrine, nitidine, harmine, harmaline, cyclopamine, cocaine, and brucine may pose greater risks than benefits...Overall, while plant alkaloids show promise in glioblastoma therapy, progress in assessing their BBB penetration remains limited. More comprehensive studies integrating glioma research and advanced drug delivery technologies are needed.
Preclinical • Review • Journal
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BCL2 (B-cell CLL/lymphoma 2)
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cyclopamine • CBT-1 (tetrandrine)
8ms
Tetrandrine and adriamycin reverse multidrug resistance by regulating NLRP3/Caspase-1/GSDMD signaling in human breast cancer cells. (PubMed, Eur J Pharmacol)
The combined use of TET and ADR not only suppresses MCF-7/ADR cell growth but also reverses MDR by targeting the NLRP3/Caspase-1/GSDMD pyroptosis pathway. These findings propose a promising therapeutic strategy for combatting MDR in breast cancer and highlight the potential for further clinical application of this combination therapy.
Journal
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NLRP3 (NLR Family Pyrin Domain Containing 3) • GSDMD (Gasdermin D)
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LDH elevation
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doxorubicin hydrochloride • CBT-1 (tetrandrine)