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DRUG CLASS:

P-glycoprotein inhibitor

11d
Co-encapsulated fluorescent magnetic nanoparticles for potential applications in breast cancer therapy: Exploratory in vitro and in vivo studies. (PubMed, Int J Pharm)
This study describes, for the first time in literature, a suitable approach to develop co-encapsulated magnetic nanoparticles based on fluorescent biotinylated N-palmitoyl chitosan, hydrophobic magnetite, Docetaxel and Verapamil. No significant toxicity was observed for magnetic nanoparticles in the rats. Overall, these findings suggest that the developed magnetic nanoplatforms represents a promising candidate for breast cancer applications and merits further in vivo investigation needed to elucidate the action mechanism of encapsulated therapeutics and their pharmacologic activity.
Preclinical • Journal
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CXCL8 (Chemokine (C-X-C motif) ligand 8)
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docetaxel
14d
Towards identification of novel inhibitors of EGFR mutants through in-silico approach. (PubMed, Cancer Treat Res Commun)
Among the tested compounds, Tetrandrine, Dauricine, and Olmutinib exhibited robust binding affinities across both wild-type and mutant EGFR configurations, highlighting their potential as effective inhibitors. The integrated approach of combining molecular docking using CB-dock2, ADMET profiling, and Lipinski's rule of five provides a robust framework for preliminary drug candidate screening, potentially accelerating the development of more precise and effective EGFR-targeted therapies. The findings contribute to the growing body of research exploring alternative and more nuanced strategies for inhibiting EGFR-driven oncogenic mechanisms, highlighting the importance of computational methods in identifying novel molecular targets with improved specificity and reduced side effects.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR wild-type
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Olita (olmutinib) • CBT-1 (tetrandrine)
1m
New trial
1m
DRG Explant Model for Understanding Mechanism of Oxaliplatin-Induced Peripheral Neuropathy and Identifying Potential Therapeutic Targets. (PubMed, Antioxidants (Basel))
Oxaliplatin-triggered chemotherapy-induced peripheral neuropathy (CIPN) is a common and debilitating side effect of cancer treatment that limits the efficacy of chemotherapy and negatively impacts patients' quality of life dramatically. Notably, inhibition of TXNIP with verapamil reduced oxidative stress levels. Our results demonstrated the use of DRG explants as an efficient model to study the mechanisms of CIPN and screen for potential treatments.
Journal
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TXNIP (Thioredoxin Interacting Protein)
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oxaliplatin
2ms
Potency-enhancing mutations in E3-19K and i-leader increase the cytolytic activity of the PH20/SPAM1-armed oncolytic adenovirus Ad5Δ24RGD. (PubMed, Mol Ther Oncol)
In some cell lines, the fiber modification F5RGD10(2C) or verapamil treatment further improves actual spread efficiency. Nelfinavir inhibits spread and plaque formation of oncolytic adenoviruses with the 19KSS-iLQ125Ter modifications, irrespective of adenovirus death protein (ADP) expression...We identified an insertion site downstream of the L3-23K region that supports relatively high hPH20 activity while preserving the enhanced oncolytic potency of the virus. Combining 19KSS-iLQ125Ter with hPH20 expression may potentially improve therapeutic benefit in glioma.
Journal
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SPAM1 (Sperm Adhesion Molecule 1)
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Viracept (nelfinavir)
2ms
A clinical trial of Tetrandrine Tablets in combination with Mitotane for the treatment of mitotane-resistant advanced adrenocortical carcinom (ChiCTR2500113189)
P=N/A, N=62, Not yet recruiting, West China Hospital of Sichuan University; West China Hospital of Sichuan University
New trial
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Lysodren (mitotane) • CBT-1 (tetrandrine)
2ms
New P4 trial
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CBT-1 (tetrandrine)
2ms
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, Recruiting, The First Affiliated Hospital of Army Medical University (Southwest Hospital); The First Affiliated Hospital of Army Medical University (Southwest Hos | Not yet recruiting --> Recruiting | Initiation date: Aug 2025 --> Nov 2025
Enrollment open • Trial initiation date
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Rituxan (rituximab) • cyclophosphamide • prednisone • hydroxychloroquine • tofacitinib • CBT-1 (tetrandrine)
2ms
Utilization of a UPLC-MS/MS Approach to Elucidate the Role of ABCB1-Mediated Paclitaxel Resistance in Non-Small Cell Lung Cancer Cells. (PubMed, Oncol Res)
Genetic silencing of ABCB1 or pharmacological inhibition with the specific P-glycoprotein modulator elacridar or tariquidar restored intracellular paclitaxel levels, as determined by UPLC-MS/MS, and synergistically decreased cell viability as observed in CCK-8 assay. These findings reveal that the ABCB1-mediated drug efflux is a crucial mechanism underlying paclitaxel resistance in NSCLC cells, with UPLC-MS/MS serving as a sensitive analytical method to detect paclitaxel concentration. Inhibition of ABCB1 is a promising therapeutic strategy to resensitize resistant tumor cells to paclitaxel.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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paclitaxel • elacridar (GF120918)
3ms
Dual Potential of Tetrandrine: Antiangiogenic Efficacy and Safety Liabilities Revealed through In Silico, In Vitro, and Zebrafish Models. (PubMed, Food Chem Toxicol)
These findings highlight tetrandrine's dual profile: a promising natural antiangiogenic agent with demonstrable efficacy, yet with significant cardiotoxic and developmental liabilities. This study provides crucial mechanistic insight into both its therapeutic and toxicological actions, establishing a translational foundation for its further development.
Preclinical • Journal
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EGFR (Epidermal growth factor receptor) • SRPK1 (SRSF Protein Kinase 1)
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CBT-1 (tetrandrine)