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DRUG CLASS:

P-glycoprotein inhibitor

4d
New trial
8d
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
15d
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)
1m
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)
1m
New P4 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, 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)
1m
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)
1m
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)
2ms
New P4 trial
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CBT-1 (tetrandrine)
2ms
Elacridar Reverses P-gp-Mediated Drug Resistance in Ovarian Cancer Cells in 2D and 3D Culture Models. (PubMed, Int J Mol Sci)
In this study, we evaluated the ability of elacridar, a dual P-gp and BCRP inhibitor, to overcome MDR in W1, an ovarian cancer cell line sensitive to Paclitaxel (PAC) and its PAC-resistant variants. These findings highlight elacridar as a promising compound for reversing MDR in ovarian cancer and emphasize the importance of 3D models in preclinical drug evaluation. Further studies in advanced in vitro and in vivo models are required to assess the potential of elacridar better.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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paclitaxel • elacridar (GF120918)
3ms
Aminated Quinolinequinones With EDG(s) as a Prostate Cancer Inhibitor: Mechanistic Insights and Pharmacokinetic Limitations. (PubMed, Chem Biodivers)
In metabolic stability assays using human liver microsomes, AQQ6 exhibited relatively low intrinsic clearance (Clint) and an improved half-life (T1/2) compared to verapamil. However, pharmacokinetic studies in rats indicated poor oral bioavailability (%F = 4.2), likely due to extensive hepatic metabolism in rat liver microsomes. Molecular dynamics simulations targeting MAPK8, the protein likely involved in AQQ6 activity, were conducted to elucidate molecular-level binding interactions.
PK/PD data • Journal
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MAPK8 (Mitogen-activated protein kinase 8)
3ms
Atrioventricular Block and Cluster Headache (SEVA) (clinicaltrials.gov)
P4, N=60, Active, not recruiting, Centre Hospitalier Universitaire de Nice | Recruiting --> Active, not recruiting | Trial completion date: Mar 2025 --> Sep 2027 | Trial primary completion date: Mar 2025 --> Sep 2025
Enrollment closed • Trial completion date • Trial primary completion date