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21 Diseases |  |
1 Trial |
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1 Trial |  |
13 News |  |
- | lexibulin (CYT997) / Gilead
Journal: Identification and validation of microtubule depolymerizing agent, CYT997, as a potential drug candidate for hepatocellular carcinoma. (Pubmed Central) - Nov 29, 2023
CYT997 is a potentially efficacious and non-toxic drug candidate for HCC therapy. Its ability to down-regulate GPC3, ?-catenin, and c-Myc highlights a novel mechanism of action.
- | lexibulin (CYT997) / Gilead
Journal: Design, synthesis, and molecular docking study of novel cinnoline derivatives as potential inhibitors of tubulin polymerization. (Pubmed Central) - Aug 24, 2022
Subsequently, molecular docking was performed to shed light on the putative binding mode of the newly synthesized cinnolines. The docking results indicate that these derivatives are potential inhibitors of tubulin polymerization and the best interaction was achieved with a computational ki = 0.5 nM and posed correctly over the lexibulin.
- lexibulin (CYT997) / Gilead
Microtubule Polymerization Inhibition Enhances Human Hematopoietic Stem Cell Homing and Engraftment (GWCC - Hall B5, Level 1) - Nov 5, 2021 - Abstract #ASH2021ASH_5517;
Vinblastine Sulfate and Lexbulin were applied or registered as anti-cancer drugs for clinical use. Our study also indicates that MP inhibitors pretreatment of cells possesses significant translational implications, designating MP inhibitors as promising drug candidates to facilitate clinical HSCT.
- | lexibulin (CYT997) / Gilead
Journal: Mitochondrial ROS accumulation inhibiting JAK2/STAT3 pathway is a critical modulator of CYT997-induced autophagy and apoptosis in gastric cancer. (Pubmed Central) - Mar 6, 2021
CYT997 induces autophagy and apoptosis in gastric cancer by triggering mitochondrial ROS accumulation to silence JAK2/STAT3 pathway. CYT997 might be a potential antitumor drug candidate to treat GC.
- | lexibulin (CYT997) / Gilead, uridine triacetate (PN 401) / Wellstat
Journal: Predicting Drug Interactions with Human Equilibrative Nucleoside Transporters 1 and 2 Using Functional Knockout Cell Lines and Bayesian Modeling. (Pubmed Central) - Feb 20, 2021
Twenty-one compounds inhibited uridine uptake and abacavir, nevirapine, ticagrelor, and uridine triacetate had different IC values for ENT1 and ENT2...Clofarabine and cladribine were ENT1 and ENT2 substrates, whereas nevirapine and lexibulin were ENT1 and ENT2 nontransported inhibitors...Novel CRISPR/Cas9 functional knockouts of ENT1 and ENT2 in HeLa S3 cells were generated and characterized. Determining drug interactions with these transporters can be useful in identifying and predicting compounds that are ENT1 and ENT2 substrates, and can circumvent the blood-testis barrier through this transepithelial transport pathway in Sertoli cells.
- | vinorelbine tartrate / Generic mfg.
Biomarker, Journal: Identification of molecular signatures and pathways to identify novel therapeutic targets in Alzheimer's disease: Insights from a systems biomedicine perspective. (Pubmed Central) - Jan 6, 2021
In the present study, it was identified blood-cell derived molecular signatures that might be useful as candidate peripheral biomarkers in AD. It was also identified potential drugs and epigenetic data associated with these molecules that may be useful in designing therapeutic approaches to ameliorate AD.
- | lexibulin (CYT997) / Gilead
Journal: HBV Core Promoter Inhibition by Tubulin Polymerization Inhibitor (SRI-32007). (Pubmed Central) - Oct 30, 2020
Amongst the compounds tested, SRI-32007 (CYT997) demonstrated antiviral activity against HBV (genotype D) in HepG2.2.2.15 cell-based virus yield assay with 50% effective concentration (EC) and selectivity index (SI) of 60.1 nM and 7.2, respectively...Our experiments illustrate the utility of repurposing strategy to identify novel antiviral chemical leads. HBV core promoter inhibitors such as SRI-32007 might enable the development of novel therapeutic strategies to combat HBV infections.
- | lexibulin (CYT997) / Gilead
Journal: Intracellular reduction in ATP levels contributes to CYT997-induced suppression of metastasis of head and neck squamous carcinoma. (Pubmed Central) - Jun 20, 2020
These findings support a critical role of ATP levels in cell invasion and metastasis under the influence of CYT997. Collectively, our data unveil the mechanism involved in mediating CYT997 action, and provide preclinical rationale for possible clinical application of CYT997 as a novel therapeutic strategy against aggressive HNSCC.
- | lexibulin (CYT997) / Gilead
Journal: Autophagy blockade sensitizes human head and neck squamous cell carcinoma towards CYT997 through enhancing excessively high reactive oxygen species-induced apoptosis. (Pubmed Central) - Oct 31, 2019
• Blockade of autophagy augments CYT997 efficacy by enhanced ROS-associated apoptosis. • Combination of autophagy inhibitors with CYT997 is more effective against HNSCC.
- | CYT997 / Gilead, Ocuvia (elamipretide) / Stealth BioTherapeutics
Journal: CYT997(Lexibulin) induces apoptosis and autophagy through the activation of mutually reinforced ER stress and ROS in osteosarcoma. (Pubmed Central) - May 14, 2019
• Combination of autophagy inhibitors with CYT997 is more effective against HNSCC. This study suggests that CYT997 induces apoptosis and autophagy in OS cells by triggering mutually enhanced ER stress and ROS and may thus be a promising agent against OS.
- lexibulin (CYT997) / Gilead
Enrollment change, Combination therapy: Efficacy Study of CYT997 in Combination With Carboplatin in Glioblastoma (clinicaltrials.gov) - Jan 27, 2013
P1/2, N=20, Terminated, Sponsor: Gilead Sciences
This study suggests that CYT997 induces apoptosis and autophagy in OS cells by triggering mutually enhanced ER stress and ROS and may thus be a promising agent against OS. N=35 --> 20