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DRUG:

vatalanib (PTK787)

i
Other names: PTK787, ZK222584, PTK/ZK, CGP 79787
Associations
Trials
Company:
Bayer, Novartis
Drug class:
c-KIT inhibitor, VEGFR inhibitor, PDGFR β inhibitor
Related drugs:
Associations
Trials
3d
Discovery of key molecular signatures for diagnosis and therapies of glioblastoma by combining supervised and unsupervised learning approaches. (PubMed, Sci Rep)
Finally, we recommended KGs-guided four repurposable drug molecules (Fluoxetine, Vatalanib, TGX221 and RO3306) against GBM through molecular docking, drug likeness, ADMET analyses and molecular dynamics simulation studies. Thus, the discoveries of this study could serve as valuable resources for wet-lab experiments in order to take a proper treatment plan against GBM.
Journal
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TOP2A (DNA topoisomerase 2-alpha) • RAD51 (RAD51 Homolog A) • AURKA (Aurora kinase A) • CHEK1 (Checkpoint kinase 1) • RAD51AP1 (RAD51 Associated Protein 1) • CCNB2 (Cyclin B2) • CDK1 (Cyclin-dependent kinase 1) • MCM10 (Minichromosome Maintenance 10 Replication Initiation Factor) • CDCA8 (Cell Division Cycle Associated 8)
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TGX-221 • fluoxetine • vatalanib (PTK787)
1year
Inhibition of VEGFR2 and EGFR signaling cooperatively suppresses the proliferation of oral squamous cell carcinoma. (PubMed, Cancer Med)
VEGFR-mediated signaling would be an alternative signaling pathway for the survival of OSCC cells under the disruption of EGFR signaling. These results highlight the clinical application of VEGFR inhibitors in the development of multi-molecular-targeted therapeutics against OSCC.
Journal
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KDR (Kinase insert domain receptor)
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erlotinib • vatalanib (PTK787)
1year
Machine learning model for anti-cancer drug combinations: Analysis, prediction, and validation. (PubMed, Pharmacol Res)
Our prediction and validation results indicated that the combination of the RTK inhibitors Lapatinib and Pazopanib exhibited a strong therapeutic effect in breast cancer by blocking the downstream PI3K/AKT/mTOR signaling pathway. Furthermore, we incorporated molecular features to identify potential biomarkers for synergistic drug pairs, and almost all potential biomarkers found connections between drug targets and corresponding molecular features using protein-protein interaction network. Overall, this study provides valuable insights to complement and guide rational efforts to develop drug combination treatments.
Journal • Machine learning
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docetaxel • lapatinib • tamoxifen • bortezomib • pazopanib • vincristine • vatalanib (PTK787)
2years
Combinatorial delivery of CPI444 and vatalanib loaded on PEGylated graphene oxide as an effective nanoformulation to target glioblastoma multiforme: In vitro evaluation. (PubMed, Front Oncol)
Ultimately, GBM U87 cells assumed programmed cell death at a very low concentration due to nanocarrier-mediated drug delivery along with the chosen combination of drugs. Together, this study demonstrated the advantage of GO-PEG mediated combined delivery of CPI444 and vatalanib drugs with increased permeability, a three-pronged combinatorial strategy toward effective GBM treatment.
Preclinical • Journal
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KIT (KIT proto-oncogene, receptor tyrosine kinase) • CD24 (CD24 Molecule) • POU5F1 (POU Class 5 Homeobox 1) • NANOG (Nanog Homeobox)
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CD24 expression
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ciforadenant (CPI-444) • vatalanib (PTK787)
over2years
Overexpressed or hyperactivated Rac1 as a target to treat hepatocellular carcinoma. (PubMed, Pharmacol Res)
Our analysis underlines the prominent oncogenic functions of Rac1 in HCC and discuss the modalities to target this small GTPase. Rac1 shall be considered as a valid target to limit the acquired and intrinsic resistance of HCC tumors and their metastatic potential.
Review • Journal • IO biomarker
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RAC1 (Rac Family Small GTPase 1)
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NSC23766 • vatalanib (PTK787)
over3years
Inhibitory Effects of Euphorbia ebracteolata Hayata Extract ECB on Melanoma-Induced Hyperplasia of Blood Vessels in Zebrafish Embryos. (PubMed, Evid Based Complement Alternat Med)
The results showed that ECB was an active ingredient of EEH in inhibiting melanoma-induced hyperplasia of blood vessels in zebrafish embryos, similar to the angiogenic inhibitor vatalanib...Both vegfr2 and vegfr3 are essential genes that regulate blood vessel formation and upregulate the expression of p53 and casp3a genes in zebrafish. Together, the above-mentioned results indicate that ECB has a potential antimelanoma effect in vivo, which may be mediated by inhibiting vascular endothelial growth factor receptors.
Journal
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TP53 (Tumor protein P53) • KDR (Kinase insert domain receptor) • FLT4 (Fms-related tyrosine kinase 4)
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KDR expression • TP53 expression
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vatalanib (PTK787)