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over1year
Impact of Blood-Brain Barrier to Delivering a Vascular-Disrupting Agent: Predictive Role of Multiparametric MRI in Rodent Craniofacial Metastasis Models. (PubMed, Cancers (Basel))
Postmortem angiography and pathology showed a significantly larger H&E-stained area of necrosis (86.2% vs. 18.3%, p < 0.0001), lower CD31 level (42.7% vs. 54.3%, p < 0.05), and lower Ki67 level (12.2% vs. 32.3%, p < 0.01) in extracranial tumors, compared with intracranial lesions. The BBB functioned as a barrier against the delivery of VDA into intracranial tumors and multiparametric MRI may predict the efficacy of VDAs on craniofacial tumors.
Preclinical • Journal
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CD31 (Platelet and endothelial cell adhesion molecule 1) • PECAM1 (Platelet And Endothelial Cell Adhesion Molecule 1)
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Zybrestat (fosbretabulin)
over1year
The Efficacy of Fosbretabulin Disodium Combined with Radiofrequency Ablation in Lung Cancer. (PubMed, Radiat Res)
Mechanistically, we reported that FBTD inhibited the RFA-induced PD-1 and PD-L1 upregulation in vivo. In conclusion, we demonstrated that FBTD promoted the antitumor effects of RFA in lung tumor-bearing mice in this study.
Journal • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • TNFA (Tumor Necrosis Factor-Alpha)
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Zybrestat (fosbretabulin)
2years
Advances in targeted therapy for anaplastic thyroid carcinoma. (PubMed, Zhejiang Da Xue Xue Bao Yi Xue Ban)
Tyrosine kinase inhibitor lenvatinib has potential in treating ATC patients with favorable efficacy in clinical trials. The effectiveness of the v-raf murine sarcoma viral oncogene homologue B1 () gene inhibitor dabrafenib in combination with trametinib for the treatment of positive ATC patients has been demonstrated in clinical trials...The immune checkpoint inhibitor pembrolizumab can be applied to treat thyroid cancer with high tumor mutational load and may be considered as the preferred modality for the treatment of ATC patients with high programmed death ligand-1 expression. The mammalian target of rapamycin pathway inhibitors, peroxisome proliferators-activated receptor γ agonists, endothelial growth factor receptors-targeting monoclonal antibody cetuximab and novel vascular blocker fosbretabulin are still in the clinical research stage, which are expected to provide new directions for the development of novel targeted drugs. This article reviews the current research progress on targeted drugs for the treatment of ATC.
Journal • Tumor Mutational Burden • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • TMB (Tumor Mutational Burden)
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PD-L1 expression
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Keytruda (pembrolizumab) • Erbitux (cetuximab) • Mekinist (trametinib) • Tafinlar (dabrafenib) • Lenvima (lenvatinib) • Zybrestat (fosbretabulin)
over3years
Recent advances in the management of anaplastic thyroid cancer. (PubMed, Thyroid Res)
Surgery should be as complete as possible, securing the airway and ensuring access for nutritional support; the current standard of care of radiotherapy is the intensity-modulated radiation therapy; chemotherapy includes the use of doxorubicin or taxanes (paclitaxel or docetaxel) generally with platin (cisplatin or carboplatin)...These include multitarget tyrosine kinase inhibitors (Lenvatinib, Sorafenib, Sunitinib, Vandetanib, Axitinib, Pazopanib, Pyrazolo-pyrimidine compounds), single target tyrosine kinase inhibitors (Dabrafenib plus Trametinib and Vemurafenib against BRAF, Gefitinib against EGFR, PPARγ ligands (e.g. Efatutazone), Everolimus against mTOR, vascular disruptors (e.g. Fosbretabulin), and immunotherapy (e.g. Spartalizumab and Pembrolizumab, which are anti PD-1/PD-L1 molecules)...Other single target mutation agents with fair results are Everolimus when a mutation involving the PI3K/mTOR pathway is detected, Imatinib in case of PDGF-receptors overexpression, and Spartalizumab in case of PD-L1 positive tumors...Since in this tumor several genetic alterations are usually found, the aim is to inhibit or disrupt several pathways: these combination strategies use therapy targeting angiogenesis, survival, proliferation, and may act against both MAPK and PI3K pathways. Investigating new treatment options is eagerly awaited since, to date, even the molecules with the best radiological results have not been able to provide a durable disease control.
Review • Journal • PD(L)-1 Biomarker
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EGFR (Epidermal growth factor receptor) • BRAF (B-raf proto-oncogene)
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PD-L1 expression • BRAF mutation • MTOR mutation
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Keytruda (pembrolizumab) • Mekinist (trametinib) • cisplatin • Zelboraf (vemurafenib) • Tafinlar (dabrafenib) • carboplatin • gefitinib • sorafenib • paclitaxel • imatinib • docetaxel • sunitinib • everolimus • Lenvima (lenvatinib) • doxorubicin hydrochloride • Votrient (pazopanib) • Inlyta (axitinib) • Caprelsa (vandetanib) • spartalizumab (PDR001) • Zybrestat (fosbretabulin) • efatutazone (CS-7017)