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Equconazole has been re-used as an anti-cancer treatment for a variety of malignant tumors.
in preclinical models, it has anti-angiogenesic properties and inhibits Hedgehog (Hh) pathway activity.
gerber et al. conducted a window-of-opportunity trial to determine the biological effects of icconazole in patients.
the trial recruited patients with non-small cell lung cancer who were to undergo surgery for 10-14 days of equconazole (300 mg, oral, 2/day).
patients are subjected to dynamically enhanced MRI examinations and plasma collection for pharmacodynamics (PK) and pharmacological analysis.
collect tissue from pre-treatment biopsies, surgical excisions, and skin biopsies to analyze concentrations of icconazole and hydroxyciconazole, as well as biomarkers of blood vessels and Hh pathways.
recruited 13 patients.
is well resistant to icconazole.
plasma concentrations of estraconazole and hydroxyconazole vary up to 6 times between patients.
the concentration of equconazole in tumor tissue varies with the change of plasma concentration and is higher than that of plasma.
high levels of icconazole were significantly associated with decreased tumor volume and tumor perfusion, angiogenesic cytokine lebinocyte interleukin 1b and GM-CSF reduction, and reduced microvascular density in tumors.
treated with icingazole also exhibit different metabolic characteristics.
treatment of gli1 and PTCH1 mRNA was not altered.
can not predict the concentration of icconazole based on the size of the patient, kidney function and liver function.
icconazole showed early antivascular, metabolic and tumor-resistant effects of concentration dependence in patients with non-small cell lung cancer.
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